In a case where Gap corporation et al. filed a petition for a trial on invalidation of registration against Eul foreign company on the ground that the inventive step, etc. is denied as an selective invention of a patented invention named "the development-containing compound as a human Xa control unit and its inducement" and the Korean Intellectual Property Trial and Appeal Board cited it, the case holding that the nonobviousness of the claims 1 of the patented invention is denied on the ground that the selective invention does not have any physical or quantitative effect compared to the prior invention, and the inventive step is not denied.

A et al. filed for a registration invalidation trial against the patent right-holder B of a patented invention named “A,” on the ground that the inventive step is denied as an selective invention, and the Patent Tribunal cited it.

The case holding that since it is difficult for a person to use the prior invention to exclude the patented invention as a graphic compound or its limitation, the prior invention, which is one of the inventions described in paragraph (1) of the patented invention, is related to the hexame compound containing nitrogen, and all of the prior inventions, which is an invention with a vague structure identical to the thoma of the prior invention, since it is difficult for the person to use the prior invention as a graphic compound or its limitation, and it is difficult for the person to use the prior invention as a graphic compound to use it as a graphic effect, the prior invention, as well as the prior invention, to use the prior invention as a graphic effect only, to use only the subordinate concept included in its upper concept, as it is difficult for the person to use the prior invention as a graphic effect, and it is not necessary for the person to use the prior invention as an ordinarily higher concept than the prior invention to use the prior invention, and it is not necessary for the person to use the prior invention as an alternative concept that can be seen as having the same objective as an ordinarily accepted concept of the prior invention.

Articles 29(2) and 42(3) of the Patent Act

Bre-Tolu-Mab Squib Holdings Squiber Squiber comer (Bluol-Myers Squib Henland Unbremited Commonpa Company, its trade name before change: BluTool-Mabbb Squib Squib Holdings Islands (Law Firm (LLC, Attorneys Ohjin-jin et al., Counsel for the plaintiff-appellant) (Law Firm LLC)

NAP Co., Ltd. and three others (Law Firm LLC et al., Counsel for the defendant-appellant)

Sejong District Court Decision 201Na14488 delivered on August 1, 201

December 14, 2018

1. All of the plaintiff's claims are dismissed.

2. The costs of the lawsuit shall be borne by the Plaintiff, including the costs incurred by participation.

On February 28, 2018, the Korean Intellectual Property Trial and Appeal Board rendered a decision to revoke the ruling on the case related to the 2015 Party 1184, 2015 Party 1185 Party 1185 (Joint), 2015 Party 1186 (Joint), 2015 Party 174 (Joint), 2015 Party 1775 (Joint).

1. Basic facts

A. Patent invention of this case (Evidence A Nos. 1 and 2);

(i)the name of the invention: a man Xa-containing compounds and their inducements;

(ii) the international filing date / Priority Claim / Translation Submission Date / Registration Number:

September 17, 2002/ September 21, 2001/ March 19, 2004/ July 9, 2009 (registration number 1 omitted)

3) Claims

[Claim 1] Note 1] Chemical compound with chemical formula 1, or salt permitted for its limitation (hereinafter “instant Claim 1 invention,” and the remainder of the claims in the same manner)

A person shall be appointed.

[Request 2] A chemical compound with a chemical formula 1

A person shall be appointed.

[Request 3 to 20] (Dismissal)

(iv)the description of the invention and its main contents in the drawings;

본문내 포함된 표 기술분야 본 발명은 일반적으로 트립신-유사 세린 프로테아제 효소, 특히 인자 Ⅹa의 억제제인 락탐-함유 화합물 및 그의 유도체, 이들을 함유하는 제약 조성물 및 혈전색전성 장애 치료용 항응고제로서 상기 물질을 사용하는 방법에 관한 것이다. (식별번호 [1]) 배경기술 효율적이고 특이적인 인자 Ⅹa의 억제제는 혈전색전성 장애의 치료를 위해 잠재적으로 유용한 치료제로서 필요하다. 따라서 새로운 인자 Ⅹa 억제제를 발견하는 것이 바람직하다. 추가로, 공지된 인자 Ⅹa 억제제와 비교하여 개선된 약리학적 특성을 갖는 새로운 화합물을 발견하는 것이 또한 바람직하다. 예를 들어, 인자 Ⅹa 대 기타 세린 프로테아제(즉, 트립신)에 대한 개선된 인자 Ⅹa 억제 활성 및 선택성을 갖는 새로운 화합물을 발견하는 것이 바람직하다. 또한 하기 범주 중 하나 이상이지만, 이에 제한되지는 않는 것에서 유리하고 개선된 특징을 갖는 화합물을 발견하는 것이 타당하고 바람직하다: (a) 제약 성질(예를 들어, 서방성 제형에 대한 용해성, 투과성 및 순응성); (b) 투여 요구량(예를 들어, 보다 낮은 투여량 및(또는) 1일 1회 복용량); (c) 혈액 농도 최고-최저(peak-to-trough) 특성을 감소시키는 인자(예를 들어, 청정률 및(또는) 분포용적); (d) 수용체에서 활성 약물의 농도를 증가시키는 인자(예를 들어, 단백질 결합, 분포용적); (e) 임상적 약물-약물 상호작용에 대한 경향을 감소시키는 인자(예를 들어, 사이토크롬 P450 효소 억제 또는 유도); (f) 역부작용에 대한 잠재성을 감소시키는 인자(예를 들어, 세린 프로테아제 이외의 약리학적 선택성, 가능한 화학적 또는 대사적 반응성 및 제한된 CNS 침투성); (g) 제조 비용 또는 타당성을 개선하는 인자(예를 들어, 합성의 어려움, 키랄 중심의 수, 화학 안정성 및 조작 편이성). (식별번호 [49]) 〈발명의 요약〉 따라서 본 발명은 인자 Ⅹa 억제제로서 유용한 신규 락탐-함유 화합물 및 그의 유도체 또는 제약상 허용되는 그의 염 또는 프로드러그(prodrug)를 제공한다. (식별번호 [51]) 발명의 상세한 설명 〈유용성〉 본 발명의 화합물은 인자 Ⅹa의 억제제이고 포유동물에서 혈전색전성 장애(즉, 인자 Ⅹa-관련 장애)의 치료용 또는 예방용 항응고제로서 유용하다. 일반적으로, 혈전색전성 장애는 혈괴에 의한 순환 질환(즉, 섬유소 형성, 혈소판 활성화 및(또는) 혈소판 응집을 포함하는 질환)이다. 본원에서 사용되는 용어 “혈전색전성 장애”는 동맥 심장혈관 혈전색전성 장애, 정맥 심장혈관 혈전색전성 장애 및 심장방실에서의 혈전색전성 장애를 포함한다. 본원에서 사용되는 용어 “혈전색전성 장애”는 불안정한 협심증 또는 다른 급성 관상 증후군, 1차 또는 재발성 심근 경색증, 허혈성 돌연사, 일과성 허혈 발작, 졸중, 죽상경화증, 말초 폐쇄성 동맥 질환, 정맥 혈전증, 심부정맥 혈전증, 혈전정맥염, 동맥 색전증, 관상 동맥 혈전증, 대뇌 동맥 혈전증, 대뇌 색전증, 신장 색전증, 폐 색전증 및 (a) 인공 판막 또는 기타 이식물, (b) 유치 카테터, (c) 스텐트, (d) 심폐 바이패스, (e) 혈액투석 또는 (f) 혈액이 혈전증을 촉진하는 인공 표면에 노출되는 다른 처치에서 발생하는 혈전증으로부터 선택되는(이로써 제한되지는 않음) 특정 장애를 또한 포함한다. 혈전증이 폐쇄(예를 들어, 바이패스 이후) 및 재폐쇄(예를 들어, 경피 경혈관 확장술 동안 또는 그 이후)를 포함하는 것을 주목한다. 혈전색전성 장애는 죽상경화증, 수술 또는 외과수술 합병증, 지속된 부동화, 동맥 세동, 선천성 혈전기호증, 암, 당뇨병, 투약 또는 호르몬의 영향 및 임신 합병증을 포함하는(이로써 제한되지는 않음) 증상으로부터 발생할 수 있다. 본 발명의 화합물의 항응고 효과는 인자 Ⅹa 또는 트롬빈의 억제 때문인 것으로 여겨진다. (식별번호 [817]) 본 발명의 화합물의 인자 Ⅹa의 억제제로서의 효과는 정제된 인간 인자 Ⅹa 및 합성 기질을 사용하여 측정된다. 발색성 기질 S2222(Diapharma/Chromogenix, West Chester, OH)의 인자 Ⅹa 가수분해 속도는 본 발명의 화합물의 부재 및 존재하 모두에서 측정된다. 기질의 가수분해는 pNA의 방출을 일으키고, 이는 405nm에서 흡광도 증가를 측정하여 분광광도법으로 모니터링된다. 억제제 존재하에 405nm에서 흡광도 변화 속도의 감소는 효소 억제를 나타낸다. 상기 분석의 결과는 억제 상수 Ki로 표현된다. (식별번호 [818]) 상기 분석에서 시험된 화합물은 Ki ≤ 10μM로 나타나는 경우에 활성인 것으로 고려된다. 본 발명의 바람직한 화합물은 Ki ≤ 1μM이다. 본 발명의 더욱 바람직한 화합물은 Ki ≤ 0.1μM이다. 본 발명의 더욱더 바람직한 화합물은 Ki ≤ 0.01μM이다. 본 발명의 더더욱 바람직한 화합물은 Ki ≤ 0.001μM이다. 상기 기재된 방법을 사용하여, 본 발명의 다수의 화합물이 Ki ≤ 10μM를 나타내는 것으로 밝혀졌으며, 이로써 본 발명의 화합물의 효과적인 Ⅹa 억제제로서의 유용성이 확인되었다. (식별번호 [828]) 본 발명의 화합물은 단독으로 또는 1종 이상의 추가의 치료제와 함께 투여될 수 있다. “함께 투여” 또는 “조합 치료”는 본 발명의 화합물 및 1종 이상의 추가의 치료제가 치료될 포유동물에게 동시에 투여되는 것을 의미한다. 함께 투여되는 경우, 이러한 성분들은 동일한 시간에 또는 상이한 시점에서 임의의 순서로 순차적으로 투여될 수 있다. 따라서 각 성분은 별도로 투여될 수 있으나, 목적하는 치료 효과를 제공하도록 충분히 근접한 시간으로 투여될 수 있다. 추가의 치료제는 다른 항응고제 또는 응고 억제제, 항-혈소판제 또는 혈소판 억제제, 트롬빈 억제제, 혈전용해제 또는 섬유소용해제, 항부정맥제, 항고혈압제, 칼슘 채널 차단제(L-타입 및 T-타입), 심장 글리코시드, 이뇨제, 전해질코르티코이드 수용체 길항제, 포스포디에스테라제 억제제, 콜레스테롤/지질 강하제 및 지질 프로파일 요법, 항당뇨제, 항우울제, 항염증제(스테로이드 및 비스테로이드), 항골다공증제, 호르몬 대체 요법, 경구용 피임약, 항비만제, 항불안제, 항증식제, 항종양제, 항궤양제 및 위식도 역류 질환제, 성장 호르몬 및(또는) 성장 호르몬 분비 촉진제, 갑상선 모방제(갑상선 수용체 길항제 포함), 항감염제, 항바이러스제, 항박테리아제 및 항진균제를 포함한다. (식별번호 [833], [834]) 본 발명의 화합물과 함께 사용할 수 있는 다른 항응고제(또는 응고 억제제)는 와파린 및 헤파린(비분할 헤파린 또는 임의의 시판용 저분자량 헤파린), 합성 오당류, 히루딘 및 아르가트로바나스를 포함하는 직접 작용 트롬빈 억제제뿐 아니라 상기 본 발명의 기술분야에서 확인된 공개 문헌에 기재된 바와 같은 다른 인자 Ⅹa 억제제를 포함한다. (식별번호 [835]) 본원에서 사용되는 용어 항혈소판제(또는 혈소판 억제제)는 예를 들어, 혈소판의 응집, 부착 또는 과립상 분비를 억제함으로써 혈소판 기능을 억제하는 제제를 의미한다. 제제의 비제한적 예로 공지된 수많은 비스테로이드성 항염증성 약물(NSAIDS), 예컨대 아스피린, 이부프로펜, 나프록센, 술린닥, 이도메타신, 메페나메이트, 드록시캄, 디클로페낙, 술핀피라존, 피록시캄 및 제약상 허용되는 이들의 염 또는 프로드러그(prodrug)가 포함된다. NSAIDS 중에서, 아스피린(아세틸살리실산 또는 ASA) 및 피록시캄이 바람직하다. 다른 적합한 혈소판 억제제는 IIb/IIIa 길항제(예를 들어, 티로피반, 엡티피바티드 및 압식시맙), 트롬복산-A2-수용체 길항제(예를 들어, 이페트로반), 트롬복산-A2-신세타제 억제제, PDE-III 억제제(예를 들어, 디피리다몰) 및 제약상 허용되는 이들의 염 또는 프로드러그(prodrug)를 포함한다. (식별번호 [836]) 본원에서 사용되는 용어 항혈소판제(또는 혈소판 억제제)는 또한 ADP(아데노신 디포스페이트) 수용체 길항제를 포함하며, 퓨린성 수용체 P2Y1 및 P2Y12가 바람직하고, P2Y12가 더욱 바람직하다. 바람직한 P2Y12 수용체 길항제는 제약상 허용되는 염 또는 프로드러그(prodrug)를 비롯하여 티클로피딘 및 클로피도그렐을 포함한다. 클로피도그렐이 더욱더 바람직한 제제이다. 티클로피딘 및 클로피도그렐이 사용 시 위장관에서 순한 것으로 공지되어 있기 때문에 이들이 또한 바람직하다. (식별번호 [837]) 본원에서 사용되는 용어 트롬빈 억제제(또는 항트롬빈제)는 세린 프로테아제 트롬빈의 억제제를 의미한다. 트롬빈을 억제함으로써, 다양한 트롬빈-매개된 과정, 예컨대 트롬빈-매개된 혈소판 활성화[즉, 예를 들어, 혈소판의 응집 및(또는) 플라스미노겐 활성화제 억제제-1 및(또는) 세로토닌의 과립상 분비] 및(또는) 섬유소 형성이 중단된다. 다수의 트롬빈 억제제가 당업자에게 공지되어 있으며, 이들 억제제는 본 발명의 화합물과 함께 사용될 수 있는 것으로 생각된다. 이러한 억제제의 비제한적인 예로는 제약상 허용되는 염 및 프로드러그(prodrug)를 비롯한 보로아르기닌 유도체, 보로펩티드, 헤파린, 히루딘, 아르가트로반 및 멜라가트란이 포함된다. 보로아르기닌 유도체 및 보로펩티드는 보론산의 N-아세틸 및 펩티드 유도체, 예컨대 리신, 오르니틴, 아르기닌, 호모아르기닌 및 이들의 상응하는 이소티오우로늄 유사체의 C-말단 α-아미노보론산 유도체를 포함한다. 본원에서 사용되는 용어 히루딘은 본원에서 히루로그, 예컨대 디술페이토히루딘을 의미하는 히루딘의 적합한 유도체 또는 유사체를 포함한다. (식별번호 [838]) 본원에서 사용되는 용어 혈전용해제 또는 섬유소용해제는 혈괴(트롬비)를 용해시키는 제제를 의미한다. 이러한 제제는 제약상 허용되는 염 또는 프로드러그(prodrug)를 비롯한 조직 플라스미노겐 활성화제(천연 또는 재조합) 및 이들의 개질된 형태, 아니스트레플레이즈(anistreplase), 우로키나제, 스트렙토키나제, 테넥테플레이즈(tenecteplase, TNK), 라노테플레이즈(lanoteplase, nPA), 인자 VIIa 억제제, PAI-1 억제제(즉, 조직 플라스미노겐 활성화제 억제제의 비활성화제), 알파2-항플라즈민 억제제 및 아니소일레이트화(anisoylated) 플라스미노겐 스트렙토키나제 활성화제 복합체를 포함한다. 본원에서 사용되는 용어 아니스트레플레이즈는 예를 들어 본원에서 참고로 포함되는 EP 028,489에 기재된 바와 같은 아니소일레이트화 플라스미노겐 스트렙토키나제 활성화제 복합체를 의미한다. 본원에서 사용되는 용어 우로키나제는 이중 및 단일 쇄 우로키나제 모두를 의미하나, 본원에서 단일 쇄는 프로우로키나제로도 불린다. (식별번호 [839]) 본 발명의 화합물과 함께 사용하는 데 적합한 항부정맥제의 예는 클래스 I 제제(예컨대, 프로파페논); 클래스 II 제제(예컨대, 카르바디올 및 프로프라놀론); 클래스 III 제제(예컨대, 소탈롤, 도페틸리드, 아미노다론, 아지밀리드 및 이부틸리드); 클래스 IV 제제(예컨대, 디티아젬 및 베라파밀); K+ 채널 오프너, 예컨대 IAch 억제제 및 IKur 억제제(예를 들어, WO 01/40231에 기재된 바와 같은 화합물)를 포함한다. (식별번호 [840]) 본 발명의 화합물과 함께 사용하기에 적합한 항고혈압제의 예는 알파 아드레날린성 차단제; 베타 아드레날린성 차단제; 칼슘 채널 차단제(예를 들어, 디티아젬, 베라파밀, 니페디핀, 암로디핀 및 미베프라딜); 이뇨제(예를 들어, 클로로티 아지드, 히드로클로로티아지드, 플루메티아지드, 히드로플루메티아지드, 벤드로플루메티아지드, 메틸클로로티아지드, 트리클로로메티아지드, 폴리티아지드, 벤즈티아지드, 에타크린산 트리크리나펜, 클로르탈리돈, 푸로세미드, 무솔리민, 부메타니드, 트리암트레넨, 아밀로리드, 스피로놀락톤); 레닌 억제제; ACE 억제제(예를 들어, 카프토프릴, 조페노프릴, 포시노프릴, 에날라프릴, 세라노프릴, 실라조프릴, 델라프릴, 펜토프릴, 퀴나프릴, 라미프릴, 리시노프릴); AT-1 수용체 길항제(예를 들어, 로사르탄, 이르베사르탄, 발사르탄); ET 수용체 길항제(예를 들어, 시탁센탄, 아트센탄 및 미국 특허 제5,612,359호 및 제6,043,265호에 개시된 화합물); 이중 ET/AII 길항제(예를 들어, WO 00/01389에 개시된 화합물); 중성 엔도펩티다제(NEP) 억제제; 바소펩시다제 억제제(이중 NEP-ACE 억제제)(예를 들어, 오마파트릴랏, 게모파트릴랏 및 니트레이트)를 포함한다. (식별번호 [841]) 본 발명의 화합물과 함께 사용하기에 적합한 칼슘 채널 차단제(L-타입 또는 T-타입)의 예는 딜티아젬, 베라파밀, 니페디핀, 아몰디핀 및 미베프라딜을 포함한다. (식별번호 [842]) 본 발명의 화합물과 함께 사용하기에 적합한 심장 글리코시드의 예는 디지탈리스 및 오우아바인을 포함한다. (식별번호 [843]) 본 발명의 화합물과 함께 사용하기에 적합한 이뇨제의 예는 클로로티아지드, 히드로클로로티아지드, 플루메티아지드, 히드로플루메티아지드, 벤드로플루메티아지드, 메틸클로로티아지드, 트리클로로메티아지드, 폴리티아지드, 벤즈티아지드, 에타크린산 트리크리나펜, 클로르탈리돈, 푸로세미드, 무솔리민, 부메타니드, 트리 암트레넨, 아밀로리드 및 스피로놀락톤을 포함한다. (식별번호 [844]) 본 발명의 화합물과 함께 사용하기에 적합한 전해질코르티코이드 수용체 길항제의 예는 스피오놀락톤 및 에플리리논을 포함한다. (식별번호 [845]) 본 발명의 화합물과 함께 사용하기에 적합한 포스포디에스테라제 억제제의 예는 PDE III 억제제(예컨대 실로스타졸); 및 PDE V 억제제(예컨대 실데나필)를 포함한다. (식별번호 [846]) 본 발명의 화합물과 함께 사용하기에 적합한 콜레스테롤/지질 강하제 및 지질 프로파일 요법의 예는 HMG-CoA 리덕타제 억제제[예를 들어, 프로바스타틴, 로바스타틴, 아트로바스타틴, 심바스타틴, 플루바스타틴, NK-104(a.k.a. 이타바스타틴 또는 니스바스타틴) 및 ZD-4522(a.k.a. 로수바스타틴 또는 아타바스타틴 또는 비사스타틴)]; 스쿠알렌 신세타제 억제제; 피브레이트; 담즙산 제거제(sequestrant)(예컨대, 퀘스트란); ACAT 억제제; MTP 억제제; 리포옥시게나제 억제제; 콜레스테롤 흡수 억제제; 및 콜레스테롤 에스테르 전달 단백질 억제제(예를 들어, CP-529414)를 포함한다. (식별번호 [847]) 본 발명의 화합물과 함께 사용하기에 적합한 항당뇨제의 예는 비구아니드(예를 들어, 메트포르민); 글루코시다제 억제제(예를 들어, 아카르보스); 인슐린(인슐린 분비촉진제 또는 인슐린 감작제 포함); 메글리티니드(예를 들어, 레파글리니드); 술포닐우레아(예를 들어, 글리메피리드, 글리부리드 및 글리피지드); 비구아니드/글리부리드 조합물(예를 들어, 글리코반스), 티오졸리딘디온(예를 들어, 트로글리타존, 로시글리타존 및 피오글리타존), PPAR-알파 아고니스트, PPAR-감마 아고니스트, PPAR 알파/감마 이중 아고니스트, SGLT2 억제제, WO 00/59506에 개시된 것과 같은 지방산 결합 단백질(aP2)의 억제제, 글루카곤-유사 펩티드-1(GLP-1) 및 디펩티딜 펩티다제 IV(DP4) 억제제를 포함한다. (식별번호 [848]) 본 발명의 화합물과 함께 사용하기에 적합한 항우울제의 예는 네파조돈 및 세르트랄린을 포함한다. (식별번호 [849]) 본 발명의 화합물과 함께 사용하기에 적합한 항염증제의 예는 프레드니손; 덱사메타손; 엔브렐; 단백질 티로신 키나제(PTK) 억제제; 시클로옥시게나제 억제제[NSAID 및 COX-1 및(또는) COX-2 억제제 포함]; 아스피린; 인도메타신; 이부프로펜; 프리옥시캄; 나프록센; 셀레콕시브 및(또는) 로페콕시브를 포함한다. (식별번호 [850]) 본 발명의 화합물과 함께 사용하기에 적합한 항골다공증제의 예는 알렌드로네이트 및 랄록시펜을 포함한다. (식별번호 [851]) 본 발명의 화합물과 함께 사용하기에 적합한 호르몬 대체 요법의 예는 에스트로겐(예를 들어, 컨쥬게이트된 에스트로겐) 및 에스트라디올을 포함한다. (식별번호 [852]) 본 발명의 화합물과 함께 사용하기에 적합한 항응고제의 예는 헤파린(예를 들어, 비분할 저분자량의 헤파린, 예컨대 에톡사파린 및 달테파린)을 포함한다. (식별번호 [853]) 본 발명의 화합물과 함께 사용하기에 적합한 항비만제의 예는 오릴리스타트 및 aP2 억제제(예컨대, WO 00/59506에 개시된 억제제)를 포함한다. (식별번호 [854]) 본 발명의 화합물과 함께 사용하기에 적합한 항불안제의 예는 디아제팜, 롤라제팜, 부스피론 및 히드록시진 파모에이트를 포함한다. (식별번호 [855]) 본 발명의 화합물과 함께 사용하기에 적합한 항증식제의 예는 시클로스포린 A, 파클리탁셀, 아드리아미신; 에피틸론, 시스플라틴 및 카르보플라틴을 포함한다. (식별번호 [856]) 본 발명의 화합물과 함께 사용하기에 적합한 항궤양제 및 위식도 역류 질환제의 예는 파모티딘, 라니티딘 및 오메프라졸을 포함한다. (식별번호 [857]) 본 발명의 화합물(즉, 제1 치료제)을 1종 이상의 추가의 치료제(즉, 제2 치료제)와 함께 투여하는 것은, 바람직하게는 각각을 더 낮은 투여량으로 사용할 수 있도록 하면서(즉, 상승효과 조합물), 바람직하게는 화합물 및 제제를 단독으로 투여한 것에 비해 효능의 이점을 제공한다. 낮은 투여량은 부작용의 가능성을 최소화하여, 안전성을 증가시킨다. 1종 이상의 치료제를 치료 투여량 미만으로 투여하는 것이 바람직하다. 모든 치료제를 치료 투여량 미만으로 투여하는 것이 더욱 바람직하다. 투여량 미만은 치료제 자체로 치료할 증상 또는 질환에 대해 목적하는 치료 효과를 제공하지 못하는 치료제의 양을 의미한다. 상승 효과 조합은 조합의 관찰된 효과가 단독으로 투여된 개별 제제의 합계보다 더 큰 것을 의미한다. (식별번호 [858])

5) A patentee: The plaintiff

6) An inventor: Nonparty 1 (English name 1 omitted), Nonparty 2 (English name 2 omitted), etc.

(b) A preceding invention (a evidence No. 4-1);

Prior Invention is an invention related to “Nitrogen content as a human subject Xa control unit” inserted in the International Publication 00/39131 published on July 6, 200, which is published on July 6, 200, Nonparty 1 (English name 1 omitted), Nonparty 2 (English name 2 omitted), etc. among the inventors of the instant patent invention, is a joint inventor, and is an invention with respect to “Nitrogeny content as a human subject xa control unit (Nitrogens 2)” and is an invention with respect to “Nitroblister xa” or its protegor. The main issues are as follows.

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Note 3) Major claims

(State 3)

C. Details of the instant trial decision (Evidence A No. 3)

1) Pursuant to Section 4, Defendant NVA Co., Ltd., Defendant NVA Co., Ltd., Defendant NVA, and Defendant Sympima filed a petition for each of the instant patent inventions with the Intellectual Property Trial and Appeal Board (hereinafter referred to as “instant petition for each of the instant petition for trial”) on the grounds that: (a) the instant patent invention is selective invention and does not contain a detailed description that makes it possible for the patent applicant to easily grasp its effects and has a substantial difference in its physical effects or quantity; and (b) the nonobviousness of the instant patent invention is denied on the grounds that the nonobviousness of the patent invention is not indicated in a detailed description that makes it possible for the patent applicant to practice the invention; and (c) the patent invention is non-obviousness.

2) On February 28, 2018, the Korean Intellectual Property Tribunal joined each of the instant appeals on the ground that “The patented invention of this case is an selective invention whose elements are stated in the preceding invention as an upper concept and whose subordinate concepts are included in the above upper concept, and which is part of the elements, and there is no qualitative difference compared to the effects of the preceding invention, as well as there is no significant difference in both aspects, and thus, its nonobviousness is denied.”

[Reasons for Recognition] Facts without dispute, Gap evidence Nos. 1 through 4 (including branch numbers; hereinafter the same shall apply), the purport of the whole pleadings

2. Summary of the parties' arguments;

A. The plaintiff's assertion

For the following reasons, the instant patent invention is unlawful, even though its nonobviousness is not denied.

1) Prior inventions do not specifically commence a compound including 5) a chemical with which a variety of unions can begin only in a general form, and do not specifically commence a compound including 5) a crypian in a desirable working pattern, and do not present any motive to derive the patented invention of this case. Thus, the patented invention of this case does not constitute selective inventions since a person with ordinary skills can recognize the upper concept from the description of the prior inventions and can easily derive it.

(ju5) Scacon structure means a structure, including a CON-human scafic body, within a high scafic body, which includes a scafic body. A scafic body of a scafic body(scafic body) is a part indicated as a scafic body from the right chemical structural formula.

2) Even if the patented invention in this case constitutes a selective invention, prior inventions start only several hundred million or more compounds in general, and do not include any description at all capable of verifying the existence of a traffic response of the patented invention in this case, and thus it is extremely difficult for ordinary technicians to derive a traffic response of the patented invention in this case from the prior inventions. Thus, the patented invention in this case shall be deemed to have difficulty in forming the patented invention in comparison with the prior inventions, and thus, the strict requirements for stating the effects of the selective invention shall not be applied.

3) On the other hand, the patented invention of this case contains ① an outstandingly dynamic characteristics in comparison with the prior invention, ② a dynamic effect is indicated in the specification, whereas the prior invention does not contain any description of such effect, the said effect constitutes a dual effect compared to the prior invention. In addition, the patented invention of this case is remarkably effective in relation to the prior invention, ③ human Xa-friendly relationship (low Ki value) in comparison with the prior invention, and such effect can be confirmed through the additional submitted experimental data.

B. The defendants and the defendants' assistant intervenor's assertion

For the following reasons, the nonobviousness of the patented invention of this case is denied, and the trial decision of this case in the same conclusion is legitimate.

1) The instant patent invention constitutes a selective invention that constitutes only the subordinate concepts included in the elements of a higher concept in the prior invention, and therefore, there is no room to consider the complexity of composition in determining the inventive step of the instant selective invention.

2) Even if considering the difficulty of composition, the implementation of prior inventions has already commenced the nuclear structure and ventilation of the graphic team, so it can easily derive the upper concept of the graphic team from the prior inventions.

3) In order to recognize the inventive step as a selective invention, the patented invention of this case must clearly state the nature or significant effect of the invention in the specification. The specification of the patented invention of this case cannot be deemed to clearly state the nature or quantitative effect of the patented invention when compared to the prior invention.

3. Whether the trial decision of this case is legitimate

A. Whether the instant Claim 1 invention constitutes a selective invention

1) Criteria for determination

The selective invention refers to an invention in which the elements of an invention prior to or publicly announced are written as an upper concept, and only the subordinate concepts included in the above upper concept are all or part of the components (see, e.g., Supreme Court Decisions 2012Hu3664, May 16, 2014; 2014Hu1631, May 11, 2017).

2) Preparation for composition

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Note 7 / [2] The desirable implementation mode

Note 8) / [9] The desirable implementation mode

3) Determination

A) The instant Claim 1 invention and the prior invention are both related to the Herovirative compound containing nitrogen.

선행발명에 개시된 화합물은 이 사건 제1항 발명의 아픽사반과 동일한 모핵 구조( )를 가지는 화합물( )로서, G, Z, A, B 위치에 선택적으로 치환될 수 있는 구성요소가 병렬적으로 나열된 이른바 마쿠쉬(Markush) 형식으로 기재되어 있는데, 구체적으로 이 사건 제1항 발명의 아픽사반과 대비할 수 있는 화합물은 치환기에 관한 다음의 내용을 포함하는 개념의 것이다. 즉 ① 치환기 Z는 N 또는 이고, 는 H, 등으로부터 선택되며, 여기서 r은 0, 1, 2, 3으로부터, R1′는 H, 알킬, 등으로부터, R² 및 는 각 H, CF₃ 등으로부터 각 선택된다. ② 치환기 G는 화학식 I( ) 또는 화학식 Ⅱ( )이고, 여기서 고리 D가 부재하는 경우 고리 E는 페닐, 피리딜 등으로부터 선택되며, 고리 E는 R″ 및 R′로 치환되되, R″는 F, Cl, 알콕시 등으로부터, R′는 H, F, Cl 등으로부터 각 선택된다. ③ 치환기 A는 0∼2개의 R⁴로 치환된 카르보시클릭 잔기 등으로부터 선택된다. ④ 치환기 B는 등과 N, O 및 S로 구성된 군에서 선택된 1∼4개의 헤테로원자를 함유하고 0∼2개의 로 치환된 5∼10원의 헤테로시클릭계로부터 선택되고, 여기서 는 H, =O 등으로부터 선택된다.

이와 대비하여 보건대, 이 사건 제1항 발명의 아픽사반은 선행발명에 개시된 화합물과 동일한 모핵 구조( )를 가지는 화합물( )로서 다음과 같은 치환기의 선택에 따른 것으로 볼 수 있다. 즉 ① 선행발명의 치환기 Z에 대해서는 를 선택하면서 는 (r=0)로 선택하고, 여기서 R1′에 대하여는 를, R² 및 에 대하여는 각 H를 선택한 카르복시아미드( )로 한정되었다. ② 선행발명의 치환기 G에 대하여 화학식 I인 ‘ ’을 선택하고, 다시 고리 D가 부재하는 경우로서 고리 E에 대하여 페닐로 선택하면서 R″ 및 R′으로 알콕시( 주9) 메톡시) 및 H를 각 선택한 4-메톡시페닐( )로 한정되었다. ③ 선행발명의 치환기 A에 대해서는 0개의 R⁴로 치환된 카르보시클릭 잔기를 선택하고, 그중 C가 6개인 페닐( )로 한정되었다. ④ 선행발명의 치환기 B에 대해서는 N, O 및 S로 구성된 군에서 선택된 1∼4개의 헤테로원자를 함유하고 0∼2개의 로 치환된 5∼10원의 헤테로시클릭계(1개의 N을 함유한 6원의 헤테로시클릭)를 선택하되, 여기서 1개의 에 대하여 =O를 선택한 옥소피페리디닐( )로 한정되었다.

Therefore, the Claim 1 invention of this case is a selective invention that contains the elements stated in the preceding invention as the upper concept and only the subordinate concepts included in the upper concept as its constituent elements (this point is to be examined in detail in the following (b) A).

B) On this issue, the Plaintiff asserts that, according to the legal principles of judicial precedents on selective inventions, the invention can be deemed selective inventions only in cases where ordinary technicians can reasonably expect that the upper concept can be recognized and that the patented invention can be easily derived from the description of the prior invention. In this case, the prior invention commences more than several hundred million chemical compounds in general, and no motive is provided to derive it by excluding from the desirable structure the graphic team structure, including the ex-explacy and the ex-explacy, from the desirable structure, the patented invention in this case cannot be seen as selective inventions because it is difficult to reasonably expect that the upper concept should be recognized from the prior invention, and that the patented invention in this case can not be seen as an selective invention.

However, whether an ordinary skilled person can recognize the upper concept from the preceding invention and easily derive the selective invention from the preceding invention is not easy to distinguish the grounds for determining the originality or inventive step of the selective invention from that of the preceding invention, but it is not necessary to distinguish whether the invention is an selective invention according to the ordinary skill's perception level at the preceding stage. If the concept of selective invention is not recognized, it may not be recognized, but if the elements of the preceding or publicly notified invention are stated in the upper concept and only the subordinate concepts included in the above upper concept are selective inventions as part or whole of the elements of the invention, it is necessary to treat the invention differently from the ordinary invention in determining the patent requirement as seen earlier. Accordingly, if the concept is introduced for the division, it is necessary to distinguish whether the invention is an selective invention according to the ordinary skill's recognition level, and it is only difficult to distinguish the aforementioned selective invention from that of the preceding invention. If it conforms to the definition of the above concept, it is not sufficient to understand that the judgment of the court below is an selective invention that falls under the preceding invention's general skill, but is an selective invention with the ground for patent invention described above.

B. Whether the invention of this case is inventive step

1) Criteria for determination

A) The attitude and intent of the precedent established in relation to the selective invention

(1) In order to deny the newness of a selective invention, prior inventions must specifically start the subordinate concepts comprising selective inventions. This includes cases where prior art holders can recognize the existence of selective inventions directly from prior art based on the content of prior art and the common sense of technology at the time of filing an application, as well as cases where the text of prior art exists in the prior literature describing the prior invention (see Supreme Court Decision 2011Hu2985, Apr. 25, 2013, etc.).

In order for the inventive step of a selective invention not to be denied, all subordinate concepts included in the selective invention have different effects from those of the preceding invention in quality, or there should be substantial differences in quantity even without qualitative differences. In such cases, the description of the invention in the specification of the selective invention must clearly state that the above effects are effective compared to the preceding invention. In order to clearly state such effects, the description of the invention must state the specific contents that can confirm qualitative differences in the description of the invention and the quantitative material that can confirm that there are significant differences in quantity (see, e.g., Supreme Court Decision 2010Hu3424, Aug. 23, 2012): Provided, That the effect of the selective invention is not to be stated in the comparative experiment material that can confirm clearly the existence of its effects, and if the effect is doubtful, the effect of the invention should be specifically asserted and presented by the method of submitting specific comparative experiment material after the filing date of the application (see, e.g., Supreme Court Decision 201Hu2740, Apr. 25, 2003).

(2) The grounds for demanding strict patent requirements as above to determine the inventive step of a selective invention are because, in order to recognize the inventive step of an invention selected as a component only the subordinate concepts included in the upper concept having a specific effect already launched in the prior invention, the choice of such subordinate concepts should be linked to the special technical effect unforeseeable in the prior invention. In other words, the purpose of the Patent Act is to promote the development of technology and contribute to industrial development by promoting the use of the invention, and granting exclusive rights to patent holders, considering that granting exclusive rights to the prior invention is a cost for the technical contribution in the relevant technical field, barring special circumstances, it is difficult to deem that the choice of the subordinate concepts among the upper concepts of the prior invention is made only by selecting a voluntary subordinate concepts from the upper concept of the prior invention, as it contributes to new technological development because it does not deviate from the scope of the duplicate invention, barring special circumstances. Accordingly, if a new invention is derived from the lower concept of the prior invention, the technical meaning of the subordinate concepts can be recognized, and in this case, the inventive step of the prior invention needs to be recognized in light of the special nature of the prior invention.

In addition, an inventor must be aware of the fact that he/she has a special technical effect in the subordinate concepts of his/her choice at the time of application. The inventor has recognized the same effect at the time of application through the specification. Thus, the inventor must clearly state the description of the selective invention, which requires a clear statement of the obvious effect of the invention, in the description of the selective invention, 11). Therefore, even if the inventor does not state any experimental data that can be specifically verified in order to recognize the inventive step of the selective invention, the inventor must clearly state that he/she knows that the invention has a different or significant effect compared to the prior invention, even if the inventor does not state any experimental data that can be specifically identified, it should clearly state the fact that the inventor knows that the selective invention would have a different or significant effect in comparison with the prior invention. If the subsequent selective invention can prove a specific effect by submitting the experimental data, etc. at the time of application for registration invalidation, patent infringement litigation, etc., if the inventor did not recognize the effects of the selective invention at the time of application, thereby unfairly maintaining the patent holder's exclusive relation to the prior invention.

B) Where strict patent requirements on determining the inventive step of a selective invention are mitigated;

(1) On the other hand, it is difficult to readily conclude that the above strict patent requirements should be met in determining the inventive step of a selective invention. The purport of the above precedents is to: (a) if the technical effect of the prior invention is anticipated to appear in the entire higher concept commenced in the prior invention, regardless of the size of the upper concept, subordinate concepts belonging to the higher concept can be seen equally as a technical composition that can achieve the effects presented by the prior invention; and (b) in this case, the selective invention of the lower concept is a duplicate invention of the upper concept in its nature and its choice cannot be recognized unless it has achieved special effects that cannot be recognized in the prior invention. On the other hand, the strict patent requirements can be mitigated when it is difficult to deem the selective invention as essentially overlapping. In fact, since the invention does not fall within the technical scope of the prior invention or the scope of rights (hereinafter referred to as “the scope of rights” without distinguishing it, it is necessary to treat it as an selective invention as a overlap, and to consider the effects of the selective invention as a general invention as well as its complexity and difficulty.

(2) If so, the issue is whether the selective invention is in essence a case where it is not a duplicate invention. Accordingly, the Plaintiff asserts that it is not reasonable to demand a strict effect on the invention where it is difficult to derive the selective invention from the preceding invention, and thus, it is not reasonable to require a strict effect on the invention where it is difficult to choose.

However, as long as the prior invention of a higher concept is initiated, the selective invention of a lower concept basically falls within the scope of the right. If the difficulty of choosing is recognized in the selective invention, if the prior invention is not a duplicate invention, it may reduce the scope of the right in the case of the prior invention. In other words, it may result in an unreasonable reduction of the scope of the right in the case of the prior invention to the extent that the prior invention is practicable or equivalent thereto. In particular, if the prior invention is described as a mash claims, it would lead to an unreasonable conclusion that a patent may be granted by recognizing the inventive step based on the difficulty of selecting all subordinate concepts of the prior invention. Of course, it is unreasonable to combine a number of options in the prior invention and find an optimal association through repeated implementation error, and find out the optimal efforts of the inventor leading to the selection, but only if it is not clear or uncertain that the prior invention has made a new substance different or unexpected from the structure, it would be difficult to recognize the inventive step of the prior invention without considering the difference between the prior invention and the prior invention in its structure.

(3) Ultimately, whether a selective invention is essentially overlapping must be accessed from the perspective of the scope of a patent right to the patented invention and the prior invention. However, if the scope of a patent right is determined by the claims stated in the specification attached to a patent application, and the technical scope is apparent solely with the description of the claims, in principle, it cannot be interpreted by other descriptions in the specification. However, if the literal interpretation of the claims is clearly unreasonable in light of other descriptions in the specification, such as where a part of the literal interpretation as included in the claims is not supported by the description of the invention, or where an applicant seems to exclude some of them from the scope of a patent right, it is possible to limit the scope of a patent right by taking into account the contents different from the description of the application and other descriptions in the specification and the legal stability of the applicant’s intent and third parties (see Supreme Court Decision 2001Hu2856, Jul. 11, 2003). Such legal doctrine is based on the essence of a patent right granted as a consideration for disclosure of the invention.

In light of the purport of the above legal doctrine, it is reasonable to deem that the prior invention does not fall under the scope of a right to the prior invention as cases where (1) negative outcomes or implications are excluded from the prior invention, or (2) generalization of the prior invention as an upper concept in light of the technological level at the time of patent application does not begin with the contents that can extend to the lower concept of the prior invention. In other words, it is natural that the prior invention cannot deny the inventive step of the prior invention even if it is an ordinary skilled person’s consideration of the prior invention, or it is said that the prior invention does not fall under the upper concept of the prior invention. In other words, it is difficult to strictly apply such requirement in light of the risk that the prior invention does not fall under the upper concept of the prior invention, because it is difficult to find that the prior invention does not fall under the upper concept of the prior invention as an ordinarily superior concept, even if it is difficult to find that the prior invention does not fall under the upper concept of the prior invention as an ordinarily superior concept.

(4) In arranging the above points, it cannot be anticipated that if there is a negative teaching or implication excluding the patented invention in the prior invention, or if the contents that can generalize the prior invention as the upper concept of the prior invention in light of the technological level at the time of the patent application to expand it to the lower concept of the relevant patented invention are equal as a means to achieve the same purpose, a person with ordinary skill cannot expect that the said patented invention included in the upper concept commenced in the prior invention is in conformity with the means to achieve the same purpose. Therefore, it is difficult to expand the contents of the prior invention to the above patented invention, which is a subordinate concept that cannot be anticipated to have common characteristics with the lower concept that has expressed the technical significance in the prior invention, and in such a case, it is necessary to determine the inventive step like the general invention. In other words, it is necessary to relax the detailed requirements for the effect of the prior invention.

(5) Meanwhile, the Plaintiff asserts that, inasmuch as it is not appropriate to require the inventor to strictly state the effects of the selective invention in the specification from the time of filing the application where the inventor did not recognize the fact that the invention is a selective invention, a strict patent requirement should be mitigated in determining the inventive step of the selective invention. This is reasonable to allow the inventor to state the significant effects of the selective invention in the specification where it is possible for the inventor to easily identify and recognize that the invention constitutes an selective invention. However, on the contrary, if it is difficult for the inventor to understand whether the selective invention is an selective invention because it is not easy to derive the selective invention in the prior invention, even if it is difficult for the inventor to ascertain the excellent and outstanding effects of the invention, there is a problem that the inventor could not obtain a patent, even if it is confirmed in the specification, and how the invention has a different effect than the prior invention indicating the superior concepts, and what is how much the inventor has to clearly state, and how to require the inventor to state the quantitative effects of the selective invention in the specification.

However, it is reasonable to objectively evaluate the relationship between the inventor and ordinarily skilled person when comparing the selective invention with the prior invention. It is a matter of whether the invention contributed to technology as an selective invention at the time of the filing of the application. Thus, its determination may not vary depending on the inventor’s subjective circumstances. Even in the case of a general invention, other than the selective invention, if the inventor had already started the same invention in any publication distributed before the filing of the application, newness is denied. In such a case, even if the inventor did not recognize and examine all the prior inventions, if it is difficult to say that all the prior inventions existing before the filing of the application were to be subjectively recognized, it is difficult to view the invention as an invention. Ultimately, it is reasonable to determine whether the invention constitutes the selective invention. Moreover, in this case, it is difficult to see that all the prior invention and the prior inventor were the Plaintiff, and that part of the prior invention is not identical to the prior invention’s name [the prior invention], and thus, it is difficult to see that the prior invention is identical to the prior invention’s description 17th of the invention.

2) Determination

A) Comparing the instant Claim 1 with the structure of the prior invention

A person shall be appointed.

(1) Selection element 1

The selected elements 1(1) of the instant Claim 1, which are the nuclear structure of the traffic response, are specifically launched in the prior invention. As seen below, the nuclear structure is continuously included in the prior invention in the process of limiting the desirable nuclear structure from the 12th phase to the 3rd phase, and the prior invention is also specifically launched in the seven phase “a more desirable implementation mode” and the prior invention specifically starts in the process of manufacturing the 1st nuclear structure of the selective element 1. In addition, the prior invention contains multiple examples of implementation, including the two types of nuclear structure, together with the complex method, and includes the representative implementation process initiated by the combination of limited nuclear structure and ventilation.

A person shall be appointed.

A person shall be appointed.

(2) Selection elements 2

The structure of the prior invention in response to the selective element 2 (k) of the instant Claim No. 1 invention is an air ventilation Z, and the prior invention is gradually reduced and stated in the scope of the ventilation indicated in the choice element 2 through the first and five stages, and 2 selective elements are specifically commenced even in the “a more desirable mode of implementation” in the seventh stage. In addition, the prior invention has many options including selective elements 2, and there are many selective elements in the prior invention, and the representative examples of implementation initiated by the combination of limited mother nuclear structure and ventilation also include two selective elements.

A person shall be appointed.

A person shall be appointed.

(3) Selection elements 3

The structure of the prior invention corresponding to the selective element 3 (4-mephenyl) of the instant Claim No. 1 (hereinafter referred to as “instant Claim No. 1”). The prior invention is gradually limiting the structure of the ventilation through step No. 1 through step No. 4, and explicitly starts it, and 3 of the selective elements are specified in the “a more desirable mode of implementation” in the 7-stage 7. Furthermore, the prior invention has a considerable number of options including selective elements 3, and the selective elements are also included in the case of a representative implementation that is launched by the combination of limited Mo nuclear structure and ventilation, even in the case of a representative implementation that is launched by the combination of limited Monuclear structure and ventilation.

A person shall be appointed.

A person shall be appointed.

(4) Alternative elements 4

The structure of the prior invention corresponding to the selective element 4 (3) of the instant Claim No. 1 is a ventilation A. In the prior invention, the structure of the prior invention is gradually limited through the stage 1,2,5, and 6, and it explicitly starts up by limiting the structure of the ventilation through the stage 1,2,5, and 4 of the prior invention is also indicated in the “a more desirable mode of implementation” in the 7th stage. Moreover, the prior invention has a considerable number of options including selective elements 4, and there are many choice elements in the prior invention, and the representative practices launched by the combination of limited Mo nuclear structure and ventilation.

A person shall be appointed.

A person shall be appointed.

Note 13)phenyls;

(5) Alternative elements 5

The structure of the prior invention corresponding to the selective element 5 (2) of the instant Claim No. 1 (2) invention is b, and the structure of the prior invention is 5 (2). The prior invention contains 1 to 4 hex elements selected in N,O, and S, and 5 to 10 hexines (6 hexines containing 1N) returned from 0 to 2 parts. The prior invention is confirmed through the description of the prior invention. However, the prior invention does not directly commence with respect to the search for the structure of the Pest invention, such as whether the Pesta (1N) is connected to the Pesta (1N) adjacent to Pesta, and whether the Pestaxa is refunded from any location of Pesta (2).

A person shall be appointed.

B) Whether a strict patent requirement on determining the inventive step of an selective invention is mitigated

(1) First, according to the aforementioned review, it is difficult to view that there is a negative view or implication to exclude the traffic response, which is the invention of this case, from the prior invention.

(2) Next, we examine whether the starting content of the prior invention can be generalized into the upper concept of the prior invention and expand it to the lower concept such as the traffic response team of the instant Claim 1.

(A) Prior inventions start a compound capable of suppressing Xa in a large number of general forms that can be possible, and suggest the various stages of implementation, reducing and embodying the scope of the ambiguous nuclear structure and ventilation. Therefore, in full view of the process and the examples of the implementation of the prior inventions selected, such as “the top concept of the prior inventions” (stage 2), “the more desirable mode of implementation (stage 3),” and “the more desirable mode of implementation (stage 4),” the higher concept of the prior inventions should be determined by a person with ordinary skills to generalize them as the top concept of the prior inventions and expand them to the lower concept, such as the traffic response of the instant Claim 1.

(B) In light of the aforementioned facts and the following circumstances revealed through the entire purport of Gap evidence Nos. 2, 4, and 21 and the entire arguments, it is reasonable to view that a person with ordinary skills can generalize the invention as the upper concept of the prior invention and expand it to the lower concept, such as the traffic response team of the invention No. 1 of this case.

① Prior inventions limited to compounds that can show the activation of a human Xa control system through multiple stages, and significantly reduce the size of a candidate group that can be selected by each selective element. Therefore, among the higher concepts launched in prior inventions, a person with ordinary skill is deemed to have a physical and chemical nature limited at least in individual stages, or which is structurally similar or similar to the lower concepts launched in the process of implementation, from among the higher concepts launched in prior inventions.

② In addition, the specification of the prior invention not only includes the specific name of all selective elements of the Pacific Team except the transvenation B, but also includes how to specifically urban and subvenors can connect with the core. Moreover, it is reasonable to see that the prior invention also includes both the selective elements of the Pacific Team 2 through 4 (for example, 6, 10, 13). Although the aforementioned implementation periods are not combined with the core structure of the same graphic group, it is reasonable to see that the two selective elements of the prior invention are one of the two main elements of the graphic group 14, 17 structural formula and the ventilation G (elective elements 3) structure of the graphic group 14, 17 structural formula and all of the selective elements including the graphic group 2, 14, and 104, and 154, respectively.

③ Furthermore, the search structure of the prior invention does not directly commence in the specific course of the prior invention’s implementation with respect to the ventilation B of the prior invention corresponding to the selective element 5 of the instant Claim No. 1, however, it is reasonable to view that there is no particular difficulty for a person of ordinary skill to expand the call B of the prior invention from the description of the prior invention to the upper concept of the prior invention by generalizing it from the description of the prior invention to the upper concept of the prior invention for the following reasons.

According to the specification of the prior invention, the prior invention is able to define the Hater, the total number of desirable Hater, and the location of the H themeacle, which can form the “H themeacle” in the Hate B, and it can be seen that the prior invention commences the Heacr compound and uses the PHacr compound as an example.

It shall be included in the 5-H, stroke 1, stroke, 6-H, stroke 1, stroke 5-H, stroke 1, stroke 5-H, stroke 4 or 4, independent of the armed forces comprising of the 5-H, stroke 5-H, stroke 1, stroke stroke 5, stroke 4 or 7-Hton stroke stroke stroke stroke stroke, 5 or 10-Hol stroke stroke stroke stroke stroke, 5 or less.

Furthermore, in the basic structure of the desirable implementation pattern (claim 2), the desirable implementation pattern (claim 9), the 9-level model ( Claim 9) has been explicitly included, and the specific implementation pattern of the prior invention has also been initiated 14) a Hague character structure including nitrogen B(N) in the specific implementation pattern of the prior invention.

( Note 14) Although the structure of the 5th is the 5th structure, the 11-14, 24, 27-29, 32, 35, 36, 39-41, 47, 48, 58, 60, 61, 64, 66, 68-70, 74, 79, 82-84, 88, 89, 89, 92, 94, 95, 97, 97, 100, 102, 103), stroke (e.g., implementation 9, 10, 15, 25, 44, 45, 63, 104-108) has already been initiated.

(C) The (B) prior invention has been clearly launched to limit the subordinate concepts set forth in the choice of air ventilation B through two stages, and the (a) the basic structure of air ventilation B may be combined into a bed (O) body, and (b) the specification of the prior invention clearly states that “If the bed body is in the bed (O), two hydrogens on the original body shall be replaced.” (c) If the bed body is in the bed (O), two hydrogens on the original body shall be replaced.” (d) In addition, the specification of the prior invention states that “if the bed body is in the bed (O), two hydrogens on the original body shall be replaced. (d)

In the case of a prior invention caused by a cause, both the cases of the combination of gens into the basic structure of the Hven B and the examples of implementation that do not combine the gens. Considering the description of the prior invention in the specification of the prior invention, it is difficult for a person with ordinary skills to expand the scope of the prior invention even in the case of a herotocin structure where at least 5 to 6 nitrogens with one sediment B are the herotocin with one gens.

According to the evidence No. 21, prior inventions can be recognized as having been registered as a patent for a traffic response in the U.S. and Canada. According to the above recognition facts, the patentee of the instant patent invention also seems to have been aware that prior inventions include a traffic response (However, the Plaintiff asserts that the inventor of the instant patent invention was unaware of such fact at the time of the application for the patent of the instant patent invention and was aware of such fact. However, according to his own assertion, the Plaintiff did not answer to the statement of this court as to the prior invention without any suggesting suggesting that the inventor would be specifically aware of the graphic response.

(C) The Plaintiff asserts that the prior invention contains more than a hundred billion chemical compounds in general, and that it is extremely difficult to derive a traffic response from the prior invention without any motive or implication to derive a traffic response. Therefore, the Plaintiff’s assertion cannot be accepted for the following reasons: (a) generalization of the prior invention into the upper concept of the prior invention into the lower concept of the traffic response team; and (b) generalization of the prior invention into the upper concept of the prior invention; and (c) extension to the lower concept, such as the traffic response team of the instant Claim 1. However, the Plaintiff’s assertion cannot be accepted:

(1) An ordinary skilled person would like to identify and find out the characteristics of the invention that are expected to have characteristics similar to the prior invention in consideration of the start of the subordinate concepts that are selectively indicated on the basis of the example of the prior invention in practice, and the structurally similar subordinate concepts that are directly perceived as the upper concept of the prior invention. Therefore, it is difficult to conclude that the prior invention does not give a motive to choose the subordinate concepts of the selective invention or that the contents that can expand the scope of the upper concept of the selective invention are not commenced in the prior literature that can grasp the upper concept of the prior invention, solely on the ground that the number of the prior inventions is written in general, and all the elements of the selective invention have not been explicitly commenced in the process of executing it (or, in case where all the constituent elements of the selective invention are explicitly stated in the prior invention or can be directly recognized, newness of the selective invention can be an issue).

② As seen earlier, prior inventions have limited the structure that can be selected over several stages, and present the direction of desirable compound. Through this, prior inventions have significantly decreased the size of the prior inventions in which the selective elements of the instant Claim No. 1 can be derived, and have presented the structure with specific chemical formula rather than general formula.

③ It is not clearly indicated in prior inventions as to how the Pestidine connects to Pest A, the adjacent structure of the Pestidine, and whether the Pest (O) is introduced into any of the Pestidine. However, considering the following factors: (a) the location of Pestidine, where Pest (O) can be converted into the Pestest; (b) the location of the Pestidine is only five (the part marked as Pesting Pest), and the two factors are more than five (5) when considering the overall structure of Pestidine, in addition to the general structure of Pestest, it is difficult to consider that the Pestidine can be converted into another structure; and (c) the location at which Pestidine can be connected to Pest A (excluding one location set up as Pest (O) at six (6) locations indicated as red chloblosis). In light of the fact that Pest B has a H structure, it is difficult to see that the Pest et al. can not be introduced into Pest (hereinafter referred to as “PH”).

④ The Plaintiff asserts to the effect that it is difficult to predict 5 selective elements because it is highly likely to cause an unexpected reaction. However, considering the fact that the process of selecting individual structure commenced in the prior invention and the process of combining the actual selected structure cannot be the same, the process of selecting the individual structure initiated in the prior invention cannot be said to be the same, the (b) the selection of the PPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPPP

(3) Comprehensively taking account of the above, it cannot be deemed that there is a negative response or implication to exclude the graphic elements of the instant Claim No. 1 in the prior invention, and it can be deemed that a person with ordinary skills generalizing the instant Claim No. 1 into the upper concept of the prior invention and expanding it to the lower concept such as the graphic group. Therefore, in determining the inventive step of the instant Claim No. 1, it cannot be deemed that a strict patent requirement should be mitigated in determining the inventive step of the instant selective invention.

C) Whether there is a dual or significant effect;

Therefore, it is necessary to examine whether the aforementioned selective invention has a qualitative or quantitative effect compared to the prior invention in order to determine whether the inventive step of the instant Claim No. 1 is inventive step.

(1) As to the dual effect of the instant Claim 1 invention

(A) Effects of improving pharmacologicalal characteristics

According to the specification of the instant patent invention, the Plaintiff asserts to the effect that the instant Claim No. 1 invention has both (a) through (g) as indicated below, and that the effect of improving the pharmacological characteristics that have not been commenced at all on the prior invention is sufficient to have a positive effect. As such, the Plaintiff asserts to the effect that the qualitative effect of the instant Claim No. 1 invention can be clearly known through the specification of the instant patent invention is “low clean rate of 18), Note 19, and simple whites.”

(x)The distribution volume means the volume of volume (Vd) required for containing the total quantity of drugs in the body when the drugs are assumed to exist in the body as a concentration such as blood concentration in the body as a whole.

It is also desirable to find a new chemical compound with improved pharmacological characteristics compared to publicly known human Xa control system. For example, it is desirable to find a new chemical compound with improved emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emeric emerc.

However, for the following reasons, it is difficult to view that the instant Claim 1 invention has a dynamic effect to improve the pharmacological characteristics when compared with the prior invention.

① The effect of the invention refers to whether the invention can be used specifically for any industrial purpose. In light of the language and text of the specification of the patented invention in this case, it must be included in the specification. In light of the language and text of the specification of the patented invention in this case, the effect claimed by the Plaintiff is merely stated generally and abstractly so that it can be interpreted, and the technical significance or usefulness of the patented invention in this case does not clearly be clearly notified. (B) The patented invention in this case starts with a large number of general chemical compounds containing not only traffic team as a human Xa control system, but also a large number of general chemical compounds including it. (c) The above description is included in the specification of the patented invention in this case as well as in the specification of the patented invention in this case. (d) how efficient and special graphics can be used for the purpose of treating the patented invention. (e) In addition, it is not desirable to find out the characteristics of the patented invention in this case as a potential solution for treatment of the thirropical disorder.

② There is a characteristic that it is difficult to see that the Plaintiff is in fact consistent with the graphic team among the features indicated in the graphic group that the Plaintiff claims that the instant Claim No. 1 pertains to the Pacific Team. In other words, the ELquis set, which includes the Pacific Team as an active ingredient, is a drug that takes 2.5§¯ or 5§¯ prescribed at two times a day (Article 33-1, 2), and it is difficult to see that the characteristics indicated in (b) above (a) (i.e., taking once a day) correspond to the characteristics of the graphic group, and there is no objective material to see that (a) characteristics (i) are consistent with the characteristics of the graphic group.

(3) Even if only the characteristics of (c) and (d) above are described in the “effective effect on the combination of traffic lines, clean rate, and cross-steination,” the invention of paragraph (1) of this case, considering the following circumstances, it is difficult to see that the effect of improving the combination of desirable distribution, clean rate, and cross-steination can be clearly known from the above mentioned.

In addition, if Gap evidence Nos. 17, 18, 22, and Eul evidence Nos. 24 added the purport of the whole pleadings, it is acknowledged that the characteristics of blood’s maximum concentration-minimum (pek-to-to-be) weight in blood are reduced, barring special circumstances, in proportion to the distribution volume and against clean rate. The highest-minimum blood concentration ratio in blood products are expressed to a certain degree of change depending on the hours of the drug concentration in blood products. The highest-minimum blood concentration ratio in blood products is reduced when the clean rate is lower. Meanwhile, as the blood concentration in drugs are reduced slowly, it seems desirable to reduce the characteristics of blood’s maximum-to-minimum (pek-to-beug) level in blood products. Accordingly, it seems desirable for a person with ordinary skills adjacent to the characteristics to describe the characteristics of the drugs, to have made it clear that the distribution rate is high and low.

(State 20)

(B) Meanwhile, according to the evidence Nos. 24 and 48, when assumed that the drugs exist in the body as a concentration such as blood concentration in the body as a whole, the drugs aimed at raising the volume of the drugs in the body, which are necessary to contain the total quantity, are widely distributed within the body. Therefore, considering the fact that the single-bred substance, which the invention in paragraph (1) of this case is a body Xa in blood, is located in the body, it may be interpreted that it is desirable that the drugs are not distributed within the body and the blood distribution is combined with the blood distribution at a lower level than that of the blood distribution in order to increase the concentration in the body. Accordingly, it would be desirable for a person of ordinary skill abutting on the characteristics of paragraph (d) to have low distribution volume and the blood distribution percentage, which is desirable to have lower the blood distribution percentage.

In light of the technological awareness at the time of the filing date of the priority claim for the patented invention of this case, the instant clause provides for desirable characteristics from the description on the characteristics of (c) and (d) to derive the opposite direction in the distribution of ordinarily skilled persons. Therefore, it is difficult to see that the instant clause provides a clear direction-setting for the pharmacological characteristics of the traffic response group. Furthermore, according to the instant clause, according to the instant clause, the combination rate of traffic response is lower. In fact, the Plaintiff also recognized that the combination rate of traffic response is 87% (as of October 22, 2018, the briefs No. 14), and the said number is more than the graphic characteristics of the instant clause 1 invention of this case, and it is difficult to see that the combination rate of traffic response is more than the graphic characteristics of the instant clause 1 invention of this case (as of October 22, 2018, the Plaintiff also recognized that the combination rate of traffic response is more than 87%.

④ According to the statements in Eul evidence Nos. 24 and 48, blood supplied to the organization, the combination with the blood stegrology, the combination with the blood stegrology, the stegrology of tissue cells, the pH difference between the external size of tissue cells and the internal organ of tissue cells, the molecule of drugs, and the molecule of drugs, etc. are recognized as having an impact on the molecule's geographical features or the combination with the tissue components, etc. However, the specification of the patented invention in this case does not appear to have a difference in the molecule characteristics such as the throid's electrical characteristics, geographical features, etc. Therefore, it seems difficult for a drug molecule to have a molecule's comprehensive technological characteristics, such as the distribution rate, the molecule's molecule's molecule, the combination with the tissue components, the combination with the tissue components, and the distribution of drugs, etc. in this case's average properties in the shape of an electric molecule.

⑤ According to the evidence evidence Nos. 3, 4, and 9, the identification number of the patented invention of this case is included in the plaintiff's specification of other applied invention. Among them, Xa control of the patented invention of this case and the goal of the pharmacologicalal characteristics of the patented invention of this case is different from that of the patented invention of this case.

(6) Unlike the common sense of an ordinary engineer at the time of filing an application, the Plaintiff asserts that it is desirable for the applicant to have a low distribution volume of the instant Claim 1 invention. If the dynamic nature of the traffic response is contrary to the ordinary engineer’s common sense, as alleged by the Plaintiff, the Plaintiff’s assertion that it is a dual effect against the ordinary engineer’s common sense would be understood that the ordinary engineer would be more specific and clear in the specification of the patented invention, and that it would have such a dual effect. Ultimately, the Plaintiff’s assertion that a person with ordinary skills would have sufficiently understood the dynamic nature of the traffic response, and that it is inconsistent with the ordinary technological sense, is inconsistent with the assertion that a person with the foregoing specification alone would be able to understand the dynamic nature of the traffic response.

7) The Plaintiff asserts that, even if it is based on the additional experimental data (Evidence A9 and 10) prior to the date on which the priority claim for the instant patent invention was claimed, the dynamic characteristics can be confirmed. However, it cannot be readily concluded that the above additional experimental data cannot be confirmed prior to the date on which the instant patent invention was claimed. The structure of the 55,61,221, and 1053, which is to be compared with the additional experimental data, is difficult to readily conclude that it is the most similar structure with the graphic team among the compounds explicitly launched in the prior invention, due to the difference between the two parts of the complex’s nuclear structure or dental ventilation. Even if it is confirmed prior to the date on which the priority claim was made, it is difficult to clearly consider the effect of the instant patent invention’s completion on the basis of comparative data not included in the specification as long as it is possible to confirm the qualitative difference in the description on the invention’s priority claim, and it is difficult to clearly consider the effect of the patent invention’s completion of the instant invention’s invention’s selection to a third party.

(b) The effects of the soldier's operations;

The Plaintiff asserts to the effect that the instant Claim No. 1 invention confirmed the possibility of co-treatment with the various drugs not disclosed in the prior invention, and that the dual effect is recognized.

However, considering the aforementioned facts, the evidence Nos. 2, 4, 10, 12, Eul’s evidence Nos. 12-14, Eul’s evidence Nos. 55 and the following circumstances, it is difficult to view that the instant Claim No. 1 invention has a qualitative effect in terms of pathination when compared with the prior invention.

1. According to the specification of the prior invention, “the chemical compound of this invention may be administered independently or in combination with more than one kind of additional medicine. They include other anti-incrimination or anti-incrimination, anti-psychotropic blood plateination, or blood plate control agents, CD-incrimination, or emulation or removal from blood exclusive use or fibers for fiber,” the prior invention does not limit the scope of the additional medicine as shown above, while presenting an additional medicine that may be combined with the chemical compound of the prior invention, such as anti-incrimination, anti-incrimination, anti-incrimination, blood plateination, e-incination, e-incination, removal from blood exclusive use, and removal from fiber.”

2. The specification of the patented invention of this case contains other anti-corromatic agents or colonies, anti-diverosisic agents or blood-malivation agents, anti-divation agents, removal from blood exclusive use or fiber removal, anti-divation agents, anti-climatic pressure agents, calcium blocking agents (L-T-T-T-T-T-T-T-T-T-T), heart glycium clocks, climaticcium clocks, sposte E-Ethroids control agents, cliffics/ geological degradations, hurology, and geological file method, anti-hurine urine, anti-hymosis (slod and non-slodroids), thalivosiss, alternative anti-gymosiss, hyphalodic agents' growth factors, and all kinds of thirralkine climatics, etc. of this case, which are difficult to do.

③ According to the statements in Eul evidence Nos. 11 and 12, the plaintiff stated the same medical drugs as the patented invention of this case in the specification of patent application for different medicines, the structure of which differs from that of the Claim No. 1 invention of this case. Thus, it is difficult to view that the plaintiff actually confirmed that the medical drugs listed in the specification of the patented invention of this case can be used concurrently with the graphic team.

④ Among the medicines listed in the specification of the instant patent invention (identification No. 12, No. 12, No. 8, No. 12, and No. 12, No. 8, No. 837) are included in the “GPIIbb/IIIa receptors,” which are not recommended for traffic and pathology, and Tropiaidine (Clopidogggggggggggggggggs)”.

⑤ The Plaintiff asserts that, when there is a risk of a stroke and a large strophal chronological chronological chronological chronological chronological chronological chronological chronological chronological chronological chronological chronological chronological chronological cronological chronological chronological cronological chronological cronological chronological cronological c

However, as seen earlier, insofar as it is difficult to find it clear that there is no specific content to confirm the qualitative difference in the pedagogic administration in the specification of the instant patent invention, it cannot be the basis for the determination of inventive step by taking account of the results of the additional test, insofar as it is difficult to deem such a qualitative effect to have been clearly indicated. Furthermore, even if the examination results were to be considered, it is difficult to see that the examination results include only the rate of each classification of patients as a result of classifying the ARISTRE test, the excessive side effects of the pedagogic administration, the pedagogic administration group, and the pedagogic administration group, and it is difficult to see that the pedagogic administration and the pedagogic administration were to have a relatively relative safety in comparison with the pedagogic administration, and that it is difficult to see that the pedagogic administration and the pedagogic administration were all likely to cause serious side effects on the pedagogic administration and the pedral administration test.

(2) As to the substantial effect of the instant Claim 1 invention

(A) Effect of the preceding invention

Prior inventions provide human Xa-friendly chemical compounds with low levels of Ki, which are related to the Hague-containing compounds containing nitrogens as human Xa's control, and are capable of combining with additional treatment materials, including anti-pactic agents or anti-pactic agents, etc.

(B) Effect of the instant Claim 1 invention

The specification of the instant patent invention contains the following as to the effects of the instant Claim No. 1 invention. According to the foregoing, the instant Claim No. 1 invention pertains to the pharmaceutical products containing the human Xaly control-containing compounds and the anti-conception agents for treatment of chronological disorder, and the compound of the instant Claim No. 1 invention is capable of infection with other drugs and human friendly friendly friendliness, so it can be seen that the instant Claim No. 1 invention has excellent effect as a co-control system.

본문내 포함된 표 본 발명은 일반적으로 트립신-유사 세린 프로테아제 효소, 특히 인자 Ⅹa의 억제제인 락탐-함유 화합물 및 그의 유도체, 이들을 함유하는 제약 조성물 및 혈전색전성 장애 치료용 항응고제로서 상기 물질을 사용하는 방법에 관한 것이다. (식별번호 [1]) 상기 분석에서 시험된 화합물은 Ki ≤ 10μM로 나타나는 경우에 활성인 것으로 고려된다. 본 발명의 바람직한 화합물은 Ki ≤ 1μM이다. 본 발명의 더욱 바람직한 화합물은 Ki ≤ 0.1μM이다. 본 발명의 더욱더 바람직한 화합물은 Ki ≤ 0.01μM이다. 본 발명의 더더욱 바람직한 화합물은 Ki ≤ 0.001μM이다. 상기 기재된 방법을 사용하여, 본 발명의 다수의 화합물이 Ki ≤ 10μM를 나타내는 것으로 밝혀졌으며, 이로써 본 발명의 화합물의 효과적인 Ⅹa 억제제로서의 유용성이 확인되었다. (식별번호 [828]) 본 발명의 화합물은 또한 세린 프로테아제, 특히 인간 트롬빈, 인자 Ⅶa, 인자 Ⅸa, 인자 XIa, 우로키나제, 혈장 칼리크레인 및 플라즈민의 억제제로서 유용하다. 이들의 억제 작용때문에, 이들 화합물은 상기 효소군으로 촉매화되는, 생리적 반응인 혈액 응고 및 염증의 예방 또는 치료에 사용되는 것으로 나타난다. 구체적으로, 화합물은 상승된 트롬빈 활성으로부터 발생하는 질환, 예컨대 심근 경색증 치료용 약물로서, 및 진단 및 다른 상업적 목적을 위한 혈액에서 혈장으로의 처리에서 항응고제로 사용되는 시약으로서의 유용성을 갖는다. (식별번호 [830]) 본 발명의 화합물은 단독으로 또는 1종 이상의 추가의 치료제와 함께 투여될 수 있다. “함께 투여” 또는 “조합 치료”는 본 발명의 화합물 및 1종 이상의 추가의 치료제가 치료될 포유동물에게 동시에 투여되는 것을 의미한다. 함께 투여되는 경우, 이러한 성분들은 동일한 시간에 또는 상이한 시점에서 임의의 순서로 순차적으로 투여될 수 있다. 따라서 각 성분은 별도로 투여될 수 있으나, 목적하는 치료 효과를 제공하도록 충분히 근접한 시간으로 투여될 수 있다. 추가의 치료제는 다른 항응고제 또는 응고 억제제, 항-혈소판제 또는 혈소판 억제제, 트롬빈 억제제, 혈전용해제 또는 섬유소용해제, 항부정맥제, 항고혈압제, 칼슘 채널 차단제(L-타입 및 T-타입), 심장 글리코시드, 이뇨제, 전해질코르티코이드 수용체 길항제, 포스포디에스테라제 억제제, 콜레스테롤/지질 강하제 및 지질 프로파일 요법, 항당뇨제, 항우울제, 항염증제(스테로이드 및 비스테로이드), 항골다공증제, 호르몬 대체 요법, 경구용 피임약, 항비만제, 항불안제, 항증식제, 항종양제, 항궤양제 및 위식도 역류 질환제, 성장 호르몬 및(또는) 성장 호르몬 분비 촉진제, 갑상선 모방제(갑상선 수용체 길항제 포함), 항감염제, 항바이러스제, 항박테리아제 및 항진균제를 포함한다. (식별번호 [833], [834]) 본 발명의 화합물(즉, 제1 치료제)을 1종 이상의 추가의 치료제(즉, 제2 치료제)와 함께 투여하는 것은, 바람직하게는 각각을 더 낮은 투여량으로 사용할 수 있도록 하면서(즉, 상승효과 조합물), 바람직하게는 화합물 및 제제를 단독으로 투여한 것에 비해 효능의 이점을 제공한다. 낮은 투여량은 부작용의 가능성을 최소화하여, 안전성을 증가시킨다. 1종 이상의 치료제를 치료 투여량 미만으로 투여하는 것이 바람직하다. 모든 치료제를 치료 투여량 미만으로 투여하는 것이 더욱 바람직하다. 투여량 미만은 치료제 자체로 치료할 증상 또는 질환에 대해 목적하는 치료 효과를 제공하지 못하는 치료제의 양을 의미한다. 상승 효과 조합은 조합의 관찰된 효과가 단독으로 투여된 개별 제제의 합계보다 더 큰 것을 의미한다. (식별번호 [858])

Thus, the prior invention and the instant Claim No. 1 invention are identical in effect in that both of them intend to provide human Xa-friendly and with other medicines that are highly luxa-friendly and that are able to lusent with other medicines. On the other hand, the specification of the instant patent invention is identical in that the instant patent invention is subject to further commencement of medicine, such as navigation fraud, appeal blood pressure, knium channel blocking (L-other and T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-T-E-E-E-E-

(c)an assessment of the effects of human Xa-friendly;

이 사건 특허발명의 명세서에는 Ki 값에 대하여 “상기 분석에서 시험된 화합물은 Ki ≤ 10μM로 나타나는 경우에 활성인 것으로 고려된다. 본 발명의 바람직한 화합물은 Ki ≤ 1μM이다. 본 발명의 더욱 바람직한 화합물은 Ki ≤ 0.1μM이다. 본 발명의 더욱더 바람직한 화합물은 Ki ≤ 0.01μM이다. 본 발명의 더더욱 바람직한 화합물은 Ki ≤ 0.001μM이다. 상기 기재된 방법을 사용하여, 본 발명의 다수의 화합물이 Ki ≤ 10μM를 나타내는 것으로 밝혀졌으며, 이로써 본 발명의 화합물의 효과적인 Ⅹa 억제제로서의 유용성이 확인되었다.”(식별번호 [828])라고 기재되어 있고, 일반적으로 Ki 값이 낮을수록 인자 Xa 친화력이 높다고 평가되는데, 이 사건 제1항 발명의 Ki 값이 앞서 살펴본 선행발명에 개시된 화합물의 바람직한 Ki 값의 범위(≤ 0.001μM)와 유사하므로 인자 Xa 친화력 측면에서 양 발명의 효과가 양적으로 현저한 차이가 있다고 보기 어렵다.

게다가 이 사건 특허발명 명세서에는 개별 화합물의 Ki 값을 확인할 수 있는 기재가 전혀 없고, “본 발명의 더더욱 바람직한 화합물은 Ki ≤ 0.001μM이다. 상기 기재된 방법을 사용하여, 본 발명의 다수의 화합물이 Ki ≤ 10μM를 나타내는 것으로 밝혀졌으며”라고만 기재하여 Ki 값을 측정하는 일반적인 방법을 개시하고 있을 뿐이어서, 이 사건 특허발명 명세서에 기재된 화합물의 Ki 값이 이 사건 제1항 발명의 아픽사반에 관한 것이라고 단정할 수도 없으므로 이 사건 제1항 발명이 선행발명에 비해 양적으로 현저한 차이가 있음을 확인할 수 있는 정량적 기재가 있다고 보기도 어렵다.

As to this, the Plaintiff asserts to the effect that the instant Claim No. 1 invention has a remarkably low level of Ki value compared with that of prior inventions, which are the most similar structure, 99, and that it should be recognized as an excellent Xa control effect of the instant Claim No. 1 invention.

① However, as seen earlier, insofar as the structure different from the invention of this case can be directly recognized from the prior invention, 9,221, which is the most similar to the invention of this case, 9,221, which is the first invention of this case, are deemed to have different structure, and thus, it cannot be compared with the human Xa control effect (Ki value). ② Furthermore, 99,221, which includes the halogen source (F and fire), which is to be located in the air ventilation Z, is anticipated to have a very different nature of ventilation compared with the first invention of this case, and thus, it is difficult to see that it is inappropriate to select the first invention of this case as a compound to prepare for the invention of this case among the prior invention of this case, and ③ the Plaintiff’s assertion that the effect of the second invention of this case is obvious compared to that of the first invention of this case, it is difficult to see that the first invention of this case, which has a significant effect on the second invention of this case, is clearly accepted.

On the other hand, the plaintiff asserts that even though the 61st and 1053 prior inventions were held in low Ki value, it can not be developed as a drug due to toxic and heating dynamic characteristics, so only the graphic team of the claim 1 invention of this case should be recognized as a suppression effect.

However, whether the instant Claim 1 invention has significantly improved the human Xa control effect compared to the prior invention can only be determined on the basis of human Xa-friendly (Ki value). As a separate effect that reduces toxicity or improves the pharmacological characteristics, each of the effects of which is different from the prior invention is determined individually, and thus, the Plaintiff’s assertion itself is without merit. Furthermore, as seen earlier, the effect of the reduction of toxicity or the improvement of the pharmacological characteristics is not specified in the specification of the instant patent invention, and thus, such effect cannot be considered in the determination of the inventive step of the instant Claim 1 invention. The Plaintiff’s assertion also cannot be rejected.

(3) Results of review

In full view of the above circumstances, it is difficult to view the instant Claim 1 invention as having the same effect as above, since it cannot be deemed that the instant Claim 1 invention has a qualitative effect, such as improving the pharmacologicalal characteristics and parallel effects compared to the prior invention, or that there is a clear statement on the quantitative effect of human Xa-friendly friendliness.

(iii) reorganization;

Therefore, the nonobviousness of the instant Claim 1 invention is denied, since it is a selective invention and does not have a quantitative or quantitative effect compared to the prior invention.

C. Whether the invention of this case was inventive step

The Claim 2 invention of this case contains only a traffic response to the Claim 1 invention, and does not add a new inventive step to the “a compound indicated as the next chemical formula 1 (traffic response)”. Accordingly, the nonobviousness of the Claim 2 invention of this case is denied on the ground that it is an selective invention and is identical to Claim 1 invention of this case.

D. Sub-committee

In full view of the above, since the nonobviousness of the patented invention of this case is denied, the patent should be invalidated, and the trial decision of this case, which is consistent with the conclusion, is legitimate.

4. Conclusion

Thus, the plaintiff's claim seeking the revocation of the trial decision of this case is dismissed as it is without merit.

Judges Yoon Sung-sung(Presiding Judge) (Presiding Judge)

Note 1) Chemical Type 1’s chemical name is “1-(4-mephenyl), 7-prox-6- [4-(2-pentine-1-Padidiphenyl) -4,5,6,7-tetrade-1H-Pastro [3.4-c], 4-c], 4, 6,7-tetrade-1 H-Pastro (3-c], and the general name is Aapban; hereinafter referred to as “Athaban”.

Note2) The Heterterocycle or the heterocycide compound refers to a compound of a structure (the heterocycide) which contains the original part of the main part of the siterium among those of the hetera structure (e.g. Heterterocycle) carbon compounds. The Heterobiocycle refers to a solid structure compound in which two or more compounds of the heterocide are jointly owned by one or more combinations.

Note 3)

(4) On March 26, 2018, the Plaintiff withdrawn the lawsuit against Aju Drugs Co., Ltd., which was pending in the instant lawsuit.

Note 5)

6) Defendant NVA Co., Ltd. did not submit a reply or a preparatory document in the instant lawsuit. However, the procedural acts, such as the assertion of non-obviousness by other Defendants, which are similar indispensable co-litigation, are more beneficial to the said Defendant.

Note 7) The desirable implementation pattern at the second stage is the same as the claim 2.

Note 8) The desirable implementation pattern at 9 levels is the same as the claim 9.

주9) 알콕시기 가운데 탄소가 하나인 것을 메톡시기(-OCH₃)라 한다.

10) As can be seen, in the case of selective inventions, patentability is recognized to the effect that the upper concept was publicly announced but has an unexpected special effect. As such, instead of applying strict standards to the requirements for inventive step among the requirements for patents, it can be deemed that the specific requirements for inventive step are applied to the specific requirements.

11) Furthermore, as in this case, inventions in the field of chemistry or medicine, which are experimental science, may differ depending on the content and level of technology of the invention in question, but it is considerably short of predictability. Therefore, even if the composition of a substance is known, it is difficult to recognize or understand the effects of the invention by commencing only the composition of the invention in the specification.

Note 12) Prior Invention limits the structure described in the general formula to the 7th stage, but there is a difference in the choice of each stage to the 7th stage. The 2nd stage is to limit the choice of mother nuclear structure G, A, and B, and the 3nd stage is to limit the choice of mother nuclear structure and unit G, and the 4,5,6th stage is to limit the choice of festing G, Z, A, and B (the 4nd stage is to the air ventilation G, the 5th stage is to the air ventilation G, and the 6th stage is to limit the choice of festing A and B). The 7th stage is to limit the compound described in the general formula to the 9th stage in the general formula. In addition, the 8th stage is to limit the structure that is described in the 9th stage to the 9th stage in the general formula.

Note 13) During the 7-stage ventilation, it is also indicated as “blorinated”. This seems to include a large number of selective elements 4 in the event that two biphenyls have the dynamics of 5-Hion B, which are examined below, a compound directly combined with the two biphenyls, and the structure of the -A-B is in the form of two biphenyls.

Note 14)

Note 15) Also, prior inventions initiate the method of synthesis of the mother structure, and explain that prior inventions may be manufactured by a publicly known method to ordinary technicians, WT 97/23212, WT 97/30971, WT 97/38984, WT 98/0694, WT 98/0694, WT 98/01428, WT 98/28269, and WT 98/2828282, and WT 98/28289 (96 pages 1-5), among which WT 98/28269, WT 98/28269 began to have been integrated into the air ventilation B(O) (the reference materials are 6 international patent disclosure 98-28269).

(16) While the Plaintiff cannot extend or generalize the technical features of the prior invention to the subordinate concepts containing the traffic response of the instant Claim No. 1, the Plaintiff asserts that, in light of the legal principles of the Supreme Court Decision 2004Hu1120 Decided May 11, 2006, it is difficult to view the aforementioned legal principles as applicable to the prior invention. Although the purport of the Plaintiff’s assertion is not clear, the Plaintiff’s assertion is not clear, but rather, with the focus on the former proposal.

17) Moreover, it is difficult to view the prior invention as an invention with the characteristic of the introduction of the Kenya after having introduced the Hague Cate. Moreover, since the method of adopting a structure that includes the structure of search structure into the chemical process (such as subsponsing, etc.) has already been widely known in the organic synthetic field prior to the date on which the priority claim for the patent invention of this case was claimed, it would not be difficult to introduce the pentpinus itself into the air ventilation B by using it. Furthermore, the combined reaction of the combination between A and the air ventilation B in the instant Claim 1 invention takes place between the elements of carbon and nitrogen, and the implementation of the prior invention took place between the elements of carbon and nitrogen. In light of the fact that a high compound, including the nitrogen, is initiated through a nitrogen, and the method of combining it is also indicated in the specification, it cannot be seen that such combination is not initiated at all (the plaintiff 2015).

Note 18) Clean rate: Cleaning rate, removal rate, and telegraphic clater, and the volume of the blood clater, in which drugs per unit are removed, means the volume of the blood clater, in which drugs are removed. The drugs and ambassadors absorptiond into the human body are finally emitted through kids, sap, etc. The major claters removed from the body are new clater (Clr) which are born through kid by kids, and the clateral clater (Clhhhh) which is born through kids and cocolons converted into the body of an ambassador. Ordinary drugs are most novels through them, and thus, claters (Clt) can be combined into claters (Clr) and claters (Clhhhhh).

Note 19)

Note 20)

Note 21) 21) LAW-Minimum (pek-to-be) characteristics: The highest and minimum drug concentration in blood changes depending on time, taking into account the highest and minimum concentration in blood and the ratio of the highest and minimum level of the blood in drugs.

Note 22) Even based on Gap evidence Nos. 33 submitted by the Plaintiff after the closing of argument, distribution volume of blood products cannot be determined solely by the intercombined ratio of non-combined type and the relationship between non-combined type and distribution volume of tissue. The relationship between non-combined type and distribution volume of blood products ought to be indicated by the non-combined type ratio of blood products in the organization. Therefore, it cannot be said that the distribution volume of blood products is low solely on the ground that the ratio of non-combined type of blood products is high.

Note 23) In particular, with regard to the implementation, 1053, 1043: (i) the option elements 1 to 4 are the same; (ii) the structure includes the Hague Tech, including the Kenya (O) and nitrogen (N); and (iii) the implementation process 1048 is the structure including the Hague Tech including the nitrogen (N) in which the selective elements 1 to 4 are the same and the nitrogen (N) are all the same, and there is no objective data that can be otherwise recognized.

Note 24) Even if the description of the patented invention of this case, unlike the Plaintiff’s assertion, states that “The administration of the compound of this invention (i.e., the first-class medicine) together with one or more additional medicine (i.e., the second-class medicine) would make it more desirable to use it as a lower-level medicine (i.e., the combination of rise effects), an desirable combination of compounds, and preparations, provide an advantage of efficacy, compared to the administration of the first class medicine (i.e. the first-class medicine),” which states that “The low-level dosage will increase safety by minimizing the possibility of side effects,” which is the same as the preceding invention (i.e., the first-class medicine). In light of the fact that it is difficult to view that there is a significant difference between the two inventions in terms of parallel effects.