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1. 发明公开

KR1020100043293A 펩티드유사 프로테아제 억제제 无效
公开(公告)号：KR1020100043293A
公开(公告)日：2010-04-28
申请号：KR1020107007135
申请日：2001-08-31
申请人： 버텍스 파마슈티칼스 인코포레이티드
发明人： 베이빈,로버트,에드워드 , 첸,슈,후이 , 라마,제이슨,에릭 , 스나이더,낸시,준 , 선,자이쳉,데이비드 , 테베,마크,조우지프 , 빅토르,프란쯔 , 왕,큐.,메이 , 잎,이본느,예,메이 , 콜라도,이반 , 가르시아-파레데스,크리스티나 , 파커,레이몬드사무엘3세 , 진,링 , 구오,데퀴 , 글래스,존,어빈
IPC分类号： C07D403/12 , C07D401/12 , A61K31/496 , A61P1/16
CPC分类号： C07K7/02 , A61K38/07 , A61K38/08 , A61K38/21 , A61K38/212 , A61K38/215 , A61K45/06 , C07D209/02 , C07D209/52 , C07K5/0202 , C07K5/0205 , C07K5/06052 , C07K5/0808 , C07K5/101 , C07K5/1016 , C07K7/06 , C07K14/005 , C12N2770/24222 , Y02P20/55 , A61K2300/00
摘要： The present invention relates to peptidomimetic compounds useful as protease inhibitors (1), particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.

2. 发明公开

KR1020080104382A 펩티드유사 프로테아제 억제제 失效
公开(公告)号：KR1020080104382A
公开(公告)日：2008-12-02
申请号：KR1020087025503
申请日：2001-08-31
申请人： 버텍스 파마슈티칼스 인코포레이티드
发明人： 베이빈,로버트,에드워드 , 첸,슈,후이 , 라마,제이슨,에릭 , 스나이더,낸시,준 , 선,자이쳉,데이비드 , 테베,마크,조우지프 , 빅토르,프란쯔 , 왕,큐.,메이 , 잎,이본느,예,메이 , 콜라도,이반 , 가르시아-파레데스,크리스티나 , 파커,레이몬드사무엘3세 , 진,링 , 구오,데퀴 , 글래스,존,어빈
IPC分类号： C07D401/12 , C07D403/12
CPC分类号： C07K7/02 , A61K38/07 , A61K38/08 , A61K38/21 , A61K38/212 , A61K38/215 , A61K45/06 , C07D209/02 , C07D209/52 , C07K5/0202 , C07K5/0205 , C07K5/06052 , C07K5/0808 , C07K5/101 , C07K5/1016 , C07K7/06 , C07K14/005 , C12N2770/24222 , Y02P20/55 , A61K2300/00
摘要： The present invention relates to peptidomimetic compounds useful as protease inhibitors (1), particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient. ® KIPO & WIPO 2009

3. 发明公开

KR1020100042296A 펩티드유사 프로테아제 억제제 无效
标题翻译：致敏蛋白抑制剂
公开(公告)号：KR1020100042296A
公开(公告)日：2010-04-23
申请号：KR1020107007138
申请日：2001-08-31
申请人： 버텍스 파마슈티칼스 인코포레이티드
发明人： 베이빈,로버트,에드워드 , 첸,슈,후이 , 라마,제이슨,에릭 , 스나이더,낸시,준 , 선,자이쳉,데이비드 , 테베,마크,조우지프 , 빅토르,프란쯔 , 왕,큐.,메이 , 잎,이본느,예,메이 , 콜라도,이반 , 가르시아-파레데스,크리스티나 , 파커,레이몬드사무엘3세 , 진,링 , 구오,데퀴 , 글래스,존,어빈
IPC分类号： C07C219/24 , C07D401/12 , C07D403/12 , A61P31/12
CPC分类号： C07K7/02 , A61K38/07 , A61K38/08 , A61K38/21 , A61K38/212 , A61K38/215 , A61K45/06 , C07D209/02 , C07D209/52 , C07K5/0202 , C07K5/0205 , C07K5/06052 , C07K5/0808 , C07K5/101 , C07K5/1016 , C07K7/06 , C07K14/005 , C12N2770/24222 , Y02P20/55 , A61K2300/00
摘要： The present invention relates to peptidomimetic compounds useful as protease inhibitors (1), particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及可用作蛋白酶抑制剂（1）的拟肽化合物，特别是作为丝氨酸蛋白酶抑制剂，更特别地涉及丙型肝炎NS3蛋白酶抑制剂; 中间体; 它们的制备方法包括对中间体的新型置换步骤。本发明还涉及药物组合物以及使用该化合物抑制HCV蛋白酶或治疗患有HCV感染或感染相关生理状况的患者的方法。还提供了药物组合，除一种或多种HCV丝氨酸蛋白酶抑制剂外还包含一种或多种表现出抗HCV活性的干扰素和/或一种或多种具有抗HCV活性的化合物和药学上可接受的载体，以及用于治疗或预防的方法使用该组合物的患者中的HCV感染。本发明还涉及用于治疗或预防患者HCV感染的试剂盒或药物包装。

4. 发明授权

KR100876472B1 펩티드유사 프로테아제 억제제 失效
标题翻译：空值
公开(公告)号：KR100876472B1
公开(公告)日：2008-12-31
申请号：KR1020037002880
申请日：2001-08-31
申请人： 버텍스 파마슈티칼스 인코포레이티드
发明人： 베이빈,로버트,에드워드 , 첸,슈,후이 , 라마,제이슨,에릭 , 스나이더,낸시,준 , 선,자이쳉,데이비드 , 테베,마크,조우지프 , 빅토르,프란쯔 , 왕,큐.,메이 , 잎,이본느,예,메이 , 콜라도,이반 , 가르시아-파레데스,크리스티나 , 파커,레이몬드사무엘3세 , 진,링 , 구오,데퀴 , 글래스,존,어빈
IPC分类号： C07D401/12
CPC分类号： C07K7/02 , A61K38/07 , A61K38/08 , A61K38/21 , A61K38/212 , A61K38/215 , A61K45/06 , C07D209/02 , C07D209/52 , C07K5/0202 , C07K5/0205 , C07K5/06052 , C07K5/0808 , C07K5/101 , C07K5/1016 , C07K7/06 , C07K14/005 , C12N2770/24222 , Y02P20/55 , A61K2300/00
摘要： The present invention relates to peptidomimetic compounds according to formula 1 useful as protease inhibitors (1), particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective process to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti-HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient. a pharmaceutically acceptable salt or prodrug thereof, or a solvate of such a compound, its salt or its prodrug, wherein: R 0 is a bond or difluoromethylene; R 1 is hydrogen, optionally substituted aliphatic group, optionally substituted cyclic group or optionally substituted aromatic group; R 2 and R 9 are each independently optionally substituted aliphatic group, optionally substituted cyclic group or optionally substituted aromatic group; R 3 , R 5 and R 7 are each independently an optionally substituted (1,1- or 1,2-) cycloalkylene, an optionally substituted (1,1- or 1,2-)heterocyclylene, methylene or ethylene, each substituted with one substituent selected from the group consisting -of an optionally substituted aliphatic group, an optionally substituted cyclic group or an optionally substituted aromatic group, and wherein the methylene or ethylene is further optionally substituted with an aliphatic group substituent; R 4 , R 6 , R 8 and R 10 are each independently is hydrogen or optionally substituted aliphatic group; is a substituted monocyclic azaheterocyclyl wherein the unsaturatation is in the ring distal to the ring bearing the R 9 -L-(N(R 8 )-R 7 -C(O)-) n N(R 6 )-R 5 -C(O)-N moiety and to which the -C(O)-N(R 4 )-R 3 -C(O)C(O)NR 2 R 1 moiety is attached; L is -C(O)-, -OC(O)-, -NR 10 C(O)-, -S(O) 2 -, or -NR 10 S(O) 2 -; and n is 0 or 1;
摘要翻译：本发明涉及可用作蛋白酶抑制剂（1）的式1的拟肽化合物，特别是作为丝氨酸蛋白酶抑制剂，更具体地，作为丙型肝炎NS3蛋白酶抑制剂; 中间体; 它们的制备方法包括对中间体的新型置换反应方法。本发明还涉及药物组合物以及使用该化合物抑制HCV蛋白酶或治疗患有HCV感染或感染相关生理状况的患者的方法。还提供了药物组合，除一种或多种HCV丝氨酸蛋白酶抑制剂外还包含一种或多种表现出抗HCV活性的干扰素和/或一种或多种具有抗HCV活性的化合物和药学上可接受的载体，以及用于治疗或使用组合物预防患者的HCV感染。本发明还涉及用于治疗或预防患者HCV感染的试剂盒或药物包装。其药学上可接受的盐或前药，或这种化合物，其盐或其前药的溶剂合物，其中：R 0是键或二氟亚甲基; R 1为氢，任选取代的脂族基团，任选取代的环状基团或任选取代的芳族基团; R 2和R 9各自独立地是任选取代的脂族基团，任选取代的环状基团或任选取代的芳族基团; R 3，R 5和R 7各自独立地为任选取代的（1,1-或1,2-）亚环烷基，任选取代的（1,1-或1,2-）亚杂环，亚甲基或亚乙基，各自被一个取代基，其选自任选取代的脂族基团，任选取代的环状基团或任选取代的芳族基团，并且其中所述亚甲基或亚乙基进一步任选被脂族基团取代基取代; R 4，R 6，R 8和R 10各自独立地为氢或任选取代的脂族基; 是取代的单环氮杂环基，其中不饱和位于带有R 9 -L-（N（R 8）-R 7 -C（O） - ）n N（R 6）-R 5 -C （O）-N部分并且连接有-C（O）-N（R 4）-R 3 -C（O）C（O）NR 2 R 1部分; L是-C（O） - ， - OC（O） - ， - NR 10 C（O） - ， - S（O）2 - 或-NR 10 S（O）并且n为0或1;

5. 发明公开

KR1020080096718A 펩티드유사 프로테아제 억제제 无效
标题翻译：致敏蛋白抑制剂
公开(公告)号：KR1020080096718A
公开(公告)日：2008-10-31
申请号：KR1020087025506
申请日：2001-08-31
申请人： 버텍스 파마슈티칼스 인코포레이티드
发明人： 베이빈,로버트,에드워드 , 첸,슈,후이 , 라마,제이슨,에릭 , 스나이더,낸시,준 , 선,자이쳉,데이비드 , 테베,마크,조우지프 , 빅토르,프란쯔 , 왕,큐.,메이 , 잎,이본느,예,메이 , 콜라도,이반 , 가르시아-파레데스,크리스티나 , 파커,레이몬드사무엘3세 , 진,링 , 구오,데퀴 , 글래스,존,어빈
IPC分类号： C07D403/12 , C07D401/12
CPC分类号： C07K7/02 , A61K38/07 , A61K38/08 , A61K38/21 , A61K38/212 , A61K38/215 , A61K45/06 , C07D209/02 , C07D209/52 , C07K5/0202 , C07K5/0205 , C07K5/06052 , C07K5/0808 , C07K5/101 , C07K5/1016 , C07K7/06 , C07K14/005 , C12N2770/24222 , Y02P20/55 , A61K2300/00
摘要： The present invention relates to peptidomimetic compounds useful as protease inhibitors (1), particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及可用作蛋白酶抑制剂的拟肽化合物（1），特别是作为丝氨酸蛋白酶抑制剂，更特别地涉及丙型肝炎NS3蛋白酶抑制剂; 中间体; 它们的制备方法包括对中间体的新型置换步骤。本发明还涉及药物组合物以及使用该化合物抑制HCV蛋白酶或治疗患有HCV感染或感染相关生理状况的患者的方法。还提供了药物组合，除一种或多种HCV丝氨酸蛋白酶抑制剂外还包含一种或多种表现出抗HCV活性的干扰素和/或一种或多种具有抗HCV活性的化合物和药学上可接受的载体，以及用于治疗或预防的方法使用该组合物的患者中的HCV感染。本发明还涉及用于治疗或预防患者HCV感染的试剂盒或药物包装。

6. 发明公开

KR1020080007515A 펩티드유사 프로테아제 억제제 失效
标题翻译： 펩티드유사프로테아제억제제
公开(公告)号：KR1020080007515A
公开(公告)日：2008-01-21
申请号：KR1020077029814
申请日：2001-08-31
申请人： 버텍스 파마슈티칼스 인코포레이티드
发明人： 베이빈,로버트,에드워드 , 첸,슈,후이 , 라마,제이슨,에릭 , 스나이더,낸시,준 , 선,자이쳉,데이비드 , 테베,마크,조우지프 , 빅토르,프란쯔 , 왕,큐.,메이 , 잎,이본느,예,메이 , 콜라도,이반 , 가르시아-파레데스,크리스티나 , 파커,레이몬드사무엘3세 , 진,링 , 구오,데퀴 , 글래스,존,어빈
IPC分类号： C07D401/12 , C07D403/12
CPC分类号： C07K7/02 , A61K38/07 , A61K38/08 , A61K38/21 , A61K38/212 , A61K38/215 , A61K45/06 , C07D209/02 , C07D209/52 , C07K5/0202 , C07K5/0205 , C07K5/06052 , C07K5/0808 , C07K5/101 , C07K5/1016 , C07K7/06 , C07K14/005 , C12N2770/24222 , Y02P20/55 , A61K2300/00
摘要： The present invention relates to peptidomimetic compounds useful as protease inhibitors (1), particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及用作蛋白酶抑制剂（1）的拟肽化合物，特别是作为丝氨酸蛋白酶抑制剂，更具体地作为丙型肝炎NS3蛋白酶抑制剂; 中间体; 其制备包括对中间体的新的选择性过程。本发明还涉及药物组合物和使用该化合物抑制HCV蛋白酶或治疗患有HCV感染或与感染有关的生理状况的患者的方法。还提供了除一种或多种HCV丝氨酸蛋白酶抑制剂之外还包含一种或多种表现出抗HCV活性的干扰素和/或一种或多种具有抗HCV活性的化合物和药学上可接受的载体的药物组合，以及治疗或预防使用该组合物的患者的HCV感染。本发明还涉及用于治疗或预防患者HCV感染的试剂盒或药物包装。

7. 发明授权

KR100945975B1 펩티드유사 프로테아제 억제제 失效
标题翻译：肽样蛋白酶抑制剂
公开(公告)号：KR100945975B1
公开(公告)日：2010-03-09
申请号：KR1020077029814
申请日：2001-08-31
申请人： 버텍스 파마슈티칼스 인코포레이티드
发明人： 베이빈,로버트,에드워드 , 첸,슈,후이 , 라마,제이슨,에릭 , 스나이더,낸시,준 , 선,자이쳉,데이비드 , 테베,마크,조우지프 , 빅토르,프란쯔 , 왕,큐.,메이 , 잎,이본느,예,메이 , 콜라도,이반 , 가르시아-파레데스,크리스티나 , 파커,레이몬드사무엘3세 , 진,링 , 구오,데퀴 , 글래스,존,어빈
IPC分类号： C07D401/12 , C07D403/12
CPC分类号： C07K7/02 , A61K38/07 , A61K38/08 , A61K38/21 , A61K38/212 , A61K38/215 , A61K45/06 , C07D209/02 , C07D209/52 , C07K5/0202 , C07K5/0205 , C07K5/06052 , C07K5/0808 , C07K5/101 , C07K5/1016 , C07K7/06 , C07K14/005 , C12N2770/24222 , Y02P20/55 , A61K2300/00
摘要： 본 발명은 프로테아제 억제제, 특히 세린 프로테아제 억제제 및 더욱 구체적으로는 C형 간염 NS3 프로테아제 억제제로서 유용한 하기 화학식 1의 펩티드유사 화합물; 그의 중간체; 신규 입체선택적 방법을 포함하는 중간체의 제조 방법에 관한 것이다. 또한, 본 발명은 제약 조성물, 및 HCV 프로테아제를 억제하거나 HCV 감염 또는 그와 관련된 생리적 증상을 앓는 환자를 치료하기 위해 화합물을 사용하는 방법에 관한 것이다. 또한, 1종 이상의 HCV 세린 프로테아제 억제제 외에, 항-HCV 활성을 나타내는 인터페론 및(또는) 항 HCV 활성을 나타내는 1종 이상의 화합물 및 제약상 허용되는 담체를 포함하는 제약 조성물, 및 상기 조성물을 사용하여 환자에서 HCV 감염증을 치료 또는 예방하는 방법이 제공된다. 또한, 본 발명은 환자에서 HCV 감염증을 치료 또는 예방하기 위한 키트 또는 약제 팩에 관한 것이다.

펩티드유사 프로테아제 억제제, C형 간염 바이러스 ("HCV") NS3 프로테아제 억제제, 키트, 약제 팩, 입체선택적 방법, 인터페론
摘要翻译：本发明是下述通式（1）是作为蛋白酶抑制剂，尤其是丝氨酸蛋白酶抑制剂，更具体地说，涉及丙型肝炎NS3蛋白酶抑制剂有用的肽类化合物; 它的中间; 还有一种新颖的立体选择方法。此外，本发明涉及使用该化合物治疗患者中抑制的药物组合物，和HCV蛋白酶，或从与HCV感染，或类似物相关的生理病症的患者的方法。另外，至少除了或多种HCV丝氨酸蛋白酶抑制剂，使用的药物组合物，其包含干扰素和（或），其中至少一个代表HCV活性化合物和示出抗-HCV活性的药学上可接受的载体，并且所述组合物的患者提供了治疗或预防HCV感染的方法。本发明还涉及用于治疗或预防患者中的HCV感染的试剂盒或药物包装。

8. 发明公开

KR1020090120013A 펩티드유사 프로테아제 억제제 无效
标题翻译：致敏蛋白抑制剂
公开(公告)号：KR1020090120013A
公开(公告)日：2009-11-23
申请号：KR1020097022810
申请日：2001-08-31
申请人： 버텍스 파마슈티칼스 인코포레이티드
发明人： 베이빈,로버트,에드워드 , 첸,슈,후이 , 라마,제이슨,에릭 , 스나이더,낸시,준 , 선,자이쳉,데이비드 , 테베,마크,조우지프 , 빅토르,프란쯔 , 왕,큐.,메이 , 잎,이본느,예,메이 , 콜라도,이반 , 가르시아-파레데스,크리스티나 , 파커,레이몬드사무엘3세 , 진,링 , 구오,데퀴 , 글래스,존,어빈
IPC分类号： C07D403/12 , C07D401/12
CPC分类号： C07K7/02 , A61K38/07 , A61K38/08 , A61K38/21 , A61K38/212 , A61K38/215 , A61K45/06 , C07D209/02 , C07D209/52 , C07K5/0202 , C07K5/0205 , C07K5/06052 , C07K5/0808 , C07K5/101 , C07K5/1016 , C07K7/06 , C07K14/005 , C12N2770/24222 , Y02P20/55 , A61K2300/00
摘要： The present invention relates to peptidomimetic compounds useful as protease inhibitors (1), particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及可用作蛋白酶抑制剂的拟肽化合物（1），特别是作为丝氨酸蛋白酶抑制剂，更特别地涉及丙型肝炎NS3蛋白酶抑制剂; 中间体; 它们的制备方法包括对中间体的新型置换步骤。本发明还涉及药物组合物以及使用该化合物抑制HCV蛋白酶或治疗患有HCV感染或感染相关生理状况的患者的方法。还提供了药物组合，除一种或多种HCV丝氨酸蛋白酶抑制剂外还包含一种或多种表现出抗HCV活性的干扰素和/或一种或多种具有抗HCV活性的化合物和药学上可接受的载体，以及用于治疗或预防的方法使用该组合物的患者中的HCV感染。本发明还涉及用于治疗或预防患者HCV感染的试剂盒或药物包装。

9. 发明公开

KR1020080104383A 펩티드유사 프로테아제 억제제 无效
标题翻译： 펩티드유사프로테아제억제제
公开(公告)号：KR1020080104383A
公开(公告)日：2008-12-02
申请号：KR1020087025504
申请日：2001-08-31
申请人： 버텍스 파마슈티칼스 인코포레이티드
发明人： 베이빈,로버트,에드워드 , 첸,슈,후이 , 라마,제이슨,에릭 , 스나이더,낸시,준 , 선,자이쳉,데이비드 , 테베,마크,조우지프 , 빅토르,프란쯔 , 왕,큐.,메이 , 잎,이본느,예,메이 , 콜라도,이반 , 가르시아-파레데스,크리스티나 , 파커,레이몬드사무엘3세 , 진,링 , 구오,데퀴 , 글래스,존,어빈
IPC分类号： C07D401/12 , C07D403/12
CPC分类号： C07K7/02 , A61K38/07 , A61K38/08 , A61K38/21 , A61K38/212 , A61K38/215 , A61K45/06 , C07D209/02 , C07D209/52 , C07K5/0202 , C07K5/0205 , C07K5/06052 , C07K5/0808 , C07K5/101 , C07K5/1016 , C07K7/06 , C07K14/005 , C12N2770/24222 , Y02P20/55 , A61K2300/00
摘要： The present invention relates to peptidomimetic compounds useful as protease inhibitors (1), particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient. ® KIPO & WIPO 2009
摘要翻译：本发明涉及用作蛋白酶抑制剂（1）的拟肽化合物，特别是作为丝氨酸蛋白酶抑制剂，更具体地作为丙型肝炎NS3蛋白酶抑制剂; 中间体; 其制备包括对中间体的新的选择性过程。本发明还涉及药物组合物和使用该化合物抑制HCV蛋白酶或治疗患有HCV感染或与感染有关的生理状况的患者的方法。还提供了除一种或多种HCV丝氨酸蛋白酶抑制剂之外还包含一种或多种表现出抗HCV活性的干扰素和/或一种或多种具有抗HCV活性的化合物和药学上可接受的载体的药物组合，以及治疗或预防使用该组合物的患者的HCV感染。本发明还涉及用于治疗或预防患者HCV感染的试剂盒或药物包装。 ®KIPO＆WIPO 2009

10. 发明公开

KR1020110088600A 펩티드유사 프로테아제 억제제 无效
标题翻译：致敏蛋白抑制剂
公开(公告)号：KR1020110088600A
公开(公告)日：2011-08-03
申请号：KR1020117015737
申请日：2001-08-31
申请人： 버텍스 파마슈티칼스 인코포레이티드
发明人： 베이빈,로버트,에드워드 , 첸,슈,후이 , 라마,제이슨,에릭 , 스나이더,낸시,준 , 선,자이쳉,데이비드 , 테베,마크,조우지프 , 빅토르,프란쯔 , 왕,큐.,메이 , 잎,이본느,예,메이 , 콜라도,이반 , 가르시아-파레데스,크리스티나 , 파커,레이몬드사무엘3세 , 진,링 , 구오,데퀴 , 글래스,존,어빈
IPC分类号： C07D403/12 , C07C219/24 , A61K31/497 , A61P31/12
CPC分类号： C07K7/02 , A61K38/07 , A61K38/08 , A61K38/21 , A61K38/212 , A61K38/215 , A61K45/06 , C07D209/02 , C07D209/52 , C07K5/0202 , C07K5/0205 , C07K5/06052 , C07K5/0808 , C07K5/101 , C07K5/1016 , C07K7/06 , C07K14/005 , C12N2770/24222 , Y02P20/55 , A61K2300/00
摘要： 본 발명은 프로테아제 억제제, 특히 세린 프로테아제 억제제 및 더욱 구체적으로는 C형 간염 NS3 프로테아제 억제제로서 유용한 하기 화학식 1의 펩티드유사 화합물; 그의 중간체; 신규 입체선택적 방법을 포함하는 중간체의 제조 방법에 관한 것이다. 또한, 본 발명은 제약 조성물, 및 HCV 프로테아제를 억제하거나 HCV 감염 또는 그와 관련된 생리적 증상을 앓는 환자를 치료하기 위해 화합물을 사용하는 방법에 관한 것이다. 또한, 1종 이상의 HCV 세린 프로테아제 억제제 외에, 항-HCV 활성을 나타내는 인터페론 및(또는) 항 HCV 활성을 나타내는 1종 이상의 화합물 및 제약상 허용되는 담체를 포함하는 제약 조성물, 및 상기 조성물을 사용하여 환자에서 HCV 감염증을 치료 또는 예방하는 방법이 제공된다. 또한, 본 발명은 환자에서 HCV 감염증을 치료 또는 예방하기 위한 키트 또는 약제 팩에 관한 것이다.
摘要翻译：本发明涉及可用作蛋白酶抑制剂（1）的式1的拟肽化合物，特别是作为丝氨酸蛋白酶抑制剂，更具体地，作为丙型肝炎NS3蛋白酶抑制剂; 中间体; 它们的制备方法包括对中间体的新型置换反应方法。本发明还涉及药物组合物以及使用该化合物抑制HCV蛋白酶或治疗患有HCV感染或感染相关生理状况的患者的方法。还提供了药物组合，除一种或多种HCV丝氨酸蛋白酶抑制剂外还包含一种或多种表现出抗HCV活性的干扰素和/或一种或多种具有抗HCV活性的化合物和药学上可接受的载体，以及用于治疗或使用组合物预防患者的HCV感染。本发明还涉及用于治疗或预防患者HCV感染的试剂盒或药物包装。其药学上可接受的盐或前药，或这种化合物，其盐或其前药的溶剂合物，其中：R 0是键或二氟亚甲基; R 1为氢，任选取代的脂族基团，任选取代的环状基团或任选取代的芳族基团; R 2和R 9各自独立地是任选取代的脂族基团，任选取代的环状基团或任选取代的芳族基团; R 3，R 5和R 7各自独立地为任选取代的（1,1-或1,2-）亚环烷基，任选取代的（1,1-或1,2-）亚杂环，亚甲基或亚乙基，各自被一个取代基，其选自任选取代的脂族基团，任选取代的环状基团或任选取代的芳族基团，并且其中所述亚甲基或亚乙基进一步任选被脂族基团取代基取代; R 4，R 6，R 8和R 10各自独立地为氢或任选取代的脂族基; 是取代的单环氮杂环基，其中不饱和位于带有R 9 -L-（N（R 8）-R 7 -C（O） - ）n N（R 6）-R 5 -C （O）-N部分并且连接有-C（O）-N（R 4）-R 3 -C（O）C（O）NR 2 R 1部分; L是-C（O） - ， - OC（O） - ， - NR 10 C（O） - ， - S（O）2 - 或-NR 10 S（O）并且n为0或1;

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