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    • 4. 发明授权
    • 펩티드유사 프로테아제 억제제
    • 空值
    • KR100876472B1
    • 2008-12-31
    • KR1020037002880
    • 2001-08-31
    • 버텍스 파마슈티칼스 인코포레이티드
    • 베이빈,로버트,에드워드첸,슈,후이라마,제이슨,에릭스나이더,낸시,준선,자이쳉,데이비드테베,마크,조우지프빅토르,프란쯔왕,큐.,메이잎,이본느,예,메이콜라도,이반가르시아-파레데스,크리스티나파커,레이몬드사무엘3세진,링구오,데퀴글래스,존,어빈
    • C07D401/12
    • C07K7/02A61K38/07A61K38/08A61K38/21A61K38/212A61K38/215A61K45/06C07D209/02C07D209/52C07K5/0202C07K5/0205C07K5/06052C07K5/0808C07K5/101C07K5/1016C07K7/06C07K14/005C12N2770/24222Y02P20/55A61K2300/00
    • 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;
    • 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;