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1. 发明授权

US08877761B2 N-pyrimidin-4-yl-3-amino-pyrrolo[3,4-c]pyrazole derivatives as PKC kinase inhibitors 有权
标题翻译： N-嘧啶-4-基-3-氨基 - 吡咯并[3,4-c]吡唑衍生物作为PKC激酶抑制剂
公开(公告)号：US08877761B2
公开(公告)日：2014-11-04
申请号：US13450388
申请日：2012-04-18
申请人： Hui Li , Seiji Nukui , Stephanie Anne Scales , Min Teng , Chunfeng Yin
发明人： Hui Li , Seiji Nukui , Stephanie Anne Scales , Min Teng , Chunfeng Yin
IPC分类号： A01N43/54 , C07D403/00 , C07D487/04
CPC分类号： C07D519/00 , C07D487/04
摘要： The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disase pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.
摘要翻译：本发明涉及式A和B的化合物和药学上可接受的盐：其中A，B，R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和R 10如上所定义。本发明还涉及包含该化合物和药学上可接受的盐的药物组合物以及治疗糖尿病及其并发症，癌症，局部缺血，炎症，中枢神经系统疾病，心血管疾病，阿尔茨海默氏病和皮肤病学抑制的病毒病，炎性疾病疾病或肝脏是靶器官的疾病。

2. 发明申请

US20120108588A1 NOVEL 3-AMIDO-PYRROLO[3,4-C]PYRAZOLE-5(1H, 4H,6H) CARBALDEHYDE DERIVATIVES 审中-公开
标题翻译：新的3-氨基吡咯并[3,4-C]吡唑-5（1H，4H，6H）二氢苯并噻吩衍生物
公开(公告)号：US20120108588A1
公开(公告)日：2012-05-03
申请号：US13345528
申请日：2012-01-06
申请人： Iriny Botrous , Yufeng Hong , Hui Li , Kevin Kun-Chin Liu , Seiji Nukui , Min Teng , Eileen Valenzuela Tompkins , Chunfeng Yin
发明人： Iriny Botrous , Yufeng Hong , Hui Li , Kevin Kun-Chin Liu , Seiji Nukui , Min Teng , Eileen Valenzuela Tompkins , Chunfeng Yin
IPC分类号： A61K31/5377 , A61K31/4985 , A61K31/499 , A61K31/496 , A61K31/506 , A61P3/10 , A61P35/00 , A61P9/10 , A61P29/00 , A61P25/00 , A61P9/00 , A61P25/28 , A61P17/00 , A61P31/12 , A61P1/16 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ.
摘要翻译：本发明涉及式（I）的化合物和药学上可接受的盐：其中X，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8如上所定义。本发明还涉及包含该化合物和药学上可接受的盐的药物组合物以及治疗糖尿病及其并发症（特别是糖尿病性视网膜病变，肾病或神经病变），癌症，缺血，炎症，中枢神经系统疾病，心血管疾病，阿尔茨海默病和皮肤病疾病，病毒性疾病，炎症性疾病或肝脏是靶器官的疾病。

3. 发明授权

US08119624B2 Fused phenyl amido heterocyclic compounds 有权
标题翻译：稠合苯基酰氨基杂环化合物
公开(公告)号：US08119624B2
公开(公告)日：2012-02-21
申请号：US12913059
申请日：2010-10-27
申请人： Hao Bai , Simon Bailey , Dilip Ramakant Bhumralkar , Feng C. Bi , Fengli Guo , Mingying He , Paul Stuart Humphries , Anthony Lai Ling , Jihong Lou , Seiji Nukui , Ru Zhou
发明人： Hao Bai , Simon Bailey , Dilip Ramakant Bhumralkar , Feng C. Bi , Fengli Guo , Mingying He , Paul Stuart Humphries , Anthony Lai Ling , Jihong Lou , Seiji Nukui , Ru Zhou
IPC分类号： A61K31/44 , A61K31/415 , A61K31/47 , A61K31/42 , A61K31/397 , A61K31/4965 , A61K31/41 , C07D215/00 , C07D401/00 , C07D413/00 , C07D405/00 , C07D403/00 , C07D231/00
CPC分类号： C07D405/14 , C07D401/12 , C07D405/12
摘要： The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein:Ring A is (4-12)-membered heterocyclyl;Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐或溶剂化物，其中：环A是（4-12） - 杂环基; 环B是选自环A，环B，环C，R 1，R 1a，R 2，R 3，R 4，L 2，n，t，w和z的稠合苯环如说明书中所定义。本发明还涉及包含式（I）化合物的药物组合物和治疗由葡萄糖激酶调节介导的病症的方法，所述方法包括向哺乳动物施用有效量的式（I）化合物。

4. 发明授权

US07842713B2 Fused phenyl amido heterocyclic compounds 有权
标题翻译：稠合苯基酰氨基杂环化合物
公开(公告)号：US07842713B2
公开(公告)日：2010-11-30
申请号：US11746359
申请日：2007-05-09
申请人： Hao Bai , Simon Bailey , Dilip Ramakant Bhumralkar , Feng C. Bi , Fengli Guo , Mingying He , Paul Stuart Humphries , Anthony Lai Ling , Jihong Lou , Seiji Nukui , Ru Zhou
发明人： Hao Bai , Simon Bailey , Dilip Ramakant Bhumralkar , Feng C. Bi , Fengli Guo , Mingying He , Paul Stuart Humphries , Anthony Lai Ling , Jihong Lou , Seiji Nukui , Ru Zhou
IPC分类号： A61K31/4155 , C07D231/10
CPC分类号： C07D405/14 , C07D401/12 , C07D405/12
摘要： The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein:Ring A is (4-12)-membered heterocyclyl;Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐或溶剂化物，其中：环A是（4-12） - 杂环基; 环B是选自环A，环B，环C，R 1，R 1a，R 2，R 3，R 4，L 2，n，t，w和z的稠合苯环如说明书中所定义。本发明还涉及包含式（I）化合物的药物组合物和治疗由葡萄糖激酶调节介导的病症的方法，所述方法包括向哺乳动物施用有效量的式（I）化合物。

5. 发明授权

US07141580B2 Aryl or heteroaryl fused imidazole compounds as anti-inflammatory and analgesic agents 有权
标题翻译：芳基或杂芳基稠合咪唑化合物作为抗炎和止痛剂
公开(公告)号：US07141580B2
公开(公告)日：2006-11-28
申请号：US10771696
申请日：2004-02-04
申请人： Kazunari Nakao , Yoshiyuki Okumura , Miyako Matsumizu , Naomi Ueno , Yoshinobu Hashizume , Tomoki Kato , Akiyoshi Kawai , Yoriko Miyake , Seiji Nukui , Katsuhiro Shinjyo , Kana Taniguchi
发明人： Kazunari Nakao , Yoshiyuki Okumura , Miyako Matsumizu , Naomi Ueno , Yoshinobu Hashizume , Tomoki Kato , Akiyoshi Kawai , Yoriko Miyake , Seiji Nukui , Katsuhiro Shinjyo , Kana Taniguchi
IPC分类号： A61K31/437
CPC分类号： C07D213/75 , A61K31/00 , A61K31/4178 , A61K31/437 , A61K31/64 , C07D231/12 , C07D233/56 , C07D235/06 , C07D235/08 , C07D235/12 , C07D235/14 , C07D235/16 , C07D235/18 , C07D235/30 , C07D249/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D471/04 , C07D473/00 , C07D491/04 , Y02P20/55
摘要： This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof, wherein Y1, Y2, Y3 and Y4 are independently selected from N, CH, etc.; R1 is H, C1-8 alkyl, etc.; Q1 is a 5–12 membered monocyclic or bicyclic aromatic ring optionally containing up to 4 heteroatoms selected from O, N and S, etc.; A is a 5–6 membered monocyclic aromatic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.; B is C1-6 alkylene optionally substituted with an oxo group, etc.; W is NH, O, etc.; R2 is H, C1-4 alkyl, etc.; Z is a 5–12 membered monocyclic or bicyclic aromatic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.; L is halo, C1-4 alkyl, etc.; m is 0, 1 or 2; R3 and R4 are independently selected from H and C1-4 alkyl; R5 is H, C1-4 alkyl, etc.; Q2 is a 5–12 membered monocyclic or bicyclic aromatic ring or tricyclic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc. These compounds are useful for the treatment of medical conditions mediated by prostaglamndin such as pain, fever or inflammation, etc. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，其中Y 1，Y 2，Y 3和 Y 4独立地选自N，CH等; R 1是H，C 1-8烷基等; Q 1是5-12元单环或双环芳族环，任选地含有至多4个选自O，N和S的杂原子等; A是任选含有至多3个选自O，N和S的杂原子的5-6元单环芳环等; B是任选被氧代基取代的C 1-6亚烷基等; W是NH，O等; R 2是H，C 1-4烷基等; Z是任选地含有至多3个选自O，N和S的杂原子的5-12元单环或双环芳环等; L为卤素，C 1-4烷基等; m为0,1或2; R 3和R 4独立地选自H和C 1-4烷基; R 5是H，C 1-4烷基等; Q 2是5-12元单环或双环芳族环或三环，任选地含有至多3个选自O，N和S的杂原子等。这些化合物可用于治疗介导的医学病症通过前列腺素如疼痛，发烧或炎症等。本发明还提供了包含上述化合物的药物组合物。

6. 发明授权

US06710054B2 Aryl or heteroaryl fused imidazole compounds as anti-inflammatory and analgesic agents 有权
标题翻译：芳基或杂芳基稠合咪唑化合物作为抗炎和止痛剂
公开(公告)号：US06710054B2
公开(公告)日：2004-03-23
申请号：US09977621
申请日：2001-10-15
申请人： Kazunari Nakao , Yoshiyuki Okumura , Miyako Matsumizu , Naomi Ueno , Yoshinobu Hashizume , Tomoki Kato , Akiyoshi Kawai , Yoriko Miyake , Seiji Nukui , Katsuhiro Shinjyo , Kana Taniguchi
发明人： Kazunari Nakao , Yoshiyuki Okumura , Miyako Matsumizu , Naomi Ueno , Yoshinobu Hashizume , Tomoki Kato , Akiyoshi Kawai , Yoriko Miyake , Seiji Nukui , Katsuhiro Shinjyo , Kana Taniguchi
IPC分类号： A61K31437
CPC分类号： C07D213/75 , A61K31/00 , A61K31/4178 , A61K31/437 , A61K31/64 , C07D231/12 , C07D233/56 , C07D235/06 , C07D235/08 , C07D235/12 , C07D235/14 , C07D235/16 , C07D235/18 , C07D235/30 , C07D249/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D471/04 , C07D473/00 , C07D491/04 , Y02P20/55
摘要： This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof, wherein Y1, Y2, Y3 and Y4 are independently selected from N, CH, etc.; R1 is H, C1-8 alkyl, etc.; Q1 is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 4 heteroatoms selected from O, N, and S, etc.; A is 5-6 membered monocyclic aromatic ring optionally containing up to 3 heteroatoms selected form O, N and S, etc.; B is C1-6 alkylene optionally substituted with an oxo group, etc.; W is NH, O, etc.; R2 is H, C1-4 alkyl, etc.; Z is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 3 heteroatoms selected form O, N and S, etc.; L is halo, C1-4 alkyl, etc.; m is 0, 1 or 2; R3 and R4 are independently selected from H and C1-4 alkyl; R5 is H, C1-4 alkyl; etc.; Q2 is a 5-12 membered monocyclic or bicyclic aromatic ring or tricyclic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc. These compounds are useful for the treatment of medical conditions mediated by prostaglamndin such as pain, fever or inflammation, etc. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，其中Y 1，Y 2，Y 3和Y 4独立地选自N，CH等; R 1是H，C 1-8烷基等; Q 1是任选地含有至多4个选自O，N和S的杂原子的5-12元单环或双环芳环等; A是任选含有至多3个选自O，N和S的杂原子的5-6元单环芳环等; B是任选被氧代基取代的C 1-6亚烷基等; W是NH，O等; R 2是H，C 1-4烷基等; Z是任选地含有至多3个选自O，N和S等的杂原子的5-12元单环或双环芳环; L是卤素，C 1-4烷基等; m为0,1或2; R 3和R 4独立地选自H和C 1-4烷基; R 5是H，C 1-4烷基; 等等。; Q 2是任选地含有至多3个选自O，N和S的杂原子的5-12元单环或双环芳族环或三环，这些化合物可用于治疗由前列腺素介导的医学病症如疼痛，发热或炎症等。本发明还提供包含上述化合物的药物组合物。

7. 发明授权

US08183255B2 N-pyrimidin-4-yl-3-amino-pyrrolo[3,4-c]pyrazole derivatives as PKC kinase inhibitors 有权
标题翻译： N-嘧啶-4-基-3-氨基 - 吡咯并[3,4-c]吡唑衍生物作为PKC激酶抑制剂
公开(公告)号：US08183255B2
公开(公告)日：2012-05-22
申请号：US12523965
申请日：2008-02-04
申请人： Hui Li , Seiji Nukui , Stephanie Anne Scales , Min Teng , Chunfeng Yin
发明人： Hui Li , Seiji Nukui , Stephanie Anne Scales , Min Teng , Chunfeng Yin
IPC分类号： A61K31/505
CPC分类号： C07D519/00 , C07D487/04
摘要： The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: (A) and (B) wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.
摘要翻译：本发明涉及式A和B的化合物和药学上可接受的盐：（A）和（B）其中A，B，R1，R2，R3，R4，R5，R6，R7，R8，R9和R10如上所定义以上。本发明还涉及包含该化合物和药学上可接受的盐的药物组合物以及治疗糖尿病及其并发症，癌症，局部缺血，炎症，中枢神经系统疾病，心血管疾病，阿尔茨海默病和皮肤病疾病压迫，病毒疾病，炎性反应的方法疾病或肝脏是靶器官的疾病。

8. 发明授权

US08114871B2 3-amido-pyrrolo[3,4-C]pyrazole-5(1H,4H,6H) carbaldehyde derivatives 有权
标题翻译： 3-氨基 - 吡咯并[3,4-C]吡唑-5（1H，4H，6H）甲醛衍生物
公开(公告)号：US08114871B2
公开(公告)日：2012-02-14
申请号：US12532051
申请日：2008-04-10
申请人： Iriny Botrous , Yufeng Hong , Hui Li , Kevin Kun-Chin Liu , Seiji Nukui , Min Teng , Eileen Valenzuela Tompkins , Chunfeng Yin
发明人： Iriny Botrous , Yufeng Hong , Hui Li , Kevin Kun-Chin Liu , Seiji Nukui , Min Teng , Eileen Valenzuela Tompkins , Chunfeng Yin
IPC分类号： A61K31/535 , A61K31/495 , A61K31/497 , A61K31/4965 , C07D413/14 , C07D237/00 , C07D239/00 , C07D403/14 , C07D241/36 , C07D401/14
CPC分类号： C07D487/04
摘要： The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ.
摘要翻译：本发明涉及式（I）的化合物和药学上可接受的盐：其中X，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8如上所定义。本发明还涉及包含该化合物和药学上可接受的盐的药物组合物以及治疗糖尿病及其并发症（特别是糖尿病性视网膜病变，肾病或神经病变），癌症，缺血，炎症，中枢神经系统疾病，心血管疾病，阿尔茨海默病和皮肤病疾病，病毒性疾病，炎症性疾病或肝脏是靶器官的疾病。

9. 发明授权

US07479564B2 Aryl or heteroaryl fused imidazole compounds as anti-inflammatory and analgesic agents 有权
标题翻译：芳基或杂芳基稠合咪唑化合物作为抗炎和止痛剂
公开(公告)号：US07479564B2
公开(公告)日：2009-01-20
申请号：US11556523
申请日：2006-11-03
申请人： Kazunari Nakao , Yoshiyuki Okumura , Miyako Matsumizu , Naomi Ueno , Yoshinobu Hashizume , Tomoki Kato , Akiyoshi Kawai , Yoriko Miyake , Seiji Nukui , Katsuhiro Shinjyo , Kana Taniguchi
发明人： Kazunari Nakao , Yoshiyuki Okumura , Miyako Matsumizu , Naomi Ueno , Yoshinobu Hashizume , Tomoki Kato , Akiyoshi Kawai , Yoriko Miyake , Seiji Nukui , Katsuhiro Shinjyo , Kana Taniguchi
IPC分类号： A61K31/4184 , C07D235/06
CPC分类号： C07D213/75 , A61K31/00 , A61K31/4178 , A61K31/437 , A61K31/64 , C07D231/12 , C07D233/56 , C07D235/06 , C07D235/08 , C07D235/12 , C07D235/14 , C07D235/16 , C07D235/18 , C07D235/30 , C07D249/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D471/04 , C07D473/00 , C07D491/04 , Y02P20/55
摘要： This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof, wherein Y1, Y2, Y3 and Y4 are independently selected from N, CH, etc.; R1 is H, C1-8 alkyl, etc.; Q1 is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 4 heteroatoms selected from O, N and S, etc.; A is a 5-6 membered monocyclic aromatic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.; B is C1-6 alkylene optionally substituted with an oxo group, etc.; W is NH, O, etc.; R2 is H, C1-4 alkyl, etc.; Z is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.; L is halo, C1-4 alkyl, etc.; m is 0, 1 or 2; R3 and R4 are independently selected from H and C1-4 alkyl ; R5 is H, C1-4 alkyl, etc.; Q2 is a 5-12 membered monocyclic or bicyclic aromatic ring or tricyclic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc. These compounds are useful for the treatment of medical conditions mediated by prostaglamadin such as pain, fever or inflammation, etc. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，其中Y 1，Y 2，Y 3和Y 4独立地选自N，CH等; R1是H，C1-8烷基等; Q1是任选地含有至多4个选自O，N和S的杂原子的5-12元单环或双环芳环; A是任选含有至多3个选自O，N和S的杂原子的5-6元单环芳环等; B是任选被氧代基取代的C 1-6亚烷基等; W是NH，O等; R2是H，C1-4烷基等; Z是任选地含有至多3个选自O，N和S的杂原子的5-12元单环或双环芳环等; L是卤素，C 1-4烷基等; m为0,1或2; R 3和R 4独立地选自H和C 1-4烷基; R5是H，C1-4烷基等; Q2是任选地含有至多3个选自O，N和S等杂原子的5-12元单环或双环芳族环或三环，这些化合物可用于治疗前列腺素介导的医学病症，例如疼痛，发热或炎症等。本发明还提供包含上述化合物的药物组合物。

10. 发明授权

US06686373B2 Pyrazoloquinolinone derivatives as protein kinase C inhibitors 失效
标题翻译：吡唑啉酮衍生物作为蛋白激酶C抑制剂
公开(公告)号：US06686373B2
公开(公告)日：2004-02-03
申请号：US10191593
申请日：2002-07-09
申请人： Kiyoshi Kawamura , Sachiko Mihara , Seiji Nukui , Chikara Uchida
发明人： Kiyoshi Kawamura , Sachiko Mihara , Seiji Nukui , Chikara Uchida
IPC分类号： A61K314745
CPC分类号： C07D471/04
摘要： This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof wherein the dashed lines represent optional double bonds; C1, C2, C3 and C4 are carbon atom; R1 is C1-4 alkyl; R2 is H, amino, etc.; R3 is H, halo-CH2—, C2-8 alkyl or Q1-, wherein said C2-8 alkyl is optionally substituted with up to 3 substituents selected from halo, C1-3 alkyl, R4(R5)N, etc.; R4 is H, C1-7 alkyl, etc.; R5 is H, C1-7alkyl, etc.; R6 and R7 are independently selected from H and C1-4 alkyl; R8 is aryl or heteroaryl; Q1 is a 4-12 membered monocyclic or bicyclic aromatic, partially saturated or fully saturated ring optionally containing up to 4 heteroatoms selected from O, N and S, and is optionally substituted with halo, C1-4 alkyl, etc.; Y5, Y6, Y7 and Y8 are hydrogen; Y1, Y2, Y3 and Y4 are independently selected from hydrogen, halo, etc.; Q2 is a 5-12 membered monocyclic or bicyclic aromatic, partially saturated or fully saturated ring optionally containing up to 3 heteroatoms selected from O, N and S, and is optionally substituted with halo, C1-4alkyl-, etc.; These compounds have protein kinase C inhibitory activity and thus are useful for the treatment of neuropathic pain, acute or chronic inflammatory pain, auditory deficiency (synaptic repair), or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，其中虚线表示任选的双键; C 1，C 2，C 3和C 4是碳原子; R 1是C 1-4烷基; R 2是H，氨基等; R 3是H，卤代-CH 2 - ，C 2-8烷基或Q 1 - ，其中所述C 2-8烷基任选被至多3个选自卤素，C 1-3烷基，R 4，（R 5）N等; R 4是H，C 1-7烷基等; R 5是H，C 1-7烷基等; R 6和R 7独立地选自H和C 1-4烷基; R 8是芳基或杂芳基; Q 1是4-12元单环或双环芳族，部分饱和或完全饱和的环，任选地含有至多4个选自O，N和S的杂原子，并且任选地被卤素，C 1-4烷基等取代; Y 5，Y 6，Y 7和Y 8是氢; Y 1，Y 2，Y 3和Y 4独立地选自氢，卤素等; Q 2是5-12元单环或双环芳族，部分饱和或完全饱和的环，任选地含有至多3个选自O，N和S的杂原子，并且任选被卤素，C 1-4烷基等取代; 这些化合物具有蛋白激酶C抑制活性，因此可用于治疗哺乳动物，特别是人类的神经性疼痛，急性或慢性炎性疼痛，听觉缺陷（突触修复）等。本发明还提供了包含上述化合物的药物组合物。

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