公开(公告)号：US07514409B2

公开(公告)日：2009-04-07

申请号：US10591820

申请日：2005-03-07

申请人： William K. Hagmann ,  Linus S. Lin ,  Ping Liu ,  Richard A. Mumford ,  Thomas S. Reger ,  Nicholas D. Smith ,  Nicholas S. Stock ,  Jasmine Zunic

发明人： William K. Hagmann ,  Linus S. Lin ,  Ping Liu ,  Richard A. Mumford ,  Thomas S. Reger ,  Nicholas D. Smith ,  Nicholas S. Stock ,  Jasmine Zunic

IPC分类号： A61K38/05

CPC分类号： C07K5/06026 ,  C07D401/12 ,  C07D401/14

摘要： Compounds of Formula I are antagonists of VLA-4, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of inflammatory bowel disease including ulcerative colitis and Crohn's disease, multiple sclerosis, asthma, and rheumatoid arthritis.

摘要翻译： 式I的化合物是VLA-4的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病症。 这些化合物可以配制成药物组合物，并且适用于治疗包括溃疡性结肠炎和克罗恩病，多发性硬化，哮喘和类风湿性关节炎的炎性肠病。

公开(公告)号：US06559174B2

公开(公告)日：2003-05-06

申请号：US10097028

申请日：2002-03-13

申请人： Linus S. Lin ,  Shrenik K. Shah ,  Linda L. Chang ,  William K. Hagmann ,  Richard A. Mumford

发明人： Linus S. Lin ,  Shrenik K. Shah ,  Linda L. Chang ,  William K. Hagmann ,  Richard A. Mumford

IPC分类号： A61K3147

CPC分类号： C07D401/12 ,  A61K31/4709 ,  A61K31/4745 ,  C07D401/14 ,  C07D487/04

摘要： Compounds of Formula I are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.

公开(公告)号：US06943180B2

公开(公告)日：2005-09-13

申请号：US10472303

申请日：2002-03-15

申请人： George Doherty ,  Linus S Lin ,  William K. Hagmann ,  Ginger Xu-qiang Yang ,  Linda L. Chang ,  Shrenik K. Shah ,  Richard A. Mumford ,  Theodore Kamenecka

发明人： George Doherty ,  Linus S Lin ,  William K. Hagmann ,  Ginger Xu-qiang Yang ,  Linda L. Chang ,  Shrenik K. Shah ,  Richard A. Mumford ,  Theodore Kamenecka

IPC分类号： A61K38/00 ,  A61P1/04 ,  A61P11/02 ,  A61P11/06 ,  A61P25/00 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D401/12 ,  C07D401/14 ,  C07K5/078 ,  C07D215/20 ,  A61K31/47

CPC分类号： C07D401/12 ,  C07D401/14

摘要： Compounds of formula (I) are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, rhinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.

摘要翻译： 式（I）化合物是VLA-4和/或α4/β7的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病症。 这些化合物可以配制成药物组合物，适用于治疗AIDS相关的痴呆，过敏性结膜炎，过敏性鼻炎，阿尔茨海默病，哮喘，动脉粥样硬化，自体骨髓移植，某些类型的毒性和免疫性肾炎， 接触皮肤过敏，包括溃疡性结肠炎和克罗恩病的炎性肠病，炎性肺病，病毒感染的炎症后遗症，脑膜炎，多发性硬化，多发性骨髓瘤，心肌炎，器官移植，牛皮癣，肺纤维化，再狭窄，鼻炎，类风湿性关节炎，败血症 关节炎，中风，肿瘤转移，葡萄膜炎和I型糖尿病。

公开(公告)号：US06855708B2

公开(公告)日：2005-02-15

申请号：US10096607

申请日：2002-03-13

申请人： Linus S. Lin ,  George Doherty ,  Shrenik K. Shah ,  Linda L. Chang ,  William K. Hagmann ,  Richard A. Mumford

发明人： Linus S. Lin ,  George Doherty ,  Shrenik K. Shah ,  Linda L. Chang ,  William K. Hagmann ,  Richard A. Mumford

IPC分类号： C07D401/12 ,  C07D487/04 ,  C07D498/04 ,  A61K31/55 ,  A61K31/47

CPC分类号： C07D401/12 ,  C07D487/04

摘要： Compounds of Formula I are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.

摘要翻译： 式I的化合物是VLA-4和/或α4/β7的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病理学。 这些化合物可以配制成药物组合物，适用于治疗AIDS相关的痴呆，过敏性结膜炎，过敏性鼻炎，阿尔茨海默病，哮喘，动脉粥样硬化，自体骨髓移植，某些类型的毒性和免疫性肾炎， 接触皮肤过敏，包括溃疡性结肠炎和克罗恩病的炎性肠病，炎症性肺病，病毒感染的炎症后遗症，脑膜炎，多发性硬化，多发性骨髓瘤，心肌炎，器官移植，牛皮癣，肺纤维化，再狭窄，视网膜炎，类风湿性关节炎，败血症 关节炎，中风，肿瘤转移，葡萄膜炎和I型糖尿病。

公开(公告)号：US07816534B2

公开(公告)日：2010-10-19

申请号：US12386336

申请日：2009-04-16

申请人： William K. Hagmann ,  Linus S. Lin ,  Shrenik K. Shah ,  Ravindra N. Guthikonda ,  Hongbo Qi ,  Linda L. Chang ,  Ping Liu ,  Helen M. Armstrong ,  James P. Jewell ,  Thomas J. Lanza, Jr.

发明人： William K. Hagmann ,  Linus S. Lin ,  Shrenik K. Shah ,  Ravindra N. Guthikonda ,  Hongbo Qi ,  Linda L. Chang ,  Ping Liu ,  Helen M. Armstrong ,  James P. Jewell ,  Thomas J. Lanza, Jr.

IPC分类号： A61K31/44 ,  C07D213/04 ,  C07D401/02 ,  C07D403/02 ,  C07D239/02

CPC分类号： C07D213/64 ,  C07C233/13 ,  C07C235/06 ,  C07C235/20 ,  C07C235/34 ,  C07C235/74 ,  C07C235/78 ,  C07C237/06 ,  C07C255/55 ,  C07C255/60 ,  C07C271/14 ,  C07C271/22 ,  C07C275/30 ,  C07C311/03 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07D209/34 ,  C07D209/94 ,  C07D211/34 ,  C07D213/65 ,  C07D213/68 ,  C07D215/06 ,  C07D231/12 ,  C07D233/56 ,  C07D233/70 ,  C07D237/28 ,  C07D237/32 ,  C07D239/34 ,  C07D249/04 ,  C07D249/08 ,  C07D249/12 ,  C07D263/58 ,  C07D267/14 ,  C07D277/30 ,  C07D277/36 ,  C07D295/13 ,  C07D295/15 ,  C07D513/04

摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

摘要翻译： 结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗，预防和抑制由CB1受体介导的疾病。 本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症，脑血管 事故和头部创伤，焦虑症，压力，癫痫，帕金森病，运动障碍和精神分裂症。 这些化合物还可用于治疗药物滥用障碍，治疗肥胖或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。

公开(公告)号：US07550489B2

公开(公告)日：2009-06-23

申请号：US12012463

申请日：2008-02-01

申请人： William K. Hagmann ,  Linus S. Lin ,  Shrenik K. Shah ,  Ravindra N. Guthikonda ,  Hongbo Qi ,  Linda L. Chang ,  Ping Liu ,  Helen M. Armstrong ,  James P. Jewell ,  Thomas J. Lanza, Jr.

发明人： William K. Hagmann ,  Linus S. Lin ,  Shrenik K. Shah ,  Ravindra N. Guthikonda ,  Hongbo Qi ,  Linda L. Chang ,  Ping Liu ,  Helen M. Armstrong ,  James P. Jewell ,  Thomas J. Lanza, Jr.

IPC分类号： A61K31/435

CPC分类号： C07D213/64 ,  C07C233/13 ,  C07C235/06 ,  C07C235/20 ,  C07C235/34 ,  C07C235/74 ,  C07C235/78 ,  C07C237/06 ,  C07C255/55 ,  C07C255/60 ,  C07C271/14 ,  C07C271/22 ,  C07C275/30 ,  C07C311/03 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07D209/34 ,  C07D209/94 ,  C07D211/34 ,  C07D213/65 ,  C07D213/68 ,  C07D215/06 ,  C07D231/12 ,  C07D233/56 ,  C07D233/70 ,  C07D237/28 ,  C07D237/32 ,  C07D239/34 ,  C07D249/04 ,  C07D249/08 ,  C07D249/12 ,  C07D263/58 ,  C07D267/14 ,  C07D277/30 ,  C07D277/36 ,  C07D295/13 ,  C07D295/15 ,  C07D513/04

摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

公开(公告)号：US07754188B2

公开(公告)日：2010-07-13

申请号：US10559228

申请日：2004-06-25

申请人： H. Donald Burns ,  Alex M. Chen ,  Raymond E. Gibson ,  Mark T. Goulet ,  William K. Hagmann ,  Terence G. Hamill ,  James P. Jewell ,  Linus S. Lin ,  Ping Liu ,  Andrey V. Peresypkin

发明人： H. Donald Burns ,  Alex M. Chen ,  Raymond E. Gibson ,  Mark T. Goulet ,  William K. Hagmann ,  Terence G. Hamill ,  James P. Jewell ,  Linus S. Lin ,  Ping Liu ,  Andrey V. Peresypkin

IPC分类号： A61K51/00 ,  A61M36/14

CPC分类号： C07D213/64 ,  A61K51/0406 ,  A61K51/0455 ,  A61K51/0459 ,  C07D239/34

摘要： The present invention relates to particular radiolabeled Cannabinoid-1 (CB1) receptor modulators, and methods of using these modulators for labeling and diagnostic imaging of Cannabinoid-1 receptors in mammals, particularly humans. In addition, intermediates useful for the synthesis of the radiolabeled Cannabinoid-1 receptor modulators are also disclosed, as well as the processes for synthesizing the radiolabeled Cannabinoid-1 receptor modulators. Still further, formulations of the radiolabeled Cannabinoid-1 receptor compounds are described.

摘要翻译： 本发明涉及特定的放射性标记的大麻素-1（CB1）受体调节剂，以及使用这些调节剂用于哺乳动物，特别是人类中大麻素-1受体的标记和诊断成像的方法。 此外，还公开了可用于合成放射性标记的大麻素-1受体调节剂的中间体，以及合成放射性标记的大麻素-1受体调节剂的方法。 此外，描述了放射性标记的大麻素-1受体化合物的制剂。

公开(公告)号：US06972295B2

公开(公告)日：2005-12-06

申请号：US10387265

申请日：2003-03-12

申请人： William K. Hagmann ,  Linus S. Lin ,  Shrenik K. Shah ,  Ravindra N. Guthikonda ,  Hongbo Qi ,  Linda L. Chang ,  Ping Liu ,  Helen M. Armstrong ,  James P. Jewell ,  Thomas J. Lanza, Jr.

发明人： William K. Hagmann ,  Linus S. Lin ,  Shrenik K. Shah ,  Ravindra N. Guthikonda ,  Hongbo Qi ,  Linda L. Chang ,  Ping Liu ,  Helen M. Armstrong ,  James P. Jewell ,  Thomas J. Lanza, Jr.

IPC分类号： A61K31/165 ,  A61K31/27 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/403 ,  A61K31/405 ,  A61K31/415 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/42 ,  A61K31/423 ,  A61K31/426 ,  A61K31/428 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4409 ,  A61K31/4436 ,  A61K31/445 ,  A61K31/4453 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/50 ,  A61K31/501 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/553 ,  A61P1/04 ,  A61P1/10 ,  A61P1/16 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P5/24 ,  A61P9/04 ,  A61P9/06 ,  A61P9/10 ,  A61P9/12 ,  A61P9/14 ,  A61P11/06 ,  A61P13/12 ,  A61P15/00 ,  A61P15/10 ,  A61P17/00 ,  A61P19/02 ,  A61P19/06 ,  A61P25/00 ,  A61P25/06 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  C07C233/12 ,  C07C233/13 ,  C07C235/06 ,  C07C235/18 ,  C07C235/20 ,  C07C235/34 ,  C07C235/74 ,  C07C235/78 ,  C07C237/06 ,  C07C255/55 ,  C07C255/60 ,  C07C271/14 ,  C07C271/22 ,  C07C275/30 ,  C07C311/03 ,  C07C323/41 ,  C07D207/27 ,  C07D209/08 ,  C07D209/34 ,  C07D209/52 ,  C07D209/94 ,  C07D211/34 ,  C07D213/36 ,  C07D213/40 ,  C07D213/56 ,  C07D213/61 ,  C07D213/64 ,  C07D213/65 ,  C07D213/68 ,  C07D213/89 ,  C07D215/06 ,  C07D231/12 ,  C07D233/36 ,  C07D233/70 ,  C07D233/80 ,  C07D237/14 ,  C07D237/28 ,  C07D237/32 ,  C07D239/34 ,  C07D249/04 ,  C07D249/08 ,  C07D249/12 ,  C07D249/18 ,  C07D261/08 ,  C07D261/20 ,  C07D263/58 ,  C07D267/14 ,  C07D277/20 ,  C07D277/30 ,  C07D277/36 ,  C07D277/64 ,  C07D277/74 ,  C07D295/12 ,  C07D295/13 ,  C07D295/14 ,  C07D295/15 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12 ,  C07D471/04 ,  C07D513/04 ,  C07D521/00 ,  A61K31/4412 ,  C07D213/70

CPC分类号： C07D213/64 ,  C07C233/13 ,  C07C235/06 ,  C07C235/20 ,  C07C235/34 ,  C07C235/74 ,  C07C235/78 ,  C07C237/06 ,  C07C255/55 ,  C07C255/60 ,  C07C271/14 ,  C07C271/22 ,  C07C275/30 ,  C07C311/03 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07D209/34 ,  C07D209/94 ,  C07D211/34 ,  C07D213/65 ,  C07D213/68 ,  C07D215/06 ,  C07D231/12 ,  C07D233/56 ,  C07D233/70 ,  C07D237/28 ,  C07D237/32 ,  C07D239/34 ,  C07D249/04 ,  C07D249/08 ,  C07D249/12 ,  C07D263/58 ,  C07D267/14 ,  C07D277/30 ,  C07D277/36 ,  C07D295/13 ,  C07D295/15 ,  C07D513/04

摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

摘要翻译： 结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗，预防和抑制由CB1受体介导的疾病。 本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症，脑血管 事故和头部创伤，焦虑症，压力，癫痫，帕金森病，运动障碍和精神分裂症。 这些化合物还可用于治疗物质滥用障碍，治疗肥胖或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。

公开(公告)号：US20090258884A1

公开(公告)日：2009-10-15

申请号：US12386336

申请日：2009-04-16

申请人： William K. Hagmann ,  Linus S. Lin ,  Shrenik K. Shah ,  Ravindra N. Guthikonda ,  Hongbo Qi ,  Linda L. Chang ,  Ping Liu ,  Helen M. Armstrong ,  James P. Jewell ,  Thomas J. Lanza, JR.

发明人： William K. Hagmann ,  Linus S. Lin ,  Shrenik K. Shah ,  Ravindra N. Guthikonda ,  Hongbo Qi ,  Linda L. Chang ,  Ping Liu ,  Helen M. Armstrong ,  James P. Jewell ,  Thomas J. Lanza, JR.

IPC分类号： A61K31/497 ,  C07D213/56 ,  A61K31/4412 ,  C07C235/00 ,  A61K31/165 ,  C07D401/12 ,  A61K31/444 ,  A61K31/4439 ,  A61K31/506 ,  C07D249/04 ,  A61K31/4192 ,  C07D409/12 ,  A61K31/4436 ,  C07D413/12 ,  A61K31/4709 ,  A61P3/04

CPC分类号： C07D213/64 ,  C07C233/13 ,  C07C235/06 ,  C07C235/20 ,  C07C235/34 ,  C07C235/74 ,  C07C235/78 ,  C07C237/06 ,  C07C255/55 ,  C07C255/60 ,  C07C271/14 ,  C07C271/22 ,  C07C275/30 ,  C07C311/03 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07D209/34 ,  C07D209/94 ,  C07D211/34 ,  C07D213/65 ,  C07D213/68 ,  C07D215/06 ,  C07D231/12 ,  C07D233/56 ,  C07D233/70 ,  C07D237/28 ,  C07D237/32 ,  C07D239/34 ,  C07D249/04 ,  C07D249/08 ,  C07D249/12 ,  C07D263/58 ,  C07D267/14 ,  C07D277/30 ,  C07D277/36 ,  C07D295/13 ,  C07D295/15 ,  C07D513/04

摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

公开(公告)号：US20080171692A1

公开(公告)日：2008-07-17

申请号：US12012463

申请日：2008-02-01

申请人： William K. Hagmann ,  Linus S. Lin ,  Shrenik K. Shah ,  Ravindra N. Guthikonda ,  Hongbo Qi ,  Linda L. Chang ,  Ping Liu ,  Helen M. Armstrong ,  James P. Jewell ,  Thomas J. Lanza

发明人： William K. Hagmann ,  Linus S. Lin ,  Shrenik K. Shah ,  Ravindra N. Guthikonda ,  Hongbo Qi ,  Linda L. Chang ,  Ping Liu ,  Helen M. Armstrong ,  James P. Jewell ,  Thomas J. Lanza

IPC分类号： A61K38/22 ,  A61K31/44 ,  A61K31/444 ,  A61K31/4439 ,  A61K31/365 ,  A61P3/04 ,  A61K31/485 ,  A61K31/357 ,  A61K31/155

CPC分类号： C07D213/64 ,  C07C233/13 ,  C07C235/06 ,  C07C235/20 ,  C07C235/34 ,  C07C235/74 ,  C07C235/78 ,  C07C237/06 ,  C07C255/55 ,  C07C255/60 ,  C07C271/14 ,  C07C271/22 ,  C07C275/30 ,  C07C311/03 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07D209/34 ,  C07D209/94 ,  C07D211/34 ,  C07D213/65 ,  C07D213/68 ,  C07D215/06 ,  C07D231/12 ,  C07D233/56 ,  C07D233/70 ,  C07D237/28 ,  C07D237/32 ,  C07D239/34 ,  C07D249/04 ,  C07D249/08 ,  C07D249/12 ,  C07D263/58 ,  C07D267/14 ,  C07D277/30 ,  C07D277/36 ,  C07D295/13 ,  C07D295/15 ,  C07D513/04

摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.