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1. 发明授权

US07667053B2 Bicyclic amides 失效
标题翻译：双环酰胺
公开(公告)号：US07667053B2
公开(公告)日：2010-02-23
申请号：US10509584
申请日：2003-04-08
申请人： Laurie A. Castonguay , William K. Hagmann , Linus S. Lin , Shrenik K. Shah
发明人： Laurie A. Castonguay , William K. Hagmann , Linus S. Lin , Shrenik K. Shah
IPC分类号： C07D319/14
CPC分类号： C07D405/12 , C07C233/59 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07D307/84 , C07D311/58 , C07D319/20
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。

2. 发明授权

US06559174B2 N-arylsulfonyl aryl aza-bicyclic derivatives as potent cell adhesion inhibitors 失效
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.

3. 发明授权

US07816534B2 Substituted amides 有权
标题翻译：取代酰胺
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。

4. 发明授权

US07550489B2 Substituted pyridyoxy amides 失效
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.

5. 发明授权

US06943180B2 Substituted N-arylsulfonyl-proline derivatives as potent cell adhesion inhibitors 失效
标题翻译：取代的N-芳基磺酰基 - 脯氨酸衍生物作为有效的细胞粘附抑制剂
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。

6. 发明授权

US06972295B2 Substituted amides 有权
标题翻译：取代酰胺
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。

7. 发明申请

US20090258884A1 Substituted amides 有权
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.

8. 发明授权

US07423067B2 Diphenyl cyclopentyl amides as cannabinoid-1 receptor inverse agonists 失效
标题翻译：二苯基环戊基酰胺作为大麻素-1受体反向激动剂
公开(公告)号：US07423067B2
公开(公告)日：2008-09-09
申请号：US10507864
申请日：2003-03-21
申请人： William K. Hagmann , Linus S. Lin , Shrenik K. Shah , Mark T. Goulet , James P. Jewell
发明人： William K. Hagmann , Linus S. Lin , Shrenik K. Shah , Mark T. Goulet , James P. Jewell
IPC分类号： A61K31/165
CPC分类号： C07D207/38 , C07C233/59 , C07C235/40 , C07C235/82 , C07C237/24 , C07C255/60 , C07C271/24 , C07C317/44 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D205/04 , C07D207/16 , C07D207/48 , C07D211/60 , C07D211/62 , C07D213/56 , C07D213/61 , C07D213/82 , C07D213/89 , C07D265/30 , C07D307/24 , C07D307/68 , C07D309/08 , C07D401/04
摘要： Novel compounds of 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 psychotropic 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, Parkinsons 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，包括多发性硬化症和神经 - 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，脑血管意外的精神药物，头部创伤，焦虑障碍，压力，癫痫，帕金森病，运动障碍和精神分裂症。这些化合物也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。

9. 发明申请

US20080171692A1 Substituted amides 失效
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.

10. 发明授权

US06855708B2 N-arylsulfonyl aza-bicyclic derivatives as potent cell adhesion inhibitors 失效
标题翻译： N-芳基磺酰基氮杂双环衍生物作为有效的细胞粘附抑制剂
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。

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