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。

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.

公开(公告)号：US08518911B2

公开(公告)日：2013-08-27

申请号：US13057510

申请日：2009-07-27

申请人： Jason D. Katz ,  Sandra L. Knowles ,  James P. Jewell ,  David L. Sloman ,  Matthew G. Stanton ,  Njamkou Noucti

发明人： Jason D. Katz ,  Sandra L. Knowles ,  James P. Jewell ,  David L. Sloman ,  Matthew G. Stanton ,  Njamkou Noucti

IPC分类号： A61K31/675 ,  A61K31/437 ,  A61K31/496 ,  A61K31/397

CPC分类号： A61K31/425 ,  C07D417/04 ,  C07D417/14

摘要： The invention encompasses pyrazolo[1,5-a]pyridine derivatives which selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease. Pharmaceutical compositions and methods of use are also included.

摘要翻译： 本发明包括选择性抑制微管亲和调节激酶（MARK）的吡唑并[1,5-a]吡啶衍生物，因此可用于治疗或预防阿尔茨海默氏病。 还包括药物组合物和使用方法。

公开(公告)号：US08207186B2

公开(公告)日：2012-06-26

申请号：US11921350

申请日：2006-06-22

申请人： James P. Jewell ,  Jason D. Katz

发明人： James P. Jewell ,  Jason D. Katz

IPC分类号： A01N43/42 ,  A61K31/44 ,  C07D221/00

CPC分类号： C07D471/04 ,  C07D221/16 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D487/04 ,  C07D491/10 ,  C07D491/113 ,  C07F7/1804

摘要： The present invention relates to 5H-benzo[4,5]cyclohepta[1,2-b]pyridine compounds, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

摘要翻译： 本发明涉及用于治疗细胞增殖性疾病，用于治疗与MET活性相关的疾病和用于抑制受体酪氨酸激酶MET的5H-苯并[4,5]环庚并[1,2-b]吡啶化合物。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。

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.