公开(公告)号：US20050234061A1

公开(公告)日：2005-10-20

申请号：US11109076

申请日：2005-04-19

申请人： William Hagmann ,  Linus Lin ,  Shrenik Shah ,  Ravindra Guthikonda ,  Hongbo Qi ,  Linda Chang ,  Ping Liu ,  Helen Armstrong ,  James Jewell ,  Thomas Lanza

发明人： William Hagmann ,  Linus Lin ,  Shrenik Shah ,  Ravindra Guthikonda ,  Hongbo Qi ,  Linda Chang ,  Ping Liu ,  Helen Armstrong ,  James Jewell ,  Thomas Lanza

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 ,  A61K31/502 ,  A61K31/401

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：US20060115425A1

公开(公告)日：2006-06-01

申请号：US10559228

申请日：2004-06-25

申请人： H. Donald Burns ,  Alex Chen ,  Raymond Gibson ,  Mark Goulet ,  William Hagmann ,  Terence Hamill ,  James Jewell ,  Linus Lin ,  Ping Liu ,  Andrey Peresypkin

发明人： H. Donald Burns ,  Alex Chen ,  Raymond Gibson ,  Mark Goulet ,  William Hagmann ,  Terence Hamill ,  James Jewell ,  Linus Lin ,  Ping Liu ,  Andrey Peresypkin

IPC分类号： A61K51/00 ,  C07D213/70

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：US20070179190A1

公开(公告)日：2007-08-02

申请号：US10591820

申请日：2005-03-07

申请人： William Hagmann ,  Linus Lin ,  Ping Liu ,  Richard Mumford ,  Thomas Reger ,  Nicholas Smith ,  Nicholas Stock ,  Jasmine Zunic

发明人： William Hagmann ,  Linus Lin ,  Ping Liu ,  Richard Mumford ,  Thomas Reger ,  Nicholas Smith ,  Nicholas Stock ,  Jasmine Zunic

IPC分类号： A61K31/44 ,  A01N43/40

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：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.

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：US20080076805A1

公开(公告)日：2008-03-27

申请号：US11661834

申请日：2005-10-03

申请人： Linus Lin ,  Ping Liu

发明人： Linus Lin ,  Ping Liu

IPC分类号： A61K31/4412 ,  A61K31/165 ,  A61P25/00 ,  C07C243/12 ,  C07D213/63

CPC分类号： C07C255/66 ,  C07C243/28 ,  C07C243/32 ,  C07C243/36 ,  C07C2601/08 ,  C07D213/64

摘要： The acyclic hydrazides of the invention 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 (including smoking cessation), 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： 本发明的无环酰肼是大麻素-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（包括戒烟），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：US11944384B2

公开(公告)日：2024-04-02

申请号：US16969817

申请日：2019-01-29

申请人： Xuemin Xu ,  Aili Zhang ,  Jianqi Sun ,  Ping Liu ,  Jingfeng Bai

发明人： Xuemin Xu ,  Aili Zhang ,  Jianqi Sun ,  Ping Liu ,  Wentao Li

IPC分类号： A61B34/10 ,  A61B18/00 ,  A61B18/02 ,  A61B18/14

CPC分类号： A61B34/10 ,  A61B18/02 ,  A61B2018/00041 ,  A61B2018/00404 ,  A61B2018/00577 ,  A61B2018/00791 ,  A61B2018/00863 ,  A61B2018/00988 ,  A61B2018/0293 ,  A61B18/1477 ,  A61B2034/104 ,  A61B2034/105 ,  A61B2034/107

摘要： The present application relates to computer-based preoperative planning technology, and discloses a preoperative planning method for multimodal ablation treatment and apparatus thereof, which can automatically provide objective, scientific, and quantitative multimodal ablation planning information. In this method, acquiring parameters of an volume to be ablated; calculating property changes of the tissue caused by performing freezing on the volume according to the parameters of the volume to be ablated, and acquiring a first planning data required for the property changes of the tissue to satisfy a first predetermined condition; further calculating property changes of the tissue caused by performing heating on the volume to acquire a second planning data required for the property changes of the tissue to satisfy a second predetermined condition based on the properties satisfying the first predetermined condition; outputting the first planning data and the second planning data.