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公开(公告)号:US20080076805A1
公开(公告)日:2008-03-27
申请号:US11661834
申请日:2005-10-03
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。
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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
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。
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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.
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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。
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公开(公告)号:US20050203112A1
公开(公告)日:2005-09-15
申请号:US10509584
申请日:2003-04-08
申请人: Laurie Castonguay , William Hagmann , Linus Lin , Shrenik Shah
发明人: Laurie Castonguay , William Hagmann , Linus Lin , Shrenik Shah
IPC分类号: A61K31/165 , A61K31/343 , A61K31/353 , A61K31/36 , A61K31/403 , A61K31/4433 , A61K31/454 , A61K31/4709 , A61K31/4745 , A61K31/517 , A61P1/00 , A61P1/10 , A61P1/16 , A61P3/04 , A61P9/10 , A61P11/06 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/36 , A61P43/00 , C07C233/59 , C07D209/88 , C07D307/84 , C07D307/85 , C07D311/58 , C07D311/66 , C07D319/20 , C07D405/12
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。
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公开(公告)号:US20050154202A1
公开(公告)日:2005-07-14
申请号:US10509277
申请日:2003-04-01
申请人: William Hagmann , Linus Lin , Shrenik Shah
发明人: William Hagmann , Linus Lin , Shrenik Shah
IPC分类号: C07D295/14 , A61K31/166 , A61K31/343 , A61K31/381 , A61K31/40 , A61K31/402 , A61K31/403 , A61K31/41 , A61K31/415 , A61K31/416 , A61K31/4166 , A61K31/4184 , A61K31/42 , A61K31/423 , A61K31/4245 , A61K31/426 , A61K31/428 , A61K31/437 , A61K31/4375 , A61K31/44 , A61K31/4402 , A61K31/4409 , A61K31/4439 , A61K31/4453 , A61K31/455 , A61K31/47 , A61K31/4965 , A61K31/505 , A61K31/517 , A61K31/519 , A61P1/00 , A61P1/10 , A61P1/16 , A61P3/04 , A61P9/00 , A61P11/06 , A61P25/00 , A61P25/02 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/30 , A61P43/00 , C07B61/00 , C07C233/66 , C07C235/42 , C07C235/84 , C07C237/20 , C07C237/30 , C07D207/26 , C07D207/27 , C07D207/32 , C07D207/325 , C07D207/327 , C07D209/88 , C07D213/40 , C07D213/61 , C07D213/81 , C07D213/82 , C07D215/48 , C07D215/50 , C07D217/02 , C07D217/08 , C07D217/26 , C07D231/12 , C07D231/14 , C07D231/56 , C07D233/32 , C07D233/34 , C07D233/90 , C07D235/24 , C07D239/28 , C07D239/80 , C07D241/24 , C07D257/04 , C07D261/18 , C07D263/58 , C07D271/08 , C07D277/20 , C07D277/56 , C07D277/68 , C07D295/155 , C07D307/85 , C07D401/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07D521/00 , C07D471/02 , C07C233/39
CPC分类号: C07D249/08 , C07C233/66 , C07C235/42 , C07C235/84 , C07C237/20 , C07D207/27 , C07D207/325 , C07D209/88 , C07D213/40 , C07D213/61 , C07D213/81 , C07D213/82 , C07D215/48 , C07D215/50 , C07D217/02 , C07D231/12 , C07D231/14 , C07D231/56 , C07D233/32 , C07D233/56 , C07D233/90 , C07D235/24 , C07D239/28 , C07D239/80 , C07D241/24 , C07D257/04 , C07D261/18 , C07D263/58 , C07D271/08 , C07D277/56 , C07D277/68 , C07D295/155 , C07D307/85 , C07D401/04 , C07D471/04 , C07D487/04 , C07D495/04 , C40B40/00
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, 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。
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公开(公告)号:US20060106071A1
公开(公告)日:2006-05-18
申请号:US10538395
申请日:2003-12-15
申请人: Linus Lin , William Hagmann , Sanjeev Kumar , Wenji Yin , George Doss
发明人: Linus Lin , William Hagmann , Sanjeev Kumar , Wenji Yin , George Doss
IPC分类号: A61K31/44 , A61K31/277 , C07D213/63 , C07C255/50
CPC分类号: C07D213/64 , C07C255/60 , C07C275/24 , C07C2601/04
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.
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公开(公告)号:US6053309A
公开(公告)日:2000-04-25
申请号:US246357
申请日:1999-02-08
申请人: Linus Lin
发明人: Linus Lin
IPC分类号: A45C11/04
CPC分类号: A45C11/04
摘要: A pair of far-sighted eyeglasses with a case includes a case consisting of an upper half case and a lower half case, and a pair of far-sighted eyeglasses. The eyeglasses have two elastic temples with curved portions that protrude slightly beyond an upper edge of the lower half case when placed in the case such that the temples are compressed by the upper half case when the case is closed. When the upper half case is disengaged from the lower half case for opening, the upper half case is pushed away from the lower half case by the temples recovering the elasticity of the curved portions so as to facilitate the opening of the case, without the possibility of the eyeglasses falling out of the case during opening.
摘要翻译: 具有外壳的一副具有远见的眼镜包括由上半壳和下半壳组成的壳体以及一对有远见的眼镜。 眼镜具有两个弹性体,其弯曲部分在放置在壳体中时稍微突出于下半壳体的上边缘,使得当壳体关闭时,这些镜腿被上半部分压缩。 当上半壳与用于打开的下半壳脱开时,上半壳被恢复弯曲部分的弹性的寺庙从下半壳推开,以便于壳体的打开,而不会有可能 的眼镜在打开期间脱离外壳。
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公开(公告)号:US20050239828A1
公开(公告)日:2005-10-27
申请号:US10507864
申请日:2003-03-21
申请人: William Hagmann , Linus Lin , Shrenik Shah , Mark Goulet , James Jewell
发明人: William Hagmann , Linus Lin , Shrenik Shah , Mark Goulet , James Jewell
IPC分类号: C07D307/24 , A61K31/165 , A61K31/27 , A61K31/275 , A61K31/341 , A61K31/351 , A61K31/397 , A61K31/40 , A61K31/401 , A61K31/4015 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4425 , A61K31/445 , A61K31/4545 , A61K31/5375 , A61P1/10 , A61P1/14 , A61P1/16 , A61P3/04 , A61P9/10 , A61P11/06 , A61P25/00 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P25/36 , A61P29/00 , A61P43/00 , C07C233/59 , C07C235/40 , C07C235/82 , C07C237/24 , C07C255/60 , C07C271/24 , C07C317/44 , C07D205/04 , C07D207/16 , C07D207/28 , C07D207/38 , C07D207/48 , C07D211/60 , C07D211/62 , C07D213/40 , C07D213/56 , C07D213/61 , C07D213/82 , C07D213/89 , C07D265/30 , C07D307/68 , C07D309/08 , C07D401/04 , C07D41/02
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。
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