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    Substituted pyrimidines
    3.
    发明申请
    Substituted pyrimidines 失效
    取代的嘧啶

    公开(公告)号：US20050245554A1

    公开(公告)日：2005-11-03

    申请号：US10527561

    申请日：2003-09-23

    申请人： Ihor Kopka ,  Bing Li ,  William Hagmann

    发明人： Ihor Kopka ,  Bing Li ,  William Hagmann

    IPC分类号： A61K31/505 ,  A61K31/513 ,  A61P25/18 ,  A61P25/28 ,  C07D239/28 ,  C07D239/34 ,  C07D239/38 ,  C07D239/42 ,  C07D239/46 ,  C07D239/52 ,  C07D239/54 ,  C07D239/56 ,  C07D401/12 ,  C07D487/08 ,  C07D43/02

    CPC分类号： C07D239/28 ,  C07D239/34 ,  C07D239/38 ,  C07D239/42 ,  C07D239/47 ,  C07D239/52 ,  C07D239/54 ,  C07D239/56 ,  C07D401/12 ,  C07D487/08

    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。

    N-(mercaptoacyl) peptidyl derivatives as antidegenerative agents
    4.
    发明授权
    N-(mercaptoacyl) peptidyl derivatives as antidegenerative agents 失效
    N-（巯基乙酰基）肽基衍生物作为抗代谢剂

    公开(公告)号：US5629343A

    公开(公告)日：1997-05-13

    申请号：US392730

    申请日：1995-02-23

    申请人： William Hagmann ,  Ihor Kopka

    发明人： William Hagmann ,  Ihor Kopka

    IPC分类号： A61K41/00 ,  C07C323/60 ,  A61K31/21

    CPC分类号： C07C323/60 ,  A61K41/00

    摘要： Novel N-(mercaptoacyl)peptidyl compounds are useful as inhibitors of matrix metalloendoproteinases which degrade major components of articular cartilage and basement membranes causing degenerative diseases such as arthritis, periodontal disease, corneal ulceration, are described. For example, N-(2-thiomethyl-4-phenyl-butanoyl)-L-leucinamide was prepared and its inhibitory activity against stromelysin was tested in vitro.

    摘要翻译： PCT No.PCT / US93 / 09137 Sec。 371日期1995年2月23日 102（e）1995年2月23日PCT PCT 1993年9月27日PCT公布。 公开号WO94 / 07481 日期1994年04月14日新型N-（巯基酰基）肽基化合物可用作降解引起关节炎，牙周病，角膜溃疡等退行性疾病的关节软骨和基底膜的主要成分的基质金属蛋白酶抑制剂。 例如，制备了N-（2-硫代甲基-4-苯基 - 丁酰基）-L-亮氨酰胺，并且在体外测试了其对溶基质蛋白酶的抑制活性。

    Substituted amides
    8.
    发明申请
    Substituted amides 有权

    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.

    Substituted sulfonamides
    9.
    发明申请
    Substituted sulfonamides 审中-公开
    取代磺酰胺

    公开(公告)号：US20070105914A1

    公开(公告)日：2007-05-10

    申请号：US10571842

    申请日：2004-09-14

    申请人： Helen Armstrong ,  Linda Chang ,  Ravindra Guthikonda ,  William Hagmann ,  Linus Lin ,  Shrenik Shah

    发明人： Helen Armstrong ,  Linda Chang ,  Ravindra Guthikonda ,  William Hagmann ,  Linus Lin ,  Shrenik Shah

    IPC分类号： A61K31/44 ,  A61K31/277 ,  A61K31/18

    CPC分类号： C07C311/06 ,  A61K31/18 ,  A61K31/277 ,  A61K31/44 ,  C07C311/03 ,  C07C311/13 ,  C07C311/16 ,  C07C311/17 ,  C07C311/19 ,  C07C311/29 ,  C07D209/08

    摘要： The substituted sulfonamides 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, 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： 本发明的取代磺酰胺是大麻素-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。该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。