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1. 发明申请

US20050234061A1 Substituted amides 审中-公开
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.

2. 发明授权

US5747485A Substituted azetidiones as anti-inflammatory and antidegenerative agents 失效
标题翻译：取代的氮杂环丁酮作为抗炎剂和抗再生剂
公开(公告)号：US5747485A
公开(公告)日：1998-05-05
申请号：US848076
申请日：1997-06-05
申请人： James Doherty , Conrad Dorn , Philippe Durette , Paul Finke , Malcolm Maccoss , Sander Mills , Shrenik Shah , Soumya Sahoo , William Hagmann , Jeffrey Hale , Thomas Lanza
发明人： James Doherty , Conrad Dorn , Philippe Durette , Paul Finke , Malcolm Maccoss , Sander Mills , Shrenik Shah , Soumya Sahoo , William Hagmann , Jeffrey Hale , Thomas Lanza
IPC分类号： A61K31/397 , A61K31/496 , A61K31/5377 , A61K31/395
CPC分类号： A61K31/496 , A61K31/397 , A61K31/5377
摘要： Substituted azetidinones are herein disclosed for use in the treatment of various elastase-mediated diseases.
摘要翻译：本文公开了取代的氮杂环丁酮，用于治疗各种弹性蛋白酶介导的疾病。

3. 发明授权

US5821261A Substituted saturated aza heterocycles as inhibitors of nitric oxide synthase 失效
标题翻译：取代的饱和杂环杂环作为一氧化氮合酶的抑制剂
公开(公告)号：US5821261A
公开(公告)日：1998-10-13
申请号：US745355
申请日：1996-11-08
申请人： Philippe L. Durette , Thomas Lanza, Jr.
发明人： Philippe L. Durette , Thomas Lanza, Jr.
IPC分类号： A61K31/401 , C07D207/16 , C07D211/06 , A01N43/40
CPC分类号： C07D207/16 , A61K31/401
摘要： Disclosed herein are compounds of Formula (I) ##STR1## and pharmaceutically acceptable salts thereof which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders, including neurodegenerative disorders, disorders of gastrointestinal motility and inflammation. These disease and disorders include hypotension, septic shock, toxic shock syndrom, hemodialysis, IL-2 therapy such as in cancer patients, cachexia, immnunosuppression such as in transplant therapy, autoimmune and/or inflammatory indications including sunburn or psoriasis and respiratory conditions such as bronchitis, asthma, and acure respiratory distress (ARDS), myocarditis, heart failure, atherosclerosis, arthritis, rheumatoid arthritis, chronic or inflammatory bowel disease, ulcerative colitis, Crohn's disease, systemic lupus erythematosis (SLE), ocular conditions such as ocular hypertension and uveitis, type 1 diabetes, insulin-dependent diabetes mellitus and cystic fibrosis. Compounds of Formula I are also useful in the treatment of hypoxia, hyperbaric oxygen convulsions and toxicity, dementia, Sydenham's chorea, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, multiple sclerosis, Korsakoffs disease, imbecility related to cerebral vessel disorder, ischemic brain edema, sleeping disorders, schizophrenia, depression, PMS, anxiety, drug addiction, pain, migraine, immune complex disease, as immunosupressive agents and for preventing or reversing tolerance to opiates and diazepines.
摘要翻译：本文公开了已经发现可用于治疗一氧化氮合酶介导的疾病和病症（包括神经变性疾病，胃肠蠕动和炎症疾病）的式（I）化合物及其药学上可接受的盐。这些疾病和病症包括低血压，脓毒性休克，中毒性休克综合征，血液透析，诸如癌症患者中的IL-2治疗，恶病质，移植治疗中的免疫抑制，自身免疫和/或炎性适应症，包括晒伤或牛皮癣和呼吸病症，例如支气管炎，哮喘和急性呼吸窘迫（ARDS），心肌炎，心力衰竭，动脉粥样硬化，关节炎，类风湿性关节炎，慢性或炎性肠病，溃疡性结肠炎，克罗恩病，系统性红斑狼疮（SLE），眼部疾病如眼高压和葡萄膜炎，1型糖尿病，胰岛素依赖性糖尿病和囊性纤维化。式I的化合物还可用于治疗缺氧，高压氧惊厥和毒性，痴呆，Sydenham's舞蹈病，帕金森病，亨廷顿舞蹈病，肌萎缩性侧索硬化，多发性硬化，柯萨科夫病，与脑血管障碍有关的缺血性，缺血性脑水肿，睡眠障碍，精神分裂症，抑郁症，PMS，焦虑，药物成瘾，疼痛，偏头痛，免疫复合物疾病，作为免疫抑制剂，以及用于预防或逆转对阿片剂和二氮杂类药物的耐受性。

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