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1. 发明申请

US20050154202A1 Substituted aryl amides 审中-公开
标题翻译：取代的芳基酰胺
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。

2. 发明授权

US5972975A Substituted 2-aminopyridines as inhibitors of nitric oxide synthase 失效
标题翻译：取代的2-氨基吡啶作为一氧化氮合酶的抑制剂
公开(公告)号：US5972975A
公开(公告)日：1999-10-26
申请号：US836953
申请日：1997-05-22
申请人： Craig Esser , William Hagmann , William Hoffman , Shrenik Shah , Kenny Wong , Renee Chabin , Ravindra Guthikonda , Malcolm Maccoss , Charles Caldwell , Philippe Durette
发明人： Craig Esser , William Hagmann , William Hoffman , Shrenik Shah , Kenny Wong , Renee Chabin , Ravindra Guthikonda , Malcolm Maccoss , Charles Caldwell , Philippe Durette
IPC分类号： A61K31/44 , C07D213/75
CPC分类号： A61K31/44
摘要： Substituted 2-aminopyridine compounds of Formula (I) and pharmaceutically acceptable salts which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders. ##STR1##
摘要翻译： PCT No.PCT / US95 / 16151 Sec。 371日期：1997年5月22日 102（e）日期1997年5月22日PCT提交1995年12月8日PCT公布。出版物WO96 / 18616 PCT 日期：1996年6月20日公知的可用于治疗一氧化氮合酶介导的疾病和病症的式（I）的取代的2-氨基吡啶化合物和药学上可接受的盐。

3. 发明授权

US5403952A Substituted cyclic derivatives as novel antidegenerative agents 失效
标题翻译：取代的环状衍生物作为新的抗代谢剂
公开(公告)号：US5403952A
公开(公告)日：1995-04-04
申请号：US133493
申请日：1993-10-08
申请人： William Hagmann , Charles G. Caldwell , Paul R. Gooley
发明人： William Hagmann , Charles G. Caldwell , Paul R. Gooley
IPC分类号： C07C237/22 , C07K7/100
CPC分类号： C07C237/22 , C07C2101/08 , C07C2101/10 , C07C2101/14 , C07C2101/16
摘要： Novel substituted cyclic compounds of Formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophic epidermolysis bullosa, and coronary thrombosis associated with atherosclerotic plaque rupture. The matrix metalloendoproteinases are a family of zinc-containing proteinases including but not limited to stromelysin, collagenase, and gelatinase, that are capable of degrading the major components of articular cartilage and basement membranes. The inhibitors claimed herein may also be useful in preventing the pathological sequelae following a traumatic injury that could lead to a permanent disability. These compounds may also be useful as novel birth control agents by preventing ovulation or implantation. ##STR1##
摘要翻译：发现式I的新型取代的环状化合物是基质金属蛋白酶介导的疾病的有用的抑制剂，包括骨关节炎，类风湿性关节炎，脓毒性关节炎，某些癌症中的肿瘤侵袭，牙周病，角膜溃疡，蛋白尿，营养不良的表皮松解性大疱性和冠状动脉血栓相关动脉粥样硬化斑块破裂。基质金属蛋白酶是含有蛋白酶的家族，包括但不限于基质溶素，胶原酶和明胶酶，其能够降解关节软骨和基底膜的主要成分。本文所要求的抑制剂也可用于预防可能导致永久性残疾的外伤性损伤后的病理后遗症。这些化合物也可以通过防止排卵或植入而用作新的避孕药。我

4. 发明授权

US5359071A 15-substituted 4-azasteroids 失效
标题翻译： 15-取代的4-azasteroids
公开(公告)号：US5359071A
公开(公告)日：1994-10-25
申请号：US30508
申请日：1993-03-12
申请人： Philippe L. Durette , Craig K. Esser , William Hagmann , Ihor E. Kopka
发明人： Philippe L. Durette , Craig K. Esser , William Hagmann , Ihor E. Kopka
IPC分类号： C07J41/00 , A61K31/58 , A61P5/28 , C07J1/00 , C07J21/00 , C07J51/00 , C07J73/00 , A61K31/535
CPC分类号： C07J73/005 , C07J1/0011 , C07J21/003 , C07J51/00
摘要： Compounds of the formula ##STR1## or a pharmaceutically acceptable salt or ester thereof, wherein R.sup.1 is selected from the group consisting of hydrogen and C.sub.1-10 alkyl;R.sup.2 is selected from the group consisting of hydrogen and C.sub.1-10 alkyl;R.sup.3 is selected from the group consisting of C.sub.1-10 alkoxyl, C.sub.1-10 alkyl and cyano;R.sup.4 is selected from the group consisting of C.sub.1-10 alkenyloxyl, C.sub.1-10 alkoxyl, C.sub.1-10 alkyl, C.sub.1-10 alkylcarbamic, C.sub.1-10 alkylcarbonyloxyl, carbonyl, hydroxyl, and --NHR.sup.5, andR.sup.5 is selected from the group consisting of hydrogen and C.sub.1-10 alkylcarbonyl. Such compounds are useful as selective antagonists of testosterone 5.alpha.-reductase 1.
摘要翻译：式IMA的化合物或其药学上可接受的盐或酯，其中R 1选自氢和C 1-10烷基; R2选自氢和C 1-10烷基; R3选自C1-10烷氧基，C1-10烷基和氰基; R4选自C1-10烯氧基，C1-10烷氧基，C1-10烷基，C1-10烷基氨基甲酸，C1-10烷基羰基氧基，羰基，羟基和-NHR5，R5选自氢和C 1-10烷基羰基。这些化合物可用作睾酮5α-还原酶1的选择性拮抗剂。

5. 发明申请

US20060106071A1 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.

6. 发明申请

US20070088058A1 Aralkyl amines as cannabinoid receptor modulators 失效
标题翻译：芳烷基胺作为大麻素受体调节剂
公开(公告)号：US20070088058A1
公开(公告)日：2007-04-19
申请号：US10576381
申请日：2004-10-27
申请人： Shrenik Shah , Quang Truong , Hongbo Qi , William Hagmann
发明人： Shrenik Shah , Quang Truong , Hongbo Qi , William Hagmann
IPC分类号： A61K31/4412 , C07D249/08 , C07D213/63 , A61K31/415 , A61K31/277 , C07D231/12 , A61K31/4196
CPC分类号： C07D213/74 , C07C255/58 , C07C317/28 , C07C317/48 , C07C323/63 , C07C2601/04 , C07C2601/14 , C07D207/32 , C07D207/325 , C07D213/38 , C07D213/57 , C07D213/61 , C07D213/64 , C07D231/12 , C07D231/38 , C07D239/26 , C07D249/06 , C07D249/08 , C07D249/14
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, including alcohol and nicotine addiction, 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。该化合物还可用于治疗药物滥用障碍，包括酒精和尼古丁成瘾，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。

7. 发明申请

US20050203112A1 Bicyclic amides 失效
标题翻译：双环酰胺
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。

8. 发明授权

US5952321A Substituted azetidinones as anti-inflammatory and antidegenerative agents 失效
标题翻译：取代的氮杂环丁酮作为抗炎和抗再生剂
公开(公告)号：US5952321A
公开(公告)日：1999-09-14
申请号：US764775
申请日：1996-12-12
申请人： James Doherty , Conrad Dorn , Philippe Durette , Paul Finke , Malcolm Maccoss , Sander Mills , Shrenik Shah , Soumya Sahoo , William Hagmann , Scott Polo
发明人： James Doherty , Conrad Dorn , Philippe Durette , Paul Finke , Malcolm Maccoss , Sander Mills , Shrenik Shah , Soumya Sahoo , William Hagmann , Scott Polo
IPC分类号： A61K31/395 , A61K31/397 , A61K31/40 , A61K31/4427 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/54 , A61P29/00 , C07D205/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
CPC分类号： C07D401/12 , C07D205/08 , C07D403/12 , C07D405/12
摘要： New substituted azetidinones of the general Formula (I) which have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents are described, wherein n is
摘要翻译：描述了已经被发现是有效的弹性蛋白酶抑制剂和由此有用的抗炎和抗代谢剂的通式（I）的新的取代的氮杂环丁酮，其中n为0

9. 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。

10. 发明授权

US5672583A Carboxy-peptidyl derivatives as antidegenerative active agents 失效
标题翻译：羧基肽基衍生物作为抗再生活性剂
公开(公告)号：US5672583A
公开(公告)日：1997-09-30
申请号：US436347
申请日：1995-05-17
申请人： Kevin Chapman , William Hagmann , Philippe Durette , Craig Esser , Ihor Kopka , Charles Caldwell
发明人： Kevin Chapman , William Hagmann , Philippe Durette , Craig Esser , Ihor Kopka , Charles Caldwell
IPC分类号： C07D275/02 , A61K31/195 , A61K31/275 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/421 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/445 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5355 , A61K31/5377 , A61K41/00 , A61P1/02 , A61P9/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07C237/22 , C07C255/23 , C07C271/22 , C07C275/28 , C07C279/14 , C07D207/16 , C07D209/34 , C07D209/46 , C07D209/48 , C07D211/76 , C07D213/55 , C07D213/75 , C07D213/81 , C07D235/16 , C07D261/08 , C07D263/32 , C07D263/56 , C07D277/64 , C07D295/185 , A61K37/02 , C07C237/52 , C07C259/06 , C07D277/62
CPC分类号： C07D209/48 , A61K41/00 , C07C237/22 , C07C255/23 , C07C271/22 , C07C275/28 , C07C279/14 , C07D209/34 , C07D213/75 , C07D235/16 , C07D263/56 , C07D277/64 , C07D295/185 , C07C2101/08
摘要： Novel Carboxy-peptidyl compounds of Formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophobic epidermolysis bullosa, coronary thrombosis associated with atherosclerotic plaque rupture, and aneurysmal aortic disease. The matrix metalloendoproteinases are a family of zinc-containing proteinases including but not limited to stromelysin, collagenase, and gelatinase, that are capable of degrading the major components of articular cartilage and basement membranes. The inhibitors claimed herein may also be useful in preventing the pathological sequelae following a traumatic injury that could lead to a permanent disability. These compounds may also have utility as a means for birth control by preventing ovulation or implantation. ##STR1##
摘要翻译： PCT No.PCT / US93 / 11207 Sec。 371日期1995年5月17日 102（e）日期1995年5月17日PCT 1993年11月18日PCT公布。 WO94 / 12169 PCT出版物 1994年6月9日发现式I的新型羧基肽基化合物是有用的基质金属蛋白酶介导的疾病的抑制剂，包括骨关节炎，类风湿性关节炎，脓毒性关节炎，某些癌症中的肿瘤侵袭，牙周病，角膜溃疡，蛋白尿，疏水性表皮松解与大动脉粥样硬化斑块破裂相关的冠状动脉血栓形成和动脉瘤性主动脉疾病。基质金属蛋白酶是含有蛋白酶的家族，包括但不限于基质溶素，胶原酶和明胶酶，其能够降解关节软骨和基底膜的主要成分。本文所要求的抑制剂也可用于预防可能导致永久性残疾的外伤性损伤后的病理后遗症。这些化合物也可以通过预防排卵或植入作为避孕的手段。

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