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公开(公告)号：US06472418B1
公开(公告)日：2002-10-29
申请号：US09868449
申请日：2001-06-18
申请人： Mark Wallace Creswell , Michael Higginbottom , David Christopher Horwell , Russel Andrew Lewthwaite , Martyn Clive Pritchard , Jennifer Raphy
发明人： Mark Wallace Creswell , Michael Higginbottom , David Christopher Horwell , Russel Andrew Lewthwaite , Martyn Clive Pritchard , Jennifer Raphy
IPC分类号： A61K31404
CPC分类号： C07D401/12 , C07D209/20 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14
摘要： Non-peptide acetamide derivatives of Formula I are specific NK1 antagonist, where R is aryl, R1 and R2 are H or alkyl, m, n and q are integers from 0 to 4, X is NR8 or NHCONH, R3 and R9 are H or alkyl, R4 is naphthyl or indolyl, R5 and R2 are H or alkyl, and R6 is aryl. The compounds are useful agents for treating inflammatory and allergic disorders, pain, anxiety, depression, schizophrenia and emesis.
摘要翻译： 式I的非肽乙酰胺衍生物是特异性NK1拮抗剂，其中R是芳基，R1和R2是H或烷基，m，n和q是0-4的整数，X是NR8或NHCONH，R3和R9是H或 烷基，R4是萘基或吲哚基，R5和R2是H或烷基，R6是芳基。这些化合物是治疗炎性和过敏性疾病，疼痛，焦虑，抑郁，精神分裂症和呕吐的有用的药剂。
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公开(公告)号：US5767088A
公开(公告)日：1998-06-16
申请号：US697992
申请日：1996-09-04
IPC分类号： A61K38/00 , A61P1/00 , A61P9/00 , A61P11/00 , A61P25/00 , A61P25/04 , A61P25/24 , A61P25/26 , A61P29/00 , C07C271/10 , C07C271/20 , C07C317/28 , C07K5/02 , C07K5/06 , C07K5/065 , C07K7/06 , A61K38/05
CPC分类号： C07K7/06 , C07C271/20 , C07K5/021 , C07K5/06078 , C07K5/06191 , A61K38/00
摘要： The small compounds of the instant invention are tachykinin antagonists. The compounds are highly selective and functional NK.sub.3 antagonists expected to be useful in the treatment of pain, depression, anxiety, panic, schizophrenia, neuralgia, addiction disorders, inflammatory diseases, gastrointestinal disorders, vascular disorders, and neuropathological disorders.
摘要翻译： 本发明的小化合物是速激肽拮抗剂。 这些化合物是高选择性和功能性的NK3拮抗剂，预期可用于治疗疼痛，抑郁症，焦虑症，恐慌症，精神分裂症，神经痛，成瘾症，炎性疾病，胃肠道疾病，血管疾病和神经病理学障碍。
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公开(公告)号：US5981755A
公开(公告)日：1999-11-09
申请号：US168512
申请日：1998-10-08
申请人： David Christopher Horwell , William Howson , Martyn Clive Pritchard , Edward Roberts , David Charles Rees
发明人： David Christopher Horwell , William Howson , Martyn Clive Pritchard , Edward Roberts , David Charles Rees
IPC分类号： C07D333/68 , A61K31/27 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K49/00 , A61P1/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P25/00 , A61P25/04 , A61P27/02 , A61P27/14 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07C271/18 , C07C271/22 , C07D209/20 , C07D209/30 , C07D231/56 , C07D333/60 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/12 , C07D209/04 , C07D209/18 , C07D405/06
CPC分类号： C07D209/30 , C07C271/22 , C07D209/20 , C07D231/56 , C07D333/60 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/12
摘要： The invention concerns tachykinin antagonists. The compounds are nonpeptides which have utility in treating disorders mediated by tachykinins. Such disorders are respiratory, inflammatory, gastrointestinal, ophthalmic, allergies, pain, vascular, diseases of the central nervous system, and migraine. Methods of preparing compounds and novel intermediates are also included. The compounds are expected to be especially useful in asthma and rheumatoid arthritis.
摘要翻译： 本发明涉及速激肽拮抗剂。 这些化合物是可用于治疗由速激肽介导的疾病的非肽。 这些疾病是呼吸道，炎性，胃肠道，眼睛，过敏，疼痛，血管，中枢神经系统疾病和偏头痛。 还包括制备化合物和新型中间体的方法。 化合物预期在哮喘和类风湿性关节炎中特别有用。
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4.发明授权Use of a tachykinin antagonist for the manufacture of a medicament for the treatment of emesis 失效速激肽拮抗剂在制备用于治疗呕吐的药物中的用途
公开(公告)号：US05998435A
公开(公告)日：1999-12-07
申请号：US194620
申请日：1998-12-01
IPC分类号： B82B1/00 , A61K31/4045 , A61K31/405 , A61K31/40
CPC分类号： A61K31/405 , A61K31/4045
摘要： The instant invention is directed to a method for the treatment of emesis comprising administering the compound [R,S]-[2-(1H-Indol-3-yl)-1-methyl-1-(1-phenyl-ethylcarbamoly)-ethyl]-carbamic acid benzofuran-2ylmethyl ester.
摘要翻译： PCT No.PCT / US97 / 10503 Sec。 371 1998年12月1日第 102（e）日期1998年12月1日PCT提交1997年6月18日PCT公布。 第WO97 / 49393号公报 日本1997年12月31日本发明涉及一种治疗呕吐的方法，包括给予化合物[R，S] - [2-（1H-吲哚-3-基）-1-甲基-1-（1- 苯基 - 乙基氨基甲酰基） - 乙基] - 氨基甲酸苯并呋喃-2-基甲基酯。
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公开(公告)号：US5856354A
公开(公告)日：1999-01-05
申请号：US953037
申请日：1997-10-17
申请人： David Christopher Horwell , William Howson , Martyn Clive Pritchard , Edward Roberts , David Charles Rees
发明人： David Christopher Horwell , William Howson , Martyn Clive Pritchard , Edward Roberts , David Charles Rees
IPC分类号： C07D333/68 , A61K31/27 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K49/00 , A61P1/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P25/00 , A61P25/04 , A61P27/02 , A61P27/14 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07C271/18 , C07C271/22 , C07D209/20 , C07D209/30 , C07D231/56 , C07D333/60 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/12 , A61K31/165 , C07C229/36 , C07C271/20
CPC分类号： C07D209/30 , C07C271/22 , C07D209/20 , C07D231/56 , C07D333/60 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/12
摘要： The invention concerns tachykinin antagonists. The compounds are neopeptides which have utility in treating disorders mediated by tachykinins. Such disorders are respiratory, inflammatory, gastrointestinal, ophthalmic, allergies, pain, vascular, diseases of the central nervous system, and migraine. Methods of preparing compounds and novel intermediates are also included. The compounds are expected to be especially useful in asthma and rheumatoid arthritis.
摘要翻译： 本发明涉及速激肽拮抗剂。 这些化合物是可用于治疗由速激肽介导的疾病的新肽。 这些疾病是呼吸道，炎性，胃肠道，眼睛，过敏，疼痛，血管，中枢神经系统疾病和偏头痛。 还包括制备化合物和新型中间体的方法。 化合物预期在哮喘和类风湿性关节炎中特别有用。
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公开(公告)号：US5726200A
公开(公告)日：1998-03-10
申请号：US661254
申请日：1996-06-10
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/405 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/47 , A61K38/00 , A61P1/00 , A61P1/04 , A61P3/04 , A61P25/00 , A61P43/00 , C07D209/14 , C07D209/20 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/14 , C07K5/02 , C07K5/023 , C07K5/06 , C07K5/08 , C07K5/097 , C07K14/575 , C07K14/655
CPC分类号： C07D401/12 , C07D209/14 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/021 , C07K5/0821 , A61K38/00
摘要： Novel pro-drugs to new and unnatural dipeptoids of .alpha.-substituted Trp-Phe derivatives useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, or as antipsychotics are disclosed. Further, the dipeptoids are antianxiety agents and antiulcer agents. They are agents useful for preventing the response to the withdrawal from chronic treatment or with use of nicotine, diazepam, alcohol, cocaine, caffeine, or opioids. The pro-drugs are also useful in treating and/or preventing panic attacks. Also disclosed are pharmaceutical compositions and methods of treatment using the pro-drugs as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject pro-drug compounds in diagnostic compositions.
摘要翻译： 公开了用于治疗肥胖，胃肠胃分泌过多，胃泌素依赖性肿瘤或作为抗精神病药物的α-取代的Trp-Phe衍生物的新型和非天然罂粟素的新型前体药物。 此外，趾甲是抗焦虑剂和抗溃疡剂。 它们是用于预防慢性治疗戒断或使用尼古丁，地西泮，酒精，可卡因，咖啡因或阿片样物质的反应的药剂。 前药也可用于治疗和/或预防恐慌发作。 还公开了药物组合物和使用前药的治疗方法以及其制备方法和可用于其制备的新型中间体。 本发明的另一个特征是本发明的前药化合物在诊断组合物中的用途。
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公开(公告)号：US06194437B1
公开(公告)日：2001-02-27
申请号：US09230933
申请日：1999-02-03
IPC分类号： C07D40112
CPC分类号： C07D213/40 , C07D209/20 , C07D213/56 , C07D213/89 , C07D401/12 , C07D403/12 , C07D405/12 , C07D417/12
摘要： The compounds of the instant invention are novel compounds of Formula I or a pharmaceutically acceptable salt thereof wherein Ar is phenyl or pyridyl unsubstituted or substituted. Ar1 can be independently selected from Ar and can also include pyridyl-N-oxide, indolyl, imidazole, and pyridyl; R3 can be independently selected from Ar or is hydrogen, hydroxy, NMe2, N-methyl-pyrrole, imidazole, tetrazole, thiazole (a), (b), (c), or (d), wherein Ar2 is phenyl or pyridyl. The instant compounds antagonize the bombesin receptors in mammals and are therefore effective in treating and/or preventing depression, psychoses, seasonal affective disorders, cancer, feeding disorders, gastrointestinal disorders, inflammatory bowel disease, sleep disorders, and memory impairment.
摘要翻译： 本发明的化合物是式I的新化合物或其药学上可接受的盐，其中Ar是未取代或取代的苯基或吡啶基。 Ar 1可以独立地选自Ar，也可以包括吡啶基-N-氧化物，吲哚基，咪唑和吡啶基; R3可以独立地选自Ar或氢，羟基，NMe2，N-甲基 - 吡咯，咪唑，四唑，噻唑（a），（b），（c）或（d），其中Ar2是苯基或吡啶基。 本发明化合物拮抗哺乳动物中的铃蟾肽受体，因此有效地治疗和/或预防抑郁症，精神病，季节性情感障碍，癌症，进食障碍，胃肠道疾病，炎症性肠病，睡眠障碍和记忆障碍。
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公开(公告)号：US5716979A
公开(公告)日：1998-02-10
申请号：US727067
申请日：1996-10-08
申请人： David Christopher Horwell , William Howson , Martyn Clive Pritchard , Edward Roberts , David Charles Rees
发明人： David Christopher Horwell , William Howson , Martyn Clive Pritchard , Edward Roberts , David Charles Rees
IPC分类号： C07D333/68 , A61K31/27 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K49/00 , A61P1/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P25/00 , A61P25/04 , A61P27/02 , A61P27/14 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07C271/18 , C07C271/22 , C07D209/20 , C07D209/30 , C07D231/56 , C07D333/60 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/12 , C07D307/70 , C07D307/79 , C07D333/26
CPC分类号： C07D209/30 , C07C271/22 , C07D209/20 , C07D231/56 , C07D333/60 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/12
摘要： The invention concerns tachykinin antagonists. The compounds are nonpeptides which have utility in treating disorders mediated by tachykinins. Such disorders are respiratory, inflammatory, gastrointestinal, ophthalmic, allergies, pain, vascular, diseases of the central nervous system, and migraine. Methods of preparing compounds and novel intermediates are also included. The compounds are expected to be especially useful in asthma and rheumatoid arthritis.
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公开(公告)号：US07122678B2
公开(公告)日：2006-10-17
申请号：US11078961
申请日：2005-03-11
申请人： Justin Stephen Bryans , David Christopher Horwell , Andrew John Thorpe , David Juergen Wustrow , Po-Wai Yuen
发明人： Justin Stephen Bryans , David Christopher Horwell , Andrew John Thorpe , David Juergen Wustrow , Po-Wai Yuen
IPC分类号： C07D209/54 , C07C69/74 , C07C61/06
CPC分类号： C07D221/20 , C07C49/417 , C07C69/608 , C07C69/612 , C07C205/51 , C07C205/53 , C07C229/28 , C07C229/34 , C07C2601/04 , C07C2601/08 , C07C2602/50 , C07D209/96 , C07D307/94 , C07D311/96
摘要： The invention is a novel series of cyclic amino acids which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), and inflammation, especially arthritis. A pharmaceutical composition containing a compound of the invention as well as methods of preparing the compounds and novel intermediates useful in the preparation of the final compounds are included.
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公开(公告)号：US06489352B2
公开(公告)日：2002-12-03
申请号：US09924803
申请日：2001-08-08
IPC分类号： C07D20954
CPC分类号： C07D209/96 , C07D205/12 , C07D209/44 , C07D209/46 , C07D209/54
摘要： Novel substituted amino acids of formula are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, and neuropathological disorders. Processes for the preparation and intermediates useful in the preparation are also disclosed.
摘要翻译： 公开的新型取代的氨基酸被公开并且可用作治疗癫痫，微弱发作，运动功能减退，颅内障碍，神经变性疾病，抑郁症，焦虑症，恐慌症，疼痛和神经病理学障碍的药物。 还公开了用于制备的方法和可用于制备的中间体。
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