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1. 发明授权

US5637593A Tryptamine analogues as 5-ht1-like agonists 失效
标题翻译：色胺类似物为5-ht1样激动剂
公开(公告)号：US5637593A
公开(公告)日：1997-06-10
申请号：US448544
申请日：1995-06-20
申请人： Roderick A. Porter , John G. Ward
发明人： Roderick A. Porter , John G. Ward
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/44 , A61K31/4427 , A61P9/00 , A61P25/04 , A61P25/06 , C07D209/14 , C07D209/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12
CPC分类号： C07D401/04 , C07D209/14 , C07D209/16 , C07D401/12 , C07D401/14 , C07D403/12
摘要： A compound of structure (I), in which A.sup.1 is O, S(O).sub.n in which n is 0, 1 or 2, NR, CH.sub.2, or CH(OH); A.sup.2 is a bond or CH.sub.2 ; or A.sup.1 A.sup.2 is CH.dbd.CH; R is hydrogen or C.sub.1-4 alkyl; R.sup.1 is an optionally substituted 6- to 10-membered aryl or heteroaryl ring; suitably R.sup.1 is an optionally substituted 6- 10-membered aryl ring such as phenyl or naphthyl; suitably R.sup.1 is optionally substituted 6- to 10-membered heteroaryl ring, containing from 1 to 4 nitrogen atoms; R.sup.2 is hydrogen, halogen, C.sub.1-4 alkyl, CN, NO.sub.2 or CF.sub.3 ; R.sup.3 is C(R.sup.4)(R.sup.5)CH.sub.2 NR.sup.6 R.sup.7, --CH.dbd.NNHC(NH)NH.sub.2 or a; R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1-4 alkyl; R.sup.6 and R.sup.7 are the same or different and are each hydrogen or C.sub.1-4 alkyl or together with the nitrogen atom to which they are attached form a ring; R.sup.8 is hydrogen, C.sub.1-4 alkyl, or C.sub.3-6 alkenyl; the dotted lines represent an optional bond; and q and m are independently 1 or 2; and pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds are 5-HT.sub.1 -like agonists (or partial agonists) and as such are expected to have utility in medicine in the treatment and/or prophylaxis of migraine, and other conditions associated with cephalic pain, such as cluster headache, headache associated with vascular disorders and other neuralgia. They are also expected to have utility in the treatment of prophylaxis of portal hypertension. ##STR1##
摘要翻译： PCT No.PCT / EP93 / 03563 371日期：1995年6月20日 102（e）1995年6月20日PCT 1993年12月14日PCT PCT。公开号WO94 / 14770 日期：1994年7月7日A结构（I）化合物，其中A 1为O，S（O）n，其中n为0,1或2，NR，CH 2或CH（OH）; A2是键或CH2; 或A1A2是CH = CH; R是氢或C 1-4烷基; R1是任选取代的6-至10-元芳基或杂芳基环; 合适地R 1是任选取代的6- 10元芳基环，例如苯基或萘基; 合适地R 1是含有1至4个氮原子的任选取代的6至10元杂芳基环; R2是氢，卤素，C1-4烷基，CN，NO2或CF3; R3是C（R4）（R5）CH2NR6R7，-CH = NNHC（NH）NH2或a; R4和R5独立地是氢或C1-4烷基; R 6和R 7相同或不同，各自为氢或C 1-4烷基，或与它们所连接的氮原子一起形成环; R8是氢，C1-4烷基或C3-6烯基; 虚线表示可选的键; q和m独立地为1或2; 及其药学上可接受的盐，溶剂化物和水合物。化合物是5-HT1样激动剂（或部分激动剂），因此预期在医学中可用于治疗和/或预防偏头痛以及与头痛相关的其它病症，例如丛集性头痛，与头痛相关的头痛血管疾病等神经痛。它们也预期可用于治疗门静脉高压的预防。（一）图像（一）

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