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    • 4. 发明授权
      US5663352A 4-phenyl-4-phenylpropyl(enyl)-piperidines as tachykinin antagonists 失效
    • 4-phenyl-4-phenylpropyl(enyl)-piperidines as tachykinin antagonists
    • US5663352A
    • 1997-09-02
    • US583014
    • 1996-01-19
    • Angus Murray MacLeod , Kevin John Merchant , Graeme Irvine Stevenson
    • Angus Murray MacLeod , Kevin John Merchant , Graeme Irvine Stevenson
    • A61K31/4427 , A61K31/445 , A61K31/4465 , A61K31/451 , A61K31/53 , A61P1/08 , A61P25/04 , A61P25/06 , A61P29/00 , A61P43/00 , C07D211/18 , C07D211/22 , C07D211/32 , C07D401/06 , C07D211/14 , C07D211/12
    • C07D401/06 , C07D211/18 , C07D211/22 , C07D211/32
    • The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts and prodrugs thereof, wherein X represents a propylene or propenylene chain optionally substituted by one or more of R.sup.4, R.sup.5, R.sup.6 and R.sup.7 ; m is 2, 3 or 4; n is 0, 1 or 2 when m is 2 or 3, and n is 0 or 1 when m is 4; R.sup.1 represents optionally substituted phenyl; R.sup.2 represents optionally substituted phenyl, heteroaryl, benzhydryl or benzyl; R.sup.3 represents H, COR.sup.9, CO.sub.2 R.sup.10, COCONR.sup.10 R.sup.11, COCO.sub.2 R.sup.10, SO.sub.2 R.sup.15, CONR.sup.10 SO.sub.2 R.sup.15, C.sub.1-6 alkyl optionally substituted by a group selected from (CO.sub.2 R.sup.10, CONR.sup.10 R.sup.11, hydroxy, cyano, COR.sup.9, NR.sup.10 R.sup.11, C(NOH)NR.sup.10 R.sup.11, CONHphenyl(C.sub.1-4 alkyl), COCO.sub.2 R.sup.10, COCONR.sup.10 R.sup.11, SO.sub.2 R.sup.15, CONR.sup.10 SO.sub.2 R.sup.15 and optionally substituted phenyl), Y--R.sup.8 or CO--Z--(CH.sub.2).sub.q --R.sup.12 ; R.sup.4 and R.sup.5 each independently represent H, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-5 cycloalkylmethyl, hydroxy or C.sub.1-6 alkoxy, or R.sup.4 and R.sup.5 together form a group .dbd.O; R.sup.6 and R.sup.7 each independent represents H, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-5 cycloalkylmethyl, hydroxy or C.sub.1-6 alkoxy or R.sup.6 and R.sup.7 together form a group .dbd.O; R.sup.8 represents an optionally substituted aromatic heterocycle; R.sup.9 represents H, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-5 cycloalkylmethyl, or phenyl; R.sup.10 and R.sup.11 each independently represent H, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl or C.sub.3-5 cycloalkylmethyl; R.sup.12 represents NR.sup.13 R.sup.14 or an optionally substituted aromatic or non-aromatic azacyclic or azabicyclic group; R.sup.13 and R.sup.14 each independently represent H, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-5 cycloalkylmethyl, optionally substituted phenyl or phenylC.sub.1-4 alkyl; R.sup.15 represents C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-5 cycloalkylmethyl, trifluoromethyl or optionally substituted phenyl; Y represents a hydrocarbon chain of 1, 2, 3 or 4 carbon atoms which may optionally be substituted by oxo; Z represents CH.sub.2, O, S or NR.sup.10 ; and q represents 0, 1, 2, 3, 4, 5 or 6. The compounds are tachykinin antagonists useful for treating pain or inflammation, migraine or emesis.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 6. 发明授权
      US5985896A Piperidine and morpholine derivatives and their use as therapeutic agents 失效
    • Piperidine and morpholine derivatives and their use as therapeutic agents
    • 哌啶和吗啉衍生物及其作为治疗剂的用途
    • US5985896A
    • 1999-11-16
    • US981526
    • 1997-12-18
    • Raymond Baker , Jason Matthew Elliott , Graeme Irvine Stevenson , Christopher John Swain
    • Raymond Baker , Jason Matthew Elliott , Graeme Irvine Stevenson , Christopher John Swain
    • C07D405/12 , A61K31/443 , A61K31/445 , A61P25/04 , A61P25/06 , C07D405/14
    • C07D405/14
    • The present invention provides compounds of formula (I), wherein R.sup.1 is phenyl or a 5- or 6-membered aromatic heterocyclic group containing 1, 2, 3 or 4 heteroatoms, selected from nitrogen, oxygen and sulphur, which aryl or heteroaryl group is optionally substituted; R.sup.2 is hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, CF.sub.3, OCF.sub.3, NO.sub.2, CN, SR.sup.a, SOR.sup.a, SO.sub.2 R.sup.a, CO.sub.2 R.sup.a, CONR.sup.a R.sup.b, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl or C.sub.1-4 alkyl substituted by C.sub.1-4 alkoxy, where R.sup.a and R.sup.b each independently represent hydrogen or C.sub.1-4 alkyl; R.sup.4, R.sup.5, R.sup.6, R.sup.9a and R.sup.9b, A, X, and Y are as defined in the specification; the dotted line is an optional double bond; Q.sup.1 is oxygen, sulphur or --NH--; Q.sup.2 is --N.dbd., --NH--, --CH.dbd. or --CH.sub.2 --; and m is zero or 1; and pharmaceutically acceptable salts and prodrugs thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia. ##STR1##
    • PCT No.PCT / GB96 / 01477 Sec。 371 1997年12月18日第 102（e）1997年12月18日PCT PCT 1996年6月20日PCT公布。 第WO97 / 01554号公报 日期1997年1月16日本发明提供式（I）化合物，其中R 1是苯基或含有1,2,3或4个选自氮，氧和硫的杂原子的5-或6-元芳族杂环基，其中 芳基或杂芳基任选被取代; R2是氢，卤素，C1-6烷基，C1-6烷氧基，CF3，OCF3，NO2，CN，SRa，SORa，SO2Ra，CO2Ra，CONRaRb，C2-6烯基，C2-6炔基或被C1-4烷氧基取代的C1-4烷基， R a和R b各自独立地表示氢或C 1-4烷基; R4，R5，R6，R9a和R9b，A，X和Y如说明书中所定义; 虚线是可选的双键; Q1是氧，硫或-NH-; Q2是-N =，-NH-，-CH =或-CH 2 - ; m为0或1; 及其药学上可接受的盐和前药。 该化合物特别用于治疗或预防疼痛，炎症，偏头痛，呕吐和带状疱疹后神经痛。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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