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    • 8. 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
    • 9. 发明授权
      US5260317A Piperidine, tetrahydropyridine and pyrrolidine compounds 失效
    • Piperidine, tetrahydropyridine and pyrrolidine compounds
    • 哌啶，四氢吡啶和吡咯烷化合物
    • US5260317A
    • 1993-11-09
    • US972127
    • 1992-11-05
    • Gilbert Lavielle , Michel Laubie , Francis Colpaert
    • Gilbert Lavielle , Michel Laubie , Francis Colpaert
    • C07D207/20 , C07D211/12 , C07D211/14 , C07D211/22 , C07D211/70 , C07D295/13 , C07D295/185 , C07D401/04 , C07D405/04 , C07D401/40 , A61K31/47
    • C07D295/185 , C07D207/20 , C07D211/12 , C07D211/14 , C07D211/22 , C07D211/70 , C07D295/13 , C07D401/04 , C07D405/04
    • The invention relates to compounds of formula I: ##STR1## in which R.sub.1 represents a naphthyl radical, a dihydronaphthyl radical, a tetrahydronaphthyl radical, a quinolyl radical or a 1,4-benzodioxanyl radical, A represents a single bond, a double bond, a methylene radical, a radical of formula z.sub.1 :--CH.dbd. (z.sub.1)or a radical of formula z.sub.2 :.dbd.CH-- (z.sub.2)the ring B represents a piperidyl radical, a pyrrolidinyl radical, or a 1,2,3,6-tetrahydropyridyl radical, and R.sub.2 represents: a hydrogen atom, a benzyl radical, or an alkyl radical having 1 to 6 carbon atoms, on condition that in one of these cases R.sub.1 is other than a naphthyl (y.sub.1), dihydronaphthyl (y.sub.2) or tetrahydronaphthyl (y.sub.3) radical and B is other than a piperidinyl radical, or an aminoalkyl radical having 1 to 6 carbon atoms, a cyanoalkyl radical having 1 to 6 carbon atoms, or a radical of formula w.sub.1 : ##STR2## in which n is 1-6 and R.sub.4 represents a hydrogen atom, a halogen atom, an alkyl radical having 1 to 6 carbon atoms, or an alkoxy radical having 1 to 6 carbon atoms, and their addition salts with a pharmaceutically-acceptable inorganic or organic acid, and medicaments containing the same.
    • 本发明涉及式I化合物：其中R 1表示萘基，二氢萘基，四氢萘基，喹啉基或1,4-苯并二恶烷基，A表示单键，双键， 亚甲基，式z1的基团：-CH =（z1）或式z2的基团：= CH-（z2）环B表示哌啶基，吡咯烷基或1,2,3,6 并且R 2表示：氢原子，苄基或具有1至6个碳原子的烷基，条件是在这些情况之一中，R 1不同于萘基（y1），二氢萘基（y2）或 四氢萘基（y3）基团，B不是哌啶基或具有1-6个碳原子的氨基烷基，具有1至6个碳原子的氰基烷基或式w1的基团：其中其中 n为1-6，R 4表示氢原子，卤素原子，碳原子数1〜6的烷基或烷氧基 具有1至6个碳原子的化合物及其与药学上可接受的无机酸或有机酸的加成盐，以及含有它们的药物。
    • 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
    • 10. 发明授权
      US5242933A Piperidine, tetrahydropyridine and pyrrolidine compounds 失效
    • Piperidine, tetrahydropyridine and pyrrolidine compounds
    • 哌啶，四氢吡啶和吡咯烷化合物
    • US5242933A
    • 1993-09-07
    • US972126
    • 1992-11-05
    • Gilbert Lavielle , Michel Laubie , Francis Colpaert
    • Gilbert Lavielle , Michel Laubie , Francis Colpaert
    • C07D207/20 , C07D211/12 , C07D211/14 , C07D211/22 , C07D211/70 , C07D295/13 , C07D295/185 , C07D401/04 , C07D405/04
    • C07D295/185 , C07D207/20 , C07D211/12 , C07D211/14 , C07D211/22 , C07D211/70 , C07D295/13 , C07D401/04 , C07D405/04
    • The invention relates to compounds of formula I: ##STR1## in which R.sub.1 represents a naphthyl radical, a dihydronaphthyl radical, a tetrahydronaphthyl radical, a quinolyl radical or a 1,4-benzodioxanyl radical, A represents a single bond, a double bond, a methylene radical, a radical of formula z.sub.1 :--CH.dbd. (z.sub.1)or a radical of formula z.sub.2 :.dbd.CH-- (z.sub.2)the ring B represents a piperidyl radical, a pyrrolidinyl radical, or a 1,2,3,6-tetrahydropyridyl radical, and R.sub.2 represents: a hydrogen atom, a benzyl radical, or an alkyl radical having 1 to 6 carbon atoms, on condition that in one of these cases R.sub.1 is other than a naphthyl (y.sub.1), dihydronaphthyl (y.sub.2) or tetrahydronaphthyl (y.sub.3) radical and B is other than a piperidinyl radical, or an aminoalkyl radical having 1 to 6 carbon atoms, a cyanoalkyl radical having 1 to 6 carbon atoms, or a radical of formula w.sub.1 : ##STR2## in which n is 1-6 and R.sub.4 represents a hydrogen atom, a halogen atom, an alkyl radical having 1 to 6 carbon atoms, or an alkoxy radical having 1 to 6 carbon atoms , and their addition salts with a pharmaceutically- acceptable inorganic or organic acid, and medicaments containing the same.
    • 本发明涉及式I化合物：其中R 1表示萘基，二氢萘基，四氢萘基，喹啉基或1,4-苯并二恶烷基，A表示单键，双键， 亚甲基，式z1的基团：-CH =（z1）或式z2的基团：= CH-（z2）环B表示哌啶基，吡咯烷基或1,2,3,6 并且R 2表示：氢原子，苄基或具有1至6个碳原子的烷基，条件是在这些情况之一中，R 1不同于萘基（y1），二氢萘基（y2）或 四氢萘基（y3）基，B不是哌啶基或具有1-6个碳原子的氨基烷基，具有1-6个碳原子的氰基烷基或式w1的基团：其中其中 n为1-6，R 4表示氢原子，卤素原子，碳原子数1〜6的烷基或烷氧基 其具有1至6个碳原子，以及它们与药学上可接受的无机酸或有机酸的加成盐，以及含有它们的药物。
    • 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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