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    8-(heterocyclylmethyl)quinoline derivatives for treating urinary incontinence
    1.
    发明授权
    8-(heterocyclylmethyl)quinoline derivatives for treating urinary incontinence 失效
    用于治疗尿失禁的8-（杂环基甲基）喹啉衍生物

    公开(公告)号：US06413984B1

    公开(公告)日：2002-07-02

    申请号：US09890526

    申请日：2001-08-01

    申请人： Christophe Philippo ,  Alain Braun ,  Philippe R. Bovy

    发明人： Christophe Philippo ,  Alain Braun ,  Philippe R. Bovy

    IPC分类号： A61K3147

    CPC分类号： C07D401/06 ,  Y10S514/844 ,  Y10S514/873 ,  Y10S514/937 ,  Y10S514/938 ,  Y10S514/939

    摘要： The invention concerns compounds of formula (I) wherein: A represents either a hydrogen atom or a hydroxyl group; B represents a pyrrolidin-2-yl (D) or 2-piperidyl (E), B capable of being substituted by one or two R5 groups; R1 represents a hydrogen atom, a C1-C6 alkyl, a C2-C6 alkenyl, a C1-C2 perfluoroalkyl or a C1-C6 fluoroalkyl group; R2, R3 or R4, independently of one another, represent a hydrogen atom, a C1-C6 alkyl, group or a C2-C6 alkenyl group, or R1 and R2 can together form a C1-C6 alkylene chain, or a C3-C6 alkenylene chain; R5 represents a C1-C6 alkyl group, and R6 represents a hydrogen atom, a C1-C6 alkyl group, a C2-C6 alkenyl group, C3-C6 cycloalkyl, C3-C6 cycloalkenyl or a benzyl. Said compounds have therapeutic applications

    摘要翻译： 本发明涉及式（I）的化合物，其中：A表示氢原子或羟基; B表示可被一个或两个R 5基团取代的吡咯烷-2-基（D）或2-哌啶基（E），B。 R1表示氢原子，C1-C6烷基，C2-C6烯基，C1-C2全氟烷基或C1-C6氟代烷基; R2，R3或R4彼此独立地表示氢原子，C1-C6烷基，基团或C2-C6烯基，或者R1和R2可以一起形成C1-C6亚烷基链，或C3-C6 亚烯基链; R5表示C1-C6烷基，R6表示氢原子，C1-C6烷基，C2-C6烯基，C3-C6环烷基，C3-C6环烯基或苄基。 所述化合物具有治疗应用

    Benzylamine derivatives, their preparation and their application in therapeutics
    2.
    发明授权
    Benzylamine derivatives, their preparation and their application in therapeutics 失效
    苄胺衍生物，其制备及其在治疗中的应用

    公开(公告)号：US6060508A

    公开(公告)日：2000-05-09

    申请号：US254121

    申请日：1999-02-26

    申请人： Christophe Philippo ,  Marie Claire Orts ,  Olivier Crespin ,  Philippe R. Bovy

    发明人： Christophe Philippo ,  Marie Claire Orts ,  Olivier Crespin ,  Philippe R. Bovy

    IPC分类号： C07D333/54 ,  A61K31/343 ,  A61K31/381 ,  A61P1/00 ,  A61P9/00 ,  A61P13/00 ,  A61P25/06 ,  A61P27/16 ,  C07D307/79 ,  C07D307/85 ,  C07D307/91 ,  A61K31/34 ,  A61K31/38 ,  C07D307/78 ,  C07D333/52

    CPC分类号： C07D307/79

    摘要： Compounds of general formula (I) ##STR1## in which: A represents either a hydrogen atom, a hydroxyl, a C.sub.1-6 hydroxyalkyl group, a thiol, a C.sub.1-6 alkylsulphanyl group, an amino group, a C.sub.1-6 alkylamino group, a di(C.sub.1-6 alkyl)amino group, a C.sub.1-6 alkylhydroxylamine group, a C.sub.1-6 alkoxy group, a hydroxylamine group, an N,O-di(C.sub.1-6 alkyl)hydroxylamine group, an azido or a halogen such as fluorine, chlorine or bromine, B represents a hydrogen atom, a linear or branched C.sub.1-6 alkyl group, a C.sub.2-6 alkenyl group, a C.sub.1-6 fluoroalkyl group, a C.sub.1-2 perfluoroalkyl group, a C.sub.1-6 alkoxy group, a phenyl group or an oxo group, X represents an oxygen or sulphur atom.Application in therapeutics.

    摘要翻译： PCT No.PCT / FR97 / 01514 Sec。 371日期1999年2月26日 102（e）1999年2月26日PCT 1997年8月22日提交PCT公布。 公开号WO98 / 08834 日期：1998年3月5日通式（I）的化合物，其中：A表示氢原子，羟基，C1-6羟基烷基，硫醇，C1-6烷基硫烷基，氨基，C1-6 烷基氨基，二（C 1-6烷基）氨基，C 1-6烷基羟胺基，C 1-6烷氧基，羟胺基，N，O-二（C 1-6烷基）羟胺基，叠氮基或 卤素如氟，氯或溴，B表示氢原子，直链或支链C 1-6烷基，C 2-6烯基，C 1-6氟烷基，C 1-2全氟烷基，C 1〜 6烷氧基，苯基或氧代基，X表示氧或硫原子。 在治疗中的应用。

    CYCLOHEXYL(ALKYL)PROPANOLAMINES, PREPARATION METHOD AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
    3.
    发明申请
    CYCLOHEXYL(ALKYL)PROPANOLAMINES, PREPARATION METHOD AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 有权

    公开(公告)号：US20080261949A1

    公开(公告)日：2008-10-23

    申请号：US12144843

    申请日：2008-06-24

    申请人： Philippe R. Bovy ,  Roberto Cecchi ,  Gilles Courtemanche ,  Tiziano Croci ,  Ambrogio Oliva ,  Nunzia Viviani

    发明人： Philippe R. Bovy ,  Roberto Cecchi ,  Gilles Courtemanche ,  Tiziano Croci ,  Ambrogio Oliva ,  Nunzia Viviani

    IPC分类号： A61K31/553 ,  C07C311/01 ,  A61K31/24 ,  A61K31/421 ,  C07D263/54 ,  C07D267/02

    CPC分类号： C07C311/21 ,  C07C229/46 ,  C07C311/08 ,  C07C317/22 ,  C07C2601/14

    摘要： The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —SO2NH(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1-C4)alkyl group or with a (C1-C4)alkoxy group; R1 represents a hydrogen atom or a (C1-C4)alkyl group, a —CO(C1-C4)alkyl group, a phenyl-(C1-C4)alkyl group or a —COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1-C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1-C4)alkyl group, an —SO2phenyl-(C1-C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1-C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogen atom, a (C1-C6)alkyl group, a (C1-C4)alkoxy group, a —COO(C1-C4)alkyl group, a —CO(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl groups, —NO2, —CN, —CONR4R5, —COOH, or a 4,5-dihydro-1,3-oxazol-2-yl or 4,4-dimethyl-4,5-dihydro-1,3-oxazol-2-yl group; R4 and R5 represent, independently, a hydrogen atom, a phenyl, a (C1-C4)alkyl group or a phenyl-(C1-C4)alkyl group or R4 and R5 with the nitrogen atom to which they are attached, may form a ring of 5 to 7 atoms in total; and to the salts or solvates thereof, to the pharmaceutical compositions containing them, to a process for the preparation thereof and to intermediates in this process.

    Pharmaceutical compositions for treatment of circulatory disorders using N-substituted (.alpha.-imidazolyl-toluyl) pyrrole aniotensin II antagonists
    4.
    发明授权
    Pharmaceutical compositions for treatment of circulatory disorders using N-substituted (.alpha.-imidazolyl-toluyl) pyrrole aniotensin II antagonists 失效
    使用N-取代的（α-咪唑基 - 甲苯酰基）吡咯类抗生素II拮抗剂治疗循环障碍的药物组合物

    公开(公告)号：US6008368A

    公开(公告)日：1999-12-28

    申请号：US976757

    申请日：1997-11-24

    申请人： Philippe R. Bovy ,  Joe T. Collins ,  Robert E. Manning

    发明人： Philippe R. Bovy ,  Joe T. Collins ,  Robert E. Manning

    IPC分类号： C07D233/90 ,  C07D403/10 ,  A61K31/415 ,  A61K31/41 ,  C07D403/04 ,  C07D403/14

    CPC分类号： C07D403/10

    摘要： Pharmaceutical compositions comprising a compound selected from a class of N-substituted (.alpha.-imidazolyl-toluyl)pyrrole compounds are described for use in treatment of circulatory disorders. Compositions of particular interest comprise angiotensin II antagonist compounds of the formula ##STR1## wherein m is one; wherein R.sup.0 is selected from CH.sub.2 OH, CO.sub.2 H, CHO, CO.sub.2 CH.sub.3, CO.sub.2 C.sub.2 H.sub.5, CH.sub.2 OCH.sub.3, CH.sub.2 OCHOCH.sub.3 and CH.sub.2 --CO.sub.2 C.sub.2 H.sub.5 ; wherein R.sup.1 is selected from Cl, CF.sub.3, CHO, n-butyl, cyano, CO.sub.2 CH.sub.3 and CO.sub.2 CH.sub.2 CH.sub.3 ; wherein R.sup.2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, propylthio, butylthio and hydroxyalkyl; wherein each of R.sup.3, R.sup.4, R.sup.6, R.sup.7, R.sup.9 and R.sup.10 is hydrido; wherein each of R.sup.5 and R.sup.8 is independently selected from hydrido, halo, nitro, trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl, methoxycarbonyl with the proviso that at least one of R.sup.5 and R.sup.8 is an acidic group selected from C02H and tetrazolyl; or a tautomer thereof or a pharmaceutically-aceptable salt thereof. These compositions are particularly useful in treatment or control of hypertension and congestive heart failure.

    摘要翻译： 描述了包含选自一类N-取代的（α-咪唑基 - 甲苯酰基）吡咯化合物的化合物的药物组合物用于治疗循环障碍。 特别感兴趣的组合物包括下式的血管紧张素II拮抗剂化合物其中m是1; 其中R 0选自CH 2 OH，CO 2 H，CHO，CO 2 CH 3，CO 2 C 2 H 5，CH 2 OCH 3，CH 2 OCHOCH 3和CH 2 -CO 2 C 2 H 5; 其中R 1选自Cl，CF 3，CHO，正丁基，氰基，CO 2 CH 3和CO 2 CH 2 CH 3; 其中R2选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，叔丁基，正戊基，异戊基，新戊基，苯基，苄基，苯乙基，环己基，环己基甲基，环己基乙基， ，丁硫基和羟烷基; 其中R3，R4，R6，R7，R9和R10各自为氢; 其中R 5和R 8各自独立地选自氢，卤素，硝基，三氟甲基，羟基，烷氧基，氰基，羧基，甲氧基羰基，条件是R 5和R 8中的至少一个是选自CO 2 H和四唑基的酸性基团; 或其互变异构体或其药学上可接受的盐。 这些组合物特别可用于治疗或控制高血压和充血性心力衰竭。

    N-substituted N-(.alpha.-triazolyl-toluyl)pyrrole compounds for treatment of circulatory disorders
    9.
    发明授权
    N-substituted N-(.alpha.-triazolyl-toluyl)pyrrole compounds for treatment of circulatory disorders 失效
    用于治疗循环障碍的N-取代的N-（α-三唑基 - 甲苯酰基）吡咯化合物

    公开(公告)号：US5484937A

    公开(公告)日：1996-01-16

    申请号：US117269

    申请日：1993-09-07

    申请人： Philippe R. Bovy ,  David B. Reitz ,  Robert E. Manning

    发明人： Philippe R. Bovy ,  David B. Reitz ,  Robert E. Manning

    IPC分类号： C07D521/00 ,  C07D403/10 ,  A61K31/41

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： A class of N-substituted N-(.alpha.-triazolyltoluyl)pyrrole compounds described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein m is one; wherein R.sup.1 is selected from alkyl; and wherein R.sup.2 is selected from alkyl; and wherein each of R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 is independently selected from hydrido, halo, nitro, trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl and methoxycarbonyl; with the proviso that at least one of R.sup.5 and R.sup.8 must be selected from COOH, SH, PO.sub.3 H.sub.2, SO.sub.3 H, CONHNH.sub.2, CONHNHSO.sub.2 CF.sub.3, OH, ##STR2## wherein each of R.sup.42 and R.sup.43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; or a tautomer thereof or a pharmaceutically-acceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.

    摘要翻译： 描述用于治疗循环系统疾病的一类N-取代的N-（α-三唑基甲苯磺酰基）吡咯化合物。 特别感兴趣的化合物是式IMAMA的血管紧张素II拮抗剂，其中m是1; 其中R1选自烷基; 并且其中R 2选自烷基; R 3，R 4，R 5，R 6，R 7，R 8，R 9和R 10各自独立地选自氢，卤素，硝基，三氟甲基，羟基，烷氧基，氰基，羧基和甲氧基羰基; 条件是R 5和R 8中的至少一个必须选自COOH，SH，PO3H2，SO3H，CONHNH2，CONHNHSO2CF3，OH，其中R42和R43各自独立地选自氯，氰基，硝基，三氟甲基， 甲氧基羰基和三氟甲基磺酰基; 或其互变异构体或其药学上可接受的盐。 这些化合物特别可用于治疗或控制高血压和充血性心力衰竭。