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322 条记录 (耗时 0.022 秒)

    Method for preparing 4-methylamino-4-phenylpiperidine
    1.
    发明授权
    Method for preparing 4-methylamino-4-phenylpiperidine 失效
    4-甲基氨基-4-苯基哌啶的制备方法

    公开(公告)号：US06916929B2

    公开(公告)日：2005-07-12

    申请号：US10483475

    申请日：2002-07-15

    申请人： Gilles Anne-Archard ,  Patrick Gros-Claude

    发明人： Gilles Anne-Archard ,  Patrick Gros-Claude

    IPC分类号： C07D211/58

    CPC分类号： C07D211/58

    摘要： The invention relates to a process for preparing a 4-alkoxycarbonylamino-1-benzyl-4-phenylpiperidine of formula (I) via hydrolysis of 1-benzyl-4-cyano-4-phenylpiperidine (II) in acidic medium and treatment of the 1-benzyl-4-phenyl-4-piperidinecarboxamide (III) thus obtained with bromine in the presence of an alkali metal alkoxide. The invention also relates to a process for preparing 4-methylamino-4-phenylpiperidine from compound (II).

    摘要翻译： 本发明涉及通过酸性介质中1-苄基-4-氰基-4-苯基哌啶（II）的水解制备式（I）的4-烷氧基羰基氨基-1-苄基-4-苯基哌啶的方法， - 苄基-4-苯基-4-哌啶甲酰胺（III），由溴在碱金属醇盐存在下得到。 本发明还涉及由化合物（II）制备4-甲基氨基-4-苯基哌啶的方法。

    Phenoxypropanolamines, method for producing them and pharmaceutical compositions containing them
    2.
    发明授权
    Phenoxypropanolamines, method for producing them and pharmaceutical compositions containing them 失效
    苯氧基丙胺胺，其制备方法和含有它们的药物组合物

    公开(公告)号：US06867220B2

    公开(公告)日：2005-03-15

    申请号：US10149497

    申请日：2000-12-14

    申请人： Roberto Cecchi

    发明人： Roberto Cecchi

    IPC分类号： C07D211/26 ,  A61K31/4468 ,  A61K31/451 ,  A61K31/4545 ,  A61P1/00 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10 ,  A61P15/06 ,  A61P25/00 ,  A61P25/24 ,  A61P27/06 ,  C07D211/58 ,  C07D401/04 ,  A61K31/445 ,  C07D401/12

    CPC分类号： C07D401/04 ,  C07D211/58

    摘要： The invention relates to compounds of formula (I) where R1 represents a hydrogen or halogen atom or an —S(O)z—(C1-C4)alkyl, —S(O)z—(C1-C4)R3, —SO2—NH—(C1-C4)alkyl, —NHCO(C1-C4) alkyl, —CO(C1-C4)alkyl or —NHSO2—(C1-C4)alkyl group; m and n independently represent 0, 1 or 2; A represents a group of formula (a) or (b): where X is N or CH; R2 represents an —SO2—R3, —CO—R3 or —CO—(C1-C4)—alkyl group; R3 represents a phenyl group, optionally substituted by a (C1-C4)alkyl or (C1-C4)alkoxy group, one or two halogen atoms or a heterocycle; R4 represents a hydrogen or halogen atom or a (C1-C6)alkyl, (C1-C4)alkoxy, —COOH, —COO(C1-C4)alkyl, —CN, —CONR5R6, —NO2, —NHSO2(C1-C4)alkyl or —SO2NR5R6 group; z is 1 or 2; R5 and R6 independently represent a hydrogen atom or a (C1-C4)alkyl, phenyl or phenyl (C1-C4)alkyl group; and their salts or solvates, to a process for their preparation, to synthetic intermediates and to the pharmaceutical compositions comprising them.

    摘要翻译： 本发明涉及式（I）化合物，其中R 1表示氢或卤素原子或-S（O）z - （C 1 -C 4）烷基，-S（O）z - （C 1 -C 4） NH-（C 1 -C 4）烷基，-NHCO（C 1 -C 4）烷基，-CO（C 1 -C 4）烷基或-NHSO 2 - （C 1 -C 4）烷基; m和n独立地表示0,1或2; A 表示式（a）或（b）的基团：其中X是N或CH; R 2表示-SO 2 -R 3，-CO-R 3或-CO-（C 1 -C 4） - 烷基; R 3表示苯基， 任选地被（C 1 -C 4）烷基或（C 1 -C 4）烷氧基，一个或两个卤素原子或杂环取代; R 4表示氢或卤素原子或（C 1 -C 6）烷基，（C 1 -C 4）烷氧基 ，-COOH，-COO（C1-C4）烷基，-CN，-CONR5R6，-NO2，-NHSO2（C1-C4）烷基或-SO2NR5R6基; z为1或2; R5和R6独立地表示氢原子或 （C 1 -C 4）烷基，苯基或苯基（C 1 -C 4）烷基;及其盐或溶剂合物，其制备方法，合成中间体和包含它们的药物组合物。

    Pharmaceutical microspheres containing valproic acid for oral administration
    5.
    发明申请
    Pharmaceutical microspheres containing valproic acid for oral administration 审中-公开
    用于口服给药的含有丙戊酸的药物微球

    公开(公告)号：US20030157177A1

    公开(公告)日：2003-08-21

    申请号：US10270159

    申请日：2002-10-15

    申请人： Sanofi-Synthelabo, a corporation of France.

    发明人： Christian Langlois ,  Jean-Yves Lanne

    IPC分类号： A61K009/14 ,  A61K031/19

    CPC分类号： A61K31/19 ,  A61K9/1617

    摘要： The subject of the invention is pharmaceutical microspheres containing, as active principle, a mixture of valproic acid and of one of its pharmaceutically acceptable salts in combination with a matrix vehicle selected from glycerol esters, hydrogenated oils, esterified polyethylene glycols, waxes and their mixtures.

    摘要翻译： 本发明的主题是药物微球，其作为活性成分含有丙戊酸及其药学上可接受的盐之一与选自甘油酯，氢化油，酯化聚乙二醇，蜡及其混合物的基质载体的混合物。

    Compositions containing an association of aspirin and an anti-Xz oligosaccharide and use of an anti-Xa oligosaccharide optionally in combination with aspirin
    6.
    发明申请
    Compositions containing an association of aspirin and an anti-Xz oligosaccharide and use of an anti-Xa oligosaccharide optionally in combination with aspirin 审中-公开
    含有阿斯匹林和抗Xz寡糖的组合物的组合物和任选与阿司匹林组合的抗Xa寡糖的用途

    公开(公告)号：US20020160981A1

    公开(公告)日：2002-10-31

    申请号：US10155221

    申请日：2002-05-28

    申请人： Sanofi-Synthelabo

    发明人： Roger Guilcaume Cariou ,  Jacobus Christianus Johannes Stiekema

    IPC分类号： A61K031/737

    CPC分类号： A61K45/06 ,  A61K31/60 ,  A61K31/616 ,  A61K31/737 ,  A61K2300/00

    摘要： The invention relates to the use of a synthetic oligosaccharide which is a selective inhibitor of factor Xa acting via antithrombin III, alone or in association with aspirin, for the preparation of medicaments intended for preventing or treating thromboembolic diseases occurring in a mammal which has undergone a percutaneous transluminal angioplasty. The subject of the invention is moreover pharmaceutical compositions for the treatment or prophylaxy of thromboembolic diseases occurring in a mammal which has undergone a percutaneous transluminal angioplasty, comprising the association of an effective quantity of at least one synthetic oligosaccharide, which is a selective inhibitor of factor Xa acting via antithrombin III, and of an effective quantity of aspirin, optionally mixed with one or more pharmaceutically acceptable excipients.

    摘要翻译： 本发明涉及合成寡糖，其是通过单独或与阿司匹林联合的抗凝血酶III作用的因子Xa的选择性抑制剂，用于制备用于预防或治疗发生在已经经历过的哺乳动物中的血栓栓塞性疾病的药物 经皮腔内血管成形术。 本发明的主题是用于治疗或预防已经经历经皮腔内血管成形术的哺乳动物中的血栓栓塞性疾病的药物组合物，其包含有效量的至少一种合成寡糖的缔合，所述合成寡糖是选择性因子因子 Xa通过抗凝血酶III起作用，并且有效量的阿斯匹林，任选地与一种或多种药学上可接受的赋形剂混合。

    Benzylamine derivatives, their preparation and their application in therapeutics
    9.
    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。