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    Indol-5-yl sulfonamide derivatives, their preparation and their use 5-ht-6 as modulators
    84.
    发明申请
    Indol-5-yl sulfonamide derivatives, their preparation and their use 5-ht-6 as modulators 审中-公开
    吲哚-5-基磺酰胺衍生物，它们的制备及其用途5-ht-6作为调节剂

    公开(公告)号：US20070032520A1

    公开(公告)日：2007-02-08

    申请号：US10566094

    申请日：2004-07-29

    Applicant: Ramon Merce Vidal ,  Xavier Codony Soler ,  Alberto Dordal Zueras

    Inventor： Ramon Merce Vidal ,  Xavier Codony Soler ,  Alberto Dordal Zueras

    IPC: A61K31/4745 ,  A61K31/454 ,  A61K31/405 ,  C07D455/02 ,  C07D403/02

    CPC classification number: C04B35/632 ,  C07D209/08 ,  C07D401/12 ,  C07D409/12 ,  C07D417/12 ,  C07D513/04

    Abstract: The present invention refers to new sulfonamide derivatives, of general formula (1a, 1b, 1c) optionally in form of one of their stereoisomers, preferably enantiomers or diastereomers, their racemate, or in form of a mixture of at least two of their stereoisomers, preferably enantiomers or diastereomers, in any mixing ratio, or their salts, preferably the corresponding, physiologically acceptable salts, or corresponding solvates; to the processes for their preparation, to their application as medicaments in human and/or veterinary therapeutics, and to the pharmaceutical compositions containing them.

    Abstract translation: 本发明涉及通式（1a，1b，1c）的新磺酰胺衍生物，其任选为其立体异构体之一，优选对映异构体或非对映异构体，其外消旋体或其至少两种立体异构体的混合物形式， 优选对映体或非对映体，以任何混合比例，或其盐，优选相应的生理学上可接受的盐或相应的溶剂合物; 其制备方法，作为人和/或兽医治疗剂中的药物的应用，以及含有它们的药物组合物。

    Derivatives of aryl (or heteroaryl) azolylcarbinoles for the treatment of urinary incontinence
    87.
    发明申请
    Derivatives of aryl (or heteroaryl) azolylcarbinoles for the treatment of urinary incontinence 审中-公开
    用于治疗尿失禁的芳基（或杂芳基）唑基甲醇衍生物

    公开(公告)号：US20030022925A1

    公开(公告)日：2003-01-30

    申请号：US10189915

    申请日：2002-07-03

    Applicant: Laboratorios del Dr. Esteve, S.A.

    Inventor： Ramon Merce-Vidal ,  Blas Andaluz-Mataro ,  Jordi Frigola-Constansa

    IPC: A61K031/4196 ,  A61K031/4164 ,  A61K031/415 ,  A61K031/40

    CPC classification number: A61K31/4196 ,  A61K31/40 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4164

    Abstract: Derivatives of aryl(or heteroaryl)azolylcarbinoles of general formula (I), in which Ar represents a phenyl radical or a thienyl radical, optionally substituted, R1 represents a hydrogen atom or a lower alkyl group, R2 represents a dialkylaminoalkyl or azaheterocylclylalkyl and Het represents an azole unsubstituted or optionally substituted by one or two substituents, and their physiologically acceptable salts; are useful as drugs in human and/or veterinary therapeutics to treat urinary incontinence in mammals, including man. 1

    Abstract translation: 其中Ar表示苯基或噻吩基，任意取代的R 1表示氢原子或低级烷基，R 2表示二烷基氨基烷基或氮杂环己基烯基烷基，Het表示芳基（或杂芳基）唑基偶氮衍生物， 未取代或任选被一个或两个取代基取代的唑类及其生理上可接受的盐; 可用作人类和/或兽医治疗药物以治疗哺乳动物（包括人）中的尿失禁。

    Process for the preparation of aryl (or heteroaryl) piperazinylbutylazole derivatives
    89.
    发明授权
    Process for the preparation of aryl (or heteroaryl) piperazinylbutylazole derivatives 失效
    制备亚芳基（或杂芳基）哌嗪基吡唑衍生物的方法

    公开(公告)号：US5227486A

    公开(公告)日：1993-07-13

    申请号：US847625

    申请日：1992-03-06

    Applicant: Ramon Merce-Vidal ,  Jordi Frigola-Constansa ,  Juan Pares-Corominas

    Inventor： Ramon Merce-Vidal ,  Jordi Frigola-Constansa ,  Juan Pares-Corominas

    IPC: A61K31/40 ,  A61K31/435 ,  A61K31/495 ,  A61K31/496 ,  A61K31/505 ,  A61P9/12 ,  A61P25/00 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  C07D207/32 ,  C07D207/325 ,  C07D231/12 ,  C07D231/16 ,  C07D231/20 ,  C07D231/38 ,  C07D231/56 ,  C07D233/61 ,  C07D233/68 ,  C07D239/26 ,  C07D241/04 ,  C07D277/64 ,  C07D403/12 ,  C07D403/14 ,  C07D417/12 ,  C07D471/04 ,  C07D521/00

    CPC classification number: C07D207/325 ,  C07D231/12 ,  C07D231/16 ,  C07D233/56 ,  C07D233/68 ,  C07D249/08 ,  C07D403/12 ,  C07D403/14 ,  C07D417/12 ,  C07D471/04

    Abstract: The present invention relates to a process for the preparation of aryl (or heteroaryl) piperazinyl-butylazole derivatives corresponding to the general formula I ##STR1## in which Ar denotes a nitrogenous or other aromatic radical chosen from differently substituted aryls, differently substituted 2-pyrimidine, 2-N-methyl-imidazole and 3-(1,2-benzisothiazole)Z.sub.1 denotes a nitrogen atom or an optionally substituted carbon atom which may be denoted by: C-R.sub.1Z.sub.2 denotes a nitrogen atom or an optionally substituted carbon atom which may be denoted by: C-R.sub.2Z.sub.4 denotes a nitrogen atom or an optionally substituted carbon atom which may be denoted by: C-R.sub.4 and R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which are identical or different and may also form a part of another ring, aromatic or otherwise, denote a hydrogen atom, a halogen, a lower alkyl radical, a nitro radical, a hydroxyl radical, an alkoxy radical, a cyano radical, a carboxylic radical, a carboxamido radical, an alkylcarboxylate radical, an aryl or substituted aryl radical, a sulfonic radical, a sulfonamido radical optionally substituted on the amino group or an amino or substituted amino radicalwherein ##STR2## in which Ar has the meanings referred to above and X denotes a halogen atom, is reacted with a compound of general formula III ##STR3## in which Z.sub.1, Z.sub.2, Z.sub.4 and R.sub.3 have the meanings referred to above.

    Abstract translation: 本发明涉及一种制备相应于通式I（I）的芳基（或杂芳基）哌嗪基 - 丁唑衍生物的方法，其中Ar表示选自不同取代的芳基的含氮或其它芳族基团， 2-嘧啶，2-N-甲基咪唑和3-（1,2-苯并异噻唑）Z1表示氮原子或任选取代的碳原子，可以用以下表示：C-R 1 Z 2表示氮原子或任选取代的 碳原子，其可以由以下表示：C-R 2 Z 4表示氮原子或任选取代的碳原子，其可以由以下表示：C-R 4和R 1，R 2，R 3和R 4，其相同或不同，并且也可以形成 另一个芳环或其它环的一部分表示氢原子，卤素，低级烷基，硝基，羟基，烷氧基，氰基，羧基，甲酰胺基，烷基羧酸根， 芳基或取代基 在氨基或氨基或取代的氨基上任选取代的磺酰基，磺酰氨基，其中Ar具有上述含义，X表示卤素原子的氨基或取代的氨基，与其反应，与 其中Z1，Z2，Z4和R3具有上述含义的通式III的化合物（III）。

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