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    Phenothiazine derivatives, their preparation and pharmaceutical compositions containing them
    5.
    发明授权
    Phenothiazine derivatives, their preparation and pharmaceutical compositions containing them 失效
    吩噻嗪衍生物，其制备方法和含有它们的药物组合物

    公开(公告)号：US5321026A

    公开(公告)日：1994-06-14

    申请号：US825753

    申请日：1992-01-27

    申请人： Claude Garret ,  Claude Guyon ,  Bernard Plau ,  Gerard Taurand

    发明人： Claude Garret ,  Claude Guyon ,  Bernard Plau ,  Gerard Taurand

    IPC分类号： A61K31/00 ,  A61K31/54 ,  A61P25/04 ,  A61P25/20 ,  C07D279/28 ,  C07D417/06

    CPC分类号： C07D279/28

    摘要： New phenothiazine derivatives of general formula (I) in whichR represents 4- to 6-membered cycloalkyl, or represents --CH.sub.2 R" in which R" is hydrogen, alkyl containing 1 to 5 carbon atoms, alkenyl or alkynyl containing 2 to 4 carbon atoms, cycloalkyl (3- to 6-membered), phenyl, optionally substituted (with 1 or 2 halogen atoms or with a hydroxyl, alkyl, alkyloxy, trifluoromethyl or nitro radical) or heterocyclic selected from furyl, thienyl or pyridyl, andR' either represents a radical of general formula (IIa) in which R.sub.1 and R.sub.2, which may be identical or different, are alkyl, cycloalkylalkyl, hydroxyalkyl or acetyloxyalkyl or, together with the nitrogen atom to which they are attached, form a saturated or partially unsaturated 4- to 7-membered heterocycle optionally substituted with 1 or 2 alkyl, hydroxyalkyl or acetyloxyalkyl radicals, andR.sub.3 is phenethyl or alkyl optionally substituted with cycloalkyl (3 to 6 carbons) or benzoyl, or represents a radical of general formula (IIb) in which R.sub.1 and R.sub.2 are defined as above.The new products are useful as antispasmodics. ##STR1##

    摘要翻译： 通式（I）的新吩噻嗪衍生物，其中R表示4-至6-元环烷基，或表示其中R“为氢的-CH 2 R”，含有1至5个碳原子的烷基，含有2至4个碳原子的烯基或炔基 碳原子，环烷基（3-至6-元），苯基，任选取代的（具有1或2个卤素原子或与羟基，烷基，烷氧基，三氟甲基或硝基）或选自呋喃基，噻吩基或吡啶基的杂环，R “表示通式（IIa）的基团，其中可以相同或不同的R 1和R 2是烷基，环烷基烷基，羟基烷基或乙酰氧基烷基，或者与它们连接的氮原子一起形成饱和或部分 任选被1或2个烷基，羟基烷基或乙酰氧基烷基取代的不饱和4-至7-元杂环，R 3为任选被环烷基（3-6个碳）或苯甲酰基取代的苯乙基或烷基，或表示通式（IIb）的基团， 在 其中R1和R2如上定义。 新产品可用作解痉药。 （I）（IIa）（IIb）

    2-aminothiazoline derivatives and process for preparing the same
    6.
    发明授权
    2-aminothiazoline derivatives and process for preparing the same 失效
    2-氨基噻唑啉衍生物及其制备方法

    公开(公告)号：US06699895B2

    公开(公告)日：2004-03-02

    申请号：US10159498

    申请日：2002-05-31

    申请人： Jean-Christophe Carry ,  Dominique Damour ,  Claude Guyon ,  Serge Mignani ,  Antony Bigot ,  Eric Bacque ,  Michel Tabart

    发明人： Jean-Christophe Carry ,  Dominique Damour ,  Claude Guyon ,  Serge Mignani ,  Antony Bigot ,  Eric Bacque ,  Michel Tabart

    IPC分类号： C07D41706

    CPC分类号： C07D417/06 ,  A61K31/426 ,  A61K31/4439 ,  C07D277/18

    摘要： The present invention relates to a class of 2-aminothiazoline derivatives of formula I: in which either R1 is a hydrogen atom or an alkyl radical and R2 is an alkyl, -alk-NH2, —CH2—R3, —CH2—S—R4 or phenyl radical substituted with a nitro or —NH—C(═NH)CH3 radical, or R1 is an alkyl radical and R2 is a hydrogen atom, R3 is a (3-6C) cycloalkyl, pyridyl, pyridyl N-oxide, thienyl, thiazolyl, imidazolyl, pyrazinyl, triazolyl or phenyl radical or a phenyl radical substituted with a nitro, hydroxy or carboxyl radical, R4 represents a pyridyl or pyridyl N-oxide radical, alk represents an alkylene radical, or pharmaceutically acceptable salts thereof, which are useful as inhibitors of inducible NO-synthase.

    摘要翻译： 本发明涉及一类式I的2-氨基噻唑啉衍生物：其中R1是氢原子或烷基，R2是烷基，-alk-NH2，-CH2-R3，-CH2-S-R4 或被硝基或-NH-C（= NH）CH 3基团取代的苯基，或R 1是烷基，R 2是氢原子，R 3是（3-6C）环烷基，吡啶基，吡啶基N-氧化物，噻吩基 ，噻唑基，咪唑基，吡嗪基，三唑基或苯基或被硝基，羟基或羧基取代的苯基，R4表示吡啶基或吡啶基N-氧化物基，alk表示亚烷基或其药学上可接受的盐，它们是 可用作诱导型NO合成酶的抑制剂。

    Analgesic phenothiazine derivatives
    8.
    发明授权
    Analgesic phenothiazine derivatives 失效
    镇痛吩噻嗪衍生物

    公开(公告)号：US5049669A

    公开(公告)日：1991-09-17

    申请号：US364155

    申请日：1989-06-12

    申请人： Claude Garret ,  Claude Guyon ,  Bernard Plau ,  Gerard Taurand

    发明人： Claude Garret ,  Claude Guyon ,  Bernard Plau ,  Gerard Taurand

    IPC分类号： A61K31/00 ,  A61K31/54 ,  A61K31/5415 ,  A61P7/10 ,  A61P25/04 ,  C07D279/28

    CPC分类号： C07D279/28

    摘要： Phenothiazine derivatives of general formula (I), in which R is a linear or branched (1 to 6 C) alkyl radical and R.sub.1 and R.sub.2, which may be identical or different, are linear or branched (1 to 4 C) alkyl radicals or form, with the nitrogen atom to which they are attached, a 4- to 7-membered heterocycle, their isomeric forms and mixtures thereof as well as their addition salts with acids, possess analgesic and diuretic activity. ##STR1##

    摘要翻译： 其中R为直链或支链（1至6个C）烷基的通式（I）的吩噻嗪衍生物，R 1和R 2可以相同或不同，为直链或支链（1-4个碳）烷基或 与它们所连接的氮原子一起形成4-至7-元杂环，其异构形式及其混合物以及它们与酸的加成盐，具有止痛和利尿活性。 （一）