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    USE OF 2-AMINO-THIAZOLINE DERIVATIVES AS INHIBITORS OF INDUCIBLE NO-SYNTHASE
    71.
    发明申请
    USE OF 2-AMINO-THIAZOLINE DERIVATIVES AS INHIBITORS OF INDUCIBLE NO-SYNTHASE 审中-公开
    作为可诱导的非合成酶抑制剂的2-氨基 - 噻唑啉衍生物的使用

    公开(公告)号：US20070203337A1

    公开(公告)日：2007-08-30

    申请号：US11742048

    申请日：2007-04-30

    申请人： Antony BIGOT ,  Jean-Christophe CARRY ,  Serge MIGNANI

    发明人： Antony BIGOT ,  Jean-Christophe CARRY ,  Serge MIGNANI

    IPC分类号： C07D241/04 ,  C07D279/12

    CPC分类号： C07D295/13 ,  C07D241/04 ,  C07D277/18 ,  C07D295/15 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

    摘要： The present invention relates to a process for preparing 2-amino-thiazoline derivatives of formula (II): in which either Y is a methylene (CH2) and X is chosen from the following groups: O, NH, (C1-C4) N-Alkyl, N-Bn, N-Ph, N-(2-Py), N-(3-Py), N-(4-Py), N-2-pyrimidyl, N-5-pyrimidyl, S, SO, SO2, CH2 or CHPh; or Y is a carbonyl (C═O) and X is chosen from the following groups: NH, N-Ph, N-(2-Py), N-(3-Py), N-(4-Py), N-2-pyrimidyl or N-5-pyrimidyl.

    摘要翻译： 本发明涉及制备式（II）的2-氨基 - 噻唑啉衍生物的方法：其中Y是亚甲基（CH 2 CH 2），X选自下列基团：O， NH，（C 1 -C 4）N-烷基，N-Bn，N-Ph，N-（2-Py），N-（3-Py），N-（4-Py），N-2-嘧啶基，N -5-嘧啶基，S，SO，SO 2，CH 2或CHPh; 或者Y是羰基（CO），X选自下列基团：NH，N-Ph，N-（2-Py），N-（3-Py），N-（4-Py），N-2 - 嘧啶基或N-5-嘧啶基。

    Quinolylpropylpiperidine derivatives, preparation process and intermediates, and compositions including them
    76.
    发明授权
    Quinolylpropylpiperidine derivatives, preparation process and intermediates, and compositions including them 失效
    醌基丙基哌啶衍生物，制备方法和中间体，以及包括它们的组合物

    公开(公告)号：US06806277B2

    公开(公告)日：2004-10-19

    申请号：US10622655

    申请日：2003-07-18

    申请人： Eric Bacqué ,  Jean-Luc Malleron ,  Serge Mignani ,  Michel Tabart

    发明人： Eric Bacqué ,  Jean-Luc Malleron ,  Serge Mignani ,  Michel Tabart

    IPC分类号： A61K3147

    CPC分类号： C07D401/06 ,  C07D409/12

    摘要： Quinolylpropylpiperidine derivatives of general formula (I) in which: R1 is NH2, alkylamino, dialkylamino, hydroxyamino, alkyl(alkyloxy)amino or alkyloxyamino, R2 is a carboxyl, carboxymethyl or hydroxymethyl radical, R3 is alkyl (1 to 6C) substituted by phenylthio which can itself carry 1 to 3 substituents selected from halogen, OH, alkyl, alkyloxy, CF3, OCF3, COOH, alkyloxycarbonyl, CN and NH2, by cycloalkylthio (3 to 7 members) or by heteroarylthio (5 to 6 members) comprising 1 to 4 heteroatoms selected from N, S and O and optionally itself substituted [by halogen, OH, alkyl, alkyloxy, CF3, OCF3, ═O, COOH, alkyloxycarbonyl, CN or NH2] or R3 is propargyl substituted by phenyl which can itself carry 1 to 3 substituents selected from halogen, OH, alkyl, alkyloxy, CF3, OCF3, COOH, alkyloxycarbonyl, CN and NH2 or substituted by cycloalkyl comprising 3 to 7 members or substituted by 5- to 6-membered heteroaryl comprising 1 to 4 heteroatoms chosen from N, O or S and optionally itself substituted by halogen, OH, alkyl, alkyloxy, CF3, OCF3, ═O, COOH, alkyloxycarbonyl, CN or NH2, and R4 is alkyl (1 to 6C), alkenyl-CH2—, alkynyl-CH2— (3 to 7C), cycloalkyl or (cycloalkyl)alkyl, in their diastereoisomeric forms or their mixtures, and their pharmaceutically acceptable salts. These novel derivatives are particularly advantageous antimicrobial agents.

    摘要翻译： 通式（I）的喹啉基丙基哌啶衍生物，其中：R1是NH2，烷基氨基，二烷基氨基，羟基氨基，烷基（烷氧基）氨基或烷氧基氨基，R2是羧基，羧甲基或羟甲基，R3是被苯硫基取代的（1-6） 其可以自身携带1至3个选自卤素，OH，烷基，烷氧基，CF 3，OCF 3，COOH，烷氧基羰基，CN和NH 2的取代基，被环烷硫基（3至7个成员）或通过杂芳硫基（5至6个成员）包含1至 4个选自N，S和O的杂原子，并且任选地本身被[由卤素，OH，烷基，烷氧基，CF 3，OCF 3，= O，COOH，烷氧基羰基，CN或NH 2]取代的R 3或被苯基取代的苯基， 被选自卤素，OH，烷基，烷氧基，CF 3，OCF 3，COOH，烷氧基羰基，CN和NH 2的3个取代基，或被包含3至7个成员的环烷基或被包含1至4个选自 N，O或S，以及任选的其自身取代基 CN，NH 2，R 4是烷基（1-6），链烯基-CH 2 - ，炔基-CH 2 - （3至7C），环烷基（C 1 -C 6）烷基，烷氧基羰基， 或（环烷基）烷基，其非对映异构体形式或其混合物及其药学上可接受的盐。这些新型衍生物是特别有利的抗微生物剂。

    Polyhydroxyalkylpyrazine derivatives, their preparation and the medicaments comprising them
    79.
    发明授权
    Polyhydroxyalkylpyrazine derivatives, their preparation and the medicaments comprising them 有权
    聚羟基烷基吡嗪衍生物，其制备方法和包含它们的药物

    公开(公告)号：US06362185B1

    公开(公告)日：2002-03-26

    申请号：US09483939

    申请日：2000-01-14

    申请人： Georges Bashiardes ,  Jean-Christophe Carry ,  Michel Evers ,  Bruno Filoche ,  Serge Mignani

    发明人： Georges Bashiardes ,  Jean-Christophe Carry ,  Michel Evers ,  Bruno Filoche ,  Serge Mignani

    IPC分类号： A61K314965

    CPC分类号： A61K31/495 ,  C07D241/12

    摘要： The present invention relates to medicaments comprising at least one compound of formula: wherein either R1 represents a —CH(Ra)—CHOH—CHOH—CH2OH chain and R2 represents a —CH2—CHOH—CHOH—CH2OH chain, or R1 represents a —CHOH—CHF—CHOH—CH2OH chain and R2 represents a —CH2—CHF—CHOH—CH2OH chain, or R1 represents a —CHOH—CHOH—CHOH—Rb chain and R2 represents a —CH2—CHOH—CHOH—Rb chain, or R1 represents a —CH2—CHOH—CHOH—CH2OH chain and R2 represents a —CH2—CHOH—CHOH—CH2OH chain, or R1 and R2 are identical and each represent a —(CHOH)n—CH2OH chain in which n is equal to 1, 2, 3 or 4, Ra represents an alkoxy radical (1-6 C in a straight or branched chain) or a fluorine atom, and Rb represents a carboxyl, —CO—NH2 or —CH2—NH2 radical, or one of their stereoisomers or their salts with an inorganic or organic acid, to novel compounds of formula (I) and to their preparation.

    摘要翻译： 本发明涉及包含至少一种下式的化合物的药物：其中R1表示-CH（Ra）-CHOH-CHOH-CH2OH链，R2表示-CH2-CHOH-CHOH-CH2OH链，或R1表示-CHOH- CHF-CHOH-CH2OH链，R2表示-CH2-CHF-CHOH-CH2OH链，或R1表示-CHOH-CHOH-CHOH-Rb链，R2表示-CH2-CHOH-CHOH-Rb链，或R1表示 -CH 2 -CHOH-CHOH-CH 2 OH链，R 2表示-CH 2 -CHOH-CHOH-CH 2 OH链，或R 1和R 2相同，各自表示其中n等于1的 - （CHOH）n -CH 2 OH链， 2,3或4中，Ra表示烷氧基（直链或支链中1-6C）或氟原子，Rb表示羧基，-CO-NH2或-CH2-NH2基，或其立体异构体或 它们与无机或有机酸的盐，与式（I）的新型化合物及其制备。