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    New derivatives of echinocandine, their preparation process and their use as antifungals
    1.
    发明申请
    New derivatives of echinocandine, their preparation process and their use as antifungals 失效
    棘皮菌素的新衍生物，其制备方法及其作为抗真菌剂的用途

    公开(公告)号：US20060035820A1

    公开(公告)日：2006-02-16

    申请号：US11225627

    申请日：2005-09-13

    申请人： Patrick Fauveau ,  Stephen Hawser ,  Gilles Lebourg ,  Laurent Schio

    发明人： Patrick Fauveau ,  Stephen Hawser ,  Gilles Lebourg ,  Laurent Schio

    IPC分类号： A61K38/12 ,  C07K5/12

    CPC分类号： C07K7/56 ,  A61K38/00 ,  Y10S930/27

    摘要： A subject of the invention, in all possible isomer forms as well as their mixtures, is the compounds of formula (I): in which either R1: H or CH3 and R2: cyclohexyl substituted by an amine, a (CH2)b—C≡N radical or R1 and R2 together with the nitrogen which carries-them form a ring with 3, 4 or 5 carbons optionally substituted by an amine R3: hydrogen, methyl or hydroxyl R4: hydrogen or hydroxyl R: represents a linear,. branched or cyclic chain T: hydrogen, methyl, CH2CONH2, CH2C≡N, a (CH2)2NH2 or (CH2)2Nalk+X− radical, X halogen and alk alkyl Y: hydrogen, hydroxyl, halogen or OSO3H, W: H or OH, Z: H, CH3. The compounds of formula (I) have antifungal properties.

    摘要翻译： 本发明的所有可能的异构体形式以及它们的混合物的主题是式（I）的化合物：其中R 1，H或CH 3 和R 2：被胺取代的环己基，（CH 2 H 2）bC≡N基或R 1和R 2， / SUB与携带它们的氮形成具有3,4或5个碳原子的环，任选被胺R 3取代：氢，甲基或羟基R 4， 氢或羟基R：代表线性。 支链或环状链T：氢，甲基，CH 2 CONH 2，CH 2C≡N，a（CH 2） / SUB 2）或（CH 2）2 N 2 O 2 N 2 O 2 N 2 N 2 O 2 X，卤素和烷基Y：氢，羟基，卤素或OSO 3 H，W：H或OH，Z：H，CH 3 。 式（I）化合物具有抗真菌性质。

    1-pyrazolo[4,3-c]isoquinoline derivatives, preparation thereof and therapeutic use thereof
    2.
    发明授权
    1-pyrazolo[4,3-c]isoquinoline derivatives, preparation thereof and therapeutic use thereof 有权
    1-吡唑并[4,3-c]异喹啉衍生物，其制备及其治疗用途

    公开(公告)号：US08461175B2

    公开(公告)日：2013-06-11

    申请号：US13265981

    申请日：2010-04-22

    申请人： Georges Delettre ,  Stéphanie Deprets ,  Frank Halley ,  Laurent Schio ,  Fabienne Thompson

    发明人： Georges Delettre ,  Stéphanie Deprets ,  Frank Halley ,  Laurent Schio ,  Fabienne Thompson

    IPC分类号： C07D471/04 ,  A61K31/4745 ,  A61P35/00

    CPC分类号： C07D471/04

    摘要： The invention relates to a compound of formula (I), where: R1 is a phenyl group optionally substituted by one or more halogen atoms; R2 is: a hydrogen atom or a halogen atom or a cyano group; a —C(═O)Y group where Y is a hydrogen atom, or a —NH2 or —OR3 group; a —C(═S)NH2 group; a —C(═NH)NH—OH group; a —CH2OH or —CH2F group; a —CH═N—OH group; a —CH═CH2 or —C═C—R3 group; a H or H R1 group being a hydrogen or (C1-C4)alkyl group; R3 is a hydrogen atom or (C1-C4)alkyl group; and R4 is a —NH2, (C1-C4)alkyl, (C1-C4)fluoroalkyl or (C3-C7)cycloalkyl group.

    摘要翻译： 本发明涉及式（I）化合物，其中：R 1是任选被一个或多个卤素原子取代的苯基; R2是：氢原子或卤素原子或氰基; Y为氢原子的-C（= O）Y基团，或-NH2或-OR3基团; -C（= S）NH 2基团; -C（= NH）NH-OH基团; -CH 2 OH或-CH 2 F基团; -CH = N-OH基团; -CH = CH 2或-C = C-R 3基团; H或H R 1基团为氢或（C 1 -C 4）烷基; R3是氢原子或（C1-C4）烷基; 并且R 4是-NH 2，（C 1 -C 4）烷基，（C 1 -C 4）氟烷基或（C 3 -C 7）环烷基。

    Echinocandin derivatives, method for preparing same and application as antifungal agents
    4.
    发明授权
    Echinocandin derivatives, method for preparing same and application as antifungal agents 失效
    棘白菌素衍生物，其制备方法和作为抗真菌剂的应用

    公开(公告)号：US07022669B1

    公开(公告)日：2006-04-04

    申请号：US10018073

    申请日：2000-06-08

    申请人： Patrick Fauveau ,  Stephen Hawser ,  Gilles Lebourg ,  Laurent Schio

    发明人： Patrick Fauveau ,  Stephen Hawser ,  Gilles Lebourg ,  Laurent Schio

    IPC分类号： A61K38/12

    CPC分类号： C07K7/56 ,  A61K38/00 ,  Y10S930/27

    摘要： A subject of the invention, in all possible isomer forms as well as their mixtures, is the compounds of formula (I): in which either R1: H or CH3 and R2: cyclohexyl substituted by an amine, a (CH2)b-C≡N radical or R1 and R2 together with the nitrogen which carries them form a ring with 3, 4 or 5 carbons optionally substituted by an amine R3: hydrogen, methyl or hydroxyl R4: hydrogen or hydroxyl R: represents a linear, branched or cyclic chain T: hydrogen, methyl, CH2CONH2, CH2C≡N, a (CH2)2NH2 or (CH2)2Nalk+X− radical, X halogen and alk alkyl Y: hydrogen, hydroxyl, halogen or OSO3H, W: H or OH, Z: H, CH3. The compounds of formula (I) have antifungal properties.

    摘要翻译： 本发明的所有可能的异构体形式以及它们的混合物的主题是式（I）的化合物：其中R 1，H或CH 3 和R 2：被胺取代的环己基，（CH 2 H 2）bC≡N基或R 1和R 2， / SUB与携带它们的氮一起形成具有3,4或5个碳原子的环，任选被胺R 3取代：氢，甲基或羟基R 4： 氢或羟基R：表示直链，支链或环状的链T：氢，甲基，CH 2 CONH 2，CH 2C≡N （CH 2）2 NH 2或（CH 2 CH 2）2，或（CH 2）2 卤素，烷基Y：氢，羟基，卤素或OSO 3 H，W：H或OH， Z：H，CH 3。 式（I）的化合物具有抗真菌性质。