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    HSP90 inhibitory carbazole derivatives, compositions containing same and use thereof
    1.
    发明授权
    HSP90 inhibitory carbazole derivatives, compositions containing same and use thereof 有权
    HSP90抑制性咔唑衍生物，含有该组合物的组合物及其应用

    公开(公告)号：US08309721B2

    公开(公告)日：2012-11-13

    申请号：US12881414

    申请日：2010-09-14

    申请人： Jean-Marie Ruxer ,  Victor Certal ,  Marcel Alasia ,  Luc Bertin ,  Herve Minoux ,  Patrick Mailliet ,  Frank Halley ,  Maria Mendez-Perez

    发明人： Jean-Marie Ruxer ,  Victor Certal ,  Marcel Alasia ,  Luc Bertin ,  Herve Minoux ,  Patrick Mailliet ,  Frank Halley ,  Maria Mendez-Perez

    IPC分类号： C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D413/14 ,  C07D471/04

    CPC分类号： C07D403/04 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D451/04 ,  C07D453/00 ,  C07D471/04 ,  C07D493/08

    摘要： The invention relates to the novel substances in Formula (I): wherein Het is a heterocycle optionally substituted by one or a plurality of radicals R1 or R′1; R is selected from the group comprising Formula (A′), (B), (C), (D), or (E), with R1 and/or R′1 selected from H, halogen, CF3, nitro, cyano, alkyl, hydroxyl, mercapto, amino, alkylamino, dialkylamino, alkoxy, phenylalcoxy, alkylhio, or carboxy that is free or esterified by an alkyl, carboxamide, CO—NH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—S02-alkyl, S(0)2-NHalkyl, or S(02)-N(alkyl)2 radical; all these radicals are optionally substituted; W1, W2, and W3 independently are CH or N; X is 0, S, NR2, C(O), S(O), or S(0)2; Z is optionally substituted H, Hal, -0-R2 or —NH—R2 with R2 being H, alkyl, cycloalkyl, or heterocycloalkyl; and these substances are all isomeric forms and salts thereof, used as drugs.

    摘要翻译： 本发明涉及式（I）中的新物质：其中Het是任选被一个或多个基团R 1或R 11取代的杂环; R选自式（A'），（B），（C），（D）或（E）中的R 1和/或R 1选自H，卤素，CF 3，硝基，氰基， 烷基，羟基，巯基，氨基，烷基氨基，二烷基氨基，烷氧基，苯基氧基，烷基或羧基，它们被烷基，甲酰胺，CO-NH（烷基），CON（烷基）2，NH-CO-烷基， 磺酰胺，NH-SO 2 - 烷基，S（O）2 -NH烷基或S（O 2）-N（烷基）2基团; 所有这些基团任选被取代; W1，W2和W3独立地为CH或N; X为0，S，NR2，C（O），S（O）或S（0）2; Z是任选取代的H，Hal，-O-R 2或-NH-R 2，其中R 2是H，烷基，环烷基或杂环烷基; 并且这些物质都是用作药物的异构形式及其盐。

    HSP90 INHIBITING INDAZOLE DERIVATIVES, COMPOSITIONS CONTAINING SAME AND USE THEREOF
    3.
    发明申请
    HSP90 INHIBITING INDAZOLE DERIVATIVES, COMPOSITIONS CONTAINING SAME AND USE THEREOF 审中-公开
    HSP90抑制吲哚衍生物，其组合物及其用途

    公开(公告)号：US20120010241A1

    公开(公告)日：2012-01-12

    申请号：US13257516

    申请日：2010-03-18

    申请人： Luc Bertin ,  Jean-Christophe Carry ,  Patrick Mailliet ,  Herve Minoux ,  Fabienne Pilorge ,  Jean-Marie Ruxer

    发明人： Luc Bertin ,  Jean-Christophe Carry ,  Patrick Mailliet ,  Herve Minoux ,  Fabienne Pilorge ,  Jean-Marie Ruxer

    IPC分类号： A61K31/4709 ,  A61P35/00 ,  A61K31/4184 ,  C07D401/10 ,  C07D403/10

    CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D407/14 ,  C07D493/08

    摘要： The invention relates to novel products having formula (I), wherein: R4 represents H, CH3, CH2CH3, CF3, F, Cl, Br, I; Het represents a heterocycle optionally substituted by one or more R1 or R′1 radicals selected from H, halogen, CF3, nitro, cyano, alkyl, hydroxy, mercapto, amino, alkylamino, dialkylamino, alkoxy, phenylalkoxy, alkylthio, carboxy that is free or sterified with an alkyl radical, carboxamide, CO—NH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—SO2-alkyl, S(O)2-NHalkyl, S(O2)-N(alkyl)2, all of the alkyl, alkoxy and alkylthio radicals being optionally substituted; R being selected from the group comprising (A′), (B), (C), (D) and (F), wherein W1, W2, W3 represent independently CH or N, X represents O, S, NR2, C(O), S(O) or S(O)2; V represents H, Hal, —O—R2 or —NH—R2 with R2 representing H, alkyl, cycloalkyl or heterocycloalkyl, optionally substituted; said products being in all isomer forms, as well as the salts and intended for use as drugs.

    摘要翻译： 本发明涉及具有式（I）的新产物，其中：R 4表示H，CH 3，CH 2 CH 3，CF 3，F，Cl，Br，I; Het表示任选地被一个或多个选自H，卤素，CF 3，硝基，氰基，烷基，羟基，巯基，氨基，烷基氨基，二烷基氨基，烷氧基，苯基烷氧基，烷硫基，烷硫基，R 1或R' 或烷基，羧酰胺，CO-NH（烷基），CON（烷基）2，NH-CO-烷基，磺酰胺，NH-SO 2 - 烷基，S（O）2 -NH烷基，S（O 2） （烷基）2，所有烷基，烷氧基和烷硫基任选被取代; R选自包含（A'），（B），（C），（D）和（F）的基团，其中W 1，W 2，W 3独立地表示CH或N，X表示O，S，NR 2，C（ O），S（O）或S（O）2; V代表H，Hal，-O-R2或-NH-R2，其中R2表示H，烷基，环烷基或杂环烷基，任选取代; 所述产物为所有异构体形式，以及所述盐并且用作药物。

    NOVEL DERIVATIVES OF PYRROLOINDOLE WHICH ARE INHIBITORS OF HSP90, COMPOSITIONS CONTAINING SAME, AND USE THEREOF
    5.
    发明申请
    NOVEL DERIVATIVES OF PYRROLOINDOLE WHICH ARE INHIBITORS OF HSP90, COMPOSITIONS CONTAINING SAME, AND USE THEREOF 有权
    作为HSP90的抑制剂的吡咯烷的新型衍生物，其组合物及其用途

    公开(公告)号：US20110184015A1

    公开(公告)日：2011-07-28

    申请号：US12970458

    申请日：2010-12-16

    申请人： Marcel Alasia ,  Hervé Minoux ,  Jean-Marie Ruxer

    发明人： Marcel Alasia ,  Hervé Minoux ,  Jean-Marie Ruxer

    IPC分类号： A61K31/437 ,  C07D471/04 ,  A61P25/16 ,  A61P25/28 ,  A61P31/12 ,  A61P27/02 ,  A61P17/06 ,  A61P13/00 ,  A61P35/00

    CPC分类号： C07D519/00 ,  A61K31/13 ,  Y02A50/385 ,  Y02A50/411

    摘要： Pyrroloindoles of formula (I) are provided wherein Het is an aromatic or partially unsaturated, monocyclic or bicyclic heterocycle containing between 1 and 4 heteroatoms N, O or S, optionally substituted by R1 or R′1 which are the same or different; R is X-(A-B)n-CONH2, X-(A-B)n-O—CONH2, X-(A-B)n-NH—CONH2, X—(CH2)m-heterocycloalkyl, X(CH2)m-aryl and X—(CH2)m-heteroaryl wherein X is —O—C(O), —NH—C(O), NH—CS, —NH—CO—CH2-O—; —NH—COCH2-S—CH2-CO—NH—; —NH—CO—(CH2)2-SO2-; and —NH—CO—CH2-N(CH3)-CO—; A and B are the same or different and are each independently a single bond, CH2, CH-alkyl, and CH-aralkyl; n=1,2 and m=0, 1; R1 and/or R′1 are H, halogen, CF3, nitro, cyano, alkyle, hydroxy, mercapto, amino, alkylamino, dialkylamino, alkoxy, alkylthio, and carboxy, free or esterified by an alkyl, carboxamide, CONH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—SO2-alkyl, S(O)2-NHalkyl, and S(O2)-N(alkyl)2 group, all of said alkyl, alcoxy and alkylthio groups being optionally substituted themselves, said products being in all isomer forms and salts, as medicaments.

    摘要翻译： 提供式（I）的吡咯并吲哚，其中Het是含有1至4个杂原子N，O或S的芳族或部分不饱和的单环或双环杂环，任选被相同或不同的R1或R'1取代; R是X-（AB）n-CONH 2，X-（AB）n O-CONH 2，X-（AB）n -NH-CONH 2，X-（CH 2）m-杂环烷基， （CH 2）m - 杂芳基，其中X是-O-C（O），-NH-C（O），NH-CS，-NH-CO-CH 2 -O- -NH-COCH 2 -S-CH 2 -CO-NH-; -NH-CO-（CH 2）2 -SO 2 - ; 和-NH-CO-CH 2 -N（CH 3）-CO-; A和B相同或不同，各自独立地为单键，CH 2，CH-烷基和CH-芳烷基; n = 1,2和m = 0,1; R 1和/或R'1是烷基，羧酰胺，CONH（烷基）烷基，C 1 -C 6烷基，C 1 -C 6烷基， ，CON（烷基）2，NH-CO-烷基，磺酰胺，NH-SO 2 - 烷基，S（O）2 -NH烷基和S（O 2）-N（烷基）2基团，所有烷基，烷氧基和烷硫基 基团任选地被取代，所述产物是所有异构体形式和盐，作为药物。

    Derivatives of pyrroloindole which are inhibitors of Hsp90, compositions containing same, and use thereof
    6.
    发明授权
    Derivatives of pyrroloindole which are inhibitors of Hsp90, compositions containing same, and use thereof 有权
    作为Hsp90抑制剂的吡咯并吲哚的衍生物，含有它们的组合物及其用途

    公开(公告)号：US08178687B2

    公开(公告)日：2012-05-15

    申请号：US12970458

    申请日：2010-12-16

    申请人： Marcel Alasia ,  Hervé Minoux ,  Jean-Marie Ruxer

    发明人： Marcel Alasia ,  Hervé Minoux ,  Jean-Marie Ruxer

    IPC分类号： C07D215/38

    CPC分类号： C07D519/00 ,  A61K31/13 ,  Y02A50/385 ,  Y02A50/411

    摘要： Pyrroloindoles of formula (I) are provided wherein Het is an aromatic or partially unsaturated, monocyclic or bicyclic heterocycle containing between 1 and 4 heteroatoms N, O or S, optionally substituted by R1 or R′1 which are the same or different; R is X-(A-B)n-CONH2, X-(A-B)n-O—CONH2, X-(A-B)n-NH—CONH2, X—(CH2)m-heterocycloalkyl, X(CH2)m-aryl and X—(CH2)m-heteroaryl wherein X is —O—C(O), —NH—C(O), NH—CS, —NH—CO—CH2-O—; —NH—COCH2-S—CH2-CO—NH—; —NH—CO—(CH2)2-SO2-; and —NH—CO—CH2-N(CH3)-CO—; A and B are the same or different and are each independently a single bond, CH2, CH-alkyl, and CH-aralkyl; n=1, 2 and m=0, 1; R1 and/or R′1 are H, halogen, CF3, nitro, cyano, alkyle, hydroxy, mercapto, amino, alkylamino, dialkylamino, alkoxy, alkylthio, and carboxy, free or esterified by an alkyl, carboxamide, CONH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—SO2-alkyl, S(O)2-NHalkyl, and S(O2)-N(alkyl)2 group, all of said alkyl, alcoxy and alkylthio groups being optionally substituted themselves, said products being in all isomer forms and salts, as medicaments.

    摘要翻译： 提供式（I）的吡咯并吲哚，其中Het是含有1至4个杂原子N，O或S的芳族或部分不饱和的单环或双环杂环，任选被相同或不同的R1或R'1取代; R是X-（AB）n-CONH 2，X-（AB）n O-CONH 2，X-（AB）n -NH-CONH 2，X-（CH 2）m-杂环烷基， （CH 2）m - 杂芳基，其中X是-O-C（O），-NH-C（O），NH-CS，-NH-CO-CH 2 -O- -NH-COCH 2 -S-CH 2 -CO-NH-; -NH-CO-（CH 2）2 -SO 2 - ; 和-NH-CO-CH 2 -N（CH 3）-CO-; A和B相同或不同，各自独立地为单键，CH 2，CH-烷基和CH-芳烷基; n = 1,2，m = 0,1; R 1和/或R'1是烷基，羧酰胺，CONH（烷基）烷基，C 1 -C 6烷基，C 1 -C 6烷基， ，CON（烷基）2，NH-CO-烷基，磺酰胺，NH-SO 2 - 烷基，S（O）2 -NH烷基和S（O 2）-N（烷基）2基团，所有烷基，烷氧基和烷硫基 基团任选地被取代，所述产物是所有异构体形式和盐，作为药物。