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    HSP90 INHIBITING INDAZOLE DERIVATIVES, COMPOSITIONS CONTAINING SAME AND USE THEREOF
    11.
    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。

    Guanidino derivatives as inhibitors of cell adhesion
    14.
    发明授权
    Guanidino derivatives as inhibitors of cell adhesion 有权
    胍基衍生物作为细胞粘附抑制剂

    公开(公告)号：US07259159B2

    公开(公告)日：2007-08-21

    申请号：US10343173

    申请日：2001-07-23

    申请人： Anuschirwan Peyman ,  David Will ,  Thomas R Gadek ,  Robert McDowell ,  Jean Francois Gourvest ,  Jean-Marie Ruxer ,  Jochen Knolle

    发明人： Anuschirwan Peyman ,  David Will ,  Thomas R Gadek ,  Robert McDowell ,  Jean Francois Gourvest ,  Jean-Marie Ruxer ,  Jochen Knolle

    IPC分类号： C07D471/04 ,  C07D487/04 ,  C07D473/16 ,  C07D473/24 ,  C07D473/28 ,  C07D473/32 ,  C07D473/34 ,  C07D473/36 ,  C07D473/40 ,  A61K31/437 ,  A61K31/519

    CPC分类号： C07D473/00 ,  C07D487/04

    摘要： The present invention relates to acylguanidino derivatives of formula (I), in which R1, R2, R3, A, B, X, Y and n have the meanings indicated in claim 1, their physiologically tolerable salts and their prodrugs. The compounds of the formula (I) are valuable pharmaceutically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion and bone resorption by osteoclasts. This renders them suitable, for example, for the therapy and prophylaxis of illness which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or proliferation of cells of the vascular smooth muscles. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as pharmaceutical active ingredients, and pharmaceutical compositions comprising them

    摘要翻译： 本发明涉及式（I）的酰基胍基衍生物，其中R 1，R 2，R 3，A，B，X ，Y和n具有权利要求1所述的含义，其生理上可耐受的盐及其前药。 式（I）的化合物是有价值的药物活性化合物。 它们是玻连蛋白受体拮抗剂和破骨细胞的细胞粘附和骨吸收的抑制剂。 这使得它们适合于例如基于玻连蛋白受体及其配体在细胞 - 细胞或细胞 - 基质相互作用过程中的相互作用的疾病的治疗和预防，或通过影响这些相互作用可以预防，缓解或治愈 。 例如，它们可以用于治疗和预防骨质疏松症，或用于抑制血管平滑肌细胞的不期望的血管生成或增殖。 本发明还涉及制备式（I）化合物的方法，其用途，特别是作为药物活性成分，以及包含它们的药物组合物

    NOVEL DERIVATIVES OF PYRROLOINDOLE WHICH ARE INHIBITORS OF HSP90, COMPOSITIONS CONTAINING SAME, AND USE THEREOF
    18.
    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。