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    Benzimidazole derivatives and their use as kdr kinase protein inhibitors
    1.
    发明申请
    Benzimidazole derivatives and their use as kdr kinase protein inhibitors 审中-公开
    苯并咪唑衍生物及其作为kdr激酶蛋白抑制剂的用途

    公开(公告)号：US20080125418A1

    公开(公告)日：2008-05-29

    申请号：US11943008

    申请日：2007-11-20

    申请人： Didier Babin ,  Alain Le Brun ,  Laurence Gauzy-Lazo ,  Herve Bouchard

    发明人： Didier Babin ,  Alain Le Brun ,  Laurence Gauzy-Lazo ,  Herve Bouchard

    IPC分类号： A61K31/541 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/454 ,  A61K31/4196 ,  A61K31/4184 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D487/04 ,  C07D491/04

    摘要： The invention discloses and claims benzimidazole compounds of formula (I): wherein X is C—R2; Y is C—R2 or C—R3; W and Z are each C—R3; R1 is an optionally substituted aryl, heteroaryl or a saturated 5- or 6-membered monocyclic heterocyclic radical or a bicyclic heterocyclic radical; and A5 is H or alkyl; or a stereoisomer, a racemate, an enantiomer or a diastereoisomer of said compound of formula (I) or a pharmaceutically acceptable salt thereof; the use of compounds of formula (I) for the treatment of a disorder of proliferation of blood vessels, uncontrolled angiogenesis, a fibrotic disorder, a disorder of proliferation of mesangial cells, a metabolic disorder, allergy, asthma, thrombosis, a disease of the nervous system, retinopathy, psoriasis, rheumatoid arthritis, diabetes, muscle degeneration, solid tumors and cancers, pharmaceutical compositions comprising a compound of formula (I) and one or more pharmaceutically acceptable adjuvants or diluents and pharmaceutical compositions comprising a compound of formula (I) and one or more. antimitotic agents.

    摘要翻译： 本发明公开并要求式（I）的苯并咪唑化合物：其中X是C-R2; Y为C-R2或C-R3; W和Z各自为C-R3; R 1是任选取代的芳基，杂芳基或饱和的5-或6-元单环杂环基或双环杂环基; A5是H或烷基; 或所述式（I）化合物的立体异构体，外消旋物，对映异构体或非对映异构体或其药学上可接受的盐; 使用式（I）化合物治疗血管增生障碍，不受控制的血管生成，纤维化病症，肾小球膜细胞增殖障碍，代谢紊乱，过敏，哮喘，血栓形成，疾病 神经系统，视网膜病变，银屑病，类风湿性关节炎，糖尿病，肌肉变性，实体瘤和癌症，包含式（I）化合物和一种或多种药学上可接受的佐剂或稀释剂的药物组合物和包含式（I）化合物的药物组合物， 和一个或多个。 抗有丝分裂剂。

    Aminoindazole derivatives as medicaments and pharmaceutical compositions including them
    2.
    发明授权
    Aminoindazole derivatives as medicaments and pharmaceutical compositions including them 有权
    氨基吲唑衍生物作为药物和药物组合物，包括它们

    公开(公告)号：US07166629B2

    公开(公告)日：2007-01-23

    申请号：US10654703

    申请日：2003-09-04

    申请人： Dominique Lesuisse ,  Gilles Dutruc-Rosset ,  Franck Halley ,  Didier Babin ,  Thomas Rooney

    发明人： Dominique Lesuisse ,  Gilles Dutruc-Rosset ,  Franck Halley ,  Didier Babin ,  Thomas Rooney

    IPC分类号： A61K31/416 ,  C07D231/56

    CPC分类号： C07D231/56 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

    摘要： The present invention relates to novel derivatives of general formula (I) in which R3 is a (1–6C)alkyl, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, aryl or heteroaryl fused to a (1–10C)cycloalkyl, heterocycle, heterocycloalkyl, cycloalkyl, adamantyl, polycycloalkyl, alkenyl, alkynyl, CONR1R2, COOR1, SO2R1, C(═NH)R1 or C(═NH)NR1 radical; R5 and R6 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, —O—SO2R8, —SO2—O—R8, trifluoromethyl, trifluoromethoxy, (1–6C)alkyl, (1–6C)alkoxy, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl or polycycloalkyl.

    摘要翻译： 本发明涉及通式（I）的新型衍生物，其中R3是（1-6C）烷基，芳基，芳基（1-6C）烷基，杂芳基，杂芳基（1-6C）烷基，芳基或杂芳基 （1-10C）环烷基，杂环，杂环烷基，环烷基，金刚烷基，多环烷基，烯基，炔基，CONR1R2，COOR1，SO2R1，C（-NH）R1或C（-NH）NR1 激进; R 5和R 6彼此独立地选自以下基团：卤素，CN，NO 2，NH 2，OH，COOH，C（O）OR 8， -OC（O）R8，NR8R9，NHC（O）R8，C（O）NR8R9，NHC（S）R8，C（S）NR8R9，SR8，S（O） R 8，NHSO 2 R 8，SO 2 NR 8 R 9，-O-SO 2 R 8，-SO 2 -O （1-6C）烷氧基，芳基，芳基（1-6C）烷基，杂芳基，杂芳基（1-6C）烷基，杂环，环烷基，链烯基，炔基，金刚烷基 或多环烷基。

    9H-PYRROLO[2,3-B: 5,4-C'] DIPYRIDINE AZACARBOLINE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF
    8.
    发明申请
    9H-PYRROLO[2,3-B: 5,4-C'] DIPYRIDINE AZACARBOLINE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF 审中-公开
    9H-吡咯并[2,3-B：5,4-C']二吡啶基咪唑啉衍生物，其制备方法及其治疗用途

    公开(公告)号：US20120208809A1

    公开(公告)日：2012-08-16

    申请号：US13258924

    申请日：2009-11-30

    申请人： Didier Babin ,  Olivier Bedel ,  Thierry Gouyon ,  Serge Mignani ,  David Papin

    发明人： Didier Babin ,  Olivier Bedel ,  Thierry Gouyon ,  Serge Mignani ,  David Papin

    IPC分类号： A61K31/444 ,  A61K31/496 ,  A61K31/5377 ,  C07D519/00 ,  A61K31/55 ,  C07F5/02 ,  C07D401/04 ,  C07D213/64 ,  C07D213/61 ,  A61P35/00 ,  A61K31/4545 ,  A61K31/4375 ,  C07F5/04 ,  C07F7/22 ,  C07D471/14

    CPC分类号： C07D471/14 ,  C07D207/34 ,  C07D213/24

    摘要： The invention relates to novel 9H-pyrrolo[2,3-b:5,4-c′]dipyridine azacarbolines of formula (I), where: Z2, Z3, and Z4 are CH, CRa, CRs, or N; R3 is H, Hal; CF3, CHF2; OH, alkoxy; NH2, NH (alkyl), N(alkyl)2; C(O)O alkyl; CONH(alkyl), CON(alkyl)2; C1-C10 alkyl; aryl; heteroaryl; R6 is heteroaryl; Ra is CONH2, CONH alkyl, CONH cycloalkyl; CONH heterocycloalkyl; CON(alkyl)2; CON(alkyl)(heterocycloalkyl); CONHN(alkyl)2; C(O)heterocycloalkyl; Rs is H; Hal, OH; O-alkyl(C1-C10); NH2; N(alkyl(C1-C10) or cycloalkyl(C3-C7))2; NHC(O)R3a; N(alkyl(C1-C10)C(O)R3a; NHS(O2)R3a; N(alkyl)(C1-C10)S(O2)R3a; CO2R3a; SR3a; S(O)R3a; S(O2)R3a; Ra and Rs optionally form a cycle; R3a is selected from among Hal, CF3, C1-C10 alkyl; C3-C7 cycloalkyl; C2-C6 alkenyl; C2-C6 alkynyl; OH; O-alkyl(C1-C10); (C3-C7); heterocycloalkyl (C3-C7); NH2; NH-(alkyl(C1-C10) or cycloalkyl(C3-C7)); N(alkyl(C1-C10) or cycloalkyl(C3-C7))2; NH-(alkyl(C1-C10) or heterocycloalkyl(C3-C7)); N(alkyl(C1-C10) or heterocycloalkyl(C3-C7))2, as well as to the isomers and salts of said substances of formula (I) and to the therapeutic use thereof for treating cancer.

    摘要翻译： 本发明涉及式（I）的新型9H-吡咯并[2,3-b：5,4-c']二吡啶并吡唑啉，其中：Z2，Z3和Z4为CH，CRa，CRs或N; R3为H，Hal; CF 3，CHF 2; OH，烷氧基; NH 2，NH（烷基），N（烷基）2; C（O）O烷基; CONH（烷基），CON（烷基）2; C1-C10烷基; 芳基; 杂芳基; R6是杂芳基; R a是CONH 2，CONH烷基，CONH环烷基; CONH杂环烷基; CON（烷基）2; CON（烷基）（杂环烷基）; CONHN（烷基）2; C（O）杂环烷基; Rs是H; Hal，OH; O-烷基（C1-C10）; NH2; N（烷基（C1-C10）或环烷基（C3-C7））2; NHC（O）R 3a; N（烷基（C1-C10）C（O）R3a; NHS（O2）R3a; N（烷基）（C1-C10）S（O2）R3a; CO2R3a; SR3a; S（O）R3a; S（O2） ; R a和R 5任选地形成一个周期; R 3a选自Hal，CF 3，C 1 -C 10烷基; C 3 -C 7环烷基; C 2 -C 6烯基; C 2 -C 6炔基; OH; O-烷基（C 1 -C 10） C 3 -C 7烷基（C 3 -C 7）; NH 2; NH-（烷基（C 1 -C 10）或环烷基（C 3 -C 7））; N（烷基（C 1 -C 10） NH-（烷基（C1-C10）或杂环烷基（C3-C7））; N（烷基（C1-C10）或杂环烷基（C3-C7））2，以及所述式 I）及其用于治疗癌症的治疗用途。

    Aminoindazole derivatives as medicaments and pharmaceutical compositions including them
    10.
    发明授权
    Aminoindazole derivatives as medicaments and pharmaceutical compositions including them 有权
    氨基吲唑衍生物作为药物和药物组合物，包括它们

    公开(公告)号：US07582669B2

    公开(公告)日：2009-09-01

    申请号：US11567442

    申请日：2006-12-06

    申请人： Dominique Lesuisse ,  Gilles Dutruc-Rosset ,  Franck Halley ,  Didier Babin ,  Thomas Rooney

    发明人： Dominique Lesuisse ,  Gilles Dutruc-Rosset ,  Franck Halley ,  Didier Babin ,  Thomas Rooney

    IPC分类号： A61K31/416

    CPC分类号： C07D231/56 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

    摘要： The present invention relates to novel derivatives of general formula (I) in which R3 is a (1-6C)alkyl, aryl, aryl(1-6C)alkyl, heteroaryl, heteroaryl(1-6C)alkyl, aryl or heteroaryl fused to a (1-10C) cycloalkyl, heterocycle, heterocycloalkyl, cycloalkyl, adamantyl, polycycloalkyl, alkenyl, alkynyl, CONR1R2, COOR1, SO2R1, C(═NH)R1 or C(═NH)NR1 radical; R5 and R6 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, —O—SO2R8, —SO2—O—R8, trifluoromethyl, trifluoromethoxy, (1-6C)alkyl, (1-6C)alkoxy, aryl, aryl(1-6C)alkyl, heteroaryl, heteroaryl(1-6C)alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl or polycycloalkyl.

    摘要翻译： 本发明涉及通式（I）的新型衍生物，其中R3是（1-6C）烷基，芳基，芳基（1-6C）烷基，杂芳基，杂芳基（1-6C）烷基，芳基或杂芳基 （1-10C）环烷基，杂环，杂环烷基，环烷基，金刚烷基，多环烷基，烯基，炔基，CONR1R2，COOR1，SO2R1，C（-NH）R1或C（-NH）NR1基; R 5和R 6彼此独立地选自以下基团：卤素，CN，NO 2，NH 2，OH，COOH，C（O）OR 8，-OC（O）R 8，NR 8 R 9，NHC（O） （O）NR8R9，NHC（S）R8，C（S）NR8R9，SR8，S（O）R8，SO2R8，NHSO2R8，SO2NR8R9，-O-SO2R8，-SO2-O-R8，三氟甲基，三氟甲氧基，（1- 6C）烷基，（1-6C）烷氧基，芳基，芳基（1-6C）烷基，杂芳基，杂芳基（1-6C）烷基，杂环，环烷基，烯基，炔基，金刚烷基或多环烷基。