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    Taxoids, their preparation and pharmaceutical compositions containing them
    22.
    发明授权
    Taxoids, their preparation and pharmaceutical compositions containing them 失效
    紫杉烷类，它们的制备方法和含有它们的药物组合物

    公开(公告)号：US5840931A

    公开(公告)日：1998-11-24

    申请号：US817742

    申请日：1997-04-24

    Applicant: Herve Bouchard ,  Jean-Dominique Bourzat ,  Alain Commer.cedilla.on ,  Corinne Terrier ,  Martine Zucco

    Inventor： Herve Bouchard ,  Jean-Dominique Bourzat ,  Alain Commer.cedilla.on ,  Corinne Terrier ,  Martine Zucco

    IPC: A61K31/335 ,  A61K31/337 ,  A61P35/00 ,  C07D305/14

    CPC classification number: C07D305/14

    Abstract: This invention relates to compounds of the formula (I), preparation thereof, and pharmaceutical compositions containing them: ##STR1## wherein: R.sub.a is hydrogen, hydroxyl, alkoxy, acyloxy, or an alkoxyacetoxy radical; R.sub.b is hydrogen; or R.sub.a and R.sub.b, together with the carbon atom to which they are attached, form a ketone function; Z represents a hydrogen atom or a radical of formula (II): ##STR2## in which: R.sub.1 represents an optionally substituted benzoyl, thenoyl, furoyl, or R.sub.2 --O--CO-- radical where R.sub.2 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, or an optionally substituted phenyl or heterocyclic radical; R.sub.3 is an aromatic heterocyclic, alkyl, alkenyl, alkynyl, cycloalkyl, or a phenyl or naphthyl radical; R.sub.4 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, aryl, or heterocyclic radical; and R.sup.5 is an optionally substituted cycloalkenyl, alkyl, alkenyl, alkynyl, or cycloalkyl radical. The compounds of formula (I), where Z is a formula (II) radical, have remarkable antitumoral and antineoplastic properties

    Abstract translation: PCT No.PCT / FR95 / 01393 Sec。 371日期1997年04月24日 102（e）日期1997年4月24日PCT提交1995年10月23日PCT公布。 公开号WO96 / 13494 日期：1996年5月9日本发明涉及式（I）化合物及其制备方法及含有它们的药物组合物：其中：R a为氢，羟基，烷氧基，酰氧基或烷氧基乙酰氧基; Rb是氢; 或R a和R b与它们所连接的碳原子一起形成酮官能团; Z表示氢原子或式（II）的基团：nally取代的苯甲酰基，噻吩甲酰基，呋喃甲酰基或R2-O-CO-基，其中R2是烷基，烯基，炔基，环烷基，环烯基，双环烷基或任选取代的 苯基或杂环基; R3是芳族杂环，烷基，烯基，炔基，环烷基或苯基或萘基; R4是烷基，烯基，炔基，环烷基，环烯基，双环烷基，芳基或杂环基; 并且R 5是任选取代的环烯基，烷基，烯基，炔基或环烷基。 式（I）化合物，其中Z为式（II）基团，具有显着的抗肿瘤和抗肿瘤性质

    Benzimidazole derivatives and their use as kdr kinase protein inhibitors
    25.
    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

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

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

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

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

    Abstract: 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.

    Abstract translation: 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。

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