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    Bisimide compounds
    4.
    发明授权
    Bisimide compounds 失效
    双酰亚胺化合物

    公开(公告)号：US5854273A

    公开(公告)日：1998-12-29

    申请号：US899289

    申请日：1997-07-23

    申请人： Gilbert Lavielle ,  Patrick Hautefaye ,  Ghanem Atassi ,  Alain Pierre ,  Laurence Kraus-Berthier ,  Stephane Leonce

    发明人： Gilbert Lavielle ,  Patrick Hautefaye ,  Ghanem Atassi ,  Alain Pierre ,  Laurence Kraus-Berthier ,  Stephane Leonce

    IPC分类号： C07D221/10 ,  A61K31/435 ,  A61K31/47 ,  A61K31/473 ,  A61K31/55 ,  A61P35/00 ,  C07D209/80 ,  C07D401/12 ,  C07D403/12 ,  C07D519/00 ,  A61K31/40 ,  C07D403/06

    CPC分类号： C07D209/80 ,  C09B57/08

    摘要： A compound of formula (I) ##STR1## in which: X and Y, which may be identical or different, represent hydrogen or halogen or alkyl, trihaloalkyl, alkoxy, hydroxyl, cyano, nitro, amino, alkylamino, or dialkylamino, Z represent a linear or branched C.sub.4 to C.sub.12 alkylene chain in which one or more --CH.sub.2 -- are optionally replaced by any one of the following atoms or groups: --NR--, --O--, --S--, --SO--, --SO.sub.2 --, or --CONH--, A forms, with two adjacent carbon atoms of the phenyl ring, a phenyl, naphthyl or tetrahydronaphthyl ring or a heterocycle, ##STR2## represents any one of the groups as defined in the description, its optical isomers and its addition salts with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful as anticancer agents.

    摘要翻译： 式（I）化合物其中：X和Y可以相同或不同，表示氢或卤素或烷基，三卤代烷基，烷氧基，羟基，氰基，硝基，氨基，烷基氨基或二烷基氨基 Z表示直链或支链的C 4至C 12亚烷基链，其中一个或多个-CH 2 - 任选被以下原子或基团中的任何一个取代：-NR - ， - O - ， - S - ， - SO-， - SO 2 - 或-CONH-，A形式，其具有苯环的两个相邻碳原子，苯基，萘基或四氢萘基环或杂环，IMAGE表示说明书中定义的任何一个基团，其旋光异构体 及其与药学上可接受的酸或碱的加成盐，以及含有该盐的药物，可用作抗癌剂。

    Camptothecin analogue compounds
    5.
    发明授权
    Camptothecin analogue compounds 失效
    喜树碱类似物

    公开(公告)号：US06509345B2

    公开(公告)日：2003-01-21

    申请号：US10010380

    申请日：2001-11-05

    申请人： Gilbert Lavielle ,  Patrick Hautefaye ,  Alain Pierre ,  Ghanem Atassi ,  John Hickman ,  Bernard Cimetiere

    发明人： Gilbert Lavielle ,  Patrick Hautefaye ,  Alain Pierre ,  Ghanem Atassi ,  John Hickman ,  Bernard Cimetiere

    IPC分类号： C07D47114

    CPC分类号： C07D471/14 ,  A61K31/4745 ,  Y02P20/55

    摘要： Compound of formula (I): wherein: n is 0, 1 or 2, R1, R2, R3, R4 and R5 are selected from hydrogen, halogen, alkyl, alkenyl, alkynyl, perhaloalkyl, cycloalkyl, cycloalkylalkyl, hydroxy, hydroxyalkyl, alkoxy, alkoxyalkyl, alkoxycarbonyl, acyloxy, carboxy, nitro, cyano, aminocarbonyl (optionally substituted), and the groups (CH2)p—NRaRb and —O—C(O)—N—RaRb, with p, Ra and Rb being as defined in the description, or two adjacent groups R2, R3, R4 and R5 together form a group —O—(CH2)t—O, t being an integer from 1 to 3, R60, R70n, R80 and R90 represent a hydrogen atom, a hydroxy group, an alkoxy group, or an O—(CO)—X or O—(CO)—NXW group as defined in the description, R61, R71n, R81 and R91 represent a hydrogen atom, alkyl, alkenyl or alkynyl, or taken in pairs together form a bond or an oxirane group, or two groups together form an oxo group. and medicinal products containing the same are useful for the treatment of cancerous diseases.

    摘要翻译： 式（I）化合物：其中：n为0,1或2，R1，R2，R3，R4和R5选自氢，卤素，烷基，烯基，炔基，全卤代烷基，环烷基，环烷基烷基，羟基，羟烷基，烷氧基 ，烷氧基烷基，烷氧基羰基，酰氧基，羧基，硝基，氰基，氨基羰基（任选取代的）和基团（CH 2）p -NR a R b和-OC（O）-NR a R b，其中p，R a和R b如 描述或两个相邻基团R 2，R 3，R 4和R 5一起形成基团-O-（CH 2）t O，t为1至3的整数，R 60，R 70n，R 80和R 90表示氢原子，羟基， 烷氧基或描述中定义的O-（CO）-X或O-（CO）-NXW基团，R61，R71n，R81和R91表示氢原子，烷基，烯基或炔基，或成对取代 一起形成键或环氧乙烷基团，或两个基团一起形成氧代基，并且含有该氧基的药物可用于治疗癌性疾病。

    Camptothecin analogue compounds
    6.
    发明授权
    Camptothecin analogue compounds 失效
    喜树碱类似物

    公开(公告)号：US06699876B2

    公开(公告)日：2004-03-02

    申请号：US10300330

    申请日：2002-11-20

    申请人： Gilbert Lavielle ,  Patrick Hautefaye ,  Alain Pierre ,  Ghanem Atassi ,  John Hickman ,  Bernard Cimetiere

    发明人： Gilbert Lavielle ,  Patrick Hautefaye ,  Alain Pierre ,  Ghanem Atassi ,  John Hickman ,  Bernard Cimetiere

    IPC分类号： A61K314375

    CPC分类号： C07D471/14 ,  A61K31/4745

    摘要： Compound of formula (I): wherein: n is 0, 1 or 2, R1 represents (C3-C11)cycloalkyl or (C3-C11)cycloalkylalkyl, R2, R3, R4 and R5 are selected from hydrogen, halogen, alkyl, alkenyl, alkynyl, perhaloalkyl, cycloalkyl, cycloalkylalkyl, hydroxy, hydroxyalkyl, alkoxy, alkoxyalkyl, alkoxycarbonyl, acyloxy, carboxy, nitro, cyano, aminocarbonyl (optionally substituted), and the groups (CH2)p—NaRb and —O—C(O)—N—RaRb, with p, Ra and Rb being as defined in the description, or two adjacent groups R2, R3, R4 and R5 together form a group —O—(CH2)t—O, t being integer from 1 to 3, R60, R70n, R80 and R90 represent a hydrogen atom, a hydroxy group, an alkoxy group, or an O—(CO)—X or O—(CO)—NXW group as defined in the description, R61, R71n, R81, and R91 represent a hydrogen atom, alkyl, alkenyl or alkynyl, or taken in pairs together form a bond or an oxirane group, or two groups together form an oxo group. and medicinal products containing the same are useful for the treatment of cancerous disesases.

    摘要翻译： 式（I）化合物：其中：n为0,1或2，R1代表（C3-C11）环烷基或（C3-C11）环烷基烷基，R2，R3，R4和R5选自氢，卤素，烷基，烯基 ，炔基，全卤代烷基，环烷基，环烷基烷基，羟基，羟基烷基，烷氧基，烷氧基烷基，烷氧基羰基，酰氧基，羧基，硝基，氰基，氨基羰基（任选取代的）和基团（CH 2）p-NaRb和-OC（O） -RaRb，其中p，Ra和Rb如说明书中所定义，或两个相邻基团R 2，R 3，R 4和R 5一起形成基团-O-（CH 2）t O，t为1至3的整数，R 60，R 70n R 80和R 90表示如说明书中定义的氢原子，羟基，烷氧基或O-（CO）-X或O-（CO）-NXW基团，R61，R71n，R81和R91表示 氢原子，烷基，烯基或炔基，或成对取成一起形成键或环氧乙烷基，或两个基团一起形成氧代基，并且含有该氧基的药物可用于治疗癌性疾病。

    N-(23-vincristinoyl) and N-(5'-noranhydro-23-vinblastinoyl) compounds of 1-aminomethylphosphonic acid useful for the treatment of neoplastic diseases
    7.
    发明授权
    N-(23-vincristinoyl) and N-(5'-noranhydro-23-vinblastinoyl) compounds of 1-aminomethylphosphonic acid useful for the treatment of neoplastic diseases 失效
    用于治疗神经疾病的1-氨基乙基磷酸的N-（23-VINCRISTINOYL）和N-（5'-去甲基-23-VINBLASTINOYL）化合物

    公开(公告)号：US5100881A

    公开(公告)日：1992-03-31

    申请号：US561065

    申请日：1990-08-01

    申请人： Gilbert Lavielle ,  Patrick Hautefaye ,  Alain Pierre

    发明人： Gilbert Lavielle ,  Patrick Hautefaye ,  Alain Pierre

    IPC分类号： A61K31/675 ,  A61P35/00 ,  C07F9/32 ,  C07F9/6558 ,  C07F9/6561

    CPC分类号： C07F9/6561

    摘要： The invention relates to the compounds of general formula I: ##STR1## in which: R.sub.1 represents a hydrogen atom, a linear or branched alkyl radical containing from 1 to 6 carbon atoms, a linear or branched alkenyl radical containing from 2 to 6 carbon atoms, an arylalkyl radical having 7 to 10 carbon atoms and which can bear a halogen atom as a substituent on the aromatic ring, a hydroxyl radical or an alkyl or alkoxy radical each containing from 1 to 5 carbon atoms, a 2-indolylmethyl radical, a 4-imidazolylmethyl radical or an alkoxycarbonylmethyl radical containing from 3 to 11 carbon atoms,R.sub.2 and R.sub.3, which may be identical or different, each represents a linear or branched alkyl radical containing from 1 to 6 carbon atoms,n is equal to 1 or 2,R.sub.4 represents a hydrogen atom, a formyl radical or a methyl radical, with the proviso, however, that R.sub.4 is never the methyl radical when n is equal to 2, andeither R.sub.5 and R.sub.6 together form a double bond, or R.sub.5 represents a hydrogen atom and R.sub.6 a hydroxyl radical,in the form of a mixture of diastereoisomers or of pure isomers, their N.sub.b,-oxides and their addition salts with a pharmaceutically acceptable inorganic or organic acid.These compounds are antitumor agents.

    摘要翻译： 本发明涉及通式I的化合物：其中：R 1表示氢原子，含有1至6个碳原子的直链或支链烷基，含有直链或支链烯基的基团 2至6个碳原子，具有7至10个碳原子的芳基烷基，其可以带有卤素原子作为芳族环上的取代基，羟基或每个含有1至5个碳原子的烷基或烷氧基， 2-吲哚基甲基，4-咪唑基甲基或含有3至11个碳原子的烷氧基羰基甲基，可以相同或不同的R 2和R 3各自表示含有1至6个碳原子的直链或支链烷基，n 等于1或2，R4表示氢原子，甲酰基或甲基，但条件是，当n等于2时，R 4不是甲基，R 5和R 6一起形成双 键，或R 5表示氢 原子和R6是非对映异构体或纯异构体的混合物形式的羟基，它们的Nb， - 氧化物及其与药学上可接受的无机酸或有机酸的加成盐。 这些化合物是抗肿瘤剂。

    Bisimide compounds
    8.
    发明授权
    Bisimide compounds 失效
    双酰亚胺化合物

    公开(公告)号：US06300340B1

    公开(公告)日：2001-10-09

    申请号：US09616857

    申请日：2000-07-14

    申请人： Gilbert Lavielle ,  Patrick Hautefaye ,  Ghanem Atassi ,  Alain Pierre ,  Laurence Kraus-Berthier ,  Stéphane Leonce

    发明人： Gilbert Lavielle ,  Patrick Hautefaye ,  Ghanem Atassi ,  Alain Pierre ,  Laurence Kraus-Berthier ,  Stéphane Leonce

    IPC分类号： C07D48704

    CPC分类号： C07D209/80 ,  C09B57/08

    摘要： A compound of formula (I) in which: m, and n, which may be identical or different, represent 0 or 1, X and Y, which may be identical or different, represent hydrogen or halogen or alkyl, trihaloalkyl, alkoxy, hydroxyl, cyano, nitro, amino, alkylamino, or dialkylamino, Z represent a linear or branched C4 to C12 alkylene chain in which one or more —CH2— are optionally replaced by any one of the following atoms or groups: —NR—, —O—, —S—, —SO—, SO2—, or —CONH—, or by a substituted or unsubstituted heterocylcic, A forms, with two adjacent carbon atoms of the phenyl ring, a phenyl, naphthyl or tetrahydronaphthyl ring or a heterocycle, represents any one of the groups as defined in the description, its optical isomers and its addition salts with a pharamaceutically and acceptable acid or base, and medicinal products containing the same which are useful as anticancer agents.

    摘要翻译： 式（I）化合物，其中m和n可以相同或不同，表示0或1，X和Y可以相同或不同，表示氢或卤素或烷基，三卤代烷基，烷氧基，羟基 ，氰基，硝基，氨基，烷基氨基或二烷基氨基，Z表示直链或支链的C 4至C 12亚烷基链，其中一个或多个-CH 2 - 任选被以下任何一个原子或基团取代：-NR-，-O - ， - S - ， - SO - ，SO2-或-CONH-，或通过取代或未取代的杂环A形式与苯环的两个相邻碳原子，苯基，萘基或四氢萘基环或杂环， 表示在描述中定义的任何一个基团，其光学异构体及其与药物和可接受的酸或碱的加成盐，以及含有该组的药物，其可用作抗癌剂。