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    Complexes derived from platinum, their preparation and the pharmaceutical compositions which contain them
    1.
    发明授权
    Complexes derived from platinum, their preparation and the pharmaceutical compositions which contain them 失效
    衍生自铂的复合物，其制备物和含有它们的药物组合物

    公开(公告)号：US5225207A

    公开(公告)日：1993-07-06

    申请号：US775410

    申请日：1991-10-15

    申请人： Michel Barreau ,  Jean-Claude Chottard ,  Jean-Bernard Le Peco ,  Patrick Mailliet

    发明人： Michel Barreau ,  Jean-Claude Chottard ,  Jean-Bernard Le Peco ,  Patrick Mailliet

    IPC分类号： C07F15/00

    CPC分类号： C07F15/0093

    摘要： New complexes of general formula (I) in whichR.sub.1 and R.sub.2 together form a saturated or unsaturated polycyclic carbocyclic radical containing 7 to 12 carbon atoms, or a saturated or partially saturated mono-, bi- or tricyclic heterocyclic radical containing 5 to 11 chain members and a hetero-atom chosen from oxygen, sulphur or nitrogen, which latter atom can optionally be substituted by an alkoxycarbonyl radical, and,X.sub.1 and X.sub.2 represent chlorine atoms or together formeither a radical of structure: ##STR1## in which n is 0 to 2 and R.sub.6 and R.sub.7, which are identical or different, are hydrogen atoms or, when n=1, can be alkyl radicals or form, together with the carbon atom to which they are attached, a cyclobutyl radical,or a radical of structure: ##STR2## in which n, R.sub.6 and R.sub.7 are defined as above, or their salts where such exist, and their hydrates, their preparation and the pharmaceutical compositions which contain them. ##STR3##

    摘要翻译： 通式（I）的新络合物，其中R 1和R 2一起形成含有7至12个碳原子的饱和或不饱和多环碳环基团，或含有5至11个链成员的饱和或部分饱和的单，双或三环杂环基团 和选自氧，硫或氮的杂原子，其后一个原子可任选被烷氧基羰基取代，并且，X 1和X 2表示氯原子或一起形成结构式如下的基团：其中 n为0〜2，R6和R7为相同或不同的氢原子，n = 1时，可以为烷基，也可以与它们所连接的碳原子一起形成环丁基或 结构基团：其中n，R6和R7如上所定义，或其盐，如此存在，以及它们的水合物，它们的制备和含有它们的药物组合物。 （一）

    Farnesyl transferase inhibitors, their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments
    5.
    发明授权
    Farnesyl transferase inhibitors, their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments 失效
    法呢基转移酶抑制剂，它们的制备，含有它们的药物组合物及其在制备药物中的用途

    公开(公告)号：US6124465A

    公开(公告)日：2000-09-26

    申请号：US346540

    申请日：1999-07-02

    申请人： Jean-Dominique Bourzat ,  Alain Commer.cedilla.on ,  Norbert Dereu ,  Patrick Mailliet ,  Fabienne Sounigo-Thompson ,  Jean-Paul Martin ,  Marc Capet ,  Michel Cheve

    发明人： Jean-Dominique Bourzat ,  Alain Commer.cedilla.on ,  Norbert Dereu ,  Patrick Mailliet ,  Fabienne Sounigo-Thompson ,  Jean-Paul Martin ,  Marc Capet ,  Michel Cheve

    IPC分类号： C07D209/56 ,  C07D233/56 ,  C07D401/08 ,  C07D209/80 ,  C07F9/28

    CPC分类号： C07D209/56

    摘要： Novel products of formula (I), their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments. ##STR1## In the formula (I), the following substituents are among the preferred: Ar represents a substituted or condensed phenyl radical or a polycyclic or heterocyclic aromatic radical, R represents a radical of general formula --(CH.sub.2).sub.m --X.sub.1 --(CH.sub.2).sub.n --Z in which X.sub.1 =single bond, O, S; m=0, 1; n=0, 1, 2; it being possible for the CH.sub.2 radicals to be substituted; Z represents carboxyl, COOR.sub.6 (R.sub.6 =alkyl), CON(R.sub.7)(R.sub.8) (R.sub.7 =hydrogen or alkyl and R.sub.8 =hydrogen, hydroxyl, arylsulphonyl, heterocyclyl, optionally substituted amino, optionally substituted alkyloxy or optionally substituted alkyl), PO(OR.sub.9).sub.2 (R.sub.9 =hydrogen or alkyl), an --NH--CO--T (T=hydrogen or optionally substituted alkyl) radical, or else--a ##STR2## radical, R.sub.1 and R.sub.2 =hydrogen or halogen or alkyl, alkyloxy, which is optionally substituted, alkylthio, alkyloxycarbonyl or else R.sub.1 and R.sub.2, at the ortho position with respect to one another, form an optionally substituted heterocycle containing 1 or 2 heteroatoms, R.sub.3 and R.sub.4 =hydrogen or halogen or alkyl, alkenyl, alkyloxy, alkylthio. carboxyl or alkyloxycarbonyl, R.sub.5 =hydrogen, alkyl, alkylthio, X=O or S or --NH--, --CO--, methylene, vinyldiyl, alkene-1,1-diyl or cycloalkane-1,1-diyl, and Y=O or S, in the racemic form, as well as the optical isomers (diastereomers and enantiomers) and the salts of the product of formula (I). The compounds of formula (I) are farnesyl transferase inhibitors which exhibit notable antitumor and antileukemic properties.

    摘要翻译： 式（I）的新产品，其制备方法，含有它们的药物组合物及其在制备药物中的用途。 在式（I）中，以下取代基是优选的：Ar表示取代或稠合的苯基或多环或杂环芳族基，R表示通式 - （CH 2）m -X1（CH 2）n Z 其中X1 =单键，O，S; m = 0,1， n = 0,1,2; CH2基可以被取代; Z代表羧基，COOR6（R6 =烷基），CON（R7）（R8）（R7 =氢或烷基，R8 =氢，羟基，芳基磺酰基，杂环基，任选取代的氨基，任选取代的烷氧基或任选取代的烷基），PO OR 9）2（R 9 =氢或烷基），-NH-CO-T（T =氢或任选取代的烷基）基团，或者 - 基团，R 1和R 2 =氢或卤素或烷基，烷氧基， 取代的烷硫基，烷氧基羰基，或者R1和R2相对于彼此的邻位，形成含有1或2个杂原子的任选取代的杂环，R 3和R 4 =氢或卤素或烷基，烯基，烷氧基，烷硫基。 羧基或烷氧基羰基，R5 =氢，烷基，烷硫基，X = O或S或-NH-，-CO-，亚甲基，乙烯基二烯基，烯-1,1-二基或环烷烃-1,1-二基，Y = O 或S，外消旋形式，以及光学异构体（非对映体和对映体）和式（I）的产物的盐。 式（I）化合物是具有显着的抗肿瘤和抗白血病性质的法呢基转移酶抑制剂。

    Farnesyl transferase inhibitors, their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments
    9.
    发明授权
    Farnesyl transferase inhibitors, their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments 失效
    法呢基转移酶抑制剂，它们的制备，含有它们的药物组合物及其在制备药物中的用途

    公开(公告)号：US06218406B1

    公开(公告)日：2001-04-17

    申请号：US09346303

    申请日：1999-07-02

    申请人： Jean-Dominique Bourzat ,  Alain Commerçon ,  Norbert Dereu ,  Patrick Mailliet ,  Fabienne Sounigo-Thompson ,  Jean-Paul Martin ,  Marc Capet ,  Michel Cheve

    发明人： Jean-Dominique Bourzat ,  Alain Commerçon ,  Norbert Dereu ,  Patrick Mailliet ,  Fabienne Sounigo-Thompson ,  Jean-Paul Martin ,  Marc Capet ,  Michel Cheve

    IPC分类号： A61K314439

    CPC分类号： C07D401/12 ,  C07D209/56 ,  C07D209/72 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14

    摘要： Novel products of formula (I), their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments. In the formula (I), the following substituents are among the preferred: Ar represents a substituted or condensed phenyl radical or a polycyclic or heterocyclic aromatic radical, R represents a radical of general formula —(CH2)m—X1—(CH2)n—Z in which X1=single bond, O, S; m=0, 1; n=0, 1, 2; it being possible for the CH2 radicals to be substituted; Z represents carboxyl, COOR6 (R6=alkyl), CON(R7)(R8) (R7=hydrogen or alkyl and R8=hydrogen, hydroxyl, arylsulphonyl, heterocyclyl, optionally substituted amino, optionally substituted alkyloxy or optionally substituted alkyl), PO(OR9)2 (R9=hydrogen or alkyl), an —NH—CO—T (T=hydrogen or optionally substituted alkyl) radical, or else—a radical, R1 and R2=hydrogen or halogen or alkyl, alkyloxy, which is optionally substituted, alkylthio, alkyloxycarbonyl or else R1 and R2, at the ortho position with respect to one another, form an optionally substituted heterocycle containing 1 or 2 heteroatoms, R3 and R4=hydrogen or halogen or alkyl, alkenyl, alkyloxy, alkylthio, carboxyl or alkyloxycarbonyl, R5=hydrogen, alkyl, alkylthio, X=O or S or —NH—, —CO—, methylene, vinyldiyl, alkene-1,1-diyl or cycloalkane-1,1-diyl, and Y=O or S, in the racemic form, as well as the optical isomers (diastereomers and enantiomers) and the salts of the product of formula (I). The compounds of formula (I) are farnesyl transferase inhibitors which exhibit notable antitumor and antileukemic properties.

    摘要翻译： 式（I）的新型产物，其制备方法，含有它们的药物组合物及其在制备药物中的用途。在式（I）中，以下取代基是优选的：Ar表示取代或缩合的苯基或 多环或杂环芳族基团，R表示通式为（CH 2）m -X1（CH 2）n Z的基团，其中X1 =单键，O，S; m = 0,1， n = 0,1,2; CH2基可以被取代; Z代表羧基，COOR6（R6 =烷基），CON（R7）（R8）（R7 =氢或烷基，R8 =氢，羟基，芳基磺酰基，杂环基，任选取代的氨基，任选取代的烷氧基或任选取代的烷基），PO OR 9）2（R 9 =氢或烷基），-NH-CO-T（T =氢或任选取代的烷基）基团，或不相关的，R 1和R 2 =氢或卤素或烷基，烷氧基，其被任选取代 ，烷硫基，烷氧基羰基或其它R1和R2在相邻的邻位形成含有1或2个杂原子的任选取代的杂环，R 3和R 4 =氢或卤素或烷基，烯基，烷氧基，烷硫基，羧基或烷氧基羰基 ，R5 =氢，烷基，烷硫基，X = O或S或-NH-，-CO-，亚甲基，乙烯基二烯基，烯-1,1-二基或环烷烃-1,1-二基，Y = O或S， 外消旋形式，以及光学异构体（非对映异构体和对映体）和式（I）的产物的盐。 式（I）化合物是具有显着的抗肿瘤和抗白血病性质的法呢基转移酶抑制剂。