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    Farnesyl transferase inhibitors, their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments
    34.
    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

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

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

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

    CPC classification number: C07D209/56

    Abstract: 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.

    Abstract translation: 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。

    Pyrrole derivatives, and pharmaceutical compositions which contain them and pharmacological methods of use
    36.
    发明授权
    Pyrrole derivatives, and pharmaceutical compositions which contain them and pharmacological methods of use 失效
    吡咯衍生物和含有它们的药物组合物和药理学方法

    公开(公告)号：US4960779A

    公开(公告)日：1990-10-02

    申请号：US360122

    申请日：1989-06-01

    Applicant: Jean-Dominique Bourzat ,  Marc Capet ,  Claude Cotrel ,  Richard Labaudiniere ,  Philippe Pitchen ,  Gerard Roussel

    Inventor： Jean-Dominique Bourzat ,  Marc Capet ,  Claude Cotrel ,  Richard Labaudiniere ,  Philippe Pitchen ,  Gerard Roussel

    IPC: C07D209/46 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/47 ,  A61K31/495 ,  A61P21/02 ,  A61P25/08 ,  A61P25/20 ,  C07D221/12 ,  C07D401/04 ,  C07D401/14 ,  C07D471/04 ,  C07D519/00

    CPC classification number: C07D401/04 ,  C07D471/04

    Abstract: Pyrrole derivatives of formula (I): ##STR1## in which A forms with the pyrrole ring an isoindoline, 6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine, 2,3,6,7-tetrahydro-5H-[1,4]oxathiino[2,3-c]pyrrole or 2,3,6,7-tetrahydro-5H-[1,4]dithiino[2,3-c]pyrrole ring-system, Het.dbd.naphthyridinyl, pyridyl or quinolyl which are unsubstituted or substituted with halogen, (1 to 4 C) alkyl, (1 to 4 C) alkyloxy, (1 to 4 C) alkylthio or CF.sub.3, Y.dbd.CO, C.dbd.NOH or CHOH and R.dbd.(3 to 10 C) alkenyl, alkyl which is unsubstituted or substituted with OH, alkyloxy, alkylthio, (3 to 6 C) cycloalkyl, NH.sub.2, alkylamino, dialkylamino, alkylcarbonylamino, piperazinyl, piperidyl, 1-azetidinyl, morpholino, pyrrolidinyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, (1-piperazinyl)carbonyl, piperidinocarbonyl, pyrrolidinocarbonyl, phenyl, pyridyl, 1-imidazolyl or alternatively R.dbd.2- or 3-pyrrolididnyl, 2-, 3- or 4-piperidyl, (3 to 6 C) cycloalkyl or phenyl which is unsubstituted or substituted with halogen, (1 to 4 C) alkyl, (1 to 4 C) alkyloxy, (1 to 4 C) alkylthio, the said alkyl radicals and portions containing, except where specifically stated, 1 to 10 C, and the piperazinyl, piperidino, piperidyl, pyrrolidinyl, azetidinyl radicals being unsubstituted or substituted at any position by alkyl, alkylcarbonyl, benzyl or hydroxyalkyl, or can alternatively form a lactam group with the nitrogen atom of the ring, and their salts and optical isomers are useful as anxiolytics.

    Abstract translation: 式（I）的吡咯衍生物：其中A与吡咯环形成异吲哚啉，6,7-二氢-5H-吡咯并[3,4-b]吡嗪，2,3,6,7 - 四氢-5H- [1,4]氧硫杂环[2,3-c]吡咯或2,3,6,7-四氢-5H- [1,4]二噻唑并[2,3-c]吡咯环体系， Het =未被取代或被卤素取代的（1-4C）烷基，（1-4C）烷氧基，（1-4C）烷硫基或CF3，Y = CO，C = NOH或CHOH的萘啶基，吡啶基或喹啉 （3〜6）环烷基，NH 2，烷基氨基，二烷基氨基，烷基羰基氨基，哌嗪基，哌啶基，1-氮杂环丁烷基，吗啉代，吗啉代， 吡咯烷基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，（1-哌嗪基）羰基，哌啶子基羰基，吡咯烷基羰基，苯基，吡啶基，1-咪唑基或R = 2-或3-吡咯烷二基，2-，3-或4-哌啶基 6 C）未被取代或被卤素取代的环烷基或苯基，（1-4C）烷基，（1-4C） 烷氧基，（1〜4个C）烷硫基，所述烷基及其部分除特别说明为1-10个以外，其中哌嗪基，哌啶子基，哌啶基，吡咯烷基，氮杂环丁烷基在任意位置未被取代或被烷基取代， 烷基羰基，苄基或羟基烷基，或者可以与环的氮原子形成内酰胺基，其盐和旋光异构体可用作抗焦虑剂。

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