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    52.
    发明专利
    未知

    公开(公告)号：ES2198863T3

    公开(公告)日：2004-02-01

    申请号：ES99402016

    申请日：1999-08-09

    Applicant: SERVIER LAB

    Inventor： HANESSIAN STEPHEN ,  ATASSI GHANEM ,  TUCKER GORDON ,  CAIGNARD DANIEL-HENRI ,  RENARD PIERRE

    IPC: A61K31/18 ,  A61K31/185 ,  C12N9/99 ,  A61K31/35 ,  A61K31/351 ,  A61K31/4406 ,  A61K31/4418 ,  A61K31/445 ,  A61P43/00 ,  C07C319/14 ,  C07C319/20 ,  C07C323/60 ,  C07D211/20 ,  C07D213/34 ,  C07D309/04

    Abstract: Hydroxamic acid derivatives (I) are new. Hydroxamic acid derivatives of formula (I) and their acid and base addition salts are new. R1 = 1-6C alkyl (optionally substituted by at least one OH, halo, 1-6C alkoxy, mercapto, 1-6C alkylthio, aryl, 1-6C acyl or amino (optionally substituted by one or two 1-6C alkyl, cycloalkyl or aryl)), 1-6C acyl, cycloalkyl, aryl, heterocyclic group or aminocarbonyl-1-6C alkyl (with amino optionally substituted by one 1-6C alkyl (optionally substituted by at least one aryl, 1-6C arylalkyl, cycloalkyl or 1-6C alkylaminocarbonyl; R2 = 1-4C alkylene; R3 = X or T-U'-V'- X = 1-6C alkyl, 1-6C acyl, 1-6C alkoxycarbonyl, 1-6C aminoalkyl (amino optionally substituted by one or two 1-6C alkyl), 1-6C hydroxyalkyl, 1-6C carboxyalkyl, 1-6C aminocarbonylalkyl, 1-6C mercaptoalkyl, cycloalkyl, aryl or heterocyclic; T = aryl or heterocyclic; U' = single bond, S, O, NH, carbonyl, -R8O-, -R8S-, -R8NH-, -R8OR9-, -R8-NH-R9-, -R8-CO-R9- or -R9- (with R8 bound to T and R9 bound to V'); R8 = 1-6C alkylene; R9 = arylene or heteroarylene; V' = 1-6C alkylene; R4 = biaryl, arylheteroaryl, heteroarylaryl, 1-6C alkyl (optionally substituted by one heterocyclic group), cycloalkyl, aryl, 1-6C arylalkyl, cycloalkyl-1-6C alkyl or heterocyclic; and provided that R4 is 1-6C alkyl (optionally substituted by one heterocyclic group), cycloalkyl, aryl, 1-6C arylalkyl, cycloalkyl-1-6C alkyl or heterocyclic, when R3 is T-U'-V'-. An Independent claim is also included for the preparation of (I).

    New quinazoline derivatives are farnesyl transferase inhibitors, useful for treating cancer, restenosis following angioplasty or vascular surgery, and type 1 neurofibromatosis
    54.
    发明专利
    New quinazoline derivatives are farnesyl transferase inhibitors, useful for treating cancer, restenosis following angioplasty or vascular surgery, and type 1 neurofibromatosis 未知

    公开(公告)号：FR2837201A1

    公开(公告)日：2003-09-19

    申请号：FR0203299

    申请日：2002-03-18

    Applicant: SERVIER LAB

    Inventor： GOLDSTEIN SOLO ,  DHAINAUT ALAIN ,  TIZOT ANDRE ,  FAUCHERE JEAN LUC ,  KUCHARCZYK NATHALIE ,  HICKMAN JOHN ,  PIERRE ALAIN ,  TUCKER GORDON ,  KRAUS BERTHIER LAURENCE

    IPC: C07D401/06 ,  A61K31/517 ,  A61P9/00 ,  A61P25/00 ,  A61P35/00 ,  C07D401/14 ,  C07D403/06 ,  C07D407/14 ,  C07D409/14 ,  C07D521/00 ,  C07D403/14

    Abstract: Quinazoline derivatives (I) are new. Quinazoline derivatives of formula (I), their enantiomers, diastereomers and salts are new. A = bond, 1-6C alkylene, 2-6C alkenylene, 2-6C alkynylene, T, A1-T, T-A1, A1-T-A1, or A1-T-A'1-T'; T, T' = carbonyl, carbonyloxy, thio, sulfirylsulfonyl, oxy, amino, 1-6C aminoalkyl, aminoaryl, carbonylamino, carbonylamino-1-6C alkyl, carbonylaminoaryl, oxycarbonyl, aminocarbonyl, 1-6C aminoalkylcarbonyl, aminoarylcarbonyl, sulfonylamino, sulfonylamino-1-6C alkyl, sulfonylaminoaryl, aminosulfonyl, amino-1-6C alkylsulfonyl or aminoarylsulfonyl; A1, A'1 = 1-6C alkylene, 2-6C alkenylene or 2-6C alkynylene; B = 1-6C alkyl, aryl, 3-10C cycloalkyl, Het1, Het2, arylaminoaryl or aryl-1-6C alkylaryl (all optionally substituted by 1-3 Z); D = 1-6C alkylene (where 1 C atom may be substituted by B); X = O or S; Z, R1 = halo, 1-6C alkyl, 1-6C alkoxy, OH, SH, CN, NO2, NH2, 1-6C alkylamino, di-1-6C alkylamino, 1-4C perhaloalkyl, carboxy, 1-6C alkoxycarbonyl, aminocarbonyl, 1-6C alkylaminocarbonyl, di-1-6C alkylaminocarbonyl, carbamoyl or 1-6C alkoxycarbonylamino; R2 = H, or 1-6C alkyl, aryl, 3-10C cycloalkyl, Het1, Het2, aryl-1-6C alkyl or Het2-1-6C alkyl-3-10C cycloalkyl-1-6C alkyl or Het1-1-6C alkyl (all optionally substituted by halo, 1-6C alkyl, 1-6C alkoxy, OH, SH, CN, NO2, NH2, 1-6C alkylamino, di-1-6C alkylamino, 1-4C perhaloalkyl, carboxy, 1-6C alkoxycarbonyl, aminocarbonyl, 1-6C alkylaminocarbonyl, di-1-6C alkylaminocarbonyl, carbamoyl, 1-6C alkoxycarbonylamino, or aryl-1-6C alkyl or arylamino (both optionally substituted by 1-3 Z)); aryl = phenyl, naphthyl or biphenyl; Het1 = 5-7 membered saturated or partially unsaturated mono- or polycyclic heterocycloalkyl containing 1-3 N, O or S atoms; Het2 = 5-11 membered mono- or bicyclic aromatic ring containing 1-3 N, O or S; m = 0-4; and n = 0-3; provided that when the 2 N atoms of the imidazol ring are substituted, the imidazole moiety becomes a cationic imidazolium moiety. An Independent claim is also included for the preparation of (I).

    New hydroxamic acid compounds, a process for their preparation and pharmaceutical compositions containing them
    59.
    发明专利
    New hydroxamic acid compounds, a process for their preparation and pharmaceutical compositions containing them 未知

    公开(公告)号：AU750691B2

    公开(公告)日：2002-07-25

    申请号：AU4346699

    申请日：1999-08-10

    Applicant: SERVIER LAB

    Inventor： HANESSIAN STEPHEN ,  ATASSI GHANEM ,  TUCKER GORDON ,  CAIGNARD DANIEL-HENRI ,  RENARD PIERRE

    IPC: C12N9/99 ,  A61K31/18 ,  A61K31/185 ,  A61K31/35 ,  A61K31/351 ,  A61K31/4406 ,  A61K31/4418 ,  A61K31/445 ,  A61P43/00 ,  C07C319/14 ,  C07C319/20 ,  C07C323/60 ,  C07D211/20 ,  C07D213/34 ,  C07D309/04 ,  C07D213/56 ,  C07D309/32 ,  C07C323/67

    Abstract: Hydroxamic acid derivatives (I) are new. Hydroxamic acid derivatives of formula (I) and their acid and base addition salts are new. R1 = 1-6C alkyl (optionally substituted by at least one OH, halo, 1-6C alkoxy, mercapto, 1-6C alkylthio, aryl, 1-6C acyl or amino (optionally substituted by one or two 1-6C alkyl, cycloalkyl or aryl)), 1-6C acyl, cycloalkyl, aryl, heterocyclic group or aminocarbonyl-1-6C alkyl (with amino optionally substituted by one 1-6C alkyl (optionally substituted by at least one aryl, 1-6C arylalkyl, cycloalkyl or 1-6C alkylaminocarbonyl; R2 = 1-4C alkylene; R3 = X or T-U'-V'- X = 1-6C alkyl, 1-6C acyl, 1-6C alkoxycarbonyl, 1-6C aminoalkyl (amino optionally substituted by one or two 1-6C alkyl), 1-6C hydroxyalkyl, 1-6C carboxyalkyl, 1-6C aminocarbonylalkyl, 1-6C mercaptoalkyl, cycloalkyl, aryl or heterocyclic; T = aryl or heterocyclic; U' = single bond, S, O, NH, carbonyl, -R8O-, -R8S-, -R8NH-, -R8OR9-, -R8-NH-R9-, -R8-CO-R9- or -R9- (with R8 bound to T and R9 bound to V'); R8 = 1-6C alkylene; R9 = arylene or heteroarylene; V' = 1-6C alkylene; R4 = biaryl, arylheteroaryl, heteroarylaryl, 1-6C alkyl (optionally substituted by one heterocyclic group), cycloalkyl, aryl, 1-6C arylalkyl, cycloalkyl-1-6C alkyl or heterocyclic; and provided that R4 is 1-6C alkyl (optionally substituted by one heterocyclic group), cycloalkyl, aryl, 1-6C arylalkyl, cycloalkyl-1-6C alkyl or heterocyclic, when R3 is T-U'-V'-. An Independent claim is also included for the preparation of (I).

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