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    New compounds derived from quinazoline, a process for their preparation and pharmaceutical compositions containing them
    72.
    发明专利
    New compounds derived from quinazoline, a process for their preparation and pharmaceutical compositions containing them 未知

    公开(公告)号：AU2003201326A1

    公开(公告)日：2003-10-02

    申请号：AU2003201326

    申请日：2003-03-18

    Applicant: SERVIER LAB

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

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

    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 DERIVATIVES OF QUINOSOLINE, METHOD OF PRODUCTION OF NEW DERIVATIVES OF QUINOSOLINE AND PHARMACEUTICAL PREPARATIONS
    73.
    发明专利
    NEW DERIVATIVES OF QUINOSOLINE, METHOD OF PRODUCTION OF NEW DERIVATIVES OF QUINOSOLINE AND PHARMACEUTICAL PREPARATIONS 未知

    公开(公告)号：PL359208A1

    公开(公告)日：2003-09-22

    申请号：PL35920803

    申请日：2003-03-17

    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

    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).

    74.
    发明专利
    未知

    公开(公告)号：PT979816E

    公开(公告)日：2003-08-29

    申请号：PT99402016

    申请日：1999-08-09

    Applicant: SERVIER LAB

    Inventor： HANESSIAN STEPHEN ,  CAIGNARD DANIEL-HENRI ,  TUCKER GORDON ,  ATASSI GHANEM ,  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).

    COMPUESTOS BICICLICOS ANTAGONISTAS DE LOS RECEPTORES DE LA VITRONECTINA, SU PROCEDIMIENTO DE PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN
    76.
    发明专利
    COMPUESTOS BICICLICOS ANTAGONISTAS DE LOS RECEPTORES DE LA VITRONECTINA, SU PROCEDIMIENTO DE PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN 未知

    公开(公告)号：AR029485A1

    公开(公告)日：2003-07-02

    申请号：ARP010101058

    申请日：2001-03-07

    Applicant: SERVIER LAB

    Inventor： CASARA PATRICK ,  PERRON-SIERRA FRANCOISE ,  ATASSI GHANEM ,  TUCKER GORDON ,  SAINT-DIZIER DOMINIQUE

    IPC: C07D233/24 ,  A61K31/4164 ,  A61K31/4168 ,  A61K31/417 ,  A61K31/4184 ,  A61K31/426 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/505 ,  A61K31/55 ,  A61P9/00 ,  A61P19/10 ,  A61P27/02 ,  A61P29/00 ,  A61P33/14 ,  A61P35/00 ,  A61P43/00 ,  C07D213/36 ,  C07D213/74 ,  C07D223/04 ,  C07D223/12 ,  C07D233/48 ,  C07D233/54 ,  C07D235/10 ,  C07D235/14 ,  C07D235/30 ,  C07D239/14 ,  C07D277/18 ,  C07D277/20 ,  C07D277/42 ,  C07D401/12 ,  C07D403/12 ,  C07D471/04 ,  A61K31/402

    Abstract: Compuestos de formula (1) en la cual: G representa un grupo fenilo o un grupo heterocíclico aromático o parcialmente insaturado, de 6 eslabones, que contiene de 1 a 2 heteroátomos elegidos entre nitrogeno y oxígeno, no substituido o substituido por R1, R2, R3 y/o R4; G1 y G2 representan independientemente, un átomo de carbono o de nitrogeno; -T1- representa un grupo elegido entre -CH2-CH2-, -CH=CH-, =CH-CH2-, y en ese caso, -T2- representa un enlace, o bien -T1- representa un grupo elegido entre -CH2- y -CH- y en ese caso -T2- representa un grupo -CH2-, =CH-, (a) o (b); R1, R2, R3 y R4, representan independientemente, un átomo de halogeno, un grupo alquilo, perhalogenoalquilo, ciano, nitro, OR7, NR6R6', COOR6, CONR6R6', COR6, S(O)nR6, siendo n igual a 0, 1 o 2; R5 representa un grupo -(CH2)m-COOR6; R6 y R6' representan independientemente, un átomo de hidrogeno, un grupo alquilo, arilo eventualmente substituido o arilalquilo eventualmente substituido; R7 representa un átomo de hidrogeno o un grupo alquilo; -W- representa un grupo -CH-, =C-, o -C= y -A- representa un grupo -CO-, -CH2-, =CH- o -CH=, o bien -W- representa un átomo de nitrogeno y -A- representa un grupo -CO- o -CH2-; -X- representa un grupo elegido entre -CO-X1-, -CO-NR6-X1-, -NR6-CO-X1-, -O-X1-, -SO2-NR6-X1-, y -S(O)n-X1-, en los cuales n está comprendido inclusivamente entre 0 y 2, y X1 representa un grupo alquileno; -Y- representa un grupo elegido entre -Y1-, -Y2-Y1- y -Y1-Y2-Y1-, en los cuales Y1 representa un grupo alquileno, alquenileno o alquinileno, e Y2 representa un grupo arileno, heteroarileno, cicloalquileno o heterocicloalquileno; Z- representa un grupo elegido entre Z1-, Z10-NR6-, y Z10-NR6-CO- en los cuales Z10 representa un grupo alquilo o Z1, y Z1 representa un grupo elegido entre Z2-, Z20-NR6-, Z20-NR6-CO-, o (c), en los cuales Z20 representa un grupo alquilo, heteroalquilo o Z2, y Z2 representa un grupo heteroarilo eventualmente substituido, heterocicloalquilo eventualmente substituido, heteroarilalquilo eventualmente substituido, heterocicloalquilalquilo eventualmente substituido, arilheteroarilo fusionado eventualmente substituido, arilheterocicloalquilo fusionado eventualmente substituido, heterocicloalquilheteroarilo fusionado eventualmente substituido, heteroarilheteroarilo fusionado eventualmente substituido, o cicloalquilheterocicloalquilo fusionado; y m es un entero comprendido en forma incluida entre 1 y 6. Estos compuestos son utiles en la preparacion de medicamentos.

    77.
    发明专利
    未知

    公开(公告)号：DE69907337D1

    公开(公告)日：2003-06-05

    申请号：DE69907337

    申请日：1999-08-09

    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

    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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