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21.
公开(公告)号:SI1268429T1
公开(公告)日:2004-12-31
申请号:SI200130167
申请日:2001-03-06
Applicant: SERVIER LAB
Inventor: CASARA PATRICK , PERRON-SIERRA FRANCOISE , ATASSI GHANEM , TUCKER GORDON , SAINT-DIZIER DOMINIQUE
IPC: A61K31/4164 , A61K31/4168 , A61K31/417 , A61K31/4184 , A61K31/426 , A61K31/4375 , A61K31/44 , A61K31/4402 , A61K31/505 , A61K31/55 , A61P9/00 , C07D233/24 , 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
Abstract: Compounds of formula (1):wherein:G represents an optionally substituted phenyl or optionally substituted heterocycle, G1 and G2 being N or C,T1 represents -CH2-CH2-, -CH=CH- or =CH-CH2-, and T2 is a bond, or T1 represents -CH2- or =CH- and T2 is -CH2-, =CH-,R5 represents -(CH2)m-COOR6,R6 and R6' represent hydrogen, alkyl, optionally substituted aryl or optionally substituted arylalkyl,A represents -CO-, -CH2-, =CH- or -CH= and W represents -CH-, =C- or -C=, or A represents -CO- or -CH2- and W represents N,X represents -CO-X1-, -CO-NR6-X1-, -NR6-CO-X1-, -O-X1-, -SO2-NR6-X1- or -S(O)n-X1-,Y represents -Y1-, -Y2-Y1- or -Y1-Y2-Y1-, Y1 being an alkylene, alkenylene or alkynylene, and Y2 being an arylene, heteroarylene, cycloalkylene or heterocycloalkylene,Z represents -Z1-, -Z10-NR6-, and -Z10-NR6-CO-, Z1 being a heteroaryl, heterocycloalkyl, heteroarylalkyl, heterocycloalkylalkyl, fused arylheteroaryl, fused arylheterocycloalkyl, fused heteroarylheterocycloalkyl, fused heterocycloalkylheteroaryl or fused heteroarylheteroaryl, each of which is optionally substituted, or a group,Z2-NR6 or Z2-NR6-CO, Z2 being a group Z1, alkyl or heteroalkyl, andZ10 represents Z1 or an alkyl,its enantiomers, diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid or base,and medicinal products containing the same which are useful as vitronectin receptor antagonists.
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公开(公告)号:EA005155B1
公开(公告)日:2004-12-30
申请号:EA200200878
申请日:2001-03-06
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
Abstract: Визобретенииописанысоединенияформулы (I)вкоторой G обозначаетфенильнуюгруппу, a Gи GобозначаютС, Тобозначает -СН-СН-, -СН=СН- или =СН-СН-, иТобозначаетсвязь, Rобозначаетгруппу -(СН)-COOR, Rобозначаетводород, алкил, арильнуюгруппу, котораяможетбытьзамещенной, илиарилалкильнуюгруппу, котораяможетбытьзамещенной, Аобозначает -СН- или =СН-, X обозначает -СО-Х-, -CO-NR-X-, -NR-CO-X-, -O-X-, -SO-NR-X- или -S(O)-X- , Y обозначает -Y-, -Y-Y- или -Y-Y-Y-, где Yобозначаеталкиленовую, алкениленовуюилиалкиниленовуюгруппуи Yобозначаетариленовую, гетероариленовую, циклоалкиленовуюилигетероциклоалкиленовуюгруппу, Z имеетзначения, указанныев формулеизобретения. Такжеописанымедицинскиепрепараты.
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公开(公告)号:PT1217002E
公开(公告)日:2004-11-30
申请号:PT01403333
申请日:2001-12-21
Applicant: SERVIER LAB
Inventor: NANTEUIL GUILLAUME DE , PIERRE ALAIN , PASTOUREAU PHILIPPE , TUCKER GORDON , SABATINI MASSIMO , BENOIST ALAIN , HICKMAN JOHN
IPC: C07D491/048 , A61K31/4433 , A61K31/444 , A61K31/541 , A61P9/10 , A61P19/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D405/14 , C07D417/14 , C07D491/04
Abstract: 5-Sulfonyl-2-(4-pyridinyl)-benzofuran, benzothiophene or indole derivatives (I), containing a hydroxamic acid function, are new. Benzofuran, benzothiophene or indole derivatives of formula (I) and their isomers, N-oxides and acid or base addition salts are new. R1 = H, halo, 1-6C alkyl or 1-6C alkoxy; X = O, S or NR; R = H or 1-6C alkyl; A = N-hydroxy-carboxamido-substituted tetrahydrofuropyridine, thiomorpholine or tetrahydropyranylmethyl group of formula (i)-(iii); Ra = H, halo, 1-6C alkyl or 1-6C alkoxy; Rb, Rc = H or 1-6C alkyl; and n = 0-2. An Independent claim is also included for the preparation of (I).
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公开(公告)号:BR0300698A
公开(公告)日:2004-09-08
申请号:BR0300698
申请日:2003-03-18
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 , C07D403/10
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).
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公开(公告)号:FR2819509B1
公开(公告)日:2004-04-16
申请号:FR0100641
申请日:2001-01-18
Applicant: SERVIER LAB
Inventor: CASARA PATRICK , LE DIGUARHER THIERRY , DOREY GILBERT , HICKMAN JOHN , PIERRE ALAIN , TUCKER GORDON , GUILBAUD NICOLAS
IPC: C07C317/00 , A61K31/4164 , A61K31/417 , A61K31/4178 , A61K31/4406 , A61K31/4409 , A61K31/454 , A61P9/00 , A61P9/10 , A61P25/00 , A61P35/00 , C07D213/36 , C07D213/38 , C07D213/57 , C07D233/54 , C07D233/58 , C07D233/61 , C07D233/64 , C07D401/06 , C07D213/04 , A61K31/4174 , A61K31/44
Abstract: Compound of formula (I):wherein:X represents a bond or alkylene, CO, S(O)n, -S(O)n-A1-, -CO-A1-, -A-S(O)n-A'1- or -A1-CO-A'1-,Y represents aryl, heteroaryl, cycloalkyl or heterocycloalkyl, each unsubstituted or substituted,R1, R2, R3 and R4 each independently of the others represent hydrogen or aryl, heteroaryl, cycloalkyl or heterocycloalkyl, each unsubstituted or substituted,or R1, R2, R3 and R4, taken in pairs, together form a bond, or form a fused benzene ring or a fused aromatic or partially unsaturated heterocycle,T represents -CH(R5)-, -N(R5)- or -N(R5)CO-,V represents hydrogen or unsubstituted or substituted aryl or heteroaryl,A2 represents [C(R6)(R'6)]p,R7 and R8 are as defined in the description,their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as farnesyl transferase inhibitors.
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公开(公告)号:DE69907337T2
公开(公告)日:2004-02-26
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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公开(公告)号:FR2819510B1
公开(公告)日:2003-10-31
申请号:FR0100642
申请日:2001-01-18
Applicant: SERVIER LAB
Inventor: CASARA PATRICK , LE DIGUARHER THIERRY , DOREY GILBERT , HICKMAN JOHN , PIERRE ALAIN , TUCKER GORDON , GUILBAUD NICOLAS , FAUCHERE JEAN LUC , ORTUNO JEAN CLAUDE
IPC: A61P9/00 , A61P25/00 , A61P35/00 , C07D401/12 , C07D401/14 , C07D403/12 , A61K31/55 , C07D401/04
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公开(公告)号:ZA200302159B
公开(公告)日:2003-09-23
申请号:ZA200302159
申请日:2003-03-18
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 , C07D , A61K , A61P
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).
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公开(公告)号:NO20031219L
公开(公告)日:2003-09-19
申请号:NO20031219
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).
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公开(公告)号:AT238985T
公开(公告)日:2003-05-15
申请号:AT99402016
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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