公开(公告)号：SI1092716T1

公开(公告)日：2005-06-30

申请号：SI200030642

申请日：2000-10-13

Applicant: SERVIER LAB

Inventor： DE NANTEUIL GUILLAUME ,  LILA CHRISTINE ,  VERBEUREN TONY ,  RUPIN ALAIN

IPC: A61K31/381 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/4709 ,  C07D333/64 ,  A61P7/02 ,  A61P7/04 ,  A61P43/00 ,  C07B61/00 ,  C07D333/58 ,  C07D333/60 ,  C07D401/06 ,  C07D409/06 ,  C07D409/14 ,  C07D521/00

Abstract: Benzothiophene, benzofuran and indole derivatives (I), their isomers and salts with acids and bases, their preparation, and pharmaceutical compositions containing them. Benzothiophene, benzofuran and indole derivatives of formula (I) are new: X = O, S, or NR3; R3 = H, 1-6C alkyl or acyl, aryl, aryl 1-6C alkyl, or heteroaryl 1-6C alkyl; Y' = O, S, NR3 or when X is N-heteroaryl alkyl, it may be a single bond; when T' is linked by a single bond it = N or C; when it is linked by a double bond, T' = C; A = a single bond, 1-6C alkylene optionally substituted as defined below, arylene, cycloalkylene, heterocycloalkylene, heteroarylene, -SO2-R4- linked to T' through the S atom; R4 = 1-6C alkylene, arylene, aralkylene, cycloalkylene, heterocycloalkylene, or heteroarylene; W' = OH, 1-6C alkoxy, aryloxy, aryl 1-6C alkoxy, cycloalkoxy, heterocycloalkoxy, heteroaryloxy, amino, hydroxyamino, or amino mono- or di substituted by alkyl, aryl, aralkyl, or cycloalkyl; U1 = O, S, or 1-6C alkylene in which 1 or more C atoms may be replaced by O, N, or S heteroatoms, and optionally substituted as defined below; V1 = arylene, heteroarylene, or heterocycloalkylene; U2 = a single bond, O, S, N, SO2, 1-6C alkylene in which 1 or more C atoms may be replaced by O, N, or S heteroatoms, and the N may be substituted by H or 1-6C alkyl; V2 = aryl, heteroaryl, or heterocycloalkyl; Ra, Rb, and Rc = H, halogen, OH, CN, NO2, 1-6C alkyl, alkoxy, or acyl, carboxy, alkoxycarbonyl, 1-6C trihaloalkyl, amino optionally substituted by 1 or 2 alkyl, aryl, or aralkyl groups, aryloxy, arylalkoxy, heteroaryloxy, heteroarylalkoxy, or a group of formula -U1-V1-U2-V2, or two of these groups together form methylenedioxy or ethylenedioxy optionally substituted; R1 = aryl optionally substituted as defined below, 1,3-dihydro-2H-indol-2-one, 3,4-dihydro-2(1H)-quinolone, 1-hydroxy-2(1H)pyridinone, or an optionally substituted heterocyclic group; R2 = H, 1-6C alkyl, aryl, aryl 1-6C alkyl, cycloalkyl, heterocycloalkyl, heterocycloalkyl alkyl, heteroaryl, or heteroaryl alkyl.

公开(公告)号：NO319101B1

公开(公告)日：2005-06-20

申请号：NO991957

申请日：1999-04-23

Applicant: SERVIER LAB

Inventor： NANTEUIL GUILLAUME DE ,  LILA CHRISTINE ,  VERBEUREN TONY ,  RUPIN ALAIN

IPC: A61K31/00 ,  A61K31/38 ,  A61K31/381 ,  A61K31/44 ,  C07D333/58 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/505 ,  A61K31/506 ,  A61P7/00 ,  A61P7/02 ,  A61P43/00 ,  C07D333/60 ,  C07D333/64 ,  C07D401/06 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D495/04 ,  C07D521/00

Abstract: Benzothiophene, benzofuran and indole derivatives (I) are new. Benzothiophene, benzofuran and indole derivatives of formula (I) and their salts are new: X = O, S or NR3; R3 = H, 1-6C alkyl, 1-6C acyl, aryl, 1-6C arylalkyl or 1-6C heteroarylalkyl; Y = O, S, NR3 or single bond when X is NR3 and R3 is 1-6C heteroarylalkyl; Z' = N when the bond to the carbon (i) is single, or C or CH when the bond is single or double; A = single bond, 1-6C alkylene (optionally substituted by one or more 1-6C alkyl, aryl, 1-6C arylalkyl, cycloalkyl or heterocyclic ring), arylene, cycloalkylene, heterocyclic ring or -SO2-R4- (Z' being bond to SO2); R4 = 1-6C alkylene, arylene, 1-6C arylalkylene, cycloalkylene or heterocyclic ring; W1 = OH, 1-6C alkoxy, aryloxy, 1-6C arylalkoxy, cycloalkyloxy, heterocyclic ring (bond to O or amino (optionally substituted by 1-6C alkyl, aryl, 1-6C arylalkyl or cycloalkyl) or hydroxyamino; Ra-Rd = H, halo, OH, CN, NO2, 1-6C alkyl, 1-6C alkoxy, 1-6C acyl, carboxy, 1-6C alkoxycarbonyl , 1-6C trihalogenated alkyl, amino (optionally substituted by one or two 1-6C alkyl) or 1-6C arylalkoxy; R1 = aryl (substituted by 1-5 halo, OH, CN, NO2, carboxy, 1-6C alkyl, 1-6C alkoxy, 1-6C trihalogenated alkyl, 1-6C trihalogenated alkoxy, amino (optionally substituted by one or two 1-6C alkyl (one optionally substituted by amino, 1-6C alkylamino or dialkylamino)), 1-6C arylalkoxy, 1-6C aminoalkoxy (amino optionally substituted by one or two 1-6C alkyl) or heteroaryl (optionally substituted); and R2 = H, 1-6C alkyl, aryl, 1-6C arylalkyl, cycloalkyl, heterocyclic ring, 1-6C alkyl-heterocyclic ring or, when Z' is C or CH, 1-6C alkylamino or 1-6C arylalkoxycarbonylamino; provided that Ra-Rd can not be all H. An Independent claim is also included for the preparation of (I).

公开(公告)号：ES2174579T3

公开(公告)日：2002-11-01

申请号：ES99401010

申请日：1999-04-26

Applicant: SERVIER LAB

Inventor： NANTEUIL GUILLAUME DE ,  LILA CHRISTINE ,  VERBEUREN TONY ,  RUPIN ALAIN

IPC: A61K31/00 ,  A61K31/38 ,  A61K31/381 ,  A61K31/44 ,  A61K31/4427 ,  C07D333/58 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/505 ,  A61K31/506 ,  A61P7/00 ,  A61P7/02 ,  A61P43/00 ,  C07D333/60 ,  C07D333/64 ,  C07D401/06 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D495/04 ,  C07D521/00

Abstract: Benzothiophene, benzofuran and indole derivatives (I) are new. Benzothiophene, benzofuran and indole derivatives of formula (I) and their salts are new: X = O, S or NR3; R3 = H, 1-6C alkyl, 1-6C acyl, aryl, 1-6C arylalkyl or 1-6C heteroarylalkyl; Y = O, S, NR3 or single bond when X is NR3 and R3 is 1-6C heteroarylalkyl; Z' = N when the bond to the carbon (i) is single, or C or CH when the bond is single or double; A = single bond, 1-6C alkylene (optionally substituted by one or more 1-6C alkyl, aryl, 1-6C arylalkyl, cycloalkyl or heterocyclic ring), arylene, cycloalkylene, heterocyclic ring or -SO2-R4- (Z' being bond to SO2); R4 = 1-6C alkylene, arylene, 1-6C arylalkylene, cycloalkylene or heterocyclic ring; W1 = OH, 1-6C alkoxy, aryloxy, 1-6C arylalkoxy, cycloalkyloxy, heterocyclic ring (bond to O or amino (optionally substituted by 1-6C alkyl, aryl, 1-6C arylalkyl or cycloalkyl) or hydroxyamino; Ra-Rd = H, halo, OH, CN, NO2, 1-6C alkyl, 1-6C alkoxy, 1-6C acyl, carboxy, 1-6C alkoxycarbonyl , 1-6C trihalogenated alkyl, amino (optionally substituted by one or two 1-6C alkyl) or 1-6C arylalkoxy; R1 = aryl (substituted by 1-5 halo, OH, CN, NO2, carboxy, 1-6C alkyl, 1-6C alkoxy, 1-6C trihalogenated alkyl, 1-6C trihalogenated alkoxy, amino (optionally substituted by one or two 1-6C alkyl (one optionally substituted by amino, 1-6C alkylamino or dialkylamino)), 1-6C arylalkoxy, 1-6C aminoalkoxy (amino optionally substituted by one or two 1-6C alkyl) or heteroaryl (optionally substituted); and R2 = H, 1-6C alkyl, aryl, 1-6C arylalkyl, cycloalkyl, heterocyclic ring, 1-6C alkyl-heterocyclic ring or, when Z' is C or CH, 1-6C alkylamino or 1-6C arylalkoxycarbonylamino; provided that Ra-Rd can not be all H. An Independent claim is also included for the preparation of (I).

公开(公告)号：PT955299E

公开(公告)日：2002-07-31

申请号：PT99401010

申请日：1999-04-26

Applicant: SERVIER LAB

Inventor： NANTEUIL GUILLAUME DE ,  VERBEUREN TONY ,  RUPIN ALAIN ,  LILA CHRISTINE

IPC: A61K31/00 ,  A61K31/38 ,  A61K31/381 ,  A61K31/44 ,  A61K31/4427 ,  C07D333/58 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/505 ,  A61K31/506 ,  A61P7/00 ,  A61P7/02 ,  A61P43/00 ,  C07D333/60 ,  C07D333/64 ,  C07D401/06 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D495/04 ,  C07D521/00

Abstract: Benzothiophene, benzofuran and indole derivatives (I) are new. Benzothiophene, benzofuran and indole derivatives of formula (I) and their salts are new: X = O, S or NR3; R3 = H, 1-6C alkyl, 1-6C acyl, aryl, 1-6C arylalkyl or 1-6C heteroarylalkyl; Y = O, S, NR3 or single bond when X is NR3 and R3 is 1-6C heteroarylalkyl; Z' = N when the bond to the carbon (i) is single, or C or CH when the bond is single or double; A = single bond, 1-6C alkylene (optionally substituted by one or more 1-6C alkyl, aryl, 1-6C arylalkyl, cycloalkyl or heterocyclic ring), arylene, cycloalkylene, heterocyclic ring or -SO2-R4- (Z' being bond to SO2); R4 = 1-6C alkylene, arylene, 1-6C arylalkylene, cycloalkylene or heterocyclic ring; W1 = OH, 1-6C alkoxy, aryloxy, 1-6C arylalkoxy, cycloalkyloxy, heterocyclic ring (bond to O or amino (optionally substituted by 1-6C alkyl, aryl, 1-6C arylalkyl or cycloalkyl) or hydroxyamino; Ra-Rd = H, halo, OH, CN, NO2, 1-6C alkyl, 1-6C alkoxy, 1-6C acyl, carboxy, 1-6C alkoxycarbonyl , 1-6C trihalogenated alkyl, amino (optionally substituted by one or two 1-6C alkyl) or 1-6C arylalkoxy; R1 = aryl (substituted by 1-5 halo, OH, CN, NO2, carboxy, 1-6C alkyl, 1-6C alkoxy, 1-6C trihalogenated alkyl, 1-6C trihalogenated alkoxy, amino (optionally substituted by one or two 1-6C alkyl (one optionally substituted by amino, 1-6C alkylamino or dialkylamino)), 1-6C arylalkoxy, 1-6C aminoalkoxy (amino optionally substituted by one or two 1-6C alkyl) or heteroaryl (optionally substituted); and R2 = H, 1-6C alkyl, aryl, 1-6C arylalkyl, cycloalkyl, heterocyclic ring, 1-6C alkyl-heterocyclic ring or, when Z' is C or CH, 1-6C alkylamino or 1-6C arylalkoxycarbonylamino; provided that Ra-Rd can not be all H. An Independent claim is also included for the preparation of (I).

公开(公告)号：PL198579B1

公开(公告)日：2008-06-30

申请号：PL34314700

申请日：2000-10-12

Applicant: SERVIER LAB

Inventor： DE NANTEUIL GUILLAUME ,  LILA CHRISTINE ,  VERBEUREN TONY ,  RUPIN ALAIN

IPC: A61K31/38 ,  C07D333/64 ,  A61K31/381 ,  C07D409/06 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/4709 ,  A61P7/00 ,  A61P7/02 ,  A61P7/04 ,  A61P43/00 ,  C07B61/00 ,  C07D333/58 ,  C07D333/60 ,  C07D401/06 ,  C07D409/14 ,  C07D521/00

公开(公告)号：NO320693B1

公开(公告)日：2006-01-16

申请号：NO20005166

申请日：2000-10-13

Applicant: SERVIER LAB

Inventor： NANTEUIL GUILLAUME DE ,  VERBEUREN TONY ,  RUPIN ALAIN ,  LILA CHRISTINE

IPC: C07D333/64 ,  A61K31/381 ,  C07D409/06 ,  A61K31/404 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/4709 ,  A61P7/02 ,  A61P7/04 ,  A61P43/00 ,  C07B61/00 ,  C07D333/52 ,  C07D333/58 ,  C07D333/60 ,  C07D401/06 ,  C07D409/14 ,  C07D521/00

Abstract: Benzothiophene, benzofuran and indole derivatives (I), their isomers and salts with acids and bases, their preparation, and pharmaceutical compositions containing them. Benzothiophene, benzofuran and indole derivatives of formula (I) are new: X = O, S, or NR3; R3 = H, 1-6C alkyl or acyl, aryl, aryl 1-6C alkyl, or heteroaryl 1-6C alkyl; Y' = O, S, NR3 or when X is N-heteroaryl alkyl, it may be a single bond; when T' is linked by a single bond it = N or C; when it is linked by a double bond, T' = C; A = a single bond, 1-6C alkylene optionally substituted as defined below, arylene, cycloalkylene, heterocycloalkylene, heteroarylene, -SO2-R4- linked to T' through the S atom; R4 = 1-6C alkylene, arylene, aralkylene, cycloalkylene, heterocycloalkylene, or heteroarylene; W' = OH, 1-6C alkoxy, aryloxy, aryl 1-6C alkoxy, cycloalkoxy, heterocycloalkoxy, heteroaryloxy, amino, hydroxyamino, or amino mono- or di substituted by alkyl, aryl, aralkyl, or cycloalkyl; U1 = O, S, or 1-6C alkylene in which 1 or more C atoms may be replaced by O, N, or S heteroatoms, and optionally substituted as defined below; V1 = arylene, heteroarylene, or heterocycloalkylene; U2 = a single bond, O, S, N, SO2, 1-6C alkylene in which 1 or more C atoms may be replaced by O, N, or S heteroatoms, and the N may be substituted by H or 1-6C alkyl; V2 = aryl, heteroaryl, or heterocycloalkyl; Ra, Rb, and Rc = H, halogen, OH, CN, NO2, 1-6C alkyl, alkoxy, or acyl, carboxy, alkoxycarbonyl, 1-6C trihaloalkyl, amino optionally substituted by 1 or 2 alkyl, aryl, or aralkyl groups, aryloxy, arylalkoxy, heteroaryloxy, heteroarylalkoxy, or a group of formula -U1-V1-U2-V2, or two of these groups together form methylenedioxy or ethylenedioxy optionally substituted; R1 = aryl optionally substituted as defined below, 1,3-dihydro-2H-indol-2-one, 3,4-dihydro-2(1H)-quinolone, 1-hydroxy-2(1H)pyridinone, or an optionally substituted heterocyclic group; R2 = H, 1-6C alkyl, aryl, aryl 1-6C alkyl, cycloalkyl, heterocycloalkyl, heterocycloalkyl alkyl, heteroaryl, or heteroaryl alkyl.

公开(公告)号：DK1092716T3

公开(公告)日：2005-05-17

申请号：DK00402831

申请日：2000-10-13

Applicant: SERVIER LAB

Inventor： DE NANTEUIL GUILLAUME ,  VERBEUREN TONY ,  RUPIN ALAIN ,  LILA CHRISTINE

IPC: C07D333/64 ,  A61K31/381 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/4709 ,  A61P7/02 ,  A61P7/04 ,  A61P43/00 ,  C07B61/00 ,  C07D333/58 ,  C07D333/60 ,  C07D401/06 ,  C07D409/06 ,  C07D409/14 ,  C07D521/00

Abstract: Benzothiophene, benzofuran and indole derivatives (I), their isomers and salts with acids and bases, their preparation, and pharmaceutical compositions containing them. Benzothiophene, benzofuran and indole derivatives of formula (I) are new: X = O, S, or NR3; R3 = H, 1-6C alkyl or acyl, aryl, aryl 1-6C alkyl, or heteroaryl 1-6C alkyl; Y' = O, S, NR3 or when X is N-heteroaryl alkyl, it may be a single bond; when T' is linked by a single bond it = N or C; when it is linked by a double bond, T' = C; A = a single bond, 1-6C alkylene optionally substituted as defined below, arylene, cycloalkylene, heterocycloalkylene, heteroarylene, -SO2-R4- linked to T' through the S atom; R4 = 1-6C alkylene, arylene, aralkylene, cycloalkylene, heterocycloalkylene, or heteroarylene; W' = OH, 1-6C alkoxy, aryloxy, aryl 1-6C alkoxy, cycloalkoxy, heterocycloalkoxy, heteroaryloxy, amino, hydroxyamino, or amino mono- or di substituted by alkyl, aryl, aralkyl, or cycloalkyl; U1 = O, S, or 1-6C alkylene in which 1 or more C atoms may be replaced by O, N, or S heteroatoms, and optionally substituted as defined below; V1 = arylene, heteroarylene, or heterocycloalkylene; U2 = a single bond, O, S, N, SO2, 1-6C alkylene in which 1 or more C atoms may be replaced by O, N, or S heteroatoms, and the N may be substituted by H or 1-6C alkyl; V2 = aryl, heteroaryl, or heterocycloalkyl; Ra, Rb, and Rc = H, halogen, OH, CN, NO2, 1-6C alkyl, alkoxy, or acyl, carboxy, alkoxycarbonyl, 1-6C trihaloalkyl, amino optionally substituted by 1 or 2 alkyl, aryl, or aralkyl groups, aryloxy, arylalkoxy, heteroaryloxy, heteroarylalkoxy, or a group of formula -U1-V1-U2-V2, or two of these groups together form methylenedioxy or ethylenedioxy optionally substituted; R1 = aryl optionally substituted as defined below, 1,3-dihydro-2H-indol-2-one, 3,4-dihydro-2(1H)-quinolone, 1-hydroxy-2(1H)pyridinone, or an optionally substituted heterocyclic group; R2 = H, 1-6C alkyl, aryl, aryl 1-6C alkyl, cycloalkyl, heterocycloalkyl, heterocycloalkyl alkyl, heteroaryl, or heteroaryl alkyl.

公开(公告)号：CY2223B1

公开(公告)日：2003-04-18

申请号：CY0100009

申请日：2001-05-17

Applicant: SERVIER LAB

Inventor： NANTEUIL DE GUILLAUME ,  GLOANEC PHILIPPE ,  LILA CHRISTINE ,  PORTEVIN BERNARD ,  VERBEUREN TONY ,  RUPIN ALAIN ,  SIMONET SERGE

IPC: A61K31/69 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  A61P43/00 ,  C07F5/02

Abstract: Boronic acid derivatives of formula (I), their isomers and their acid and base addition salts are new. R1, R2 = H or 1-6C alkyl; or CR1R2 = 3-8C cycloalkyl; R3 = H, 1-6C alkyl or phenyl or benzyl (both optionally substituted); R4 = heterocyclyl, amino, amidino, guanidino isothioureido iminomethylamino or mercapto (all optionally substituted); R5, R6 = H or 1-6C alkyl; or B(OR5)(OR6) = boronic ester of pinanediol; m = 0-6; n = 1-6; A1 = -CO-, -CS- or -SO2-; A = 5-10C bicycloalkyl-phenyl (optionally substituted) or -A2-N(R7)(R8), provided that m is not 0; A2 = -CO- or -CS-; R7, R8 = H, 1-6C alkyl (optionally substituted), 1-6C alkylsulphonyl, arylsulphonyl, aryl, heterocyclyl or 5-10C bicycloalkyl-phenyl (optionally substituted), indanyl or a group of formula (i) or (ii); Ra = 1-6C alkyl or phenyl (optionally substituted); Rb, Rc = H, halo, 1-6C alkyl, 1-6C alkoxy, hydroxy, optionally substituted amino or trihalomethyl.

公开(公告)号：AT214387T

公开(公告)日：2002-03-15

申请号：AT99401010

申请日：1999-04-26

Applicant: SERVIER LAB

Inventor： NANTEUIL GUILLAUME DE ,  LILA CHRISTINE ,  VERBEUREN TONY ,  RUPIN ALAIN

IPC: C07D333/58 ,  A61K31/00 ,  A61K31/38 ,  A61K31/381 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/505 ,  A61K31/506 ,  A61P7/00 ,  A61P7/02 ,  A61P43/00 ,  C07D333/60 ,  C07D333/64 ,  C07D401/06 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D495/04 ,  C07D521/00

Abstract: Benzothiophene, benzofuran and indole derivatives (I) are new. Benzothiophene, benzofuran and indole derivatives of formula (I) and their salts are new: X = O, S or NR3; R3 = H, 1-6C alkyl, 1-6C acyl, aryl, 1-6C arylalkyl or 1-6C heteroarylalkyl; Y = O, S, NR3 or single bond when X is NR3 and R3 is 1-6C heteroarylalkyl; Z' = N when the bond to the carbon (i) is single, or C or CH when the bond is single or double; A = single bond, 1-6C alkylene (optionally substituted by one or more 1-6C alkyl, aryl, 1-6C arylalkyl, cycloalkyl or heterocyclic ring), arylene, cycloalkylene, heterocyclic ring or -SO2-R4- (Z' being bond to SO2); R4 = 1-6C alkylene, arylene, 1-6C arylalkylene, cycloalkylene or heterocyclic ring; W1 = OH, 1-6C alkoxy, aryloxy, 1-6C arylalkoxy, cycloalkyloxy, heterocyclic ring (bond to O or amino (optionally substituted by 1-6C alkyl, aryl, 1-6C arylalkyl or cycloalkyl) or hydroxyamino; Ra-Rd = H, halo, OH, CN, NO2, 1-6C alkyl, 1-6C alkoxy, 1-6C acyl, carboxy, 1-6C alkoxycarbonyl , 1-6C trihalogenated alkyl, amino (optionally substituted by one or two 1-6C alkyl) or 1-6C arylalkoxy; R1 = aryl (substituted by 1-5 halo, OH, CN, NO2, carboxy, 1-6C alkyl, 1-6C alkoxy, 1-6C trihalogenated alkyl, 1-6C trihalogenated alkoxy, amino (optionally substituted by one or two 1-6C alkyl (one optionally substituted by amino, 1-6C alkylamino or dialkylamino)), 1-6C arylalkoxy, 1-6C aminoalkoxy (amino optionally substituted by one or two 1-6C alkyl) or heteroaryl (optionally substituted); and R2 = H, 1-6C alkyl, aryl, 1-6C arylalkyl, cycloalkyl, heterocyclic ring, 1-6C alkyl-heterocyclic ring or, when Z' is C or CH, 1-6C alkylamino or 1-6C arylalkoxycarbonylamino; provided that Ra-Rd can not be all H. An Independent claim is also included for the preparation of (I).

公开(公告)号：NZ507524A

公开(公告)日：2002-03-01

申请号：NZ50752400

申请日：2000-10-13

Applicant: SERVIER LAB

Inventor： DE NANTEUIL GUILLAUME ,  LILA CHRISTINE ,  VERBEUREN TONY ,  RUPIN ALAIN

IPC: A61K31/381 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  C07D333/64 ,  A61K31/47 ,  A61K31/4709 ,  A61P7/02 ,  A61P7/04 ,  A61P43/00 ,  C07B61/00 ,  C07D333/58 ,  C07D333/60 ,  C07D401/06 ,  C07D409/06 ,  C07D409/14 ,  C07D521/00 ,  C07D333/52 ,  C07D409/12 ,  A61K31/38

Abstract: In formula I: X is S, or an NR3 group, wherein R3 is H, (C1-6)alkyl, (C1-6)acyl, aryl, aryl-(C1-6)alkyl or heteroaryl-(C1-6)alkyl group; Y is O, T is CH or N when the bond that links it is a single bond, or a carbon atom if the bond is a double bond; A is a single bond or an optionally substituted (C1-6)alkylene, arylene, cycloalkylene, heterocycloalkylene, heteroarylene or an SO2R4 group, where R4 is (C1-6)alkylene, arylene, aryl-(C1-6)alkylene, cycloalkylene, heterocycloalkylene and heteroarylene; W is hydroxy, (C1-6)alkyoxy, aryloxy, aryl-(C1-6)alkyoxy, cycloalkoxy, heterocyloalkyoxy, heteraryloxy, amino and hydroxyamino; U1 is O, S or optionally substituted (C1-6)alkylene, wherein one or more of the carbon atoms may be optionally replaced by one or more hetero atoms selected from O, N and S; V1 is arylene, heteroarylene or heterocycloalkylene, U2 is a single bond, SO2, O, N or S, or an optionally substituted (C1-6)alkylene, wherein one or more of the carbon atoms may be optionally replaced by one or more hetero atoms selected from O, N and S; V2 is aryl, heteoaryl or heterocycloalkyl group; Ra, Rb and Rc are identical or different and represent a group selected from: - H, halogen; - hydroxy, cyano, nitro; - (C1-6)alkyl, (C1-6)alkoxy, (C1-6)acyl, carboxy, (C1-6)alkoxycarbonyl, (C1-6)trihaloalkyl; - optionally substituted amino; - aryloxy, aryl-(C1-6)alkoxy, heteroaryloxy, heteroaryl-(C1-6)alkoxy; - -U1-V1-U2-V2 (where U1, U2, V1 and V2 are as defined above); or - two of Ra, Rb and Rc together form an optionally substituted methylenedioxy or ethylenedioxy group, R1 is an optionally substituted phenyl, quinolyl or pridyl; and R2 is H, aryl or heteroaryl. The compounds of formula I may be used in pharmaceutical compositions for use as inhibitors of PAI-1, and to treat thrombosis and associated pathologies.