公开(公告)号：FR2850654A1

公开(公告)日：2004-08-06

申请号：FR0301181

申请日：2003-02-03

Applicant: SERVIER LAB

Inventor： GALLET SEBASTIEN ,  BERTHELOT PASCAL ,  LEBEGUE NICOLAS ,  FLOUQUET NATHALIE ,  CARATO PASCAL ,  HICKMAN JOHN ,  PIERRE ALAIN ,  PFEIFFER BRUNO ,  RENARD PIERRE

IPC: A61P35/00 ,  C07D513/04 ,  C07D515/04 ,  A61K31/554

Abstract: A compound of formula (I): wherein: represents benzo or pyrido, optionally fused in the 2-3, 3-4 or 4-5 position to a phenyl, (C 4 -C 8 )cycloalkyl or heterocyclic group, which may be optionally substituted, W represents X-Y or Y-X, wherein: X represents and Y represents oxygen or N-R 3 , n represents zero or an integer from 1 to 6, G, R 1 , R 2 and R 3 are as defined in the description, its enantiomers and diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same which are useful for the treatment of cancerous diseases.

公开(公告)号：BR0304575A

公开(公告)日：2004-07-20

申请号：BR0304575

申请日：2003-10-15

Applicant: SERVIER LAB

Inventor： PRUDHOMME MICHELLE ,  HUGON BERNADETTE ,  ANIZON FABRICE ,  HICKMAN JOHN ,  PIERRE ALAIN ,  GOLSTEYN ROY ,  RENARD PIERRE ,  PFEIFFER BRUNO

IPC: A61K31/40 ,  A61K31/407 ,  A61K31/437 ,  A61K31/7056 ,  A61K31/706 ,  A61P35/00 ,  A61P43/00 ,  C07D471/22 ,  C07D487/14 ,  C07D491/14 ,  C07D491/147 ,  C07H19/23 ,  C07D487/22 ,  C07D407/04

Abstract: (3,4-a:3,4-c) Carbazole derivatives (I), their enantiomers, diastereoisomers and salts with acids and bases. (3,4-a:3,4-c) Carbazole derivatives of formula (I), their enantiomers, diastereoisomers and salts with acids and bases A = ring that is saturated, partially, or fully unsaturated, and that may be aromatic; W' = phenyl or pyridinyl; Z' = U'-V', methylene dioxy or ethylenedioxy; U' = bond, 1-6C alkylene, 2-6C alkenylene, optionally substituted by 1 or 2 halo or OH groups; V' = H, halo, CN, NO2, azido, 1-6C alkyl or alkoxy, aryl, aralkyl, OH, aryloxy, arylalkoxy, formyl, COOH, NH2CO, NR3R4, -C(O)-T1, -C(O)-NR3-T1, NR3C(O)T1, -O-C(O)-T1, -C(O)-OT1, -NR3-T2-NR3R4, -NR3-T2-OR3, -NR3-T2-COOR3, -O-T'2-NR3R4, -O-T'2-OR3, -O-T'2-COOR3, or -S(O)t-R3; R3, R4 = H, 1-6C alkyl, aryl, aralkyl or together form 5-10 membered saturated mono or bicyclic heterocycle, optionally with a second hetero atom (O or N) and optionally substituted by alkyl, aryl, aralkyl, OH, alkoxy, amino mono- or dialkylamino; T1 = alkyl (optionally substituted by -OR3, -NR3R4, -COOR3, -C(O)R3, or -C(O)NR3R4), 2-6C alkenyl, optionally substituted; T2 = 1-6C alkylene; T'2 = 1-6C alkylene optionally substituted by one or more OH groups; t = 0, 1, or 2; Q1 = O or NR2; R2 = H, 1-6C alkyl, aryl, aralkyl, cycloalkyl, cycloalkyl alkyl, -OR3, -NR3R4, -O-T2-NR3R4, NR3-T2-NR3R4, mono- or di-hydroxyalkylamino, -C(O)R3, -NH-C(O)-R3, or 1-6C alkylene optionally substituted by halo, CN, NO2, -OR3, -NR3R4, -COOR3, -C(O)R3, hydroxyalkylamino, dihydroxyalkylamino, -C(O)-NHR3; Q2 = O or NR'2; R'2 = H, 1-6C alkyl, aryl, aralkyl, cycloalkyl, cycloalkyl alkyl, -OR3, -NR3R4, -O-T2-NR3R4, NR3-T2-NR3R4, mono- or di-hydroxyalkylamino, -C(O)R3, -NH-C(O)-R3, or 1-6C alkylene optionally substituted by halo, CN, NO2, -OR3, -NR3R4, -COOR3, -C(O)R3, hydroxyalkylamino, dihydroxyalkylamino, -C(O)-NHR3; X1 = H, OH, alkoxy, mercapto, alkylthio; Y1 = H or X1 and Y1 together form carbonyl or thiocarbonyl; X2 = H, OH, alkoxy, mercapto, alkylthio; Y2 = H or X2 and Y2 together form carbonyl or thiocarbonyl; X'1 = H, OH, alkoxy, mercapto, alkylthio; Y'1 = H or X'1 and Y'1 together form carbonyl or thiocarbonyl; X'2 = H, OH, alkoxy, mercapto, alkylthio; Y'2 = H or X'2 and Y'2 together form carbonyl or thiocarbonyl; R1 = H, 1-6C alkyl (optionally substituted by one or more OH, alkoxy, hydroxyalkoxy, or NR3R4 groups) or it is a group of formula (a); Ra - Rd = a bond, H, halo, OH, alkoxy, aryloxy, arylalkoxy, alkyl, aralkyl, aryl, -NR3R4, azido, -N=NR3, or -O-C(O)-R5; R5 = alkyl optionally substituted by one or more halo, OH, amino, mono- or dialkylamino, aryl, aralkyl, cycloalkyl, or heterocycloalkyl; Re = methylene or -U1-Ra; U1 = a bond or methylene; and n = 0 or 1. with the proviso that the following compounds are not within the scope of (I): 3b, 6a, 6b, 7-tetrahydro-1H-dipyrrolo(3,4-a:3,4-c) carbazole-1,3,4,6(2H, 3aH, 5H)-tetrone; 5-ethyl-3b, 6a, 6b, 7-tetrahydro-1H-dipyrrolo(3,4-a:3,4-c) carbazole-1,3,4,6(2H, 3aH, 5H)-tetrone; 3b, 6a, 7, 11c-tetrahydro-1H-dipyrrolo(3,4-a:3,4-c) carbazole-1,3,4,6(2H, 3aH, 5H)-tetrone; and 3b, 6a, 6b, 7-tetrahydrofuro(3,4a)pyrrolo(3,4-c) carbazole-1,3,4,6(2H, 3aH, 5H)-tetrone.

公开(公告)号：AU2003301531A1

公开(公告)日：2004-05-13

申请号：AU2003301531

申请日：2003-10-17

Applicant: SERVIER LAB

Inventor： LEPIFRE FRANCK ,  CAIGNARD DANIEL-HENRI ,  RENARD PIERRE ,  HICKMAN JOHN ,  PIERRE ALAIN ,  KRAUS-BERTHIER LAURENCE ,  COUDERT GERARD

IPC: A61P35/00 ,  C07D497/04 ,  C07D497/14 ,  C07D498/04 ,  A61K31/535 ,  C07D498/14 ,  C07D265/38

Abstract: Benzo(e)(1,4)oxazino(3,2-g)isoindole derivatives (I), and their enantiomers, diastereoisomers, N-oxides and addition salts with acids and bases are new. Benzo(e)(1,4)oxazino(3,2-g)isoindole derivatives of formula (I), and their enantiomers, diastereoisomers, N-oxides and addition salts with acids and bases are new W1 = atoms that complete phenyl or pyridyl; Z = hydrogen, halo, 1-6C alkyl or alkoxy (both optionally substituted by aryl), aryl, aryloxy or hydroxy; R1 = hydrogen, 1-6C alkyl, optionally substituted by aryl, aryl, COR5 or 1-6C alkylene, substituted by one or more of halo, cyano, OR6, NR6R7, COOR6, COR6 or CONHR6; R2 = hydrogen or -CH2CH2OR8; R3 and R4 = hydrogen, 1-6C alkyl, optionally substituted by aryl, or aryl, or together they complete a 5 or 6-membered, monocyclic heterocycle, optionally including an additional oxygen or nitrogen; n = 1-6; R5 = hydrogen, 1-6C alkyl or alkoxy, hydroxy, aryl, aryl(1-6C)alkyl or aryloxy; R6 and R7 = hydrogen, 1-6C alkyl, aryl(1-6C)alkyl or aryl, or together they complete a heterocycle as above; R8 = hydrogen, 1-6C alkyl, aryl, aryl(1-6C)alkyl, S(O)tR6 or -T1-R9; t = 0-2; T1 = 1-6C alkylene; R9 = halo, cyano, OR6, NR6R7, CHO, COOR6 or CONR6R7; and aryl = phenyl, naphthyl, di- or tetra-hydronaphthyl, indenyl or indanyl, all optionally substituted by one or more of halo, 1-6C (trihalo)alkyl or alkoxy, hydroxy or amino, optionally substituted by 1 or 2 1-6C alkyl. Independent claims are also included for the following:0041658 (1) methods for the preparation of (I); and (2) intermediates of formulae (X), (XI) and (XIV). Boc = tert-butoxycarbonyl; and Pg = Boc or phenoxycarbonyl.

公开(公告)号：AU772609B2

公开(公告)日：2004-05-06

申请号：AU7168300

申请日：2000-11-17

Applicant: SERVIER LAB

Inventor： LAVIELLE GILBERT ,  HAUTEFAYE PATRICK ,  PIERRE ALAIN ,  ATASSI GHANEM ,  HICKMAN JOHN ,  CIMETIERE BERNARD

IPC: C07D491/22 ,  A61K31/4375 ,  A61K31/4745 ,  A61P35/00 ,  C07D401/02 ,  C07D471/14 ,  C07D471/04 ,  A61K31/407

Abstract: Camptothecin analogs (I), their enantiomers, diastereoisomers, and salts with acids and bases are new. Camptothecin analogs of formula (I), their enantiomers, diastereoisomers, and salts are new. n = 0-2; R1-R5 = H, halogen, alkyl, alkenyl, alkynyl, perhaloalkyl, 3-11C cycloalkyl, 3-11C cycloalkyl-alkyl, OH, hydroxyalkyl, alkoxy, alkoxyalkyl, alkoxycarbonyl, acyloxy, NO2, CN, aminocarbonyl (optionally substituted on the N by one or two alkyl groups), -(CH2)p-NRaRb, or -O-CO- NRaRb; or two adjacent groups of R2-R5 = -O-(CH2)t-O-; p = 0 - 6; Ra, Rb = H, alkyl, 3-11C cycloalkyl, 3-11C cycloalkyl-alkyl, acyl, optionally substituted aryl or optionally substituted arylalkyl; or NRaRb = pyrrolyl, piperidinyl, or piperazinyl each of the cyclic groups being optionally substituted; t = 1-3; R60, R70n, R80, and R90 = H, OH, alkoxy, or -O-CO-X or -O-CO-NXW; X, W = alkyl, alkenyl, alkynyl, 3-11C cycloalkyl, 3-11C cycloalkyl-alkyl, optionally substituted aryl, or optionally substituted aryl alkyl; R61, R71n, R81, and R91 = H, alkyl, alkenyl or alkynyl; or vicinal pairs may together form a bond or an oxirane group; or R60+R61, R70n+R71n, R80+R81n and/or R90+R91 = oxo or -O-(CH2)t1-O-; t1 = 1-3 with the proviso that R60, R70n, R80, R90, R61, R71n, R81, and R91 are not all H. Alkyl, alkoxy and acyl groups have 1-6C; alkenyl have 2-6C and 1-3 double bonds; alkynyl have 2-6C and 1-3 triple bonds; aryl = phenyl or naphthyl; 'substituted' on aryl or aryl alkyl groups means by one or more halogens, alkyl, alkoxy, OH, CN, NO2, amino or mono- or dialkylamino groups; 'substituted' on heterocyclic groups means by one or more alkyl, alkoxy, aryl, aryl alkyl, aryloxy and/or aryloxy alkyl groups. An Independent claim is included for the preparation of (I).

公开(公告)号：AU2003254746A1

公开(公告)日：2004-05-06

申请号：AU2003254746

申请日：2003-10-16

Applicant: SERVIER LAB

Inventor： PFEIFER BRUNO ,  RENARD PIERRE ,  GOLSTEYN ROY ,  PIERRE ALAIN ,  HICKMAN JOHN ,  ANIZON FABRICE ,  HUGON BERNADETTE ,  PRUDHOMME MICHELLE

IPC: A61K31/40 ,  A61K31/407 ,  A61K31/437 ,  A61K31/7056 ,  A61K31/706 ,  A61P35/00 ,  A61P43/00 ,  C07D471/22 ,  C07D487/14 ,  C07D491/14 ,  C07D491/147 ,  C07H19/23 ,  A61K31/5365 ,  C07H5/04 ,  C07D491/22 ,  C07D487/22

Abstract: (3,4-a:3,4-c) Carbazole derivatives (I), their enantiomers, diastereoisomers and salts with acids and bases. (3,4-a:3,4-c) Carbazole derivatives of formula (I), their enantiomers, diastereoisomers and salts with acids and bases A = ring that is saturated, partially, or fully unsaturated, and that may be aromatic; W' = phenyl or pyridinyl; Z' = U'-V', methylene dioxy or ethylenedioxy; U' = bond, 1-6C alkylene, 2-6C alkenylene, optionally substituted by 1 or 2 halo or OH groups; V' = H, halo, CN, NO2, azido, 1-6C alkyl or alkoxy, aryl, aralkyl, OH, aryloxy, arylalkoxy, formyl, COOH, NH2CO, NR3R4, -C(O)-T1, -C(O)-NR3-T1, NR3C(O)T1, -O-C(O)-T1, -C(O)-OT1, -NR3-T2-NR3R4, -NR3-T2-OR3, -NR3-T2-COOR3, -O-T'2-NR3R4, -O-T'2-OR3, -O-T'2-COOR3, or -S(O)t-R3; R3, R4 = H, 1-6C alkyl, aryl, aralkyl or together form 5-10 membered saturated mono or bicyclic heterocycle, optionally with a second hetero atom (O or N) and optionally substituted by alkyl, aryl, aralkyl, OH, alkoxy, amino mono- or dialkylamino; T1 = alkyl (optionally substituted by -OR3, -NR3R4, -COOR3, -C(O)R3, or -C(O)NR3R4), 2-6C alkenyl, optionally substituted; T2 = 1-6C alkylene; T'2 = 1-6C alkylene optionally substituted by one or more OH groups; t = 0, 1, or 2; Q1 = O or NR2; R2 = H, 1-6C alkyl, aryl, aralkyl, cycloalkyl, cycloalkyl alkyl, -OR3, -NR3R4, -O-T2-NR3R4, NR3-T2-NR3R4, mono- or di-hydroxyalkylamino, -C(O)R3, -NH-C(O)-R3, or 1-6C alkylene optionally substituted by halo, CN, NO2, -OR3, -NR3R4, -COOR3, -C(O)R3, hydroxyalkylamino, dihydroxyalkylamino, -C(O)-NHR3; Q2 = O or NR'2; R'2 = H, 1-6C alkyl, aryl, aralkyl, cycloalkyl, cycloalkyl alkyl, -OR3, -NR3R4, -O-T2-NR3R4, NR3-T2-NR3R4, mono- or di-hydroxyalkylamino, -C(O)R3, -NH-C(O)-R3, or 1-6C alkylene optionally substituted by halo, CN, NO2, -OR3, -NR3R4, -COOR3, -C(O)R3, hydroxyalkylamino, dihydroxyalkylamino, -C(O)-NHR3; X1 = H, OH, alkoxy, mercapto, alkylthio; Y1 = H or X1 and Y1 together form carbonyl or thiocarbonyl; X2 = H, OH, alkoxy, mercapto, alkylthio; Y2 = H or X2 and Y2 together form carbonyl or thiocarbonyl; X'1 = H, OH, alkoxy, mercapto, alkylthio; Y'1 = H or X'1 and Y'1 together form carbonyl or thiocarbonyl; X'2 = H, OH, alkoxy, mercapto, alkylthio; Y'2 = H or X'2 and Y'2 together form carbonyl or thiocarbonyl; R1 = H, 1-6C alkyl (optionally substituted by one or more OH, alkoxy, hydroxyalkoxy, or NR3R4 groups) or it is a group of formula (a); Ra - Rd = a bond, H, halo, OH, alkoxy, aryloxy, arylalkoxy, alkyl, aralkyl, aryl, -NR3R4, azido, -N=NR3, or -O-C(O)-R5; R5 = alkyl optionally substituted by one or more halo, OH, amino, mono- or dialkylamino, aryl, aralkyl, cycloalkyl, or heterocycloalkyl; Re = methylene or -U1-Ra; U1 = a bond or methylene; and n = 0 or 1. with the proviso that the following compounds are not within the scope of (I): 3b, 6a, 6b, 7-tetrahydro-1H-dipyrrolo(3,4-a:3,4-c) carbazole-1,3,4,6(2H, 3aH, 5H)-tetrone; 5-ethyl-3b, 6a, 6b, 7-tetrahydro-1H-dipyrrolo(3,4-a:3,4-c) carbazole-1,3,4,6(2H, 3aH, 5H)-tetrone; 3b, 6a, 7, 11c-tetrahydro-1H-dipyrrolo(3,4-a:3,4-c) carbazole-1,3,4,6(2H, 3aH, 5H)-tetrone; and 3b, 6a, 6b, 7-tetrahydrofuro(3,4a)pyrrolo(3,4-c) carbazole-1,3,4,6(2H, 3aH, 5H)-tetrone.

公开(公告)号：CA2502515A1

公开(公告)日：2004-04-29

申请号：CA2502515

申请日：2003-10-14

Applicant: SERVIER LAB

Inventor： PFEIFFER BRUNO ,  RENARD PIERRE ,  PIERRE ALAIN ,  GOLSTEYN ROY ,  ANIZON FABRICE ,  HUGON BERNADETTE ,  HICKMAN JOHN ,  PRUDHOMME MICHELLE

IPC: A61P35/00 ,  C07D471/22 ,  C07D487/14 ,  C07D209/00 ,  C07D221/00 ,  C07D235/00 ,  A61K31/407 ,  A61K31/437

Abstract: Composés de formule (I): dans laquelle: Z représente un groupement de formul e U-V telle que définie dans la description, W1 représente, avec les atomes de carbone auxquels il est lié, un groupement phényle ou un groupement pyridinyle, W2 est tel que défini dans la description, X1, X2 représentent chacun un atome d'hydrogène, un groupement hydroxy, alkoxy, mercapto ou alkylthio, Y1, Y2 représentent chacun un atome d'hydrogène, ou X1 et Y1, X2 et Y2 représentent chacun un groupement choisi parmi atome d'hydrogène, groupement hydroxy, alkoxy (C1-C6) linéaire ou ramifié, mercapto, et alkylth io (C1-C6) linéaire ou ramifié, R1 est tel que défini dans la description, Q représente un atome d'oxygène ou un groupement NR2 tel que défini dans la description.

公开(公告)号：DK1103554T5

公开(公告)日：2004-04-26

申请号：DK00403255

申请日：2000-11-22

Applicant: SERVIER LAB

Inventor： HUSSON HENRI-PHILIPPE ,  GIORGI-RENAULT SYLVIANE ,  TRATRAT CHRISTOPHE ,  ATASSI GHANEM ,  PIERRE ALAIN ,  RENARD PIERRE ,  PFEIFFER BRUNO

IPC: C07D215/14 ,  A61K31/47 ,  A61K31/473 ,  A61K31/4741 ,  A61K31/4743 ,  A61K31/4745 ,  A61P35/00 ,  C07D219/06 ,  C07D221/06 ,  C07D221/16 ,  C07D221/18 ,  C07D491/04 ,  C07D491/044 ,  C07D491/048 ,  C07D491/056 ,  C07D491/14 ,  C07D491/147 ,  C07D491/153 ,  C07D491/16 ,  C07D491/22 ,  C07D495/04 ,  C07D495/14 ,  C07D495/16

Abstract: Tricyclic quinoline derivatives (I) are new. Tricyclic quinoline derivatives of formula (I) and their optical isomers, hydrates, solvates and acid-addition salts are new: R0 = H, OH or 1-6C alkoxy; R1, R2 = H, halogen, 1-6C alkyl, 1-6C alkoxy, OH, 1-6C polyhaloalkyl, NO2, NH2, mono- or di(1-6C alkyl)amino or 3- to 6-membered 1-azacycloalkyl, or together form a 5- to 12-membered mono- or bicyclic group optionally containing 1-2 heteroatoms selected from O, S and N; R3 = H or R4; R4 = aryl, heteroaryl or 3-8C cycloalkyl; 1-6C alkyl optionally substituted by aryl, heteroaryl, OH, 1-6C alkoxy or NR5R6; or COR7; R5, R6 = 1-6C alkyl or 1-6C hydroxyalkyl, or NR5R6 is a 5- to 7-membered saturated ring optionally containing 1-2 additional heteroatoms selected from O, S and N; R7 = aryl; 1-6C alkyl optionally substituted by NR5R6; amino optionally substituted by aryl, heteroaryl or optionally NR5R6-substituted 1-6C alkyl; or OR10; R10 = H, aryl or optionally NR5R6-substituted 1-6C alkyl; X = O, S, CH2 or CH2CH2; Ar = aryl, heteroaryl or aryl(1-6C)alkyl; aryl = phenyl, biphenylyl, naphthyl or tetrahydronaphthyl optionally substituted by halogen, 1-6C alkyl, OH, 1-6C alkoxy, 1-6C polyhaloalkyl, NH2, mono- or di(1-6C alkyl)amino, NO2, 1-6C acyl and/or 1-2C alkylenedioxy; heteroaryl = a 5- to 12-membered mono- or bicyclic aromatic group that contains 1-3 heteroatoms selected from O, S and N and is optionally substituted by halogen, 1-6C alkyl, OH, 1-6C alkoxy, 1-6C polyhaloalkyl, NH2 and/or mono- or di(1-6C alkyl)amino. Independent claims are also included for: (1) the preparation of (I) by reacting a compound of formula (II) with a compound of formula (III) to yield a compound of formula (Ia) which can then be reduced to form (Ib); (2) the one-pot preparation of (I) by reacting a compound of formula (II) with compounds of formulae (VIII) and (IX) to yield (Ia) which can then be reduced to form (Ib).

公开(公告)号：TR200400592T4

公开(公告)日：2004-04-21

申请号：TR200400592

申请日：2001-06-19

Applicant: SERVIER LAB

Inventor： MONNERET CLAUDE ,  BERTOUNESQUE EMMANUEL ,  MERESSE PHILIPPE ,  ATASSI GHANEM ,  PIERRE ALAIN ,  HICKMAN JOHN ,  PFEIFFER BRUNO ,  RENARD PIERRE

IPC: A61K31/36 ,  A61P35/00 ,  C07D493/04 ,  A61K31/365 ,  C07D4 ,  C07D

Abstract: A compound selected from these of formula (I):wherein:R1 represents hydrogen, alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkoxycarbonyl, aryloxycarbonyl, arylalkoxycarbonyl, heterocycloalkoxycarbonyl, alkylsulfonyl, arylsulfonyl, arylalkylsulfonyl or phosphono,R2 represents oxygen or sulphur,R3 represents hydrogen or alkyl, cycloalkyl or arylalkyl,X represents linear or branched (C1-C6)alkylene,R4 represents a group selected from amino optionally substituted by one or two groups, -N(R3)-X1-OR5 wherein R3, X1 and R5 are as defined in the description, -N(R3)-X1-NR6R7 wherein R3, X1, R6 and R7 are as defined in the description, hydroxy, alkoxy, aryloxy, -O-X1-OR5 wherein R5 and X1 are as defined in the description, and -O-X1-NR6R7 wherein R6, R7 and X1 are as defined in the description,its isomers, and also addition salts thereof with a pharmaceutically acceptable acid or base, and medical products containing the same which are useful in the treatment of cancer.

公开(公告)号：NO20034614A

公开(公告)日：2004-04-19

申请号：NO20034614

申请日：2003-10-15

Applicant: SERVIER LAB

Inventor： PIERRE ALAIN ,  RENARD PIERRE ,  PRUDHOMME MICHELLE ,  ANIZON FABRICE ,  HICKMAN JOHN ,  HUGON BERNADETTE ,  GOLSTEYN ROY ,  PFEIFFER BRUNO

IPC: A61K31/40 ,  A61K31/407 ,  A61K31/437 ,  A61K31/7056 ,  A61K31/706 ,  A61P35/00 ,  A61P43/00 ,  C07D471/22 ,  C07D487/14 ,  C07D491/14 ,  C07D491/147 ,  C07H19/23 ,  C07D487/04

CPC classification number: C07D487/14 ,  A61K9/0019 ,  C07D491/14 ,  C07H19/23

公开(公告)号：AT261975T

公开(公告)日：2004-04-15

申请号：AT01947525

申请日：2001-06-19

Applicant: SERVIER LAB

Inventor： MONNERET CLAUDE ,  BERTOUNESQUE EMMANUEL ,  MERESSE PHILIPPE ,  ATASSI GHANEM ,  PIERRE ALAIN ,  HICKMAN JOHN ,  PFEIFFER BRUNO ,  RENARD PIERRE

IPC: A61K31/36 ,  A61P35/00 ,  C07D493/04 ,  A61K31/365 ,  C07D317/00 ,  C07D307/00

Abstract: A compound selected from these of formula (I):wherein:R1 represents hydrogen, alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkoxycarbonyl, aryloxycarbonyl, arylalkoxycarbonyl, heterocycloalkoxycarbonyl, alkylsulfonyl, arylsulfonyl, arylalkylsulfonyl or phosphono,R2 represents oxygen or sulphur,R3 represents hydrogen or alkyl, cycloalkyl or arylalkyl,X represents linear or branched (C1-C6)alkylene,R4 represents a group selected from amino optionally substituted by one or two groups, -N(R3)-X1-OR5 wherein R3, X1 and R5 are as defined in the description, -N(R3)-X1-NR6R7 wherein R3, X1, R6 and R7 are as defined in the description, hydroxy, alkoxy, aryloxy, -O-X1-OR5 wherein R5 and X1 are as defined in the description, and -O-X1-NR6R7 wherein R6, R7 and X1 are as defined in the description,its isomers, and also addition salts thereof with a pharmaceutically acceptable acid or base, and medical products containing the same which are useful in the treatment of cancer.