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    New[3,4-a:3,4-c]carbazole compounds, a process for their preparation and pharmaceutical compositions containing them
    111.
    发明专利
    New[3,4-a:3,4-c]carbazole compounds, a process for their preparation and pharmaceutical compositions containing them 未知

    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.

    112.
    发明专利
    未知

    公开(公告)号：FR2846328A1

    公开(公告)日：2004-04-30

    申请号：FR0213194

    申请日：2002-10-23

    Applicant: SERVIER LAB

    Inventor： RAULT SYLVAIN ,  KOPP MARINA ,  LANCELOT JEAN CHARLES ,  LEMAITRE STEPHANE ,  CAIGNARD DANIEL HENRI ,  BIZOT ESPIARD JEAN GUY ,  RENARD PIERRE

    IPC: A61K31/381 ,  A61K31/402 ,  A61K31/417 ,  A61K31/4178 ,  A61K31/44 ,  A61K31/4439 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  C07D401/06 ,  C07D403/06 ,  C07D409/06 ,  A61K31/4025 ,  A61K31/4402

    Abstract: Imidazoline derivatives (I), their enantiomers, diastereoisomers, tautomers, and salts with acids and bases, are new. Imidazoline derivatives of formula (I), their enantiomers, diastereoisomers, tautomers, and salts with acids and bases, are new: R1 = heteroaryl optionally substituted by T1; R2 = cycloalkyl optionally substituted by T1; T1 = halogen, alkyl, alkoxy, OH, CN, NO2, (di)(alkyl)amino, COOH, COO-alkyl or CONH2-C(O)Rd; Rd = OH, alkoxy or amino; R4 , R5 = H, halogen, (polyhalo)alkyl, R10-C(X)-R11-, R10-Y-C(X)-R11-, R11-Y-R11-, or R10-S-(O)n-R11-; R11 = a bond, alkylene, alkenylene or alkynylene; X = O, S, or NR12; R3, R10, R12 = H or alkyl; Y = O, S or (alkyl)amino; and n = 1 or 2. Alkyl, alkoxy and alkylene have 1-6C, alkenylene have 2-6C and 1-3 double bonds, alkynylene have 2-6C and 1-3 triple bonds, polyhaloalkyl have 1-3C and 1-7 halogens, heteroaryl has 5 - 11 members and is mono or bicyclic with at least one aromatic ring and with 1-3 heteroatoms selected from O, N and S and may be substituted by an oxo group on a non-aromatic part of the structure, cycloalkyl has 3-10C, is mono or bicyclic and may have 1 or 2 unsaturations. An Independent claim is also included for the preparation of (I).

    114.
    发明专利
    未知

    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).

    115.
    发明专利
    未知

    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.

    118.
    发明专利
    未知

    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.

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