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    NEW CARBAZOLE COMPOUNDS [3,4-A:3,4-C], METHOD OF MANUFACTURE OF NEW CARBAZOLE COMPOUNDS [3,4-A:3,4-C] AS WELL AS COMPOUND PHARMACEUTICALS CONTAINING THEM
    1.
    发明专利
    NEW CARBAZOLE COMPOUNDS [3,4-A:3,4-C], METHOD OF MANUFACTURE OF NEW CARBAZOLE COMPOUNDS [3,4-A:3,4-C] AS WELL AS COMPOUND PHARMACEUTICALS CONTAINING THEM 未知

    公开(公告)号：PL362885A1

    公开(公告)日：2004-04-19

    申请号：PL36288503

    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 ,  C07D487/04

    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.

    DERIVADOS (3,4-A:3,4-C) CARBAZOL, PROCEDIMIENTO PARA SU PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN.
    3.
    发明专利
    DERIVADOS (3,4-A:3,4-C) CARBAZOL, PROCEDIMIENTO PARA SU PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN. 未知

    公开(公告)号：ES2240927T3

    公开(公告)日：2005-10-16

    申请号：ES03292545

    申请日：2003-10-14

    Applicant: SERVIER LAB

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

    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

    Abstract: Compuestos de fórmula (I): **(Fórmula)** donde: ¿ A representa un ciclo saturado, parcial o totalmente insaturado que puede, si es el caso, conferir un carácter aromático al ciclo, ¿ W1 representa, junto con los átomos de carbono a los cuales está unido, un grupo fenilo o un grupo piridinilo, ¿ Z representa uno o varios grupos idénticos o diferentes de fórmula U-V en la cual: U representa un enlace simple, una cadena alquileno de 1 a 6 carbonos lineal o ramificada o una cadena alquenilo de 2 a 6 carbonos lineal o ramificada, eventualmente sustituida con uno o varios grupos, idénticos o diferentes, seleccionados entre halógeno e hidroxilo, y/o que presenta eventualmente una o varias insaturaciones, V representa un grupo seleccionado entre átomos de hidrógeno, de halógeno, un grupo ciano, nitro, azido, alquilo de 1 a 6 carbonos lineal o ramificado, arilo, arilalquilo de 1 a 6 carbonos lineal o ramificado, hidroxilo, alcoxi de 1 a 6 carbonos lineal o ramificado, ariloxi, arilalcoxi de 1 a 6 carbonos lineal o ramificado, formilo, carboxilo, aminocarbonilo, NR3R4, -C(O)-T1, -C(O)-NR3-T1, -NR3-C (O)-T1, -O-C(O)-T1, -C(O)-O-T1, -NR3-T2-NR3R4, -NR3-T2-OR3, -NR3-T2-CO2R3, -O-T¿2-NR3R4, -O-T¿2-OR3, -O-T¿2-CO2R3, y -S(O)t-R3, donde: - R3 y R4, idénticos o diferentes, representan cada uno un grupo seleccionado entre átomos de hidrógeno, un grupo alquilo de 1 a 6 carbonos lineal o ramificado, arilo y arilalquilo de 1 a 6 carbonos lineal o ramificado, o R3+R4 forman juntos, con el átomo de nitrógeno que los porta, un heterociclo de 5 a 10 átomos, monocíclico o bicíclico, saturado, que puede contener en el seno del sistema cíclico un segundo heteroátomo seleccionado entre oxígeno y nitrógeno, y estando eventualmente sustituido con un grupo seleccionado entre alquilo de 1 a 6 carbonos lineal o ramificado, arilo, arilalquilo de 1 a 6 carbonos lineal o ramificado, hidroxilo, alcoxi de 1 a 6 carbonos lineal o ramificado, amino, monoalquilamino de 1 a 6 carbonos lineal o ramificado, y dialquilamino de 1 a 6 carbonos lineal o ramificado, E> T1 representa un grupo seleccionado entre alquilo de 1 a 6 carbonos lineal o ramificado, eventualmente sustituido con un grupo seleccionado entre -OR3, -NR3R4, CO2R3, C(O)R3 y -C(O) NR3R4 donde R3 y R4 son como se ha definido anteriormente, arilo, arilalquilo de 1 a 6 carbonos lineal o ramificado, o T1 representa una cadena alquenilo de 2 a 6 carbonos lineal o ramificada eventualmente sustituida con un grupo seleccionado entre -OR3, -NR3R4, -CO2R3, -C(O)R3 y -C (O)NR3R4 donde R3 y R4 son como se ha definido anteriormente, > T2 representa una cadena alquileno de 1 a 6 carbonos lineal o ramificada, '' T¿2 representa una cadena alquileno de 1 a 6 carbonos lineal o ramificada, eventualmente sustituida por uno o varios grupos hidroxilo, '' t representa un número entero comprendido entre 0 y 2 ambos inclusive, ó Z representa un grupo metilendioxi o un grupo etilendioxi.

    4.
    发明专利
    未知

    公开(公告)号：AT294181T

    公开(公告)日：2005-05-15

    申请号：AT03292545

    申请日：2003-10-14

    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 ,  C07D209/00

    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.

    5.
    发明专利
    未知

    公开(公告)号：NO20052338D0

    公开(公告)日：2005-05-12

    申请号：NO20052338

    申请日：2005-05-12

    Applicant: SERVIER LAB

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

    IPC: A61P35/00 ,  C07D471/22 ,  C07D487/14 ,  C07D

    Abstract: Fused carbazole and indole derivatives (I), their enantiomers, diastereoisomers and addition salts with acids and bases are new. Fused carbazole and indole derivatives of formula (I), their enantiomers, diastereoisomers and addition salts with acids and bases are new. A = 6-membered ring, saturated, partially or totally unsaturated, including aromatic; Z' = -U'-V'; U' = single bond or 1-6C alkylene, optionally substituted by one or more of halo and hydroxy and optionally containing one or more unsaturations; V' = hydrogen or various substituents; W1 = atoms that complete a phenyl or pyridyl group; W2 = any of 9 specified 5-membered (di)aza heterocyclic groups; X1/X2 = hydrogen, hydroxy, 1-6C alkoxy or alkylthio, or mercapto and then Y1/Y2 = hydrogen, or X1/Y1 and/or X2/Y2 together complete (thio)carbonyl; R1 = hydrogen, 1-6C alkyl (optionally substituted by one or more hydroxy, 1-6C (hydroxy)alkoxy or the group (a), linked to nitrogen through any of Ra to Re; Q = oxygen or NR2; R2 = substituent; Ra to Rd = bond, hydrogen, halo, hydroxy, 1-6C alkoxy or alkyl, aryloxy, aryl(1-6C)alkoxy, aryl, aryl(1-6C)alkyl, NR3R4, -N=N-R3, OCOR5; Re = methylene or -U1-Ra; R3-R5 = substituents; and n = 0 or 1. The full definitions are given in the DEFINITIONS (Full Definitions) Field. An Independent claim is also included for several methods for preparing (I),

    [3,4-A:3,4-C]carbazole compounds, a process for their preparation and pharmaceutical compositions containing them.
    6.
    发明专利
    [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：ZA200308053B

    公开(公告)日：2004-07-08

    申请号：ZA200308053

    申请日：2003-10-16

    Applicant: SERVIER LAB

    Inventor： PRUDHOMME MICHELLE ,  HUGON BERNADETTE ,  ANIZON FABRICE ,  HICKMAN JOHN ,  PIERRE ALAIN ,  PIERRE GOLSTEYN ROY RENARD ,  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 ,  C07D ,  A61P

    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.

    (3,4-a:3,4-c)carbazole derivatives, process for their preparation and pharmaceutical compositions containing them
    8.
    发明专利
    (3,4-a:3,4-c)carbazole derivatives, process for their preparation and pharmaceutical compositions containing them 未知

    公开(公告)号：SI1411057T1

    公开(公告)日：2005-08-31

    申请号：SI200330032

    申请日：2003-10-14

    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

    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.

    10.
    发明专利
    未知

    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.

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