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    31.
    发明专利
    未知

    公开(公告)号：FR2826009B1

    公开(公告)日：2003-08-15

    申请号：FR0107718

    申请日：2001-06-13

    Applicant: SERVIER LAB

    Inventor： WIERZBICKI MICHEL ,  BOUSSARD MARIE FRANCOISE ,  ROUSSEAU ANNE ,  ATASSI GHANEM ,  HICKMAN JOHN ,  PIERRE ALAIN ,  LEONCE STEPHANE ,  GUILBAUD NICOLAS ,  KRAUS BERTHIER LAURENCE

    IPC: C07D209/80 ,  A61K31/403 ,  A61K31/433 ,  A61K31/4439 ,  A61P35/00 ,  C07D209/94 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D491/04 ,  C07D491/056 ,  C07D405/14 ,  C07D403/12 ,  A61K31/4045 ,  A61K31/4402 ,  A61K31/4453

    Abstract: Indenoindolone derivatives (I), their isomers and salts with acids and bases are new. Indenoindolone derivatives (I), their isomers and salts with acids and bases are new; R = H, alkyl (optionally substituted by carboxy, alkoxycarbonyl, or NR10R11), or alkenyl; R1-R8 = H, alkyl (optionally substituted by aryl, carboxy or alkoxycarbonyl), OH, acyloxy, NR12R13, carboxy, alkoxy (optionally substituted by aryl or NR14R15), alkenyloxy, or to adjacent groups R1-R8 = 1 or 2C alkylenedioxy; R9 = H, aryl, heteroaryl or alkyl (optionally containing one or more unsaturations and optionally substituted by one or more aryl, heteroaryl, 3-8C cycloalkyl, CN, or NR17R18 groups); X = O or NR16; R10, R11, R14, R15, R17, R18 = alkyl; NR10+R11, NR14+R15, NR17+R18 = nitrogen heterocycle; R12, R13 = H, alkyl, or NR14R15; R16 = H, alkyl, aryl, or aryl alkyl. Where alkyl, alkoxy, acyloxy, alkenyl and alkenyloxy groups have up to 6 C atoms, aryl is defined as phenyl, biphenyl, or naphthyl (optionally substituted by one or more halogen, alkyl, alkenyl, alkoxy, phenoxy, nitro, CN, amino, mono- and di-alkylamino or 1-2C alkylenedioxy groups) and heteroaryl groups may be mono- or bicyclic of 5-12 members with 1-3 heteroatoms (O, N, S) and optionally substituted by halogen, alkyl, OH, alkoxy, polyhaloalkyl, amino, mono- and di-alkylamino groups, and nitrogen heterocycles are monocyclic having 5-7 members including 1-3 heteroatoms, one of which is N and the others may be O, N, or S. An Independent claim is also included for the preparation of (I).

    New cyclo (d)-fused bicyclic azepane derivatives, are selective farnesyl transferase inhibitors useful for treating cancer diseases, restenosis or type I neurofibromatosis
    37.
    发明专利
    New cyclo (d)-fused bicyclic azepane derivatives, are selective farnesyl transferase inhibitors useful for treating cancer diseases, restenosis or type I neurofibromatosis 未知

    公开(公告)号：FR2819512A1

    公开(公告)日：2002-07-19

    申请号：FR0100639

    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: A61P35/00 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/06 ,  A61K31/55

    Abstract: N-Substituted cyclo (d)-fused bicyclic azepane or azepanone derivatives (I) are new. Bicyclic azepane derivatives of formula (I) and their enantiomers, diastereomers and acid or base addition salts are new. W = CO or CH2; X = direct bond, alkylene, CO, S(O)n, S(O)n-A1, CO-A1, A1-S(O)n-A1 or A1-CO-A1 (bonded to the ring at the left-hand terminal); A1 = alkylene; n = 0-2; Y = aryl, heteroaryl, cycloalkyl or heterocycloalkyl (all optionally substituted (os) by R6); R1, R2 = H or as for Y; or together form a bond; T = CHR3, NR3 or NR3CO (bonded to the ring at the left-hand terminal); R3 = H; or alkyl, aryl, heteroaryl, aralkyl or heteroaralkyl (all os by one or more R5); V = H; or aryl or heteroaryl (both os by one or more R5); A2 = -(CR4R'4)p; p = 0-4 (but not 0 if T = NR3); R4, R'4 = H, alkyl (os by R7), alkenyl, alkynyl or R7; R7 = OR3, NR3R'3, S(O)nR3, CONR3R'3, NR3COR'3, NR3SO2R'3, SO2NR3R'3 or NR3COOR'3; R'3 = as R3; R5 = halo, alkyl, alkoxy, OH, SH, alkylthio, CN, NH2 (os by 1 or 2 alkyl), NO2, COOH, alkoxycarbonyl, CONH2 (os by 1 or 2 alkyl), carbamoyl, os aryl, os aralkyl, os heteroaryl, os heteroaralkyl, os cycloalkyl, os cycloalkylalkyl, os heterocycloalkyl or os heterocycloalkylalkyl; R6 = halo, =O, OH, CN, NO2, COOH, alkoxycarbonyl, U-R60 or A60-U-R60; A60 = alkylene; U = direct bond, O, NH, S(O)n, NHCO, CONH, SO2NH or NHSO2; R60 = alkyl, aryl, aralkyl, heteroaryl or heteroarylalkyl; B' = group completing an optionally partially hydrogenated aryl or heteroaryl group (os by one or more of CN, alkyl, alkoxy, OH or halo); alkyl or alkylene moieties have 1-6C; cycloalkyl moieties have 3-8C; heterocycloalkyl moieties are 5-7 membered and contain 1-3 of N, O and S as heteroatom(s); aryl moieties are phenyl or naphthyl; heteroaryl moieties are mono- or bicyclic 5-11 membered systems containing at least one aromatic ring and 1-5 of N, O and S as heteroatom(s); the substituents in os aryl, heteroaryl, aralkyl or heteroaralkyl are one or more of CN, alkylcarbonyl, CONH2 (os by 1 or 2 alkyl) or halo (in the ring part); the substituents in os cycloalkyl, heterocycloalkyl, cycloalkylalkyl or heterocycloalkylalkyl are one or more of =O, CN, alkylcarbonyl, CONH2 (os by 1 or 2 alkyl) or halo (in the ring part). An Independent claim is included for the preparation of (I).

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