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    New N-substituted azepane or azepanone derivatives, are selective farnesyl transferase inhibitors useful for treating cancer diseases, restenosis or type I neurofibromatosis
    2.
    发明专利
    New N-substituted azepane or azepanone derivatives, are selective farnesyl transferase inhibitors useful for treating cancer diseases, restenosis or type I neurofibromatosis 未知

    公开(公告)号：FR2819511A1

    公开(公告)日：2002-07-19

    申请号：FR0100638

    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 ,  ORTUNO JEAN CLAUDE ,  FAUCHERE JEAN LUC

    IPC: A61P35/00 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D403/06 ,  A61K31/55

    Abstract: N, 3-Disubstituted azepane or azepan-2-one derivatives (I) are new. Azepane derivatives of formula (I) and their enantiomers, diastereomers and acid or base addition salts are new. W = CO or CH2; X = 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); or X may also be a direct bond if W = CH2; A1 = alkylene; n = 0-2; Y = aryl, heteroaryl, cycloalkyl or heterocycloalkyl (all optionally substituted (os) by R8); R1 - R4 = H or as for Y; or pairs of adjacent groups R1 - R4 may together form bonds; T = CHR5, NR5 or NR5CO (bonded to the ring at the left-hand terminal); R5 = H; or alkyl, aryl, heteroaryl, aralkyl or heteroaralkyl (all os by one or more R7); V = H; or aryl or heteroaryl (both os by one or more R7); A2 = -(CR6R'6)p; p = 0-4 (but not 0 if T = NR5); R6, R'6 = H, alkyl (os by R9), alkenyl, alkynyl or R9; R9 = OR5, NR5R'5, S(O)nR5, CONR5R'5, NR5COR'5, NR5SO2R'5, SO2NR5R'5 or NR5COOR'5; R'5 = as R5; R7 = 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; R8 = halo, =O, OH, CN, NO2, COOH, alkoxycarbonyl, U-R80 or A80-U-R80; A80 = alkylene;and U = direct bond, O, NH, S(O)n, NHCO, CONH, SO2NH or NHSO2; R80 = alkyl, aryl, aralkyl, heteroaryl or heteroarylalkyl; 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); and 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).

    New cyclo (c)-fused bicyclic azepane derivatives, are selective farnesyl transferase inhibitors useful for treating cancer diseases, restenosis or type I neurofibromatosis
    8.
    发明专利
    New cyclo (c)-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：FR2819510A1

    公开(公告)日：2002-07-19

    申请号：FR0100642

    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: A61P9/00 ,  A61P25/00 ,  A61P35/00 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  A61K31/55 ,  C07D401/04

    Abstract: N-Substituted cyclo (c)-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; 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 = os aralkyl, os heteroaryl, os heteroaralkyl, os cycloalkylalkyl 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; and B' = an optionally partially hydrogenated aryl or heteroaryl ring (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); and 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).

    10.
    发明专利
    未知

    公开(公告)号：FR2883876B1

    公开(公告)日：2007-05-04

    申请号：FR0503071

    申请日：2005-03-30

    Applicant: SERVIER LAB

    Inventor： DE NANTEUIL GUILLAUME ,  PORTEVIN BERNARD ,  GLOANEC PHILIPPE ,  MILLAN MARK ,  ORTUNO JEAN CLAUDE ,  MANNOURY LA COUR CLOTILDE ,  GOBERT ALAIN

    IPC: C07D295/10 ,  A61K31/495 ,  A61P1/00 ,  A61P1/08 ,  A61P3/04 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P29/00

    Abstract: Indanyl-piperazine derivatives (I) are new. Indanyl-piperazine derivatives of formula (I) and their optical isomers, salts, enantiomers or diastereoisomers are new. R 3 = H and R 1+R 2 = benzene, naphthalene or quinoline (optionally substituted by H, halo or 1-6C alkyl (optionally substituted by halo)); or R 1 = H; and R 2+R 3 = benzene, naphthalene or quinoline (optionally substituted by H, halo or 1-6C alkyl (optionally substituted by halo)); n = 1-2; X = (CH 2) m-OT, (CH 2) m-NR 4T, C(O)NR 4T or (CH 2) mNR 4C(O); m = 1-6; T = 1-6C alkyl optionally substituted by OH; R 4 = H or 1-6C alkyl; A = (hetero)aryl; aryl = phenyl, biphenyl or naphthyl (optionally substituted by halo, 1-6C alkyl, 1-6C alkoxy, OH, CN or 1-6C trihaloalkyl); and heteroaryl = 5-12 membered aromatic mono- or bicyclic rings containing O, N or S heteroatoms and optionally substituted by halo, 1-6C alkyl, 1-6C alkoxy, OH or 1-6C trihaloalkyl. An independent claim is also included for preparation of (I). [Image] ACTIVITY : Antidepressant; Tranquilizer; Anorectic; Analgesic; Antiinflammatory; Neuroleptic; Antiemetic; Gastrointestinal-Gen. MECHANISM OF ACTION : Serotonin receptor inhibitor; Neurokinin-1 antagonist. The ability of (1RS)-1-[1-(3,5-difluorobenzyloxymethyl)indan-1-yl]piperazine dihydrochloride to inhibit serotonin receptor in rats was tested using biological assays. The result showed that (1RS)-1-[1-(3,5-difluoro-benzyloxymethyl)-indan-1-yl]-piperazine dichlorhydrate exhibits a pK i (negative log of inhibitory constant) value of 8.49.

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