公开(公告)号：PL351732A1

公开(公告)日：2002-07-29

申请号：PL35173202

申请日：2002-01-16

Applicant: SERVIER LAB

Inventor： CASARA PATRICK ,  LE DIGUARHER THIERRY ,  DOREY GILBERT ,  HICKMAN JOHN ,  PIERRE ALAIN ,  TUCKER GORDON ,  GUILBAUD NICOLAS

IPC: C07C317/00 ,  A61K31/4164 ,  A61K31/417 ,  A61K31/4178 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/454 ,  A61P9/00 ,  A61P9/10 ,  A61P25/00 ,  A61P35/00 ,  C07D213/36 ,  C07D213/38 ,  C07D213/57 ,  C07D233/54 ,  C07D233/58 ,  C07D233/61 ,  C07D233/64 ,  C07D401/06

Abstract: Compound of formula (I):wherein:X represents a bond or alkylene, CO, S(O)n, -S(O)n-A1-, -CO-A1-, -A-S(O)n-A'1- or -A1-CO-A'1-,Y represents aryl, heteroaryl, cycloalkyl or heterocycloalkyl, each unsubstituted or substituted,R1, R2, R3 and R4 each independently of the others represent hydrogen or aryl, heteroaryl, cycloalkyl or heterocycloalkyl, each unsubstituted or substituted,or R1, R2, R3 and R4, taken in pairs, together form a bond, or form a fused benzene ring or a fused aromatic or partially unsaturated heterocycle,T represents -CH(R5)-, -N(R5)- or -N(R5)CO-,V represents hydrogen or unsubstituted or substituted aryl or heteroaryl,A2 represents [C(R6)(R'6)]p,R7 and R8 are as defined in the description,their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as farnesyl transferase inhibitors.

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).

公开(公告)号：FR2819509A1

公开(公告)日：2002-07-19

申请号：FR0100641

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

IPC: C07C317/00 ,  A61K31/4164 ,  A61K31/417 ,  A61K31/4178 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/454 ,  A61P9/00 ,  A61P9/10 ,  A61P25/00 ,  A61P35/00 ,  C07D213/36 ,  C07D213/38 ,  C07D213/57 ,  C07D233/54 ,  C07D233/58 ,  C07D233/61 ,  C07D233/64 ,  C07D401/06 ,  C07D213/04 ,  A61K31/4174 ,  A61K31/44

Abstract: 1,3-Disubstituted cycloheptene derivatives (I) are new. Cycloheptene derivatives of formula (I) and their enantiomers, diastereomers and acid or base addition salts are new. 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 R8); R1 - R4 = H or as for Y; or pairs of adjacent groups R1 - R4 may together form bonds; or R1 + R2, R2 + R3 or R3 + R4 = group completing a fused benzene ring or fused 5- or 6-membered aromatic or partially aromatic heterocycle containing 1 or 2 of N, O and S as heteroatom(s); 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; 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); 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).

公开(公告)号：AU4930597A

公开(公告)日：1998-07-02

申请号：AU4930597

申请日：1997-12-30

Applicant: SERVIER LAB

Inventor： GUILLONNEAU CLAUDE ,  CHARTON YVES ,  BISAGNI EMILE ,  ATASSI GHANEM ,  PIERRE ALAIN ,  GUILBAUD NICOLAS

IPC: A61K31/435 ,  A61P35/00 ,  C07D471/04 ,  A61K31/47 ,  A61K31/495

Abstract: Ellipticine derivatives of formula (I), their optical isomers, N-oxides and salts are new. R1 = 1-6C alkyl; R2, R5, R6 = H or 1-6C alkyl; R3 = H, 3-8C cycloalkyl, 1-20C alkyl, 2-20C alkenyl, 4-20C alkadienyl (all optionally substituted by 1-3 of 1-6C alkoxy, carboxy, 1-6C alkoxycarbonyl, benzyloxycarbonyl, mono-, di- and tricyclic aryl, or heteroaryl containing O, N, or S), mono-, di- or tricyclic aryl (optionally totally or partially hydrogenated), 5-6-membered heterocycle containing 1-3 O, N or S atoms (all optionally substituted by 1-3 of 1-6C alkoxycarbonyl, benzyloxycarbonyl, carboxy, 1-6C alkyl (optionally substituted by 1 or 2 phenyl groups), 1-6C alkoxy or carboxy), amino, mono- or disubstituted amino (substituted by one or two 1-6C alkyl (optionally substituted by carboxy, 1-6C alkoxycarbonyl, or benzyloxycarbonyl), mono- or bicyclic aryl or heteroaryl (optionally partially or totally hydrogenated and substituted by one or two carboxy, 1-6C alkoxycarbonyl or benzyloxycarbonyl)), amino forming part of a 5-6-membered ring which may contain a second heteroatom selected from O, N and S and optionally substituted by one or two of 1-6C alkyl, benzhydryl, 1-6C alkoxy, 1-6C alkoxycarbonyl, benzyloxycarbonyl, carboxy or piperidino; R4 = H, 1-6C alkyl (optionally substituted by 1-6C alkylamino) or 2-6C alkenyl; R7,R8 = H, 1-6C alkyl or 2-6C alkenyl; or NR7R8 = heterocycle which may contain a second heteroatom selected from O, N, and S; or R7+R6 = ethylene or propylene bridge; and A = 1-10C saturated or unsaturated hydrocarbon chain.