公开(公告)号：DK1050530T3

公开(公告)日：2004-03-01

申请号：DK00401199

申请日：2000-05-02

Applicant: SERVIER LAB

Inventor： RAULT SYLVAIN ,  RENAULT OLIVIER ,  GUILLON JEAN ,  DALLEMAGNE PATRICK ,  RENARD PIERRE ,  PFEIFFER BRUNO ,  LESTAGE PIERRE ,  LEBRUN MARIE-CECILE

IPC: C07D223/00 ,  A61K31/395 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/4465 ,  A61K31/45 ,  A61K31/451 ,  A61K31/4523 ,  A61K31/4535 ,  A61K31/4545 ,  A61K31/55 ,  A61P25/04 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P43/00 ,  C07B61/00 ,  C07D211/38 ,  C07D211/46 ,  C07D211/54 ,  C07D211/72 ,  C07D211/74 ,  C07D211/84 ,  C07D211/86 ,  C07D223/08 ,  C07D401/04 ,  C07D409/04

Abstract: 1-Aza-2-alkyl-6-aryl cycloalkanes (I) are new. 1-Aza-2-alkyl-6-aryl cycloalkanes of formula (I), their isomers and acid addition salts, are new. n = 0 or 1; R1 = H, aryl-1-6C alkyl, 1-6C alkyl or acyl, 1-6C alkoxycarbonylaryl-1-6C alkoxy carbonyl, or CF3; R2 = 1-6C alkyl; X = O, Cl, OR3, SR4, or NOR5; R3 = H, 1-6C alkyl or acyl, 1-6C alkoxycarbonyl, or aryl 1-6C alkoxycarbonyl; R4 = H, 1-6C alkyl, or aryl; R5 = H, 1-6C alkyl(optionally substituted by one or more groups selected from OH, amino that may be substituted by one or two alkyl groups, or 1-6C alkoxy; the dotted line = an optional bond; and Ar = aryl or heteroaryl; with the proviso that (I) is not any of the following: 6-methyl-2-phenyl-2,3-dihydro-4-pyridinone; 2-methyl-6-phenyl-4-piperidinone; N-benzyl-2-(R'2)-6-phenyl-4-piperidinones where R'2 is methyl, ethyl, propyl, or isopropyl; or 2-(R2)-6-phenyl-4-piperidinols where R2 is isopropyl or butyl.

公开(公告)号：EA004291B1

公开(公告)日：2004-02-26

申请号：EA200200636

申请日：2000-12-21

Applicant: SERVIER LAB

Inventor： DUFLOS MURIEL ,  ROBERT JEAN-MICHEL ,  NOURRISSON MARIE-RENEE ,  LE BAUT GUILLAUME ,  CAGNARD DANIEL-HENRI ,  BIZOT-ESPIARD JEAN-GUY ,  RENARD PIERRE

IPC: C07D213/74 ,  A61K31/427 ,  A61K31/4436 ,  A61K31/497 ,  A61K31/506 ,  A61P17/06 ,  A61P19/02 ,  A61P29/00 ,  C07D409/14 ,  C07D417/14 ,  A61K31/444

Abstract: Соединениеформулы (I)вкоторой Hetи Het, которыемогутбытьодинаковыилиразличны, каждыйпредставляетсобойгетероарильнуюгруппу,Апредставляетсобойсвязьилилинейнуюилиразветвленную (C-С)алкиленовуюгруппу,егооптическиеизомеры, еслионисуществуют, атакжеегоаддитивныесолис фармацевтическиприемлемойкислотой. Лекарственныепрепараты.

公开(公告)号：ES2198863T3

公开(公告)日：2004-02-01

申请号：ES99402016

申请日：1999-08-09

Applicant: SERVIER LAB

Inventor： HANESSIAN STEPHEN ,  ATASSI GHANEM ,  TUCKER GORDON ,  CAIGNARD DANIEL-HENRI ,  RENARD PIERRE

IPC: A61K31/18 ,  A61K31/185 ,  C12N9/99 ,  A61K31/35 ,  A61K31/351 ,  A61K31/4406 ,  A61K31/4418 ,  A61K31/445 ,  A61P43/00 ,  C07C319/14 ,  C07C319/20 ,  C07C323/60 ,  C07D211/20 ,  C07D213/34 ,  C07D309/04

Abstract: Hydroxamic acid derivatives (I) are new. Hydroxamic acid derivatives of formula (I) and their acid and base addition salts are new. R1 = 1-6C alkyl (optionally substituted by at least one OH, halo, 1-6C alkoxy, mercapto, 1-6C alkylthio, aryl, 1-6C acyl or amino (optionally substituted by one or two 1-6C alkyl, cycloalkyl or aryl)), 1-6C acyl, cycloalkyl, aryl, heterocyclic group or aminocarbonyl-1-6C alkyl (with amino optionally substituted by one 1-6C alkyl (optionally substituted by at least one aryl, 1-6C arylalkyl, cycloalkyl or 1-6C alkylaminocarbonyl; R2 = 1-4C alkylene; R3 = X or T-U'-V'- X = 1-6C alkyl, 1-6C acyl, 1-6C alkoxycarbonyl, 1-6C aminoalkyl (amino optionally substituted by one or two 1-6C alkyl), 1-6C hydroxyalkyl, 1-6C carboxyalkyl, 1-6C aminocarbonylalkyl, 1-6C mercaptoalkyl, cycloalkyl, aryl or heterocyclic; T = aryl or heterocyclic; U' = single bond, S, O, NH, carbonyl, -R8O-, -R8S-, -R8NH-, -R8OR9-, -R8-NH-R9-, -R8-CO-R9- or -R9- (with R8 bound to T and R9 bound to V'); R8 = 1-6C alkylene; R9 = arylene or heteroarylene; V' = 1-6C alkylene; R4 = biaryl, arylheteroaryl, heteroarylaryl, 1-6C alkyl (optionally substituted by one heterocyclic group), cycloalkyl, aryl, 1-6C arylalkyl, cycloalkyl-1-6C alkyl or heterocyclic; and provided that R4 is 1-6C alkyl (optionally substituted by one heterocyclic group), cycloalkyl, aryl, 1-6C arylalkyl, cycloalkyl-1-6C alkyl or heterocyclic, when R3 is T-U'-V'-. An Independent claim is also included for the preparation of (I).

公开(公告)号：DE69906000T2

公开(公告)日：2004-01-08

申请号：DE69906000

申请日：1999-10-12

Applicant: SERVIER LAB

Inventor： LANGLOIS MICHEL ,  MATHE-ALLAINMAT MONIQUE ,  LEFAS-LE GALL MARIE ,  BENNEJEAN CAROLINE ,  RENARD PIERRE ,  DELAGRANGE PHILIPPE

IPC: A61K31/16 ,  A61K31/165 ,  A61K31/17 ,  A61K31/335 ,  A61K31/343 ,  A61K31/352 ,  A61K31/353 ,  A61K31/38 ,  A61K31/381 ,  A61K31/395 ,  C07D339/00 ,  A61K31/4355 ,  A61K31/437 ,  A61P1/00 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P15/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07C233/18 ,  C07C233/23 ,  C07C233/74 ,  C07C235/34 ,  C07C235/40 ,  C07C275/26 ,  C07D307/79 ,  C07D307/80 ,  C07D307/81 ,  C07D311/92 ,  C07D333/58 ,  C07D333/60 ,  C07D471/04 ,  C07D491/04 ,  C07D491/048 ,  C07D493/04

Abstract: Cycloalkene substituted cyclic derivatives (I) are new. Cycloalkene substituted cyclic derivatives of formula (I), their enantiomers, diastereoisomers and their acid or base addition salts are new. A = a group of formula (i) or (ii) (optionally substituted by Ra, ORa, OH, CORa, formyl, COORa, COOH or OCORa; Ra = 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, 1-6C polyhaloalkyl, 3-8C cycloalkyl, 3-8C cycloalkyl-(1-6C) alkyl, 3-8C cycloalkenyl, 3-8C cycloalkenyl-(1-6C) alkyl (all optionally substituted with at least one OH, 1-6C alkoxy, 1-6C alkyl, 1-6C polyhaloalkyl, amino or halo), aryl, aryl-(1-6C) alkyl, heteroaryl or heteroaryl-(1-6C) alkyl; X, Y' = O, S or CH2; D' = benzene or naphthalene; a-d = single or double bond; Z = O, S, CH2 or NR ; R = H, 1-6C alkyl, aryl or aryl-(1-6C) alkyl; D'' = benzene or pyridine; R = H, halo, OH, SH, Ra, ORa, S(O)nRa or a (un)saturated 5- to 7-membered ring of formula (iii) (optionally substituted with at least one 1-6C alkyl, 1-6C alkoxy, carboxy, 1-6C alkoxycarbonyl, OH or =O); n = 0-2; E = O or -S(O)n-; G1, G2 = single bond, -(CH2)t- (optionally substituted with at least one OH, COOH, formyl, Ra, ORa, COORa, CORa or halo; p, q = 0-4; p + q = 1-4; B' = -NR aC(Q)R a, -NR aC(Q)NR aR a or -C(Q)NR aR a; R a-R a = H or Ra; Q = O or S; aryl = phenyl, naphthyl, biphenyl (all optionally substituted with at least one OH, 1-6C alkoxy, 1-6C alkyl, 1-6C polyhaloalkyl, CN, COOH, 1-6C alkoxycarbonyl, NO2, amino or halo); heteroaryl = 5- to 10-membered mono- or polycyclic aromatic ring containing 1-3 N, O or S (optionally substituted with at least one OH, 1-6C alkoxy, 1-6C alkyl, 1-6C polyhaloalkyl, CN, COOH, 1-6C alkoxycarbonyl, NO2, amino or halo); and provided that q = 0 and p = 4, or q = 4 and p = 0 do not apply, when A is naphthyl (optionally substituted with methoxy or methyl), G1 and G2 are single bonds and B' is a group of formula (iv) or NHCOCH3; that A is other than halo substituted naphthyl, when G1 is a single bond and p + q is 1; B' is other than urea, when A is indolyl substituted on position 2 with a group of formula (v); and that B' is other than CONH-aryl, when A is indolyl substituted on position 2 with carboxyl or alkoxycarbonyl, p is 1, q is 0 (p is 0 and q is 1) and G1 is single bond. A Independent claim is also included for the preparation of (I).

公开(公告)号：DE69905524T2

公开(公告)日：2003-12-11

申请号：DE69905524

申请日：1999-07-26

Applicant: SERVIER LAB

Inventor： RAULT SYLVAIN ,  ENGUEHARD CECILE ,  LANCELOT JEAN-CHARLES ,  ROBBA MAX ,  ATASSI GHANEM ,  PIERRE ALAIN ,  CAIGNARD DANIEL-HENRI ,  RENARD PIERRE

IPC: A61K31/00 ,  A61K31/40 ,  A61K31/407 ,  A61P35/00 ,  C07D495/14

Abstract: A compound selected from those of formula (I): wherein: R1 represents hydrogen, halogen, alkyl, nitro, hydroxy, alkoxy, trihaloalkyl, trihaloalkoxy or optionally substituted amino, R2 represents optionally substituted aryl or heteroaryl, R3 represents hydrogen, halogen, alkyl, nitro, hydroxy, alkoxy, trihaloalkyl, trihaloalkoxy or optionally substituted amino, their isomers and addition pharmaceutically-acceptable acid or base salts thereof and medicinal products containing the same are useful in the treatment of cancer.

公开(公告)号：ES2193926T3

公开(公告)日：2003-11-16

申请号：ES00403399

申请日：2000-12-05

Applicant: SERVIER LAB

Inventor： VIAUD MARIE-CLAUDE ,  GUILLAUMET GERALD ,  DAUBOS PHILIPPE ,  BENNEJEAN CAROLINE ,  DELAGRANGE PHILIPPE ,  RENARD PIERRE

IPC: A61K31/538 ,  A61K31/5415 ,  A61P1/00 ,  A61P1/14 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D265/36 ,  C07D279/16 ,  C07D413/06 ,  C07D413/12

Abstract: 1,4-Benzoxazine and 1,4-benzothiazine compounds (I) and their acid or base addition salts, enantiomers and diastereomers, are new. 1,4-Benzoxazine and 1,4-benzothiazine compounds of formula (I) and their acid or base addition salts, enantiomers and diastereomers, are new. R1 = R, OR, SR, SO2NRR', NRR', -N(R)C(=Z)R', -N(R)SO2R', -N(R)C(=Z)OR', -N(R)C(=Z)NR'R'', C(=Z)OR, -OC(=Z)R or -C(=Z)NRR'; Z = S or O; R, R', R'' = H or 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, 3-8C cycloalkyl or 3-8C cycloalkyl-1-6C alkyl (all optionally substituted by one or more B), or aryl, aryl-1-6C alkyl, heteroaryl or heteroaryl-1-6C alkyl (all optionally substituted by one or more D; or NRR' or NR'R'' = morpholinyl, piperidinyl, piperazinyl or pyrrolidinyl; G = 1-4C alkylene (optionally substituted by R, OR, COR or COOR; A = -C(=Z)NRR', -N(R)C(=Z)R' or -N(R)C(=Z)NR'R''; R2 = halo, R, OR, COR, COOR or OCOR; X = O or S; dotted line = single or double bond; B = OH, alkoxy, alkyl, polyhaloalkyl, NH2, NH(1-6C alkyl), N(1-6C alkyl)2 or halo; D = OH, alkoxy, amino, alkylamino, dialkylamino, nitro, cyano, polyhaloalkyl, formyl, carboxyl, alkoxycarbonyl, amido or halo; aryl = phenyl, naphthyl or biphenyl; and heteroaryl = mono- or bicyclic aromatic group containing 1-3 O, S or N; provided that when A = -C(=Z)NRR', G = 2-4C alkylene.

公开(公告)号：SI1255757T1

公开(公告)日：2003-10-31

申请号：SI200130016

申请日：2001-02-16

Applicant: INST NAT SANTE RECH MED ,  SERVIER LAB

Inventor： ROQUES BERNARD P ,  FOURNIE-ZALUSKI MARIE-CLAUDE ,  INGUIMBERT NICOLAS ,  PORAS HERVE ,  SCALBERT ELIZABETH ,  BENNEJEAN CAROLINE ,  RENARD PIERRE

IPC: C07D471/04

公开(公告)号：PT1255757E

公开(公告)日：2003-10-31

申请号：PT01907822

申请日：2001-02-16

Applicant: INST NAT S ET DE LA REC MEDI I ,  SERVIER LAB

Inventor： FOURNIE-ZALUSKI MARIE-CLAUDE ,  ROQUES BERNARD PIERRE ,  BENNEJEAN CAROLINE ,  RENARD PIERRE ,  SCALBERT ELIZABETH ,  INGUIMBERT NICOLAS ,  PORAS HERVE

IPC: A61K31/381 ,  C07D233/64 ,  A61K31/405 ,  A61K31/4172 ,  A61K31/437 ,  A61K31/4406 ,  A61K31/47 ,  A61K31/473 ,  A61K31/4745 ,  A61P7/00 ,  A61P9/04 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/12 ,  A61P43/00 ,  C07D209/20 ,  C07D213/55 ,  C07D215/12 ,  C07D215/14 ,  C07D219/02 ,  C07D333/60 ,  C07D471/04

Abstract: Compounds of formula (I): wherein 0

公开(公告)号：FR2830012B1

公开(公告)日：2003-10-31

申请号：FR0112205

申请日：2001-09-21

Applicant: SERVIER LAB

Inventor： LESIEUR DANIEL ,  BLANC DELMAS ELODIE ,  BENNEJEAN CAROLINE ,  CHAVATTE PHILIPPE ,  GUILLAUMET GERALD ,  DACQUET CATHERINE ,  LEVENS NIGEL ,  BOUTIN JEAN ALBERT ,  RENARD PIERRE

IPC: A61P3/10 ,  A61P9/10 ,  A61P17/06 ,  A61P19/10 ,  A61P35/00 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  A61K31/428

公开(公告)号：NO20034722D0

公开(公告)日：2003-10-22

申请号：NO20034722

申请日：2003-10-22

Applicant: SERVIER LAB

Inventor： RAULT SYLVAIN ,  KOPP MARINE ,  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 ,  C07D

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).