-
公开(公告)号:PT1010693E
公开(公告)日:2003-12-31
申请号:PT99403190
申请日:1999-12-17
Applicant: SERVIER LAB
Inventor: NEWMAN-TANCREDI ADRIAN , GOBERT ALAIN , CORDI ALEX , LACOSTE JEAN-MICHEL , MILLAN MARK
IPC: A61K31/4164 , A61K31/4178 , A61P3/04 , A61P15/10 , A61P25/00 , A61P25/16 , A61P25/22 , C07D233/06 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07D233/10 , C07D233/20 , C07D233/22 , C07D401/06 , C07D405/06
Abstract: Imidazoline derivatives (I) are new. Imidazoline derivatives of formula (I) and their acid or base addition salts are new. R -R = H, 1-6C alkyl, 1-6C alkoxy, OH, 1-6C polyhalogenoalkyl, cyano, nitro, amino, 1-6C alkylamino, di-1-6C alkyl amino, thioalkyl, 1-6C sulfonylalkyl, 1-6C sulfinylalkyl, carboxy, alkoxycarbonyl, 1-6C alkylcarbonyloxy, formyl, carbamoyl, carboxamide, phenyl, benzyl or halo; B' = a group of formula (i) or (ii); X = CR , CR R , N, NR , O, S, SO or SO2; Z = C or CR ; R , R , R = H or 1-6C alkyl; R , R = H, 1-6C alkyl or benzyl; Y' = CH, CH2 or a bond; R -R = H or 1-6C alkyl; or R and R or R and R = form a cyclopropane; and a, b = single or double bonds. Independent claims are also included for: (1) the preparation of (I); and (2) pharmaceutical compositions comprising at least one compound (I).
-
公开(公告)号:AT254102T
公开(公告)日:2003-11-15
申请号:AT01400940
申请日:2001-04-12
Applicant: SERVIER LAB
Inventor: PEGLION JEAN-LOUIS , DESSINGES AIMEE , GOUMENT BERTRAND , MILLAN MARK , LEJEUNE FRANCOISE , BROCCO MAURICETTE
IPC: A61K31/138 , A61K31/343 , A61K31/357 , A61K31/381 , A61K31/403 , A61K31/404 , A61K31/4045 , A61P3/04 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/30 , A61P43/00 , C07B61/00 , C07C213/08 , C07C215/42 , C07D209/16 , C07D209/30 , C07D209/40 , C07D209/70 , C07D307/93 , C07D317/70 , C07D319/14 , C07D333/78 , C07D407/12
Abstract: Heterocycloalkyl and heteroaryl benzocyclobutane derivatives (I) are new. Heterocycloalkyl and heteroaryl benzocyclobutane derivatives (I), their isomers and salts, acids and bases are new. dotted line = single or double bond; n = 1-6; R1, R2 = H, 1-6C alkyl, aryl, arylalkyl, cycloalkyl, cycloalkyl alkyl, 2-6C alkenyl or alkynyl, heterocycloalkyl, heterocycloalkyl alkyl, heteroaryl, or heteroaryl alkyl; X = -CH=CH-, -O-, -S(O)m-, or -N(R3)-; n = 0-2; R3 = H, 1-6C alkyl, aryl, arylalkyl, cycloalkyl, cycloalkyl alkyl, or 2-6C alkenyl or alkynyl; Y = CH or CH2 depending on whether it is linked by a single or double bond, or it may be O when X is O; T = 3-12C mono- or polycyclic cycloalkyl in which one of the C atoms may be replaced by O, Se, SOp, R3 or SiR4R5; p = 0-2; R4, R5 = 1-6C alkyl. Within the definition of (I), aryl groups may be phenyl, biphenyl, naphthyl, dihydronaphthyl, tetrahydronaphthyl, indanyl, indenyl, or benzocyclobutyl, each of which may be substituted by one or more of the following: halogen, 1-6C alkyl or alkoxy, OH, NO2, CN, 1-6C trihaloalkyl, NH2, or mono- or di-alkylamino, heteroaryl groups comprise an aryl group as defined above containing 1-3 hetero atoms (O, N, S) in the cyclic system and optionally substituted as before, cycloalkyl groups may be mono- or polycyclic of 3-12 members, optionally containing unsaturations and optionally substituted as before, and heterocycloalkyl groups comprise a cycloalkyl groups as defined that may have one or more unsaturations and containing 1-3 heteroatoms (O, N, S) in the ring. An Independent claim is also included for preparations of (I).
-
公开(公告)号:FI111948B
公开(公告)日:2003-10-15
申请号:FI952802
申请日:1995-06-07
Applicant: INST NAT SANTE RECH MED , SERVIER LAB
Inventor: PEGLION JEAN-LOUIS , VIAN JOEL , GOUMENT BERTRAND , MILLAN MARK , AUDINOT VALERIE , SCHWARTZ JEAN-CHARLES , SOKOLOFF PIERRE
IPC: A61K31/435 , A61K31/4741 , A61K31/535 , A61K31/5383 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , C07D491/04 , C07D491/048 , C07D491/153 , C07D498/04 , C07D498/14 , A61K31/34
Abstract: 1,4-Oxazine tetracyclic derivatives of formula (I) and their acid addition salts in racemic, optically active or enantiomeric forms are new. X, Y = O or CH2; A-B = -(CH2)2- or -HC=CH-, and when Y = O, then A-B may also be -(CH2)3-, when Y = CH2 then A-B may also be -H2C-CO- or -H2C-CHOH-; R = H, 1-10C alkyl, 3-10C alkenyl, 3-10C alkynyl, all of which opt. substd. by 3-8C cycloalkyl, or by phenyl, thienyl, and pyridyl, each of which may be substd. by one or more halogens, OH, or 1-6C alkyl or alkoxy; n = 0 or 1 when X = CH2, or is 1 when X = O.
-
公开(公告)号:AT250586T
公开(公告)日:2003-10-15
申请号:AT99403190
申请日:1999-12-17
Applicant: SERVIER LAB
Inventor: CORDI ALEX , LACOSTE JEAN-MICHEL , MILLAN MARK , NEWMAN-TANCREDI ADRIAN , GOBERT ALAIN
IPC: C07D233/06 , A61K31/4164 , A61K31/4178 , A61P3/04 , A61P15/10 , A61P25/00 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07D233/10 , C07D233/20 , C07D233/22 , C07D401/06 , C07D405/06
Abstract: Imidazoline derivatives (I) are new. Imidazoline derivatives of formula (I) and their acid or base addition salts are new. R -R = H, 1-6C alkyl, 1-6C alkoxy, OH, 1-6C polyhalogenoalkyl, cyano, nitro, amino, 1-6C alkylamino, di-1-6C alkyl amino, thioalkyl, 1-6C sulfonylalkyl, 1-6C sulfinylalkyl, carboxy, alkoxycarbonyl, 1-6C alkylcarbonyloxy, formyl, carbamoyl, carboxamide, phenyl, benzyl or halo; B' = a group of formula (i) or (ii); X = CR , CR R , N, NR , O, S, SO or SO2; Z = C or CR ; R , R , R = H or 1-6C alkyl; R , R = H, 1-6C alkyl or benzyl; Y' = CH, CH2 or a bond; R -R = H or 1-6C alkyl; or R and R or R and R = form a cyclopropane; and a, b = single or double bonds. Independent claims are also included for: (1) the preparation of (I); and (2) pharmaceutical compositions comprising at least one compound (I).
-
公开(公告)号:FR2837823A1
公开(公告)日:2003-10-03
申请号:FR0203788
申请日:2002-03-27
Applicant: SERVIER LAB
Inventor: LAVIELLE GILBERT , MULLER OLIVIER , MILLAN MARK , GOBERT ALAIN
IPC: A61K31/435 , A61K31/4439 , A61P1/14 , A61P3/04 , A61P15/00 , A61P15/10 , A61P25/00 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D401/12
Abstract: New pyridinyl benzo indole carboxamide derivatives (I) their enantiomers and diastereoisomers, and addition salts with acids and bases. New pyridinyl benzo indole carboxamide derivatives of formula (I) their enantiomers and diastereoisomers, and addition salts with acids and bases. R1+R2 together = a benzo ring that may be substituted by halogen, 1-6C alkyl, 1-6C alkoxy, CN, OH, NH2, 1-6C alkylamino, 1-6C dialkylamino, or CF3; R3 = H; or alternatively R1 = H; and R2+R3 together = a benzo ring optionally substituted as defined. An Independent claim is also included for the preparation of compounds of formula (I).
-
公开(公告)号:NO20031371L
公开(公告)日:2003-09-29
申请号:NO20031371
申请日:2003-03-26
Applicant: SERVIER LAB
Inventor: LAVIELLE GILBERT , MULLER OLIVIER , MILLAN MARK , GOBERT ALAIN
IPC: A61K31/435 , A61K31/4439 , A61P1/14 , A61P3/04 , A61P15/00 , A61P15/10 , A61P25/00 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D401/12 , A61P3/00
Abstract: New pyridinyl benzo indole carboxamide derivatives (I) their enantiomers and diastereoisomers, and addition salts with acids and bases. New pyridinyl benzo indole carboxamide derivatives of formula (I) their enantiomers and diastereoisomers, and addition salts with acids and bases. R1+R2 together = a benzo ring that may be substituted by halogen, 1-6C alkyl, 1-6C alkoxy, CN, OH, NH2, 1-6C alkylamino, 1-6C dialkylamino, or CF3; R3 = H; or alternatively R1 = H; and R2+R3 together = a benzo ring optionally substituted as defined. An Independent claim is also included for the preparation of compounds of formula (I).
-
公开(公告)号:NO315513B1
公开(公告)日:2003-09-15
申请号:NO20001542
申请日:2000-03-24
Applicant: SERVIER LAB
Inventor: PEGLION JEAN-LOUIS , GOUMENT BERTRAND , DESSINGES AIMEE , MILLAN MARK , DEKEYNE ANNE , RIVET JEAN-MICHEL
IPC: C07D491/056 , A61K31/40 , A61K31/403 , A61K31/407 , A61K31/4245 , A61P25/00 , A61P25/22 , A61P25/24 , A61P25/30 , A61P43/00 , C07D209/00 , C07D209/70 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D209/56
Abstract: cis-Benzo(3,4)cyclobuta(1,2-c)pyrrole derivatives (I) are new. cis-Benzo(3,4)cyclobuta(1,2-c)pyrrole derivatives of formula (I) and their isomers and salts are new. R1 - R3 = H, halogen, 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, OH, 1-6C alkoxy, cycloalkyl, cycloalkyl(1-6C)alkyl, aryl, aryl(1-6C)alkyl, aryloxy, aryl(1-6C)alkoxy, 1-6C trihaloalkyl, 1-6C trihaloalkoxy,CN, NO2, OSO2Me, OSO2CF3, NR6R7 or COOR6; or two adjacent R1 - R3 groups = 4-8C optionally saturated ring in which 1-2 C atoms can be replaced by O, N and/or S; R6, R7 = H, 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, cycloalkyl, cycloalkyl(1-6C)alkyl, aryl or aryl(1-6C)alkyl; R4 = H, 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, cycloalkyl, cycloalkyl(1-6C)alkyl, aryl, aryl(1-6C)alkyl, heterocycloalkyl, heterocycloalkyl(1-6C)alkyl, heteroaryl or heteroaryl(1-6C)alkyl; R5 = aryl or heteroaryl optionally substituted by halogen, OH, 1-6C alkyl, 1-6C alkoxy, 2-6C alkenyl, cycloalkyl, adamantyl, cycloalkyl(1-6C)alkyl, aryl, aryl(1-6C)alkyl, aryloxy, aryl(1-6C)alkoxy, 1-6C trihaloalkyl, CN, NO2, oxo, OSO2Me, OSO2CF3, NR6R7 or COOR6; n = 1 - 3; cycloalkyl = a 3-8C mono- or bicyclic optionally saturated ring system optionally substituted by halogen and/or 1-6C alkyl; heterocycloalkyl = cycloalkyl as defined in which the ring system contains 1-3 heteroatoms selected from O, N and S; aryl = phenyl, naphthyl, dihydronaphthyl, tetrahydronaphthyl, indenyl or indanyl; heteroaryl = aryl as defined containing 1-3 heteroatoms selected from O, N and S. An Independent claim is also included for a process for preparing (I).
-
公开(公告)号:BR0201312A
公开(公告)日:2003-06-10
申请号:BR0201312
申请日:2002-04-18
Applicant: SERVIER LAB
Inventor: LAVIELLE GILBERT , DUBUFFET THIERRY , MULLER OLIVIER , MILLAN MARK , DEKEYNE ANNE , BROCCO MAURICETTE
IPC: A61K31/519 , A61P1/14 , A61P15/10 , A61P15/12 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D471/00 , C07D471/04 , C07D491/048 , C07D491/052 , C07D513/00 , C07D519/00 , C07D403/06 , C07D413/06 , A61K31/513
Abstract: Compound of formula (I): wherein: R1, R2, R3 and R4, which may be the same or different, each represent a hydrogen atom, a halogen atom or a group selected from alkyl, alkoxy, polyhaloalkyl, hydroxy, cyano, nitro and amino, or R1 with R2, R2 with R3, or R3 with R4, together with the carbon atoms carrying them, form an optionally substituted benzene ring or an optionally substituted heteroaromatic ring, X represents an oxygen atom or a methylene group, A represents an alkylene chain, represents an optionally substituted, unsaturated, nitrogen-containing heterocycle and R5 represents an alkyl group, its enantiomers and diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid. a medicinal products containing the same are useful as a double alpha2/5-HT2c antagonist.
-
公开(公告)号:HK1049669A1
公开(公告)日:2003-05-23
申请号:HK03101849
申请日:2003-03-14
Applicant: SERVIER LAB
Inventor: LAVIELLE GILBERT , DUBUFFET THIERRY , MULLER OLIVIER , MILLAN MARK , DEKEYNE ANNE , BROCCO MAURICETTE
IPC: A61K31/519 , A61P1/14 , A61P15/10 , A61P15/12 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D471/00 , C07D471/04 , C07D491/048 , C07D491/052 , C07D513/00 , C07D519/00 , C07D , A61K , A61P
Abstract: Compound of formula (I): wherein: R1, R2, R3 and R4, which may be the same or different, each represent a hydrogen atom, a halogen atom or a group selected from alkyl, alkoxy, polyhaloalkyl, hydroxy, cyano, nitro and amino, or R1 with R2, R2 with R3, or R3 with R4, together with the carbon atoms carrying them, form an optionally substituted benzene ring or an optionally substituted heteroaromatic ring, X represents an oxygen atom or a methylene group, A represents an alkylene chain, represents an optionally substituted, unsaturated, nitrogen-containing heterocycle and R5 represents an alkyl group, its enantiomers and diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid. a medicinal products containing the same are useful as a double alpha2/5-HT2c antagonist.
-
公开(公告)号:NO314402B1
公开(公告)日:2003-03-17
申请号:NO996285
申请日:1999-12-17
Applicant: SERVIER LAB
Inventor: CORDI ALEX , MILLAN MARK , NEWMAN-TANCREDI ADRIAN , BROCCO MAURICETTE
IPC: A61K31/4184 , A61P3/04 , A61P15/10 , A61P25/00 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07D235/02
Abstract: Spiro(imidazoline-anthracene) derivatives (I) are new. Spiro(imidazoline-anthracene) derivatives of formula (I) and their base or acid addition salts are new. R1-R4 = H, 1-6C alkyl, 1-6C alkoxy, OH, 1-6C polyhalogenoalkyl, cyano, nitro, amino, 1-6C alkylamino, di (1-6C) alkylamino, 1-6C thioalkyl, 1-6C sulfonylalkyl, 1-6C sulfinylalkyl, carboxy, 1-6C alkoxycarbonyl, 1-6C alkylcarbonyloxy, formyl, carbamoyl, carboxamide, phenyl, benzyl or halo; B' = a group of formula (i) or (ii); R = H, 1-6C alkyl or benzyl. Independent claims are also included for: (1) the preparation of (I); and (2) pharmaceutical compositions comprising at least one compound (I).
-
-
-
-
-
-
-
-
-