公开(公告)号：NO314307B1

公开(公告)日：2003-03-03

申请号：NO980803

申请日：1998-02-26

Applicant: SERVIER LAB

Inventor： PEGLION JEAN-LOUIS ,  GOUMENT BERTRAND ,  MILLAN MARK ,  GOBERT ALAIN

IPC: A61K31/40 ,  A61K31/4025 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/495 ,  A61P3/04 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P43/00 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D411/04 ,  C07D413/14 ,  C07D491/056 ,  A61K31/4523

Abstract: 2-Amino indane derivatives formula (I), their racemic mixtures and optical isomers, and their salts are new: n = 1 or 2; Ar = heterocyclic rings (some substituted by X); X = H or F; R = H, 1-5C alkyl or aralkyl; E =H or Me; X1-X4 = H, halo, 1-5C alkyl, 1-5C alkoxy, CF3, OH, CN, NO2, NR1R2, CONR1R2, CO2R3, OCOR4 or a group of heterocyclic rings; or taken together, two adjacent X groups form a 5-6 membered ring containing C, S, O and/or N atoms; R1-R3 = H, 1-5C alkyl; and R4 = 1-5C alkyl.

公开(公告)号：DE69810560D1

公开(公告)日：2003-02-13

申请号：DE69810560

申请日：1998-10-01

Applicant: SERVIER LAB

Inventor： PEGLION JEAN-LOUIS ,  GOUMENT BERTRAND ,  MILLAN MARK ,  NEWMAN-TANCREDI ADRIAN ,  DEKEYNE ANNE

IPC: A61K31/4418 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61P25/00 ,  A61P25/04 ,  A61P43/00 ,  C07D311/18 ,  C07D319/18 ,  C07D401/10 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  A61K31/335 ,  A61K31/40

公开(公告)号：EA002979B1

公开(公告)日：2002-12-26

申请号：EA199901049

申请日：1999-12-17

Applicant: SERVIER LAB

Inventor： CIRDI 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: Изобретениеотноситсяк новымспироимидазолиновымсоединениямформулы (I)вкоторойА представляетнеобязательнозамещенноебензольноекольцо,Впредставляетимидазолиновоекольцоформулы (Ia) или (Ib)кспособуихполученияи лекарственнымсредствам.

公开(公告)号：ES2176156T3

公开(公告)日：2002-12-01

申请号：ES00400812

申请日：2000-03-24

Applicant: SERVIER LAB

Inventor： PEGLION JEAN-LOUIS ,  GOUMENT BERTRAND ,  DESSINGES AIMEE ,  MILLAN MARK ,  RIVET JEAN-MICHEL ,  DEKEYNE ANNE

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

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：DE69900961T2

公开(公告)日：2002-11-07

申请号：DE69900961

申请日：1999-08-20

Applicant: SERVIER LAB

Inventor： PEGLION JEAN-LOUIS ,  GOUMENT BERTRAND ,  MILLAN MARK ,  NEWMAN-TANCREDI ADRIAN

IPC: C07D211/58 ,  A61K31/00 ,  A61K31/443 ,  A61K31/445 ,  A61P3/00 ,  A61P3/04 ,  A61P9/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00 ,  C07D405/04 ,  A61K31/35

Abstract: A compound selected from those of formula (I): wherein: R1, R2, R3 and R4, which may be identical or different, represent hydrogen, halogen, alkyl, alkenyl, alkynyl, hydroxy, alkoxy, trihaloalkyl, or any pair may form a heterocycle, R5 represents hydrogen, alkyl, or arylalkyl, R6 represents hydrogen, halogen, alkyl, hydroxy, alkoxy, or trihaloalkyl, A, together with the carbons of the phenyl, represents a heterocycle, their isomers and addition pharmaceutically-acceptable acid or base salts thereof, and medicinal products containing the same which are useful in the treatment of pathologies in which 5HT1B receptors are involved.

公开(公告)号：EA200200379A2

公开(公告)日：2002-10-31

申请号：EA200200379

申请日：2002-04-17

Applicant: SERVIER LAB

Inventor： LAVIELLE GIBERT ,  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

Abstract: Соединениеформулы (I)вкоторой R, R, Rи R, которыемогутбытьодинаковымиилиразличными, каждыйпредставляютсобойатомводорода, атомгалогенаилигруппу, выбираемуюизалкила, алкокси, полигалоалкил, гидрокси, циано, нитрои амино, или Rи R, Rи R, или Rи R, совместнос атомамиуглерода, ихнесущими, образуютнеобязательнозамещенноебензоловоекольцоилинеобязательнозамещенноегетероароматическоекольцо,Хпредставляетсобойатомкислородаилиметиленовуюгруппу,Апредставляетсобойлинейнуюилиразветвленную (С-С)алкиленовуюцепь,представляетсобойненасыщенныйазотсодержащийгетероцикл, иRпредставляетсобойалкильнуюгруппу,егоэнантиомерыи диастереоизомеры, атакжеегоаддитивныесолис фармацевтическиприемлемойкислотойилиоснованием,Лекарственныепрепараты.

公开(公告)号：NO20021806L

公开(公告)日：2002-10-21

申请号：NO20021806

申请日：2002-04-17

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 ,  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：ES2172294T3

公开(公告)日：2002-09-16

申请号：ES99402092

申请日：1999-08-20

Applicant: SERVIER LAB

Inventor： PEGLION JEAN-LOUIS ,  GOUMENT BERTRAND ,  MILLAN MARK ,  NEWMAN-TANCREDI ADRIAN

IPC: C07D211/58 ,  A61K31/00 ,  A61K31/443 ,  A61K31/445 ,  A61P3/00 ,  A61P3/04 ,  A61P9/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00 ,  C07D405/04 ,  A61K31/35

Abstract: A compound selected from those of formula (I): wherein: R1, R2, R3 and R4, which may be identical or different, represent hydrogen, halogen, alkyl, alkenyl, alkynyl, hydroxy, alkoxy, trihaloalkyl, or any pair may form a heterocycle, R5 represents hydrogen, alkyl, or arylalkyl, R6 represents hydrogen, halogen, alkyl, hydroxy, alkoxy, or trihaloalkyl, A, together with the carbons of the phenyl, represents a heterocycle, their isomers and addition pharmaceutically-acceptable acid or base salts thereof, and medicinal products containing the same which are useful in the treatment of pathologies in which 5HT1B receptors are involved.

公开(公告)号：SI1038873T1

公开(公告)日：2002-08-31

申请号：SI200030008

申请日：2000-03-24

Applicant: SERVIER LAB

Inventor： PEGLION JEAN-LOUIS ,  GOUMENT BERTRAND ,  DESSINGES AIMEE ,  MILLAN MARK ,  RIVET JEAN-MICHEL ,  DEKEYNE ANNE

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

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：DE60000142D1

公开(公告)日：2002-06-06

申请号：DE60000142

申请日：2000-03-24

Applicant: SERVIER LAB

Inventor： PEGLION JEAN-LOUIS ,  GOUMENT BERTRAND ,  DESSINGES AIMEE ,  MILLAN MARK ,  RIVET JEAN-MICHEL ,  DEKEYNE ANNE

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

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).