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公开(公告)号:AT291577T
公开(公告)日:2005-04-15
申请号:AT00402799
申请日:2000-10-11
Applicant: SERVIER LAB
Inventor: LAVIELLE GILBERT , MULLER OLIVIER , MILLAN MARK , CUSSAC DIDIER , DEKEYNE ANNE
IPC: A61K31/395 , A61K31/40 , A61K31/4045 , A61K31/428 , A61K31/437 , A61K31/502 , A61K31/505 , A61K31/513 , A61K31/517 , A61K31/519 , A61K31/53 , A61K31/54 , A61P1/08 , A61P25/00 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/30 , A61P43/00 , C07D401/14 , C07D403/14 , C07D405/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
Abstract: Cyano indoles (I), their enantiomers, diastereoisomers, and their salts with acids and bases, their preparation, and pharmaceutical compositions containing them. Cyano indoles of formula (I): R1 and R2 = H or 1-6C alkyl; T1 and T2 = 1-6C alkylene; G = a heterocyclic group of formula (a) or (b); W1, W2 and W3 = N, CR5, NR4 or CO; W4 = N, CR3, NR4, or CO; W5 = C or N; X1 = a bond, N, CR3 or NR4; X2 to X4 = CR3, NR4, CO, SR4, SO2, O, S, or N; R3 = H, halogen, 1-6C alkyl, OH, 1-6C perhaloalkyl, NO2, NH2, mono- or di alkylamino, or benzylamino; R4 = H, 1-6C alkyl, or optionally substituted aryl or aralkyl; and R5 = a group R3 or two adjacent groups R5 form, together with the C atoms to which they are attached, a saturated or unsaturated mono- or bicyclic group that may contain 1-5 O, N, or S hetero atoms and which may be substituted by R3 or oxo.
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公开(公告)号:ES2227088T3
公开(公告)日:2005-04-01
申请号:ES01401712
申请日:2001-06-29
Applicant: SERVIER LAB
Inventor: LAVIELLE GILBERT , MULLER OLIVIER , MILLAN MARK , DEKEYNE ANNE , BROCCO MAURICETTE
IPC: A61K31/4164 , A61K31/4168 , A61K31/4174 , A61K31/4178 , A61K31/4725 , A61K31/495 , A61K31/496 , A61K31/497 , C07D295/08 , A61P15/00 , A61P15/10 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , C07C275/28 , C07D209/08 , C07D233/24 , C07D233/50 , C07D233/54 , C07D233/64 , C07D233/66 , C07D235/10 , C07D235/14 , C07D235/30 , C07D295/12 , C07D295/135 , C07D319/20 , C07D401/04 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/12
Abstract: Compuestos de **Fórmula** en la cual: R1, R2, R3, R4 representan independientemente un átomo de hidrógeno, de halógeno, un grupo alquilo, alcoxilo, hidroxilo, alquiltio, mercapto, ciano, amino (eventualmente sustituido por uno o dos grupos alquilo), nitro, carboxilo, alcoxicarbonilo, aminocarbonilo (eventualmente sustituido por uno o dos grupos alquilo) o carbamoilo, o bien R3 y R4 forman junto con los átomos de carbono a los cuales están unidos un ciclo fenilo y L1, L2 forman juntos un grupo -CH2-CH2-, L1 y L2 representan cada uno un átomo de hidrógeno o forman juntos un grupo -CH2-CH2-, X1, unido en la posición 2 o 3 del ciclo aromático, representa un enlace y en este caso X2 representa un átomo de hidrógeno, de halógeno o un grupo alquilo, alcoxilo, hidroxilo, nitro, ciano o amino (eventualmente sustituido por uno o dos grupos alquilo).
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公开(公告)号:ES2227082T3
公开(公告)日:2005-04-01
申请号:ES01400939
申请日:2001-04-12
Applicant: SERVIER LAB
Inventor: PEGLION JEAN-LOUIS , GOUMENT BERTRAND , MILLAN MARK , LEJEUNE FRANCOISE , CUSSAC DIDIER
IPC: A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4545 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/30 , C07D401/12 , C07D401/14
Abstract: Compuesto de **Fórmula** en la cual: n representa un número entero comprendido entre 0 y 6, R1 representa un grupo seleccionado entre hidrógeno, hidroxi, ciano, alcoxi(C1-C6) lineal o ramificado, alcoxicarbonilo(C1-C6) lineal o ramificado, carboxi, aminocarbonilo (siendo la parte amino eventualmente sustituida por uno o dos grupos, idénticos o diferentes, seleccionados entre alquilo(C1-C6) lineal o ramificado, arilo y arilalquilo(C1-C6) lineal o ramificado), y NR4R5 donde R4 y R5, idénticos o diferentes, representan un grupo seleccionado entre alquilo(C1-C6) lineal o ramificado, arilo, arilalquilo(C1-C6) lineal o ramificado, heteroarilo, heteroarilalquilo(C1-C6) lineal o ramificado, cicloalquilo, cicloalquilalquilo(C1-C6) lineal o ramificado, alquenilo(C2-C6) lineal o ramificado, y alquinilo(C2-C6) lineal o ramificado, R2 representa un grupo seleccionado entre un átomo de hidrógeno, un grupo alquilo(C1-C6) lineal o ramificado, hidroximetilo.
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64.
公开(公告)号:AU780022B2
公开(公告)日:2005-02-24
申请号:AU5414401
申请日:2001-06-29
Applicant: SERVIER LAB
Inventor: LAVIELLE GILBERT , MULLER OLIVIER , MILLAN MARK , DEKEYNE ANNE , BROCCO MAURICETTE
IPC: C07D295/08 , A61K31/4164 , A61K31/4168 , A61K31/4174 , A61K31/4178 , A61K31/4725 , A61K31/495 , A61K31/496 , A61K31/497 , A61P15/00 , A61P15/10 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , C07C275/28 , C07D209/08 , C07D233/24 , C07D233/50 , C07D233/54 , C07D233/64 , C07D233/66 , C07D235/10 , C07D235/14 , C07D235/30 , C07D295/12 , C07D295/135 , C07D319/20 , C07D401/04 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/12 , C07D209/40 , C07D209/42 , C07D211/34 , C07D233/48 , C07D401/12 , C07D403/12 , C07D405/10 , C07D413/04
Abstract: Heterocyclic-substituted N,N'-diphenylurea derivatives (I) are new. Urea derivatives of formula (I) and their enantiomers, diastereomers and acid or base addition salts are new. R1 - R4 = H, halo, alkyl, alkoxy, OH, alkylthio, SH, CN, NH2, mono- or dialkylamino, NO2, COOH, alkoxycarbonyl, CONH2 or mono- or dialkylaminocarbonyl; or two adjacent groups together complete a fused benzene ring or a 5-7 membered heteroaryl ring containing 1-3 of N, O and/ore S as heteroatoms; L1, L2 = H or together form CH2CH2; X1 = direct bond (bonded in the 2- or 3-position of the ring); and X2 = H, halo, alkyl, alkoxy, OH, NO2, CN, NH2 or mono- or dialkylamino; or X1 + X2 = group forming a 4-7C ring with the C atoms in the 3- and 4-positions of the ring, 1 or 2 CH2 units of the ring optionally being replaced by O, NH or N(alkyl) and G being bonded to a ring C; X3 = H, halo, alkyl, alkoxy, OH, NO2, CN, NH2 or mono- or dialkylamino; G = heterocyclic group of formula (G1)-(G3); dotted line = optional bond; Alk = 1-6C alkylene, which must be bonded at the 2-position in an imidazoline ring of (G1); n, m = 0 or 1; T3, T4 = alkyl; or aryl, arylalkyl, heteroaryl or heteroarylalkyl (all optionally ring-substituted by one or more of halo, alkyl, alkoxy, OH, SH, alkylthio, CN, NH2, mono- or dialkylamino, NO2, COOH, alkoxycarbonyl, CONH2 or mono- or dialkylaminocarbonyl; heteroaryl rings may additionally be mono-substituted by oxo); aryl moieties = phenyl, naphthyl or biphenylyl; heteroaryl moieties = mono- or bicyclic group in which at least one ring is aromatic, containing 1-5 of N, O and/or S as heteroatom(s); alkyl moieties have 1-6C. Independent claims are included for the preparation of (I).
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公开(公告)号:DE69823411T2
公开(公告)日:2005-02-17
申请号:DE69823411
申请日:1998-02-27
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 , C07D491/04 , A61K31/38
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.
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公开(公告)号:ES2223110T3
公开(公告)日:2005-02-16
申请号:ES98400711
申请日:1998-03-26
Applicant: SERVIER LAB
Inventor: PEGLION JEAN-LOUIS , GOUMENT BERTRAND , MILLAN MARK , GOBERT ALAIN , AUDINOT VALERIE
IPC: A61K31/443 , A61K31/4433 , A61K31/445 , A61P3/00 , A61P9/00 , A61P25/04 , A61P25/18 , A61P25/30 , C07D405/04 , C07D409/04 , C07D411/04 , C07D471/04 , A61K31/40
Abstract: N - ARIL PIPERIDINAS DE FORMULA I: DONDE M = 1-5; N = 1,2; R REPRESENTA UN ATOMO DE HIDROGENO, UN RADICAL ALQUILO O ARALQUILO; E REPRESENTA UN ATOMO DE HIDROGENO O UN RADICAL METILO; AR REPRESENTA: A REPRESENTA: Y X, X 1 , X 2 , X 3 Y X 4 REPRESENTAN UN ATOMO DE HIDROGENO O CIERTOS SUSTITUTIVOS. ESTOS COMPUESTOS SON LIGANDOS DEL RECEPTOR 5 - HT 1 B Y RESULTAN UTILES PARA EL TRATAMIENTO DE ENFERMEDADES EN LAS QUE ESTE IMPLICADO EL SISTEMA SEROTONINERGICO.
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公开(公告)号:NO318158B1
公开(公告)日:2005-02-07
申请号:NO20011862
申请日:2001-04-11
Applicant: SERVIER LAB
Inventor: BROCCO MAURICETTE , PEGLION JEAN-LOUIS , GOUMENT BERTRAND , MILLAN MARK , LEJEUNE FRANCOISE , DESSINGES AIMEE
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 , C07C211/27
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).
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公开(公告)号:MA27109A1
公开(公告)日:2004-12-20
申请号:MA27861
申请日:2004-09-16
Applicant: SERVIER LAB
Inventor: LAVIELLE GILBERT , MULLER OLIVIER , MILLAN MARK , GOBERT ALAIN , DI-CARA BENJAMIN
IPC: A61K31/496 , A61P15/00 , A61P15/10 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D209/60 , C07D401/12 , C07D403/12 , C07D403/02 , A61K31/395
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69.
公开(公告)号:ES2220359T3
公开(公告)日:2004-12-16
申请号:ES00402359
申请日:2000-08-25
Applicant: SERVIER LAB
Inventor: PEGLION JEAN-LOUIS , DESSINGES AIMEE , POITEVIN CHRISTOPHE , MILLAN MARK , DEKEYNE ANNE
IPC: C07D409/14 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/4545 , A61K31/496 , A61P25/00 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , C07D471/04 , C07D491/04 , C07D491/048 , C07D495/04
Abstract: Compuestos de **Fórmula** en la cual: W representa: - bien un grupo naftilo eventualmente sustituido por uno o varios grupos, idénticos o diferentes, elegidos entre halógeno, alquilo de 1 a 6 átomos de carbono lineal o ramificado, hidroxilo, alcoxilo de 1 a 6 carbonos lineal o ramificado, ciano, nitro, trihalogenoalquilo de 1 a 6 carbonos lineal o ramificado, metilendioxilo y etilendioxilo, - bien un grupo en la cual E representa, con los átomos de carbono del ciclo fenilo a los cuales está unido, un sistema monocíclico, no saturado, parcialmente saturado, o aromático, de 5 a 7 eslabones, que constan de al menos un heteroátomo elegido entre oxígeno, nitrógeno, azufre, pudiendo estar unido dicho grupo Y al grupo (CH2)n de los compuestos de Fórmula (I), bien sea por la parte fenilo, bien sea por el sistema monocíclico E, pudiendo estar cada uno de dichos grupos Y, eventualmente sustituidos por uno o varios grupos, idénticos o diferentes, elegidos entre halógeno, hidroxilo, ciano, nitro, alquilo de 1 a 6 carbonos lineal o ramificado, alcoxilo de 1 a 6 carbonos lineal o ramificado, tri- halogenoalquilo de 1 a 6 carbonos lineal o ramificado, heterocicloalquilalquileno de 1 a 6 carbonos lineal o ramificado (en el cual el heterociclo es un sistema monocíclico no saturado o aromático, de 5 a 6 eslabones, que contiene de 1 a 4 heteroátomos elegidos entre nitrógeno, azufre y oxígeno) y el grupo oxo.
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公开(公告)号:PT1146044E
公开(公告)日:2004-11-30
申请号:PT01400939
申请日:2001-04-12
Applicant: SERVIER LAB
Inventor: PEGLION JEAN-LOUIS , MILLAN MARK , LEJEUNE FRANCOISE , GOUMENT BERTRAND , CUSSAC DIDIER
IPC: A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4545 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/30 , C07D401/12 , C07D401/14
Abstract: Cyclobuta-indole derivatives (I), their isomers and salts are new. The new compounds are of formula (I): n = 0 - 6; R1 = H, OH, CN, alkoxy, alkoxycarbonyl, carboxy, amino carbonyl (optionally substituted by one or two alkyl, aryl, or aralkyl groups), or NR4R5; R2 = H, alkyl, CH2OH, a croup -(OH)(T), or -U'-V'-W'; T = 3-12C mono- or polycyclic cycloalkyl that may have one C atom replaced by O, Se, S, SO, SO2, or SiR6R7; R3 = H, alkyl, aryl, or heteroaryl; R4 and R5 = alkyl, aryl, aralkyl, heteroaryl, heteroaryl alkyl, cycloalkyl, cycloalkyl alkyl, alkenyl or alkynyl; R6 and R7 = alkyl; U' = methylene or a bond; V' = a bond, O, S, SO, or SO2; and W' = aryl aralkyl, cycloalkyl, or cycloalkyl alkyl. All alkyl, alkoxy, alkenyl and alkynyl groups having up to 6 C atoms, aryl, heteroaryl and cycloalkyl groups may be mono or polycyclic, aryl and heteroaryl groups may be mono or polysubstituted and cycloalkyl groups may contain unsaturation.
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