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公开(公告)号:HU226059B1
公开(公告)日:2008-04-28
申请号:HU9801951
申请日:1998-08-31
Applicant: SERVIER LAB
Inventor: HARMANGE JEAN-CHRISTOPHE , LEJEUNE FRANCOISE , MILLAN MARK , PEGLION JEAN-LOUIS
IPC: C07D265/36 , A61K31/535 , A61K31/538 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , A61P43/00 , C07D265/34
Abstract: Trans-3,4,4a,5,6,10b-hexahydro-2H-naphthÄ1,2-bÜ-1,4-oxazines of formula (I), their optical isomers, and their acid addition salts are new. A = 1-10C alkyl, 3-10C alkenyl, or 3-10 alkynyl (all optionally substituted by one or more 3-8C cycloalkyl or by aryl (phenyl, thienyl or pyridyl (optionally substituted by one or more halo, hydroxy, 1-6C alkyl or 1-6C alkoxy))); E = CN, C(=O)-CH3, C(=O)-NR1R2, or C(=O)-OR3; R1, R2 = H or A; and R3 = H or 1-5C alkyl.
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公开(公告)号:TR200402685T4
公开(公告)日:2004-11-22
申请号:TR200402685
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: 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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公开(公告)号:EA004473B1
公开(公告)日:2004-04-29
申请号:EA200100343
申请日:2001-04-12
Applicant: SERVIER LAB
Inventor: PEGLION JEAN-LOUIS , DESSINGES AIMEE , GOUMENT BERNARD , 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 , C07D209/14 , A61P25/00
Abstract: Визобретенииописанысоединенияформулы (I)гдеобозначаетпростуюилидвойнуюсвязь,n обозначаетцелоечислоот 1 до 6 включительно,Rи Rобозначаютгруппу, выбраннуюизряда, включающегоатомводорода, линейнуюилиразветвленнуюС-Салкильнуюгруппу, арильнуюгруппу, арилалкильнуюгруппу, циклоалкильнуюгруппу, циклоалкилалкильнуюгруппу, алкенильнуюгруппу, алкинильнуюгруппу, гетероциклоалкильнуюгруппу, гетероциклоалкилалкильнуюгруппу, гетероарильнуюгруппуи гетероарилалкильнуюгруппу,Хобозначаетгруппу, выбраннуюизряда, включающего -СН=СН-, атомкислорода, группу S(O), где m обозначаетцелоечислоот 0 до 2 включительно, и NR, где Rимеетзначения, указанныев описании,Y обозначаетСН- илиСН-группу, взависимостиоттого, обозначаетлипростуюсвязьилидвойнуюсвязь, илиможеттакжеобозначатьатомкислорода, когдаХ обозначаетатомкислорода,Тобозначаетциклопентильнуюилициклогексильнуюгруппу,ихизомерыи аддитивныесолис фармацевтическиприемлемойкислотойилиоснованием.Такжеописанылекарственныесредства.
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公开(公告)号:HU222728B1
公开(公告)日:2003-09-29
申请号:HU9801423
申请日:1998-06-23
Applicant: SERVIER LAB
Inventor: DUBUFFET THIERRY , HAUTEFAYE PATRICK , LAVIELLE GILBERT , LEJEUNE FRANCOISE , MILLAN MARK
IPC: A61K31/40 , A61K31/435 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07B53/00 , C07D491/04 , C07D491/052
Abstract: Hexahydro-chromeno-Ä3,4-cÜ-pyrrole derivatives of formula (I), their enantiomers, diastereoisomers and salts are new. m = 0-3; n = 0-3; n+m = 2 or 3; p = 1-6; the junction between rings B and C is trans; X = CN or -CONR4R5; R4, R5 = H, 1-6C alkyl, 3-7C cycloalkyl or optionally substituted aryl; A = sigma bond or -NR-CO-, -CO-NR-, -NR-SO2-, or -SO2-NR-; R = H or 1-6C alkyl; R1, R2 = H or 1-6C alkyl; R3 = H or phenyl, naphthyl or heteroaryl (all optionally substituted by one or more halo, 1-6C alkyl or alkoxy, OH, CN, NH2, NO2, COOH, 1-6C perhaloalkyl, sulphonyl, acylamino, 1-6C alkylsulphonyl, or 1-6C alkyl sulphonylamino), aryl or heteroaryl (both substituted by A'-Cy), 2-indolinon-5-yl, or, when A is a sigma bond, aryloxy or arylthio; A' = sigma bond or 1-6C alkylene or alkenylene, (in which one C atom may be replaced by O or S), -NR-CO-, -CO-NR-, -NR-SO2-, or -SO2-NR-; Cy = aryl or heteroaryl (optionally substituted); provided that when n = 0, then m is other than 2, when n = 1, R1, R2 = H, A = sigma bond and p = 1, then R3 is not phenyl nor pyridyl, when n = 1, R1 & R2 = H, A = sigma bond, R3 is not H, when n = 1, R1 & R2 = H, A = -NH-CO-, then R3 is other than H, phenyl, naphthyl, thienyl, furyl, pyrrolyl, pyridyl, (all optionally substituted by one or more halo, trihalomethyl, alkoxy or OH).
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公开(公告)号:PT899267E
公开(公告)日:2003-04-30
申请号:PT98402155
申请日:1998-09-01
Applicant: SERVIER LAB
Inventor: PEGLION JEAN-LOUIS , MILLAN MARK , HARMANGE JEAN-CHRISTOPHE , LEJEUNE FRANCOISE
IPC: A61K31/535 , A61K31/538 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07D265/34
Abstract: Trans-3,4,4a,5,6,10b-hexahydro-2H-naphthÄ1,2-bÜ-1,4-oxazines of formula (I), their optical isomers, and their acid addition salts are new. A = 1-10C alkyl, 3-10C alkenyl, or 3-10 alkynyl (all optionally substituted by one or more 3-8C cycloalkyl or by aryl (phenyl, thienyl or pyridyl (optionally substituted by one or more halo, hydroxy, 1-6C alkyl or 1-6C alkoxy))); E = CN, C(=O)-CH3, C(=O)-NR1R2, or C(=O)-OR3; R1, R2 = H or A; and R3 = H or 1-5C alkyl.
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公开(公告)号:HU0101503A2
公开(公告)日:2002-05-29
申请号:HU0101503
申请日:2001-04-12
Applicant: SERVIER LAB
Inventor: BROCCO MAURICETTE , DESSINGES AIMEE , GOUMENT BERTRAND , LEJEUNE FRANCOISE , MILLAN MARK , PEGLION JEAN-LOUIS
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 , C07D307/79
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:EA200100343A3
公开(公告)日:2002-02-28
申请号:EA200100343
申请日:2001-04-12
Applicant: SERVIER LAB
Inventor: PEGLION JEAN-LOUIS , DESSINGES AIMEE , GOUMENT BERNARD , 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: Взаявкеописанысоединенияформулы (I)гдеобозначаетпростуюилидвойнуюсвязь,n обозначаетцелоечислоот 1 до 6 включительно,Rи Rобозначаютгруппу, выбраннуюизряда, включающегоатомводорода, линейнуюилиразветвленнуюС-Салкильнуюгруппу, арильнуюгруппу, арилалкильнуюгруппу, циклоалкильнуюгруппу, циклоалкилалкильнуюгруппу, алкенильнуюгруппу, алкинильнуюгруппу, гетероциклоалкильнуюгруппу, гетероциклоалкилалкильнуюгруппу, гетероарильнуюгруппуи гетероарилалкильнуюгруппу,Хобозначаетгруппу, выбраннуюизряда, включающего -СН=СН-, атомкислорода, группу S(O), где m обозначаетцелоечислоот 0 до 2 включительно, и NR, где Rимеетзначения, указанныев описании,Y обозначаетСН- илиСН-группув зависимостиоттого, обозначаетлипростуюсвязьилидвойнуюсвязь, илиможеттакжеобозначатьатомкислорода, когдаХ обозначаетатомкислорода,ТобозначаетмоноциклическуюилиполициклическуюС-Сциклоалкильнуюгруппу, необязательносодержащуюв кольцевойсистемеатомкислорода, атомселена, группуформулы S(O), NRили SiRR, гдер, R, Rи R, имеютзначения, указанныев описании,ихизомерыи аддитивныесолис фармацевтическиприемлемойкислотойилиоснованием. Такжеописанылекарственныесредства.
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公开(公告)号:AR042379A1
公开(公告)日:2005-06-22
申请号:ARP010101714
申请日:2001-04-11
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 , A61K31/403
Abstract: Compuestos de fórmula (1) en la cual: n representa un entero comprendido entre 0 y 6; R1 representa un grupo elegido entre H, hidroxi, ciano, alcoxi, alcoxicarbonilo, carboxi, aminocarbonilo eventualmente sustituidos y NR4R5 en el cual R4 y R5, son tal como se los ha definido en la descripción; R2 representa un grupo elegido entre H, alquilo, hidroximetilo, un grupo de fórmula (2) y -U-V-W en la cual T, U, V, y W son tal como se los ha definido en la descripción, y R3 representa un grupo elegido entre H, alquilo C1-6 lineal o ramificado, arilo y heteroarilo, sus isómeros, así como sus sales de adición con un ácido o con una base farmacéuticamente aceptable. Medicamentos útiles para el tratamiento de la ansiedad, de los ataques de pánico, desórdenes obsesivo compulsivos, fobias, desórdenes impulsivos, abuso de drogas, desórdenes cognitivos, psicosis, depresiones, desórdenes del humor.
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公开(公告)号:AU779366B2
公开(公告)日:2005-01-20
申请号:AU3518601
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 , A61K31/4462 , A61P25/28
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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公开(公告)号:SI1146044T1
公开(公告)日:2004-12-31
申请号:SI200130181
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: 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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