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    95.
    发明专利
    未知

    公开(公告)号：BR0315996A

    公开(公告)日：2005-09-27

    申请号：BR0315996

    申请日：2003-11-04

    Applicant: SERVIER LAB

    Inventor： RAULT SYLVAIN ,  LEFLEMME NICOLAS ,  DALLEMAGNE PATRICK ,  LESTAGE PIERRE ,  LOCKHART BRIAN ,  DANOBER LAURENCE ,  PFEIFFER BRUNO ,  RENARD PIERRE

    IPC: A61P25/04 ,  A61P25/28 ,  C07D211/86 ,  C07D401/04 ,  C07D409/04 ,  A61K31/44

    Abstract: 2,3-Dihydro-4(1H)-pyridinone derivatives (I), their enantiomers, diastereoisomers, and acid addition salts are new. 2,3-Dihydro-4(1H)-pyridinone derivatives (I), their enantiomers, diastereoisomers, and acid addition salts are new. R1 = H, 1-6C alkyl, acyl, alkoxycarbonyl, aralkyl aralkoxycarbonyl, or trifluoroacetyl; R2 = 1-6C alkyl; X = O or NOR3; R3 = H, 1-6C alkyl (optionally substituted by OH, amino, alkylamino, dialkylamino and alkoxy); Ar = aryl or heteroaryl where aryl groups may be phenyl, biphenylyl, naphthyl, or tetrahydronaphthyl, all of which are optionally substituted by halogens, alkyl, OH, alkoxy, trihalomethyl, nitro, amino, alkylamino and dialkylamino groups, and heteroaryl groups may be mono or bicyclic and may be substituted by halogens, alkyl, OH, alkoxy, trihalomethyl, nitro, amino, alkylamino and dialkylamino groups.

    Octahydro-2H-pyrido(1,2-a)pyrazine derivatives, process for their preparation and pharmaceutical compositions containing them
    98.
    发明专利
    Octahydro-2H-pyrido(1,2-a)pyrazine derivatives, process for their preparation and pharmaceutical compositions containing them 未知

    公开(公告)号：SI1275647T1

    公开(公告)日：2004-02-29

    申请号：SI200230005

    申请日：2002-07-11

    Applicant: SERVIER LAB

    Inventor： GOLDSTEIN SOLO ,  POISSONNET GUILLAUME ,  PARMENTIER JEAN-GILLES ,  LESTAGE PIERRE ,  LOCKHART BRIAN

    IPC: A61K31/4985 ,  A61K31/5025 ,  A61P3/04 ,  A61P25/00 ,  A61P25/04 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00 ,  C07D221/00 ,  C07D241/00 ,  C07D471/04

    Abstract: Octahydro-2H-pyrido(1,2-a) pyrazine derivatives (I), their enantiomers, diastereoisomers, and salts with acids and bases are new. Octahydro-2H-pyrido(1,2-a) pyrazine derivatives of formula (I), their enantiomers, diastereoisomers, and salts with acids and bases are new. Ra = 1-6C alkylene chain; Y = aryl, heteroaryl, or a fused bicyclic ring of formula (a); W1 and W2 = O, S, or NR2; R2 = H, 1-6C alkyl or acyl, aryl, or arylalkyl; R1 = H or 1-6C alkyl; A = a 4-7 membered N heterocycle which is unsaturated or partially saturated (optionally containing a second hetero atom (O, N or S) and optionally substituted by oxo, or 1-6C alkyl); and B = phenyl (optionally substituted by one or more groups selected from halogens, nitro, CN, OH, 1-6C (alkoxy, alkyl, trihaloalkyl, acyl, acyloxy, alkoxycarbonyl or alkylsulfanyl), sulfanyl or amino (optionally substituted by one or two 1-6C alkyl, aryl and 1-6C arylalkyl groups). Provided that: (1) when Y is aryl or heteroaryl, then X is W1, -C(W1)-W2-, -W2-C(W1)-, -W2-C(W1)W2-, -W2-Ra, or -CH(OR1); (2) when Y is a fused bicyclic ring, then X is a simple bond, -C(W1)-, -W2-C(W1)-, -W2-Ra, or -CH(OR1); and (3) compounds 2-octahydro-2H-pyrido(1,2-a)pyrazin-2-yl-1-phenyl ethanol;3-octahydro-2H-pyrido(1,2-a)pyrazin-2-yl propyl-3,4,5-trimethoxy benzoate; and 2-octahydro-2H-pyrido(1,2-a)pyrazin-2-yl ethyl-3,4,5-trimethoxy benzoate are excluded.

    New octahydro-2h-pyridoÄ1,2-aÜpyrazine compounds, a process for their preparation and pharmaceuticalcompositions containing them.
    99.
    发明专利
    New octahydro-2h-pyridoÄ1,2-aÜpyrazine compounds, a process for their preparation and pharmaceuticalcompositions containing them. 未知

    公开(公告)号：HK1050682A1

    公开(公告)日：2003-07-04

    申请号：HK03102800

    申请日：2003-04-17

    Applicant: SERVIER LAB

    Inventor： GOLDSTEIN SOLO ,  POISSONNET GUILLAUME ,  PARMENTIER JEAN-GILLES ,  LESTAGE PIERRE ,  LOCKHART BRIAN

    IPC: A61K31/4985 ,  A61K31/5025 ,  A61P3/04 ,  A61P25/00 ,  A61P25/04 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00 ,  C07D221/00 ,  C07D241/00 ,  C07D471/04 ,  C07D ,  A61K ,  A61P

    Abstract: Octahydro-2H-pyrido(1,2-a) pyrazine derivatives (I), their enantiomers, diastereoisomers, and salts with acids and bases are new. Octahydro-2H-pyrido(1,2-a) pyrazine derivatives of formula (I), their enantiomers, diastereoisomers, and salts with acids and bases are new. Ra = 1-6C alkylene chain; Y = aryl, heteroaryl, or a fused bicyclic ring of formula (a); W1 and W2 = O, S, or NR2; R2 = H, 1-6C alkyl or acyl, aryl, or arylalkyl; R1 = H or 1-6C alkyl; A = a 4-7 membered N heterocycle which is unsaturated or partially saturated (optionally containing a second hetero atom (O, N or S) and optionally substituted by oxo, or 1-6C alkyl); and B = phenyl (optionally substituted by one or more groups selected from halogens, nitro, CN, OH, 1-6C (alkoxy, alkyl, trihaloalkyl, acyl, acyloxy, alkoxycarbonyl or alkylsulfanyl), sulfanyl or amino (optionally substituted by one or two 1-6C alkyl, aryl and 1-6C arylalkyl groups). Provided that: (1) when Y is aryl or heteroaryl, then X is W1, -C(W1)-W2-, -W2-C(W1)-, -W2-C(W1)W2-, -W2-Ra, or -CH(OR1); (2) when Y is a fused bicyclic ring, then X is a simple bond, -C(W1)-, -W2-C(W1)-, -W2-Ra, or -CH(OR1); and (3) compounds 2-octahydro-2H-pyrido(1,2-a)pyrazin-2-yl-1-phenyl ethanol;3-octahydro-2H-pyrido(1,2-a)pyrazin-2-yl propyl-3,4,5-trimethoxy benzoate; and 2-octahydro-2H-pyrido(1,2-a)pyrazin-2-yl ethyl-3,4,5-trimethoxy benzoate are excluded.

    100.
    发明专利
    未知

    公开(公告)号：AT236129T

    公开(公告)日：2003-04-15

    申请号：AT99402624

    申请日：1999-10-22

    Applicant: SERVIER LAB

    Inventor： CASARA PATRICK ,  DOREY GILBERT ,  LESTAGE PIERRE ,  LOCKHART BRIAN

    IPC: C07D215/06 ,  A61K31/47 ,  A61K31/497 ,  A61K31/517 ,  A61P9/10 ,  A61P25/00 ,  A61P25/08 ,  A61P25/16 ,  A61P25/28 ,  A61P27/12 ,  A61P43/00 ,  C07D215/20 ,  C07D221/20 ,  C07D401/06 ,  C07D471/10 ,  C07D221/00

    Abstract: Dihydro- and tetrahydro-quinoline derivatives (I) are new. Dihydro- and tetrahydro-quinoline derivatives of formula (I) and their acid or base addition salts are new. R1 = H or a group of formula (i); A = H or -B'NZ1Z2; B' = 1-6C alkylene; Z1, Z2 = H, alkyl, 3-8C cycloalkyl or optionally substituted aryl; or NZ1Z2 = heterocycloalkyl or heteroaryl (optionally substituted); R2, R3 = alkyl, 3-8C cycloalkyl, heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, optionally substituted arylalkyl, optionally substituted heteroarylalkyl or aminoalkyl (optionally substituted on N with 1 or 2 alkyl, cycloalkyl, aryl or arylalkyl); or R2 + R3 = form with C of quinoline, 3-8C cycloalkyl or heterocycloalkyl (optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl); R40 = alkyl, 2-6C alkenyl, 2-6C alkynyl (all optionally substituted), H, Q or -V'-Q; V' = 1-6C alkylene, 2-6C alkenylene or 2-6C alkynylene; Q = 3-8C cycloalkyl, aryl, heterocycloalkyl, heteroaryl (all optionally substituted); R5, R41 = H; or R5 + R41 = bond; R6-R9 = H, halo, alkyl, 3-8C cycloalkyl or -OW'; W' = aryl, heteroaryl, arylalkyl, heteroarylalkyl (all optionally substituted), H, alkyl, acyl, 3-8C cycloalkyl or heterocycloalkyl; alkyl = 1-6C; aryl = phenyl, naphthyl or biphenyl; heterocycloalkyl = partially unsaturated 4- to 11-membered mono- or bi-cyclic ring containing 1-6 N, S or O; heteroaryl = aromatic or partially aromatic 4- to 11-membered mono- or bi-cyclic ring containing 1-6 N, S or O; substituted aryl, arylalkyl = aryl or arylalkyl substituted with at least one halo, alkyl, 1-6C alkoxy, 1-6C perhaloalkyl, amino (optionally substituted by 1 or 2 alkyl), CN, carboxy, 1-6C alkoxycarbonyl, aminocarbonyl (optionally substituted with 1 or 2 alkyl on N), nitro or OH; substituted alkyl, alkenyl, alkynyl and cycloalkyl = alkyl, alkenyl, alkynyl and cycloalkyl substituted with at least one OH, 1-6C alkoxy, 1-6C alkylthio, amino (optionally substituted with 1 or 2 alkyl), carboxy, nitro, CN, 1-6C alkoxycarbonyl or aminocarbonyl (optionally substituted with 1 or 2 alkyl on N); substituted heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, heteroarylalkyl = heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, heteroarylalkyl substituted with at least one halo, alkyl, 1-6C alkoxy, 1-6C perhaloalkyl, amino (optionally substituted with 1 or 2 alkyl), CN, carboxy, 1-6C alkoxycarbonyl, aminocarbonyl (optionally substituted with 1 or 2 alkyl on N), nitro, OH or oxo; and provided that R6-R9 are not all H and at least one of R6-R9 is -OW', that R2 and R3 are alkyl when R6-R9 are H, alkyl, alkoxy, R41 and R5 form a bond, R40 is other than H or alkyl; when (I) has one OH and R40 is other than H; when (I) has one methoxy and R40 is other than hydroxyalkyl; and (I) is other than 7-methoxy-2,2-diphenyl-1,2-dihydroquinoline. An Independent claim is also included for the preparation of (I).

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