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    5.
    发明专利
    未知

    公开(公告)号：AT233744T

    公开(公告)日：2003-03-15

    申请号：AT00403399

    申请日：2000-12-05

    Applicant: SERVIER LAB

    Inventor： VIAUD MARIE-CLAUDE ,  GUILLAUMET GERALD ,  DAUBOS PHILIPPE ,  BENNEJEAN CAROLINE ,  DELAGRANGE PHILIPPE ,  RENARD PIERRE

    IPC: A61K31/538 ,  A61K31/5415 ,  A61P1/00 ,  A61P1/14 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D265/36 ,  C07D279/16 ,  C07D413/06 ,  C07D413/12

    Abstract: 1,4-Benzoxazine and 1,4-benzothiazine compounds (I) and their acid or base addition salts, enantiomers and diastereomers, are new. 1,4-Benzoxazine and 1,4-benzothiazine compounds of formula (I) and their acid or base addition salts, enantiomers and diastereomers, are new. R1 = R, OR, SR, SO2NRR', NRR', -N(R)C(=Z)R', -N(R)SO2R', -N(R)C(=Z)OR', -N(R)C(=Z)NR'R'', C(=Z)OR, -OC(=Z)R or -C(=Z)NRR'; Z = S or O; R, R', R'' = H or 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, 3-8C cycloalkyl or 3-8C cycloalkyl-1-6C alkyl (all optionally substituted by one or more B), or aryl, aryl-1-6C alkyl, heteroaryl or heteroaryl-1-6C alkyl (all optionally substituted by one or more D; or NRR' or NR'R'' = morpholinyl, piperidinyl, piperazinyl or pyrrolidinyl; G = 1-4C alkylene (optionally substituted by R, OR, COR or COOR; A = -C(=Z)NRR', -N(R)C(=Z)R' or -N(R)C(=Z)NR'R''; R2 = halo, R, OR, COR, COOR or OCOR; X = O or S; dotted line = single or double bond; B = OH, alkoxy, alkyl, polyhaloalkyl, NH2, NH(1-6C alkyl), N(1-6C alkyl)2 or halo; D = OH, alkoxy, amino, alkylamino, dialkylamino, nitro, cyano, polyhaloalkyl, formyl, carboxyl, alkoxycarbonyl, amido or halo; aryl = phenyl, naphthyl or biphenyl; and heteroaryl = mono- or bicyclic aromatic group containing 1-3 O, S or N; provided that when A = -C(=Z)NRR', G = 2-4C alkylene.

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