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    PROCESS FOR PREPARING CRYSTALLINE FORM I OF CABERGOLINE
    7.
    发明公开
    PROCESS FOR PREPARING CRYSTALLINE FORM I OF CABERGOLINE 审中-公开
    工艺为结晶I型卡麦角林的制备

    公开(公告)号：EP1507777A4

    公开(公告)日：2007-03-07

    申请号：EP03721346

    申请日：2003-03-10

    申请人： PHARMACIA CORP

    发明人： SHEIKH AHMAD Y

    IPC分类号： C07D457/06 ,  C07D471/04 ,  C07D261/08

    CPC分类号： C07D457/06

    摘要： A process for producing crystalline form I of cabergoline, which process comprises crystallization of the desired form from a toluene/heptane or toluene/hexane mixture starting from raw cabergoline, followed by recovery and removal of the solvent from the resulting toluene solvate Form X. The new solvate Form X of cabergoline, useful intermediate, and its preparation are also provided.

    SEROTONINERGIC ERGOLINE DERIVATIVES
    9.
    发明授权
    SEROTONINERGIC ERGOLINE DERIVATIVES 失效
    SEROTONINGISCHE ERGOLIN DERIVATE

    公开(公告)号：EP0628042B1

    公开(公告)日：2001-08-16

    申请号：EP94901903.8

    申请日：1993-11-26

    申请人： PHARMACIA & UPJOHN S.p.A.

    发明人： MANTEGANI, Sergio ,  BRAMBILLA, Enzo ,  CACCIA, Carla ,  CARFAGNA, Nicola

    IPC分类号： C07D457/04 ,  A61K31/48 ,  C07D457/02 ,  C07D457/06

    CPC分类号： C07D457/04 ,  C07D457/02 ,  C07D457/08 ,  C07D457/12

    摘要： The present invention provides compounds of formula (I) wherein A represents OH, NH2, COOR3', OCONHR4, CONHR4, NHCOR4, NHCO2R4, NHC(X)NHR4, NHC(X)NHCOR4, (a) or (b), R1 is hydrogen or C1-4 linear or branched alkyl; R2 is hydrogen, chlorine, bromine or an S-C1-4 alkyl group; R3 and R3' are, independently, C1-5 alkyl or hydrogen, n is 0,1 or 2, m is 1 or 2; R4 is hydrogen, C1-7 alkyl, C3-7 cycloalkyl, adamantidyl (tricyclo 3.3.1.1.3,7) decan-1-yl, C¿1-5? alkylphenyl, C2 alkenylphenyl; C2 alkynylphenyl, phenyl optionally substituted by one or more groups selected from C1-4 alkyl, C1-3 alkoxy, methylendioxy, cyano, trifluoromethyl, hydroxy, nitro and acetyl; an optionally substituted naphthyl ring or phenyl condensed with a heterocyclic ring system having 5- or 6- ring members including 1 to 4 heteroatoms selected from nitrogen, oxygen and sulphur; a heterocyclic ring having 5 or 6 ring members including 1 or 2 heteroatoms selected from nitrogen, oxygen and sulphur which is optionally substituted by a group selected from C1-4 alkyl, phenyl optionally substituted as defined above, C1-3 alkoxy and halogen; R5 is hydrogen, C1-4 alkyl or a phenyl group and X is NH, O, S; or a pharmaceutically acceptable salt thereof. A process for their preparation and the pharmaceutical compositions comprising them are also provided.