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    3-SUBSTITUTED PYRIDO(4',3':4,5)THIENO(2,3-D)PYRIMIDINE DERIVATIVES, THEIR PREPARATION AND THEIR USE
    31.
    发明专利
    3-SUBSTITUTED PYRIDO(4',3':4,5)THIENO(2,3-D)PYRIMIDINE DERIVATIVES, THEIR PREPARATION AND THEIR USE 未知

    公开(公告)号：CA2265509A1

    公开(公告)日：1998-03-19

    申请号：CA2265509

    申请日：1997-08-22

    Applicant: BASF AG

    Inventor： WICKE KARSTEN ,  KERRIGAN FRANK ,  EMLING FRANZ ,  CHEETHAM SHARON ,  BEHL BERTHOLD ,  LUBISCH WILFRIED ,  BACH ALFRED ,  TESCHENDORF HANS-JUERGEN ,  STEINER GERD

    IPC: A61K31/435 ,  A61K31/519 ,  A61P25/24 ,  A61P43/00 ,  C07D211/00 ,  C07D239/00 ,  C07D333/00 ,  C07D495/14

    Abstract: The invention concerns 3-substituted 3,4,5,6,7,8-hexahydro-pyrido¢4,3':4,5!thieno-¢2,3-d!pyrimidine derivatives of formula (I) in which: R1 designates a hydrogen atom, a C1-C4 alkyl group, an acetyl or benzoyl group, a phenylalkyl C1-C4 group - the aromatic optionally being substituted by halogen, C1-C4 alkyl, trifluoromethyl, hydroxy, C1-C4 alkoxy, amino, cyano or nitro groups - a naphthylalkyl C1-C3 group, a phenylalkanone C2-C3 group or a phenylcarbamoylalkyl C2 group, wherein the phenyl group can be substituted by halogen; R2 designates a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which can optionally be mono-, di- or tri-substituted by halogen atoms, C1-C4 alkyl, trifluoromethyl, trifluoromethoxy, hydroxy, C1-C4 alkoxy, amino, monomethylamino, dimethylamino, cyano or nitro groups and can optionally be anellated with a benzene nucleus, which can optionally be mono- or disubstituted by halogen atoms, C1-C4 alkyl, hydroxy, trifluoromethyl, C1-C4 alkoxy, amino, cyano or nitro groups and can optionally contain 1 nitrogen atom, or with a 5- or 6-member ring which can contain between 1 and 2 oxygen atoms, or can be substituted by a phenyl-C1-C2 alkyl or alkoxy group, wherein the phenyl group can be substituted by halogen, a methyl, trifluoromethyl or methoxy group; A designates NH or an oxygen atom; B designates hydrogen or methyl; C designates hydrogen, methyl or hydroxy; X designates a nitrogen atom; Y is CH2, CH2-CH2, CH2-CH2-CH2 or CH2-CH; Z designates a nitrogen atom, a carbon atom or CH, wherein the bond between Y and Z can also be a double bond; and n is the number 2, 3 or 4, and their physiologically compatible salts. These compounds are suitable as medicaments for treating diseases in which the serotonin concentration is reduced and in which the activity of the presynaptic receptors 5-HT1B, 5-HT1A, 5HT1D is to be blocked within a therapeutic context without greatly influencing other receptors. Such diseases include, for example, depression.

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