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    7.
    发明专利
    未知

    公开(公告)号：DE19636769A1

    公开(公告)日：1998-03-12

    申请号：DE19636769

    申请日：1996-09-10

    Applicant: BASF AG

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

    IPC: A61K31/435 ,  A61K31/519 ,  A61P25/24 ,  A61P43/00 ,  C07D211/00 ,  C07D239/00 ,  C07D333/00 ,  C07D495/14 ,  A61K31/44 ,  A61K31/38 ,  A61K31/505

    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: R 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; R 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 di-substituted 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.

    8.
    发明专利
    未知

    公开(公告)号：DE19532050A1

    公开(公告)日：1997-03-06

    申请号：DE19532050

    申请日：1995-08-31

    Applicant: BASF AG

    Inventor： LUBISCH WILFRIED DR ,  BEHL BERTHOLD DR ,  HOFMANN HANS PETER DR ,  TESCHENDORF HANS-JUERGEN DR ME

    IPC: A61K31/00 ,  A61K31/495 ,  A61K31/498 ,  A61P25/04 ,  C07D401/14 ,  C07D403/04

    Abstract: Pyrrolyl tetrahydroquinoxalin diones of formula (I) and their tautomeric and isomeric forms, and their physiologically acceptable salts, in which the variables are: R - hydrogène, cyclohexyl radical, an aliphatic radical with 1 to 4 atoms which can bear the radical COOR , where R is hydrogen or C1-C4 alkyl, R -COOH, -COO-C1-C4, -COO-(CH2)m-Ph, -CONR R and (a), where m may be a whole number from 1 to 6, R is hydrogen, -C1-C4 alkyl or OH and R is hydrogen, -C1-C4 alkyl, -(CH2)m-Ph or (b), where all the phenyl or pyridyl rings contained in R may be substituted by up to 3 of the following radicals: -C1-C4 alkyl, halogen, -O-C1-C4 alkyl, -OCF3, -NO2, -CN, -COOR or -CONHR ; R is -CF3, -NO2, -CN and R is hydrogen; or R and R together may be an anellated benzole ring. The compounds are suitable as medicaments in human and veterinary medicine.

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