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    2.
    发明专利
    未知

    公开(公告)号：DE19724980A1

    公开(公告)日：1998-12-17

    申请号：DE19724980

    申请日：1997-06-13

    Applicant: BASF AG

    Inventor： STEINER GERD DR ,  DULLWEBER UTA DR ,  STARCK DOROTHEA DR ,  BACH ALFRED DR ,  WICKE KARSTEN DR ,  TESCHENDORF HANS-JUERGEN DR ,  GARCIA-LADONA FRANCISCO-JAVI D ,  EMLING FRANZ DR

    IPC: A61K31/495 ,  A61K31/519 ,  A61P25/00 ,  A61P25/24 ,  A61P43/00 ,  C07D495/04 ,  A61K31/505 ,  A61K31/55

    Abstract: The invention relates to 3-substituted 3,4 dihydro-thieno[2, 3-d] pyrimidine derivatives of formula (I) wherein R and R mean a hydrogen atom or a C1-C4 alkyl group, R represents a phenyl, pyridyl, pyrimidinyl or pyrazinyl group optionally mono- or disubstituted by halogen atoms, C1-C4 alkyl, trifluoromethyl, trifluoromethoxy, hydroxy, C1-C4 alkoxy, amino, monomethylamino, dimethylamino, cyano or nitro groups, said group being optionally anellated with a benzene nucleus which is optionally mono- or disubstituted by halogen atoms, C1-C4 alkyl, hydroxy, trifluoromethyl, C1-C4 alkoxy, amino, cyano or nitro groups and may contain optionally 1 nitrogen atom, or with a 5 or 6-membered ring which may contain 1-2 oxygen atoms, A represents NH or an oxygen atom, Y is CH2, CH2-CH2, CH2-CH2-CH2 or CH2-CH, Z represents a nitrogen atom, carbon atom or CH and the bond between Y and Z can also be a double bond, and n is the number 2, 3 or 4. The invention also relates to the physiologically compatible salts of the inventive 3-substituted 3,4 dihydro-thieno[2,3-d] pyrimidine derivatives.

    4.
    发明专利
    未知

    公开(公告)号：DE19724979A1

    公开(公告)日：1998-12-17

    申请号：DE19724979

    申请日：1997-06-13

    Applicant: BASF AG

    Inventor： STEINER GERD DR ,  DULLWEBER UTA DR ,  STARCK DOROTHEA DR ,  BACH ALFRED DR ,  WICKE KARSTEN DR ,  TESCHENDORF HANS-JUERGEN DR ,  GARCIA-LADONA XAVIER DR ,  EMLING FRANZ DR

    IPC: A61K31/505 ,  A61K31/519 ,  A61P25/00 ,  A61P25/24 ,  A61P43/00 ,  C07D495/14 ,  A61K31/55

    Abstract: The invention relates to 3-substituted 3,4,5,6,7,8-hexahydro-pyrido [3',4':4,5] thieno [2,3-d] pyrimidine derivatives of formula (I) wherein R is a hydrogen atom, a C1-C4 alkyl group, an acetyl group, a phenyl alkyl C1-C4 radical, the aromatic being optionally substituted by halogen, C1-C4 alkyl, trifluoromethyl, hydroxy, C1-C4 alkoxy, amino, cyano or nitro groups, or a phenylalkanon radical in which the phenyl group can be substituted by halogen, R means a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which is optionally mono- or disubstituted by halogen atoms, C1-C4 alkyl, trifluoromethyl, trifluoromethoxy, hydroxy, C1-C4 alkoxy, amino, monomethylamino, dimethylamino, cyano or nitro groups and said group can be optionally anellated with a benzene nucleus which can be optionally mono- or disubstituted by halogen atoms, C1-C4 alkyl, hydroxy, trifluoromethyl, C1-C4 alkoxy, amino, cyano or nitro groups and may contain one nitrogen atom, or with a 5 or 6-membered ring which may contain 1-2 oxygen atoms, A represents NH or an oxygen atom, Y is CH2, CH2-CH2, CH2-CH2-CH2 or CH2CH, Z represents a nitrogen atom, carbon atom or CH and the bond between Y and Z can also be a double bond, and n represents the number 2, 3 or 4. The invention also relates to the physiologically compatible salts of the inventive 3-substituted pyrido [3',4':4,5] thieno [2,3-d] pyrimidine derivatives. The inventive compounds show a high level of affinity for the serotonin receptors 5-HT1B, 5-HT1D and 5-HT1A. The affinity for said receptors is approximately equal, at least on the same scale. Some of the inventive compounds also have a good capacity for inhibiting serotonin reuptake, a property used in most antidepressants.

    8.
    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.

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