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    5.
    发明专利
    未知

    公开(公告)号：NO991132D0

    公开(公告)日：1999-03-09

    申请号：NO991132

    申请日：1999-03-09

    Applicant: BASF AG

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

    IPC: A61K31/435 ,  A61K31/519 ,  A61P25/24 ,  A61P43/00 ,  C07D211/00 ,  C07D239/00 ,  C07D333/00 ,  C07D495/14 ,  C07D221/00

    Abstract: A 3-substituted 3,4,5,6,7,8-hexahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidine compound of formula IwhereinR1 is hydrogen, C1-C4-alkyl, acetyl or benzoyl, optionally substituted phenyl-C1-C4-alkyl, naphthyl-C1-C3-alkyl, phenyl-C2-C3-alkanone or a phenylcarbamoyl-C2-alkyl,R2 is optionally substituted phenyl, pyridyl, pyrimidyl or pyrazinyl, or an optionally substituted bicyclus wherein one of the two fused rings is a phenyl, a pyridyl, a pyrimidyl or a pyrazinyl ring,A is NH or oxygen,B is hydrogen or methyl,C is hydrogen, methyl or hydroxyl,X is nitrogen,Y is CH2, CH2-C2, CH2-C2-CH2 or CH2-CH,Z is nitrogen, C or CH, and the linkage between Y and Z is a single or a double bond, andn is 2, 3 or 4,or a physiologically tolerated salt thereof, and compositions comprising them and their use as antagonists of 5HT1B and 5HT1A and for the treatment of depression and related disorders.

    6.
    发明专利
    未知

    公开(公告)号：ID18260A

    公开(公告)日：1998-03-19

    申请号：ID973146

    申请日：1997-09-10

    Applicant: BASF AG

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

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

    Abstract: A 3-substituted 3,4,5,6,7,8-hexahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidine compound of formula IwhereinR1 is hydrogen, C1-C4-alkyl, acetyl or benzoyl, optionally substituted phenyl-C1-C4-alkyl, naphthyl-C1-C3-alkyl, phenyl-C2-C3-alkanone or a phenylcarbamoyl-C2-alkyl,R2 is optionally substituted phenyl, pyridyl, pyrimidyl or pyrazinyl, or an optionally substituted bicyclus wherein one of the two fused rings is a phenyl, a pyridyl, a pyrimidyl or a pyrazinyl ring,A is NH or oxygen,B is hydrogen or methyl,C is hydrogen, methyl or hydroxyl,X is nitrogen,Y is CH2, CH2-C2, CH2-C2-CH2 or CH2-CH,Z is nitrogen, C or CH, and the linkage between Y and Z is a single or a double bond, andn is 2, 3 or 4,or a physiologically tolerated salt thereof, and compositions comprising them and their use as antagonists of 5HT1B and 5HT1A and for the treatment of depression and related disorders.

    3-SUBSTITUTED PYRIDO[4', 3': 4,5]THIENO[2,3-D]PYRIMIDINE DERIVATIVES, THEIR PREPARATION AND APPLICATION
    7.
    发明专利
    3-SUBSTITUTED PYRIDO[4', 3': 4,5]THIENO[2,3-D]PYRIMIDINE DERIVATIVES, THEIR PREPARATION AND APPLICATION 未知

    公开(公告)号：BG63602B1

    公开(公告)日：2002-06-28

    申请号：BG10312299

    申请日：1999-01-27

    Applicant: BASF AG

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

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

    Abstract: The 3-substituted 3,4,5,6,7.8-hexahydro-pyrido[4', 3': 4,5]-thieno [2,3-d] pyrimidine derivatives can be used as medicamentous forms for diseases where there is redud serotonin concentration and where, within the therapy, the activity of the presnaptic receptors 5-HT1B-, 5-HT1A-, 5-HT1D-, should be blocked without seriously affecting any other receptors. Depression is an example for such morbid state. The compounds have formula in which R1 is hydrogen, C1-C4-alkyl group, acetyl, benzoyl, phenylalkyl-C1-C4-residue where the aromatic residue is optionally substituted with halogen, C1-C4-alkyl, trifluoromethyl, hydroxy-, C1-C4-alkoxy-, amino-, cyano- or nitrogroups or is naphtalene-C1-C4-alkyl residue, phenylalkanon-C2-C4-residue or phenylcarbamoylalkyl-C2-residue where the phenyl group can be substituted by halogen; R2 optionally is mono-, di- or trisubstituted with halogen atoms, C1-C4-alkyl, trifluoromethyl, trifluormethoxy, hydroxy, C1-C4-alkoxy, amino-, monomethylamino-, diethylamino-, cyano- or nitrogroup, phenyl, pyridyl, pyrimidinyl or pyrasinyl reside which can optionally be ringed by one benzene ring which optionally can be mono- or disubstituted with halogen atom, C1-C4-alkyl, hydroxy, trifluormethyl, C1-C4-alkoxy, amino-, cyano- or nitrogroup, and optionally can contain one nitrogen atom or be ringed by 5- or 6-member ring which can contain one to two oxygen atoms, or can be substituted by phenyl-C1-C2-alkyl, or alkoxygroup, respectively, where the phenyl residue can be substituted with halogen, methyl, trifluormethyl or methoxygroup. A is NH or oxygen, B is hydrogen or methyl, C is hydrogen, methyl or hydroxy, X is nitrogen atom, Y is the group CH2, CH2- CH2, CH2-CH2-CH2 or CH2-CH, Z is nitrogen atom, carbon or CH where the bond between Y and Z can be double, n has the value of 2, 3 or 4. The invention also relates to physiologically acceptable salts of the above compounds. 6 claims

    3-SUBSTITUTED PYRIDO[4', 3': 4,5]THIENO[2,3-D]PYRIMIDINE DERIVATIVES, THEIR PREPARATION AND APPLICATION
    8.
    发明专利
    3-SUBSTITUTED PYRIDO[4', 3': 4,5]THIENO[2,3-D]PYRIMIDINE DERIVATIVES, THEIR PREPARATION AND APPLICATION 未知

    公开(公告)号：BG103122A

    公开(公告)日：1999-09-30

    申请号：BG10312299

    申请日：1999-01-27

    Applicant: BASF AG

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

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

    Abstract: The 3-substituted 3,4,5,6,7.8-hexahydro-pyrido[4', 3':4,5]-thieno [2,3-d] pyrimidine derivatives can be used asmedicamentous forms for diseases where there is redud serotoninconcentration and where, within the therapy, the activity of thepresnaptic receptors 5-HT1B-, 5-HT1A-, 5-HT1D-, should be blockedwithout seriously affecting any other receptors. Depression is anexample for such morbid state. The compounds have formulain which R1 is hydrogen, C1-C4-alkyl group, acetyl, benzoyl,phenylalkyl-C1-C4-residue where the aromatic residue is optionallysubstituted with halogen, C1-C4-alkyl, trifluoromethyl, hydroxy-,C1-C4-alkoxy-, amino-, cyano- or nitrogroups or isnaphtalene-C1-C4-alkyl residue, phenylalkanon-C2-C4-residue orphenylcarbamoylalkyl-C2-residue where the phenyl group can besubstituted by halogen; R2 optionally is mono-, di- ortrisubstituted with halogen atoms, C1-C4-alkyl, trifluoromethyl,trifluormethoxy, hydroxy, C1-C4-alkoxy, amino-, monomethylamino-,diethylamino-, cyano- or nitrogroup, phenyl, pyridyl, pyrimidinylor pyrasinyl reside which can optionally be ringed by one benzenering which optionally can be mono- or disubstituted with halogenatom, C1-C4-alkyl, hydroxy, trifluormethyl, C1-C4-alkoxy, amino-,cyano- or nitrogroup, and optionally can contain one nitrogen atomor be ringed by 5- or 6-member ring which can contain one to twooxygen atoms, or can be substituted by phenyl-C1-C2-alkyl, oralkoxygroup, respectively, where the phenyl residue can besubstituted with halogen, methyl, trifluormethyl or methoxygroup.A is NH or oxygen, B is hydrogen or methyl, C is hydrogen, methylor hydroxy, X is nitrogen atom, Y is the group CH2, CH2- CH2,CH2-CH2-CH2 or CH2-CH, Z is nitrogen atom, carbon or CH where thebond between Y and Z can be double, n has the value of 2, 3 or 4.The invention also relates to physiologically acceptable salts ofthe above compounds.6 claims

    9.
    发明专利
    未知

    公开(公告)号：BR9711724A

    公开(公告)日：1999-08-24

    申请号：BR9711724

    申请日：1997-08-22

    Applicant: BASF AG

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

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

    Abstract: A 3-substituted 3,4,5,6,7,8-hexahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidine compound of formula IwhereinR1 is hydrogen, C1-C4-alkyl, acetyl or benzoyl, optionally substituted phenyl-C1-C4-alkyl, naphthyl-C1-C3-alkyl, phenyl-C2-C3-alkanone or a phenylcarbamoyl-C2-alkyl,R2 is optionally substituted phenyl, pyridyl, pyrimidyl or pyrazinyl, or an optionally substituted bicyclus wherein one of the two fused rings is a phenyl, a pyridyl, a pyrimidyl or a pyrazinyl ring,A is NH or oxygen,B is hydrogen or methyl,C is hydrogen, methyl or hydroxyl,X is nitrogen,Y is CH2, CH2-C2, CH2-C2-CH2 or CH2-CH,Z is nitrogen, C or CH, and the linkage between Y and Z is a single or a double bond, andn is 2, 3 or 4,or a physiologically tolerated salt thereof, and compositions comprising them and their use as antagonists of 5HT1B and 5HT1A and for the treatment of depression and related disorders.

    3-SUBSTITUTED PYRIDO(4',3':4,5)THIENO(2,3-D)PYRIMIDINE DERIVATIVES, THEIR PREPARATION AND THEIR USE
    10.
    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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