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    3-SUBSTITUTED PYRIDO[4', 3': 4,5]THIENO[2,3-D]PYRIMIDINE DERIVATIVES, THEIR PREPARATION AND APPLICATION
    1.
    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 and treatment of depression
    4.
    发明专利
    3-substituted pyrido[4',3':4,5]thieno[2,3-d]pyrimidine derivatives and treatment of depression 未知

    公开(公告)号：NZ334350A

    公开(公告)日：2000-07-28

    申请号：NZ33435097

    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 ,  KERRRIGAN FRANK

    IPC: A61K31/435 ,  A61K31/519 ,  A61P25/24 ,  A61P43/00 ,  C07D211/00 ,  C07D239/00 ,  C07D333/00 ,  C07D495/14 ,  A61K31/495

    Abstract: In the compounds of formula I: R1 is a hydrogen atom, a C1-C4 alkyl group, an acetyl or benzoyl group, a phenylalkyl C1-C4 radical (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 radical or a phenylcarbamoylalkyl C2 radicalgroup (wherein the phenyl group can be substituted by halogen). R2 is a phenyl, pyridyl, pyrimidinyl or pyrazinyl group, each of which can optionally be mono-di- or tri-substituted by halogen atoms, C1-C4 alkyl, trifluoromethyl, trifluoromethoxy, hydroxyl, C1-C4 alkoxy, amino, monomethylamino, dimethylamino, cyano or nitro groups, and each of these may be fused to a benzene nucleus optionally mono- or di-substituted by halogen atoms, C1-C4 alkyl, hydroxyl, trifluoromethyl, C1-C4 alkoxy, amino, cyano or nitro groups, and optionally containing 1 nitrogen atom, or a 5- or 6-member ring which can contain between 1 and 2 oxygen atoms or 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 is NH or an oxygen atom; B is hydrogen or methyl; C is hydrogen, methyl or hydroxyl; X is a nitrogen atom; Y is CH2, CH2-CH2, CH2-CH2-CH2 or CH2-CH; Z is 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. 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.

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

    6.
    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
    8.
    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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