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    3-SUBSTITUTED PYRIDO[4', 3': 4,5]THIENO[2,3-D]PYRIMIDINE DERIVATIVES, THEIR PREPARATION AND APPLICATION
    52.
    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

    53.
    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.

    2-SUBSTITUTED 1,2-BENZISOTHIAZOLE DERIVATIVES AND THEIR USE AS SEROTONIN ANTAGONISTS (5-HT1A, 5-HT1B AND 5-HT1D)
    55.
    发明专利
    2-SUBSTITUTED 1,2-BENZISOTHIAZOLE DERIVATIVES AND THEIR USE AS SEROTONIN ANTAGONISTS (5-HT1A, 5-HT1B AND 5-HT1D) 未知

    公开(公告)号：CA2307199A1

    公开(公告)日：1999-04-29

    申请号：CA2307199

    申请日：1998-10-05

    Applicant: BASF AG

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

    IPC: A61K31/428 ,  A61P25/24 ,  A61P43/00 ,  C07D275/06 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  A61K31/425

    Abstract: The invention relates to 2-substituted 1,2-benzisothiazole derivatives of formula (I), wherein R1 and R2 represent (C1-6) alkyl, independently of each other; A represents branched or unbranched (C1-10)-alkylene or straightchained or branched (C2-10)-alkylene comprising at least one group Z which is selected from O, S, NR7, cyclopropyl, CHOH, a double or triple bond; B represents 4-piperidine, 4-tetrahydro-1, 2, 3, 6 pyridine, 4-piperazine and the corresponding ring compounds enlarged with a methylene group, an N-atom of B providing the link with A; Ar represents phenyl which is optionally substituted by (C1-6) alkyl -branched or unbranched-, O-( C1-6)-alkyl branched or unbranched-, OH, F, Cl, Br, I, trifluoromethyl, NR5R6, CO2R7, cyano or phenyl; tetralin, indan, highly condensed aromatics such as naphthalin optionally substituted by (C1-4) alkyl or O(C1-4) alkyl; anthracene or 5- or 6-membered aromatic heterocyclene with 1 to 2 heteroatoms which are selected independently of each other from O and N and which can still be anellated with further aromatic radicals such as quinoline, isoquinoline, phthalazine, indole and quinazoline which can itself be substituted again with phenyl; and R3 and R4 have the meanings given in the description. The invention also relates to the production of the inventive derivatives and to their use as serotonin antagonists.

    3-substituted pyrido {3',4':4,5} thieno {2,3-d} pyrimidine derivatives, and production and use of the same
    56.
    发明专利
    3-substituted pyrido {3',4':4,5} thieno {2,3-d} pyrimidine derivatives, and production and use of the same 未知

    公开(公告)号：AU8535798A

    公开(公告)日：1998-12-30

    申请号：AU8535798

    申请日：1998-05-29

    Applicant: BASF AG

    Inventor： STEINER GERD ,  DULLWEBER UTA ,  STARCK DOROTHEA ,  BACH ALFRED ,  WICKE KARSTEN ,  TESCHENDORF HANS-JURGEN ,  GARCIA-LADONA FRANCISCO-JAVIER ,  EMLING FRANZ

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

    Abstract: PCT No. PCT/EP98/03231 Sec. 371 Date Dec. 8, 1999 Sec. 102(e) Date Dec. 8, 1999 PCT Filed May 29, 1998 PCT Pub. No. WO98/56793 PCT Pub. Date Dec. 17, 19983-Substituted 3,4,5,6,7,8-hexahydropyrido [3',4':4,5]-thieno[2,3-d]pyrimidine derivatives of the formula I where R1 is a hydrogen atom, a C1-C4-alkyl group, an acetyl group, a phenylalkyl C1-C4 radical, the aromatic system being unsubstituted or substituted by halogen, C1-C4-alkyl, trifluoromethyl, hydroxyl, C1-C4-alkoxy, amino, cyano or nitro groups, or is a phenylalkanone radical, it being possible for the phenyl group to be substituted by halogen, R2 is a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which is unsubstituted or mono- or disubstituted by halogen atoms, C1-C4-alkyl, trifluoromethyl, trifluoromethoxy, hydroxyl, C1-C4-alkoxy, amino, monomethylamino, dimethylamino, cyano or nitro groups and which may be fused to a benzene nucleus which can be unsubstituted or mono- or disubstituted by halogen atoms, C1-C4-alkyl, hydroxyl, trifluoromethyl, C1-C4-alkoxy, amino, cyano or nitro groups and may contain 1 nitrogen atom, or to a 5- or 6-membered ring which may contain 1-2 oxygen atoms, A is NH or an oxygen atom, Y is CH2, CH2-CH2, CH2-CH2-CH2 or CH2-CH, Z is a nitrogen atom, carbon atom or CH, it also being possible for the linkage between Y and Z to be a double bond, and n is 2, 3 or 4, and the physiologically tolerated salts thereof.

    3-SUBSTITUTED PYRIDO(4',3':4,5)THIENO(2,3-D)PYRIMIDINE DERIVATIVES, THEIR PREPARATION AND THEIR USE
    58.
    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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