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1. 发明授权

EP1023296B1 3-SUBSTITUIERTE PYRIDO 3',4':4,5] THIENO 2,3-d] PYRIMIDIN-DERIVATE, IHRE HERSTELLUNG UND VERWENDUNG 失效
标题翻译： 3-取代的吡啶并3”，4' ：4,5]噻吩并2,3-d]嘧啶衍生物，其生产和使用
公开(公告)号：EP1023296B1
公开(公告)日：2003-12-17
申请号：EP98936299.1
申请日：1998-05-29
申请人： Abbott GmbH & Co. KG
发明人： STEINER, Gerd , DULLWEBER, Uta , STARCK, Dorothea , BACH, Alfred , WICKE, Karsten , TESCHENDORF, Hans-Jürgen , GARCIA-LADONA, Francisco-Javier , EMLING, Franz
IPC分类号： C07D495/14 , A61K31/505
CPC分类号： C07D495/14
摘要： 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 R1 is a hydrogen atom, a C¿1?-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?2¿ means a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which is optionally mono- or disubstituted by halogen atoms, C¿1?-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.

2. 发明授权

EP0927184B1 3-SUBSTITUIERTE PYRIDO 4',3':4,5] THIENO 2,3-D]PYRIMIDIN-DERIVATE, IHRE HERSTELLUNG UND VERWENDUNG 失效
标题翻译： 3-取代的吡啶并4”，3' ：4,5]噻吩并-2,3--D]嘧啶衍生物，其生产和使用
公开(公告)号：EP0927184B1
公开(公告)日：2003-10-22
申请号：EP97940118.9
申请日：1997-08-22
申请人： ABBOTT GmbH & Co. KG
发明人： STEINER, Gerd , LUBISCH, Wilfried , BACH, Alfred , EMLING, Franz , WICKE, Karsten , TESCHENDORF, Hans-Jürgen , BEHL, Berthold , KERRRIGAN, Frank , CHEETHAM, Sharon
IPC分类号： C07D495/14 , A61K31/435
CPC分类号： C07D495/14
摘要： 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 C¿1?-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?2¿ designates a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which can optionally be mono-, di- or tri-substituted by halogen atoms, C¿1?-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.

3. 发明授权

EP0988306B1 3-SUBSTITUIERTE 3,4-DIHYDRO-THIENO 2,3-D]PYRIMIDIN-DERIVATE, IHRE HERSTELLUNG UND VERWENDUNG 失效
标题翻译： 3-取代的-3,4-二氢 - 噻吩并-2,3--D]嘧啶衍生物，其生产和使用
公开(公告)号：EP0988306B1
公开(公告)日：2003-07-09
申请号：EP98929405.3
申请日：1998-05-29
申请人： Abbott GmbH & Co. KG
发明人： STEINER, Gerd , DULLWEBER, Uta , STARCK, Dorothea , BACH, Alfred , WICKE, Karsten , TESCHENDORF, Hans-Jürgen , GARCIA-LADONA, Francisco-Javier , EMLING, Franz
IPC分类号： C07D495/04 , A61K31/495
CPC分类号： C07D495/04
摘要： The invention relates to 3-substituted 3,4 dihydro-thieno[2, 3-d] pyrimidine derivatives of formula (I) wherein R?1 and R2¿ mean a hydrogen atom or a C¿1?-C4 alkyl group, R?3¿ represents a phenyl, pyridyl, pyrimidinyl or pyrazinyl group optionally mono- or disubstituted by halogen atoms, C¿1?-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.

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