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公开(公告)号：EP0043858A1
公开(公告)日：1982-01-20
申请号：EP81900262.7
申请日：1981-01-13
IPC分类号： C07D471/04 , C07D513/04 , A61K31/425 , A61K31/435
CPC分类号： C07D471/04 , C07D513/04
摘要： Hetero ring-substituted oxoalkanoic acid derivatives having an immunity-controlling action and represented by the following general formula:
wherein R' represents a hydrogen atom, a lower alkyl group, or a phenyl, thienyl or furyl group optionally having in an optional position of the nucleus at least one substitutent of halogen, lower alkyl, lower alkoxy, mono- or di-lower alkylamino-substituted lower alkoxy, lower alkylthio, lower alkylsulfinyl, amino, nitro or cyano, R 2 and R 3 each represents a hydrogen atom or a lower alkyl group, A represents a lower alkylene group, X represents a sulfur atom or a vinylene group, Y represents a nitrogen atom or a methine group optionally having lower alkyl as a substituent, and Z represents a carbonyl group or a single bond.摘要翻译： 具有免疫控制作用并由下列通式表示的杂环取代的氧代链烷酸衍生物：其中R'表示氢原子，低级烷基或苯基，噻吩基或呋喃基，其任选地在 低级烷基，低级烷氧基，一或二低级烷基氨基取代的低级烷氧基，低级烷硫基，低级烷基亚磺酰基，氨基，硝基或氰基，R2和R3分别代表氢原子或低级烷基 A表示低级亚烷基，X表示硫原子或亚乙烯基，Y表示氮原子或可以具有低级烷基作为取代基的次甲基，Z表示羰基或单键。
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2.发明公开THIENO(TRIAZOLO)DIAZEPINE COMPOUNDS AND MEDICINAL APPLICATION OF THE SAME 失效THIENO（TRIAZOLO）DIAZEPINVERBINDUNGEN，UND MEDISINISCHE VERWENDUNG DERSELBEN。
公开(公告)号：EP0315698A1
公开(公告)日：1989-05-17
申请号：EP88904639.7
申请日：1988-05-25
IPC分类号： C07D495/14 , C07D495/04 , A61K31/55
CPC分类号： C07D495/04 , C07D495/14
摘要： A thienotriazolodiazepine compound represented by general formula (l), wherein Ar is phenyl, pyridyl, substituted phenyl or substituted pyridyl. R 1 and R 3 which may be the same or different are each hydrogen or alkyl having 1 to 4 carbon atoms, R 2 is hydrogen, alkyl having 1 to 4 carbon atoms or trifluoromethyl and R' is straight-chain or branched alkyl alkenyl or alkinyl having 6 to 18 carbon atoms, or a thienodiazepine compound represented by general formula (ll), wherein Ar, R 1 , R 2 and R' are as defined above, a pharmaceutically acceptable salt thereof, and a medicinal application thereof. These compounds are useful as a therapeutic agent for circulatory diseases and various diseases induced by a platelet activating factor. Further, the compound (ll) is also useful as an intermediate for synthesis of the compound (l).
摘要翻译： 式（I）的噻吩并三唑并氮杂并且其中Ar为Ph或吡啶基（优选）的式（II）的噻吩并二氮杂，R1和R3为H或1-4C烷基，R2为H，1-4C烷基或三氟甲基，R4为 6-18C直链或支链烷基，烯基或炔基。 具体要求的是4-（2-氯苯基）-2-己基-9-甲基-6H-噻吩并（3,2-f）（1,2,4）三唑并（4,3-a）（1,4-二氮杂 ，2-己基-4-（2-甲基苯基）-6,9-二甲基-6H-噻吩并（3,2-f）（1,2,4）三唑并（4,3-a）（1,4） 二氮杂和其他9个。
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公开(公告)号：EP0043858B1
公开(公告)日：1984-04-18
申请号：EP81900262.7
申请日：1981-01-13
IPC分类号： C07D471/04 , C07D513/04 , A61K31/425 , A61K31/435
CPC分类号： C07D471/04 , C07D513/04
摘要： Hetero ring-substituted oxoalkanoic acid derivatives having an immunity-controlling action and represented by the following general formula: (FORMULA) wherein R1 represents a hydrogen atom, a lower alkyl group, or a phenyl, thienyl or furyl group optionally having in an optional position of the nucleus at least one substitutent of halogen, lower alkyl, lower alkoxy, mono- or di-lower alkylamino-substituted lower alkoxy, lower alkylthio, lower alkylsulfinyl, amino, nitro or cyano, R2 and R3 each represents a hydrogen atom or a lower alkyl group, A represents a lower alkylene group, X represents a sulfur atom or a vinylene group, Y represents a nitrogen atom or a methine group optionally having lower alkyl as a substituent, and Z represents a carbonyl group or a single bond.
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4.发明授权THIENO(TRIAZOLO)DIAZEPINE COMPOUNDS AND MEDICINAL APPLICATION OF THE SAME 失效噻吩（TRIAZOLO）DIAZEPINE化合物及其药物应用
公开(公告)号：EP0315698B1
公开(公告)日：1993-03-03
申请号：EP88904639.7
申请日：1988-05-25
IPC分类号： C07D495/14 , C07D495/04 , A61K31/55
CPC分类号： C07D495/04 , C07D495/14
摘要： A thienotriazolodiazepine compound represented by general formula (I), wherein Ar is phenyl, pyridyl, substituted phenyl or substituted pyridyl, R1 and R3 which may be the same or different are each hydrogen or alkyl having 1 to 4 carbon atoms, R2 is hydrogen, alkyl having 1 to 4 carbon atoms or trifluoromethyl and R4 is straight-chain or branched alkyl alkenyl or alkinyl having 6 to 18 carbon atoms, or a thienodiazepine compound represented by general formula (II), wherein Ar, R1, R2, and R4 are as defined above, a pharmaceutically acceptable salt thereof, and a medicinal application thereof. These compounds are useful as a therapeutic agent for circulatory diseases and various diseases induced by a platelet activating factor. Further, the compound (II) is also useful as an intermediate for synthesis of the compound (I).
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5.发明公开ESTER-SUBSTITUTED THIENOTRIAZOLODIAZEPINE COMPOUNDS AND THEIR MEDICINAL USE 失效ESTER-SUBSTITUIERTE THIENOTRIAZOLDIAZEPIN-VERBINDUNGEN UND DEREN VERWENDUNG ALS ARZNEIMITTEL。
公开(公告)号：EP0316456A1
公开(公告)日：1989-05-24
申请号：EP88904671.0
申请日：1988-06-06
IPC分类号： C07D495/14 , A61K31/55
CPC分类号： C07D495/14
摘要： Ester-substituted thienotriazolodiazepine compoundsre- presented by general formula (1)
(wherein Ar represents pyridyl, phenyl or phenyl having one to three same or different substituents R 1 and R 3 , which may be the same or different, each represents hydrogen or C 1-4 alkyl, R 2 represents hydrogen, C 1-4 alkyl ortrifluoromethyl, and R represents C 1-18 straight or branched-chain alkyl, C 2-18 straight or branched-chain alkenyl, aryl, aryl having one to three same or different substituents, aralkyl, aralkyl having one or more same or different substituents on the aromatic ring or alkyl chain, aralkyl fused with a heterocyclic ring, aralkenyl, aralkenyl having one to three same or different substituents, heteroarylalkyl, or optionally substituted indenylalkyl), pharmaceutically acceptable salts thereof, and their medicinal use are disclosed. These compounds are useful as drugs for treating various diseases induced by thrombocyte activator.摘要翻译： 式（I）的噻吩并（3,2-f）（1,2,4）三唑并（4,3-a）（1,4）二氮杂是新的，其中Ar是吡啶基或苯基（优选地被取代 至3卤素，1-4C烷基或1-4C烷氧基）; R1和R3是H或1-4C烷基; R2是H，1-4C烷基或三氟甲基; R是1-18C直链或支链烷基，2-18C直链或支链烯基，芳基（优选取代至多3个卤素，OH，1-4C烷基，1-8C烷氧基或芳烷氧基），芳烷基 OH，1-4C烷基，1-8C烷氧基，芳烷氧基，环烷基，2-4C烯氧基，酰基，苯基，吡啶基，苯氧基或至多3个苯基氨基（取代基） 卤素，1-4C烷基或1-4C烷氧基）或N-对杂环基;或在烷基链上通过氧代或1-4C烷基），杂环稠合的芳烷基（通过芳基，杂环基 或烷基），芳烯基（优选在环上至多3个OH，1-4C烷基或1-4C烷氧基），杂芳烷基（通过杂芳基或烷基取代），或（选择取代）茚基烷基 。 4-（2-氯苯基）-2-（1-（4-甲氧基苯甲酰基）氧乙基）-9-甲基-6H-噻吩并（3,2-f）（1,2,4） - 三唑并（4,3-a ）（1,4）二氮杂; 4-（2-氯苯基）-9-甲基-2-（1-新戊酰氧基乙基）-6H-噻吩并（3,2-f）（1,2,4）三唑并（4,3-a）（1,4） 二氮杂卓; 和其他12个被特别声明。
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