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1. 发明授权

US4180662A Thiazine derivatives 失效
标题翻译：噻嗪衍生物
公开(公告)号：US4180662A
公开(公告)日：1979-12-25
申请号：US938274
申请日：1978-08-31
申请人： Rudolf Pfister , Paul Zeller , Dieter Binder , Otto Hromatka
发明人： Rudolf Pfister , Paul Zeller , Dieter Binder , Otto Hromatka
IPC分类号： A61K31/54 , A61P7/02 , A61P25/04 , A61P29/00 , C07D333/34 , C07D333/38 , C07D513/04
CPC分类号： C07D513/04 , C07D333/34 , C07D333/38
摘要： Anti-inflammatory, analgesic, anti-rheumatic and anti-thrombotic thienothiazine derivatives having the formula ##STR1## wherein A together with the two carbon atoms forms the group ##STR2## and the dotted line indicates the double bond present in the first and last thieno structures above, R.sup.1 is lower alkyl, R.sup.2 is the radical of an aromatic heterocycle with 1 to 4 hetero atoms optionally substituted by one or two lower alkyl groups, or a phenyl radical optionally substituted by halogen, hydroxy, lower alkyl, trifluoromethyl or lower alkoxy, R.sup.3 is halogen and R.sup.3' is hydrogen or halogen,and pharmaceutically acceptable salts thereof are described.
摘要翻译：具有下式的抗炎，止痛，抗风湿和抗血栓形成噻吩噻嗪衍生物其中A与两个碳原子一起形成基团，虚线表示存在于第一和最后一个 R 1为低级烷基，R 2为任选被一个或两个低级烷基取代的具有1至4个杂原子的芳族杂环的基团，或任选被卤素，羟基，低级烷基，三氟甲基或低级烷基取代的苯基烷氧基，R 3为卤素，R 3'为氢或卤素，及其药学上可接受的盐。

2. 发明授权

US4544655A Antiinflammatory, analgesic, and antirheumatic 4-hydroxy-2-methyl-n-(2-pyridyl)-6-trifluoromethyl-2H-thieno[2,3-e]-1,2- thiazine-3-carboxamide 1,1-dioxide, corresponding compositions, and 3-carboxylic acid lower alkyl ester intermediates 失效
标题翻译：抗炎，镇痛和抗风湿4-羟基-2-甲基 - （2-吡啶基）-6-三氟甲基-2H-噻吩并[2,3-e] -1,2-噻嗪-3-甲酰胺1,1- 二氧化物，相应的组合物和3-羧酸低级烷基酯中间体
公开(公告)号：US4544655A
公开(公告)日：1985-10-01
申请号：US528341
申请日：1983-08-31
申请人： Rudolf Pfister , Paul Zeller , Dieter Binder , Otto Hromatka
发明人： Rudolf Pfister , Paul Zeller , Dieter Binder , Otto Hromatka
IPC分类号： A61K31/54 , A61P25/04 , A61P29/00 , C07D333/38 , C07D513/04
CPC分类号： C07D513/04 , C07D333/38
摘要： 4-Hydroxy-2-methyl-3-(2-pyridylcarbamoyl)-6-trifluoromethyl-2H-thieno[2,3-e]-1,2-thiazine 1,1-dioxide of the formula ##STR1## and its pharmaceutically acceptable salts which possess valuable pharmacodynamic properties are described. More particularly, the compound and its salts display antiinflammatory, analgesic and antirheumatic activities and they are readily accessible by reacting a corresponding alkyl ester with 2-aminopyridine and, if desired, subsequent salt formation.
摘要翻译： 4-羟基-2-甲基-3-（2-吡啶基氨基甲酰基）-6-三氟甲基-2H-噻吩并[2,3-e] -1,2-噻嗪1,1-二氧化物，其式描述了具有有价值的药效学性质的药学上可接受的盐。更具体地，化合物及其盐显示出抗炎，止痛和抗风湿活性，并且通过使相应的烷基酯与2-氨基吡啶反应，并且如果需要，随后的盐形成可以容易地获得。

3. 发明授权

US4175085A Thienothiazine derivatives 失效
标题翻译：噻吩嗪衍生物
公开(公告)号：US4175085A
公开(公告)日：1979-11-20
申请号：US882723
申请日：1978-03-02
申请人： Dieter Binder , Otto Hromatka , Rudolf Pfister , Paul Zeller
发明人： Dieter Binder , Otto Hromatka , Rudolf Pfister , Paul Zeller
IPC分类号： C07D333/34 , C07D333/38 , C07D333/24 , A01N9/00
CPC分类号： C07D333/38 , C07D333/34
摘要： Thienothiazine derivatives of the formula ##STR1## wherein R.sub.1 is lower alkyl; R.sub.2 is an unsubstituted aromatic heterocyclic radical which contains from 1 to 4 hetero atoms or one which is substituted by one or two lower alkyl groups, or is an unsubstituted phenyl radical or one substituted by halogen, hydroxy, lower alkyl, nitro, trifluoromethyl or lower alkoxy; and R.sub.3 and R.sub.4, independently, are hydrogen or lower alkyl,prepared inter alia, from novel intermediates, are described. The end products are useful as anti-inflammatory, analgesic and anti-rheumatic agents.
摘要翻译：式I的噻吩并噻嗪衍生物，其中R 1是低级烷基; R2是未取代的芳族杂环基，其含有1至4个杂原子或被一个或两个低级烷基取代的芳族杂环基，或是未被取代的苯基或被卤素，羟基，低级烷基，硝基，三氟甲基或低级烷氧基 R 3和R 4独立地是氢或低级烷基，特别是由新的中间体制备。最终产品可用作抗炎，镇痛和抗风湿药。

4. 发明授权

US4076709A Thienothiazines 失效
标题翻译：噻吩嗪
公开(公告)号：US4076709A
公开(公告)日：1978-02-28
申请号：US606563
申请日：1975-08-21
申请人： Otto Hromatka , Dieter Binder , Rudolf Pfister , Paul Zeller
发明人： Otto Hromatka , Dieter Binder , Rudolf Pfister , Paul Zeller
IPC分类号： C07D333/38 , C07D513/04
CPC分类号： C07D513/04 , C07D333/38
摘要： The present invention relates to compounds of the formula ##STR1## wherein A together with the two carbon atoms to which it is attached forms the group ##STR2## AND THE BROKEN LINE REPRESENTS THE DOUBLE BOND IN GROUP (A); R.sub.1 represents a lower alkyl group; R.sub.2 represents the residue of an aromatic heterocyclic ring containing from 1 to 4 hetero atoms, which may be substituted by one or two lower alkyl groups, or a phenyl group which may be substituted by halogen, hydroxy, lower alkyl, trifluoromethyl or lower alkoxy and R.sub.3 and R.sub.4 each represent a hydrogen atom or a lower alkyl group.Also provided are methods for their preparation. The thienothiazine derivatives provided by this invention have anti-flammatory, analgesic and antirheumatic activity.
摘要翻译：本发明涉及下式的化合物：其中A与其所连接的两个碳原子一起形成组（A），并且断线表示组（A）中的双键; R1表示低级烷基; R2表示可以被一个或两个低级烷基取代的含有1至4个杂原子的芳族杂环的残基或可以被卤素，羟基，低级烷基，三氟甲基或低级烷氧基取代的苯基， R3和R4各自表示氢原子或低级烷基。

5. 发明授权

US4177193A Thienothiazine derivatives 失效
标题翻译：噻吩嗪衍生物
公开(公告)号：US4177193A
公开(公告)日：1979-12-04
申请号：US955567
申请日：1978-10-30
申请人： Otto Hromatka , Dieter Binder , Rudolf Pfister , Paul Zeller
发明人： Otto Hromatka , Dieter Binder , Rudolf Pfister , Paul Zeller
IPC分类号： C07D333/38 , C07D513/04
CPC分类号： C07D513/04 , C07D333/38
摘要： The present invention relates to compounds of the formula ##STR1## wherein A together with the two carbon atoms to which it is attached forms the group ##STR2## and the broken line represents the double bond in group (a); R.sub.1 represents a lower alkyl group; R.sub.2 represents the residue of an aromatic heterocyclic ring containing from 1 to 4 hetero atoms, which may be substituted by one or two lower alkyl groups, or a phenyl group which may be substituted by halogen, hydroxy, lower alkyl, trifluoromethyl or lower alkoxy and R.sub.3 and R.sub.4 each represent a hydrogen atom or a lower alkyl group.Also provided are methods for their preparation. The thienothiazine derivatives provided by this invention have anti-flammatory, analgesic and anti-rheumatic activity.
摘要翻译：本发明涉及下式化合物其中A与连接的两个碳原子一起形成基团，虚线代表组（a）中的双键; R1表示低级烷基; R2表示可以被一个或两个低级烷基取代的含有1至4个杂原子的芳族杂环的残基或可以被卤素，羟基，低级烷基，三氟甲基或低级烷氧基取代的苯基， R3和R4各自表示氢原子或低级烷基。还提供了它们的制备方法。本发明提供的噻吩并噻嗪衍生物具有抗炎，镇痛和抗风湿活性。

6. 发明授权

US4134898A N-Carbalkoxymethylsulfamoyl thiophene carboxylic acid alkyl esters 失效
标题翻译： N-烷氧基甲基氨磺酰基噻吩羧酸烷基酯
公开(公告)号：US4134898A
公开(公告)日：1979-01-16
申请号：US852385
申请日：1977-11-17
申请人： Otto Hromatka , Dieter Binder , Rudolf Pfister , Paul Zeller
发明人： Otto Hromatka , Dieter Binder , Rudolf Pfister , Paul Zeller
IPC分类号： C07D333/38
CPC分类号： C07D333/38
摘要： The present invention relates to compounds of the formula ##STR1## wherein A together with the two carbon atoms to which it is attached forms the group ##STR2## AND THE BROKEN LINE REPRESENTS THE DOUBLE BOND IN GROUP (A); R.sub.1 represents a lower alkyl group; R.sub.2 represents the residue of an aromatic heterocyclic ring containing from 1 to 4 hetero atoms, which may be substituted by one or two lower alkyl groups, or a phenyl group which may be substituted by halogen, hydroxy, lower alkyl, trifluoromethyl or lower alkoxy and R.sub.3 and R.sub.4 each represent a hydrogen atom or a lower alkyl group.
摘要翻译：本发明涉及下式的化合物：其中A与其所连接的两个碳原子一起形成组（A），并且断线表示组（A）中的双键; R1表示低级烷基; R2表示可以被一个或两个低级烷基取代的含有1至4个杂原子的芳族杂环的残基或可以被卤素，羟基，低级烷基，三氟甲基或低级烷氧基取代的苯基， R3和R4各自表示氢原子或低级烷基。

7. 发明授权

US4090020A Thienothiazine derivatives 失效
标题翻译：噻吩嗪衍生物
公开(公告)号：US4090020A
公开(公告)日：1978-05-16
申请号：US767016
申请日：1977-02-09
申请人： Dieter Binder , Otto Hromatka , Rudolf Pfister , Paul Zeller
发明人： Dieter Binder , Otto Hromatka , Rudolf Pfister , Paul Zeller
IPC分类号： A61K31/54 , A61P7/02 , A61P25/04 , A61P29/00 , C07D333/34 , C07D333/38 , C07D513/04 , A61K31/38
CPC分类号： C07D513/04 , C07D333/34 , C07D333/38
摘要： Thienothiazine derivatives of the formula ##STR1## wherein R.sub.1 is lower alkyl; R.sub.2 is an unsubstituted aromatic heterocyclic radical which contains from 1 to 4 hetero atoms or one which is substituted by one or two lower alkyl groups, or is an unsubstituted phenyl radical or one substituted by halogen, hydroxy, lower alkyl, nitro, trifluoromethyl or lower alkoxy; and R.sub.3 and R.sub.4, independently, are hydrogen or lower alkyl,Prepared inter alia, from novel intermediates, are described. The end products are useful as anti-inflammatory, analgesic and anti-rheumatic agents.
摘要翻译：式I的噻吩并噻嗪衍生物，其中R 1是低级烷基; R2是未取代的芳族杂环基，其含有1至4个杂原子或被一个或两个低级烷基取代的芳族杂环基，或是未被取代的苯基或被卤素，羟基，低级烷基，硝基，三氟甲基或低级烷氧基并且R3和R4独立地是氢或低级烷基，来自新式中间体的制备的相互作用。最终产品可用作抗炎，镇痛和抗风湿药。

8. 发明授权

US4224445A Thienothiazine derivatives 失效
标题翻译：噻吩嗪衍生物
公开(公告)号：US4224445A
公开(公告)日：1980-09-23
申请号：US955568
申请日：1978-10-30
申请人： Otto Hromatka , Dieter Binder , Rudolf Pfister , Paul Zeller
发明人： Otto Hromatka , Dieter Binder , Rudolf Pfister , Paul Zeller
IPC分类号： C07D333/38 , C07D513/04 , C07D333/40
CPC分类号： C07D513/04 , C07D333/38
摘要： The present invention relates to compounds of the formula ##STR1## wherein A together with the two carbon atoms to which it is attached forms the group ##STR2## and the broken line represents the double bond in group (a); R.sub.1 represents a lower alkyl group; R.sub.2 represents the residue of an aromatic heterocyclic ring containing from 1 to 4 hetero atoms, which may be substituted by one or two lower alkyl groups, or a phenyl group which may be substituted by halogen, hydroxy, lower alkyl, trifluoromethyl or lower alkoxy and R.sub.3 and R.sub.4 each represent a hydrogen atom or a lower alkyl group.Also provided are methods for their preparation. The thienothiazine derivatives provided by this invention have anti-flammatory, analgesic and anti-rheumatic activity.
摘要翻译：本发明涉及下式化合物其中A与连接的两个碳原子一起形成基团，虚线代表组（a）中的双键; R1表示低级烷基; R2表示可以被一个或两个低级烷基取代的含有1至4个杂原子的芳族杂环的残基或可以被卤素，羟基，低级烷基，三氟甲基或低级烷氧基取代的苯基， R3和R4各自表示氢原子或低级烷基。还提供了它们的制备方法。本发明提供的噻吩并噻嗪衍生物具有抗炎，镇痛和抗风湿活性。

9. 发明授权

US4187303A Thiazine derivatives 失效
标题翻译：噻嗪衍生物
公开(公告)号：US4187303A
公开(公告)日：1980-02-05
申请号：US933682
申请日：1978-08-15
申请人： Otto Hromatka , Dieter Binder , Paul Zeller , Rudolf Pfister
发明人： Otto Hromatka , Dieter Binder , Paul Zeller , Rudolf Pfister
IPC分类号： A61K31/54 , A61P7/02 , A61P25/04 , A61P29/00 , C07D333/34 , C07D333/38 , C07D513/04 , C07D279/02
CPC分类号： C07D513/04 , C07D333/34 , C07D333/38
摘要： Thienothiazine derivatives of the formula ##STR1## wherein A, R.sub.1 and R.sub.2 are as hereinafter set forth, and their tautomers are described. The thienothiazine derivatives are useful as anti-inflammatory, analgesic, antirheumatic and antithrombotic agents.
摘要翻译：其中A，R 1和R 2如下文所述的式Ⅰ的噻吩噻嗪衍生物及其互变异构体。噻吩并噻嗪衍生物可用作抗炎，镇痛，抗风湿和抗血栓形成剂。

10. 发明授权

US4155913A Thienotriazolodiazepine derivatives 失效
标题翻译：噻吩并三唑并噻嗪衍生物
公开(公告)号：US4155913A
公开(公告)日：1979-05-22
申请号：US842028
申请日：1977-10-14
申请人： Joseph Hellerbach , Paul Zeller , Dieter Binder , Otto Hromatka
发明人： Joseph Hellerbach , Paul Zeller , Dieter Binder , Otto Hromatka
IPC分类号： C07D333/36 , C07D495/04 , C07D495/14
CPC分类号： C07D495/04 , C07D333/36 , C07D495/14 , Y10S514/906 , Y10S514/937 , Y10S514/962 , Y10S514/966
摘要： Novel thienotriazolodiazepine derivatives and processes for their preparation are described. These compounds are useful as anticonvulsants, muscle-relaxants and sedatives.
摘要翻译：描述了新的噻吩并三唑并氮杂衍生物及其制备方法。这些化合物可用作抗惊厥药，肌肉松弛剂和镇静剂。

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