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1. 发明授权

US4137313A 2,5-Dihydro-1,2-thiazino(5,6-b)indole-3-carboxamide-1,1-dioxides and salts thereof 失效
标题翻译： 2,5-二氢-1,2-噻嗪（5,6-b）吲哚-3-甲酰胺-1,1-二氧化物及其盐
公开(公告)号：US4137313A
公开(公告)日：1979-01-30
申请号：US872889
申请日：1978-01-27
申请人： Gunter Trummlitz , Wolfhard Engel , Ernst Seeger , Walter Haarmann , Gunther Engelhardt
发明人： Gunter Trummlitz , Wolfhard Engel , Ernst Seeger , Walter Haarmann , Gunther Engelhardt
IPC分类号： A61K31/54 , A61P7/02 , A61P29/00 , C07D209/42 , C07D513/04 , C07D513/14 , A61K31/38
CPC分类号： C07D513/04 , C07D209/42 , C07D513/14 , Y10S514/822
摘要： Compounds of the formula ##STR1## WHEREIN R.sub.1 is hydrogen, methyl or ethyl;R.sub.2 is methyl or ethyl;Y is hydrogen, fluorine, chlorine, bromine, methoxy, methyl, ethyl or trifluoromethyl; andAr is 2-thiazolyl which may have one or two methyl or ethyl substituents attached thereto; 5,6-dihydro-4H-cyclopentathiazol-2-yl; 4,5,6,7-tetrahydro-2-benzothiazolyl; 2-benzothiazolyl; 3-isothiazolyl which may have a methyl substituent attached thereto; 2-pyridyl which may have a methyl or hydroxyl substituent attached thereto; 3-pyridyl; 4-pyridyl; 4-pyrimidinyl; pyrazinyl; 2-benzimidazolyl; 2-oxazolyl which may have a methyl substituent attached thereto; 2-benzoxazolyl; or phenyl which may have a fluoro, chloro, bromo, methyl, ethyl, trifluoromethyl or methoxy substituent attached thereto; and non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases. The compounds as well as their salts are useful as antiphlogistics and blood platelet aggregation inhibitors.
摘要翻译：式中的化合物，其中R1是氢，甲基或乙基; R2是甲基或乙基; Y是氢，氟，氯，溴，甲氧基，甲基，乙基或三氟甲基; 并且Ar是可以具有一个或两个连接到其上的甲基或乙基取代基的2-噻唑基; 5,6-二氢-4H-环戊基噻唑-2-基; 4,5,6,7-四氢-2-苯并噻唑基; 2-苯并噻唑基可具有与其连接的甲基取代基的3-异噻唑基; 可以具有连接到其上的甲基或羟基取代基的2-吡啶基; 3-吡啶基; 4-吡啶基; 4-嘧啶基; 吡嗪基 2-苯并咪唑基; 可具有与其连接的甲基取代基的2-恶唑基; 2-苯并恶唑基; 或可具有与其连接的氟，氯，溴，甲基，乙基，三氟甲基或甲氧基取代基的苯基; 和与无机或有机碱形成的无毒的，药学上可接受的盐。化合物及其盐可用作消炎剂和血小板聚集抑制剂。

2. 发明授权

US4259336A 4-Hydroxy-2H-[1]-benzothieno [2,3-e]-1,2-thiazine-3-carboxamide-1,1-dioxides and salts thereof 失效
标题翻译： 4-羟基-2H- [1] - 苯并噻吩并[2,3-e] -1,2-噻嗪-3-甲酰胺-1,1-二氧化物及其盐
公开(公告)号：US4259336A
公开(公告)日：1981-03-31
申请号：US86743
申请日：1979-10-22
申请人： Wolfhard Engel , Gunter Trummlitz , Ernst Seeger , Walter Haarmann , Gunther Engelhardt , Rainer Zimmermann
发明人： Wolfhard Engel , Gunter Trummlitz , Ernst Seeger , Walter Haarmann , Gunther Engelhardt , Rainer Zimmermann
IPC分类号： A61K31/54 , A61P9/08 , A61P9/10 , A61P29/00 , C07D333/70 , C07D513/04 , A61K31/38
CPC分类号： C07D513/04 , C07D333/70 , Y10S514/822
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, halogen or alkyl of 1 to 3 carbon atoms; R.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms; andR.sub.3 is aromatic hydrocarbyl of 6 to 10 carbon atoms or an aromatic heterocycle of 2 to 9 carbon atoms and 1 to 2 nitrogen atoms and/or an oxygen or a sulfur atom, where each of said aromatic substituents may in turn be substituted with one or two alkyls of 1 to 6 carbon atoms, halogen, hydroxyl, trifluoromethyl, halophenyl or alkoxy of 1 to 3 carbon atoms;and non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases; the compounds as well as their salts are useful as analgesics, antipyretics, antithrombotic and antiphlogistics.
摘要翻译：其中R 1是氢，卤素或1至3个碳原子的烷基; R2是氢或1至3个碳原子的烷基; 并且R 3是6至10个碳原子的芳族烃基或2至9个碳原子和1至2个氮原子和/或氧或硫原子的芳族杂环，其中每个所述芳族取代基可以依次被一个或两个1至6个碳原子的烷基，卤素，羟基，三氟甲基，卤代苯基或具有1至3个碳原子的烷氧基; 和与无机或有机碱形成的无毒的，药理学上可接受的盐; 化合物及其盐可用作镇痛药，解热药，抗血栓和消炎药。

3. 发明授权

US3992535A 4-Hydroxy-2H-naphtho[2,1-e]-1,2-thiazine-3-carboxamide-1,1-dioxides and salts thereof 失效
标题翻译： 4-羟基-2H-萘并（{2,1-e {9-1,2-噻嗪-3-甲酰胺-1,1-二氧化物及其盐
公开(公告)号：US3992535A
公开(公告)日：1976-11-16
申请号：US626623
申请日：1975-10-29
申请人： Gunter Trummlitz , Helmut Teufel , Wolfhard Engel , Ernst Seeger , Walter Haarmann , Gunther Engelhardt
发明人： Gunter Trummlitz , Helmut Teufel , Wolfhard Engel , Ernst Seeger , Walter Haarmann , Gunther Engelhardt
IPC分类号： C07D275/06 , C07D279/02 , C07D417/12 , C07D513/04 , A61K31/54
CPC分类号： C07D275/06 , C07D279/02
摘要： Compounds of the formula ##SPC1##WhereinR.sub.1 is hydrogen, methyl or ethyl, andAr is phenyl, 3-chlorophenyl, 3-bromophenyl, 2-fluorophenyl, 3-fluorophenyl, 4-fluorophenyl, 3-tolyl, 2-methoxyphenyl, 3-methoxyphenyl, 2-pyridyl, 4-methyl-2-pyridyl, 6-methyl-2-pyridyl, 3-hydroxy-2-pyridyl, 3-pyridyl, 4-pyridyl, 6-chloro-3-pyridazinyl, 2-pyrazinyl, 6-chloro-2-pyrazinyl, 6-chloro-4-pyrimidinyl, 2-thiazolyl, 4-methyl-2-thiazolyl, 4-ethyl-2-thiazolyl, 5-methyl-2-thiazolyl, 5-ethyl-2-thiazolyl, 4,5-dimethyl-2-thiazolyl, 4-ethyl-5-methyl-2-thiazolyl, 5-ethyl-4-methyl-2-thiazolyl, 2-benzothiazolyl, 4,5,6,7-tetrahydro-2-benzothiazolyl, 5,6-dihydro-7H-thiopyrano[4,3-d]thiazol-2-yl, 3-methyl-5-isothiazolyl, 1,3,4-thiadiazolyl, 5-methyl-1,3,4-thiadiazol-2-yl or 5-methyl-3-isoxazolyl,And non-toxic, pharmacologically acceptable salts thereof formed with an inorganic or organic base; the compounds as well as their salts are useful as inhibitors of platelet adhesion and aggregation.
摘要翻译：式WHERE R1的化合物是氢，甲基或乙基，Ar是苯基，3-氯苯基，3-溴苯基，2-氟苯基，3-氟苯基，4-氟苯基，3-甲苯基，2-甲氧基苯基，3-甲氧基苯基， 2-吡啶基，4-甲基-2-吡啶基，6-甲基-2-吡啶基，3-羟基-2-吡啶基，3-吡啶基，4-吡啶基，6-氯-3-哒嗪基，2-吡嗪基，6-吡啶基， 4-氯-2-吡嗪基，6-氯-4-嘧啶基，2-噻唑基，4-甲基-2-噻唑基，4-乙基-2-噻唑基，5-甲基-2-噻唑基，5-乙基-2-噻唑基， 4,5-二甲基-2-噻唑基，4-乙基-5-甲基-2-噻唑基，5-乙基-4-甲基-2-噻唑基，2-苯并噻唑基，4,5,6,7-四氢-2- 苯并噻唑基，5,6-二氢-7H-噻喃并[4,3-d]噻唑-2-基，3-甲基-5-异噻唑基，1,3,4-噻二唑基，5-甲基-1,3,4-噻二唑基，噻二唑-2-基或5-甲基-3-异恶唑基，以及与无机或有机碱形成的非毒性，药理学上可接受的盐; 化合物作为它们的盐作为板材粘合和聚集的抑制剂有用。

4. 发明授权

US4533664A Antithrombotic N-(6-chloro-pyrazin-2-yl)-4-Hydroxy-2H-1,2-benzothiazine-3-carboxamide-1 ,1-dioxide derivatives, composition, and method of use 失效
标题翻译：抗血栓形成的N-（6-氯 - 吡嗪-2-基）-4-羟基-2H-1,2-苯并噻嗪-3-甲酰胺-1,1-二氧化物衍生物，组合物和使用方法
公开(公告)号：US4533664A
公开(公告)日：1985-08-06
申请号：US537592
申请日：1983-09-30
申请人： Gunter Trummlitz , Wolfhard Engel , Ernst Seeger , Walter Haarmann
发明人： Gunter Trummlitz , Wolfhard Engel , Ernst Seeger , Walter Haarmann
IPC分类号： A61K31/497 , A61K31/54 , A61K31/5415 , A61P7/02 , C07D417/12 , A61K31/38 , C07D417/02
CPC分类号： C07D417/12
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, methyl, methoxy, fluorine or chlorine; andR.sub.2 is hydrogen, methyl, ethyl or n-propyl;and non-toxic, pharmacologically acceptable salts thereof formed with an inorganic or organic base. The compounds as well as the salts are useful as antithrombotics.
摘要翻译：其中R 1是氢，甲基，甲氧基，氟或氯的式IMA化合物; R2是氢，甲基，乙基或正丙基; 和与无机或有机碱形成的无毒的，药学上可接受的盐。化合物以及盐可用作抗血栓形成剂。

5. 发明授权

US5188940A Method of determining the total fibrinolytic activity in the plasma 失效
标题翻译：确定等离子体中的总纤维素活性的方法
公开(公告)号：US5188940A
公开(公告)日：1993-02-23
申请号：US463177
申请日：1990-01-10
申请人： Jurgen Krause , Walter Haarmann
发明人： Jurgen Krause , Walter Haarmann
IPC分类号： C12Q1/37 , C12Q1/56 , G01N33/86
CPC分类号： G01N33/86 , C12Q1/56 , G01N2333/75 , G01N2333/968 , G01N2333/9726
摘要： A method of determining the total fibrinolytic activity in plasma, is characterized in thata) a quantity of fibrin sufficient to produce turbidity is added to a dilute platelet poor plasma sample or is produced in situ and the time dependent change in turbidity or the time-dependent formation of fibrin cleavage products is measured; orb) a chromogenic plasmin substrate and a quantity of fibrin, fibrinogen cleavage products or an enzyme which produces fibrin in situ, insufficient to produce turbidity, is added to a dilute platelet poor plasma sample and the time dependent color formation is measured.
摘要翻译：确定血浆中总的纤维蛋白溶解活性的方法的特征在于：a）足以产生浊度的纤维蛋白量被加入稀释的血小板贫血血浆样品中，或者原位产生，并且浊度或时间依赖性时间依赖性变化，测量纤维蛋白裂解产物的依赖性形成; 或b）色素性纤溶酶底物和一定量的纤维蛋白，纤维蛋白原裂解产物或原位产生纤维蛋白的酶，不足以产生浊度，加入稀释的血小板不良血浆样品中，并测量时间依赖性色素形成。

6. 发明授权

US4560685A 2-Piperazino-pteridines useful as antithrombotics and antimetastatics 失效
标题翻译： 2-Piperazino-pteridines可用作抗血栓形成和抗转移
公开(公告)号：US4560685A
公开(公告)日：1985-12-24
申请号：US621438
申请日：1984-06-18
申请人： Josef Roch , Josef Nickl , Erich Muller , Berthold Narr , Johannes Weisenberger , Rainer Zimmermann , Walter Haarmann
发明人： Josef Roch , Josef Nickl , Erich Muller , Berthold Narr , Johannes Weisenberger , Rainer Zimmermann , Walter Haarmann
IPC分类号： C07D475/06 , C07D475/08 , A61K31/505
CPC分类号： C07D475/06 , C07D475/08
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is phenylalkylamino, alkylamino, dialkylamino, piperidino, morpholino, thiomorpholino or 1-oxido-thiomorpholino;R.sub.2 is dialkylamino, piperidino, morpholino, thiomorpholino or 1-oxido-thiomorpholino; andR.sub.3 is halogen, alkoxy, alkylthio, phenylalkoxy or phenylalkylthio;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antithrombotics and antimetastatics.
摘要翻译：其中R 1是苯基烷基氨基，烷基氨基，二烷基氨基，哌啶子基，吗啉代，硫代吗啉代或1-氧代硫代吗啉代; R2是二烷基氨基，哌啶子基，吗啉代，硫代吗啉代或1-氧代硫代吗啉代; R3是卤素，烷氧基，烷硫基，苯基烷氧基或苯基烷硫基; 和无毒的，药学上可接受的酸加成盐。化合物及其盐可用作抗血栓形成和抗转移酶。

7. 发明授权

US4551464A Antithrombotic sulfoximino carbostyrils 失效
标题翻译：抗血栓形式的磺酰亚胺喹诺酮类
公开(公告)号：US4551464A
公开(公告)日：1985-11-05
申请号：US573964
申请日：1984-01-26
申请人： Erich Muller , Josef Nickl , Berthold Narr , Josef Roch , Walter Haarmann , Johannes M. Weisenberger
发明人： Erich Muller , Josef Nickl , Berthold Narr , Josef Roch , Walter Haarmann , Johannes M. Weisenberger
IPC分类号： A61K31/40 , A61K31/455 , A61K31/47 , C07D209/34 , C07D215/22 , C07D215/227 , C07D401/02 , C07D401/12 , C07D409/02 , C07D409/12
CPC分类号： C07D215/227 , C07D209/34 , C07D401/12 , C07D409/12
摘要： Compounds of the formula ##STR1## wherein n is 0 or 1;A is methylene, vinylene or ethylene optionally substituted by lower alkyl;B is alkylene;R.sub.1 is an optionally substituted alkyl, phenyl or naphthyl group, or a cycloalkyl or pyridyl group; andR.sub.2 is hydrogen or acyl;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antithrombotics.
摘要翻译：其中n为0或1的式（I）的化合物; A是任选被低级烷基取代的亚甲基，亚乙烯基或乙烯基; B是亚烷基; R1是任选取代的烷基，苯基或萘基，或环烷基或吡啶基; 并且R 2是氢或酰基; 和无毒的，药学上可接受的酸加成盐。化合物及其盐可用作抗血栓形成剂。

8. 发明授权

US4260621A 3-Amino-4-phenyl-6-piperidino-1H-pyrazolo[3,4-b]-pyridines and salts thereof 失效
标题翻译： 3-氨基-4-苯基-6-哌啶子基-1H-吡唑并[3,4-b] - 吡啶及其盐
公开(公告)号：US4260621A
公开(公告)日：1981-04-07
申请号：US75100
申请日：1979-09-13
申请人： Josef Roch , Erich Muller , Berthold Narr , Josef Nickl , Walter Haarmann
发明人： Josef Roch , Erich Muller , Berthold Narr , Josef Nickl , Walter Haarmann
IPC分类号： A61K31/435 , A61P7/02 , A61P29/00 , C07D213/85 , C07D471/04 , A61K31/445
CPC分类号： C07D471/04 , C07D213/85 , Y10S514/822
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is unsubstituted, mono-substituted or di-substituted piperidino, where the substituents are selected from the group consisting of methyl, hydroxymethyl, hydroxyl, phenyl and benzyl;R.sub.2 is hydrogen, methyl or benzyl; andR.sub.3 is hydrogen, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 3 carbon atoms;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antiphlogistics and antithrombotics.
摘要翻译：其中R 1是未取代的，单取代的或二取代的哌啶子基，其中取代基选自甲基，羟甲基，羟基，苯基和苄基; R2是氢，甲基或苄基; R3为氢，卤素，1〜3个碳原子的烷基或1〜3个碳原子的烷氧基; 和无毒的，药学上可接受的酸加成盐。化合物及其盐可用作消炎和抗血栓形成。

9. 发明授权

US4191776A Biphenyl derivatives 失效
标题翻译：联苯衍生物
公开(公告)号：US4191776A
公开(公告)日：1980-03-04
申请号：US852714
申请日：1977-11-18
申请人： Josef Nickl , Erich Muller , Berthold Narr , Walter Haarmann , Wolfgang Schroter , Rudolf Kadatz
发明人： Josef Nickl , Erich Muller , Berthold Narr , Walter Haarmann , Wolfgang Schroter , Rudolf Kadatz
IPC分类号： C07C67/00 , C07C69/76 , C07C313/00 , C07C315/04 , C07C317/10 , C07C317/18 , C07C317/24 , C07C317/44 , C07C323/16 , C07C323/45 , C07C323/52 , C07C323/60 , C07C323/65 , C07D213/30 , C07D295/185 , C07C147/107 , A61K31/235 , A61K31/44 , C07C147/14
CPC分类号： C07D213/30 , C07C317/10 , C07C317/18 , C07C317/24 , C07C317/44 , C07C323/16 , C07C323/45 , C07C323/52 , C07C323/60 , C07C323/65 , C07D295/185 , Y10S514/822
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, fluorine, chlorine, bromine, methyl, methoxy, methylthio or cyano;R.sub.2 is hydrogen or fluorine;R.sub.3 is carboxyl, (alkoxy of 1 to 6 carbon atoms)-carbonyl, methoxy-(alkoxy of 1 to 6 carbon atoms)-carbonyl, (alkenyloxy of 2 to 6 carbon atoms)-carbonyl, (aralkoxy of 7 to 12 carbon atoms)-carbonyl, phenoxy-carbonyl or pyridyl-methoxy-carbonyl,A is (alkyl of 1 to 3 carbon atoms)-methylene,m is 1 or 2; andn is 0, 1, 2 or 3;and, when R.sub.3 is carboxyl, non-toxic salts thereof formed with an inorganic or organic base. The compounds as well as the salts are useful as antithrombotics, anticholesteremics and anticoagulants.
摘要翻译：其中R 1是氢，氟，氯，溴，甲基，甲氧基，甲硫基或氰基的式 R2是氢或氟; R 3为羧基，（碳原子数1〜6的烷氧基） - 羰基，甲氧基 - （1〜6个碳原子的烷氧基） - 羰基，（2〜6个碳原子的烯氧基） - 羰基，（碳原子数为7〜12）） - 羰基，苯氧基 - 羰基或吡啶基 - 甲氧基 - 羰基，A是（1至3个碳原子的烷基） - 亚甲基，m是1或2; 并且n为0,1,2或3; 并且当R 3为羧基时，其无毒盐与无机或有机碱形成。化合物以及盐可用作抗血栓形成剂，抗胆固醇剂和抗凝剂。

10. 发明授权

US3993683A Biphenylyl derivatives 失效
标题翻译：联苯衍生物
公开(公告)号：US3993683A
公开(公告)日：1976-11-23
申请号：US577169
申请日：1975-05-14
申请人： Josef Nickl , Erich Muller , Berthold Narr , Walter Haarmann , Wolfgang Schroter , Rudolf Kadatz
发明人： Josef Nickl , Erich Muller , Berthold Narr , Walter Haarmann , Wolfgang Schroter , Rudolf Kadatz
IPC分类号： C07C67/00 , C07C69/76 , C07C313/00 , C07C315/04 , C07C317/10 , C07C317/18 , C07C317/24 , C07C317/44 , C07C323/16 , C07C323/45 , C07C323/52 , C07C323/60 , C07C323/65 , C07D213/30 , C07D295/185 , C07C149/40
CPC分类号： C07D213/30 , C07C317/10 , C07C317/18 , C07C317/24 , C07C317/44 , C07C323/16 , C07C323/45 , C07C323/52 , C07C323/60 , C07C323/65 , C07D295/185 , Y10S514/822
摘要： Compounds of the formula ##SPC1##WhereinR.sub.1 is hydrogen, fluorine, bromine, methyl, methoxy, methylthio, nitro, cyano or, when A is other than methylene, R.sub.2 is hydrogen, R.sub.3 is carboxyl, m is 2 and n is 0, also chlorine;R.sub.2 is hydrogen or fluorine;R.sub.3 is hydrogen, methyl, hydroxymethyl, carboxyl, (alkoxy of 1 to 6 carbon atoms)-carbonyl, methoxy-(alkoxy of 1 to 6 carbon atoms)-carbonyl, (alkenyloxy of 2 to 6 carbon atoms)-carbonyl, (aralkoxy of 7 to 12 carbon atoms)-carbonyl, phenoxy-carbonyl, pyridylmethoxy-carbonyl, amino-carbonyl, (alkyl of 1 to 3 carbon atoms-amino)-carbonyl, (dialkyl of 1 to 3 carbon atoms-amino)-carbonyl, phenylamino-carbonyl, morpholino-carbonyl, piperidino-carbonyl, thiomorpholino-carbonyl, (1-oxidothiomorpholino)-carbonyl or (1,1-dioxido-thiomorpholino)-carbonyl;A is methylene, (alkyl of 1 to 3 carbon atoms)-methylene, di-(alkyl of 1 to 3 carbon atoms)-methylene, hydroxymethyl-methylene, hydroxymethylene or carbonyl;m is 1 or 2; andn is 0, 1, 2 or 3;And, when R.sub.3 is carboxyl, non-toxic salts thereof formed with an inorganic or organic base. The compounds as well as the salts are useful as antithrombotics, anticholesteremics and anticoagulants.
摘要翻译：式A的化合物是氢，氟，溴，甲基，甲氧基，甲硫基，硝基，氰基，或当A不是亚甲基时，R 2是氢，R 3是羧基，m是2，n是0，也是氯; R2是氢或氟; R 3是氢，甲基，羟甲基，羧基，（1至6个碳原子的烷氧基） - 羰基，甲氧基 - （1至6个碳原子的烷氧基） - 羰基，（2至6个碳原子的链烯氧基） - 羰基 7至12个碳原子的羰基，苯氧基 - 羰基，吡啶基甲氧羰基，氨基 - 羰基，（1至3个碳原子的烷基 - 氨基） - 羰基，（1至3个碳原子的二烷基 - 氨基） - 羰基，苯基氨基羰基，吗啉代羰基，哌啶子基 - 羰基，硫代吗啉代羰基，（1-氧硫基吗啉代）羰基或（1,1-二氧化硫代吗啉代）羰基。 A是亚甲基，（1至3个碳原子的烷基） - 亚甲基，二（1至3个碳原子的烷基） - 亚甲基，羟甲基 - 亚甲基，羟基亚甲基或羰基; M IS 1 OR 2; 和N是0,1,2或3; 当R 3为羧基时，其无机盐与无机或有机碱形成。化合物以及盐可用作抗血栓形成剂，抗胆固醇剂和抗凝剂。

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