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1. 发明授权

US4929754A Benzenesulphonamidoindanyl compounds 失效
标题翻译：苯磺酰胺基茚满基化合物
公开(公告)号：US4929754A
公开(公告)日：1990-05-29
申请号：US305255
申请日：1989-02-01
申请人： Josef Nickl , Armin Heckel , Erich Muller , Berthold Narr , Johannes Weisenberger , Wolfgang Eisert , Thomas Muller
发明人： Josef Nickl , Armin Heckel , Erich Muller , Berthold Narr , Johannes Weisenberger , Wolfgang Eisert , Thomas Muller
IPC分类号： A61K31/195 , A61K31/215 , A61K31/235 , A61K31/50 , A61P7/02 , A61P43/00 , B01J23/44 , C07C311/21 , C07C311/29 , C07D237/04
CPC分类号： C07D237/04
摘要： The invention relates to new benzenesulphonamidoindanyl compounds useful in the treatment and prophylaxis of thromboembolic diseases, arteriosclerosis and tumor metastasis.

2. 发明授权

US4722929A Novel 2-phenyl-imidazoles and pharmaceutical compositions containing same 失效
标题翻译：新的2-苯基 - 咪唑和含有它们的药物组合物
公开(公告)号：US4722929A
公开(公告)日：1988-02-02
申请号：US684052
申请日：1984-12-20
申请人： Volkhard Austel , Joachim Heider , Norbert Hauel , Manfred Reiffen , Josef Nickl , Jacobus C. A. van Meel , Willi Diederen
发明人： Volkhard Austel , Joachim Heider , Norbert Hauel , Manfred Reiffen , Josef Nickl , Jacobus C. A. van Meel , Willi Diederen
IPC分类号： A61K31/435 , A61K31/50 , A61K31/53 , A61P9/00 , A61P9/04 , A61P9/12 , C07D213/75 , C07D239/54 , C07D239/545 , C07D471/04 , C07D473/00 , C07D473/04 , C07D473/06 , C07D473/28 , C07D473/30 , C07D473/40 , C07D487/04
CPC分类号： C07D213/75 , C07D239/545 , C07D471/04 , C07D473/00 , C07D473/04 , C07D473/06 , C07D473/40 , C07D487/04
摘要： The invention relates to novel 2-phenyl-imidazoles of the formula ##STR1## and the tautomers and acid addition salts thereof, particularly the pharmacologically acceptable acid addition salts, which exhibit valuable pharmacological properties, particularly an effect on the contractility of the heart muscle. The compounds of Formula I may be prepared by methods conventionally used for similar compounds.
摘要翻译：本发明涉及新颖的式（I）的2-苯基 - 咪唑及其互变异构体及其酸加成盐，特别是药理学上可接受的酸加成盐，其具有有价值的药理学性质，特别是对心脏肌肉式I的化合物可以通过常规用于类似化合物的方法制备。

3. 发明授权

US4329347A Cardiotonic and antithrombotic sulfur-containing derivatives of carbostyril 失效
标题翻译：喹诺酮的强心和抗血栓硫含量衍生物
公开(公告)号：US4329347A
公开(公告)日：1982-05-11
申请号：US172009
申请日：1980-07-24
申请人： Erich Muller , Josef Nickl , Josef Roch , Berthold Narr , Walter Haarmann , Johannes M. Weisenberger
发明人： Erich Muller , Josef Nickl , Josef Roch , Berthold Narr , Walter Haarmann , Johannes M. Weisenberger
IPC分类号： A61K31/47 , C07D209/34 , C07D215/22 , C07D215/227 , C07D215/24 , C07D215/26 , C07D215/36 , C07D215/38
CPC分类号： C07D215/227 , A61K31/47 , C07D209/34 , C07D215/24 , C07D215/26 , C07D215/36 , C07D215/38
摘要： Compounds of the formula ##STR1## wherein W is vinylene, methyl-vinylene, methylene or ethylene;m is 0, 1 or 2;D is straight or branched alkylene of 2 to 6 carbon atoms, straight or branched hydroxy-alkylene of 3 to 6 carbon atoms, or xylylene;R.sub.1 is hydrogen or alkyl of 1 to 3 carbon atoms;R.sub.2 is cycloalkyl of 3 to 6 carbon atoms, aryl of 6 to 10 carbon atoms, aralkyl of 7 to 11 carbon atoms, heteroaryl, heteroarlkyl, 1,2,4-triazolyl, triphenylmethyl, 4,5-bis-(p-chlorophenyl)-oxazol-2-yl, N-methyl-cyclohexylamino-carbonylmethyl,-amino-iminomethyl or, when m is 1 or D is hydroxyalkylene or xylylene, also alkyl of 1 to 6 carbon atoms; andR.sub.3 and R.sub.4 are each hydrogen, halogen, alkyl of 1 to 4 carbon atoms, amino, acetylamino or nitro.The compounds of the invention are useful as cardiotonics and as antithrombotics.
摘要翻译：其中W是亚乙烯基，甲基亚乙烯基，亚甲基或亚乙基的式“IMAGE”的化合物; m为0,1或2; D是2至6个碳原子的直链或支链亚烷基，3至6个碳原子的直链或支链羟基 - 亚烷基，或亚二甲苯; R1是氢或1至3个碳原子的烷基; R 2是3至6个碳原子的环烷基，6至10个碳原子的芳基，7至11个碳原子的芳烷基，杂芳基，杂芳烷基，1,2,4-三唑基，三苯基甲基，4,5-双 - （对氯苯基）） - 恶唑-2-基，N-甲基 - 环己基氨基 - 羰基甲基， - 氨基 - 亚氨基甲基，或者当m为1或D为羟基亚烷基或亚二甲苯基时，也为1至6个碳原子的烷基; R 3和R 4各自为氢，卤素，1至4个碳原子的烷基，氨基，乙酰氨基或硝基。本发明的化合物可用作强心剂和抗血栓药。

4. 发明授权

US4021479A Derivatives of 4-(4-biphenylyl)-butyric acid 失效
标题翻译： 4-（4-联苯基） - 丁酸的衍生物
公开(公告)号：US4021479A
公开(公告)日：1977-05-03
申请号：US406196
申请日：1973-10-15
申请人： Ernst Seeger , Wolfhard Engel , Josef Nickl , Helmut Teufel
发明人： Ernst Seeger , Wolfhard Engel , Josef Nickl , Helmut Teufel
IPC分类号： C07C57/58 , C07C63/333 , C07C65/14
CPC分类号： C07C205/56 , C07C57/58 , Y10S514/916
摘要： Compounds of the formulas ##STR1## and ##STR2## wherein A is --CH.sub.2 -- or --CH(OH)--,R.sub.1 is hydrogen, halogen or, when R.sub.2 and R.sub.3 are other than both hydrogen, also methyl,R.sub.2 is hydrogen, halogen, cyano, nitro, amino or (alkanoyl of 1 to 4 carbon atoms)-amino,R.sub.3 is hydrogen or halogen,Provided, however, that at least one of R.sub.1, R.sub.2 and R.sub.3 is other than hydrogen, andR.sub.4 is hydrogen or alkyl of 1 to 4 carbon atoms, and non-toxic salts of the free acids (R.sub.4 = H) formed with inorganic or organic bases; the compounds as well as their salts are useful as antiphlogistics and antiproliferatives.
摘要翻译：其中A是-CH 2 - 或-CH（OH） - ，R 1是氢，卤素，或者当R 2和R 3不同于氢时，也是甲基，R 2是氢，卤素，氰基，硝基，氨基或（1至4个碳原子的烷酰基） - 氨基，R3是氢或卤素，提供，然而，至少一个R 1，R 2和R 3不是氢，并且R 4是氢或烷基 1至4个碳原子的无毒盐和无机或有机碱形成的游离酸（R4 = H）的无毒盐; 化合物及其盐可用作消炎剂和抗增殖剂。

5. 发明授权

US5426119A Arylsulphonamides, pharmaceutical compositions containing these compounds 失效
标题翻译：芳基磺酰胺，含有这些化合物的药物组合物
公开(公告)号：US5426119A
公开(公告)日：1995-06-20
申请号：US154647
申请日：1993-11-18
申请人： Armin Heckel , Josef Nickl, deceased , Rainer Soyka , Wolfgang Eisert , Thomas Muller , Johannes Weisenberger , Christopher Meade , Gojko Muacevic
发明人： Armin Heckel , Josef Nickl, deceased , Rainer Soyka , Wolfgang Eisert , Thomas Muller , Johannes Weisenberger , Christopher Meade , Gojko Muacevic
IPC分类号： C07D213/55 , A61K31/145 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61P7/02 , A61P9/00 , A61P9/10 , A61P11/00 , A61P37/08 , A61P43/00 , C07D213/56 , C07D401/06 , C07D405/06 , C07D409/06 , C07D409/10 , C07D409/12 , C07D409/14
CPC分类号： C07D401/06 , C07D213/55 , C07D213/56 , C07D409/06 , C07D409/12
摘要： The invention relates to new arylsulphonamides of the formula ##STR1## (wherein A, B and R.sub.1 to R.sub.6 are as defined in claim 1, the enantiomers, the cis- and trans-isomers thereof where R.sub.4 and R.sub.5 together represent a carbon-carbon bond, and the addition salts thereof, more particularly for pharmaceutical use the physiologically acceptable addition salts thereof with inorganic or organic bases, if R.sub.6 represents a hydroxy group) which have useful pharmacological properties, particularly antithrombotic activities and thromboxane-mediating activities. Furthermore, the new compounds are also thromboxane antagonists (TRA) and thromboxane synthesis inhibitors (TSH). They also have an effect on PGE.sub.2 production.
摘要翻译：本发明涉及新的式（I）芳基磺酰胺（其中A，B和R 1至R 6如权利要求1中所定义，其对映异构体，顺式和反式异构体，其中R 4和R 5一起代表碳碳键和其加成盐，更特别是药物用途，其与无机或有机碱的生理上可接受的加成盐，如果R6表示羟基），其具有有用的药理学特性，特别是抗血栓形成活性和血栓烷烷介导活性。此外，新化合物还是血栓烷拮抗剂（TRA）和血栓烷合成抑制剂（TSH）。它们也对PGE2产生影响。

6. 发明授权

US5008290A Sulphonamidoethyl compounds and pharmaceutical compositions comprising these compounds 失效
标题翻译：磺酰氨基乙基化合物和包含这些化合物的药物组合物
公开(公告)号：US5008290A
公开(公告)日：1991-04-16
申请号：US319397
申请日：1989-03-03
申请人： Armin Heckel , Josef Nickl , Erich Muller , Berthold Narr , Johannes Weisenberger , Wolfgang Eisert , Thomas Muller
发明人： Armin Heckel , Josef Nickl , Erich Muller , Berthold Narr , Johannes Weisenberger , Wolfgang Eisert , Thomas Muller
IPC分类号： A61K31/40 , A61P9/12 , C07D207/32 , C07D207/335 , C07D207/337 , C07D307/52 , C07D307/54 , C07D333/20 , C07D333/24 , C07D405/04 , C07D409/04 , C07D409/12
CPC分类号： C07D207/335 , C07D207/337 , C07D307/52 , C07D307/54 , C07D333/20 , C07D333/24 , C07D405/04 , C07D409/04
摘要： The invention relates to new sulphonamidoethyl compounds having valuable pharmacological properties, particularly anti-thrombotic properties, and which are also thromboxane antagonists.

7. 发明授权

US4690923A 2-(Perhydro-1,4-diazino)-pyrimido(5,4-D)-pyrimidines, pharmaceutical compositions and use 失效
标题翻译： 2-（全氢-1,4-二氮杂） - 嘧啶并（5,4-D） - 嘧啶，药物组合物和用途
公开(公告)号：US4690923A
公开(公告)日：1987-09-01
申请号：US712341
申请日：1985-03-15
申请人： Josef Roch , Erich Muller , Berthold Narr , Josef Nickl , Walter Haarmann , Johannes M. Weisenberger
发明人： Josef Roch , Erich Muller , Berthold Narr , Josef Nickl , Walter Haarmann , Johannes M. Weisenberger
IPC分类号： C07D498/04 , A61K31/54 , C07D417/14 , C07D487/04
CPC分类号： C07D487/04 , Y10S514/822
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is a substituted alkoxy group, or an optionally substituted mercapto or amino group,R.sub.2 is a cyclic imino group,R.sub.3 is hydrogen, phenyl, alkyl or acyl, andn is 2 or 3,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R 1是取代的烷氧基，或任意取代的巯基或氨基，R 2是环状亚氨基，R 3是氢，苯基，烷基或酰基，n是2或3，其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

US4518596A Antithrombotic use of 2-(perhydro-1,4-diazino)-pyrimido (5,4,D)-pyrimidines 失效
标题翻译： 2-（全氢-1,4-二氮杂） - 嘧啶并（5,4，D） - 嘧啶的抗血栓形成
公开(公告)号：US4518596A
公开(公告)日：1985-05-21
申请号：US575333
申请日：1984-01-31
申请人： Josef Roch , Erich Muller , Berthold Narr , Josef Nickl , Walter Haarmann , Johannes M. Weisenberger
发明人： Josef Roch , Erich Muller , Berthold Narr , Josef Nickl , Walter Haarmann , Johannes M. Weisenberger
IPC分类号： C07D498/04 , A61K31/535 , A61K31/54
CPC分类号： C07D487/04 , Y10S514/822
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is a substituted alkoxy group, or an optionally substituted mercapto or amino group,R.sub.2 is a cyclic imino group,R.sub.3 is hydrogen, phenyl, alkyl or acyl, andn is 2 or 3,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R 1是取代的烷氧基，或任意取代的巯基或氨基，R 2是环状亚氨基，R 3是氢，苯基，烷基或酰基，n是2或3，其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。

9. 发明授权

US4182887A 3-Amino-4-phenyl-1H-pyrazolo[3,4-b]pyridines and salts thereof 失效
标题翻译： 3-氨基-4-苯基-1H-吡唑并[3,4-b]吡啶及其盐
公开(公告)号：US4182887A
公开(公告)日：1980-01-08
申请号：US834114
申请日：1977-09-19
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
CPC分类号： C07D471/04 , C07D213/85 , Y10S514/822
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is mono- or di-substituted amino, where the substituents are selected from the group consisting of alkyl of 1 to 6 carbon atoms, cyclohexyl, allyl and benzyl; unsubstituted, mono-substituted or di-substituted pyrrolidino, piperidino, hexamethyleneimino, morpholino, piperazino, thiomorpholino, 1-oxido-thiomorpholino or 1,1-dioxido-thiomorpholino, where the substituents are selected from the group consisting of methyl, hydroxymethyl, hydroxyl, phenyl and benzyl; 1,2,5,6-tetrahydropyridino; 1,2,3,4-tetrahydroisoquinolino; indolino; or 3,6-ethylene-hexamethyleneimino;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是单取代或二取代的氨基，其中取代基选自1至6个碳原子的烷基，环己基，烯丙基和苄基; 未取代的单取代或二取代的吡咯烷子基，哌啶子基，六亚甲基亚氨基，吗啉代，哌嗪子基，硫代吗啉代，1-氧代硫代吗啉代或1,1-二氧化硫代吗啉代，其中取代基选自甲基，羟甲基，羟基，苯基和苄基; 1,2,5,6-四氢吡啶子; 1,2,3,4-四氢异喹啉; indolino; 或3,6-亚乙基 - 六亚甲基亚氨基; 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。

10. 发明授权

US4820705A Benzenesulphonamidoindanyl compounds, medicaments thereof, and processes of preparation 失效
标题翻译：苯磺酰胺基茚满基化合物，其药物及其制备方法
公开(公告)号：US4820705A
公开(公告)日：1989-04-11
申请号：US73950
申请日：1987-07-16
申请人： Josef Nickl , Armin Heckel , Erich Muller , Berthold Narr , Johannes Weisenberger , Wolfgang Eisert , Thomas Muller
发明人： Josef Nickl , Armin Heckel , Erich Muller , Berthold Narr , Johannes Weisenberger , Wolfgang Eisert , Thomas Muller
IPC分类号： A61K31/195 , A61K31/215 , A61K31/235 , A61K31/50 , A61P7/02 , A61P43/00 , B01J23/44 , C07C311/21 , C07C311/29 , C07D237/04 , C07D237/14 , C07D237/24
CPC分类号： C07D237/04
摘要： The invention relates to new benzenesulphonamidoindanyl compounds having the following formula ##STR1## wherein the substituents are defined herein useful in the treatment and prophylaxis of thromboembolic diseases, arteriosclerosis and tumor metastasis.
摘要翻译：本发明涉及具有下式的新的苯磺酰胺基茚满基化合物（Ⅰ），其中本文定义的取代基可用于治疗和预防血栓栓塞性疾病，动脉硬化和肿瘤转移。

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