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1. 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。

2. 发明授权

US4442111A Antithrombotic sulfimino and sulfoximino indolinones-2 失效
标题翻译：抗血栓形成亚硫酰亚氨基和磺酰肟基吲哚啉酮-2
公开(公告)号：US4442111A
公开(公告)日：1984-04-10
申请号：US395631
申请日：1982-07-06
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。

3. 发明授权

US4062973A Sulfur-containing derivatives of cyclohexylphenyl-ethane 失效
标题翻译：环己基苯基乙烷的含硫衍生物
公开(公告)号：US4062973A
公开(公告)日：1977-12-13
申请号：US730122
申请日：1976-10-06
申请人： Josef Nickl , Berthold Narr , Erich Muller , Josef Roch , Walter Haarmann
发明人： Josef Nickl , Berthold Narr , Erich Muller , Josef Roch , Walter Haarmann
IPC分类号： C07D295/18 , A61K31/16 , A61K31/165 , A61K31/19 , A61K31/215 , A61K31/22 , A61K31/445 , A61K31/535 , A61K31/5375 , A61P7/02 , C07C67/00 , C07C313/00 , C07C315/02 , C07C317/44 , C07C323/52 , C07C323/60 , C07C323/65 , C07D295/185 , C07C149/40 , C07C147/107
CPC分类号： C07D295/185 , C07C317/44 , C07C323/52 , C07C323/60
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or halogen,R.sub.2 is hydroxyl, alkoxy of 1 to 6 carbon atoms, aralkoxy of 7 to 10 carbon atoms, amino, (alkyl of 1 to 3 carbon atoms)-amino, piperidino or morpholino, andn is 0, 1 or 2,Diastereoisomers thereof and, when R.sub.2 is hydroxyl, non-toxic, pharmacologically acceptable salts thereof formed with an inorganic or organic base; the compounds, their diastereoisomers and the salts are useful as antithrombotics, anti-hypercholesteremics and anti-hyperglyceridemics.
摘要翻译：式的化合物，其中R 1是氢或卤素，R 2是羟基，1至6个碳原子的烷氧基，7至10个碳原子的芳烷氧基，氨基，（1至3个碳原子的烷基） - 氨基，哌啶子基或吗啉代和N是0,1或2，其二异构体，以及当R2是羟基时，与无机或有机碱形成的无毒的，药理上可接受的盐; 化合物，它们的非对映异构体和盐可用作抗血栓形成剂，抗高胆固醇血症和抗高甘油三酯药物。

4. 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。

5. 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。

6. 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。

7. 发明授权

US4728646A 2-(perhydro-1,4-diazino)-pyrimido[5,4-d]-pyrimidines and salts thereof 失效
标题翻译： 2-（全氢-1,4-二氮杂） - 嘧啶并[5,4-d] - 嘧啶及其盐
公开(公告)号：US4728646A
公开(公告)日：1988-03-01
申请号：US7990
申请日：1987-01-28
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

US4518597A Substituted benzoxazin-2-ones and pharmaceutical compositions containing them 失效
标题翻译：取代的苯并恶嗪-2-酮和含有它们的药物组合物
公开(公告)号：US4518597A
公开(公告)日：1985-05-21
申请号：US617797
申请日：1984-06-06
申请人： Berthold Narr , Josef Nickl , Erich Muller , Josef Roch , Walter Haarmann , Johannes-Maximilian Weisenberger
发明人： Berthold Narr , Josef Nickl , Erich Muller , Josef Roch , Walter Haarmann , Johannes-Maximilian Weisenberger
IPC分类号： A61K31/535 , A61K31/536 , A61P7/02 , C07D265/18 , C07D413/12 , C07D417/12
CPC分类号： C07D265/18 , C07D413/12 , C07D417/12
摘要： This invention is directed to novel benzoxazin-2-ones of the formula ##STR1## wherein A is a sulfur atom or an SO, SO.sub.2, R--N.dbd.S, or R--N.dbd.SO.sub.2 group where R is a hydrogen atom or an acyl group;D is an alkylene group;R.sub.1 is an alkyl, phenylalkyl, cycloalkyl, or phenyl group;R.sub.4 is a hydrogen atom or an alkyl group;R.sub.5 is a hydrogen or halogen atom or a nitro or alkyl group; andR.sub.6 is a hydrogen or halogen atom or an alkyl group,having valuable pharmacological properties, particularly an antithrombotic activity. The compounds of Formula I may be prepared by the methods used for analogous compounds.
摘要翻译：本发明涉及新颖的式（I）的苯并恶嗪-2-酮，其中A为硫原子或SO，SO 2，RN = S或RN = SO 2基团，其中R为氢原子或酰基组; D是亚烷基; R1是烷基，苯基烷基，环烷基或苯基; R4是氢原子或烷基; R5是氢或卤素原子或硝基或烷基; R6是具有有价值的药理学特性的氢或卤原子或烷基，特别是抗血栓形成活性。式I的化合物可以通过用于类似化合物的方法制备。

9. 发明授权

US4478833A Trisubstituted pyrimido[5,4-d]pyrimidines and salts thereof 失效
标题翻译：三取代嘧啶并[5,4-d]嘧啶及其盐
公开(公告)号：US4478833A
公开(公告)日：1984-10-23
申请号：US331285
申请日：1981-12-16
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： A61K31/535 , A61K31/54 , A61P7/02 , C07D487/04 , C07D401/14 , A61K31/505 , C07D417/14
CPC分类号： C07D487/04
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is optionally substituted alkyl;R.sub.2 is hydrogen or optionally substituted alkyl; orR.sub.1 and R.sub.2, together with each other and the nitrogen atom to which they are attached, form an optionally substituted cyclic imino group;R.sub.3 is an optionally substituted cyclic imino group; andR.sub.4 is substituted hydroxyl, mercapto or amino;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为任选取代的烷基; R2是氢或任选取代的烷基; 或R 1和R 2彼此连接并与它们相连的氮原子形成任选取代的环状亚氨基; R3是任选取代的环状亚氨基; R4为取代羟基，巯基或氨基; 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。

10. 发明授权

US4224322A 3-Amino-4-phenyl-6-thiomorpholino-1H-pyrazolo-[3,4-b]pyridines and salts thereof 失效
标题翻译： 3-氨基-4-苯基-6-硫代吗啉代-1H-吡唑并[3,4-b]吡啶及其盐
公开(公告)号：US4224322A
公开(公告)日：1980-09-23
申请号：US75493
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 , A61K31/54
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 thiomorpholino, 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硫代吗啉代，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。

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