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1. 发明授权

US4714698A 8-alkylthio-2-piperazino-pyrimido[5,4-d]-pyrimidines 失效
标题翻译： 8-烷硫基-2-哌嗪基 - 嘧啶并[5,4-d] - 嘧啶
公开(公告)号：US4714698A
公开(公告)日：1987-12-22
申请号：US745095
申请日：1985-06-17
申请人： Josef Roch , Armin Heckel , Josef Nickl , Erich Muller , Berthold Narr , Rainer Zimmermann , Johannes Weisenberger
发明人： Josef Roch , Armin Heckel , Josef Nickl , Erich Muller , Berthold Narr , Rainer Zimmermann , Johannes Weisenberger
IPC分类号： A61K31/505 , A61K31/55 , A61P7/02 , A61P9/10 , A61P35/00 , C07D487/04 , C07D471/04
CPC分类号： C07D487/04
摘要： The invention relates to new compounds of general formula ##STR1## wherein R.sub.1 represents an alkyl group,R.sub.2 represents a hydrogen atom, an alkyl group optionally substituted (except at the .alpha. carbon atom) by a hydroxy group, or represents a cycloalkyl group or an allyl, phenyl or benzyl group,R.sub.3 represents an allyl group, an alkyl group optionally substituted (except at the .alpha. carbon atom) by a hydroxy group, or represents a cycloalkyl group orR.sub.2 and R.sub.3 together with the nitrogen atom between them represent a straight-chained alkyleneimino group,the acid addition salts thereof, particularly the acid addition salts thereof with physiologically acceptable inorganic or organic acids which have valuable pharmacological properties, particularly a metastasis-inhibiting effect based on their selective tumour-PDE inhibiting effect, and pharmaceutical compositions containing these compounds or the physiologically acceptable acid addition salts thereof.The new compounds may be prepared according to methods known for analogous compounds.
摘要翻译：本发明涉及通式（I）的新化合物，其中R 1表示烷基，R 2表示氢原子，任选被羟基取代的烷基（除了在α碳原子上），或表示环烷基基团或烯丙基，苯基或苄基，R 3表示烯丙基，任选被羟基取代的烷基（除了在α碳原子上），或表示环烷基或R 2和R 3以及它们之间的氮原子代表直链亚烷基亚氨基，其酸加成盐，特别是其酸加成盐与具有有价值的药理学性质的生理上可接受的无机或有机酸，特别是基于其选择性肿瘤-PDE抑制作用的转移抑制作用，以及含有这些化合物的药物组合物或其生理上可接受的酸加成盐。新化合物可以根据类似化合物已知的方法制备。

2. 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。

3. 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.

4. 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。

5. 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.

6. 发明授权

US4870076A Sulphonamidoethyl compounds, pharmaceutical compositions comprising these compounds and processes for preparing them 失效
标题翻译：磺酰氨基乙基化合物，包含这些化合物的药物组合物及其制备方法
公开(公告)号：US4870076A
公开(公告)日：1989-09-26
申请号：US92742
申请日：1987-09-03
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 sulphonamido-ethyl compounds having the following structure: ##STR1## wherein R.sub.1 is substituted or unsubstituted phenyl, benzyl, nitrophenyl, acetamidophenyl or thienyl, R.sub.2 is hydroxycarbonyl or alkoxycarbonyl bonded via alkylene or alkenylene, or a 4,5-dihydro-pyridazin-3-one-6-yl or pyridazin-3-on-6-yl group optionally substituted on a ring carbon by C.sub.1 -C.sub.3 alkyl and X is substituted or unsubstituted imino, oxygen or sulphur, which compounds may be used to prevent arteriosclerosis or tumor metastasis, and are antitrombotic and thromboxane antagonists.
摘要翻译：本发明涉及具有以下结构的新型磺酰氨基乙基化合物：其中R1是取代或未取代的苯基，苄基，硝基苯基，乙酰氨基苯基或噻吩基，R2是通过亚烷基或亚烯基键合的羟基羰基或烷氧基羰基，二环哒嗪-3-酮-6-基或哒嗪-3-基-6-基，任选在环碳上被C 1 -C 3烷基取代，X是取代或未取代的亚氨基，氧或硫，可以使用该化合物以防止动脉硬化或肿瘤转移，并且是抗血栓形成和血栓素拮抗剂。

7. 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。

8. 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。

9. 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。

10. 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。

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