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21. 发明授权

US4725617A Alkylamino-furanon-derivatives 失效
标题翻译：烷基氨基 - 呋喃酮衍生物
公开(公告)号：US4725617A
公开(公告)日：1988-02-16
申请号：US828011
申请日：1986-02-10
申请人： Tamas Fodor , Laszlo Dobay , Janos Fischer , Bela Stefko , Bela Kiss , Zsolt Szombathelyi , Egon Karpati , Istvan Laszlovszky , Laszlo Szporny
发明人： Tamas Fodor , Laszlo Dobay , Janos Fischer , Bela Stefko , Bela Kiss , Zsolt Szombathelyi , Egon Karpati , Istvan Laszlovszky , Laszlo Szporny
IPC分类号： C07K14/81 , A61K38/00 , A61P9/12 , A61P27/02 , A61P27/06 , C07K1/113 , C07K5/02 , C07K5/06 , A61K31/395 , C07D207/09
CPC分类号： C07K5/0222 , A61K38/00 , Y02P20/55
摘要： The present invention relates to a compound of the formula (I) ##STR1## wherein R.sup.1 stands for methyl or a group of the formula R.sup.3 --NH--(CH.sub.2).sub.4 --wherein R.sup.3 is hydrogen or a protective group being compatible with the peptide bond,R.sup.2 represents hydrogen, a protective group being compatible with the peptide bond or a cation derived from an organic or inorganic basethe pharmaceutically acceptable salts and diastereomers thereof.The compounds of the invention are useful for inhibiting the effect of the angiotensin converting ensime and they can be used in the therapy as blood pressure reducing agents and for the treatment of cardiac failure and glaucoma.
摘要翻译：本发明涉及式（I）化合物（I）其中R1代表甲基或式R3-NH-（CH2）4-基团，其中R3是氢或保护基与肽键，R2表示氢，与肽键相容的保护基或衍生自有机或无机碱的阳离子，其药学上可接受的盐和非对映异构体。本发明的化合物可用于抑制血管紧张素转化酶的作用，可用于作为降血压剂的治疗和用于治疗心脏衰竭和青光眼。

22. 发明授权

US4209442A Angiotensin II analogs and process for the preparation thereof 失效
标题翻译：血管紧张素II类似物及其制备方法
公开(公告)号：US4209442A
公开(公告)日：1980-06-24
申请号：US923663
申请日：1978-07-11
申请人： Lajos Kisfaludy , Gyorgyne Nyeki nee Olga Kuprina , Laszlone Szirmai nee Maria Sarkozi , Egon Karpati , Katalin Gidai , Laszlo Szporny
发明人： Lajos Kisfaludy , Gyorgyne Nyeki nee Olga Kuprina , Laszlone Szirmai nee Maria Sarkozi , Egon Karpati , Katalin Gidai , Laszlo Szporny
IPC分类号： A61K38/00 , A61K38/22 , A61P9/12 , A61P43/00 , B02C13/22 , B02C21/00 , C07K1/113 , C07K7/14 , C07C103/52 , A61K37/00
CPC分类号： C07K7/14 , A61K38/00
摘要： Novel Angiotensin II peptides of the formula:X-Arg-Val-Tyr-Ile-His-Pio-Ywhere X is hydroxyacetyl or .alpha.-hydroxypropyl and Y is leucyl, isoleucyl, alanyl or threonyl or an acid addition salt or a complex thereof are disclosed and a process for the preparation thereof are disclosed having the ability to lower renal hypertension.
摘要翻译：新型的式：X-Arg-Val-Tyr-Ile-His-Pio-Y的血管紧张素II肽，其中X是羟乙酰或α-羟丙基，Y是亮氨酰，异亮氨酰，丙氨酰或苏氨酰或其酸加成盐或其复合物并且公开了其制备方法，其具有降低肾性高血压的能力。

23. 发明授权

US4196206A Pyridyl-piperazine derivative with anti-arrythmic effect 失效
标题翻译：具有抗arrythmic效应的吡啶基 - 哌嗪衍生物
公开(公告)号：US4196206A
公开(公告)日：1980-04-01
申请号：US880364
申请日：1978-02-23
申请人： Arpad Molnar , Karoly Felfoldi , Mihaly Bartok , Egon Karpati , Laszlo Szporny
发明人： Arpad Molnar , Karoly Felfoldi , Mihaly Bartok , Egon Karpati , Laszlo Szporny
IPC分类号： C07D401/04 , A61K31/44 , A61K31/4402 , A61K31/496 , A61P9/06 , C07D213/74 , C07D295/08 , A61K31/495
CPC分类号： C07D213/74 , Y10S514/821
摘要： 3-[4-(2'-Pyridyl)-piperazin-1-yl]-1-(3,4,5-trimethoxybenzoyloxy)-propane or a pharmaceutically acceptable acid-addition salt thereof in a composition with anti-arrhythmic activity.
摘要翻译： 3- [4-（2'-吡啶基） - 哌嗪-1-基] -1-（3,4,5-三甲氧基苯甲酰氧基） - 丙烷或其药学上可接受的酸加成盐在具有抗心律不齐活性的组合物中。

24. 发明授权

US4179433A Angiotensin II antagonist peptides containing an alpha-aminooxyacid in the position-1 失效
标题翻译：血管紧张素II拮抗剂肽在第1位含有α-氨氧基酸
公开(公告)号：US4179433A
公开(公告)日：1979-12-18
申请号：US923681
申请日：1978-07-11
申请人： Lajos Kisfaludy , Olga Nyeki nee Kuprina , Maria Skirmai nee Sarkozi , Egon Karpati , Katalin Gidai , Laszlo Szporny
发明人： Lajos Kisfaludy , Olga Nyeki nee Kuprina , Maria Skirmai nee Sarkozi , Egon Karpati , Katalin Gidai , Laszlo Szporny
IPC分类号： C07K7/06 , A61K38/00 , A61K38/08 , A61P43/00 , C07C231/00 , C07K7/14 , C07C103/52 , A61K37/00
CPC分类号： C07K7/14 , A61K38/00
摘要： Angiotensin II analog of the formula IX-Arg-Val-Tyr-Ile-His-Pro-Y (I)whereinX is a radical derived from an aliphatic .alpha.-aminooxy-carboxylic acid andY is a radical derived from an aliphatic .alpha.-amino-carboxylic acid,and acid addition salts and complexes thereof with antagonistic properties useful in the diagnosis and treatment of hypertensions depending on renin.
摘要翻译：式I X-Arg-Val-Tyr-Ile-His-Pro-Y（I）的血管紧张素II类似物，其中X是衍生自脂族α-氨基氧基羧酸的基团，Y是衍生自脂族α - 氨基 - 羧酸及其具有拮抗性质的酸加成盐和复合物，其用于诊断和治疗依赖于肾素的高血压。

25. 发明授权

US4101545A Diamino-androstanes and a process for the preparation of the said compounds 失效
标题翻译：二氨基 - 雄甾烷二醇及其制备方法
公开(公告)号：US4101545A
公开(公告)日：1978-07-18
申请号：US709325
申请日：1976-07-28
申请人： Zoltan Tuba , Maria Marsai , Katalin Biro , Laszlo Szporny , Egon Karpati , Szaboles Szeberenyi
发明人： Zoltan Tuba , Maria Marsai , Katalin Biro , Laszlo Szporny , Egon Karpati , Szaboles Szeberenyi
IPC分类号： C07J1/00 , A61K31/14 , A61K31/58 , A61P21/02 , C07J13/00 , C07J41/00 , C07J43/00 , C07J71/00
CPC分类号： C07J41/0005 , C07J13/005 , C07J43/003 , C07J71/001
摘要： Curare-type salts of the formula ##STR1## WHEREIN Ac is an alkyl carbonyl group containing 1 to 4 carbon atoms in the alkyl moiety and one ofR.sub.1 and R.sub.2, is a methylene group and the other is a group of the formula >N-R.sub.2 wherein R.sub.2 is an alkyl group containing 1 to 3 carbon atoms,A is halogen andR.sub.3 is an alkyl group containing 1 to 4 carbon atoms, or an alkyl group; andA process for the preparation thereof are disclosed.
摘要翻译：式（1a）或（ⅠB）的式（Ⅰ）化合物的盐是在烷基部分和R1和R2之一中含有1至4个碳原子的烷基羰基是亚甲基，另一种是式> N-R 2的基团，其中R 2是含有1至3个碳原子的烷基，A是卤素，R 3是含有1至4个碳原子的烷基或烷基; 及其制备方法被披露。

26. 发明授权

US4052404A Indolo (2,3-.alpha.)quinolizines 失效
标题翻译：吲哚（2,3'）喹啉
公开(公告)号：US4052404A
公开(公告)日：1977-10-04
申请号：US635092
申请日：1975-11-25
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
IPC分类号： C07D459/00 , A61K31/404 , A61K31/435 , A61K31/4375 , A61P9/08 , C07D471/02 , C07D471/14 , C07D455/02
CPC分类号： C07D471/14 , Y10S514/929
摘要： The invention relates to new indolo-quinolizidine derivatives of the general formula (I) or salts or optically active isomers thereof, ##STR1## wherein R stands for an alkyl group, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME, AS WELL AS TO A PROCESS FOR THE PREPARATION THEREOF.The new compounds according to the invention possess vasodilatating and hypotensive effects and can be used in the therapy as medicines. The new compounds according to the invention are completely devoid of harmful side-effects.

27. 发明授权

US5340823A Organosilane derivatives, pharmaceutical compositions containing them and process for preparing same 失效
标题翻译：有机硅烷衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：US5340823A
公开(公告)日：1994-08-23
申请号：US993139
申请日：1992-12-18
申请人： Sandor Farkas , Sandor Foldeak , Egon Karpati , Peter Hegyes , Janos Kreidl , Laszlo Szporny , Laszlo Czibula , Szilvia Petofi-Vass
发明人： Sandor Farkas , Sandor Foldeak , Egon Karpati , Peter Hegyes , Janos Kreidl , Laszlo Szporny , Laszlo Czibula , Szilvia Petofi-Vass
IPC分类号： A61K31/695 , C07F7/08 , C07F7/10 , A61K31/445 , C07D7/10
CPC分类号： C07F7/0812 , C07F7/0818
摘要： A method of treating a mammalian subject for Parkinson's disease or to provide a central muscle relaxant effect, which comprises the step of administering to the mammalian subject in need of the treatment, a therapeutically effective amount of a compound of the Formula (I) ##STR1## wherein m is 1,2 or 3;R.sub.1 and R.sub.2 each independently stand for hydrogen, C.sub.1 to C.sub.4 straight or branched chain alkyl, C.sub.1 to C.sub.4 alkoxy, C.sub.5 to C.sub.7 cycloalkyl, or halogen; andB is a 5- or 6-membered saturated or unsaturated heterocyclic group containing a nitrogen heteroatom, the heterocyclic group being bound through its heterocyclic nitrogen atom to the remainder of the compound, and which can contain one or two additional heteroatoms selected from the group consisting of an oxygen heteroatom, a sulfur heteroatom, and one or two additional nitrogen heteroatoms, which may be as an .dbd.N--, --NH-- or --NR-- group, where R is a C.sub.1 to C.sub.5 alkyl or C.sub.1 to C.sub.5 alkycarbonyl group, the nitrogen-containing heterocyclic group is unsubstituted or substituted on one of its carbon atoms by C.sub.1 to C.sub.4 alkyl or C.sub.1 to C.sub.4 alkoxycarbonyl; or a pharmaceutically acceptable salt thereof.
摘要翻译：一种治疗哺乳动物受试者帕金森病或提供中枢肌肉松弛作用的方法，其包括向需要治疗的哺乳动物受试者施用治疗有效量的式（I）化合物的步骤（I）其中m是1,2或3; R1和R2各自独立代表氢，C1至C4直链或支链烷基，C1至C4烷氧基，C5至C7环烷基或卤素; 并且B是含有氮杂原子的5或6元饱和或不饱和杂环基，杂环基通过其杂环氮原子与化合物的其余部分结合，并且其可以含有一个或两个另外的杂原子，由氧杂原子，硫杂原子和一个或两个另外的氮杂原子组成，其可以是= N，-NH-或-NR-基，其中R是C1-C5烷基或C1-C5烷羰基，所述含氮杂环基是未取代的或在其碳原子之一被C1-C4烷基或C1-C4烷氧基羰基取代; 或其药学上可接受的盐。

28. 发明授权

US4806545A (-)-1.beta.-ethyl-1.alpha.-hydroxymethyl-1,2,3,4,6,7,12, 12B.alpha.-octahydroindolo(2,3-A)quinolizine, process for its preparation and pharmaceutical compositions containing same 失效
标题翻译：（ - ） - 1β-乙基-1α-羟甲基-1,2,3,4,6,7,12,12aαα-八氢吲哚（2,3-A）喹嗪，其制备方法和含有它们的药物组合物
公开(公告)号：US4806545A
公开(公告)日：1989-02-21
申请号：US851327
申请日：1986-04-14
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Zsolt Szombathelyi , Egon Karpati , Bela Kiss , Katalin Csomor , Istvan Laszlovszky , Erzsebet Lapis , Laszlo Szporny , Lilla Forgacs , Csaba Kuthi , Aniko Gere
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Zsolt Szombathelyi , Egon Karpati , Bela Kiss , Katalin Csomor , Istvan Laszlovszky , Erzsebet Lapis , Laszlo Szporny , Lilla Forgacs , Csaba Kuthi , Aniko Gere
IPC分类号： A61K31/435 , A61P9/00 , A61P9/08 , C07D471/14 , C07D455/00
CPC分类号： C07D471/14
摘要： The invention relates to the new (-)-1.beta.-ethyl-1.alpha.-hydroxymethyl-1,2, 3,4,6,7,12,12b.alpha.-octa-hydroindolo[2,3-a] quinolizine of the formula (I) ##STR1## and acid addition salts thereof. According to another aspect of the invention there is provided a process for the preparation of the compound of formula (I) and acid addition salts thereof by resolution of the corresponding racemic compound and optionally by subsequent hydrolysis and/or salt formation.The compound of formula (I) shows a remarkable peripheral vasodilating and antihypoxial activity. Pharmaceutical compositions comprising it as active ingredient are also within the scope of the invention.
摘要翻译：本发明涉及新的（ - ） - 1β-乙基-1α-羟基甲基-1,2,3,4,6,7,12,12bα-正 - 氢吲哚并[2,3-a]喹嗪式（I）化合物（I）及其酸加成盐。根据本发明的另一方面，提供了通过拆分相应的外消旋化合物和任选地随后的水解和/或盐形成来制备式（I）化合物及其酸加成盐的方法。式（I）化合物显示出显着的外周血管扩张和抗低氧活性。包含其作为活性成分的药物组合物也在本发明的范围内。

29. 发明授权

US4769373A Anti-arrhythmic azabicyclic compounds 失效
标题翻译：抗心律不齐的氮杂双环化合物
公开(公告)号：US4769373A
公开(公告)日：1988-09-06
申请号：US674773
申请日：1984-11-26
申请人： Karoly Nador , Gabor Kraiss , Margit Paroczay , Egon Karpati , Laszlo Szporny
发明人： Karoly Nador , Gabor Kraiss , Margit Paroczay , Egon Karpati , Laszlo Szporny
IPC分类号： A61K31/435 , A61P9/06 , A61P25/02 , C07D211/72 , C07D221/22 , C07D405/12 , C07D409/12 , A61K31/44
CPC分类号： C07D221/22 , C07D211/72 , C07D405/12 , C07D409/12
摘要： The invention relates to new anti-arrythmic azabicyclo[3.3.1]nonanes of the general formula (I) ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are C.sub.1-4 alkyl groups which are the same or different, or one of them is a benzyl group and the others are C.sub.1-4 alkyl groups, andR.sup.4 is a hydroxy group, or an etherified hydroxy group of the formula --OR.sup.5, or an esterified hydroxy group of the formula --OOCR.sup.6, in which the esterifying groupR.sup.5 is a phenyl or benzyl group which optionally each can have a trihalomethyl substituent or one or more halogen or C.sub.1-4 substituents, or is a diphenyl or benzhydryl group, and the esterifying groupR.sup.6 is a C.sub.1-8 alkyl or a C.sub.3-6 cycloalkyl group, or a phenyl or benzyl group which optionally each can have a halo-substituent or one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy, nitro or phenyl substituents, or is an optionally halogenated or hydrogenated naphthyl group, or a cinnamyl group optionally substituted by a halogen atom or C.sub.1-4 alkoxy groups, or is a benzhydryl or 1,1-diphenyl-hydroxymethyl group, or is a heterocyclic substituent selected from the group consisting of thenyl, 9-xanthenyl or 3-indolyl-(C.sub.1-3 alkyl) groups,as well as the stereoisomers and pharmaceutically acceptable acid addition salts thereof.The invention also provides a process for the preparation of the new compounds of the general formula (I), in which new intermediates of the general formula (IV), ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, are utilized.
摘要翻译：本发明涉及通式（I）的新的抗焦虑氮杂二氮杂双环[3.3.1]壬烷，其中R1，R2和R3是相同或不同的C1-4烷基，或其中之一它们是苄基，其它是C 1-4烷基，R4是羟基，或式-OR5的醚化羟基或式-OOCR6的酯化羟基，其中酯化基团R5 是任选地可以具有三卤代甲基取代基或一个或多个卤素或C 1-4取代基的苯基或苄基，或者是二苯基或二苯甲基，酯化基团R6是C 1-8烷基或C 3-6环烷基基团或苯基或苄基，其任选地各自可以具有卤素取代基或一个或多个C 1-4烷基，C 1-4烷氧基，硝基或苯基取代基，或者是任选卤代或氢化的萘基或肉桂基任选被卤素原子或C 1-4烷氧基取代，或者是二苯甲基或1,1-二苯基 - 氢或者是选自草酰基，9-呫吨基或3-吲哚基 - （C 1-3烷基）基团的杂环取代基，以及它们的立体异构体和药学上可接受的酸加成盐。本发明还提供了制备通式（I）的新化合物的方法，其中通式（IV）的新中间体，其中R 1，R 2和R 3如上所定义，被利用。

30. 发明授权

US4428877A Cis-10-bromo-E-homoeburnanes 失效
标题翻译：顺式-10-溴-E-高乙炔二醇
公开(公告)号：US4428877A
公开(公告)日：1984-01-31
申请号：US234577
申请日：1981-02-13
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Lajos Dancsi , Tibor Keve , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Lajos Dancsi , Tibor Keve , Egon Karpati , Laszlo Szporny
IPC分类号： C07D209/16 , C07D209/42 , C07D461/00 , C07D471/14 , C07D471/22 , C07D459/00
CPC分类号： C07D471/14 , C07D209/16 , C07D209/42 , C07D461/00
摘要： A novel process for preparing 10-bromo-vincaminic acid esters and homologous compounds of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each stand for a C.sub.1-6 alkyl group is disclosed.All the intermediate products are new and exhibit valuable therapeutical effect on the blood circulation.
摘要翻译：公开了一种制备10-溴 - 长春胺酸酯和通式为“IMAGE”的同系化合物的新方法，其中R1和R2各自代表C1-6烷基。所有的中间产品都是新的，对血液循环具有宝贵的治疗作用。

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