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21. 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。

22. 发明授权

US5118687A 1-oxa-2-oxo-8-azaspiro(4,5)decane derivatives, pharmaceutical compositions containing them and process for preparing same 失效
标题翻译： 1-OXA-2-OXO-8-AZASPIRO（4,5）十二烷衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：US5118687A
公开(公告)日：1992-06-02
申请号：US566275
申请日：1990-08-10
申请人： Edit Toth , Jozsef Torley , Laszlo Szporny , Bela Kiss , Egon Karpati , Eva Palosi , Dora Groo , Istvan Laszlovszky , Zsolt Szombathelyi , Adam Sarkadi , Aniko Gere , Katalin Csomor , Mihaly Bodo , Judit Laszy , Zsolt Szentirmay
发明人： Edit Toth , Jozsef Torley , Laszlo Szporny , Bela Kiss , Egon Karpati , Eva Palosi , Dora Groo , Istvan Laszlovszky , Zsolt Szombathelyi , Adam Sarkadi , Aniko Gere , Katalin Csomor , Mihaly Bodo , Judit Laszy , Zsolt Szentirmay
IPC分类号： A61K31/33 , A61K31/335 , A61K31/42 , A61K31/435 , A61K31/445 , A61P3/00 , A61P9/00 , A61P9/10 , A61P25/28 , C07D221/00 , C07D263/00 , C07D317/00 , C07D491/10 , C07D491/107 , C07D491/113 , C07D493/10 , C07D498/10
CPC分类号： C07D491/10
摘要： The invention relates to novel compounds 1-oxa-2-oxo-8- of the formula (I), ##STR1## wherein X means oxygen or an >NR group, whereinR stands for hydrogen, a C.sub.1-12 alkyl, C.sub.3-6 cycloalkyl, carbocyclic C.sub.6-10 aryl or carbocyclic C.sub.6-10 aryl-C.sub.10-4 alkyl group, the latter two groups are optionally substituted on their aromatic moiety by one or more, same or different halogen(s), one or more C.sub.1-4 alkyl or C.sub.1-4 alkoxy group(s);R.sup.1 and R.sup.2 together represent a methylene group or, when X stands for an >NR group, wherein R is as defined above, one of R.sup.1 and R.sup.2 may represent a hydroxyl group whereas the other is a methyl group;R.sup.3 stands for hydrogen or a phenyl group optionally substituted by one or more halogen(s), one or more C.sub.1-4 alkyl or C.sub.1-4 alkoxy or hydroxyl group(s);R.sup.4 means hydrogen, one or more halogen(s), C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxyl or trihalomethyl group(s); andn is 1, 2 or 3as well as their acid addition and quaternary ammonium salts.

23. 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。

24. 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。

25. 发明授权

US4481204A E-Homo-eburnane derivatives, process for their preparation, and pharmaceutical compositions containing these compounds 失效
标题翻译： E-Homo-eburnane衍生物，其制备方法和含有这些化合物的药物组合物
公开(公告)号：US4481204A
公开(公告)日：1984-11-06
申请号：US509150
申请日：1983-06-29
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Sapi , Eva Palosi , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Sapi , Eva Palosi , Egon Karpati , Laszlo Szporny
IPC分类号： C07D471/22 , A61K31/395 , C07D459/00 , C07D461/00
CPC分类号： C07D471/22
摘要： The invention relates to racemic or optically active E-homo-eburnane derivatives of the formula /I/, ##STR1## wherein R.sup.1 and R.sup.2 independently represent an alkyl group having 1 to 6 carbon atoms,and acid addition salts thereof.The new compounds are pharmaceutically active, for example their certain representatives, in particular from the cis-series, show antidepressive activity, while others, especially the compounds of the trans-series, are potent anthypoxial agents. The compounds of the formula /I/ and pharmaceutically acceptable acid addition salts thereof can therefore be employed as active ingredients of pharmaceutical compositions.
摘要翻译：本发明涉及式/ I /，其中R 1和R 2独立地表示具有1至6个碳原子的烷基的式/ I /，/ IMAGE / I / C的外消旋或光学活性的E-均 - burn烷衍生物及其酸加成盐。新化合物是药学上活性的，例如它们的特定代表，特别是顺式的化合物显示出抗抑郁活性，而其它代表，特别是反式系列的化合物是有效的抗氧化剂。因此，式/ I /的化合物及其药学上可接受的酸加成盐可用作药物组合物的活性成分。

26. 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。

27. 发明授权

US4199598A Method of treating noradrenaline dysfunction or for dopamine-.beta.-hydroxylase inhibition 失效
标题翻译：治疗去甲肾上腺素功能障碍或多巴胺-β-羟化酶抑制的方法
公开(公告)号：US4199598A
公开(公告)日：1980-04-22
申请号：US29475
申请日：1979-04-12
申请人： Gyorgy Matolcsy , Piroska Bartok nee Berencsy , Bela Kiss , Eva Palosi , Egon Karpati , Laszlo Szporny
发明人： Gyorgy Matolcsy , Piroska Bartok nee Berencsy , Bela Kiss , Eva Palosi , Egon Karpati , Laszlo Szporny
IPC分类号： A61K31/185
CPC分类号： A61K31/185
摘要： A method of treating mammalian noradrenaline malfunctions or dysfunction or effecting dopamine-.beta.-hydroxylase inhibition comprises administering an effective dose of an acid derivative of the formula (I), ##STR1## wherein R is C.sub.2-4 alkenyl, C.sub.3-8 cycloalkyl, benzyl or C.sub.1-6 alkyl which has a C.sub.1-4 alkoxy or a hydroxy substituent, or C.sub.2-6 alkyl with a carboxy and/or amino substituent, or C.sub.5 - or C.sub.6 -unsubtituted alkyl.
摘要翻译：治疗哺乳动物去甲肾上腺素功能障碍或功能障碍或影响多巴胺-β-羟化酶抑制的方法包括施用有效剂量的式（I）的酸衍生物，其中R是C 2-4链烯基，C 3-8 环烷基，苄基或具有C1-4烷氧基或羟基取代基的C1-6烷基，或具有羧基和/或氨基取代基的C2-6烷基或C5-或C6-未取代的烷基。

28. 发明授权

US4184040A Hydroxymethyl-pyridine esters and a process for the preparation thereof 失效
标题翻译：羟甲基 - 吡啶酯及其制备方法
公开(公告)号：US4184040A
公开(公告)日：1980-01-15
申请号：US839605
申请日：1977-10-05
申请人： Ferenc Noteisz , Mihaly Bartok , Karoly Felfoldi , Egon Karpati , Laszlo Szporny
发明人： Ferenc Noteisz , Mihaly Bartok , Karoly Felfoldi , Egon Karpati , Laszlo Szporny
IPC分类号： C07D213/16 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/443 , A61P9/06 , C07D213/30 , C07D405/12 , C07D213/55
CPC分类号： C07D213/30
摘要： New hydroxymethyl-pyridine esters of the formula (I) ##STR1## wherein R represents a 9-xanthenyl group or a phenyl group substituted by a halogen atom or a trifluoromethyl group or by an alkyl or alkoxy group, either having 1 to 4 carbon atoms, and pharmaceutically acceptable acid addition salts and quaternary salts thereof are prepared by acylating the corresponding hydroxymethyl pyridines with a carboxylic acid of the formula R--COOH, or with a reactive derivative thereof, and, if desired, converting the obtained product of the formula I into a pharmaceutically acceptable acid addition salt or quaternary salt thereof. The new compounds exert beneficial effects on functional disorders of the heart.
摘要翻译：式（I）的新羟甲基 - 吡啶酯其中R表示9-呫吨基或被卤素原子或三氟甲基取代的苯基或被烷基或烷氧基取代的苯基，其具有1至 4个碳原子及其药学上可接受的酸加成盐和季盐通过用式R-COOH的羧酸或其反应性衍生物酰化相应的羟甲基吡啶来制备，如果需要，将所得产物式I化合成其药学上可接受的酸加成盐或其季盐。新化合物对心脏功能障碍有益。

29. 发明授权

US4120858A 14-Substituted vincanes 失效
标题翻译： 14取代的维根素
公开(公告)号：US4120858A
公开(公告)日：1978-10-17
申请号：US719066
申请日：1976-08-30
申请人： Otto Clauder , Jozsef Kokosi , Laszlo Szporny , Egon Karpati
发明人： Otto Clauder , Jozsef Kokosi , Laszlo Szporny , Egon Karpati
IPC分类号： A61K31/435 , A61P9/08 , A61P9/12 , A61P25/02 , A61P43/00 , C07D461/00 , C07D519/04
CPC分类号： C07D461/00 , Y10S514/824
摘要： A compound of the formula (I) ##STR1## wherein X stands for a hydrogen atom, an optionally substituted aliphatic or aromatic sulfonyloxy group, a thiocyanato group, an azido group or an amino group optionally mono- or disubstituted by aliphatic, cycloaliphatic, aromatic or araliphatic hydrocarbon groups, acyl, alkyloxycarbonyl, cycloalkyloxycarbonyl, aryloxycarbonyl, aralkyloxycarbonyl, aminocarboimido groups or the substituents of the said amino group may form with the nitrogen atom thereof a five-, six- or seven-membered saturated or unsaturated heterocyclic ring optionally containing a further nitrogen, oxygen or sulfur hetero atom, and a quaternary salt or acid addition salt thereof. The compounds are useful in the treatment of arteriosclerosis and high blood pressure.
摘要翻译：式（I）的化合物其中X代表氢原子，任选取代的脂族或芳族磺酰氧基，硫氰酸酯基，叠氮基或氨基，任选被脂族，脂环族，芳族或芳脂族烃基，酰基，烷氧基羰基，环烷氧基羰基，芳氧基羰基，芳烷氧基羰基，氨基羧基亚氨基或所述氨基的取代基可以与其氮原子一起形成五元，六元或七元饱和或不饱和杂环，任选地含有进一步的氮，氧或硫杂原子，及其季盐或酸加成盐。该化合物可用于治疗动脉硬化和高血压。

30. 发明授权

US4044146A Xanthene-9-carboxylates 失效
标题翻译：呫吨-9-羧酸盐
公开(公告)号：US4044146A
公开(公告)日：1977-08-23
申请号：US761402
申请日：1977-01-21
申请人： Egon Karpati , Laszlo Szporny , Mihaly Bartok , Jozsef Czombos , Karoly Felfoldi , Marta Laszlavik , Ferenc Notheisz
发明人： Egon Karpati , Laszlo Szporny , Mihaly Bartok , Jozsef Czombos , Karoly Felfoldi , Marta Laszlavik , Ferenc Notheisz
IPC分类号： C07D295/13 , C07D311/84
CPC分类号： C07D295/13 , C07D311/84
摘要： The invention relates to xanthene-9-carboxylates of the formula ##STR1## wherein R.sub.1 and R.sub.3 may be the same or different and represent a lower alkyl group,n and m each are integers of 2 to 5, or pharmaceutically-effective salts thereof. The compounds according to the invention possess cholinolytic and bronchospasmolytic effects and are completely devoid of harmful side-effects. Thus these compounds can be used to great advantage in therapy.
摘要翻译：本发明涉及下式的呫吨-9-羧酸盐：其中R 1和R 3可以相同或不同，表示低级烷基，N和M为2至5的整数，或药物化学其有效的销售。根据本发明的化合物具有胆汁溶解和支气管痉挛分解作用，并且完全没有有害的副作用。因此，这些化合物可用于治疗中的极大优势。

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