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11. 发明授权

US4425358A 13-Thia-prostacycline derivatives 失效
标题翻译： 13-前列环素衍生物
公开(公告)号：US4425358A
公开(公告)日：1984-01-10
申请号：US370503
申请日：1982-04-21
申请人： Csaba Szantay , Lajos Novak , Jozsef Aszodi , Vilmos Simonidesz , Geza Galambos , Gabor Kovacs , Sandor Virag , Istvan Stadler , Peter Kormoczy
发明人： Csaba Szantay , Lajos Novak , Jozsef Aszodi , Vilmos Simonidesz , Geza Galambos , Gabor Kovacs , Sandor Virag , Istvan Stadler , Peter Kormoczy
IPC分类号： C07D307/935 , A61K31/557 , A61P7/02 , A61P9/12 , C07C405/00 , C07D307/937 , C07D407/12
CPC分类号： C07D307/937 , C07C405/0033 , C07D407/12 , Y10S514/822
摘要： The invention relates to new optically active or racemic 13-thia-prostacycline derivatives of the Formula I ##STR1## wherein R.sup.1 is hydrogen, a pharmaceutically acceptable cation or a straight or branched chain alkyl group having 1-5 carbon atoms;R.sup.2 is straight or branched chain alkyl having 4-9 carbon atoms or monosubstituted phenoxymethyl;--A--B-- is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- of Z-- or E-- configuration or --C.tbd.C--;one of the symbols X and Y is hydrogen, methyl or ethyl and the other is hydroxy, tetrahydropyranyoxy, 1-ethoxy-ethoxy or trialkylsilyloxy; orX and Y together form a --O--CH.sub.2 --CH.sub.2 --O-- group;Z is a sulfur atom or a --SO-- group.The compounds of the Formula I can be prepared by reacting a 13-thia-prostaglandine of the Formula III ##STR2## if desired after oxidation into the corresponding 13-oxide derivative--with a halogenating agent; and treating the 5-halogeno-13-thia-prostacycline of the Formula II ##STR3## thus obtained wherein E is halogen with an organic or inorganic base; and thereafter if desired removing the protecting groups X and/or Y and if desired converting a compound of the Formula I obtained into a salt or setting free the same from a salt. The new compounds of the Formula I possess anti-coagulant and hypotensive properties and can be used in therapy.
摘要翻译：本发明涉及式I的新的光学活性或外消旋的13-前列环素衍生物，其中R1是氢，可药用阳离子或具有1-5个碳原子的直链或支链烷基; R2是具有4-9个碳原子的直链或支链烷基或单取代的苯氧基甲基; -A-B-是Z-或E-构型的-CH 2 -CH 2 - ， - CH = CH-或-C 3 D C-; 符号X和Y之一是氢，甲基或乙基，另一个是羟基，四氢吡喃基氧基，1-乙氧基 - 乙氧基或三烷基甲硅烷氧基; 或X和Y一起形成-O-CH 2 -CH 2 -O-基团; Z是硫原子或-SO-基。式I的化合物可以通过使式III的13-前 - 前列腺素（III）反应来制备。

12. 发明授权

US5424327A Combined compositions 失效
标题翻译：组合成分
公开(公告)号：US5424327A
公开(公告)日：1995-06-13
申请号：US303712
申请日：1994-09-09
申请人： Laszlo Pap , Istvan Szekely , Lajos Nagy , Andras Szego , Andrea Toth , Eva Somfai , Csaba Szantay , Lajos Novak , Laszlo Poppe
发明人： Laszlo Pap , Istvan Szekely , Lajos Nagy , Andras Szego , Andrea Toth , Eva Somfai , Csaba Szantay , Lajos Novak , Laszlo Poppe
IPC分类号： A01N43/30 , A01N43/50 , A01N43/54 , A01N43/653 , A01N47/38 , A01N53/00 , A01N53/02 , A01N53/04 , A01N53/06 , A01N53/08 , A01N53/14
CPC分类号： A01N53/00
摘要： The invention relates to novel combined compositions for combatting plant, animal and sanitarian as well as forestry, horticultural and warehouse pests. These compositions contain a pyrethroid-type insecticide as an insecticidally active ingredient and at least one fungicide inhibiting the ergosterol biosynthesis as activity-strengthening agent as well as optionally piperonylbutoxide and other additives.The advantages of the compositions according to the invention consist therein that the activity-strengthening substances used are fungicidal agents widely used and have an advantageous toxicology. The activity-strengthening agent exerts a synergistic effect together with the pyrethroid-type insecticide.The combinations according to the invention bear an outstanding importance in the protection of stored crops.
摘要翻译：本发明涉及用于对抗植物，动物和卫生以及林业，园艺和仓库害虫的新型组合组合物。这些组合物含有拟除虫菊酯型杀虫剂作为杀虫活性成分和至少一种抑制麦角甾醇生物合成作为活性增强剂以及任选的胡椒基丁醚和其它添加剂的杀真菌剂。根据本发明的组合物的优点在于其中使用的活性增强物质是广泛使用的杀真菌剂并且具有有利的毒理学。活性增强剂与拟除虫菊酯类杀虫剂一起发挥协同作用。根据本发明的组合在保护作物方面具有突出的重要性。

13. 发明授权

US6093720A Trans apovincaminic acid ester derivatives 失效
标题翻译：转氨基丁酸酯衍生物
公开(公告)号：US6093720A
公开(公告)日：2000-07-25
申请号：US91260
申请日：1998-06-09
申请人： Csaba Szantay , Istvan Moldvai , Andras Vedres , Maria Incze , Janos Kreidl , Laszlo Czibula , Maria Farkas Nee Kiriak , Ida Deutsch Nee Juhasz , Aniko Gere , Margit Pellionisz Nee Paroczai , Erzsebet Lapis , Andras Szekeres , Maria Zajer Nee Balazs , Adam Sarkadi , Ferenc Auth , Bela Kiss , Egon Karpati , Sandor Farkas
发明人： Csaba Szantay , Istvan Moldvai , Andras Vedres , Maria Incze , Janos Kreidl , Laszlo Czibula , Maria Farkas Nee Kiriak , Ida Deutsch Nee Juhasz , Aniko Gere , Margit Pellionisz Nee Paroczai , Erzsebet Lapis , Andras Szekeres , Maria Zajer Nee Balazs , Adam Sarkadi , Ferenc Auth , Bela Kiss , Egon Karpati , Sandor Farkas
IPC分类号： A61K31/00 , A61K31/395 , A61K31/435 , A61K31/4353 , A61K31/4375 , A61P9/00 , A61P9/10 , A61P25/28 , C07D461/00 , C07D471/22
CPC分类号： C07D461/00
摘要： The invention relates to novel racemic and optically active trans apovincaminic acid ester derivatives of formula (I), ##STR1## wherein R means hydrogen or a group (a), wherein Z stands for C.sub.1-4 alkyl, optionally substituted aryl, aralkyl, heteroaryl or 14-eburnameninyl group; and n is an integer of 2, 3 or 4, as well as therapeutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing these compounds as well as a process for the preparation of the above compounds and compositions, and in addition, to a method of treatment. The novel compounds of Formula (I) exhibit particularly antioxidant, antiischemic as well as antiamnesic effects and are useful for inhibiting lipid peroxidation and for protection from or treatment of ischemia and amnesia as well as for treating various degenerative neurological diseases, e.g. Alzheimer's disease.
摘要翻译： PCT No.PCT / HU96 / 00075 Sec。 371日期1998年6月9日第 102（e）1998年6月9日PCT 1996年12月13日PCT PCT。公开号WO97 / 23481 日期1997年7月3日本发明涉及式（I）的新型外消旋和光学活性反氨基丁酸酯衍生物，其中R表示氢或基团（a），其中Z表示C1-4烷基，任选取代的芳基，芳烷基，杂芳基或14-桦烷亚胺基; 和n为2,3或4的整数，以及其可治疗的盐。本发明还涉及含有这些化合物的药物组合物以及制备上述化合物和组合物的方法，此外还涉及治疗方法。式（I）的新化合物显示出特别的抗氧化，抗缺血和抗病毒作用，并且可用于抑制脂质过氧化和保护或治疗缺血和遗忘以及用于治疗各种退行性神经系统疾病，例如，阿尔茨海默氏病。

14. 发明授权

US4659816A Process for the preparation of dimeric alkaloids 失效
标题翻译：二聚生物碱的制备方法
公开(公告)号：US4659816A
公开(公告)日：1987-04-21
申请号：US688932
申请日：1985-01-04
申请人： Csaba Szantay , Katalin Honty , Lajos Szabo , Tibor Keve , Tibor cs
发明人： Csaba Szantay , Katalin Honty , Lajos Szabo , Tibor Keve , Tibor cs
IPC分类号： A61K31/475 , A61P35/00 , C07D519/04
CPC分类号： C07D519/04
摘要： A process is disclosed for the preparation of dimeric alkaloids of formula (II) ##STR1## wherein R stands for methyl or formyl, as well as acid addition salts thereof which comprises oxidizing the vinblastine of formula (III) ##STR2## with chromium (VI) oxide or bichromate or chromic acid alcohol ester in an inert solvent, converting the compound of formula (II), wherein R stands for methyl, so obtained to the acid addition salt and optionally further oxidizing the acid addition salt obtained with an oxidizing agent as defined above and optionally converting the compound of formula (II), wherein R stands for formyl, so obtained to the acid addition salt.
摘要翻译：公开了用于制备式（II）的二聚生物碱的方法，其中R代表甲基或甲酰基，以及其酸加成盐，其包括氧化式（III）的长春花碱（IMA） III）与惰性溶剂中的重铬酸铬（VI）或重铬酸盐或铬酸醇酯反应，将得到的式（II）化合物（其中R代表甲基）转化成酸加成盐，并任选地进一步氧化酸加成盐用如上定义的氧化剂获得，并任选地将所得到的式（II）化合物（其中R代表甲酰基）转化成酸加成盐。

15. 发明授权

US4464534A Process for the preparation of vincaminic acid esters 失效
标题翻译：用于制备长春酸酯的方法
公开(公告)号：US4464534A
公开(公告)日：1984-08-07
申请号：US425866
申请日：1982-09-28
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Kreidl , Andras Nemes , Maria Farkas nee Kirjak , Gyorgy Visky , Laszlo Czibula
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Kreidl , Andras Nemes , Maria Farkas nee Kirjak , Gyorgy Visky , Laszlo Czibula
IPC分类号： C07D461/00 , C07D455/00
CPC分类号： C07D461/00
摘要： The invention relates to a new process for the preparation of apovincaminic acid esters. More particularly, the invention concerns a process for preparing racemic and optionally active vincaminic acid esters of the formula (I) ##STR1## in which R.sup.1 and R.sup.2 independently stand for alkyl having from one to 6 carbon atoms, and 14-epimers thereof.According to the invention an octahydroindolo[2,3-a]quinolizine-oxime ester of the formula (II) ##STR2## in which R.sup.1 and R.sup.2 have the same meaning as defined above, is reacted with an aqueous solution of sulfurous acid or a salt thereof at a temperature of 80.degree. to 110.degree. C. and the 14-epimeric mixture obtained is epimerized or separated in a known manner and if desired, the racemic vincaminic acid esters are resolved.The valuable, pharmaceutically active compounds of the formula (I) can be prepared according to the invention in a considerably improved yield and the undesired side reactions can be suppressed and/or the by-products can easily be converted into other pharmaceutically active materials.
摘要翻译：本发明涉及一种用于制备氨磷酸酯的新方法。更具体地说，本发明涉及一种制备式（I）的外消旋和任选活性的长春胺酸酯的方法，其中R 1和R 2独立代表具有1至6个碳原子的烷基，和14-差向异构体其中。根据本发明，其中R 1和R 2具有与上述相同的含义的式（II）的二氢吲哚并[2,3-a]喹嗪肟酯与其中的亚硫酸酯水溶液酸或其盐，并且所得的14-差向异构体混合物以已知方式进行差向异构化或分离，如果需要，外消旋的长春碱酯被分解。式（I）的有价值的药物活性化合物可以按照本发明以显着提高的产量制备，并且可以抑制不期望的副反应和/或副产物可以容易地转化成其它药物活性物质。

16. 发明授权

US4356305A Process for the preparation of halovincamone derivatives 失效
标题翻译：制备Halovincone酮衍生物的方法
公开(公告)号：US4356305A
公开(公告)日：1982-10-26
申请号：US175384
申请日：1980-08-05
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Lajos Dancsi , Tibor Keve , Ferenc Drexler
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Lajos Dancsi , Tibor Keve , Ferenc Drexler
IPC分类号： A61K31/435 , A61P9/08 , C07D461/00
CPC分类号： C07D461/00
摘要： The invention relates to new halovincamone derivatives of the general formula (I), ##STR1## wherein R is a C.sub.1-6 alkyl group and X is halogen, and pharmaceutically acceptable acid addition salts and optically active isomers thereof. These compounds possess valuable vasodilating effect, and can be applied to advantage in the therapy.The new compounds defined above are prepared according to the invention so that a single epimer or an epimeric mixture of a racemic or optically active halogenated 14-oxo-15-hydroxy-E-homoeburnane derivative of the general formula (II), ##STR2## wherein R and X are as defined above, or an acid addition salt thereof is treated with an oxidizing agent, and, if desired, the resulting compound of the general formula (I) is converted into its pharmaceutically acceptable acid addition salt and/or resolved.
摘要翻译：本发明涉及通式（I）的新的Halovincone酮衍生物，其中R是C 1-6烷基，X是卤素的化合物及其药学上可接受的酸加成盐和旋光异构体。这些化合物具有有价值的血管扩张作用，可用于治疗中的优势。根据本发明制备上述新化合物，使得通式（II）的外消旋或光学活性的卤代14-氧代-15-羟基-E-高拜尔班恩衍生物的单个差向异构体或差向异构体混合物（II）其中R和X如上所定义，或其酸加成盐用氧化剂处理，如果需要，将所得的通式（I）化合物转化为其药学上可接受的酸加成盐和 /或解决。

17. 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.

18. 发明授权

US6103724A 2-methoxyphenylpiperazine derivatives 失效
标题翻译： 2-甲氧基苯基哌嗪衍生物
公开(公告)号：US6103724A
公开(公告)日：2000-08-15
申请号：US284313
申请日：1999-04-27
申请人： Istvan Laszlovszky , Gyorgy Domany , Tibor Acs , Gyorgy Ferenczy , Csaba Szantay , Eszter Thuroczyne Kalman , Erzsebet Lapis , Ferenc Trischler , Bela Hegedus , Feranc Auth , Monika Csejtei , Egon Karpati , Bela Kiss , Judit Laszy , Margit Pellioniszne Paroczai , Adam Sarkadi , Sandor Szabo
发明人： Istvan Laszlovszky , Gyorgy Domany , Tibor Acs , Gyorgy Ferenczy , Csaba Szantay , Eszter Thuroczyne Kalman , Erzsebet Lapis , Ferenc Trischler , Bela Hegedus , Feranc Auth , Monika Csejtei , Egon Karpati , Bela Kiss , Judit Laszy , Margit Pellioniszne Paroczai , Adam Sarkadi , Sandor Szabo
IPC分类号： C07D241/00 , A61K31/496 , A61K31/519 , A61K31/542 , A61P25/18 , A61P25/22 , C07D471/04 , C07D487/04 , C07D513/04
CPC分类号： C07D471/04 , C07D487/04 , C07D513/04
摘要： The invention relates to fused heterocyclic compounds with ring junction nitrogen atom of the formula: ##STR1## wherein Q stands for 2-indolizinyl, 2-imidazo[1,2-a]pyridinyl, 2-imidazo[1,2-a]pyrimidinyl, 6-(2,3-dihydroimidazo[2,1-b]thiazol)-yl or 6-imidazo[2,1-b]thiazolyl group; and n is an integer from 2 to 4, as well as therapeutically useful salts thereof. The invention further relates to pharmaceutical compositions containing these compounds as well as a process for the preparation of the above compounds and compositions. The compounds of formula (I) exhibit mainly antipsychotic effects so the invention relates also to a method of treatment of schizophrenia, organic mental disorders, affective disorders, anxiety and personality disorders.
摘要翻译： PCT No.PCT / HU97 / 00069 Sec。一九九九年四月二十七日 102（e）1999年4月27日PCT PCT 1997年10月22日PCT公布。第WO98 / 18797号公报日期：1998年5月7日本发明涉及具有下列通式的环连氮原子的稠合杂环化合物：其中Q代表2-中氮茚基，2-咪唑并[1,2-a]吡啶基，2-咪唑并[1,2-a] 嘧啶基，6-（2,3-二氢咪唑并[2,1-b]噻唑）基或6-咪唑并[2,1-b]噻唑基; 且n为2至4的整数，以及其治疗上有用的盐。本发明还涉及含有这些化合物的药物组合物以及制备上述化合物和组合物的方法。式（I）化合物主要表现为抗精神病作用，因此本发明还涉及治疗精神分裂症，有机精神障碍，情感障碍，焦虑和人格障碍的方法。

19. 发明授权

US5707976A Substituted propane-2-OL derivatives 失效
标题翻译：取代的丙烷-2-OL衍生物
公开(公告)号：US5707976A
公开(公告)日：1998-01-13
申请号：US605052
申请日：1996-03-04
申请人： Janos Kreidl , Csaba Szantay , Laszlo Czibula , Maria nee Kirjak Farkas , Ida nee Juhasz Deutsch , Mihaly Szegedi , Istvan Hegedus
发明人： Janos Kreidl , Csaba Szantay , Laszlo Czibula , Maria nee Kirjak Farkas , Ida nee Juhasz Deutsch , Mihaly Szegedi , Istvan Hegedus
IPC分类号： A61K31/695 , A61P31/04 , A61P31/10 , C07F7/18
CPC分类号： C07F7/1856
摘要： Anti-Fungal compounds are disclosed of the Formula (I) ##STR1## wherein R.sup.1 is C.sub.1 to C.sub.10 alkyl, phenyl, or phenyl-C.sub.1 to C.sub.6 alkyl, and the phenyl moiety of the two latter groups may carry at least one substituent selected from the group consisting of a halogen atom, C.sub.1 to C.sub.6 alkoxy group, phenyl group, phenoxy group, and trifluorome thyl group; R.sup.2 is a hydrogen atom, a C.sub.1 to C.sub.10 alkyl group or a phenyl group; R.sup.3 and R.sup.4 are independently from each other a C.sub.1 to C.sub.10 alkyl group or a phenyl group; X is a hydrogen atom, halogen atom or a group of the formula (A) ##STR2## and in this formula Y.sup.1 and Y.sup.2 are independently from each other, a --N.dbd. atom or a group of the formula --CH.dbd., or an optical antipode thereof.
摘要翻译： PCT No.PCT / HU94 / 00040 Sec。 371日期：1996年3月4日 102（e）1996年3月4日PCT PCT 1994年9月22日PCT公布。出版物WO95 / 08552 日期：1995年3月30日公开了式（I）的化合物：其中R 1为C 1至C 10烷基，苯基或苯基-C 1至C 6烷基，并且后两个基团的苯基部分可以携带至少一个选自卤素原子，C1-C6烷氧基，苯基，苯氧基和三氟甲基三基的取代基; R2是氢原子，C1〜C10烷基或苯基; R 3和R 4彼此独立地为C 1至C 10烷基或苯基; X是氢原子，卤素原子或式（A）基团（A），在该式中Y1和Y2彼此独立地是-N =原子或式-CH = ，或其光学对映体。

20. 发明授权

US4757077A Bis-indole derivatives and pharmaceutical compositions containing them 失效
标题翻译：双吲哚衍生物和含有它们的药物组合物
公开(公告)号：US4757077A
公开(公告)日：1988-07-12
申请号：US873540
申请日：1986-06-12
申请人： Csaba Szantay , Lajos Szabo , Katalin Honty , Tibor Keve , Tibor Acs , Sandor Eckhardt , Janos Sugar , Zsuzsa Somfai , Eva Ivan , Zsuzsa Kneffel
发明人： Csaba Szantay , Lajos Szabo , Katalin Honty , Tibor Keve , Tibor Acs , Sandor Eckhardt , Janos Sugar , Zsuzsa Somfai , Eva Ivan , Zsuzsa Kneffel
IPC分类号： A61K31/475 , A61P35/00 , C07D519/04
CPC分类号： C07D519/04
摘要： The invention relates to novel bis-indole derivatives of the general formula (I) ##STR1## wherein R.sub.1 stands for a hydrogen atom or an acetyl group;R.sub.2 stands for a hydrogen atom;R.sub.3 means an ethyl group of .alpha.-position; orR.sub.2 and R.sub.3 together represent an oxygen bridge;R.sub.4 represents an ethyl or hydroxyl group of .beta.-position; andR.sub.5 stands for a hydrogen atom or a hydroxyl group;A represents a C.sub.1-10 straight-chain or C.sub.3-10 branched-chain alkyl group, hydroxy-alkyl, acetyl-alkyl, benzyl, C.sub.3-6 alkenyl or alkynyl or C.sub.5-7 cycloalkyl group or an aromatic group or a heteroaromatic group containing one nitrogen or one oxygen atom, andX stands for oxygen or sulphur atom,as well as their acid addition salts and pharmaceutical preparations containing these compounds.Further on, the invention relates to a process for preparing these compounds and preparations.The compounds of the general formula (I) show a cytostatic activity with less toxicity than that of the known vinblastine-type bis-indole alkaloid drugs which are commercially available.
摘要翻译：本发明涉及通式（I）的新的双吲哚衍生物：其中R1代表氢原子或乙酰基; R2代表氢原子; R3表示α-位的乙基; 或R2和R3一起表示氧桥; R4表示β-位的乙基或羟基; R5代表氢原子或羟基; A表示C 1-10直链或C 3-10支链烷基，羟基 - 烷基，乙酰基 - 烷基，苄基，C 3-6烯基或炔基或C 5-7环烷基或芳族基团或含杂芳基一个氮原子或一个氧原子，X代表氧或硫原子，以及它们的酸加成盐和含有这些化合物的药物制剂。此外，本发明涉及一种制备这些化合物和制剂的方法。通式（I）的化合物显示出具有比可商购的已知长春花碱型双吲哚生物碱药物毒性小的细胞生长抑制活性。

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