专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 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。

2. 发明授权

US4839362A Eburnamenine derivatives, pharmaceutical compositions and methods employing them and processes for their preparation 失效
标题翻译：伊本海宁衍生物，药物组合物和使用它们的方法及其制备方法
公开(公告)号：US4839362A
公开(公告)日：1989-06-13
申请号：US853844
申请日：1986-04-18
申请人： Janos Kreidl , Gyorgy Visky , Laszlo Czibula , Bela Stefko , Maria Farkas nee Kirjak , Zsolt Szombathelyi , Egon Karpati , Bela Kiss , Katalin Csomor , Laszlo Szporny , Lilla Forgacs , Csaba Kuthi , Aniko Gere
发明人： Janos Kreidl , Gyorgy Visky , Laszlo Czibula , Bela Stefko , Maria Farkas nee Kirjak , Zsolt Szombathelyi , Egon Karpati , Bela Kiss , Katalin Csomor , Laszlo Szporny , Lilla Forgacs , Csaba Kuthi , Aniko Gere
IPC分类号： A61K31/47 , A61P9/08 , C07D461/00
CPC分类号： C07D461/00
摘要： The invention relates to the preparation of cis and trans stereoisomers of racemic and optically active eburnamenine derivatives of the general formula (Ia) ##STR1## or (Ib), ##STR2## wherein R.sub.1 stands for a C.sub.1-4 alkyl group; andR stands for hydrogen, a C.sub.1-6 alkyl group, a C.sub.2-6 alkenyl group, an acyl or substituted acyl group,as well as their acid addition salts, of which the trans compounds are novel.The invention also relates to the compounds of the general formula (IIIa) ##STR3## and (IIIb), ##STR4## wherein R.sub.1 and R' represent a C.sub.1-4 alkyl group. The compounds of the general formulae (Ia) and (Ib) possess a vasodilatory effect which is substantially higher than that of pentoxifyllin, a known peripheral vasodilator.
摘要翻译：本发明涉及制备通式（Ia），（Ia）或（Ib），（Ⅰb）的外消旋和光学活性依勃他宁衍生物的顺式和反式立体异构体，其中R1代表C1-4 烷基; R代表氢，C1-6烷基，C2-6链烯基，酰基或取代的酰基，以及它们的酸加成盐，其反式化合物是新的。本发明还涉及通式（IIIa）的化合物（IIIa）和（IIIb），其中R1和R'代表C1-4烷基。通式（Ia）和（Ib）的化合物具有明显高于已知外周血管扩张剂己酮可可林的血管扩张作用。

3. 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。

4. 发明授权

US5198446A Organosilane derivatives, pharmaceutical compositions containing them and process for preparing same 失效
标题翻译：有机衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：US5198446A
公开(公告)日：1993-03-30
申请号：US736962
申请日：1991-07-29
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
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 form 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.

5. 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。

6. 发明授权

US4474960A Apovincaminic acid esters 失效
标题翻译：氨基丁酸酯
公开(公告)号：US4474960A
公开(公告)日：1984-10-02
申请号：US387676
申请日：1982-06-11
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Kreidl , Laszlo Czibula , Gyorgy Visky , Andras Nemes , Maria Farkas nee Kirlyak
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Kreidl , Laszlo Czibula , Gyorgy Visky , Andras Nemes , Maria Farkas nee Kirlyak
IPC分类号： C07B57/00 , C07D461/00 , C07D471/14 , A61K31/475
CPC分类号： C07D471/14 , C07D461/00
摘要： A process is disclosed for the preparation of racemic cis or trans apovincaminic acid esters of the formula (I) ##STR1## and the corresponding optically active derivatives of the formulae (Ia) ##STR2## wherein R.sup.1 and R.sup.2 are identical or different alkyl groups having 1 to 6 carbon atoms. Apovincaminic acid alkyl esters are well-known vasodilating compounds.
摘要翻译：公开了一种制备式（I）的外消旋顺式或反式亚氨基酸酯和式（Ia）和/或（Ib）的相应的光学活性衍生物的方法。（Ⅰb）和/或（Ⅰc）（Ⅰc）和（ⅰ）其中R1和R2是具有1-6个碳原子的相同或不同的烷基。氨基丁酸烷基酯是众所周知的血管扩张化合物。

7. 发明授权

US4614824A Novel apovincaminic acid derivatives 失效
标题翻译：新型氨基丁酸衍生物
公开(公告)号：US4614824A
公开(公告)日：1986-09-30
申请号：US754671
申请日：1985-07-11
申请人： Janos Kreidl , Laszlo Czibula , Gyorgy Visky , Maria Farkas nee Kirjak , Judit Meszaros nee Brill , Dora Groo , Eva Palosi , Egon Karpati , Laszlo Szporny
发明人： Janos Kreidl , Laszlo Czibula , Gyorgy Visky , Maria Farkas nee Kirjak , Judit Meszaros nee Brill , Dora Groo , Eva Palosi , Egon Karpati , Laszlo Szporny
IPC分类号： A61K31/435 , A61P9/00 , C07D461/00
CPC分类号： C07D461/00
摘要： The invention relates to new racemic and optically active apovincaminic acid derivatives of the general formula (I) ##STR1## wherein A is hydroxyl, halogen or a group --O--(CH.sub.2).sub.n --OR.sup.1 or --OMe, in whichR.sup.1 is alkyl having from one to 6 carbon atoms,n is an integer between 2 and 6,Me is an alkali metal,R.sup.2 stands for an alkyl group having from one to 6 carbon atoms, which may be identical with or different from R.sup.1,and the hydrogen in the 3-position and the R.sup.2 group have an .alpha.,.alpha.- and/or .beta.,.beta.- or .alpha.,.beta.- and/or .beta.,.alpha.-configuration, and pharmaceutically acceptable acid addition salts thereof, which are pharmaceutically active, e.g. show antihypoxial activity or are potent peripheral vasodilators. Their preparation and pharmaceutical composition containing them are also within the scope of the invention.
摘要翻译：本发明涉及通式（I）的新的外消旋和光学活性氨基丁酸衍生物，其中A是羟基，卤素或-O-（CH2）n-OR1或-OMe基团，其中R1 是具有1至6个碳原子的烷基，n是2和6之间的整数，Me是碱金属，R 2表示具有1至6个碳原子的烷基，其可以与R 1相同或不同， 3-位和R2基团中的氢具有药学活性的α，α - 和/或β，β-或α，β-和/或β，α-构型及其药学上可接受的酸加成盐，例如显示抗低氧活性或是有效的外周血管扩张剂。它们的制备和含有它们的药物组合物也在本发明的范围内。

8. 发明授权

US4735946A Eburnane derivatives, process for their preparation and pharmaceutical compositions containing them 失效
标题翻译：伊本恩衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US4735946A
公开(公告)日：1988-04-05
申请号：US718917
申请日：1985-04-02
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Kreidl , Maria Farkas nee Kirjak , Laszlo Czibula , Bela Stefko , Gyorgy Visky , Judit Meszaros nee Brill
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Kreidl , Maria Farkas nee Kirjak , Laszlo Czibula , Bela Stefko , Gyorgy Visky , Judit Meszaros nee Brill
IPC分类号： A61K31/435 , A61P25/00 , A61P25/08 , B01J31/00 , B01J31/04 , C07B61/00 , C07D461/00 , C07D471/14 , A61K31/44
CPC分类号： C07D461/00
摘要： The invention relates to new eburnane derivatives of the formula (I) ##STR1## wherein R.sup.1 is alkyl having from 1 to 6 carbon atoms, and acid addition salts thereof.The invention further relates to a process for the preparation of these compounds and pharmaceutical compositions containing them.Compounds of formula (I) show remarkable CNS-activity and are useful intermediates in the preparation of other, pharmaceutically active compounds.
摘要翻译：本发明涉及式（I）的新的伊本恩衍生物，其中R1是具有1至6个碳原子的烷基，及其酸加成盐。本发明还涉及制备这些化合物的方法和含有它们的药物组合物。式（I）化合物显示出显着的CNS活性，并且是制备其它药学活性化合物的有用中间体。

9. 发明授权

US4464535A Process for the preparation of eburnamonine derivatives 失效
标题翻译：制备苯丙胺衍生物的方法
公开(公告)号：US4464535A
公开(公告)日：1984-08-07
申请号：US438288
申请日：1982-11-01
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Kreidl , Gyorgy Visky , Andras Nemes , Laszlo Czibula , Maria Farkas nee Kirjak
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Kreidl , Gyorgy Visky , Andras Nemes , Laszlo Czibula , Maria Farkas nee Kirjak
IPC分类号： C07D461/00 , C07D471/14 , C07D455/00
CPC分类号： C07D471/14 , C07D461/00
摘要： The invention relates to a new process for the preparation of eburnamonine derivatives of the general Formula I ##STR1## (wherein R.sup.1 is an alkyl group having 1-6 carbon atoms) and optical and geometrical isomers thereof which comprises reacting a hydroxyimino-octahydro-indolo[2,3-a]quinolizine derivative of the general Formula II ##STR2## (wherein R.sup.1 is as stated above and R.sup.2 stands for an alkyl group having 1-6 carbon atoms being identical with or different from R.sup.1, or a hydrogen atom) or an acid addition salt thereof in an organic protic solvent or solvent mixture with an inorganic base, optionally under the addition of water or an aqueous mineral acid, at a temperature between 60.degree. C. and 200.degree. C.The compounds of the present invention are known drugs having blood pressure decreasing and cerebral vasodilatatory effect. The advantage of the process of the present invention is that it is readily feasible on industrial scale too, provides isomer-free pure products with high yield and requires the use of readily available simple starting materials.
摘要翻译：本发明涉及一种制备通式Ⅰ（I）（Ⅰ）（其中R1是具有1-6个碳原子的烷基）及其光学和几何异构体的本发明化合物的新方法，其包括使羟基亚氨基 - 通式II的八氢 - 吲哚并[2,3-a]喹嗪衍生物（II）（其中R 1如上所述，R 2表示具有1-6个碳原子的烷基，与R 1相同或不同），或氢原子）或其酸加成盐在无机碱的有机质子溶剂或溶剂混合物中，任选在水或无机酸水溶液中，在60℃至200℃的温度下进行。本发明的化合物是具有降血压和脑血管扩张作用的已知药物。本发明方法的优点是在工业规模上也容易实现，提供高产率的无异构体纯产品，并且需要使用容易获得的简单起始原料。

10. 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。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式