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1. 发明授权

US4780537A Pyrimidine derivatives and process preparing the same 失效
标题翻译：嘧啶衍生物及其制备方法
公开(公告)号：US4780537A
公开(公告)日：1988-10-25
申请号：US72010
申请日：1987-07-10
申请人： Andras Vedres , Csaba Szantay , Bela Stefko , Janos Kreidl , Andras Nemes , Gabor Blasko , Erik Bogsch , Denes Mathe , Istvan Hegedus , Adrien Szuchovszky nee Gergely , Tamas Mester
发明人： Andras Vedres , Csaba Szantay , Bela Stefko , Janos Kreidl , Andras Nemes , Gabor Blasko , Erik Bogsch , Denes Mathe , Istvan Hegedus , Adrien Szuchovszky nee Gergely , Tamas Mester
IPC分类号： C07D239/48 , C07D239/50 , C07D239/02
CPC分类号： C07D239/48 , C07D239/50
摘要： A pyrimidine derivative of the formulae (Ia), (Ib) and (Ic), ##STR1## wherein R stands for an alkyl group group with 1 to 6 carbon atoms or an aryl group optionally substituted by halogen atom; andX stands for chlorine or bromine atom or an arylsulfonyloxy group optionally substituted by 1 to 3 lower alkyl groups.The subject pyrimidine derivatives are intermediates for preparing 6-amino-1,2-dihydro-1-hydroxy-2-imino-4-piperidinopyrimidine.
摘要翻译：（Ia），（Ib）和（Ic）的嘧啶衍生物，其中R代表具有1至6个碳原子的烷基基团或任选被卤素原子取代的芳基; X代表氯或溴原子或任选被1至3个低级烷基取代的芳基磺酰氧基。本发明的嘧啶衍生物是制备6-氨基-1,2-二氢-1-羟基-2-亚氨基-4-哌啶并嘧啶的中间体。

2. 发明授权

US4960888A Preparation of 6-amino-1,2-dihydro-1-hydroxy-2-imino-4-piperidinopyrimidine compounds 失效
标题翻译： 6-氨基-1,2-二氢-1-羟基-2-亚氨基-4-哌啶基嘧啶化合物的制备
公开(公告)号：US4960888A
公开(公告)日：1990-10-02
申请号：US320875
申请日：1989-03-09
申请人： Andras Vedres , Csaba Szantay , Bela Stefko , Janos Kreidl , Andras Nemes , Gabor Blasko , Erik Bogsch , Denes Mathe , Istvan Hegedus , Adrien Szuchovszky, nee Gergely , Tamas Mester
发明人： Andras Vedres , Csaba Szantay , Bela Stefko , Janos Kreidl , Andras Nemes , Gabor Blasko , Erik Bogsch , Denes Mathe , Istvan Hegedus , Adrien Szuchovszky, nee Gergely , Tamas Mester
IPC分类号： C07D401/04 , C07D239/50 , C07D295/12
CPC分类号： C07D239/50
摘要： The invention relates to a new process for preparing 6-amino-1,2-dihydro-1-hydroxy-2-imino-4-piperidinopyrimidine of the formula (I), ##STR1## which comprises reacting a pyrimidine derivative of the general formula (II), ##STR2## wherein R.sub.1 stantds for hydrogen or a ##STR3## group, wherein R means a C.sub.1-6 alkyl group or an aryl group optionally substituted by halogen;R.sub.2 stands for a hydroxyl group or an ##STR4## group, wherein R is as defined above; andX represents chlorine or bromine or an optionally mono- or polysubstituted arenesulfonyloxy group,with the proviso that R.sub.2 is different from a hydroxyl group when R.sub.1 stands for hydrogen, with piperidine and hydrolyzing, optionally after isolation, the thus-obtained 4-piperidino derivative of the general formula (III), ##STR5## wherein R.sub.1 and R.sub.2 are as defined above.
摘要翻译：本发明涉及一种制备式（I），（I）的6-氨基-1,2-二氢-1-羟基-2-亚氨基-4-哌啶并嘧啶的新方法，其包括将其中R1代表氢或一个或者两个基团的通式（II），其中R表示任选被卤素取代的C 1-6烷基或芳基; R2代表羟基或基团，其中R如上定义; 并且X表示氯或溴或任选的单取代或多取代的芳烃磺酰氧基，条件是当R1代表氢时，R2不同于羟基，哌啶并水解，任选地在分离后，将由此得到的4-哌啶子基衍生物的通式（III），其中R 1和R 2如上所定义。

3. 发明授权

US5122607A Racemic and optically active octahydro-indolo(2,3-a) tetrahydropyranyl (2,3-c) quinolizine diester derivatives and process for preparing the same 失效
标题翻译：（2,3-A）四氢呋喃（2,3-C）喹啉衍生物及其制备方法
公开(公告)号：US5122607A
公开(公告)日：1992-06-16
申请号：US542485
申请日：1990-06-21
申请人： Janos Kreidl , Csaba Szantay , Lajos Szaho , Maria Farkas nee Kirjak , Gyorgy Kalaus , Katalin Nogradi , Andras Nemes , Judit Meszaros nee Brill , Zsuzsanna Aracs nee Tischler , Bela Stefko , Janos Sapi , Ida Deutsch nee Juhasz , Istvan Hegedus , Bela Benke , Kalman Graf , Kalmam Gaf , Katalin Horvath nee Berki
发明人： Janos Kreidl , Csaba Szantay , Lajos Szaho , Maria Farkas nee Kirjak , Gyorgy Kalaus , Katalin Nogradi , Andras Nemes , Judit Meszaros nee Brill , Zsuzsanna Aracs nee Tischler , Bela Stefko , Janos Sapi , Ida Deutsch nee Juhasz , Istvan Hegedus , Bela Benke , Kalman Graf , Kalmam Gaf , Katalin Horvath nee Berki
IPC分类号： C07D461/00 , C07D471/14 , C07D491/22
CPC分类号： C07D471/14 , C07D461/00
摘要： New intermediate compounds are disclosed of the formula I, ##STR1## wherein R.sub.1 and R.sub.2 are independently alkyl having 1 to 4 carbon atoms,or acid-addition salts thereof of formula Ib, ##STR2## wherein X represents an acid residue, and a process for the preparation of the intermediate compounds.
摘要翻译：公开了新的中间体化合物，其中R 1和R 2独立地为具有1至4个碳原子的烷基，或其酸式加成盐，其中X代表酸残基，中间体化合物的制备方法。

4. 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。

5. 发明授权

US4710323A Nitrodiaryl sulfoxide derivatives, process for their preparation and pharmaceutical and pesticidal compositions containing them as active ingredient 失效
标题翻译：硝基二芳基亚砜衍生物，其制备方法以及含有它们作为活性成分的药物和杀虫组合物
公开(公告)号：US4710323A
公开(公告)日：1987-12-01
申请号：US833834
申请日：1986-02-26
申请人： Janos Kreidl , Peter Turcsanyi , Zsuzsanna Aracs , Bela Stefko , Judit Meszaros , Ida Deutsch , Jeno Szilbereky , Eva Csizer , Szilard Vezer , Erik Bogsch , Jozsef Bakos , Laszlo Szotyori , Balint Heil
发明人： Janos Kreidl , Peter Turcsanyi , Zsuzsanna Aracs , Bela Stefko , Judit Meszaros , Ida Deutsch , Jeno Szilbereky , Eva Csizer , Szilard Vezer , Erik Bogsch , Jozsef Bakos , Laszlo Szotyori , Balint Heil
IPC分类号： A01N41/10 , A61K31/10 , C07C145/00
CPC分类号： A01N41/10 , A61K31/10 , C07C313/04 , C07C317/00 , C07C321/00 , C07C323/00
摘要： The invention relates to a new process for the preparation of aminodiaryl sulfoxide derivatives of the formula (I), ##STR1## wherein X is halogen, alkoxy having from 1 to 6 carbon atoms or a group --(N,R,R.sup.1), in whichR and R.sup.1 are hydrogen or alkyl having from 1 to 6 carbon atoms,R.sup.2 is hydrogen, halogen, alkyl having from 1 to 6 carbon atoms, alkoxy having from 1 to 6 carbon atoms or phenyl or phenylthio both optionally substituted by one or more identical or different halogen(s) and/or amino group(s),and acid addition salts thereof.The compounds of formula (I) are pharmaceutically active, in particular are potent anthelmintics, or can be used as active ingredients in pesticidal compositions. The invention therefore relates to pharmaceutical and pesticidal compositions containing compounds of formula (I) or salts thereof as active ingredient.Compounds of formula (I), in which the substituents are as defined above, but if X stands for a group --N(R,R.sup.1) in which R and R.sup.1 both represent hydrogen, and X is in para-position related to the sulfoxide group, then R.sup.2 is other than hydrogen, halogen, alkyl having from 1 to 6 carbon atoms and alkoxy having from 1 to 6 carbon atoms, and the acid addition salts thereof, are new. These new compounds are also subject of the present invention.
摘要翻译：本发明涉及制备式（I）的氨基二芳基亚砜衍生物的新方法，其中X是卤素，具有1至6个碳原子的烷氧基或基团 - （N，R 1，R 2，），其中R和R 1为氢或具有1至6个碳原子的烷基，R 2为氢，卤素，具有1至6个碳原子的烷基，具有1至6个碳原子的烷氧基或苯基或苯硫基，一个或多个相同或不同的卤素和/或氨基，及其酸加成盐。式（I）的化合物是药学活性的，特别是有效的驱肠虫剂，或可用作杀虫组合物中的活性成分。因此，本发明涉及含有式（I）化合物或其盐作为活性成分的药用和杀虫组合物。式（I）的化合物，其中取代基如上所定义，但如果X代表基团-N（R，R 1），其中R和R 1都代表氢，并且X在对位上与亚砜相关基团，则R2不是氢，卤素，具有1至6个碳原子的烷基和具有1至6个碳原子的烷氧基及其酸加成盐是新的。这些新化合物也是本发明的主题。

6. 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。

7. 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。

8. 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。

9. 发明授权

US4399069A Process for an enantioselective synthesis of optically active 14-oxo-E-homo-eburnane derivatives 失效
标题翻译：光学活性的14-氧代 - 均 - 伊本恩衍生物的对映选择性合成方法
公开(公告)号：US4399069A
公开(公告)日：1983-08-16
申请号：US312128
申请日：1981-10-16
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Sapi , Janos Kreidl , Maria Farkas nee Kirjak , Andras Nemes , Laszlo Cibula
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Janos Sapi , Janos Kreidl , Maria Farkas nee Kirjak , Andras Nemes , Laszlo Cibula
IPC分类号： C07D461/00 , C07D471/14 , C07D471/22
CPC分类号： C07D471/14
摘要： The invention relates to a new enantioselective synthesis for the preparation of optically active 14-oxo-E-homo-eburnane derivatives of the formula (Ia) ##STR1## wherein R.sup.1 is alkyl having from 1 to 4 carbon atom. In the synthesis optically active 6-alkoxycarbonylhexahydroindoloquinolizinium salts are employed as starting materials, which contain a center of chirality at the site of attachment of the carboxyl group. This center of chirality preserves the optical activity of the optically active tryptophan ester from which this compound has been prepared until a new center of chirality is formed in the molecule in a configuration corresponding to the desired end product. The carboxyl group, which is not needed in the end product and only serves to preserving the optical activity can then be eliminated.Compounds of the formula (Ia) are known in the art and may be used in the synthesis of (+)-vincamine and (+)-apovincaminic acid ethylester.
摘要翻译：本发明涉及用于制备式（Ia）的光学活性的14-氧代-E-高 - 同型异烟酸衍生物的新的对映选择性合成。其中R 1是具有1至4个碳原子的烷基。在合成光学活性中，使用6-烷氧基羰基六氢吲哚喹啉鎓盐作为起始原料，其在羧基连接位点含有手性中心。该手性中心保留了光学活性色氨酸酯的光学活性，从该化合物已经制备出光学活性，直至在分子中形成对应于所需最终产物的构型的新的手性中心。然后可以消除最终产物中不需要的仅用于保持光学活性的羧基。式（Ia）的化合物是本领域已知的，可用于合成（+） - 长春胺和（+） - 氨基丁酸乙酯。

10. 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。

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