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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

US4810709A Nintrovincaminic acid derivatives having pharmaceutical utility 失效
标题翻译：具有药用效用的新一代氨基酸衍生物
公开(公告)号：US4810709A
公开(公告)日：1989-03-07
申请号：US105959
申请日：1987-10-07
申请人： Andras Vedres , Csaba Szantay , Istvan Moldvai , Bela Stefko , Dora Groo , Egon Karpati , Bela Kiss , Eva Palosi , Miklos Riesz , Zsolt Szombathelyi , Laszlo Szporny , Maria Zajer nee Balazs
发明人： Andras Vedres , Csaba Szantay , Istvan Moldvai , Bela Stefko , Dora Groo , Egon Karpati , Bela Kiss , Eva Palosi , Miklos Riesz , Zsolt Szombathelyi , Laszlo Szporny , Maria Zajer nee Balazs
IPC分类号： A61K31/435 , A61P9/00 , A61P9/08 , A61P25/08 , C07D461/00 , A61K31/475
CPC分类号： C07D461/00
摘要： The invention relates to a new process for preparing novel racemic and optically active 9- or 11-nitroapovincaminic acid derivatives of the general formula (I) ##STR1## wherein R stands for a --CO--X group, wherein X means a halogen atom; orfor a --CO--OR.sup.1 group, wherein R.sup.1 means an optionally mono- or polysubstituted C.sub.1-10 aliphatic group, a C.sub.3-8 alicyclic group or an aromatic C.sub.6-14 hydrocarbyl group; orfor a --CO--NR.sup.2 R.sup.3 group, wherein R.sup.2 and R.sup.3 are the same or different and stand for a hydrogen atom or a C.sub.1-8 alkyl group optionally forming a saturated heterocycle together with the adjacent nitrogen atom and optionally with one or more further nitrogen atoms or other heteroatoms, and R.sup.3 may also represent an amino group when R.sup.2 stands for a hydrogen atom; orfor a cyano group,as well as their salts and pharmaceutical preparations containing these compounds. Furthermore the invention relates to a process for preparing these compounds and preparations.The racemic and optically active substances of the general formula (I) as well as their pharmaceutically acceptable acid addition and quaternary salts have valuable therapeutic properties, namely vasodilating, spasmolytic, antihypoxic and anticonvulsive effects.
摘要翻译：本发明涉及制备通式（I）的新型外消旋和光学活性的9-或11-硝基
氨基嘌呤酸衍生物的新方法，其中R代表-CO-X基团，其中X表示卤素原子; 或-CO-OR 1基团，其中R 1表示任选的单取代或多取代的C 1-10脂族基团，C 3-8脂环族基团或芳族C 6-14烃基; 或-CO-NR 2 R 3基团，其中R 2和R 3相同或不同，代表氢原子或任选地与相邻的氮原子一起形成饱和杂环的C 1-8烷基，并且任选地与一个或多个另外的氮原子或其它杂原子，当R 2代表氢原子时，R 3也可以表示氨基; 或氰基，以及它们的含有这些化合物的盐和药物制剂。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）的外消旋和光学活性物质及其药学上可接受的酸加成盐和季盐具有有价值的治疗性质，即血管舒张，解痉，抗缺氧和抗惊厥作用。

5. 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。

6. 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。

7. 发明授权

US4831194A Process for the preparation of nitrodiaryl sulfoxides 失效
标题翻译：制备硝基二芳基亚砜的方法
公开(公告)号：US4831194A
公开(公告)日：1989-05-16
申请号：US76675
申请日：1987-07-23
申请人： Janos Kreidl , Peter Turcsanyi , Zsuzsanna Aracs nee Trischler , Bela Stefko , Judit Meszaros nee Brill , Ida Deutsch nee Juhasz , Jeno Szilbereky , Eva Csizer , Szilard Vezer , Erik Bogsch , Jozsef Bakos , Laszlo Szotyori , Balint Heil
发明人： Janos Kreidl , Peter Turcsanyi , Zsuzsanna Aracs nee Trischler , Bela Stefko , Judit Meszaros nee Brill , Ida Deutsch nee Juhasz , Jeno Szilbereky , Eva Csizer , Szilard Vezer , Erik Bogsch , Jozsef Bakos , Laszlo Szotyori , Balint Heil
IPC分类号： A01N41/10 , A61K31/10
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 which p1 R 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p1 R和R1是氢或具有1至6个碳原子的烷基，R2是氢，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，通过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。

8. 发明授权

US5312622A Acaricidal compositions and process for preparing same 失效
标题翻译：杀螨组合物及其制备方法
公开(公告)号：US5312622A
公开(公告)日：1994-05-17
申请号：US828870
申请日：1992-01-30
申请人： Tibor Nagy , Karoly Zalai , Denes Mathe , Bela Stefko , Arpad Hadhazy , Gyula Csokas , Istvan Gebhardt
发明人： Tibor Nagy , Karoly Zalai , Denes Mathe , Bela Stefko , Arpad Hadhazy , Gyula Csokas , Istvan Gebhardt
IPC分类号： A01N63/02 , A01K51/00 , A01N63/00 , C12N1/20 , C12P1/04 , C12R1/07 , C12R1/38
CPC分类号： C12R1/07 , A01K51/00 , C12R1/38
摘要： The invention relates to acaricidal compositions containing as active ingredient: the fermentation broth or cell-free fermentation broth, of a concentrate of the fermentation broth or cell-free fermentation broth, or a solidified form of the fermentation broth or cell-free fermentation broth of one or two bacterium strains deposited at the National Collection of Agricultural and Industrial Microorganisms, Budapest, Hungary under the identification Nos. 001083 and 001086 or of their mixed micropopulation, if desired, in a sterilized state, optionally together with the metabolism products arising during the fermentation and inutilized nutriments, as well as one or more solid and/or liquid carrier(s) (preferably sugar or a grist of natural minerals), or an inert solvent (e.g. water) and, if desired, with surface active (preferably anionic or nonionic emulsifying or dispersing) agents. The compositions according to the invention can be used for protecting Apis mellifera (honey bee) against mites, particularly Varroa jacobsoni.
摘要翻译： PCT No.PCT / HU90 / 00042 Sec。 371日期：1992年1月30日 102（e）日期1992年1月30日PCT Filed 1990年6月25日PCT公布。公开号WO91 / 00013 日本1991年1月10日。本发明涉及含有作为活性成分的发酵液或无细胞发酵液，发酵液或无细胞发酵液的浓缩物或发酵液的固化形式的杀螨组合物或无菌发酵液，保藏在匈牙利布达佩斯国家农业和工业微生物保藏中心，根据鉴定号为001083和001086的一种或两种细菌菌株，或者如果需要，将其混合在一起，在灭菌状态下，任选地一起发酵期间产生的新陈代谢产物和未使用的营养物质，以及一种或多种固体和/或液体载体（优选糖或天然矿物质颗粒）或惰性溶剂（例如水），如果需要，具有表面活性（优选阴离子或非离子乳化或分散）剂。根据本发明的组合物可用于保护蚜虫（蜂蜜蜂）抵抗螨虫，特别是瓦氏罗汉果。

9. 发明授权

US4334910A Plant-protective and pest-control agent 失效
标题翻译：植物保护和害虫控制剂
公开(公告)号：US4334910A
公开(公告)日：1982-06-15
申请号：US718990
申请日：1976-08-30
申请人： Csaba Lorincz , Eva Lorincz nee Csapo , Istvan Gebhardt , Antal Gimesi , Bela Stefko , Erik Bogsch , Zsuzsanna Foldesi nee Szasz , Kalman Szasz
发明人： Csaba Lorincz , Eva Lorincz nee Csapo , Istvan Gebhardt , Antal Gimesi , Bela Stefko , Erik Bogsch , Zsuzsanna Foldesi nee Szasz , Kalman Szasz
IPC分类号： A01N47/10 , A01N20060101 , A01N25/32 , A01N43/54 , A01N43/66 , A01N57/10 , A01N59/02
摘要： A herbicidal composition capable of preventing weed growth of potatoes or soybean plants consists of a triazene or an aromatic nitro compound together with an inorganic salt, especially sodium bisulfate or potassium bisulfate which reduced the quantity of the organic herbicide below that usually required to obtain a corresponding herbicidal effect and hence prevents phytotoxic damage. The composition contains 0.1:1 to 15:1 parts by weight of the inorganic compound to the organic compound and is applied in an amount of 0.1 to 30 kg of the composition per hectare.
摘要翻译：能够防止马铃薯或大豆植物杂草生长的除草组合物由三氮烯或芳族硝基化合物以及无机盐，特别是硫酸氢钠或硫酸氢钾组成，其将有机除草剂的量降低到通常需要的量以下，以获得相应的除草效果，从而防止植物毒性损害。该组合物含有0.1:1至15:1重量份的无机化合物与有机化合物，其用量为每公顷0.1至30kg组合物。

10. 发明授权

US4243660A Composite insect attractant for male cabbage moths and a process for preparing its active agents 失效
标题翻译：用于大白菜蛾的复合昆虫引诱剂及其活性剂的制备方法
公开(公告)号：US4243660A
公开(公告)日：1981-01-06
申请号：US31583
申请日：1979-04-19
申请人： Csaba Szantay , Lajos Novak , Miklos Toth , Jozsef Balla , Bela Stefko , Attila Kis-Tamas
发明人： Csaba Szantay , Lajos Novak , Miklos Toth , Jozsef Balla , Bela Stefko , Attila Kis-Tamas
IPC分类号： A01N37/02 , A01N49/00 , C07C29/10 , C07C41/30 , C07C43/15 , C07C43/17 , C07C69/145 , C07D309/12 , C07F9/54 , A01N25/00 , A01N37/06
CPC分类号： C07D309/12 , A01N37/02 , C07C29/10 , C07C41/30 , C07C43/15 , C07C43/17 , C07C67/08 , C07C67/293 , C07C69/145 , C07F9/5407
摘要： The invention relates to a composite insect attractant for male cabbage moths (Mamestra brassicae) containing (Z)-11-hexadecenyl acetate and (Z)-11-heptadecenyl acetate as active agents in a weight ratio of 70 to 90:80 to 1, optionally along with a liquid or solid adjuvant. An insect trap can contain the composition which is used for attracting and trapping cabbage moth. Their mating is disrupted by air permeation techniques. (Z)-11-heptadecenyl acetate is a synergistically active new compound. The composition according to the invention produces a significantly stronger stimulating reaction on male cabbage moths than the known sex lure compositions.
摘要翻译：本发明涉及含有（Z）-11-十六碳烯基乙酸酯和（Z）-11-十七碳烯酸乙酯作为活性剂的重量比为70至90:80至1的男性白菜蛾（Mamestra brassicae）的复合昆虫引诱剂，任选地与液体或固体佐剂一起。昆虫陷阱可以包含用于吸引和捕获白菜蛾的组合物。它们的交配被空气渗透技术所破坏。（Z）-11-十七碳烯酸乙酯是协同活性的新化合物。根据本发明的组合物比已知的性诱剂组合物对雄性白菜蛾产生显着更强的刺激反应。

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