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21. 发明授权

US4681887A Pharmaceutical compositions with a neuroleptic action and process for preparing same 失效
标题翻译：具有精神抑制作用的药物组合物及其制备方法
公开(公告)号：US4681887A
公开(公告)日：1987-07-21
申请号：US877298
申请日：1986-06-23
申请人： Gabor Megyeri , Tibor Keve , Bela Stefko , Erik Bogsch , Janos Galambos , Anna Kassainee Zieger , Ferenc Trischler , Eva Palosi , Dora Groo , Egon Karpati , Zsolt Szombathelyi , Laszlo Szporny , Bela Kiss , Istvan Laszlovszky , Erzsebet Lapis
发明人： Gabor Megyeri , Tibor Keve , Bela Stefko , Erik Bogsch , Janos Galambos , Anna Kassainee Zieger , Ferenc Trischler , Eva Palosi , Dora Groo , Egon Karpati , Zsolt Szombathelyi , Laszlo Szporny , Bela Kiss , Istvan Laszlovszky , Erzsebet Lapis
IPC分类号： A61K31/48 , A61P25/18 , A61P25/20 , A61P43/00 , C07D457/02 , A61K31/44
CPC分类号： A61K31/48 , C07D457/02
摘要： The invention relates to pharmaceutical compositions with a neuroleptic action as well as to a process for preparing these compositions.The active ingredients of the compositions of the invention are 2-halo-6-methyl-9-ergolene derivatives of the formula (I), ##STR1## wherein X represents a chlorine, bromine or iodine atom as well as their acid addition salts.The compositions of the invention contain an effective dose of compound of the general formula (I) or an acid addition salt thereof.
摘要翻译：本发明涉及具有精神抑制作用的药物组合物以及制备这些组合物的方法。本发明组合物的活性成分是式（I）的2-卤代-6-甲基-9-麦角烯衍生物，其中X代表氯，溴或碘原子，以及它们的酸加成盐。本发明的组合物含有有效剂量的通式（I）化合物或其酸加成盐。

22. 发明授权

US4645774A Aminoethoxybenzylalcohol derivatives, process for their preparation and pharmaceutical compositions containing them 失效
标题翻译：氨基乙氧基苄醇衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US4645774A
公开(公告)日：1987-02-24
申请号：US803792
申请日：1985-12-02
申请人： Edit Toth , Jozsef Torley , Eva Palosi , Szabolcs Szeberenyi , Laszlo Szporny , Sandor Gorog , Istvan Hajdu
发明人： Edit Toth , Jozsef Torley , Eva Palosi , Szabolcs Szeberenyi , Laszlo Szporny , Sandor Gorog , Istvan Hajdu
IPC分类号： A61K31/135 , A61K31/40 , A61K31/445 , A61K31/535 , A61K31/5375 , A61P43/00 , C07C67/00 , C07C213/00 , C07C217/18 , C07D207/20 , C07D295/08 , C07D295/092 , C12N9/02
CPC分类号： C07D295/088
摘要： The invention relates to new aminoethoxybenzylalcohol derivatives of the formula (I) ##STR1## wherein R.sub.1 is hydrogen, halogen, trihalomethyl, alkyl having from one to 4 carbon atoms or alkoxy having from one to 4 carbon atoms;R.sub.2 is halogen, trihalomethyl, or alkoxy having from one to 4 carbon atoms;R.sub.3 and R.sub.4 stand for methyl or together with the adjacent nitrogen form an up to 8-membered ring optionally containing oxygen,and acid addition or quaternary ammonium salts thereof.The compounds of formula (I) are pharmacologically active, thus show enzyme-inducing effect. The pharmaceutical compositions containing them as active ingredient are also within the scope of the invention.
摘要翻译：本发明涉及式（I）的新的氨基乙氧基苄醇衍生物：其中R 1是氢，卤素，三卤代甲基，具有1至4个碳原子的烷基或具有1至4个碳原子的烷氧基; R2是卤素，三卤甲基或具有1至4个碳原子的烷氧基; R3和R4代表甲基或与相邻的氮一起形成任选含有氧的至多8元环，及其酸加成或季铵盐。式（I）化合物具有药理活性，因此显示出酶诱导作用。含有它们作为活性成分的药物组合物也在本发明的范围内。

23. 发明授权

US4618611A 1-(aminoalkoxyphenyl)-1-phenyl-propanols, process for their preparation and pharmaceutical compositions containing them 失效
标题翻译： 1-（氨基烷氧基苯基）-1-苯基 - 丙醇，其制备方法和含有它们的药物组合物
公开(公告)号：US4618611A
公开(公告)日：1986-10-21
申请号：US565901
申请日：1983-12-27
申请人： Edit Toth , Jozsef Torley , Gyorgy Fekete , Laszlo Szporny , Laszlo Vereczkey , Eva Palosi , Imre Klebovich , Pal Vittay , Sandor Gorog , Istvan Hajdu
发明人： Edit Toth , Jozsef Torley , Gyorgy Fekete , Laszlo Szporny , Laszlo Vereczkey , Eva Palosi , Imre Klebovich , Pal Vittay , Sandor Gorog , Istvan Hajdu
IPC分类号： A61K31/135 , A61K31/415 , A61K31/495 , A61K31/53 , A61P25/30 , C07C67/00 , C07C213/00 , C07C217/18 , C07D233/60 , C07D295/08 , C07D295/092 , C07C149/32 , C07D295/02
CPC分类号： C07D295/088
摘要： The invention relates to new aminopropanol derivatives of the formula (I) ##STR1## wherein R.sub.1 is halogen, trihalomethyl, alkoxy having from one to 3 carbon atoms or alkyl having from one to 3 carbon atoms,R.sub.2 is alkyl having from one to 3 carbon atoms, andR.sub.3 is cycloalkyl having from 3 to 6 carbon atoms, orR.sub.2 and R.sub.3 together with the nitrogen they are attached to form an up to 8 membered ring optionally containing oxygen or a further nitrogen as an additional hetero atom, and optionally substituted with alkyl having from one to 4 carbon atoms or benzyl,and acid addition and quaternary ammonium salts thereof.According to another aspect of the invention there are provided processes for the preparation of these compounds.The new compounds are suitable for the treatment of acute ethanolic intoxication. Pharmaceutical compositions containing them are also within the scope of the invention.
摘要翻译：本发明涉及式（I）的新的氨基丙醇衍生物其中R 1为卤素，三卤代甲基，具有1至3个碳原子的烷氧基或具有1至3个碳原子的烷基，R 2为具有一个 3个碳原子，R3是具有3至6个碳原子的环烷基，或者R 2和R 3与它们连接的氮一起形成任选含有氧或另外的氮作为另外的杂原子的至多8元环，以及任选被具有1至4个碳原子的烷基取代或苄基，及其酸加成盐和季铵盐。根据本发明的另一方面，提供了这些化合物的制备方法。新化合物适用于急性乙醇中毒治疗。含有它们的药物组合物也在本发明的范围内。

24. 发明授权

US4588685A Process for the preparation of a new-type active substance selectively inhibiting food intake 失效
标题翻译：制备选择性抑制食物摄入的新型活性物质的方法
公开(公告)号：US4588685A
公开(公告)日：1986-05-13
申请号：US632439
申请日：1984-07-19
申请人： Jozsef Knoll , Janos Nagy , Huba Kalasz , Berta Knoll
发明人： Jozsef Knoll , Janos Nagy , Huba Kalasz , Berta Knoll
IPC分类号： A61K35/14 , A61K35/16 , A61K38/00 , A61K38/16 , A61P3/04 , C07K1/16 , C07K1/34 , C07K14/435 , C07K14/47 , C12P21/06
CPC分类号： C07K14/4702 , A61K38/00 , Y10S530/83
摘要： The invention involves isolating a food intake suppressant by subjecting blood serum to ultrafiltration transmitting up to a molecular weight of 30,000 daltons, partially evaporating the filtrate, removing the insoluble part from the concentrate obtained, adding trichloroacetic acid up to a concentration of 5 to 25 weight/volume percent to the liquid phase at a temperature of 0.degree. to 10.degree. C., removing the proteins precipitated, subjecting the obtained solution to chromatography on a gel with a void volume below a molecular weight of 4000 daltons, eluting with a solution of pH 6.0 to 7.0, concentrating the biologically active fractions, chromatographing again on a gel with a void volume below a molecular weight of 4000 daltons, fractionating by elution with water, lyophilizing the active fractions, dissolving the lyophilized fractions in a buffer of pH 8.1 to 8.2, adding trypsin and chymotrypsin to the solution in a substantially identical amount of 0.01 to 0.2 by weight as calculated for the total weight of the lyophilized product, subjecting the mixture to digestion at a temperature of 36.degree. C. to 39.degree. C., preferably with occasionally shaking from 20 to 30 hours, adding after the first 5 hours trypsin and chymotrypsin in a substantially half amount as calculated for the original enzyme quantity and continuing the digestion, then adding trichloroacetic acid to the reaction mixture up to a concentration of 4 to 6 weight/volume percent at a temperature between 0.degree. and 10.degree. C., keeping the mixture at a temperature between -15.degree. C. and 5.degree. C. for 1 to 24 hours, removing the insoluble part, subjecting the reaction mixture to chromatography on a gel with a void volume below a molecular weight of 4000 daltons, fractionating by elution with water and lyophilizing the biologically active fractions.
摘要翻译：本发明涉及通过使血清进行超滤，分子量为30,000道尔顿，部分蒸发滤液，从所得浓缩物中除去不溶部分，加入高达5至25重量％的三氯乙酸，分离食物摄取抑制剂 /体积％至液相，在0℃至10℃的温度下，除去沉淀的蛋白质，将得到的溶液在孔隙体积低于4000道尔顿的凝胶上进行色谱分离，用浓缩生物活性级分，再次在空白体积低于4000道尔顿的凝胶上进行色谱分离，用水洗脱分级，冻干活性级分，将冻干级分溶解在pH8.1缓冲液中至 8.2，将胰蛋白酶和胰凝乳蛋白酶以基本相同的量加入到溶液中，计算为0.01至0.2重量份 d，冻干产物的总重量，在36℃至39℃的温度下进行消化，优选在20至30小时内偶尔振荡，在第一个5小时后加入胰蛋白酶和胰凝乳蛋白酶基本上为原始酶量计算的一半量并继续消化，然后在0℃和10℃之间的温度下，向反应混合物中加入高达4至6重量/体积百分数的浓度的三氯乙酸，保持混合物在-15℃至5℃的温度下反应1至24小时，除去不溶部分，将反应混合物在空隙体积低于4000道尔顿的凝胶上进行色谱分离，通过用水并冻干生物活性级分。

25. 发明授权

US4564630A Carbamyloxybenzhydrol derivatives and pharmaceutical compositions containing them 失效
标题翻译：氨基甲酰氧基二苯甲醇衍生物和含有它们的药物组合物
公开(公告)号：US4564630A
公开(公告)日：1986-01-14
申请号：US565922
申请日：1983-12-27
申请人： Edit Toth , Jozsef Torley , Istvan Hajdu , Sander Gorog , Andrea Maderspach , Gyorgy Hajos , Laszlo Szporny , Andras Javor
发明人： Edit Toth , Jozsef Torley , Istvan Hajdu , Sander Gorog , Andrea Maderspach , Gyorgy Hajos , Laszlo Szporny , Andras Javor
IPC分类号： A61K31/27 , A61K31/325 , A61P3/06 , C07C67/00 , C07C239/00 , C07C271/08 , C07C271/44 , C07C271/46 , C07C271/56 , C07C271/58 , C07C125/067 , C07C125/075
CPC分类号： A61K31/325
摘要： The invention relates to new carbamyloxybenzhydrol derivatives of the formula (I) ##STR1## wherein R.sub.1 is hydrogen, halogen, trihalomethyl, alkyl having from one to 4 carbon atoms or alkoxy having from one to 4 carbon atoms;R.sub.2 is hydrogen or an R.sub.3 --NH--COO-- group;R.sub.3 is alkyl having from one to 6 carbon atoms, cycloalkyl having up to 7 carbon atoms, or phenyl, optionally substituted with one or more halogen(s).The compounds of the formula (I) show antilipaemic activity and can therefore be used in therapy for treating hyperlipaemia and coronary diseases. Pharmaceutical compositions containing them as active ingredient are also within the scope of the invention.
摘要翻译：本发明涉及式（I）的新的氨基甲酰氧基二苯甲醇衍生物其中R 1是氢，卤素，三卤甲基，具有1至4个碳原子的烷基或具有1至4个碳原子的烷氧基的式（I） R2是氢或R3-NH-COO-基团; R3是具有1至6个碳原子的烷基，具有至多7个碳原子的环烷基，或任选被一个或多个卤素取代的苯基。式（I）的化合物显示抗血脂活性，因此可用于治疗高脂血症和冠状动脉疾病。含有它们作为活性成分的药物组合物也在本发明的范围内。

26. 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。

27. 发明授权

US4450608A Apparatus for producing tempered plate parts 失效
标题翻译：回火板部件的制造装置
公开(公告)号：US4450608A
公开(公告)日：1984-05-29
申请号：US389539
申请日：1982-06-18
申请人： Janos Balazs , Tibor Bano , Arpad Kollar , Tibor Kovacs , Denes Lengyel , Ferenc Mozer
发明人： Janos Balazs , Tibor Bano , Arpad Kollar , Tibor Kovacs , Denes Lengyel , Ferenc Mozer
IPC分类号： B21D43/11 , B23D15/06 , B26D1/09 , C21D1/673 , C21D9/46 , B23P13/00
CPC分类号： B26D1/095 , B21D43/11 , B23D15/06 , C21D1/673 , C21D9/46 , Y10T29/51 , Y10T29/5197
摘要： An apparatus for producing tempered plate spare parts, planar shaped products, shear platus, blades cut from band material, and particularly ampule files, comprises a band hobbing and feeding unit, in certain cases a mechanical forming unit, particularly a serrating and/or sharpening unit, a heating and cooling unit and a cutting mechanism. The apparatus is equipped with a cutting-cooling mechanism arranged on a cross slide that can alternately be displaced crosswise to the transfer trace of the band material and it is provided with pairs of cutting tools arranged in two parallel or approximately parallel--expediently flat--clamp plates that can be pressed to one another.
摘要翻译：一种用于生产回火板备件，平面形状产品，剪切片，从带材切割的刀片，特别是安瓿文件的设备包括带滚动和进给单元，在某些情况下，机械成形单元，特别是锯齿和/或磨削单元，加热和冷却单元以及切割机构。该装置配备有切割冷却机构，该切割冷却机构布置在十字滑道上，其可以交替地与带材的传送轨迹交叉地移动，并且设置有成对的切割工具，其布置成两个平行或大致平行方便的平夹可以彼此挤压的板。

28. 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。

29. 发明授权

US4329341A 5-Phenyl-1,3,4,5-tetrahydro-2H-1,4-benzodiazepin-2-ones, and pharmaceutical compositions containing them 失效
标题翻译： 5-苯基-1,3,4,5-四氢-2H-1,4-苯并二氮杂-2-和含有它们的药物组合物
公开(公告)号：US4329341A
公开(公告)日：1982-05-11
申请号：US178679
申请日：1980-11-26
申请人： Julianna Rochricht , Lajos Kisfaludy , Marton Kajtar , Eva Palosi , Laszlo Szporny
发明人： Julianna Rochricht , Lajos Kisfaludy , Marton Kajtar , Eva Palosi , Laszlo Szporny
IPC分类号： C07D243/24 , A61K31/55
CPC分类号： C07D243/24
摘要： The invention relates to new optically active or racemic 5-phenyl-1,3,4,5-tetrahydro-2H-1,4-benzodiazepin-2-one derivatives of the general formula (I) ##STR1## wherein R.sup.1 stands for hydrogen, halogen, trifluoromethyl or a nitro group;R.sup.2 stands for hydrogen or alkyl having 1 to 6 carbon atoms;R.sup.3 represents a group conventionally attached to the --CH(NH.sub.2)--COOH group of the known optically active or racemic .alpha.-amino-acids, preferably an optionally substituted lower alkyl group;R.sup.4 is hydrogen, chlorocarbonyl or carbamoyl; andX is hydrogen, halogen or trifluoromethyl, with the proviso that if in the racemic compounds R.sup.4 stands for hydrogen R.sup.3 is other than alkyl having 1 to 6 carbon atoms, in which the centers of asymmetry in the 3- and 5-positions have the same absolute configuration, and pharmaceutically acceptable acid addition salts thereof, and a process for their preparation. The new compounds show valuable enzyme inducing activity and can therefore be employed as active ingredients of pharmaceutical compositions, which are also within the scope of the present invention.
摘要翻译：本发明涉及通式（I）的新的光学活性或外消旋的5-苯基-1,3,4,5-四氢-2H-1,4-苯并二氮杂-2-酮衍生物，其中R 1 代表氢，卤素，三氟甲基或硝基; R2代表氢或具有1至6个碳原子的烷基; R3表示通常与已知光学活性或外消旋的α-氨基酸的-CH（NH 2）-COOH基团连接的基团，优选任选取代的低级烷基; R4是氢，氯代羰基或氨基甲酰基; 并且X是氢，卤素或三氟甲基，条件是如果在外消旋化合物中R4代表氢，R3不是具有1至6个碳原子的烷基，其中3-和5-位的不对称中心具有相同的绝对构型及其药学上可接受的酸加成盐及其制备方法。新化合物显示有价值的酶诱导活性，因此可用作药物组合物的活性成分，其也在本发明的范围内。

30. 发明授权

US4298525A Bis-indole-alkaloid 失效
标题翻译：双吲哚生物碱
公开(公告)号：US4298525A
公开(公告)日：1981-11-03
申请号：US61353
申请日：1979-07-27
申请人： Karola Jovanovics , Sandor Gorog
发明人： Karola Jovanovics , Sandor Gorog
IPC分类号： A61K31/475 , A61P35/00 , C07D519/04
CPC分类号： C07D519/04
摘要： A process for the preparation of diindolealkaloids, especially new compounds corresponding to vinblastine or leurosine, in which the N-methyl group is replaced by an N--CH.sub.2 --OC.sub.2 H.sub.5 group having antitumor properties. The starting compounds are subjected to oxidation by chromic acid or an alkali metal dichromate at temperatures from -90.degree. C. to -30.degree. C. but preferably below about -45.degree. C. when the new compounds are to be produced, ethanol being present in this case.
摘要翻译：制备二吲哚类生物碱的方法，特别是对应于长春花碱或亮氨酸的新化合物，其中N-甲基被具有抗肿瘤性质的N-CH 2 -OC 2 H 5基团代替。当待生产新化合物时，起始化合物在-90℃至-30℃的温度下经铬酸或碱金属重铬酸盐氧化，但优选低于约-45℃。在这种情况下。

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