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1. 发明授权

US4564706A Process for the preparation of propargyl amines 失效
标题翻译：炔丙胺的制备方法
公开(公告)号：US4564706A
公开(公告)日：1986-01-14
申请号：US514149
申请日：1983-07-14
申请人： Zoltan Ecsery , Eva Somfai , Judit Hermann nee Voros , Lajos Nagy , Gabor Szabo , Otto Orban , Laslzo Arvai
发明人： Zoltan Ecsery , Eva Somfai , Judit Hermann nee Voros , Lajos Nagy , Gabor Szabo , Otto Orban , Laslzo Arvai
IPC分类号： C07C67/00 , C07C209/00 , C07C209/08 , C07C211/63 , C07C87/28 , C07C85/04
CPC分类号： C07C209/08
摘要： The invention relates to a new process for the preparation of propargyl ammonium chlorides of the Formula I ##STR1## by alkaline decomposition of the d-tartarate of the 1-isomer of an amine of the Formula II ##STR2## and subsequent reaction of the amine of the Formula II with a halide of the Formula IIIX--CH.sub.2 --C.tbd.CH (III)in the presence of an organic solvent, alkali and waterin which in Formulae II and III respectively,n is 1 or 0 andX stands for halogenwhich comprises reacting the d-tartarate of the 1-isomer of an amine of the Formula II in aqueous suspension with an alkali, dissolving the base of the Formula II, thus set free without isolation in a water non-miscible organic solvent and reacting the same in the said phase with a halide of the Formula III, and thereafter--preferably after separating the aqueous layer--reacting the mixture which contains the amines of the Formulae II and IV ##STR3## in the organic phase in the presence of water with an organic acid or a solution which has a pH value of 1.5-6 and consists of an inorganic acid and water, thus dissolving in the two-phase mixture formed the salt of the amine of the Formula II in the aqueous layer and selectively separating the amine of the Formula II from the amine of the Formula IV, and thereafter adding after the separation of the phases hydrogen chloride to the amine of the Formula IV being in the organic phase and thus precipitating the salt of the Formula I.The compounds of Formula I are known pharmaceutical active ingredients. The advantage of the process of the present invention that it is highly economical and enables the recovery of the starting materials on large scale production too.
摘要翻译：本发明涉及通过碱式分解通式II（XIIX）的胺的1-异构体的d-酒石酸来制备式I的炔丙基氯化铵的新方法（I）和随后的式II的胺与式III的X-CH 2 -C 3 CH 3（III）的卤化物在有机溶剂，碱和水的存在下分别反应，其中式II和III分别为n为1 或0和X表示卤素，其包括使式II的胺的1-异构体在水悬浮液中与碱反应，溶解式II的碱，因此在不分离的情况下在水中非游离在所述相中与其反应，与式III的卤化物反应，然后优选在将含有式II和IV的胺的混合物（IV）的水层分离成在有机酸存在下的有机相或pH值为1.5-6且由无机酸和水组成的溶液，因此溶解在两相混合物中形成水性层中式II的胺的盐，并选择性地分离式II的式II化合物，然后在将相氯化氢分离为式IV的胺之后加入有机相，由此沉淀式I的盐。式I的化合物是已知的药用活性成分。本发明方法的优点是高度经济且能够在大规模生产中回收原料。

2. 发明授权

US4162327A N,N-Disubstituted-2-furylethyl amines 失效
标题翻译： N，N-二取代-2-呋喃乙基胺
公开(公告)号：US4162327A
公开(公告)日：1979-07-24
申请号：US754278
申请日：1976-12-27
申请人： Jozsef Knoll , Zoltan Ecsery , Judit Hermann nee Voros , Zoltan Torok , Eva Somfai , Gabor Bernath
发明人： Jozsef Knoll , Zoltan Ecsery , Judit Hermann nee Voros , Zoltan Torok , Eva Somfai , Gabor Bernath
IPC分类号： C07D307/52 , A61K31/34
CPC分类号： C07D307/52
摘要： A compound of the formula ##STR1## or a pharmaceutically effective salt thereof in which R.sup.1 and R.sup.2 are hydrogen or lower alkyl and R.sup.3 is halogenoalkenyl or propinyl. The compounds have pharmacological effects similar to those of phenylethylamine but are free from the amphetamine effect with an excellent therapeutic index and selectivity especially with respect to inhibition of monoaminooxidase.
摘要翻译：其中R 1和R 2为氢或低级烷基且R 3为卤代烯基或丙烯基的式IMA化合物或其药学上有效的盐。该化合物具有与苯乙胺类似的药理作用，但是没有苯丙胺作用，具有优异的治疗指数和选择性，特别是在抑制单氨基氧化酶方面。

3. 发明授权

US4113868A 5,6-Dihydropyrimidin-4(3H)one derivatives, and antiedema compositions and methods employing them 失效
标题翻译： 5,6-DIHYDROPYRIMIDIN-4（3H）一种衍生物，抗微生物组合物及其使用方法
公开(公告)号：US4113868A
公开(公告)日：1978-09-12
申请号：US728459
申请日：1976-09-29
申请人： Gabor Bernath , Lajos Gera , Gyorgy Gondos , Zoltan Ecsery , Judit Hermann nee Voros , Matyas Szentivanyi , Erzsebet Janvari, nee Kanyo
发明人： Gabor Bernath , Lajos Gera , Gyorgy Gondos , Zoltan Ecsery , Judit Hermann nee Voros , Matyas Szentivanyi , Erzsebet Janvari, nee Kanyo
IPC分类号： C07D239/60 , A61K31/505 , A61K31/517 , A61P23/00 , A61P25/04 , A61P29/00 , C07D221/26 , C07D239/70 , C07D239/88 , C07D239/90 , C07D239/91
CPC分类号： C07D239/91 , C07D239/70 , C07D239/88 , C07D239/90
摘要： An antiedema compound of the formula: ##STR1## in which R.sup.1 is methyl, ethyl, cyclohexyl, phenyl, m-tolyl, p-tolyl, p-tert-butylphenyl, m-trifluoromethylphenyl, m-fluorophenyl, p-fluorophenyl, m-chlorophenyl, p-chlorophenyl, m-bromophenyl, p-bromophenyl, o-hydroxyphenyl, p-methoxyphenyl, p-nitrophenyl, benzyl, p-chlorobenzyl, m,p-dimethoxybenzyl, and o-pyridyl;R.sup.2 is hydrogen, p-tolyl, p-ethoxyphenyl, m-pyridyl, methyl or phenyl; andn is 1, 2 or 3And a process for the preparation thereof are disclosed.

4. 发明授权

US5008292A Pesticidal method 失效
标题翻译：杀虫方法
公开(公告)号：US5008292A
公开(公告)日：1991-04-16
申请号：US129342
申请日：1987-11-25
申请人： Zoltan Ecsery , Jozsef Knoll , Eva Somfai , Zoltan Torok , Eva Szinnyei , Karoly Mozsolits
发明人： Zoltan Ecsery , Jozsef Knoll , Eva Somfai , Zoltan Torok , Eva Szinnyei , Karoly Mozsolits
IPC分类号： A61K31/135 , A01N33/04 , A61K20060101 , A61K31/13 , A61K31/137 , A61K31/37 , A61P13/02 , A61P15/00 , A61P25/00 , A61P25/02 , A61P25/24 , A61P25/26 , A61P25/28 , A61P43/00 , C07C20060101 , C07C67/00 , C07C209/00 , C07C209/04 , C07C209/08 , C07C209/16 , C07C209/22 , C07C209/24 , C07C209/28 , C07C209/52 , C07C209/60 , C07C209/68 , C07C209/74 , C07C209/84 , C07C209/88 , C07C211/00 , C07C211/03 , C07C211/27 , C07C211/29 , C07C211/48 , C07F13/00
CPC分类号： C07C211/29
摘要： The invention relates to N-[2-(4-fluorophenyl)-1-methyl]-ethyl-N-methyl-N-propynyl amine of the Formula I ##STR1## and isomers and salts thereof. The compound of the Formula I is useful as an insecticide.

5. 发明授权

US4880833A Synergistic pharmaceutical compositions, their production and use 失效
标题翻译：协同药物组合物，其生产和使用
公开(公告)号：US4880833A
公开(公告)日：1989-11-14
申请号：US908865
申请日：1986-09-12
申请人： Jozsef Knoll , Walter Birkmayer , Katalin Kalloy , Jeno Marton , Zoltan Ecsery
发明人： Jozsef Knoll , Walter Birkmayer , Katalin Kalloy , Jeno Marton , Zoltan Ecsery
IPC分类号： A61K31/135 , A61K31/195 , A61K31/198 , A61P25/00 , A61P25/24 , A61P25/26 , A61P43/00 , C07C229/36
CPC分类号： A61K31/195
摘要： The invention relates to a synergistic pharmaceutical composition, which comprises as an active ingredient a combination of 1-phenylalanine and (-)-deprenyl [(-)-N-(1-phenylisopropyl)-N-methyl-N-propinylamine hydrochloride] and optionally carbidopa [3-(3,4-dihydroxyphenyl)-2-hydrazino-2-methyl-propionic acid monohydrate] or benzerazide [N-(DL-seryl)-N'-( 2,3,4-trihydroxybenzyl)-hydrazine] in association with conventional inert, non-toxic solid or liquid pharamaceutical carriers. The invention further relates to the preparation of these compositions and to the use thereof for the treatment of depressive symptoms.
摘要翻译：本发明涉及一种协同药物组合物，其包含作为活性成分的1-苯丙氨酸和（ - ） - 芴丙基[（ - ） - N-（1-苯基异丙基）-N-甲基-N-丙基胺盐酸盐]和任选的卡比多巴[3-（3,4-二羟基苯基）-2-肼基-2-甲基 - 丙酸一水合物]或苯并氮杂[N-（DL-丝氨酰基）-N' - （2,3,4-三羟基苄基） - 肼 ]与常规的惰性，无毒的固体或液体药物载体相关联。本发明还涉及这些组合物的制备及其用于治疗抑郁症状的用途。

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