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

US4906622A Optically active 2-chloro-12-(3-dimethylamino-2-methyl-propyl)-12H-dibenzo[d.g] [1,3,6] dioxazocines and a process for the preparation thereof 失效
标题翻译：光学活性的2-氯-12-（3-二甲基氨基-2-甲基 - 丙基）-12H-二苯并[d] [1,3,6]二氧杂吖庚因及其制备方法
公开(公告)号：US4906622A
公开(公告)日：1990-03-06
申请号：US195691
申请日：1988-05-18
申请人： Laszlo Rozsa , Lujza Petocz , Eniko Szirt nee Kiszelly , Peter Tompe , Gabor Gigler
发明人： Laszlo Rozsa , Lujza Petocz , Eniko Szirt nee Kiszelly , Peter Tompe , Gabor Gigler
IPC分类号： A61K31/395 , A61P25/00 , A61P25/16 , C07D273/00 , C07D273/01
CPC分类号： C07D273/00
摘要： The invention relates to optically active 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]dioxazocine of the Formula ##STR1## and pharmaceutically acceptable acid additional salts thereof. The enantiomers are especially active against Parkinsion's disease.The optically active enantiomers are prepared by(a) resolving the racemic 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]-dioxazocine with a optically active organic acid and separating the enantiomers; or(b) dissolving the racemic 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]-dioxazocine in an organic solvent, crystallizing and isolating one of the enantiomers, optionally dissolving additional racemic 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]-dioxazocine in the mother liquor obtained and crystallizing and isolating the other enantiomer, and, if desired, repeating the whole process.
摘要翻译：本发明涉及式（I）的光学活性2-氯代 - 12-（3-二甲基氨基-2-甲基丙基）-12H-二苯并[d，g] [1,3,6]二恶唑辛嗪和药学上其可接受的酸性附加盐。对映异构体对帕金森氏病特别活跃。旋光对映异构体通过以下步骤制备：（a）用光学拆分外消旋的2-氯代 - 12-（3-二甲基氨基-2-甲基丙基）-12H-二苯并[d，g] [1,3,6] 活性有机酸并分离对映异构体; 或（b）将外消旋的2-氯代 - 12-（3-二甲基氨基-2-甲基丙基）-12H-二苯并[d，g] [1,3,6] - 二氧杂吖嗪在有机溶剂中溶解，的对映异构体，任选地将另外的外消旋的2-氯-12-（3-二甲基氨基-2-甲基丙基）-12H-二苯并[d，g] [1,3,6] - 二氧杂吖嗪应用于所获得和结晶的母液中，分离另一个对映体，如果需要，重复整个过程。

2. 发明授权

US4965259A Dioxazocine derivatives compositions and methods containing them having antidepressive, spasmolytic, anticonvulsive, and antiarrhythmic properties 失效
标题翻译：二恶唑辛衍生物组合物和含有它们的方法具有抗抑郁，解痉，抗惊厥和抗心律失常性质
公开(公告)号：US4965259A
公开(公告)日：1990-10-23
申请号：US292450
申请日：1988-12-30
申请人： Laszlo Rozsa , Lujza Petocz , Eniko Szirt nee Kiszelly , Marton Fekete , Maria Szecsey nee Hegedus , Gabor Gigler , Istvan Gacsalyi
发明人： Laszlo Rozsa , Lujza Petocz , Eniko Szirt nee Kiszelly , Marton Fekete , Maria Szecsey nee Hegedus , Gabor Gigler , Istvan Gacsalyi
IPC分类号： A61K31/357 , A61K31/395 , A61P9/06 , A61P21/02 , A61P23/00 , A61P23/02 , A61P25/00 , A61P25/02 , A61P25/08 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , C07D273/00 , C07D273/01
CPC分类号： C07D273/00
摘要： Dioxazocine derivatives, their preparation and composition containing them, said derivatives being represented by the formula I ##STR1## wherein R.sub.1 represents hydrogen or alkyl having from 1 to 4 carbon atoms,R.sub.2 represents alkyl having from 1 to 4 carbon atoms, andn is equal to 0 or 1,and pharmaceutically acceptable acid addition salts thereof formed with an inorganic or organic acid.Two different reactions are described for making these compounds. They can be formulated into pharmaceutical compositions in the usual manner and exhibit central nervous system affecting activities.
摘要翻译：二恶唑辛衍生物及其制备方法和含有它们的组合物，所述衍生物由式I（I）表示，其中R 1表示氢或具有1至4个碳原子的烷基，R 2表示具有1至4个碳原子的烷基，以及 n等于0或1，并且其药学上可接受的酸加成盐与无机或有机酸形成。描述了制备这些化合物的两种不同的反应。它们可以以通常的方式配制成药物组合物，并显示中枢神经系统影响活性。

3. 发明授权

US4208410A Dibenzo[d,g][1,3,6]dioxazocine derivatives 失效
标题翻译：二苯并[d，g] [1,3,6]二氧杂吖庚因衍生物
公开(公告)号：US4208410A
公开(公告)日：1980-06-17
申请号：US927934
申请日：1978-07-25
申请人： Laszlo Rozsa , Lujza Petocz , Katalin Grasser , Ibolya Kosoczky , Eniko Kiszelly , Jozsef Nagy
发明人： Laszlo Rozsa , Lujza Petocz , Katalin Grasser , Ibolya Kosoczky , Eniko Kiszelly , Jozsef Nagy
IPC分类号： A61K31/553 , C07D273/00 , C07D273/01 , C07D267/22 , A61K31/395
CPC分类号： C07D273/00 , Y10S514/818
摘要： This invention relates to novel dibenzo[d,g][1,3,6]dioxazocine derivatives represented by the general formula I ##STR1## wherein R.sub.1 and R.sub.2 independently represent hydrogen, halogen, cyano or trifluoromethyl,Y stands for hydrogen or a group of formula ##STR2## wherein A stands for a straight or branched chained alkylene having from 2 to 5 carbon atoms andR.sub.3 and R.sub.4 independently stand for an alkyl having from 1 to 4 carbon atoms, orR.sub.3 and R.sub.4 together with the nitrogen atom they are attached to and optionally together with a further nitrogen atom or with an additional oxygen atom may form a five- or six-membered heterocyclic ring optionally substituted with an alkyl having from 1 to 4 carbon atoms,and pharmaceutically acceptable acid addition salts thereof formed with an inorganic or organic acid.The above compounds possess valuable pharmaceutical properties, for instance they are effective local anaesthetics and can be used for treating Parkinson syndrome.
摘要翻译：本发明涉及由通式I（I）表示的新的二苯并[d，g] [1,3,6]二氧杂吖庚因衍生物，其中R 1和R 2独立地表示氢，卤素，氰基或三氟甲基，Y代表氢或一组式（I）其中A代表具有2至5个碳原子的直链或支链链状亚烷基，R3和R4独立代表具有1至4个碳原子的烷基，或R3和R4与氮原子一起它们与另外的氮原子或与另外的氧原子连接并且可选地与另外的氧原子连接的原子可以形成任选被具有1至4个碳原子的烷基取代的五元或六元杂环，及其药学上可接受的酸加成盐由无机或有机酸形成。上述化合物具有有价值的药物性质，例如它们是有效的局部麻醉剂，并且可用于治疗帕金森综合征。

4. 发明授权

US4229350A Dibenzo[d,g][1,3,6]dioxazocine derivatives 失效
标题翻译：二苯并[d，g] [1,3,6]二氧杂吖庚因衍生物
公开(公告)号：US4229350A
公开(公告)日：1980-10-21
申请号：US61042
申请日：1979-07-26
申请人： Laszlo Rozsa , Lujza Petocz , Katalin Grasser , Ibolya Kosoczky , Eniko Kiszelly , Jozsef Nagy
发明人： Laszlo Rozsa , Lujza Petocz , Katalin Grasser , Ibolya Kosoczky , Eniko Kiszelly , Jozsef Nagy
IPC分类号： A61K31/553 , C07D273/00 , C07D273/01 , C07D413/06
CPC分类号： C07D273/00 , Y10S514/818
摘要： This invention relates to novel dibenzo[d,g][1,3,6]dioxazocine derivatives represented by the general formula I ##STR1## wherein R.sub.1 and R.sub.2 independently represent hydrogen, halogen, cyano or trifluoromethyl,Y stands for hydrogen or a group of formula ##STR2## wherein A stands for a straight or branched chained alkylene having from 2 to 5 carbon atoms andR.sub.3 and R.sub.4 independently stand for an alkyl having from 1 to 4 carbon atoms, orR.sub.3 and R.sub.4 together with the nitrogen atom they are attached to and optionally together with a further nitrogen atom or with an additional oxygen atom may form a five- or six-membered heterocyclic ring optionally substituted with an alkyl having from 1 to 4 carbon atoms,and pharmaceutically acceptable acid addition salts thereof formed with an inorganic or organic acid.A process for the preparation of these compounds is also within the scope of this invention.The above compounds possess valuable pharmaceutical properties, for instance they are effective local anaesthetics and can be used for treating Parkinson syndrome.
摘要翻译：本发明涉及由通式I（I）表示的新的二苯并[d，g] [1,3,6]二氧杂吖庚因衍生物，其中R 1和R 2独立地表示氢，卤素，氰基或三氟甲基，Y代表氢或一组式（I）其中A代表具有2至5个碳原子的直链或支链链状亚烷基，R3和R4独立代表具有1至4个碳原子的烷基，或R3和R4与氮原子一起它们与另外的氮原子或与另外的氧原子连接并且可选地与另外的氧原子连接的原子可以形成任选被具有1至4个碳原子的烷基取代的五元或六元杂环，及其药学上可接受的酸加成盐由无机或有机酸形成。制备这些化合物的方法也在本发明的范围内。上述化合物具有有价值的药物性质，例如它们是有效的局部麻醉剂，并且可用于治疗帕金森综合征。

5. 发明授权

US4258010A Solvent extraction apparatus 失效
标题翻译：溶剂萃取仪
公开(公告)号：US4258010A
公开(公告)日：1981-03-24
申请号：US849448
申请日：1977-11-07
申请人： Laszlo Rozsa , Lajos Meszaros , Ferenc Mogyorodi
发明人： Laszlo Rozsa , Lajos Meszaros , Ferenc Mogyorodi
IPC分类号： B01D11/04
CPC分类号： B01D11/0449 , C07C68/08
摘要： Apparatus for solvent extraction of a mother liquor with a solvent that is immiscible with and has a different specific gravity than the mother liquor, is disclosed. Means are provided for introducing into an extraction chamber, the solvent, the mother liquor and a carrier gas. Such means simultaneously serve to atomize the solvent and the mother liquor and disperse same in the carrier gas whereby upon introduction a cloud phase is produced in the chamber.The introducing and simultaneously atomizing is carried out through one and the same spray nozzle. Condensation means are arranged in the extraction chamber and function to terminate the cloud phase and produce a condensed extracted mother liquor phase and a condensed solvent phase containing the substance to be extracted. Means are provided for separating the condensed extracted mother liquor phase from the condensed solvent phase on the basis of the different specific gravities of same.
摘要翻译：公开了一种用与母液不混溶且具有不同比重的溶剂溶剂萃取母液的设备。提供用于将萃取室，溶剂，母液和载气引入的装置。这种装置同时用于雾化溶剂和母液并将其分散在载体气体中，由此在引入时在室中产生云相。引入并同时雾化通过同一个喷嘴进行。在提取室中设置冷凝装置，并且起作用以终止浊相，并产生冷凝的提取母液相和含有待提取物质的冷凝溶剂相。提供了用于根据不同的比重将浓缩的萃取母液相与冷凝的溶剂相分离的方法。

6. 发明授权

US3936489A Process and equipment for solvent extraction 失效
标题翻译：溶剂萃取的工艺和设备
公开(公告)号：US3936489A
公开(公告)日：1976-02-03
申请号：US306059
申请日：1972-11-13
申请人： Laszlo Rozsa , Lajos Meszaros , Ferenc Mogyorodi
发明人： Laszlo Rozsa , Lajos Meszaros , Ferenc Mogyorodi
IPC分类号： B01D11/04 , C07C51/48 , C07C68/08
CPC分类号： B01D11/0449
摘要： Process for the solvent extraction of liquids mutually immiscible with each other and having different specific gravity, in which both the mother liquor and the solvent(s) are dispersed in a gas or vapour, thereafter the disperse state of the system is terminated by condensation, and the immiscible phases are separated from each other.
摘要翻译：溶剂萃取相互不混溶并具有不同比重的液体的溶剂萃取方法，其中母液和溶剂都分散在气体或蒸气中，此后系统的分散状态通过冷凝终止，并且不混溶相彼此分离。

7. 发明授权

US4332725A Process for the preparation of 1-[3-mercapto-(2S)-methylpropionyl]-pyrrolidine-(2S)-carboxylic acid 失效
标题翻译：制备1- [3-巯基 - （2S） - 甲基丙酰基] - 吡咯烷 - （2S） - 羧酸的方法
公开(公告)号：US4332725A
公开(公告)日：1982-06-01
申请号：US218814
申请日：1980-12-22
申请人： Janos Fischer , Laszlo Rozsa , Pal Vago , Anna Bakonyi , Gabor Fazekas
发明人： Janos Fischer , Laszlo Rozsa , Pal Vago , Anna Bakonyi , Gabor Fazekas
IPC分类号： A61K31/40 , A61K31/401 , A61P9/12 , C07C53/19 , C07C53/50 , C07D207/16
CPC分类号： C07D207/16 , C07C53/19 , C07C53/50
摘要： The invention relates to a novel process for the preparation of 1-[3-mercapto-(2S)-methylpropionyl]-pyrrolidine-(2S)-carboxylic acid through the N-acylation of L-proline.According to the process of the invention L-proline is acylated with a 3-halogen-2-methylpropionyl chloride of the formula III ##STR1## wherein Hal is a halogen atom, preferably chlorine or bromine, the obtained 1-[3-halogen-(2S)-methylpropionyl]-pyrrolidine-(2S)-carboxylic acid, wherein Hal is as stated above, is reacted with an alkali thiosulfate or alkali trithiocarbonate and the reaction product is hydrolized with an acid.The process of the invention is very economical as compared with the known processes. The desired product is prepared from methacrylic acid in 4 reaction steps with a total yield of 25 percent and from L-proline in 2 reaction steps with a total yield of 30 percent.
摘要翻译：本发明涉及通过L-脯氨酸的N-酰化制备1- [3-巯基 - （2S） - 甲基丙酰基] - 吡咯烷 - （2S） - 羧酸的新方法。根据本发明的方法，L-脯氨酸用式III III的3-卤素-2-甲基丙酰氯酰化，其中Hal是卤素原子，优选氯或溴，得到的1- [3-卤素 - （2S） - 甲基丙酰基] - 吡咯烷 - （2S） - 羧酸（其中Hal如上所述）与碱金属硫代硫酸盐或碱式三硫代碳酸酯反应，反应产物用酸水解。与已知方法相比，本发明的方法是非常经济的。所需产物由甲基丙烯酸在4个反应步骤中制备，总产率为25％，在2个反应步骤中由L-脯氨酸制备，总产率为30％。

8. 发明授权

US3966786A Method for producing chloroformates 失效
标题翻译：氯甲酸酯的制备方法
公开(公告)号：US3966786A
公开(公告)日：1976-06-29
申请号：US221504
申请日：1972-01-28
申请人： Laszlo Rozsa , Lajos Meszaros , Ferenc Mogyorodi
发明人： Laszlo Rozsa , Lajos Meszaros , Ferenc Mogyorodi
IPC分类号： B01J10/00 , C07C68/02
CPC分类号： B01J10/002 , C07C68/02 , B01J2219/00083 , B01J2219/00094
摘要： Various chloroformates are produced from aliphatic, substituted aliphatic, cycloaliphatic, aromatic and arylaliphatic alcohols having up to 20 carbon atoms and of phosgene in a continuous, concurrent flow process, with the alcohol starting material being atomized into the reactor, whereby the reaction takes place largely in the fog phase. The vapor pressure of the phosgene can be utilized for the creation of the fog phase and the termination of the atomized state can be used for efficiently separating the chloroformate end product from the hydrogen chloride by product. The process can be carried out in a reactor comprising a reaction zone, a charged zone and a zone for the recovery of the end product.
摘要翻译：各种氯甲酸酯由具有至多20个碳原子的脂肪族，取代的脂肪族，脂环族，芳香族和芳基脂族醇和光气在连续的同时流动过程中生成，醇原料被雾化到反应器中，由此反应发生在很大程度上在雾化阶段。光气的蒸气压可用于产生雾化相，并且雾化状态的终止可用于通过产物有效地将氯甲酸酯最终产物与氯化氢分离。该方法可以在包含反应区，带电区和回收最终产物的区的反应器中进行。

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