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1. 发明授权

US4315861A Process for O-acylating phenol derivatives and acylating compositions for this purpose 失效
标题翻译：用于此目的的O-酰化苯酚衍生物和酰化组合物的方法
公开(公告)号：US4315861A
公开(公告)日：1982-02-16
申请号：US246412
申请日：1981-03-23
申请人： Gyorgy Lugosi , Antal Simay , Janos Bodnar , Istvan Turcsan , Istvan Jelinek , Eva Somfai , Laszlo Simandi
发明人： Gyorgy Lugosi , Antal Simay , Janos Bodnar , Istvan Turcsan , Istvan Jelinek , Eva Somfai , Laszlo Simandi
IPC分类号： C07D307/86 , C07D317/10 , C07C125/067
CPC分类号： C07D307/86
摘要： A process is disclosed for preparing a carbamic acid phenyl ester of the formula (I) ##STR1## wherein R is alkyl having 1 to 8 carbon atoms, aryl, cycloalkyl having 5 or 6 carbon atoms, or aralkyl having 7 to 16 carbon atoms, wherein the aryl, cycloalkyl or aralkyl is unsubstituted or substituted by at least one alkyl group having 1 to 8 carbon atoms;R.sub.1 is hydrogen, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, cyanomethyl, 1,3-dioxolan-2-yl, or carboalkoxyamino wherein the alkoxy group contains 1 to 4 carbon atoms;R.sub.2 is hydrogen, halogen, alkyl having 1 to 4 carbon atoms or alkoxy having 1 to 4 carbon atoms; orR.sub.1 and R.sub.2 form together a carbocyclic ring or a heterocyclic ring fused to the phenyl ring wherein the carbocyclic ring of the heterocyclic ring is unsubstituted or substituted by at least one alkyl having 1 to 8 carbon atoms, which comprises acylating a phenol of the formula (II) ##STR2## with a compound of the formula (IV) ##STR3## in the presence of a base. The compounds obtained are valuable intermediates.
摘要翻译：公开了制备式（I）的氨基甲酸苯酯的方法，其中R是具有1至8个碳原子的烷基，具有5或6个碳原子的芳基，环烷基或具有7至16个碳原子的芳烷基，其中芳基，环烷基或芳烷基是未取代的或被至少一个具有1至8个碳原子的烷基取代; R1是氢，具有1至4个碳原子的烷基，具有1至4个碳原子的烷氧基，氰基甲基，1,3-二氧戊环-2-基或烷氧基氨基，其中烷氧基含有1至4个碳原子; R2是氢，卤素，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; 或者R 1和R 2一起形成稠合到苯环的碳环或杂环，其中杂环的碳环是未取代的或被至少一个具有1至8个碳原子的烷基取代，其包括酰化式（II）的化合物与式（IV）的化合物在碱的存在下反应。所得化合物是有价值的中间体。

2. 发明授权

US4323469A Process for O-acylating phenol derivatives and acylating compositions for this purpose 失效
标题翻译：用于此目的的O-酰化苯酚衍生物和酰化组合物的方法
公开(公告)号：US4323469A
公开(公告)日：1982-04-06
申请号：US201508
申请日：1980-10-28
申请人： Gyorgy Lugosi , Antal S. May , Janos Bodnar , Istvan Turcsan , Istvan Jelinek , Eva Somfai , Laszlo Simandi
发明人： Gyorgy Lugosi , Antal S. May , Janos Bodnar , Istvan Turcsan , Istvan Jelinek , Eva Somfai , Laszlo Simandi
IPC分类号： C07D307/86 , C09K3/00
CPC分类号： C07D307/86
摘要： The invention relates to a process for the preparation of carbamic acid phenyl esters of the formula (I) ##STR1## by acylating phenol derivatives of the formula (II) ##STR2## wherein R is alkyl having 1 to 8 carbon atoms, aryl, cycloalkyl having 5 or 6 carbon atoms, aralkyl having 7 to 16 carbon atoms which groups can be substituted by one or more alkyl groups,R.sup.1 is hydrogen, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms or acylamino,R.sup.2 is hydrogen, halogen, alkyl having 1 to 4 carbon atoms or alkoxy having 1 to 4 carbon atoms, or ifR.sup.1 and R.sup.2 represent alkyl and/or alkoxy, they can form together a carbocyclic ring.According to the invention the phenol derivatives of the general formula (II), wherein R.sup.1 and R.sup.2 are as defined above, are reacted with N-carbamoyl-saccharin derivatives of the formula (IV) ##STR3## wherein R has the same meaning as defined above, in the presence of a base.
摘要翻译：本发明涉及通过酰化式（II）的苯酚衍生物（II）制备式（I）的氨基甲酸苯酯的方法，其中R是具有1至8个碳原子的烷基碳原子，芳基，具有5或6个碳原子的环烷基，具有7至16个碳原子的芳基，该基团可以被一个或多个烷基取代，R 1是氢，具有1至4个碳原子的烷基，具有1至4个碳原子的烷氧基原子或酰氨基，R 2是氢，卤素，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，或者如果R 1和R 2表示烷基和/或烷氧基，则它们可以一起形成碳环。根据本发明，其中R 1和R 2如上定义的通式（II）的酚衍生物与式（Ⅳ）的N-氨基甲酰基 - 糖精衍生物反应其中R具有相同的意义如上所述，在碱的存在下。

3. 发明授权

US4435567A Process for preparing substituted urea derivatives 失效
标题翻译：制备取代脲衍生物的方法
公开(公告)号：US4435567A
公开(公告)日：1984-03-06
申请号：US334470
申请日：1981-12-28
申请人： Gyorgy Lugosi , Antal Simay , Janos Bodnar , Laszlo Simandi , Eva Somfai
发明人： Gyorgy Lugosi , Antal Simay , Janos Bodnar , Laszlo Simandi , Eva Somfai
IPC分类号： C07D295/20 , C07C67/00 , C07C239/00 , C07C273/18 , C07C275/02 , C07C275/06 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07D213/75 , C07D217/06 , C07D235/32 , C07D275/06 , C07D277/82 , C07D285/12 , C07D285/135 , C07D295/215 , C07C127/00 , C07C127/15 , C07C127/17 , C07C127/19
CPC分类号： C07D213/75 , C07C273/1809 , C07D217/06 , C07D235/32 , C07D277/82 , C07D285/135 , C07D295/215
摘要： A process for the preparation of substituted urea derivatives, and compositions and concentrates for the same purpose are disclosed. According to the process the substituted urea derivatives of formula (I) ##STR1## wherein R is hydrogen, alkyl, aryl, cycloalkyl or aralkyl, R.sup.1 and R.sup.2 are hydrogen, alkyl, alkenyl, alkinyl, alkoxy, oxyalkyl, cycloalkyl, aralkyl, alkoxycarbonylalkyl, aryl or heteroaryl, or R.sup.1 and R.sup.2 together with the adjacent nitrogen atom may form a saturated or unsaturated heterocycle, or a condensed and/or substituted ring system, and said heterocycle or said condensed and/or substituted ring system may contain also a sulfo group,can be manufactured by reacting an amine of formula (II) ##STR2## with an N-carbamoyl-benzoic acid sulfimide derivative of formula (III) ##STR3## The disclosed N-acylating composition comprises of from 3 to 60% by weight, preferably of from 5 to 50% by weight sulfimide derivative of formula (III), of from 97 to 40% by weight, preferably of from 95 to 50% by weight solvent, and if desired, an organic or inorganic base.The disclosed N-acylating concentrate comprises of from 60 to 95.5% by weight N-acylating agent of formula (III) and of from 4.5 to 40% by weight additives.
摘要翻译：公开了用于制备取代的脲衍生物的方法，以及用于相同目的的组合物和浓缩物。根据该方法，式（I）的取代脲衍生物其中R是氢，烷基，芳基，环烷基或芳烷基，R1和R2是氢，烷基，烯基，炔基，烷氧基，烷氧基，环烷基，芳烷基，烷氧基羰基，芳基或杂芳基，或R 1和R 2与相邻的氮原子一起可以形成饱和或不饱和的杂环或稠合和/或取代的环系，并且所述杂环或所述缩合和/或取代的环系可以含有磺基可以通过使式（II）的胺与式（III）的N-氨基甲酰基 - 苯甲酸硫酰亚胺衍生物反应来制备。所公开的N-酰化组合物包含3至60重量％，优选为5至50重量％的式（III）的亚磺酰亚胺衍生物，为97至40重量％，优选为95至50重量％的溶剂，如果需要，为有机或无机碱。所公开的N-酰化浓缩物包含60至95.5重量％的式（III）的N-酰化剂和4.5至40重量％的添加剂。

4. 发明授权

US4126615A Process for the manufacture of pure isoquinoline derivatives 失效
标题翻译：制备纯色素衍生物的方法
公开(公告)号：US4126615A
公开(公告)日：1978-11-21
申请号：US748221
申请日：1976-12-07
申请人： Istvan Turcsan , Istvan Jelinek , Jozsef Ugrics , Istvan Csik , Eva Somfai , Iren Csaszar nee Toth
发明人： Istvan Turcsan , Istvan Jelinek , Jozsef Ugrics , Istvan Csik , Eva Somfai , Iren Csaszar nee Toth
IPC分类号： C07C51/08 , C07D217/20
CPC分类号： C07D217/20 , C07C51/08
摘要： In the production of perparine or papaverine and their hydrochlorides, the formation of impurities in the reaction mixture is suppressed by fractionating a 3,4-di-R-benzyl-cyanide in the presence of an organic base (e.g. pyridine, dimethylformamide, ethylenediamine or triethylamine) followed by hydrogenation with a Raney-nickel catalyst treated with aqueous ammonium carbonate solution. R is methoxy or ethoxy.

5. 发明授权

US5220068A Psychostimulant agent 失效
标题翻译：精神刺激剂
公开(公告)号：US5220068A
公开(公告)日：1993-06-15
申请号：US649239
申请日：1991-01-29
申请人： Jozsef Knoll , Antal Simay , Eva Szinnyei , Eva Somfai , Zoltan Torok , Karoly Mozsolits , Janos Bergmann
发明人： Jozsef Knoll , Antal Simay , Eva Szinnyei , Eva Somfai , Zoltan Torok , Karoly Mozsolits , Janos Bergmann
IPC分类号： A61K31/135
CPC分类号： A61K31/135
摘要： The present invention relates to a pharmaceutical composition comprising as active ingredient a compound of the Formula I ##STR1## wherein R.sup.1 stands for straight or branched chain alkyl comprising 1 to 8 carbon atoms; phenyl alkyl having 7 to 10 carbon atoms; phenyl; or cycloalkyl comprising 3 to 8 carbon atoms;R.sup.2 stands for straight or branched chain alkyl comprising 1 to 8 carbon atoms; alkyl comprising 1 to 8 carbon atoms substituted by halogen, hydroxy, alkoxy having 1 to 4 carbon atoms or by one or two phenyl groups; phenyl; or cycloalkyl having 3 to 8 carbon atoms,with the proviso that groups R.sup.1 and R.sup.2 together contain at least three carbon atoms. The invention also relates to a process for the preparation of compounds of the Formula I by methods known per se. The compounds of the Formula I are phychostimulants having a new spectrum of effect which can be used in therapy for increasing psychical activity (learning and retention) and for treating clinical patterns of depression and deficiencies of learning and retention like in Alzheimer's disease, and are void of side effects (e.g. due to catecholamine release) of known stimulants.
摘要翻译：本发明涉及包含作为活性成分的式I化合物（I）的药物组合物，其中R1代表包含1至8个碳原子的直链或支链烷基; 具有7至10个碳原子的苯基烷基; 苯基; 或包含3至8个碳原子的环烷基; R2代表包含1至8个碳原子的直链或支链烷基; 被卤素，羟基，具有1至4个碳原子的烷氧基或一个或两个苯基取代的碳原子数为1〜8的烷基; 苯基; 或具有3至8个碳原子的环烷基，条件是基团R 1和R 2一起含有至少3个碳原子。本发明还涉及通过本身已知的方法制备式I化合物的方法。式I的化合物是具有新的效应谱的phychostimulants，其可用于增加心理活动（学习和保留）的治疗和用于治疗抑郁症的临床模式和学习和保留的缺陷，如阿尔茨海默病，并且是无效的的已知兴奋剂的副作用（例如由于儿茶酚胺释放）。

6. 发明授权

US5075338A Method of treatment of learning deficiency 失效
标题翻译：治疗学习缺陷的方法
公开(公告)号：US5075338A
公开(公告)日：1991-12-24
申请号：US420058
申请日：1989-10-11
申请人： Jozsef Knoll , Antal Simay , Eva Szinnyei , Eva Somfai , Zoltan Torok , Karoly Mozsolits , Janos Bergmann
发明人： Jozsef Knoll , Antal Simay , Eva Szinnyei , Eva Somfai , Zoltan Torok , Karoly Mozsolits , Janos Bergmann
IPC分类号： C07C211/27 , A61K31/135 , A61K31/137 , A61P25/24
CPC分类号： A61K31/135
摘要： A method of treating a learning deficiency is disclosed wherein a patient in need of stimulating learning ability is treated with a therapeutically effective amount of a compound of the Formula (I) ##STR1## wherein R.sup.1 is C.sub.1 to C.sub.8 straight or branched chain alkyl, C.sub.7 to C.sub.10 phenylalkyl, phenyl, or C.sub.3 to C.sub.8 cycloalkyl; andR.sup.2 is C.sub.1 to C.sub.8 straight or branched chain alkyl, unsubstituted or substituted by halogen, hydroxy, C.sub.1 to C.sub.4 alkoxy or by 1 or 2 phenyl groups; or is C.sub.3 to C.sub.8 cycloalkyl;with the proviso that R.sup.1 and R.sup.2 together contain at least 3 carbon atoms; or a pharmaceutically acceptable salt thereof.
摘要翻译：公开了一种治疗学习缺陷的方法，其中需要刺激学习能力的患者用治疗有效量的式（I）化合物（I）治疗，其中R1为C1至C8直链或支链烷基，C7至C10苯基烷基，苯基或C3至C8环烷基; R2为C1至C8直链或支链烷基，未取代或被卤素，羟基，C1至C4烷氧基取代或被1或2个苯基取代; 或为C3至C8环烷基; 条件是R1和R2一起含有至少3个碳原子; 或其药学上可接受的盐。

7. 发明授权

US5389662A Combined compositions 失效
标题翻译：组合成分
公开(公告)号：US5389662A
公开(公告)日：1995-02-14
申请号：US687938
申请日：1991-05-31
申请人： Laszlo Pap , Istvan Szekely , Lajos Nagy , Andras Szego , Andrea Toth , Eva Somfai , Csaba Szantay , Lajos Novak , Laszlo Poppe
发明人： Laszlo Pap , Istvan Szekely , Lajos Nagy , Andras Szego , Andrea Toth , Eva Somfai , Csaba Szantay , Lajos Novak , Laszlo Poppe
IPC分类号： A01N43/30 , A01N43/50 , A01N43/54 , A01N43/653 , A01N47/38 , A01N53/00 , A01N53/02 , A01N53/04 , A01N53/06 , A01N53/08 , A01N53/14 , A01N43/28
CPC分类号： A01N53/00
摘要： The invention relates to novel combined compositions for combatting plant, animal and sanitarian as well as forestry, horticultural and warehouse pests. These compositions contain a pyrethroid-type insecticide as an insecticidally active ingredient and at least one fungicide inhibiting the ergosterol biosynthesis as activity-strengthening agent as well as optionally piperonylbutoxide and other additives.The advantages of the compositions according to the invention consist therein that the activity-strengthening substances used are fungicidal agents widely used and have an advantageous toxicology. The activity-strengthening agent exerts a synergistic effect together with the pyrethroid-type insecticide.The combinations according to the invention bear an outstanding importance in the protection of stored crops.
摘要翻译： PCT No.PCT / HU90 / 00055 Sec。 371日期1991年5月31日 102（e）日1991年5月31日PCT提交1990年7月30日PCT公布。出版物WO91 / 01640 日期1991年2月21日。本发明涉及用于对抗植物，动物和卫生以及林业，园艺和仓库害虫的新型组合物。这些组合物含有拟除虫菊酯型杀虫剂作为杀虫活性成分和至少一种抑制麦角甾醇生物合成作为活性增强剂以及任选的胡椒基丁醚和其它添加剂的杀真菌剂。根据本发明的组合物的优点在于其中使用的活性增强物质是广泛使用的杀真菌剂并且具有有利的毒理学。活性增强剂与拟除虫菊酯类杀虫剂一起发挥协同作用。根据本发明的组合在保存作物方面具有突出的重要性。

8. 发明授权

US5239077A Highly pure amidoximes 失效
标题翻译：高纯度AMIDOXIMES
公开(公告)号：US5239077A
公开(公告)日：1993-08-24
申请号：US602287
申请日：1990-11-09
申请人： Bela Bertok , Istvan Szekely , Angelika Thurna , Lajos Nagy , Eva Somfai , Sandor Bota , Antal Gajary , Kalman Takacs
发明人： Bela Bertok , Istvan Szekely , Angelika Thurna , Lajos Nagy , Eva Somfai , Sandor Bota , Antal Gajary , Kalman Takacs
IPC分类号： C07C259/12 , C07C259/14 , C07C259/16 , C07C259/18 , C07D213/78 , C07D295/088
CPC分类号： C07D213/78 , C07C259/12 , C07D295/088
摘要： The inventions is a purer form of O-(2-hydroxy-3-piperidino-1-propyl)nicotinic acid amidoxime hydrochloride.
摘要翻译： PCT No.PCT / HU90 / 00003 Sec。 371日期1990年11月9日 102（e）1990年11月9日PCT PCT 1990年1月10日PCT公布。公开号WO90 / 08131 日期：1990年7月26日。本发明是O-（2-羟基-3-哌啶-1-基 - 丙基）烟酸偕胺肟盐酸盐的更纯的形式。

9. 发明授权

US5189062A Plant protecting agent 失效
标题翻译：植物保护剂
公开(公告)号：US5189062A
公开(公告)日：1993-02-23
申请号：US827514
申请日：1992-01-28
申请人： Andras Szego , Laszlo Pap , Lajos Nagy , Eva Somfai , Gyorgy Szucsany , Istvan Szekely , Aniko D. nee Molnar , Agnes Hegedus
发明人： Andras Szego , Laszlo Pap , Lajos Nagy , Eva Somfai , Gyorgy Szucsany , Istvan Szekely , Aniko D. nee Molnar , Agnes Hegedus
IPC分类号： A01N25/02
CPC分类号： A01N25/02
摘要： ULV plant protecting arthropodicidal formulation comprising alkyl aryl polyglycol ether as further additives in addition to the active ingredient(s) dissolved in the mixture of alphatic hydrocarbons and sunflower oil. The formulation according to the invention has an initial contact angle on the plant surface of >13.degree., after 20 minutes of >6.degree. and it is often 120 minutes still at least 2.degree..
摘要翻译： ULV植物保护节肢动物杀菌制剂包含烷基芳基聚乙二醇醚作为另外的添加剂，除了溶解在脂肪烃和向日葵油的混合物中的活性成分之外。根据本发明的制剂在> 13°的植物表面上具有初始接触角，20分钟> 6°后，通常为120分钟至少为2℃。

10. 发明授权

US4925878A Method to prevent seasickness 失效
标题翻译：防止晕船的方法
公开(公告)号：US4925878A
公开(公告)日：1990-05-15
申请号：US273851
申请日：1988-08-17
申请人： Gyorgy Bodo , Jozsef Knoll , Eva Somfai , Sandor Virag , Ferenc Zak
发明人： Gyorgy Bodo , Jozsef Knoll , Eva Somfai , Sandor Virag , Ferenc Zak
IPC分类号： A61K31/137 , A23G3/34 , A23G4/00 , A23K1/00 , A23K1/16 , A23L1/00 , A23L2/52 , A61K9/00 , A61K9/20 , A61K31/135 , A61P1/08 , A61P25/00 , C07C211/48
CPC分类号： A61K31/135
摘要： The compounds of the Formula I ##STR1## (wherein R is hydrogen or halogen) and pharmaceutically acceptable acid addition salts thereof are suitable for the prophylaxis of undesired and unfavorable symptoms (e.g. perspiration, nausea, vomiting, dizziness, etc.) which occur when healthy humans or mammal animals are subjected to unusual moving (e.g. during transportation on aeroplane, or vehicles, ships, etc.)
摘要翻译： PCT No.PCT / HU87 / 00058 Sec。 371日期1988年8月17日 102（e）日期1988年8月17日PCT提交1987年12月18日PCT公布。公开号WO88 / 04552 日本时间：1988年6月30日。式I化合物（I）（其中R是氢或卤素）及其药学上可接受的酸加成盐适用于预防不良和不利症状（例如出汗，恶心，当健康的人类或哺乳动物受到异常移动时（例如在飞机或车辆，船舶等运输过程中发生的情况，发生呕吐，眩晕等）

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