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21. 发明授权

US4921960A Quinoline thioethers 失效
标题翻译：喹啉硫醚
公开(公告)号：US4921960A
公开(公告)日：1990-05-01
申请号：US184796
申请日：1988-04-22
申请人： Jozsef Knoll , Katalin Budai nee Simonyi , Edit Berenyi nee Poldermann , Ildiko Miklya , Marton Fekete , Gabriella Zsilla , Berta Knoll , Attila Mandi , Lujza Petocz , Istvan Gyertyan , Istvan Gacsalyi
发明人： Jozsef Knoll , Katalin Budai nee Simonyi , Edit Berenyi nee Poldermann , Ildiko Miklya , Marton Fekete , Gabriella Zsilla , Berta Knoll , Attila Mandi , Lujza Petocz , Istvan Gyertyan , Istvan Gacsalyi
IPC分类号： A61K31/47 , A61P25/20 , A61P25/22 , C07D215/38
CPC分类号： C07D215/38
摘要： The new compounds of the general Formula I ##STR1## (wherein R.sub.1 stands for C.sub.1-5 alkyl, C.sub.2-5 alkenyl, C.sub.2-5 alkinyl, C.sub.3-7 cycloalkyl or optionally substituted phenyl-(C.sub.1-4 alkyl);R.sub.2 represents hydrogen or C.sub.1-5 alkanoyl;X.sub.1 and X.sub.2 can be identical or different and each stands for hydrogen, halogen, trifluoromethyl or C.sub.1-4 alkoxy;(with the proviso that if R.sub.1 stands for ethyl, at least one of R.sub.2, X.sub.1 and X.sub.2 is different from hydrogen) and pharmaceutically acceptable acid additions salts possess valuable anxiolytic properties devoid of sedative effect and can be used in therapy.The compounds of the general Formula I can be prepared by methods known per se.
摘要翻译：通式Ⅰ的新化合物（Ⅰ）（其中R1代表C1-5烷基，C2-5链烯基，C2-5炔基，C3-7环烷基或任意取代的苯基 - （C 1-4烷基）; R 2表示氢或C 1-5烷酰基; X 1和X 2可以相同或不同，各自表示氢，卤素，三氟甲基或C 1-4烷氧基;（条件是如果R1代表乙基，则R2，X1中的至少一个和X2不同于氢）和药学上可接受的酸加成盐具有不具有镇静作用的有价值的抗焦虑性质，并且可用于治疗。通式I的化合物可以通过本身已知的方法制备。

22. 发明授权

US4921861A Pharmaceutical compositions 失效
标题翻译：药物组合物
公开(公告)号：US4921861A
公开(公告)日：1990-05-01
申请号：US185049
申请日：1988-04-22
申请人： Jozsef Knoll , ne Simonyi; Katalin Budai , Edit Berenyi ne Poldermann , Ildiko Miklya , Marton Fekete , Gabriella Zsilla , Berta Knoll , Attila Mandi , Lujza Petocz , Istvan Gyertyan , Istvan Gacsalyi
发明人： Jozsef Knoll , ne Simonyi; Katalin Budai , Edit Berenyi ne Poldermann , Ildiko Miklya , Marton Fekete , Gabriella Zsilla , Berta Knoll , Attila Mandi , Lujza Petocz , Istvan Gyertyan , Istvan Gacsalyi
IPC分类号： C07D215/38 , A61K31/47 , A61P23/00 , A61P23/02 , A61P25/02 , A61P25/20
CPC分类号： A61K31/47
摘要： The 3-amino-4-ethylthio-quinoline of the Formula I ##STR1## and pharmaceutically acceptable acid addition salts thereof possess useful therapeutical properties. They exhibit a potent and highly selective anxiolytic and narcosis potentiating effect and are devoid of sedative and anti-convulsive effect. Consequently, the invention relates to pharmaceutical compositions comprising the compound of Formula I or a salt thereof as active agent.The invention also relates to a new and improved process for the preparation of the compound of Formula I.
摘要翻译：式I的3-氨基-4-乙硫基 - 喹啉（I）及其药学上可接受的酸加成盐具有有用的治疗性质。它们具有强效和高选择性的抗焦虑和麻醉增效作用，没有镇静和抗惊厥作用。因此，本发明涉及包含式I化合物或其盐作为活性剂的药物组合物。本发明还涉及制备式I化合物的新的和改进的方法。

23. 发明授权

US4904669A Thiazolo/4,5-c/quinolines as major tranquilizers 失效
标题翻译：噻唑醇/ 4,5-c /喹啉为主要镇静剂
公开(公告)号：US4904669A
公开(公告)日：1990-02-27
申请号：US929353
申请日：1986-11-12
申请人： Jozsef Knoll , Edit Berenyi nee Poldermann , Katain Budainee Simonyi , Berta Knoll , Zsuzsa Furts , Julia Timar , Gabriella Zsila , Ildiko Niklya , Lujza Petocz , Attila Mandi
发明人： Jozsef Knoll , Edit Berenyi nee Poldermann , Katain Budainee Simonyi , Berta Knoll , Zsuzsa Furts , Julia Timar , Gabriella Zsila , Ildiko Niklya , Lujza Petocz , Attila Mandi
IPC分类号： A61K31/425 , A61K31/47 , A61K31/4738 , A61P25/22 , A61P25/24 , A61P25/26 , C07D513/04
CPC分类号： C07D513/04
摘要： The invention relates to new thiazolo[4,5-c]quinoline derivatives of the general Formula I ##STR1## and acid addition salts thereof, a process for the preparation of the same and pharmaceutical compositions comprising the said compounds.The substituent definition of the general Formula I is as follows:R stands for hydrogen; a straight or branched chained alkyl group having 2-5 carbon atoms optionally substituted by one or more halogen atom(s); phenyl or phenyl-(lower alkyl) optionally bearing one or more substituent(s) on the phenyl ring;R.sup.1 and R.sup.2 are identical or different and stand for hydrogen, halogen or lower alkyl).The compounds of the general Formula I possess valuable central nervous depressive properties.
摘要翻译：本发明涉及通式I（I）的新的噻唑并[4,5-c]喹啉衍生物及其酸加成盐，其制备方法和包含所述化合物的药物组合物。通式I的取代基定义如下：R代表氢; 任选被一个或多个卤素原子取代的具有2-5个碳原子的直链或支链烷基; 苯基或苯基 - （低级烷基），任选地在苯环上带有一个或多个取代基; R1和R2相同或不同，代表氢，卤素或低级烷基）。通式I的化合物具有有价值的中枢神经抑制性质。

24. 发明授权

US4591524A Chromatographic sheet of layer for pressurized layer chromatographic apparatus 失效
标题翻译：用于加压层色谱仪的色谱层
公开(公告)号：US4591524A
公开(公告)日：1986-05-27
申请号：US285090
申请日：1981-07-15
申请人： Erno Tyihak , Emil Mincsovics , Jozsef Knoll , Sandor Zoltan , Istvan Lak , Peter Tetenyi , Huba Kalasz , Janos Nagy
发明人： Erno Tyihak , Emil Mincsovics , Jozsef Knoll , Sandor Zoltan , Istvan Lak , Peter Tetenyi , Huba Kalasz , Janos Nagy
IPC分类号： G01N31/00 , G01N30/90 , G01N30/92 , G01N30/93 , G01N30/94 , B32B3/02 , B32B3/30
CPC分类号： G01N30/94 , G01N2030/906 , G01N30/90 , Y10T428/24314 , Y10T428/24322 , Y10T428/24331 , Y10T428/24488 , Y10T428/2457 , Y10T428/2462 , Y10T428/24777 , Y10T428/24793 , Y10T428/24843 , Y10T428/24926 , Y10T428/252
摘要： An adsorbent layer (stationary phase) for a pressurized layer chromatographic apparatus, for the development of linear chromatogram, is sealed at the edges by impregnation. For the purpose of solvent control some of the adsorbent material is removed in one or several zones of the adsorbent layer near the place of solvent admission, or one or several baffle plates or wires are arranged behind the place(s) of sample application, or if necessary, the adsorbent layer is provided with a conventionally formed concentration zone in the area of the solvent admission. As a result of the impregnation, the migrating solvent composite does not escape at the edges of the adsorbent layer according to the invention in case of overpressure. As a result of the removal of adsorbent material, or the arrangement of baffles or wires, or the application of a concentration zone, the solvent migrates with a straight-line front.
摘要翻译： PCT No.PCT / HU80 / 00006 Sec。 371日期1981年7月15日 102（e）日期1981年7月15日PCT提交1980年12月5日PCT公布。出版物WO81 / 01746 日期：1981年6月25日。用于开发线性色谱图的用于加压层色谱仪的吸附剂层（固定相）通过浸渍在边缘密封。为了溶剂控制的目的，一些吸附剂材料在吸附剂层的一个或几个区域中被吸附到溶剂进入位置附近，或者一个或多个挡板或导线布置在样品施加位置的后面，或如果需要，吸附剂层在溶剂入口区域中设置有常规形成的浓缩区。作为浸渍的结果，在超压的情况下，迁移溶剂复合材料在本发明的吸附剂层的边缘处不逸出。作为除去吸附剂材料或挡板或导线的布置或应用浓缩区的结果，溶剂以直线前沿迁移。

25. 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。

26. 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）。

27. 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.

28. 发明授权

US4294825A Process for the production of an andrexogenic substance having specific effect on the central regulation of food intake 失效
标题翻译：生产具有对食物摄入中枢调节作用的促发生物质的方法
公开(公告)号：US4294825A
公开(公告)日：1981-10-13
申请号：US68766
申请日：1979-08-23
申请人： Jozsef Knoll , Huba Kalasz , Berta Knoll , Janos Nagy
发明人： Jozsef Knoll , Huba Kalasz , Berta Knoll , Janos Nagy
IPC分类号： C07K14/435 , A23J1/06 , A61K35/14 , A61K35/16 , A61K38/00 , A61K38/16 , A61P3/04 , C07B31/00 , C07B37/00 , C07C67/00 , C07K14/00 , C07K14/47 , A23K1/04 , C07G7/00
CPC分类号： A23J1/06 , C07K14/4702 , A61K38/00
摘要： Described is the method of preparing satietin, a peptide separated from plasma or serum and possessing the effect of inhibiting food intake. Also described is the product satietin.
摘要翻译：描述了制备satietin（一种从血浆或血清中分离出来的肽并具有抑制食物摄入的作用）的方法。还描述了产品satietin。

29. 发明授权

US5151419A Composition for the treatment of schizophrenia 失效
标题翻译：用于治疗精神病药的组合物
公开(公告)号：US5151419A
公开(公告)日：1992-09-29
申请号：US536658
申请日：1990-06-18
申请人： Andras Perenyi , Goswami Utpal , Mihaly Arato , Ede Frescka , Jozsef Knoll , D. Arpad Bela
发明人： Andras Perenyi , Goswami Utpal , Mihaly Arato , Ede Frescka , Jozsef Knoll , D. Arpad Bela
IPC分类号： A61K31/00 , A61K31/135 , A61K31/445 , A61K31/54 , A61P25/18
CPC分类号： A61K31/135
摘要： The present invention is related to a pharmaceutical composition suitable for the treatment of schizophrenia comprising an acid addition salt of (1)-N-(1-phenyl-isopropyl)-N-methyl-1-propynyl-amine in a therapeutically effective amount and optionally one or more neuroleptica and pharmaceutically acceptable carriers, and other excipients.
摘要翻译： PCT No.PCT / HU89 / 00044 Sec。 371 1990年6月18日第 102（e）1990年6月18日PCT PCT 1989年8月17日PCT公布。出版物WO90 / 0192800 1990年3月8日。本发明涉及适用于治疗精神分裂症的药物组合物，其包含（1）-N-（1-苯基 - 异丙基）-N-甲基-1-丙炔基 - 胺和任选的一种或多种神经灵敏剂和药学上可接受的载体，以及其它赋形剂。

30. 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。

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