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1. 发明授权

US5179089A Isoquinoline compounds, compositions and use 失效
标题翻译：异喹啉化合物，组合物和用途
公开(公告)号：US5179089A
公开(公告)日：1993-01-12
申请号：US792255
申请日：1991-11-14
申请人： Kalman Takacs , Iloma Kiss neAjzert , Istvan Hermecz , Janos Ori , Maria H. Pap , Zsolt Bencze , Peter S. Kormoczy , Maria Szabo , Judit Szeredy nee Varga , Csaba Vertesi , Lorand Debreczeni , Jozsef Gaal , Zoltan Kapui
发明人： Kalman Takacs , Iloma Kiss neAjzert , Istvan Hermecz , Janos Ori , Maria H. Pap , Zsolt Bencze , Peter S. Kormoczy , Maria Szabo , Judit Szeredy nee Varga , Csaba Vertesi , Lorand Debreczeni , Jozsef Gaal , Zoltan Kapui
IPC分类号： A61K31/47 , A61K31/33 , A61K31/472 , A61K31/4725 , A61P11/08 , A61P29/00 , A61P37/08 , C07D217/12 , C07D217/16 , C07D217/26
CPC分类号： C07D217/16
摘要： The invention relates to novel compounds of the general formula (I), ##STR1## wherein R means hydrogen or a straight or branched chain C.sub.1-6 alkoxy group;R.sup.1 stands for hydrogen or a straight or branched chain C.sub.1-6 alkyl group;R.sup.2 represents hydrogen or a straight or branched chain C.sub.1-6 alkyl group;R.sup.3 means hydrogen, a straight or branched chain C.sub.1-6 alkyl group optionally substituted by one or two hydroxyl and/or one or two straight or branched chain C.sub.1-4 alkoxy group(s); or a C.sub.4-7 cycloalkyl group;R.sup.4 stands for hydrogen or a straight or branched chain C.sub.1-6 alkyl group optionally substituted by one or two hydroxyl and/or one or two straight or branched chain C.sub.1-4 alkoxy group(s); or a C.sub.4-7 cycloalkyl group; orR.sup.3 and R.sup.4 together with the nitrogen atom, to which they are attached form a 4 to 8-membered cyclic group of formula ##STR2## optionally substituted by one or two straight or branched chain C.sub.1-4 alkoxy and/or one or two straight or branched chain C.sub.1-4 alkyl group(s), where optionally an oxygen or sulfur atom or an N-R.sup.5 group may be substituted for a ring carbon atom, where R.sup.5 means hydrogen or a straight or branched chain C.sub.1-6 aliphatic alkyl group, the 4- to 8-membered cycle optionally being condensed with a benzene ring;R.sup.6 stands for hydrogen or a C.sub.1-10 acyl group and the salts and hydrates thereof as well as pharmaceutical compositions containing these compounds.The compounds of the invention antagonize the effects of constrictive mediators, e.g. histamine, acetylcholine or serotonin; they show an antiallergic action and possess an antiinflammatory effect. Thus, these compounds can therapeutically be used as bronchodilators as well as antiallergic or antiinflammatory drugs, particularly in the treatment of bronchial asthma.

2. 发明授权

US5218117A Process for preparing isoquinoline compounds 失效
标题翻译：异喹啉化合物的制备方法
公开(公告)号：US5218117A
公开(公告)日：1993-06-08
申请号：US951448
申请日：1992-09-25
申请人： Kalman Takacs , Iloma Kiss nee Ajzert , Istvan Hermecz , Janos Ori , Maria H. Pap , Zsolt Bencze , Peter Szekely Kormoczy , Maria Szabo , Judit Szeredy , Csaba Vertesi , Lorand Debreczeni , Jozsef Gaal , Zoltan Kapui
发明人： Kalman Takacs , Iloma Kiss nee Ajzert , Istvan Hermecz , Janos Ori , Maria H. Pap , Zsolt Bencze , Peter Szekely Kormoczy , Maria Szabo , Judit Szeredy , Csaba Vertesi , Lorand Debreczeni , Jozsef Gaal , Zoltan Kapui
IPC分类号： C07D217/16
CPC分类号： C07D217/16
摘要： The invention relates to novel compounds of the general formula (I), ##STR1## The compounds of the invention antagonize the effects of constrictive mediators, e.g. histamine, acetylcholine or serotonin; they show an antiallergic action and possess an antiinflammatory effect. Thus, these compounds can therapeutically be used as bronchodilators as well as antiallergic or antiinflammatory drugs, particularly in the treatment of bronchial asthma.
摘要翻译：本发明涉及通式（I）的新化合物，（I）本发明的化合物拮抗收缩性介质的作用，例如，组胺，乙酰胆碱或5-羟色胺; 它们显示抗过敏作用并具有抗炎作用。因此，这些化合物可以治疗性地用作支气管扩张剂以及抗过敏药或抗炎药，特别是用于治疗支气管哮喘。

3. 发明授权

US5403840A Inclusion complexes of N-ethoxycarbonyl 1-3-morpholino-sydnonimine or salts formed with cyclodextrin-derivatives, preparation thereof and pharmaceutical compositions containing the same 失效
标题翻译： N-乙氧基羰基-3-吗啉代 - 脱水亚胺或与环糊精衍生物形成的盐的包合物，其制备方法和含有它们的药物组合物
公开(公告)号：US5403840A
公开(公告)日：1995-04-04
申请号：US807852
申请日：1992-01-02
申请人： Maria Vikmon , Jozsef Szejtli , Jozsef Gaal , Istvan Hermecz , Agnes Horvath , Katalin Marmarosi , Gabor Horvath , Iren Munkacsi
发明人： Maria Vikmon , Jozsef Szejtli , Jozsef Gaal , Istvan Hermecz , Agnes Horvath , Katalin Marmarosi , Gabor Horvath , Iren Munkacsi
IPC分类号： C07D413/04 , A61K31/41 , A61K31/42 , A61K31/4245 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K47/40 , A61K47/48 , A61P9/08 , A61P9/10 , C07D265/28 , C07D271/04 , C07D271/10 , C08B37/00 , C08B37/06 , C08B37/16 , C06B37/16
CPC分类号： C08B37/0015 , C07D271/04
摘要： The invention relates to inclusion complexes of N-ethoxycarbonyl-3-morpholino-sydnonimine or its salts formed with a cyclodextrin derivatives, preparation thereof and pharmaceutical compositions containing the same.The inclusion complex of N-ethoxycarbonyl-3-morpholino-sydnonimine or its salt formed with cyclodextrin derivative is prepared bya) reacting the N-ethoxycarbonyl-3-morpholino-sydnonimine or its salt and the cyclodextrin derivative in a solvent medium, and if desired recovering the complex from the solution by dehydration, orb) high energy milling of the N-ethoxycarbonyl-3-morpholino-sydnonimine or its salt and the cyclodextrin derivative.
摘要翻译： PCT No.PCT / HU91 / 00012 Sec。 371日期1992年1月2日 102（e）日期1992年1月2日PCT 1991年3月28日PCT公布。公开号WO91 / 14680 日本1991年10月3日。本发明涉及N-乙氧基羰基-3-吗啉代 - 脱水亚胺或其与环糊精衍生物形成的盐的包合络合物，其制备方法和含有它们的药物组合物。通过以下步骤制备N-乙氧基羰基-3-吗啉代 - 脱水亚胺或其与环糊精衍生物形成的盐的包合络合物：a）在溶剂介质中使N-乙氧基羰基-3-吗啉代 - 脱水亚胺或其盐与环糊精衍生物反应，如果需要通过脱水从溶液中回收配合物，或b）N-乙氧基羰基-3-吗啉代 - 脱水亚胺或其盐和环糊精衍生物的高能研磨。

4. 发明授权

US5589513A Pharmaceutical composition and process for the preparation thereof 失效
标题翻译：药物组合物及其制备方法
公开(公告)号：US5589513A
公开(公告)日：1996-12-31
申请号：US256128
申请日：1994-06-17
申请人： Kalman Magyar , Jozsef Gaal , Istvan Sziraki , Jozsef Lengyel , Anna Z. Szabo , Katalin Marmarosi , Istvan Hermecz , Istvan Szatmari , Zoltan Torok , Peter Kormoczy
发明人： Kalman Magyar , Jozsef Gaal , Istvan Sziraki , Jozsef Lengyel , Anna Z. Szabo , Katalin Marmarosi , Istvan Hermecz , Istvan Szatmari , Zoltan Torok , Peter Kormoczy
IPC分类号： A61K45/00 , A61K20060101 , A61K31/135 , A61K31/137 , A61K45/06 , A61P25/24 , A61P25/26 , A61P25/28 , C07C43/00 , C07C205/00 , C07C217/00 , A01N33/02
CPC分类号： A61K31/135
摘要： The invention relates to two phase pharmaceutical compositions comprising as active ingredient a MAO inhibitor and an uptake inhibitor together with usual pharmaceutical auxiliaries. The compositions can be used for the treatment of neurodegenerative diseases. As active ingredient optionally N-(1-phenyl-isopropyl)-N-methyl-propinylamine or N-(4-fluoro-phenyl)-isoprop-1-yl-N-methyl-propinylamine or their salts, optically active isomers or metabolites are used both as MAO inhibitor and as uptake inhibitor.
摘要翻译： PCT No.PCT / HU92 / 00060 Sec。 371日期：1994年6月17日 102（e）日期1994年6月17日PCT提交1992年12月18日PCT公布。公开号WO93 / 12775 PCT 日期：1993年7月8日本发明涉及包含作为活性成分的MAO抑制剂和吸收抑制剂以及通常的药物助剂的两相药物组合物。该组合物可用于治疗神经变性疾病。作为活性成分，任选地N-（1-苯基 - 异丙基）-N-甲基 - 丙烯胺或N-（4-氟 - 苯基） - 异丙基-1-基-N-甲基 - 丙基胺或其盐，旋光异构体或代谢物被用作MAO抑制剂和摄取抑制剂。

5. 发明申请

US20080061520A1 Chuck for Flexible Manufacturing 有权
标题翻译：卡盘灵活制造
公开(公告)号：US20080061520A1
公开(公告)日：2008-03-13
申请号：US11660864
申请日：2005-08-25
申请人： Jozsef Tajnafoi , Jozsef Gaal , Jozsef Kertesz
发明人： Jozsef Tajnafoi , Jozsef Gaal , Jozsef Kertesz
IPC分类号： B23B31/16
CPC分类号： B23B31/16233 , B23B31/16245 , B23B31/16295 , Y10T279/1291 , Y10T279/1966 , Y10T279/1973 , Y10T279/1986 , Y10T279/32 , Y10T279/33
摘要： The invention relates to a chuck for flexible manufacturing, said chuck comprising a chuck body (1), a central drawhead (5) guided axially in a central hole of the chuck body (1) and connected to inner jaws (4) radially guided in the chuck body (1) through a straight-wedge mechanism, and outer jaws (7) also radially guided in the chuck body (1) and adapted to be equipped with chuck jaws for chucking a work-piece and to be engaged with coupling heads (5) through rack toothings (6). The coupling heads (5) are built in the inner jaws (4) and guided axially therein, wherein said coupling heads (5) comprise a double locking coupling device. The first locking stage of said coupling device includes wedge-shaped control members (10) fixed to a control ring (9), whereas the second locking stage includes an additional locking member directly connected to the control ring (9). According to the invention, the chuck body (1) is in the form of a one-piece unit, wherein the control ring (9) is encased by the chuck body (1) and the rear centring disc (12) so that the control ring (9) can be rotated therebetween, and the locking member of the second locking stage is in the form of a cylindrical stud-shaped lock (11) guided in an axial hole (35) of the control ring (9), said lock (11) being connected, in its locked state, through its front surface, to an axially guided push-rod (15), wherein said push-rod (15) is arranged either in an entirely closed hole of the chuck body (1).
摘要翻译：本发明涉及一种用于柔性制造的卡盘，所述卡盘包括卡盘主体（1），在卡盘主体（1）的中心孔中轴向引导并连接到径向引导的内卡爪（4）的中心拉头（5）卡盘主体（1）通过直楔形机构和外卡爪（7）也在卡盘主体（1）中径向引导，并且适于装配有用于夹紧工件的卡盘爪并与联接头（5）通过齿条齿（6）。联接头（5）内置在内爪（4）中并在其中轴向引导，其中所述联接头（5）包括双重锁定联接装置。所述联接装置的第一锁定台包括固定到控制环（9）的楔形控制构件（10），而第二锁定台包括直接连接到控制环（9）的附加锁定构件。根据本发明，卡盘主体（1）为一体式的单元，其中控制环（9）由卡盘体（1）和后定心盘（12）包围，使得控制环（9）可以在其间旋转，并且第二锁定台的锁定构件是在控制环（9）的轴向孔（35）中引导的圆柱形柱形锁（11）的形式，所述锁（11）在其锁定状态下通过其前表面连接到轴向引导的推杆（15），其中所述推杆（15）布置在卡盘主体（1）的完全闭合的孔中，。

6. 发明授权

US5298496A Inclusion complexes of 3-morpholino-sydnonimine or its salts or its tautomer isomer, process for the preparation thereof, and pharmaceutical compositions containing the same 失效
标题翻译： 3-吗啉代 - 脱水亚胺或其盐或其互变异构体的包合物，其制备方法和含有它们的药物组合物
公开(公告)号：US5298496A
公开(公告)日：1994-03-29
申请号：US793389
申请日：1992-01-02
申请人： Maaria Vikmon , Jozsef Szejtli , Lajos Szente , Jozsef Gaal , Hermecz: Istvan , Agnes Horvath , Katalin Marmarosi , Gabor Horvath , Iren Munkacsi
发明人： Maaria Vikmon , Jozsef Szejtli , Lajos Szente , Jozsef Gaal , Hermecz: Istvan , Agnes Horvath , Katalin Marmarosi , Gabor Horvath , Iren Munkacsi
IPC分类号： A61K31/41 , A61K31/4245 , A61K31/535 , A61K31/5375 , A61K47/40 , A61K47/48 , A61P9/08 , A61P9/10 , C07D265/28 , C07D271/04 , C07D295/30 , C07D413/04 , C08B37/00 , C08B37/06 , C08B37/16
CPC分类号： C08B37/0015 , C07D271/04 , Y10S514/821 , Y10S514/969
摘要： The invention relates to inclusion complexes of 3-morpholino-sydnonimine or its salts or its tautomer isomer, process for the preparation thereof and pharmaceutical compositions containing the same.The inclusion complex of 3-morpholino-sydnonimine or its salt formed with cyclodextrin derivative is prepared bya) reacting the 3-morpholino-sydnonimine or its salt in an aqueous medium with a cyclodextrin derivative and the complex is isolated from the solution by dehydratation, orb) high energy milling of 3-morpholino-sydnonimine or its salt and a cyclodextrin derivative.
摘要翻译： PCT No.PCT / HU91 / 00013 Sec。 371日期1992年1月2日 102（e）日期1992年1月2日PCT 1991年3月28日PCT。本发明涉及3-吗啉代 - 脱水亚胺或其盐或其互变异构体的包合物，其制备方法和含有它们的药物组合物。由环糊精衍生物形成的3-吗啉代 - 顺式亚胺或其盐的包合络合物是通过以下步骤制备的：a）使3-吗啉代 - 脱水亚胺或其盐在水性介质中与环糊精衍生物反应，并通过脱水从溶液中分离复合物，或b）3-吗啉代 - 二氢亚胺或其盐和环糊精衍生物的高能研磨。

7. 发明申请

US20090226036A1 SETUP FOR CONSTRUCTING A WEED MAP 有权
标题翻译：建立地毯的设置
公开(公告)号：US20090226036A1
公开(公告)日：2009-09-10
申请号：US12298945
申请日：2006-04-28
申请人： Jozsef Gaal
发明人： Jozsef Gaal
IPC分类号： G06K9/00
CPC分类号： A01M21/04 , A01M7/0089 , E01H11/00 , G06K9/00657 , G06K9/00697
摘要： The present invention relates to a setup (100) for constructing a weed map. The setup (100) comprises an image recording unit (110; 110′) having a video camera (112) and a relief-tracking laser camera (114), an image processing and evaluating unit (120), a data storage unit (130) connected to the latter, as well as a weed database (135). The setup (100) also comprises a light source (160), a position detection unit (150) equipped with a location finding element (152) and a location refining element (154) for determining the spatial coordinates supplied by the former more accurately. The image recording unit (110; 110′), the position detection unit (150) and the light source (160) are all in data communication connection with the image processing and evaluating unit (120). Furthermore, the image processing and evaluating unit (120) is provided with one or more controlling outputs (122, 124), wherein one of the outputs (124) is capable of establishing a data communication connection with the control unit (190) of a separate weeding apparatus.
摘要翻译：本发明涉及一种用于构建杂草地图的装置（100）。该设置（100）包括具有摄像机（112）和浮雕跟踪激光摄像机（114）的图像记录单元（110; 110'），图像处理和评估单元（120），数据存储单元），以及杂草数据库（135）。设置（100）还包括光源（160），配备有位置检测元件（152）的位置检测单元（150）和用于更精确地确定由前者提供的空间坐标的位置精炼元件（154）。图像记录单元（110,110'），位置检测单元（150）和光源（160）都与图像处理和评估单元（120）进行数据通信连接。此外，图像处理和评估单元（120）设置有一个或多个控制输出（122,124），其中输出（124）中的一个能够建立与控制单元（190）的数据通信连接单独除草设备。

8. 发明授权

US5888536A Liposome composition containing selegilin 失效
标题翻译：含有selegilin的脂质体组成
公开(公告)号：US5888536A
公开(公告)日：1999-03-30
申请号：US817433
申请日：1997-08-05
申请人： Michael Mezei , Jozsef Gaal , Gabor Szekacs , Gyula Szebeni , Katalin Marmarosi , Kalman Magyar , Jozsef Lengyel , Istvan Szatmari , Agnes Turi
发明人： Michael Mezei , Jozsef Gaal , Gabor Szekacs , Gyula Szebeni , Katalin Marmarosi , Kalman Magyar , Jozsef Lengyel , Istvan Szatmari , Agnes Turi
IPC分类号： A61K9/127 , A61K31/135 , A61K31/137 , A61K47/42 , A61P25/00 , A61P25/28 , A61K31/13
CPC分类号： A61K31/137 , A61K9/127
摘要： This invention provides liposomic composition, containing as active ingredient (-)-N-.alpha.-dimethyl-N-(2-propynylphenylethylamine) (selegilin) and/or salt thereof. This composition contains: 0.1-40% by weight of selegilin and/or a salt thereof, 2 to 40% by weight of lipids, preferably phospholipids, 0 to 10% by weight of cholesterol, 0 to 20% by weight of an alcohol, 0 to 25% by weight of a glycol, 0 to 3% by weight of an antioxidant, 0 to 3% by weight of a preserving agent, 0 to 2% by weight of a viscosity influencing agent, 0 to 50% by weight of cyclodextrin or a cyclodextrin derivative and 30 to 90% by weight of water. This invention relates to pharmaceutical composition, containing the liposomic composition described and if desired, usual filling and diluting agents and other auxiliaries, preferably in oral, parenteral or transdermal form. This invention provides the process for the preparation of liposomic compositions containing selegilin and/or salt thereof. Accordingly liposomic composition of this invention may be administered for the treatment of Alzheimeir's disease, Parkinson's disease, depression, stroke, motion sickness or myelitis.
摘要翻译： PCT No.PCT / HU95 / 00052 Sec。 371日期：1997年8月5日 102（e）日期1997年8月5日PCT 1995年10月20日PCT PCT。第WO96 / 12472号公报日期：1996年5月2日本发明提供含有作为（ - ） - N-α-二甲基-N-（2-丙炔基苯乙胺）（selegilin）和/或其盐的活性成分的脂质体组合物。该组合物含有：0.1-40重量％的赛莱格林和/或其盐，2〜40重量％的脂质，优选磷脂，0〜10重量％的胆固醇，0〜20重量％的醇， 0〜25重量％的二醇，0〜3重量％的抗氧化剂，0〜3重量％的防腐剂，0〜2重量％的粘度影响剂，0〜50重量％环糊精或环糊精衍生物和30〜90重量％的水。本发明涉及包含所述脂质体组合物和如果需要的通常的填充和稀释剂和其它助剂的药物组合物，优选口服，肠胃外或透皮形式。本发明提供了制备含有塞来昔林和/或其盐的脂质体组合物的方法。因此，本发明的脂质体组合物可以用于治疗阿尔茨海默病，帕金森病，抑郁症，中风，运动病或脊髓炎。

9. 发明授权

US4851416A Berban derivatives as .alpha..sub.2 -adrenergic antagonists 失效
标题翻译： Berban衍生物作为α2-肾上腺素能拮抗剂
公开(公告)号：US4851416A
公开(公告)日：1989-07-25
申请号：US867323
申请日：1986-05-23
申请人： Szilveszter Vizi , Csaba Szantai , Lajos Szabo , Istvan Toth , Gabor Kovacs , Jeno Marton , Laszlo Harsing , Gyorgy Somogyi , Jozsef Gaal
发明人： Szilveszter Vizi , Csaba Szantai , Lajos Szabo , Istvan Toth , Gabor Kovacs , Jeno Marton , Laszlo Harsing , Gyorgy Somogyi , Jozsef Gaal
IPC分类号： C07D453/00 , A61K31/47 , A61P25/02 , A61P25/24 , A61P25/26 , C07D455/03 , C07D471/04
CPC分类号： C07D455/00
摘要： The invention relates to novel racemic or optically active berban derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 represent independently from the other a hydroxyl, straight or branched chain alkoxy group 1 to 6 carbon atoms or R.sup.1 and R.sup.2 together represent a C.sub.1-3 alkylenedioxy group;R.sup.3 and R.sup.4 represent independently from the other hydrogen, straight or branched chain alkyl group, having 1 to 6 carbon atoms and optionally substituted by hydroxyl group, or a C.sub.2-6 alkoxycarbonyl or cyano group; andR.sup.5 represents hydrogen, straight or branched chain alkyl group having 1 to 6 carbon atoms, C.sub.1-7 aliphatic or aromatic acyl group or C.sub.1-7 alkylsulphonyl or arylsulphonyl group, anda salt thereof, to pharmaceutical compositions containing them, to the use as well as to process for preparing the novel compounds. The compounds of the formula (I) are selective .alpha..sub.2 -adrenergic receptor-blocking substances and thus, they may be used for the treament of depressive illnesses.
摘要翻译：本发明涉及式（I）的新型外消旋或光学活性伯类衍生物，其中R 1和R 2彼此独立地表示1至6个碳原子的羟基，直链或支链烷氧基或R1和R2 一起代表C1-3亚烷基二氧基; R3和R4独立地表示独立于具有1-6个碳原子并且任选被羟基取代的另一个氢，直链或支链烷基或C 2-6烷氧羰基或氰基; 并且R 5表示氢，具有1〜6个碳原子的直链或支链烷基，C 1-7脂族或芳族酰基或C 1-7烷基磺酰基或芳基磺酰基及其盐与含有它们的药物组合物以及用于制备新化合物的方法。式（I）化合物是选择性α2-肾上腺素能受体阻断物质，因此可用于抑郁症的治疗。

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