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1. 发明授权

US5008386A Methylated cyclodextrin type compounds and process for preparing same 失效
标题翻译：甲基化环糊精型化合物及其制备方法
公开(公告)号：US5008386A
公开(公告)日：1991-04-16
申请号：US256857
申请日：1988-10-12
申请人： Tibor Szabo , Laszlo Institoris , Jozsef Szejtli , Lajos Szente , Ildiko Jodal
发明人： Tibor Szabo , Laszlo Institoris , Jozsef Szejtli , Lajos Szente , Ildiko Jodal
IPC分类号： A61K9/00 , A61K47/40 , A61K47/48 , C08B37/16
CPC分类号： B82Y5/00 , A61K47/40 , A61K47/48969 , A61K9/0019 , C08B37/0012
摘要： The invention relates to novel partially methylated carboxyacyl-cyclodextrins of the general formula (I), ##STR1## wherein A means the cyclodextrin skeleton of the general formula (II) ##STR2## containing the substituents in the position labelled by the wavy line; W stands for an alkylene, alkenylene or arylene group or the substituted derivatives thereof;R means hydrogen, an alkyl, aryl or aralkyl group;m is 6, 7 or 8;n is an integer from 1 to 2m; andp is 2m-n+z, wherein the value of z is from 0 to 3as well as their salts.The novel derivatives induce less haemolytic effect than the cyclodextrin compounds used as starting materials.

2. 发明授权

US4257962A Derivatives of bicyclic lactols 失效
标题翻译：双环乳糖的衍生物
公开(公告)号：US4257962A
公开(公告)日：1981-03-24
申请号：US942819
申请日：1978-09-15
申请人： Tibor Szabo , Laszlo Institoris , Gabor Kovacs , Gyula Dalmadi , Bela Koszegi , Istvan Stadler
发明人： Tibor Szabo , Laszlo Institoris , Gabor Kovacs , Gyula Dalmadi , Bela Koszegi , Istvan Stadler
IPC分类号： C07C405/00 , A61K31/34 , A61K31/343 , A61P7/02 , A61P25/02 , A61P35/00 , C07D307/935
CPC分类号： C07D307/935
摘要： Racemic or optically active compounds with antitumor activity of the formula: ##STR1## wherein X is oxygen or sulfur;R.sup.1 is hydrogen, C.sub.1 to C.sub.4 alkanoyl, benzoyl or phenyl-substituted benzoyl;R.sup.2 is hydrogen or C.sub.1 to C.sub.4 alkanoyl;R.sup.3 is C.sub.2 to C.sub.40 straight or branched chain alkyl substituted by hydroxy, epoxy, amino, C.sub.1 to C.sub.6 alkylamino, C.sub.1 to C.sub.6 dialkylamino, C.sub.1 to C.sub.6 alkanoyloxy or, C.sub.1 to C.sub.4 alkoxycarbonyl; cyclohexyl, phenyl unsubstituted or substituted by halogen, amino, C.sub.1 to C.sub.4 alkyl-substituted amino, C.sub.1 to C.sub.4 alkoxy, nitro, or hydroxy; C.sub.1 to C.sub.6 alkanoyl; allyl or phenyl-C.sub.1 to C.sub.4 alkyl unsubstituted or substituted by a C.sub.2 to C.sub.6 alkene group; or where X is sulfur R.sup.3 is as defined above or is C.sub.1 to C.sub.40 straight or branched chain alkyl; and.about. represents the exo- or endo-steric position in the ring and indicates an .alpha.- or .beta.-steric position in the side chain are disclosed.
摘要翻译：具有下式的抗肿瘤活性的外消旋或光学活性化合物：其中X是氧或硫; R1是氢，C1至C4烷酰基，苯甲酰基或苯基取代的苯甲酰基; R2是氢或C1-C4烷酰基; R3为C2至C40被羟基，环氧基，氨基，C1至C6烷基氨基，C1至C6二烷基氨基，C1至C6烷酰氧基或C1至C4烷氧基羰基取代的直链或支链烷基; 环己基，未取代或被卤素取代的苯基，氨基，C1至C4烷基取代的氨基，C1至C4烷氧基，硝基或羟基; C1至C6烷酰基; 烯丙基或未被取代或被C2至C6烯基取代的苯基-C1至C4烷基; 或其中X为硫的R 3如上所定义或为C 1至C 40直链或支链烷基; 而DIFFERENCE表示环中的外 - 或内 - 立体位置，并且表示侧链中的α或β-甾族位置。

3. 发明授权

US4283413A Method for inhibiting aggregation of human thrombocytes 失效
标题翻译：抑制人凝血细胞聚集的方法
公开(公告)号：US4283413A
公开(公告)日：1981-08-11
申请号：US102649
申请日：1979-12-12
申请人： Tibor Szabo , Laszlo Institoris , Gabor Kovacs , Istvan Stadler , Bela Koszegi
发明人： Tibor Szabo , Laszlo Institoris , Gabor Kovacs , Istvan Stadler , Bela Koszegi
IPC分类号： A61K31/5575 , A61P7/02 , A61P35/00 , C07C405/00 , C07D307/935 , A61K31/34
CPC分类号： C07D307/935 , Y10S514/822
摘要： New compounds and a process for making the same, for use in inhibiting aggregation in human blood and inhibiting the growth of tumors, said compounds being of the general formula: ##STR1## wherein R is hydrogen, alkanoyl, substituted alkanoyl, aralkanoyl or aroyl and represents .alpha. or .beta. steric position or .alpha. and .beta. position, with the provision that if R stands for p-phenyl-benzoyl then methoxy in the position 2 may stand only in .alpha. or only in .beta. steric position.
摘要翻译：新化合物及其制备方法，用于抑制人血液中的聚集和抑制肿瘤的生长，所述化合物具有以下通式：其中R是氢，烷酰基，取代的烷酰基，芳烷酰基或芳酰基并且表示α或β空间位置或α和β位置，条件是如果R表示对苯基苯甲酰，则位置2中的甲氧基可以仅在α或仅在β空间位置。

4. 发明申请

US20080146604A1 Triazolo-Quinolin Derivatives Useful as Adenosine Receptor Ligands 失效
标题翻译：可用作腺苷受体配体的三唑并喹啉衍生物
公开(公告)号：US20080146604A1
公开(公告)日：2008-06-19
申请号：US12039272
申请日：2008-02-28
申请人： Peter Aranyi , Laszlo Balazs , Sandor Batori , Judit Bence , Kinga Boer , Felix Hajdu , Zoltan Kapui , Endre Mikus , Tibor Szabo , Lajos T. Nagy , Geza Timari , Katalin Urban-Szabo , Erzsebet Walcz
发明人： Peter Aranyi , Laszlo Balazs , Sandor Batori , Judit Bence , Kinga Boer , Felix Hajdu , Zoltan Kapui , Endre Mikus , Tibor Szabo , Lajos T. Nagy , Geza Timari , Katalin Urban-Szabo , Erzsebet Walcz
IPC分类号： A61K31/437 , A61P11/06 , A61P11/00 , A61P13/12 , A61P37/00 , A61P35/00
CPC分类号： C07D471/04 , C07D215/54 , C07D215/56
摘要： The present invention relates to adenosine A3 receptor ligands of the general formula (I), within those preferably antagonists, as well as their salts, solvates and isomers, and the pharmaceutical compositions containing them, to the use of the compounds of the general formula (I), as well as their salts, solvates and isomers, to the preparation of the compounds of the general formula (I) and their salts, solvates and isomers, furthermore to the new intermediates of the general formulae (II) and to the preparation thereof.
摘要翻译：本发明涉及通式（I）的腺苷A 3 N 3受体配体，其中优选的是拮抗剂，以及它们的盐，溶剂化物和异构体，以及含有它们的药物组合物的通式（I）化合物及其盐，溶剂合物和异构体制备通式（I）化合物及其盐，溶剂合物和异构体，此外还涉及一般的新的中间体式（II）及其制备方法。

5. 发明授权

US6069269A Process for the preparation of prostaglandin E1 有权
标题翻译：前列腺素E1的制备方法
公开(公告)号：US6069269A
公开(公告)日：2000-05-30
申请号：US91479
申请日：1998-09-18
申请人： Gyula Dalmadi , Felix Hajdu , Istvan Hermecz , Karoly Mozsolits , Tibor Szabo , Zoltan Szeverenyi , Ervin Vajda
发明人： Gyula Dalmadi , Felix Hajdu , Istvan Hermecz , Karoly Mozsolits , Tibor Szabo , Zoltan Szeverenyi , Ervin Vajda
IPC分类号： B01J23/44 , C07B61/00 , C07C405/00 , C07C455/00
CPC分类号： C07C405/00
摘要： New process for the preparation of prostaglandin E1 of formula (I) starting from the compound of formula (II).
摘要翻译： PCT No.PCT / HU96 / 00078 Sec。 371日期：1998年9月18日 102（e）1998年9月18日PCT 1996年12月18日PCT PCT。第WO97 / 22581号公报日期1996年6月26日从式（II）化合物制备式（I）前列腺素E1的新方法。

6. 发明授权

US4820852A Process for the preparation of diacyl-dianhydro hexitols 失效
标题翻译：二酰基二氢己二醇的制备方法
公开(公告)号：US4820852A
公开(公告)日：1989-04-11
申请号：US178876
申请日：1988-03-31
申请人： Tibor Szabo , Ildiko Vidra nee Sandor , Gyula Dalmadi , Judit Kaczmarek nee Sebestyen , Janos ri
发明人： Tibor Szabo , Ildiko Vidra nee Sandor , Gyula Dalmadi , Judit Kaczmarek nee Sebestyen , Janos ri
IPC分类号： C07D303/16 , C07D301/00
CPC分类号： C07D303/16
摘要： The subject of the invention is an improved process for the industrial scale preparation of the compounds of the formula ##STR1## and salts thereof by acylating the hexitols of the formula (II) with an anhydride of the formula (II) at a temperature of 0.degree.-30.degree. C. in the presence of an organic base and a catalyst of the formula (IV) in a dipolar-aprotic or aprotic solvent.
摘要翻译： PCT No.PCT / HU85 / 00002 Sec。 371日期：1985年11月4日 102（e）1985年11月4日，PCT PCT。公开号WO85 / 03293 1985年8月1日。本发明的主题是通过用式（II）的酸酐将式（II）的己醇溶剂酰化来制备式（I）化合物及其盐的工业规模制备的改进方法：式（II）在有机碱存在下，在0-30℃的温度下，在式（Ⅳ）催化剂中，在偶极非质子或非质子传递溶剂中。

7. 发明授权

US08044078B2 Amino-alkyl amide derivatives as CCR3 receptor ligands 失效
标题翻译：氨基 - 烷基酰胺衍生物作为CCR3受体配体
公开(公告)号：US08044078B2
公开(公告)日：2011-10-25
申请号：US12050964
申请日：2008-03-19
申请人： Agnes Pappne Behr , Zoltan Kapui , Peter Aranyi , Sandor Batori , Veronika Bartane Bodor , Lajos T. Nagy , Mihalyne Santa, legal representative , Marton Varga , Endre Mikus , Katalin Urban-Szabo , Judit Vargane Szeredi , Tibor Szabo , Edit Susan , Marianna Kovacs
发明人： Agnes Pappne Behr , Zoltan Kapui , Peter Aranyi , Sandor Batori , Veronika Bartane Bodor , Lajos T. Nagy , Marton Varga , Endre Mikus , Katalin Urban-Szabo , Judit Vargane Szeredi , Tibor Szabo , Edit Susan , Marianna Kovacs
IPC分类号： A61K31/428 , A61K31/165 , A61K31/4184 , A61P31/18 , C07D277/68 , C07D235/26 , C07C233/00
CPC分类号： C07C233/36 , C07D263/58 , C07D277/68 , C07D277/82
摘要： The invention relates to a compound of the general formula (I), as defined herein which is useful for the treatment of a pathology in a patient wherein a CCR3 receptor plays a role in the development of the pathology, and pharmaceutical preparations containing such compound. The invention is also directed to a process for preparing the compound of the general formula (I), and intermediate useful in the preparation.
摘要翻译：本发明涉及如本文所定义的通式（I）化合物，其可用于治疗CCR3受体在病理发展中起作用的患者的病理学，以及含有该化合物的药物制剂。本发明还涉及制备通式（I）化合物和制备中使用的中间体的方法。

8. 发明授权

US07713992B2 Triazolo-quinolin derivatives useful as adenosine receptor ligands 失效
标题翻译：用作腺苷受体配体的三唑并喹啉衍生物
公开(公告)号：US07713992B2
公开(公告)日：2010-05-11
申请号：US12039272
申请日：2008-02-28
申请人： Peter Aranyi , Laszlo Balazs , Sandor Batori , Judit Bence , Kinga Boer , Felix Hajdu , Zoltan Kapui , Endre Mikus , Tibor Szabo , Lajos T. Nagy , Geza Timari , Katalin Urban-Szabo , Erzsebet Walcz
发明人： Peter Aranyi , Laszlo Balazs , Sandor Batori , Judit Bence , Kinga Boer , Felix Hajdu , Zoltan Kapui , Endre Mikus , Tibor Szabo , Lajos T. Nagy , Geza Timari , Katalin Urban-Szabo , Erzsebet Walcz
IPC分类号： A61K31/4355 , A61K31/4196
CPC分类号： C07D471/04 , C07D215/54 , C07D215/56
摘要： The present invention relates to adenosine A3 receptor ligands of the general formula (I), within those preferably antagonists, as well as their salts, solvates and isomers, and the pharmaceutical compositions containing them, to the use of the compounds of the general formula (I), as well as their salts, solvates and isomers, to the preparation of the compounds of the general formula (I) and their salts, solvates and isomers, furthermore to the new intermediates of the general formulae (II) and to the preparation thereof.
摘要翻译：本发明涉及通式（I）的腺苷A3受体配体，其中优选为拮抗剂，以及它们的盐，溶剂化物和异构体，以及含有它们的药物组合物，以及通式 I）以及它们的盐，溶剂合物和异构体，通式（I）的化合物及其盐，溶剂合物和异构体的制备，以及通式（II）的新中间体和制备其中。

9. 发明授权

US07659298B2 Pyrazole derivatives and use thereof as orexin receptor antagonists 有权
标题翻译：吡唑衍生物及其作为食欲素受体拮抗剂的用途
公开(公告)号：US07659298B2
公开(公告)日：2010-02-09
申请号：US11425583
申请日：2006-06-21
申请人： Michel Aletru , Peter Aranyi , Maria Balogh , Sandor Batori , Judit Bence , Philippe Bovy , Zoltan Kapui , Endre Mikus , Claudie Namane , Christophe Philippo , Tibor Szabo , Zsuzsanna Tomoskozi , Katalin Urban-Szabo
发明人： Michel Aletru , Peter Aranyi , Maria Balogh , Sandor Batori , Judit Bence , Philippe Bovy , Zoltan Kapui , Endre Mikus , Claudie Namane , Christophe Philippo , Tibor Szabo , Zsuzsanna Tomoskozi , Katalin Urban-Szabo
IPC分类号： A61K31/4155 , A61K31/44 , C07D231/10 , C07D401/14
CPC分类号： C07D409/04 , C07D231/16 , C07D231/56 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要： The present invention relates to the orexin receptor antagonists compounds of the general formula (I) as well as to their isomers, salts and solvates, to the pharmaceutical compositions containing them and to the therapeutic application thereof.
摘要翻译：本发明涉及食欲素受体拮抗剂通式（I）化合物及其异构体，盐和溶剂合物，其含有它们的药物组合物及其治疗应用。

10. 发明申请

US20080161310A1 FLUOROPYRROLIDINES HAVING DIPEPTIDYL PEPTIDASE ENZYME INHIBITORY ACTIVITY 失效
标题翻译：具有脯氨酸肽酶抑制活性的氟罗哌啶
公开(公告)号：US20080161310A1
公开(公告)日：2008-07-03
申请号：US12042595
申请日：2008-03-05
申请人： Peter Aranyi , Laszlo Balazs , Imre Bata , Sandor Batori , Eva Boronkay , Philippe Bovy , Karoly Kanai , Zoltan Kapui , Edit Susan , Tibor Szabo , Lajos T. Nagy , Katalin Urban-Szabo , Marton Varga
发明人： Peter Aranyi , Laszlo Balazs , Imre Bata , Sandor Batori , Eva Boronkay , Philippe Bovy , Karoly Kanai , Zoltan Kapui , Edit Susan , Tibor Szabo , Lajos T. Nagy , Katalin Urban-Szabo , Marton Varga
IPC分类号： A61K31/53 , C07D239/24 , C07D471/04 , C07D401/04 , C07D251/02 , A61P3/10 , A61K31/506 , A61K31/519 , A61K31/501
CPC分类号： C07D451/04 , C07D207/16 , C07D211/58 , C07D401/04 , C07D401/14 , C07D405/06 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D451/14
摘要： The present invention relates to new, potent DPP-IV enzyme inhibitors of the general formula (I), which contain fluorine atoms.
摘要翻译：本发明涉及含有氟原子的新的具有通式（I）的DPP-IV酶抑制剂。

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