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1. 发明授权

US07858791B2 Process for the preparation of cabergoline 失效
标题翻译：卡麦角林的制备方法
公开(公告)号：US07858791B2
公开(公告)日：2010-12-28
申请号：US10591202
申请日：2005-03-02
申请人： Janos Galambos , Laszlo Czibula , Ferenc Sebök , Sandorné Balint , Ferencné Kassai , Gyorgyi Ignaczné Szendrei , Adam Demeter
发明人： Janos Galambos , Laszlo Czibula , Ferenc Sebök , Sandorné Balint , Ferencné Kassai , Gyorgyi Ignaczné Szendrei , Adam Demeter
IPC分类号： C07D457/04 , C07D457/02
CPC分类号： C07D457/06
摘要： A process for preparing cabergoline (I) from ergoline-8β-carboxylic acid ester (XIII) comprising the following steps. (XIII), (XVI), (XVII), (XVIII), (XIX), (I). The present case also relates to the intermediates (XVI), (XVII), (XVIII) and (XIX) as well as the polymorphic amorphous form of Cabergoline (I) and the production thereof.
摘要翻译：一种从麦角灵八羧酸酯（XIII）制备卡麦角林（I）的方法，包括以下步骤。（XIII），（XVI），（XVII），（XVIII），（XIX），（I）。本例还涉及中间体（XVI），（XVII），（XVIII）和（XIX）以及卡麦角林（I）的多晶型形式及其生产。

2. 发明授权

US07723370B2 1, 2-diaryl pyrazoles useful as analgetic and antiinflammatory agents 失效
标题翻译： 1,1-二芳基吡唑可用作止痛和抗炎剂
公开(公告)号：US07723370B2
公开(公告)日：2010-05-25
申请号：US11989439
申请日：2006-07-27
申请人： János Fischer , Istvánné Kis-Varga , György Szabo , János Leibinger
发明人： János Fischer , Istvánné Kis-Varga , György Szabo , János Leibinger
IPC分类号： A61K31/415 , A61P29/00 , C07D231/12
CPC分类号： C07D231/12
摘要： The present invention relates to new compounds of formula (I), (I) wherein the meaning of R1 is hydrogen atom, C1-C5 acyl group, benzoyl group or R2—COOR3 group, Y is hydrogen atom or alkali ion, R2 is C1-C4 straight or branched alkylidene group and R3 is hydrogen atom, C1-C4 alkyl group or alkali ion, and/or stereoisomers and/or diastereomers and/or pharmaceutically acceptable salts and/or hydrates and/or solvates thereof, which are suitable for the treatment of pain of acute and chronic inflammation origin as well as postoperative pain and dysmenorrhea. The invention also relates to the process of the synthesis of compounds of formula (I) as well as the pharmaceutical composition containing the same and the use for treatment of pain, inflammation and disorders associated with inflammation.
摘要翻译：本发明涉及式（I），（I）的新化合物，其中R1的含义是氢原子，C1-C5酰基，苯甲酰基或R2-COOR3基，Y是氢原子或碱离子，R2是C1 -C4直链或支链亚烷基和R 3是氢原子，C 1 -C 4烷基或碱金属离子，和/或立体异构体和/或非对映异构体和/或其药学上可接受的盐和/或水合物和/或溶剂化物，治疗急性和慢性炎症原因的疼痛以及术后疼痛和痛经。本发明还涉及式（I）化合物的合成方法以及含有该化合物的药物组合物和用于治疗与炎症相关的疼痛，炎症和病症的用途。

3. 发明授权

US07375116B2 Amide derivatives as NMDA receptor antagonists 失效
标题翻译：酰胺衍生物作为NMDA受体拮抗剂
公开(公告)号：US07375116B2
公开(公告)日：2008-05-20
申请号：US11025287
申请日：2004-12-29
申请人： Csilla Horvath , Sandor Farkas , György Domany , Istvan Borza , Gizella Bartane Szalai , Jozsef Nagy , Sandor Kolok
发明人： Csilla Horvath , Sandor Farkas , György Domany , Istvan Borza , Gizella Bartane Szalai , Jozsef Nagy , Sandor Kolok
IPC分类号： A61K31/445 , C07D401/06
CPC分类号： C07D401/06 , A61K31/404 , A61K31/445 , A61K31/4523 , C07D209/42 , C07D211/16 , C07D403/06 , C07D405/06 , C07D409/06 , C07D417/06 , C07D487/04
摘要： Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) where two of the neighboring R1, R2, R3 and R4 groups form an imidazole ring fused to the benzene ring of the indole nucleus, and the other two of R1, R2, R3 and R4 groups are hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a —CH— group, or pharmaceutically acceptable salts thereof formed with acids or bases.
摘要翻译：公开了具有NR2B选择性NMDA受体拮抗剂活性的化合物，其中相邻的R 1，R 2，R 3， R 4和R 4组合形成与吲哚核的苯环稠合的咪唑环，另外两个R 1，R 2， R 3和R 4基团是氢原子，R 5和R 6和它们之间的氮原子一起形成被苯氧基，苯基 - （C 1 -C 4烷基），苯基 - （C 1 -C 4）烷基取代的饱和或不饱和的4-6元杂环， C 1 -C 4烷氧基），苯氧基 - （C 1 -C 4 -C 4烷基）或苯甲酰基，任选在一个或多个卤素原子的芳香环，氰基或羟基，C 1 -C 4 -C 4烷基或C 1 -C 4 烷氧基，X是NH-，Y是-CH-基或其与酸或碱形成的药学上可接受的盐。

4. 发明授权

US07361670B2 Amide derivatives as NMDA receptor antagonists 失效
标题翻译：酰胺衍生物作为NMDA受体拮抗剂
公开(公告)号：US07361670B2
公开(公告)日：2008-04-22
申请号：US11024637
申请日：2004-12-28
申请人： Csilla Horvath , Sandor Farkas , György Domany , Istvan Borza , Gizella Bartane Szalai , Jozsef Nagy , Sandor Kolok
发明人： Csilla Horvath , Sandor Farkas , György Domany , Istvan Borza , Gizella Bartane Szalai , Jozsef Nagy , Sandor Kolok
IPC分类号： A61K31/445 , C07D401/06
CPC分类号： C07D401/06 , A61K31/404 , A61K31/445 , A61K31/4523 , C07D209/42 , C07D211/16 , C07D403/06 , C07D405/06 , C07D409/06 , C07D417/06 , C07D487/04
摘要： Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) wherein one of the neighboring R1, R2, R3 and R4 groups is hydroxy, and the others are each hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a —CH— group, or pharmaceutically acceptable salts thereof formed with acids or bases.
摘要翻译：具有NR2B选择性NMDA受体拮抗剂活性的化合物公开于式（I）中，其中相邻的R 1，R 2，R 3， R 4和R 4各自为羟基，其余各为氢原子，R 5和R 6与它们之间的氮一起形成饱和的或被苯氧基，苯基 - （C 1 -C 4烷基），苯基 - （C 1 -C 4烷基）取代的不饱和的4-6元杂环， / C 1 -C 4烷氧基），苯氧基 - （C 1 -C 4 -C 4烷基）或任选在芳环上被取代的苯甲酰基一个或多个卤素原子，氰基或羟基，C 1 -C 4 -C 4烷基或C 1 -C 4 - N是NH-，Y是-CH-基或其与酸或碱形成的药学上可接受的盐。

5. 发明授权

US07199257B1 Process for the synthesis of N-(4-cyano-3-trifluoromethylphenyl)-3-(4-fluorophenylsulfonyl)-2-hydroxy-2-methylpropionamide 失效
标题翻译：合成N-（4-氰基-3-三氟甲基苯基）-3-（4-氟苯基磺酰基）-2-羟基-2-甲基丙酰胺的方法
公开(公告)号：US07199257B1
公开(公告)日：2007-04-03
申请号：US10030665
申请日：2000-05-26
申请人： Bela Sörös , Zoltan Tuba , György Galik , Adam Bor , Adam Demeter , Ferenc Trischler , Janos Horvath , Janos Brlik
发明人： Bela Sörös , Zoltan Tuba , György Galik , Adam Bor , Adam Demeter , Ferenc Trischler , Janos Horvath , Janos Brlik
IPC分类号： C07C255/50
CPC分类号： C07C253/30 , C07C303/28 , C07C315/02 , C07C319/14 , C07D327/10 , C07C317/46 , C07C255/60 , C07C309/66 , C07C323/60
摘要： A new process is disclosed for the synthesis of racemic or optically pure N-[4-cyano-3-trifluoro-methyl-phenyl]-3[4-fluorophenyl-sulfonyl]-2-hydroxy-2-methylpropionamide. The process includes the formation of several novel intermediates in the synthesis.
摘要翻译：公开了合成外消旋或光学纯的N- [4-氰基-3-三氟 - 甲基 - 苯基] -3 [4-氟苯基 - 磺酰基] -2-羟基-2-甲基丙酰胺的新方法。该方法包括在合成中形成几种新的中间体。

6. 发明授权

US6140336A Spiro[2H-1-benzopyran-2,4'-piperidine]-4(3H)-one derivatives, acid addition salts thereof and pharmaceutical compositions containing them 失效
标题翻译：螺[2H-1-苯并吡喃-2,4'-哌啶] -4（3H） - 酮衍生物，其酸加成盐和含有它们的药物组合物
公开(公告)号：US6140336A
公开(公告)日：2000-10-31
申请号：US973612
申请日：1998-02-12
申请人： Kalman Harsanyi , Istvan Szabadkai , Istvan Borza , Egon Karpati , Bela Kiss , Margit Pellionisz , Sandor Farkas , Csilla Horvath , Katalin Csomor , Erzsebet Lapis , Istvan Laszlowsky , Sandor Szabo , Agnes Kis-Varga , Judit Laszy , Aniko Gere
发明人： Kalman Harsanyi , Istvan Szabadkai , Istvan Borza , Egon Karpati , Bela Kiss , Margit Pellionisz , Sandor Farkas , Csilla Horvath , Katalin Csomor , Erzsebet Lapis , Istvan Laszlowsky , Sandor Szabo , Agnes Kis-Varga , Judit Laszy , Aniko Gere
IPC分类号： C07D491/107 , A61K31/438 , A61K31/445 , A61P25/28 , C07D491/10 , C07D487/10 , A61K31/44
CPC分类号： C07D491/10
摘要： The invention relates to novel spiro[2H-1-benzopyran-2,4'-piperidine]-4(3H)-one derivatives of formula (I), ##STR1## wherein R stands for halogen, nitro group or a straight or branched chain C.sub.1-6 alkyl group, and their acid addition salts, as well as their quaternary salts of formula (Ia) ##STR2## wherein R and R' are the same or different and are identical to the meaning of said (above) R or can mean also hydrogen; and Z represents one equivalent of an anion. The compounds of formulas (I) and (Ia) exert an improving effect on dementias of various pathological origin and accompanying symptoms thereof. Furthermore, the invention relates to a process for the preparation of compounds of formulas (I) and (Ia); to pharmaceutical compositions containing as active gents the above compounds of formulas (I) and (Ia); and to a method of treatment.
摘要翻译： PCT No.PCT / HU97 / 00012 Sec。 371日期1998年2月12日 102（e）日期1998年2月12日PCT 1997年4月3日PCT公布。公开号WO97 / 37630 日期：1997年10月16日本发明涉及式（I）的新的螺[2H-1-苯并吡喃-2,4'-哌啶] -4（3H） - 酮衍生物，其中R代表卤素，硝基或直链或支链C 1-6烷基，以及它们的酸加成盐，以及它们的式（Ia）的季盐，其中R和R'相同或不同并且与所述（上）R或C 也是氢; Z表示1当量的阴离子。式（I）和（Ia）的化合物对各种病理来源及其伴随症状的痴呆发挥改善作用。此外，本发明涉及制备式（I）和（Ia）化合物的方法; 包含上述式（I）和（Ia）化合物作为活性成分的药物组合物; 以及一种治疗方法。

7. 发明授权

US5589486A N-hydroxyalkyl-substituted 1,2,3,6-tetrahydro-pyridine and piperidine derivatives 失效
标题翻译： N-羟基烷基取代的1,2,3,6-四氢 - 吡啶和哌啶衍生物
公开(公告)号：US5589486A
公开(公告)日：1996-12-31
申请号：US244867
申请日：1995-01-17
申请人： Kalman Harsanyi , Tibor Gizur , Eva Agai-Csongor , Anna Kallai-Sohonyai , Marta Kapolnas-Pap , Eva Csizer , Bela Heged us , Laszlo Szporny , Bela Kiss , Egon Karpati , Eva Palosi , Zsolt Szombathelyi , Adam Sarkadi , Aniko Gere , Mihaly Bodo , Katalin Csomor , Judit Laszy , Zsolt Szentirmai , Erzsebet Lapis , Sandor Szabo , Peter Bod , Attila Csehi
发明人： Kalman Harsanyi , Tibor Gizur , Eva Agai-Csongor , Anna Kallai-Sohonyai , Marta Kapolnas-Pap , Eva Csizer , Bela Heged us , Laszlo Szporny , Bela Kiss , Egon Karpati , Eva Palosi , Zsolt Szombathelyi , Adam Sarkadi , Aniko Gere , Mihaly Bodo , Katalin Csomor , Judit Laszy , Zsolt Szentirmai , Erzsebet Lapis , Sandor Szabo , Peter Bod , Attila Csehi
IPC分类号： A61K31/44 , A61K31/445 , A61K31/451 , A61P9/00 , A61P9/08 , A61P9/10 , A61P25/28 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/52 , C07D211/70
CPC分类号： C07D211/52 , C07D211/14 , C07D211/70
摘要： The invention relates to novel N-hydroxy-substituted 1,2,3,6-tetrahydropyridine and piperidine derivatives of the formula ##STR1## wherein A, B, D, E, G, I and R are as defined in the specification, m is 0, 1 or 2, with the proviso that:m is 0 or 2, or both G and I are hydrogen, when A is benzyl or halogen-monosubstituted benzyl group; andm is 1, when A is 2-picolyl, as well as their pharmaceutically acceptable acid addition salts. The compounds of formula (I) are useful for enhancing the tolerance of mammals (including man) against hypoxic and/or ischaemic states as well as for treating the degenerative and functional disturbances arising from hypoxic and/or ischaemic results.
摘要翻译： PCT No.PCT / HU92 / 00050 Sec。 371日期1995年1月17日 102（e）日期1995年1月17日PCT提交1992年12月1日PCT公布。公开号WO93 / 11107 日期：1993年6月10日本发明涉及式（I）的新型N-羟基取代的1,2,3,6-四氢吡啶和哌啶衍生物，其中A，B，D，E，G，I和R m为0,1或2，条件是：当A为苄基或卤素 - 单取代的苄基时，m为0或2，或G和I均为氢。当A为2-吡啶甲基时，m为1，以及其药学上可接受的酸加成盐。式（I）化合物可用于增强哺乳动物（包括人）对缺氧和/或缺血状态的耐受性，以及用于治疗由缺氧和/或缺血结果引起的退行性和功能障碍。

8. 发明授权

US5547949A Steroids with pregnane skeleton, pharmaceutical compositions containing them 失效
标题翻译：具有孕烷骨架的类固醇，含有它们的药物组合物
公开(公告)号：US5547949A
公开(公告)日：1996-08-20
申请号：US351448
申请日：1994-12-08
申请人： Sandor Maho , Zoltan Tuba , Aniko Gere , Pal Vittay , Bela Kiss , Eva Palosi , Laszlo Szporny , Erzsebet C. Francsicsne , Anna M. Boorne , Gabor Balogh , Sandor Gorog
发明人： Sandor Maho , Zoltan Tuba , Aniko Gere , Pal Vittay , Bela Kiss , Eva Palosi , Laszlo Szporny , Erzsebet C. Francsicsne , Anna M. Boorne , Gabor Balogh , Sandor Gorog
IPC分类号： A61K31/57 , A61K31/58 , A61P3/06 , C07D239/42 , C07D239/48 , C07D239/50 , C07D491/10 , C07J20060101 , C07J9/00 , C07J43/00 , A61K31/56
CPC分类号： C07D239/42 , C07D239/48 , C07D239/50 , C07D491/10 , C07J43/003
摘要： Novel, therapeutically active 21-aminosteroids of formula (I) ##STR1## with pregnane skeleton, are disclosed wherein two of X, Y and Z are a nitrogen atom each and the third one is a methine group; R.sup.1 and R.sup.2 are independently from each other, a primary amino group bearing as substituent a branched-chain C.sub.4-8 alkyl -alkenyl or -alkynyl group, or a C.sub.4-10 cycloalkyl group comprising 1 to 3 ring(s) and being optionally substituted by at least one C.sub.1-3 alkyl group; or R.sup.1 and R.sup.2 are each a spiro-heterocyclic secondary amino group containing at most 10 carbon atoms and optionally at least one oxygen atom as additional heteroatom; or one of R.sup.1 and R.sup.2 is an unsubstituted heterocyclic secondary amino group containing 4 to 7 carbon atoms and the other one is an above-identified primary amino group, an above-identified spiro-heterocyclic secondary amino group, or a heterocyclic secondary amino group containing 4 to 7 carbon atoms and substituted by at least one C.sub.1-4 alkyl group; and n is 1 or 2, as well as their acid addition salts and pharmaceutical compositions containing these compounds.
摘要翻译： PCT No.PCT / HU93 / 00035 Sec。 371日期1994年12月8日第 102（e）日期1994年12月8日PCT提交1993年6月8日PCT公布。公开号WO93 / 25570 日期：1993年12月23日公开了具有孕烷骨架的式（I）＆lt; IMAGE＆gt;（I）＆lt; IMAGE＆gt;中的新型治疗活性的21-氨基甾体，其中X，Y和Z中的两个各自为氮原子，次甲基; R1和R2彼此独立地是带有支链C4-8烷基 - 烯基或 - 炔基的取代基的伯氨基或包含1〜3个环的C4-10环烷基，并且任选地被至少一个C 1-3烷基; 或R 1和R 2各自为含有至多10个碳原子的螺杂环仲氨基和任选的至少一个氧原子作为其它杂原子; R 1和R 2中的一个是含有4至7个碳原子的未取代的杂环仲氨基，另一个是上述的伯氨基，上述的螺杂环仲氨基或含有 4至7个碳原子并被至少一个C 1-4烷基取代; 和n为1或2，以及它们的酸加成盐和含有这些化合物的药物组合物。

9. 发明授权

US5198446A Organosilane derivatives, pharmaceutical compositions containing them and process for preparing same 失效
标题翻译：有机衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：US5198446A
公开(公告)日：1993-03-30
申请号：US736962
申请日：1991-07-29
申请人： Sandor Farkas , Sandor Foldeak , Egon Karpati , Peter Hegyes , Janos Kreidl , Laszlo Szporny , Laszlo Czibula , Szilvia Petofi-Vass
发明人： Sandor Farkas , Sandor Foldeak , Egon Karpati , Peter Hegyes , Janos Kreidl , Laszlo Szporny , Laszlo Czibula , Szilvia Petofi-Vass
IPC分类号： A61K31/695 , C07F7/08 , C07F7/10
CPC分类号： C07F7/0812 , C07F7/0818
摘要： A method of treating a mammalian subject for Parkinson's disease or to provide a central muscle relaxant effect, which comprises the step of administering to the mammalian subject in need of the treatment, a therapeutically effective amount of a compound of the Formula (I) ##STR1## wherein m is 1,2 or 3;R.sub.1 and R.sub.2 each independently stand for hydrogen, C.sub.1 to C.sub.4 straight or branched chain alkyl, C.sub.1 to C.sub.4 alkoxy, C.sub.5 to C.sub.7 cycloalkyl, or halogen; andB is a 5- or 6-membered saturated or unsaturated heterocyclic group containing a nitrogen heteroatom, the heterocyclic group being bound through its heterocyclic nitrogen atom to the remainder of the compound, and which can contain one or two additional heteroatoms selected form the group consisting of an oxygen heteroatom, a sulfur heteroatom, and one or two additional nitrogen heteroatoms, which may be as an .dbd.N--, --NH-- or --NR-- group, where R is a C.sub.1 to C.sub.5 alkyl or C.sub.1 to C.sub.5 alkycarbonyl group, the nitrogen-containing heterocyclic group is unsubstituted or substituted on one of its carbon atoms by C.sub.1 to C.sub.4 alkyl or C.sub.1 to C.sub.4 alkoxycarbonyl; or a pharmaceutically acceptable salt thereof.

10. 发明授权

US5194152A Apparatus to contact liquids of different density 失效
标题翻译：接触液体不同密度的装置
公开(公告)号：US5194152A
公开(公告)日：1993-03-16
申请号：US671904
申请日：1991-03-18
申请人： Istvan Takacs , Gyula Beszedics , Gyorgy Fabry , Peter Rudolf
发明人： Istvan Takacs , Gyula Beszedics , Gyorgy Fabry , Peter Rudolf
IPC分类号： B01D11/04
CPC分类号： B01D11/043
摘要： The apparatus has a column (1) of closed interior. Pipe (7b) leading into its upper part to admit liquid of higher density, and pipe (7a) leading into the lower part to admit liquid of lower density. Pipes (8, 10) emerge from the lower part to discharge liquid of higher density, and from its upper part to discharge liquid of lower density. Level control and propelling force adjusting mechanism (9) is connected with the pipe discharging liquid of higher density. Dispersing-mixing elements surrounding cells are beneath and above each other in the column (1). Pulsator (4) is connected with the lower part of column (1). The dispersing-mixing elements are formed by discs (5) having elastic tongues (13a) in the plane of discs capable for vibration and to move out of the disc's plane during vibration, and gap (14) runs along the periphery of the tongues (13a).
摘要翻译： PCT No.PCT / HU90 / 00048 Sec。 371日期1991年3月18日 102（e）1991年3月18日PCT PCT 1990年7月18日PCT公布。 WO91 / 01170 PCT出版物日期1991年2月7日。该装置具有封闭内部的柱（1）。管道（7b）进入其上部以允许较高密度的液体，以及通向下部的管（7a）以允许较低密度的液体。管道（8,10）从下部排出，排出较高密度的液体，从上部排出至较低密度的排出液体。液位控制和推进力调节机构（9）与较高密度的排放管连接。细胞周围的分散混合元件在柱（1）中彼此之下和之上。脉冲器（4）与柱（1）的下部连接。分散混合元件由在振动盘的平面中具有弹性舌片（13a）的盘（5）形成，并且在振动期间从盘的平面移出，并且间隙（14）沿着舌片的周边（ 13a）。

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