专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

21. 发明授权

US5716986A Oxaindene derivatives and process for the preparation thereof 失效
标题翻译：氧化烯衍生物及其制备方法
公开(公告)号：US5716986A
公开(公告)日：1998-02-10
申请号：US671515
申请日：1996-06-27
申请人： Csaba Szantay , Lajos Novak , Peter Kovacs , Klara Gado , Gabor Gigler , Julianna Takacs nee Bitai , Andras Egyed , Daniel Bozsing , Gyorgy Pirok , Katalin Szemeredi , Margit Csorgo , Sandor Drabant , Gabor Blasko , Gyula Simig , Gabor Kovacs
发明人： Csaba Szantay , Lajos Novak , Peter Kovacs , Klara Gado , Gabor Gigler , Julianna Takacs nee Bitai , Andras Egyed , Daniel Bozsing , Gyorgy Pirok , Katalin Szemeredi , Margit Csorgo , Sandor Drabant , Gabor Blasko , Gyula Simig , Gabor Kovacs
IPC分类号： C07D307/79 , A61K31/34 , A61K31/343 , A61K31/445 , A61K31/535 , A61P1/00 , A61P13/02 , A61P15/00 , A61P17/00 , A61P29/00 , A61P37/08 , C07D307/91 , C07D307/93
CPC分类号： C07D307/91 , C07D307/93
摘要： This invention relates to new oxaindene derivatives, a process for the preparation thereof and pharmaceutical compositions comprising the same. The compounds according to the invention are characterized by the general formula (1) ##STR1## wherein R.sup.1 represents lower C.sub.1-4 alkyl, lower C.sub.1-4 alkoxy or lower C.sub.3-6 cycloalkyl, R.sup.2 stands for hydrogen, lower C.sub.1-4 alkyl or lower C.sub.3-6 cycloalkyl, R.sup.3 stands for hydrogen, lower C.sub.1-4 alkyl, lower C.sub.1-4 alkoxy or benzyloxy, X denotes hydrogen, an aliphatic C.sub.1-4 -acyl or benzoyl or naphthoyl group, optionally substituted by 1 or more nitro or C.sub.1-4 -alkoxy group(s) or a group of the formula R.sup.5 R.sup.6 N--R.sup.7 --, wherein R.sup.7 represents lower C.sub.1-4 alkylene and R.sup.5 and R.sup.6 each represent lower C.sub.1-4 alkyl, or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached form a piperidyl or morpholinyl group, A and B together form an ethylene or a vinylene group, and n is 1, 2 or 3, and have a strong 5-lipoxygenase (5-LO) enzyme inhibiting activity.
摘要翻译：本发明涉及新的氧杂茚衍生物，其制备方法和包含其的药物组合物。根据本发明的化合物的特征在于通式（1）其中R 1表示低级C 1-4烷基，低级C 1-4烷氧基或低级C 3-6环烷基，R 2表示氢，低级C 1〜 4烷基或低级C3-6环烷基，R3代表氢，低级C1-4烷基，低级C1-4烷氧基或苄氧基，X表示氢，脂族C1-4酰基或苯甲酰基或萘甲酰基，任选被1或更多的硝基或C 1-4 - 烷氧基或式R 5 R 6 N-R 7 - 的基团，其中R 7表示低级C 1-4亚烷基，R 5和R 6各自表示低级C 1-4烷基，或者R 5和R 6连同它们所连接的氮原子形成哌啶基或吗啉基，A和B一起形成乙烯或亚乙烯基，n为1,2或3，具有强的5-脂氧合酶（5-LO）酶抑制活性。

22. 发明授权

US5597822A Pharmaceutical compositions for the prevention and/or treatment a gastrointestinal diseases 失效
标题翻译：用于预防和/或治疗胃肠道疾病的药物组合物
公开(公告)号：US5597822A
公开(公告)日：1997-01-28
申请号：US443487
申请日：1995-05-18
申请人： Eniko Szirt nee Kislelly , Zoltan Budai , Tibor Mezei , Gabor Blasko , Klara Kazo nee Daroczi , Andras Egyed , Gabor Gigler , Marton Fekete , Klara Reiter nee Esses , Gyula Simig , Katalin Szemeredi
发明人： Eniko Szirt nee Kislelly , Zoltan Budai , Tibor Mezei , Gabor Blasko , Klara Kazo nee Daroczi , Andras Egyed , Gabor Gigler , Marton Fekete , Klara Reiter nee Esses , Gyula Simig , Katalin Szemeredi
IPC分类号： A61K31/15 , A61K31/495 , A61K31/50 , A61K31/505
CPC分类号： A61K31/15 , A61K31/495
摘要： The invention refers to pharmaceutical compositions for the prevention and/or treatment of gastrointestinal diseases connected with infections caused by Helicobacter pylori and a method for the treatment of such diseases.The pharmaceutical composition of the invention comprises as active ingredient a cyclic ketone derivative of the formula I ##STR1## wherein and R.sup.1 mean independently hydrogen or halo;R.sup.0 stands for hydrogen or a C.sub.1-4 alkoxy group;R.sup.2 and R.sup.3 independently represent hydrogen; a straight or branched chain C.sub.1-8 alkyl optionally substituted by a dimethylamino group; a C.sub.2-6 alkenyl or a C.sub.3-7 cycloalkyl group; orR.sup.2 and R.sup.3 together with the adjacent nitrogen atom form a 6-membered heterocyclic group containing an additional nitrogen atom that may bear a phenyl group optionally substituted by a C.sub.1-4 alkoxy group;or its stereoisomer or optical isomer or a possible mixture thereof, or a pharmaceutically acceptable acid addition salt or quaternary ammonium salt thereof in admixture with carrier(s) commonly used in pharmaceutical compositions.
摘要翻译：本发明涉及用于预防和/或治疗与由幽门螺杆菌引起的感染有关的胃肠道疾病的药物组合物和治疗这些疾病的方法。本发明的药物组合物包含作为活性成分的式I（I）的环酮衍生物，其中R 1独立地表示氢或卤素; R0表示氢或C1-4烷氧基; R2和R3独立地表示氢; 任选被二甲基氨基取代的直链或支链C 1-8烷基; C 2-6烯基或C 3-7环烷基; 或者R 2和R 3与相邻的氮原子一起形成含有另外的氮原子的6元杂环基，其可以具有任选被C 1-4烷氧基取代的苯基; 或其立体异构体或光学异构体或其可能的混合物，或其药学上可接受的酸加成盐或季铵盐与药物组合物中通常使用的载体混合。

23. 发明授权

US5240918A 2-(substituted imino)-thiazolidines and process for the preparation thereof 失效
标题翻译： 2-（取代的亚氨基） - 噻唑啉及其制备方法
公开(公告)号：US5240918A
公开(公告)日：1993-08-31
申请号：US857067
申请日：1992-03-24
申请人： Karoly Lempert , Gyula Hornyak , Jozsef Fetter , Antal Feller , Klara Gaso , Gabor Gigler , Laszlo Kapolnai , Lujza Petocz , Katalin Szemeredi , Marton Fekete
发明人： Karoly Lempert , Gyula Hornyak , Jozsef Fetter , Antal Feller , Klara Gaso , Gabor Gigler , Laszlo Kapolnai , Lujza Petocz , Katalin Szemeredi , Marton Fekete
IPC分类号： C07D277/18
CPC分类号： C07D277/18
摘要： The invention relates to new 2-(substituted imino)-thiazolidines, a process for the preparation thereof, pharmaceutical compositions comprising the same, the use of the said 2-(substituted imino)thiazolidines for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases.The new 2-(substituted imino)-thiazolidine derivatives provided by the present invention correspond to the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 each represent halogen, nitro, C.sub.1-4 alkoxy or C.sub.1-4 alkyl, which latter may optionally carry one or more halogen substituent(s),R.sup.3 and R.sup.4 each represent hydrogen or C.sub.1-4 alkyl,Z denotes oxygen, sulfur or imino, which latter is substituted by a C.sub.1-6 alkyl or a C.sub.1-6 alkenyl group,R.sup.5 stands for hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkylthio or a group or the formula --NH--R, wherein R represents C.sub.1-6 alkyl, aryl, aralkyl or C.sub.1-6 alkenyl optionally carrying a halogen or a di-(C.sub.1-4 alkyl)-amino substituent; orZ and R.sup.5 together stand for a trivalent nitrogen atom, with the proviso that if Z denotes a substituted imino group, R.sup.5 stands for C.sub.1-4 alkylthio, and if R.sup.5 is C.sub.1-4 alkylthio, Z represents a substituted imino, and with the further proviso that if Z denotes sulfur, R.sup.5 is other than hydrogen or C.sub.1-4 alkyl,and possess valuable antianginal and analgesic properties.
摘要翻译：本发明涉及新的2-（取代的亚氨基） - 噻唑烷，其制备方法，包含该方法的药物组合物，所述2-（取代的亚氨基）噻唑烷用于治疗疾病和用于制备药物适用于治疗疾病的组合物。本发明提供的新的2-（取代亚氨基） - 噻唑烷衍生物对应于通式（I），其中R 1和R 2各自表示卤素，硝基，C 1-4烷氧基或C 1-4烷基，其可以任选地带有一个或多个卤素取代基，R 3和R 4各自表示氢或C 1-4烷基，Z表示氧，硫或亚氨基，后者被C 1-6烷基或C 1-6 烯基，R5代表氢，C1-4烷基，C1-4烷硫基或基团-NH-R，其中R表示C1-6烷基，芳基，芳烷基或任选携带卤素或二（C 1-4烷基） - 氨基取代基; 或Z和R5一起代表三价氮原子，条件是如果Z表示取代的亚氨基，则R5表示C1-4烷硫基，如果R5是C1-4烷硫基，则Z表示取代的亚氨基，并且与进一步的条件是，如果Z表示硫，R5不是氢或C1-4烷基，并且具有有价值的抗心绞痛和止痛特性。

24. 发明授权

US07053082B1 2,3-benzodiazepine derivatives 失效
公开(公告)号：US07053082B1
公开(公告)日：2006-05-30
申请号：US10030436
申请日：2000-07-04
申请人： Zoltan Greff , Geza Szabo , Jozsef Barkoczy , Zoltan Ratkai , Gabor Blasko , Gyula Simig , Gabor Gigler , Bernadett Martonné Marko , György Levay , Karoly Tihanyi , Andras Egyed , Annamaria Simo
发明人： Zoltan Greff , Geza Szabo , Jozsef Barkoczy , Zoltan Ratkai , Gabor Blasko , Gyula Simig , Gabor Gigler , Bernadett Martonné Marko , György Levay , Karoly Tihanyi , Andras Egyed , Annamaria Simo
IPC分类号： A61P25/00 , A61K31/551 , C07D491/04
CPC分类号： C07D491/04
摘要： The invention relates to new 2,3-benzodiazepine derivatives of general Formula (I), (wherein R1 stands for methyl, formyl, carboxy, cyano, —CH═NOH, —CH═NNHCONH2 or —NR5R6, wherein R5 and R6 independently from each other represent hydrogen or lower alkyl or together with the nitrogen atom, they are attached to, form a 5- or 6-membered, saturated or unsaturated heterocyclic ring optionally containing one or more further nitrogen, sulfur and/or oxygen atom(s); R2 is nitro or amino; R3 stands for hydrogen, lower alkanoyl or CO—NR7R8, wherein R7 and R8 independently from each other stand for hydrogen, lower alkoxy, lower alkyl or lower cycloalkyl or together with the nitrogen atom, they are attached to, form a 5- or 6-membered, saturated or unsaturated heterocyclic ring optionally containing one or more further nitrogen, sulfur and/or oxygen atom(s); R4 is hydrogen or lower alkyl; the dotted lines have the following meaning: if R3 and R4 are not present, the bond between positions C8 and C9 is a single bond and the bond between positions C8 and N7 is a double bond; if R3 and R4 are present, the bonds between positions C8 and C9 and between position C8 and N7 are single bonds; and if R3 is present and R4 is missing, the bond between positions C8 and C9 is a double bond and the bond between positions C8 and N7 is a single bond) and salts thereof. The invention compounds have neuroprotective effect.

25. 发明授权

US5130487A Aminopropanol derivatives, process for their preparation and pharmaceutical compositions comprising the same 失效
标题翻译：氨基壬酸衍生物，其制备方法和包含其的药物组合物
公开(公告)号：US5130487A
公开(公告)日：1992-07-14
申请号：US572641
申请日：1991-08-27
申请人： Zoltan Budai , Tibor Mezei , Klara Reiter nee Esses , Eniko Sziri neKiszelly , Gizella Zsila , Gabor Gigler , Lujza Petocz , Maria Szecsey nee Hegedus , Marton Fekete , Valeria Hoffmann , Laszlo Kapolnai
发明人： Zoltan Budai , Tibor Mezei , Klara Reiter nee Esses , Eniko Sziri neKiszelly , Gizella Zsila , Gabor Gigler , Lujza Petocz , Maria Szecsey nee Hegedus , Marton Fekete , Valeria Hoffmann , Laszlo Kapolnai
IPC分类号： A61K31/15 , A61K31/133 , A61K31/357 , A61K31/36 , A61K31/40 , A61K31/445 , A61K31/452 , A61K31/495 , A61K31/55 , A61P1/04 , A61P9/06 , A61P9/08 , A61P9/10 , A61P25/02 , A61P25/04 , A61P25/20 , A61P29/00 , C07C249/08 , C07C249/12 , C07C251/58 , C07D213/16 , C07D251/58 , C07D295/08 , C07D295/088 , C07D317/56
CPC分类号： C07D213/16 , C07C251/58 , C07D295/088 , C07C2101/02 , C07C2101/08 , C07C2101/14 , C07C2101/18
摘要： The invention relates to novel racemic or optically active aminopropanol derivatives of formula I ##STR1## wherein R and R.sup.1 are independently hydrogen atom, halogen atom, lower alkoxy, or together represent a methylene dioxy group,R.sup.2 and R.sup.3 together represent a chemical bond or independently stand for a hydrogen atom,R.sup.4 and R.sup.5 are independently hydrogen atom, C.sub.3-7 cycloalkyl group or straight or branched, saturated or unsaturated C.sub.1-12 alkyl group optionally substituted by one or more dialkylaminoalkyl, dimethoxyphenyl or phenyl groups, orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a 4 to 7 membered ring optionally comprising an oxygen, sulfur or a further nitrogen atom, which ring is optionally substituted by a phenyl, benzyl or C.sub.1-3 alkyl group and the said substituents may carry a hydroxyl group, one or two methoxy groups, halogen atoms or trifluoromethyl groups, orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a piperidine ring which is optionally substituted by a phenyl or benzyl group and, if desired, it comprises a double bond,R.sup.6 stands for hydrogen atom or benzoyl group, andn represents an integer from 3 to 6, acid-addition salts and quaternary ammonium derivatives thereof.Further the invention relates to processes for preparing these compounds.The compounds of the invention exert cardiac circulation controlling and/or improving, central nervous system tranquillizing and/or digestive system irregulations improving effects.
摘要翻译：本发明涉及式I的新型外消旋或光学活性氨基丙醇衍生物其中R和R 1独立地为氢原子，卤素原子，低级烷氧基或一起代表亚甲基二氧基，R2和R3一起表示化学键或独立地代表氢原子，R4和R5独立地是氢原子，C3-7环烷基或任选被一个或多个二烷基氨基烷基，二甲氧基苯基或苯基取代的直链或支链，饱和或不饱和的C1-12烷基，或R4和R5 与相邻的氮原子一起形成任选地包含氧，硫或另外的氮原子的4至7元环，该环任选被苯基，苄基或C 1-3烷基取代，所述取代基可以带有羟基，一个或两个甲氧基，卤素原子或三氟甲基，或R4和R5与相邻的氮原子一起形成哌啶环，其是任选取代的由苯基或苄基组成，如果需要，它包含双键，R6代表氢原子或苯甲酰基，n代表3-6的整数，其酸加成盐和季铵衍生物。本发明还涉及制备这些化合物的方法。本发明的化合物发挥心脏循环控制和/或改善，中枢神经系统镇定和/或消化系统不调节改善作用。

26. 发明授权

US5478825A 5-(substituted amino)-1,2,4-triazolo (1,5-A) pyrimidine derivatives 失效
标题翻译： 5-（取代氨基）-1,2,4-三唑并（1,5-A）嘧啶衍生物
公开(公告)号：US5478825A
公开(公告)日：1995-12-26
申请号：US261214
申请日：1994-06-15
申请人： Jozsef Reiter , Gabor Berecz , Gizella Zsila , Lujza Pet cz , Gabor Gigler , Marton Fekete , Maria Szecsey nee Heged s , Enik Szirt nee Kiszelly , Ludmila Rohacs nee Zamkovaja , Frigyes Gorgenyi , Margit Csorg
发明人： Jozsef Reiter , Gabor Berecz , Gizella Zsila , Lujza Pet cz , Gabor Gigler , Marton Fekete , Maria Szecsey nee Heged s , Enik Szirt nee Kiszelly , Ludmila Rohacs nee Zamkovaja , Frigyes Gorgenyi , Margit Csorg
IPC分类号： C07D471/14 , C07D487/04 , C07D495/14 , A61K31/535 , A61K31/505
CPC分类号： C07D471/14 , C07D487/04 , C07D495/14
摘要： The disclosed compounds have the formula ##STR1## wherein Q is a 6-membered saturated heterocyclic group or a group S(O)pR.sup.3, whereinp is 0, 1, or 2, andR.sup.3 is alkyl, alkenyl, or phenyl-, which may have halogen or nitro substituents, or phenyl optionally substituted;or NR.sup.4 R.sup.5 whereinR.sup.4 and R.sup.5 are hydrogen, alkyl, alkenyl, phenyl-alkyl, or di-alkyl-amino-alkyl;R.sup.1 and R.sup.2 are hydrogen or alkyl, ortogether form a group (CH.sub.2)n--Y--(CH.sub.2)m, wherein Y is CH.sub.2, or NR.sup.6, wherein R.sup.6 is phenyl-alkyl,n and m are 0 or 1 to 5;Z is NR.sup.7 R.sup.8, whereinR.sup.7 and R.sup.8 each are hydrogen, alkenyl, cycloalkyl, adamantayl, or phenyl-alkyl, which may have one or more substituents ortogether form a group of (CH.sub.2)j--W--(CH.sub.2)k, wherein j and k each are 1 to 3, and W is oxygen, CH.sub.2, CHOH, or NR.sup.10 , wherein R.sup.10 is hydrogen, alkoxycarbonyl, or alkyl, which latter may be substituted.or SR.sup.9, whereinR.sup.9 is alkyl substituted by alkoxy-carbonyl and possess inotropic and antianginal effects, complemented by antiinflammatory, ulcus, and gastric acid secretion inhibiting, and by weaker tranquillant, spasmolytic, and analgesic properties.
摘要翻译：所公开的化合物具有式“IMAGE”，其中Q为6元饱和杂环基团或S（O）pR 3基团，其中p为0,1或2，R 3为烷基，烯基或苯基，其中可以具有卤素或硝基取代基，或任选取代的苯基; 或NR4R5，其中R4和R5是氢，烷基，烯基，苯基 - 烷基或二 - 烷基 - 氨基 - 烷基; 或者一起形成基团（CH 2）n -Y-（CH 2）m，其中Y是CH 2或NR 6，其中R 6是苯基 - 烷基，n和m是0或1至5; Z是NR7R8，其中R7和R8各自是氢，烯基，环烷基，金刚烷基或苯基 - 烷基，其可以具有一个或多个取代基或一起形成（CH 2）j W-（CH 2）k的基团，其中j和k 各自为1至3，W为氧，CH 2，CHOH或NR 10，其中R 10为氢，烷氧基羰基或烷基，后者可以被取代。 - 或SR9，其中R9是被烷氧基 - 羰基取代的烷基，并且具有各向同性和抗心绞痛作用，由抗炎，溃疡和胃酸分泌抑制以及较弱的镇静剂，解痉药和镇痛药物补充。

27. 发明授权

US5391737A Process for the preparation of 6,7-dichloro-1,5-dihydroimidazo[2,1-b]quinazolin-2[3H]-one 失效
标题翻译：制备6,7-二氯-1,5-二氢咪唑并[2,1-b]喹唑啉-2 [3H] - 酮的方法
公开(公告)号：US5391737A
公开(公告)日：1995-02-21
申请号：US156974
申请日：1993-11-24
申请人： Jozsef Reiter , Peter Trinka , Peter Tompe , Eva Szabo , Peter Slegel , Janos Brlik , Agnes Halbauer nee Nagy , Ilona Sztruhar , Magdolna Kenyeres nee Feher , Frigyes Gorgenyi , Margit Csorgo , Szvetlana Zsarnoczai nee Kurnyecova , Sarolta Benko nee Markus , Gabor Gigler , Dezso Danyi , Pal Fekete , Maria Kiraly nee Ignacz
发明人： Jozsef Reiter , Peter Trinka , Peter Tompe , Eva Szabo , Peter Slegel , Janos Brlik , Agnes Halbauer nee Nagy , Ilona Sztruhar , Magdolna Kenyeres nee Feher , Frigyes Gorgenyi , Margit Csorgo , Szvetlana Zsarnoczai nee Kurnyecova , Sarolta Benko nee Markus , Gabor Gigler , Dezso Danyi , Pal Fekete , Maria Kiraly nee Ignacz
IPC分类号： C07D239/84 , C07D487/04
CPC分类号： C07D487/04 , C07D239/84
摘要： This invention relates to a new and improved process for the preparation of 6,7-dichloro-1,5-dihydroimidazo[2,1-b]-quinazolin-2[3H]-one of formula ##STR1## (anagrelide), a valuable blood platelet antiaggregative compound. According to the process of the invention the compound of formula (I) is prepared by subjecting a new 2-cyanoiminoquinazoline derivative of the general formula ##STR2## wherein R stands for cyano or a group of the formula COOR.sup.1, in the latter R.sup.1 representing lower alkyl optionally carrying a phenyl substituent, to thermal cyclization in an acidic medium.The invention also relates to new 2-cyanoiminoquinazo-lines of the general formula (III) used for the production of anagrelide and to the preparation of the said compounds.The invention provides an advantageous process for the preparation of anagrelide which is devoid of the drawbacks of the hitherto known processes and renders possible the production of the compound of the formula (I) on industrial scale, too.
摘要翻译：本发明涉及制备式（I）（阿那格雷）的6,7-二氯-1,5-二氢咪唑并[2,1-b] - 喹唑啉-2（3H）酮的新的和改进的方法），一种有价值的血小板抗凝聚化合物。根据本发明的方法，式（I）化合物通过使新的具有式COOR1的2-氰基亚氨基喹唑啉衍生物在代表任选携带苯基取代基的低级烷基的后面的R1中经受热在酸性介质中环化。本发明还涉及用于生产阿那格雷的通式（III）的新的2-氰基亚氨基喹诺酮和所述化合物的制备。本发明提供了一种制备阿那格雷的有利方法，其没有迄今已知方法的缺点，并且使得可能以工业规模生产式（I）化合物。

28. 发明授权

US5234934A Aminopropanol derivatives, process for their preparation and pharmaceutical compositions comprising the same 失效
标题翻译：氨基丙醇衍生物，其制备方法和包含其的药物组合物
公开(公告)号：US5234934A
公开(公告)日：1993-08-10
申请号：US876091
申请日：1992-04-30
申请人： Zoltan Budai , Klara Reiter nee Esses , Eniko Sziri nee Kiszelly , Gizella Zsila , Gabor Gigler , Lujza Petocz , Maria Szecsey nee Hegedus , Marton Fekete , Valeria Hoffmann , Laszlo Kapolnai
发明人： Zoltan Budai , Klara Reiter nee Esses , Eniko Sziri nee Kiszelly , Gizella Zsila , Gabor Gigler , Lujza Petocz , Maria Szecsey nee Hegedus , Marton Fekete , Valeria Hoffmann , Laszlo Kapolnai
IPC分类号： C07C251/58 , C07D213/16 , C07D295/088
CPC分类号： C07D213/16 , C07C251/58 , C07D295/088 , C07C2101/02 , C07C2101/08 , C07C2101/14 , C07C2101/18
摘要： The invention relates to novel racemic or optically active aminopropanol derivatives of formula I ##STR1## wherein R and R.sup.1 are independently hydrogen atom, halogen atom, lower alkoxy, or together represent a methylene dioxy group,R.sup.2 and R.sup.3 together represent a chemical bond or independently stand for a hydrogen atom,R.sup.4 and R.sup.5 are independently hydrogen atom, C.sub.3-7 cycloalkyl group or straight or branched, saturated or unsaturated C.sub.1-12 alkyl group optionally substituted by one or more dialkyl-aminoalkyl, dimethoxyphenyl or phenyl groups, orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a 4 to 7 membered ring optionally comprising an oxygen, sulfur or a further nitrogen atom, which ring is optionally substituted by a phenyl, benzyl or C.sub.1-3 alkyl group and the said substituents may carry a hydroxyl group, one or two methoxy groups, halogen atoms or trifluoromethyl groups, orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a piperidine ring which is optionally substituted by a phenyl or benzyl group and, if desired, it comprises a double bond,R.sup.6 stands for hydrogen atom or benzoyl group, andn represents an integer from 3 to 6,acid-addition salts and quaternary ammonium derivatives thereof.Further the invention relates to processes for preparing these compounds.The compounds of the invention exert cardiac circulation controlling and/or improving, central nervous system tranquillizing and/or digestive system irregulations improving effects.
摘要翻译：本发明涉及式I的新型外消旋或光学活性氨基丙醇衍生物其中R和R 1独立地为氢原子，卤素原子，低级烷氧基或一起代表亚甲基二氧基，R2和R3一起表示化学键或独立地代表氢原子，R4和R5独立地是氢原子，C3-7环烷基或任选被一个或多个二烷基氨基烷基，二甲氧基苯基或苯基取代的直链或支链，饱和或不饱和的C 1-12烷基，或R 4 和R5与相邻的氮原子一起形成任选地包含氧，硫或另外的氮原子的4至7元环，该环任选被苯基，苄基或C 1-3烷基取代，所述取代基可以携带羟基，一个或两个甲氧基，卤素原子或三氟甲基，或R4和R5与相邻的氮原子一起形成哌啶环，其任选地是由苯基或苄基构成，如果需要，它包含双键，R6代表氢原子或苯甲酰基，n代表3-6的整数，其酸加成盐和季铵衍生物。本发明还涉及制备这些化合物的方法。本发明的化合物发挥心脏循环控制和/或改善，中枢神经系统镇定和/或消化系统不调节改善作用。

29. 发明授权

US4994448A Condensed quinolinium and isoquinolinium derivatives 失效
标题翻译：浓缩的喹啉和异喹啉衍生物
公开(公告)号：US4994448A
公开(公告)日：1991-02-19
申请号：US251445
申请日：1988-09-30
申请人： Andras Messmer , Gyorgy Hajos , Zsuzsa Juhasz nee Riedl , Pal Benko , Laszlo Pallos , Lujza Petocz , Eniko Szirt nee Kiszelly , Gabor Gigler , Istvan Gyertyan , Maria Hegedus
发明人： Andras Messmer , Gyorgy Hajos , Zsuzsa Juhasz nee Riedl , Pal Benko , Laszlo Pallos , Lujza Petocz , Eniko Szirt nee Kiszelly , Gabor Gigler , Istvan Gyertyan , Maria Hegedus
IPC分类号： A61K31/53 , A61P25/02 , A61P25/04 , A61P25/20 , A61P25/24 , A61P25/26 , C07D471/04
CPC分类号： C07D471/04
摘要： The new compounds of the general Formula I ##STR1## (wherein R.sub.1 stands for C.sub.1-4 alkyl or aralkyl; andR.sub.2 represents hydroxy; orR.sub.1 and R.sub.2 together form a valency bond;R.sub.3 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenyl, amino, alkylthio or a group of the Formula --NR.sub.7 R.sub.8 in which R.sub.7 and R.sub.8 may be the same or different and stand for hydrogen, C.sub.1-4 alkyl, phenyl-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkyl or di-(C.sub.1-4 alkyl)-amino-C.sub.1-4 alkyl or together with the nitrogen atom they are attached to form a 6-membered heterocyclic ring which may optionally contain a further nitrogen, oxygen or sulfur atom; orR.sub.2 and R.sub.3 together form an oxo (.dbd.O) or thixo (.dbd.S) group;R.sub.4 represents hydrogen, C.sub.1-4 alkyl or phenyl which may optionally bear one or two halogen or nitro substituent(s);Z is a group of the Formula (a) or (b) ##STR2## A.sup.- represents an anion) and isomers thereof possess useful local anaesthetic, antidepressant, tranquillo-sedative and smooth muscle relaxant properties accompanied by a weaker analgesic effect and are useful in therapy.
摘要翻译：通式I的新化合物Ⅰ（其中R1代表C1-4烷基或芳烷基，R2代表羟基;或R1和R2一起形成价键; R3是氢，C1-4烷基，C1- 烷氧基，苯基，氨基，烷硫基或式-NR7R8的基团，其中R 7和R 8可以相同或不同，代表氢，C 1-4烷基，苯基-C 1-4烷基，羟基-C 1-4烷基或二 - （C 1-4烷基） - 氨基-C 1-4烷基或与它们连接的氮原子一起形成可任选地含有另外的氮，氧或硫原子的6元杂环;或R 2和R 3 一起形成氧代（= O）或触变（= S）基团; R4代表氢，C1-4烷基或苯基，其可任选地带有一个或两个卤素或硝基取代基; Z是式（a ）或（b）和A-表示阴离子）及其异构体具有有用的局部麻醉剂，抗抑郁药，镇痛镇痛和平滑肌松弛剂性质，伴随较弱的镇痛剂 c效应，可用于治疗。

30. 发明授权

US4906622A Optically active 2-chloro-12-(3-dimethylamino-2-methyl-propyl)-12H-dibenzo[d.g] [1,3,6] dioxazocines and a process for the preparation thereof 失效
标题翻译：光学活性的2-氯-12-（3-二甲基氨基-2-甲基 - 丙基）-12H-二苯并[d] [1,3,6]二氧杂吖庚因及其制备方法
公开(公告)号：US4906622A
公开(公告)日：1990-03-06
申请号：US195691
申请日：1988-05-18
申请人： Laszlo Rozsa , Lujza Petocz , Eniko Szirt nee Kiszelly , Peter Tompe , Gabor Gigler
发明人： Laszlo Rozsa , Lujza Petocz , Eniko Szirt nee Kiszelly , Peter Tompe , Gabor Gigler
IPC分类号： A61K31/395 , A61P25/00 , A61P25/16 , C07D273/00 , C07D273/01
CPC分类号： C07D273/00
摘要： The invention relates to optically active 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]dioxazocine of the Formula ##STR1## and pharmaceutically acceptable acid additional salts thereof. The enantiomers are especially active against Parkinsion's disease.The optically active enantiomers are prepared by(a) resolving the racemic 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]-dioxazocine with a optically active organic acid and separating the enantiomers; or(b) dissolving the racemic 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]-dioxazocine in an organic solvent, crystallizing and isolating one of the enantiomers, optionally dissolving additional racemic 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]-dioxazocine in the mother liquor obtained and crystallizing and isolating the other enantiomer, and, if desired, repeating the whole process.
摘要翻译：本发明涉及式（I）的光学活性2-氯代 - 12-（3-二甲基氨基-2-甲基丙基）-12H-二苯并[d，g] [1,3,6]二恶唑辛嗪和药学上其可接受的酸性附加盐。对映异构体对帕金森氏病特别活跃。旋光对映异构体通过以下步骤制备：（a）用光学拆分外消旋的2-氯代 - 12-（3-二甲基氨基-2-甲基丙基）-12H-二苯并[d，g] [1,3,6] 活性有机酸并分离对映异构体; 或（b）将外消旋的2-氯代 - 12-（3-二甲基氨基-2-甲基丙基）-12H-二苯并[d，g] [1,3,6] - 二氧杂吖嗪在有机溶剂中溶解，的对映异构体，任选地将另外的外消旋的2-氯-12-（3-二甲基氨基-2-甲基丙基）-12H-二苯并[d，g] [1,3,6] - 二氧杂吖嗪应用于所获得和结晶的母液中，分离另一个对映体，如果需要，重复整个过程。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式