公开(公告)号：US4883798A

公开(公告)日：1989-11-28

申请号：US221529

申请日：1988-07-20

申请人： Lujza Petocz ,  Istvan Simonyi ,  Ivan Beck ,  Gabor Gigler ,  Marton Fekete ,  Eniko Szirt nee Kiszelly ,  Attila Mandi ,  Frigyes Gorgenyi ,  Andras Dietz ,  Elemer Jakfalvi ,  Katalin Zukovics nee Sumeg ,  Klara Gado ,  Maria Hegedus

发明人： Lujza Petocz ,  Istvan Simonyi ,  Ivan Beck ,  Gabor Gigler ,  Marton Fekete ,  Eniko Szirt nee Kiszelly ,  Attila Mandi ,  Frigyes Gorgenyi ,  Andras Dietz ,  Elemer Jakfalvi ,  Katalin Zukovics nee Sumeg ,  Klara Gado ,  Maria Hegedus

IPC分类号： A61K31/505 ,  A61P25/04 ,  A61P29/00 ,  A61P43/00 ,  C07D239/49 ,  C07D405/06

CPC分类号： A61K31/505

摘要： The compounds of the general Formula I ##STR1## (wherein R.sup.1 and R.sup.2 may be the same or different and each stands for hydrogen, hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkoxy-C.sub.1-6 alkoxy, C.sub.2-6 alkenyloxy or phenyl-(C.sub.1-3 alkoxy), or R.sup.1 and R.sup.2 together form C.sub.1-2 alkylenedioxy; with the proviso that at least one of symbols R.sup.1 and R.sup.2 is other than hydrogen and with the further proviso that R.sup.1 and R.sup.2 can not represent 3,4-dimethoxy substitution) andtheir pharmaceutically acceptable acid addition salts exhibit useful analgesic, antipyretic, anti-inflammatory, anti-anginal and antioxidant effect.

摘要翻译： 通式I的化合物（I）（其中R 1和R 2可以相同或不同，各自代表氢，羟基，C 1-6烷氧基，C 1-6烷氧基-C 1-6烷氧基，C 2-6 烯基氧基或苯基 - （C1-3烷氧基），或R1和R2一起形成C1-2亚烷基二氧基;条件是符号R1和R2中的至少一个不是氢，另外条件是R1和R2不能表示 3,4-二甲氧基取代）及其药学上可接受的酸加成盐显示出有用的镇痛，解热，抗炎，抗心绞痛和抗氧化作用。

公开(公告)号：US4873249A

公开(公告)日：1989-10-10

申请号：US17090

申请日：1987-02-20

申请人： Lujza Petocz ,  Istvan Simonyi ,  Ivan Beck ,  Gabor Gigler ,  Marton Fekete ,  Eniko Kiszelly ,  Attila Mandi ,  Frigyes Gorgenyi ,  Andras Dietz ,  Katalin Sumeg nee Zukovics ,  Elemer Jakfalvi

发明人： Lujza Petocz ,  Istvan Simonyi ,  Ivan Beck ,  Gabor Gigler ,  Marton Fekete ,  Eniko Kiszelly ,  Attila Mandi ,  Frigyes Gorgenyi ,  Andras Dietz ,  Katalin Sumeg nee Zukovics ,  Elemer Jakfalvi

IPC分类号： C07D239/49 ,  A61K31/505 ,  A61P25/04 ,  A61P29/00

CPC分类号： A61K31/505 ,  Y10S514/825

摘要： The invention relates to pharmaceutical compositions having analgesic and/or anti-inflammatory effect comprising as active ingredient 2,4-diamino-5-(3,4-dimethoxy-benzyl)-pyrimidine or a pharmaceutically acceptable acid addition salt thereof.The pharmaceutical compositions of the present invention exhibit the desired analgesic and anti-inflammatory effect without causing undesired ulcerogenic side-effects.

摘要翻译： 本发明涉及包含作为活性成分2,4-二氨基-5-（3,4-二甲氧基 - 苄基） - 嘧啶或其药学上可接受的酸加成盐的镇痛和/或抗炎作用的药物组合物。 本发明的药物组合物显示出期望的止痛和抗炎作用，而不引起不希望的溃疡发生副作用。

公开(公告)号：US5135928A

公开(公告)日：1992-08-04

申请号：US604486

申请日：1990-10-25

申请人： Jozsef Reiter ,  Jozsef Barkoczy ,  Lujza Petocz ,  Frigyes Gorgenyi ,  Marton Fekete ,  Eniko Szirt nee Kiszelly ,  Gabor Gigler ,  Istvan Gacsalyi ,  Istvan Gyertyan ,  Klara Reiter nee Esses

发明人： Jozsef Reiter ,  Jozsef Barkoczy ,  Lujza Petocz ,  Frigyes Gorgenyi ,  Marton Fekete ,  Eniko Szirt nee Kiszelly ,  Gabor Gigler ,  Istvan Gacsalyi ,  Istvan Gyertyan ,  Klara Reiter nee Esses

IPC分类号： A61K31/41 ,  A61K31/50 ,  A61K31/535 ,  A61K31/55 ,  A61P9/08 ,  A61P9/10 ,  A61P29/00 ,  C07D249/14 ,  C07D403/04 ,  C07D405/12 ,  C07D413/04 ,  C07D487/04

CPC分类号： C07D405/12 ,  C07D249/14 ,  C07D487/04

摘要： This invention relates to novel triazolo derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, to the use of the said triazolo derivatives for the treatment of diseases and also for the preparation of pharmaceutical compositions suitable for the treatment of the said diseases.The new triazolo derivatives of the general formulae (Ia) and (Ib), ##STR1## wherein Q represents hydrogen or a heterocyclic group optionally bearing one or more C.sub.1-4 alkyl substituent(s); or a group of the formula SR.sup.1, whereinR.sup.1 stands for straight or branched chained C.sub.1-4 alkyl or phenyl-(C.sub.1-4 alkyl); or q represents a group of the formula NR.sup.2 R.sup.3, whereinR.sup.2 and R.sup.3 each represent hydrogen, straight or branched chain C.sub.1-12 alkyl, C.sub.2-6 alkenyl or phenyl-(C.sub.1-4 alkyl);R.sup.4 and R.sup.7 each represent hydrogen, C.sub.1-6 alkyl or phenyl-(C.sub.1-4 alkyl) optionally bearing one or more halogen substituent(s);R.sup.5 and R.sup.6 each stand for C.sub.1-4 alkyl optionally substituted by a C.sub.1-4 alkoxycarbonyl group; a heterocyclic group or a phenyl group optionally bearing one or more halogen, hydroxyl, cyano, nitro, alkyl, methylene dioxy and carbamoylmethoxy, di-(C.sub.1-4 alkyl)-amino or C.sub.1-4 alkoxy substituent(s) which latter may carry a di-(C.sub.1-4 alkyl)-amino group; furthermore one of R.sup.5 and R.sup.6 may represent hydrogen, orR.sup.5 and R.sup.6 together stand for C.sub.4-15 alkylene, or together with the adjacent carbon atom they are attached to form a heterocyclic group bearing a phenyl(C.sub.1-4 alkyl) substituent,possess valuable antianginal and tranquillant/sedative properties and are useful in therapy.

公开(公告)号：US5225410A

公开(公告)日：1993-07-06

申请号：US604488

申请日：1990-10-25

申请人： Jozsef Barkoczy ,  Jozsef Reiter ,  Laszlo Pongo ,  Lujza Petocz ,  Frigyes Gorgenyi ,  Marton Fekete ,  Eniko Szirt nee Kiszelly ,  Maria Szecsey nee Hegedus ,  Istvan Gacsalyi ,  Istvan Gyertyan

发明人： Jozsef Barkoczy ,  Jozsef Reiter ,  Laszlo Pongo ,  Lujza Petocz ,  Frigyes Gorgenyi ,  Marton Fekete ,  Eniko Szirt nee Kiszelly ,  Maria Szecsey nee Hegedus ,  Istvan Gacsalyi ,  Istvan Gyertyan

IPC分类号： A61K31/41 ,  A61K31/50 ,  A61K31/55 ,  A61P1/04 ,  A61P9/08 ,  A61P9/10 ,  C07D249/14 ,  C07D403/04 ,  C07D413/04

CPC分类号： C07D249/14

摘要： This invention relates to novel triazolyl hydrazide derivatives and a process for the preparation thereof.The new triazolyl hydrazide derivatives of the general formula (I). ##STR1## wherein Q represents hydrogen or a heterocyclic group optionally substituted by a C.sub.1-4 alkyl group; or a group of general formula SR.sup.1, whereinR.sup.1 stands for C.sub.1-4 alkyl or phenyl-(C.sub.1-4 alkyl) optionally substituted by halogen, C.sub.1-4 alkyl or nitro substitute therefor substituents; or Q represents a group of the formula NR.sup.2 R.sup.3, wherein R.sup.2 and R.sup.3 each represents hydrogen, straight or branched chain C.sub.1-6 alkyl or C.sub.2-6 alkenyl;Z represents hydrogen or a group of the formula (C.dbd.X)--(N--R.sup.4)--NR.sup.5 R.sup.6, whereinX stands for oxygen or sulfur,R.sup.4, R.sup.5 and R.sup.6 each stand for hydrogen or C.sub.1-4 alkyl;R.sup.7 stands for hydrogen, C.sub.1-4 alkyl or phenyl-(C.sub.1-4 alkyl) optionally substituted by one or more halogen atom(s) or an amino group optionally substituted by one or two C.sub.1-4 alkyl substituents,R.sup.8 stands for hydrogen or a group of the formula --(C.dbd.X)--(N--R.sup.4)--NR.sup.5 R.sup.6, wherein X, R.sup.4, R.sup.5 and R.sup.6 are as stated above,with the proviso that if Z represents a group of the formula --(C.dbd.X)--(N--R.sup.4)--NR.sup.5 R.sup.6, R.sup.8 stands for hydrogen, and if Z represents hydrogen, R.sup.8 stands for a group of the formula (C.dbd.X)--(N--R.sup.4)--NR.sup.5 R.sup.6, and pharmaceutically acceptable acid addition salts thereof excert valuable antianginal and/or gastric ulcer inhibiting properties and are useful in therapy.

公开(公告)号：US5276030A

公开(公告)日：1994-01-04

申请号：US755219

申请日：1991-09-09

申请人： Josef Barkoczy ,  Josef Reiter ,  Laszlo Pongo ,  Lujza Petocz ,  Marton Fekete ,  Frigyes Gorgenyi ,  Gabor Gigler ,  Istvan Gacsalyi ,  Istvan Gyertyan

发明人： Josef Barkoczy ,  Josef Reiter ,  Laszlo Pongo ,  Lujza Petocz ,  Marton Fekete ,  Frigyes Gorgenyi ,  Gabor Gigler ,  Istvan Gacsalyi ,  Istvan Gyertyan

IPC分类号： A61K31/41 ,  A61K31/4196 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  A61P13/06 ,  A61P25/08 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/26 ,  A61P29/00 ,  C07D249/14 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D413/04 ,  C07D413/14

CPC分类号： C07D249/14

摘要： The invention relates to novel triazolyl thioamides of the general formula (I), ##STR1## wherein Q represents hydrogen or a heterocyclic group optionally bearing one or more C.sub.1-4 alkyl substituent(s), or a group of the formula SR.sup.1, whereinR.sup.1 stands for straight or branched chained alkyl group comprising 1 to 6 carbon atom(s), or a group of the formula NR.sup.2 R.sup.3, whereinR.sup.2 and R.sup.3 each represent hydrogen, straight or branched chained C.sub.1-4 alkyl or C.sub.2-6 alkenyl group,Y denotes C.sub.1-4 alkyl bearing one or more hydroxyl or C.sub.1-4 alkoxy substituent(s), phenyl-(C.sub.1-4 alkyl) optionally bearing on the phenyl ring one or more C.sub.1-4 alkoxy group(s), or phenoxy-(C.sub.1-4 alkyl) optionally substituted on the phenyl ring by a C.sub.1-4 alkyl bearing a heterocyclic group containing a nitrogen atom, with the proviso that if Q represents methylthio, dimethylamino, piperidino or morpholino, Y is other than benzyl,and pharmaceutically acceptable acid additional salts thereof.Furthermore the invention relates to a process for preparing these compounds.The compounds according to the invention possess tranquillant, antidepressant, spasmolytic, antiinflammatory, analgesic and antiperistaltic effects.

摘要翻译： 本发明涉及通式（I）的新型三唑基硫代酰胺，其中Q表示氢或任选带有一个或多个C 1-4烷基取代基的杂环基或式SR1的基团，其中R 1 代表包含1至6个碳原子的直链或支链烷基或式NR2R3基团，其中R2和R3各自表示氢，直链或支链C 1-4烷基或C 2-6烯基，Y 表示具有一个或多个羟基或C 1-4烷氧基取代基的C 1-4烷基，任选地在苯环上带有一个或多个C 1-4烷氧基的苯基 - （C 1-4烷基）或苯氧基 - （ C 1-4烷基），其任选在苯环上被带有含氮原子的杂环基的C 1-4烷基取代，条件是如果Q表示甲硫基，二甲基氨基，哌啶子基或吗啉代，则Y不是苄基， 其酸加成盐。 此外，本发明涉及一种制备这些化合物的方法。 根据本发明的化合物具有镇静，抗抑郁，解痉，抗炎，止痛和抗静脉作用。

公开(公告)号：US5175163A

公开(公告)日：1992-12-29

申请号：US617126

申请日：1990-11-21

申请人： Jozsef Barkoczy ,  Jozsef Reiter ,  Laszlo Pongo ,  Lujza Petocz ,  Marton Fekete ,  Frigyes Gorgenyi ,  Gabor Gigler ,  Istvan Gacsalyi ,  Istvan Gyertyan

发明人： Jozsef Barkoczy ,  Jozsef Reiter ,  Laszlo Pongo ,  Lujza Petocz ,  Marton Fekete ,  Frigyes Gorgenyi ,  Gabor Gigler ,  Istvan Gacsalyi ,  Istvan Gyertyan

IPC分类号： A61K31/41 ,  A61K31/4196 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  A61P13/06 ,  A61P25/08 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/26 ,  A61P29/00 ,  C07D249/14 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D413/04 ,  C07D413/14

CPC分类号： C07D249/14

摘要： The invention relates to novel triazolyl thioamides of the general formula (I), ##STR1## wherein Q represents hydrogen or a heterocyclic group optionally bearing one or more C.sub.1-4 alkyl substituent(s), or a group of the formula SR.sup.1, whereinR.sup.1 stands for straight or branched chained alkyl group comprising 1 to 6 carbon atom(s), or a group of the formula NR.sup.2 R.sup.3, whereinR.sup.2 and R.sup.3 each represent hydrogen, straight or branched chained C.sub.1-4 alkyl or C.sub.2-6 alkenyl group,Y denotes C.sub.1-4 alkyl optionally bearing one or more hydroxyl or C.sub.1-4 alkoxy substituent(s), phenyl-(C.sub.1-4 alkyl) optionally bearing on the phenyl ring one or more C.sub.1-4 alkoxy group(s), or phenoxy-(C.sub.1-4 alkyl) optionally substituted on the phenyl ring by a C.sub.1-4 alkyl bearing a heterocyclic group containing a nitrogen atom,and pharmaceutically acceptable acid addition salts thereof.Furthermore the invention relates to a process for preparing these compounds.The compounds according to the invention possess tranquillant, antidepressant, spacmolytic, antiinflammatory, analgesic and antiperistaltic effects.

摘要翻译： 本发明涉及通式（I）的新型三唑基硫代酰胺，其中Q表示氢或任选带有一个或多个C 1-4烷基取代基的杂环基或式SR 1的基团 其中R1代表包括1至6个碳原子的直链或支链烷基或式NR2R3基团，其中R2和R3各自表示氢，直链或支链C 1-4烷基或C 2-6烯基 基团，Y表示任选带有一个或多个羟基或C 1-4烷氧基取代基的C 1-4烷基，任选地在苯环上带有一个或多个C 1-4烷氧基的苯基 - （C 1-4烷基） 或在苯环上被含有含有氮原子的杂环基的C 1-4烷基任选取代的苯氧基 - （C 1-4烷基）及其药学上可接受的酸加成盐。 此外，本发明涉及一种制备这些化合物的方法。 根据本发明的化合物具有镇静，抗抑郁，间质，抗炎，止痛和抗静脉作用。

公开(公告)号：US5126457A

公开(公告)日：1992-06-30

申请号：US321293

申请日：1989-03-08

申请人： Pal Benko ,  Daniel Bozsing ,  Laszlo Levai ,  Gyorgyi Kovanyi nee Lax ,  Gyorgy Mikite ,  Peter Tompe ,  Eva Furdyga ,  Ilona Dinnyes nee Nagy ,  Eva Poczik ,  Gyorgyi Zalavari nee Dosa ,  Ivan Beck ,  Istvan Simonyi ,  Kalman Nagy ,  Janos Imre ,  Erzsebet Kiss nee Bertok ,  Eva J. Tajthy nee Juhasz ,  Attila Mandi ,  Frigyes Gorgenyi

发明人： Pal Benko ,  Daniel Bozsing ,  Laszlo Levai ,  Gyorgyi Kovanyi nee Lax ,  Gyorgy Mikite ,  Peter Tompe ,  Eva Furdyga ,  Ilona Dinnyes nee Nagy ,  Eva Poczik ,  Gyorgyi Zalavari nee Dosa ,  Ivan Beck ,  Istvan Simonyi ,  Kalman Nagy ,  Janos Imre ,  Erzsebet Kiss nee Bertok ,  Eva J. Tajthy nee Juhasz ,  Attila Mandi ,  Frigyes Gorgenyi

IPC分类号： C07C251/24 ,  C07D211/90

CPC分类号： C07D211/90 ,  C07C251/24

摘要： The invention is directed to processes for the preparation of dimethyl-1,4-dihydro-2,6-dimethyl-4-(2'-nitrophenyl)-pyridine-3,5-dicarboxylate by reacting 1-methoxy-1-(2'-nitrophenyl)-N-(2'-nitrophenyl)methylene methanamie or 1-(2'-nitrophenyl)-N,N'-bis-(2'-nitrophenyl) methylene methanediamine with methyl acetoacetate in the presence of an amine compound or by reacting the monomeric or trimeric from of 2-nitrobenzaldimine with methyl acetoacetate.

摘要翻译： 本发明涉及制备二甲基-1,4-二氢-2,6-二甲基-4-（2'-硝基苯基） - 吡啶-3,5-二羧酸二甲酯的方法，通过1-甲氧基-1-（ 2'-硝基苯基）-N-（2'-硝基苯基）亚甲基甲酰胺或1-（2'-硝基苯基）-N，N'-双 - （2'-硝基苯基）亚甲基甲二胺与乙酰乙酸甲酯在胺 化合物或通过使2-硝基苯甲酰亚胺与乙酰乙酸甲酯的单体或三聚体反应。

公开(公告)号：US5216157A

公开(公告)日：1993-06-01

申请号：US686443

申请日：1991-04-17

申请人： Pal Benko ,  Daniel Bozsing ,  Laszlo Levai ,  Gyorgyi Kovanyi nee Lax ,  Gyorgy Mikite ,  Peter Tompe ,  Eva Furdyga ,  Ilona Dinnyes nee Nagy ,  Eva Poczik ,  Gyorgyi Zalavari nee Dosa ,  Ivan Beck ,  Istvan Simonyi ,  Kalman Nagy ,  Janos Imre ,  Erzsebet Kiss nee Bertok ,  Eva J. Tajthy nee Juhasz ,  Attila Mandi ,  Frigyes Gorgenyi

发明人： Pal Benko ,  Daniel Bozsing ,  Laszlo Levai ,  Gyorgyi Kovanyi nee Lax ,  Gyorgy Mikite ,  Peter Tompe ,  Eva Furdyga ,  Ilona Dinnyes nee Nagy ,  Eva Poczik ,  Gyorgyi Zalavari nee Dosa ,  Ivan Beck ,  Istvan Simonyi ,  Kalman Nagy ,  Janos Imre ,  Erzsebet Kiss nee Bertok ,  Eva J. Tajthy nee Juhasz ,  Attila Mandi ,  Frigyes Gorgenyi

IPC分类号： C07C251/24 ,  C07D211/90

CPC分类号： C07D211/90 ,  C07C251/24

摘要： The invention relates to a process for the preparation of dimethyl-1,4-dihydro-2,6-dimethyl-4-(2'-nitro-phenyl)-pyridine-3,5-dicarboxylate of the Formula I ##STR1## which comprises a) reacting a compound of the general Formula II ##STR2## (wherein n is 1 or 3; if n is 1, then R stands for a group of the Formula (a) ##STR3## and if n is 3, then R represents hydrogen) with methyl acetoacetate of the Formula IIICH.sub.3 --CO--CH.sub.2 --COOCH.sub.3 (III) and optionally with an amino compound of the general Formula IV ##STR4## (wherein Z is a group of the Formula (c), ##STR5## k is 1 and both symbols p are 0; or Z stands for a C.sub.1-5 straight or branched chain alkanoyloxy group or a carbonate, hydrocarbonate or hydroxy anion, k is 1 and both symbols p are 1; or k is 0, one of both symbols p is 0 and the other is 1) in an inert solvent; orb) reacting 2-nitro-benzaldehyde and methyl acetoacetate of the Formula III and aqueous ammonium hydroxide in the presence of an inert solvent in one step, at a temperature of 101.degree.-120.degree. C., under a pressure of 2.0-6.0 bar.

摘要翻译： 本发明涉及制备式I的二甲基-1,4-二氢-2,6-二甲基-4-（2'-硝基 - 苯基） - 吡啶-3,5-二羧酸的方法， （I），其包括a）使通式II的化合物（II）（其中n为1或3;使n为1，则R代表式（a）的基团） （III）的乙酰乙酸甲酯和任选与通式IV的氨基化合物的化合物（a）（b）并且如果n是3，那么R代表氢）与式IIICH 3 -CO-CH 2 -COOCH 3 （IV）（其中Z为式（c）的基团，（c）k为1，两个符号p为0; Z表示碳原子数1〜5的直链或支链烷酰氧基或碳酸酯， 烃基或羟基阴离子，k为1，两个符号p为1;或k为0，两个符号p中的一个为0，另一个为1）; 或b）在惰性溶剂存在下，在一个步骤中，在101-120℃，2.0-6.0的压力下，使式III的2-硝基 - 苯甲醛和乙酰乙酸甲酯与氢氧化铵水溶液反应 酒吧。

公开(公告)号：US4868172A

公开(公告)日：1989-09-19

申请号：US38656

申请日：1987-04-15

申请人： Gyula Sebestyen ,  Istvan Simonyi ,  Gizella Miholics ,  Marta Kovacs ,  Frigyes Gorgenyi ,  Marton Fekete ,  Pal Vago ,  Istvan Seres ,  Egri Janos ,  Maria Szeli

发明人： Gyula Sebestyen ,  Istvan Simonyi ,  Gizella Miholics ,  Marta Kovacs ,  Frigyes Gorgenyi ,  Marton Fekete ,  Pal Vago ,  Istvan Seres ,  Egri Janos ,  Maria Szeli

IPC分类号： A61K31/555 ,  A61P31/04 ,  A61P31/10 ,  C07D215/30

CPC分类号： C07D215/30

摘要： The invention refers to a novel pharmaceutical composition having especially antimycotic activity and comprising the zinc complex of 5-chloro-7-iodo-8-hydroxyquinoline of formula (I) ##STR1## and one or more pharmaceutically acceptable carriers. The pharmaceutical composition of the invention can be used for the effective treatment of mycotic infections on the skin surface, mucous membranes or nails.The complex of formula (I) is prepared by reacting a solution of an alkali metal salt of 5-chloro-7-iodo-8-hydroxyquinoline with a solution containing an excess of an inorganic or organic zinc salt or a zinc complex having a lower stability constant than that of the complex of formula (I) and separating the product precipitated.

公开(公告)号：US5108757A

公开(公告)日：1992-04-28

申请号：US493283

申请日：1990-03-14

申请人： Sandor Erdos ,  Jozsef Kenderfi ,  Erzsebet Barczay ,  Aranka Hegedus nee Szima ,  Maria Krisztian ,  Attila Mandi ,  Eva Tajthy nee Juhasz ,  Peter Tompe ,  Margit Csorgo ,  Marton Fekete ,  Frigyes Gorgenyi ,  Zoltan Torma

发明人： Sandor Erdos ,  Jozsef Kenderfi ,  Erzsebet Barczay ,  Aranka Hegedus nee Szima ,  Maria Krisztian ,  Attila Mandi ,  Eva Tajthy nee Juhasz ,  Peter Tompe ,  Margit Csorgo ,  Marton Fekete ,  Frigyes Gorgenyi ,  Zoltan Torma

IPC分类号： A61K9/14 ,  A61K9/16 ,  A61K9/20 ,  A61K9/22 ,  A61K9/28 ,  A61K9/48 ,  A61K9/52 ,  A61K31/44 ,  A61K31/4422 ,  A61K31/455 ,  A61K47/10 ,  A61K47/32 ,  A61K47/38 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12

CPC分类号： A61K31/44 ,  A61K9/146 ,  A61K9/1676 ,  A61K9/2077

摘要： The present invention relates to a process for the preparation of regulated release solid pharmaceutical compositions comprising 4-(2'-nitro-phenyl)-2,6-dimethyl-3,5-dimethoxycarbonyl-1,4-dihydro-pyridine (referred to further on as "nifedipine") as active ingredient which comprises admixing a solution or solutions of 1 part by weight of nifedipine, 0.1-1.5 parts by weight of one or more hydrophilizing agent(s) and 0.05-1.5 parts by weight of one or more retarding agent(s) formed with one or more identical or different solvent(s) completely or partly and applying the solution(s) thus obtained simultaneously or in succession onto an inert carrier, drying and sieving the product thus obtained and subsequently admixing the same with suitable conventional auxiliary agents and compressing the mixture thus obtained to tablets in a known manner and coating the tablets or filling the mixture into capsules.

摘要翻译： 本发明涉及一种制备包含4-（2'-硝基 - 苯基）-2,6-二甲基-3,5-二甲氧基羰基-1,4-二氢 - 哒嗪的调释性固体药物组合物的方法 进一步作为“硝苯地平”）作为活性成分，其包括将1重量份硝苯地平，0.1-1.5重量份的一种或多种亲水剂和0.05-1.5重量份的一种 或更多的阻滞剂，其由一种或多种相同或不同的溶剂完全或部分形成，并将由此获得的溶液同时或相继地施加到惰性载体上，干燥和筛分由此获得的产物，随后混合 与合适的常规辅助剂相同，并以已知方式将所得到的混合物压制成片剂，并涂覆片剂或将混合物填充到胶囊中。