公开(公告)号：US5380724A

公开(公告)日：1995-01-10

申请号：US78601

申请日：1993-06-16

申请人： Zoltan Zubovics ,  Katalin Goldschmidt ,  Katalin Szilagyi ,  Ferenc Andrasi ,  Eszter Hodula ,  Lajos Toldy ,  Klara Sutka ,  Zsuzsanna Fittler ,  Laszlo Sebestyen ,  Katalin Gorgenyi ,  Istvan Sziraki ,  Jozsef Gyimesi ,  Valeria Vitkoczi

发明人： Zoltan Zubovics ,  Katalin Goldschmidt ,  Katalin Szilagyi ,  Ferenc Andrasi ,  Eszter Hodula ,  Lajos Toldy ,  Klara Sutka ,  Zsuzsanna Fittler ,  Laszlo Sebestyen ,  Katalin Gorgenyi ,  Istvan Sziraki ,  Jozsef Gyimesi ,  Valeria Vitkoczi

IPC分类号： A61K31/50 ,  A61K31/496 ,  A61K31/505 ,  A61K31/517 ,  A61K31/519 ,  A61P1/04 ,  A61P1/16 ,  A61P3/00 ,  A61P3/10 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P11/08 ,  A61P13/12 ,  A61P29/00 ,  A61P37/06 ,  C07D237/20 ,  C07D239/48 ,  C07D239/50 ,  C07D239/94 ,  C07D239/95 ,  C07D403/06 ,  C07D475/00 ,  C07D475/06 ,  C07D475/08 ,  A61K31/495 ,  C07D239/02 ,  C07D403/04 ,  C07D487/00

CPC分类号： C07D239/95 ,  C07D237/20 ,  C07D239/50 ,  C07D475/06 ,  C07D475/08 ,  Y02P20/55

摘要： This invention relates to novel compounds of the general formula (I) and the pharmaceutically acceptable acid addition salts thereof. In the general formula (I) ##STR1## wherein Lip, A.sup.1, A.sup.2, Het and n are defined as in the specification. The compounds of the general formula (I) inhibit the lipid peroxidation and therefore, they are useful for the treatment or prevention of diseases and conditions wherein the inhibition of lipid peroxidation is desirable.

摘要翻译： 本发明涉及通式（I）的新化合物及其药学上可接受的酸加成盐。 在通式（I）中，其中Lip，A1，A2，Het和n如说明书中所定义。 通式（I）的化合物抑制脂质过氧化，因此它们可用于治疗或预防需要脂质过氧化抑制的疾病和病症。

公开(公告)号：US5854250A

公开(公告)日：1998-12-29

申请号：US908602

申请日：1997-08-08

申请人： Peter Matyus ,  Erzsebet Zara ,  Lajos Farkas ,  Agnes Papp ,  Antal Simay ,  Lajos Toldy ,  Ferenc Andrasi ,  Katalin Goldschmidt ,  Eszter Hodula ,  Ildiko Mathe ,  Klara Sutka ,  Zsuzsanna Fittler ,  Valeria Vitkoczi ,  Laszlo Sebestyen ,  Istvan Sziraki ,  Marta Rusz ,  Eva Gal

发明人： Peter Matyus ,  Erzsebet Zara ,  Lajos Farkas ,  Agnes Papp ,  Antal Simay ,  Lajos Toldy ,  Ferenc Andrasi ,  Katalin Goldschmidt ,  Eszter Hodula ,  Ildiko Mathe ,  Klara Sutka ,  Zsuzsanna Fittler ,  Valeria Vitkoczi ,  Laszlo Sebestyen ,  Istvan Sziraki ,  Marta Rusz ,  Eva Gal

IPC分类号： C07C235/60 ,  C07C237/22 ,  C07C259/06 ,  C07D207/26 ,  C07D207/263 ,  C07D239/50 ,  C07D295/185 ,  A61K31/495 ,  A61K31/505 ,  C07D241/04

CPC分类号： C07D207/27 ,  C07C235/60 ,  C07C237/22 ,  C07C259/06 ,  C07D239/50 ,  C07D295/185

摘要： An N-benzoylamino acid compound of the formula (I), ##STR1## wherein R.sup.3 is an NR.sup.4 R.sup.5 group where R.sup.4 and R.sup.5 which are the same or different are selected from the group consisting of hydrogen, a hydroxyl group, a C.sub.1-12 alkyl group, a C.sub.1-4 alkyl group substituted by a hydroxyl group and a C.sub.1-4 alkyl group substituted by an amino group; R.sup.4 and R.sup.5 when taken together with the adjacent nitrogen form a substituted or unsubstituted 5- or 6-membered heterocyclic group, a 5- or 6-membered heterocyclic group containing an additional nitrogen atom, a 5- or 6-membered heterocyclic group containing an additional nitrogen atom and being substituted by an oxo group, a phenyl-substituted C.sub.1-4 alkyl group or C.sub.3-5 alkenyl group; with the proviso that when the heterocyclic group is piperazine, this heterocyclic group may also be substituted by a diaminopyrimidinyl or di(pyrrolidino)-pyrimidinyl group; n is an integer from 2 to 15; and their tautomers, racemates and the pure optically active individual isomers or mixtures thereof, and a pharmaceutically acceptable salt thereof is described. These compounds are useful for the treatment of patients suffering from disorders being in an indirect or direct connection with pathological oxidation processes occurring in the organism, particularly ischaemic and reperfusion tissue injuries, inflammations, atherosclerosis, or degenerative neurological disorders.

摘要翻译： 式（I）的N-苯甲酰氨基酸化合物，其中R 3是NR 4 R 5基团，其中R 4和R 5相同或不同，选自氢，羟基，C 1-12烷基 基团，被羟基取代的C 1-4烷基和被氨基取代的C 1-4烷基; R 4和R 5与相邻的氮原子一起形成取代或未取代的5元或6元杂环基，含有另外的氮原子的5元或6元杂环基，含有 另外的氮原子被氧代基取代，苯基取代的C 1-4烷基或C 3-5烯基; 条件是当杂环基为哌嗪时，该杂环基也可以被二氨基嘧啶基或二（吡咯烷子基） - 嘧啶基取代; n为2〜15的整数。 及其互变异构体，外消旋体和纯的光学活性单体异构体或其混合物及其药学上可接受的盐。 这些化合物可用于治疗患有与生物体内发生的病理氧化过程间接或直接相关的疾病的患者，特别是缺血和再灌注组织损伤，炎症，动脉粥样硬化或退行性神经障碍。

公开(公告)号：US5705529A

公开(公告)日：1998-01-06

申请号：US540924

申请日：1995-10-11

申请人： Peter Matyus ,  Erzsebet Zara ,  Lajos Farkas ,  Agnes Papp ,  Antal Simay ,  Lajos Toldy ,  Ferenc Andrasi ,  Katalin Goldschmidt ,  Eszter Hodula ,  Ildiko Mathe ,  Klara Sutka ,  Zsuzsanna Fittler ,  Valeria Vitkoczi ,  Laszlo Sebestyen ,  Istvan Sziraki ,  Marta Rusz ,  Eva Gal

发明人： Peter Matyus ,  Erzsebet Zara ,  Lajos Farkas ,  Agnes Papp ,  Antal Simay ,  Lajos Toldy ,  Ferenc Andrasi ,  Katalin Goldschmidt ,  Eszter Hodula ,  Ildiko Mathe ,  Klara Sutka ,  Zsuzsanna Fittler ,  Valeria Vitkoczi ,  Laszlo Sebestyen ,  Istvan Sziraki ,  Marta Rusz ,  Eva Gal

IPC分类号： A61K31/165 ,  A61K31/19 ,  A61K31/215 ,  A61K31/505 ,  A61P3/06 ,  C07C231/02 ,  C07C235/52 ,  C07C235/60 ,  C07C237/22 ,  C07C259/06 ,  C07D207/26 ,  C07D207/263 ,  C07D239/50 ,  C07D295/185 ,  C07C229/14

CPC分类号： C07D207/27 ,  C07C235/60 ,  C07C237/22 ,  C07C259/06 ,  C07D239/50 ,  C07D295/185

摘要： The invention relates to novel N-benzoylamino acid derivatives of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2, which are the same or different, stand for a hydroxyl group optionally bearing an acetyl group; or a C.sub.1-6 alkoxy group optionally substituted by a phenyl group; n means an integer from 2 to 15 as well as their tautomers, racemates and optically active individual (pure) isomers or mixtures thereof and the salts of these compounds and pharmaceutical compositions containing these compounds. The invention relates also to a process for the preparation of compounds of the general formula (I). The compounds of general formula (I) inhibit the peroxidation of lipids and therefore, they are expected to be useful for the treatment of diseases being in an indirect or direct connection with pathological oxidation processes, chiefly for the treatment and/or prevention of ischaemic and reperfusion tissue injuries, inflammatory reactions, atherosclerosis, various degenerative neurological disorders as well as for delaying the natural process of the ageing of cells.

摘要翻译： 本发明涉及通式（I）的新型N-苯甲酰氨基酸衍生物，其中R1和R2相同或不同，代表任选带有乙酰基的羟基; 或任选被苯基取代的C 1-6烷氧基; n表示2至15的整数，以及它们的互变异构体，外消旋体和光学活性个体（纯）异构体或其混合物，以及这些化合物的盐和含有这些化合物的药物组合物。 本发明还涉及制备通式（I）化合物的方法。 通式（I）的化合物抑制脂质的过氧化，因此预期它们可用于治疗与病理氧化过程间接或直接相关的疾病，主要用于治疗和/或预防缺血和 再灌注组织损伤，炎症反应，动脉粥样硬化，各种退行性神经障碍以及延缓细胞老化的自然过程。

公开(公告)号：US5037830A

公开(公告)日：1991-08-06

申请号：US500936

申请日：1990-03-29

申请人： Gabor Zolyomi ,  Ferenc Andrasi ,  Pal Berzsenyi ,  Elemer Ezer ,  Tibor Hasko ,  Erzsebet F. Birkas ,  Erno Koltai ,  Judit Matuz ,  Lajos Toldy ,  Laszlo Sebestyen ,  Zsuzsanna Fittler ,  Katalin Saghy ,  Laszlo Szporny ,  Peter Aranyi

发明人： Gabor Zolyomi ,  Ferenc Andrasi ,  Pal Berzsenyi ,  Elemer Ezer ,  Tibor Hasko ,  Erzsebet F. Birkas ,  Erno Koltai ,  Judit Matuz ,  Lajos Toldy ,  Laszlo Sebestyen ,  Zsuzsanna Fittler ,  Katalin Saghy ,  Laszlo Szporny ,  Peter Aranyi

IPC分类号： A61K31/505 ,  A61K31/513 ,  A61P1/04 ,  A61P43/00 ,  C07D239/56 ,  C07D401/02 ,  C07D401/12

CPC分类号： C07D239/56 ,  C07D401/12

摘要： The present invention relates to novel compounds of the formula (I), ##STR1## wherein R.sub.1 and R.sub.2 stand independently from each other, for hydrogen, C.sub.1-4 alkyl, phenyl, phenyl-C.sub.1-4 alkyl, piridyl or piridyl-C.sub.1-4 alkyl group;E means a straight or branched, saturated hydrocarbon chain containing 1 to 6 carbon atoms;R.sub.3 represents: a phenyl group ortho-substituted by a C.sub.2-5 alkanoylamino, N-C.sub.2-5 alkanoyl-N-C.sub.1-4 alkylamino or di(C.sub.1-4 alkyl)amino group and optionally further substituted by halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or C.sub.2-5 alkanoyloxy group; or a pyridyl group optionally mono- or polysubstituted by halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.2-5 alkanoyloxy or phenyl-C.sub.1-4 alkoxy groupas well as their acid addition salts and tautomeric forms of these compounds.The compounds according to the invention show gastric acid secretion-inhibiting and cytoprotective effects and are useful for the treatment of ulcers of the gastrointestinal system.

公开(公告)号：US4748175A

公开(公告)日：1988-05-31

申请号：US947700

申请日：1986-12-30

申请人： Endre Kasztreiner ,  Gyorgy Rabloczky ,  Nandor Makk ,  Gyorgy Cseh ,  Maria Kuhar nee Kurthy ,  Eszter Diesler ,  Laszlo Jaszlits ,  Laszlo Sebestyen ,  Janos Wellmann ,  Aniko Tegdes ,  Judit Sarossy nee Kincsesy ,  Peter Matyus ,  Andras Varro ,  Laszlo Szam ,  Sarolta Vegvari nee Gyurki

发明人： Endre Kasztreiner ,  Gyorgy Rabloczky ,  Nandor Makk ,  Gyorgy Cseh ,  Maria Kuhar nee Kurthy ,  Eszter Diesler ,  Laszlo Jaszlits ,  Laszlo Sebestyen ,  Janos Wellmann ,  Aniko Tegdes ,  Judit Sarossy nee Kincsesy ,  Peter Matyus ,  Andras Varro ,  Laszlo Szam ,  Sarolta Vegvari nee Gyurki

IPC分类号： A61K31/535 ,  A61K31/5383 ,  A61P9/00 ,  A61P9/04 ,  A61P9/08 ,  A61P9/10 ,  C07D498/04

CPC分类号： C07D498/04

摘要： The invention relates to novel pyrimido [5,4-b][1,4]oxazine derivatives of the formula (I), and the acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the formula (I) ##STR1## wherein R.sup.1 stands for a C.sub.1-4 alkyl group;R.sup.2 stands for hydrogen or halogen or an azido group or an --NR.sup.5 R.sup.6 group, whereinR.sup.5 represents hydrogen or a benzyl group, or a C.sub.1-4 alkyl group unsubstituted or substituted by a hydroxyl group,R.sup.6 stands for hydrogen, an amino group, a C.sub.3-6 cycloalkyl group, a straight or branched-chain C.sub.1-4 alkyl group optionally substituted by a hydroxyl, mercapto, aminocarbonyl, furyl, 2-benzo[1,4]dioxanyl, di(C.sub.1-4 alkyl)amino group or by a phenyl or phenoxy group optionally mono- or polysubstituted by halogen or C.sub.1-4 alkoxy group (s) or by a 6-membered, saturated nitrogen-containing heterocycle optionally containing an additional nitrogen or oxygen atom and optionally substituted by a C.sub.1-4 alkyl or benzyl group; furtherNR.sup.5 R.sup.6 may also represents a 6-membered, saturated, nitrogen-containing heterocycle optionally containing an additional nitrogen or oxygen atom and optionally substituted by a C.sub.2-4 alkoxycarbonyl or C.sub.1-4 hydroxyalkyl group;R.sup.3 and R.sup.4 are the same or different and stand for hydrogen or a C.sub.1-4 alkyl group;R.sup.9 stands for hydrogen or a C.sub.1-4 alkyl group unsubstituted or monosubstituted by an oxo, cyano, aminocarbonyl, C.sub.2-5 alkoxycarbonyl, pyridiyl, morpholinocarbonyl, or phenyl group or mono- or polysubstituted by OH group(s), with the proviso that R.sup.2 is different from chlorine, 4-morpholinyl and piperidyl group when R.sup.9 stands for hydrogen; orR.sup.2 is different from chlorine and 4-morpholinyl group when R.sup.9 stands for a methyl or benzyl group.The compounds of the formula (I) are capable to increase the myocardial contractile force (the performance of the failing heart) and the coronary blood flow, thus they can therapeutically be used for the treatment of the chronic heart failure and coronary disturbances.