公开(公告)号：US4691017A

公开(公告)日：1987-09-01

申请号：US912999

申请日：1986-09-26

申请人： Elemer Ezer ,  Kalman Harsanyi ,  Hajnalka Vikar nee Petho ,  Judit Matuz ,  Laszlo Szporny ,  Eszter Cholnoky ,  Osaba Kuthi ,  Ferenc Trischler ,  Bela Hegedus ,  Marta Kapolnas nee Pap ,  Anna Kallay nee Sohonyai

发明人： Elemer Ezer ,  Kalman Harsanyi ,  Hajnalka Vikar nee Petho ,  Judit Matuz ,  Laszlo Szporny ,  Eszter Cholnoky ,  Osaba Kuthi ,  Ferenc Trischler ,  Bela Hegedus ,  Marta Kapolnas nee Pap ,  Anna Kallay nee Sohonyai

IPC分类号： C07D213/70 ,  C07D213/80 ,  C07D213/82 ,  C07D401/12

CPC分类号： C07D213/70 ,  C07D213/80 ,  C07D213/82 ,  C07D401/12

摘要： New intermediate compounds of the formula (I) are disclosed ##STR1## wherein R is hydrogen or C.sub.1 to C.sub.4 alkyl;Z is phenyl optionally substituted by one or more halogen atoms and/or alkyl groups having 1 to 4 carbon atoms; andD is hydroxy, mesyloxy, p-tosyloxy, or halogen; or pharmaceutically acceptable acid addition salt thereof. The compounds of the Formula (I) are intermediates in the preparation of new compounds having anti-ulcer activity.

摘要翻译： 公开了式（I）的新的中间体化合物：其中R是氢或C1-C4烷基; Z是任选被一个或多个卤素原子和/或具有1至4个碳原子的烷基取代的苯基; 和D是羟基，甲磺酰氧基，对甲苯磺酰氧基或卤素; 或其药学上可接受的酸加成盐。 式（I）的化合物是制备具有抗溃疡活性的新化合物的中间体。

公开(公告)号：US4782052A

公开(公告)日：1988-11-01

申请号：US783911

申请日：1985-10-03

申请人： Ferenc Soti ,  Csaba Szantay ,  Maria Incze ,  Zsuzsanna Balogh nee Kardos ,  Elemer Ezer ,  Judit Matuz ,  Laszlo Szporny ,  Gyorgy Hajos ,  Csaba Kuthi

发明人： Ferenc Soti ,  Csaba Szantay ,  Maria Incze ,  Zsuzsanna Balogh nee Kardos ,  Elemer Ezer ,  Judit Matuz ,  Laszlo Szporny ,  Gyorgy Hajos ,  Csaba Kuthi

IPC分类号： C07D487/14 ,  A61K31/404 ,  A61K31/435 ,  A61K31/4375 ,  A61K31/454 ,  A61K31/475 ,  A61P1/04 ,  A61P9/06 ,  A61P9/08 ,  A61P21/02 ,  C07D209/04 ,  C07D221/00 ,  C07D471/14 ,  C07D471/22 ,  A61K31/55 ,  A61K31/535 ,  C07D471/04

CPC分类号： C07D471/14

摘要： The invention relates to new 1,2,3,4,6,7,12,12b-octahydroindolo[2,3,-a]quinolizin-1-yl-alkanecarboxylic acid amides of the formula (I), ##STR1## wherein R.sub.1 and R.sub.2 stand independently for a hydrogen or halogen atom, or a hydroxyl, nitro or C.sub.1-4 alkoxy group;R.sub.3 and R.sub.4 stand independently for a hydrogen atom or a C.sub.1-4 alkyl group;R.sub.5 and R.sub.6 stand independently for a hydrogen atom, C.sub.1-8 alkyl group, C.sub.3-8 alkenyl or cycloalkyl group, aryl or aralkyl group, heteroaryl or heteroaralkyl group containing oxygen, nitrogen or sulphur atom, all these groups being optionally substituted; orR.sub.5 and R.sub.6 together form an optionally substituted C.sub.2-8 .alpha.,.omega.-alkylene group, wherein one carbon atom may optionally be replaced by an oxygen or nitrogen atom; andG means a C.sub.1-4 straight chained alkylene group, as well as to their therapeutically suitable acid addition salts and pharmaceutical compositions containing these compounds. The compounds of the formula (I) have valuable therapeutic properties, namely vasodilatory, spasmolytic, antiarrhythmic and gastrocytoprotective effects. The gastrocytoprotective effect is particularly important.

摘要翻译： 本发明涉及式（I）的新的1,2,3,4,6,7,12,12b-八氢吲哚并[2,3-a]喹嗪-1-基 - 烷脒酰胺， （I）其中R1和R2独立地代表氢或卤素原子，或羟基，硝基或C1-4烷氧基; R3和R4独立地表示氢原子或C1-4烷基; R5和R6独立地表示氢原子，C1-8烷基，C3-8烯基或环烷基，芳基或芳烷基，含氧，氮或硫原子的杂芳基或杂芳烷基，所有这些基团都可以被取代; 或R 5和R 6共同形成任选取代的C 2-8α，ω-亚烷基，其中一个碳原子可任选地被氧或氮原子代替; 和G表示C 1-4直链亚烷基，以及它们的治疗上合适的酸加成盐和含有这些化合物的药物组合物。 式（I）化合物具有有价值的治疗特性，即血管舒张，解痉，抗心律失常和胃肠保护作用。 胃肠保护作用尤其重要。

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：US5214045A

公开(公告)日：1993-05-25

申请号：US551518

申请日：1990-07-11

申请人： Tamas Fodor ,  Janos Fischer ,  Laszlo Dobay ,  Elemer Ezer ,  Judit Matuz ,  Laszlo Szporny ,  Gyorgy Hajos

发明人： Tamas Fodor ,  Janos Fischer ,  Laszlo Dobay ,  Elemer Ezer ,  Judit Matuz ,  Laszlo Szporny ,  Gyorgy Hajos

IPC分类号： A61K31/16 ,  A61K31/10 ,  A61K31/195 ,  A61K31/255 ,  A61K31/425 ,  A61K31/426 ,  A61P1/04 ,  C07C317/32 ,  C07C317/44 ,  C07C323/32 ,  C07C323/54 ,  C07C323/60 ,  C07D207/16 ,  C07D277/06 ,  C07D295/16 ,  C07D295/18 ,  C07D295/185 ,  C07D295/20

CPC分类号： C07D295/185 ,  C07C317/44 ,  C07C323/54 ,  C07D207/16

摘要： Novel acrylic amide derivatives of the Formula (I) ##STR1## wherein R.sup.1 represents a hydrogen or a halogen atom or a C.sub.1-4 alkyl, a C.sub.1-4 alkoxy or a nitro group.n is an integer of 0 to 2,A represents an amino acid residue derived from a naturally occurring amino acid or an antipode thereof which is bonded to the acrylic acyl residue through its amino group; or a residue derived from thiazolidinecarboxylic acid, bonded to the acrylic acyl group through its nitrogen, or a derivative of the above residues wherein any free carboxy group is esterified with a C.sub.1-4 alkyl group or is amidated; or A represents a group of the formula ##STR2## wherein R.sub.2 is a hydrogen atom or a phenyl, C.sub.1-4 alkyl or C.sub.1-4 alkoxycarbonyl group,and their salts which have cytoprotective and antiulcer to activities. A process is also described for the preparation of said compounds.

公开(公告)号：US4762944A

公开(公告)日：1988-08-09

申请号：US25339

申请日：1987-03-13

申请人： Janos Fischer ,  Laszlo Dobay ,  Elemer Ezer ,  Judit Matuz ,  Laszlo Szporny ,  Tibor Wagner

发明人： Janos Fischer ,  Laszlo Dobay ,  Elemer Ezer ,  Judit Matuz ,  Laszlo Szporny ,  Tibor Wagner

IPC分类号： A61K31/215 ,  A61P1/04 ,  A61P43/00 ,  C07C69/00 ,  C07C69/738 ,  C07C69/76

CPC分类号： A61K31/215 ,  C07C69/00 ,  C07C69/738

摘要： The invention relates to novel butenoic acid derivatives of the general formula (Ia) having E-configuration ##STR1## as well as to their Z-izomers of the general formula ##STR2## wherein R stands for a (-)-menthyl or a (+)-menthyl group. as well as pharmaceutical compositions containing these compounds.The novel butenoic acid derivatives of the general formulae (Ia) and (Ib) possess valuable pharmacological properties, mainly gastric cytoprotective effect.

公开(公告)号：US06656921B1

公开(公告)日：2003-12-02

申请号：US09403714

申请日：2000-09-21

申请人： Janos Illes ,  Judit Matuz ,  Erzsabet Neszmelyi ,  Gaborne Forrai ,  Bela Stefko ,  Katalin Saghy ,  Laszlo Szporny

发明人： Janos Illes ,  Judit Matuz ,  Erzsabet Neszmelyi ,  Gaborne Forrai ,  Bela Stefko ,  Katalin Saghy ,  Laszlo Szporny

IPC分类号： A61K31715

CPC分类号： A61K31/728 ,  A61K47/61

摘要： The invention relates to pharmaceutical compositions against peptic ulcer as well as to a method of treating peptic ulcer. The compositions contain and the method of treatment employs zinc hyaluronate as an active ingredient having a molecular weight in the range of 500,000 to 1,200,000 daltons.

摘要翻译： 本发明涉及消化性溃疡的药物组合物以及治疗消化性溃疡的方法。 组合物含有和治疗方法使用透明质酸锌作为分子量在500,000至1,200,000道尔顿范围内的活性成分。

公开(公告)号：US4923888A

公开(公告)日：1990-05-08

申请号：US248969

申请日：1988-09-26

申请人： Tamas Fodor ,  Laaszlo Dobay ,  Jaanos Fischer ,  Bela Stefkoo ,  Elemeer Ezer ,  Judit Matuz ,  Katalin Saghy ,  Laaszlo Szporny

发明人： Tamas Fodor ,  Laaszlo Dobay ,  Jaanos Fischer ,  Bela Stefkoo ,  Elemeer Ezer ,  Judit Matuz ,  Katalin Saghy ,  Laaszlo Szporny

IPC分类号： C07C231/02 ,  A61K31/195 ,  A61K31/22 ,  A61P1/04 ,  A61P43/00 ,  C07C67/00 ,  C07C231/00 ,  C07C233/12 ,  C07C235/78

CPC分类号： A61K31/195 ,  C07C233/12 ,  Y02P20/55

摘要： The present invention relates to novel compounds of the general formula (I), ##STR1## wherein R stands for hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or C.sub.1-4 acylamino group;R.sub.1 means hydrogen or a carboxyl-protective group; andR.sub.2 represents a --(CH.sub.2).sub.n --CO.sub.2 R.sub.5 group, whereinn is 1, 2, 3 or 4; andR.sub.5 stands for hydrogen or a carboxyl-protective group; orR.sub.2 means a --(CH.sub.2).sub.n --NH.sub.2 group, whereinn is 1, 2, 3 or 4of E and/or Z configurtion as well as their salts.The compounds according to the invention show a cytoprotective effect and promote the healing of the stomach ulcer. Their toxicity is low.