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.

公开(公告)号：US4826845A

公开(公告)日：1989-05-02

申请号：US924445

申请日：1986-10-29

申请人： Endre Kasztreiner ,  Gyorgy Rablocsky ,  Nandor Makk ,  Laszlo Jaszlits ,  Peter Matyus ,  Gyorgy Cseh ,  Ildiko Pribusz nee Rapp ,  Klara Czako ,  Eszter Diesler ,  Istvan Elekes ,  Laszlo Kaufer ,  Maria Kuhar nee Kurthy ,  Judit Kincsessy ,  Judit Kosary ,  Gyongyi Nagy nee Csokas

发明人： Endre Kasztreiner ,  Gyorgy Rablocsky ,  Nandor Makk ,  Laszlo Jaszlits ,  Peter Matyus ,  Gyorgy Cseh ,  Ildiko Pribusz nee Rapp ,  Klara Czako ,  Eszter Diesler ,  Istvan Elekes ,  Laszlo Kaufer ,  Maria Kuhar nee Kurthy ,  Judit Kincsessy ,  Judit Kosary ,  Gyongyi Nagy nee Csokas

IPC分类号： C07D237/00 ,  A61K31/50 ,  A61K31/535 ,  A61P9/12 ,  C07D237/08 ,  C07D237/12 ,  C07D237/14 ,  C07D237/20 ,  C07D237/22 ,  C07D319/00 ,  C07D403/04 ,  C07D405/12 ,  C07D521/00 ,  C07D405/06

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D237/08 ,  C07D237/12 ,  C07D237/20 ,  C07D249/08 ,  C07D403/04 ,  C07D405/12

摘要： The invention relates to novel 3(2H)-pyridazinone-derivatives of the general formula (I), pharmaceutical compositions containing them and process for their preparation. In the general formula (I) ##STR1## stands for an ethyl or propyl group substituted by a terminal halogen atom or a hydroxyl or NR.sup.1 R.sup.2 group, whereinR.sup.1 represents hydrogen atom or an unsubstituted or optionally substituted benzyl group;R.sup.2 represents hydrogen atom or an unsubstituted or optionally substituted benzo[1,4]dioxan-2-yl-methyl or -ethyl group or a (CH.sub.2).sub.n --R.sup.3 group, whereinn is 2 or 3; andR.sup.3 stands for an unsubstituted or optionally substituted phenoxy or phenylthio group; andX stands for a hydrogen or halogen atom or an unsubstituted or optionally substituted, saturated or unsaturated 5- or 6-membered heterocyclic group containing a nitrogen atom and optionally an additional heteroatom, e.g. an oxygen, sulfur or nitrogen atom,with the proviso that R is different from an ethyl or propyl group substituted terminally by a hydroxyl group or halogen atom when X represents a hydrogen or chlorine atom.The compounds of general formula (I) selectively inhibit the adrenergic alpha.sub.1 receptors, have a calcium-antagonistic effect and exert blood pressure lowering action.

摘要翻译： 本发明涉及通式（I）的新的3（2H） - 哒嗪酮衍生物，含有它们的药物组合物及其制备方法。 在通式（I）中，（I）表示被末端卤素原子或羟基或NR 1 R 2基团取代的乙基或丙基，其中R 1表示氢原子或未取代或任意取代的苄基; R 2表示氢原子或未取代或任选取代的苯并[1,4]二氧杂环己烷-2-基 - 甲基或 - 乙基或（CH 2）n -R 3基团，其中n为2或3; R3代表未取代或任选取代的苯氧基或苯硫基; X代表氢或卤素原子，或未取代或任选取代的饱和或不饱和的含有氮原子和任选另外的杂原子的5或6元杂环基团。 氧，硫或氮原子，条件是当X表示氢或氯原子时，R不同于被羟基或卤素原子末端取代的乙基或丙基。 通式（I）的化合物选择性地抑制肾上腺素α1受体，具有钙拮抗作用并发挥降血压作用。

公开(公告)号：US4840948A

公开(公告)日：1989-06-20

申请号：US51777

申请日：1987-05-20

申请人： Tibor Lang ,  Jeno Korosi ,  Gyorgy Rabloczky ,  Tamas Hamori ,  Maria Kuhar nee Kurthy ,  Istvan Polgari ,  Istvan Elekes ,  Gabor Zolyomi ,  Krisztina Heltai ,  Judit Sarossy nee Kincsesy ,  Zsuzsanna Lang nee Rihmer ,  Imre Moravcsik

发明人： Tibor Lang ,  Jeno Korosi ,  Gyorgy Rabloczky ,  Tamas Hamori ,  Maria Kuhar nee Kurthy ,  Istvan Polgari ,  Istvan Elekes ,  Gabor Zolyomi ,  Krisztina Heltai ,  Judit Sarossy nee Kincsesy ,  Zsuzsanna Lang nee Rihmer ,  Imre Moravcsik

IPC分类号： A61K31/55 ,  A61K31/551 ,  A61P9/04 ,  C07D243/02 ,  C07D243/04 ,  C07D491/056

CPC分类号： C07D243/02

摘要： This invention relates to new 1-(hydroxystyryl)-5H-2,3-benzodiazepine derivatives of the general formula (I) and to a process for the preparation thereof, furthermore to pharmaceutical compositions containing the same, ##STR1## wherein R stands for a hydrogen or halogen atom, or a C.sub.1-4 alkoxy group,R.sup.1 represents a hydrogen atom or a C.sub.1-4 alkyl group,R.sup.2 and R.sup.3 are identical and denote a C.sub.1-4 alkyl group, or combined they denote a methylene group.The compounds of the general formula (I) possess valuable positive inotropic (cardiotonic) potency, are capable to increase the myocardiac contractile force (heart performance in cardiac insufficiency), thus they can be applied in the therapy of chronic heart failure and coronary ailments.

摘要翻译： 本发明涉及通式（I）的新的1-（羟基苯乙烯基）-5H-2,3-苯并二氮杂衍生物及其制备方法，此外还涉及含有它们的药物组合物，其中 R代表氢或卤素原子，或C1-4烷氧基，R1代表氢原子或C1-4烷基，R2和R3相同并表示C1-4烷基，或组合它们表示亚甲基 组。 通式（I）的化合物具有有价值的正性肌力（强心）效能，能够增加心肌收缩力（心脏功能不全的心脏性能），因此可用于慢性心力衰竭和冠状动脉疾病的治疗。

公开(公告)号：US4731383A

公开(公告)日：1988-03-15

申请号：US925489

申请日：1986-10-29

申请人： Istvan Erczi ,  Jeno Marosfalvi ,  Gyorgy Rabloczky ,  Andras Varro ,  Maria Kuhar nee Kurthy ,  Istvan Elekes ,  Laszlo Szatmary ,  Laszlo Jaszlits

发明人： Istvan Erczi ,  Jeno Marosfalvi ,  Gyorgy Rabloczky ,  Andras Varro ,  Maria Kuhar nee Kurthy ,  Istvan Elekes ,  Laszlo Szatmary ,  Laszlo Jaszlits

IPC分类号： C07C281/16 ,  A61K31/155 ,  A61K31/40 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/55 ,  A61P9/06 ,  C07C281/10 ,  C07D211/10 ,  C07D265/30 ,  C07D295/14 ,  C07D295/215 ,  C07C133/10

CPC分类号： C07D295/215 ,  C07D265/30

摘要： The invention relates to new aminoguanidine derivatives of the general formula (I), ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each represent hydrogen or halogen atom, C.sub.1-4 alkyl, nitro, trifluoromethyl or C.sub.1-4 alkoxy group,R.sup.4 and R.sup.5 represent a C.sub.1-4 alkyl group, furthermore NR.sup.4 R.sup.5 may form a 5 to 7 membered saturated heterocyclic group containing either one or two nitrogen atoms or a nitrogen and an oxygen atom and being optionally substituted by one or two methyl, hydroxymethyl or hydroxyethyl groups,R.sup.6 and R.sup.7 each represent a hydrogen atom, normal or branched C.sub.1-4 alkyl or C.sub.2-4 alkenyl group,and to their pharmaceutically acceptable acid addition salts as well as to a process for the preparation thereof.The new compounds of the invention possess valuable antiarrhythmic activity and are devoid of the undesired circulatory side effects of the known antiarrhythmic compounds.

摘要翻译： 本发明涉及通式（I）的新氨基胍衍生物，其中R 1，R 2和R 3各自表示氢或卤素原子，C 1-4烷基，硝基，三氟甲基或C 1-4烷氧基，R 4和R 5 代表C1-4烷基，此外，NR4R5可以形成含有一个或两个氮原子或氮和氧原子的5至7元饱和杂环基，并且任选被一个或两个甲基，羟甲基或羟乙基取代，R6 和R 7各自表示氢原子，正构或支链C 1-4烷基或C 2-4链烯基，以及它们的药学上可接受的酸加成盐以及其制备方法。 本发明的新化合物具有有价值的抗心律不齐活性，并且没有已知抗心律失常化合物的不期望的循环副作用。

公开(公告)号：US4785104A

公开(公告)日：1988-11-15

申请号：US51767

申请日：1987-05-20

申请人： Gyorgy Rabloczky ,  Jeno Korosi ,  Tibor Lang ,  Istvan Ling ,  Tamas Hamori ,  Maria Kuhar nee Kurthy ,  Istvan Elekes ,  Peter Botka ,  Andras Varro ,  Sandor Elek ,  Judit Sarossy nee Kincsessy ,  Gabor Zolyomi ,  Zsuzsanna Lang nee Rihmer ,  Imre Moravcsik

发明人： Gyorgy Rabloczky ,  Jeno Korosi ,  Tibor Lang ,  Istvan Ling ,  Tamas Hamori ,  Maria Kuhar nee Kurthy ,  Istvan Elekes ,  Peter Botka ,  Andras Varro ,  Sandor Elek ,  Judit Sarossy nee Kincsessy ,  Gabor Zolyomi ,  Zsuzsanna Lang nee Rihmer ,  Imre Moravcsik

IPC分类号： C07D217/08 ,  A61K31/47 ,  A61K31/472 ,  A61P9/04 ,  A61P9/08 ,  A61P9/10 ,  A61P43/00 ,  C07D217/16 ,  C07D491/04 ,  C07D491/056

CPC分类号： C07D491/04 ,  C07D217/16

摘要： This invention relates to new 3-(hydroxymethyl)-isoquinoline derivatives of the general formula (I), their acid addition salts, and to a process for the preparation thereof, furthermore to pharmaceutical compositions containing the same, ##STR1## wherein R and R.sup.1 are identical or different and stand for a hydrogen or halogen atom, a nitro or a C.sub.1-4 alkoxy group,R.sup.2 stands for a hydrogen atom or a C.sub.1-4 alkyl group,R.sup.3 and R.sup.4 are identical or different and stand for a hydrogen atom or a C.sub.1-4 alkyl group, or R.sup.3 and R.sup.4 combined denote a methylene group,with the proviso that when R stands for 3-methoxy, R.sup.1 for 4-methoxy, R.sup.3 and R.sup.4 are identical and represent methyl or ethyl groups, R.sup.2 is other than hydrogen atom.The compounds of the general formula (I) exert valuable positive inotropic (cardiotonic) potency, they are capable to increase the myocardiac contractile force (heart performance in cardiac insufficiency), thus they can be applied in the therapy of chronic heart failure and coronary ailments.

摘要翻译： 本发明涉及通式（I）的新的3-（羟甲基） - 异喹啉衍生物及其酸加成盐，以及其制备方法，此外还涉及含有它们的药物组合物，其中 R和R1相同或不同，代表氢或卤素原子，硝基或C1-4烷氧基，R2代表氢原子或C1-4烷基，R3和R4相同或不同，代表 氢原子或C1-4烷基，或R3和R4组合表示亚甲基，条件是当R代表3-甲氧基时，R1代表4-甲氧基，R3和R4相同，代表甲基或乙基 R2不是氢原子。 通式（I）的化合物发挥有价值的正性肌力（强心）效能，它们能够增加心肌收缩力（心脏功能不全的心脏性能），因此可用于治疗慢性心力衰竭和冠状动脉疾病 。