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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.
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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。
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