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1. 发明授权

US4418205A 16-Amino-18,19,20-trinor-prostaglandin derivatives, and acid addition salts 失效
标题翻译： 16-氨基-18,19,20-三肽前列腺素衍生物和酸加成盐
公开(公告)号：US4418205A
公开(公告)日：1983-11-29
申请号：US329039
申请日：1981-12-09
申请人： Eva Toth-Sarudy , Gabor Ambrus , Gyorgy Cseh , Janos Borvendeg , Imre Moravcsik , Gabriella Mezei
发明人： Eva Toth-Sarudy , Gabor Ambrus , Gyorgy Cseh , Janos Borvendeg , Imre Moravcsik , Gabriella Mezei
IPC分类号： A61K31/557 , A61K31/5575 , A61P15/00 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07C177/00
CPC分类号： C07C405/0041 , Y02P20/55
摘要： The invention relates to new 16-amino-18,19,20-trinor-prostaglandin derivatives of general formula I, having at C-17 a substituted or unsubstituted phenyl group, wherein C-15 and C-16 may have either S or R configuration, Y stands for a hydrogen atom or a lower alkyl group, W stands for a hydrogen atom, halogen atom, hydroxy group, lower alkyl or alkoxy group, and their acid addition salts. These compounds can be prepared by removing the ester group and the p-nitrobenzyloxycarbonyl protective group of a 9.alpha.,11.alpha.,15-trihydroxy-16-p-nitrobenzyloxycarbonylamido-17-phenyl-5-cis,13-trans-18,19,20-trinor-prostadienoic acid derivative of general formula XII--wherein C-15 and C-16 may have either S or R configuration, W is as defined above, and Y stands for a lower alkyl group--in an optional sequence with the limitation that in those compounds of general formula I where W is as defined above and Y stands for a lower alkyl group, solely the p-nitrobenzyloxycarbonyl group is removed, and the resulting product of general formula I is optionally converted with an organic or inorganic acid into a salt.The new prostaglandin derivatives of the invention have valuable therapeutical properties, and can be applied in cattle raising for estrus and birth synchronization, furthermore in the veterinary praxis for the treatment of sterility, chronic endometritis and pyometry.
摘要翻译：本发明涉及具有C-17取代或未取代的苯基的通式I的新的16-氨基-18,19,20-三核 - 前列腺素衍生物，其中C-15和C-16可具有S或R 构型中，Y表示氢原子或低级烷基，W表示氢原子，卤素原子，羟基，低级烷基或烷氧基，以及它们的酸加成盐。这些化合物可以通过除去9α，11α，15-三羟基-16-对硝基苄氧羰基酰胺基-17-苯基-5-顺式，13-trn-18的酯基和对硝基苄氧羰基保护基来制备，其中C-15和C-16可以具有S或R构型，W如上所定义，Y代表低级烷基 - 在任选的序列中，具有通式XII-的19,20-三过 - 前列腺素酸衍生物 - 在通式I的那些化合物中的限制，其中W如上所定义，Y代表低级烷基，仅除去对硝基苄氧基羰基，所得到的通式I的产物任选地用有机或无机酸变成盐。本发明的新型前列腺素衍生物具有有价值的治疗特性，可用于发情期和出生同步的养牛，此外还适用于无菌治疗，慢性子宫内膜炎和高血压的兽医学应用。

2. 发明授权

US4372973A 16-Amino-postaglandin derivatives, their acid addition salts, and a process for the preparation thereof 失效
标题翻译： 16-氨基 - Postaglandin衍生物及其酸加成盐及其制备方法
公开(公告)号：US4372973A
公开(公告)日：1983-02-08
申请号：US332840
申请日：1981-12-21
申请人： Gabor Ambrus , Eva Toth-Sarudy , Gyorgy Cseh , Istvan Barta , Gyula Horvath
发明人： Gabor Ambrus , Eva Toth-Sarudy , Gyorgy Cseh , Istvan Barta , Gyula Horvath
IPC分类号： A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C12P31/00 , C07C177/00
CPC分类号： C12P31/00 , C07C405/0041 , Y02P20/55
摘要： The invention relates to new 16-amino-prostaglandin derivatives of general formula I, ##STR1## wherein C-15 and C-16 may have either S or R configuration, Z stands for a hydrogen atom or a lower alkyl group, and their acid addition salts. These compounds can be prepared by removing the ester group and the p-nitrocarbobenzyloxy protective group of a 9.alpha., 11.alpha., 15-trihydroxy-16-p-nitrobenzyloxycarbonylamido-5-cis,13-trans-prostadienoic acid derivative of general formula XII--wherein C-15 and C-16 may have either S or R configuration and Z stands for a lower alkyl group--in an optional sequence with the limitation that in those compounds of general formula I where Z stands for a lower alkyl group solely the p-nitrocarbobenzyloxy group is removed, and the resulting product of general formula I is optionally converted with an organic or inorganic acid into a salt.The new prostaglandin derivatives of the invention have valuable therapeutical properties, and can be applied as abortive or oxytocic agents.
摘要翻译：本发明涉及通式I的新的16-氨基前列腺素衍生物，其中C-15和C-16可以具有S或R构型，Z代表氢原子或低级烷基，它们的酸加成盐。这些化合物可以通过除去通式9的9α，11α，15-三羟基-16-对硝基苄氧基羰基酰胺基-5-顺式，13-反式 - 前列腺烯酸衍生物的酯基和对硝基苄氧基保护基来制备 XII-其中C-15和C-16可以具有S或R构型，Z表示低级烷基 - 在任选的序列中，限制在通式I的那些化合物中，其中Z仅代表低级烷基除去对硝基羰基苄氧基，将所得的通式I的产物任选地用有机或无机酸转化成盐。本发明的新型前列腺素衍生物具有有价值的治疗性质，可用作流产或催产素。

3. 发明授权

US4826845A 3(2H)-pyridazinones and pharmaceutical compositions thereof 失效
标题翻译： 3（2H） - 哒嗪酮及其药物组合物
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。

4. 发明授权

US4623641A Method of treating ulcers and erosions in the gastrointestinal system using PGI.sub.2 -methyl ester-beta cyclodextrin inclusion complexes 失效
标题翻译：使用PGI2-甲酯-β环糊精包合物治疗胃肠系统溃疡和糜烂的方法
公开(公告)号：US4623641A
公开(公告)日：1986-11-18
申请号：US774177
申请日：1985-09-09
申请人： Jozsef Szejtli , Magdolna Szejtli nee Rengei , Gyorgy Cseh , Istvan Stadler
发明人： Jozsef Szejtli , Magdolna Szejtli nee Rengei , Gyorgy Cseh , Istvan Stadler
IPC分类号： A61K31/557 , A61K31/715 , A61K47/48 , A61K31/70
CPC分类号： B82Y5/00 , A61K31/557 , A61K31/715 , A61K47/48969
摘要： A new method is disclosed for the treatment and prevention of gastrointestinal ulcers or erosions which comprises the administration of a pharmaceutically effective amount of a PGI.sub.2 methyl ester-beta cyclodextrin complex to a patient in need of said treatment wherein the amount of the PGI.sub.2 methyl ester constitutes 1 to 15% by weight of the complex.
摘要翻译：公开了用于治疗和预防胃肠溃疡或糜烂的新方法，其包括向需要所述治疗的患者施用药学有效量的PGI 2甲酯-β环糊精复合物，其中PGI 2甲酯的量构成 1至15重量％的络合物。

5. 发明授权

US4259328A Morpholino pyridazinylhydrazones 失效
标题翻译：吗啉代哒嗪基腙
公开(公告)号：US4259328A
公开(公告)日：1981-03-31
申请号：US914778
申请日：1978-06-12
申请人： Geza Szilagyi , Endre Kasztreiner , Judit Kosary , Peter Matyus , Zsuzsa Huszti , Gyorgy Cseh , Agnes Kenessey , Laszlo Tardos , Edit Kosa , Laszlo Jaszlits , Sandor Elek , Istvan Elekes , Istvan Polgari
发明人： Geza Szilagyi , Endre Kasztreiner , Judit Kosary , Peter Matyus , Zsuzsa Huszti , Gyorgy Cseh , Agnes Kenessey , Laszlo Tardos , Edit Kosa , Laszlo Jaszlits , Sandor Elek , Istvan Elekes , Istvan Polgari
IPC分类号： A61K31/50 , A61P9/12 , C07D237/20 , C07D237/22 , C07D237/24 , C07D401/04 , C07D295/00 , A61K31/535
CPC分类号： C07D237/24 , C07D237/20 , C07D237/22
摘要： Pyridazinylhydrazones capable of lowering blood pressure having the formula ##STR1## wherein R.sup.1 is hydrogen, chlorine, alkyl having from 1 to 4 carbon atoms, methoxy, hydroxyl, carbamoyl or cyano;R.sup.2 is morpholino; andK is a group having the formula ##STR2## wherein one of R.sup.3, R.sup.4, R.sup.5 or R.sup.6 is carboxyl or alkoxycarbonyl.
摘要翻译：能够降低血压的哒嗪基腙类具有下式：其中R1是氢，氯，具有1-4个碳原子的烷基，甲氧基，羟基，氨基甲酰基或氰基; R2是吗啉代; 并且K是具有式“IMAGE”的基团，其中R 3，R 4，R 5或R 6中的一个是羧基或烷氧基羰基。

6. 发明授权

US4224325A 3-(1-Pyrazolyl)-pyridazine derivatives and hypotensive compositions thereof 失效
标题翻译： 3-（1-吡唑基） - 哒嗪衍生物及其低血压组合物
公开(公告)号：US4224325A
公开(公告)日：1980-09-23
申请号：US923623
申请日：1978-07-11
申请人： Geza Szilagyi , Endre Kasztreiner , Laszlo Tardos , Edit Kosa , Laszlo Jaszlits , Gyorgy Cseh , Ilona Kovacs, nee Szabo , Pal Tolnay , Sandor Elek , Istvan Elekes , Istvan Polgari
发明人： Geza Szilagyi , Endre Kasztreiner , Laszlo Tardos , Edit Kosa , Laszlo Jaszlits , Gyorgy Cseh , Ilona Kovacs, nee Szabo , Pal Tolnay , Sandor Elek , Istvan Elekes , Istvan Polgari
IPC分类号： C07D403/04 , A61K31/50 , A61K31/501 , A61P9/12 , A61P43/00 , C07D403/14 , C07D521/00 , A61K31/535 , C07D413/14
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： The invention relates to compounds of general formula ##STR1## wherein R.sup.1 stands for a hydrogen atom or a C.sub.1-6 alkyl-, a C.sub.2-4 hydroxyalkyl, a C.sub.3-6 cycloalkyl or a phenyl group,R.sup.2 stands for a hydrogen, fluorine, chlorine or bromine atom or a C.sub.1-6 alkyl, a C.sub.2-4 hydroxyalkyl, a nitro or an --NR.sup.5 R.sup.6 group, wherein R.sup.5 and R.sup.6 may have the same or different meaning and stand each for a hydrogen atom or a C.sub.1-4 alkyl or a C.sub.2-4 hydroxyalkyl group,R.sup.3 stands for a hydrogen atom or a C.sub.1-6 alkyl, a C.sub.2-4 hydroxyalkyl, a C.sub.3-6 cycloalkyl or a phenyl group, a chlorine atom or a hydroxyl, amino or methoxy group,R.sup.4 stands for a carbamoyl, a cyano or an --NR.sup.7 --NHR.sup.8 group, wherein R.sup.7 and R.sup.8 may have the same or different meaning and stand each for a hydrogen atom or a C.sub.1-4 alkyl, a C.sub.2-4 hydroxyalkyl, a C.sub.1-4 alkoxycarbonyl or an --NR.sup.9 R.sup.10 group, wherein R.sup.9 and R.sup.10 may have the same or different meaning and stand each for a hydrogen atom or a C.sub.1-5 alkyl, a C.sub.2-4 hydroxyalkyl, a C.sub.3-6 cycloalkyl, a phenyl or a benzyl group, or --NR.sup.9 R.sup.10 may represent a morpholine, piperidine or piperazine ring,and their pharmaceutically acceptable acid-addition salts. Furthermore, the invention relates to a process for preparing these compounds.The novel compounds of general formula I have valuable pharmacological properties. Thus they show a considerable hypotensive effect and are capable to inhibit enzymes regulating the catabolism of prostaglandins.
摘要翻译：本发明涉及通式为“IMAGE”的化合物，其中R1代表氢原子或C1-6烷基，C2-4羟基烷基，C3-6环烷基或苯基，R2代表氢，氟，氯或溴原子或C 1-6烷基，C 2-4羟基烷基，硝基或-NR 5 R 6基团，其中R 5和R 6可以具有相同或不同的含义，并且各自代表氢原子或C 1-4烷基或 C2-4羟基烷基，R3代表氢原子或C1-6烷基，C2-4羟烷基，C3-6环烷基或苯基，氯原子或羟基，氨基或甲氧基，R4代表对于氨基甲酰基，氰基或-NR 7 -NHR 8基团，其中R 7和R 8可以具有相同或不同的含义，各自代表氢原子或C 1-4烷基，C 2-4羟烷基，C 1-4烷氧基羰基或-NR 9 R 10基团，其中R 9和R 10可以具有相同或不同的含义，并且各自表示氢原子或C 1-5烷基，C 2-4的羟基烷基，C 3-6环烷基，苯基或苯基或-NR9R10可以表示吗啉，哌啶或哌嗪环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。通式Ⅰ的新化合物具有有价值的药理学性质。因此，它们显示出相当的降血压作用，并且能够抑制调节前列腺素分解代谢的酶。

7. 发明授权

US4632928A Pyrazole derivatives with an ergoline skeleton, their acid addition salts, and a process for the preparation thereof 失效
标题翻译：具有麦角无骨骨架的吡唑衍生物及其酸加成盐及其制备方法
公开(公告)号：US4632928A
公开(公告)日：1986-12-30
申请号：US615387
申请日：1984-05-30
申请人： Tivadar Rettegi , Erzsebet Mago nee Karacsony , Lajos Toldy , Jozsef Borsy , Ilona Berzetei , Andras Ronai , Aliz Druga , Gyorgy Cseh
发明人： Tivadar Rettegi , Erzsebet Mago nee Karacsony , Lajos Toldy , Jozsef Borsy , Ilona Berzetei , Andras Ronai , Aliz Druga , Gyorgy Cseh
IPC分类号： A61K31/48 , A61P1/00 , A61P9/12 , A61P11/00 , A61P43/00 , C07D457/02
CPC分类号： C07D457/02
摘要： The invention relates to novel pyrazole derivatives with an ergoline skeleton of the general formula I, ##STR1## wherein x . . . y stands for a ##STR2## R is a hydrogen atom or methyl group, R.sub.1 stands for a hydrogen atom, C.sub.1-4 alkyl, carbethoxy or pyridyl-group,R.sub.2 stands for a hydrogen atom, C.sub.1-4 alkyl, allyl, C.sub.2-4 oxoalkyl-, C.sub.2-4 hydroxyalkyl or C.sub.2-4 hydroxyiminoalkyl group,R.sub.3 stands for a hydrogen atom, C.sub.1-4 alkyl, hydroxy or pyridyl group, furthermoreR.sub.2 and R.sub.3 may stand together for a group of general formula (II), ##STR3## wherein Z stands for a methylene, carbonyl, hydroxymethylene or hydroxyiminomethylene group,R.sub.4 stands for a hydrogen atom or one or two C.sub.1-4 alkyl group(s), andn is 1 or 2,and pharmaceutically acceptable salts thereof.Furthermore the invention relates to a process for the preparation of these compounds.The novel compounds are potent PGF.sub.2.alpha. receptor antagonists.
摘要翻译：本发明涉及具有通式I的麦角灵骨架的新型吡唑衍生物，其中x。。。 y表示氢原子或甲基，R1表示氢原子，C1-4烷基，乙氧基或吡啶基，R2表示氢原子，C1-4烷基，烯丙基，C2- 4个氧代烷基 - ，C2-4羟基烷基或C2-4羟基亚氨基烷基，R3代表氢原子，C1-4烷基，羟基或吡啶基，此外R2和R3可以连在一起为通式（II）图像II其中Z表示亚甲基，羰基，羟基亚甲基或羟基亚氨基亚甲基，R4表示氢原子或一个或两个C1-4烷基，n为1或2，及其药学上可接受的盐。此外，本发明涉及一种制备这些化合物的方法。新型化合物是有效的PGF2α受体拮抗剂。

8. 发明授权

US4251658A 3-(1-Pyrazolyl)-pyridazine derivatives 失效
标题翻译： 3-（1-吡唑基） - 哒嗪衍生物
公开(公告)号：US4251658A
公开(公告)日：1981-02-17
申请号：US914084
申请日：1978-06-09
申请人： Geza Szilagyi , Endre Kasztreiner , Laszlo Tardos , Edit Kosa , Laszlo Jaszlits , Gyorgy Cseh , Andras Divald , Pal Tolnay , Sandor Elek , Istvan Elekes , Istvan Polgari
发明人： Geza Szilagyi , Endre Kasztreiner , Laszlo Tardos , Edit Kosa , Laszlo Jaszlits , Gyorgy Cseh , Andras Divald , Pal Tolnay , Sandor Elek , Istvan Elekes , Istvan Polgari
IPC分类号： C07D401/14 , A61K31/50 , A61K31/501 , A61P9/12 , A61P43/00 , C07D403/04 , C07D403/14 , C07D405/14
CPC分类号： C07D403/04
摘要： 3-(1-Pyrazolyl)-pyridazine derivatives of the formula I, or pharmaceutically acceptable acid addition salts thereof, which decrease high blood pressure and inhibit catabolism or prostaglandins, ##STR1## wherein R.sup.1 is hydrogen or C.sub.1-4 alkyl,R.sup.2 is hydrogen, cyano, carboxyl, carbamoyl, carbaxoyl or C.sub.1-4 alkoxycarbonyl,R.sup.3 is hydrogen or chlorine or --NR.sup.4 NHR.sup.5 or NR.sup.6 R.sup.7, wherein R.sup.4 and R.sup.5 are each hydrogen or C.sub.1-4 alkyl, wherein R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-5 alkyl, C.sub.1-5 hydroxyalkyl, C.sub.3-7 cycloalkyl, phenyl or benzyl, or benzyl or phenylethyl substituted with one or two chlorine atoms or methoxy groups, or a furylmethyl, pyridylmethyl, pyrrolidine or piperazine ring, or when R.sup.7 is hydrogen, R.sup.6 is --(CH.sub.2).sub.n --NR.sup.4 R.sup.5 wherein n is an integer from 1 to 3.
摘要翻译：降低高血压并抑制分解代谢或前列腺素的式I的3-（1-吡唑基） - 哒嗪衍生物或其药学上可接受的酸加成盐，其中R 1是氢或C 1-4烷基， R2是氢，氰基，羧基，氨基甲酰基，碳酰基或C1-4烷氧基羰基，R3是氢或氯或-NR4NHR5或NR6R7，其中R4和R5分别是氢或C1-4烷基，其中R6和R7各自是氢或C1 或烷基，C 1-5羟基烷基，C 3-7环烷基，苯基或苄基，或被一个或两个氯原子或甲氧基取代的苄基或苯乙基，或呋喃基甲基，吡啶基甲基，吡咯烷或哌嗪环，或者当R7为氢时， R 6为 - （CH 2）n -NR 4 R 5，其中n为1至3的整数。

9. 发明授权

US4829076A Novel dihydropyridines having calcium antagonistic and antihypertensive activity 失效
标题翻译：具有钙拮抗作用和抗高血压活性的新型二氢吡啶类
公开(公告)号：US4829076A
公开(公告)日：1989-05-09
申请号：US97111
申请日：1987-09-16
申请人： Geza Szilagyi , Eva Bozo , Laszlo Czollner , Laszlo Jaszlits , Gyorgy Rabloczky , Jozsef Borsi , Istvan Elekes , Gyongyi Nagy nee Csokas , Andras Varro , ZSuzanne Lang nee Rihmer , Gyorgy Cseh , Gyula Horvath , Ilona Bodi
发明人： Geza Szilagyi , Eva Bozo , Laszlo Czollner , Laszlo Jaszlits , Gyorgy Rabloczky , Jozsef Borsi , Istvan Elekes , Gyongyi Nagy nee Csokas , Andras Varro , ZSuzanne Lang nee Rihmer , Gyorgy Cseh , Gyula Horvath , Ilona Bodi
IPC分类号： A61K31/445 , A61K31/451 , A61K31/455 , A61P3/00 , A61P9/10 , A61P9/12 , C07D211/90 , C07D401/12 , C07D405/12
CPC分类号： C07D401/12 , C07D211/90 , C07D405/12
摘要： The invention relates to new substituted dihydropyridine derivatives of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.6 are as defined herein after, the racemic and optically active variants as well as mixtures thereof, furthermore the acid addition salts of these compounds, pharmaceutical compositions containing the same and a process for the preparation thereof.The compounds of the general formula (I) can be advantageously applied for the treatment of pathologically severe hypertensions, their toxicity is low and they possess an advantageous therapeutic index.
摘要翻译：本发明涉及通式（I）的新的取代二氢吡啶衍生物，其中R 1和R 6如本文所定义，外消旋和光学活性变体及其混合物，此外，这些化合物的酸加成盐，含有该组合物的药物组合物及其制备方法。通式（I）的化合物可以有利地用于治疗病态严重的高血压，其毒性低，并且具有有利的治疗指标。

10. 发明授权

US4748175A Pyrimido[5,4-B][1,4]oxazine derivatives and pharmaceutical compositions containing them 失效
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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