专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 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。

2. 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。

3. 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。

4. 发明授权

US4308386A Novel pyridazinylhydrazones and method of administering same 失效
标题翻译：新型哒嗪基腙及其施用方法
公开(公告)号：US4308386A
公开(公告)日：1981-12-29
申请号：US89859
申请日：1979-10-31
申请人： Szilagyi Geza , 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： Szilagyi Geza , 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
CPC分类号： C07D237/24 , C07D237/20 , C07D237/22
摘要： Pyridazinylhydrazones capable of lowering blood pressure have 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 chloro; 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具有式“IMAGE”，其中R 1是氢，氯，具有1至4个碳原子的烷基，甲氧基，羟基，氨基甲酰基或氰基; R2是氯; 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。

5. 发明授权

US4287194A Compositions with potentiated hypotensive effects 失效
标题翻译：具有强化降压作用的组合物
公开(公告)号：US4287194A
公开(公告)日：1981-09-01
申请号：US55263
申请日：1979-07-06
申请人： Edit Kosa , Janos Borvendeg , Zsuzsanna Huszti , Judit Kosary , Geza Szilagyi , Laszlo Tardos , Endre Kasztreiner , Laszlo Nagy , Erzsebet Szuucs , Gabriella Kiss
发明人： Edit Kosa , Janos Borvendeg , Zsuzsanna Huszti , Judit Kosary , Geza Szilagyi , Laszlo Tardos , Endre Kasztreiner , Laszlo Nagy , Erzsebet Szuucs , Gabriella Kiss
IPC分类号： A61K31/13 , A61K31/135 , A61K31/165 , A61K31/40 , A61K31/50 , A61K31/535 , A61P9/12 , A61K31/235 , A61K31/495
CPC分类号： A61K31/50 , A61K31/40
摘要： A pharmaceutical compositions with hypotensive effects which comprise a compound of formula (I) or a pharmaceutically acceptable acid addition salt thereof, ##STR1## wherein R.sup.1 is formula (II) ##STR2## wherein R.sup.4 and R.sup.5 each represent hydrogen, hydroxy, nitro at the same timeR.sup.2 and R.sup.3 are hydrogen, orR.sup.1 are 3-chloro-6-pyridazinylamino, 3-methyl-6-pyridazinylamino or 3-carbamoyl-6-pyridazinylamino, and at the same timeR.sup.2 and R.sup.3 form together formula (III), ##STR3## wherein R.sup.6 is C.sub.1-4 alkyl group,R.sup.7 is hydrogen or a C.sub.1-4 alkyl group, andn is an integer of 1 to 3, orR.sup.2 and R.sup.3 form together a group of the general formula (IV),=Q-R.sup.8 (IV)whereinQ is C.sub.5-7 cycloaliphatic, andR.sup.8 is hydrogen, a C.sub.1-4 alkoxycarbonyl or a C.sub.2-4 alkyl,and a compound of formula (V) or a pharmaceutically acceptable acid addition salt thereof, ##STR4## wherein R.sup.9 is naphthyl, 4-indolyl or 4-morpholino-1,2,5-thiadiazol-3-yl group or ##STR5## .
摘要翻译：具有降血压作用的药物组合物，其包含式（I）化合物或其药学上可接受的酸加成盐，其中R 1为式（II）其中R 4和R 5各自表示氢，羟基，硝基，同时R2和R3是氢，或R1是3-氯-6-哒嗪基氨基，3-甲基-6-哒嗪基氨基或3-氨基甲酰基-6-哒嗪基氨基，同时R2和R3形成（III），其中R6为C1-4烷基，R7为氢或C1-4烷基，n为1〜3的整数，或R2和R3一起形成基团通式（IV）的化合物= Q-R8（Ⅳ）其中Q为C5-7环脂族基，R8为氢，C1-4烷氧基羰基或C2-4烷基，式（Ⅴ）化合物或式（V）其中R 9为萘基，4-吲哚基或4-吗啉代-1,2,5-噻二唑-3-基或Ⅵ（VI）。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式