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1. 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。

2. 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.

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

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。

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

US4244871A Sulfonamido-benzoic acid derivatives 失效
标题翻译：磺酰氨基 - 苯甲酸衍生物
公开(公告)号：US4244871A
公开(公告)日：1981-01-13
申请号：US58363
申请日：1979-07-12
申请人： Judit Kosary , Endre Kasztreiner , Zsuzsa Huszti , Agnes Kenessey , Gyorgy Cseh , Veronika Szilagyi nee Pap , Judit Stverteczky nee Sztrokay
发明人： Judit Kosary , Endre Kasztreiner , Zsuzsa Huszti , Agnes Kenessey , Gyorgy Cseh , Veronika Szilagyi nee Pap , Judit Stverteczky nee Sztrokay
IPC分类号： A61K31/63 , A61P9/12 , C07C20060101 , C07C67/00 , C07C301/00 , C07C311/39 , C07D295/08 , C07D295/14 , C07D295/155 , C07D295/16 , C07D295/18 , C07D295/192 , C07D413/10 , C07C103/22 , C07C143/80 , C07D265/28
CPC分类号： C07D295/192 , A61K31/63 , C07D295/14 , C07D295/155 , C07D295/18 , C07D413/10 , C07C2101/14
摘要： The invention relates to novel sulfonamidobenzoic acid derivatives having the general formula ##STR1## wherein R.sup.1 denotes a C.sub.1-4 alkoxy group or a hydrazino group or an NR.sup.4 R.sup.5 group, wherein R.sup.4 and R.sup.5 denote each a hydrogen atom or an identical or different C.sub.1-4 alkyl group; furthermore R.sup.4 may denote an aralkyl or substituted aralkyl group provided that R.sup.5 denotes a hydrogen atom; furthermore NR.sup.4 R.sup.5 may denote a morpholine or piperazine ring;R.sup.2 and R.sup.3 may denote each a hydrogen atom or an identical or different C.sub.1-4 aliphatic group; furthermore R.sup.2 may denote a cycloaliphatic, aralkyl, substituted aralkyl or amino group provided that R.sup.3 denotes a hydrogen atom; furthermore R.sup.2 and R.sup.3 may denote together with the adjacent nitrogen atom a morpholino ring, an unsubstituted piperazine ring or a substituted piperazine ring,and to their pharmaceutically acceptable acid addition salts. Furthermore, the invention relates to a process for preparing these compounds.The novel sulfonamidobenzoic acid derivatives having the general formula I possess significant tyrosine-paralyzing activity and thus they retard the biosynthesis of noradrenaline.
摘要翻译：本发明涉及具有通式的新型磺酰胺基苯甲酸衍生物，其中R 1表示C 1-4烷氧基或肼基或NR 4 R 5基，其中R 4和R 5各自表示氢原子或相同或不同的C 1-4 烷基; 此外，R 4可以表示芳烷基或取代的芳烷基，条件是R 5表示氢原子; 此外NR4R5可以表示吗啉或哌嗪环; R2和R3可以表示氢原子或相同或不同的C1-4脂族基团; 此外，R 2可以表示脂环族，芳烷基，取代的芳烷基或氨基，条件是R 3表示氢原子; 此外R2和R3可以与相邻的氮原子一起表示吗啉代环，未取代的哌嗪环或取代的哌嗪环，以及它们的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。具有通式I的新型磺酰胺基苯甲酸衍生物具有显着的酪氨酸 - 麻痹活性，因此它们延缓了去甲肾上腺素的生物合成。

8. 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）。

9. 发明授权

US3963735A Acylated 2-aminothiazole derivatives 失效
标题翻译：酰化2-氨基噻唑衍生物
公开(公告)号：US3963735A
公开(公告)日：1976-06-15
申请号：US518732
申请日：1974-10-29
申请人： Lajos Farkas , Endre Kasztreiner , Ferenc Andrasi , Jozsef Borsi , Istvan Elekes , Istvan Polgari
发明人： Lajos Farkas , Endre Kasztreiner , Ferenc Andrasi , Jozsef Borsi , Istvan Elekes , Istvan Polgari
IPC分类号： C07D277/20 , C07D277/46 , C07D295/14 , C07D417/04 , C07D417/14 , C07D213/56
CPC分类号： C07D417/04 , C07D277/46 , C07D417/14 , Y10S514/927
摘要： New acylated 2-aminothiazole derivatives of the general formula (I), ##SPC1##whereinR.sup.1 stands for phenyl group or a pyridyl group,R.sup.2 stands for hydrogen or lower alkyl,R.sup.3 stands for hydrogen, a lower alkyl group or benzyl group, andR.sup.4 and R.sup.5 each represent hydrogen, a C.sub.1-8 alkyl group, allyl group, a hydroxyalkyl group, a C.sub.3-6 cycloalkyl group, .beta.-dimethylaminoethyl group, .beta.-diethylaminoethyl group, benzyl group, 2-furylmethyl group, or a phenyl group having optionally a halogen, methyl, methoxy or trifluoromethyl substituent, orR.sup.4 and R.sup.5 may form, together with the adjacent nitrogen atom, a 5 to 8 membered polymethyleneimino group, morpholino group, piperazino group, N-methylpiperazino group or N-phenylpiperazino group, the compounds of formula I are anticholinergics.
摘要翻译：新的通式（I）的酰化2-氨基噻唑衍生物，其中R1代表苯基或吡啶基，R2代表氢或低级烷基，R3代表氢，低级烷基或苄基，R4和R5 各自表示氢，C1-8烷基，烯丙基，羟基烷基，C3-6环烷基，β-二甲基氨基乙基，β-二乙基氨基乙基，苄基，2-呋喃基甲基或任选具有卤素，甲基，甲氧基或三氟甲基取代基，或者R4和R5可以与相邻的氮原子一起形成5至8元多亚甲基亚氨基，吗啉代基，哌嗪基，N-甲基哌嗪基或N-苯基哌嗪基，配方I是抗胆碱能药。

10. 发明授权

US4329457A Process for the preparation of 6-(substituted amino)-3-pyridazinylhydrazines and their salts 失效
公开(公告)号：US4329457A
公开(公告)日：1982-05-11
申请号：US147224
申请日：1980-05-06
申请人： Geza Szilagyi , Peter Matyus , Endre Kasztreiner , Tibor Balogh , Lajos Ila
发明人： Geza Szilagyi , Peter Matyus , Endre Kasztreiner , Tibor Balogh , Lajos Ila
IPC分类号： A61K31/50 , A61P9/12 , C07D237/20 , C07D413/02
CPC分类号： C07D237/20
摘要： The invention relates to a novel process for the preparation of 6-(substituted amino)-3-pyridazinylhydrazines having the general formula I ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R.sup.1 stands for hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms;R.sup.2 and R.sup.3 may be the same or different and stand for alkyl groups containing from 1 to 6 carbon atoms, alkenyl groups containing from 2 to 6 carbon atoms, hydroxyalkyl groups containing from 2 to 4 carbon atoms, cycloalkyl groups containing from 3 to 8 carbon atoms, phenyl or benzyl groups or phenyl, benzyl or phenylethyl groups containing one or two halogen atoms, nitro, methoxy or hydroxyl groups, and one of R.sup.2 and R.sup.3 may stand also for a hydrogen atom, or R.sup.2 and R.sup.3 together with the neighboring nitrogen atom may build up also a morpholino, pyrrolidino, piperidino, heptamethyleneimino or N-methylpiperazino group.The process consists in that a compound having the general formula II ##STR2## wherein R.sup.1 is as defined above, R.sup.4 stands for a chlorine or bromine atom or methylthio group, while A stands for a 1,7,7-trimethyl-2-bicyclo(2,2,1)heptylidene or a benzylidene group substituted by an R.sup.5 group, wherein R.sup.5 stands for hydrogen, chlorine or bromine atom, or a methoxy, nitro or methylsulphonyl group - is reacted with an amine having the general formula IIIR.sup.2 R.sup.3 NH (III)wherein R.sup.2 and R.sup.3 are as defined above - and the compound thus obtained having the general formula IV ##STR3## wherein R.sup.1, R.sup.2, R.sup.3 and A are as defined above - is subjected to acidic hydrolysis.The 6-(substituted amino)-3-pyridazinylhydrazines having the general formula I and prepared by the novel process of invention, possess a significant hypotensive effect as well as they are used as starting materials for the preparation of 6-(substituted amino)-3-pyridazinylhydrazines having a very significant hypotensive action.

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