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1. 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。

2. 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。

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）。

6. 发明授权

US4101552A Novel lysergic acid amides and process for preparing same 失效
标题翻译：新的麦角酸酰胺及其制备方法
公开(公告)号：US4101552A
公开(公告)日：1978-07-18
申请号：US679866
申请日：1976-04-23
申请人： Erzsebet Mago nee Karacsony , Jozsef Borsi , Laszlo Tardos , Ildiko Kiraly , Sandor Elek , Istvan Elekes
发明人： Erzsebet Mago nee Karacsony , Jozsef Borsi , Laszlo Tardos , Ildiko Kiraly , Sandor Elek , Istvan Elekes
IPC分类号： A61K31/48 , A61P43/00 , C07D457/06 , C07D457/08
CPC分类号： C07D457/06 , Y10S514/823
摘要： 9,10-Dihydrolysergic acid-(3'-/pyrrolid-2"-on-1'-yl/-propyl)-amide, 1-methyl-9,10-dihydrolysergic acid-(thiazoline-2'-yl)-amide and lysergic acid-(3'-allyloxy-2'-oxy-propyl)-amide and their pharmaceutically acceptable acid addition salts possess antihypertensive and antiserotonin effect and exert an action on the central nervous system.
摘要翻译： 9,10-二氢肉豆蔻酸 - （3' - /吡咯烷-2“ - 在1'-基 - 丙基） - 酰胺，1-甲基-9,10-二氢麦芽糖酸 - （噻唑啉-2'-基） - 酰胺和麦角酸 - （3'-烯丙氧基-2'-氧 - 丙基） - 酰胺及其药学上可接受的酸加成盐具有抗高血压和抗血清素作用并对中枢神经系统发挥作用。

7. 发明授权

US5252572A Pyridopyrimidine derivatives, pharmaceutical compositions containing them and process for preparing same 失效
标题翻译：吡啶并嘧啶衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：US5252572A
公开(公告)日：1993-10-12
申请号：US903246
申请日：1992-06-23
申请人： Istvan Hermecz , Jozsef Knoll , Lelle Vasvari nee Debreczy , Klara Gyires , Judit Sipos , Agnes Horvath , Laszlo Tardos , Maria Blaogh
发明人： Istvan Hermecz , Jozsef Knoll , Lelle Vasvari nee Debreczy , Klara Gyires , Judit Sipos , Agnes Horvath , Laszlo Tardos , Maria Blaogh
IPC分类号： C07D471/04 , A61K31/505
CPC分类号： C07D471/04
摘要： The present invention relates to novel 4-oxo-4H-pyrido[1,2-a]pyrimidine-3-carboxamide derivatives of the general formula (I) and the acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I) ##STR1## R stands for a C.sub.1-12 alkyl group optionally substituted by a C.sub.1-4 alkoxycarbonyl group; a C.sub.3-9 cycloalkyl, adamantyl or optionally substituted phenyl group;R.sup.1 means hydrogen or a C.sub.1-4 alkyl group; orR and R.sup.1 together form a --(CH.sub.2).sub.n -- chain, wherein n is 4, 5 or 6;R.sup.2 stands for hydrogen, a C.sub.1-4 alkyl group or halogen;R.sup.3 represents hydrogen or a C.sub.1-4 alkyl group; andm is 0 or 1.The compounds of the general formula (I) possess a gastroprotective effect and are useful for the prevention and therapy of ulcers of the stomach and the small intestine.
摘要翻译：本发明涉及通式（I）的新型4-氧代-4H-吡啶并[1,2-a]嘧啶-3-甲酰胺衍生物及其酸加成盐，含有它们的药物组合物及其制备方法。在通式（I）中，R 1表示任选被C 1-4烷氧基羰基取代的C 1-12烷基; C3-9环烷基，金刚烷基或任选取代的苯基; R1表示氢或C1-4烷基; 或R和R 1一起形成 - （CH 2）n - 链，其中n为4,5或6; R2代表氢，C1-4烷基或卤素; R3表示氢或C1-4烷基; m为0或1.通式（I）的化合物具有胃保护作用，可用于预防和治疗胃和小肠溃疡。

8. 发明授权

US5158951A Pyridopyrimidine derivatives useful in treatment of ulcers 失效
标题翻译：用于治疗溃疡的吡啶并嘧啶衍生物
公开(公告)号：US5158951A
公开(公告)日：1992-10-27
申请号：US307665
申请日：1989-02-06
申请人： Istvan Hermecz , Jozsef Knoll , Lelle Vasvari nee Debreczy , Klara Gyires , Judit Sipos , Agnes Horvath , Laszlo Tardos , Maria Blaogh
发明人： Istvan Hermecz , Jozsef Knoll , Lelle Vasvari nee Debreczy , Klara Gyires , Judit Sipos , Agnes Horvath , Laszlo Tardos , Maria Blaogh
IPC分类号： A61K31/505 , A61K31/513 , A61K31/519 , A61P1/04 , C07D221/00 , C07D239/26 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention relates to novel 4-oxo-4H-pyrido[1,2-a]pyrimidine -3-carbonamide derivatives of the general formula (I) and the acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I) ##STR1## wherein: R stands for a C.sub.1-12 alkyl group optionally substituted by a C.sub.1-4 alkoxycarbonyl group; a C.sub.3-9 cycloalkyl, adamantyl or optionally substituted phenyl group;R.sup.1 means hydrogen or a C.sub.1-4 alkyl group; orR and R.sup.1 together form a --(CH.sub.2).sub.n -- chain, wherein n is 4, 5 or 6;R.sup.2 stands for hydrogen, a C.sub.1-4 alkyl group or halogen;R.sup.3 repesents hydrogen or a C.sub.1-4 alkyl group; andm is 0 or 1.The compounds of the general formula (I) possess a gastroprotective effect and are useful for the prevention and therapy of ulcers of the stomach and the small intestine.
摘要翻译：本发明涉及通式（I）的新型4-氧代-4H-吡啶并[1,2-a]嘧啶-3-甲酰胺衍生物及其酸加成盐，含有它们的药物组合物及其制备方法。通式（I）其中：R表示任选被C 1-4烷氧基羰基取代的C 1-12烷基; C3-9环烷基，金刚烷基或任选取代的苯基; R1表示氢或C1-4烷基; 或R和R 1一起形成 - （CH 2）n - 链，其中n为4,5或6; R2代表氢，C1-4烷基或卤素; R3代表氢或C1-4烷基; m为0或1.通式（I）的化合物具有胃保护作用，可用于预防和治疗胃和小肠溃疡。

9. 发明授权

US4988730A Diphenkylpropylamines for the therapy of heart disease 失效
标题翻译：用于治疗心脏病的二苯基丙胺
公开(公告)号：US4988730A
公开(公告)日：1991-01-29
申请号：US385539
申请日：1989-07-21
申请人： Dezso Korbonits , Pal Kiss , Laszlo Szekeres , Gyula Papp , Gabor Kovacs , Andrea Santane Csutor , Sandor Virag , Eva Udvari , Imre Bata , Katalin Marmarosi nee Kellner , Laszlo Tardos , Peter Kormoczy , Vera Gergely , Zoltan Vargai
发明人： Dezso Korbonits , Pal Kiss , Laszlo Szekeres , Gyula Papp , Gabor Kovacs , Andrea Santane Csutor , Sandor Virag , Eva Udvari , Imre Bata , Katalin Marmarosi nee Kellner , Laszlo Tardos , Peter Kormoczy , Vera Gergely , Zoltan Vargai
IPC分类号： C07C215/50 , A61K31/13 , A61K31/135 , A61K31/137 , A61K31/16 , A61K31/165 , A61K31/335 , A61K31/36 , A61P3/00 , A61P9/06 , A61P9/08 , A61P9/10 , C07C20060101 , C07C27/00 , C07C67/00 , C07C209/00 , C07C209/08 , C07C209/24 , C07C209/26 , C07C209/62 , C07C209/68 , C07C211/00 , C07C211/03 , C07C211/16 , C07C211/26 , C07C211/27 , C07C211/29 , C07C211/43 , C07C213/00 , C07C217/10 , C07C217/54 , C07C217/56 , C07C217/58 , C07C227/10 , C07C227/16 , C07C229/34 , C07C229/38 , C07C231/00 , C07C231/12 , C07C233/42 , C07C233/43 , C07C233/67 , C07D311/48 , C07D317/00 , C07D317/48 , C07D317/58
CPC分类号： C07D317/58 , C07C211/27 , C07C211/29 , C07C217/58 , C07C233/43
摘要： The invention relates to novel diphenylpropylamine derivatives of the general formula (I). ##STR1## R.sup.1 stands for hydrogen or a methyl group; R.sup.2 stands for hydrogen, a methyl or n-decyl group;Z means a phenyl group substituted by R.sup.3, R.sup.4 and R.sup.5, whereinR.sup.3 means hydrogen, fluorine, chlorine or bromine, or a nitro, C.sub.1-12 alkyl, C.sub.1-4 alkoxy, phenoxy or benzyloxy group;R.sup.4 and R.sup.5 represent hydrogen, chlorine or a hydroxy, alkoxy, benzyloxy, acetamino or carboxy group; orR.sup.4 and R.sup.5 together form a methylendioxy group; orZ may stand for a 4-methoxynaphtyl or 4-ethoxy-naphthyl group; andR.sup.6 stands for hydrogen or fluorine, with the proviso that each of R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.6 cannot simultaneously stand for hydrogen, as well as their physiologically acceptable acid addition salts.The invention also relates to a process for the preparation of these compounds and to the pharmaceutical compositions containing these compounds.The compounds of the general formula (I) can preferably be used for the treatment of cardiovascular diseases.
摘要翻译：本发明涉及通式（I）的新型二苯基丙胺衍生物。（I）R1代表氢或甲基; R2代表氢，甲基或正癸基; Z表示被R 3，R 4和R 5取代的苯基，其中R 3表示氢，氟，氯或溴，或硝基，C 1-12烷基，C 1-4烷氧基，苯氧基或苄氧基; R4和R5代表氢，氯或羟基，烷氧基，苄氧基，乙酰氨基或羧基; 或R4和R5一起形成甲基二氧基; 或Z可以代表4-甲氧基萘基或4-乙氧基 - 萘基; 并且R6代表氢或氟，条件是R1，R2，R3，R4和R6各自不能同时代表氢，以及它们的生理上可接受的酸加成盐。本发明还涉及制备这些化合物的方法和含有这些化合物的药物组合物。通式（I）的化合物可优选用于治疗心血管疾病。

10. 发明授权

US4299836A Novel ergol-8-ene and ergolin compounds and process for preparing same 失效
标题翻译：新型麦角苷8-烯和麦角蛋白化合物及其制备方法
公开(公告)号：US4299836A
公开(公告)日：1981-11-10
申请号：US167341
申请日：1980-07-10
申请人： Erzsebet Mago nee Karacsony , Lajos Toldy , Jozsef Borsy , Laszlo Tardos , Ildiko Kiraly , Andras Ronay
发明人： Erzsebet Mago nee Karacsony , Lajos Toldy , Jozsef Borsy , Laszlo Tardos , Ildiko Kiraly , Andras Ronay
IPC分类号： A61K31/48 , A61P9/12 , A61P25/24 , A61P25/26 , A61P43/00 , C07D457/02
CPC分类号： C07D457/02
摘要： The invention relates to new ergol-8-ene and ergoline derivatives of the general formula /I/ ##STR1## wherein x y stands for --CH.dbd.C.dbd. or --CH.sub.2 --CH.dbd. group,R stands for hydrogen atom or methyl group,R.sub.1 stands for hydrogen or halogen atom,R.sub.2 stands for lower alkylsulfonyloxy group, phenylsulfonyloxy group optionally substituted with a lower alkyl group, or azido group,R.sub.3 stands for lower alkylsulfonyloxy group or phenylsulfonyloxy group optionally substituted with a lower alkyl group, and acid addition salts thereof. These compounds can be prepared from compounds of the general formula II ##STR2## wherein x y and R are as defined above, by reacting at least two equivalents of a lower alkylsulfonic acid chloride or phenylsulfonic acid chloride substituted with lower alkyl group. The resulting compound can be reacted with an alkali metal azide, and, if desired, the compound obtained is treated with a halogenating agent to form the 2-halogenide derivative, and, if desired, any resulting compound of general formula I is treated with an acid to form a therapeutically acceptable acid addition salt, or the free base is liberated from a salt.The compounds of general formula I possess valuable antiserotonine, antidepressant, dopamine receptor stimulant and hypotensive effects.
摘要翻译：本发明涉及通用化合物/ I / IMAGE> / I /的新的麦角8-ene和麦角灵衍生物，其中xy代表-CH = C =或-CH 2 -CH =基团，R代表氢原子或甲基基团，R1代表氢或卤素原子，R2代表低级烷基磺酰氧基，任选被低级烷基取代的苯基磺酰氧基或叠氮基，R3代表低级烷基磺酰氧基或任选被低级烷基取代的苯基磺酰氧基，其加成盐。这些化合物可以通过使至少两当量的低级烷基磺酰氯或被低级烷基取代的苯基磺酰氯反应，由通式II＆lt; IMAGE＆gt; / II /的化合物制备，其中x y和R如上定义。所得化合物可以与碱金属叠氮化物反应，如果需要，用卤化剂处理所得化合物以形成2-卤化物衍生物，如果需要，将所得到的通式I化合物用酸形成治疗上可接受的酸加成盐，或游离碱从盐中释放出来。通式I的化合物具有有价值的抗塞冬糖，抗抑郁药，多巴胺受体兴奋剂和降血压作用。

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