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1.发明授权Pyrazole derivatives with an ergoline skeleton, their acid addition salts, and a process for the preparation thereof 失效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
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。
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2.发明授权Biologically active new 8.beta.-hydrazinomethyl-ergoline derivatives and a process for the preparation thereof 失效生物活性的新的8β-肼基甲基 - 麦角灵衍生物及其制备方法
公开(公告)号：US4235912A
公开(公告)日：1980-11-25
申请号：US21947
申请日：1979-03-19
CPC分类号： C07D457/02
摘要： The invention relates to new 8.beta.-hydrazinomethyl-ergoline derivatives of the general formula (I), ##STR1## wherein x y stands for a ##STR2## or ##STR3## group, R stands for hydrogen or methyl group, andR.sub.1 stands for hydrogen, a lower acyl group, a di-(lower-alkylaminocarbonyl group, a group of the general formula (VI), ##STR4## wherein Z.sub.1, Z.sub.2 and Z.sub.3 each represent hydrogen, halogen or a trifluoromethyl group, or a group of the general formula (VII), ##STR5## wherein Y represents a lower alkyl group, allyl group or phenyl group, and acid addition salts thereof. These compounds possess valuable antiserotonine, antidepressant and hypotensive effects, furthermore they can be applied as starting substances in the preparation of other biologically active ergoline derivatives.The new compounds of the general formula (I) are prepared according to the invention by reacting the respective 6-methyl-8.beta.-mesyloxymethyl or -tosyloxymethyl-ergoline derivatives with dry hydrazine. In order to obtain the N-substituted hydrazinomethyl compounds, the N-unsubstituted derivatives are reacted with an acylating agent or with an isothiocyanate.
摘要翻译： 本发明涉及通式（I）的新的8β-肼基甲基 - 麦角灵衍生物，其中xy代表
或 基团，R代表氢或甲基，R1表示 代表氢，低级酰基，二 - （低级烷基氨基羰基，通式（VI）的基团，其中Z 1，Z 2和Z 3各自表示氢，卤素或三氟甲基， 或者通式（VII）的基团，其中Y代表低级烷基，烯丙基或苯基，及其酸加成盐，这些化合物具有有价值的抗塞冬糖，抗抑郁药和降压作用，而且它们 可以将其用作制备其它生物活性麦角灵衍生物的起始物质，通式（I）的新化合物根据本发明通过使各自的6-甲基-8β-甲氧基甲基或 - 苯甲氧基甲基 - 麦角灵衍生物 用干肼。 为了得到N-取代的肼基甲基化合物，N-未取代的衍生物与酰化剂或异硫氰酸酯反应。 -
3.发明授权
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
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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公开(公告)号：US4005089A
公开(公告)日：1977-01-25
申请号：US579979
申请日：1975-05-22
IPC分类号： A61K31/48 , A61P25/24 , A61P25/26 , A61P43/00 , C07D457/02 , C07D457/06
CPC分类号： C07D457/06 , C07D457/02 , Y10S514/823
摘要： New compounds of the general formula (I) ##STR1## wherein R stands for hydrogen or methyl group,x y stands for a group of the formula ##STR2## and R.sub.1 stands for a group of the formula (III), (IV) or (V) ##STR3## wherein n is an integer from 4 to 10, ARE PREPARED BY ACYLATING A COMPOUND OF THE GENERAL FORMULA (II), ##STR4## wherein R and x y each have the same meanings as defined above, and R.sub.2 stands for a group of the formula (VI), (VII) or (VIII), ##STR5## with a C.sub.6-12 carboxylic acid or a C.sub.6-12 carboxylic acid halide. The new compounds of the general formula (I) and their acid addition salts can be used as antidepressants and antiserotonine agents with prolonged effects.
摘要翻译： 通式（I）的新化合物其中R表示氢或甲基，XY表示式的化合物，R1表示式（III），（IV ）或（V）其中n为4至10的整数，（IV）其中n为4至10的整数，ARE为通用化合物（II）制备的ARE， （II）其中R和xy各自具有与上述相同的含义，并且R 2表示式（VI），（VII）或（VIII），（VI），（VII） （VIII）与C6-12羧酸或C6-12羧酸卤化物反应。
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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。
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6.发明授权Compounds of ergolene and ergoline structure and method for the preparation thereof 失效己二烯和麦角灵结构的化合物及其制备方法
公开(公告)号：US4108855A
公开(公告)日：1978-08-22
申请号：US773792
申请日：1977-03-02
申请人： Erzsebet Mago nee Karacsony , Sandor Bajusz , Jozsef Borsi , Ildiko Kiraly , Endre Csanyi , Istvan Polgari
发明人： Erzsebet Mago nee Karacsony , Sandor Bajusz , Jozsef Borsi , Ildiko Kiraly , Endre Csanyi , Istvan Polgari
CPC分类号： C07D457/02 , Y02P20/55
摘要： The invention relates to a novel compound of the formula ##STR1## and the pharmaceuticlly acceptable acid addition salts thereof, wherein R stands for a hydrogen atom or methyl group, x y designates a ##STR2## Q is a hydrogen atom or a benzyloxycarbonyl- or N-tert.-butyloxycarbonyl protective group, and R.sub.1 is the side chain of a natural .alpha.-amino acid selected from the group consisting of Arg--, Tryp-13 , Phe--, Ser--, Leu--, Val--, Meth--, Tyr--, His-- or Prol---side-chain.The compounds according to the invention possess antiserotonin and hypotensive effects and act upon the central nervous system.
摘要翻译： 本发明涉及式（I）的新化合物及其药学上可接受的酸加成盐，其中R代表氢原子或甲基，xy表示Q是氢原子或苄氧基羰基 - 或N-叔丁氧基羰基保护基，R1是天然α-氨基酸的侧链，其选自Arg-，Tryp-13，Phe-，Ser-，Leu-，Val-，Meth - ，Tyr-，His-或Prol - 侧链。
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公开(公告)号：US4064249A
公开(公告)日：1977-12-20
申请号：US749398
申请日：1976-12-10
IPC分类号： C07D457/02 , C07D457/06 , A61K31/48
CPC分类号： C07D457/06 , C07D457/02
摘要： New compounds of the formula ##STR1## wherein R is hydrogen or methyl group,X y is a group of the formula ##STR2## and N IS AN INTEGER OF FROM 4 TO 10, ARE PREPARED BY ACYLATING THE APPROPRIATE LYSERGIC ACID-(3'-ALLYLOXY-2'-OXY-PROPYL)-AMIDE COMPOUNDS WITH CARBOXYLIC ACIDS OF 6 TO 12 CARBON ATOMS OR WITH THEIR REACTIVE DERIVATIVES. If desired, the new compounds can be converted into their pharmaceutically acceptable acid addition salts.The above compounds possess prolonged antidepressive activities.
摘要翻译： 式（I）的新化合物其中R是氢或甲基，XY是组合式的组合，N是4至10的整数，是通过合成适当的LYSERGIC ACID-（ 3-ALLYLOXY-2'-OXY-PROPYL） - 酰胺化合物与6至12个碳原子或其反应衍生物的羧酸反应。 如果需要，新化合物可以转化成其药学上可接受的酸加成盐。
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