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1. 发明授权

US09670199B2 Ergoline derivatives as dopamine receptor modulators 有权
公开(公告)号：US09670199B2
公开(公告)日：2017-06-06
申请号：US14443576
申请日：2013-11-19
申请人： REGENTS OF THE UNIVERSITY OF MINNESOTA
发明人： Peter Dosa , Suck Won Kim , Michael Walters
IPC分类号： A61K31/48 , C07D457/06 , C07D457/02 , C07D457/04
CPC分类号： C07D457/06 , C07D457/02 , C07D457/04
摘要： The invention provides compounds of formula I: wherein R1-R4 have any of the values defined in the specification, and salts thereof. The compounds are useful as dopamine receptor modulators for the treatment of diseases where modulation of dopamine receptors is implicated (e.g. sexual dysfunction, prolactinoma, Parkinson's disease, and Cushings disease).

2. 发明申请

US20020054904A1 Stable pergolide mesylate and process for making same 失效
标题翻译：稳定的甲磺酸pergolide和制备相同的方法
公开(公告)号：US20020054904A1
公开(公告)日：2002-05-09
申请号：US09923499
申请日：2001-08-07
发明人： Ruth Tenengauzer , Minutza Leibovici
IPC分类号： A61K009/20 , A61K009/14
CPC分类号： A61K9/2059 , A61K9/1623 , A61K9/1652 , A61K9/1682 , A61K9/2018 , A61K9/205 , A61K9/2054 , A61K31/48 , C07D457/02
摘要： A formulation and a method for manufacturing pergolide mesylate is disclosed whereby substantially stable pergolide mesylate can be manufactured without having to introduce stabilizing additives.
摘要翻译：公开了一种制备速溶甲磺酸盐的制剂和方法，其中可以制备基本上稳定的甲磺酸高甘膦，而不必引入稳定添加剂。

3. 发明授权

US06358967B1 Ergoline amine derivatives with blood pressure lowering effect 失效
标题翻译：艾曲林胺衍生物具有降血压作用
公开(公告)号：US06358967B1
公开(公告)日：2002-03-19
申请号：US09743869
申请日：2001-04-19
申请人： Ralf Wyrwa , Albert Haertl , Erika Glusa , Susanne Grabley , Ralf Thiericke
发明人： Ralf Wyrwa , Albert Haertl , Erika Glusa , Susanne Grabley , Ralf Thiericke
IPC分类号： A61K3148
CPC分类号： C07F15/025 , C07D457/02 , C07F17/02
摘要： The invention relates to novel derivatives of ergoline of the general formula 1 in which R1 together with the two adjacent N atoms is the residue of a diamine and R4 together with the two adjacent carbonyl groups is the residue of a dicarboxylic acid. R2, R3, R6, R7, R8 can be H or an organic radical. R7 and R8 are H or together are a bond. The compounds show a strong antihypertensive effect. These effects moreover occur after intravenous and enteral administration even at dosages in the region of a few &mgr;g/kg (body weight). The compounds can accordingly be used as pharmaceuticals for hypertensive diseases in human medicine.
摘要翻译：本发明涉及通用1的麦角灵素的新衍生物，其中R1与两个相邻的N原子一起是二胺的残基，R4与两个相邻的羰基一起是二羧酸的残基。 R2，R3，R6，R7，R8可以是H或有机基团。 R7和R8是H或一起是一个键。化合物显示出强烈的抗高血压作用。即使在几公斤/公斤（体重）的剂量下，静脉内和肠内给药也会发生这些影响。因此，这些化合物可以用作人类医学中的高血压疾病的药物。

4. 发明授权

US5334385A New alkaloid derivatives, their use and pharmaceutical formulations containing them 失效
标题翻译：新生物碱衍生物，其用途和含有它们的药物制剂
公开(公告)号：US5334385A
公开(公告)日：1994-08-02
申请号：US922689
申请日：1992-07-30
申请人： Ezio Bombardelli
发明人： Ezio Bombardelli
IPC分类号： A61K8/55 , A61K8/00 , A61K8/49 , A61K8/58 , A61K8/97 , A61K9/00 , A61K31/435 , A61K31/66 , A61K31/685 , A61P9/00 , A61P9/10 , A61Q19/00 , C07D457/02 , C07D457/04 , C07D457/06 , C07D459/00 , C07D461/00 , C07D491/22 , C07D519/04 , C07F9/10 , C07G5/00 , A61K35/78 , A61K7/00
CPC分类号： C07D461/00 , C07D457/02 , C07D519/04 , C07F9/106 , C07G5/00
摘要： Salts of a pharmacologically active, naturally occurring or synthetic alkaloids, or alkaloid derivatives and a phosphatidic acid are provided, which preferably have the formula[Alk].sub.x [PA].sub.ywhereinAlk represents a cation derived from said pharmacologically active, naturally occurring or synthetic alkaloid, or alkaloid derivative,PA represents a phosphatidic acid or a mixture of different phosphatidic acids, andx:y is from 2:1 to 1:2.The therapeutic use of the salts of the invention in the treatment of syndromes affecting the elderly, particularly conditions that are related to changes in cerebral metabolism and reduced blood flow are decribed, as well as cosmetic methods.
摘要翻译：提供药理活性的天然存在或合成的生物碱或生物碱衍生物和磷脂酸的盐，其优选具有式[Alk] x [PA] y，其中Alk表示衍生自所述药理学活性的天然存在或合成的阳离子生物碱或生物碱衍生物，PA代表磷脂酸或不同磷脂酸的混合物，x：y为2:1至1:2。本发明的盐在治疗影响老年人的综合征中的治疗用途，特别是与脑代谢变化和血流量减少有关的病症，以及美容方法。

5. 发明授权

US5097031A Steroselective hydrogenation process 失效
标题翻译： STEROSELECTIVE氢化方法
公开(公告)号：US5097031A
公开(公告)日：1992-03-17
申请号：US542168
申请日：1990-06-22
申请人： Istvan Polgar , Jozsef Foldesi , Janos Kiss , Piroska Major nee Forstner , Karoly Molnar , Andras Sugar , Tamas Szen , Katalin Balogh nee Nemes
发明人： Istvan Polgar , Jozsef Foldesi , Janos Kiss , Piroska Major nee Forstner , Karoly Molnar , Andras Sugar , Tamas Szen , Katalin Balogh nee Nemes
IPC分类号： C07D457/02 , C07D457/04
CPC分类号： C07D457/02
摘要： The invention relates to a novel stereoselective process for the preparation of dihdyrolysergol from lysergol by hydrogenation in the presence of solvent and palladium catalyst applied on a carrier, which comprises hydrogenating lysergol in the presence of one or more aprotic solvent(s) containing tertiary nitrogen atom(s) and a palladium catalyst applied on activated carbon, and recovering the product obtained from the reaction mixture in a known manner.
摘要翻译：本发明涉及一种新颖的立体选择性方法，其用于在载体上施加溶剂和钯催化剂的氢化作用下，通过氢化制备二硅胶，其包括在含有叔氮原子的一种或多种非质子溶剂存在下氢化麦角凝胶以及施加在活性炭上的钯催化剂，以已知的方式回收由反应混合物获得的产物。

6. 发明授权

US5079364A t-alkyl ergoline derivatives 失效
标题翻译： T-ALKYL ERGOLINE DERIVATIVES
公开(公告)号：US5079364A
公开(公告)日：1992-01-07
申请号：US328518
申请日：1989-03-24
申请人： Aldemio Temperilli , Enzo Brambilla , Mauro Gobbini , Maria A. Cervini
发明人： Aldemio Temperilli , Enzo Brambilla , Mauro Gobbini , Maria A. Cervini
IPC分类号： A61K31/48 , A61P25/28 , C07D457/02
CPC分类号： C07D457/02
摘要： t-alkyl eroline derivatives of formula I are produced ##STR1## wherein (R.sub.1 =H, OCH.sub.3 and R.sub.2 H) or (R.sub.1 +R.sub.2 =a ring bond and R.sub.3 =H, optionally substituted nicotinynoyl or 1-oxo-2-cyclopenten-3-yl); and their pharmaceutically acceptable salts.A process for the preparation of these derivatives from lysergol and a t-alkyl alcohol is also described, as are pharmaceutical compositions containing them.

7. 发明授权

US4816587A Process for the preparation of 2-halogenated ergoline derivatives 失效
标题翻译： 2-卤代麦角灵衍生物的制备方法
公开(公告)号：US4816587A
公开(公告)日：1989-03-28
申请号：US58576
申请日：1987-06-05
申请人： Gabor Megyeri , Tibor Keve , Lajos Kovacs, Jr. , Bela Stefko , Erik Bogsch , Anna Kassia nee Zieger , Ferenc Trischler , Gabor Szepesi , Maria Gazdag
发明人： Gabor Megyeri , Tibor Keve , Lajos Kovacs, Jr. , Bela Stefko , Erik Bogsch , Anna Kassia nee Zieger , Ferenc Trischler , Gabor Szepesi , Maria Gazdag
IPC分类号： C07B39/00 , C07B31/00 , C07C67/00 , C07D457/00 , C07D457/02 , C07D457/04 , C07D519/00 , C07D519/02
CPC分类号： C07D457/04 , C07D457/00 , C07D457/02 , C07D519/02
摘要： The invention relates to a novel process for the halogenation in 2-position of ergot alkaloids. The process is characterized by that as a halogenating agent a system consisting of dimethylsulfoxide, a trialkylhalosilane or triarylhalosilane and optionally a hydrogen halide is used.
摘要翻译：本发明涉及麦角生物碱2-位卤化的新方法。该方法的特征在于，作为卤化剂，使用由二甲基亚砜，三烷基卤硅烷或三芳基卤代硅烷和任选的卤化氢组成的体系。

8. 发明授权

US4753949A 2-chloronicergoline having antihypoxic activity 失效
标题翻译：具有抗低氧活性的2-氯麦角林
公开(公告)号：US4753949A
公开(公告)日：1988-06-28
申请号：US877294
申请日：1986-06-23
申请人： Gabor Megyeri , Tibor Keve , Bala Stefko , Erik Bogsch , Janos Galambos , Anna Kassi nee Zieger , Ferenc Trischler , Eva Palosi , Dora Groo , Egon Karpati , Zsolt Szombathelyi , Laszlo Szporny , Bela Kiss , Istvan Laszlovszky , Erzsebet Lapis
发明人： Gabor Megyeri , Tibor Keve , Bala Stefko , Erik Bogsch , Janos Galambos , Anna Kassi nee Zieger , Ferenc Trischler , Eva Palosi , Dora Groo , Egon Karpati , Zsolt Szombathelyi , Laszlo Szporny , Bela Kiss , Istvan Laszlovszky , Erzsebet Lapis
IPC分类号： A61K31/48 , A61P3/00 , A61P3/14 , A61P9/00 , A61P25/02 , A61P25/28 , C07D457/02
CPC分类号： C07D457/02
摘要： The invention relates to a novel process for the preparation of partially new 2-halonicergoline derivatives of the formula (I), ##STR1## wherein X stands for chlorine, bromine or iodine atom, as well as their acid addition salts.The process of the invention comprises esterifying a novel 2-halo-1-methyllumilysergol of the formula (II), ##STR2## wherein X is the same as defined above, or an acid addition salt thereof and, if desired, converting the thus-obtained 2-halonicergoline derivative of the formula (I) to an acid addition salt.The compounds of the invention improve the cognitive function of the brain and show an antihypoxic as well as a strong .alpha.-adrenerg blocking and calcium-antagonistic action.
摘要翻译：本发明涉及制备式（I）的部分新的2-卤代麦角灵衍生物的新方法，其中X代表氯，溴或碘原子，以及它们的酸加成盐。本发明的方法包括酯化式（II）的新的2-卤代-1-甲基烯丙基谷维素，其中X与上述定义相同，或其酸加成盐，如果需要，转化将由此获得的式（I）的2-卤代麦角灵衍生物与酸加成盐反应。本发明的化合物改善了脑的认知功能，并且显示出抗低氧以及强的α-肾上腺素能阻断和钙拮抗作用。

9. 发明授权

US4728649A 3-oxo-piperazin-1-yl-ergolines exhibiting antidopaminergic activity 失效
标题翻译：具有抗癌剂活性的3-氧代 - 哌嗪-1-基 - 麦角酰胺
公开(公告)号：US4728649A
公开(公告)日：1988-03-01
申请号：US817135
申请日：1986-01-08
申请人： Sergio Mantegani , Aldemio Temperilli , Gabriella Traquandi , Alessandro Rossi , Lorenzo Pegrassi
发明人： Sergio Mantegani , Aldemio Temperilli , Gabriella Traquandi , Alessandro Rossi , Lorenzo Pegrassi
IPC分类号： A61K31/48 , A61P9/12 , A61P25/00 , A61P25/20 , C07D457/02 , C07D457/12 , A61K31/445
CPC分类号： C07D457/02
摘要： The invention relates to ergoline derivatives having the general formula (I): ##STR1## where R=H, CH.sub.3 ; R.sub.1 =H, halogen, CH.sub.3, phenylthio, C.sub.1 -C.sub.4 alkylthio; R.sub.2 =H, CH.sub.3 O, and R.sub.3 =H or R.sub.2 +R.sub.3 =chemical bond; R.sub.4 =C.sub.1 -C.sub.4 hydrocarbon; R.sub.5, R.sub.6, R.sub.8, R.sub.9 independently=H, C.sub.1 -C.sub.4 alkyl, or R.sub.5, R.sub.8 independently=H, C.sub.1 -C.sub.4 alkyl and R.sub.6 +R.sub.9 =CH.sub.2 CH.sub.2, CH.sub.2 CH.sub.2 CH.sub.2 ; R.sub.7 =H, C.sub.1 -C.sub.4 alkyl, phenyl, NR'R"; R',R" independently=H, C.sub.1 -C.sub.4 alkyl, acyl or NR'R"=heterocyclic ring; W=0, H.sub.2 ; n=0, 1, 2, and their pharmaceutically acceptable salts, these compounds exhibiting antihypertensive activity making them useful anxiolytic and antipsychotic agents. A process for their preparation and pharmaceutical compositions containing them are also described.
摘要翻译：本发明涉及具有通式（I）的麦角灵衍生物：其中R = H，CH 3; R1 = H，卤素，CH3，苯硫基，C1-C4烷硫基; R2 = H，CH3O，R3 = H或R2 + R3 =化学键; R4 = C1-C4烃; R5，R6，R8，R9独立地为H，C1-C4烷基或R5，R8独立地为H，C1-C4烷基和R6 + R9 = CH2CH2，CH2CH2CH2; R7 = H，C1-C4烷基，苯基，NR'R“ R'，R“独立地为H，C 1 -C 4烷基，酰基或NR'R”=杂环; W = 0，H2; n = 0,1,2及其药学上可接受的盐，这些具有抗高血压活性的化合物使它们成为抗焦虑药和抗精神病药。还描述了其制备方法和含有它们的药物组合物。

10. 发明授权

US4690929A Ergolines exhibiting protactin secretion inhibition activity 失效
标题翻译： Ergolines表现出protactin分泌抑制活性
公开(公告)号：US4690929A
公开(公告)日：1987-09-01
申请号：US604041
申请日：1984-04-26
申请人： Luigi Bernardi , Laura Chiodini , Sergio Mantegani , Daniela Ruggieri , Aldemio Temperilli , Patricia Salvati
发明人： Luigi Bernardi , Laura Chiodini , Sergio Mantegani , Daniela Ruggieri , Aldemio Temperilli , Patricia Salvati
IPC分类号： C07D457/02 , C07D457/12 , A61K31/48 , C07D457/04
CPC分类号： C07D457/02 , C07D457/12
摘要： Compounds of formula I: ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group; R.sub.2 represents a hydrogen or halogen atom or a methyl, cyano, C.sub.1 -C.sub.4 alkylthio or phenylthio group; R.sub.7 and R.sub.8 represent hydrogen atoms and R.sub.3 represents a hydrogen atom or a methoxy group, or R.sub.7 represents a hydrogen atom and R.sub.3 and R.sub.8 taken together represent a bond, or R.sub.3 represents a hydrogen atom or a methoxy group and R.sub.7 and R.sub.8 taken together represent a bond; R.sub.4 represents a hydrocarbon group having from 1 to 4 carbon atoms; R.sub.5 represents a hydrogen atom or a hydrocarbon group having from 1 to 4 carbon atoms or a phenyl group; X represents an oxygen or sulphur atom or an imino group, R.sub.9 represents a hydrogen atom and B represents a cyano, a C.sub.2 -C.sub.5 alkoxycarbonyl or carbamoyl group, or R.sub.9 and B taken together represent a ##STR2## group wherein W represents an oxygen atom or an imino group; A represents a group of the formula CHR.sub.6, CH.sub.2 --CHR.sub.6 or CH.dbd.CR.sub.6 group wherein R.sub.6 represents a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; and n is 0, 1 or 2; and their pharmaceutically acceptable salts are disclosed, along with the use of these compounds as antiprolactinic and antihypertensive agents. The preparation of these compounds and pharmaceutical compositions containing them are also described.
摘要翻译：式I的化合物：其中R 1表示氢原子或甲基; R 2表示氢或卤素原子或甲基，氰基，C 1 -C 4烷硫基或苯硫基; R7和R8表示氢原子，R3表示氢原子或甲氧基，或R7表示氢原子，R3和R8表示一个键，或R3表示氢原子或甲氧基，R7和R8表示一个债券 R4表示具有1至4个碳原子的烃基; R5表示氢原子或碳原子数1〜4的烃基或苯基; X表示氧或硫原子或亚氨基，R9表示氢原子，B表示氰基，C2-C5烷氧基羰基或氨基甲酰基，或R9和B表示“IMA”基团，其中W表示氧原子或亚氨基; A表示式CHR 6，CH 2 -CHR 6或CH = CR 6基团的基团，其中R 6表示氢原子或C 1 -C 4烷基; 且n为0,1或2; 以及它们的药学上可接受的盐以及这些化合物作为抗孕激素和抗高血压药的用途。还描述了这些化合物的制备和含有它们的药物组合物。

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