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1. 发明授权

EP2948449B1 PROCESS FOR PRODUCING 1, 4, 7, 10-TETRAAZACYCLODODECANE-1, 4, 7, 10-TETRAACETIC ACID AND COMPLEXES THEREOF 有权
标题翻译：生产1,4,7,10-四氮杂十二烷-1,4,7,10-四乙酸及其配合物的方法
公开(公告)号：EP2948449B1
公开(公告)日：2016-12-21
申请号：EP14701349.4
申请日：2014-01-22
申请人： AGFA Healthcare
发明人： BUFFEL, Diederik , GANORKAR, Rakesh , BURT, Jennifer , BOI, Xavier
IPC分类号： C07D457/04
CPC分类号： C07D257/02 , A61K49/108 , C07D457/04

2. 发明公开

EP2313405A1 AUFARBEITUNG VON MIKROBIOLOGISCH HERGESTELLTEN MUTTERKORNALKALOIDEN 审中-公开
标题翻译： PROCESSING微生物产生麦角生物碱
公开(公告)号：EP2313405A1
公开(公告)日：2011-04-27
申请号：EP09772376.1
申请日：2009-06-26
申请人： Sandoz AG
发明人： BERTEL, Stephan
IPC分类号： C07D457/04 , C12P17/18
CPC分类号： C12P17/183 , C07D457/04
摘要： The present invention relates to a method for preparing microbiologically produced ergot alkaloids of the following formula (I), comprising the step of: a) extracting the fermentation product occurring during the biological production, said product containing at least one ergot alkaloid of formula (I), at a pH of 8 - 14 using an extractant with a solubility in water of 0.2 g/100g of water to 25 g/100 g water at 20 °C, wherein the amount of extractant is sufficient to form a 2-phase system together with the fermentation product.

3. 发明公开

EP1507777A2 PROCESS FOR PREPARING CRYSTALLINE FORM I OF CABERGOLINE 审中-公开
标题翻译：工艺为结晶I型卡麦角林的制备
公开(公告)号：EP1507777A2
公开(公告)日：2005-02-23
申请号：EP03721346.9
申请日：2003-03-10
申请人： Pharmacia Corporation
发明人： SHEIKH, Ahmad, Y.
IPC分类号： C07D457/04 , C07D457/06
CPC分类号： C07D457/06
摘要： A process for producing crystalline form I of cabergoline, which process comprises crystallization of the desired form from a toluene/heptane or toluene/hexane mixture starting from raw cabergoline, followed by recovery and removal of the solvent from the resulting toluene solvate Form X. The new solvate Form X of cabergoline, useful intermediate, and its preparation are also provided.

4. 发明授权

EP0219257B1 Esters of dihydrolysergic acid 失效
标题翻译：二氢麦角酸酯
公开(公告)号：EP0219257B1
公开(公告)日：1994-03-09
申请号：EP86307443.1
申请日：1986-09-29
申请人： ELI LILLY AND COMPANY
发明人： Garbrecht, William Lee , Marzoni, Gifford Purnell , Parli, Carol John , Whitten, Kathleen Rose , Cohen, Marlene Lois , Fuller, Ray Ward
IPC分类号： C07D457/04 , A61K31/48
CPC分类号： C07D457/04 , A61K31/48

5. 发明公开

EP0219257A3 Esters of dihydrolysergic acid 失效
标题翻译：二氢胆酸酯
公开(公告)号：EP0219257A3
公开(公告)日：1988-12-28
申请号：EP86307443
申请日：1986-09-29
申请人： ELI LILLY AND COMPANY
发明人： Garbrecht, William Lee , Marzoni, Gifford Purnell , Parli, Carol John , Whitten, Kathleen Rose , Cohen, Marlene Lois , Fuller, Ray Ward
IPC分类号： C07D457/04 , A61K31/48
CPC分类号： C07D457/04 , A61K31/48
摘要： Compounds of the formula
wherein R is primary or secondary C₁-C₈ alkyl, C₂-C₄ alkenyl-CH₂, C₃-C₈ cycloalkyl or C₃-C₆ cycloalkyl-substituted C₁-C₅ primary or secondary alkyl, the total number of carbon atoms in R not to exceed 8; R¹ is allyl, H, or C₁-C₄ straight chain alkyl, and R² is C₁-C₃ alkoxy-C₅-C₇ cycloalkyl; a primary or secondary C₁-C₃ alkoxy-C₂-C₆-alkyl or di(C₁-C₃ alkoxy)-C₂-C₆alkyl; C₃-C₇ ketoalkyl; or C₅-C₇ cycloalkyl or keto-substituted C₅-C₇ cycloalkyl; or 4-hydroxycyclohexyl; or a pharmaceutically-acceptable salt thereof, are useful as 5HT₂ receptor antagonists.

6. 发明公开

EP0251732A2 Process for the preparation of 2-halogenated ergoline derivatives 失效
标题翻译： Verfahren zur Herstellung von 2-haloierten Ergolinderivaten。
公开(公告)号：EP0251732A2
公开(公告)日：1988-01-07
申请号：EP87305716.0
申请日：1987-06-26
申请人： RICHTER GEDEON VEGYESZETI GYAR R.T.
发明人： Megyeri, Gabor , Keve, Tibor , Kovacs, Lajos , Stefko, Bela , Bogsch, Erik , Kassai, Anna , Trischler, Ferenc , Szepesi, Gabor , Gazdag, Maria
IPC分类号： C07D457/02 , C07D457/04 , C07D519/02 , A61K31/48
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，三烷基卤代硅烷或三芳基卤代硅烷和任选的卤化氢组成的体系。

7. 发明公开

EP0228876A2 Esters of dihydrolysergic acid and related compounds 失效
标题翻译： Ester vonDihydrolysergsäureund verwandte Verbindungen。
公开(公告)号：EP0228876A2
公开(公告)日：1987-07-15
申请号：EP86309917.2
申请日：1986-12-18
申请人： ELI LILLY AND COMPANY
发明人： Whitten, Kathleen Rose , Garbrecht, William Lee , Marzoni, Gifford Purnell
IPC分类号： C07D457/04 , A61K31/48
CPC分类号： C07D457/04
摘要： Esters of 1-substituted-6-C 1-4 straight chain alkyl (or allyl)ergoline-8β-carboxylic acid, having the following formula (III):
wherein R is primary or secondary C 1-8 alkyl, C 2 - 4 alkenyl-CH 2 , C 3-8 cycloalkyl or C 3-6 cycloalkyl substituted C 1-5 primary or secondary alkyl, the total number of carbon atoms in R not to exceed 8; R' is allyl, H or C 1-4 straight-chain alkyl; and R 2 is
wherein n is 0-4 and m is 1 or 2 except that, when n is 0, the ester function may not be attached to the cyclic ether ring alpha to the ring oxygen;
wherein R 3 and R 4 can be individually H, CH 3 or C 2 H 5 ; n can be 0,1 or 2; R 5 can be OH, OC 1-3 alkyl, chloro, bromo, fluoro, CH 3 , CF 3 or C 2 H 5 when n is 1 or 2; R 5 can be phenyl when n is 1; and R 5 can be methylenedioxy when n is 2; or
(c) monofluoro-, difluoro- or trifluoro-C 2-5 alkyl; or a pharmaceutically acceptable salt thereof. The compounds are useful as 5HT receptor antagonists.
摘要翻译：具有下式（III）的1-取代-6-C 1-4直链烷基（或烯丙基）麦角灵素-ββ-羧酸的酯：其中R是伯或仲C 1-8烷基， 4个烯基-CH 2，C 3-8环烷基或C 3-6环烷基取代的C 1-5伯或仲烷基，R中碳原子总数不超过8; R 1是烯丙基，H或C 1-4直链烷基; 并且R 2是，其中n为0-4且m为1或2，不同之处在于当n为0时，酯官能团不能连接到环氧环的环醚环α上; 其中R 3和R 4可以分别是H，CH 3或C 2 H 5; n可以是0,1或2; 当n为1或2时，R 5可以是OH，OC 1-3烷基，氯，溴，氟，CH 3，CF 3或C 2 H 5; 当n为1时，R 5为苯基; 当n为2时，R 5为亚甲二氧基; 或（c）单氟，二氟或三氟-C 2-5烷基; 或其药学上可接受的盐。该化合物可用作5HT受体拮抗剂。

8. 发明公开

EP0185392A3 Novel ergolinyl compounds nitrogen-substituted in the 8-position, their preparation, and use as medicinal agents 失效
标题翻译：在8位置替代新戊酰胆碱化合物，其制备和用作药物代用品
公开(公告)号：EP0185392A3
公开(公告)日：1987-05-13
申请号：EP85116397
申请日：1982-12-23
申请人： SCHERING AKTIENGESELLSCHAFT Berlin und Bergkamen
发明人： Haffer, Gregor, Dr. , Sauer, Gerhard, Dr. , Wachtel, Helmut. Dr. , Schneider, Herbert, Dr. , Eder, Ulrich, Dr. , Lorenz, Hans-Peter, Dr.
IPC分类号： C07D457/12 , A61K31/48 , C07D457/06 , C07D457/04
CPC分类号： C07D457/04 , C07D457/06 , C07D457/12
摘要： Ergolinyl compounds which are nitrogen-substituted in the 8-position and have Formula (I)
and physiologically compatible salts thereof, wherein the 8-substituent can be in the a- or β-position and
represents a single or a double bond. R 2 is hydrogen, C 1-4 -alkyl or C 1-7 -acyl, R 3 is hydrogen, chlorine or bromine, and R 4 is C 2-6 -alkyl, C 3-6 -cycloalkyl-C 1-3 -afkyl, C 3-6 -alkenyl, or C 2-6 -alkynyl;

9. 发明公开

EP0095091A2 Process for the preparation of dihydrolysergic acid esters 有权
标题翻译： Verfahren zur Herstellung vonDihydrolysergsäure-Estern。
公开(公告)号：EP0095091A2
公开(公告)日：1983-11-30
申请号：EP83104635.4
申请日：1983-05-11
申请人： SCHERING AKTIENGESELLSCHAFT
发明人： Sauer, Gerhard, Dr.
IPC分类号： C07D457/04
CPC分类号： C07D457/04
摘要： A process for the preparation of dihydrolysergic acid esters of the formula
wherein

R is alkyl of up to 3 carbon atoms and the substituent in the 8-position can be in the a- or β-position, comprising reacting the corresponding acid amide with an alcohol at temperatures of 20° to 55°C for 8 to 50 hours in the presence of an acid or an acidic ion exchange resin at a pH of 0-1.
摘要翻译：制备式CHEM的二氢关节酸酯的方法，其中R是至多3个碳原子的烷基和8位的取代基可以是α-或β-位，包括使相应的酰胺在酸或酸性离子交换树脂的存在下，在0〜1℃的温度下，用醇在20〜55℃下反应8〜50小时。

10. 发明授权

EP0000533B1 N-Substituierte 9,10-Dihydrolysergsäureester sowie ein Verfahren zu deren Herstellung 失效
标题翻译： N-取代的9,10-二氢吡咯烷酮酯及其制备方法
公开(公告)号：EP0000533B1
公开(公告)日：1981-08-05
申请号：EP78100419.7
申请日：1978-07-18
申请人： LEK, tovarna farmacevtskih in kemicnih izdelkov, n.sol.o.
发明人： Rucman, Rudolf
IPC分类号： C07D457/04
CPC分类号： C07D457/04

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