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    PROCESS FOR PRODUCING 1,4,7,10-TETRAAZACYCLODODECANE-1,4,7,10-TETRAACETIC ACID AND COMPLEXES THEREOF
    2.
    发明申请
    PROCESS FOR PRODUCING 1,4,7,10-TETRAAZACYCLODODECANE-1,4,7,10-TETRAACETIC ACID AND COMPLEXES THEREOF 有权
    生产1,4,7,10-四氮杂环十二烷-1,4,7,10-四氢酸的方法及其复合物

    公开(公告)号：US20160024030A1

    公开(公告)日：2016-01-28

    申请号：US14763550

    申请日：2014-01-22

    申请人： AGFA HEALTHCARE

    发明人： Diederik BUFFEL ,  Rakesh GANORKAR ,  Jennifer BURT ,  Xavier BOI

    IPC分类号： C07D257/02 ,  A61K49/10

    CPC分类号： C07D257/02 ,  A61K49/108 ,  C07D457/04

    摘要： A process for producing 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) including salts and hydrates thereof of general formula (I) from the respective cyclen. The process involves the use of cationic- and anionic exchange resins and solvent treatments to remove the organic and inorganic contaminants. Any cations present in the raw DOTA or other contaminants resulting from the reaction of cyclen are largely reduced in early stages of the process allowing to obtain good yields of DOTA in a purified grade and in an easier and reliable way. The process is useful for the production of DOTA, of macrocyclic compounds including metal ions complexes thereof and of compositions including the macrocyclic compounds that can be used as contrast agents for magnetic resonance imaging.

    摘要翻译： 从各自的环烯烃生产包含通式（I）的盐和水合物的1,4,7,10-四氮杂环十二烷-1,4,7,10-四乙酸（DOTA）的方法。 该方法涉及使用阳离子和阴离子交换树脂和溶剂处理来去除有机和无机污染物。 存在于原始DOTA中的任何阳离子或由环化物反应产生的其它污染物在该方法的早期阶段大大降低，从而在纯化级别中以更容易和可靠的方式获得良好的DOTA产率。 该方法可用于生产DOTA，包括其金属离子络合物的大环化合物和包含可用作磁共振成像造影剂的大环化合物的组合物。

    ERGOLINE DERIVATIVES AS DOPAMINE RECEPTOR MODULATORS
    3.
    发明申请
    ERGOLINE DERIVATIVES AS DOPAMINE RECEPTOR MODULATORS 有权
    ERGOLINE衍生物作为多巴胺受体调节剂

    公开(公告)号：US20150307486A1

    公开(公告)日：2015-10-29

    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： 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).

    摘要翻译： 本发明提供式（I）化合物，其中R 1 -R 4具有说明书中定义的任何值及其盐。 该化合物可用作多巴胺受体调节剂，用于治疗涉及多巴胺受体调节的疾病（例如性功能障碍，催乳素瘤，帕金森病和缓冲疾病）。

    NOVEL SUBSTITUTED INDOLO 4,3 FG QUINOLINES USEFUL FOR TREATING MIGRAINE
    4.
    发明申请
    NOVEL SUBSTITUTED INDOLO 4,3 FG QUINOLINES USEFUL FOR TREATING MIGRAINE 审中-公开

    公开(公告)号：US20140194434A1

    公开(公告)日：2014-07-10

    申请号：US14202744

    申请日：2014-03-10

    申请人： MAP Pharmaceuticals, Inc.

    发明人： Robert O. Cook ,  THOMAS A. ARMER ,  Sergey Alexandrovich KOSAREV ,  Dejian Xie ,  Jian Zhang

    IPC分类号： C07D519/02

    CPC分类号： C07D519/02 ,  C07D457/04

    摘要： Provided herein are novel ergoline derivatives and pharmaceutical compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1D and or 5-HT1B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing or inhibiting activity at receptors such as, for example, the 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of regulating serotonin transport using the compounds and compositions disclosed herein.

    Process for preparing crystalline from I of cabergoline
    6.
    发明申请
    Process for preparing crystalline from I of cabergoline 失效
    从卡麦角林的I制备结晶的方法

    公开(公告)号：US20030149067A1

    公开(公告)日：2003-08-07

    申请号：US10239636

    申请日：2003-02-03

    发明人： Attilio Tomasi ,  Stefania Magenes ,  Mario Ungari ,  Giuliano Ramella ,  Gianfranco Pallanza

    IPC分类号： A61K031/48 ,  C07D457/02

    CPC分类号： C07D457/04

    摘要： A process for producing crystalline form I of cabergoline, which process comprises crystallization of the desired form from a toluene/diethyl ether mixture comprising raw cabergoline, followed by recovery and drying of the resulting crystals. A new solvate form V of cabergoline, useful as an intermediate, is also provided.

    摘要翻译： 一种生产卡麦角林I型结晶的方法，该方法包括将所需形式从含有原卡麦角林的甲苯/二乙醚混合物中结晶，然后回收和干燥所得晶体。 还提供了可用作中间体的新的卡麦角林型V型。

    Process of preparing lysergic acid
    7.
    发明授权
    Process of preparing lysergic acid 有权
    制备麦角酸的方法

    公开(公告)号：US06242603B1

    公开(公告)日：2001-06-05

    申请号：US09598425

    申请日：2000-06-21

    申请人： Jean-Claude Gaullier

    发明人： Jean-Claude Gaullier

    IPC分类号： C07D45702

    CPC分类号： C07D457/04

    摘要： The present invention relates to a novel process for preparing lysergic acid by isomerizing paspalic acid, using a tetraalkylammonium hydroxide.

    摘要翻译： 本发明涉及使用四烷基氢氧化铵通过异构化帕斯卡酸来制备麦角酸的新方法。

    Novel ergolinyl compounds nitrogen-substituted in the 8-position, useful for treating dopamine deficiency
    9.
    发明授权
    Novel ergolinyl compounds nitrogen-substituted in the 8-position, useful for treating dopamine deficiency 失效
    在8-位氮取代的新型麦角酰基化合物，可用于治疗多巴胺缺乏症

    公开(公告)号：US4826852A

    公开(公告)日：1989-05-02

    申请号：US878762

    申请日：1986-06-26

    申请人： Gregor Haffer ,  Gerhard Sauer ,  Helmut Wachtel ,  Herbert Schneider ,  Ulrich Eder

    发明人： Gregor Haffer ,  Gerhard Sauer ,  Helmut Wachtel ,  Herbert Schneider ,  Ulrich Eder

    IPC分类号： A61K31/48 ,  A61P9/12 ,  A61P25/00 ,  A61P25/18 ,  A61P25/28 ,  A61P43/00 ,  C07D457/04 ,  C07D457/06 ,  C07D457/12 ,  A61K31/44 ,  A61K31/54 ,  C07D417/14

    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) ##STR1## and physiologically compatible salts thereof, wherein (a) R.sup.1 is hydrogen, the 8-substituent can be in the .alpha.- or .beta.-position and ##STR2## represents a single or a double bond, R.sup.2 is hydrogen, C.sub.1-4 -alkyl or C.sub.1-7 -acyl,R.sup.3 is hydrogen, chlorine or bromine, andR.sup.4 is C.sub.1-6 -alkyl, C.sub.3-6 -cycloalkyl-C.sub.1-3 -alkyl, C.sub.3-6 -alkenyl, or C.sub.3-6 -alkynyl; or(b) R.sup.1 is ##STR3## and the 8-substituent can be in the .alpha.- or .beta.-position, ##STR4## represents a single or double bond, R.sup.2, R.sup.3 are as defined above,R.sup.4, is C.sub.1.varies.6 -alkyl, C.sub.3-6 -cycloalkyl-C.sub.1-3 -alkyl, C.sub.3-6 -alkenyl, or C.sub.3-6 -alkynyl; andR.sup.5 is hydrogen, C.sub.-10 -alkyl, C.sub.3-10 -alkenyl, or C.sub.3-10 -alkynyl, andR.sup.6 is C.sub.1-10 -alkyl, C.sub.3-10 -alkenyl, C.sub.3-10 -alkynyl, or aryl, orR.sup.5 and R.sup.6 together with the connecting N-atom form a 5- to 10-membered heterocyclic ring, preferably 5- or 6-membered, which optionally can contain further heteroatoms.

    摘要翻译： 在8-位上被氮取代且具有式（I）的化合物和其生理上相容的盐，其中（a）R 1是氢，所述8-取代基可以是α-或β- - 位和表示单键或双键，R 2为氢，C 1-4 - 烷基或C 1-7 - 酰基，R 3为氢，氯或溴，且R 4为C 1-6 - 烷基，C 3-6 环烷基-C 1-3 - 烷基，C 3-6 - 烯基或C 3-6 - 炔基; 或（b）R 1是，并且8-取代基可以是α-或β-位，表示单键或双键，R2，R3如上所定义，R4是C1， 烷基，C 3-6 - 环烷基-C 1-3 - 烷基，C 3-6 - 烯基或C 3-6 - 炔基; 和R 5是氢，C 1-10烷基，C 3-10 - 烯基或C 3-10 - 炔基，R 6是C 1-10烷基，C 3-10 - 烯基，C 3-10 - 炔基或芳基或R 5 和R6连同连接的N-原子形成5-至10-元杂环，优选5-或6-元，其任选地可含有其它杂原子。

    Process for preparing n-methyl derivatives of methyl dihydrolysergate and methyl methoxylumilysergate
    10.
    发明授权
    Process for preparing n-methyl derivatives of methyl dihydrolysergate and methyl methoxylumilysergate 失效
    制备甲基二氢盐酸盐和甲基甲氧基乳糖凝胶的正甲基衍生物的方法

    公开(公告)号：US4739061A

    公开(公告)日：1988-04-19

    申请号：US884036

    申请日：1986-07-10

    申请人： Christian Gervais

    发明人： Christian Gervais

    IPC分类号： B01J31/00 ,  B01J31/02 ,  C07B61/00 ,  C07D457/04

    CPC分类号： C07D457/04

    摘要： A process for preparing an N-methyl derivative of methyl dihydrolysergate and methyl methoxylumilysergate, of formula: ##STR1## in which R.sub.1 denotes a hydrogen atom or a methoxy group, which comprises reacting a methylating agent with a compound of formula: ##STR2## in which R.sub.1 is defined as above, in the presence of a quaternary salt, in the presence of a solid metal alcoholate of formula CH.sub.3 --OM in which M denotes an alkali metal atom, or an alkali metal hydride, and in the presence of a dehydrating agent of formula R.sub.2 --COO--CH.sub.3 in which R.sub.2 denotes a hydrogen atom or an alkyl, alkyloxy, alkyloxycarbonyl or aryl group or of formula R.sub.3 --C(OCH.sub.3).sub.3 in which R.sub.3 denotes a hydrogen atom, an alkyl group or an aryl group.

    摘要翻译： 一种制备甲基二氢赖氨酸N-甲基衍生物和甲基甲氧基月桂酰胺的方法，其结构式为：其中R 1表示氢原子或甲氧基，其中包括使甲基化剂与下式化合物反应： 在其中M表示碱金属原子或碱金属氢化物的式CH3-OM的固体金属醇化物存在下，在季盐的存在下，将R1定义如上所述，并且在脱水 式R2-COO-CH3的试剂，其中R2表示氢原子或烷基，烷氧基，烷氧基羰基或芳基或式R3-C（OCH3）3，其中R3表示氢原子，烷基或芳基 。