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    • 2. 发明申请
    • DELTA 9 TETRAHYDROCANNABINOL DERIVATIVES
    • DELTA 9四氯氰菊酯衍生物
    • US20110171300A1
    • 2011-07-14
    • US12527183
    • 2008-02-14
    • Parveen BhatarahKevin John BatchelorDerek MchattieAlan Kenneth Greenwood
    • Parveen BhatarahKevin John BatchelorDerek MchattieAlan Kenneth Greenwood
    • A61K9/64C07D311/80A61K31/353A61P1/08
    • C07D311/80
    • A compound of formula (I) wherein R is selected from (i) a 5 to 7 membered heterocyclic ring containing 1 to 3 heteroatoms independently selected from nitrogen, oxygen and sulfur, which is optionally substituted by one or more groups independently selected from halo, CN, NO2, (C1-C6)alkyl, (C1-C6)alkoxy and phenyl; (ii) (C1-C6)alkyl, which is optionally substituted by one or more substituents each independently selected from halo, oxo, CN, NO2, (C1-C6)alkyl, (C1-C6)alkoxy and phenyl; (iii) (C1-C6)alkyl substituted by (C3-C13)cycloalkyl, which is optionally substituted by one or more substituents each independently selected from halo, oxo, CN, NO2, (C1-C6)alkyl, (C1-C6)alkoxy and phenyl; and (iv) (C3-C13)cycloalkyl, which is optionally substituted by one or more substituents each independently selected from halo, oxo, CN, NO2, (C1-C6)alkyl, (C1-C6)alkoxy and phenyl.
    • 式(I)化合物,其中R选自(i)含有1至3个独立地选自氮,氧和硫的杂原子的5至7元杂环,其任选被一个或多个独立地选自以下的基团取代:卤素, CN,NO 2,(C 1 -C 6)烷基,(C 1 -C 6)烷氧基和苯基; (C 1 -C 6)烷基,(C 1 -C 6)烷基,其任选被一个或多个各自独立地选自卤素,氧代,CN,NO 2,(C 1 -C 6)烷基,(C 1 -C 6)烷氧基和苯基的取代基取代; (C 3 -C 13)环烷基取代的(C 3 -C 13)烷基,其任选被一个或多个独立地选自卤素,氧代,CN,NO 2,(C 1 -C 6)烷基,(C 1 -C 6) )烷氧基和苯基; 任选被一个或多个独立地选自卤素,氧代,CN,NO 2,(C 1 -C 6)烷基,(C 1 -C 6)烷氧基和苯基的取代基取代的(ⅳ)(C 3 -C 13)环烷基。
    • 5. 发明授权
    • Preparation of cabergoline
    • 卡麦角林的制备
    • US07339060B2
    • 2008-03-04
    • US11268118
    • 2005-11-07
    • Alan Kenneth GreenwoodDerek McHattieParveen BhatarahMahmoud Aloui
    • Alan Kenneth GreenwoodDerek McHattieParveen BhatarahMahmoud Aloui
    • C07D457/04C07D457/02
    • C07D457/06
    • A method of preparing cabergoline Form I, comprising forming a solvate including cabergoline and a p-disubstituted benzene of formula (A) or 1,3,5-trimethylbenzene and obtaining cabergoline Form I from the solvate. Another aspect of the present invention provides a method for preparing cabergoline Form I comprising dissolving cabergoline in p-disubstituted benzene or 1,3,5-trimethylbenzene and recovering the cabergoline Form I polymorph, suitably by direct crystallization of Form I or by recovery of a solvate which can be converted to Form I. Another aspect of the present invention provides a novel cabergoline polymorph designated cabergoline Form FB and a method of preparing said polymorph by dissolving or forming a solvate of cabergoline in fluorobenzene and recovering cabergoline Form FB.
    • 制备卡麦角林型I的方法,包括形成包含卡麦角林和式(A)的对二取代的苯或1,3,5-三甲基苯的溶剂合物,并从溶剂合物中获得卡麦角林I型。 本发明的另一方面提供了一种制备卡麦角林型I的方法,其包括将卡麦角林溶解在对二取代的苯或1,3,5-三甲基苯中,并适当地通过形式I的直接结晶或通过回收 本发明的另一方面提供了一种新颖的卡麦角林多晶型物,称为卡麦角林型F B B,以及通过溶解或形成卡麦角林溶剂化物在氟苯中制备所述多晶型物的方法,以及 恢复卡麦角林F型B。