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102 条记录 (耗时 0.059 秒)

    1,2,3,4,5,6-Hexahydro-2,6-methano-3-benzazocin-10-ols
    25.
    发明授权
    1,2,3,4,5,6-Hexahydro-2,6-methano-3-benzazocin-10-ols 有权
    1,2,3,4,5,6-六氢-2,6-亚甲基-3-苯并吖庚因-10-ols

    公开(公告)号：US06455538B1

    公开(公告)日：2002-09-24

    申请号：US09523473

    申请日：2000-03-10

    申请人： Matthias Grauert ,  Adrian Carter ,  Wolf-Dietrich Bechtel ,  Thomas Weiser ,  Rainer Palluk ,  Uwe Pschorn

    发明人： Matthias Grauert ,  Adrian Carter ,  Wolf-Dietrich Bechtel ,  Thomas Weiser ,  Rainer Palluk ,  Uwe Pschorn

    IPC分类号： A61K31439

    CPC分类号： C07D221/26

    摘要： Compounds of general formula I wherein X is a single bond, —O—, C-C4-alkylene, or an alkylene bridge having 1 to 8 carbon atoms which may be branched or unbranched and optionally have one or two oxygen atom(s) anywhere in the bridge; R1 is hydrogen, methyl, ethyl, or phenyl; R2 is hydrogen or methyl; R3 is hydrogen, fluorine, chlorine, bromine, hydroxy, methyl, or methoxy; R4 is hydrogen, methyl, or ethyl; R5 is hydrogen, methyl, or ethyl; R6 is hydrogen, methyl, or ethyl; R7 is tert-butyl, cyclohexyl, phenyl optionally substituted by R9 and R10, which may be identical or different, or; R8 is hydrogen or C1-C4-alkyl; Z is oxygen, NH, or sulfur; R9 is hydrogen, methyl, fluorine, chlorine, bromine, or methoxy; R10 is hydrogen, methyl, fluorine, chlorine, bromine, or methoxy; optionally in the form of the individual optical isomers, mixtures of the individual enantiomers or racemates as well as in the form of the free bases or the corresponding acid addition salts with pharmaceutically acceptable acids.

    摘要翻译： 通式I的化合物，其中X是单键，-O-，C-C4-亚烷基或具有1至8个碳原子的亚烷基桥，其可以是支链或非支链的，并且任选地在一个或多个氧原子中具有一个或两个氧原子 桥梁 R1是氢，甲基，乙基或苯基; R2是氢或甲基; R3是氢，氟，氯，溴，羟基，甲基或甲氧基; R4是氢，甲基或乙基; R5是氢，甲基或乙基; R6是氢，甲基或乙基; R 7是叔丁基，环己基，任选被R 9和R 10取代的苯基，其可以相同或不同，或者R 8是氢或C 1 -C 4 - 烷基; Z是氧，NH或硫; R9是氢，甲基，氟，氯，溴或甲氧基; R 10为氢，甲基，氟，氯，溴或甲氧基; 任选以各种旋光异构体的形式，各个对映异构体或外消旋体的混合物，以及游离碱的形式或与药学上可接受的酸的相应的酸加成盐。

    Specific salt, anhydrous and crystalline form of a dihydropteridione derivative
    28.
    发明授权
    Specific salt, anhydrous and crystalline form of a dihydropteridione derivative 有权
    特殊的盐，无水和结晶形式的二氢异二萜衍生物

    公开(公告)号：US08664222B2

    公开(公告)日：2014-03-04

    申请号：US13457991

    申请日：2012-04-27

    申请人： Guenter Linz ,  Peter Sieger ,  Matthias Grauert ,  Rolf Schmid

    发明人： Guenter Linz ,  Peter Sieger ,  Matthias Grauert ,  Rolf Schmid

    IPC分类号： C07D475/00 ,  A61K31/4985 ,  A61P35/00

    CPC分类号： C07D475/00

    摘要： The present invention relates to a specific salt of a dihydropteridione derivative, namely the trihydrochloride salt of the compound N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxy-benzamide, to its crystallization in the form of an hydrate with water, to a process for the manufacture thereof, and to the use thereof in a pharmaceutical composition.

    摘要翻译： 本发明涉及二氢二萜二酮衍生物的具体盐，即化合物N- [反式-4- [4-（环丙基甲基）-1-哌嗪基]环己基] -4 - [[（7R）-7 - 乙基-5,6,7,8-四氢-5-甲基-8-（1-甲基乙基）-6-氧代-2-蝶啶基]氨基] -3-甲氧基 - 苯甲酰胺，以其结晶形式为 水合物，其制备方法及其在药物组合物中的用途。