1,2,3,4,5,6-Hexahydro-2,6-methano-3-benzazocin-10-ols
    2.
    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

    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。

    Pharmaceutical compositions containing triazolones and methods of treating neurodegenerative disease using triazolones
    7.
    发明授权
    Pharmaceutical compositions containing triazolones and methods of treating neurodegenerative disease using triazolones 有权
    含有三唑酮的药物组合物和使用三唑酮治疗神经变性疾病的方法

    公开(公告)号:US06492407B2

    公开(公告)日:2002-12-10

    申请号:US09840281

    申请日:2001-04-23

    IPC分类号: A61K3141

    CPC分类号: C07D401/04 C07D249/12

    摘要: A method for treating a neurodegenerative disease or cerebral ischemia arising from conditions selected from the group consisting of Status epilepticus, hypoglycaemia, hypoxia, anoxia, brain trauma, brain oedema, amyotropic lateral sclerosis, Huntington's disease, Alzheimer's disease, hypotonia, cardiac infarction, brain pressure (elevated intracranial pressure), ischaemic and haemorrhagic stroke, global cerebral ischaemia with heart stoppage, diabetic polyneuropathy, tinnitus, perinatal asphyxia, psychosis, schizophrenia, depression, and Parkinson's disease, the method of treatment comprising administering to a host in need of such treatment a therapeutic amount of a compound of formula (I) wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions containing a compound of formula (I).

    摘要翻译: 一种用于治疗由选自癫痫持续状态,低血糖,缺氧,缺氧,脑外伤,脑水肿,肌萎缩性侧索硬化,亨廷顿舞蹈病,阿尔茨海默氏病,低张力,心肌梗死,脑中的病症引起的神经变性疾病或脑缺血的方法 压力(颅内压升高),缺血性和出血性中风,心脏停止的全球性脑缺血,糖尿病性多发性神经病,耳鸣,围产期窒息,精神病,精神分裂症,抑郁症和帕金森病,治疗方法包括向需要这种 治疗治疗量的式(I)化合物,其中R 1,R 2,R 3,R 4,R 5,R 6和R 7如本文所定义,或其药学上可接受的盐,以及含有式(I)化合物的药物组合物, 。