Substituted heterocyclic compounds and methods of use
    91.
    发明授权
    Substituted heterocyclic compounds and methods of use 失效
    取代的杂环化合物及其使用方法

    公开(公告)号:US06967254B2

    公开(公告)日:2005-11-22

    申请号:US10658298

    申请日:2003-09-08

    CPC classification number: C07D401/04 C07D401/14

    Abstract: The present invention relates to compounds having the general formula or a pharmaceutically acceptable salt thereof. Also included is a method of prophylaxis or treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic β cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer's disease, stroke, myocardial infarction, ischemia reperfusion injury, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shock syndrome, fever, myalgias due to HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses or herpes zoster infection in a mammal comprising administering an effective amount a compound as described above.

    Abstract translation: 本发明涉及具有通式的化合物或其药学上可接受的盐。 还包括预防或治疗炎症,类风湿性关节炎,斑节病,骨质疏松症,多发性骨髓瘤,葡萄膜炎,急性或慢性骨髓性白血病,胰腺β细胞破坏,骨关节炎,类风湿性脊椎炎,痛风性关节炎,炎性肠病,成人呼吸 窘迫综合征(ARDS),牛皮癣,克罗恩病,过敏性鼻炎,溃疡性结肠炎,过敏反应,接触性皮炎,哮喘,肌肉退化,恶病质,赖特综合征,I型糖尿病,II型糖尿病,骨吸收疾病,移植物抗宿主反应, 阿尔茨海默病,中风,心肌梗死,缺血再灌注损伤,动脉粥样硬化,脑外伤,多发性硬化,脑疟疾,败血症,败血性休克,中毒性休克综合征,发热,HIV-1,HIV-2,HIV-3,巨细胞病毒引起的肌痛 (CMV),流感,腺病毒,哺乳动物中的疱疹病毒或带状疱疹感染,包括给予有效量的化合物d 以上所述。

    Aralkyl diazabicycloalkane derivatives for CNS disorders
    96.
    发明授权
    Aralkyl diazabicycloalkane derivatives for CNS disorders 失效
    用于CNS病症的芳烷基二氮杂双环烷烃衍生物

    公开(公告)号:US5958920A

    公开(公告)日:1999-09-28

    申请号:US954284

    申请日:1997-10-20

    CPC classification number: C07D471/04 A61K31/495 C07D487/04

    Abstract: Certain aralkyl diazabicycloalkyl compounds are disclosed for treatment of CNS disorders, such as cerebral ischemia, psychosis and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein m is three or four; wherein z is selected from the group consisting of ##STR2## wherein when Z is ##STR3## n and p are integers of from one to four, with a sum of four or five, and when Z is ##STR4## n and p are integers of from one to three, with a sum of three or four; wherein A is selected from the group consisting of aryl, heteroaryl, aryloxy, heteroaryloxy, aralkoxy, heteroaralkoxy, arylamino, heteroarylamino, aralkylamino, heteroaralkylamino, arylthio, heteroarylthio, aralkylthio, and heteroaralkylthio; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from the group consisting of hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, aralkyl, aryl, alkoxy, aryloxy, aralkoxy, alkoxyalkyl, halo, haloalkyl, hydroxyalkyl, cyano, amino, monoalkylamino, dialkylamino, carboxy, carboxyalkyl, alkanoyl, alkenyl and alkynyl; or a pharmaceutically acceptable salt thereof.

    Abstract translation: 公开了某些芳烷基二氮杂双环烷基化合物用于治疗中枢神经系统疾病,如脑缺血,精神病和抽搐。 特别感兴趣的化合物具有下式:其中m为三或四; 其中z选自其中当Z为n且p为1至4的整数时,其总数为4或5,当Z为n且p为1至3的整数时,其总和为 三或四; 其中A选自芳基,杂芳基,芳氧基,杂芳氧基,芳烷氧基,杂芳烷氧基,芳基氨基,杂芳基氨基,芳烷基氨基,杂芳烷基氨基,芳硫基,杂芳硫基,芳烷硫基和杂芳烷硫基。 其中前述A基团中的任一个可以进一步被一个或多个独立地选自羟基,羟基,烷基,环烷基,环烷基烷基,芳烷基,芳基,烷氧基,芳氧基,芳烷氧基,烷氧基烷基,卤素,卤代烷基, ,氰基,氨基,单烷基氨基,二烷基氨基,羧基,羧基烷基,烷酰基,烯基和炔基; 或其药学上可接受的盐。

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