您的位置: 首页 > 农业专利 > 详情页

NEW AZABICYCLO[3.2.0]HEPT-3-YL COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
专利权人:
发明人:
카사라, 패트릭,촐렛, 안네-마리,다이나우트, 알랭,레스테이지, 피에르,파나이, 파니
申请号:
KR1020100124116
公开号:
KR1012927050000B1
申请日:
2010.12.07
申请国别(地区):
KR
年份:
2013
代理人:
摘要:
Azabicyclo [3.2.0] hept-3-yl derivatives (I) and their enantiomers, diastereoisomers, or addition salts with an acid or a base are new. Azabicyclo [3.2.0] hept-3-yl derivatives of formula (I) and their enantiomers, diastereoisomers, or addition salts with an acid or a base are new. ALK : an alkylene chain; W1 : amide group of formula (-NR1a-C(=O)-R) or (-C(=O)-NR1a-R); and R1a, R : H or 1-6C alkyl optionally substituted by one or more groups comprising halo, hydroxy or alkoxy, provided that the alkylene denotes 2-6C divalent radical, and the alkoxy is 1-6C alkyloxy. Independent claims are included for: (1) the preparation of (I); and (2) intermediates comprising alkylene benzoic acid substituted aza-bicycloheptane compounds of formula (VI), alkylene benzoyl chloride substituted aza-bicycloheptane compounds of formula (VII), alkylene benzoic acid ester substituted aza-bicyclo-heptane compounds of formula (VIII), and alkylene oxy phenyl substituted aza-bicyclo-heptane compounds of formula (IX), for preparing (I) (where W1 represents -CONRR1a). R2a : 1-6C alkyl or benzyl. [Image] [Image] ACTIVITY : Nootropic; Neuroleptic; Neuroprotective; Cerebroprotective; Vulnerary; Hypnotic; Tranquilizer; Antidepressant; CNS-Gen. MECHANISM OF ACTION : Histamine H3 receptor antagonist. The histamine H3 receptor antagonistic activity of (I) was tested in Naval medical research institute (NMRI) mice. The result showed that 4-{3-[(1R,5S)-3-aza-bicyclo[3.2.0]hept-6-yl]-propoxy}benzamide hydrochloride increased the endogenous cerebral concentration of N-methylhistamine to 100%, at 3 mg/kg.본 발명은 하기 화학식(Ⅰ)의 화합물 및 이를 함유하는 약제에 관한 것이다:상기 식에서,ALK는 알킬렌 사슬이고,W는 기 또는 이고, 여기서, R 및 R'은 본 발명의 상세한 설명에 정의된 바와 같다.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

意 见 箱

匿名:登录

个人用户登录

找回密码

第三方账号登录

忘记密码

个人用户注册

必须为有效邮箱
6~16位数字与字母组合
6~16位数字与字母组合
请输入正确的手机号码

信息补充