发明授权
- 专利标题: ARYL BORONIC ACIDS FOR TREATING OBESITY
- 专利标题(中): 芳基硼酸用于治疗肥胖
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申请号: EP02746808.1申请日: 2002-07-01
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公开(公告)号: EP1404685B1公开(公告)日: 2006-09-13
- 发明人: HOLMES-FARLEY, Stephen, Randall , MANDEVILLE, W., Harry, III , HUVAL, Chad, Cori , LI, Xinhua , DHAL, Pradeep, K.
- 申请人: GENZYME CORPORATION
- 申请人地址: 153 Second Avenue Waltham, MA 02451 US
- 专利权人: GENZYME CORPORATION
- 当前专利权人: GENZYME CORPORATION
- 当前专利权人地址: 153 Second Avenue Waltham, MA 02451 US
- 代理机构: Stevens, Ian Edward
- 优先权: US302081P 20010629; US359467P 20020222
- 国际公布: WO2003002570 20030109
- 主分类号: C07F5/02
- IPC分类号: C07F5/02 ; A61K31/015 ; A61P3/04
摘要:
Disclosed is a phenyl boronic acid compound represented by Structural Formula (I): Ar is a substituted or unsubstituted aryl group. Z and Z' are independently -O-. -NH- or -S-. X is an electron withdrawing group. R is a substituted or unsubstituted straight chained hydrocarbyl group optionally comprising one or more amine, ammonium, ether, thioether or phenylene linking groups and Y is -H, an amine, -[NH-(NH2)q]-NH2, halogen, -CF3, thiol, ammonium, alcohol, -COOH, -SO3H, -OSO3H or phosphonium group covalently bonded to the terminal position of R. Each -NH- in -[NH-)CH2)q]r-NH2 is optionally N-alkylated or N,N-dialkylated and -NH2 in -[NH-(CH2)q]r-NH2 is optionally N-alkylated, N,N-dialkylated or N,N,N-triakylated. q is an integer from 2 to about 10 and r is an integer from 1 to about 5. R1 and R1' are independently -H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or, taken together, are a C2-C5 substituted or unsubstituted alkylene group optionally comprising an amine linking group [-N+(R1a)-]. Each R¿1?, is Structural Formula (I) is preferably -H. R?1a¿ is-H, alkyl, substituted alkyl, phenyl or substituted phenyl. Also disclosed is a method of treating obesity in a subject by administering an effective amount of a compound represented by Structural Formula (I) and a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carier or diluent.
公开/授权文献
- EP1404685A1 ARYL BORONIC ACIDS FOR TREATING OBESITY 公开/授权日:2004-04-07
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