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1. 发明授权

EP1404685B1 ARYL BORONIC ACIDS FOR TREATING OBESITY 有权
标题翻译：芳基硼酸用于治疗肥胖
公开(公告)号：EP1404685B1
公开(公告)日：2006-09-13
申请号：EP02746808.1
申请日：2002-07-01
申请人： GENZYME CORPORATION
发明人： HOLMES-FARLEY, Stephen, Randall , MANDEVILLE, W., Harry, III , HUVAL, Chad, Cori , LI, Xinhua , DHAL, Pradeep, K.
IPC分类号： C07F5/02 , A61K31/015 , A61P3/04
CPC分类号： C07F5/025 , A61K31/74 , A61K31/785
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.

2. 发明公开

EP1578816A1 POLYMERIC BORONIC ACID DERIVATIVES AS LIPASE INHIBITORS 审中-公开
标题翻译：聚合物硼酸衍生物作为脂肪酶抑制剂
公开(公告)号：EP1578816A1
公开(公告)日：2005-09-28
申请号：EP03768974.2
申请日：2003-11-19
申请人： GENZYME CORPORATION
发明人： HUVAL, Chad Cori , LI, Xinhua , HOLMES-FARLEY, Stephen, Randall , DHAL, Pradeep, K.
IPC分类号： C08F20/00
CPC分类号： C08F230/06 , A61K31/69 , A61K45/06 , C08F30/06 , C08F220/56 , C08F220/60 , C08F226/10 , C08F265/00 , C08F289/00 , C08F290/06 , C08F290/14 , C08F291/00 , C08F293/005 , C08F297/00 , C08F297/02 , C08F2438/02
摘要： Human obesity is a health problem affecting a significant proportion of the American population. Numerous methods of treating obesity have been developed, but all have serious drawbacks. The present invention discloses a novel class of polymers with either a sulfur atom or an electron withdrawing group between a polymer backbone and pendant aryl boronic acid group. Polymers having such an electron withdrawing group have been found to be particularly effective in inhibiting lipase in vitro and in vivo. Methods of treating obesity and reducing absorption of fat are also disclosed.

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