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    • 8. 发明授权
    • Aryl boronic acids for treating obesity
    • 用于治疗肥胖症的芳基硼酸
    • US06858592B2
    • 2005-02-22
    • US10187397
    • 2002-06-27
    • Stephen Randall Holmes-FarleyW. Harry Mandeville, IIIPradeep K. DhalChad Cori HuvalXinhua Li
    • Stephen Randall Holmes-FarleyW. Harry Mandeville, IIIPradeep K. DhalChad Cori HuvalXinhua Li
    • A61K31/69A61K31/74A61K31/785A61P3/04A61P3/06C07F5/02
    • C07F5/025A61K31/74A61K31/785
    • 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—(CH2)q]r—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-trialkylated. 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 R1 is Structural Formula (I) is preferably —H. R1a 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 carrier or diluent.
    • 公开了由结构式(I)表示的苯基硼酸化合物:Ar是取代或未取代的芳基.Z和Z'独立地是-O-。 -NH-或-S-X是吸电子基团.R是任选地包含一个或多个胺,铵,醚,硫醚或亚苯基连接基团的取代或未取代的直链烃基,Y是-H,胺, - [NH-(CH 2)q] r -NH 2,卤素,-CF 3,硫醇铵,醇,-COOH,-SO 3 H,-OSO 3 H或共价键合到R的末端的鏻基团。 NH-(CH 2)q] r -NH 2任选被N-烷基化或N,N-二烷基化,-NH 2在 - [NH-(CH 2)q] r -NH 2中任选地N-烷基化,N,N-二烷基化或N ,N,N-三烷基化.q为2至约10的整数,r为1至约5.R1的整数,R1'独立地为-H,脂族基团,取代的脂族基团,芳基或 取代的芳基,或者一起是任选地包含胺连接基团[-N +(R 1a) - ] - 的C 2 -C 5取代或未取代的亚烷基。 每个R1是结构式(I)优选-HR 1a是-H,烷基,取代的烷基,苯基或取代的苯基。还公开了通过给予有效量的由 结构式(I)和包含该化合物和药学上可接受的载体或稀释剂的药物组合物。