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    • 12. 发明申请
    • Phosphate transport inhibitors
    • 磷酸盐转运抑制剂
    • US20070021509A1
    • 2007-01-25
    • US11489286
    • 2006-07-19
    • Thomas JozefiakCecilia BastosAndrew PapoulisStephen Holmes-Farley
    • Thomas JozefiakCecilia BastosAndrew PapoulisStephen Holmes-Farley
    • A61K31/18
    • A61K45/06A61K31/166A61K31/17A61K31/18A61K31/415A61K31/63A61K33/38A61K2300/00
    • Disclosed are compounds which have been identified as inhibitors of phosphate transport. Many of the compounds are represented by Structural Formula (I): Ar1—W—X—Y—Ar2; or a pharmaceutically acceptable salt thereof. Ar1 and Ar2 are independently a substituted or unsubstituted aryl group or an optionally substituted five membered or six membered non-aromatic heterocylic group fused to an optionally substituted monocylic aryl group. W and Y are independently a covalent bond or a C1-C3 substituted or unsubstituted alkylene group. X is a heteroatom-containing functional group, an aromatic heterocyclic group, substituted aromatic heterocyclic group, non-aromatic heterocyclic group, substituted non-aromatic heterocyclic group, an olefin group or a substituted olefin group. Also disclosed are methods of treating a subject with a disease associated with hyperphosphatemia, as well as a disease mediated by phosphate-transport function. The methods comprise the step of administering an effective amount of the one of the compounds described above.
    • 公开了已被鉴定为磷酸盐转运抑制剂的化合物。 许多化合物由结构式(I)表示:<?in-line-formula description =“In-line Formulas”end =“lead”?> Ar -WXY-Ar 2 <?in-line-formula description =“In-line Formulas”end =“tail”?>或其药学上可接受的盐。 Ar 1和Ar 2独立地是与任选取代的单环芳基稠合的取代或未取代的芳基或任选取代的五元或六元非芳族杂环基。 W和Y独立地是共价键或C1-C3取代或未取代的亚烷基。 X为含杂原子的官能团,芳香族杂环基,取代芳香族杂环基,非芳香族杂环基,取代非芳香族杂环基,烯基或取代烯基。 还公开了治疗患有与高磷酸盐血症相关的疾病的受试者以及由磷酸盐转运功能介导的疾病的方法。 所述方法包括施用有效量的上述一种化合物的步骤。
    • 18. 发明申请
    • Aryl boronic acids for treating obesity
    • US20060128664A1
    • 2006-06-15
    • US11343598
    • 2006-01-31
    • Stephen Holmes-FarleyW. MandevillePradeep DhalChad HuvalXinhua Li
    • Stephen Holmes-FarleyW. MandevillePradeep DhalChad HuvalXinhua Li
    • A61K31/69C07F5/02
    • 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.