Novel glucokinase activators and methods of using same

Details Novel glucokinase activators and methods of using same Novel glucokinase activators and methods of using same

C - Chemistry, Metallurgy

07

F

C07F 9/32 (2006.01) A61K 31/675 (2006.01) A61P 3/00 (2006.01) C07F 9/40 (2006.01)

Patent

CA 2658001

Compounds are provided which are phosphonate and phosphinate activators and thus are useful in treating diabetes and related diseases and have the structure of Formula (I), wherein Formula (II) is a heteroaryl ring; R4 is -(CH2)n-Z-(CH2)m-PO(OR7)(OR8), -(CH2)nZ-(CH2)m-PO(OR7)R9, -(CH2)n-Z-(CH2)m-OPO(OR7)R9, -(CH2)nZ-(CH2)m-OPO(R9)(R10), or -(CH2)nZ-(CH2)m-PO(R9)(R10); R5 and R6 are independently selected from H, alkyl and halogen; Y is R7(CH2)s or is absent; and X, n, Z, m, R4, R5, R6, R7, and s are as defined herein; or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.

L'invention concerne des composés qui sont des activateurs de phosphonate et de phosphinate, qui sont donc utiles dans le traitement des diabètes et des maladies apparentées et qui possèdent la structure de la formule (I), où la formule (II) représente un noyau hétéroaryle; R<SUB>4</SUB> représente un groupe -(CH<SUB>2</SUB>)<SUB>n</SUB>-Z-(CH<SUB>2</SUB>)<SUB>m</SUB>-PO(OR<SUB>7</SUB>)(OR<SUB>8</SUB>), -(CH<SUB>2</SUB>)<SUB>n</SUB>Z-(CH<SUB>2</SUB>)<SUB>m</SUB>-PO(OR<SUB>7</SUB>)R<SUB>9</SUB>, -(CH<SUB>2</SUB>)<SUB>n</SUB>-Z-(CH<SUB>2</SUB>)<SUB>m</SUB>-OPO(OR<SUB>7</SUB>)R<SUB>9</SUB>, -(CH<SUB>2</SUB>)<SUB>n</SUB>Z-(CH<SUB>2</SUB>)<SUB>m</SUB>-OPO(R<SUB>9</SUB>)(R<SUB>10</SUB>), ou -(CH<SUB>2</SUB>)<SUB>n</SUB>Z-(CH<SUB>2</SUB>)<SUB>m</SUB>-PO(R<SUB>9</SUB>)(R<SUB>10</SUB>); R<SUB>5</SUB> et R<SUB>6</SUB> sont indépendamment choisis parmi un atome H, un groupe alkyle et un atome d'halogène; Y représente R<SUB>7</SUB>(CH<SUB>2</SUB>)<SUB>s</SUB> ou est absent; et X, n, Z, m, R<SUB>4</SUB>, R<SUB>5</SUB>, R<SUB>6</SUB>, R<SUB>7</SUB>, et s sont tels que définis ci-après; ou un sel pharmaceutiquement acceptable de ces activateurs. L'invention concerne également un procédé pour traiter les diabètes et les maladies apparentées en employant les composés précédents.

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