Macrocyclic sh2 domain binding inhibitors

Details Macrocyclic sh2 domain binding inhibitors Macrocyclic sh2 domain binding inhibitors

A - Human Necessities

61

K

A61K 38/12 (2006.01) A61K 31/675 (2006.01) A61P 35/00 (2006.01) C07F 9/553 (2006.01) C07K 5/12 (2006.01)

Patent

CA 2582908

Disclosed are compounds for inhibiting the binding of an SH2 domain-containing protein, for example, a compound of formula (I): FORMULA (I) wherein R1 is a lipophile; R2, in combination with the phenyl ring, is a phenylphosphate mimic group or a protected phenylphosphate mimic group; R3 is, for example, hydrogen, azido, amino, oxalylamino, carboxy alkyl, alkoxycarbonyl alkyl, aminocarbonyl alkyl, or alkyl carbonylamino; R6 is a linker; AA is an amino acid; and n is 1 to 6; or a pharmaceutically acceptable salt, stereoisomer, solvate, or hydrate thereof. Also disclosed are pharmaceutical compositions and methods of use of such compounds.

L'invention concerne des composés qui inhibent la liaison d'une protéine contenant un domaine SH2, par exemple de formule (I) ci-après. Dans cette formule, R1 est un lipophile; R2, en combinaison avec le cycle phényle, est un groupe analogue phénylphosphate ou un groupe analogue phénylphosphate protégé; R3 est, par exemple, hydrogène, azido, amino, oxalylamino, carboxy alkyle, alcoxycarbonyle alkyle, aminocarbonyle alkyle, ou alkyle carbonylamino; R6 est un lieur; AA est un acide aminé; et n vaut de 1 à 6; y compris un sel, stéréoisomère, solvate ou hydrate pharmaceutiquement acceptable correspondant. L'invention concerne aussi des compositions pharmaceutiques et des procédés d'utilisation relatifs aux composés considérés.

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