Macrocyclic peptides and use in inhibiting SH2 domain binding with a phosphoprotein such as treatment of cancer


Ontology type: sgo:Patent     


Patent Info

DATE

2005-12-20T00:00

AUTHORS

BURKE JR TERRENCE R , WEI CHANG-QING , VOIGT JOHANNES H , GAO YANG

ABSTRACT

Disclosed are compounds for SH2 domain binding inhibition. For example, disclosed is a compound of formula (I) wherein R1 is a lipophile; R2, in combination with the phenyl ring, forms a phenylphosphate mimic group or a protected phenylphosphate mimic group; R3 is hydrogen, azido, amino, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, or alkylcarbonylamino, wherein the alkyl portion of R3 may be optionally substituted with a substituent selected from the group consisting of halo, hydroxy, carboxyl, amino, aminoalkyl, alkyl, alkoxy, and keto; R6 is a linker; AA is an amino acid; and n is 1 to 6; or a salt thereof. Also disclosed are a pharmaceutical composition, a method for inhibiting an SH2 domain from binding with a phosphoprotein and a method of treating breast cancer. More... »

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