Sloan-kettering Institute for Cancer Research

Memorial Sloan Kettering Cancer Center

Weilin Sun

Gabriela Chiosis

Tony Taldone

Pallav Patel

Stefan O Ochiana

Hardik J Patel

Pengrong Yan

Chenghua Yang

The disclosure relates to novel selective Grp94 inhibitors, compositions comprising an effective amount of such compounds, and methods to treat or prevent a condition, such as cancer, comprising administering to an animal in need thereof an effective amount of such compounds.

Selective Grp94 inhibitors and uses thereof

The present application provides substituted purine derivatives and related compounds of the formulas shown. These compounds are useful as inhibitors of HSP90, and hence in the treatment of related diseases. (Formulae) Z-Z, X-X, X, X, Y and R are as defined in the specification. 

Purine derivatives useful as HSP90 inhibitors

The disclosure relates to Compounds of Formulae (IA) and (IB), and pharmaceutically acceptable salts thereof wherein Z, Z, Z, Xa, Xb, Xc, Xd, Y, X, and Xare as defined herein, compositions comprising an effective amount of a Compound of Formula (IA) and/or (IB), and methods to treat or prevent a condition, such cancer which overexpresses Her-kinases, comprising administering to an patient in need thereof a therapeutically effective amount of a Compound of Formula (IA) or (IB). The disclosure further relates to compounds of Formulae (IA) and (IB) in which Xis a leaving for introducing a radiolabeled atom, such asI orI and to methods of using such compounds in the preparation of radiolabeled compounds, particularly for use in imaging. 

Hsp90 inhibitors

The disclosure relates to Compounds of Formulae (IA) and (IB): and pharmaceutically acceptable salts thereof wherein Z, Z, Z, Xa, Xb, Xc, Xd, Y, X, and Xare as defined herein, compositions comprising an effective amount of a Compound of Formula (IA) and/or (IB), and methods to treat or prevent a condition, such cancer which overexpresses Her-kinases, comprising administering to an patient in need thereof a therapeutically effective amount of a Compound of Formula (IA) or (IB). The disclosure further relates to compounds of Formulae (IA) and IB) in which Xis a leaving for introducing a radiolabeled atom, such asI orI and to methods of using such compounds in the preparation of radiolabeled compounds, particularly for use in imaging.

The present application provides compounds useful in the inhibition of Hsp90, and hence in the treatment of disease.

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Princeton, NJ, United States of America

Weilin Sun