Memorial Sloan Kettering Cancer Center

Sloan-kettering Institute for Cancer Research

Steve Larson

Gabriela Chiosis

Huazhong He

Peter Smith-Jones

Joungnam Kim

Laura Llauger-Bufi

Ouathek Ouerfelli

Guangbin Yang

Sarah M Cheal

The present disclosure provides compositions and methods for the treatment of cancer. Specifically, the compositions of the present technology include novel clearing agents that may be used in pretargeted radioimmunotherapy.

N-acetylgalactosamino dendron-clearing agent for dota-pretargeted radioimmunotherapy

Hsp90 inhibitors having are provided having the formula: (I) with a 2',4&#x2032;,5&#x2032;-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4&#x2032; and 5&#x2032; positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO-alkyl, COO-alkyl, KH, OH, CN, SOX, NO, NO, C&#x2550;SRNSOX, C&#x2550;OR, where Xis F, NH2, alkyl or H, and Ris alkyl, NH, NH-alkyl or O-alkyl, Cto Calkyl or alkoxy; or wherein Xhas the formula &#x2014;O&#x2014;(CH)&#x2014;O&#x2014;, wherein n is an integer from 0 to 2, preferably 1 or 2, and one of the oxygens is bonded at the 5&#x2032;-position and the other at the 4&#x2032;-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands. 

Small-molecule HSP90 inhibitors

The present disclosure provides inhibitors of Hsp90 and methods of making and using the same. Such compounds are useful as radioimaging ligands and for the treatment of cancer and other conditions where cell growth or maintenance depend on Hsp90 activity.

Small-molecule Hsp90 inhibitors

Hsp90 inhibitors are provided having the formula: with a 2',4&#x2032;,5&#x2032;-substitution pattern on the right-side aryl moiety. Xrepresents two substituents, which may be the same or different, disposed in the 4&#x2032; and 5&#x2032; positions on the aryl group, wherein Xis selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SOalkyl, COO-alkyl, KH, OH, CN, SOX, NO, NO, C&#x2550;SRNSOX, C&#x2550;OR, where Xis F, NH2, alkyl or H, and Ris alkyl, NH, NH-alkyl or O-alkyl, Cto Calkyl or alkoxy; or wherein Xhas the formula &#x2014;O&#x2014;(CH)&#x2014;O&#x2014;, wherein n is an integer from 0 to 2, preferably 1 or 2, and one of the oxygen is bonded at the 5&#x2032;-position and the other at the 4&#x2032;-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands.

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New York, NY, United States of America

Steve Larson