Synta Pharmaceuticals Corporation

Madrigal Pharmaceuticals, Inc.

Teresa Kowalczyk-Przewloka

Lijun Sun

Weiwen Ying

Dinesh U Chimmanamada

Shijie Zhang

Zachary Demko

Keizo Koya

David James

Hao Li

Howard P Ng

Kevin Paul Foley

Zhenjian Du

Junghyun Chae

Dan Zhou

Shuzhen Qin

Shoujun Chen

Jun Jiang

Stefan M Schweizer

Genliang Lu

Zhi-Qiang Xia

Christopher Borella

Joseph A Burlison

Chi-Wan Lee

Junyi Zhang

Minghu Song

James Loch

Dharma Vutukuri

Sami Osman

The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.

Targeted therapeutics

The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.

Triazole compounds that modulate Hsp90 activity

Triazole compounds that modualte HSP90 activity

Triazole compounds that modulate HSP90 activity

Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.

Compounds for treating proliferative disorders

The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to the use of a substituted triazole compound of the invention, or a composition comprising such a compound in the preparation of a medicament for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof.

The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included. 

Sulfonylhydrazide compounds for treating proliferative disorders

Disclosed are compounds of Formula (I) and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier. 

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Tewksbury, MA, United States of America

Teresa Kowalczyk-Przewloka