Synta Pharmaceuticals Corporation

Madrigal Pharmaceuticals, Inc.

Weiwen Ying

Dinesh U Chimmanamada

Shijie Zhang

Lijun Sun

Kevin Paul Foley

Zhenjian Du

Teresa Przewloka

David James

Junghyun Chae

Keizo Koya

Hao Li

Howard P Ng

Mitsunori Ono

Elena Kostik

Dan Zhou

Shuzhen Qin

Zachary Demko

Shoujun Chen

Joseph A Burlison

Minghu Song

Teresa Kowalczyk-Przewloka

Chi-Wan Lee

Jun Jiang

Stefan M Schweizer

James G Barsoum

Yaming Wu

Christopher Borella

Takayo Inoue

Mei Zhang

Yumiko Wada

Kevin M Foley

Yuniko Wada

Genliang Lu

Noriaki Tatsuta

Junyi Zhang

David Proia

Neera Jain

Teresa Kowalczyk-Prezewloka

Teresa Kowalcyzk-Przewloka

K Koya

Amit Kale

Sami Osman

Dharma Vutukuri

James Loch

Stefan Michael Schweizer

Shije Zhang

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.

Combination therapies comprising targeted therapeutics

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 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 pharmaceutical composition comprising such a compound.

Triazole compounds that modulate HSP90 activity

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

Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. Variable Ris an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R. Substituent Ris defined herein.

Imidazole compounds that modulate HSP90 activity

The present invention relates to substituted tricyclic triazole compounds and compositions comprising substituted tricyclic 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 compound of the invention, or a composition comprising such a compound.

Tricyclic triazole compounds that modulate HSP90 activity

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

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Lexington, MA, United States of America

Weiwen Ying