Araxes Pharma LLC

Intellikine LLC

Infinity Pharmaceuticals, Inc.

Kura Oncology, Inc.

University of Michigan

Irm LLC

Kumquat Biosciences Inc.

Novartis Ag

Janssen Biotech, Inc.

University of California

The Scripps Research Institute

Millennium Pharmaceuticals Limited

Sigma-aldrich Co. LLC

Itellikine LLC

Irm LLC (a Delaware Limited Liability Corporation)

Pingda Ren

Yi Liu

Liansheng Li

Jun Feng

Katrina Chan

Tao Wu

Troy Edward Wilson

Yuan Liu

Yun Long

Alfredo C Castro

Catherine Anne Evans

Christian Rommel

Yi Wang

Daniel A Snyder

Jolanta Grembecka

Tomasz Cierpicki

Dmitry Borkin

Jonathan Pollock

Martin R Tremblay

Tao Liu

Andre Lescarbeau

Xia Wang

Nathanael Schiander Gray

Somarajannair Janardanannair

Taebo Sim

Michael Martin

Guobao Zhang

Paul Isbester

Baogen Wu

Szymon Klossowski

Benjamin S Lane

Jason Kropp

Simon F Campbell

Zhiyong Chen

Shuli You

Qiang Ding

Pamela Ann Albaugh

Xiuwen Zhu

Yongping Xie

Xiaoming Li

Katayoun Jessen

Xin Guo

Zhimin Zhu

Yun He

Qiong Zhang

Duxin Sun

Tetsuo Uno

Xing Wang

Xiaohu Deng

Bing Li

Zuosheng Liu

Songchun Jiang

Barun Okram

Matthew Patricelli

Hongzhi Miao

Hyun Soo Lee

Lintong Li

Siling Zhao

Chengzhi Zhang

Paul A Renhowe

Kevan M Shokat

Neelakandha S Mani

Xiaolin Li

Daniel J Poon

Valentina Molteni

Martin Sendzik

Xiaodong Wang

Shifeng Pan

Shenlin Huang

Jon Christopher Loren

Andrew Gaheem Hsieh

Juliet Nabakka

Advait Suresh Nagle

Brett D Allison

Xiaodong Liu

Donatella Chianelli

Ha-Soon Choi

Gregory B Chopiuk

Jimmy T Liang

Xuefeng Zhu

Victor Ivanovich Nikulin

Zachary S Sales

Christopher Cow

Greg Chopiuk

Beth Apsel

Wanping Mai

Dan Xu

Davide Ruggero

David Fruman

Morris Feldman

David Pearce

Matthew Janes

Christopher Peter Worrall

Susanna Del Rio Gancedo

Nathanel Gray

Francisco Adrian

Xiangzhu Wang

Zhu Bai

Wanting Xiong

Yahu Arthur Liu

Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.

Covalent inhibitors of KRAS G12C

The present disclosure provides compounds and pharmaceutically acceptable salt thereof, and methods of using the same. The compounds and methods have a range of utilities as therapeutics, diagnostics, and research tools. In particular, the subject compositions and methods are useful for reducing signaling output of oncogenic proteins.

Heterocyclic compounds and uses thereof

Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have one of the following structures (I), (II) or (III): or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R, R, R, R, R, R, R, R, R, R, R, A, B, G, G, L, L, m, m, n, x, y, X and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

Substituted quinazoline compounds and methods of use thereof

Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds, or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, have the following structure: wherein A, L, L, Q, R, R, R, R, R, R, R, R, Y, and Z are as exemplified herein. Pharmaceutical compositions comprising such compounds, methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, and methods associated with preparation of such compounds are also provided.

Substituted piperazines as inhibitors of KRAS G12C

The present disclosure provides compounds and pharmaceutically acceptable salts thereof, and methods of using the same. The compounds and methods have a range of utilities as therapeutics, diagnostics, and research tools. In particular, the subject compositions and methods are useful for reducing signaling output of oncogenic proteins.

Macrocyclic heterocycles and uses thereof

Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, stereoisomer, isotopic form or prodrug thereof, wherein R, L, L, L, A, A, A, A, G, G, E, W, X, Y, Z, m, and n are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

Heterocyclic spiro compounds and methods of use thereof for the treatment of cancer

The present disclosure provides compounds and pharmaceutically acceptable salts thereof, and methods of using the same. The compounds and methods have a range of utilities as therapeutics, diagnostics, and research tools. In particular, the subject compositions and methods are useful for reducing signaling output of certain oncogenic proteins.

The present invention relates to macrocyclic compounds of any one of Formula (I), or a pharmaceutically acceptable form thereof, pharmaceutical compositions comprising the same, methods of preparing the same, and methods of treating cancer dependent on a farnesylated protein, using the same.

Macrocyclic compounds and compositions, and methods of preparing and using the same

The present disclosure provides methods for treating hematological malignancies and Ewings sarcoma using menin inhibitors. Compositions for use in these methods are also provided.

Methods for treating hematological malignancies and Ewing's sarcoma

Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R, R, R, R, R, R, G, G, L, L, m, m, A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

Substituted quinazolines as inhibitors of KRAS G12C

The present disclosure provides compounds and methods for inhibiting the interaction of menin with its upstream or downstream signaling molecules including but not limited to MLL1, MLL2 and MLL-fusion oncoproteins. Compounds of the disclosure may be used in methods for the treatment of a wide variety of cancers and other diseases associated with one or more of MLL1, MLL2, MLL fusion proteins, and menin.

Thienopyrimidine and thienopyridine compounds and methods of use thereof

The present disclosure provides methods of inhibiting the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins with compositions of Formula (II-A). The methods are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin. Compositions of Formula (II-A) for use in these methods are also provided. 

Substituted inhibitors of menin-MLL and methods of use

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Pingda Ren