Araxes Pharma LLC

Capella Therapeutics, Inc.

Novartis Ag

Ligand Pharmaceuticals, Inc.

Yun Long

Pingda Ren

Liansheng Li

Yi Liu

Jun Feng

Yuan Liu

Tao Wu

Lin Zhi

Esther Martinborough

Neelakandha S Mani

Xiaohu Deng

Brett D Allison

Pierre-Yves Michellys

Robert Epple

Badry Bursulaya

Songchun Jiang

Thomas H Marsilje, Iii

Yixing Shen

Bei Chen

Jimmy T Liang

Wenshuo Lu

Zachary S Sales

Gerald Lelais

Thomas Lot Stevens Lau

Matthew McNeill

Min Wu

Matthew H McNeill

Iii Thomas H Marsilje

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

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

Provided herein are benzimidazole derivatives, for example, of Formula I, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease.

Benzimidazole derivatives, and pharmaceutical compositions and methods of use thereof

Provided herein are benzimidazole derivatives, for example, or Formula (I), and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease.

Benzimidazole derivatives as ERBB tyrosine kinase inhibitors for the treatment of cancer

Provided herein are methods for treating, preventing, or ameliorating one or more symptoms of a condition, disorder, or disease mediated by a lipid kinase or a protein kinase with benzimidazoles, for example, of Formula I or II, and pharmaceutical compositions thereof. Also provided herein are benzimidazoles, and pharmaceutical compositions thereof; and methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease. 

Benzimidazoles for use in the treatment of cancer and inflammatory diseases

Provided herein are benzimidazole derivatives, for example, of Formula (I), and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease. 

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 or prodrug thereof, wherein R, R, R, R, R, R, R, R, R, R, R, A, G, G, L, L, m, m, n, X and E are as defined herein, and wherein at least one of R, R, Ror Ris not H. 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.

2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use 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, tautomer, stereoisomer or prodrug thereof, wherein A, B R, R, R, R, R, R, R, G, G, m, m, L, Land 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. 

Inhibitors of KRAS G12C mutant proteins

Substituted cinnolines as inhibitors of KRAS G12C

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, stereoisomer or prodrug thereof, wherein R, R, R, R, R, G, G, G, G, G, m, m, m, m, L, Land 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. 

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, stereoisomer or prodrug thereof, wherein R, R, R, R, R, G, G, G, G, m, m, m, m, L, Land 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. 

Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): (I) or a pharmaceutically acceptable salt, tautomer, stereoisomer or prodrug thereof wherein Z, Y R, R, R, R, G, G, G, G, L, m, m, m, m, n 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. 

Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): (I) or a pharmaceutically acceptable salt, tautomer, stereoisomer or prodrug thereof, wherein A, R, R, R, R, G, G, G, G, m, m, m, m, L, Land 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. 

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San Diego, CA, United States of America

Yun Long