Medivation Technologies, Inc.

Pharmacyclics, Inc.

Myoforte Therapeutics, Inc.

Smithkline Beecham Corporation

Axys Pharmaceuticals, Inc.

Isosterix, Inc.

Roopa Rai

William Dvorak Shrader

Sarvajit Chakravarty

Son Minh Pham

Brahmam Pujala

Aleksandr Kolesnikov

Wendy B Young

Kieron E Wesson

Bharat Uttam Shinde

Michael J Green

Anjan Kumar Nayak

Steven M Torkelson

Anil Kumar Agarwal

Sreekanth A Ramachandran

Daniel A Dickman

Dange Vijay Kumar

Colin O'Bryan

Robert Booth

Mark Bures

Naveen Chaklan

Ramniwas Jangir

Rambabu Guguloth

Christopher Don Roberts

Erik Joel Verner

Ronald Griffith

Sebastian Bernales

Mausumee Guha

Richard L Mackman

Jeffrey Lindquist

Bhawana Bhatt

Amantullah Ansari

Franz Ulrich Schmitz

Ali Dehghani Mohammad Abadi

Martin Robert Leivers

Darin A Allen

Jason M Hataye

Witold N Hruzewicz

Satyanarayana Kallem

Spencer R Jeffrey

Vikas Ramdas Bhagwat

Vijay Kumar Sharma

Irina Slobodov

Provided herein are compounds of Formula (I). Methods for the preparation of the compounds of Formula (I) and intermediates useful in the preparation of the compounds of Formula (I) are described herein. The compounds of Formula (I) may be useful as inhibitors of the MYST family of lysine acetyltransferases (KATs) for the treatment of and/or prophylaxis of hyperproliferative diseases, disorders or conditions such as cancer. In particular, the compounds of Formula (I) are useful for the inhibition of KAT6A and KAT6B which are enzymes frequently mutated, overexpressed, amplified and/or translocated in cancer altering their normal expression, activity and function. The use of the compounds of Formula (I) in the manufacture of pharmaceutical compositions or for treating cancers is further described, including for treating cancer in combination with other anti-cancer agents.

Inhibitors of the myst family of lysine acetyl transferases

Inhibitors of the MYST family of lysine acetyl transferases

Disclosed herein are compounds that can inhibit 15-hydroxyprostaglandin dehydrogenase. Such compounds may be administered to subjects that may benefit from modulation of prostaglandin levels.

PGDH inhibitors and methods of making and using

This disclosure provides compounds and compositions and methods of using those compounds and compositions to treat diseases and disorders associated with excessive transforming growth factor-beta (TGF&#x3b2;) activity. This disclosure also provides methods of using the compounds in combination with one or more cancer immunotherapies.

Compounds and methods of use

This disclosure provides compounds and methods of using those compounds to treat metabolic disorders and hyperproliferative disorders, including administration of the compounds in conjunction with hormone receptor antagonists.

Heterocyclic compounds and methods of use

Fused pyrimidine compounds as kinase inhibitors, such as multi-kinase inhibitors, are provided. Fused pyrimidine compounds as IGF-IR inhibitors are provided. Fused pyrimidine compounds that are inhibitors of Trk receptors (e.g., Trk A, Trk B and Trk C) are provided also. The compounds may be used in a method of treating cancer. Pharmaceutical compositions containing a fused pyrimidine compound and a pharmaceutically acceptable carrier are also provided, as are kits containing a fused pyrimidine compound or salt thereof and instructions for use, e.g., in a method of treating cancer.

Fused pyrimidine compounds and use thereof

The present invention provides fused pyrimidine compounds of the general Formula (I): or a salt thereof, wherein the variables are as defined in the specification. Fused pyrimidine compounds of the general Formula (I) are provided as kinase inhibitors, such as multi-kinase inhibitors. In one aspect, fused pyrimidine compounds of the general Formula (I) are provided as IGF-IR inhibitors. The compounds may be used in a method of treating cancer. Pharmaceutical compositions containing a fused pyrimidine compounds of the general Formula (I) and a pharmaceutically acceptable carrier are also provided, as are kits containing a fused pyrimidine compound of the general Formula (I) or salt thereof and instructions for use, e.g., in a method of treating cancer.

The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.

Factor VIIa inhibitor

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2-(2-hydroxybiphenyl-3-yl)-1H-Benzoimidazole-5-carboxamidine derivatives as factor VIIA inhibitors

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San Carlos, CA, United States of America

Roopa Rai