The United States of America, as Represented by the Secretary, Department of Health and Human Services

The Brigham and Women's Hospital, Inc.

Cincinnati Children's Hospital Medical Center

The Rockefeller University

Icahn School of Medicine at Mount Sinai

Jian-kang Jiang

Craig J Thomas

Matthew Brian Boxer

James Inglese

Douglas S Auld

Amanda P Skoumbourdis

Wenwei Huang

Wei Ping Zheng

Arthur Lee

Asaf Alimardanov

Paul B Yu

Khalida Shamim

Daniel T Starczynowski

Xiuli Huang

Garrett W Rhyasen

Gregory J Tawa

Philip Edward Sanderson

Junfeng Huang

Katelyn Melgar

Morgan MacKenzie Walker

Barry S Coller

Min Shen

John A Beutler

Marta Filizola

Joshua McCoy

Stuart F J LeGrice

Suhman Chung

Jennifer Wilson

The present invention provides small-molecule inhibitors of BMP signaling and compositions and methods for inhibiting BMP signaling. These compounds and compositions may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. These compounds and compositions may also be used to treat subjects with Sj&#xf6;gren's syndrome, or diffuse intrinsic pontine glioma (DIPG).

ALK2 inhibitors and methods for inhibiting BMP signaling

Some embodiments of the invention include inventive compounds (e.g., compounds of Formula (I)) and compositions (e.g., pharmaceutical compositions) which can be used for treating, for example, certain diseases. Some embodiments include methods of using the inventive compound (e.g., in compositions or in pharmaceutical compositions) for administering and treating (e.g., diseases such as head and neck squamous cell carcinoma (HNSCC), cancer, blood disorders, etc.). Additional embodiments provide synergistic combinations of a BCL2 inhibitor with an IRAK inhibiting compound, and methods of using same. 

Substituted Imidazo[1,2-a]-pyridines as IRAK 1/4 and FLT3 inhibitors

Some embodiments of the invention include inventive compounds (e.g., compounds of Formula (I)). Other embodiments include compositions (e.g., pharmaceutical compositions) comprising the inventive compound. Still other embodiments of the invention include compositions (e.g., pharmaceutical compositions) for treating, for example, certain diseases using the inventive compounds. Some embodiments include methods of using the inventive compound (e.g., in compositions or in pharmaceutical compositions) for administering and treating (e.g., diseases such as cancer or blood disorders). Further embodiments include methods for making the inventive compounds. Additional embodiments of the invention are also discussed herein. 

Substituted imidazo[1,2-A]pyridines as IRAK 1/4 and flt3 inhibitors

Disclosed are pyruvate kinase M2 activators, which are, bis sulfonamide piperazinyl compounds of Formula (I) and 2,4-disubstituted 4H-thieno[3,2-b]pyrrole-2-(substituted benzyl)pyridazin-3(2H)ones of Formula (II), wherein L and Rto Rare as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia, 

Activators of human pyruvate kinase

The present invention relates to compounds and compositions of Formula P useful for inhibiting and/or reducing platelet deposition, adhesion and/or aggregation. The definitions of variables A, B, R, R, R, R, R', R, R&#x2032;, R, R, R&#x2032;, R, and R&#x2032; are provided in the disclosure. The present invention further relates to methods for the treatment or prophylaxis of thrombotic disorders, including stroke, myocardial infarction, unstable angina, peripheral vascular disease, abrupt closure following angioplasty or stent placement and thrombosis as a result of vascular surgery.

7-(piperazin-1-yl)-5H-[1,3,4]thiadiazolo[3,2-A]pyrimidin-5-ones for the treatment of thrombotic disorders

Disclosed are pyruvate kinase M2 activators, which are, bis sulfonamide piperazinyl compounds of Formula (I) and 2,4-disubstituted 4H-thieno[3,2-b]pyrrole-2-(substituted benzyl)pyridazin-3(2H)ones of Formula (II), wherein L and Rto Rare as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia, Formulas (I); (II). 

Disclosed are compounds that inhibit RNase H activity of retroviruses, for example, a compound of formula (I) wherein R, R, and Rare as described herein, as well as pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment or prevention of infection by human immunodeficiency virus (HIV). 

Tropolone compounds for treating or preventing retroviral infection

Disclosed are pyruvate kinase M2 activators, which are bis sulfonamide piperazinyl and piperidinyl compounds of Formula (I), 2,4-disubstituted 4H-thieno[3,2-c]pyrrole-2-(substituted benzyl)pyridazin-3(2H)-ones of Formula (II) and 6-(3,4-dimethylphenylaminosulfonyl)-3,4-dihydro-1H-quinolin-2-one of formula (III), wherein L, R, R, Rto R, Rand Rare as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia. 

Activators of the human pyruvate kinase M2 receptor

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Columbia, MD, United States of America

Jian-kang Jiang