National Institutes of Health, a Component of the US Dept. of Health & Human Services

Loyola University of Chicago

The Brigham and Women's Hospital, Inc.

University of Houston System

Paresma R Patel

Wei Ping Zheng

Philip Edward Sanderson

Xiuli Huang

Wenwei Huang

Gregory J Tawa

Hao Li

Kim C Williamson

Wei Sun

Hangmao Sun

Xiao Lu

Myunghoon Kim

Meghan J Orr

Gregory D Cuny

Kirk R Gustafson

James Brislin McMahon

Arthur Lee

William Douglas Figg

Martin John Schnermann

Paul B Yu

John C McKew

Agustin H Mohedas

Susanna T S Chan

Disclosed are compounds of formula (I) and formula (II): wherein R, R, A, and B are as defined herein. Also disclosed is a method of blocking transmission of aparasite and a method of treating or preventing malaria comprising administering to an animal an effective amount of a first compound of formula (I) or (II) either alone or in combination with a second compound selected from elesclomol, NSC174938, NVP-AUY922, Maduramicin, Narasin, Alvespimycin, Omacetaxine, Thiram, Zinc pyrithione, Phanquinone, Bortezomib, Salinomycin sodium, Monensin sodium, Dipyrithione, Dicyclopentamethylene-thiuram disulfide, YM155, Withaferin A, Adriamycin, Romidepsin, AZD-1152-HQPA, CAY10581, Plicamycin, CUDC-101, Auranofin, Trametinib, GSK-458, Afatinib, and Panobinostat.

Compounds and method for blocking transmission of malarial parasite

Disclosed are compounds of formula (I) and formula (II): (I) (II) wherein R, R, A, and B are as defined herein. Also disclosed is a method of blocking transmission of aparasite and a method of treating or preventing malaria comprising administering to an animal an effective amount of a first compound of formula (I) or (II) either alone or in combination with a second compound selected from elesclomol, NSC174938, NVP-AUY922, Maduramicin, Narasin, Alvespimycin, Omacetaxine, Thiram, Zinc pyrithione, Phanquinone, Bortezomib, Salinomycin sodium, Monensin sodium, Dipyrithione, Dicyclopentamethylene-thiuram disulfide, YM155, Withaferin A, Adriamycin, Romidepsin, AZD-1152-HQPA, CAY10581, Plicamycin, CUDC-101, Auranofin, Trametinib, GSK-458, Afatinib, and Panobinostat. 

The present invention provides bicyclic heteroaryl inhibitors of BMP signaling and compositions and methods for inhibiting BMP signaling. Exemplary compounds include those of Formula I:  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 reduce circulating levels of ApoB-100 or LDL and treat or prevent acquired or congenital hypercholesterolemia or hyperlipoproteinemia; diseases, disorders, or syndromes associated with defects in lipid absorption or metabolism; or diseases, disorders, or syndromes caused by hyperlipidemia.

Compositions and methods for inhibiting BMP

Embodiments of small molecule inhibitors of hypoxia inducible factor 1 (HIF-1) and pharmaceutical compositions thereof are disclosed. The disclosed compounds suppress HIF-1 activity by inhibiting the interaction between the HIF-1 &#x3b1; subunit and transcriptional co-activator protein p300. Embodiments of methods for making and using the small molecule inhibitors are also disclosed.

Hypoxia-inducible factor 1 (HIF-1) inhibitors

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Rockville, MD, United States of America

Paresma R Patel