Tolero Pharmaceuticals, Inc.

University of Utah Research Foundation

University of Arizona

Sumitomo Pharma Oncology, Inc.

Sumitomo Dainippon Pharma Oncology, Inc.

Montigen Pharmaceuticals, Inc.

Mannkind Corporation

Supergen, Inc

Astex Pharmaceuticals, Inc.

Astex Pharmaceutials, Inc.

Steven L Warner

David J Bearss

Hariprasad Vankayalapati

Adam Siddiqui-Jain

Sunil Sharma

Venkataswamy Sorna

Clifford J Whatcott

Laurence H Hurley

Daruka Mahadevan

Sridevi Bashyam

Alexis Mollard

Gary A Flynn

Bret Stephens

Jason Marc Foulks

Paul Flynn

Wontak Kim

Peter W Peterson

Lars Mouritsen

Mary Faris

Qingping Zeng

James Welsh

Jeyaprakashnarayanan Seenisamy

Yuka Arikawa

Hiroki Umehara

Yuji Fujiwara

Akihito Nonoyama

Akihito Kiguchiya

Siva Reddy Basireddy

Srinivas Padakanti

Nozomi Tomimatsu

Stephen Patrick Anthony

Ken Fujimura

Bettina Franz

Naresh Kumar

Provided herein are compounds (e.g., compounds of Formulae (I), (II), (III) and (IV), or of Table 1 or Table 4), and pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and kits comprising the same. The compounds provided herein are activin receptor-like kinase (e.g., ALK-5) inhibitors and are, therefore, useful, for example, for treating and/or preventing diseases (e.g., proliferative diseases, such as cancer) in a subject, inhibiting tumor growth in a subject, or inhibiting the activity of an activin receptor-like kinase (e.g., ALK-5) in vitro or in vivo. Also provided herein are methods and synthetic intermediates useful in the preparation of compounds described herein.

ALK-5 inhibitors and uses thereof

A compound of Structure (I): or a pharmaceutically acceptable salt thereof, alone or in combination with a second therapeutic agent, as well as methods of treating a PKM2-mediated disease or disorder using the same are provided herein.

Compositions comprising PKM2 modulators and methods of treatment using the same

Provided herein is a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein values for the variables (e.g., X, X, R, R, R, R, R, R, R, m, n) are as described herein. Compounds of Formula I, pharmaceutically acceptable salts thereof, pharmaceutical compositions of either of the foregoing, and combinations of any of the foregoing can be used to treat tyrosine kinase non-receptor 1 (TNK1)-mediated diseases, disorders and conditions.

Tyrosine kinase non-receptor 1 (TNK1) inhibitors and uses thereof

Methods for treating BCL-2 inhibitor-resistant cancer in subjects using an MCL-1 inhibitor as well as compositions associated with the same are disclosed.

Treatment regimen for cancers that are insensitive to BCL-2 inhibitors using the MCL-1 inhibitor alvocidib

Provided is a composition comprising a polyglycolized glyceride and a compound having the following structure (I): or a pharmaceutically acceptable salt thereof. Also provided are crystalline forms of the compound of structure (I), or a pharmaceutically acceptable salt thereof. Methods of making the same, and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated diseases, disorders or conditions are also disclosed.

Formulations comprising heterocyclic protein kinase inhibitors

Tartrate salts of the compound of structure (I), crystalline forms thereof, and therapeutic applications thereof for treating solid tumors (e.g., advanced solid tumor) or hematopoietic cancers. Also provided herein are methods for synthesizing the tartrate salts and the crystalline forms thereof.

AXL kinase inhibitors and use of the same

Methods for treating a disease in a subject in need thereof by administering an ACVR1 inhibitor having the following formula (I) are disclosed: including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R, R, R, and Rare as defined herein. Subjects that may benefit from treatment may have mutations in their ACVR1 gene. Various diseases may be treated using the described methods, including cancers (e.g., diffuse intrinsic pontine glioma (DIPG)) and genetic disorders (e.g., fibrodysplasia ossificans progressiva (FOP)).

Methods for treating diseases associated with abnormal ACVR1 expression and ACVR1 inhibitors for use in the same

Combination therapies for treatment of cancer are provided. The disclosed methods comprise administration of a cyclin-dependent kinase inhibitor and a DNA methyltransferase inhibitor to a mammal in need thereof.

Combination therapies for treatment of cancer

Compounds having activity as inhibitors of ALK2 kinase and/or JAK2 kinase are disclosed. The compounds have the following structure (I): including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R, R, R, R, R, R, R, R, X, z and A are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

JAK1 and ALK2 inhibitors and methods for their use

The present disclosure provides diagnostic methods useful for predicting a patient's response to alvocidib and guiding a physician decision to administer alvocidib to the patient.

Predicting response to alvocidib by mitochondrial profiling

The present disclosure is generally directed to profiling peptides, compositions, and kits, as well as methods of use thereof. The profiling peptides comprise an Mcl-1 binding domain, and optionally a cellular uptake moiety. The methods of using such profiling peptides include predicting sensitivity of a cancer, selecting a treatment, treating a cancer, producing a sensitivity profile, and the like.

Profiling peptides and methods for sensitivity profiling

Growing community of inventors

Sandy, UT, United States of America

Steven L Warner