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Patent
MannKind Corporation and Tolero Pharmaceuticals, Inc. | Date: 2016-09-26

Kinase with inhibitory activity against kinases disposed in multiple signaling pathways and their therapeutic uses.


Bearss D.J.,Tolero Pharmaceuticals, Inc.
Science Translational Medicine | Year: 2016

A nanoparticle formulation of an Aurora B inhibitor increases antitumor efficacy and reduces toxicity, which may be a precedent for the use of this technology with other small molecules (Ashton et al., this issue).


Patent
MannKind Corporation and Tolero Pharmaceuticals, Inc. | Date: 2013-09-25

Kinase with inhibitory activity against kinases disposed in multiple signaling pathways and their therapeutic uses.


Patent
Tolero Pharmaceuticals, Inc. | Date: 2013-10-16

Compounds having activity as PKM2 activators are disclosed. The compounds have the following structure (I): including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.


Patent
Tolero Pharmaceuticals, Inc. | Date: 2016-07-11

The present invention provides protein kinase having one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R_(1), R_(2 )and X are as defined herein. Compositions and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated conditions are also disclosed.


Grant
Agency: Department of Health and Human Services | Branch: | Program: SBIR | Phase: Phase I | Award Amount: 200.00K | Year: 2012

TP-0413 is a novel small molecule inhibitor of the BMP pathway that has significant potential to be developed to treat anemia of cancer. Anemia of cancer is cytokine driven and results in the up-regulation of a liver hormone called hepcidin through the function of BMP receptors. Increased hepcidin levels result in the storage of iron in cellular compartments resulting in low serum iron and anemia. Anemia of cancer is a significant health issue in a majority of cancer patients and is currently only treatableby blood transfusion. As an inhibitor of BMP signaling, TP-0413 has shown promise in cell-based and animal models. TP-0413 inhibits cytokine signaling and raises serum iron and red blood cells in mouse models of anemia. Ideally, TP-0413 will be developedas an oral agent and to this end, the studies described in this proposal aim at identifying and optimizing a pharmaceutical salt form of the compound that is orally available with enhanced efficacy. Furthermore, five-day repeat dose toxicity studies will be performed in rats in preparation for choosing a dose and schedule for GLP toxicity studies. The overarching goal of this work is to develop an optimized oral agent for the treatment of anemia in cancer.


Patent
Tolero Pharmaceuticals, Inc. | Date: 2014-03-13

Compounds having activity as inhibitors of ALK2 kinase and/or JAK2 kinase are disclosed. The compounds have the following structure (I): [FORMULA SHOULD BE INSERTED HERE] including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R^(1), R^(2), R^(3), R^(4), R^(5), R^(6), R^(7), R^(8), 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.


Patent
Tolero Pharmaceuticals, Inc. | Date: 2016-04-20

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


Patent
Tolero Pharmaceuticals, Inc. | Date: 2016-05-18

Compounds having the following structure (I): or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein one of R^(1), R^(2 )or R^(3 )is P(O)(OH)_(2), and the other two of R^(1), R^(2 )and R^(3 )are each H, are provided. Pharmaceutical compositions comprising the compounds, and methods for use of the compounds for treating diseases associated with overexpression of a cyclin-dependent kinase (CDK) are also provided.


Patent
Tolero Pharmaceuticals, Inc. | Date: 2016-06-15

Compounds having activity as PKM2 activators are disclosed. The compounds have the following structure (I): including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R^(1), R^(2), R^(3), R^(4), R^(5 )and R^(6 )are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

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