848639-97-4Relevant academic research and scientific papers
Thrombopoietin Receptor Agonists
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Page/Page column 15, (2010/11/30)
A compound of the formula (I) useful as promoters of thrombopoiesis and megakaryocytopoiesis, wherein A, B, D, E, W, X, Y, Z, R1 and R2 are defined as above.
Pyrimidine benzamide-based thrombopoietin receptor agonists
Reiter, Lawrence A.,Subramanyam, Chakrapani,Mangual, Emilio J.,Jones, Christopher S.,Smeets, Marc I.,Brissette, William H.,McCurdy, Sandra P.,Lira, Paul D.,Linde, Robert G.,Li, Qifang,Zhang, Fangning,Antipas, Amy S.,Blumberg, Laura C.,Doty, Jonathan L.,Driscoll, James P.,Munchhof, Michael J.,Ripp, Sharon L.,Shavnya, Andrei,Shepard, Richard M.,Sperger, Diana,Thomasco, Lisa M.,Trevena, Kristen A.,Wolf-Gouveia, Lilli A.,Zhang, Liling
, p. 5447 - 5454 (2008/03/11)
A series of pyrimidine benzamide-based thrombopoietin receptor agonists is described. The lead molecule contains a 2-amino-5-unsubstituted thiazole, a group that has been associated with idiosyncratic toxicity. The potential for metabolic oxidation at C-5 of the thiazole, the likely source of toxic metabolites, was removed by substitution at C-5 or by replacing the thiazole with a thiadiazole. Potency in the series was improved by modifying the substituents on the pyrimidine and/or on the thiazole or thiadiazole pendant aryl ring. In vivo examination revealed that compounds from the series are not highly bioavailable. This is attributed to low solubility and poor permeability.
PHARMACEUTICALLY ACTIVE 4,6-DISUBSTITUTED AMINOPYRIMIDINE DERIVATIVES AS MODULATORS OF PROTEIN KINASES
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, (2010/02/11)
The present invention relates to 4,6-disubstituted aminopyrimidine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, prion diseases, immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke, and pharmaceutical compositions containing at least one of said 4,6-di substituted aminopyrimidine derivatives and/or pharmaceutically acceptable salts thereof. Furhtermore, the present invention relates to the use of said 4,6-disubstituted aminopyrimidine derivatives as inhibitors for a protein kinase and a medium comprising at least one of said 4,6-disubstituted aminopyrimidine derivatives in an immobilized form and the use of said medium for enriching, purifying and/or depleting nucleotide binding proteins which bind to the immobilized 4,6-disubstituted aminopyrimidine derivatives.
