1095010-47-1Relevant articles and documents
INHIBITORS OF MYOCARDIN-RELATED TRANSCRIPTION FACTOR AND SERUM RESPONSE FACTOR (MRTF/SRF)-MEDIATED GENE TRANSCRIPTION AND METHODS FOR USE OF THE SAME
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Paragraph 00209, (2016/06/01)
Disclosed herein are inhibitors of gene transcription mediated by myocardin-related transcription factor and serum response factor, or both myocardin-related transcription factor and serum response factor ("MRTF/SRF"), and methods for their use in treating or preventing cancer and fibrosis. In particular, disclosed herein are compounds of Formula (I) and Formula (II), and pharmaceutically acceptable salts thereof: wherein the substituents are as described.
SERINE/THREONINE KINASE INHIBITORS
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, (2015/07/16)
Compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such diseases, or associated pathological conditions are disclosed.
SUBSTITUTED [1,2,4] TRIAZOLO [1,5-A] PYRIMIDIN-7-YL COMPOUNDS AS PDE2 INHIBITORS
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, (2015/11/10)
The invention provides a chemical entity of Formula (I): wherein R1, R2, X, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of
1,5-Substituted nipecotic amides: Selective PDE8 inhibitors displaying diastereomer-dependent microsomal stability
DeNinno, Michael P.,Wright, Stephen W.,Visser, Michael S.,Etienne, John B.,Moore, Dianna E.,Olson, Thanh V.,Rocke, Benjamin N.,Andrews, Melissa P.,Zarbo, Cynthia,Millham, Michele L.,Boscoe, Brian P.,Boyer, David D.,Doran, Shawn D.,Houseknecht, Karen L.
, p. 3095 - 3098 (2011/06/24)
The first highly potent and selective PDE8 inhibitors are disclosed. The initial tetrahydroisoquinoline hit was transformed into a nipecotic amide series in order to address a reactive metabolite issue. Reduction of lipophilicity to address metabolic liab