Pyrrolopyrazines as Selective Spleen Tyrosine Kinase Inhibitors
摘要:
We describe the discovery of several pyrrolopyrazines as potent and selective Syk inhibitors and the efforts that eventually led to the desired improvements in physicochemical properties and human whole blood potencies. Ultimately, our mouse model revealed unexpected toxicity that precluded us from further advancing this series.
[EN] SUBSTITUTED DIAMINOCARBOXAMIDE AND DIAMINOCARBONITRILE PYRIMIDINES, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH<br/>[FR] DIAMINOCARBOXAMIDEPYRIMIDINES ET DIAMINOCARBONITRILEPYRIMIDINES SUBSTITUÉES, COMPOSITIONS DE CELLES-CI ET PROCÉDÉS DE TRAITEMENT À L'AIDE DE CELLES-CI
申请人:SIGNAL PHARM LLC
公开号:WO2012145569A1
公开(公告)日:2012-10-26
Provided herein are Diaminopyrimidine Compounds having the following structures: wherein R1, R2, R3, and R4 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidine Compound, and methods for treating or preventing liver fibrotic disorders or a condition treatable or preventable by inhibition of a JNK pathway.
The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I,
wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.