Discovery of pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors
摘要:
We have made a novel series of pyrazolo[1,5-a]pyridines as PI3 kinase inhibitors, and demonstrated their selectivity for the p110 alpha isoform over the other Class Ia PI3 kinases. We investigated the SAR around the pyrazolo[1,5-a] pyridine ring system, and found compound 5x to be a particularly potent example (p110 alpha IC50 0.9 nM). This compound inhibits cell proliferation and phosphorylation of Akt/PKB, a downstream marker of PI3 kinase activity, and showed in vivo activity in an HCT-116 human xenograft model. (C) 2011 Elsevier Ltd. All rights reserved.
[EN] INHIBITORS OF CYSTEINE PROTEASES AND METHODS OF USE THEREOF [FR] INHIBITEURS DE CYSTÉINE PROTÉASES ET LEURS MÉTHODES D'UTILISATION
摘要:
The disclosure provides compounds with nitrile warheads and their use in treating medical diseases or disorders, such as viral infections. Pharmaceutical compositions and methods of making various compounds with nitrile warheads are provided. The compounds are contemplated to inhibit proteases, such as the 3C, CL- or 3CL-like protease.
[EN] PYRAZOLO[1,5-A]PYRIDINES AND THEIR USE IN CANCER THERAPY<br/>[FR] PYRAZOLO[1,5-A]PYRIDINES ET LEUR UTILISATION EN CANCÉROTHÉRAPIE
申请人:AUCKLAND UNISERVICES LTD
公开号:WO2009008748A1
公开(公告)日:2009-01-15
Pyrazolo[1,5-a]pyridines are described, including methods for their preparation, and their use as agents or drugs for cancer therapy, both alone or in combination with radiation and/or other anticancer drugs.
PYRAZOLO[1,5-a]PYRIDINES AND THEIR USE IN CANCER THERAPY
申请人:Kendall Jackie Diane
公开号:US20100226881A1
公开(公告)日:2010-09-09
Pyrazolo[1,5-a]pyridines are described, including methods for their preparation, and their use as agents or drugs for cancer therapy, both alone or in combination with radiation and/or other anticancer drugs.