[EN] ARYLPYRAZOLES AND ARYLISOXAZOLES AND THEIR USE AS PKD MODULATORS<br/>[FR] ARYLPYRAZOLES ET ARYLISOXAZOLES ET LEUR UTILISATION EN TANT QUE MODULATEURS DE LA PROTÉINE KINASE C (PKD)
申请人:NOVARTIS AG
公开号:WO2011009484A1
公开(公告)日:2011-01-27
The present invention provides novel organic compounds of formula (I) or (Ia): which may be inhibitors of a selective subset of kinases belonging to the AGC or calmodulin kinase family, such as for example PKD-1/2/3, inhibitors of histone deacetylase (HDAC) phosphorylation, or inhibitors of other kinases. The selectivity of which would depend on the structural variation thereof, and for treatment of a disorder or disease mediated by those selected AGC or calmodulin family kinases. These organic compounds can be used to treat various PKD associated states such as heart failure, colorectal cancer, regulation of cell growth, autoimmune disorders, or hyperproliferative skin disorders.
GLUCOKINASE ACTIVATORS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS AN ACTIVE INGREDIENT
申请人:Kim Soon Ha
公开号:US20100267708A1
公开(公告)日:2010-10-21
The present invention relates to new compounds of formula (1) exhibiting excellent activity for glucokinase, and pharmaceutical compositions comprising the same as an active ingredient.
The invention is directed to aminopyrimidine compounds of Formula I:
where R
3
, B, Z, Q, p, q and R
1
are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of FLT3 and/or c-kit and/or TrkB, the use of such compounds to reduce or inhibit kinase activity of FLT3 and/or c-kit and/or TrkB in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to FLT3 and/or c-kit and/or TrkB. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.
The invention relates to compounds of the formula (I), their use as kinase inhibitors, new pharmaceutical formulations comprising said compounds, said compounds for use in the diagnostic or therapeutic treatment of warm-blooded animals, especially humans, their use in the treatment of diseases or for the manufacture of pharmaceutical formulations useful in the treatment of diseases that respond to modulation of kinase activity, methods of treatment comprising administration of said compounds to a warm-blooded animal, especially a human, and processes for the manufacture of said compounds.
[EN] EphA4 INHIBITORS AS NEUROPROTECTIVE AGENTS<br/>[FR] INHIBITEURS D'EPHA4 EN TANT QU'AGENTS NEUROPROTECTEURS
申请人:UNIV HONG KONG SCIENCE & TECHN
公开号:WO2015007222A1
公开(公告)日:2015-01-22
Provided is the discovery of the role of EphA4 signaling in neurodegenerative disorders involving β-amyloid induced neurotoxicity such as Alzheimer's Disease. New therapeutic methods, therapeutic agents, and kits for treating diseases caused or exacerbated by overactivated EphA4 signaling are provided. Also provided are methods for identifying additional compounds as therapeutic agents useful for treating conditions involving overly active EphA4 signaling.