PHTHALAZINONE AND RELATED ANALOGS AS SIRTUIN MODULATORS
申请人:Vu Chi B.
公开号:US20130190309A1
公开(公告)日:2013-07-25
Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
PYRIMIDINE-2-AMINE COMPOUNDS AND THEIR USE AS INHIBITORS OF JAK KINASES
申请人:Rigel Pharmaceuticals, Inc.
公开号:US20140213585A1
公开(公告)日:2014-07-31
This invention is directed to methods of treating diseases or conditions associated with JAK2 activity in a mammal comprising the administration of a compound of formula (I):
where
n, m, Y, R
1
, R
2
, R
3
, R
4
and R
5
are disclosed herein, or a pharmaceutically acceptable salt.
The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTC”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
6,7-DIHYDROPYRAZOLO[1,5-a]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
申请人:JANSSEN PHARMACEUTICA NV
公开号:US20160115169A1
公开(公告)日:2016-04-28
The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.
HETEROCYCLIC COMPOUNDS AND USE THEREOF AS ERK INHIBITORS
申请人:Sun Robert
公开号:US20110038876A1
公开(公告)日:2011-02-17
Disclosed are the ERK inhibitors of formula 1.0: [Formula (1.0)] and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.