A series of aminopyrazines as inhibitors of Syk kinase activity and showing inhibition of LAD2 cells degranulation is described. Optimization of the carboxamide motif with aminomethylpiperidines provided high potency inhibiting Syk but low cellular activity. Amides of cis and trans adamantanol showed good inhibitory activity against Syk as well as remarkable activity in LAD2 cells degranulation assay. (C) 2012 Elsevier Ltd. All rights reserved.
A process for preparing a compound represented by the formula (I):
comprising reacting a compound represented by the formula (II) or salt thereof:
with a compound represented by the formula (III):
in the presence of a condensation reagent,
wherein R
1
represents 1) optionally substituted azetidin-1-yl, 2) optionally substituted pyrrolidin-1-yl, 3) optionally substituted piperidin-1-yl, etc.; R
2
, R
3
, R
4
and R
5
may be the same or different and each represents hydrogen or fluorine; and R
6
represents hydrogen or fluorine.
This invention relates to compounds that are agonists of the muscarinic receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula (1a) or a salt thereof, wherein p, q, r, s, Q, R3 and R4 are as defined herein.
[EN] 6-(5-HYDROXY-1H-PYRAZOL-1-YL)NICOTINAMIDE DERIVATIVES AND THEIR USE AS PHD INHIBITORS<br/>[FR] INHIBITEURS 6-(5-HYDROXY-1H-PYRAZOL-1-YL)NICOTINAMIDE DE PHD
申请人:TAKEDA PHARMACEUTICAL
公开号:WO2014160810A1
公开(公告)日:2014-10-02
The present invention provides compounds of formula (I) which are useful as inhibitors of PHD, pharmaceutical compositions thereof, methods for treatment of conditions associated with HIF, processes for making the compounds and intermediates thereof.
TYROSINE AMIDE DERIVATIVES AS RHO- KINASE INHIBITORS
申请人:CHIESI FARMACEUTICI S.P.A.
公开号:US20180215758A1
公开(公告)日:2018-08-02
Bicyclic dihydropyrimidine-carboxamide compounds of formula I described herein inhibit Rho Kinase and may be used for the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
The present invention relates to certain novel 6-amino-7-azaquinazoline derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. One important use is in the treatment of pain.