A general and facile one-pot amination procedure for the synthesis of 2-aminopyridines from the corresponding pyridine-N-oxides is presented as a mild alternative to S(N)Ar chemistry. A variety of amines and heterocyclic-N-oxides participate effectively in this transformation which uses the phosphonium salt, PyBroP, as a means of substrate activation.
The present invention provides compounds and pharmaceutical compositions that are selective antagonists of A
2B
adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.
The present invention provides compounds and pharmaceutical compositions that are selective antagonists of A
2B
adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.
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.
Compounds of general formula (I):
wherein R
1
, R
11
, Y, R
2
, n and A are as defined herein are useful as inhibitors or metallo-β-lactamase (MBL) enzymes and can be used for reducing or removing antibiotic resistance in bacteria.