Novel high affinity quinoline-based kinase ligands
申请人:Deng Yongqi
公开号:US20080045568A1
公开(公告)日:2008-02-21
Quinoline-based inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.
[EN] TETRAZOLE CONTAINING COMPOUNDS<br/>[FR] COMPOSÉS CONTENANT DU TÉTRAZOLE
申请人:BAYER PHARMA AG
公开号:WO2018114783A1
公开(公告)日:2018-06-28
The present invention relates to tetrazole containing compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease syndrome, condition, or symptoms, in particular related to chronic pain and inflammation, as a sole agent or in combination with other active ingredients.
Microwave-Assisted Silver(I)-Mediated
Selective O-Alkylation of Aromatic Imidate Systems
作者:Erik Van der Eycken、Brajendra Singh、Claudia Cavalluzzo、Marc De
Maeyer、Zeger Debyser、Virinder Parmar
DOI:10.1055/s-0029-1216878
日期:——
A novel microwave-assisted protocol has been developed for the selective O-alkylation of aromatic imidate systems with various halides under microwave irradiation using silver carbonate as the base. Products were obtained in short reaction time and in excellent yields.
SUBSTITUTED AZA-BICYCLIC IMIDAZOLE DERIVATIVES USEFUL AS TRPM8 RECEPTOR MODULATORS
申请人:PLAYER Mark R.
公开号:US20110218197A1
公开(公告)日:2011-09-08
The present invention is directed to substituted aza-bicyclic imidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold.
In competition experiments, alkenes tethered to pyridyl groups were found to undergo iridium catalysed hydrogenation more quickly than alkenes tethered to phenyl groups. This is in marked contrast to the results for hydrogenation of some of the individual substrates where alkenes tethered to pyridyl groups were reduced much more slowly than their phenyl counterparts.