Kulinkovich, O. G.; Sviridov, S. V.; Vasilevskii, D. A., Journal of Organic Chemistry USSR (English Translation), 1989, vol. 25, # 10.2, p. 2027 - 2028
SUBSTITUTED 4-PYRIDONES AND THEIR USE AS INHIBITORS OF NEUTROPHIL ELASTASE ACTIVITY
申请人:OOST Thorsten
公开号:US20140057916A1
公开(公告)日:2014-02-27
This invention relates to substituted 4-pyridones of formula 1
and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.
The invention relates to substituted spirocyclic cyclohexane derivatives which have an affinity for the μ opioid receptor and the ORL1 receptor, processes for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.
Simple access to β-trifluoromethyl-substituted ketones via copper-catalyzed ring-opening trifluoromethylation of substituted cyclopropanols
作者:Dzmitry G. Kananovich、Yulia A. Konik、Dzmitry M. Zubrytski、Ivar Järving、Margus Lopp
DOI:10.1039/c5cc02386f
日期:——
A variety of β-trifluoromethyl ketones have been easily prepared by CuCl-catalyzed ring-opening trifluoromethylation of cyclopropanols with Togni reagent.
一种多样的β-三氟甲基酮已经通过CuCl催化的环丙醇与Togni试剂的环开三氟甲基化反应轻松制备。
One-Pot Synthesis of 1-Substituted Cyclopropanols from Carboxylic Acid Chlorides
作者:José Barluenga、José L. Fernandez-Simon、José M. Concellon、Miguel Yus
DOI:10.1055/s-1987-28016
日期:——
The in situ generated chloromethyl-lithium reacts at -78°C to - 30°C with different acid chlorides (2:1 molar ratio) to afford, after lithiation with lithium powder, 1-substituted cyclopropanols.
Spiro compounds for treatment of inflammatory disorders
申请人:Weingarten M. David
公开号:US20080280974A1
公开(公告)日:2008-11-13
Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of an inflammatory condition, in particular asthma. The compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof:
wherein Y, Z and R
1
-R
12
are defined herein.