- SUBSTITUTED QUINAZOLINE COMPOUNDS AND THEIR USE AS INHIBITORS OF G12C MUTANT KRAS, HRAS AND/OR NRAS PROTEINS
-
Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I) or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R, R1, R2a, R2b, R2c, A, B, L1 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
- -
-
Page/Page column 105
(2017/02/09)
-
- Benzimidazole derivatives
-
This invention provides novel benzimidazole derivatives represented by the formula (I); a process for producing the same; a drug containing at least one of such compounds as its active ingredient, in particular, a drug for preventing and/or treating diseases exhibiting eosinophilia, bronchial asthma and allergic diseases; and an enhancer for IFN-γ production, and in particular, an antitumor agent or an antiviral agent based on the action of enhancing the IFN-γ production which exhibits excellent oral bioavailability.
- -
-
-
- Solid state nuclear bromination with N-bromosuccinimide. Part 1. Experimental and theoretical studies on some substituted aniline, phenol and nitro aromatic compounds
-
Solid state bromination of a number of substituted phenol, aniline and nitro aromatic compounds with N-bromosuccinimide yields exclusively the nuclear brominated products. Reactivity in the solid state depends on the reaction time, temperature and nature of the substituent on the substrate. The reaction apparently proceeds by an electrophilic aromatic substitution pathway. Molecular orbital and reaction free energy calculations also support such a view. Thermal analysis and video microscopic observation reveal the nature of the solid state reaction. Crystallinity is required for the reactivity and product selectivity. Product yield decreases with loss of selectivity when the reaction is carried out in a melt or in solution. Unlike the topochemical solid state reactions wherein molecular packing is more important than the intrinsic reactivity, these reactions demonstrate the importance of both these factors.
- Sarma, Jagarlapudi A.R.P.,Nagaraju, Akula
-
p. 1113 - 1118
(2007/10/03)
-