148671-87-8Relevant articles and documents
Low-valent dialkoxytitanium(ii): a useful tool for the synthesis of functionalized seven-membered ring compounds
Bodinier, Florent,Sanogo, Youssouf,Ardisson, Janick,Lannou, Marie-Isabelle,Sorin, Geoffroy
, p. 3603 - 3606 (2021/04/14)
Herein, we describe unprecedented access to all-carbon or heterocyclic seven-membered ring frameworks from 1,8-ene-ynes promoted by inexpensive low-valent titanium(ii) species, readily available from Ti(OiPr)4and Grignard reagent. A broad range of cycloheptane, azepane or oxepane derivatives has been obtained (19 examples) with moderate to good yields and an excellent selectivity (up to 95/5 d.r.).
Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain
Law, Robert P.,Atkinson, Stephen J.,Bamborough, Paul,Chung, Chun-Wa,Demont, Emmanuel H.,Gordon, Laurie J.,Lindon, Matthew,Prinjha, Rab K.,Watson, Allan J. B.,Hirst, David J.
supporting information, p. 4317 - 4334 (2018/05/14)
The bromodomain and extra-terminal domain (BET) family of proteins bind acetylated lysine residues on histone proteins. The four BET bromodomains - BRD2, BRD3, BRD4, and BRDT - each contain two bromodomain modules. BET bromodomain inhibition is a potential therapy for various cancers and immunoinflammatory diseases, but few reported inhibitors show selectivity within the BET family. Inhibitors with selectivity for the first or second bromodomain are desired to aid investigation of the biological function of these domains. Focused library screening identified a series of tetrahydroquinoxalines with selectivity for the second bromodomains of the BET family (BD2). Structure-guided optimization of the template improved potency, selectivity, and physicochemical properties, culminating in potent BET inhibitors with BD2 selectivity.
BENZO-FUSED AZEPINONE AND PIPERIDINONE COMPOUNDS USEFUL IN THE INHIBITION OF ACE AND NEP
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, (2008/06/13)
Compounds having the following formula I, and pharmaceutically acceptable salts thereof, including dual inhibitors of ACE and NEP and selective ACE inhibitors: STR1 wherein: Y 1 and Y 2 are each independently hydrogen, alkyl, aryl, halogen, or alkoxy;