18791-99-6Relevant articles and documents
Gol'dfarb et al.
, (1974)
2-AMINO-N-(AMINO-OXO-ARYL-LAMBDA6-SULFANYLIDENE)ACETAMIDE COMPOUNDS AND THEIR THERAPEUTIC USE
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Page/Page column 228, (2021/06/26)
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 2-amino-N-(amino-oxo-aryl-λ6- sulfanylidene)acetamide compounds (referred to herein as ANASIA compounds) that, inter alia, inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase (aaRS) (e.g., bacterial leucyl-tRNA synthetase, LeuRS). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase; to treat disorders that are ameliorated by the inhibition (e.g., selective inhibition) of bacterial aminoacyl-tRNA synthetase; to treat bacterial infections; etc.
QUINOLINE DERIVATIVES AND THEIR USE FOR TREATING ENDOPLASMIC RETICULUM STRESS-RELATED DISEASES AND DISORDERS
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Paragraph 0926; 0927, (2017/07/01)
Provided herein are quinolines, e.g., a compound of Formula I, pharmaceutical compositions thereof, and methods of their use for treating, preventing, or ameliorating one or more symptoms of an endoplasmic reticulum stress-caused disease. Also provided herein are methods of their use for reducing endoplasmic reticulum stress and modulating the activity of a sarcoplasmic/endoplasmic reticulum Ca2+ ATPase.
Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: Structure-activity relationship of the aryl region
Probst, Gary D.,Bowers, Simeon,Sealy, Jennifer M.,Stupi, Brian,Dressen, Darren,Jagodzinska, Barbara M.,Aquino, Jose,Gailunas, Andrea,Truong, Anh P.,Tso, Luke,Xu, Ying-Zi,Hom, Roy K.,John, Varghese,Tung, Jay S.,Pleiss, Michael A.,Tucker, John A.,Konradi, Andrei W.,Sham, Hing L.,Jagodzinski, Jacek,Toth, Gergely,Brecht, Eric,Yao, Nanhua,Pan, Hu,Lin, May,Artis, Dean R.,Ruslim, Lany,Bova, Michael P.,Sinha, Sukanto,Yednock, Ted A.,Gauby, Shawn,Zmolek, Wes,Quinn, Kevin P.,Sauer, John-Michael
scheme or table, p. 6034 - 6039 (2010/11/04)
The structure-activity relationship of the prime region of hydroxyethylamine BACE inhibitors is described. Variation in the aryl linker region with 5- and 6-membered heterocycles provided compounds such as 33 with improved permeability and reduced P-gp liability compared to benzyl amine analog 1.