594839-90-4Relevant articles and documents
PIPERIDIN-4-YL-AZETIDINE DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS
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, (2013/05/08)
Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (I) as follows: wherein Y, Z, and R are defined herein.
Benzoxazole and benzothiazole amides as novel pharmacokinetic enhancers of HIV protease inhibitors
Jonckers, Tim H.M.,Rouan, Marie-Claude,Hache, Geerwin,Schepens, Wim,Hallenberger, Sabine,Baumeister, Judith,Sasaki, Jennifer C.
supporting information; experimental part, p. 4998 - 5002 (2012/09/07)
A new class of benzoxazole and benzothiazole amide derivatives exhibiting potent CYP3A4 inhibiting properties was identified. Extensive lead optimization was aimed at improving the CYP3A4 inhibitory properties as well as overall ADME profile of these amide derivatives. This led to the identification of thiazol-5-ylmethyl (2S,3R)-4-(2-(ethyl(methyl)amino)-N-isobutylbenzo[d]oxazole- 6-carboxamido)-3-hydroxy-1-phenylbutan-2-ylcarbamate (C1) as a lead candidate for this class. This compound together with structurally similar analogues demonstrated excellent 'boosting' properties when tested in dogs. These findings warrant further evaluation of their properties in an effort to identify valuable alternatives to Ritonavir as pharmacokinetic enhancers.
DI-AZETIDINYL DIAMIDE AS MONOACYLGLYCEROL LIPASE INHIBITORS
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, (2012/03/26)
Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Q and Z are defined herein.
OXOPIPERAZINE-AZETIDINE AMIDES AND OXODIAZEPINE-AZETIDINE AMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS
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, (2012/04/05)
Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (Ia) and Formula (Ib) as follows: wherein Y, Z, and n are defined herein; and wherein Yb and Zb are as defined herein.
AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS
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Page/Page column 75, (2010/11/05)
Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I), wherein Y, Z, R1, and s are defined herein.
Benzoxazoles as transthyretin amyloid fibril inhibitors: Synthesis, evaluation, and mechanism of action
Razavi, Hossein,Palaninathan, Satheesh K.,Powers, Evan T.,Wiseman, R. Luke,Purkey, Hans E.,Mohamedmohaideen, Nilofar N.,Deechongkit, Songpon,Chiang, Kyle P.,Dendle, Maria T. A.,Sacchettini, James C.,Kelly, Jeffery W.
, p. 2758 - 2761 (2007/10/03)
Benzoxazoles pevent misfolding: Benzoxazole-based inhibitors of transthyretin (TTR) amyloid fibril formation are among the most effective found to date. They stabilize TTR against both acid-mediated misfolding and urea denaturation by raising the activati