65626-22-4Relevant academic research and scientific papers
Fragment-Based Approach to the Development of an Orally Bioavailable Lactam Inhibitor of Lipoprotein-Associated Phospholipase A2 (Lp-PLA2)
Woolford, Alison J.-A.,Day, Philip J.,Bénéton, Véronique,Berdini, Valerio,Coyle, Joseph E.,Dudit, Yann,Grondin, Pascal,Huet, Pascal,Lee, Lydia Y. W.,Manas, Eric S.,McMenamin, Rachel L.,Murray, Christopher W.,Page, Lee W.,Patel, Vipulkumar K.,Potvain, Florent,Rich, Sharna J.,Sang, Yingxia,Somers, Don O.,Trottet, Lionel,Wan, Zehong,Zhang, Xiaomin
supporting information, p. 10738 - 10749 (2016/12/16)
Lp-PLA2 has been explored as a target for a number of inflammation associated diseases, including cardiovascular disease and dementia. This article describes the discovery of a new fragment derived chemotype that interacts with the active site of Lp-PLA2. The starting fragment hit was discovered through an X-ray fragment screen and showed no activity in the bioassay (IC50 > 1 mM). The fragment hit was optimized using a variety of structure-based drug design techniques, including virtual screening, fragment merging, and improvement of shape complementarity. A novel series of Lp-PLA2 inhibitors was generated with low lipophilicity and a promising pharmacokinetic profile.
HETEROCYCLIC MODULATORS OF LIPID SYNTHESIS AND COMBINATIONS THEREOF
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, (2015/07/07)
Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds and combinations of such compounds and other therapeutic agents.
Discovery of vinylcycloalkyl-substituted benzimidazole TRPM8 antagonists effective in the treatment of cold allodynia
Calvo, Raul R.,Meegalla, Sanath K.,Parks, Daniel J.,Parsons, William H.,Ballentine, Shelley K.,Lubin, Mary Lou,Schneider, Craig,Colburn, Raymond W.,Flores, Christopher M.,Player, Mark R.
, p. 1903 - 1907 (2012/04/04)
Thermosensitive transient receptor potential melastatin 8 (TRPM8) antagonists are considered to be potential therapeutic agents for the treatment of cold hypersensitivity. The discovery of a new class of TRPM8 antagonists that shows in vivo efficacy in the rat chronic constriction injury (CCI)-induced model of neuropathic pain is described.
HEPATITIS C VIRUS INHIBITORS
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, (2012/03/09)
The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment o
IMIDAZOPYRIDIN-2-ONE DERIVATIVES
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Page/Page column 26, (2011/04/24)
A compound represented by formula (I) having mTOR inhibitory activity or a pharmacologically acceptable salt thereof.
2-Aminopyrimidine modulators of the histamine H4 receptor
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Page/Page column 26, (2008/12/07)
2-Aminopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 /su
NOVEL PIPERIDINE/8-AZABICYCLO [3.2.1] OCTAN DERIVATIVES AS MODUILATORS OF CHEMOKINE RECEPTOR CCR5
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Page/Page column 92, (2010/02/15)
Compounds of formula (I) wherein neither R4 nor R5 is hydrogen; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).
CHEMICAL COMPOUNDS
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Page/Page column 30-31, (2010/02/12)
Compounds of formula (I): [Chemical formula should be inserted here. Please see paper copy] compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).
REVERSE HYDROXAMIC ACID DERIVATIVES
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Page 107, (2008/06/13)
Reverse hydroxamic acid derivatives having specific structure represented by a general formula (Ia): (wherein A is a hydrogen atom or the like; Ar1 is an arylene or the like; Ar2 is an optionally substituted aryl, a heteroaryl or the
