301185-40-0Relevant articles and documents
PIPERIDINE DERIVATIVES AS LIVER X RECEPTOR β AGONISTS, COMPOSITIONS, AND THEIR USE
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, (2018/04/27)
Piperidine compounds of the Formular: (I) and pharmaceutically acceptable salts thereof, wherein X, Y, R 1, R 2, R 3, L, R 4, L 1, Q and R 5 are as defined herein. The compounds and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
Copper(i)-catalysed stereoselective debromoborylation of aliphatic 1,1-dibromo-1-alkenes with bis(pinacolato)diboron
Pang, Yadong,Kojima, Ryoto,Ito, Hajime
supporting information, p. 6187 - 6190 (2018/09/10)
A stereoselective debromoborylation of aliphatic 1,1-dibromo-1-alkenes to prepare (Z)-1-bromo-1-alkenylboronate esters using copper(i) catalysts was developed. The debromoborylation of various aliphatic 1,1-dibromo-1-alkenes in the presence of a copper(i) catalyst and bis(pinacolato)diboron proceeded smoothly to produce (Z)-1-bromo-1-alkenylboronate esters in good yields with only Z geometry.
Design of potent and selective GPR119 agonists for type II diabetes
Szewczyk, Jason W.,Acton, John,Adams, Alan D.,Chicchi, Gary,Freeman, Stanley,Howard, Andrew D.,Huang, Yong,Li, Cai,Meinke, Peter T.,Mosely, Ralph,Murphy, Elizabeth,Samuel, Rachel,Santini, Conrad,Yang, Meng,Zhang, Yong,Zhao, Kake,Wood, Harold B.
scheme or table, p. 2665 - 2669 (2011/06/20)
Screening of the Merck sample collection identified compound 1 as a weakly potent GPR119 agonist (hEC50 = 3600 nM). Dual termini optimization of 1 led to compound 36 having improved potency, selectivity, and formulation profile, however, modest
SUBSTITUTED CYCLOPROPYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
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Page/Page column 42-43, (2009/12/02)
Substituted cyclopropyl compounds of formula (I) are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
ARYL- AND HETEROARYLPIPERIDINECARBOXYLATE-DERIVATIVES METHODS FOR THEIR PREPARATION AND USE THEREOF AS FATTY ACID AMIDO HYDROLASE ENZYME INHIBITORS
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Page/Page column 10, (2010/11/25)
The present invention comprises compounds corresponding to the general formula (I): in which m, n=1 to 3 and m+n=2 to 5; p=1 to 7; A=single bond or X, Y and/or Z; X=optionally substituted methylene; Y=C2-alkenylene, which is optionally substitu
Pyrrolidine modulators of chemokine receptor activity
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, (2008/06/13)
The present invention is directed to pyrrolidine compounds of the formula 1: (wherein R1, R2, R3, R4, R5, R6and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.
Regioselective synthesis of bridged azabicyclic compounds using radical translocation/cyclization reactions of 4-alkynyl-1-(o-iodobenzoyl)piperidines
Sato, Tatsunori,Okamoto, Kazuya,Nakano, Y?ko,Uenishi, Jun'ichi,Ikeda, Masazumi
, p. 747 - 755 (2007/10/03)
Bu3SnH-mediated radical translocation/cyclization reactions of 4-alkynyl-1-(o-iodobenzoyl)piperidines were examined. The 4-[3-(trimethylsilyl)-prop-2-ynyl]- (12) and 4-[4-(trimethylsilyl)but-3-ynyl]piperidine derivatives (16), upon treatment wi
