PROTEIN CROSSLINKING INHIBITOR AND USE OF THE SAME
申请人:Mikoshiba Katsuhiko
公开号:US20120277423A1
公开(公告)日:2012-11-01
The present invention relates to: a ketone compound having transglutaminase-inhibiting activity, which is represented by the following Formula 1, 2, or 3:
wherein R
1
is a substituted or unsubstituted aryl or heterocyclyl group, R
2
, R
3
, and R
4
are hydrogen atoms, n is 2, X is halogen, R
5
and R
6
independently represent a hydrogen atom or a substituted or unsubstituted C1-C10 alkyl, aryl, or aralkyl group, wherein R
5
and R
6
are not hydrogen atoms at the same time, or R
5
and R
6
may be taken together to form a saturated or unsaturated and substituted or unsubstituted heterocyclyl group containing a nitrogen atom (N); an inhibitor of protein crosslinking comprising the compound; and a composition for preventing or treating a protein-crosslinking causative disease, which comprises the compound or the protein crosslinking inhibitor.
The scope of the novel ruthenium‐catalyzed tandem cross‐metathesis/intramolecular‐hydroarylation sequence is described. This methodology offers a practical and efficient synthesis of structurally diverse and complex tetrahydrocarbazoles in good to excellent yields (up to 98 %). Moreover, preliminary efforts towards the development of an enantioselective version of the current process by sequential
The present invention relates to novel PPAR agonist compounds as well as pharmaceutical compositions containing them.
The compounds according to the invention are of quite particular therapeutic interest, notably for treating diabetes and/or dyslipidemias, as well as for preventing cardiovascular pathologies.
From Alkenes to Isoxazolines via Copper-Mediated Alkene Cleavage and Dipolar Cycloaddition
作者:Mingchun Gao、Yuansheng Gan、Bin Xu
DOI:10.1021/acs.orglett.9b02748
日期:2019.9.20
transformation is reported, along with selective C═C double bond cleavage and dipolar cycloaddition reaction from simple alkenes and inexpensive copper nitrate. Various transformations demonstrate the generality of this method. Further mechanistic investigation indicates a novel ionic pathway for alkene cleavage and highlights the coeffect of iodide and boric acid as additives on the inhibition of well-documented
The hydration of α,β‐unsaturatedketones with water proceeded efficiently in the presence of In(OTf)3 (20 mol%) in aqueous media to afford synthetically versatile β‐hydroxyketones in moderate to good yields with good functional group compatibility. The method also can be extended to the hydroalkoxylation of α,β‐unsaturatedketones with various alcohols for the efficient synthesis of β‐alkoxyketones as