[EN] GLUCOSE UPTAKE INHIBITORS<br/>[FR] INHIBITEURS DE L'ABSORPTION DU GLUCOSE
申请人:KADMON CORP LLC
公开号:WO2020005935A1
公开(公告)日:2020-01-02
This invention provides compounds that modulate glucose uptake activity and cellular transport/uptake of glucose, and particularly GLUTS3, but also including but not limited to GLUT1-14 (SLC2A1-SLC2A14). Compounds of the invention are useful for treating diseases, including cancer, autoimmune diseases and inflammation, infectious diseases, and metabolic diseases.
作者:Aurpon W. Mitra、Marvin M. Hansen、Michael E. Laurila、Stanley P. Kolis、Joseph R. Martinelli
DOI:10.1016/j.tetlet.2013.09.099
日期:2013.11
α-Aminoamides are shown to be useful as ligands in Goldberg amidations. A number of α-aminoamides are examined and the importance of substitution on the α-aminoamides is explored. Acetamide is focused on as the nucleophilic coupling partner due to its low cost, stability and convenience as a protecting group. The initial substrate scope for these catalysts is explored and includes electronically activated
Reversible and Sensitive Hg<sup>2+</sup> Detection by a Cell-Permeable Ytterbium Complex
作者:Guochen Bao、Shuai Zha、Zhenyu Liu、Yan-Ho Fung、Chi-Fai Chan、Hongguang Li、Pak-Ho Chu、Dayong Jin、Peter A. Tanner、Ka-Leung Wong
DOI:10.1021/acs.inorgchem.7b02243
日期:2018.1.2
A cell-permeable ytterbium complex shows reversible binding with Hg2+ in aqueous solution and in vitroby off–on visible and NIR emission. The fast response and 150 nM sensitivity of Hg2+ detection is based upon FRET and the lanthanide antenna effect. The reversible Hg2+ detection can be performed in vitro, and the binding mechanism is suggested by NMR employing the motif structure in a La complex and
The object of the present invention is to provide vitamin D derivatives that have excellent physiological activities as medicines, particularly as therapeutic agents for skin diseases such as psoriasis, and that have a reduced hypercalcemic effect.
The present invention provides a vitamin D derivative of Formula (1):
1
wherein
X represents an oxygen atom or a sulfur atom;
m represents a number of 1 to 3;
R
1
and R
2
each represent a hydrogen atom or an alkyl group;
R
4
and R
5
each represent a hydrogen atom or a hydroxyl group, etc.;
R
3
represents —YR
8
, etc.;
R
6
represents a hydrogen atom, etc.; and
R
7
represents a hydrogen atom, etc.
本发明的目的是提供作为药物的维生素D衍生物,特别是作为治疗银屑病等皮肤疾病的治疗剂,并且具有减少高钙血症作用的维生素D衍生物。
本发明提供了化学式(1)的维生素D衍生物:
1
其中
X代表氧原子或硫原子;
m代表1至3的数字;
R
1
和R
2
分别代表氢原子或烷基;
R
4
和R
5
分别代表氢原子或羟基等;
R
3
代表—YR
8
等;
R
6
代表氢原子等;以及
R
7
代表氢原子等。