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.
A convenient enantioselective CBS-reduction of arylketones in flow-microreactor systems
作者:Sonia De Angelis、Maddalena De Renzo、Claudia Carlucci、Leonardo Degennaro、Renzo Luisi
DOI:10.1039/c6ob00336b
日期:——
A convenient, versatile, and green CBS-asymmetric reduction of aryl and heteroaryl ketones has been developed by using the microreactor technology.
一种便捷、多用途且环保的CBS不对称还原芳基和杂芳基酮的方法已经通过使用微反应器技术得以开发。
The friedel-crafts reaction of acid chlorides with ethene ; Di-addition and molecular rearrangement
作者:Francis X Bates、John A Donnelly、John R Keegan
DOI:10.1016/s0040-4020(01)80962-5
日期:1991.1
Acid chlorides, complexed with excess aluminiumchloride, reacted with ethene to form 3-methyl-2-buten-1-ones, i.e. rearranged di-addition products having a terminal isoprenoid skeleton, together with the usual β-chloropropanones. The latter were the sole products in the absence of excess catalyst. Acid chlorides containing a suitably situated π-system underwent intramolecular cyclization, e.g. 2-
[EN] QUINOLINE DERIVATIVES AND USE THEREOF AS MYCOBACTERIAL INHIBITORS<br/>[FR] DERIVES DE QUINOLINE ET UTILISATION DE CEUX-CI EN TANT QU'INHIBITEURS MYCOBACTERIENS
申请人:JANSSEN PHARMACEUTICA NV
公开号:WO2005070430A1
公开(公告)日:2005-08-04
The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or the general Formula (Ib) the pharmaceutically acceptable acid or base addition salts thereof, the quaternary amines thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof and the N-oxide forms thereof. The claimed compounds are useful for the treatment of mycobacterial diseases.
1-(Naphthylalkyl)-1H-imidazole derivatives, a new class of anticonvulsant agents
作者:Keith A. M. Walker、Marshall B. Wallach、Donald R. Hirschfeld
DOI:10.1021/jm00133a015
日期:1981.1
anticonvulsant activity has been demonstrated for a large number of 1-(naphthylalkyl)-1H-imidazoles containing a variety of functional groups in the alkylene bridge. The presence of a small oxygen function in the bridge, in general, confers a high therapeutic index between anticonvulsant and depressant activity. Clinical expectations are discussed for 1-(2-naphthoylmethyl)imidazole hydrochloride (5), which is