This communication details the evolution of the screening lead SB-203580, a known CSBP/p38 kinase inhibitor, into a potent and selective Tie2 tyrosine kinase inhibitor. The optimized compound 5 showed efficacy in an in vivo model of angiogenesis and a MOPC-315 plasmacytoma xenograft model. (c) 2007 Elsevier Ltd. All rights reserved.
This communication details the evolution of the screening lead SB-203580, a known CSBP/p38 kinase inhibitor, into a potent and selective Tie2 tyrosine kinase inhibitor. The optimized compound 5 showed efficacy in an in vivo model of angiogenesis and a MOPC-315 plasmacytoma xenograft model. (c) 2007 Elsevier Ltd. All rights reserved.
[EN] ARYLCARBOXAMIDES AND USES THEREOF<br/>[FR] ARYLCARBOXAMIDES ET LEURS UTILISATIONS
申请人:INCEPTION 1 INC
公开号:WO2017192304A1
公开(公告)日:2017-11-09
The present disclosure is directed to compounds of formula (I): or a pharmaceutically acceptable salt, solvate or solvate of the salt thereof. Compounds of formula (I) are inhibitors of NOX4 and are useful in the treatment of fibrotic diseases such as scleroderma; lung disease, such as pulmonary fibrosis including idiopathic pulmonary fibrosis (IPF); heart disease, such as heart failure due to ischaemic heart disease, valvular heart disease and hypertensive heart disease, diabetic cardiomyopathy and hypertension; liver disease, such as cirrhosis of the liver; and kidney disease, such as progressive kidney disease glomerulonephritis and diabetic nephropathy; and eye disease such as diabetic retinopathy; skin or subcutaneous scarring, such as keloids, adhesions, hypertrophic scarring or cosmetic scarring; or as an adjuvant or anti-fibrotic in pancreatic cancer to increase chemotherapeutic drug penetration by reducing the density of the connective tissue stroma.
Ananthakrishnanadar, P.; Varghesedharumaraj, G., Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 1983, vol. 22, # 5, p. 506 - 507
作者:Ananthakrishnanadar, P.、Varghesedharumaraj, G.
DOI:——
日期:——
SMMR (SMALL MOLECULE METABOLITE REPORTERS) FOR USE AS IN VIVO GLUCOSE BIOSENSORS
申请人:Bellott Emile M.
公开号:US20120052018A1
公开(公告)日:2012-03-01
Small Molecule Metabolite Reporters (SMMRs) for use as in vivo glucose biosensors, sensor compositions, and methods of use, are described. The SMMRs include boronic acid-containing xanthene, coumarin, carbostyril and phenalene-based small molecules which are used for monitoring glucose in vivo, advantageously on the skin.
US8466286B2
申请人:——
公开号:US8466286B2
公开(公告)日:2013-06-18
Pyridinylimidazole inhibitors of Tie2 kinase
作者:Marcus Semones、Yanhong Feng、Neil Johnson、Jerry L. Adams、Jim Winkler、Michael Hansbury
DOI:10.1016/j.bmcl.2007.06.068
日期:2007.9
This communication details the evolution of the screening lead SB-203580, a known CSBP/p38 kinase inhibitor, into a potent and selective Tie2 tyrosine kinase inhibitor. The optimized compound 5 showed efficacy in an in vivo model of angiogenesis and a MOPC-315 plasmacytoma xenograft model. (c) 2007 Elsevier Ltd. All rights reserved.