5′-Phenyl-3′H-spiro[indoline-3,2′-[1,3,4]thiadiazol]-2-one inhibitors of ADAMTS-5 (Aggrecanase-2)
摘要:
5'-Phenyl-3' H-spiro[indoline-3,2'-[1,3,4]thiadiazol]-2-one inhibitors of ADAMTS-5 (Aggrecanase-2) have been prepared via commercially available starting materials. Selected compounds 23, 33-35 show sub-micromolar ADAMTS-5 potency and strong SAR trends with selectivity over the related metalloproteases ADAMTS-4 (Aggrecanase-1), MMP12, and MMP13. This series of compounds represents progress toward a selective ADAMTS-5 inhibitor as a disease modifying osteoarthritis drug. (c) 2007 Elsevier Ltd. All rights reserved.
PROCESS FOR THE PREPARATION OF CYCLOPENTA[G]QUINAZOLINE DERIVATIVES
申请人:BTG International Limited
公开号:EP1421069B1
公开(公告)日:2011-08-10
TRICYCLIC 1,2,4-TRIAZINE OXIDES AND COMPOSITIONS THEREFROM FOR THERAPEUTIC USE IN CANCER TREATMENTS
申请人:AUCKLAND UNISERVICES LIMITED
公开号:EP1866292B1
公开(公告)日:2010-12-15
AROMATIC POLYCARBONATE, ELECTROPHOTOGRAPHIC PHOTORECEPTOR, AND IMAGE FORMING APPARATUS
申请人:KIHARA Akiko
公开号:US20080199215A1
公开(公告)日:2008-08-21
In an electrophotographic photoreceptor including a conductive substrate and a single layer type photosensitive layer, the aromatic polycarbonate is contained to a single layer type photosensitive layer, which aromatic polycarbonate includes a constituent unit represented by the following general formula (1) derived from a compound having a basic asymmetric bishydroxy enamine skeleton represented by the general formula:
Accordingly, the electrophotographic photoreceptor is obtained which is excellent in charge transportability, mechanical strength, electric property, durability, etc. and can form good images for a long time.