545348-98-9Relevant academic research and scientific papers
HETEROCYCLIC COMPOUNDS AS RSV INHIBITORS
-
Page/Page column 183-184, (2017/08/07)
The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: Formula (I) which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions
NOVEL TRICYCLIC DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
-
Page/Page column 17, (2011/10/02)
The present invention relates to a novel tricyclic derivative with efficient inhibitory activity against poly(ADP-ribose)polymerases (PARP) or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition containing the same. The tricyclic derivative of the invention is useful for the prevention or treatment of diseases caused by excess PARP activity, especially neuropathic pain, neurodegenerative diseases, cardiovascular diseases, diabetic nephropathy, inflammatory diseases, osteoporosis, and cancer, by inhibiting the activity of poly(ADP-ribose)polymerases.
NOVEL TRICYCLIC DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
-
Page/Page column 23, (2011/10/04)
The present invention relates to a novel tricyclic derivative with efficient inhibitory activity against poly(ADP-ribose)polymerases (PARP) or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition containing the same. The tricyclic derivative of the invention is useful for the prevention or treatment of diseases caused by excess PARP activity, especially neuropathic pain, neurodegenerative diseases, cardiovascular diseases, diabetic nephropathy, inflammatory diseases, osteoporosis, and cancer, by inhibiting the activity of poly(ADP-ribose)polymerases.
Heteroaryl-Fused 2-Phenylisothiazolone Inhibitors of Cartilage Breakdown
Wright, Stephen W.,Petraitis, Joseph J.,Abelman, Matthew M.,Batt, Douglas G.,Bostrom, Lori L.,et al.
, p. 3071 - 3078 (2007/10/02)
The synthesis, biological evaluation, and structure-activity relationships of a series of N-phenyl heteroaryl-fused isothiazolones are described.These isothiazolones have been shown to exhibit potent, dose-dependent inhibition of IL-1β-induced breakdown of proteoglycan in a cartilage organ culture assay.This effect is likely due to inhibition of MMP activation and a consequent reduction in MMP activity following IL-1β stimulation.Thus these compounds potentially represent simple, non-peptidic disease-modifying agents for the treatment of arthritic diseases.To examine the effects of structure on in vitro activity, three general features of the molecules were varied, substituents on the pendant N-phenyl group, the position of ring fusion to the isothiazolone, and substituents on the fused ring peri to the isothiazolone sulfur.
