791834-53-2Relevant academic research and scientific papers
AZA SPIRO ALKANE DERIVATIVES AS INHIBITORS OF METALLPROTEASES
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, (2015/12/18)
The present invention provides a compound of Formula (I) or Formula (II): enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula (I) and (II) are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.
Compelling P1 substituent affect on metalloprotease binding profile enables the design of a novel cyclohexyl core scaffold with excellent MMP selectivity and HER-2 sheddase inhibition
Burns, David M.,Li, Yun-Long,Shi, Eric,He, Chunhong,Xu, Meizhong,Zhuo, Jincong,Zhang, Colin,Qian, Ding-Quan,Li, Yanlong,Wynn, Richard,Covington, Maryanne B.,Katiyar, Kamna,Marando, Cindy A.,Fridman, Jordan S.,Scherle, Peggy,Friedman, Steve,Metcalf, Brian,Yao, Wenqing
scheme or table, p. 3525 - 3530 (2010/03/24)
A serendipitous discovery that the metalloprotease binding profile of a novel class of 2-carboxamide-3-hydroxamic acid piperidines could be significantly attenuated by the modification of the unexplored P1 substituent enabled the design and synthesis of a
Discovery of novel selective HER-2 sheddase inhibitors through optimization of P1 moiety
Li, Yun-Long,Shi, Eric,Burns, David,Li, Yanlong,Covington, Maryanne B.,Pan, Maxwell,Scherle, Peggy,Friedman, Steve,Metcalf, Brian,Yao, Wenqing
scheme or table, p. 5037 - 5042 (2010/03/31)
A novel series of carbamates was discovered as potent and selective HER-2 sheddase inhibitors. Significant enhancement in potency and selectivity was achieved through attenuating the P1 moiety, which was conventionally believed to be exposed to solvent.
SUBSTITUTED CYCLIC HYDROXAMATES AS INHIBITORS OF MATRIX METALLOPROTEINASES
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Page/Page column 89, (2008/06/13)
The present invention provides compounds of the formula I: its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof, solvates thereof, metabolites thereof, and pharmaceutically acceptable salts, wherein the ring A substituent groups are fully defined in the following disclosure. The compounds of formula I are inhibitors of metalloproteases such as matrix metalloproteases and sheddases, and are useful in treating diseases such as rheumatoid arthritis, psoriasis, neoplastic diseases, allergies and all those diseases wherein inhibition of MMPs is desirable.
