- AZA SPIRO ALKANE DERIVATIVES AS INHIBITORS OF METALLPROTEASES
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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.
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Paragraph 0134
(2015/12/18)
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- Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer
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The design, synthesis, evaluation, and identification of a novel class of (6S,7S)-N-hydroxy-6-carboxamide-5-azaspiro[2.5]octane-7-carboxamides as the first potent and selective inhibitors of human epidermal growth factor receptor-2 (HER-2) sheddase is des
- Yao, Wenqing,Zhuo, Jincong,Burns, David M.,Xu, Meizhong,Zhang, Colin,Li, Yun-Long,Qian, Ding-Quan,He, Chunhong,Weng, Lingkai,Shi, Eric,Lin, Qiyan,Agrios, Costas,Burn, Timothy C.,Caulder, Eian,Covington, Maryanne B.,Fridman, Jordan S.,Friedman, Steven,Katiyar, Kamna,Hollis, Gregory,Li, Yanlong,Liu, Changnian,Liu, Xiangdong,Marando, Cindy A.,Newton, Robert,Pan, Max,Scherle, Peggy,Taylor, Nancy,Vaddi, Kris,Wasserman, Zelda R.,Wynn, Richard,Yeleswaram, Swamy,Jalluri, Ravi,Bower, Michael,Zhou, Bing-Bing,Metcalf, Brian
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p. 603 - 606
(2007/10/03)
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- Asymmetric synthesis of conformationally constrained trans-2,3-piperidine- dicarboxylic acid derivatives
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An efficient asymmetric synthesis of conformationally constrained (2S,3S)-piperidinedicarboxylic acid derivatives starting from L-aspartic acid β-tert-butyl ester and 3-chloro-2-(chloromethyl)-1-propene is described. The key steps involve N-alkylation of
- Zhuo, Jincong,Burns, David M.,Zhang, Colin,Xu, Meizhong,Weng, Lingkai,Qian, Ding-Quan,He, Chunhong,Lin, Qiyan,Li, Yun-Long,Shi, Eric,Agrios, Costas,Metcalf, Brian,Yao, Wenqing
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p. 460 - 464
(2008/01/06)
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