The discovery and preparation of disubstituted novel amino-aryl-piperidine-based renin inhibitors |
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| Authors: | Cody Wayne L Holsworth Daniel D Powell Noel A Jalaie Mehran Zhang Erli Wang Wei Samas Brian Bryant John Ostroski Robert Ryan Michael J Edmunds Jeremy J |
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| Affiliation: | Department of Chemistry, Pfizer Global Research and Development, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, USA. wayne.cody@pfizer.com |
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| Abstract: | Recently, trans-disubstituted oxo-aryl-piperidines have been identified as small molecule nonpeptide renin inhibitors for the modulation of hypertension. Herein, we report on the discovery and preparation of a new class of novel cis-disubstituted amino-aryl-piperidines as a mixture of enantiomers that are potent in vitro renin inhibitors and also, possess in vivo antihypertensive activity in a double transgenic mouse model. |
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