Extended lifetimes in vivo renin inhibitors

Details Extended lifetimes in vivo renin inhibitors Extended lifetimes in vivo renin inhibitors

1999-03-12

2000-08-22

Moezie, F. T.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

5483351, 514 19, 514 18, 530330, 530331, C07D23354, A61K 3805

Patent

active

061074896

ABSTRACT:
Novel compounds comprising chemically reactive intermediates which can react with available reactive functionalities on blood components to form covalent linkages, where the resulting covalently-bound conjugates are found to have renin inhibition activity are provided. Specifically, the renin inhibitor compounds of the present invention are tripeptide derivatives of a known renin inhibitor which can be covalently linked to chemically reactive functionalities on various blood components. The conjugated renin inhibitors thereby have extended lifetimes in the bloodstream, as compared to the unconjugated parent drug, and are, therefore, capable of maintaining renin inhibitory activity for extended periods of time as compared to the unconjugated parent drug. Also provided herein are methods for inhibiting renin activity in vivo comprising administering to the bloodstream of a mammalian host the novel compounds of the present invention.

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The Merck Index, Budavari Editor, 12th ed., Merck & Co., Inc. Whitehouse Station, N.J. Entry No. 1272, 3209, 3210, 1996.

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