895240-80-9Relevant academic research and scientific papers
The P1 N-isopropyl motif bearing hydroxyethylene dipeptide isostere analogues of aliskiren are in vitro potent inhibitors of the human aspartyl protease renin
Yamaguchi, Yasuchika,Menear, Keith,Cohen, Nissim-Claude,Mah, Robert,Cumin, Frédéric,Schnell, Christian,Wood, Jeanette M.,Maibaum, Jürgen
scheme or table, p. 4863 - 4867 (2010/05/18)
Novel nonpeptide small molecule renin inhibitors bearing an N-isopropyl P1 motif were designed based on initial lead structures 1 and aliskiren (2). (P3-P1)-Benzamide derivatives such as 9a and 34, as well as the corresponding P1 basic tertiary amine derivatives 10 and 35 were found to display low nanomolar inhibition against human renin in vitro.
3, 4-SUBSTITUTED PYRROLIDINE DERIVATIVES FOR THE TREATMENT OF HYPERTENSION
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, (2010/11/24)
The invention relates to the use of (3,4-di-, 3,3,4-tri, 3,4,4-tri- or 3,3,4,4-tetra-)substituted pyrrolidine compounds for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; compounds that are part of a subclass of these substituted pyrrolidine compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (= disorder) that depends on activity of renin; new compounds that are part of a subclass of these substituted pyrrolidine compounds; pharmaceutical formulations comprising said substituted pyrrolidine compounds, and/or a method of treatment comprising administering said substituted pyrrolidine compounds, a method for the manufacture especially of said new substituted pyrrolidine compounds, as well as novel intermediates, starting materials and/or partial steps for their synthesis. The substituted pyrrolidine compounds are of the formula (I), wherein R1, R2, R3, R4, R5 and T are defined as in the specification.
