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US 8,895,755 B2Granted
Intermediates for preparing dual-acting benzyl triazole antihypertensive agents having angiotensin II type I receptor antagonist activity and neprilysin-inhibition activity
AssigneeTheravance Biopharma R&D IP, LLC
InventorsPaul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
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Abstract
The invention is directed to intermediates for preparing compounds having the formula: wherein: Ar, X, R3 ,and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity.
Claims1
A compound selected from the group consisting of:
- Ar is:
- Ar* is Ar-R1*;
- R1 is —COOR1a, where R1a is selected from H and —C1-6alkyl;
- R1* is —C(O)O—P2, where P2 is a carboxy-protecting group;
- R3 is —C1-10alkyl;
- X is —CH2—NHC(O)—;
- R5 is selected from —C0-3alkylene-SR5a and —C0-3alkylene-C(O)N(OH)H, where R5a is selected from H and —C(O)C1-6alkyl;
- R5* is selected from —C0-3alkylene-S—P3 and —C0-3alkylene-C(O)NH(O—P5), where P3 is a thiol-protecting group and P5 is a hydroxyl-protecting group;
- R6 is selected from —C1-6alkyl and —C0-3alkylenearyl;
- R7 is H;
- and salts thereof.
8 more elements
Dependencies are inferred from the claim text.