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US 2012/0071514 A1Published application
Benzoxazolone derivatives as aldosterone synthase inhibitors
AssigneeNovartis AG
InventorsQi-Ying Hu, Julien Papillon
Life of this patent
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Abstract
The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Claims12
A compound of Formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is C1-7alkyl, C6-10aryl-C1-7alkyl, hydroxy-C1-7alkyl, C3-8cycloalkyl or —CH2C(O)NR8R9;
- R2 and R4 are each independently hydrogen or halogen;
- R3 is hydrogen or C1-7alkoxy;
- R5 is hydrogen, halogen, C1-7alkoxy, C1-7alkyl, C3-8cycloalkyl, cyano, —CH2NR8R9, —CH2NR8(SO2)—C1-7alkyl, —CH2NR8(SO2)—C3-8cycloalkyl, —NR8(SO2)—C1-7alkyl, —NR8(SO2)—C3-8cycloalkyl or —NHC(O)NR8R9;
- in which each alkyl and cycloalkyl is optionally substituted with one or more substitutents selected from the group consisting of C1-7alkoxy, halogen, hydroxy, —NH2, —NH(C1-7alkyl) and —N(C1-7alkyl)2;
- R6 hydrogen, C1-7alkyl, C3-8cycloalkyl, heterocyclyl, —C(O)—C1-7alkyl, —C(O)NR8R9, —C1-7alkyl-NR8C(O)—C1-7alkyl, —CH2NR8(SO2)—C1-7alkyl, —C1-7alkyl-NR8—S(O)n—C1-7alkyl, —CH2NR8—S(O)n—C3-8cycloalkyl or —CH2NR8(SO2)—C1-7alkyl;
- in which each alkyl and cycloalkyl is optionally substituted with one or more substitutents selected from the group consisting of C6-10aryl, C1-7alkoxy, halogen, hydroxy and —NH2, —NH(C1-7alkyl) and —N(C1-7alkyl)2;
- and
- R8 and R9 are each independently hydrogen, C1-7alkyl or C6-10aryl-C1-7alkyl;
- and
- n is 1 or 2;
- wherein each heteroaryl is a mono- or bicyclic aromatic moiety comprising 5-10 ring atoms selected from carbon atoms and 1 to 5 heteroatoms, and
- each heterocyclyl is a mono- or bicyclic saturated or partially saturated but non-aromatic moiety comprising 4-10 ring atoms selected from carbon atoms and 1 to 5 heteroatoms;
- and each heteroatoms being O, N or S.
12 more elements
12-15. (canceled)
Dependencies are inferred from the claim text.