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US 2010/0249163 A1Published application
Renin inhibitors
OwnerDaniel Dube, Erich L. Grimm +2inventors
InventorsDaniel Dube, Erich L. Grimm, Dwight MacDonald, Bruce MacKay
Life of this patent
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Abstract
The present invention relates to piperidinyl-based renin inhibitor compounds having the formula containing amino-terminal groups, and their use in treating cardiovascular events and renal insufficiency.
Claims11
A compound of formula I, or a pharmaceutically acceptable salt thereof, having the formula (I)
- wherein
- R1 is selected from the group consisting of C1-6alkyl or C3-8cycloalkyl;
- R2 is an aryl ring, a 5 or 6-membered heteroaryl ring containing 1, 2, 3 or 4 heteroatoms selected from N, O or S, or a fused 9 or 10-membered heteroaryl ring system containing 1, 2, 3 or 4 heteroatoms selected from N, O or S, wherein said aryl or heteroaryl ring is unsubstituted or mono-, di-, tri- or tetra-substituted with a group independently selected from
- 1) halogen,
- 2) O—C1-5alkylene-O—C1-5alkyl,
- 3) C1-5alkylene-O—C1-5alkyl,
- 4) C1-5alkylene-N(C1-5alkyl)-C(O)—C1-5alkyl,
- 5) C1-5alkylene-NH—C(O)—C1-5alkyl, and
- 6) oxo;
- R3 is an aryl ring, a 5 or 6-membered heteroaryl ring containing 1, 2, 3 or 4 heteroatoms selected from N, O or S, a fused 9 or 10-membered heteroaryl ring system containing 1, 2, 3 or 4 heteroatoms selected from N, O or S, or C3-8 cycloalkyl, wherein said aryl ring, heteroaryl ring, or C3-8 cycloalkyl is unsubstituted or mono-, di-, tri- or tetra-substituted with a group independently selected from
- 1) halogen,
- 2) C1-5alkoxy,
- 3) CF3,
- 4) NH2,
- 5) O—(C1-5alkylene)-aryl,
- 6) C1-5 alkyl, and
- 7) oxo,
- R4 is selected from the group consisting of
- hydrogen,
- C1-5alkyl,
- C1-5alkylene-aryl,
- C1-5allylene-O—C1-5alkyl,
- C3-8cycloalkyl,
- C1-5alkyleneNHC(O)—C1-5alkyl,
- C(O)—O—C1-5alkyl, and
- C1-5alkylene-heteroaryl,
- wherein aryl is unsubstituted or mono- or di-substituted with halogen, alkyl is unsubstituted or mono- or di-substituted with OH, and heteroaryl is a 5 or 6 membered unsaturated ring containing 1, 2, 3 or 4 heteroatoms selected from the group consisting of N, O and S.
24 more elements
Dependencies are inferred from the claim text.