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US 2024/0174638 A1Published application
Heteroaryl derivatives as apelin receptor agonists
AssigneeResearch Triangle Institute
InventorsScott P. RUNYON, Rangan MAITRA, Sanju NARAYANAN
Life of this patent
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Abstract
This disclosure is directed to agonists of the apelin receptor (APJ) and uses of such agonists.
Claims27
A compound represented by the Formula I:
- or a pharmaceutically acceptable salt thereof,
- wherein
- each of G1, G2, G3, and G4 is C, CH, or N, wherein:
- (a) G1 is CH, G2 is C, G3 is N, and G4 is N;
- (b) G1 is CH, G2 is N, G3 is C, and G4 is N;
- (c) G1 is N, G2 is N, G3 is C, and G4 is CH;
- or
- (d) G1 is N, G2 is N, G3 is C, and G4 is N;
- and
- the dashed ring A is heteroaromatic;
- R1 is
- wherein
- R11 is halogen, C1-6 alkoxy, or C1-6 haloalkyl;
- R12 is H, halogen, C1-6 alkoxy, or C1-6 haloalkyl;
- R2 is a 5- to 7-membered heteroaromatic ring with one or more heteroatom selected from O, N, or S, wherein R2 may be optionally substituted with one or more R21,
- wherein each R21 is halogen, C1-6 alkyl, C1-6 alkoxy, or C1-6 haloalkyl;
- R3 is
- wherein
- ring B is a 5- or 6-membered heterocyclic ring, optionally containing one or more degrees of unsaturation, and substituted with one or more R31,
- wherein each R31 is halogen, C1-6 alkyl, or oxo;
- each of R4 and R5 is H, CH3, or R4 and R5 combine with the atom to which they are attached to form a 3- to 6-membered cycloalkyl ring;
- and
- R6 is OH or NH—R61, wherein R61 is a 3- to 6-membered cycloalkyl ring.
20 more elements
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-15. (canceled)
-18. (canceled)
-35. (canceled)
-86. (canceled)
Dependencies are inferred from the claim text.