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US 12,006,321 B2Granted
Substituted pyrazolo[1,5-a]pyrimidines as apelin receptor agonists
AssigneeSanford Burnham Prebys Medical Discovery Institute
InventorsLayton H. Smith, Anthony B. Pinkerton, Paul Hershberger, Patrick Maloney, Danielle McAnally
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Abstract
Provided herein are agonists of the apelin receptor of Formula (I): for the treatment of disease. The compounds disclosed herein are useful for the treatment of a range of cardiovascular, renal and metabolic conditions.
Claims21
A compound of Formula (I):
- or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof,
- wherein:
- R1 is H, halogen, CN, alkyl, C(O)N(R7)2, C(O)OH, C(O)OR6, NH2, O(alkyl), O(phenyl), or aryl, wherein the alkyl is optionally substituted with one or more substituents independently selected from the group consisting of OH and O(alkyl);
- R2 is H, halogen, CN, alkyl, C(O)N(R7)2, C(O)OH, C(O)OR6, NH2, O(alkyl), O(phenyl), or aryl, wherein the alkyl is optionally substituted with one or more substituents independently selected from the group consisting of OH and O(alkyl);
- R3 is alkyl;
- R4 is alkyl, haloalkyl, or cycloalkyl;
- R5 is C(O)N(R9)2, C(O)OH, or C(O)OR8;
- each R6 is independently H, alkyl, haloalkyl, NH2, O(alkyl), O(haloalkyl), cycloalkyl, heterocycloalkyl, phenyl, or 5- or 6-membered heteroaryl;
- each R7 is independently H, alkyl, haloalkyl, NH2, O(alkyl), O(haloalkyl), cycloalkyl, heterocycloalkyl, phenyl, or 5- or 6-membered heteroaryl;
- R8 is H, alkyl, haloalkyl, NH2, O(alkyl), O(haloalkyl), cycloalkyl, heterocycloalkyl, phenyl, or 5- or 6-membered heteroaryl;
- and
- each R9 is independently H, alkyl, haloalkyl, NH2, O(alkyl), O(haloalkyl), cycloalkyl, heterocycloalkyl, phenyl, or 5- or 6-membered heteroaryl.
9 more elements
Dependencies are inferred from the claim text.