DIAMINOMETHYLENE-PYRIMIDINE-2,4,6-TRIONES CONTAINING SPIROCYCLE AS AGONISTS OF PARATHYROID HORMONE 1 AND INCRETIN RECEPTORS

Claims

Compounds that are parathyroid hormone receptor 1 agonists and methods useful for preventing or treating osteoporosis, fractures, osteomalacia, arthritis, thrombocytopenia, hypoparathyroidism, hyperphosphatemia, or tumor calcinosis are described. GLP-1R, GCGR, and / or GIPR agonists and methods for treating various therapeutic indications by administering an effective amount of a GLP-1R, GCGR, and / or GIPR agonist are also described.

1. A compound characterized in that it is according to formula (1), or a pharmaceutically acceptable salt thereof, wherein: R1 is (C1-C6)alkyl optionally substituted with one or more instances of fluoro, carboxy, (C1-C6)carboxyalkoxy, 4- to 7-membered heterocycloalkyl or (C3-C8)cycloalkyl, wherein (C3-C8)cycloalkyl and 4- to 7-membered heterocycloalkyl are optionally substituted with one or more instances of (C1-C6)alkyl, carboxy, and fluoro; R2 is (C1-C6)alkyl optionally substituted with cyano; R 3 is: a) (C1-C6)alkyl substituted with SO2R 3a , (C1-C6)alkoxy, (C3-C8)cycloalkyl, phenyl, 4- to 7-membered heterocycloalkyl, or 5- to 6-membered heteroaryl, wherein (C3-C8)cycloalkyl, phenyl, 4- to 7-membered heterocycloalkyl, or 5- to 6-membered heteroaryl are optionally substituted with one or more instances of (C1-C6)alkyl and fluoro, ob) unsubstituted branched (C1-C6)alkyl; and R 3a is (C1-C6)alkyl.

73. A pharmaceutical composition characterized in that it comprises a compound of any of claims 1 to 72, or a pharmaceutically acceptable salt thereof; and at least one pharmaceutically acceptable excipient.