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US 10,294,225 B2Granted
N1-pyrazolospiroketone acetyl-CoA carboxylase inhibitors
AssigneePfizer Inc.
InventorsMary Didiuk, Robert Lee Dow, David Andrew Griffith
Life of this patent
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Abstract
The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3, Z, A1, L and A2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
Claims8
A method for treating a diabetes-related disease in a human comprising the step of administering to the human in need of such treatment a therapeutically effective amount of a compound of Formula (I)
- or a pharmaceutically acceptable salt thereof, wherein
- R1 is (C1-C6)alkyl, (C3-C7)cycloalkyl, tetrahydrofuranyl or oxetanyl, wherein said (C1-C6)alkyl is optionally substituted with 1 to 3 substituents independently selected from (C1-C3)alkoxy, hydroxy, fluoro, phenyl, tetrahydrofuranyl or oxetanyl;
- R2 is hydrogen, halo, (C1-C3)alkyl, or cyano;
- R3 are each independently hydrogen or (C1-C3)alkyl;
- L is a direct bond or a (C1-C6)alkylene wherein one carbon of the (C1-C6)alkylene is optionally replaced by —C(O)—, —C(O)NH—, —NHC(O)—, —O—, —S—, NH or N(C1-C3)alkyl;
- Z is CH2 or O;
- A1 and A2 are each independently (C6-C10)aryl, 5 to 12 membered heteroaryl or 8 to 12 membered fused heterocyclicaryl;
- wherein said (C6-C10)aryl, 5 to 12 membered heteroaryl or 8 to 12 membered fused heterocyclicaryl are each optionally substituted with one to three substituents independently selected from (C1-C3)alkyl, (C1-C3)alkoxy, halo, amino, (C1-C3)alkylamino, di(C1-C3)alkylamino, hydroxy, cyano and amido wherein the alkyl portion of the (C1-C3)alkyl, (C1-C3)alkoxy, (C1-C3)alkylamino and di(C1-C3)alkylamino are optionally substituted with one to five fluoro;
- and wherein one of A1 or A2 is substituted by CO2R4, (C1-C6)CO2R4, tetrazolyl or (C1-C6)tetrazolyl;
- and
- R4 is (C1-C8)alkyl, (C3-C8)cycloalkyl or (C1-C6)alkyl-(C3-C8)cycloalkyl.
8 more elements
Dependencies are inferred from the claim text.