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US 8,133,907 B2Granted
Pyridine derivatives as dipeptedyl peptidase inhibitors
AssigneeEli Lilly and Company
InventorsLarry Chris Blaszczak, Brian Michael Mathes, Shon Roland Pulley, Michael Alan Robertson, Scott Martin Sheehan, Qing Shi, Brian Morgan Watson, Michael Robert Wiley
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Abstract
The present invention is directed to compounds of formula (I) or a pharmaceutically acceptable salt thereof; wherein A is (1); X is selected from CH, CF and N; R5 is selected from H, C1-C6 alkyl, C1-C6 fluoroalkyl, and —OR12; R9 is selected from H —NR13C(O)R14 and —C(O)NR10R11; R12 is selected from H, C1-C6 alkyl and C3-C6 cycloalkyl, for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes.
Claims19
A compound of the formula I:
- or a pharmaceutically acceptable salt thereof;
- wherein
- A is
- R1 is selected from H, halo, C1-C4 alkyl, and C1-C4 haloalkyl;
- R2, R3, and R4 are independently selected from H, halo, methyl, and C1-C2 haloalkyl;
- X is CH;
- R5 is H or —OR12;
- R6 is H or C1-C6 haloalkyl;
- R7 and R8 are H;
- R9 is —NR13C(O)R14 or —C(O)NR10R11;
- R10 and R11 are independently selected from H, C1-C6 alkyl, C1-C6 haloalkyl, aryl, C3-C6 cycloalkyl, C1-C6 alkylaryl, C1-C6 alkyl-C3-C6 cycloalkyl or R10 and R11 combine with the N of R9 to form piperidinyl;
- where R10 or R11 are aryl or C1-C6 alkylaryl the aryl substituent is optionally substituted with 1-3 substituents selected from methoxy;
- R12 is H or C1-C6 alkyl;
- R13 H;
- R14 is C1-C6 alkyl.
12 more elements
Dependencies are inferred from the claim text.