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US 12,258,340 B2Granted
Pyrazole MAGL inhibitors
AssigneeH. Lundbeck A/S
InventorsCheryl A. Grice, John J. M. Wiener, Olivia D. Weber, Katharine K. Duncan
Life of this patent
Estimating the term…
Abstract
Provided herein are pyrazole compounds and pharmaceutical compositions comprising the same. The compounds and compositions are useful as modulators of monoacylglycerol lipase (MAGL). Furthermore, the compounds and compositions are useful for the treatment of pain.
Claims20
A method of treating inflammatory pain in a patient in need thereof, the method comprising administering to the patient a therapeutically effective amount of a compound of Formula (I):
- wherein:
- R1 is —C(O)OR15 or —C(O)NR10R11;
- R2 is H, halogen, C1-6 alkyl, or C1-6 haloalkyl;
- R3 is
- A is N or C(H);
- Y is —CH2— or —C(O)—;
- Z is —S—, —O—, or —N(R18)—;
- R4 is H, halogen, —OR7, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, —C(O)NR8R9, C3-8cycloalkyl, C2-9 heterocycloalkyl, —C1-6 alkyl-C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl, wherein C3-8 cycloalkyl, C2-9 heterocycloalkyl, —C1-6 alkyl-C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl are optionally substituted with 1 or 2 R14;
- R5 is H, halogen, C1-6 alkyl, C1-6 haloalkyl, C1-6 haloalkoxy, or phenyl;
- R6 is H, halogen, or C1-6 alkyl;
- R7 is H, C1-6 alkyl, C1-6 haloalkyl, —C1-6 alkyl-OH, C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl, wherein C2-9 heterocycloalkyl, C6-10 aryl, or C1-9 heteroaryl are optionally substituted with 1 or 2 R14;
- each R8 and each R9 are independently selected from H and C1-6alkyl;
- or R8 and R9 together with the nitrogen to which they are attached are combined to form a heterocycloalkyl ring;
- R10 and R11 are each independently H or C1-6alkyl;
- R12 is H, halogen, or C1-6alkyl;
- R13 is H or C1-6alkyl;
- each R14 is independently selected from halogen, —OH, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, —C1-6 alkyl-OH, C3-8 cycloalkyl, —C(O) OH, —C(O)NR8R9, —SO2—C1-6 alkyl, and —N(R17)C(O)—C1-6 alkyl;
- R15 is H or C1-6 alkyl;
- R17 is H or C1-6 alkyl;
- R18 is H or C1-6 alkyl;
- n is 1;
- m is 1;
- p is 2;
- and
- q is 0;
- or a pharmaceutically acceptable salt thereof.
23 more elements
Dependencies are inferred from the claim text.