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US 2014/0235580 A1Published application
Inhibitors of monoacylglycerol lipase and methods of their use
AssigneeInfinity Pharmaceuticals, Inc.
InventorsAlfredo C. Castro, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
Life of this patent
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Abstract
Provided herein are compounds which mediate the activity of monoacyglycerol lipase (MAGL). Also provided are pharmaceutical compositions comprising a compound provided herein, and methods for treating, preventing and/or managing a MAGL mediated condition using a compound or pharmaceutical composition as provided herein.
Claims30
A compound of formula (I):
- or a pharmaceutically acceptable form thereof;
- wherein:
- A is a 6 to 10 membered aryl, heteroaryl or heterocycle;
- X is a covalent bond or —NR5;
- R1 and R2 are each independently hydrogen, halogen, or an optionally substituted (C1-C6)alkyl;
- R3 is —C(O)NH2, —(CH2)n—NHR6 or —SO2R7, and R4 is hydrogen;
- or
- R3 and R4 taken together can form a 5 to 7 membered ring containing one or more heteroatoms selected from N, S and O, wherein one or more carbon or sulfur atoms on the ring can optionally be substituted with one or more oxo group;
- R5 is hydrogen or —C(O)O—Y, wherein Y is an optionally substituted 6 to 10 membered aryl or an optionally substituted (C1-C6)alkyl;
- R6 is an optionally substituted (C1-C6)alkyl, —SO2R8 or —C(O)R9;
- R7, R8 and R9 are each independently an optionally substituted (C1-C6)alkyl or an optionally substituted amino;
- and
- n is 0, 1, 2 or 3;
- wherein if R3 is —C(O)NH2, then both R1 and R2 are not each hydrogen.
11 more elements
A compound of formula (III):
- or a pharmaceutically acceptable form thereof,
- wherein:
- R18 is hydrogen, halogen, or an optionally substituted (C1-C6)alkyl;
- R19 is hydrogen or —C(O)O—Y, wherein Y is an optionally substituted 6 to 10 membered aryl or an optionally substituted (C1-C6)alkyl;
- R20 is hydrogen, —C(O)NH2, —(CH2)n—NHR21 or —SO2R22;
- R21 is an optionally substituted (C1-C6)alkyl, —SO2R23 or —C(O)R24;
- R22, R23 and R24 are each independently an optionally substituted (C1-C6)alkyl or an optionally substituted amino;
- and
- n is 0, 1, 2 or 3.
6 more elements
A compound of formula (IV):
- or a pharmaceutically acceptable form thereof,
- wherein:
- R25 is hydrogen, halogen, or an optionally substituted (C1-C6)alkyl;
- R26 is hydrogen, —C(O)NH2, —(CH2)n—NHR27 or —SO2R28;
- R27 is an optionally substituted (C1-C6)alkyl, —SO2R29 or —C(O)R30;
- R28, R29 and R30 are each independently an optionally substituted (C1-C6)alkyl or an optionally substituted amino;
- and
- n is 0, 1, 2 or 3.
5 more elements
Dependencies are inferred from the claim text.