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US 2015/0307473 A1Published application
Therapeutic compounds and compositions and their use as pkm2 modulators
AssigneeAgios Pharmaceuticals, Inc.
InventorsGiovanni Cianchetta, Janeta Popovici-Muller, Jeffrey O. Saunders, Robert Zahler
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Abstract
Compositions comprising compounds of general formula (I) that modulate pyruvate kinase are described herein. Also described herein are methods of using the compounds that modulate pyruvate kinase in the treatment of diseases.
Claims28
A compound of Formula (I):
- or a pharmaceutically acceptable salt thereof, wherein:
- A is aryl or heteroaryl, wherein the aryl or heteroaryl is optionally substituted, and the aryl or heteroaryl is optionally fused to an optionally substituted carbocyclyl or an optionally substituted heterocyclyl;
- X is selected from —NH—S(O)2—, —N(alkyl)-S(O)2—, —S(O)2—NH— and —S(O)2—N(alkyl)-;
- R1b is C2-8 alkyl, cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl or heteroaralkyl, wherein each aryl is substituted and each C2-8 alkyl, cycloalkyl, cycloalkylalkyl, aralkyl, heteroaryl or heteroaralkyl is optionally substituted;
- each R2 is independently selected from halo and haloalkyl;
- each R4 is independently selected from alkyl, alkoxy, haloalkyl and hydroxyl;
- n is 0, 1 or 2;
- and
- m is 0, 1 or 2;
- wherein when R1b is unsubstituted benzyl, X is —NH—S(O)2— and A is quinolin-8-yl;
- then n is 1.
8 more elements
17-18. (canceled)
25-31. (canceled)
Dependencies are inferred from the claim text.