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US 2017/0283401 A1Published application
Therapeutic compositions and related methods of use
AssigneeAgios Pharmaceuticals, Inc.
InventorsFrancesco G. Salituro, Jeffrey O. Saunders
Life of this patent
Estimating the term…
Abstract
Compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.
Claims20
A compound of Formula (IV) or pharmaceutically acceptable salt thereof, wherein:
- R1 (IV),
- X1 is N or CE;
- X2 is N or CD;
- X3 is N or CB;
- X4 is N or CA, wherein at least one of X, X2, X3 and X4 is N;
- and at least one of X1, X2, X3, X4, is C—SO2—NR4R5;
- A, B, D and E are each independently selected from H and —SO2—NR4R5;
- each R4 is independently selected from C1-8 alkyl, aryl and heteroaryl, each of which is substituted with n occurrences of R2;
- n is 0, 1, 2 or 3;
- each R5 is independently hydrogen or C1-8 alkyl;
- each R1 is independently selected from hydrogen, C1-8 alkyl, C1-8 alkoxy, halogen, haloalkyl and haloalkoxy;
- each R2 is independently selected from halo, haloalkyl, C1-4alkyl, C2-4 alkenyl, C2-4 alkynylheteroaryl, aryl, aralkyl, heteroaralkyl, cyano, —ORa, —COORb and —CONRcRc′;
- wherein two R2, together with the carbons to which they are attached, may form an optionally substituted ring, each of which can be further substituted;
- each R3 is independently selected from C1-8 alkyl, —ORa, halogen, haloalkyl, haloalkoxy or optionally substituted heteroaryl;
- Ra is independently selected from alkyl, haloalkyl, optionally substituted heteroaryl and optionally substituted heterocyclyl;
- each Rb is independently alkyl;
- and
- each Rc is independently selected from hydrogen and alkyl.
15 more elements
A compound of Formula (II) or pharmaceutically acceptable salt thereof, wherein:
- A, B, D and E are each independently selected from H, —SO2—NR4R5 and R3;
- wherein at least one of A, B, D, or E is —SO2—NR4R5;
- Y1, Y2, Y3 and Y4 are each independently selected from N and CR1, wherein at least one of Y1, Y2, Y3 and Y4 are N;
- each R4 is independently selected from C1-8 alkyl, aryl and heteroaryl, each of which is substituted with n occurrences of R2;
- each R5 is independently hydrogen or C1-8 alkyl;
- each R1 is independently selected from hydrogen, C1-8 alkyl, C1-8 terminal alkynyl, C1-8 alkoxy, halogen, haloalkyl and haloalkoxy;
- each R2 is independently selected from halo, haloalkyl, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, aryl, heteroaryl, aralkyl, heteroaralkyl, cyano, —ORa, —COORb and —CONRcRc′;
- wherein two R2, together with the carbons to which they are attached, may form an optionally substituted ring, each of which can be further substituted;
- each R3 is independently selected from C1-8 alkyl, —ORa, halogen, haloalkyl, haloalkoxy and optionally substituted heteroaryl;
- each Ra is independently selected from alkyl, haloalkyl, optionally substituted heteroaryl and optionally substituted heterocyclyl;
- each Rb is independently alkyl;
- each Rc is independently selected from hydrogen and alkyl;
- and
- n is 0, 1, 2 or 3.
11 more elements
Dependencies are inferred from the claim text.