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US 2020/0062693 A1Published application
Small molecule ampk activators
AssigneesUniversity of Pittsburgh—Of the Commonwealth System of Higher Education, The United States AS Represented By the Department of Veterans Affairs
InventorsBeibei CHEN, Rama K. MALLAMPALLI, Yuan LIU
Life of this patent
Estimating the term…
Abstract
Described herein are compounds that disrupt the interaction between Fbxo48 and phosphorylated-AMPK.
Claims22
A compound of Formula I:
- wherein:
- X is C0-3 alkyl, —(CH2)2—NH—(CH2)2—, —NH—CH2—, —O—CH2—, —O—(CH2)2—, —(CH2)2—O—(CH2)2—, or —(CH2)—C(NH2)—(CH2)a—;
- Z is C1-2 alkyl, —(CH2)—NH—(CH2)—, —(CH2)—O—(CH2)—, or —(CH2)a—C(NH2)—(CH2)—;
- a is 0 or 1;
- at least one of R1 and R2 is —(CHRA)b—Y, wherein each RA is independently H, or a substituted or unsubstituted aryl;
- and b is 0 or an integer of 1-3;
- the remaining one of R1 and R2 is —(CH2)c—Y or selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted carbocyclyl, and substituted or unsubstituted heterocyclyl;
- and c is 0 or an integer of 1-3;
- and
- each Y is independently a substituted or unsubstituted aryl;
- or
- R1 and R2, together with the nitrogen to which they are attached, form a substituted or unsubstituted heterocyclic ring;
- R3 is an alkyl, carbocyclyl, aryl, or heteroaryl group, wherein each alkyl, carbocyclyl, aryl, or heteroaryl group is optionally substituted by one or more
- wherein
- A is C═O, SO, SO2, or —(C(RB)2)d—, wherein each RB is independently selected from H, D, halogen, OH, substituted or unsubstituted alkyl, and substituted or unsubstituted alkoxy;
- d is 0 or an integer of 1-3;
- and
- B is selected from the group consisting of substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, and substituted or unsubstituted heteroaryl;
- or a stereoisomer thereof, or a pharmaceutically acceptable salt or ester thereof.
16 more elements
A compound of Formula II:
- wherein:
- X is C0-3 alkyl, —(CH2)2—NH—(CH2)2—, —O—CH2—, —O—(CH2)2—, —(CH2)2—O—(CH2)2—, or —(CH2)—C(NH2)—(CH2)a—;
- Z is C1-2 alkyl, —(CH2)—NH—(CH2)—, —(CH2)—O—(CH2)—, or —(CH2)a—C(NH2)—(CH2)—;
- a is 0 or 1;
- at least one of R1 and R2 is —(CHRA)b—Y, wherein each RA is independently H, or a substituted or unsubstituted aryl;
- and b is 0 or an integer of 1-3;
- the remaining one of R1 and R2 is —(CH2)c—Y or selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted carbocyclyl, and substituted or unsubstituted heterocyclyl;
- and c is 0 or an integer of 1-3;
- and
- each Y is independently a substituted or unsubstituted aryl;
- or
- R1 and R2, together with the nitrogen to which they are attached, form a substituted or unsubstituted heterocyclic ring;
- R3 is an aryl or heteroaryl group optionally substituted by one or more
- wherein
- A is C═O, SO, SO2, or —(C(RB)2)d—, wherein each RB is independently selected from H, D, halogen, OH, substituted or unsubstituted alkyl, and substituted or unsubstituted alkoxy;
- d is 0 or an integer of 1-3;
- and
- B is selected from the group consisting of C1-6 alkyl, haloalkyl, C1-6 alkoxy, substituted or unsubstituted aryl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, and substituted or unsubstituted heteroaryl;
- or a stereoisomer thereof, or a pharmaceutically acceptable salt or ester thereof.
16 more elements
20-47. (canceled)
49-55. (canceled)
Dependencies are inferred from the claim text.