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US 2022/0024876 A1Published application
Small molecule inhibition of sulfotransferase sult1a3
AssigneesUniversity of Pittsburgh—Of the Commonwealth System of Higher Education, Albert Einstein College of Medicine
InventorsAlexander Deiters, Kristie E. Darrah, Mary Frances Cacace, Ian Cook, Thomas Leyh, Ting Wang
Life of this patent
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Abstract
Provided herein are small molecule compounds and methods inhibiting human sulfotransferase 1A3 (SULT1A3) using these small molecule compounds. Methods of manufacturing and treatment are also disclosed.
Claims30
A compound having the structure of formula (I):
- or a pharmaceutically acceptable salt thereof, wherein:
- A and B are fused rings, each independently an aryl or heteroaryl ring;
- X is selected from a bond and an optionally substituted alkyl, alkene or alkyne;
- Y is selected from —OR′, —NR′2, —OCON′R′2, —SO2R′, —NR′SO2R′, —NR′COR′, —NR′SO2NR′2, —COOR′, —NR′COOR′, —NR′CONR′2, and —NRC(NR′)NR′2, optionally substituted heteroaryl, and optionally substituted heterocycle;
- R′ is H or an optionally substituted alkyl, alkene or alkyne;
- Z is independently selected from H, optionally substituted alkyl, alkene or alkyne, and —X—Y,
- wherein two Z can together form an optionally substituted cycloalkyl, heterocycle, aryl, or heteroaryl;
- and
- a is 0 or an integer of 1-4,
- wherein the compound binds to an allosteric CMP8-binding site of SULT1A3.
7 more elements
A compound having the structure of formula (II):
- or a pharmaceutically acceptable salt thereof, wherein:
- X is selected from a —C0-C6 alkyl or a —C2-C6 alkene;
- Y is selected from —OR′, —COOR′, —CONR′2, and heteroaryl;
- R′ is H or C1-C6 alkyl;
- Z1 is selected from H and —OR′;
- and
- Z2 is selected from H, —C1-C6 alkyl, and —C0-C6—COOR′, or
- Z1 and Z2 together form a substituted cycloalkyl,
- wherein when Z1 and Z2 are both H, then Y is heteroaryl, and
- wherein the compound binds to an allosteric CMP8-binding site of SULT1A3.
7 more elements
A compound having the structure of formula (III):
- or a pharmaceutically acceptable salt thereof, wherein:
- A and B are each N or CH, and at least one of A and B is N;
- X is selected from a —C0-C6 alkylene or a —C2-C6 alkene;
- Y is selected from —OR′, —COOR′, —CONR′2, and heteroaryl;
- R′ is selected from H, alkyl, alkenyl, alkynyl, and aryl;
- Z1 is selected from H and —OR′;
- and
- Z2 is selected from H, —C1-C6 alkyl, and —C0-C6—COOR′, or
- Z1 and Z2 together form a substituted cycloalkyl,
- wherein when Z1 and Z2 are not both H.
7 more elements
Dependencies are inferred from the claim text.