Modulators of nuclear receptor subfamily 4 group A member 1 (NR4A1) and uses thereof
Modulators of Nuclear Receptor Subfamily 4 Group A Member 1 (NR4A1) are described as well as their use as therapeutic agents for disease, disorders, or symptoms thereof, including those where modulation of NR4A1 is implicated. Such disease and disorders include cancer.
1 . A compound of Formula (I), or a pharmaceutically acceptable salt thereof:
wherein L is C 4-8 alkylene or C 4-9 heteroalkylene, wherein the heteroatoms in C 4-9 heteroalkylene are 1-4 oxygen atoms; and
X is
2 . The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein X is
3 . The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein X is
4 . The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein L is C 4-8 alkylene.
5 . The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein L is C 4-9 heteroalkylene.
6 . The compound of claim 1 , wherein the compound has the formula:
or a pharmaceutically acceptable salt thereof.
7 . The compound of claim 6 , wherein the compound is of the formula:
or a pharmaceutically acceptable salt thereof.
8 . The compound of claim 6 , wherein the compound is of the formula:
or a pharmaceutically acceptable salt thereof.
9 . The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein L is straight-chained C 4-8 alkylene.
10 . The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein L is straight-chained C 4-9 heteroalkylene.
11 . A pharmaceutical composition comprising an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable carrier, and a pharmaceutically acceptable adjuvant.
12 . The pharmaceutical composition of claim 11 , further comprising an additional anti-cancer agent.
13 . A method of treating cancer in a subject in need thereof, comprising administration of a compound of claim 1 , or a pharmaceutically acceptable salt thereof, to the subject in need thereof, wherein the cancer is breast cancer, colon cancer, melanoma, renal cell cancer, endometrial cancer, or lung cancer.
14 . The method of claim 13 , wherein the cancer is colon cancer.
15 . The method of claim 13 , wherein the cancer is breast cancer.
16 . The method of claim 13 , further comprising administration of an additional anti-cancer agent to the subject in need thereof.
17 . The method of claim 13 , wherein the cancer is melanoma.
18 . The method of claim 13 , wherein the cancer is renal cell cancer, endometrial cancer, or lung cancer.
19 . The method of claim 13 , wherein the subject is a human.