IP Library Granted Patent US 10,980,755
Granted Patent B2
US 10,980,755 · App. 15/758,549 · Granted Apr 20, 2021

LRH-1 modulators

Inventors: Pamela M. England (San Francisco, CA); Felipe de Jesus Cortez (San Francisco, CA)
Assignee: The Regents of the University of California
A61K31/166A61K31/381A61K31/40A61K31/415A61K31/4418A61P3/10A61P9/00A61P29/00A61P35/00C07C235/60C07C311/29C07C317/46C07D207/337C07D213/56C07D231/12C07D333/22C07D333/24
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Quick Facts
Patent No.
US 10,980,755
App. No.
15/758,549
Granted
Apr 20, 2021
Kind
B2
Abstract

Disclosed herein are compositions and methods for modulating the liver receptor homolog-1.

Claims (25)

1. A compound having the formula:

wherein

W 1 and W 2 are independently CH or N;

L 1 is C(O)NH—, —NHC(O)—,

or —NHC(NH)NH;

R 1 is

unsubstituted alkyl;

R 2 is unsubstituted tert-butyl;

R 3 is unsubstituted tert-butyl;

R 4 is —OR 22 ;

R 22 is hydrogen,

halogen, —CX 3 , —CHX 2 , —CH 2 X, —OCX 3 , —OCH 2 X, —OCHX 2 , —CN, —OH, —NH 2 , —COOH, —CONH 2 , —NO 2 , —SH, —SO 3 H, —SO 4 H, —SO 2 NH 2 , —NHNH 2 , —ONH 2 , —NHC═(O)NHNH 2 , —NHC═(O) NH 2 , —NHSO 2 H, —NHC═(O)H, —NHC(O)—OH, —NHOH, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;

X is —Cl, —Br, —I, or —F;

wherein R 1 is not unsubstituted methyl or unsubstituted tert-butyl; and

wherein the compound does not have the formula

2. The compound of claim 1 , wherein

R 1 is unsubstituted C 1 -C 8 alkyl.

3. The compound of claim 1 , having the formula:

4. The compound of claim 1 , wherein R 1 is unsubstituted C 1 -C 6 alkyl.

5. The compound of claim 1 , wherein R 4 is —OH.

6. The compound of claim 1 , wherein R 1 is unsubstituted butyl, unsubstituted pentyl, or unsubstituted hexyl.

7. The compound of claim 1 , wherein R 1 is unsubstituted C 3 -C 5 alkyl.

8. The compound of claim 1 , wherein R 1 is unsubstituted n-butyl.

9. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.

10. The compound of claim 1 , having the formula

Continuity (3)
Provisional Application 62216950 · Sep 10, 2015
Provisional Application 62217343 · Sep 11, 2015
Related Publication 20180243245A1 · Aug 30, 2018