IP Library › Granted Patent US 10,202,343
Granted Patent B2
US 10,202,343 · App. 15/656,555 · Granted Feb 12, 2019

MIF modulators

Inventors: William L. Jorgensen (Deep River, CT); Richard J. Bucala (Cos Cob, CT)
Assignee: Yale University
C07D209/18C07D235/12C07D235/24C07D249/06C07D263/58C07D275/04C07D307/80C07D307/83C07D401/04C07D401/06C07D403/04C07D405/06C07D413/04C07D417/04
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Quick Facts
Patent No.
US 10,202,343
App. No.
15/656,555
Granted
Feb 12, 2019
Kind
B2
Abstract

The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression.

Claims (12)

1. A compound of formula:

wherein:

R 5 , R 6 , R o , R m , and R p are each independently selected from the group consisting of H, OH, COOH, halogen, CN, OH, optionally substituted C 1 -C 8 alkyl, optionally substituted C 2 -C 8 alkenyl, optionally substituted C 2 -C 8 alkynyl, optionally substituted O—(C 1 -C 8 alkyl), optionally substituted O—(C 2 -C 8 alkenyl), optionally substituted O—(C 2 -C 8 alkynyl), SH, S -(C 1 -C 6 )alkyl, optionally substituted C 1 -C 8 acyl, optionally substituted C 2 -C 8 ether, optionally substituted C 2 -C 8 ester or carboxyester, optionally substituted C 2 -C 8 thioester, amide optionally substituted with one C 1 -C 6 alkyl, carboxyamide optionally substituted with one or two substituents independently selected from the group consisting of C 1 -C 6 alkyl and C 1 -C 6 alkanol, amine optionally substituted with one or two substituents independently selected from the group consisting of C 1 -C 6 alkyl and C 1 -C 6 alkanol, optionally substituted (CH 2 ) j -phenyl, optionally substituted (CH 2 ) m -heterocyclyl, optionally substituted —O—(CH 2 ) j -phenyl, and optionally substituted —O—(CH 2 ) m -heterocyclyl;

provided that at least one selected from the group consisting of R o , R m , and R p is selected from the group consisting of OH, optionally substituted O—(C 1 -C 8 alkyl), optionally substituted O—(C 2 -C 8 alkenyl), and optionally substituted O—(C 2 -C 8 alkynyl),

each j is independently 0, 1, 2, 3, 4 or 5; and

each m is independently 0, 1, 2, 3, 4, or 5;

or a pharmaceutically acceptable salt, stereoisomer, solvate or polymorph thereof.

2. The compound of claim 1 , or a pharmaceutically acceptable salt, stereoisomer, solvate or polymorph thereof, wherein:

R 5 and R 6 are each independently selected from the group consisting of H, halogen, CN, optionally substituted C 1 -C 8 alkyl, optionally substituted C 1 -C 8 alkenyl, optionally substituted C 1 -C 8 alkynyl, optionally substituted O—(C 1 -C 8 alkyl), optionally substituted O—(C 2 -C 8 alkenyl), and optionally substituted O—(C 2 -C 8 alkynyl); and

R o , R m , and R p are each independently selected from the group consisting of H, OH, halogen, CN, optionally substituted C 1 -C 8 alkyl, optionally substituted C 1 -C 8 alkenyl, optionally substituted C 1 -C 8 alkynyl, optionally substituted O—(C 1 -C 8 alkyl), optionally substituted O—(C 2 -C 8 alkenyl), optionally substituted O—(C 2 -C 8 alkynyl), optionally substituted C 1 -C 8 acyl, optionally substituted C 2 -C 8 ether, optionally substituted (CH 2 ) j -phenyl, optionally substituted (CH 2 ) m -heterocyclyl, optionally substituted —O—(CH 2 ) j -phenyl, and optionally substituted —O—(CH 2 ) m -heterocyclyl.

3. A compound selected from the group consisting of:

or a pharmaceutically acceptable salt, stereoisomer, solvate, or polymorph thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 17, 2018
From: JORGENSEN, WILLIAM L.; BUCALA, RICHARD J.
To: YALE UNIVERSITY
Reel/Frame 047794/0323 →
Continuity (6)
Continuation 15401967 · Jan 9, 2017
Continuation 13100922 · May 4, 2011
Continuation In Part 12773430 · May 4, 2010
Continuation In Part PCTUS2009004704 · Aug 18, 2009
Provisional Application 61189327 · Aug 18, 2008
Related Publication 20180162813A1 · Jun 14, 2018
Cited By (8)
US 12,187,743 US 12,247,026 US 12,247,038 US 12,378,229 US 12,404,272 US 12,466,822 US 12,516,044 US 12,617,777