IP Library Granted Patent US 10,959,966
Granted Patent B2
US 10,959,966 · App. 15/115,132 · Granted Mar 30, 2021

Compositions and methods for modulating HEXM1 expression

Inventors: Bin Su (Cleveland, OH); Monica M. Montano (Cleveland, OH)
Assignee: CASE WESTERN RESERVE UNIVERSITY
A61K31/18A61K31/16A61K45/06
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Quick Facts
Patent No.
US 10,959,966
App. No.
15/115,132
Granted
Mar 30, 2021
Kind
B2
Abstract

The potency of a series of Hexamethylene bis-acetamide (HMBA) derivatives of formula I, that induce Hexamethylene bis-acetamide inducible protein 1 (HEXIM1) was determined in cancer cells. The method of inducing HEXIM1 expression and cell differentiation in cancer and HIV cells are disclosed. Optimization of HMBA analogs that are symmetrical and unsymmetrical are also discussed.

Claims (9)

1. A method of inducing hexamethylene bis-acetamide inducible protein 1 (HEXIM1) expression in at least one of breast cancer cells and/or prostate cancer cells of a subject, comprising:

administering to the cancer cells of the subject a compound having the formula:

R 7 is selected from the group consisting of substituted or unsubstituted C 1 -C 24 alkyl, C 2 -C 24 alkenyl, C 2 -C 24 alkynyl, C 3 -C 20 aryl, heterocycloalkenyl containing from 5-6 ring atoms, heteroaryl or heterocyclyl containing from 5-14 ring atoms, C 6 -C 24 alkaryl, C 6 -C 24 aralkyl, C 1 -C 24 alkoxy, C 2 -C 24 alkenyloxy, C 2 -C 24 alkynyloxy, C 5 -C 20 aryloxy, acyl, acyloxy, and (—O-acyl);

R 8 is a linear or branched C 1 -C 12 alkyl group; and pharmaceutically acceptable salts thereof.

2. The method of claim 1 , wherein the compound is administered in vitro, in vivo and/or ex vivo to the breast cancer cells and/or prostate cancer cells of the subject.

3. The method of claim 1 , wherein the compound has the formula:

wherein n 1 is 1-7,

R 9 is an electron donating or withdrawing group selected from the group consisting of OH, OMe, OAc, CN, NO 2 , halo, —(CH 2 )n 3 CH 3 (n 2 =0-7), phenyl, benzyl, SO 2 , SO 3 , alkylsulfonyl, amine, alkylamino, and carboxyl, and pharmaceutically acceptable salts thereof.

4. The method of claim 1 , wherein the compound has the formula:

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 23, 2021
From: MONTANO, MONICA M.
To: CASE WESTERN RESERVE UNIVERSITY
Reel/Frame 056957/0762 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 23, 2021
From: SU, BIN
To: CLEVELAND STATE UNIVERSITY
Reel/Frame 056957/0806 →
CONFIRMATORY LICENSE Recorded Oct 20, 2016
From: CASE WESTERN RESERVE UNIVERSITY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 040436/0555 →
Continuity (2)
Provisional Application 61933370 · Jan 30, 2014
Related Publication 20160346236A1 · Dec 1, 2016
Cited By (1)
US 12,441,707