IP Library Granted Patent US 9,751,832
Granted Patent B2
US 9,751,832 · App. 14/907,321 · Granted Sep 5, 2017

Selective histone deactylase 6 inhibitors

Inventors: Eduardo M. Sotomayor (Tampa, FL); Joel A. Bergman (Chicago, IL); Alan P. Kozikowski (Chicago, IL); Alejandro V. Villagra (Tampa, FL); Karrune V. Woan (Gainesville, FL)
Assignees: H. Lee Moffitt Cancer Center and Research Institute, Inc.; Board of Trustees of the University of Illinois
C07C275/34A61K31/17A61K31/185A61K31/4045A61K31/416A61K31/42A61K31/437A61K31/44A61K31/505A61K45/06C07C275/28C07C275/40C07D209/14C07D213/75C07D231/56C07D233/26C07D233/74C07D233/78C07D239/42C07D261/14C07D295/13
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Quick Facts
Patent No.
US 9,751,832
App. No.
14/907,321
Granted
Sep 5, 2017
Kind
B2
Abstract

Disclosed are selective histone deactylase inhibitors (HDACi) that having Formula I. Specifically, the disclosed subject matter relates to compounds having activity as selective HDAC6 inhibitors, methods of making and using the compounds, and compositions comprising the compounds. In still further aspects, the disclosed subject matter relates to methods for treating oncological disorders in a patient. Methods of making and using these inhibitors for the treatment of cancer, in particular melanoma are also disclosed.

Claims (12)

1. A compound having Formula I:

wherein

A is aryl, heteroaryl, or C 1 -C 8 alkyl, any of which is optionally substituted with one or more groups chosen from acetyl, C 1 -C 5 alkyl, amino, —NR 6 R 7 , —C(O)NR 6 R 7 , C 1 -C 4 alkoxy, C 1 -C 4 alkylhydroxy, C 5 -C 6 cycloalkyl, C 5 -C 6 heterocycloalkyl, aryl, heteroaryl, halo, hydroxy, thiol, cyano, or nitro; and

R 1 is hydrogen and R 2 is C 1 -C 8 alkyl, C 1 -C 8 alkenyl, C 1 -C 8 alkynyl, C 1 -C 8 haloalkyl, C 5 -C 6 cycloalkyl, C 5 -C 6 heterocycloalkyl, C 1 -C 3 alkylaryl, aryl, C 1 -C 3 alkylheteroaryl, or heteroaryl, any of which is optionally substituted with acetyl, C 1 -C 5 alkyl, amino, —NR 6 R 7 , —C(O)NR 6 R 7 , C 1 -C 4 alkoxy, C 1 -C 4 alkylhydroxy, C 5 -C 6 cycloalkyl, C 5 -C 6 heterocycloalkyl, aryl, heteroaryl, carbonyl, halo, hydroxy, thiol, cyano, or nitro; and

R 6 and R 7 are independently H, C 1 -C 4 alkyl, or are joined such that together they form an alkylene bridge comprising 4 or 5 atoms so that a 5 or 6-membered ring is formed with the nitrogen;

or a pharmaceutically acceptable salt or hydrate thereof.

2. The compound of claim 1 , wherein A is phenyl, pyridyl, oxazolidyl, pyrimidyl, pyrimidinyl, or 1H-indazolyl, optionally substituted with C 1 -C 5 alkyl, amino, alkoxy, alkylhydroxy, halo, hydroxy, or thiol.

3. The compound of claim 1 , wherein A is pyrimidinyl or 1H-indazolyl substituted with C 1 -C 5 alkyl, C 1 -C 4 alkoxyl, or halo.

4. The compound of claim 1 , wherein R 2 is C 1 -C 8 alkyl, C 5 -C 6 cycloalkyl, C 5 -C 6 heterocycloalkyl, aryl, or heteroaryl, any of which is optionally substituted with C 1 -C 5 alkyl, amino, —NR 6 R 7 , C 1 -C 4 alkoxy, C 1 -C 4 alkylhydroxy, carbonyl, hydroxy, thiol, or cyano.

5. The compound of claim 1 , wherein R 2 is C 1 -C 5 alkyl, or C 1 -C 5 alkyl substituted with a methoxy, amino, —NR 6 R 7 , alkylhydroxy, carbonyl, hydroxy, cyano.

6. The compound of claim 1 , wherein R 2 is C 1 -C 4 alkyl.

7. The compound of claim 1 , wherein the compound is chosen from:

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 3, 2018
From: BERGMAN, JOEL; KOZIKOWSKI, ALAN
To: BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
Reel/Frame 044981/0967 →
CONFIRMATORY LICENSE Recorded Apr 17, 2017
From: H. LEE MOFFITT CANCER CTR & RES INST
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 042276/0313 →
Continuity (2)
Provisional Application 61860035 · Jul 30, 2013
Related Publication 20160185716A1 · Jun 30, 2016