HDAC inhibitors and therapeutic methods using the same

Patent metadata

Field	Value
Publication number	US-10836733-B2
Application number	US-201615756086-A
Country	US
Kind code	B2
Filing date	Aug 31, 2016
Priority date	Sep 3, 2015
Publication date	Nov 17, 2020
Grant date	Nov 17, 2020

Abstract

Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.

First claim

What is claimed:

1. A compound having a formula:

wherein A is selected from the group consisting

of —C(═O)NHheteroaryl, —NHC(═O)heteroaryl, aryl, heteroaryl, and

wherein B and C are, independently, aryl or heterocyclyl and n is 2 or 3;
or a pharmaceutically acceptable salt thereof.

2. A compound having a formula:

wherein A is selected from the group consisting

of —NHC(═O)alkyl, —NHC(═O)cycloalkyl, —NHC(═O)heteroaryl, aryl, and heteroaryl,
n is 0 or 1; and
p is 0 or 1,
or a pharmaceutically acceptable salt thereof.

3. A compound having a structure selected from the group consisting of

wherein Boc is tert-butoxycarbonyl; and Bz is benzoyl.

4. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier or vehicle.

5. A compound of claim 1 wherein the compound is labeled with a fluorescent dye, a radioisotope selected from 3 H, 11 C, 18 F, 123 I, 125 I, and 131 I, a molecular tag, or a mixture thereof.

6. The compound of claim 1 wherein A is —NHC(═O) heteroaryl.

7. The compound of claim 6 wherein heteroaryl is oxazolyl.

8. The compound of claim 1 having the formula

Assignees

• Univ Illinois

Inventors

• Kozikowski Alan
• Gaisina Irina

Classifications

• A61K31/4155

  non condensed and containing further heterocyclic rings · CPC title

• C07D261/10 Primary

  with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms · CPC title

• Y02A50/30

  Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change · CPC title

• C07D413/12

  linked by a chain containing hetero atoms as chain links · CPC title

• A61K31/427

  not condensed and containing further heterocyclic rings · CPC title