IP Library › Granted Patent US 9,512,083
Granted Patent B2
US 9,512,083 · App. 14/233,228 · Granted Dec 6, 2016

Histone deacetylase 6 selective inhibitors for the treatment of bone disease

Inventors: Noopur Raje (Newton, MA); Loredana Santo (Cambridge, MA)
Assignee: The General Hospital Corporation
C07D239/42A61K31/505A61K38/05A61K45/06C07C259/06
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Quick Facts
Patent No.
US 9,512,083
App. No.
14/233,228
Granted
Dec 6, 2016
Kind
B2
Abstract

This invention relates to methods for treating bone disease associated with osteoclast activation using HDAC6 selective inhibitors, e.g., small molecule inhibitors such as reverse amide compounds.

Claims (9)

1. A method of treating, or reducing risk of, osteoporosis associated with abnormally high bone catabolism in a subject, the method comprising administering to the subject a therapeutically effective amount of a reverse amide compound of formula IVa:

or a pharmaceutically acceptable salt thereof, wherein, ring B is phenyl;

R 1 is phenyl, which may be optionally substituted by OH or halo; and

R is H or C1-8-alkyl.

2. The method of claim 1 , wherein the reverse amide compound is 2-(diphenylamino)-N-(7-(hydroxyamino)-7-oxoheptyl)pyrimidine-5-carboxamide, (Compound A):

3. The method of claim 1 , wherein the abnormally high bone catabolism is associated with increased osteoclastogenesis in the subject, decreased osteoblastogenesis in the subject, increased osteoclast activity in the subject, decreased osteoblast activity in the subject, an imbalance of osteoclastogenesis and osteoblastogenesis in the subject, or an imbalance of osteoclast and osteoblast activity in the subject.

4. The method of claim 1 , further comprising administering an additional active agent selected from the group consisting of bisphosphates, RANK ligands, bortezomib, Carfilzomib, lenalidomide, and Pomalidomide.

5. The method of claim 1 , wherein the methods further include administering a bisphosphate.

6. The method of claim 1 , wherein the reverse amide compound is 2-((2-chlorophenyl)(phenyl)amino)-N-(7-(hydroxyamino)-7-oxoheptyl)pyrimidine-5-carboxamide, (Compound C):

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 23, 2014
From: RAJE, NOOPUR; SANTO, LOREDANA
To: THE GENERAL HOSPITAL CORPORATION
Reel/Frame 032733/0818 →
Continuity (1)
Related Publication 20140378385A1 · Dec 25, 2014