IP Library Granted Patent US 8,796,330
Granted Patent B2
US 8,796,330 · App. 11/959,204 · Granted Aug 5, 2014

Inhibitors of histone deacetylase and prodrugs thereof

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Quick Facts
Patent No.
US 8,796,330
App. No.
11/959,204
Granted
Aug 5, 2014
Kind
B2
Abstract

The invention relates to the inhibition of histone deacetylase. The invention provides compounds, prodrugs thereof, and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.

Claims (21)

1. A compound selected from the group consisting of

N-(1-aminocyclopropanecarbonyloxy)-2-(4-(4-phenylbutyl)phenyl)acetamide hydrochloride;

(S)-N-(2-amino-3-phenylpropanoyloxy)-2-(4-(4-phenylbutyl)phenyl)acetamide hydrochloride;

(S)-N-(2-amino-3-methylbutanoyloxy)-2-(4-(4-phenylbutyl)phenyl)acetamide hydrochloride;

(S)-N-(2-amino-3,3-dimethylbutanoyloxy)-2-(4-(4-phenylbutyl)phenyl)acetamide hydrochloride;

N-(1-aminocyclobutanecarbonyloxy)-2-(4-(4-phenylbutyl)phenyl)acetamide hydrochloride;

N-(2-amino-2-methylpropanoyloxy)-2-(4-(4-phenylbutyl)phenyl)acetamide hydrochloride;

N-(1-(aminomethyl)cyclopropanecarbonyloxy)-2-(4-(4-phenylbutyl)phenyl)acetamide hydrochloride;

(S)-N-(2,6-diaminohexanoyloxy)-2-(4-(4-phenylbutyl)phenyl)acetamide;

N-(2-hydroxyacetoxy)-2-(4-(4-phenylbutyl)phenyl)acetamide;

(S)-N-(2-amino-5-guanidinopentanoyloxy)-2-(4-(4-phenylbutyl)phenyl)acetamide;

(S)-2,6-diamino-N-(1-((2-(4-(4-phenylbutyl)phenyl)acetamidooxy)carbonyl)cyclopropyl)hexanamide;

N-(1-((2-(4-(4-phenylbutyl)phenyl)acetamidooxy)carbonyl)cyclopropyl)nicotinamide;

(S)-2-amino-3-methyl-N-(1-((2-(4-(4-phenylbutyl)phenyl)acetamidooxy)carbonyl)cyclopropyl)butanamide;

(S)-2-amino-3-phenyl-N-(1-((2-(4-(4-phenylbutyl)phenyl)acetamidooxy)carbonyl)cyclopropyl)propanamide;

2-(4-(4-phenylbutyl)phenyl)-N-((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yloxy)acetamide; and

N-(2,3-dihydroxypropanoyloxy)-2-(4-(4-phenylbutyl)phenyl)acetamide.

2. A pharmaceutically acceptable salt of a species selected from the group consisting of

1-methyl-3-(3-oxo-3-(2-(4-(4-phenylbutyl)phenyl)acetamidooxy)propyl)pyridinium, 1-methyl-4-(3-oxo-3-(2-(4-(4-phenylbutyl)phenyl)acetamidooxy)propyl)-4H-1,2,4-triazol-1-ium, and

1-methyl-3-((2-(4-(4-phenylbutyl)phenyl)acetamidooxy)carbonyl)pyridinium.

3. A composition comprising a pharmaceutically acceptable salt of claim 1 .

Assignments (4)
CHANGE OF NAME Recorded Oct 27, 2010
From: METHYLGENE, INC.
To: 92229129 QUEBEC INC.
Reel/Frame 025200/0827 →
MERGER Recorded Oct 27, 2010
From: 7503547 CANADA INC.
To: METHYLGENE, INC.
Reel/Frame 025201/0647 →
CHANGE OF NAME Recorded Oct 19, 2010
From: 922209129 QUEBEC INC., (FORMERLY "METHYLGENE, INC.")
To: 7503547 CANADA, INC.
Reel/Frame 025159/0476 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 11, 2008
From: DEZIEL, ROBERT; AJAMIAN, ALAIN
To: METHYLGENE INC.
Reel/Frame 020354/0788 →