IP Library Granted Patent US 8,026,371
Granted Patent B2
US 8,026,371 · App. 12/896,535 · Granted Sep 27, 2011

Hydroxamates as therapeutic agents

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Quick Facts
Patent No.
US 8,026,371
App. No.
12/896,535
Granted
Sep 27, 2011
Kind
B2
Abstract

The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.

Claims (20)

1. A compound of Formula (I):

wherein:

R 1 is hydrogen or alkyl;

X is —O—, —NR 2 —, or —S(O) n where n is 0-2 and R 2 is hydrogen or alkyl;

Y is alkylene optionally substituted with cycloalkyl, optionally substituted phenyl, alkylthio, alkylsulfinyl, alkysulfonyl, optionally substituted phenylalkylthio, optionally substituted phenylalkylsulfonyl, hydroxyl, or optionally substituted phenoxy;

Ar 1 is phenylene or heteroarylene wherein said Ar 1 is optionally substituted with one or two groups independently selected from alkyl, halo, hydroxyl, alkoxy, haloalkoxy, or haloalkyl;

R 3 is hydrogen, alkyl, hydroxyalkyl, or optionally substituted phenyl; and

Ar 2 is benzoxazol-2-yl; wherein benzoxazol-2-yl is optionally substituted with one or two substituents independently selected from alkyl, halo, haloalkyl, alkoxy, alkoxyalkyl, hydroxyalkoxy, hydroxyalkoxyalkyl, alkoxyalkyloxy, alkoxyalkyloxyalkyl, aminoalkyl, aminoalkoxy, haloalkoxy, haloalkoxyalkyl, optionally substituted phenylalkyl, optionally substituted phenyloxyalkyl, optionally substituted heteroaryl, optionally substituted heteroaralkyloxy, optionally substituted heteroaryloxyalkyl, optionally substituted heterocycloalkylalkyl, optionally substituted heterocycloalkyloxy, optionally substituted heterocycloalkylalkyloxy, -alkylene-S(O)nR a (where n is 0 to 2 and R a is hydroxyalkyl or optionally substituted phenyl), -alkylene-NR e -alkyleneCONR e R d (where R e is hydroxyl and R d and R e are independently hydrogen or alkyl), or carboxyalkylaminoalkyl; or

a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 wherein R 1 is hydrogen.

3. The compound of claim 1 wherein Ar 1 is phenylene.

4. The compound of claim 1 wherein X is —O—.

5. The compound of claim 1 wherein Y is alkylene.

6. The compound of claim 5 wherein alkylene is —CH 2 CH 2 —.

7. The compound of claim 1 wherein R 3 is hydrogen.

8. The compound of claim 1 wherein Ar 2 is monosubstituted.

9. The compound of claim 8 wherein Ar 2 is monosubstituted with halo.

10. The compound of claim 9 wherein halo is Cl.

11. The compound of claim 9 wherein halo is F.

12. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 1 or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable excipient.

Assignments (5)
CORRECTIVE ASSIGNMENT TO CORRECT THE CONVEYING PARTY DATA PREVIOUSLY RECORDED ON REEL 036126 FRAME 0377. ASSIGNOR(S) HEREBY CONFIRMS THE MERGER. Recorded May 17, 2016
From: OXFORD AMHERST CORPORATION; PHARMACYCLICS, INC.
To: PHARMACYCLICS, INC.
Reel/Frame 038722/0776 →
CORRECTIVE ASSIGNMENT TO CORRECT THE CONVEYING PARTY DATA PREVIOUSLY RECORDED ON REEL 036126 FRAME 0398. ASSIGNOR(S) HEREBY CONFIRMS THE MERGER AND CHANGE OF NAME. Recorded May 17, 2016
From: PHARMACYCLICS, INC.; OXFORD AMHERST LLC
To: PHARMACYCLICS LLC
Reel/Frame 038722/0849 →
MERGER Recorded Jul 16, 2015
From: OXFORD AMHERST CORPORATION
To: PHARMACYCLICS, INC.
Reel/Frame 036126/0377 →
MERGER AND CHANGE OF NAME Recorded Jul 16, 2015
From: PHARMACYCLICS, INC.; OXFORD AMHERST LLC
To: PHARMACYCLICS LLC
Reel/Frame 036126/0398 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 10, 2010
From: VERNER, ERIK J.; SENDZIK, MARTIN; BASKARAN, CHITRA; BUGGY, JOSEPH J.; ROBINSON, JAMES
To: PHARMACYCLICS, INC.
Reel/Frame 025342/0558 →