IP Library Granted Patent US 8,153,659
Granted Patent B2
US 8,153,659 · App. 12/077,715 · Granted Apr 10, 2012

4′-O-substituted isoindoline derivatives and compositions comprising and methods of using the same

Assignee: Celgene Corporation
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Quick Facts
Patent No.
US 8,153,659
App. No.
12/077,715
Granted
Apr 10, 2012
Kind
B2
Abstract

Provided are 4′-O substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.

Claims (28)

1. A compound of formula:

or a pharmaceutically acceptable salt or stereoisomer thereof, wherein:

Y is C=O or CH 2 ; and

R 1 is heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl, heteroarylcarbonyl or heterocyclylcarbonyl;

and where R 1 is optionally substituted with one or more groups selected from alkoxy, halo, alkyl, carboxy, alkylaminocarbonyl, alkoxycarbonyl, nitro, amine, nitrile, haloalkyl, hydroxy, and alkylsulfonyl.

2. The compound of claim 1 , wherein Y is C=O.

3. The compound of claim 1 , wherein Y is CH 2 .

4. The compound of claim 1 , wherein R 1 is heteroarylalkyl.

5. The compound of claim 1 , wherein the aryl group in R 1 is a 5 or 6 membered monocyclic heteroaryl group containing 1-3 heteroatoms selected from O, N and S.

6. The compound of claim 1 , wherein the heteroayl group in R 1 is a bicyclic heteroaryl group.

7. The compound of claim 1 , wherein R 1 is substituted with one or more substituents selected from alkoxy, halo, alkyl and alkylsulfonyl.

8. The compound of claim 1 , wherein R 1 substituted with one or two substituents selected from methoxy, chloro, bromo, fluoro, methyl and methylsulfonyl.

9. The compound of claim 1 , wherein R 1 is substituted with one or more substituents selected from nitro, amino, haloalkyl, nitrile, or hydroxy.

10. The compound of claim 1 , wherein R 1 is quinolymethyl benzofurylmethyl, benzothienylmethyl, furylmethyl or thienylmethyl.

11. The compound of claim 1 , wherein R 1 is 3 -quinolylmethyl, 2-quinolylmethyl, 2-benzofurylmethyl, 2-benzothienylmethyl, 3-chlorothien-2-ylmethyl, 4-fluorobenzothien-2-ylmethyl, 2-furylmethyl, or 5-chlorothien-2-ylmethyl.

12. The compound of claim 1 , wherein the compound has formula:

and wherein R 5 is heteroaryl, optionally substituted with one, two or three groups seleted from alkyl, halo, alkoxy, carboxy, alkylaminocarbonyl, alkoxycarbonyl, nitro, amine, nitrile, haloalkyl, hydroxy, and alkylsulfonyl; and n 1 is 0-5.

13. The compound of claim 12 , wherein R 5 is selected from furyl, thienyl, benzofuryl, benzothienyl and quinolyl, optionally substituted with one or two groups selected from methyl, methoxy, chloro, fluoro, bromo and methylsulfonyl.

14. The compound of claim 12 , wherein the compound has formula

15. The compound of claim 1 , selected from:

and pharmaceutically acceptable salts or stereoisomers thereof.

16. The compound of claim 1 , selected from:

and pharmaceutically acceptable salts or stereoisomers thereof.

17. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt or stereoisomer thereof.

18. A single unit dosage form comprising a compound of claim 1 , or a pharmaceutically acceptable salt or stereoisomer thereof.

19. The single unit dosage form of claim 18 , which is suitable for oral or parenteral administration.

20. The single unit dosage form of claim 19 , which is suitable for oral administration.

21. The single unit dosage form of claim 20 , which is a tablet or a capsule.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 18, 2017
From: CHEN, ROGER SHEN-CHU
To: CELGENE CORPORATION
Reel/Frame 044425/0995 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 12, 2008
From: RUCHELMAN, ALEXANDER L.; MULLER, GEORGE W.; MAN, HON-WAH
To: CELGENE CORPORATION
Reel/Frame 021526/0387 →
Continuity (2)
Provisional Application 60919323 · Mar 20, 2007
Related Publication 20090004209A1 · Jan 1, 2009