Last Updated: November 9, 2026

Claims for Patent: 8,518,972

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Summary for Patent: 8,518,972
Title:Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same
Abstract:Provided are 4'-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.
Inventor(s):Hon-Wah Man, George W. Muller, Alexander L. Ruchelman, Ehab M. Khalil, Roger Shen-Chu Chen, Weihong Zhang
Assignee: Celgene Corp
Application Number:US13/025,105
Patent Claims: 1. A compound of formula (I): or a pharmaceutically acceptable salt or stereoisomer thereof, wherein: X is C═0 or CH2; R1 is —Y—R3; R2 is H or (C1-C6)alkyl; Y is: 6 to 10 membered aryl optionally substituted with one or more halogen; R3 is: —(CH2)n-aryl, —O—(CH2)n-aryl or —(CH2)n—O-aryl, wherein the aryl is optionally substituted with one or more: (C1-C6)alkyl, itself optionally substituted with one or more halogen; (C1-C6)alkoxy, itself substituted with one or more halogen; oxo; amino; carboxyl; cyano; hydroxyl; halogen; 6 to 10 membered aryl or heteroaryl, optionally substituted with one or more (C1-C6)alkyl, (C1-C6)alkoxy or halogen; —CONH2; or —COO—(C1-C6)alkyl, wherein the alkyl may be optionally substituted with one or more halogen; —(CH2),-heterocycle, —O—(CH2)n-heterocycle or —(CH2)n, —O-heterocycle, wherein the heterocycle is optionally substituted with one or more: (C1-C6)alkyl, itself optionally substituted with one or more halogen; (C1-C6)alkoxy, itself substituted with one or more halogen; oxo; amino; carboxyl; cyano; hydroxyl; halogen; 6 to 10 membered aryl or heteroaryl, optionally substituted with one or more (C1-C6)alkyl, (C1-C6)alkoxy or halogen; —CONH2; or —COO—(C1-C6)alkyl, wherein the alkyl may be optionally substituted with one or more halogen; or —(CH2)n-heteroaryl, —O—(CH2)n-heteroaryl or —(CH2)n—O-heteroaryl, wherein the heteroaryl is optionally substituted with one or more: (C1-C6)alkyl, itself optionally substituted with one or more halogen; (C1-C6)alkoxy, itself substituted with one or more halogen; oxo; amino; carboxyl; cyano; hydroxyl; halogen; 6 to 10 membered aryl or heteroaryl, optionally substituted with one or more (C1-C6)alkyl, (C1-C6)alkoxy or halogen; —CONH2; or —COO—(C1-C6)alkyl, wherein the alkyl may be optionally substituted with one or more halogen; and n is 0, 1, 2 or 3.

2. The compound of claim 1, wherein X is CH2.

3. The compound of claim 1, wherein Y is phenyl, and R3 is —(CH2)n-heterocycle.

4. The compound of claim 1, which is: or a pharmaceutically acceptable salt or stereoisomer thereof.

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

6. A deuterium-enriched compound of the formula: or a pharmaceutically acceptable salt or stereoisomer thereof.

7. A pharmaceutical composition comprising a compound of claim 6, or a pharmaceutically acceptable salt or stereoisomer thereof.

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