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US 9,309,219 B2Granted
Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same
AssigneeCelgene Corporation
InventorsHon-Wah Man, Roger Shen-Chu Chen, George W. Muller, Alexander L. Ruchelman, Ehab M. Khalil, Weihong Zhang
Life of this patent
Estimating the term…
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.
Claims17
A method for inhibiting TNF-α secretion in a patient suffering from cancer, which comprises administering to the patient a TNF-alpha secretion inhibitory effective amount of a compound of formula (I):
- or a pharmaceutically acceptable salt or stereoisomer thereof, wherein:
- X is C═O 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)n-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.
43 more elements
Dependencies are inferred from the claim text.