Back to results
US 2002/0173658 A1Published application
Substituted 2-(2,6-dioxopiperidin-3-yl)-phthalimides and-1-oxoisoindolines and method of reducing TNFalpha levels
OwnerGeorge W. Muller, David I. Stirlinginventors
Life of this patent
Estimating the term…
Abstract
Substituted 2-(2,6-dioxopiperidin-3-yl)phthalimides and 1-oxo-2-(2,6-dioxopiperidin-3-yl)isoindolines reduce the levels of TNFα in a mammal. A typical embodiment is 1-oxo-2-(2,6-dioxo-3-methylpiperidin-3-yl)-4,5,6,7-tetrafluoroisoindoline.
Claims12
A 2,6-dioxopiperidine selected from the group consisting of (α) a compound of the formula:
- 6
- in which:
- one of X and Y is C═O and the other of X and Y is C═O or CH2;
- (i) each of R1, R2, R3, and R4, independently of the others, is halo, alkyl of 1 to 4 carbon atoms, or alkoxy of 1 to 4 carbon atoms or (ii) one of R1, R2, R3, and R4 is —NHR and the remaining of R1, R2, R3, and R4 are hydrogen;
- R5 is hydrogen, alkyl of 1 to 8 carbon atoms, or CO—R7—CH(R10)NR8R9;
- R6 is hydrogen, alkyl of 1 to 8 carbon atoms, benzo, chloro, or fluoro;
- R7 is m-phenylene or p-phenylene or —(CnH2n)— in which n has a value of 0 to 4;
- each of R8 and R9 taken independently of the other is hydrogen or alkyl of 1 to 8 carbon atoms, or R8 and R9 taken together are tetramethylene, pentamethylene, hexamethylene, or —CH2CH2XCH2CH2— in which X is —O—, —S— or —NH—;
- R10 is hydrogen, alkyl of 1 to 8 carbon atoms, or phenyl;
- and
- (b) the acid addition salts of said compounds which contain a nitrogen atom capable of being protonated.
8 more elements
A 2,6-dioxopiperidine selected from the group consisting of (α) a compound of the formula:
- 7
- in which:
- one of X and Y is C═O and the other of X and Y is C═O or CH2;
- (i) each of R1, R2, R3, and R4, independently of the others, is halo, alkyl of 1 to 4 carbon atoms, or alkoxy of 1 to 4 carbon atoms or (ii) one of R1, R2, R3, and R4 is —NHR and the remaining of R1, R2, R3, and R4 are hydrogen;
- R5 is hydrogen, alkyl of 1 to 8 carbon atoms, or CO—R7—CH(R10)NR8R9;
- R6 is alkyl of 1 to 8 carbon atoms, benzo, chloro, or fluoro;
- R7 is m-phenylene or p-phenylene or —(CnH2n)— in which n has a value of 0 to 4;
- each of R8 and R9 taken independently of the other is hydrogen or alkyl of 1 to 8 carbon atoms, or R8 and R9 taken together are tetramethylene, pentamethylene, hexamethylene, or —CH2CH2XCH2CH2— in which X is —O—, —S— or —NH—;
- R10 is hydrogen, alkyl of 1 to 8 carbon atoms, or phenyl;
- and
- (b) the acid addition salts of said compounds which contain a nitrogen atom capable of being protonated.
8 more elements
Dependencies are inferred from the claim text.