Isoindolines, method of use, and pharmaceutical compositions
AssigneeCelgene Corporation
InventorsGeorge W. Muller, David I. Stirling, Roger Shen-Chu Chen
Life of this patent
Estimating the term…
Abstract
Substituted 1-oxo-2-(2,6-dioxopiperidin-3-yl)isoindolines are useful in treating inflammation, inflammatory disease, autoimmune disease, and oncogenic or cancerous conditions in a mammal. Typical embodiments are 1-oxo-2-(2,6-dioxopiperidin-3yl)4-aminoisoindoline and 1-oxo-2-(2,6-dioxo-3-methylpiperidin-3-yl)aminoisoindoline.
Claims28
A method of treating inflammation, inflammatory disease or autoimmune disease in a mammal which comprises administering thereto an effective amount of a compound of the formula:
- in which:
- 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 —NHR5 and the remaining of R1, R2, R3, and R4 are hydrogen;
- R5 is hydrogen or alkyl of 1 to 8 carbon atoms;
- R6 is hydrogen, alkyl of 1 to 8 carbon atoms, benzyl, or halo;
- or
- an acid addition salt of said compound which contain a nitrogen atom capable of being protonated.
A method of treating an oncogenic or cancerous condition in a mammal
- which comprises administering thereto an effective amount of a compound of the formula:
- in which:
- 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 —NHR5 and the remaining of R1, R2, R3, and R4 are hydrogen;
- R5 is hydrogen or alkyl of 1 to 8 carbon atoms;
- R6 is hydrogen, alkyl of 1 to 8 carbon atoms, benzyl, or halo;
- or
- an acid addition salt of said compound which contain a nitrogen atom capable of being protonated.
A method of reducing undesirable levels of TNFα in a mammal which comprises administering thereto an effective amount of a compound of the formula:
- in which:
- 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 —NHR5 and the remaining of R1, R2, R3, and R4 are hydrogen;
- R5 is hydrogen or alkyl of 1 to 8 carbon atoms;
- R6 is hydrogen, alkyl of 1 to 8 carbon atoms, benzyl, or halo;
- or
- an acid addition salt of said compound which contain a nitrogen atom capable of being protonated.
A pharmaceutical composition comprising, in combination with a pharmaceutically and physiologically suitable carrier, a compound of the formula:
- in which:
- 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 —NHR5 and the remaining of R1, R2, R3, and R4 are hydrogen;
- R5 is hydrogen or alkyl of 1 to 8 carbon atoms;
- R6 is hydrogen, alkyl of 1 to 8 carbon atoms, benzyl, or halo;
- or
- an acid addition salt of said compound which contain a nitrogen atom capable of being protonated, in a quantity sufficient upon administration in a single or multiple dose regimen to a mammal to produce at least one of the effects of reducing the level of TNFα, improving an oncogenic or cancerous condition, reducing inflammation, or improving autoimmune disease.
Dependencies are inferred from the claim text.