US 6,642,249 B2 · Immunomodulating compounds

Abstract

The present invention relates to a novel heterocyclic compound, a pharmaceutical composition comprisining said compound, a method and use of said compound for clinical treatment of medical conditions which may benefit from immunomodulation, e.g. rheumatoid arthritis, multiple sclerosis, diabetes, asthma, transplantation, systemic lupus erythematosis and psoriasis. More particularly the present invention relates to novel heterocyclic compounds, which are CD80 antagonists capable of inhibiting the interactions between CD80 and CD28. A method of screening compounds for their ability of inhibiting ligand-induced co-stimulatory receptor internalization pathways in immune competent human cells is described. Said immune competent human cells are incubated at conditions capable of inducing co-stimulatory receptor internalization in the presence of at least one test compound and the suppression of the ligand-induced co-stimulatory receptor internalization determined. There is also described a kit for use in such a method, as well as an immunoregulatory drug capable of blocking down-modulation of a ligand-induced receptor.

Claims22

Dependent claims

A compound having the general formula (I)

wherein X represents a bond or a group selected from substituted or unsubstituted C1-3-alkyl, NH—C(O)—C1-3-alkyl, NH—C(O)—CH2—O—CH2, or C(O)—NH—C(Z)H wherein Z represents side chains in naturally occurring amino acids;
Y represents NR4, O or
R1 represents halo, CF3, lower alkyl or lower alkoxy;
n is an integer from 0 to 2;
R2 and R4 represents independently H or lower alkyl;
and
R3 represents H, halo, lower alkyl or lower alkoxy, wherein halo is F, Cl or Br;
wherein lower alkyl represents saturated or unsaturated, straight, branched or cyclic alkyl groups having 1-6 carbon atoms;
and wherein lower alkoxy represents saturated or unsaturated, straight, branched or cyclic alkoxy groups having 1-6 carbon atoms, with the proviso that R2 is not H, when X is a bond, Y is NH and R3 is H, or pharmaceutically acceptable salts thereof.

6 more elements

Dependencies are inferred from the claim text.

Immunomodulating compounds

Life of this patent

Immunomodulating compounds

Life of this patent

Abstract

Claims22