Immuno inhibitory pyrazolone compounds

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C514S254050, C514S318000, C514S326000, C514S403000, C544S364000, C544S371000, C546S211000, C548S364100, C548S369400

Reexamination Certificate

active

07816361

ABSTRACT:
Compounds of formula (IA) or (IB) are inhibitors of CD80 and useful in immunomodulation therapy: wherein Ar represents an optionally substituted monocyclic or bicyclic aromatic or heteroaromatic group having from 5 to 10 ring atoms; R1and R2independently represent H, or C1-C6alkyl; R3represents H; F; CI; Br, —NO2; —CN; C1-C6alkyl optionally substituted by F or CI; or C1-C6alkoxy optionally substituted by F; R4represents a carboxylic acid group (—COOH) or an ester thereof, or —C(═O)NR6R7, —NR7C(═O)R6, —NR7C(═O)OR6, —NHC(═O)NR7R6or —NHC(═S)NR7R6wherein R6represents H, or a radical of formula -(Alk)m-Q wherein m is 0 or 1, Alk is an optionally substituted divalent straight or branched C1-C12alkylene, or C2-C12alkenylene, or C2-C12alkynylene radical or a divalent C3-C12carbocyclic radical, any of which radicals may be interrupted by one or more —O—, —S— or —N(R8)— radicals wherein R8represents H or C1-C4alkyl, C3-C4alkenyl, C3-C4alkynyl, or C3-C6cycloalkyl, and Q represents H; —CF3; —OH; —SH; —NR8R8wherein each R8may be the same or different, or form a ring when taken together with the nitrogen to which they are attached; an ester group; or an optionally substituted aryl, aryloxy, cycloalkyl, cycloalkenyl or heterocyclic group; and R7represents H or C1-C6alkyl; or when taken together with the atom or atoms to which they are attached R6and R7form a monocyclic heterocyclic ring having 5, 6 or 7 ring atoms; and X represents a bond or a divalent radical of formula -(Z)n-(Alk)- or -(Alk)-(Z)n- wherein Z represents —O—, —S— or —NH—, Alk is as defined in relation to R6and n is 0 or 1.

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