Immunomodulating heterocyclic compounds

Details Immunomodulating heterocyclic compounds Immunomodulating heterocyclic compounds

2007-08-28

2009-10-06

Wilson, James O (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C514S248000, C514S255050

Reexamination Certificate

active

07598247

ABSTRACT:
Compounds of formula (I) are inhibitors of CD80 and useful in immunomodulation therapy:wherein R1and R3independently represent H; F; Cl; Br; —NO2; —CN; C1-C6alkyl optionally substituted by F or Cl; 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 contain one or more —O—, —S— or —N(R8)— links wherein R8represents H or C1-C4alkyl, C3-C4alkenyl, C3-C4alkynyl, or C3-C6cycloalkyl, and Q represents H; —NR9R10wherein R9and R10independently represents H; C1-C4alkyl; C3-C4alkenyl; C3-C4alkynyl; C3-C6cycloalkyl; an ester group; an optionally substituted carbocyclic or heterocyclic group; or R9and R10form a ring when taken together with the nitrogen to which they are attached, which ring is optionally substituted; and R7represents H or C1-C6alkyl; or when taken together with the atom or atoms to which they are attached R6and R7form an optionally substituted 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.

REFERENCES:
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Salomon, Benoit, et al., B7/CD28 Costimulation Is Essential for the Homeostasis of the CD4+CD25+ Immunoregulatory T Cells that Control Autoimmune Diabetes, Immunity, vol. 12, 431-440, Apr. 2000.

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