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US 4,543,248 AGranted
Method for immunoregulation with 6-aryl pyrimidine compounds
AssigneeThe Upjohn Company
InventorsDale A. Stringfellow, Patricia E. Fast
Life of this patent
Estimating the term…
Abstract
A method for altering the immunoregulatory system of humans and animals by administering a 6 aryl pyrimidine compound or a salt thereof in association with a pharmaceutical carrier.
Claims4
A process for treating an animal or human having acquired or congenital hypogammaglobulinemia, acquired or congenital agammaglobulinemia, comprising the systemic administration of an effective amount for treating said diseases of a compound of the formula:
- ##STR27## wherein X.sub.3 is equal to X, X.sub.4, or X.sub.5 wherein X.sub.4 is fluoro, chloro, bromo or iodo, and X.sub.5 is mono-, di- or trihalo methyl, mono-, di- or trifluoroethyl, perfluoropropyl and X is alkyl of from 1 to 3 carbon atoms, inclusive, 2-propynyl, 2-propenyl, and alkyloxyacyl where alkyl is as defined above, and X.sub.1 is a member selected from the group consisting of:
- (a) phenyl,
- (b) a monosubstituted phenyl of the formula:
- ##STR28## wherein provided that only one of groups R, R.sub.1, R.sub.2, R.sub.3, R.sub.4 is other than hydrogen and R or R.sub.4 is alkyl of from 1 to 8 carbon atoms, inclusive, including isomeric forms, alkoxy of from 1 to 8 carbon atoms, inclusive, including isomeric forms, fluoro, chloro, bromo, iodo, or nitro;
- R.sub.1 or R.sub.3 is fluoro, chloro, bromo, iodo, nitro, trifluoromethyl or alkoxy of from one to eight carbon atoms, alkoxyethyloxy wherein alkoxy is from 1 to 5 carbon atoms, inclusive, or ##STR29## wherein R.sub.5 and R.sub.6 are the same or different and are alkyl of from 1 to 8 carbon atoms, inclusive, benzyl or taken together with ##STR30## are a saturated cycloalkylamino group ##STR31## wherein n' is 3, 4, 5 or 6 or dialkyl substituted cycloalkylamino wherein each alkyl is from 1 to 3 carbon atoms, inclusive;
- and R.sub.2 is chloro, fluoro, bromo, iodo, or alkyl of from 1 to 3 carbon atoms, inclusive.
- (c) a disubstituted phenyl of the formula:
- ##STR32## wherein any two of R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are not hydrogen and are the same or different and are fluoro, chloro, bromo, iodo, alkyl of from 1 to 8 carbon atoms, including isomeric forms, alkoxy of from 1 to 8 carbon atoms, inclusive isomeric forms, nitro and trifluoromethyl;
- (d) a trihalo substituted phenyl wherein halo is chloro, bromo, iodo or fluoro,
- (e) .alpha.-naphthyl of the formula:
- ##STR33## wherein R is substituted in either ring and is hydrogen, alkyl of from 1 to 8 carbon atoms, inclusive, including isomeric forms, alkoxy of from 1 to 8 carbon atoms, inclusive, including isomeric forms, fluoro, chloro, iodo, bromo or nitro,
- (f) 2-furyl,
- (g) 3-pyridyl,
- (h) 2-pyridyl and
- (i) 2-pyrazyl,
- or a salt thereof in association with a pharmaceutical carrier to said human or animal.
13 more elements
Dependencies are inferred from the claim text.