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US4619933A Expired / Lapsed US ⏱️ 0.0 years remaining

6-aryl pyrimidines for treating aplastic anemia

Assignee: Pharmacia and Upjohn Co
•
Filing: 1983-08-25
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Granted: 1986-10-28
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Expires: 2003-08-25
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Abstract

Abstract A method for treating aplastic anemia by systemic administration of a 6-aryl pyrimidine compound or a pharmaceutically acceptable salt thereof in association with a pharmaceutical carrier to a human or animal having aplastic anemia.

Inventors

  • 👤 Dale A. Stringfellow
  • 👤 Patricia E. Fast

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-26 12:11
CPC Classifications
C; C07; C07D; C07D239/00; C07D239/02; C07D239/24; C07D239/28; C07D239/46; C07D239/47

Claims Analysis

Total Claims: 5
Claim 1
Independent Claim 423 words
A process for treating aplastic anemia comprising the systemic administration of an effective amount for treating aplastic anemia of a compound of the formula: ##STR26## wherein X 3 is equal to X, X 4 , or X 5 wherein X 4 is fluoro, chloro, bromo or iodo, and X 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 1 is a member selected from the group consisting of: (a) phenyl, (b) a monosubstituted phenyl of the formula: ##STR27## wherein provided that only one of groups R, R 1 , R 2 , R 3 , R 4 is other than hydrogen and R or R 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 1 or R 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 ##STR28## wherein R 5 and R 6 are the same or different and are alkyl of from 1 to 8 carbon atoms, inclusive, benzyl or taken together with --N< are a saturated cycloalkylamino group ##STR29## 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 2 is chloro, fluoro, bromo, iodo, or alkyl of from 1 to 3 carbon atoms, inclusive, (c) a disubstituted phenyl of the formula: ##STR30## wherein any two of R, R 1 , R 2 , R 3 and R 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) α-naphthyl of the formula: ##STR31## 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 a human or animal having aplastic anemia.
Claim 2
Dependent Claim 423 words
A process for treating aplastic anemia comprising the systemic administration of an effective amount for treating aplastic anemia of a compound of the formula: ##STR26## wherein X 3 is equal to X, X 4 , or X 5 wherein X 4 is fluoro, chloro, bromo or iodo, and X 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 1 is a member selected from the group consisting of: (a) phenyl, (b) a monosubstituted phenyl of the formula: ##STR27## wherein provided that only one of groups R, R 1 , R 2 , R 3 , R 4 is other than hydrogen and R or R 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 1 or R 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 ##STR28## wherein R 5 and R 6 are the same or different and are alkyl of from 1 to 8 carbon atoms, inclusive, benzyl or taken together with --N< are a saturated cycloalkylamino group ##STR29## 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 2 is chloro, fluoro, bromo, iodo, or alkyl of from 1 to 3 carbon atoms, inclusive, (c) a disubstituted phenyl of the formula: ##STR30## wherein any two of R, R 1 , R 2 , R 3 and R 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) α-naphthyl of the formula: ##STR31## 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 a human or animal having aplastic anemia.
Claim 3
Dependent Claim 27 words
The process of claim 1 wherein the amount of compound administered is from about 0.1 to about 10 mg/kg of body weight of the human or animal.
Claim 4
Dependent Claim 11 words
The process of claim 2 wherein the compound administered is 2-amino-5-bromo-6-phenyl-4(1H)-pyrimidinone.
Claim 5
Dependent Claim 11 words
The process of claim 2 wherein the compound administered is 2-amino-5-iodo-6-phenyl-4(1H)-pyrimidinone.

References Cited (Backward Citations)

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USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1989-10-27 1990-04-28 1990-10-28 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1993-10-27 1994-04-28 1994-10-28 $3760.00 Window Closed / Lapsed
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