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US 5,714,493 AGranted
Aryl and heteroaryl quinazoline compounds which inhibit CSF-1R receptor tyrosine kinase
AssigneeRhone-Poulenc Rorer Pharmaceuticals Inc.
InventorsMichael R. Myers, Alfred P. Spada, Martin P. Maguire, Paul E. Persons, Asher Zilberstein, Chin-Yi Jenny Hsu, Susan E. Johnson
Life of this patent
Estimating the term…
Abstract
This invention relates to the treatment of intimation in a patient suffering from such disorder. More specifically, the invention relates to mono- and/or bicyclic aryl or heteroaryl quinazoline compounds in the treatment of inflammation.
Claims1
A method for the treatment of inflammation in a patient suffering from such disorder comprising administering to said patient an effective amount of the compound of formula:
- ##STR24## wherein Ar is a substituted or unsubstituted benzene, pyrrole, thiophene, furan, thiazole, imidazole, pyrazole, 1,2,4-triazole, pyridine, 2(1H)-pyridone, 4(1H)-pyridone, pyrazine, pyrimidine, pyridazine, isothiazole, isoxazole, oxazole, tetrazole, naphthalene, tetralin, naphthyridine, benzofuran, benzothiophene, indole, 2,3-dihydroindole, 1H-indazole, indoline, benzopyrazole, 1,3-benzodioxole, benzoxazole, purine, coumarin, chromone, quinoline, tetrahydroquinoline, isoquinoline, benzimidazole, quinazoline, pyrido2,3-b!pyrazine, pyrido3,4-b!pyrazine, pyrido3,2-c!pyridazine, pyrido3,4-b!-pyridine, 1 H- pyrazole3,4-d!pyrimidine, pteridine, 2(1H)-quinolone, 1(2H)-isoquinolone, 1,4-benzisoxazine, benzothiazole, quinoxaline, quinoline-N-oxide, isoquinoline-N-oxide, quinoxaline-N-oxide, quinazoline-N-oxide, benzoxazine, phthalazine, or cinnoline;
- X is a bond, O, S, SO, SO.sub.2, OCH.sub.2, C.dbd.C, C.tbd.C, C.dbd.S, SCH.sub.2, NH, NHCH.sub.2, NR.sub.4 or NR.sub.4 CH.sub.2 ;
- R is independently, located at any appropriate position of Ar, hydrogen, alkyl, alkenyl, phenyl, aralkyl, aralkenyl, hydroxy, hydroxyalkyl, alkoxy, alkoxyalkyl, aralkoxy, aryloxy, acyloxy, halo, haloalkyl, nitro, cyano, amino, mono- and di-alkylamino, acylamino, carboxy, carboxyalkyl, carbalkoxy, carbaralkoxy, carbalkoxyalkyl, carbalkoxyalkenyl, aminoalkoxy, amido, mono-alkylamido, di-alkylamido, N, N-cycloalkylamido, sulfonyl, mono-alkyl sulfonyl, di-alkyl sulfonyl, sulfamoyl, mono-alkyl sulfamoyl, di-alkyl sulfamoyl, halophenyl or benzoyl;
- R.sub.4 is alkyl or benzyl;
- R.sub.5 is hydrogen, alkyl, alkylthio, cycloalkyl, hydroxy, alkoxy, aralkoxy, aryl, halo, haloalkyl, carboxy or carbalkoxy;
- and
- R.sub.6 and R.sub.7 are alkoxy or aralkoxy;
- or
- a pharmaceutically acceptable salt thereof,
- provided that:
- when R.sub.5 is hydrogen, R.sub.6 and R.sub.7 are methoxy, and X is a bond, then Ar is other than R substituted phenyl wherein R is hydrogen or (mono- or di-)methoxy;
- or when R.sub.5 is hydrogen, R.sub.6 and R.sub.7 are alkoxy, X is NHCH.sub.2 or NR.sub.4, and R.sub.4 is hydrogen, then Ar is other than R substituted Ar is phenyl wherein R is hydrogen;
- or when R.sub.5 is hydrogen or methoxy, R.sub.6 and R.sub.7 are methoxy, and X is NHCH.sub.2, then Ar is other than R substituted pyridinyl wherein R is hydrogen, mono-alkyl or mono-hydroxy, or Ar is other than R substituted indol-3-yl wherein R is hydrogen.
10 more elements
Dependencies are inferred from the claim text.