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US 5,475,001 AGranted
Quinazoline derivatives
AssigneeZeneca Limited
InventorAndrew J. Barker
Life of this patent
Estimating the term…
Abstract
The invention concerns quinazoline derivatives of the formula I ##STR1## wherein R.sup.1 includes hydroxy, amino, hydroxyamino, (1-4C)alkoxy, (1-4C)alkylamino and di-[(1-4C)alkyl]amino; R.sup.3 is halogeno; n is 1, 2 or 3 and R.sup.2 includes hydrogen, hydroxy, halogeno and (1-4C)alkyl; or a pharmaceutically-acceptable salt thereof; processes for their preparation; pharmaceutical compositions containing them; and the use of the receptor tyrosine kinase inhibitory properties of the compounds in the treatment of cancer.
Claims15
A quinazoline derivative of the formula I
- wherein R.sup.1 is hydroxy, amino, hydroxyamino, trifluoromethoxy, (1-4C)alkoxy, (1-4C)alkylamino, di-[(1-4C)alkyl]amino, aziridin-1-yl, azetidin-1-yl, pyrrolidin-1-yl, piperidino, morpholino, piperazin-1-yl, 4-(1-4C)alkylpiperazin-1-yl, (1-4C)alkylthio, halogeno-(2-4C)alkoxy, hydroxy-(2-4C)alkoxy, (1-4C)alkoxy-(2-4C)alkoxy, phenyl-(1-4C)alkoxy, halogeno-(2-4C)alkylamino, hydroxy-(2-4C)alkylamino, (1-4C)alkoxy-(2-4C)alkylamino, phenyl-(1-4C)alkylamino, (2-4C)alkanoylamino, benzamido, 2-oxopyrrolidin-1-yl, 2-oxopiperidin-1-yl, halogeno-(2-4C)alkanoylamino, hydroxy-(2-4C)alkanoylamino, (1-4C)alkoxy-(2-4C)alkanoylamino, (3-4C)alkenoylamino, (3-4C)alkynoylamino, N-(1-4C)alkyl-(2-4C)alkanoylamino, N-(1-4C)alkylbenzamido, N-(1-4C)alkyl-halogeno-(2-4C)alkanoylamino, N-(1-4C)alkyl-hydroxy-(2-4C)alkanoylamino, N-(1-4C)alkyl-(1-4C)alkoxy((2-4C)alkanoylamino, N-(1-4C)alkyl-(3-4C)alkenoylamino or N-(1-4C)alkyl-(3-4C)alkynoylamino, and wherein said benzamido or N-(1-4C)alkylbenzamido substituent or any phenyl group in a R.sup.1 substituent may optionally bear one or two halogeno, (1-4C)alkyl or (1-4C)alkoxy substituents;
- R.sup.3 is halogeno;
- and n is the integer 1, 2 or 3 and each R.sup.2 is independently hydrogen, hydroxy, halogeno, trifluoromethyl, amino, nitro, cyano, (1-4C)alkyl, (1-4C)alkoxy or (2-4C)alkanoylamino;
- or a pharmaceutically-acceptable salt thereof.
1 more element
Dependencies are inferred from the claim text.