Tricyclic derivatives
First Claim
1. A tricyclic derivative of the formula Iwherein R1 and R2 together form a group of the formula --N═
- CH--NH--, --N═
N--NH--, --NH--N═
CH--, --NH--CO--NH--, --NH--NH--CO--, --N═
N--CH═
CH--, --N═
CH--N═
CH--, --N═
CH--CH═
N--, or --N═
CH--CO--NH-- (with in each case a nitrogen atom being located at the 6-position of the quinazoline ring) and the 5- or 6-membered ring so formed may optionally bear one or two substituents, any substituent on an available nitrogen atom being selected from (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, halogeno-(1-4C)alkyl, hydroxy-(1-4C)alkyl, (2-4C)alkanoyloxy-(1-4C)alkyl, (1-4C)alkoxy-(1-4C)alkyl, cyano-(1-4C)alkyl, amino-(i-4C)alkyl, (1-4C)alkylamino-(1-4C)alkyl and di-[(1-4C)alkyl]amino-(1-4C)alkyl, and any substituent on an available carbon atom being selected from halogeno, amino, hydroxy, carbamoyl, cyano, (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkoxy, (1-4C)alkylthio, (1-4C)alkylsulphinyl, (1-4C)alkylsulphonyl, (1-4C)alkylamino, di-[(1-4C)alkyl]amino, (2-4C)alkanoyl, N-(1-4C)alkylcarbamoyl, N,N-di-[(1-4C)alkyl]carbamoyl, halogeno-(1-4C)alkyl, hydroxy-(1-4C)alkyl, (2-4C)alkanoyloxy-(1-4C)alkyl, (1-4C)alkoxy-(1-4C)alkyl, cyano-(1-4C)alkyl, amino-(1-4C)alkyl, (1-4C)alkylamino-(1-4C)alkyl and di-[(1-4C)alkyl]amino-(1-4C)alkyl; and
m is the integer 1, 2 or 3 and each R3 is independently hydrogen, halogeno, trifluoromethyl, hydroxy, amino, nitro, cyano, (1-4C)alkyl, (1-4C)alkoxy, (1-4C)alkylamino, di-[(1-4C)alkyl]amino or (2-4C)alkanoylamino;
or a pharmaceutically-acceptable salt thereof.
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Accused Products
Abstract
The invention concerns tricyclic derivatives of the formula I ##STR1## wherein R1 and R2 together form an optionally substituted group of the formula --N═CH--NH--, --N═CH--O--, --N═CH--S--, --N═N--NH--, --NH--N═CH--, --NH--CH═CH--. --NH--CO--NH--, --NH--CO--O--, --NH--CO--S--, --NH--NH--CO--, --N═CH--CH═N--, --N═N--CH═CH--, --N═CH--N═CH--, --N═CH--CH═N--, --NH--CO--CH═CH-- or --N═CH--CO--NH--; m is 1, 2 or 3 and R3 includes hydrogen, 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.
27 Citations
15 Claims
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1. A tricyclic derivative of the formula I
wherein R1 and R2 together form a group of the formula --N═ - CH--NH--, --N═
N--NH--, --NH--N═
CH--, --NH--CO--NH--, --NH--NH--CO--, --N═
N--CH═
CH--, --N═
CH--N═
CH--, --N═
CH--CH═
N--, or --N═
CH--CO--NH-- (with in each case a nitrogen atom being located at the 6-position of the quinazoline ring) and the 5- or 6-membered ring so formed may optionally bear one or two substituents, any substituent on an available nitrogen atom being selected from (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, halogeno-(1-4C)alkyl, hydroxy-(1-4C)alkyl, (2-4C)alkanoyloxy-(1-4C)alkyl, (1-4C)alkoxy-(1-4C)alkyl, cyano-(1-4C)alkyl, amino-(i-4C)alkyl, (1-4C)alkylamino-(1-4C)alkyl and di-[(1-4C)alkyl]amino-(1-4C)alkyl, and any substituent on an available carbon atom being selected from halogeno, amino, hydroxy, carbamoyl, cyano, (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkoxy, (1-4C)alkylthio, (1-4C)alkylsulphinyl, (1-4C)alkylsulphonyl, (1-4C)alkylamino, di-[(1-4C)alkyl]amino, (2-4C)alkanoyl, N-(1-4C)alkylcarbamoyl, N,N-di-[(1-4C)alkyl]carbamoyl, halogeno-(1-4C)alkyl, hydroxy-(1-4C)alkyl, (2-4C)alkanoyloxy-(1-4C)alkyl, (1-4C)alkoxy-(1-4C)alkyl, cyano-(1-4C)alkyl, amino-(1-4C)alkyl, (1-4C)alkylamino-(1-4C)alkyl and di-[(1-4C)alkyl]amino-(1-4C)alkyl; and
m is the integer 1, 2 or 3 and each R3 is independently hydrogen, halogeno, trifluoromethyl, hydroxy, amino, nitro, cyano, (1-4C)alkyl, (1-4C)alkoxy, (1-4C)alkylamino, di-[(1-4C)alkyl]amino or (2-4C)alkanoylamino;
or a pharmaceutically-acceptable salt thereof. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15)
- CH--NH--, --N═
Specification