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US 2003/0199502 A1Published application
Indoloquinazolinones
AssigneeNovartis AG
InventorsKaspar Zimmermann, Robert Portmann, Dean Franklin Rigel
Life of this patent
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Abstract
The invention provides compounds of formula (I) wherein R is as defined in the description, and the preparation thereof. The compounds of formula (I) are useful as pharmaceuticals, for use in the treatment of any state associated with high levels of activeted PARP. 1
Claims9
A compound of formula I
- 6
- wherein
- either R is —(CH2)n—X, wherein n is 1, 2 or 3 and X is (C1-4)alkyl, (C1-4)alkoxy, (C2-7)alkenyl,
- (C2-7)alkynyl, carboxy, (C1-4)alkoxycarbonyl, cyano, tetrazolyl, (C3-7)cycloalkylamino or imidazolyl(C1-4)alkylamino,
- or R is —CH2CON(R1)R2, wherein R1 and R2, independently, are hydrogen, hydroxy, (C1-4)alkyl, benzyl, di(C1-4)alkylamino(C1-4)alkyl, (C2-7)alkenyl, (C2-7)alkynyl, hydroxy(C1-4)alkyl, dihydroxy (C1-4)alkyl, cyanoalkyl, carbamoylalkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, 2-oxo-3-tetrahydrofuryl, (C1-4)alkoxy(C1-4)alkyl, (C1-4)alkoxycarbonyl (C3-7)cycloalkyl, naphthylamino(C1-4)alkyl, imidazolylamino(C1-4)alkyl, morpholinyl(C1-4)alkyl, pyrrolidinyl(C1-4)alkyl, piperidinyl(C1-4)alkyl or (C3-7)cycloalkylamino(C1-4)alkyl, or R1 and R2, together with the nitrogen atom to which they are attached, form a morpholino, (C1-4)alkyl-piperazinyl, hydroxy(C1-4)alkyl-piperazinyl, piperidinyl, pyrrolidinyl or
- p-chlorophenyl(C1-4)alkyl-piperazinyl,
- in free base or acid addition salt form.
4 more elements
7-(1H-Tetrazole-5-ylmethyl)-6H-indolo[1,2-a]quinazoline-5-one in free base or acid addition salt form.
Dependencies are inferred from the claim text.