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US 6,187,779 B1Granted
Method for inhibiting neoplastic cells and related conditions by exposure to 2,8-disubstituted quinazoline derivatives
AssigneeCell Pathways, Inc.
InventorsRifat Pamukcu, Gary A. Piazza
Life of this patent
Estimating the term…
Abstract
A method for inhibiting neoplastic cells and related conditions by exposing them to 2,8 disubstituted quinazolinone compounds.
Claims7
A method of treating a mammal having precancerous lesions comprising administering a pharmacologically effective amount of a compound of Formula I or pharmaceutically acceptable salt thereof:
- wherein A is an oxiranyl group, optionally substituted by straight-chain or branched alkyl with up to 8 carbon atoms, which in turn may be substituted by phenyl, or A is selected from the group consisting of
- wherein R1 is selected from the group consisting of hydrogen or a straight-chain or branched alkyl with up to 6 carbon atoms;
- R2 is selected from the group consisting of a straight-chain or branched alkyl with up to 8 carbon atoms, which is optionally substituted by phenyl;
- R3 is selected from the group consisting of a straight-chain or branched alkyl with up to 5 carbon atoms or a group with the formula —OR6,
- wherein R6 is selected from the group consisting of hydrogen, a hydroxy-protecting group, or a straight-chain or branched alkyl with up to 5 carbon atoms;
- R4 is selected from the group consisting of a straight-chain or branched alkyl with 2 to 10 carbon atoms, which is optionally substituted by phenyl;
- L is selected from the group consisting of —CO—, —CH(OH), —CH2, —CH(N3), or —CH(OSO2R7);
- wherein R7 is selected from the group consisting of a straight-chain or branched alkyl with up to 4 carbon atoms or phenyl;
- R5 is selected from the group consisting of a straight-chain or branched alkyl with 3 to 8 carbon atoms, which is optionally substituted by phenyl, or benzyl or 2-phenylethyl;
- D is selected from the group consisting of hydrogen or a group with the formula —SO2—NR 8R9;
- wherein R8 and R9 are the same or different and are selected from the group consisting of hydrogen, phenyl, or straight-chain or branched alkyl with up to 6 carbon atoms, which is optionally substituted by hydroxy, or R8 and R9 together with the nitrogen atom they form a 5- to 6-membered heterocyclic ring with up to 2 other hetero atoms selected from the group consisting of S, N, and/or O, which is optionally also substituted through a free N function by straight-chain or branched alkyl with up to 6 carbon atoms, which in turn may be substituted by hydroxy;
- E is a straight-chain or branched alkyl with up to 8 carbon atoms;
- and their tautomers and salts.
10 more elements
A method for regulating apoptosis in human cells comprising exposing said cells to an effective amount of a compound of the formula:
- wherein A is an oxiranyl group, optionally substituted by straight-chain or branched alkyl with up to 8 carbon atoms, which in turn may be substituted by phenyl, or A is selected from the group consisting of
- wherein R1 is selected from the group consisting of hydrogen or a straight-chain or branched alkyl with up to 6 carbon atoms;
- R2 is selected from the group consisting of a straight-chain or branched alkyl with up to 8 carbon atoms, which is optionally substituted by phenyl;
- R3 is selected from the group consisting of a straight-chain or branched alkyl with up to 5 carbon atoms or a group with the formula —R6,
- wherein R6 is selected from the group consisting of hydrogen, a hydroxy-protecting group, or a straight-chain or branched alkyl with up to 5 carbon atoms;
- R4 is selected from the group consisting of a straight-chain or branched alkyl with 2 to 10 carbon atoms, which is optionally substituted by phenyl;
- L is selected from the group consisting of —CO—, —CH(OH), —CH2, —CH(N3), or —CH(OSO2R7);
- wherein R7 is selected from the group consisting of a straight-chain or branched alkyl with up to 4 carbon atoms or phenyl;
- R5 is selected from the group consisting of a straight-chain or branched alkyl with 3 to 8 carbon atoms, which is optionally substituted by phenyl, or benzyl or 2-phenylethyl;
- D is selected from the group consisting of hydrogen or a group with the formula —SO2—NR8R9;
- wherein R8 and R9 are the same or different and are selected from the group consisting of hydrogen, phenyl, or straight-chain or branched alkyl with up to 6 carbon atoms, which is optionally substituted by hydroxy, or R8 and R9 together with the nitrogen atom they form a 5- to 6-membered heterocyclic ring with up to 2 other hetero atoms selected from the group consisting of S, N, and/or O, which is optionally also substituted through a free N function by straight-chain or branched alkyl with up to 6 carbon atoms, which in turn may be substituted by hydroxy;
- E is a straight-chain or branched alkyl with up to 8 carbon atoms;
- and their tautomers and salts.
10 more elements
A method of treating a mammal having neoplasia comprising administering a pharmacologically effective amount of a compound of Formula I or pharmaceutically acceptable salt thereof:
- wherein A is an oxiranyl group, optionally substituted by straight-chain or branched alkyl with up to 8 carbon atoms, which in turn may be substituted by phenyl, or A is selected from the group consisting of
- wherein R1 is selected from the group consisting of hydrogen or a straight-chain or branched alkyl with up to 6 carbon atoms;
- R2 is selected from the group consisting of a straight-chain or branched alkyl with up to 8 carbon atoms, which is optionally substituted by phenyl;
- R3 is selected from the group consisting of a straight-chain or branched alkyl with up to 5 carbon atoms or a group with the formula —OR6,
- wherein R6 is selected from the group consisting of hydrogen, a hydroxy-protecting group, or a straight-chain or branched alkyl with up to 5 carbon atoms,
- R4 is selected from the group consisting of a straight-chain or branched alkyl with 2 to 10 carbon atoms, which is optionally substituted by phenyl;
- L is selected from the group consisting of —CO—, —CH(OH), —CH2, —CH(N3), or —CH(OSO2R7);
- wherein R7 is selected from the group consisting of a straight-chain or branched alkyl with up to 4 carbon atoms or phenyl;
- R5 is selected from the group consisting of a straight-chain or branched alkyl with 3 to 8 carbon atoms, which is optionally substituted by phenyl, or benzyl or 2-phenylethyl;
- D is selected from the group consisting of hydrogen or a group with the formula —SO2—NR8R9;
- wherein R8 and R9 are the same or different and are selected from the group consisting of hydrogen, phenyl, or straight-chain or branched alkyl with up to 6 carbon atoms, which is optionally substituted by hydroxy, or R8 and R9 together with the nitrogen atom they form a 5- to 6-membered heterocyclic ring with up to 2 other hetero atoms selected from the group consisting of S, N, and/or O, which is optionally also substituted through a free N function by straight-chain or branched alkyl with up to 6 carbon atoms, which in turn may be substituted by hydroxy;
- E is a straight-chain or branched alkyl with up to 8 carbon atoms;
- and their tautomers and salts.
10 more elements
Dependencies are inferred from the claim text.