Method for inhibiting neoplastic cells and related conditions by exposure to substituted N- arylmethyl and heterocyclmethyl-1H-pyrazolo (3,4-B) quinolin-4-amines
AssigneeCell Pathways, Inc.
InventorsRifat Pamukcu, Gary A. Piazza
Life of this patent
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Abstract
A method for inhibiting neoplastic cells and related conditions by exposing them to substituted N-arylmethyl and heterocyclmethyl-1H-pyrazolo3,4-B!quinolin-4-amines.
Claims15
A method for inhibiting the growth of neoplastic cells comprising exposing the cells sensitive to such a compound to a growth inhibiting effective amount of a compound of Formula I:
- ##STR4## wherein:
- R.sub.1 is lower-alkyl;
- R.sub.2 is hydrogen, or lower-alkyl;
- R.sub.3 is hydrogen, or lower-alkyl;
- R.sub.4 is hydrogen, or lower-alkyl;
- R.sub.5 is phenyl (or phenyl substituted by from one to three, the same or different, substituents selected from the group consisting of lower-alkoxy, cyano, hydroxy, 4-morpholinylloweralkoxy, lower-alkyl, and halogen), phenyl-lower-alkyl, pyridinyl, furanyl, isoxazolyl, thienyl, oxazolyl, thiazolyl, pyridazinyl, pyrazinyl, and pyrirmidinyl;
- or R.sub.4 and R.sub.5 together with the CH group to which they are bonded form an indanyl ring;
- and
- R.sub.6 is from one to three, the same or different, substituents selected from the group consisting of hydrogen, lower-alkoxy, hydroxy, lower-alkyl, and halogen;
- or a pharmaceutically acceptable acid-addition salt and/or hydrate thereof, or, where applicable, enantiomer or a racemic mixture.
A method of treating a mammal having precancerous lesions sensitive to such a compound comprising administering to said mammal a pharmacologically effective amount of a compound of Formula I:
- ##STR5## wherein:
- R.sub.1 is lower-alkyl;
- R.sub.2 is hydrogen, or lower-alkyl;
- R.sub.3 is hydrogen, or lower-alkyl;
- R.sub.4 is hydrogen, or lower-alkyl;
- R.sub.5 is phenyl (or phenyl substituted by from one to three, the same or different, substituents selected from the group consisting of lower-alkoxy, cyano, hydroxy, 4-morpholinylloweralkoxy, lower-alkyl, and halogen), phenyl-lower-alkyl, pyridinyl, furanyl, isoxazolyl, thienyl, oxazolyl, thiazolyl, pyridazinyl, pyrazinyl, and pyrimidinyl;
- or R.sub.4 and R.sub.5 together with the CH group to which they are bonded form an indanyl ring;
- and
- R.sub.6 is from one to three, the same or different, substituents selected from the group consisting of hydrogen, lower-alkoxy, hydroxy, lower-alkyl, and halogen;
- or a pharmaceutically acceptable acid-addition salt and/or hydrate thereof, or, where applicable, enantiomer or a racemic mixture.
A method for regulating apoptosis in human cells comprising exposing said cells sensitive to such a compound to an effective amount of a compound of the formula:
- ##STR6## wherein:
- R.sub.1 is lower-alkyl;
- R.sub.2 is hydrogen, or lower-alkyl;
- R.sub.3 is hydrogen, or lower-alkyl;
- R.sub.4 is hydrogen, or lower-alkyl;
- R.sub.5 is phenyl (or phenyl substituted by from one to three, the same or different, substituents selected from the group consisting of lower-alkoxy, cyano, hydroxy, 4-morpholinylloweralkoxy, lower-alkyl, and halogen), phenyl-lower-alkyl, pyridinyl, furanyl, isoxazolyl, thienyl, oxazolyl, thiazolyl, pyridazinyl, pyrazinyl, and pyrimidinyl;
- or R.sub.4 and R.sub.5 together with the CH group to which they are bonded form an indanyl ring;
- and
- R.sub.6 is from one to three, the same or different, substituents selected from the group consisting of hydrogen, lower-alkoxy, hydroxy, lower-alkyl, and halogen;
- or a pharmaceutically acceptable acid-addition salt and/or hydrate thereof, or, where applicable, enantiomer or a racemic mixture.
Dependencies are inferred from the claim text.