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US 5,177,075 AGranted
Substituted dihydroisoquinolinones and related compounds as potentiators of the lethal effects of radiation and certain chemotherapeutic agents; selected compounds, analogs and process
AssigneeWarner-Lambert Company
InventorsMark J. Suto, William R. Turner, Leslie M. Werbel
Life of this patent
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Abstract
The invention is selected, novel, and known analogs of isoquinolinones of the formula ##STR1## and pharmaceutically acceptable salts thereof; novel pharmaceutical compositions; and a method for enhancing the lethal effects for tumor cells to treatment having DNA damaging activity such as ionizing radiation or with chemotherapeutic agents.
Claims8
A compound or its pharmacologically acceptable base or acid addition salts selected from the group consisting of
- 5-amino-3,4-dihydro-1(2H)isoquinolinone, and its monohydrochloride salt.
- 3,4-dihydro-5-[(phenylmethyl)amino]-1(2H)-isoquinolinone;
- N-(1,2,3,4-tetrahydro-1-oxo-5-isoquinolinyl)-acetamide;
- 3,4-dihydro-5-methyl-1(2H)-isoquinolinone;
- 5-ethyl-3,4-dihydro-1(2H)-isoquinolinone;
- 5-chloro-3,4-dihydro-1(2H)-isoquinolinone;
- 3,4-dihydro-5-methoxy-1(2H)-isoquinoline-thione;
- 3,4-dihydro-5-methoxy-1-(methylthio)isoquinoline;
- 3,4-dihydro-3,5-dimethyl-1(2H)isoquinolinone (+/-)
- 3,4-dihydro-5-methyl-1-(methylthio)isoquinoline;
- 3,4-dihydro-5-(dimethylamino)-1(2H)-isoquinoline and its hydrochloride salt
- 4-bromo-5-methyl-1(2H)-isoquinolinone;
- or
- 4-bromo-5-hydroxy-1(2H-isoquinolinone.
11 more elements
A compound or its pharmacologically acceptable base or acid addition salt selected from the group consisting of
- 5-methoxy-4-methyl-1(2H)-phthalazinone;
- 3,4-dihydro-5-[3-(1-piperidinyl)propoxy]-1(2H)-isoquinolinone;
- 3,4-dihydro-5-[2-(1-piperidinyl)ethoxy]-(1(2H)-isoquinolinone;
- 3,4-dihydro-5[4-(1-piperidinyl)butoxy]-1(2H)-isoquinolinone;
- 5-ethoxy-3,4-dihydro-1(2H)-isoquinolinone;
- 3,4-dihydro-5-propoxy-1(2H)-isoquinolinone;
- 5-butoxy-3,4-dihydro-1(2H)-isoquinolinone;
- 3,4-dihydro-5-(2-hydroxy-3-methoxypropxy)-1(2H)-isoquinolinone;
- 3,4-dihydro-5-(2-hydroxy-3-phenoxypropoxy)-1(2H)-isoquinolinone;
- 3,4-dihydro-5-(2-hydroxy-3-phenylpropoxy)-1(2H)-isoquinolinone;
- or
- 3,4-dihydro-5-2-phenylethoxy-1(2H)-isoquinolinone.
9 more elements
Dependencies are inferred from the claim text.