Methods for suppressing an immune response or treating a proliferative disorder
AssigneeThe United States of America, as represented by the Secretary, Department of Health and Human Services
InventorsJoel Moss, Arnold Kristof
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Abstract
Disclosed herein are methods for suppressing an immune response in a subject, treating a neoplasm in a subject, or treating a fibroproliferative vascular disease in a subject, that includes administering to the subject a therapeutically effective amount of a 2-(4-piperazinyl)-substituted 4H-1-benzopyran-4-one compound, or a pharmaceutically acceptable salt thereof, having the structure of wherein the presence of each of R1 and R2 is optional and R1 and R2 are each independently selected from alkyl, substituted alkyl, heteroalkyl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, alkoxy, halogen, hydroxy, or amino.
Claims17
A method of inhibiting proliferation of a cell, comprising contacting the cell with an effective amount of a 2-(4-piperazinyl)-substituted 4H-1-benzopyran-4-one compound, or a pharmaceutically acceptable salt thereof, having the structure of
- wherein the presence of each of R1 and R2 is optional and R1 and R2 are each independently selected from alkyl;
- substituted alkyl;
- heteroalkyl;
- cycloalkyl;
- substituted cycloalkyl;
- heterocycloalkyl;
- substituted heterocycloalky selected from piperazinyl, morpholinyl, tetrahydropyranyl, tetrahydrofuranyl, piperidinyl, pyrrolindinyl, or oxazolinyl, in which one or more hydrogen or carbon atom is replaced by another group selected from a halogen, aryl, substituted aryl, alkoxy, aryloxy, amino or a combination thereof;
- aryl selected from phenyl, naphthyl, biphenyl, diphenylether, diphenylamine or benzophenone;
- substituted aryl selected from phenyl, naphthyl, biphenyl, diphenylether, diphenylamine or benzophenone in which one or more hydrogen or carbon atom is replaced by one or more functional groups selected from alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, halogen, alkylhalos, hydroxy, amino, alkoxy, or thio;
- heteroaryl selected from thiophene, pyridine, isoxazole, phthalidimide, pyrazole, indole, or furan;
- substituted heteroaryl selected from thiophene, pyridine, isoxazole, phthalidimide, pyrazole, indole, or furan in which one or more hydrogen or carbon atom is replaced by one or more functional groups selected from alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, halogen, alkylhalo, hydroxy, amino, alkoxy, or thio;
- alkoxy;
- halogen;
- hydroxy;
- or amino, wherein the 2-(4-piperazinyl)-substituted 4H-1-benzopyran-4-one compound inhibits mammalian Target of Rapamycin or casein kinase 2, but does not significantly inhibit phosphatidylinositol 3-kinase.
A method of treating a proliferative disorder in a subject, comprising administering to the subject a therapeutically effective amount of a 2-(4-piperazinyl)-substituted 4H-1-benzopyran-4-one compound, or a pharmaceutically acceptable salt thereof, having the structure of
- wherein the presence of each of R1 and R2 is optional and R1 and R2 are each independently selected from alkyl;
- substituted alkyl;
- heteroalkyl;
- cycloalkyl;
- substituted cycloalkyl;
- heterocycloalkyl;
- substituted heterocycloalkyl selected from piperazinyl, morpholinyl, tetrahydropyranyl, tetrahydrofuranyl, piperidinyl, pyrrolindinyl, or oxazolinyl, in which one or more hydrogen or carbon atom is replaced by another group selected from a halogen, aryl, substituted aryl, alkoxy, aryloxy, amino or a combination thereof;
- aryl selected from phenyl, naphthyl, biphenyl, diphenylether, diphenylamine or benzophenone;
- substituted aryl selected from phenyl, naphthyl, biphenyl, diphenylether, diphenylamine or benzophenone in which one or more hydrogen or carbon atom is replaced by one or more functional groups selected from alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, halogen, alkylhalo, hydroxy, amino, alkoxy, or thio;
- heteroaryl selected from thiophene, pyridine, isoxazole, phthalidimide, pyrazole, indole, or furan;
- substituted heteroaryl selected from thiophene, pyridine, isoxazole, phthalidimide, pyrazole, indole, or furan in which one or more hydrogen or carbon atom is replaced by one or more functional groups selected from alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, halogen, alkylhalo, hydroxy, amino, alkoxy, or thio;
- alkoxy;
- halogen;
- hydroxy;
- or amino, wherein the 2-(4-piperazinyl)-substituted 4H-1-benzopyran-4-one compound inhibits phosphorylation of P70 S6 kinase, but does not significantly inhibit phosphatidylinositol 3-kinase.
Dependencies are inferred from the claim text.