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US 6,211,177 B1Granted
Method for treating neoplasia by exposure to substituted 2-aryl-benzimidazole derivatives
AssigneeCell Pathways, Inc.
InventorsGerhard Sperl, Ulrich Ixkes, Rifat Pamukcu, Gary A. Piazza
Life of this patent
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Abstract
A method for inhibiting neoplasia, particularly cancerous and precancerous lesions, by exposing the affected cells to substituted 2-aryl-benzimidazoles.
Claims6
A method of treating a mammal having precancerous lesions sensitive to a compound below comprising administering a pharmacologically effective amount of a compound of formula I or pharmaceutically acceptable salt thereof:
- wherein
- R1 is selected from a group consisting of hydrogen, lower alkyl, —(CH2)x—C(O)—OR4, —(CH2)x—C(O)—NH—(CH2)y—R5, (CH2)x—S(O)m—R6 or substituted or unsubstituted benzyl, wherein said substituents are one or two independently selected from a group consisting of halogen, lower alkyl, lower alkoxy or phenyl;
- R2 is substituted or unsubstituted aryl, wherein said aryl group is selected from the group consisting of phenyl, benzyl, pyridyl, pyrimidyl, pyrazinyl, imidazolyl, indolyl, triazinyl, tetrazolyl, thiophenyl, furanyl, pyrazolyl, or pyrrolyl, and wherein said substituents are one to three independently selected from the group consisting of halogen, lower alkyl or lower alkoxy;
- R3 is selected from a group consisting of halogen, lower alkoxy, lower alkyl, lower alkoxy carbonyl, carboxyl, substituted and unsubstituted carbamoyl, wherein said substituents are one or two independently selected from a group consisting of phenyl, benzyl, pyridyl, pyridylmethyl, or benzenesulfonyl;
- R4 is hydrogen or lower alkyl;
- R5 is selected from a group consisting of hydrogen, lower alkyl, benzyl, pyridyl, pyrimidinyl, pyrazinyl, imidazolyl, indolyl, triazinyl, tetrazolyl, thiophenyl, furanyl, thiazolyl, pyrazolyl, or pyrrolyl;
- R6 is substituted or unsubstituted phenyl, wherein said substituents are one to three independently selected from the group consisting of halogen, lower alkyl or lower alkoxy;
- x is 0, 1, or 2;
- m is 0, 1, or 2;
- n is 0, 1 or 2;
- and
- y is 0, 1, or 2.
9 more elements
A method for inhibiting the growth of neoplastic cells sensitive to a compound below comprising exposing the cells to a growth inhibiting effective amount of a compound of Formula I
- wherein
- R1 is selected from a group consisting of hydrogen, lower alkyl, —(CH2)x—C(O)—OR4, —(CH2)x—C(O)—NH—(CH2)y—R5, (CH2)x—S(O)m—R6 or substituted or unsubstituted benzyl, wherein said substituents are one or two independently selected from a group consisting of halogen, lower alkyl, lower alkoxy or phenyl;
- R2 is substituted or unsubstituted aryl, wherein said aryl group is selected from the group consisting of phenyl, benzyl, pyridyl, pyrimidyl, pyrazinyl, imidazolyl, indolyl, triazinyl, tetrazolyl, thiophenyl, furanyl, pyrazolyl, or pyrrolyl, and wherein said substituents are one to three independently selected from the group consisting of halogen, lower alkyl or lower alkoxy;
- R3 is selected from a group consisting of halogen, lower alkoxy, lower alkyl, lower alkoxy carbonyl, carboxyl, substituted and unsubstituted carbamoyl, wherein said substituents are one or two independently selected from a group consisting of phenyl, benzyl, pyridyl, pyridylmethyl, or benzenesulfonyl;
- R4 is hydrogen or lower alkyl;
- R5 is selected from a group consisting of hydrogen, lower alkyl, benzyl, pyridyl, pyrimidinyl, pyrazinyl, imidazolyl, indolyl, triazinyl, tetrazolyl, thiophenyl, furanyl, thiazolyl, pyrazolyl, or pyrrolyl;
- R6 is substituted or unsubstituted phenyl, wherein said substituents are one to three independently selected from the group consisting of halogen, lower alkyl or lower alkoxy;
- x is 0, 1, or 2;
- m is 0, 1, or 2;
- n is 0, 1 or 2;
- and
- y is 0, 1, or 2.
9 more elements
Dependencies are inferred from the claim text.