Identification of compounds for the treatment or prevention of proliferative diseases
OwnerMichael Alan Sturgess, Ke Yanginventors
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Abstract
The invention features compounds for the treatment of cancer and other proliferative diseases. These compounds were identified in screening assays that contact candidate compounds with a cell containing a nucleic acid that includes a HER2 regulatory element and a reporter sequence. The invention further features compounds structurally related to those identified by the screening assays. Finally, the invention features methods of treating or preventing a proliferative disease using the compounds of the invention.
Claims24
A compound having the formula:
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- or a pharmaceutically acceptable salt thereof, where R1 and R2 are independently H or lower alkyl, or R1 and R2 together are (CR4R5)m, where R4 and R5 are independently H, lower alkyl, CH2OR6, OR7, or (CH2)oNR8R9, where R6, R7, R8, and R9 are independently H, lower alkyl, aryl, or alkaryl, m is 2, 3, 4, or 5, and o is 0 or 1;
- Ar is any monocyclic or bicyclic aromatic or heteroaromatic ring system;
- each R3 is independently NR10R11, OR12, Hal, NO2, SO2NR13R14, CONR15R16,
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- where X is O, S, or NR21, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, and R21 are independently H, lower alkyl, alkaryl, or aryl, R22 is lower alkyl, alkaryl, or aryl, and n is 1 or 2.
A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound of the formula:
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- or a pharmaceutically acceptable salt thereof, where R1 and R2 are independently H or lower alkyl, or R1 and R2 together are (CR4R5)m, where R4 and R5 are independently H, lower alkyl, CH2OR6, OR7, or (CH2)oNR8R9, where R6, R7, R8, and R9 are independently H, lower alkyl, aryl, or alkaryl, m is 2, 3, 4, or 5, and o is 0 or 1;
- Ar is any monocyclic or bicyclic aromatic or heteroaromatic ring system;
- each R3 is independently NR10R11, OR12, Hal, NO2, SO2NR13R14, CONR15R16,
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- where X is O, S, or NR21, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, and R21 are independently H, lower alkyl, alkaryl, or aryl, R22 is lower alkyl, alkaryl, or aryl, and n is 1 or 2.
A method for treating or preventing a proliferative disease in a subject, said method comprising administering to said subject a therapeutically effective amount of a chemical compound having the formula:
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- or a pharmaceutically acceptable salt thereof, where R1 and R2 are independently H or lower alkyl, or R1 and R2 together are (CR4R5)m, where R4 and R5 are independently H, lower alkyl, CH2OR6, OR7, or (CH2)oNR8R9, where R6, R7, R8, and R9 are independently H, lower alkyl, aryl, or alkaryl, m is 2, 3, 4, or 5, and o is 0 or 1;
- Ar is any monocyclic or bicyclic aromatic or heteroaromatic ring system;
- each R3 is independently NR10R11, OR12, Hal, NO2, SO2NR13R14, CONR15R16,
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- where X is O, S, or NR21, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, and R21 are independently H, lower alkyl, alkaryl, or aryl, R22 is lower alkyl, alkaryl, or aryl, and n is 1 or 2.
Dependencies are inferred from the claim text.