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US 10,882,841 B2Granted
Wnt signaling pathway inhibitors for treatments of disease
AssigneeUniversity of Maryland, Baltimore
InventorsFengtian Xue, Yan Shu
Life of this patent
Estimating the term…
Abstract
Compounds and compositions are provided as inhibitors of the Wnt/β-catenin pathway for the treatment of diseases that implicate the same.
Claims28
A method of treating or preventing a disease alleviated by inhibiting Wnt/β-catenin signaling in a patient in need of said treatment or prevention, the method comprising administering a therapeutically effective amount of one or more compounds having the formula:
- wherein R1 and R2 each can independently represent a substituent selected from the group consisting of H and substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocycle, heteroaryl, alkoxy, carboxy, carbalkoxy, and carboxamido;
- R3 represents a substituent selected from the group consisting of substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocycle, and heteroaryl;
- n represents an integer of 0 to 2, Z represents one or more substituted or unsubstituted alkyl substituents when n is 1 or 2;
- X1 represents N or CR4;
- X2 represents N or CR5;
- X3 represents N or CR6;
- R4, R5, and R6 each can independently represent a substituent selected from the group consisting of H, OH, NO2, CN, halo, and substituted or unsubstituted alkyl, alkylcarbonyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocycle, heteroaryl, amino, alkoxy, carboxy, carbalkoxy, carboxamido, sulfonyl, sulfonamido, sulfinyl, monoalkylaminosulfinyl, dialkylaminosulfinyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, alkylsulfonylamino, hydroxysulfonyloxy, alkoxysulfonyloxy, alkylsulfonyloxy, hydroxysulfonyl, alkoxysulfonyl, alkylsulfonylalkyl, monoalkylaminosulfonylalkyl, dialkylaminosulfonylalkyl, monoalkylaminosulfinylalkyl, and dialkylaminosulfinylalkyl;
- wherein when both are present, R4 and R5 can be taken together to form a substituted or unsubstituted m-membered cycloalkyl or heterocycle, wherein m represents an integer of 5 to 7;
- or the pharmaceutically acceptable salts of said one or more compounds;
- with the proviso that:
- when X1 and X2 represent CR4 and CR5, respectively, then R3 is substituted aryl;
- and
- compounds wherein R1 and R2 each are H and substituted aryl, R3 is substituted aryl, n is 0, X1 is N, X2 is N, X3 is CR6, and R6 is alkyl, are excluded.
10 more elements
A compound of the formula:
- wherein R1 and R2 each can independently represent a substituent selected from the group consisting of H and substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocycle, heteroaryl, alkoxy, carboxy, carbalkoxy, and carboxamido;
- R3 represents a substituent selected from the group consisting of substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocycle, and heteroaryl;
- n represents an integer of 0 to 2, Z represents one or more substituted or unsubstituted alkyl substituents when n is 1 or 2;
- X1 represents N or CR4;
- X2 represents N or CR5;
- X3 represents N or CR6;
- R4, R5, and R6 each can independently represent a substituent selected from the group consisting of H, OH, NO2, CN, halo, and substituted or unsubstituted alkyl, alkylcarbonyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocycle, heteroaryl, amino, alkoxy, carboxy, carbalkoxy, carboxamido, sulfonyl, sulfonamido, sulfinyl, monoalkylaminosulfinyl, dialkylaminosulfinyl, monoalkylaminosulfonyl, dialkylaminosulfonyl, alkylsulfonylamino, hydroxysulfonyloxy, alkoxysulfonyloxy, alkylsulfonyloxy, hydroxysulfonyl, alkoxysulfonyl, alkylsulfonylalkyl, monoalkylaminosulfonylalkyl, dialkylaminosulfonylalkyl, monoalkylaminosulfinylalkyl, and dialkylaminosulfinylalkyl;
- wherein when both are present, R4 and R5 can be taken together to form a substituted or unsubstituted m-membered cycloalkyl or heterocycle, wherein m represents an integer of 5 to 7;
- or the pharmaceutically acceptable salts of said one or more compounds;
- with the proviso that:
- when X1 and X2 represent CR4 and CR5, respectively, then R3 is substituted aryl;
- and
- compounds wherein R1 and R2 each are H and substituted aryl, R3 is substituted aryl, n is 0, X1 is N, X2 is N, X3 is CR6, and R6 is alkyl, are excluded.
10 more elements
Dependencies are inferred from the claim text.