Small molecule inhibitors of HER2 expression
AssigneeBaylor College of Medicine
InventorsMotonari Uesugi, Shinichi Asada
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Abstract
Peptide mimetic small molecule inhibitors of Sur-2 are provided having the general formula: 1
Claims19
A compound of the formula:
- 12
- wherein R1 is an indole, indole derivative, alkyl, trihaloalkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, heteroalicyclic, hydroxy, alkoxy, aryloxy, mercapto, alkylthio, arylthio, sulfinyl, sulfonyl, carbonyl, cyano, nitro, halo, or amino;
- wherein R2 is a hydrogen, hydroxy, nitrate, halo, loweralkyl, or carbonyl;
- wherein R3 is a halo, loweralkyl, carbonyl, aryl, aralkyl, or heterocycle;
- and wherein R4 is adamantane, adamantane derivative, alkyl, trihaloalkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, heteroalicyclic, hydroxy, alkoxy, aryloxy, mercapto, alkylthio, arylthio, sulfinyl, sulfonyl, S-sulfonamido, N-sulfonamido, trihalomethane-sulfonamido, halo, carbonyl, cyano, nitro, halo, or amino;
- and wherein when R1 is an indole, R2 is a hydroxyl, and R3 is an isopropyl, R4 is not an adamantane;
- and pharmaceutically acceptable salts thereof.
A compound of the formula:
- 13
- wherein R1 and R2 are a hydrogen, halo, alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, heteroalicyclic, hydroxy, alkoxy, aryloxy, carbonyl, acetyl, carboxy, sulfonyl or trihalomethane-sulfonyl;
- and wherein R1 and R2 may be the same or different;
- and wherein R1 and R2 are not both hydrogen;
- and pharmaceutically acceptable salts thereof.
A compound of the formula:
- 14
- wherein the R1 is selected from the group of β blockers consisting of propanolol, indenolol, carpindolol, bupranolol, and mepindolol;
- and pharmaceutically acceptable salts thereof.
A compound of the formula:
- 15
- wherein R1, R2, and R3 are a hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, heteroalicyclic, hydroxy, alkoxy, aryloxy, carbonyl, halo, acetyl, carboxy, sulfonyl or trihalomethane-sulfonyl;
- and wherein R1, R2, and R3 may be the same or at least one is different;
- and wherein R1, R2, and R3 are not all hydrogen;
- and pharmaceutically acceptable salts thereof.
A compound of the formula:
- 16
- wherein R1 is a hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, heteroalicyclic, hydroxy, alkoxy, aryloxy, halo, carbonyl, acetyl, carboxy, sulfonyl, or trihalomethane-sulfonyl.
A compound of the formula:
- 19
- wherein R1 is an alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, heteroalicyclic, hydroxy, alkoxy, aryloxy, halo, carbonyl, acetyl, carboxy, sulfonyl or trihalomethane-sulfonyl;
- and wherein R1 is not isopropyl;
- and pharmaceutically acceptable salts thereof.
A compound of the formula:
- 21
A compound of the formula:
- 22
A compound of the formula:
- 23
A method of treating cancer in a mammal wherein a clinically effective amount of a small molecule inhibitor of Her2 expression is administered to said mammal.
A method of treating breast cancer in a mammal, wherein a clinically effective amount of adamanolol, a functionalized adamanolol derivative, or a pharmaceutically acceptable salt thereof is administered to said mammal.
Dependencies are inferred from the claim text.