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US 2014/0228354 A1Published application
Method for Inhibition of Deubiquitinating Activity
AssigneeVivolux AB
InventorsStig Linder, Rolf Larsson
Life of this patent
Estimating the term…
Abstract
Compounds of the general structure S-1, wherein X and R1-R5 are defined in the specification, are capable of abrogating the deubiquitinating (DUB) activity of the 19S RP DUBs and are useful in methods and compositions for treating cancer, in particular, cancer tumors refractory to treatment by state-of-the-art chemotherapy.
Claims30
A compound of the general structure S-1 capable of abrogating the deubiquitinating (DUB) activity of the 19S RP DUBs
- wherein
- R1, R2 at double bond d1 and R3, R4 at double bond d2 can, independent of each other, have a configuration opposite to that of formula S1,
- X is CO, CS, CH2, OHC1-6-alkyl, NH or NO1-6-alkyl:
- R1 and R3 are, independent of each other, H or C1-6-alkyl;
- R2 and R4 are, independent of each other, H;
- C1-6-alkyl-CO;
- phenyl or 6-membered heteroaryl optionally substituted by 1-3 of:
- C1-6-alkyl, C1-6-alkoxy, CN, —COOC1-6-alkyl, COOH, NO2, F, Cl, Br, I, CF3, NH2, NHC1-6-alkyl, N(C1-6-alkyl)2, CONR7R8, with the proviso that one or more of H in alkyl and alkoxy can be substituted by fluoro;
- R5 is any of H;
- C2-6-alkenyl;
- C1-3-alkoxy-C2-6-alkyl-;
- C1-3-alkoxy-C2-6-alkenyl-;
- aryl-C0-6-alkyl-;
- heteroaryl-C0-6-alkyl-;
- heterocyclyl-C0-6-alkyl-;
- cycloalkyl-C0-6-alkyl-;
- —C1-6-alkyl-COOC1-6-alkyl;
- —C2-6-alkyl-aryloxy;
- COR6;
- R6 is any of C1-6-alkyl;
- C2-6-alkenyl;
- C1-6-alkoxy;
- C1-3-alkoxy-C1-6-alkyl-;
- C1-3-alkoxy-C1-6alkenyl-;
- aryl-C0-6-alkyl-;
- heteroaryl-C0-6-alkyl-;
- heterocyclyl-C0-6-alkyl-;
- cycloalkyl-C0-6-alkyl-;
- —C1-6-alkyl-COOC1-6-alkyl;
- NH2;
- —NHC1-6-alkyl;
- —N(C1-6-alkyl)2;
- —C106-alkyl-aryoxy;
- and
- R7, R8 are, independent of each other, H or C1-3-alkyl.
32 more elements
Dependencies are inferred from the claim text.