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US 2026/0217656 A1Published application
Compounds Affecting KRAS
AssigneeUniversitat De Barcelona
InventorsNieves Agell Jané, María Pujol Dilme, Jaime Rubio Martínez, Montserrat Jaumot Pijoan, Eduardo Garrido Sagarzazu, Marta Vilaplana Saiz, Baraa Abuasaker, Sonia Brun Lozano
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Abstract
The present invention relates to compounds of formula I that can be used as medicaments for example in cancer therapy. The present invention further relates to pharmaceutical composition including the compounds as well as intermediates for the preparation of these compounds. In addition, the present invention concerns kits or packages including these compounds.
Claims16
A compound having the general formula I
- wherein R1 is selected from H, branched, cyclo or linear (C1-C6)-alkyl, branched, cyclo or linear (C1-C6)-alkyl-OH, branched, cyclo or linear (C1-C6)-alkyl-NH2, branched or linear (C1-C6)-alkyl comprising a secondary or tertiary amine or an ether group;
- R2 is selected from branched, cyclo or linear (C1-C6)-alkyl, heterocyclyl, substituted or unsubstituted (C6-C10)-aryl, or substituted or unsubstituted (C5-C5)-cycloalkenyl, wherein the substituted (C6-C10)-aryl or substituted (C5-C5)-cycloalkenyl is substituted with 1 or 2 groups selected from the groups consisting of
- a) OCH3,
- b) halogen,
- c) a substituent having formula II
- wherein “1” is selected from 0 to 6, “m” is 1 or 2, the aryl group has 5 to 10 atoms, and
- wherein R6 is H, branched, cyclo or linear (C1-C6)-alkyl, or halogen;
- d) a substituent having formula III
- wherein the aryl groups independently have 5 to 10 atoms, and “n”, “o” and “p” are independently selected from 0 to 6;
- and/or
- e) a substituent having formula IV
- wherein “q” and “r” are independently selected from 0 to 6, the aryl group has 5 to 10 atoms, and wherein R7 is selected from halogen, NO2, NH2, CN, CF3, and branched, cyclo or linear (C1-C6)-alkyl;
- wherein R7 cannot be Cl, when the substituent of formula IV is the only substituent of the (C6-C10)-aryl and “q” is 0 and “r” is 1;
- R3 is independently selected from H, branched, cyclo or linear (C1-C6)-alkyl, branched, cyclo or linear (C1-C6)-alkyl-OH, CF3, halogen, NO2, and CN;
- R4 is independently selected from H, OH, O, NH2, and NO2;
- and
- R5 is independently selected from N, NH, O, S, branched, cyclo or linear (C1-C6)-alkyl, branched or linear (C1-C6)-alkyl comprising a secondary or tertiary amine, an ether group or a sulfide group, N═N, and CH═N.
14 more elements
Dependencies are inferred from the claim text.