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US 2026/0217679 A1Published application
Cancer treating compounds
OwnerRobert FALCONER, David PAJTAS +2inventors
InventorsRobert FALCONER, David PAJTAS, Klaus PORS, Goreti Ribeiro MORAIS
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Abstract
The present invention relates to a group of compounds that generally fall within the class of compounds known as the duocarmycins. The present invention provides a novel group of duocarmycins with a structure according to Formula (I). The compounds have efficacy in the treatment of cancer.
Claims21
A compound of formula I, or a pharmaceutically acceptable salt thereof:
- wherein:
- A represents a 5 or 6 membered ring wherein there are 3 or 4 atoms not represented in the ring and the 3 or 4 atoms are selected as follows:
- 0, 1 or 2 of the atoms are selected independently from C═O, N, NH, S, or O with the balance of the atoms being made up of CH;
- X represents NH, S or O;
- Y represents a halo group;
- R1 represents a group selected from:
- —OR4a, —NR4aR4b, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C5-10 cycloalkyl, substituted or unsubstituted C5-10 heterocycloalkyl, substituted or unsubstituted C6-10 aryl, and substituted or unsubstituted C5-10 heteroaryl,
- wherein, when substituted, the R1 group is substituted with 1, 2, or 3 groups independently selected from:
- halo, —OR4a, —NR4aR4b, —NO2, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkyl substituted with OH, C1-6 alkyl substituted with OMe, and C1-6 alkyl substituted with ═O;
- R2 represents a group selected from:
- H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, and —C(O)—R5;
- R3 represents a group selected from:
- H, —OH, halo, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, —NR6aR6b, C1-6 alkoxy substituted with C6-10 aryl and C1-6 alkyl substituted with C6-10 aryl;
- R4a and R4b are each independently selected from:
- C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkyl substituted with OH, C1-6 alkyl substituted with OMe, C1-6 alkyl substituted with ═O, C1-6 alkyl substituted with a substituted or unsubstituted C6-10 aryl, —C(O)—C1-6alkyl, —(CR7aR7b)nC(O)OR8, —(CR7aR7b)nC(O)NHR8, substituted or unsubstituted C5-10 cycloalkyl, substituted or unsubstituted C5-10 heterocycloalkyl, substituted or unsubstituted C6-10 aryl, and substituted or unsubstituted C5-10 heteroaryl;
- or R4b is H;
- wherein, when substituted, the R4a and R4b group is substituted with 1 or 2 groups selected from:
- halo, OH, —NO2, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6 alkyl substituted with OH, C1-6 alkyl substituted with OMe, C1-6 alkyl substituted with ═O, and —NH2;
- n is 1, 2, or 3 (preferably 1);
- R5 represents a group selected from:
- C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl;
- R6a and R6b are each independently selected from:
- H and C1-6 alkyl;
- one of R7a and R7b is a group selected from:
- H, C1-6 alkyl and C1-6 alkyl substituted with —OH, —SH, —SMe, —NH2, —C(O)OH, —C(O)NH2, guanidine, C6-10 aryl, C6-10 aryl substituted with —OH, or C5-10 heteroaryl;
- and all other R7′ and R7b are H;
- and
- R8 represents a group selected from:
- H and C1-6 alkyl;
- provided that R1 is not —OBn when R2 is methyl.
27 more elements
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Dependencies are inferred from the claim text.