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US 2020/0268762 A1Published application
7-substituted sulfonimidoylpurinone compounds and derivatives for the treatment and prophylaxis of liver cancer
AssigneeHoffmann-La Roche Inc.
InventorsTHOMAS POESCHINGER, CAROLA RIES, HONG SHEN, HONGYING YUN, SABINE HOVES, CARINA HAGE
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Abstract
The present invention relates to compounds of formula (I), wherein R1, R2 and R3 are as described herein, and their prodrugs or pharmaceutically acceptable salt, enantiomer or diastereomer thereof, for (use in) the treatment and/or prophylaxis of liver cancer.
Claims31
A method for the treatment or prophylaxis of liver cancer comprising administering to a patient in need thereof, a therapeutically effective amount of a compound of formula (I), or a pharmaceutically acceptable salt, enantiomer or diastereomer thereof,
- wherein:
- R1 is C1-6alkyl;
- R2 is benzyl, said benzyl being unsubstituted or substituted by one, two or three substituents independently selected from halogen and C1-6alkyl;
- R3 is —NR4R5, wherein
- R4 is C1-6-alkyl or C1-6alkoxyC1-6alkyl;
- R5 is (C1-6alkyl)2NCOOC1-6alkyl, C1-6alkoxyC1-6alkyl, C1-6alkoxycarbonyl(C1-6alkyl)aminoC1-6 alkyl, C1-6alkoxycarbonyl(phenyl)C1-6alkyl, C1-6alkoxycarbonylC1-6alkyl, C1-6 alkoxycarbonyloxyC1-6alkyl, C1-6alkyl, C1-6alkylcarbonyl(C1-6alkyl)aminoC1-6alkyl or pyrrolidinylcarbamoyloxyC1-6alkyl;
- or
- R4 and R5 together with the nitrogen they are attached to form a heterocyclyl;
- with the proviso that the compound is not:
- 6-amino-9-benzyl-2-(propylsulfonimidoyl)-7-(pyrrolidine-1-carbonyl)purin-8-one;
- 6-amino-9-benzyl-7-(piperidine-1-carbonyl)-2-(propylsulfonimidoyl)purin-8-one;
- 6-amino-9-benzyl-7-(morpholine-4-carbonyl)-2-(propylsulfonimidoyl)purin-8-one;
- 6-amino-9-benzyl-7-(3,3-dimethylpyrrolidine-1-carbonyl)-2-(propylsulfonimidoyl)purin-8-one;
- ethyl 1-[6-amino-9-benzyl-8-oxo-2-(propylsulfonimidoyl)purine-7-carbonyl]pyrrolidine-2-carboxylate;
- 6-amino-7-(2-azaspiro[3.3]heptane-2-carbonyl)-9-benzyl-2-(propylsulfonimidoyl)purin-8-one;
- 6-amino-9-benzyl-7-(2-oxa-6-azaspiro[3.3]heptane-6-carbonyl)-2-(propylsulfonimidoyl)purin-8-one;
- 6-amino-9-benzyl-7-(3,3-difluoropyrrolidine-1-carbonyl)-2-(propylsulfonimidoyl)purin-8-one;
- or
- 6-amino-9-benzyl-7-(3-fluoro-3-methyl-pyrrolidine-1-carbonyl)-2-(propylsulfonimidoyl)purin-8-one;
- or an enantiomer or diastereomer thereof.
17 more elements
Dependencies are inferred from the claim text.