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US 10,590,146 B2Granted
Substituted aminothiazolopyrimidinediones
AssigneeHoffmann-La Roche Inc.
InventorsLisha Wang, Hongying Yun, Xiufang Zheng
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Abstract
The present invention relates to compounds of formula (I), wherein R1 to R4 are as described herein, and their prodrugs or pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.
Claims14
A compound of formula (I),
- wherein:
- R1 is H, C1-6alkyl, C3-7cycloalkyl or phenylC1-6alkyl, said phenylC1-6alkyl being unsubstituted or substituted with one to three substituents independently selected from C1-6alkyl and halogen;
- R2 is H or C1-6alkyl;
- R3 is C1-6alkyl;
- and
- R4 is C1-6alkyl;
- or pharmaceutically acceptable salt, enantiomer or diastereomer thereof.
4 more elements
A compound of formula (Ia),
- wherein
- R1 is H, C1-6alkyl, C3-7cycloalkyl or phenylC1-6alkyl, said phenylC1-6alkyl being unsubstituted or substituted with one to three substituents independently selected from C1-6alkyl and halogen;
- R2 is H or C1-6alkyl;
- R3 is C1-6alkyl;
- and
- R4 is C1-6alkyl;
- or pharmaceutically acceptable salt, enantiomer or diastereomer thereof.
4 more elements
A compound selected from:
- 5-Amino-3-[(2R,3S,5S)-3-[(1S)-1-aminoethyl]-5-[(1S)-1-hydroxypropyl]tetrahydrofuran-2-yl]-6H-thiazolo[4,5-d]pyrimidine-2,7-dione;
- 5-amino-3-[(2R,3S,5S)-3-[(1R)-1-aminoethyl]-5-[(1S)-1-hydroxypropyl]tetrahydrofuran-2-yl]-6H-thiazolo[4,5-d]pyrimidine-2,7-dione;
- 5-Amino-3-[(2R,3S,5S)-5-[(1S)-1-hydroxypropyl]-3-[(1R)-1-(methylamino)ethyl]tetrahydrofuran-2-yl]-6H-thiazolo[4,5-d]pyrimidine-2,7-dione;
- 5-Amino-3-[(2R,3S,5S)-5-[(1S)-1-hydroxypropyl]-3-[(1R)-1-(propylamino)ethyl]tetrahydrofuran-2-yl]-6H-thiazolo[4,5-d]pyrimidine-2,7-dione;
- 5-Amino-3-[(2R,3S,5S)-3-[(1R)-1-(cyclopropylamino)ethyl]-5-[(1S)-1-hydroxypropyl]tetrahydrofuran-2-yl]-6H-thiazolo[4,5-d]pyrimidine-2,7-dione;
- 5-Amino-3-[(2R,3S,5S)-3-[(1R)-1-(benzylamino)ethyl]-5-[(1S)-1-hydroxypropyl]tetrahydrofuran-2-yl]-6H-thiazolo[4,5-d]pyrimidine-2,7-dione;
- 5-Amino-3-[(2R,3S,5S)-5-[(1S)-1-hydroxypropyl]-3-[(1S)-1-(methylamino)ethyl]tetrahydrofuran-2-yl]-6H-thiazolo[4,5-d]pyrimidine-2,7-dione;
- 5-Amino-3-[(2R,3S,5S)-3-[(1S)-1-(benzylamino)ethyl]-5-[(1S)-1-hydroxypropyl]tetrahydrofuran-2-yl]-6H-thiazolo[4,5-d]pyrimidine-2,7-dione;
- and
- 5-Amino-3-[(2R,3S,5S)-3-[(1R)-1-(dimethylamino)ethyl]-5-[(1S)-1-hydroxypropyl]tetrahydrofuran-2-yl]-6H-thiazolo[4,5-d]pyrimidine-2,7-dione;
- or pharmaceutically acceptable salt, enantiomer or diastereomer thereof.
8 more elements
Dependencies are inferred from the claim text.