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US 2021/0079012 A1Published application
Substituted azetidine dihydrothienopyridines and their use as phosphodiesterase inhibitors
AssigneeLeo Pharma A/S
InventorsMark ANDREWS, Daniel Rodriguez GREVE, Bjarne NØRREMARK
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Abstract
The present invention relates to novel substituted azetidine dihydrothienopyridines with phosphodiesterase inhibitory activity, and to their use in therapy, and to pharmaceutical compositions comprising the compounds and to methods of treating diseases with the compounds (I)
Claims13
A compound of general formula (I)
- wherein:
- R1 is selected from the group consisting of phenyl, 6-membered heteroaryl, phenoxy, and 6:
- membered heteroaryloxy;
- wherein the phenyl, 6-membered heteroaryl, phenoxy, or 6-membered heteroaryloxy is optionally substituted with one or more substituents independently selected from R3;
- R2 is selected from the group consisting of (C3-C7)cycloalkyl, bridged (C3-C7)cycloalkyl, and (4-7 membered) heterocycloalkyl;
- wherein the (C3-C7)cycloalkyl, bridged (C3-C7)cycloalkyl, or (4-7 membered) heterocycloalkyl is all of which are optionally substituted with one or more substituents independently selected from R4;
- R3 is selected from the group consisting of halogen, —CN, (C1-C4)alkyl, halo(C1-C4)alkyl, hydroxy(C1-C4)alkyl, and (C3-C6)cycloalkyl;
- R4 is selected from the group consisting of fluoro, —CN, —OH, (C1-C4)alkyl, halo(C1-C4)alkyl, hydroxy(C1-C4)alkyl, —ORx, —S(O)2Rx, —S(O)2NRaRb, —C(O)Rx, —C(O)(ORx), and —C(O)NRaRb;
- Rx is selected from the group consisting of (C1-C4)alkyl and (C3-C6)cycloalkyl;
- Ra and Rb are each independently selected from the group consisting of hydrogen, (C1-C4)alkyl, and (C3-C6)cycloalkyl;
- and
- S* is a chiral sulfur atom with (R) stereochemistry;
- or a pharmaceutically acceptable salt, enantiomer, mixture of enantiomers, diastereomer, mixture of diastereomers, hydrate or solvates thereof.
10 more elements
8-14. (canceled)
Dependencies are inferred from the claim text.