18-03-2021 дата публикации
Номер: US20210079012A1
Принадлежит:
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) 2. A compound according to claim 1 , wherein Ris phenyl or phenoxy claim 1 , optionally substituted with one of R.3. A compound according to claim 1 , wherein Ris fluoro.4. A compound according to claim 1 , wherein Ris piperidinyl claim 1 , pyrrolidinyl claim 1 , or tetrahydropyranyl; wherein the piperidinyl claim 1 , pyrrolidinyl claim 1 , or tetrahydropyranyl is optionally substituted with one or more substituents independently selected from R.5. A compound according to claim 4 , wherein Ris tetrahydropyranyl.6. A compound according to selected from the group consisting of:(i) (1R)-5-(3-(4-Fluorophenyl)azetidin-1-yl)-7-((tetrahydro-2H-pyran-4-yl)amino)-2,3-dihydrothieno[3,2-b]pyridine 1-oxide;(ii) Methyl (3R)-3-[[(1R)-5-[3-(4-fluorophenyl)azetidin-1-yl]-1-oxido-2,3-dihydrothieno[3,2-b]pyridin-7-yl]amino]piperidine-1-carboxylate;(iii) Methyl (3R)-3-[[(1R)-5-(3-(4-phenylazetidin-1-yl)-1-oxido-2,3-dihydrothieno[3,2-b]pyridin-7-yl]amino]piperidine-1-carboxylate;(iv) (1R)-5-(3-(4-Fluorophenoxy)azetidin-1-yl)-7-((tetrahydro-2H-pyran-4-yl)amino)-2,3-dihydrothieno[3,2-b]pyridine-1-oxide;(v) Methyl (3S)-3-[[(1R)-5-[3-(4-fluorophenoxy)azetidin-1-yl]-1-oxido-2,3-dihydrothieno[3,2-b]pyridine-7-yl]amino]pyrolidine-1-carboxylate;(vi) 1-[(3S)-3-[[(1R)-5-[3-(4-Fluorophenoxy)azetidin-1-yl]-1-oxido-2,3-dihydrothieno[3,2-b]pyridin-7-yl]amino]pyrrolidin-1-yl]ethenone; and(vii) (1R)-5-(3-Phenylazetidin-1-yl)-7-((tetrahydro-2H-pyran-4-yl)amino)-2,3-dihydrothieno[3,2-b]pyridine-1-oxide;or a pharmaceutically acceptable salt, enantiomer, mixture of enantiomers, diastereomer, mixture of diastereomers, hydrate or solvate thereof.7. A pharmaceutical composition comprising a compound according to and one or more ...
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