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US 8,263,648 B2Granted
Diebenzofuran derivatives as inhibitors of PDE-4 and PDE-10
AssigneeMylan Laboratories Limited
InventorsGopalan Balasubramanian, Ravi Dhamjewar, Shrikant Havale, Sreedhara Swamy Keshavapura Hosamane
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Abstract
The present invention relates to novel heterocyclic compounds that are useful as phosphodiesterase inhibitors (PDEs) in particular phosphodiesterase type 4 (PDE IV) inhibitors and phosphodiesterase type 10 (PDE 10) inhibitors, processes for their preparation, pharmaceutical compositions containing them and their use in treating allergic and inflammatory diseases as well as for inhibiting the production of Tumor Necrosis Factor (TNF-α).
Claims20
A compound of formula
- and its tautomers, stereoisomers, enantiomers, diastereomers, and pharmaceutically acceptable salts wherein
- R1 is
- X1 is selected from hydrogen, optionally substituted alkyl, optionally substituted N,N-dimethylaminoalkenyl, carboxy, ═CH—NR5R6, COOR6;
- X2 is selected from optionally halo, cyano, carboxy, COOR6, substituted alkyl, NR5R6, —NR5S(O)mR6;
- X4 represents O, S, NR5, N—OR5, ═N—OCH2COOH, ═N—O-Me;
- when X1 and X2 or X1 and X4;
- are ortho to each other, they may together form a 4 to 7 membered ring system selected from an alicyclic or heterocyclic ring;
- r is 0 or 1;
- R2 represents optionally substituted groups selected from alkyl, haloalkyl, alkenyl, alkynyl, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or optionally substituted heterocyclyl;
- R5 represents hydrogen, alkoxy, R′COOR6, optionally substituted alkyl or optionally substituted aryl;
- R6 represents hydrogen, optionally substituted alkyl or optionally substituted aryl;
- R5 and R6 may together form a 3 to 12 membered mono or polycyclic ring;
- R′ represents a direct bond or an optionally substituted alkylene;
- m is an integer represented by 0, 1 or 2.
11 more elements
Dependencies are inferred from the claim text.