Benzodioxole or benzodioxepine heterocyclic compounds as phosphodiesterase inhibitors

US8980905B2 · kind B2 · utility

Assignee

• Leo Pharma A/S · DK

Inventor

• Simon Feldbæk Nielsen · Avenue Madeleine, DK

Key dates

• Filing date: Jun 24, 2011
• Grant date: Mar 17, 2015
• Expiry date: Jun 24, 2031

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D493/10
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Compounds of the general formula (I) wherein each of m and n is independently 0 or 1; R1 and R2, together with the carbon atom to which they are attached, form a heterocyclic ring comprising one or two heteroatoms selected from oxygen, sulfur, —S(O)— and —S(O)2—; R3 is —CHF2, —CF3, —OCHF2, —OCF3, —SCHF2 or —SCF3; X is a bond, —CH2—, or —NH—; A is aryl, cycloalkyl, cycloalkenyl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkenyl, optionally substituted with one or more, same or different substituents selected from R4; and R4 is hydrogen, amino, thioxo, alkyl, haloalkyl, hydroxyalkyl, alkoxy, haloalkoxy, halogen, oxo, thia, or hydroxy; or pharmaceutically acceptable salts, hydrates or solvates thereof, have been found to exhibit PDE4 inhibiting activity, and may therefore be useful in the treatment of inflammatory diseases and disorders.