Benzodioxole or benzodioxepine heterocyclic compounds as phosphodiesterase inhibitors

Patent metadata

Field	Value
Publication number	US-8980905-B2
Application number	US-201113806659-A
Country	US
Kind code	B2
Filing date	Jun 24, 2011
Priority date	Jun 24, 2010
Publication date	Mar 17, 2015
Grant date	Mar 17, 2015

Abstract

Compounds of the general formula (I) wherein each of m and n is independently 0 or 1; R 1 and R 2 , 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 —; R 3 is —CHF 2 , —CF 3 , —OCHF 2 , —OCF 3 , —SCHF 2 or —SCF 3 ; X is a bond, —CH 2 —, 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 R 4 ; and R 4 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.

First claim

The invention claimed is:

1. A compound of general formula IIb

wherein
each of m and n is independently 0 or 1;
R 1 and R 2 , 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 —; and
R 3 is —OCHF 2 , or —OCF 3 ;

or a pharmaceutically accepta…

Assignees

• Nielsen Simon Feldbæk
• Leo Pharma As

Inventors

• Nielsen Simon Feldbæk

Classifications

• A61P35/00

  Human Necessities · mapped topic

• A61P37/00

  Human Necessities · mapped topic

• A61P9/00

  Human Necessities · mapped topic

• A61P3/10

  Human Necessities · mapped topic

• A61P9/10

  Human Necessities · mapped topic