THERAPEUTICALLY ACTIVE COMPOUNDS BASED ON BIOISOSTERIC SUBSTITUTION OF CATHECHOL IN PDE4 INHIBITORS WITH INDAZOLE

摘要

The invention relates to therapeutically active compositions for the treatment or prevention of phlogistic diseases - inflammation of the joints, Crohn's disease and intestinal inflammation; respiratory diseases such as chronic obstructive pulmonary disease, asthma, chronic bronchitis and pulmonary emphysema; infectious diseases - endotoxic shock and toxic shock syndrome; immune diseases, system erythematous lupus and psoriasis and other diseases including osteal resorptions and reperfusion after injuries. The composition contains isozyme 4 (PDE4) and the indazole group is a basic part of the general chemical structure of the compound, and the group is a bioisosteric substituent of the cathechol group or of its functional derivative in a known compound having the above therapeutical effect and the same remaining components of its general chemical structure. Compounds with the following formulae are included where R2a and R2b are individually selected from the group consisting mainly of hydrogen and the substituent listed below, provided that one of them, but not both, of the R2a and R2b should be independently selected as hydrogen where the substituents include radicals as follows: 22 claims