Compound useful for the treatment of degenerative and inflammatory diseases

Inventors

Menet, Christel Jeanne Marie • SMITS, Koen Kurt

Assignees

Alfasigma SpA

Abstract

A novel compound able to inhibit JAK is disclosed, that comprises a compound of Formula I:The compound may be prepared as a pharmaceutical composition, and may be used for the treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.

Core Innovation

The invention relates to a compound of Formula I that inhibits Janus kinases, including JAK1 and JAK2, and is presented as a compound of Formula I or a pharmaceutically acceptable salt thereof. The compounds are described as being used in a pharmaceutical composition with a pharmaceutically acceptable carrier.

The document addresses conditions involving JAK-STAT signaling and inflammatory pathways, including systemic lupus erythematosus and other inflammatory, autoimmune, proliferative, and transplant-rejection conditions. It also addresses diseases involving impaired cartilage turnover and IL-6 hypersecretion, including degenerated cartilage and congenital cartilage malformations.

The core innovation is the use of the Formula I JAK inhibitor compound to achieve dramatically improved in vivo potency for treatment and prevention. This improved potency is described as potentially enabling lower dosage, while targeting JAK1 and JAK2 within the JAK family relevant to STAT transcription factors and IL-6/IL6 receptor signaling pathways.

Claims Coverage

The claim set includes two independent claims directed to treatment of systemic lupus erythematosus using a compound of Formula I or a pharmaceutically acceptable salt. Across the independent claims, the inventive features mainly cover administration of the Formula I compound, including within a pharmaceutical composition, with dependent claim options for a further therapeutic agent and combination administration.

The claims coverage centers on treating systemic lupus erythematosus by administering a Formula I JAK inhibitor or pharmaceutically acceptable salt, either directly or as part of a pharmaceutical composition with a pharmaceutically acceptable carrier, with dependent options for adding a further therapeutic agent and administering it in combination.

Stated Advantages

Documented Applications