Compound useful for the treatment of degenerative and inflammatory diseases
Inventors
Menet, Christel Jeanne Marie • SMITS, Koen Kurt
Assignees
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Publication Number
US-12558360-B2
Publication Date
2026-02-24
Expiration Date
Abstract
A novel compound able to inhibit JAK is disclosed, that comprises a compound of Formula 1: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 novel Janus kinase (JAK) inhibitor compound of Formula (I) and related variants, including pharmaceutically acceptable salts and solvates. The compounds specifically inhibit JAK1 and JAK2, with lower potency toward TYK2 and JAK3.
The invention addresses improved in vivo potency versus structurally similar compounds. This improvement is described as potentially enabling lower dosing and is associated with therapeutic use across inflammatory and autoimmune disease areas.
The document further provides pharmaceutical composition forms and chemical synthesis routes to prepare Formula (I) embodiments with variable substituents, including approaches described as preparation of intermediates and coupling/amide-formation strategies. The invention is described as supporting treatment of a wide range of conditions, including inflammatory/autoimmune/proliferative diseases, transplantation rejection, diseases involving impaired cartilage turnover and congenital cartilage malformations, and IL6-hypersecretion-associated conditions such as Castleman’s disease and mesangial proliferative glomerulonephritis.
Claims Coverage
Independent claim coverage comprises three independent methods for treating atopic dermatitis using a compound of Formula (I) or a pharmaceutically acceptable salt, either directly, as part of a pharmaceutical composition with a pharmaceutically acceptable carrier, or together with a further therapeutic agent. Three inventive features are present.
Administering a Formula (I) compound to treat atopic dermatitis
A method for the treatment of atopic dermatitis comprising administering an amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof, sufficient to effect said treatment.
Administering a pharmaceutical composition with a Formula I compound and a carrier
A method for the treatment of atopic dermatitis comprising administering an amount of a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of a compound of Formula I or a pharmaceutically acceptable salt thereof, sufficient to effect said treatment.
Treating atopic dermatitis with a pharmaceutical composition and a further therapeutic agent
A method for the treatment of atopic dermatitis comprising administering an amount of a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of a compound of Formula I or a pharmaceutically acceptable salt thereof, and a further therapeutic agent, sufficient to effect said treatment.
Across the independent claims, the core coverage lies in treating atopic dermatitis by administering a Formula (I) JAK inhibitor, either directly, as part of a pharmaceutical composition with a pharmaceutically acceptable carrier, and/or in combination with a further therapeutic agent sufficient to effect the treatment.
Stated Advantages
Improved in vivo potency versus structurally similar compounds.
Potentially enabling lower dosing.
hERG QT liability example indicating IC50 >150 μM for Compound 1.
Documented Applications
Treatment of atopic dermatitis, including direct administration of a compound of Formula (I) or a pharmaceutically acceptable salt sufficient to effect the treatment.
Treatment of atopic dermatitis using a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of a compound of Formula I or a pharmaceutically acceptable salt sufficient to effect treatment.
Treatment of atopic dermatitis using a pharmaceutical composition containing a Formula I compound or a pharmaceutically acceptable salt together with a further therapeutic agent sufficient to effect treatment.
Inflammatory/autoimmune/proliferative diseases.
Transplantation rejection.
Diseases involving impaired cartilage turnover and congenital cartilage malformations.
IL6-hypersecretion-associated conditions, including Castleman’s disease and mesangial proliferative glomerulonephritis.
In-vivo inflammatory evaluation in a collagen-induced arthritis (CIA) rat model, including clinical arthritis scoring and pharmacokinetic comparisons.
In-vitro enzymatic inhibition and kinetic assays for JAK1, JAK2, JAK3, and TYK2 and cellular JAK-STAT signaling assays with pSTAT1 and pSTAT5 readouts.
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