1263772-79-7

Upstream product

• 36140-83-7 1-cyanoacetyl-3,5-dimethylpyrazole 
• 1263774-30-6 [benzyl-(2-chloropropyl)-amino]acetic acid tert-butyl ester 
• 1263774-31-7 1-benzyl-3-methylazetidine-2-carboxylic acid tert-butyl ester 
• 1263774-32-8 3-methylazetidine-1,2-dicarboxylic acid di-tert-butyl ester 
• 1263774-33-9 3-methyl-2-(3-methyl-but-2-enyl)-azetidine-1,2-dicarboxylic acid di-tert-butyl ester 
• 1263774-34-0 3-methyl-2-(2-oxoethyl)azetidine-1,2-dicarboxylic acid di-tert-butyl ester 
• 1263774-35-1 2-(2-benzylaminoethyl)-3-methylazetidine-1,2-dicarboxylic acid di-tert-butyl ester 
• 1263774-37-3 6-benzyl-3-methyl-1,6-diazaspiro[3.4]octan-5-one 
• 1263774-38-4 6-benzyl-3-methyl-1,6-diazaspiro[3.4]octane-1-carboxylic acid tert-butyl ester 
• 1263774-39-5 3-methyl-1,6-diazaspiro[3.4]octane-1-carboxylic acid tert-butyl ester 
• 1263774-40-8 3-methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1,6-diazaspiro[3.4]octane-1-carboxylic acid tert-butyl ester 
• 3680-69-1 4-chloro-1H-pyrrolo[2,3-d]pyrimidine 

Downstream Products

• 1263774-59-9 delgocitinib 

Relevant academic research and scientific papers

Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders

Dermatologic disorders such as atopic dermatitis arise from genetic and environmental causes and are complex and multifactorial in nature. Among possible risk factors, aberrant immunological reactions are one of the leading etiologies. Immunosuppressive agents including topical steroids are common treatments for these disorders. Despite their reliability in clinical settings, topical steroids display side effects, typified by skin thinning. Accordingly, there is a need for alternate effective and well-tolerated therapies. As part of our efforts to investigate new immunomodulators, we have developed a series of JAK inhibitors, which incorporate novel three-dimensional spiro motifs and unexpectedly possess both excellent physicochemical properties and antidermatitis efficacy in the animal models. One of these compounds, JTE-052 (ent-60), also known as delgocitinib, has been shown to be effective and well-tolerated in human clinical trials and has recently been approved in Japan for the treatment of atopic dermatitis as the first drug among Janus kinase inhibitors.

NITROGEN-CONTAINING SPIROCYCLIC COMPOUNDS AND PHARMACEUTICAL USES THEREOF

A compound of the following general formula [I]: wherein each symbol has the same meaning as defined herein, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutical use of the same in treating organ transplant rejection, graft versus host reaction after transplantation, autoimmune disease, allergic disease and chronic myeloproliferative disease.