888494-37-9Relevant 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
Noji, Satoru,Hara, Yoshinori,Miura, Tomoya,Yamanaka, Hiroshi,Maeda, Katsuya,Hori, Akimi,Yamamoto, Hiroshi,Obika, Shingo,Inoue, Masafumi,Hase, Yasunori,Orita, Takuya,Doi, Satoki,Adachi, Tsuyoshi,Tanimoto, Atsuo,Oki, Chika,Kimoto, Yukari,Ogawa, Yoshihiro,Negoro, Tamotsu,Hashimoto, Hiromasa,Shiozaki, Makoto
, p. 7163 - 7185 (2020/09/11)
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.
Stereocontrolled synthesis of 3-substituted azetidinic amino acids
Sivaprakasam, Mangaleswaran,Couty, Fran?ois,Evano, Gwilherm,Srinivas,Sridhar,Rao, K. Rama
, p. 781 - 785 (2007/10/03)
A set of enantiomerically pure N-disubstituted β-amino alcohols was chlorinated by treatment with thionyl chloride. This reaction gave a mixture of regioisomeric chlorides that could be equilibrated to the more stable regioisomer by heating in DMF. The chlorides thus obtained were engaged in an intramolecular anionic ring-closure and gave access to fully protected enantio- and diastereomerically pure 2,3-cis-disubstituted azetidinic amino acids. One of the latter was deprotected and included in a short peptide sequence. Georg Thieme Verlag Stuttgart.
