1590372-40-9Relevant 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.
Cycloaddition Strategies for the Synthesis of Diverse Heterocyclic Spirocycles for Fragment-Based Drug Discovery
King, Thomas A.,Stewart, Hannah L.,Mortensen, Kim T.,North, Andrew J. P.,Sore, Hannah F.,Spring, David R.
, p. 5219 - 5229 (2019/08/12)
In recent years the pharmaceutical industry has benefited from the advances made in fragment-based drug discovery (FBDD) with more than 30 fragment-derived drugs currently marketed or progressing through clinical trials. The success of fragment-based drug
MexAB-OprM specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 7: Highly soluble and in vivo active quaternary ammonium analogue D13-9001, a potential preclinical candidate
Yoshida, Ken-ichi,Nakayama, Kiyoshi,Ohtsuka, Masami,Kuru, Noriko,Yokomizo, Yoshihiro,Sakamoto, Atsunobu,Takemura, Makoto,Hoshino, Kazuki,Kanda, Hiroko,Nitanai, Hironobu,Namba, Kenji,Yoshida, Kumi,Imamura, Yuichiro,Zhang, Jason Z.,Lee, Ving J.,Watkins, William J.
, p. 7087 - 7097 (2008/04/12)
A series of 4-oxo-4H-pyrido[1,2-a]pyrimidine derivatives, substituted at the 2-position with piperidines bearing quaternary ammonium salt side chains, were synthesized and evaluated for their ability to potentiate the activity of the fluoroquinolone levofloxacin (LVFX) and the β-lactam aztreonam (AZT) in Pseudomonas aeruginosa. Attachment of the charged entity using an N-ethylcarbamoyloxy linker led to the discovery of the highly soluble compound 22 (D13-9001), which maintained good potency in vitro and displayed excellent activity in vivo in a rat pneumonia model of P. aeruginosa.
USE OF (3-(1-(3-PHENYL-PROPENYL)-PIPERIDIN-4-YL)-2,3-DIHYDRO-INDOL-1-YL)-(PYRIDIN-4-YL)-METHANONE DERIVATIVES AND RELATED COMPOUNDS AS INSECTICIDES
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Page/Page column 137-138, (2010/02/12)
The use of a compound of formula (I): R3 N Y R1(I) wherein Y is a single bond, C=O, C=S or S(O)71 where m is 0, 1 or 2; R1, R2 , R3 , R4, R8 and Ra are specified organ
Chemokine receptor binding heterocyclic compounds with enhanced efficacy
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, (2008/06/13)
The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).
