90870-83-0Relevant articles and documents
A microwave-assisted synthetic approach to analyzing disubstituted pyrrolo[2,3-d]pyrimidine diversity via ligand-free Cu-catalyzed N-arylation
Hong, Chang Sung,Park, Seung Yeong,Byeon, Jeong Seob,Yum, Eul Kgun
, p. 1641 - 1649 (2021/10/23)
Facile introduction of diverse substituents to 2- or 4-chloro-7H-pyrrolo[2,3-d]pyrimidines was examined with microwave-assisted nucleophilic substitution and Cu-catalyzed N-arylation. Microwave-assisted Cu-catalyzed N-arylation of pyrrolo[2,3-d]pyrimidines with various nucleophiles proceeded very well with diverse heteroaryl halides. Sequential microwave-assisted substitution provided good to excellent yields of 2,7- or 4,7-disubstituted pyrrolo[2,3-d]pyrimidines, with short reaction times and energy savings compared with conventional thermal heating. The diverse pyrrolo[2,3-d]pyrimidine derivatives are useful for screening drug candidates for various diseases.
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
supporting information, 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.
NOVEL HETEROCYCLIC COMPOUNDS AS METAP-2 INHIBITORS
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Page/Page column 20; 43, (2011/11/30)
Compounds of the formula I, in which D, X, Y, Z, R and R1 have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.
COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
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Page/Page column 184, (2011/06/19)
Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one Raf protein kinase. In certain aspects and embodiments, the described compounds are active in inhibiting proliferation of a Ras mutant cell line. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of B-Raf V600E mutant protein kinase, including melanoma, glioma, glioblastoma multiforme, pilocytic astrocytoma, colorectal cancer, thyroid cancer, lung cancer, ovarian cancer, prostate cancer, liver cancer, gallbladder cancer, gastrointestinal stromal tumors, biliary tract cancer, and cholangiocarcinoma. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of c-Raf-1 protein kinase, including acute pain, chronic pain or polycystic kidney disease.
Monocyclic-7H-pyrrolo[2,3-d]pyrimidine compounds, compositions, and methods of use
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Page/Page column 17, (2008/06/13)
Novel pyrrolo[2,3-d]pyrimidine compounds useful as inhibitors of the enzyme protein tyrosine kinases such as Janus Kinase 3 as well as immunosuppressive agents for organ transplants, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, Type I diabetes and complications from diabetes, cancer, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, Leukemia and other autoimmune diseases are described.