1190861-43-8Relevant articles and documents
Preparation Method for Amide Compounds and Use Thereof in Medical Field
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, (2022/02/06)
Provided are a preparation method for amide compounds and use thereof in medical field. Specifically, provided are small molecule amide compounds. Such compounds are inhibitors of enhancer homolog 2 (EZH2) of Zeste gene, and can be used for preventing and/or treating related diseases mediated by EZH2, including tumors, myeloproliferative diseases or autoimmune diseases.
Discovery and in vivo evaluation of dual PI3Kβ/δ inhibitors
Gonzalez-Lopez De Turiso, Felix,Shin, Youngsook,Brown, Matthew,Cardozo, Mario,Chen, Yi,Fong, David,Hao, Xiaolin,He, Xiao,Henne, Kirk,Hu, Yi-Ling,Johnson, Michael G.,Kohn, Todd,Lohman, Julia,McBride, Helen J.,McGee, Lawrence R.,Medina, Julio C.,Metz, Daniela,Miner, Kent,Mohn, Deanna,Pattaropong, Vatee,Seganish, Jennifer,Simard, Jillian L.,Wannberg, Sharon,Whittington, Douglas A.,Yu, Gang,Cushing, Timothy D.
, p. 7667 - 7685 (2012/10/29)
Structure-based rational design led to the synthesis of a novel series of potent PI3K inhibitors. The optimized pyrrolopyridine analogue 63 was a potent and selective PI3Kβ/δ dual inhibitor that displayed suitable physicochemical properties and pharmacokinetic profile for animal studies. Analogue 63 was found to be efficacious in animal models of inflammation including a keyhole limpet hemocyanin (KLH) study and a collagen-induced arthritis (CIA) disease model of rheumatoid arthritis. These studies highlight the potential therapeutic value of inhibiting both the PI3Kβ and δ isoforms in the treatment of a number of inflammatory diseases.
HETEROCYCLIC COMPOUNDS AND THEIR USES
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Page/Page column 35; 49, (2011/01/12)
Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia ( T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.