- Preparation Method for Amide Compounds and Use Thereof in Medical Field
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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.
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Paragraph 0184; 0186; 0534-0536
(2022/02/06)
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- NOVEL SUBSTITUTED SPIRO-[INDOLINE HETEROCYCLOALKANE] COMPOUNDS AS PHOSPHODIESTERASE INHIBITORS
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The invention relates to novel spiro-[indoline heterocycloalkane] compounds characterized in that the compound has general formula (I) in which the chemical groupings, substituents, variables and indices are as defined in the description, and to their use as medicaments, in particular as medicaments for the treatment of conditions and diseases that can be treated by inhibition of the PDE4 enzyme.
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Page/Page column 133-134
(2017/07/14)
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- Discovery and in vivo evaluation of dual PI3Kβ/δ inhibitors
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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.
- 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.
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p. 7667 - 7685
(2012/10/29)
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- HETEROCYCLIC COMPOUNDS AND THEIR USES
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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.
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Page/Page column 49-50
(2011/01/12)
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- ALKYNYL ALCOHOLS AS KINASE INHIBITORS
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Selected compounds are effective for prophylaxis and treatment of inflammation and inflammatory disorders, such as NIK-mediated disorders. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, inflammation and the like.
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Page/Page column 61-62
(2010/01/30)
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