- Peptidylarginine deiminase inhibitor and application thereof
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The invention belongs to the technical field of medicine, and particularly relates to a peptidylarginine deiminase PAD4 inhibitor compound shown in a formula (I) or pharmaceutically acceptable salts,stereoisomers and tautomers thereof, as well as pharmaceutical compositions, pharmaceutical preparations and application thereof. X, Y, R1, R2, R3, R4, R5, R7, R8, R9, ring B and m are as defined in the specification. The compound has inhibitory effect on peptidylarginine deiminase PAD4, and can be used for treating various diseases, such as rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, multiple sclerosis, cystic fibrosis, cancer, cutaneous lupus erythematosus, asthma and psoriasis.
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Paragraph 0426; 0427; 0431; 0432; 0433
(2019/09/10)
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- PYRIMIDINE AND TRIAZINE DERIVATIVES AND THEIR USE AS AXL INHIBITORS
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Compounds of the general formula(I): (I) processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.
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Page/Page column 82
(2016/07/05)
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- Discovery of 4-azaindoles as novel inhibitors of c-Met kinase
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A series of 4-azaindole inhibitors of c-Met kinase is described. The postulated binding mode was confirmed by an X-ray crystal structure and series optimisation was performed on the basis of this structure. Future directions for series development are dis
- Porter, John,Lumb, Simon,Franklin, Richard J.,Gascon-Simorte, Jose M.,Calmiano, Mark,Riche, Kelly Le,Lallemand, Benedicte,Keyaerts, Jean,Edwards, Helen,Maloney, Alison,Delgado, Jean,King, Lloyd,Foley, Anne,Lecomte, Fabien,Reuberson, James,Meier, Christoph,Batchelor, Mark
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scheme or table
p. 2780 - 2784
(2009/12/25)
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- 6-Substituted-5H-pyrrolo[2,3-b]pyrazines via palladium-catalyzed heteroannulation from N-(3-chloropyrazin-2-yl)-methanesulfonamide and alkynes
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We herein report the efficient and convenient synthesis of 6-substituted-5H-pyrrolo[2,3-b]pyrazines. The reaction is a palladium-catalyzed heteroannulation process followed by deprotection to yield the desired pyrrolo[2,3-b]pyrazine substrates. The reacti
- Hopkins, Corey R.,Collar, Nicola
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p. 8087 - 8090
(2007/10/03)
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