677302-44-2Relevant articles and documents
Peptidylarginine deiminase inhibitor and application thereof
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Paragraph 0410; 0411; 0412; 0413; 0414, (2019/09/10)
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.
Discovery of 4-azaindoles as novel inhibitors of c-Met kinase
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
scheme or table, p. 2780 - 2784 (2009/12/25)
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