639858-63-2Relevant articles and documents
2-OXO-2,3-DIHYDRO-1H-IMIDAZO[4,5-B]PYRIDIN-6-YL)-4-METHYLBENZAMIDE DERIVATIVES AND SIMILAR COMPOUNDS AS RIPK2 INHIBITORS FOR TREATING E.G. AUTOIMMUNE DISEASES
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Paragraph 0345-0346, (2020/10/20)
Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein α, β, R2, R3, R4, R5, R8, R9, X1, X6, and X7 are defined in the specification. The compounds of formula 1 are receptor-interacting protein kinase 2 (RIPK2) inhibitors for treating e.g. type I hypersensitivity reactions, autoimmune diseases, inflammatory disorders, cancer and non-malignant proliferative disorders, such as e.g. allergic rhinitis, asthma, atopic dermatitis, rheumatoid arthritis, multiple sclerosis, systemic lupus erythematosus, lupus nephritis, psoriasis, immune thrombocytopenic purpura, inflammatory bowel disease, chronic obstructive pulmonary disease, Sjogren's syndrome, ankylosing spondylitis, Behcet's disease, graft versus host disease, pemphigus vulgaris, idiopathic plasmacytic lymphadenopathy, atherosclerosis, myocardial infarction and thrombosis. The present description discloses the preparation of exemplary compounds as well as pharmacological data thereof (e.g. pages 107 to 208; examples 1 to 109; table 1). An exemplary compound is e.g. N-cyclopropyl-2-fluoro-5-(l-(2-fluoroethyl)-3-(l-hydroxy-2-methylpropan-2-yl)-2-oxo-2,3-dihydro-lH-imidazo[4,5-b]pyridin-6-yl)-4-methylbenzamide (example 1).
Discovery and evaluation of N-cyclopropyl-2,4-difluoro-5-((2-(pyridin-2- ylamino)thiazol-5-ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2
Borzilleri, Robert M.,Bhide, Rajeev S.,Barrish, Joel C.,D'Arienzo, Celia J.,Derbin, George M.,Fargnoli, Joseph,Hunt, John T.,Jeyaseelan Sr., Robert,Kamath, Amrita,Kukral, Daniel W.,Marathe, Punit,Mortillo, Steve,Qian, Ligang,Tokarski, John S.,Wautlet, Barri S.,Zheng, Xiaoping,Lombardo, Louis J.
, p. 3766 - 3769 (2007/10/03)
Substituted 3-((2-(pyridin-2-ylamino)thiazol-5-ylmethyl)-amino)benzamides were identified as potent and selective inhibitors of vascular endothelial growth factor receptor-2 (VEGFR-2) kinase activity. The enzyme kinetics associated with the VEGFR-2 inhibi