专利号:US-10000487-B2 优先权日:2015-11-20 标 题 :Heterocyclic compounds that inhibit the kinase activity of Mnk useful for treating various cancers 发明人:SPRENGELER PAUL A; REICH SEIGFRIED H; WEBBER STEPHEN E; ERNST JUSTIN T 权利人:EFFECTOR THERAPEUTICS INC 摘要:The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula IA or Formula IB, as well as stereoisomers, tautomers or pharmaceutically acceptable salts thereof. n nFor Formula IA and Formula IB compounds A 1 , A 2 , A 3 , A 4 , W 1 , W 2 , Y, X, R 1 , R 2 , R 3 , R 4a , R 4b , R 5a , R 5b , R 6 , R 7 , R 8 , R 9 , R 9a , R 9b , R 10 and subscript n are as defined in the specification. The inventive Formula IA and Formula IB compounds are inhibitors of Mnk and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.
专利号:US-2012245199-A1 优先权日:2009-12-23 标题:[4 [4-(aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-(1h-pyrrolo-pyridin-yl)-methanones and synthesis thereof 发明人:CHOI-SLEDESKI YONG MI; NIEDUZAK THADDEUS R; POLI GREGORY B; SHUM PATRICK WAI-KWOK; STOKLOSA GREGORY T; ZHAO ZHICHENG 权利人:CHOI-SLEDESKI YONG MI; NIEDUZAK THADDEUS R; POLI GREGORY B; SHUM PATRICK WAI-KWOK; STOKLOSA GREGORY T; ZHAO ZHICHENG; SANOFI SA 摘要:The present invention relates herein to compounds and compositions for the treatment and amelioration of inflammatory disease. Specifically the present invention relates to compounds that having a tryptase inhibition activity and the intermediates thereof, pharmaceutical compositions comprising such compounds, and a method of treating subjects suffering from a condition disease or disorder that can be ameliorated by the administration of an inhibitor of tryptase.