1025721-10-1Relevant articles and documents
PHOSPHONATE CONJUGATES AND USES THEREOF
-
Paragraph 0089; 00100-00101; 00114, (2020/07/31)
Phosphonate conjugates, preferably, bisphosphonate conjugates; methods of inhibiting Ron receptor tyrosine kinase and methods of treatment of bone destruction due to cancer or other conditions utilizing the provided phosphonate conjugates.
PYRROLO PYRIMIDINE DERIVATIVE
-
Paragraph 0378, (2016/09/26)
The compound represented by general formula (I) has strong Axl inhibition activity by means of a pyridone ring structure being introduced into a pyrrolo pyrimidine skeleton, and so the result can serve as a treatment agent for Axl-related diseases, for example cancers such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glial tumors, renal disease, immune system disorders, and cardiovascular disease.
PYRIDONE AMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES
-
Paragraph 0108, (2014/09/29)
Compounds useful in the treatment of mammalian cancers and especially human cancers according to Formula I are disclosed. Formula (I). Pharmaceutical compositions and methods of treatment employing the compounds disclosed herein are also disclosed.
PYRIDONE AMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES
-
Paragraph 00189, (2013/06/06)
Compounds useful in the treatment of mammalian cancers and especially human cancers according to Formula I are disclosed. Pharmaceutical compositions and methods of treatment employing the compounds disclosed herein are also disclosed.
Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4- ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the met kinase superfamily
Schroeder, Gretchen M.,An, Yongmi,Cai, Zhen-Wei,Chen, Xiao-Tao,Clark, Cheryl,Cornelius, Lyndon A. M.,Dai, Jun,Gullo-Brown, Johnni,Gupta, Ashok,Henley, Benjamin,Hunt, John T.,Jeyaseelan, Robert,Kamath, Amrita,Kim, Kyoung,Lippy, Jonathan,Lombardo, Louis J.,Manne, Veeraswamy,Oppenheimer, Simone,Sack, John S.,Schmidt, Robert J.,Shen, Guoxiang,Stefanski, Kevin,Tokarski, John S.,Trainor, George L.,Wautlet, Barri S.,Wei, Donna,Williams, David K.,Zhang, Yingru,Zhang, Yueping,Fargnoli, Joseph,Borzilleri, Robert M.
supporting information; experimental part, p. 1251 - 1254 (2009/12/07)
Substituted N-(4-(2-aminopyridin-4-yloxy)-3-fluoro-phenyl)- 1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamides were identified as potent and selective Met kinase inhibitors. Substitution of the pyridine 3-position gave improved enzyme potency, while substitution of the pyridone 4-position led to improved aqueous solubility and kinase selectivity. Analogue 10 demonstrated complete tumor stasis in a Met- dependent GTL-16 human gastric carcinoma xenograft model following oral administration. Because of its excellent in vivo efficacy and favorable pharmacokinetic and preclinical safety profiles, 10 has been advanced into phase I clinical trials.
PYRIDINONE COMPOUNDS
-
Page/Page column 8, (2008/12/05)
The invention is directed to pyridinone compounds useful for modulating Met kinase, having the following structure: and is further directed to pharmaceutical compositions comprising the compound; and methods for treating proliferative diseases, such as ca
