1229454-86-7Relevant academic research and scientific papers
Discovery of Oral VEGFR-2 Inhibitors with Prolonged Ocular Retention That Are Efficacious in Models of Wet Age-Related Macular Degeneration
Meredith, Erik L.,Mainolfi, Nello,Poor, Stephen,Qiu, Yubin,Miranda, Karl,Powers, James,Liu, Donglei,Ma, Fupeng,Solovay, Catherine,Rao, Chang,Johnson, Leland,Ji, Nan,Artman, Gerald,Hardegger, Leo,Hanks, Shawn,Shen, Siyuan,Woolfenden, Amber,Fassbender, Elizabeth,Sivak, Jeremy M.,Zhang, Yiqin,Long, Debby,Cepeda, Rosemarie,Liu, Fang,Hosagrahara, Vinayak P.,Lee, Wendy,Tarsa, Peter,Anderson, Karen,Elliott, Jason,Jaffee, Bruce
, p. 9273 - 9285 (2015)
The benefit of intravitreal anti-VEGF therapy in treating wet age-related macular degeneration (AMD) is well established. Identification of VEGFR-2 inhibitors with optimal ADME properties for an ocular indication provides opportunities for dosing routes beyond intravitreal injection. We employed a high-throughput in vivo screening strategy with rodent models of choroidal neovascularization and iterative compound design to identify VEGFR-2 inhibitors with potential to benefit wet AMD patients. These compounds demonstrate preferential ocular tissue distribution and efficacy after oral administration while minimizing systemic exposure.
PYRIMIDIN-4-YL)OXY)-1H-INDOLE-1-CARBOXAMIDE DERIVATIVES AND USE THEREOF
-
Page/Page column 64; 65, (2014/12/12)
This invention relates to certain metabolites of N-(1-methyl-5-(trifluoromethyl)-1H- pyrazol-3-yl)-5-((6-((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide In particular, the present invention relates to pharmaceutical compositions comprising these metabolites, as well as processes for their preparation and their use in the treatment of diseases.
Pyridyloxyindoles Inhibitors of VEGF-R2 and Use Thereof for Treatment of Disease
-
Page/Page column 70-71, (2010/06/22)
The invention relates to novel organic compounds of formula (I), and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in the treatment of tumour diseases and ocular neovascular diseases.
