1053656-57-7Relevant articles and documents
ANTI-ANGIOGENESIS COMPOUND, INTERMEDIATE AND USE THEREOF
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, (2016/04/10)
Disclosed are an anti-abnormal proliferation of angiogenesis compound represented by formula I, use and intermediate thereof. The compound has good effect against abnormal proliferation of angiogenesis, and the activity of the compound is produced by inhibiting VEGFR2. The compound can be used for treating diseases, such as wet macular degeneration, inflammation, malignant tumor and the like, caused by abnormity of angiogenesis and protein kinases such as VEGFR2, FGFR2 and the like.
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 (2015/12/23)
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.
The Role of the acidity of N-heteroaryl sulfonamides as inhibitors of Bcl-2 family protein-protein interactions
Touré, B. Barry,Miller-Moslin, Karen,Yusuff, Naeem,Perez, Lawrence,Doré, Michael,Joud, Carol,Michael, Walter,Dipietro, Lucian,Van Der Plas, Simon,McEwan, Michael,Lenoir, Francois,Hoe, Madelene,Karki, Rajesh,Springer, Clayton,Sullivan, John,Levine, Kymberly,Fiorilla, Catherine,Xie, Xiaoling,Kulathila, Raviraj,Herlihy, Kara,Porter, Dale,Visser, Michael
, p. 186 - 190 (2013/04/10)
Overexpression of the antiapoptotic members of the Bcl-2 family of proteins is commonly associated with cancer cell survival and resistance to chemotherapeutics. Here, we describe the structure-based optimization of a series of N-heteroaryl sulfonamides t