1142188-60-0Relevant articles and documents
DEGRADATION OF ANDROGEN RECEPTOR (AR) BY CONJUGATION OF AR ANTAGONISTS WITH E3 LIGASE LIGAND AND METHODS OF USE
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Paragraph 0138-0140, (2021/04/02)
Provided herein are novel bifunctional compounds formed by conjugating AR antagonist moieties with E3 ligase Ligand moieties, which function to recruit targeted proteins to E3 Ubiquitin ligase for degradation, and methods of preparation and uses thereof.
KRAS G12C INHIBITORS
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Paragraph 0416, (2017/12/18)
The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
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.