67193-97-9Relevant academic research and scientific papers
HETEROCYCLE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF CNS DISORDERS
-
Paragraph 00219; 00220, (2017/05/17)
The present application relates to novel heterocycle derivatives of Formula (I), to processes for preparing them, pharmaceutical compositions containing them, and their use thereof in the treatment or prevention of acute and/or chronic neurological disord
Discovery of anilinopyrimidine-based naphthamide derivatives as potent VEGFR-2 inhibitors
Lv, Yongcong,Li, Mengyuan,Cao, Sufen,Tong, Linjiang,Peng, Ting,Wei, Lixin,Xie, Hua,Ding, Jian,Duan, Wenhu
supporting information, p. 1375 - 1380 (2015/07/15)
Vascular endothelial growth factor receptor-2 (VEGFR-2) plays an important role in tumor angiogenesis, and inhibition of the VEGFR-2 signaling pathway has emerged as an attractive strategy for the treatment of cancer. Herein, we describe the design, synthesis, and biological evaluation of anilinopyrimidine-based naphthamide derivatives as potent VEGFR-2 inhibitors. Among the new derivatives, compound 3k exhibited high VEGFR-2 inhibitory potency in both enzymatic and VEGF-induced HUVEC cellular proliferation assays (IC50 = 0.5 and 9.8 nM, respectively). Kinase selectivity profiling revealed that 3k was a highly selective VEGFR-2 inhibitor. Moreover, 3k effectively inhibited angiogenesis in HUVEC tube formation assay.
ANTI-NEOPLASTIC COMPOUNDS, COMPOSITIONS AND METHODS
-
Page/Page column 113-114, (2010/11/03)
Disclosed are novel compounds which are useful as therapeutics, especially in anti-neoplastic therapy and in other therapeutic regimes where cysteine protease inhibition is implicated.
BENZOMORPHOLINE DERIVATIVES AND METHODS OF USE
-
Page/Page column 36, (2009/06/27)
Selected benzomorpholine compounds are effective for prophylaxis and treatment of diseases, such as VEGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical composit
Novel 2,3-dihydro-1,4-benzoxazines as potent and orally bioavailable inhibitors of tumor-driven angiogenesis
La, Daniel S.,Belzile, Julie,Bready, James V.,Coxon, Angela,DeMelfi, Thomas,Doerr, Nicholas,Estrada, Juan,Flynn, Julie C.,Flynn, Shaun R.,Graceffa, Russell F.,Harriman, Shawn P.,Larrow, Jay F.,Long, Alexander M.,Martin, Matthew W.,Morrison, Michael J.,Patel, Vinod F.,Roveto, Philip M.,Wang, Ling,Weiss, Matthew M.,Whittington, Douglas A.,Teffera, Yohannes,Zhao, Zhiyang,Polverino, Anthony J.,Harmange, Jean-Christophe
, p. 1695 - 1705 (2008/09/20)
Angiogenesis is vital for solid tumor growth, and its prevention is a proven strategy for the treatment of disease states such as cancer. The vascular endothelial growth factor (VEGF) pathway provides several opportunities by which small molecules can act as inhibitors of endothelial proliferation and migration. Critical to these processes is signaling through VEGFR-2 or the kinase insert domain receptor (KDR) upon stimulation by its ligand VEGF. Herein, we report the discovery of 2,3-dihydro-1,4-benzoxazines as inhibitors of intrinsic KDR activity (IC50 50 a potent (KDR: a promising platform for generating kinase-based antiangiogenic therapeutic agents.
First syntheses of natural products with the 2,7-dihydroxy-2H-1,4-benzoxazin-3(4H)-one skeleton
Kluge,Hartenstein,Hantschmann,Sicker
, p. 395 - 402 (2007/10/02)
2,7-Dihydroxy-2H-1,4-benzoxazin-3(4H)-one 11 (DHBOA) and 2,4,7-trihydroxy-2H-1,4-benzoxazin-3(4H)-one 14 (TRIBOA) representing aglucones of naturally occurring acetal glucoside type allelo chemicals found in Gramineae have been for the first time synthesized by two pathways both involving selective reductive cyclizations of appropriate 7-benzyloxy-2-nitrophenol derivatives as precursors. TRIBOA 14 and its bioactive naturally occurring 7-methyl ether DIMBOA have been found to undergo a hitherto unknown transformation to the corresponding 2,6-dibromo substituted lactam forms 20 and 21 in the presence of hydrogen bromide in acetic acid, which is of value in a better understanding of the possible mode of bioactivity.
