307538-20-1Relevant articles and documents
COMBINATION WITH CHECKPOINT INHIBITORS TO TREAT CANCER
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Paragraph 00388-00389; 00392-00393, (2020/10/27)
A combination comprising a compound of Formula (I) and/or Formula (Ia), or a pharmaceutically acceptable salt thereof, and at least one immune checkpoint modulator. Methods for the prevention and treatment of a cancer comprises administering to a subject in need thereof, a therapeutically effective amount of a combination, the combination comprising: a compound of Formula (I) and/or Formula (Ia), or a pharmaceutically acceptable salt thereof, and at least one immune checkpoint modulator.
Synthesis and in vitro cytotoxicity of the 4-(Halogenoanilino)-6-bromoquinazolines and their 6-(4-fluorophenyl) substituted derivatives as potential inhibitors of epidermal growth factor receptor tyrosine kinase
Mphahlele, Malose Jack,Paumo, Hugues K.,Choong, Yee Siew
, (2017/12/05)
Series of the 2-unsubstituted and 2-(4-chlorophenyl)–substituted 4-anilino-6-bromoquinazolines and their 6-(4-fluorophenyl)–substituted derivatives were evaluated for in vitro cytotoxicity against MCF-7 and HeLa cells. The 2-unsubstituted 4-anilino-6-brom
SMALL MOLECULE INHIBITORS OF EGFR AND PI3K
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Page/Page column 67; 68, (2016/07/05)
This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a quinazoline structure or a quinoline structure which function as dual inhibitors of EGFR proteins and PI3K proteins, and their use as therapeutics for the treatment of cancer and other diseases.
Discovery, synthesis, and biological evaluation of thiazoloquin(az)olin(on)es as potent CD38 inhibitors
Haffner, Curt D.,Becherer, J. David,Boros, Eric E.,Cadilla, Rodolfo,Carpenter, Tiffany,Cowan, David,Deaton, David N.,Guo, Yu,Harrington, Wallace,Henke, Brad R.,Jeune, Michael R.,Kaldor, Istvan,Milliken, Naphtali,Petrov, Kim G.,Preugschat, Frank,Schulte, Christie,Shearer, Barry G.,Shearer, Todd,Smalley, Terrence L.,Stewart, Eugene L.,Stuart, J. Darren,Ulrich, John C.
, p. 3548 - 3571 (2015/05/05)
A series of thiazoloquin(az)olinones were synthesized and found to have potent inhibitory activity against CD38. Several of these compounds were also shown to have good pharmacokinetic properties and demonstrated the ability to elevate NAD levels in plasm
Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5
Felts, Andrew S.,Saleh, Sam A.,Le, Uyen,Rodriguez, Alice L.,Weaver, C. David,Conn, P. Jeffrey,Lindsley, Craig W.,Emmitte, Kyle A.
experimental part, p. 6623 - 6626 (2010/06/12)
A high-throughput cell-based screen identified a series of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of metabotropic glutamate receptor 5 (mGlu5). This Letter describes the SAR of this series and the profile of selected
METHODS AND COMPOSITIONS FOR THE TREATMENT OF PAIN, INFLAMMATION AND CANCER
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Page/Page column 44-45, (2008/12/07)
This invention relates to methods of treating, managing and preventing pain, inflammation, cancer, and ocular diseases and disorders, and to compounds and pharmaceutical compositions useful in such methods.
METHODS AND COMPOSITIONS FOR THE TREATMENT OF BODY COMPOSITION DISORDERS
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Page/Page column 47, (2008/12/07)
This invention relates to methods of treating, managing and preventing body composition disorders, and to compounds and pharmaceutical compositions useful in such methods.