861076-28-0Relevant academic research and scientific papers
QUINAZOLINE DERIVATIVES AS ANTITUMOR AGENTS
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Page/Page column 151-153, (2020/04/25)
The present application relates to novel quinazoline compounds as inhibitors of type I receptor tyrosine kinases, the pharmaceutical compositions comprising one or more of the compounds and salts thereof as an active ingredient, and the use of the compounds and salts thereof in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals and especially in humans.
AMINOPYRAZOLE DERIVATIVES
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Paragraph 0226; 0227, (2018/05/03)
An objective of the present invention is to provide low-molecular-weight compounds that can inhibit Src family kinases. The present invention relates to compounds represented by general formula (I) or pharmacologically acceptable salts thereof. In the formula, Ar1 is optionally substituted C6-10 arylene or 5- to 10-membered heteroarylene, and Ar2 is optionally substituted C6-10 aryl or 5- to 10-membered heteroaryl. R1 and R2 are defined as described in the specification.
Substituted quinolinone inhibitor
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Paragraph 0458-0461, (2018/09/08)
The invention provides a substituted quinolinone inhibitor and relates to a compound as shown in a formula (II) which is described in the specification or a pharmaceutically acceptable salt, solvate,active metabolite, polymorphic substance, ester, isomer or prodrug thereof, a pharmaceutical composition containing the compound as shown in the formula (II), and application of the compound and the pharmaceutical composition to treatment of diseases related to abnormal TOPK activity.
QUINUCLIDINES FOR MODULATING ALPHA 7 ACTIVITY
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Paragraph 0216; 0217, (2016/02/29)
Provided are substituted quinuclidine compounds, pharmaceutical compositions comprising such compounds, and methods of modulating α7 nicotinic acetylcholine receptors and treating neurological disorders using such compounds.
INHIBITORS OF KRAS G12C
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Page/Page column 247, (2015/04/28)
Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R1, R2a, R3a, R3b, R4a, R4b, G1, G2, L1, L2, m1, m2, A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
SUBSTITUTED ACETYL-COA CARBOXYLASE INHIBITORS
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Page/Page column 32, (2012/11/07)
The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; wherein G is R1, R2 and R3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
CAGED CERAMIDE-1-PHOSPHATE DERIVATIVES
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Page/Page column 33, (2011/06/11)
The invention relates to novel caged ceramide 1-phosphate (C1P) and the method of using them for delivering C1P intracellularly in vitro and in vivo, for research and therapeutic purposes.
Caged ceramide 1-phosphate analogues: Synthesis and properties
Lankalapalli, Ravi S.,Ouro, Alberto,Arana, Lide,Gomez-Munoz, Antonio,Bittman, Robert
supporting information; experimental part, p. 8844 - 8847 (2010/03/01)
(Chemical Equation Presented) Sphingolipid phosphate analogues bearing 7-(diethylamino)-coumarin (DECM) and 4-bromo-5-hydroxy-2-nitrobenzhydryl (BHNB) groups in a photolabile ester bond were synthesized. The ability of the "caged" ceramide 1-phosphate analogues to release the bioactive parent molecule upon irradiation at 400-500 nm was demonstrated by stimulation of macrophage cell proliferation. 2009 American Chemical Society.
Glucokinase Activators
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Page/Page column 109-111, (2009/12/05)
Compounds are provided for use with glucokinase that comprise the formula: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
