98977-38-9Relevant academic research and scientific papers
KRAS G12C INHIBITORS
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Paragraph 0314, (2020/03/23)
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.
BRIDGED TRICYCLIC CARBAMOYLPYRIDONE COMPOUNDS AND THEIR PHARMACEUTICAL USE
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Paragraph 0951, (2020/10/20)
Compounds for use in treating or preventing human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2, L, W1, W2, X, Y, and Z are as defined herein. Methods associated with the preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
Synthesis of azabicyclo[n.1.0]alkane-derived bifunctional building blocks via the Corey–Chaykovsky cyclopropanation
Yarmoliuk, Dmytro V.,Serhiichuk, Dmytro,Smyrnov, Vladyslav,Tymtsunik, Andriy V.,Hryshchuk, Oleksandr V.,Kuchkovska, Yuliya,Grygorenko, Oleksandr O.
supporting information, p. 4611 - 4615 (2018/11/27)
An efficient approach towards the synthesis of monoprotected azabicyclo[5.1.0]octane-derived conformationally restricted γ-amino acids and diamines is reported. Optimization of the conditions for the key Corey–Chaykovsky reaction allowed the construction
Method for preparing beixifloxacin intermediate compound
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Paragraph 0082; 0083; 0084; 0085; 0086; 0087; 0088-0099, (2018/03/01)
The invention provides a method for preparing a beixifloxacin intermediate compound VI. The method comprises the steps of: reacting a compound of a formula III with an upper protective group, an aminotransferase catalying and a deprotecting group to obtain a compound shown in a formula VI. The method can be used for preparing the beixifloxacin intermediate compound VI rapidly and effectively. Rawmaterials are simple and easy to obtain, the reaction is simple and easy to operate, harsh reaction conditions are not required, a production period is short, yield of a target product is high, separation and purification of the target product are simple, optical purity is high, the method is easy to achieve mass production.
2-AMINOPYRIMIDINE COMPOUNDS AS SEROTONIN RECEPTOR MODULATORS
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Page/Page column 32-33, (2010/06/11)
Certain 2-aminopyrimidine compounds are serotonin receptor modulators useful in the treatment of diseases mediated by serotonin receptors.
2-Alkyl-4-aryl-pyrimidine fused heterocycles as selective 5-HT2A antagonists
Shireman, Brock T.,Dvorak, Curt A.,Rudolph, Dale A.,Bonaventure, Pascal,Nepomuceno, Diane,Dvorak, Lisa,Miller, Kirsten L.,Lovenberg, Timothy W.,Carruthers, Nicholas I.
, p. 2103 - 2108 (2008/09/20)
The synthesis and SAR for a novel series of 2-alkyl-4-aryl-tetrahydro-pyrido-pyrimidines and 2-alkyl-4-aryl-tetrahydro-pyrimido-azepines is described. Representative compounds were shown to be subtype selective 5-HT2A antagonists. Optimal place
PYRIMIDINE COMPOUNDS AS SEROTONIN RECEPTOR MODULATORS
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Page/Page column 27, (2008/06/13)
Certain pyrimidine-containing compounds are serotonin receptor modulators useful in the treatment of serotonin-mediated diseases.
Glycine Antagonists. Synthesis, Structure, and Biological Effects of Some Bicyclic 5-Isoxazolol Zwitterions
Brehm, Lotte,Krogsgaard-Larsen, Povl,Schaumburg, Kjeld,Johansen, Joergen S.,Falch, Erik,Curtis, David R.
, p. 224 - 229 (2007/10/02)
The bicyclic 5-isoxazolol zwitterions 4,5,6,7-tetrahydroisoxazolopyridin-3-ol (3, iso-THPO), 5,6,7,8-tetrahydro-4H-isoxazoloazepin-3-ol (12, iso-THAO), and 5,6,7,8-tetrahydro-4H-isoxazoloazepin-3-ol (13, iso-THIA), which are structurally related to the glycine antagonist 5,6,7,8-tetrahydro-4H-isoxazoloazepin-3-ol (iso-THAZ), have been synthesized and tested biologically.All of these compounds were glycine antagonists approximetely equipotent with iso-THAZ during microelectrophoretic ejection near cat spinal neurons.In contrast to iso-THAZ, which also interacts with 4-aminobutyric acid (GABA) receptors in rat brains, neither 12 or 13 show any significant affinities for GABA binding or uptake mechanisms in vitro.The glycine antagonist 3 was, however, shown also to be a moderately potent inhibitor of GABA uptake.The structure of 12 was established by an X-ray analysis.The bond lengths of the 5-isoxazolol anionic moiety of 12 are in agreement with a pronounced delocalization of the negative charge of this compound.
