Novel quinazoline-containing compound, and intermediate and application thereof
The present invention discloses a quinazoline-containing compound having the formula (IA), (IB) or (IC), or a pharmaceutically acceptable salt or a prodrug molecule thereof. The compound is suitable for use as an Aurora kinase inhibitor and is thus suitable for the treatment of Aurora-mediated diseases characterized by excessive or abnormal cell proliferation, for example, cancer.
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Paragraph 0188; 0190; 0192
(2021/06/12)
BICYCLIC KETONE COMPOUNDS AND METHODS OF USE THEREOF
The invention provides novel compounds having the general formula (I): (I) wherein R1, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds, and methods of using the compounds.
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Page/Page column 65; 66
(2019/02/02)
A facile synthesis of pyrazoles with multi-point structural diversity by 1,3-dipolar cycloaddition
We describe the synthesis of diverse pyrazoles by 1,3-dipolar cycloaddition of ethyl diazoacetate with various acetylenes in refluxing toluene. The product pyrazoles are useful starting points for preparing a diverse collection of trisubstituted pyrazole
Cheung, Kwai Ming J.,Reynisson, Jóhannes,McDonald, Edward
supporting information; experimental part
p. 5915 - 5918
(2010/11/18)
1,3-dipolar cycloaddition of ethyl diazoacetate to alkynes in the pores of zeolite NaY
Zeolite NaY promotes 1,3-dipolar cycloaddition of ethyl diazoacetate to alkynes having an electron-withdrawing group to afford the corresponding functionalized pyrazoles in high yields. The activation of the dipolarophile inside the pores of NaY is proposed based on the 13CMASNMR analysis. Copyright
Agonist lead identification for the high affinity niacin receptor GPR109a
A strategy for lead identification of new agonists of GPR109a, starting from known compounds shown to activate the receptor, is described. Early compound triage led to the formulation of a binding hypothesis and eventually to our focus on a series of pyrazole acid derivatives. Further elaboration of these compounds provided a series of 5,5-fused pyrazoles to be used as lead compounds for further optimization.
Gharbaoui, Tawfik,Skinner, Philip J.,Shin, Young-Jun,Averbuj, Claudia,Jung, Jae-Kyu,Johnson, Benjamin R.,Duong, Tracy,Decaire, Marc,Uy, Jane,Cherrier, Martin C.,Webb, Peter J.,Tamura, Susan Y.,Zou, Ning,Rodriguez, Nathalie,Boatman, P. Douglas,Sage, Carleton R.,Lindstrom, Andrew,Xu, Jerry,Schrader, Thomas O.,Smith, Brian M.,Chen, Ruoping,Richman, Jeremy G.,Connolly, Daniel T.,Colletti, Steven L.,Tata, James R.,Semple, Graeme
p. 4914 - 4919
(2008/02/12)
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