14542-12-2Relevant academic research and scientific papers
Synthesis of novel bicyclo[4.1.0]heptane and bicyclo[3.1.0]hexane derivatives as melanin-concentrating hormone receptor R1 antagonists
Su, Jing,Tang, Haiqun,McKittrick, Brian A.,Gu, Huizhong,Guo, Tao,Qian, Gang,Burnett, Duane A.,Clader, John W.,Greenlee, William J.,Hawes, Brian E.,O'Neill, Kim,Spar, Brian,Weig, Blair,Kowalski, Timothy,Sorota, Steve
, p. 4845 - 4850 (2007)
To address the hERG liability of MCHR1 antagonists such as 1 and 2, new analogs such as 4 and 5 that incorporated a polar heteroaryl group were designed and synthesized. Biological evaluation confirmed that these new analogs retained MCH R1 activity with
BTK Inhibitors and uses thereof
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Paragraph 0962-0967, (2020/05/02)
The invention discloses a bruton's tyrosine kinase (BTK) inhibitor and use thereof. Specifically, the invention provides heteroaromatic compounds or stereoisomers, geometrical isomers, tautomers, racemates, nitrogen oxides, hydrates, solvates, metabolites and pharmaceutically acceptable salts or prodrugs thereof, and pharmaceutical compositions containing the heteroaromatic compounds; the invention also discloses use of the heteroaromatic compounds or the pharmaceutical compositions containing the heteroaromatic compounds in preparation of medicines; the medicines can be used for treating autoimmune diseases, inflammatory diseases or proliferative diseases.
Dihydroisoquinoline compound
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Paragraph 0449-0454, (2020/07/24)
The invention provides a dihydroisoquinoline compound or a pharmaceutically acceptable salt, ester, isomer, solvate, hydrate, prodrug or isotope marker thereof. The compound has a structure shown as ageneral formula I. The compound has extremely strong activity of inhibiting hepatitis B surface antigen, also has extremely strong activity of inhibiting hepatitis B DNA, has relatively high bioavailability, can play a drug effect at a relatively low dosage, and reduces the potential toxicity of the compound.
Peptidomimetic Vinyl Heterocyclic Inhibitors of Cruzain Effect Antitrypanosomal Activity
Chenna, Bala C.,Li, Linfeng,Mellott, Drake M.,Zhai, Xiang,Siqueira-Neto, Jair L.,Calvet Alvarez, Claudia,Bernatchez, Jean A.,Desormeaux, Emily,Alvarez Hernandez, Elizabeth,Gomez, Jana,McKerrow, James H.,Cruz-Reyes, Jorge,Meek, Thomas D.
, p. 3298 - 3316 (2020/04/08)
Cruzain, an essential cysteine protease of the parasitic protozoan, Trypanosoma cruzi, is an important drug target for Chagas disease. We describe here a new series of reversible but time-dependent inhibitors of cruzain, composed of a dipeptide scaffold appended to vinyl heterocycles meant to provide replacements for the irreversible reactive "warheads" of vinyl sulfone inactivators of cruzain. Peptidomimetic vinyl heterocyclic inhibitors (PVHIs) containing Cbz-Phe-Phe/homoPhe scaffolds with vinyl-2-pyrimidine, vinyl-2-pyridine, and vinyl-2-(N-methyl)-pyridine groups conferred reversible, time-dependent inhibition of cruzain (Ki? = 0.1-0.4 μM). These cruzain inhibitors exhibited moderate to excellent selectivity versus human cathepsins B, L, and S and showed no apparent toxicity to human cells but were effective in cell cultures of Trypanosoma brucei brucei (EC50 = 1-15 μM) and eliminated T. cruzi in infected murine cardiomyoblasts (EC50 = 5-8 μM). PVHIs represent a new class of cruzain inhibitors that could progress to viable candidate compounds to treat Chagas disease and human sleeping sickness.
Hetero-aromatic compound and its use in medicine (by machine translation)
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Paragraph 0798; 0799, (2017/08/29)
The invention discloses heteroaromatic compound and its use in medicine, in particular, the invention provides a hetero-aromatic compound or its stereoisomers, geometric isomers, tautomers, racemate, nitrogen oxide, hydrate, solvate, metabolite, pharmaceutically acceptable salt or prodrug, and containing said pharmaceutical composition; the invention also discloses the compound or its pharmaceutical compositions in use for preparing a medicament, and in the treatment of autoimmune diseases or proliferative diseases of application. (by machine translation)
Zinc-Mediated Efficient and Selective Reduction of Carbonyl Compounds
Mandal, Tirtha,Jana, Snehasish,Dash, Jyotirmayee
, p. 4972 - 4983 (2017/09/13)
We herein describe for the first time that an optimized combination of Zn and NH4Cl can be used for the selective reduction of aldehydes and ketones to the corresponding alcohols. The aldehyde and keto groups are selectively reduced in the presence of azide, cyano, epoxy, ester, and carbon–carbon double-bond functional groups. A broad functional-group compatibility, chemoselective reduction of aldehydes in the presence of ketones, and selective reduction of isatins at the C3 carbonyl group are the highlights of the present method.
TRIAZOLE-ISOXAZOLE COMPOUND AND MEDICAL USE THEREOF
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Paragraph 3410, (2016/06/06)
A compound represented by Formula [I]: or pharmaceutically acceptable salt thereof, wherein each symbol is as defined in the description.
Design, synthesis and bioactivities evaluation of novel quinazoline analogs containing oxazole units
Hou, Xuehui,Zhang, Jingyu,Zhao, Xuan,Chang, Liming,Hu, Ping,Liu, Hongmin
supporting information, p. 538 - 544 (2014/07/08)
A novel type of quinazoline derivatives, which were designed by the combination of quinazoline as the backbone and oxazole scaffold as the substituent, have been synthesized and their biological activities were evaluated for anti-proliferative activities and EGFR inhibitory potency. Compound 12b demonstrated the most potent inhibitory activity (IC 50=0.95 μmol/L for EGFR), which could be optimized as a potential EGFR inhibitor in the further study. The structures of the synthesized quinazoline analogs and all intermediates were comfirmed by 1H and 13C NMR, 2D NMR spectra, IR spectra and MS spectra. Copyright
SUBSTITUTED XANTHINES AND METHODS OF USE THEREOF
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Paragraph 0304; 0305, (2014/09/30)
Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5.
HETEROCYCLE-SUBSTITUED TETRACYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR TREATMENT OF VIRAL DISEASES
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Page/Page column 75, (2014/08/06)
The present invention relates to novel Heterocycle-Substituted Tetracyclic Compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, A', R 2 R 3, R 4 and R are as defined herein. The present i
