273-97-2Relevant academic research and scientific papers
COMPOUND HAVING ZNF143 INHIBITORY ACTIVITY AND USE THEREOF
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Paragraph 0090; 0102; 0104, (2016/10/27)
PROBLEM TO BE SOLVED: To provide a compound having a ZNF143 inhibitory activity as well as to provide a ZNF143 inhibitory agent and pharmaceutical composition containing the same. SOLUTION: Provided is a compound represented by formula (I) or a salt thereof as well as a ZNF143 inhibitory agent containing the same and a pharmaceutical composition having the same as an active ingredient. A-B-C-D (I)[A is H, a methyl group, a naphthyl group, a phenyl group or a nitrogen-containing heterocyclic ring; B is as shown below, and C is an amide bond or a heteroaromatic ring containing N and O; D is a substituted/unsubstituted phenyl group or a monocyclic heteroaromatic ring containing N or S; and C and D are both fused heterocyclic ring or the like optionally having a substituent group.]. SELECTED DRAWING: Figure 1 COPYRIGHT: (C)2016,JPOandINPIT
3-(Oxazolo[4,5-b]pyridin-2-yl)anilides as a novel class of potent inhibitors for the kinetoplastid Trypanosoma brucei, the causative agent for human African trypanosomiasis
Ferrins, Lori,Rahmani, Rapha?l,Sykes, Melissa L.,Jones, Amy J.,Avery, Vicky M.,Teston, Eliott,Almohaywi, Basmah,Yin, JieXiang,Smith, Jason,Hyland, Chris,White, Karen L.,Ryan, Eileen,Campbell, Michael,Charman, Susan A.,Kaiser, Marcel,Baell, Jonathan B.
, p. 450 - 465 (2013/10/01)
A whole organism high-throughput screen of approximately 87,000 compounds against Trypanosoma brucei brucei led to the recent discovery of several novel compound classes with low micromolar activity against this organism and without appreciable cytotoxici
1,3-Dibromo-5,5-dimethylhydantoin as an efficient homogeneous catalyst for synthesis of benzoxazoles, benzimidazoles, and oxazolo[4,5-b]pyridines
Hojati, Seyedeh Fatemeh,Maleki, Behrooz,Beykzadeh, Zahra
experimental part, p. 87 - 91 (2011/09/19)
A simple and highly efficient method for synthesis of benzoxazoles, benzimidazoles, and oxazolo[4,5-b]pyridines is described. Condensation of orthoesters with o-substituted anilines or 2-amino-3-hydroxypyridine was performed in the presence of catalytic amounts of commercially available, inexpensive, and moisture-stable 1,3-dibromo-5,5-dimethylhydantoin under solvent-free conditions. The corresponding heterocycles were obtained in good to excellent yields. The main advantages of the present procedure are mild reaction conditions, short reaction times, high yields of products, easy work-up, and absence of solvent. Graphical abstract: [Figure not available: see fulltext.]
Copper-catalyzed direct oxidative C-H amination of benzoxazoles with formamides or secondary amines under mild conditions
Li, Yaming,Xie, Yusheng,Zhang, Rong,Jin, Kun,Wang, Xiuna,Duan, Chunying
supporting information; experimental part, p. 5444 - 5449 (2011/08/06)
A facile, efficient, and practical method for copper-catalyzed direct C-H amination of benzoxazoles with formamides or secondary amines has been developed. The system can be performed in the absence of external base and only requires O2 or even air as oxidant. A variety of substituted benzoxazol-2-amines were synthesized with moderate to excellent yield.
Mild and efficient synthesis of benzoxazoles, benzothiazoles, benzimidazoles, and oxazolo[4,5-b]pyridines catalyzed by Bi(III) salts under solvent-free conditions
Mohammadpoor-Baltork, Iraj,Khosropour, Ahmad R.,Hojati, Seyedeh F.
, p. 663 - 667 (2008/02/07)
A series of benzoxazoles, benzothiazoles, benzimidazoles, and oxazolo[4,5-b]pyridines was efficiently synthesized from the reactions of o-aminophenols, o-aminothiophenol, o-phenylenediamines, and 2-amino-3- hydroxypyridine with orthoesters in the presence of catalytic amounts of Bi(III) salts, such as Bi(TFA)3, Bi(OTf)3, and BiOClO4 ? xH2O under solvent-free conditions. The remarkable features of this new protocol are high conversion, very short reaction times, cleaner reaction profiles under solvent-free conditions, straightforward procedure, and use of relatively non-toxic catalysts. Springer-Verlag 2007.
HALOALKYL CONTAINING COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
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Page/Page column 46; 52; 55, (2010/02/11)
The application is directed to haloalkyl-substituted compounds of Formula (I), wherein R1, R1a, R2, R3, R4’ and E are as defined in the claims. The compounds are inhibitors of cysteine proteases, in p
AMIDINO COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
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Page/Page column 21; 24, (2010/02/12)
The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
SILINANE COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
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Page/Page column 56; 59-60, (2008/06/13)
The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is also directed to pharmaceutical compositions comprising these compounds and processes for preparing them. The present invention is also directed to the use of these inhibitors in combination with a therapy that causes a deleterious immune response in patients receiving the therapy.
Process for preparing heteroaryl and unsaturated heterocycloalkylmagnesium reagents and uses thereof
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Page 18, (2010/02/05)
The present invention is directed to a novel process for preparing heteroaryl and unsaturated heterocycloalkylmagnesium reagents that are useful in the synthesis of a variety of pharmaceuticals, in particular certain cysteine protease inhibitors.
AMIDINO COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
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Page/Page column 44; 50; 53;, (2010/02/09)
The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceu
