- Nitrofuran compound, pharmaceutical composition and preparation method and application of nitrofuran compound
-
The invention discloses a nitrofuran compound, a pharmaceutical composition and a preparation method and application of the nitrofuran compound. The nitrofuran compound has a structure as shown in a formula (I) (See the specification). The nitrofuran comp
- -
-
Paragraph 0064-0069; 0177-0182
(2021/11/10)
-
- Synthesis method of imidazopyridine or pyrimidine derivative
-
The invention belongs to the technical field of synthesis, and particularly relates to a synthesis method of an imidazopyridine or pyrimidine derivative. The imidazopyridine or pyrimidine compound is obtained by taking pyridine or pyrimidinecarboxylic acid as a synthon through amidation, Hofmann degradation and cyclization reaction, and the obtained imidazopyridine or pyrimidine derivative can be further converted to generate a functional product. The method has the advantages of easily available raw materials, simple operation, high reaction efficiency, convenient post-treatment, and diversity of functional groups.
- -
-
-
- From Synthetic Simplified Marine Metabolite Analogues to New Selective Allosteric Inhibitor of Aurora B Kinase
-
Significant inhibition of Aurora B was achieved by the synthesis of simplified fragments of benzosceptrins and oroidin belonging to the marine pyrrole-2-aminoimidazoles metabolites isolated from sponges. Evaluation of kinase inhibition enabled the discovery of a synthetically accessible rigid acetylenic structural analogue EL-228 (1), whose structure could be optimized into the potent CJ2-150 (37). Here we present the synthesis of new inhibitors of Aurora B kinase, which is an important target for cancer therapy through mitosis regulation. The biologically oriented synthesis yielded several nanomolar inhibitors. The optimized compound CJ2-150 (37) showed a non-ATP competitive allosteric mode of action in a mixed-type inhibition for Aurora B kinase. Molecular docking identified a probable binding mode in the allosteric site "F"and highlighted the key interactions with the protein. We describe the improvement of the inhibitory potency and specificity of the novel scaffold as well as the characterization of the mechanism of action.
- Juillet, Charlotte,Ermolenko, Ludmila,Boyarskaya, Dina,Baratte, Blandine,Josselin, Béatrice,Nedev, Hristo,Bach, Stéphane,Iorga, Bogdan I.,Bignon, Jér?me,Ruchaud, Sandrine,Al-Mourabit, Ali
-
p. 1197 - 1219
(2021/02/05)
-
- Use of imidazo[1,2-a]pyridine as a carbonyl surrogate in a mannich-like, catalyst free, one-pot reaction
-
Derivatization of imidazo[1,2-a]pyridine scaffolds have gained considerable attention due to the biological significance of therapeutics based on the imidazopyridine core. By utilizing a catalyst-free, “Mannich type” reaction, we developed a simple and efficient protocol to aminomethylate the C-3 position of imidazo[1,2-a]pyridine through a multicomponent, de-carboxylation reaction involving imidazo[1,2-a]pyridine, a secondary amine, and glyoxylic acid. The developed protocol re-quires mild reaction conditions and furnishes diverse imid-azo[1,2-a]pyridine analogues from commercially available starting materials. Additionally, the current protocol improves prior methods, which were limited by the amine substrate scope. Taken together, this current methodology permits rapid diversification of imidazo[1,2-a]pyridines to enhance combinatorial efficiency in the drug discovery processes.
- Naresh, Gunaganti,Lakkaniga, Naga Rajiv,Kharbanda, Anupreet,Yan, Wei,Frett, Brendan,Li, Hong-Yu
-
p. 770 - 777
(2019/01/14)
-
- FUSED HETEROCYCLIC COMPOUNDS AS SELECTIVE BMP INHIBITORS
-
The present invention provides small molecule inhibitors of BMP signaling that are useful for treating diseases or conditions associated with BMP signaling, including cancers of the central nervous system.
- -
-
Page/Page column 40; 41
(2018/08/20)
-
- Computer aided drug discovery of highly ligand efficient, low molecular weight imidazopyridine analogs as FLT3 inhibitors
-
The FLT3 kinase represents an attractive target to effectively treat AML. Unfortunately, no FLT3 targeted therapeutic is currently approved. In line with our continued interests in treating kinase related disease for anti-FLT3 mutant activity, we utilized pioneering synthetic methodology in combination with computer aided drug discovery and identified low molecular weight, highly ligand efficient, FLT3 kinase inhibitors. Compounds were analyzed for biochemical inhibition, their ability to selectively inhibit cell proliferation, for FLT3 mutant activity, and preliminary aqueous solubility. Validated hits were discovered that can serve as starting platforms for lead candidates.
- Frett, Brendan,McConnell, Nick,Smith, Catherine C.,Wang, Yuanxiang,Shah, Neil P.,Li, Hong-Yu
-
p. 123 - 131
(2015/04/14)
-
- Discovery and optimization of potent broad-spectrum arenavirus inhibitors derived from benzimidazole and related heterocycles
-
A series of potent arenavirus inhibitors sharing a benzimidazole core were previously reported by our group. SAR studies were expanded beyond the previous analysis, which involved the attached phenyl rings and methylamino linker portion, to include modifications focused on the benzimidazole core. These changes included the introduction of various substituents to the bicyclic benzimidazole ring system along with alternate core heterocycles. Many of the analogs containing alternate nitrogen-based bicyclic ring systems were found to retain antiviral potency compared to the benzimidazole series from which we derived our lead compound, ST-193. In fact, 21h, built on an imidazopyridine core, possessed a near tenfold increase in potency against Lassa virus pseudotypes compared to ST-193. As found with the benzimidazole series, broad-spectrum arenavirus activity was also observed for a number of the analogs discovered during this study.
- Burgeson, James R.,Moore, Amy L.,Gharaibeh, Dima N.,Larson, Ryan A.,Cerruti, Natasha R.,Amberg, Sean M.,Hruby, Dennis E.,Dai, Dongcheng
-
p. 750 - 756
(2013/02/25)
-
- ANTIVIRAL DRUGS FOR TREATMENT OF ARENA VIRUS INFECTION
-
Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever
- -
-
-
- [5,6]HETEROCYCLIC COMPOUND
-
Abstract: An object of the present invention is to provide a novel low molecular weight compound exhibiting an osteogenesis-promoting action. This object is achieved by a compound having the general formula (I) or a pharmacologically acceptable salt thereof. In the general formula (I), R1 and R2 represent hydrogen atoms, and the like; R3 represents a hydrogen atom, and the like; X, Y, and Z represent nitrogen atoms, and the like; A represents a phenylene group, and the like; n represents 1 or 2, and the like; and V and W represent oxygen atoms, and the like.
- -
-
Paragraph 0114-0115
(2013/03/26)
-
- AZETIDINES AND CYCLOBUTANES AS HISTAMINE H3 RECEPTOR ANTAGONISTS
-
The invention relates to compounds of formula (I) wherein R, R0, R1, m, n and X1 to X4 have the meaning as cited in the description and the claims. Said compounds are useful as Histamine H3 receptor antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
- -
-
Page/Page column 80; 81
(2010/01/29)
-
- BICYCLIC HETEROCYCLIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS
-
The invention relates to new bicyclic heterocyclic derivative compounds of formula (I): wherein R1, A, X1, X2, X3, X4, X5 and R2 are as defined herein, to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
- -
-
Page/Page column 110; 111
(2009/05/30)
-
- ORGANIC COMPOUNDS
-
Compounds of formula (I): in free or salt or solvate form, where R1, R2, R3 and R20 have the meanings as indicated in the specification, are useful for treati ng diseases mediated by the ALK-5 and/or ALK-4 receptor. Pharmaceutical composit ions that contain the compounds and processes for preparing the compounds are also described.
- -
-
Page/Page column 114
(2009/05/28)
-
- IMIDAZOPYRIDINE DERIVATIVES AS INHIBITORS OF RECEPTOR TYROSINE KINASES
-
The invention relates to new bicyclic heterocyclic derivative compounds, to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
- -
-
Page/Page column 101
(2010/01/07)
-
- NEW COMPOUNDS
-
The invention relates to new bicyclic heterocyclic derivative compounds, to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
- -
-
Page/Page column 93-94
(2008/12/06)
-