74315-08-5Relevant articles and documents
KINASE INHIBITORS
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Paragraph 0341-0343, (2021/12/29)
Disclosed herein are lH-indole-7-carboxamide derivatives as protein kinase inhibitors, in particular Bruton's tyrosine kinase (BTK) inhibitors, pharmaceutical compositions comprising them, processes for preparing them and uses of such protein kinase inhib
Structure-Functional-Selectivity Relationship Studies of Novel Apomorphine Analogs to Develop D1R/D2R Biased Ligands
Liu, Chuan,Park, Hyejin,Urs, Aarti N.,Urs, Nikhil M.,Wang, Qiu,Zimmerman, Joseph
, (2020/02/06)
Loss of dopamine neurons is central to the manifestation of Parkinson's disease motor symptoms. The dopamine precursor L-DOPA, the most commonly used therapeutic agent for Parkinson's disease, can restore normal movement yet cause side-effects such as dyskinesias upon prolonged administration. Dopamine D1 and D2 receptors activate G-protein- A nd arrestin-dependent signaling pathways that regulate various dopamine-dependent functions including locomotion. Studies have shown that shifting the balance of dopamine receptor signaling toward the arrestin pathway can be beneficial for inducing normal movement, while reducing dyskinesias. However, simultaneous activation of both D1 and D2Rs is required for robust locomotor activity. Thus, it is desirable to develop ligands targeting both D1 and D2Rs and their functional selectivity. Here, we report structure-functional-selectivity relationship (SFSR) studies of novel apomorphine analogs to identify structural motifs responsible for biased activity at both D1 and D2Rs.
Radical cyclization of ynamides into six- or eight-membered rings. Application to the synthesis of a protoberberine analog
Balieu, Sébastien,Toutah, Krimo,Carro, Laura,Chamoreau, Lise-Marie,Rousselière, Hélène,Courillon, Christine
supporting information; experimental part, p. 2876 - 2880 (2011/06/21)
A straightforward formation of six- and eight-membered rings via the radical cyclization of specifically designed ynamides is reported. This strategy provides a protoberberine analog in only three steps by a radical cyclization cascade.
Identification of a new biaryl scaffold generating potent renin inhibitors
Lacombe, Patrick,Aspiotis, Renée,Bayly, Christopher,Chen, Austin,Dubé, Daniel,Fortin, Réjean,Gallant, Michel,Juteau, Hélne,Liu, Suzanna,McKay, Dan,Roy, Patrick,Wu, Tom
scheme or table, p. 5822 - 5826 (2010/12/19)
The discovery and SAR of a series of potent renin inhibitors possessing a novel biaryl scaffold are described herein. Molecular modeling revealed that the cyclopropylamide spacer present in 1 can be replaced by a simple, substituted aromatic ring such as
RENIN INHIBITORS
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Page/Page column 29, (2009/04/25)
The present invention relates to biphenyl compounds of formula (I). These compounds are renin inhibitors of a non- peptidic nature and of low molecular weight. The invention further relates to a pharmaceutical composition containing said compounds, as wel
A mild inter- and intramolecular amination of aryl halides with a combination of CuI and CsOAc
Kubo, Tetsuji,Katoh, Chiharu,Yamada, Ken,Okano, Kentaro,Tokuyama, Hidetoshi,Fukuyama, Tohru
supporting information; experimental part, p. 11230 - 11236 (2009/04/11)
A unique combination of CuI and CsOAc was found to catalyze aryl amination under mild conditions. The reaction takes place at room temperature or at 90 °C with broad functional group compatibility. The intramolecular reaction was able to form five-, six-, and seven-membered rings with various protecting groups on the nitrogen atom. The scope of the intermolecular amination, as well as its applications to unsymmetrical N,N′-dialkylated phenylenediamines, was investigated.
Photochemically induced cyclization of N-[2-(o-styryl)phenylethyl]acetamides and 5-styryl-1-methyl-1,2,3,4-tetrahydroisoquinolines: New total syntheses of 1-methyl-1,2,3,4-tetrahydronaphtho[2,1-f]isoquinolines
Martínez, Elena,Estévez, Juan C,Estévez, Ramón J,Castedo, Luis
, p. 1981 - 1986 (2007/10/03)
Two new total syntheses of 1-methyl-1,2,3,4-dihydronaphtho[1,2-f]isoquinolines are based on photochemically induced cyclization of N-{2-[(E)-2-phenyl-1-etheynyl]phenylethyl]}acetamides or 1-methyl-5-[(E)-2-phenyl-1-ethenyl]-1,2,3,4-tetrahydroisoquinolines.
Intramolecular palladium-catalyzed aryl amination and aryl amidation
Wolfe, John P.,Rennels, Roger A.,Buchwald, Stephen L.
, p. 7525 - 7546 (2007/10/03)
Upon treatment with a palladium catalyst and a suitable base, aromatic halides undergo intramolecular substitution to form five, six, and seven-membered rings. In a similar fashion aryl halides with pendant amides or sulfonamides are cyclized to form five and six-membered rings.
