23579-79-5Relevant academic research and scientific papers
Design of selective PI3Kα inhibitors starting from a promiscuous pan kinase scaffold
Barlaam, Bernard,Cosulich, Sabina,Fitzek, Martina,Green, Stephen,Harris, Craig S.,Hudson, Kevin,Lambert-Van Der Brempt, Christine,Ouvry, Gilles,Page, Ken,Ruston, Linette,Ward, Lara,Delouvrié, Bénédicte
, p. 2679 - 2685 (2015)
Starting from compound 1, a potent PI3Kα inhibitor having poor general kinase selectivity, we used structural data and modelling to identify key exploitable differences between PI3Kα and the other kinases. This approach led us to design chemical modifications of the central pyrazole, which solved the poor kinase selectivity seen as a strong liability for the initial compound 1. Amongst the modifications explored, a 1,3,4-triazole ring (as in compound 4) as a replacement of the initial pyrazole provided good potency against PI3Kα, with excellent kinase selectivity.
TRPML MODULATORS
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Paragraph 0367, (2021/06/26)
The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
SSAO INHIBITOR
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Paragraph 0420; 0421; 0422; 0566-0568, (2020/04/02)
The present invention provides an SSAO inhibitor and an application thereof in preparing a drug for treating a disease related to SSAO. In particular, the present invention provides a compound shown in formula (IV) and a pharmaceutically acceptable salt thereof.
HETEROCYCLYLAMINO-SUBSTITUTED TRIAZOLES AS MODULATORS OF RHO-ASSOCIATED PROTEIN KINASE
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Page/Page column 84, (2019/08/12)
This invention relates to novel compounds and pharmaceutical compositions comprising. Compounds of the invention useful as modulators of Rho-associated protein kinase (ROCK), for example ROCK1 and/or ROCK2 inhibitors. Methods of treatment employing the compounds are also contemplated by the present invention. The compounds of the invention are useful in treating ROCK mediated diseases.
Synthesis of 1-Alkyl-5-amino-1,2,4-triazoles Based on Nucleophilic Substitution and Reduction Reactions
Tolstyakov
, p. 1537 - 1547 (2019/01/04)
A series of 1-alkyl-5-amino-1H-1,2,4-triazoles were synthesized starting from 3,5-dibromo-1H- 1,2,4-triazole by alkylation and subsequent nucleophilic substitution of the 5-bromine atom by azido group, reduction of the latter to amino group, and hydrodebromination.
PHENOXYTRIAZOLES
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Page/Page column 55, (2018/05/27)
The present invention relates to a compound of formula I, HetAr is a five or six membered heteroaryl group, selected from wherein R1 is hydrogen, halogen, lower alkyl, lower alkoxy or lower alkyl substituted by halogen, and may be the same or d
TRIAZOLE COMPOUNDS AND THEIR USE AS GAMMA SECRETASE MODULATORS
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Page/Page column 16; 17, (2015/01/06)
The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof. The invention also relates to pharmaceutical compositions comprising these compounds, to processes for making these compounds, and to their use as medicaments for treatment and/or prevention of Aβ-related diseases.
TRIAZOLE COMPOUNDS AND THEIR USE AS GAMMA SECRETASE MODULATORS
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Page/Page column 16, (2015/01/06)
The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof. The invention also relates to pharmaceutical compositions comprising these compounds, to processes for making these compounds, and to their use as medicaments for treatment and/or prevention of Αβ-related diseases.
Anilinotriazoles as potent gamma secretase modulators
Velter, Adriana I.,Bischoff, Franois P.,Berthelot, Didier,De Cleyn, Michel,Oehlrich, Daniel,Jaroskova, Libuse,Macdonald, Gregor,Minne, Garrett,Pieters, Serge,Rombouts, Frederik,Van Brandt, Sven,Van Roosbroeck, Yves,Surkyn, Michel,Trabanco, Andrs A.,Tresadern, Gary,Wu, Tongfei,Borghys, Herman,Mercken, Marc,Masungi, Chantal,Gijsen, Harrie
, p. 5805 - 5813 (2015/01/08)
The design and synthesis of a novel series of potent gamma secretase modulators is described. Exploration of various spacer groups between the triazole ring and the aromatic appendix in 2 has led to anilinotriazole 28, which combined high in vitro and in
NOVEL SUBSTITUTED TRIAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS
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Page/Page column 27, (2012/12/13)
The present invention is concerned with novel substituted triazole derivatives of Formula (I) wherein Het1, R1, R2, A1, A2, A3, A4, L1, and L2 have the mean
