870838-56-5Relevant academic research and scientific papers
Design and Synthesis of a Novel Series of Bicyclic Heterocycles As Potent γ-Secretase Modulators
Bischoff, Francois,Berthelot, Didier,De Cleyn, Michel,MacDonald, Gregor,Minne, Garrett,Oehlrich, Daniel,Pieters, Serge,Surkyn, Michel,Trabanco, Andres A.,Tresadern, Gary,Van Brandt, Sven,Velter, Ingrid,Zaja, Mirko,Borghys, Herman,Masungi, Chantal,Mercken, Marc,Gijsen, Harrie J. M.
, p. 9089 - 9106,18 (2020/10/15)
The design and the synthesis of several chemical subclasses of imidazole containing γ-secretase modulators (GSMs) is described. Conformational restriction of pyridone 4 into bicyclic pyridone isosteres has led to compounds with high in vitro and in vivo p
NOVEL SUBSTITUTED TRIAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS
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Page/Page column 29, (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
Pyridazine-derived γ-secretase modulators
Wan, Zehong,Hall, Adrian,Jin, Yun,Xiang, Jia-Ning,Yang, Eric,Eatherton, Andrew,Smith, Beverley,Yang, Guang,Yu, Haihua,Wang, Ju,Ye, Liang,Lau, Lit-Fui,Yang, Ting,Mitchell, William,Cai, Wei,Zhang, Xiaomin,Sang, Yingxia,Wang, Yonghui,Tong, Zhaolong,Cheng, Ziqiang,Hussain, Ishrut,Elliott, John D.,Matsuoka, Yasuji
, p. 4016 - 4019 (2011/08/06)
SAR of a novel series of pyridazine-derived γ-secretase modulators is described. Compound 25 was found to be a potent modulator in vitro, which on further profiling, was found to decrease Aβ42 and Aβ40, and maintain the levels of total Aβ. Furthermore, 25
Triazoles as γ-secretase modulators
Fischer, Christian,Zultanski, Susan L.,Zhou, Hua,Methot, Joey L.,Brown, W. Colby,Mampreian, Dawn M.,Schell, Adam J.,Shah, Sanjiv,Nuthall, Hugh,Hughes, Bethany L.,Smotrov, Nadja,Kenific, Candia M.,Cruz, Jonathan C.,Walker, Deborah,Bouthillette, Melanie,Nikov, George N.,Savage, Dan F.,Jeliazkova-Mecheva, Valentina V.,Diaz, Damaris,Szewczak, Alexander A.,Bays, Nathan,Middleton, Richard E.,Munoz, Benito,Shearman, Mark S.
, p. 4083 - 4087 (2011/08/02)
Synthesis, SAR, and evaluation of aryl triazoles as novel gamma secretase modulators (GSMs) are presented in this communication. Starting from the literature and in-house leads, we evaluated a range of five-membered heterocycles as replacements for olefin
SUBSTITUTED TRIAZOLE AND IMIDAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS
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Page/Page column 117-118, (2011/02/24)
The present invention is concerned with novel substituted triazole and imidazole derivatives of Formula (I) wherein R1, R2, A1, A2, A3, A4, X, and Het1 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
NOVEL SUBSTITUTED BICYCLIC TRIAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS
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Page/Page column 72; 73, (2011/08/04)
The present invention is concerned with novel substituted bicyclic triazole derivatives of Formula (I) wherein Het1, R1, R2, A1, A2, A3, A4, L1, and L2 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
NOVEL SUBSTITUTED TRIAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS
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Page/Page column 61-62, (2011/08/04)
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 meaning defined in the claims. The compounds according to the present invention are useful as gamma sec
GAMMA SECRETASE MODULATORS
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Page/Page column 195, (2009/07/17)
This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I) wherein R2 is a fused bicyclic ring of the formula (II). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I).
GAMMA SECRETASE MODULATORS
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Page/Page column 160, (2009/07/17)
This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula [Chemical formula should be inserted here as it appears on abstract in electronic form.] Also disclosed are methods of modulating gamma secretas
PYRIDAZINE DERIVATIVES FOR INHIBITING BETA AMYLOID PEPTIDE PRODUCTION
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Page/Page column 19, (2009/05/28)
The present invention relates to novel compounds that inhibit the production of β- amyloid peptide (1-42), processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated β-amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.
