4AZY
| Design and Synthesis of BACE1 Inhibitors with In Vivo Brain Reduction of beta-Amyloid Peptides (COMPOUND 10) | 分子名称: | (1S)-4-fluoro-1-(4-fluoro-3-pyrimidin-5-ylphenyl)-1-[2-(trifluoromethyl)pyridin-4-yl]-1H-isoindol-3-amine, ACETATE ION, BETA-SECRETASE 1, ... | 著者 | Swahn, B.M, Kolmodin, K, Karlstrom, S, von Berg, S, Soderman, P, Holenz, J, Berg, S, Lindstrom, J, Sundstrom, M, Turek, D, Kihlstrom, J, Slivo, C, Andersson, L, Pyring, D, Ohberg, L, Kers, A, Bogar, K, Bergh, M, Olsson, L.L, Janson, J, Eketjall, S, Georgievska, B, Jeppsson, F, Falting, J. | 登録日 | 2012-06-27 | 公開日 | 2012-10-17 | 最終更新日 | 2024-10-16 | 実験手法 | X-RAY DIFFRACTION (1.79 Å) | 主引用文献 | Design and synthesis of beta-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors with in vivo brain reduction of beta-amyloid peptides. J. Med. Chem., 55, 2012
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4B00
| Design and Synthesis of BACE1 Inhibitors with In Vivo Brain Reduction of beta-Amyloid Peptides (COMPOUND (R)-41) | 分子名称: | 5-{(1R)-3-amino-4-fluoro-1-[3-(5-prop-1-yn-1-ylpyridin-3-yl)phenyl]-1H-isoindol-1-yl}-1-ethyl-3-methylpyridin-2(1H)-one, ACETATE ION, BETA-SECRETASE 1 | 著者 | Swahn, B.M, Kolmodin, K, Karlstrom, S, von Berg, S, Soderman, P, Holenz, J, Berg, S, Lindstrom, J, Sundstrom, M, Turek, D, Kihlstrom, J, Slivo, C, Andersson, L, Pyring, D, Ohberg, L, Kers, A, Bogar, K, Bergh, M, Olsson, L.L, Janson, J, Eketjall, S, Georgievska, B, Jeppsson, F, Falting, J. | 登録日 | 2012-06-27 | 公開日 | 2012-10-17 | 最終更新日 | 2023-12-20 | 実験手法 | X-RAY DIFFRACTION (1.83 Å) | 主引用文献 | Design and synthesis of beta-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors with in vivo brain reduction of beta-amyloid peptides. J. Med. Chem., 55, 2012
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4B05
| Preclinical characterization of AZD3839, a novel clinical candidate BACE1 inhibitor for the treatment of Alzheimer Disease | 分子名称: | (1S)-1-[2-(difluoromethyl)pyridin-4-yl]-4-fluoro-1-(3-pyrimidin-5-ylphenyl)-1H-isoindol-3-amine, ACETATE ION, BETA-SECRETASE 1, ... | 著者 | Jeppsson, F, Eketjall, S, Janson, J, Karlstrom, S, Gustavsson, S, Olsson, L.L, Radesater, A.C, Ploeger, B, Cebers, G, Kolmodin, K, Swahn, B.M, von Berg, S, Bueters, T, Falting, J. | 登録日 | 2012-06-28 | 公開日 | 2012-10-17 | 最終更新日 | 2024-05-01 | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | 主引用文献 | Discovery of AZD3839, a potent and selective BACE1 inhibitor clinical candidate for the treatment of Alzheimer disease. J. Biol. Chem., 287, 2012
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4B1C
| New Aminoimidazoles as BACE-1 Inhibitors: From Rational Design to Ab- lowering in Brain | 分子名称: | (2R)-2-cyclopropyl-5-methyl-2-[3-(5-prop-1-yn-1-ylpyridin-3-yl)phenyl]-2H-imidazol-4-amine, BETA-SECRETASE 1, DIMETHYL SULFOXIDE | 著者 | Rahm, F, Blid, J, Ginman, T, Karlstrom, S, Kihlstrom, J, Kolmodin, K, Lindstrom, J, von Berg, S, von Kieseritzky, F, Slivo, C, Swahn, B, Viklund, J, Olsson, L, Johansson, P, Eketjall, S, Falting, J, Jeppsson, F, Stromberg, K, Janson, J, Gravenfors, Y. | 登録日 | 2012-07-10 | 公開日 | 2012-10-10 | 最終更新日 | 2024-10-16 | 実験手法 | X-RAY DIFFRACTION (1.95 Å) | 主引用文献 | New aminoimidazoles as beta-secretase (BACE-1) inhibitors showing amyloid-beta (A beta ) lowering in brain. J. Med. Chem., 55, 2012
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4B1E
| New Aminoimidazoles as BACE-1 Inhibitors: From Rational Design to Ab- lowering in Brain | 分子名称: | (2R)-2-methyl-5-phenyl-2-(3-pyridin-3-ylphenyl)-2,3-dihydro-1H-imidazol-4-amine, BETA-SECRETASE 1 | 著者 | Rahm, F, Blid, J, Ginman, T, Karlstrom, S, Kihlstrom, J, Kolmodin, K, Lindstrom, J, von Berg, S, von Kieseritzky, F, Slivo, C, Swahn, B, Viklund, J, Olsson, L, Johansson, P, Eketjall, S, Falting, J, Jeppsson, F, Stromberg, K, Janson, J, Gravenfors, Y. | 登録日 | 2012-07-10 | 公開日 | 2012-10-10 | 最終更新日 | 2018-02-14 | 実験手法 | X-RAY DIFFRACTION (1.95 Å) | 主引用文献 | New aminoimidazoles as beta-secretase (BACE-1) inhibitors showing amyloid-beta (A beta ) lowering in brain. J. Med. Chem., 55, 2012
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4B1D
| New Aminoimidazoles as BACE-1 Inhibitors: From Rational Design to Ab- lowering in Brain | 分子名称: | (2S)-2-(4-methoxy-3,5-dimethylphenyl)-5-methyl-2-(3-pyrimidin-5-ylphenyl)-2H-imidazol-4-amine, ACETATE ION, BETA-SECRETASE 1 | 著者 | Rahm, F, Blid, J, Ginman, T, Karlstrom, S, Kihlstrom, J, Kolmodin, K, Lindstrom, J, von Berg, S, von Kieseritzky, F, Slivo, C, Swahn, B, Viklund, J, Olsson, L, Johansson, P, Eketjall, S, Falting, J, Jeppsson, F, Stromberg, K, Janson, J, Gravenfors, Y. | 登録日 | 2012-07-10 | 公開日 | 2012-10-10 | 最終更新日 | 2018-02-14 | 実験手法 | X-RAY DIFFRACTION (1.95 Å) | 主引用文献 | New aminoimidazoles as beta-secretase (BACE-1) inhibitors showing amyloid-beta (A beta ) lowering in brain. J. Med. Chem., 55, 2012
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6EJ3
| BACE1 compound 23 | 分子名称: | (1r,4r)-4-methoxy-6'-(5-methyl-3-pyridinyl)-3'H-dispiro[cyclohexane-1,2'-indene-1',4''-[1,3]oxazol]-2''-amine, Beta-secretase 1 | 著者 | Johansson, P. | 登録日 | 2017-09-20 | 公開日 | 2018-04-18 | 最終更新日 | 2024-05-01 | 実験手法 | X-RAY DIFFRACTION (1.94 Å) | 主引用文献 | Toward beta-Secretase-1 Inhibitors with Improved Isoform Selectivity. J. Med. Chem., 61, 2018
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6EJ2
| BACE1 compound 28 | 分子名称: | Beta-secretase 1, compound 28 | 著者 | Johansson, P. | 登録日 | 2017-09-20 | 公開日 | 2018-04-18 | 最終更新日 | 2018-05-09 | 実験手法 | X-RAY DIFFRACTION (1.46 Å) | 主引用文献 | Toward beta-Secretase-1 Inhibitors with Improved Isoform Selectivity. J. Med. Chem., 61, 2018
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4B77
| Aminoimidazoles as BACE-1 Inhibitors: From De Novo Design to Ab- lowering in Brain | 分子名称: | (5R)-5-(4-methoxyphenyl)-5-(3-pyrimidin-5-ylphenyl)-3,4-dihydropyrrol-2-amine, BETA-SECRETASE 1, DIMETHYL SULFOXIDE | 著者 | Gravenfors, Y, Blid, J, Ginman, T, Karlstrom, S, Kihlstrom, J, Kolmodin, K, Lindstrom, J, Berg, S, Kieseritzky, F, Slivo, C, Swahn, B, Viklund, J, Olsson, L, Johansson, P, Eketjall, S, Falting, J, Jeppsson, F, Stromberg, K, Janson, J, Rahm, F. | 登録日 | 2012-08-16 | 公開日 | 2013-06-26 | 最終更新日 | 2024-10-16 | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | 主引用文献 | Core Refinement Toward Permeable Beta-Secretase (Bace-1) Inhibitors with Low Herg Activity. J.Med.Chem., 56, 2013
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4B78
| Aminoimidazoles as BACE-1 Inhibitors: From De Novo Design to Ab- lowering in Brain | 分子名称: | (3R,5R)-3-methoxy-5-(4-methoxyphenyl)-5-(3-pyridin-3-ylphenyl)-3,4-dihydropyrrol-2-amine, BETA-SECRETASE 1 | 著者 | Gravenfors, Y, Blid, J, Ginman, T, Karlstrom, S, Kihlstrom, J, Kolmodin, K, Lindstrom, J, Berg, S, Kieseritzky, F, Slivo, C, Swahn, B, Viklund, J, Olsson, L, Johansson, P, Eketjall, S, Falting, J, Jeppsson, F, Stromberg, K, Janson, J, Rahm, F. | 登録日 | 2012-08-16 | 公開日 | 2013-06-26 | 最終更新日 | 2013-07-03 | 実験手法 | X-RAY DIFFRACTION (1.5 Å) | 主引用文献 | Core Refinement Toward Permeable Beta-Secretase (Bace-1) Inhibitors with Low Herg Activity. J.Med.Chem., 56, 2013
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4B72
| Aminoimidazoles as BACE-1 Inhibitors: From De Novo Design to Ab- lowering in Brain | 分子名称: | (6R)-6-(4-methoxyphenyl)-2-methyl-6-(3-pyrimidin-5-ylphenyl)pyrrolo[3,4-d][1,3]thiazol-4-amine, BETA-SECRETASE 1 | 著者 | Gravenfors, Y, Blid, J, Ginman, T, Karlstrom, S, Kihlstrom, J, Kolmodin, K, Lindstrom, J, Berg, S, Kieseritzky, F, Slivo, C, Swahn, B, Viklund, J, Olsson, L, Johansson, P, Eketjall, S, Falting, J, Jeppsson, F, Stromberg, K, Janson, J, Rahm, F. | 登録日 | 2012-08-16 | 公開日 | 2013-06-26 | 最終更新日 | 2013-07-03 | 実験手法 | X-RAY DIFFRACTION (1.6 Å) | 主引用文献 | Core Refinement Toward Permeable Beta-Secretase (Bace-1) Inhibitors with Low Herg Activity. J.Med.Chem., 56, 2013
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4B70
| Aminoimidazoles as BACE-1 Inhibitors: From De Novo Design to Ab- lowering in Brain | 分子名称: | (2S)-2-[3-(3-chlorophenyl)phenyl]-2-methyl-5,6-dihydro-1,3-oxazin-4-amine, BETA-SECRETASE 1 | 著者 | Gravenfors, Y, Blid, J, Ginman, T, Karlstrom, S, Kihlstrom, J, Kolmodin, K, Lindstrom, J, Berg, S, Kieseritzky, F, Slivo, C, Swahn, B, Viklund, J, Olsson, L, Johansson, P, Eketjall, S, Falting, J, Jeppsson, F, Stromberg, K, Janson, J, Rahm, F. | 登録日 | 2012-08-16 | 公開日 | 2013-06-26 | 最終更新日 | 2013-07-03 | 実験手法 | X-RAY DIFFRACTION (1.6 Å) | 主引用文献 | Core Refinement Toward Permeable Beta-Secretase (Bace-1) Inhibitors with Low Herg Activity. J.Med.Chem., 56, 2013
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