1346145-50-3Relevant academic research and scientific papers
Rational Design of Novel 1,3-Oxazine Based β-Secretase (BACE1) Inhibitors: Incorporation of a Double Bond to Reduce P-gp Efflux Leading to Robust Aβ Reduction in the Brain
Fuchino, Kouki,Mitsuoka, Yasunori,Masui, Moriyasu,Kurose, Noriyuki,Yoshida, Shuhei,Komano, Kazuo,Yamamoto, Takahiko,Ogawa, Masayoshi,Unemura, Chie,Hosono, Motoko,Ito, Hisanori,Sakaguchi, Gaku,Ando, Shigeru,Ohnishi, Shuichi,Kido, Yasuto,Fukushima, Tamio,Miyajima, Hirofumi,Hiroyama, Shuichi,Koyabu, Kiyotaka,Dhuyvetter, Deborah,Borghys, Herman,Gijsen, Harrie J.M.,Yamano, Yoshinori,Iso, Yasuyoshi,Kusakabe, Ken-Ichi
, p. 5122 - 5137 (2018)
Accumulation of Aβ peptides is a hallmark of Alzheimer's disease (AD) and is considered a causal factor in the pathogenesis of AD. β-Secretase (BACE1) is a key enzyme responsible for producing Aβ peptides, and thus agents that inhibit BACE1 should be bene
Trifluoromethyl Dihydrothiazine-Based β-Secretase (BACE1) Inhibitors with Robust Central β-Amyloid Reduction and Minimal Covalent Binding Burden
Anan, Kosuke,Iso, Yasuyoshi,Oguma, Takuya,Nakahara, Kenji,Suzuki, Shinji,Yamamoto, Takahiko,Matsuoka, Eriko,Ito, Hisanori,Sakaguchi, Gaku,Ando, Shigeru,Morimoto, Kenji,Kanegawa, Naoki,Kido, Yasuto,Kawachi, Tomoyuki,Fukushima, Tamio,Teisman, Ard,Urmaliya, Vijay,Dhuyvetter, Deborah,Borghys, Herman,Austin, Nigel,Van Den Bergh, An,Verboven, Peter,Bischoff, Francois,Gijsen, Harrie J. M.,Yamano, Yoshinori,Kusakabe, Kenichi
supporting information, p. 1894 - 1910 (2019/11/22)
The β-site amyloid precursor protein cleaving enzyme 1 (BACE1, also known as β-secretase) is a promising target for the treatment of Alzheimer's disease. A pKa lowering approach over the initial leads was adopted to mitigate hERG inhibition and
1,4-OXAZEPINES AS BACE1 AND/OR BACE2 INHIBITORS
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Paragraph 0169; 0170; 0171, (2013/03/26)
This invention relates to compounds of the formula wherein and R1 to R3 are as described herein, or to pharmaceutically acceptable salts thereof. These compounds are BACE1 and/or BACE2 inhibitors and can be used as pharmaceuticals fo
β-secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease
Hilpert, Hans,Guba, Wolfgang,Woltering, Thomas J.,Wostl, Wolfgang,Pinard, Emmanuel,Mauser, Harald,Mayweg, Alexander V.,Rogers-Evans, Mark,Humm, Roland,Krummenacher, Daniela,Muser, Thorsten,Schnider, Christian,Jacobsen, Helmut,Ozmen, Laurence,Bergadano, Alessandra,Banner, David W.,Hochstrasser, Remo,Kuglstatter, Andreas,David-Pierson, Pascale,Fischer, Holger,Polara, Alessandra,Narquizian, Robert
supporting information, p. 3980 - 3995 (2013/06/27)
An extensive fluorine scan of 1,3-oxazines revealed the power of fluorine(s) to lower the pKa and thereby dramatically change the pharmacological profile of this class of BACE1 inhibitors. The CF3 substituted oxazine 89, a potent and
1,4,5,6-TETRAHYDRO-PYRIMIDIN-2-YLAMINE COMPOUNDS
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Page/Page column 29, (2012/02/15)
This invention relates to compounds of the formula wherein R1 to R9 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the therapeutic and/
1,4,5,6-TETRAHYDRO-PYRIMIDIN-2-YLAMINE COMPOUNDS
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Page/Page column 65, (2012/03/09)
This invention relates to compounds of the formula wherein R1 to R9 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the therapeutic and/
1,4-OXAZEPINES AS BACE1 AND/OR BACE2 INHIBITORS
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Page/Page column 28, (2012/09/10)
This invention relates to compounds of the formula wherein and R1 to R3 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE1 and/or BACE2 inhibitors and can be used as medicaments for the therapeutic and/or pr
1,3-OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS
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Page/Page column 71, (2012/12/13)
The present invention provides compounds of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present inv
1,3-OXAZINES AS BACE 1 AND/OR BACE2 INHIBITORS
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Page/Page column 39, (2012/12/13)
The present invention provides compounds of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present inv
1,3-OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS
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Page/Page column 29, (2012/10/18)
The present invention provides 4-(3-Amino-phenyl)-5,6-dihydro-4H-[1,3]oxazin-2-ylamines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
