Pyridyl-triazabicycles
US-10047102-B2 · Aug 14, 2018 · US
Pyridyl-triazabicycles
US10414780B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10414780-B2 |
| Application number | US-201816029228-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jul 6, 2018 |
| Priority date | Jul 25, 2014 |
| Publication date | Sep 17, 2019 |
| Grant date | Sep 17, 2019 |
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Abstract
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The present invention provides a compound of formula I having BACE1 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.
First claim
Opening claim text (preview).
The invention claimed is: 1. A pharmaceutical composition, comprising a compound, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier and/or a pharmaceutically acceptable auxiliary substance, wherein said compound is selected from the group consisting of: 5-Cyano-pyridine-2-carboxylic acid [6-((3R,4aS)-1-amino-3-methyl-4a-oxo-3,4,6,7,8,9-hexahydro-4aλ 6 -thia-2,5,9a-triaza-benzocyclohepten-3-yl)-5-fluoro-pyridin-n-2-yl]-amide, N-[6-[(1S,10S)-8-Amino-10-(fluoromethyl)-1-oxo-1λ 6 -thia-2,7,9-triazabicyclo[5.4.0]undeca-1,8-dien-10-yl]-5-fluoropyridin-2-yl]-5-cyanopyridine-2-carboxamide, 5-Cyano-3-methyl-pyridine-2-carboxylic acid [6-((3R,4aS)-1-amino-3-methyl-4a-oxo-3,4,6,7,8,9-hexahydro-4aλ 6 -thia-2,5,9a-triaza-benzocyclohepten-3-yl)-5-fluoro-pyridin-2-yl]-amide, 5-Cyano-pyridine-2-carboxylic acid [6-((3R,4aR)-1-amino-3-methyl-4a-oxo-3,4,6,7,8,9-hexahydro-4aλ 6 -thia-2,5,9a-triaza-benzocyclohepten-3-yl)-5-fluoro-pyridin-2-yl]-amide, N-[6-[(1R,10S)-8-Amino-10-(difluoromethyl)-1-oxo-1λ 6 -thia-2,7,9-triazabicyclo[5.40]undeca-1,8-dien-10-yl]-5-fluoropyridin-2-yl]-5-cyanopyridine-2-carboxamide, N-[6-[(1R,10S)-8-Amino-10-(fluoromethyl)-1-oxo-1λ 6 -thia-2,7,9-triazabicyclo[5.4.0]undeca-1,8-dien-10-yl]-5-fluoropyridin-2-yl]-5-cyanopyridine-2-carboxamide, and N-[6-[(1S,10S)-8-Amino-10-(difluoromethyl)-1-oxo-1λ 6 -thia-2,7,9-triazabicyclo[5.4.0]undeca-1,8-dien-10-yl]-5-fluoropyridin-2-yl]-5-cyanopyridine-2-carboxamide. 2. A method of treating Alzheimer's disease, comprising the step of administering a therapeutically effective amount of a compound, or a pharmaceutically acceptable salt thereof, to a human being or animal in need thereof, wherein said compound is selected from the group consisting of: 5-Cyano-pyridine-2-carboxylic acid [6-((3R,4aS)-1-amino-3-methyl-4a-oxo-3,4,6,7,8,9-hexahydro-4aλ 6 -thia-2,5,9a-triaza-benzocyclohepten-3-yl)-5-fluoro-pyridin-2-yl]-amide, N-[6-[(1S,10S)-8-Amino-10-(fluoromethyl)-1-oxo-1λ 6 -thia-2,7,9-triazabicyclo[5.40]undeca-1,8-dien-10-yl]-5-fluoropyridin-2-yl]-5-cyanopyridine-2-carboxamide, 5-Cyano-3-methyl-pyridine-2-carboxylic acid [6-((3R,4aS)-1-amino-3-methyl-4a-oxo-3,4,6,7,8,9-hexahydro-4aλ 6 -thia-2,5,9a-triaza-benzocyclohepten-3-yl)-5-fluoro-pyridin-2-yl]-amide, 5-Cyano-pyridine-2-carboxylic acid [6-((3R,4 aR)-1-amino-3-methyl-4a-oxo-3,4,6,7,8,9-hexahydro-4aλ 6 -thia-2,5,9a-triaza-benzocyclohepten-3-yl)-5-fluoro-pyridin-2-yl]-amide, N-[6-[(1R10S)-8-Amino-10-(difluoronnethyl)-1-oxo-1λ 6 -thia-2,7,9-trazabicyclo[5.4.0]undeca-1,8-dien-10-yl]-5-fluoropyridin-2-yl]-5-cyanopyridine-2-carboxamide, N-[6-[(1R, 10S)-8-Amino- 10-(fluoromethyl)-1-oxo-1λ 6 -thia-2,7,9-triazabioyclo [5.4.0]undeca- 1,8-dien-10-yl]-5-fluoropyridin-2-yl]-5-cyanopyridine-2-carboxamide, and N-[6-[(1S, 10S)-8-Amino-10-(difluoromethyl)-1-oxo-1λ 6 -thia-2,7,9-triazabicyclo[5.4.0]undeca-1,8-dien-10-yl]-5-fluoropyridin-2-yl]-5-cyanopyridine-2-carboxamide.
Assignees
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Classifications
directly linked by a ring-member-to-ring-member bond · CPC title
having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide · CPC title
- C07D513/04Primary
Ortho-condensed systems · CPC title
for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia · CPC title
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Frequently asked questions
Answers are generated from the same data shown on this page.
- What does patent US10414780B2 cover?
- The present invention provides a compound of formula I having BACE1 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.
- Who is the assignee on this patent?
- Hoffmann La Roche
- What technology area does this patent fall under?
- Primary CPC classification C07D513/04. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Sep 17 2019 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 1 related publication on this page (citations in our corpus or others sharing the same primary CPC).