Biheteroaryl compounds and uses thereof
US-2016158234-A1 · Jun 9, 2016 · US
Biheteroaryl compounds and uses thereof
US10010549B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10010549-B2 |
| Application number | US-201514927267-A |
| Country | US |
| Kind code | B2 |
| Filing date | Oct 29, 2015 |
| Priority date | May 1, 2013 |
| Publication date | Jul 3, 2018 |
| Grant date | Jul 3, 2018 |
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- Title
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Abstract
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The present invention provides for compounds of Formula I-I and embodiments and salts thereof for the treatment of diseases (e.g., neurodegenerative diseases). R 1 , R 2 , R 3 , X 1 , X 2 , A and Cy variable in Formula I-I all have the meaning as defined herein.
First claim
Opening claim text (preview).
The invention claimed is: 1. A compound selected from the group consisting of: 5-[2-cyclobutyl-6-[(1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 5-[2-(3-azabicyclo[2.1.1]hexan-3-yl)-6-[(1S,4S)-5-(2-methoxyethyl)-2,5-diazabicyclo[2.2.1]heptan-2-yl]pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 5-[2-(3-azabicyclo[2.1.1]hexan-3-yl)-6-morpholino-pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 3-(difluoromethoxy)-5-[2-[cis-3,4-difluoropyrrolidin-1-yl]-6-morpholino-pyrimidin-4-yl]pyridin-2-amine; 3-(difluoromethoxy)-5-[6-[(1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]-2-pyrrolidin-1-yl-pyrimidin-4-yl]pyridin-2-amine; 3-(difluoromethoxy)-5-[2-[(3R)-3-fluoropyrrolidin-1-yl]-6-[(1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]pyrimidin-4-yl]pyridin-2-amine; 3-(difluoromethoxy)-5-[2-(3-fluoropyrrolidin-1-yl)-6-[(1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]pyrimidin-4-yl]pyridin-2-amine; (±)-5-[6-(cis-2,3,3a,4,6,6a-hexahydrofuro[2,3-c]pyrrol-5-yl)-2-(3-azabicyclo[2.1.1]hexan-3-yl)pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 5-[2-cyclopropyl-6-[(1S,5R)-3-[(3-methyloxetan-3-yl)methyl]-3-azabicyclo[3.1.0]hexan-6-yl]pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 5-[2-(3-azabicyclo[2.1.1]hexan-3-yl)-6-[(1S,5R)-3-(1-methylimidazol-2-yl)-3-azabicyclo[3.1.0]hexan-6-yl]pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 5-[2-(3-azabicyclo[2.1.1]hexan-3-yl)-6-(2-oxa-7-azaspiro[3.4]octan-7-yl)pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; (±)-5-[2-(3-azabicyclo[2.1.1]hexan-3-yl)-6-(2-oxa-7-azaspiro[4.4]nonan-7-yl)pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 5-[2-(3-azabicyclo[2.1.1]hexan-3-yl)-6-(2-oxa-7-azaspiro[3.5]nonan-7-yl)pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; (±)-5-[2-(3-azabicyclo[2.1.1]hexan-3-yl)-6-(3-methoxypyrrolidin-1-yl)pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 5-[6-(azetidin-1-yl)-2-cyclobutyl-pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; (±)-1-(3-(6-(6-amino-5-(difluoromethoxy)pyridin-3-yl)-2-cyclopropylpyrimidin-4-yl)-cis-3,6-diazabicyclo[3.2.0]heptan-6-yl)ethanone; 1-[(1S,5R)-6-[6-[6-amino-5-(difluoromethoxy)-3-pyridyl]-2-cyclopropyl-pyrimidin-4-yl]-3-azabicyclo[3.1.0]hexan-3-yl]propan-2-ol; 5-[2-(3-azabicyclo[2.1.1]hexan-3-yl)-6-(azetidin-1-yl)pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 5-[2-cyclopropyl-6-[(1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]pyrimidin-4-yl]-3-[1-(1-methylpyrazol-3-yl)ethoxy]pyridin-2-amine; 5-[6-cyclopropyl-4-[(1R,5S)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]-2-pyridyl]-3-(difluoromethoxy)pyridin-2-amine; 5-[6-(3-azabicyclo[2.1.1]hexan-3-yl)-4-[1-(oxetan-3-yl)azetidin-3-yl]-2-pyridyl]-3-(difluoromethoxy)pyridin-2-amine; 5-[6-(azetidin-1-yl)-2-[(3S)-3-fluoropyrrolidin-1-yl]pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 5-[6-(azetidin-1-yl)-2-[cis-3,4-difluoropyrrolidin-1-yl]pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 5-[2-cyclopropyl-6-[(1R,5S)-3-[tetrahydrofuran-3-yl]-3-azabicyclo[3.1.0]hexan-6-yl]pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 5-[2-cyclopropyl-6-[(1S,5R)-3-[(2S)-2-methoxypropyl]-3-azabicyclo[3.1.0]hexan-6-yl]pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 1-[3-[2-[6-amino-5-(difluoromethoxy)-3-pyridyl]-6-cyclopropyl-4-pyridyl]azetidin-1-yl]-2-methyl-propan-2-ol; 5-[2-cyclopropyl-6-[(1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]pyrimidin-4-yl]-3-[1-phenylethoxy]pyridin-2-amine; 5-[2-(azetidin-1-yl)-6-(6-oxa-2-azaspiro[3.4]octan-2-yl)pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 5-[2-(azetidin-1-yl)-6-(3-methoxy-3-methyl-azetidin-1-yl)pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 5-[2-cyclopropyl-6-(3-methoxyazetidin-1-yl)pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 5-[2-cyclopropyl-6-(3-fluoroazetidin-1-yl)pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 5-[2-cyclopropyl-6-[(1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]pyrimidin-4-yl]-3-[1-phenylethoxy]pyridin-2-amine; 5-[6-(azetidin-1-yl)-2-cyclopropyl-pyrimidin-4-yl]-3-[1-(2-pyridyl)ethoxy]pyridin-2-amine; 5-[6-(azetidin-1-yl)-2-cyclopropyl-pyrimidin-4-yl]-3-[1-thiazol-2-ylethoxy]pyridin-2-amine; 5-[6-(azetidin-1-yl)-2-cyclopropyl-pyrimidin-4-yl]-3-[1-(1-methylpyrazol-3-yl)ethoxy]pyridin-2-amine; 5-[2-(3-azabicyclo[2.1.1]hexan-3-yl)-6-(3-methoxyazetidin-1-yl)pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 5-[2-cyclopropyl-6-[(1S,4S)-5-(2-methoxyethyl)-2,5-diazabicyclo[2.2.1]heptan-2-yl]pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 3-(difluoromethoxy)-5-[2-[3-methylpyrrolidin-1-yl]-6-[(1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]pyrimidin-4-yl]pyridin-2-amine; 5-[6-(azetidin-1-yl)-2-cyclopropyl-pyrimidin-4-yl]-3-[1-(4-methylthiazol-2-yl)ethoxy]pyridin-2-amine; 3-(difluoromethoxy)-5-[2-[3-methylpyrrolidin-1-yl]-6-[(1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]pyrimidin-4-yl]pyridin-2-amine; 5-[2-cyclopropyl-6-[3-(oxetan-3-yl)-3-azabicyclo[3.3.1]nonan-7-yl]pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 5-[2-cyclopropyl-6-[3-(2-methoxyethyl)-3-azabicyclo[3.3.1]nonan-7-yl]pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 5-[2-cyclopropyl-6-[2-methyl-4-(oxetan-3-yl)piperazin-1-yl]pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 5-[2-cyclopropyl-6-[4-(2-methoxyethyl)-2-methyl-piperazin-1-yl]pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 3-(difluoromethoxy)-5-[6-ethyl-4-[(1R,5S)-3-(2-methoxyethyl)-3-azabicyclo[3.1.0]hexan-6-yl]-2-pyridyl]pyridin-2-amine; 3-(difluoromethoxy)-5-[2-[3-(difluoromethyl)pyrrolidin-1-yl]-6-[(1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]pyrimidin-4-yl]pyridin-2-amine; 5-[2-(3-azabicyclo[2.1.1]hexan-3-yl)-6-(3-ethoxy-3-methyl-azetidin-1-yl)pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 5-[2-cyclopropyl-6-[(3R)-3-fluoropyrrolidin-1-yl]pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 5-[2-cyclopropyl-6-[(3S)-3-fluoropyrrolidin-1-yl]pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 5-[6-cyclopropyl-4-[(1R,5S)-3-(2-methoxyethyl)-3-azabicyclo[3.1.0]hexan-6-yl]-2-pyridyl]-3-(difluoromethoxy)pyridin-2-amine; 3-(difluoromethoxy)-5-[2-(3-fluoro-3-methyl-pyrrolidin-1-yl)-6-[(1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]pyrimidin-4-yl]pyridin-2-amine; 3-(difluoromethoxy)-5-[2-(3,3-difluoropyrrolidin-1-yl)-6-[(1R,4R)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]pyrimidin-4-yl]pyridin-2-amine; 5-[2-(3-azabicyclo[2.1.1]hexan-3-yl)-6-[(1R,4R)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 3-(difluoromethoxy)-5-[2-[(3S)-3-fluoropyrrolidin-1-yl]-6-[(1R,4R)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]pyrimidin-4-yl]pyridin-2-amine; 5-[2-(3-azabicyclo[2.1.1]hexan-3-yl)-6-(3-morpholinoazetidin-1-yl)pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 3-(difluoromethoxy)-5-[2-(3,3-difluoropyrrolidin-1-yl)-6-(3-morpholinoazetidin-1-yl)pyrimidin-4-yl]pyridin-2-amine; 5-[2-(2,2-difluoroethyl)-6-[(1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 3-(difluoromethoxy)-5-[2-(3,3-difluoropyrrolidin-1-yl)-6-[3-morpholinopyrrolidin-1-yl]pyrimidin-4-yl]pyridin-2-amine; 3-(difluoromethoxy)-5-[2-(3,3-difluoropyrrolidin-1-yl)-6-[3-morpholinopyrrolidin-1-yl]pyrimidin-4-yl]pyridin-2-amine; 5-[2-(3-azabicyclo[2.1.1]hexan-3-yl)-6-[3-morpholinopyrrolidin-1-yl]pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 5-[2-(3-azabicyclo[2.1.1]hexan-3-yl)-6-[3-morpholinopyrrolidin-1-yl]pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 5-[2-cyclopropyl-6-[3-morpholinopyrrolidin-1-yl]pyrimidin-4-yl]-3-(difluoromethoxy)pyridin-2-amine; 3-(difluoromethoxy)-5-[2-[(3S)-3-fluoro-3-methyl-pyrrolidin-1-yl]-6-[(1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]pyrimidin-4-yl]pyridin-2-amine; 3-(difluoromethoxy)-5-[2-[(3R)-3-fluoro-3-methyl-pyrrolidin-1-yl]-6-[(1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]pyrimidin-4-yl]pyridin-2-amine; 5-[2-[2,2-difluorocyclopropyl]-6-[(1S,4S)-2-oxa-5-azabicyclo[2.2.1]h
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Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title
for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title
Drugs for disorders of the cardiovascular system · CPC title
Antidotes · CPC title
for HIV · CPC title
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- What does patent US10010549B2 cover?
- The present invention provides for compounds of Formula I-I and embodiments and salts thereof for the treatment of diseases (e.g., neurodegenerative diseases). R 1 , R 2 , R 3 , X 1 , X 2 , A and Cy variable in Formula I-I all have the meaning as defined herein.
- Who is the assignee on this patent?
- Genentech Inc
- What technology area does this patent fall under?
- Primary CPC classification A61K31/506. Mapped technology areas include Human Necessities.
- When was this patent published?
- Publication date Tue Jul 03 2018 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 3 related publications on this page (citations in our corpus or others sharing the same primary CPC).