Inhibitors of tyk2
US-2024425484-A1 · Dec 26, 2024 · US
Phosphatidylinositol 3-kinase inhibitors
US9765060B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9765060-B2 |
| Application number | US-201514747931-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jun 23, 2015 |
| Priority date | Jun 24, 2014 |
| Publication date | Sep 19, 2017 |
| Grant date | Sep 19, 2017 |
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Abstract
Official abstract text for this publication.
The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (J), or pharmaceutically acceptable salts thereof, in which A, n, m, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms. The present disclosure further provides pharmaceutical compositions that include a compound of formula (J), or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms.
First claim
Opening claim text (preview).
What is claimed is: 1. A compound selected from the group consisting of: (S)-2-(cyclopropyl((2,6-diamino-5-cyanopyrimidin-4-yl)amino)methyl)-4-oxo-3-phenyl-3,4-dihydroquinazoline-5-carbonitrile; (S)-2-(cyclopropyl((2,6-diamino-5-cyanopyrimidin-4-yl)amino)methyl)-8-fluoro-4-oxo-3-phenyl-3,4-dihydroquinazoline-5-carbonitrile; (S)-2,4-diamino-6-(((5-chloro-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)(phenyl)methyl)amino)pyrimidine-5-carbonitrile; (S)-2-(cyclopropyl((2,6-diamino-5-cyanopyrimidin-4-yl)amino)methyl)-3-(3-(difluoromethyl)-5-fluorophenyl)-4-oxo-3,4-dihydroquinazoline-5-carbonitrile; (S)-2,4-diamino-6-((cyclopropyl(3-(3-fluorophenyl)-5-(methylsulfonyl)-4-oxo-3,4-dihydroquinazolin-2-yl)methyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((cyclopropyl(3-(2-fluorophenyl)-5-(methylsulfonyl)-4-oxo-3,4-dihydroquinazolin-2-yl)methyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((cyclopropyl(3-(2-fluorophenyl)-5-(methylsulfonyl)-4-oxo-3,4-dihydroquinazolin-2-yl)methyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((cyclopropyl(3-(2,6-difluorophenyl)-5-(methylsulfonyl)-4-oxo-3,4-dihydroquinazolin-2-yl)methyl)amino)pyrimidine-5-carbonitrile; (S)-2-(cyclopropyl((2,6-diamino-5-cyanopyrimidin-4-yl)amino)methyl)-6-fluoro-3-(3-fluorophenyl)-4-oxo-3,4-dihydroquinazoline-8-carbonitrile; (S)-2-(cyclopropyl((2,6-diamino-5-cyanopyrimidin-4-yl)amino)methyl)-6-fluoro-4-oxo-3-phenyl-3,4-dihydroquinazoline-8-carbonitrile; (S)-3-(5-chloro-3-(3,5-difluorophenyl)-4-oxo-3,4-dihydroquinazolin-2-yl)-3-((2,6-diamino-5-cyanopyrimidin-4-yl)amino)-N,N-dimethylpropanamide (S)-3-(5-chloro-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)-3-((2,6-diamino-5-cyanopyrimidin-4-yl)amino)-N,N-dimethylpropanamide; (S)-2,4-diamino-6-(((3-(3-cyano-5-fluorophenyl)-5-methyl-4-oxo-3,4-dihydroquinazolin-2-yl)(cyclopropyl)methyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((cyclopropyl(3-(3,5-difluorophenyl)-5-methyl-4-oxo-3,4-dihydroquinazolin-2-yl)methyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-(((5-chloro-3-(3,5-difluorophenyl)-4-oxo-3,4-dihydroquinazolin-2-yl)(cyclopropyl)methyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((cyclopropyl(3-(3,5-difluorophenyl)-5-fluoro-4-oxo-3,4-dihydroquinazolin-2-yl)methyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((cyclopropyl(5-fluoro-3-(3-fluorophenyl)-4-oxo-3,4-dihydroquinazolin-2-yl)methyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((cyclopropyl(6-fluoro-3-(3-fluorophenyl)-4-oxo-3,4-dihydroquinazolin-2-yl)methyl)amino)pyrimidine-5-carbonitrile; (S)-2-(1-((5-acetyl-2,6-diaminopyrimidin-4-yl)amino)ethyl)-5-chloro-3-(3,5-difluorophenyl)quinazolin-4(3H)-one, 2,4-diamino-6-((2S)-2-(5-chloro-3-(3, 5-difluorophenyl)-4-oxo-3,4-dihydroquinazolin-2-yl)-4-methoxypyrrolidin-1-yl)pyrimidine-5-carbonitrile; (S)-2-(1-((6-amino-5-bromo-2-methylpyrimidin-4-yl)amino)ethyl)-5-chloro-3-phenylquinazolin-4(3H)-one; (S)-2-(1-((6-amino-5-bromo-2-methylpyrimidin-4-yl)amino)ethyl)-5-chloro-3-(3,5-difluorophenyl)quinazolin-4(3H)-one; (S)-2,4-diamino-6-((1-(5-(2-morpholinoethoxy)-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((1-(5-(2-(azepan-1-yl)ethoxy)-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((1-(4-oxo-3-phenyl-5-(2-(pyrrolidin-1-yl)ethoxy)-3,4-dihydroquinazolin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile; (S)-isopropyl 2-((2-(1-((2,6-diamino-5-cyanopyrimidin-4-yl)amino)ethyl)-4-oxo-3-phenyl-3,4-dihydroquinazolin-5-yl)oxy)acetate; (S)-2,4-diamino-6-((1-(4-oxo-5-(2-(2-oxopyrrolidin-1-yl)ethoxy)-3-phenyl-3,4-dihydroquinazolin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((1-(5-(2-(dimethylamino)ethoxy)-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((1-(4-oxo-5-(2-oxo-2-(piperidin-1-yl)ethoxy)-3-phenyl-3,4-dihydroquinazolin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((1-(5-(3-hydroxy-2-(hydroxymethyl)-2-methylpropoxy)-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((1-(4-oxo-3-phenyl-5-(2-(piperidin-1-yl)ethoxy)-3,4-dihydroquinazolin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((1-(4-oxo-3-phenyl-5-(2-(4-phenylpiperazin-1-yl)ethoxy)-3,4-dihydroquinazolin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((1-(5-(2-(2-methyl-1H-imidazol-1-yl)ethoxy)-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile; 2,4-diamino-6-(((1 S)-1-(5-(2-(1-methylpyrrolidin-2-yl)ethoxy)-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((1-(5-((3-methyloxetan-3-yl)methoxy)-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((1-(5-(2-morpholino-2-oxoethoxy)-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((1-(5-(2-(4-methylpiperidin-1-yl)-2-oxoethoxy)-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile; (S)-3-(2-(1-((2,6-diamino-5-cyanopyrimidin-4-yl)amino)ethyl)-4-oxo-3-phenyl-3,4-dihydroquinazolin-5-yl)propanamide; (S)-3-(2-(1-((2,6-diamino-5-cyanopyrimidin-4-yl)amino)ethyl)-8-fluoro-4-oxo-3-phenyl-3,4-dihydroquinazolin-5-yl)propanamide; (S)-3-(2-(1-((2,6-diamino-5-cyanopyrimidin-4-yl)amino)ethyl)-3-(3,5-difluorophenyl)-8-fluoro-4-oxo-3,4-dihydroquinazolin-5-yl)propanamide; (S)-3-(2-(1-((2,6-diamino-5-cyanopyrimidin-4-yl)amino)ethyl)-3-(3,5-difluorophenyl)-4-oxo-3,4-dihydroquinazolin-5-yl)propanamide; (S)-3-(2-(1-((2,6-diamino-5-chloropyrimidin-4-yl)amino)ethyl)-3-(3,5-difluorophenyl)-8-fluoro-4-oxo-3,4-dihydroquinazolin-5-yl)propanamide; (S)-3-(2-(1-((2,6-diamino-5-chloropyrimidin-4-yl)amino)ethyl)-3-(3,5-difluorophenyl)-4-oxo-3,4-dihydroquinazolin-5-yl)propanamide; (S)-3-(2-(1-((2,6-diamino-5-chloropyrimidin-4-yl)amino)ethyl)-4-oxo-3-phenyl-3,4-dihydroquinazolin-5-yl)propanamide; (S)-3-(2-(1-((2,6-diamino-5-chloropyrimidin-4-yl)amino)ethyl)-8-fluoro-4-oxo-3-phenyl-3,4-dihydroquinazolin-5-yl)propanamide; (S)-2,4-diamino-6-((1-(4-oxo-3-phenyl-5-(3-(pyrrolidin-1-yl)propyl)-3,4-dihydroquinazolin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((1-(4-oxo-3-phenyl-5-(3-(piperidin-1-yl)propyl)-3,4-dihydroquinazolin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((1-(5-(3-(3,3-difluoropyrrolidin-1-yl)propyl)-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((1-(5-(3-(4,4-difluoropiperidin-1-yl)propyl)-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile; 2,4-diamino-6-(((1S)-1-(5-(3-(3,5-dimethylmorpholino)propyl)-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((1-(8-fluoro-4-oxo-3-phenyl-5-(3-(pyrrolidin-1-yl)propyl)-3,4-dihydroquinazolin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((1-(3-(3,5-difluorophenyl)-4-oxo-5-(3-(pyrrolidin-1-yl)propyl)-3,4-dihydroquinazolin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((1-(5-(3-(2,2-dimethylmorpholino)propyl)-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((1-(5-(3-(3,3-dimethylmorpholino)propyl)-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((1-(4-oxo-3-phenyl-5-(3-(2,2,6,6-tetrafluoromorpholino)propyl)-3,4-dihydroquinazolin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((1-(5-(3-(3,3-difluoropyrrolidin-1-yl)propyl)-8-fluoro-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((cyclopropyl(4-oxo-3-phenyl-5-(3-(pyrrolidin-1-yl)propyl)-3,4-dihydroquinazolin-2-yl)methyl)amino)pyrimidine-5-carbonitrile; (S)-2,4-diamino-6-((cyclopropyl(4-oxo-3-phenyl-5-(3-(piper
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- What does patent US9765060B2 cover?
- The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (J), or pharmaceutically acceptable salts thereof, in which A, n, m, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms. The present disclosure further provides pharmaceu…
- Who is the assignee on this patent?
- Gilead Sciences Inc
- What technology area does this patent fall under?
- Primary CPC classification C07D403/12. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Sep 19 2017 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 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).