Inhibitors of tyk2
US-2024425484-A1 · Dec 26, 2024 · US
Phosphoinositide 3-kinase inhibitor compounds and methods of use
US9487533B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9487533-B2 |
| Application number | US-95118907-A |
| Country | US |
| Kind code | B2 |
| Filing date | Dec 5, 2007 |
| Priority date | Dec 7, 2006 |
| Publication date | Nov 8, 2016 |
| Grant date | Nov 8, 2016 |
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Abstract
Official abstract text for this publication.
Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R 3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
First claim
Opening claim text (preview).
We claim: 1. A compound selected from 4-(2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)N-methylsulfonylpiperidin-4-ol; N-((2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[2,3-d]pyrimidin-6-yl)methyl)-N-methylbenzamide; N-((2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[2,3-d]pyrimidin-6-yl)methyl)-N-methylnicotinamide; 5-(6-(3-(N-methylsulfonylaminomethyl)phenyl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine; 5-(6-(3-N-methylsulfonylaminophenyl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine; 5-(6-(6-aminopyridin-3-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine; 5-(6-(4-methoxypyridin-3-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine; 5-(7-methyl-4-morpholino-6-(pyridin-3-yl)thieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine; 5-(6-(4-(aminomethyl)phenyl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine; 5-(6-(3-(aminomethyl)phenyl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine; 5-(6-(4-amino-3-methoxyphenyl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine; N-(2-(2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)propan-2-yl)-3-methoxybenzamide; N-(2-(2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)propan-2-yl)-4-methoxybenzamide; 5-(6-(4-N-methylsulfonylaminophenyl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine; N-(2-(2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)propan-2-yl)nicotinamide; N-(2-(2-(6-methylpyridin-3-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)propan-2-yl)benzamide; 5-(4-morpholino-6-(3-morpholinosulfonyl)phenylthieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine; 5-(4-morpholino-6-(3-morpholinosulfonyl)phenylthieno[3,2-d]pyrimidin-2-yl)pyridin-2-amine; 5-(4-morpholino-6-(3-(2-hydroxyethylamino)sulfonyl)phenylthieno[3,2-d]pyrimidin-2-yl)pyridin-2-amine; 5-(4-morpholino-6-(3-aminosulfonyl)phenylthieno[3,2-d]pyrimidin-2-yl)pyridin-2-amine; (S)—N-((4-(2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)phenyl)methyl)-2-hydroxypropanamide; N-((4-(2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)phenyl)methyl)-2-hydroxyacetamide; (2S)—N-((3-(2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)phenyl)methyl)-2-hydroxypropanamide; N-((3-(2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)phenyl)methyl)acetamide; N-((3-(2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)phenyl)methyl)-2-hydroxyacetamide; (4-(2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)phenyl)(4-methylpiperazin-1-yl)methanone; (4-(2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)phenyl)(morpholino)methanone; (4-(2-(6-aminopyridin-3-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)phenyl)(4-methylpiperazin-1-yl)methanone; (4-(2-(6-aminopyridin-3-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)phenyl)(morpholino)methanone; 5-(6-(3-(1H-tetrazol-5-yl)phenyl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine; 3-(2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)benzoic acid; 3-(2-(6-aminopyridin-3-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)benzoic acid; 5-(6-(3-aminophenyl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine; 5-(6-(3-aminophenyl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyridin-2-amine; (3-(2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)phenyl)(4-methylpiperazin-1-yl)methanone; 3-(2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)-N—((S)-2-hydroxypropyl)benzamide; (3-(2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)phenyl)(morpholino)methanone; 3-(2-(6-aminopyridin-3-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)-N—((S)-2-hydroxypropyl)benzamide; N-((2-(6-aminopyridin-3-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)-N-methylacetamide; N-((2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)-N-methylacetamide; N-((2-(6-aminopyridin-3-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)-N-methylbenzamide; N-((2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)-2-methoxy-N-methylacetamide; (3-(2-(6-aminopyridin-3-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)phenyl)(4-methylpiperazin-1-yl)methanone; (3-(2-(6-aminopyridin-3-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)phenyl)(morpholino)methanone; 5-(4-morpholino-6-(3-N-2-hydroxyethylaminosulfonyl)phenylthieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine; 5-(4-morpholino-6-(6-(4-methylsulfonylpiperazin-1-yl)pyridin-3-yl)thieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine; 5-(4-morpholino-6-(6-(piperazin-1-yl)pyridin-3-yl)thieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine; 5-(2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)pyrazin-2-amine; N-((2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[2,3-d]pyrimidin-6-yl)methyl)-N-methylacetamide; 5-(6-(3-methylsulfonylaminophenyl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine; 2-(2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)propan-2-ol; 2-(2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)-1,3-dimethoxypropan-2-ol; 2-(2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)-1-methoxypropan-2-ol; N-((2-(6-aminopyridin-3-yl)-4-morpholinothieno[2,3-d]pyrimidin-6-yl)methyl)-N-methylacetamide; 5-(6-(6-aminopyridin-3-yl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine; (2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)(4-(2-hydroxyethyl)piperazin-1-yl)methanone; (2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)(4-methylpiperazin-1-yl)methanone; 2-2-aminopyrimidin-5-yl)-4-morpholino-N-(2-(piperidin-1-yl)ethyl)thieno[3,2-d]pyrimidine-6-carboxamide; (2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)(morpholino)methanone; 2-(2-aminopyrimidin-5-yl)-N-methyl-4-morpholinothieno[3,2-d]pyrimidine-6-carboxamide; 5-(6-((E)-3-methoxyprop-1-enyl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine; 2-amino-N-(3-(2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)phenyl)acetamide; 5-(6-((N-methyl,N-methylsulfonylamino)methyl)-4-morpholinothieno[2,3-d]pyrimidin-2-yl)pyrimidin-2-amine; 2-amino-N-(3-(2-(6-aminopyridin-3-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)phenyl)acetamide; 2-(3-(2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)phenyl)propan-2-ol; 5-(6-((N-methyl,N-methylsulfonylamino)methyl)-4-morpholinothieno[2,3-d]pyrimidin-2-yl)pyridin-2-amine; 5-6-(3-(N-methylsulfonylaminomethyl)phenyl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine; 5-(6-(2-(4-methylpiperazin-1-yl)pyridin-4-yl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyridin-2-amine; 5-(6-(2-(4-methylpiperazin-1-yl)pyridin-4-yl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine; 2-(3-(2-(6-aminopyridin-3-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)phenyl)propan-2-ol; 1-(3-(2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)phenyl)ethanol; 1-(3-(2-(6-aminopyridin-3-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)phenyl)ethanol; 3-(3-(2-(6-aminopyridin-3-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)phenyl)propan-1-ol; 3-(3-(2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)phenyl)propan-1-ol; (2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)(N-4-methylsulfonylpiperazin-1-yl)methanone; 5-(6-(2-aminothiazol-4-yl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyridin-2-amine; 5-(6-(4-(4-methylpiperazin-1-yl)phenyl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyridin-2-amine; 5-(6-(3,5-dimethylisoxazol-4-yl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine; 5-(4-morpholino-6-(6-morpholinopyridin-3-yl)thieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine; 5-(6-(2-fluoro-5-methoxyphenyl)-4-morpholinothieno[3,2-d]pyrimidin-2-
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Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title
Drugs for immunological or allergic disorders · CPC title
Antineoplastic agents · CPC title
for hyperglycaemia, e.g. antidiabetics · CPC title
ortho- or peri-condensed with heterocyclic rings · CPC title
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- What does patent US9487533B2 cover?
- Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R 3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of u…
- Who is the assignee on this patent?
- Castanedo Georgette, Dotson Jennafer, Goldsmith Richard, and 15 more
- What technology area does this patent fall under?
- Primary CPC classification C07D491/048. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Nov 08 2016 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).