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US-2024424002-A1 · Dec 26, 2024 · US
Optically active azabicyclo ring derivative
US10815241B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10815241-B2 |
| Application number | US-202016748191-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jan 21, 2020 |
| Priority date | Aug 27, 2018 |
| Publication date | Oct 27, 2020 |
| Grant date | Oct 27, 2020 |
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- Title
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- Abstract
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Abstract
Official abstract text for this publication.
The present invention relates to the compound of formula (1a) wherein p is 1 or 2, R 1 -R 4 are hydrogen atom or the like, and a-d are 1 or 2, or a pharmaceutically acceptable salt thereof, which has an antitumor effect by inhibiting the binding between a MLL fusion protein that is infused with AF4, AF9, or the like, which is a representative fusion partner gene causing MLL leukemia, and menin.
First claim
Opening claim text (preview).
The invention claimed is: 1. A compound, which is one of 2-[(4-{7-[1S,3S,4R,6R)-6-(cyclopropylmethyl)-2-azabicyclo[2.2.2]octane-3-carbonyl]-2,7-diazaspiro[3.5]nonan-2-yl}pyrimidin-5-yl)oxy]-5-fluoro-N,N-di(propan-2-yl)benzamide, 5-fluoro-2-[(4-{7-[(1S,3S,4R)-5-methylidene-2-azabicyclo[2.2.2]octane-3-carbonyl]-2,7-diazaspiro[3.5]nonan-2-yl}pyrimidin-5-yl)oxy]-N,N-di(propan-2-yl)benzamide and 5-fluoro-2-[(4-{7-[(1S,3S,4R)-5-( 2 H 2 )methylidene-2-azabicyclo[2.2.2]octane-3-carbonyl]-2,7-diazaspiro[3.5]nonan-2-yl}pyrimidin-5-yl)oxy]-N,N-di(propan-2-yl)benzamide, or a pharmaceutically acceptable salt, hydrate, or solvate thereof. 2. The compound of claim 1 , wherein the compound is 2-[(4-{7-[(1S,3S,4R,6R)-6-(cyclopropylmethyl)-2-azabicyclo[2.2.2]octane-3-carbonyl]-2,7-diazaspiro[3.5]nonan-2-yl}pyrimidin-5-yl)oxy]-5-fluoro-N,N-di(propan-2-yl)benzamide, or a pharmaceutically acceptable salt thereof. 3. The compound of claim 1 , wherein the compound is 5-fluoro-2-[(4-{7-[(1S,3S,4R)-5-methylidene-2-azabicyclo[2.2.2]octane-3-carbonyl]-2,7-diazaspiro[3.5]nonan-2-yl}pyrimidin-5-yl)oxy]-N,N-di(propan-2-yl)benzamide, or a pharmaceutically acceptable salt thereof. 4. The compound of claim 1 , wherein the compound is 5-fluoro-2-[(4-{7-[(1S,3S,4R)-5-( 2 H 2 )methylidene-2-azabicyclo[2.2.2]octane-3-carbonyl]-2,7-diazaspiro[3.5]nonan-2-yl}pyrimidin-5-yl)oxy]-N,N-di(propan-2-yl)benzamide, or a pharmaceutically acceptable salt thereof. 5. The compound of claim 1 , wherein the compound is 5-fluoro-2-[(4-{7-[(1S,3S,4R)-5-methylidene-2-azabicyclo[2.2.2]octane-3-carbonyl]-2,7-diazaspiro[3.5]nonan-2-yl}pyrimidin-5-yl)oxy]-N,N-di(propan-2-yl)benzamide mono-L(+)-tartrate. 6. A pharmaceutical composition, comprising: one or more of the compound of claim 1 ; and at least one member selected from the group consisting of an excipient, a disintegrant, a binder, a fluidizer, a lubricant, a coating agent, a solubilizer, a solubilizing adjuvant, a thickener, a dispersant, a stabilizing agent, a sweetening agent, and a flavor. 7. The pharmaceutical composition of claim 6 , comprising fluoro-2-[(4-{7-[1S,3S,4R)-5-methylidene-2-azabicyclo[2.2.2]octane-3-carbonyl]-2,7-diazaspiro[3.5]nonan-2-yl}pyrimidin-5-yl)oxy]-N,N-di(propan-2-yl)benzamide. 8. The pharmaceutical composition of claim 6 , comprising 5-fluoro-2-[(4-{7-[(1S,3S,4R)-5-( 2 H 2 )methylidene-2-azabicyclo[2.2.2]octane-3-carbonyl]-2,7-diazaspiro[3.5]nonan-2-yl}pyrimidin-5-yl)oxy]-N,N-di(propan-2-yl)benzamide or a pharmaceutically acceptable salt thereof. 9. The pharmaceutical composition of claim 6 , comprising 5-fluoro-2-[(4-{7-[(1S,3S,4R)-5-methylidene-2-azabicyclo[2.2.2]octane-3-carbonyl]-2,7-diazaspiro[3.5]nonan-2-yl}pyrimidin-5-yl)oxy]-N,N-di(propan-2-yl)benzamide or a hydrate or solvate thereof. 10. The pharmaceutical composition of claim 6 , comprising 5-fluoro-2-[(4-{7-[(1S,3S,4R)-5-( 2 H 2 )methylidene-2-azabicyclo[2.2.2]octane-3-carbonyl]-2,7-diazaspiro[3.5]nonan-2-yl}pyrimidin-5-yl)oxy]-N,N-di(propa-2-yl)benzamide or a pharmaceutically acceptable salt, hydrate, or solvate thereof.
Assignees
Inventors
Classifications
- A61P35/00Primary
Antineoplastic agents · CPC title
- C07D487/10Primary
Spiro-condensed systems · CPC title
Ortho-condensed systems · CPC title
Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title
spiro-condensed · CPC title
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Frequently asked questions
Answers are generated from the same data shown on this page.
- What does patent US10815241B2 cover?
- The present invention relates to the compound of formula (1a) wherein p is 1 or 2, R 1 -R 4 are hydrogen atom or the like, and a-d are 1 or 2, or a pharmaceutically acceptable salt thereof, which has an antitumor effect by inhibiting the binding between a MLL fusion protein that is infused with AF4, AF9, or the like, which is a representative fusion partner gene causing MLL leukemia, and menin.
- Who is the assignee on this patent?
- Sumitomo Dainippon Pharma Co Ltd
- What technology area does this patent fall under?
- Primary CPC classification A61P35/00. Mapped technology areas include Human Necessities.
- When was this patent published?
- Publication date Tue Oct 27 2020 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).