2,3-dihydrobenzo[b]thiophene derivatives as hypoxia inducible factor-2(alpha) inhibitors
US-12171741-B2 · Dec 24, 2024 · US
US9481685B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9481685-B2 |
| Application number | US-200913119450-A |
| Country | US |
| Kind code | B2 |
| Filing date | Oct 2, 2009 |
| Priority date | Oct 2, 2008 |
| Publication date | Nov 1, 2016 |
| Grant date | Nov 1, 2016 |
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The present invention concerns in vivo imaging and in particular in vivo imaging of the peripheral benzodiazepine receptor (PBR). A tetracyclic indole in vivo imaging agent is provided that binds with high affinity to PBR, has good uptake into the brain following administration, and which preferentially binds to tissues expressing higher levels of PBR. The present invention also provides a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said in vivo imaging agent comprising use of said precursor compound, and a kit for carrying out said method. A cassette for the automated synthesis of the in vivo imaging agent is also provided. In addition, the invention provides a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, as well as methods for the use of said in vivo imaging agent.
Opening claim text (preview).
What is claimed is: 1. An in vivo imaging agent which is selected from: 2. A precursor compound useful for the preparation of an in vivo imaging compound, wherein said imaging compound is selected from: and said precursor compound is selected from: wherein LG is selected from the group consisting of Cl, Br, I, tosylate (OTs), mesylate (OMs), and triflate. 3. A radiopharmaceutical composition comprising an in vivo imaging agent as defined in claim 1 , together with a biocompatible carrier in a form suitable for mammalian administration.
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Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations · CPC title
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