Use of substituted 2-amidobenzimidazoles, 2-amidobenzoxazoles and 2-amidobenzothiazoles or salts thereof as active substances against abiotic plant stress
US-2015216168-A1 · Aug 6, 2015 · US
Radiolabeled tracers for poly (ADP-ribose) polymerase-1 (PARP-1), methods and uses therefor
US9993570B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9993570-B2 |
| Application number | US-201615201765-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jul 5, 2016 |
| Priority date | Jan 5, 2014 |
| Publication date | Jun 12, 2018 |
| Grant date | Jun 12, 2018 |
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Abstract
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Disclosed are PARP-1 inhibitors, which can be 18 F-labeled for use as tracers in positron emission tomographic (PET) imaging. Further disclosed are methods of synthesis. Of the compounds synthesized, 2-[p-(2-Fluoroethoxy)phenyl]-1.3.10-triazatricyclo[6.4.1.0 4,13 ]trideca-2,4(13),5,7-tetraen-9-one (12) had the highest inhibition potency for PARP-1 (IC 50 =6.3 nM). Synthesis of [ 18 F]-12 is disclosed under conventional conditions in high specific activity with 40-50% decay-corrected yield. MicroPET imaging using [ 18 F]-12 in MDA-MB-436 tumor-bearing mice demonstrated accumulation of [ 18 F]-12 in a tumor. Binding, can be blocked by olaparib. The compounds have utility for tumor imaging.
First claim
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What is claimed is: 1. A compound or pharmaceutically acceptable salt thereof of structure 2. The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein the fluorine designated F is an 18 F fluorine. 3. A method of imaging a tissue in a subject, comprising: administering to a subject a compound or pharmaceutically acceptable salt thereof of structure and subjecting the subject to positron emission tomography (PET) scanning. 4. The method of imaging a tissue in a subject according to claim 3 , wherein the tissue is a tumor tissue. 5. The method of imaging a tissue in a subject according to claim 3 , wherein the tissue is an inflamed tissue.
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Antineoplastic agents · CPC title
Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title
with aryl radicals directly attached in position 2 · CPC title
Ortho-condensed systems · CPC title
Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title
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- What does patent US9993570B2 cover?
- Disclosed are PARP-1 inhibitors, which can be 18 F-labeled for use as tracers in positron emission tomographic (PET) imaging. Further disclosed are methods of synthesis. Of the compounds synthesized, 2-[p-(2-Fluoroethoxy)phenyl]-1.3.10-triazatricyclo[6.4.1.0 4,13 ]trideca-2,4(13),5,7-tetraen-9-one (12) had the highest inhibition potency for PARP-1 (IC 50 =6.3 nM). Synthesis of [ 18 F]-12 is di…
- Who is the assignee on this patent?
- Univ Washington
- What technology area does this patent fall under?
- Primary CPC classification A61K51/0468. Mapped technology areas include Human Necessities.
- When was this patent published?
- Publication date Tue Jun 12 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 1 related publication on this page (citations in our corpus or others sharing the same primary CPC).