Cb1r receptor blockers with acyclic backbones
US-2025376460-A1 · Dec 11, 2025 · US
POLQ inhibitors
US12414954B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-12414954-B2 |
| Application number | US-202519072385-A |
| Country | US |
| Kind code | B2 |
| Filing date | Mar 6, 2025 |
| Priority date | Dec 6, 2022 |
| Publication date | Sep 16, 2025 |
| Grant date | Sep 16, 2025 |
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- Title
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- Abstract
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- First independent claim
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Abstract
Official abstract text for this publication.
The specification generally relates to compounds of Formula (I):or a stereoisomer or pharmaceutically salt thereof, wherein G, Ga, Gb, X, Y, R1, R2, Q1, Q2, and Q3 have any of the meanings defined herein, together with compositions containing them and their use in therapy. The compounds are inhibitors of the polymerase, DNA polymerase theta (Polθ or POLQ), and are thereby particularly useful in the treatment of cancer.
First claim
Opening claim text (preview).
The invention claimed is: 1. A compound which is 3-(2-chloro-3-(9-(5-chloro-2-methoxybenzyl)-6-(1-methylcyclopropoxy)-9H-purin-8-yl)phenoxy)propanoic acid: or a pharmaceutically acceptable salt thereof. 2. The compound of claim 1 , which is 3-(2-chloro-3-(9-(5-chloro-2-methoxybenzyl)-6-(1-methylcyclopropoxy)-9H-purin-8-yl)phenoxy)propanoic acid: 3. The compound of claim 1 , which is a pharmaceutically acceptable salt of 3-(2-chloro-3-(9-(5-chloro-2-methoxybenzyl)-6-(1-methylcyclopropoxy)-9H-purin-8-yl)phenoxy)propanoic acid: 4. A pharmaceutical composition comprising the compound or pharmaceutically acceptable salt thereof according to claim 1 . 5. A compound which is (1s,3s)-3-(2-chloro-3-(9-(5-chloro-2-methoxybenzyl)-6-(1-methylcyclopropoxy)-9H-purin-8-yl)phenoxy)cyclobutane-1-carboxylic acid: or a pharmaceutically acceptable salt thereof. 6. The compound of claim 5 , which is (1s,3s)-3-(2-chloro-3-(9-(5-chloro-2-methoxybenzyl)-6-(1-methylcyclopropoxy)-9H-purin-8-yl)phenoxy)cyclobutane-1-carboxylic acid: 7. The compound of claim 5 , which is a pharmaceutically acceptable salt of (1s,3s)-3-(2-chloro-3-(9-(5-chloro-2-methoxybenzyl)-6-(1-methylcyclopropoxy)-9H-purin-8-yl)phenoxy)cyclobutane-1-carboxylic acid: 8. A pharmaceutical composition comprising the compound or pharmaceutically acceptable salt thereof according to claim 5 . 9. A compound selected from (R)-4-(2-chloro-3-(9-(5-chloro-2-cyanobenzyl)-6-(1-methylcyclopropoxy)-9H-purin-8-yl)phenoxy)-2-methylbutanoic acid and (S)-4-(2-chloro-3-(9-(5-chloro-2-cyanobenzyl)-6-(1-methylcyclopropoxy)-9H-purin-8-yl)phenoxy)-2-methylbutanoic acid: and or a pharmaceutically acceptable salt thereof. 10. The compound of claim 9 , which is (R)-4-(2-chloro-3-(9-(5-chloro-2-cyanobenzyl)-6-(1-methylcyclopropoxy)-9H-purin-8-yl)phenoxy)-2-methylbutanoic acid: or a pharmaceutically acceptable salt thereof. 11. The compound of claim 9 , which is (S)-4-(2-chloro-3-(9-(5-chloro-2-cyanobenzyl)-6-(1-methylcyclopropoxy)-9H-purin-8-yl)phenoxy)-2-methylbutanoic acid: or a pharmaceutically acceptable salt thereof. 12. The compound of claim 10 , which is (R)-4-(2-chloro-3-(9-(5-chloro-2-cyanobenzyl)-6-(1-methylcyclopropoxy)-9H-purin-8-yl)phenoxy)-2-methylbutanoic acid: 13. The compound of claim 11 , which is (S)-4-(2-chloro-3-(9-(5-chloro-2-cyanobenzyl)-6-(1-methylcyclopropoxy)-9H-purin-8-yl)phenoxy)-2-methylbutanoic acid: 14. The compound of claim 10 , which is a pharmaceutically acceptable salt of (R)-4-(2-chloro-3-(9-(5-chloro-2-cyanobenzyl)-6-(1-methylcyclopropoxy)-9H-purin-8-yl)phenoxy)-2-methylbutanoic acid. 15. The compound of claim 11 , which is a pharmaceutically acceptable salt of (S)-4-(2-chloro-3-(9-(5-chloro-2-cyanobenzyl)-6-(1-methylcyclopropoxy)-9H-purin-8-yl)phenoxy)-2-methylbutanoic acid. 16. A pharmaceutical composition comprising the compound or pharmaceutically acceptable salt thereof according to claim 9 . 17. A pharmaceutical composition comprising the compound or pharmaceutically acceptable salt thereof according to claim 10 . 18. A pharmaceutical composition comprising the compound or pharmaceutically acceptable salt thereof according to claim 11 .
Assignees
Inventors
Classifications
with aryl radicals directly attached in position 2 · CPC title
- C07D473/26Primary
with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both · CPC title
Ortho-condensed systems · CPC title
- C07D473/30Primary
attached in position 6, e.g. hypoxanthine · CPC title
Antineoplastic agents · CPC title
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Frequently asked questions
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- What does patent US12414954B2 cover?
- The specification generally relates to compounds of Formula (I):or a stereoisomer or pharmaceutically salt thereof, wherein G, Ga, Gb, X, Y, R1, R2, Q1, Q2, and Q3 have any of the meanings defined herein, together with compositions containing them and their use in therapy. The compounds are inhibitors of the polymerase, DNA polymerase theta (Polθ or POLQ), and are thereby particularly useful in…
- Who is the assignee on this patent?
- Astrazeneca Ab
- What technology area does this patent fall under?
- Primary CPC classification C07D473/26. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Sep 16 2025 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).