3,4,5-trimethoxystyrylarylaminopropenones as potential anticancer agents
US-9487482-B2 · Nov 8, 2016 · US
US11261152B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-11261152-B2 |
| Application number | US-201816478914-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jan 19, 2018 |
| Priority date | Jan 20, 2017 |
| Publication date | Mar 1, 2022 |
| Grant date | Mar 1, 2022 |
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The present disclosure provides compounds and methods for inhibiting or degrading the N-terminal domain of the androgen receptor, as well as methods for treating cancers such as prostate cancer.
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The invention claimed is: 1. A compound represented by formula VIIb: wherein: each R 8 is independently selected from halo, alkyl, or alkyloxy; each R 9 is independently selected from halo, alkyl, or alkyloxy; t is 0, 1, 2, 3, 4, or 5; and q is 0, 1, 2, 3, 4, or 5. 2. The compound of claim 1 , wherein each R 8 is independently selected from halo. 3. The compound of claim 1 , wherein each R 9 is independently selected from halo. 4. The compound of claim 1 , wherein t is 1, 2 or 3. 5. The compound of claim 1 , wherein q is 1, 2 or 3. 6. A pharmaceutical composition comprising the compound of claim 1 and a pharmaceutically acceptable excipient. 7. A method of inhibiting an androgen receptor, comprising contacting the androgen receptor with the compound of claim 1 . 8. A method of inducing degradation of an androgen receptor, comprising contacting the androgen receptor with the compound of claim 1 . 9. A method of treating a mammal suffering from prostate cancer, comprising administering the compound of claim 1 to a mammal in need thereof.
having one double bond between ring members or between a ring member and a non-ring member · CPC title
and containing six-membered aromatic rings · CPC title
the carbon skeleton containing rings · CPC title
Polycyclic · CPC title
to an acyclic saturated chain · CPC title
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