Use of an rxr agonist in treating her2+ cancers
US-2020390736-A1 · Dec 17, 2020 · US
Methods of using RARγ agonists for cancer treatment
US12115193B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-12115193-B2 |
| Application number | US-202318481547-A |
| Country | US |
| Kind code | B2 |
| Filing date | Oct 5, 2023 |
| Priority date | Nov 23, 2021 |
| Publication date | Oct 15, 2024 |
| Grant date | Oct 15, 2024 |
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- Title
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- Abstract
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Abstract
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The invention discloses novel RAR gamma selective agonists used in the treatment of cancer. The invention also discloses administration of RAR gamma selective agonists to mammals, including humans for the purpose of selectively activating RAR gamma receptor and treat cancer by way of activating tumor infiltrating lymphocytes.
First claim
Opening claim text (preview).
The invention claimed is: 1. A RARγ-selective agonist of the structure: or a pharmaceutically acceptable salt thereof, wherein R is H or C 1-6 alkyl; R 7 to R 12 are independently C 1-6 alkyl, a hydrogen atom, an alkoxy group, a halogen atom, a nitro group, a hydroxy group, OCF 3 , or COR 13 , wherein R 13 is C 1-6 alkyl or CF 3 ; Y is oxygen, sulfur, or NR 14 , wherein R 14 is C 1-6 alkyl; and the crossed double bond to the ═N—OH group indicates that stereochemistry is not specified. 2. The RARγ-selective agonist of claim 1 , wherein R is H, methyl, or ethyl. 3. The RARγ-selective agonist of claim 1 , wherein Y is O. 4. The RARγ-selective agonist of claim 1 , wherein the ═N—OH group is in the E configuration. 5. The RARγ-selective agonist of claim 1 , wherein the RARγ selective agonist is 4-((1E,3E)-3-(3-(tert-butyl)-2-ethyl-benzofuran-5-yl)-3-(hydroxyimino)prop-1-en-1-yl)-3-fluorobenzoic acid (GA1E), having the structure: or a pharmaceutically acceptable salt thereof. 6. The RARγ-selective agonist of claim 1 , wherein the RARγ selective agonist is 4-((1E,3Z)-3-(3-(tert-butyl)-2-ethyl=benzofuran-5-yl)-3-(hydroxyimino)prop-1-en-1-yl)-3-fluorobenzoic acid (GA1Z), having the structure: or a pharmaceutically acceptable salt thereof.
Assignees
Inventors
Classifications
having an amino group · CPC title
- A61K31/343Primary
condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone · CPC title
Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title
T-cells, e.g. tumour infiltrating lymphocytes [TIL] or regulatory T [Treg] cells; Lymphokine-activated killer [LAK] cells · CPC title
Cancer antigens · CPC title
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Frequently asked questions
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- What does patent US12115193B2 cover?
- The invention discloses novel RAR gamma selective agonists used in the treatment of cancer. The invention also discloses administration of RAR gamma selective agonists to mammals, including humans for the purpose of selectively activating RAR gamma receptor and treat cancer by way of activating tumor infiltrating lymphocytes.
- Who is the assignee on this patent?
- Io Therapeutics Inc
- What technology area does this patent fall under?
- Primary CPC classification A61K31/343. Mapped technology areas include Human Necessities.
- When was this patent published?
- Publication date Tue Oct 15 2024 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 3 related publications on this page (citations in our corpus or others sharing the same primary CPC).