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Proteolysis targeting chimeric molecule, preparation method, and application
US11504385B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-11504385-B2 |
| Application number | US-201915734960-A |
| Country | US |
| Kind code | B2 |
| Filing date | Sep 4, 2019 |
| Priority date | Jan 26, 2019 |
| Publication date | Nov 22, 2022 |
| Grant date | Nov 22, 2022 |
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- Title
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- Abstract
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Abstract
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It discloses a proteolysis targeting chimeric molecule, a preparation method and an application thereof. The proteolysis targeting chimeric molecule provided by the disclosure can inhibit the expression of BCR-ABL and/or CRBN protein in BCR-ABL and/or CRBN positive leukemia K562 cells to varying degrees, and thus can be used to prepare drugs for treating BCR-ABL and/or CRBN positive leukemia, wherein the proteolysis targeting chimeric molecule with n=3 has excellent photo-isomerization activity, and can be used in preparation of the reagents or drugs for light-regulated degradation of BCR-ABL and/or CRBN protein. The disclosure also provides a method for synthesizing the series of proteolysis targeting chimeric molecules.
First claim
Opening claim text (preview).
What is claimed is: 1. A compound of formula as shown as following: wherein n is an integer from 1 to −5. 2. Thecompound according to claim 1 , wherein n=3. 3. A process for synthesizing the compound of claim 1 comprising chemical reactions as the following: wherein n is the integer between 1 and −5. 4. A method for treating a leukemia comprising a step of administrating an effective amount of the compound of claim 1 to a subject in need of treatment; wherein the leukemia is a BCR-ABL positive or/and a CRBN positive leukemia. 5. The method according to claim 4 , wherein the compound degrades BCR-ABL and CRBN proteins.
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Classifications
containing three or more hetero rings · CPC title
the modifying agent being an organic compound · CPC title
specific for leukemia · CPC title
the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug · CPC title
- A61K31/655Primary
Azo (—N=N—), diazo (=N2), azoxy (>N—O—N< or N(=O)—N<), azido (—N3) or diazoamino (—N=N—N<) compounds · CPC title
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- What does patent US11504385B2 cover?
- It discloses a proteolysis targeting chimeric molecule, a preparation method and an application thereof. The proteolysis targeting chimeric molecule provided by the disclosure can inhibit the expression of BCR-ABL and/or CRBN protein in BCR-ABL and/or CRBN positive leukemia K562 cells to varying degrees, and thus can be used to prepare drugs for treating BCR-ABL and/or CRBN positive leukemia, w…
- Who is the assignee on this patent?
- Univ China Pharma
- What technology area does this patent fall under?
- Primary CPC classification A61K31/655. Mapped technology areas include Human Necessities.
- When was this patent published?
- Publication date Tue Nov 22 2022 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).