Mta-cooperative prmt5 inhibitors

TWI940485BActive Publication Date: 2026-10-01MIRATI THERAPEUTICS INC
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Patent Information

Application Number
TW109131387
Authority / Receiving Office
TW · TW
Patent Type
Patents
Current Assignee / Owner
Priority Date
2020-08-03
Filing Date
2020-09-11
Publication Date
2026-10-01
Estimated Expiration
2040-09-10

AI Technical Summary

Technical Problem

There is a need for new MTA-synergistic PRMT5 inhibitors capable of inhibiting PRMT5 activity in the presence of higher MTA concentrations, particularly in MTAP-deficient cells, to provide therapeutic benefit for a broad range of cancers associated with MTAP deletions.

Method used

Development of compounds represented by formula (I) and their pharmaceutically acceptable salts, which negatively modulate PRMT5 activity in the presence of MTA, specifically designed to target MTAP-deficient cells.

Benefits of technology

These compounds effectively inhibit PRMT5 activity in MTAP-deficient cells, offering therapeutic benefits for various cancers by blocking cell proliferation and increasing sensitivity to PRMT5 depletion.

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Abstract

This invention relates to compounds that inhibit the activity of protein arginine N-methyltransferase 5 (PRMT5). Specifically, this invention relates to compounds, pharmaceutical compositions, and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of this invention.
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Description

Technical field

Prior Technology

Content of invention

Implementation

Claims

1. A compound or a pharmaceutically acceptable salt thereof, selected from:

1. Or a medically acceptable salt thereof.

2. The compound of claim 1 or its pharmaceutically acceptable salt, is:

2. Or a medically acceptable salt thereof.

3. The compound of claim 1 or its pharmaceutically acceptable salt, which is...

4. The compound of claim 1 or its pharmaceutically acceptable salt is a pharmaceutically acceptable salt of the following compound:

5. A pharmaceutical composition comprising a therapeutically effective amount of a compound of any one of claims 1 to 4 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient.

6. Use of a compound of any one of claims 1 to 4 or a pharmaceutically acceptable salt thereof or a pharmaceutical composition of claim 5, for the preparation of a pharmaceutical product that inhibits PRMT5 activity in cells.

7. Use of a compound of any one of claims 1 to 4, or a pharmaceutically acceptable salt thereof, alone or in combination with a pharmaceutically acceptable carrier or excipient, for the preparation of a pharmaceutical product for treating MTAP-related cancers.

8. As requested in paragraph 7, wherein the cancer is selected from the group consisting of: heart cancer, lung cancer, gastrointestinal cancer, genitourinary tract cancer, liver cancer, biliary tract cancer, bone cancer, nervous system cancer, gynecological cancer, hematological cancer, skin cancer, and adrenal cancer.

9. As requested in paragraph 7 or 8, wherein the cancer is hepatocellular carcinoma, breast cancer, skin cancer, bladder cancer, liver cancer, pancreatic cancer, or head and neck cancer.

Citation Information

Patent Citations

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    WO2002006285A1