Stilbene Derivatives as AHR Regulators with Improved Photostability
Summary
The USPTO published patent application US20260091027A1 for stilbene derivatives serving as aryl hydrocarbon receptor (AHR) regulators with improved photostability over the marketed drug Benvitimod. The application, filed September 19, 2023 under Application No. 19113670, covers compounds of formula I-1, their stereoisomers, salts, and prodrugs, along with preparation methods for gram-to-kilogram scale synthesis.
What changed
USPTO published patent application US20260091027A1 disclosing stilbene derivatives of formula I-1 as AHR regulators. The claimed compounds demonstrate superior molecular structure stability under illumination compared to Benvitimod, overcoming that drug's photoinstability problem. The application covers stereoisomers, pharmaceutically acceptable salts, and prodrugs, along with a preparation method enabling gram-level or kilogram-level synthesis. CPC classifications span multiple compound families (A61K 31/44 through C07D 333/16) and target indications including cancer (A61P 35/00).
Patent applications do not impose compliance obligations on regulated entities. However, pharmaceutical companies and researchers developing AHR-targeted therapeutics should review this patent landscape to assess freedom-to-operate considerations. Drug developers working with stilbene compounds or AHR modulators may need to evaluate whether their research activities could infringe the claims once granted. No regulatory deadlines or penalties are associated with this patent publication.
Archived snapshot
Apr 3, 2026GovPing captured this document from the original source. If the source has since changed or been removed, this is the text as it existed at that time.
STILBENE DERIVATIVES AS WELL AS PREPARATION METHOD THEREFOR AND USE THEREOF
Application US20260091027A1 Kind: A1 Apr 02, 2026
Inventors
Yaxian CAI, Jianmin JIA, Zixing HAN, Kaiming CAI, Huanliang SUN, Mengjie TANG
Abstract
Stilbene derivatives, a preparation method therefor and the use thereof are provided. Compounds of formula (I-1), and stereoisomers, pharmaceutically acceptable salts or prodrugs thereof can serve as an aryl hydrocarbon receptor (AHR) regulator. Compared with marketed drug Benvitimod, the compounds of formula I-1 have greatly improved molecular structure stability under illumination, thus overcoming photoinstability of Benvitimod, and solving the problem of Benvitimod being liable to degrade under illumination. In addition, the compounds of formula I-1 have remarkably improved activity on AHR protein. And finally, the preparation method for the compounds of formula I-1 is simple, and can achieve gram-level or kilogram-level preparation.
CPC Classifications
A61K 31/44 A61K 31/055 A61K 31/381 A61K 31/4402 A61K 31/4406 A61K 31/4409 A61K 31/47 A61K 31/50 A61P 35/00 C07C 37/055 C07C 39/21 C07C 39/373 C07D 213/30 C07D 213/61 C07D 215/14 C07D 237/08 C07D 333/16
Filing Date
2023-09-19
Application No.
19113670
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