Polycyclic Cbl-b Inhibitor for Autoimmune and Cancer Treatment

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Solution Overview

Problem

Current treatments for diseases mediated by Cbl-b, such as autoimmune diseases and cancers, are limited in efficacy and specificity, highlighting the need for targeted therapeutic agents.

Innovation Solution

Development of a polycyclic compound that acts as a Cbl-b inhibitor, including stereoisomers and pharmaceutically acceptable salts, which can be used in pharmaceutical compositions to treat or prevent Cbl-b mediated diseases.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional treatments are used for Cbl-b mediated diseases, then treatment options are available, but efficacy and specificity are limited

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidtreatment specificity
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent modifies molecular parameters of the compound structure (formula I) to optimize binding affinity and selectivity for Cbl-b, thereby improving both efficacy and specificity simultaneously through structural parameter optimization

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention creates a composite therapeutic approach by combining the polycyclic compound with pharmaceutical compositions and formulation excipients, achieving enhanced therapeutic efficacy while maintaining specificity through controlled drug delivery systems

Inventive Principle:
Principle #40Composite materials

2Adaptability or versatility

If targeted therapeutic agents are developed, then treatment specificity improves, but development complexity increases

Engineering Contradiction:
Improvetreatment specificityVSAvoidcompound structure complexity
Core Design Contradiction:
Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The patent divides the complex polycyclic compound into distinct structural modules (formula I with defined substituents R1-R6, rings A-F, and linkers L1-L3), allowing systematic design and synthesis while maintaining high specificity for Cbl-b

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention introduces specific functional groups and substituents at particular locations within the polycyclic structure to enhance binding affinity at the Cbl-b target site, achieving localized optimization without compromising overall molecular stability

Inventive Principle:
Principle #3Local quality

Data Source

PatentUS20250042896A1Polycyclic compound as CBL-b inhibitor
Publication Date: 2025.02.06 SIMCERE ZAIMING PHARMACEUTICAL CO LTD
  • US20250042896A1 patent drawing
  • US20250042896A1 patent drawing
  • US20250042896A1 patent drawing

AI summary

The present application describes a polycyclic compound represented by general formula (I) as a Cbl-b inhibitor, or a stereoisomer or pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the compound of general formula (I) or the stereoisomer or pharmaceutically acceptable salt thereof, and a use of the compound of general formula (I) or the stereoisomer or pharmaceutically acceptable salt thereof, or the pharmaceutical composition in the prevention or treatment of diseases or conditions mediated by Cbl-b.