FAK Inhibitor Tartrate Crystal Form for Stability and Solubility

Solution Overview

Problem

Existing formulations of the FAK inhibitor compound of formula (I) lack desirable properties such as crystallinity, stability, and solubility, which hinder their druggability and effectiveness in treating various cancers.

Innovation Solution

Development of a crystalline form I of the tartrate salt of the compound of formula (I), characterized by specific X-ray powder diffraction peaks, which enhances crystallinity, stability, and solubility.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing formulations of the FAK inhibitor compound are used, then the compound can be prepared, but the formulations lack desirable crystallinity, stability, and solubility properties

Engineering Contradiction:

ImprovestabilityVSAvoidcrystallinity

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

The patent applies parameter changes by converting the compound into different salt forms (tartrate salt, sulfate salt, phosphate salt, maleate salt, citrate salt, lactate salt, benzenesulfonate salt, 2-hydroxyethanesulfonate salt, benzoate salt, p-toluenesulfonate salt, hydrobromide salt) to improve crystallinity, stability, and solubility properties while maintaining the FAK inhibitory activity

Inventive Principle:

Principle #35Parameter changes

2Reliability

If existing formulations of the FAK inhibitor compound are used, then the compound can be prepared, but the formulations lack desirable crystallinity, stability, and solubility properties

Engineering Contradiction:

ImprovesolubilityVSAvoidcrystallinity

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

The patent applies parameter changes by converting the compound into different salt forms (tartrate salt, sulfate salt, phosphate salt, maleate salt, citrate salt, lactate salt, benzenesulfonate salt, 2-hydroxyethanesulfonate salt, benzoate salt, p-toluenesulfonate salt, hydrobromide salt) to improve crystallinity, stability, and solubility properties while maintaining the FAK inhibitory activity

Inventive Principle:

Principle #35Parameter changes

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The crystalline form I of the tartrate salt improves the compound's stability and solubility, making it more effective as a FAK inhibitor for treating a range of cancers, including non-small cell lung cancer, small cell lung cancer, colorectal cancer, pancreatic cancer, leukemia, bladder cancer, cervical cancer, bile duct cancer, esophageal cancer, gastric cancer, glioblastoma, liver cancer, melanoma, mesothelioma, ovarian cancer, prostate cancer, kidney cancer, sarcoma, thyroid cancer, testicular cancer, thymoma, and uterine cancer.

Implementation Method 1

characterized by X-ray powder diffraction (XRPD) including peaks at 10.34, 17.981, 18.281 and 21.901 degrees 2θ

Methodology Applied

Scientific EffectX-ray powder diffraction: X-Ray

Implementation Method 2

characterized by X-ray powder diffraction (XRPD) including peaks at 10.34, 17.981, 18.281 and 21.901 degrees 2θ

Methodology Applied

Scientific EffectDiffraction: Diffraction

Data Source

PatentEP4190774B1Solid form of compound

Publication Date: 2025.10.01 INXMED (NANJING) CO LTD

Figure 1~2b
Figure 3~4a
Figure 4b~4c

AI summary

Provided is a solid form of a compound of formula (I) or a salt thereof, or a solvate thereof, or a solvate of a salt thereof, or a mixture thereof.