Enhanced 4-[[(7-aminopyrazolo[1,5-a]pyrimidin-5-yl)amino]methyl]piperidin-3-ol Compounds and Systems for CDK-Mediated Diseases

Publication ID: 24-11857552_0001_PTD
Published: October 28, 2025
Category:Direct Improvements & Enhancements

Legal Citation

pr1or.art Inc., “Enhanced 4-[[(7-aminopyrazolo[1,5-a]pyrimidin-5-yl)amino]methyl]piperidin-3-ol Compounds and Systems for CDK-Mediated Diseases,” Published Technical Disclosure No. 24-11857552_0001_PTD, Published October 28, 2025, available at https://archive.pr1or.art/24-11857552_0001_PTD
This technical disclosure describes improvements that would be readily apparent to a Person Having Ordinary Skill In The Art (PHOSITA) when considered in combination with the foundational architecture disclosed in U.S. Patent No. 11,857,552.

Summary of the Inventive Concept

The inventive concept presents a suite of direct improvements and enhancements to the original CDK inhibitor compounds, focusing on improved solubility, bioavailability, and synthesis efficiency, as well as novel pharmaceutical compositions and crystalline forms, to provide more effective and efficient treatments for CDK-mediated diseases.

Background and Problem Solved

The original patent disclosed CDK inhibitor compounds with limited solubility and bioavailability, resulting in reduced efficacy and increased side effects. The inventive concept addresses these limitations by introducing novel formulations, synthesis methods, and crystalline forms that enhance the compounds' properties, providing better treatment options for patients.

Detailed Description of the Inventive Concept

The inventive concept comprises five key aspects: (1) a system for treating CDK-mediated diseases with improved solubility and bioavailability compounds; (2) a method for synthesizing these compounds using novel catalysts to enhance reaction yields and reduce impurities; (3) pharmaceutical compositions with sustained release properties; (4) a process for preparing substantially purified compounds through crystallization, recrystallization, and chromatography; and (5) novel crystalline forms with improved stability and shelf life. These enhancements collectively provide more effective and efficient treatments for CDK-mediated diseases.

Novelty and Inventive Step

The inventive concept's novelty lies in the combination of improved solubility, bioavailability, and synthesis efficiency, as well as the introduction of novel pharmaceutical compositions and crystalline forms. The inventive step is the recognition of the need to address the original patent's limitations and the development of these direct improvements and enhancements.

Alternative Embodiments and Variations

Alternative embodiments may include the use of different solvents or excipients in the pharmaceutical compositions, variations in the synthesis methods, or alternative crystalline forms. These variations can provide additional flexibility in the development and commercialization of the inventive concept.

Potential Commercial Applications and Market

The inventive concept has significant commercial potential in the pharmaceutical industry, particularly in the treatment of CDK-mediated diseases such as cancer. The improved compounds and systems can provide more effective and efficient treatments, resulting in improved patient outcomes and reduced healthcare costs.

Original Patent Information

Patent NumberUS 11,857,552
Title4-[[(7-aminopyrazolo[1,5-a]pyrimidin-5-yl)amino]methyl]piperidin-3-ol compounds as CDK inhibitors
Assignee(s)CARRICK THERAPEUTICS LIMITED