Enhanced Quinone-Containing Conjugates for Targeted Cancer Therapy
Legal Citation
Summary of the Inventive Concept
Improved quinone-containing conjugates with enhanced binding affinity, reduced side effects, and increased efficacy for targeted cancer treatment
Background and Problem Solved
The original patent described quinone-containing conjugates for cancer treatment, but faced limitations in terms of binding affinity, side effects, and efficacy. This new inventive concept addresses these limitations by introducing modified amino acid sequences, reduced dosages, and novel linkers, resulting in improved conjugates with enhanced targeting capabilities and reduced toxicity
Detailed Description of the Inventive Concept
The new conjugates feature a modified cell binding moiety (Cb) with improved binding affinity, achieved through the substitution of at least one amino acid residue with a non-natural amino acid. This modification enables the conjugate to selectively target and destroy tumor cells with increased precision. Additionally, the conjugate can be administered in reduced dosages, minimizing potential side effects while maintaining efficacy. The composition of the conjugate can be further enhanced by incorporating an additional therapeutic agent, such as a chemotherapeutic agent, to augment the treatment of proliferative disorders. Furthermore, the novel linker (L1b) comprising a hydrophilic polymer improves the conjugate's stability and pharmacokinetics. The method of preparation involves a novel solid-phase synthesis approach, reducing production time and costs while maintaining high yields and purity
Novelty and Inventive Step
The new claims introduce non-obvious modifications to the original quinone-containing conjugates, including the use of non-natural amino acids, reduced dosages, and novel linkers. These modifications result in improved conjugates with enhanced targeting capabilities, reduced toxicity, and increased efficacy
Alternative Embodiments and Variations
Alternative embodiments of the inventive concept could include the use of different non-natural amino acids, varying linker compositions, or alternative therapeutic agents. Additionally, the conjugates could be adapted for use in different cancer types or in combination with other treatment modalities
Potential Commercial Applications and Market
The enhanced quinone-containing conjugates have significant commercial potential in the cancer treatment market, with potential applications in targeted therapy, diagnostics, and personalized medicine. The market for cancer treatment is growing rapidly, driven by the need for more effective and targeted therapies
CPC Classifications
| Section | Class | Group |
|---|---|---|
| A | A61 | A61K47/6889 |
| A | A61 | A61K31/122 |
| A | A61 | A61K47/6891 |
| A | A61 | A61K49/0039 |
| A | A61 | A61K49/0043 |
| A | A61 | A61K49/0052 |
| C | C07 | C07D417/12 |
| C | C07 | C07K16/30 |
| G | G01 | G01N33/582 |
Section 103 Obviousness Analysis (PHOSITA)
Field of Art
Pharmaceutical biotechnology, specifically antibody-drug conjugates (ADCs) for cancer treatment, involving organic chemistry, protein engineering, and targeted therapeutic design
Person of Ordinary Skill (PHOSITA) Profile
A PhD-level researcher with expertise in medicinal chemistry, protein modification techniques, conjugation chemistry, and experience designing targeted therapeutic molecules with advanced knowledge of linker technologies and amino acid substitution strategies
Obviousness Rationale
A PHOSITA would recognize that the PTD's modifications represent predictable variations of the source patent's core ADC technology, utilizing standard protein engineering techniques and well-established strategies for improving targeted therapeutic molecules through amino acid substitution, linker optimization, and dosage refinement.
Obvious Combinations & Variations
Original Patent Information
| Patent Number | US 11,857,638 |
|---|---|
| Title | Quinone-containing conjugates |
| Assignee(s) | Promega Corporation |