CETZOLE Compounds for Selective NSCLC Treatment

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Solution Overview

Problem

Current treatments for lung cancer, particularly non-small cell lung carcinoma (NSCLC), have reached a therapeutic plateau with existing chemotherapy drugs, necessitating the development of new agents with different mechanisms of action to improve survival rates and treatment efficacy.

Innovation Solution

Development of compounds with a 4-cyclopentyenyl-2-ethynylthiazole skeleton and terminal alkyne at the 2-position of the thiazole ring, which are synthesized through specific chemical processes and administered as pharmaceutical compositions to target and kill cancer cells selectively, potentially through an iron-dependent mechanism not involving apoptosis.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current chemotherapy drugs and targeted therapies are used for lung cancer treatment, then treatment options are available, but five-year survival rates remain low at about 16%

Engineering Contradiction:

Improvesurvival rateVSAvoidtherapeutic mechanism diversity

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent introduces a novel chemical compound structure (Formula I) with specific molecular characteristics including a thiazole ring, cyclopentene group, and ethynyl substituent. This structural parameter change creates a new mechanism of action that differs from existing chemotherapy and targeted therapies, potentially overcoming the therapeutic plateau while aiming to improve survival rates through enhanced anti-cancer activity

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The invention combines multiple functional moieties into a single composite molecular structure: a thiazole core fused with a cyclopentene ring and substituted with an ethynyl group. This composite structure integrates different chemical features that work synergistically to achieve selective cytotoxicity against NSCLC cells through a mechanism distinct from current therapies

Inventive Principle:

Principle #40Composite materials

2Reliability

If new compounds with different mechanisms of action are developed, then treatment efficacy may improve, but drug development complexity and time increase

Engineering Contradiction:

Improvetreatment efficacyVSAvoiddrug development complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The patent presents a complete, ready-to-use chemical compound structure with defined molecular formula and characteristics. By providing the finalized active pharmaceutical ingredient rather than requiring development from scratch, the invention reduces the complexity and time associated with de novo drug development while maintaining the benefit of a novel mechanism of action for improved treatment efficacy

Inventive Principle:

Principle #10Preliminary action

Data Source

PatentUS10138216B2Highly selective anti-cancer agents targeting non-small cell lung cancer and other forms of cancer

Publication Date: 2018.11.27 UNIVERSITY OF TOLEDO

AI summary

Described herein are analogues of 2-methyl-3-(2-ethynylthiazol-4-yl)cyclopent-2-enol and the corresponding ketone 3-(2-ethynylthiazol-4-yl)-2-methylcyclopent-2-enone, the analogues having terminal alkyne groups at the 2-position of the thiazole ring. These drug-like molecules, referred to as CETZOLE compounds, are useful to treat non-small cell lung cancer and other forms of cancer. Methods of making and using the compounds, methods of treating various diseases, pharmaceutical compositions, and kits are also disclosed.