Formula I Compounds Inducing Apoptosis in Cancer Cells

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current cancer treatments often lack effective molecules that can induce apoptosis or arrest the cell cycle, particularly in cancer cells, leading to inadequate therapeutic outcomes for various types of cancer.

Innovation Solution

Compounds of Formula (I), their salts, isomers, and derivatives, such as esters, ethers, or amides, are used in compositions that induce apoptosis or cause arrest in the G2/M phase of the cell cycle, with concentrations ranging from 0.20% to 90% by weight, specifically targeting cancer cells like DU145 and PC-3 cells.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current cancer treatments are used, then treatment is provided, but they lack effective molecules that can induce apoptosis or arrest the cell cycle

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidability to induce apoptosis or cell cycle arrest
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent modifies the chemical structure of withanolide compounds by varying substituents at positions R1, R2, and R3 (H, hydroxyl, halogen, methyl, ethyl, methoxy, or ethoxy) to optimize biological activity. This structural parameter optimization enables the compounds to effectively induce apoptosis and arrest cell cycle at G2/M phase, directly resolving the deficiency of current cancer treatments lacking effective apoptotic-inducing molecules

Inventive Principle:
Principle #35Parameter changes

2Object-affected harmful factors

If compounds of Formula (I) are used at high concentrations, then cytotoxic activity against cancer cells is enhanced, but the complexity of formulation and delivery increases

Engineering Contradiction:
Improvecytotoxic activity against cancer cellsVSAvoidformulation and delivery complexity
Core Design Contradiction:
Object-affected harmful factorsVSDevice complexity

Solution Approach 1:

The patent specifies optimal concentration ranges (0.20% to 90% by weight, with preferred ranges of at least 10.0%, 50.0%, or 90.0% by weight) to maximize cytotoxic activity while maintaining manageable formulation complexity. This parameter optimization allows high therapeutic efficacy without excessive formulation complexity

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates pharmaceutical compositions that combine compounds of Formula (I) with formulary ingredients and pyrogen-free water, forming composite materials that facilitate delivery while maintaining high cytotoxic activity. This composite approach enables effective cancer cell targeting without overwhelming formulation complexity

Inventive Principle:
Principle #40Composite materials

Data Source

PatentUS9492428B2Compounds, compositions, pharmaceutical compositions, and methods of use
Publication Date: 2016.11.15 UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION INC
  • US9492428B2 patent drawing
  • US9492428B2 patent drawing
  • US9492428B2 patent drawing

AI summary

Certain embodiments of the invention include compositions comprising a compound of Formula (I), and salts, isomers, and derivatives thereof. Pharmaceutical compositions of some embodiments of the present invention comprise a compound of Formula (I), and salts, isomers, and derivatives thereof. Other embodiments of this invention include methods for treating disease (e.g., cancer) and methods for administering a compound of Formula (I), and salts, isomers, and derivatives thereof.