Aminoacetonitrile Anticancer Agent Reducing Toxicity

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Solution Overview

Problem

Current cancer treatments lack a medicament with clinically effective anticancer activity while minimizing severe side effects, necessitating the development of a safer and more potent anticancer agent.

Innovation Solution

An anticancer agent comprising an aminoacetonitrile compound or its pharmacologically acceptable salt, which exhibits cell growth inhibitory action and anticancer activity, is developed, with specific structural formulations to enhance efficacy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional cancer medicaments are used to achieve clinically effective anticancer activity, then cancer treatment efficacy is improved, but severe side effects occur

Engineering Contradiction:
Improveanticancer activityVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by systematically varying the chemical structure of aminoacetonitrile compounds (changing molecular parameters such as substituent groups R1-R6, m, and R) to optimize the balance between anticancer activity and side effects. This involves modifying chemical composition and molecular configuration to achieve therapeutic efficacy while reducing toxicity

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention utilizes composite material principles by creating specific aminoacetonitrile compound structures with multiple substituent groups and complex molecular arrangements (combining cyano group, amino group, and various aromatic/heterocyclic substituents) to achieve both high anticancer activity and reduced side effects

Inventive Principle:
Principle #40Composite materials

2Reliability

If existing cancer treatments are applied to achieve tumor growth control, then cancer progression is inhibited, but treatment safety deteriorates

Engineering Contradiction:
Improvetreatment efficacyVSAvoidtoxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by introducing specific substituent groups at particular positions (R1-R6) on the aminoacetonitrile core structure, where each position's substitution pattern is optimized to provide selective anticancer activity while minimizing systemic toxicity. Different regions of the molecule are tailored for specific functions

Inventive Principle:
Principle #3Local quality

3Productivity

If conventional chemotherapeutic agents are used to inhibit cell proliferation, then cancer cell growth is controlled, but therapeutic index deteriorates

Engineering Contradiction:
Improvecell growth inhibitionVSAvoidsafety profile
Core Design Contradiction:
ProductivityVSReliability

Solution Approach 1:

The patent applies segmentation by dividing the anticancer activity into distinct functional components: the aminoacetonitrile core provides the primary antiproliferative mechanism, while specific substituent groups (R1-R6) contribute to selective targeting and reduced off-target effects, thereby improving the therapeutic index

Inventive Principle:
Principle #1Segmentation

Data Source

PatentUS10292960B2Anticancer agent comprising aminoacetonitrile compound as active ingredient
Publication Date: 2019.05.21 PITNEY PHARMACUETICALS PTY LIMITED
  • US10292960B2 patent drawing
  • US10292960B2 patent drawing
  • US10292960B2 patent drawing

AI summary

The present invention relates to an anticancer agent having a high safety and a superior anticancer activity, and an anticancer agent containing, as an active ingredient, an aminoacetonitrile compound represented by the formula (I)wherein R1 is a hydrogen atom, an alkyl group and the like, R2, R3, and R4 are the same or different and each is a hydrogen atom, an alkyl group and the like, R5 and R6 are the same or different and each is a hydrogen atom, a halogen atom and the like, m is 0 or 1, R is a halogen atom, a cyano group, a nitro group, a phenyl group optionally substituted by an alkyl group and the like, an alkyl group and the like, Ar1 is a phenyl group, a naphthyl group, a pyridyl group, a pyrazolyl group, or the like, each of which is optionally substituted by a halogen atom, a cyano group, a nitro group, alkyl group and the like, and W is —O—, —S—, —SO2—, or —N(R7)— wherein R7 is a hydrogen atom, a (C1-C6) alkyl group and the like, or a pharmacologically acceptable salt thereof.