7-Atom Nitrogenated Ring PARP Inhibitors

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Solution Overview

Problem

Current PARP inhibitors do not include compounds with a nitrogenated ring containing 7 atoms, and there is a lack of evidence on how modifying a 6-ring to a 7-ring in fused tri-heterocycles affects anti-cancer properties.

Innovation Solution

Development of compounds that inhibit poly(ADP-ribose) polymerase activity, specifically those with a 7-atom nitrogenated ring in a fused tri-heterocyclic structure, which are administered therapeutically to treat cancer and other diseases by inhibiting PARP activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If compounds with 6-atom nitrogenated rings are used as PARP inhibitors, then anti-cancer activity is achieved, but structural diversity and potential for improved efficacy are limited

Engineering Contradiction:

Improvestructural diversityVSAvoidring structure complexity

Core Design Contradiction:

Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The patent applies parameter changes by modifying the ring structure parameter from 6-atom to 7-atom nitrogenated rings in the fused tri-heterocyclic compounds. This structural parameter change creates new chemical space while maintaining the core PARP inhibition mechanism, thereby increasing structural diversity without fundamentally changing the molecular class or complexity level.

Inventive Principle:

Principle #35Parameter changes

2Adaptability or versatility

If new 7-atom nitrogenated ring compounds are developed, then potential anti-cancer properties are expanded, but lack of precedent and optimization data exists

Engineering Contradiction:

Improvetherapeutic application rangeVSAvoidefficacy predictability

Core Design Contradiction:

Adaptability or versatilityVSReliability

Solution Approach 1:

The patent employs universality by designing 7-atom nitrogenated ring compounds that maintain the fundamental PARP inhibition function while exploring new therapeutic applications. The core mechanism remains reliable and predictable based on established PARP inhibitor science, while the structural modification enables potential expansion to different cancer types and treatment scenarios.

Inventive Principle:

Principle #6Universality (Multi-functionality)

Data Source

PatentEP2114948B1Inhibitors of poly(ADP-ribose)polymerase

Publication Date: 2014.06.25 ABBVIE INC

AI summary

Inhibitors of poly(ADP-ribose)polymerase, ways to make them and methods of treating patients using them are disclosed.