Cyclic Amide Modulators for TNF-α and Interleukin Regulation

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Solution Overview

Problem

Current approaches to regulate the production of TNF-α and interleukins are limited, and there is a need for novel compounds that can modulate these biological molecules to treat conditions such as cancer, cardiovascular disease, and immune disorders effectively.

Innovation Solution

Development of synthetic and semi-synthetic compounds, including cyclic amide-containing compounds and their analogs, which can modulate TNF-α and interleukin production, and their use in pharmaceutical compositions for treating inflammatory, autoimmune, and cancer-related conditions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional approaches to regulate TNF-α and interleukin production are used, then existing treatments can be maintained, but the treatment effectiveness and specificity are limited

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidtreatment specificity
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent modifies the chemical structure of natural products by changing molecular parameters - specifically introducing cyclic amide groups at defined positions in the分子 structure. This structural parameter change enables the compounds to selectively modulate TNF-α and interleukin production with enhanced treatment effectiveness and specificity for various diseases

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention creates composite molecular structures by combining natural product frameworks with cyclic amide moieties. These composite compounds integrate the biological activity of natural products with the regulatory properties of cyclic amides, achieving both effectiveness and specificity in modulating inflammatory and immune responses

Inventive Principle:
Principle #40Composite materials

2Reliability

If natural products are used as starting materials, then the compounds have biological activity, but the synthesis complexity increases

Engineering Contradiction:
Improvebiological activityVSAvoidsynthesis complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent performs preliminary synthesis of the cyclic amide-containing compounds from natural product starting materials before final formulation. By preparing the core structured compounds in advance through controlled chemical transformations, the invention reduces the overall synthesis complexity while maintaining the biological activity derived from natural products

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The invention uses cyclic amide groups as intermediary structural elements that bridge the natural product framework and the desired biological activity. These intermediary groups facilitate the synthesis process by providing stable, easily installable functional units that lead to the active compounds

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentUS8133915B2Interleukin-1 and tumor necrosis factor-α modulators; syntheses of such modulators and methods of using such modulators
Publication Date: 2012.03.13 BEYONDSPRING INC
  • US8133915B2 patent drawing
  • US8133915B2 patent drawing
  • US8133915B2 patent drawing

AI summary

Described herein are chemical compounds and pharmaceutical compositions, including novel chemical compounds and pharmaceutical compositions thereof, useful in the treatment of various diseases and disease states. Also described are methods of synthesizing natural products and novel, structurally-related chemical compounds. More particularly, disclosed are new analogs of and processes for the preparation of compounds and pharmaceutical compositions thereof useful in the treatment of, for example, inflammation, cancer, multiple myeloma, cachexia, cardiovascular disease, anti-infectious, diabetes, otitis media, sinusitis and transplant rejection.