Piperidine-Substituted Indoles for CCR-3 Modulation
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Solution Overview
Problem
Current agents for modulating chemokine receptor CCR-3 have significant side effects, limiting their effectiveness in treating inflammatory, infectious, and autoimmune disorders such as asthma and rheumatoid arthritis.
Innovation Solution
Development of piperidine-substituted indole compounds that act as CCR-3 modulators with reduced side effects, specifically designed to target and regulate chemokine receptor activity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current agents for modulating chemokine receptor CCR-3 are used, then chemokine receptor activity is modulated, but significant side effects occur
Solution Approach 1:
The patent modifies the chemical structure of CCR-3 modulating agents by changing molecular parameters - specifically incorporating piperidine rings at the 3-position of indole compounds. This structural parameter change results in improved pharmacological properties with reduced side effects while maintaining CCR-3 modulation efficacy.
Solution Approach 2:
The invention creates composite molecular structures by combining indole core compounds with piperidine substituent groups. This composite approach allows the molecule to integrate the beneficial properties of both structural elements, achieving effective CCR-3 modulation with improved safety profile.
2Reliability
If existing CCR-3 modulating agents are administered, then inflammatory disorders are treated, but effectiveness is limited due to side effects
Solution Approach 1:
The patent systematically modifies molecular parameters of existing CCR-3 modulators by introducing piperidine substituents at specific positions (3-position) of indole compounds. This parameter modification optimizes the drug's pharmacological profile, enhancing therapeutic effectiveness while minimizing adverse effects.
Solution Approach 2:
The invention creates novel compounds that are structural analogs or copies of existing CCR-3 modulating agents, but with improved molecular architecture. The piperidine-substituted indole compounds replicate the functional activity of parent compounds while incorporating structural improvements that reduce side effects.
Data Source
AI summary
Disclosed are novel piperidine-substituted indoles- or heteroderivatives thereof of the formula 1:wherein R1, R5, R6, R7, A, B, D-E, Y, i, j, n and m are defined as below.The compounds of formula 1 are useful as agonists or antagonists of CCR-3. The present invention is also directed to pharmaceutically acceptable salts thereof, more particularly to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.