Cyclic Amine Derivatives for Selective Lp(a) Reduction

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Solution Overview

Problem

Current treatments for cardiovascular diseases associated with elevated Lp(a) levels are inadequate in effectively reducing plasma Lp(a) levels and have significant side effects.

Innovation Solution

Development of cyclic amine derivatives with strong binding affinity for apo(a) to lower Lp(a) levels, formulated into pharmaceutical compositions with low toxicity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for cardiovascular diseases are used, then Lp(a) levels are reduced to some extent, but significant side effects occur and effectiveness is inadequate

Engineering Contradiction:

Improveeffectiveness of Lp(a) reductionVSAvoidside effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent modifies the chemical structure by changing parameters such as the cyclic amine core structure, substituent groups (aryl, heteroaryl, alkyl), and molecular configuration (R/S stereochemistry) to optimize the balance between Lp(a) binding affinity and safety profile, achieving effective Lp(a) reduction with lower toxicity

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The invention creates a composite molecular structure combining cyclic amine core with various aromatic and aliphatic substituent groups, forming a sophisticated molecule that achieves selective binding to apo(a) while minimizing off-target effects and toxicity

Inventive Principle:

Principle #40Composite materials

2Strength

If stronger binding affinity for apo(a) is achieved, then Lp(a) levels are more effectively reduced, but toxicity may increase

Engineering Contradiction:

Improvebinding affinity for apo(a)VSAvoidtoxicity

Core Design Contradiction:

StrengthVSObject-generated harmful factors

Solution Approach 1:

The patent introduces specific local structural features including particular substituent groups at defined positions on the cyclic amine core, and specific stereochemical configurations (R or S) at key carbon atoms, creating localized high-affinity binding regions that selectively interact with apo(a) without causing systemic toxicity

Inventive Principle:

Principle #3Local quality

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The cyclic amine derivatives effectively reduce Lp(a) levels, inhibiting LDL particle assembly with apo(a) and providing a therapeutic option for cardiovascular diseases with minimal side effects.

Implementation Method 1

the cyclic amine derivative or the pharmaceutically acceptable salt thereof has a strong binding affinity for apo(a)

Methodology Applied

Scientific EffectMolecular binding:

Data Source

PatentEP4692073A1Cyclic amine derivative, and composition and use thereof

Publication Date: 2026.02.11 SHANGHAI JINGXIN BIOLOGICAL MEDICAL

AI summary

The present invention relates to a cyclic amine derivative or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the cyclic amine derivative or the pharmaceutically acceptable salt thereof, and the use of the cyclic amine derivative or the pharmaceutically acceptable salt thereof or the composition thereof. The cyclic amine derivative of the present invention has a relatively strong capacity of binding to apo(a), can effectively reduce the level of Lp(a), and has low toxic side effects.