Cyclohexane Derivative for Multiple Sclerosis Treatment
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Solution Overview
Problem
Current treatments for multiple sclerosis, such as steroids and interferon β-1b/1a, have transient effects and are expensive, with limited efficacy for all patients, and existing low molecular weight thrombin inhibitors lack specific data on their pharmacological effect against multiple sclerosis.
Innovation Solution
A cyclohexane derivative or its pharmaceutically acceptable salt, represented by specific structural formulas, is used as a therapeutic or prophylactic agent, administered to mammals to effectively suppress the exacerbation of multiple sclerosis symptoms by inhibiting neurological symptom scores in experimental autoimmune encephalomyelitis models.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If steroids are used for treatment of multiple sclerosis, then acute-phase symptoms can be ameliorated, but the effect is transient and long-term treatment is difficult
Solution Approach 1:
The patent changes the chemical structure parameters by developing a novel cyclohexane derivative with specific molecular characteristics (Formula I with defined substituents A, R4-R8, Y, Z) to achieve both acute and long-term therapeutic effects, resolving the transient nature of steroid treatment
2Reliability
If interferon β-1b and interferon β-1a are used to prevent recurrence of multiple sclerosis, then recurrence can be prevented, but they are expensive and ineffective for some patients
Solution Approach 1:
The patent replaces expensive biological preparations (interferons) with a chemically synthesized cyclohexane derivative that can be manufactured more economically while maintaining therapeutic efficacy for preventing recurrence
Solution Approach 2:
The patent modifies the molecular parameters by designing a specific cyclohexane derivative structure (Formula I) with optimized substituents to achieve broad-spectrum effectiveness across different patient populations, addressing the limitation of interferon ineffectiveness in some patients
3Reliability
If low molecular weight thrombin inhibitor compounds are used, then thrombin inhibition activity is achieved, but there is no specific data on pharmacological effect against multiple sclerosis
Solution Approach 1:
The patent performs preliminary pharmacological evaluations in experimental autoimmune encephalomyelitis (EAE) models before clinical application, establishing proof of concept and pharmacological effectiveness data for the cyclohexane derivative in treating multiple sclerosis
Solution Approach 2:
The patent uses EAE animal models as intermediary systems to bridge the gap between in vitro thrombin inhibition data and clinical multiple sclerosis treatment outcomes, generating essential pharmacological effect data
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 cyclohexane derivative significantly suppresses the exacerbation of multiple sclerosis symptoms, providing effective treatment and prevention with a remarkable inhibitory effect on neurological symptom scores and thrombin activity, as demonstrated in various animal models.
Implementation Method 1
Multiple sclerosis shows enhancement of the coagulation system, and it is known that the symptoms can be ameliorated with a thrombin inhibitor hirudin in a disease model for multiple sclerosis
Data Source
AI summary
A method of treating or preventing multiple sclerosis includes administering a therapeutically effective amount of a cyclohexane derivative represented by Formula (I):wherein A is a substituent represented by Formula (IIa) or (IIb):R1 and R2 are each independently a hydrogen atom, chlorine atom, C1-C3 haloalkyl, C1-C4 alkyl, C1-C4 alkoxy, or cyano; R3 is a hydrogen atom or chlorine atom; R4 is a fluorine atom, hydroxymethyl, or hydroxyl; R5 and R6 are each independently a hydrogen atom, fluorine atom, C1-C3 haloalkyl, carboxyl, methoxycarbonyl, ethoxycarbonyl, C1-C4 alkoxy, hydroxyl, or C2-C5 alkylcarbonyloxy, or optionally together form oxo; R7 and R8 are each independently a hydrogen atom or fluorine atom; Y is an oxygen atom or sulfur atom; and Z is a nitrogen atom or methine or a pharmaceutically acceptable salt thereof to a mammal.