Naphthalene-Ring Small Molecules for Refractory Disease Therapy

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Solution Overview

Problem

Current treatments for various diseases such as premature ovarian failure, systemic lupus erythematosus, sarcopenia, liver injury, oligospermia, rheumatoid arthritis, cataract, Cushing syndrome, Hashimoto's thyroiditis, chronic obstructive pulmonary disease, tinnitus, age-related macular degeneration, retinal pigmentosa, multiple sclerosis, hypothyroidism, chronic atrophic gastritis, myocarditis, alopecia, primary aldosteronism, erectile dysfunction, periodontitis, cerebral stroke, epilepsy, melasma, vitiligo, β-thalassemia, lumbar disc herniation, and polycystic ovary syndrome lack efficacy and are often associated with significant side effects.

Innovation Solution

The use of naphthalene ring-based small-molecule compounds, or their pharmaceutically acceptable salts, stereoisomers, solvates, or prodrugs, for the prevention and treatment of these diseases, targeting specific conditions like reproductive system diseases, autoimmune diseases, skin inflammation, retinal inflammation, ocular degenerative diseases, muscular or skeletal degenerative diseases, neurological diseases, anemia, adrenal diseases, chronic gastritis, myocarditis, periodontitis, hypothyroidism, alopecia, liver injury, tinnitus, and chronic obstructive pulmonary disease.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If hormone replacement therapy is used for premature ovarian failure, then menopausal symptoms are relieved, but significant side effects occur and curative efficacy is limited

Engineering Contradiction:
Improvecurative efficacyVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the chemical structure parameters by using naphthalene ring-based small molecule compounds with specific molecular weight ranges (150-300 Daltons) and defined chemical formulas, aiming to achieve better therapeutic efficacy with reduced side effects compared to conventional hormone replacement therapy

Inventive Principle:
Principle #35Parameter changes

2Reliability

If hormone pulse therapy and immunosuppressant therapy are used for lupus nephritis, then immune suppression is achieved, but severe side effects and exacerbated renal damage occur

Engineering Contradiction:
Improveimmune suppression efficacyVSAvoidrenal damage
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent introduces naphthalene ring-based small molecule compounds as intermediary substances that can suppress immune responses in lupus nephritis without causing the severe side effects and renal damage associated with conventional immunosuppressants, acting as a mediator between immune control and renal protection

Inventive Principle:
Principle #24Intermediary (Mediator)

3Strength

If resistance exercise is used for sarcopenia, then muscle strength is improved, but no cure or symptomatic medication is available

Engineering Contradiction:
Improvemuscle strengthVSAvoiddrug availability
Core Design Contradiction:
StrengthVSEase of manufacture

Solution Approach 1:

The patent develops small molecule compounds that can be administered to patients with sarcopenia to supplement and enhance the effects of resistance exercise, providing a pharmacological intervention that works synergistically with physical therapy to improve muscle mass and strength

Inventive Principle:
Principle #25Self-service

4Reliability

If antiviral therapy is used for liver injury, then viral infection is treated, but the therapy is slow-acting

Engineering Contradiction:
Improveviral treatment efficacyVSAvoidtherapy speed
Core Design Contradiction:
ReliabilityVSSpeed

Solution Approach 1:

The patent employs naphthalene ring-based small molecule compounds that can be used in combination with antiviral therapy to provide preliminary protective effects on the liver, reducing inflammation and preventing further damage while the antiviral medication works to eliminate the viral infection

Inventive Principle:
Principle #10Preliminary action

Data Source

PatentEP4684780A1Use of small-molecule naphthalene-ring compound
Publication Date: 2026.01.28 HANGZHOU PHECDAMED CO LTD
  • EP4684780A1 patent drawingFigure 1~2
  • EP4684780A1 patent drawingFigure 3~4
  • EP4684780A1 patent drawingFigure 5~7

AI summary

The present application discloses uses of naphthalene ring-based small molecule compounds. In the present application, a compound of Formula I is first found exhibiting excellent therapeutic effects on various refractory diseases comprising reproductive system diseases, autoimmune diseases, skin diseases, eye diseases, muscular or skeletal degenerative diseases, neurological diseases, anemia, adrenal diseases, chronic gastritis, myocarditis, periodontitis, hypothyroidism, alopecia, liver injury, tinnitus, chronic obstructive pulmonary disease and the like. Therefore, the compound has significant application value in the prevention and treatment of the aforementioned diseases.