Vitamin d derivative crystals or its solvate crystals

New vitamin D derivative crystals address the limitations of existing derivatives by enhancing cerebral accumulation and myelin regeneration, effectively treating demyelinating diseases and neurodegenerative conditions.

RU2864758C2Active Publication Date: 2026-06-29TEIJIN PHARMA CO LTD
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Patent Information

Application Number
RU2024126638
Authority / Receiving Office
RU · RU
Patent Type
Patents
Current Assignee / Owner
Priority Date
2022-03-11
Filing Date
2023-03-10
Publication Date
2026-06-29
Estimated Expiration
2043-03-10

AI Technical Summary

Technical Problem

Current vitamin D derivatives, such as 1α,25-dihydroxyvitamin D3, face challenges in achieving sufficient cerebral accumulation and myelin regeneration without elevating blood calcium levels, necessitating a derivative with improved brain targeting and myelin regeneration effects independent of calcium metabolism.

Method used

Development of new vitamin D derivative crystals with specific structures that promote oligodendrocyte differentiation, offering enhanced cerebral accumulation and myelin regeneration capabilities.

Benefits of technology

The new crystals effectively induce oligodendrocyte differentiation and can be used to treat conditions like multiple sclerosis, Alzheimer's-type dementia, and cerebral infarction, providing a stable and effective pharmaceutical agent for remyelination.

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Abstract

FIELD: pharmaceutical industry.SUBSTANCE: invention relates to a crystal of a vitamin D derivative, wherein the vitamin D derivative is (1R,3R)-5-(2-((1R,3aS,7aR,E)-1-((S)-1-((S)-3-(difluoromethyl)pyrrolidin-1-yl)propan-2-yl)-7a-methyloctahydro-4H-inden-4-ylidene)ethylidene)cyclohexane-1,3-diol, and the powder X-ray diffraction spectrum of the crystal has peaks at diffraction angles of (2-theta±0.2°) = 14.2°, 16.3°, 17.9° and 18.5°. The invention relates to a crystal of a vitamin D derivative, wherein the vitamin D derivative is (1R,3R)-5-(2-((1R,3aS,7aR,E)-1-((S)-1-((R)-3-(difluoromethyl)pyrrolidin-1-yl)propan-2-yl)-7a-methyloctahydro-4H-inden-4-ylidene)ethylidene)cyclohexane-1,3-diol, and the powder X-ray diffraction spectrum of the crystal has peaks at diffraction angles of (2-theta±0.2°) = 14.2°, 16.2°, 17.9°, 18.5° and 24.3°. The invention relates to a crystal of a vitamin D derivative, wherein the vitamin D derivative is (1R,3R)-5-(2-((1R,3aS,7aR,E)-1-((S)-1-((R)-3-(1,1-difluoroethyl)pyrrolidin-1-yl)propan-2-yl)-7a-methyloctahydro-4H-inden-4-ylidene)ethylidene)cyclohexane-1,3-diol, and the powder X-ray diffraction spectrum has peaks at diffraction angles of (2-theta±0.2°) = 14.1°, 15.2°, 15.8°, 16.6° and 18.8°. The invention relates to a crystal of a vitamin D derivative, wherein the vitamin D derivative is (1R,3R)-5-(2-((1R,3aS,7aR,E)-1-((S)-1-((S)-3-(2,2-difluoroethyl)pyrrolidin-1-yl)propan-2-yl)-7a-methyloctahydro-4H-inden-4-ylidene)ethylidene)cyclohexane-1,3-diol, and the powder X-ray diffraction spectrum has peaks at diffraction angles of (2-theta±0.2°) = 14.6°, 16.2°, 16.5° and 18.3°. The invention relates to a crystal of a vitamin D derivative, wherein the vitamin D derivative is (1R,3R)-5-(2-((1R,3aS,7aR,E)-7a-methyl-1-((R)-4-morpholinobutan-2-yl)octahydro-4H-inden-4-ylidene)ethylidene)cyclohexane-1,3-diol, and the powder X-ray diffraction spectrum has peaks at diffraction angles of (2-theta±0.2°) = 13.5°, 16.4°, 18.1° and 20.3°. The invention relates to a crystal of a vitamin D derivative, wherein the vitamin D derivative is (1R,3R)-5-(2-((1R,3aS,7aR,E)-1-((S)-1-(3,3-dimethylmorpholino)propan-2-yl)-7a-methyloctahydro-4H-inden-4-ylidene)ethylidene)cyclohexane-1,3-diol, and the powder X-ray diffraction spectrum has peaks at diffraction angles of (2-theta±0.2°) = 16.1°, 16.4° and 17.3°. The invention also relates to a pharmaceutical composition for stimulating the induction of differentiation from oligodendrocyte precursors into oligodendrocytes, and a medicinal product for stimulating remyelination, containing the crystal according to the invention as an active ingredient.EFFECT: crystals of vitamin D derivatives that have excellent effects in stimulating the induction of differentiation into oligodendrocytes.39 cl, 12 dwg, 3 tbl, 8 ex
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Citation Information

Patent Citations

  • Vitamin d analogs, method for their obtaining, pharmaceutical composition

    RU2183622C2