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
Patent Information
- Authority / Receiving Office
- RU · RU
- Patent Type
- Patents
- Current Assignee / Owner
- TEIJIN PHARMA CO LTD
- Filing Date
- 2023-03-10
- Publication Date
- 2026-06-29
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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