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JPWO2021159021A5
JPWO2021159021A5 JP2022547958A JP2022547958A JPWO2021159021A5 JP WO2021159021 A5 JPWO2021159021 A5 JP WO2021159021A5 JP 2022547958 A JP2022547958 A JP 2022547958A JP 2022547958 A JP2022547958 A JP 2022547958A JP WO2021159021 A5 JPWO2021159021 A5 JP WO2021159021A5
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dosage form
oral dosage
compound according
sedds
pharmaceutically acceptable
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Priority claimed from PCT/US2021/016955 external-priority patent/WO2021159021A1/en
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Claims (25)

式Ｉ－ｈの化合物Compounds of formula Ih
Figure 2021159021000001
Figure 2021159021000001
であって、式中、In the formula,
ＲR １1 及びＲand R ２2 が、各々、－Ｃ（Ｏ）Ｒare, respectively, -C(O)R ３3 であり、and
各ＲEach R ３3 が独立して、飽和または不飽和、直鎖または分岐状の、任意選択で置換されるＣare independently saturated or unsaturated, linear or branched, optionally substituted C １－３７1-37 炭化水素鎖であり、is a hydrocarbon chain,
各ＲEach R ４4 が独立して、水素またはＣare independently hydrogen or C １－６1-6 脂肪族基であり、is an aliphatic group,
－Ｍ－が、自壊性基であり、-M- is a self-destructive group,
Figure 2021159021000002
Figure 2021159021000002
が、but,
Figure 2021159021000003
Figure 2021159021000003
であり、式中、波線が－Ｍ－への結合点を指す、前記化合物。wherein the wavy line indicates the point of attachment to -M-.
Figure 2021159021000004
Figure 2021159021000004
が、but,
Figure 2021159021000005
Figure 2021159021000005
である、請求項１に記載の化合物。The compound according to claim 1, which is
Figure 2021159021000006
Figure 2021159021000006
が、but,
Figure 2021159021000007
Figure 2021159021000007
である、請求項１に記載の化合物。The compound according to claim 1, which is －Ｍ－が、-M- is,
Figure 2021159021000008
Figure 2021159021000008
である、請求項１～３のいずれか１項に記載の化合物。The compound according to any one of claims 1 to 3, which is －Ｍ－が-M- is
Figure 2021159021000009
Figure 2021159021000009
である、請求項４に記載の化合物。5. The compound according to claim 4. 各ＲEach R ３3 が独立して、飽和または不飽和の非分岐状Ｃare independently saturated or unsaturated unbranched C ２－３７2-37 炭化水素鎖である、請求項１～５のいずれか１項に記載の化合物。Compound according to any one of claims 1 to 5, which is a hydrocarbon chain. 各ＲEach R ３3 が、飽和の非分岐状Ｃis a saturated unbranched C ７7 炭化水素鎖である、請求項１～６のいずれか１項に記載の化合物。Compound according to any one of claims 1 to 6, which is a hydrocarbon chain. ＲR ４4 の少なくとも１つの出現例が、水素ではない、請求項１～７のいずれか１項に記載の化合物。8. A compound according to any one of claims 1 to 7, wherein at least one occurrence of is not hydrogen. ＲR ４4 の少なくとも１つの出現例が、ＣAt least one occurrence of C １－４1-4 脂肪族基である、請求項１～８のいずれか１項に記載の化合物。A compound according to any one of claims 1 to 8, which is an aliphatic group. ＲR ４4 の少なくとも１つの出現例が、メチルである、請求項１～９のいずれか１項に記載の化合物。A compound according to any one of claims 1 to 9, wherein at least one occurrence of is methyl. （Ｏ）(O) ０－１0-1 が、不在である、請求項１～１０のいずれか１項に記載の化合物。A compound according to any one of claims 1 to 10, wherein is absent. 式Ｉ－４７の化合物。A compound of formula I-47.
Figure 2021159021000010
Figure 2021159021000010
 請求項１～１２のいずれか１項に記載の化合物と、薬学的に許容される賦形剤とを含む、薬学的に許容される組成物。A pharmaceutically acceptable composition comprising a compound according to any one of claims 1 to 12 and a pharmaceutically acceptable excipient. 前記組成物が、経口投与用に製剤化される、請求項１３に記載の薬学的に許容される組成物。14. The pharmaceutically acceptable composition of claim 13, wherein said composition is formulated for oral administration. 請求項１～１２のいずれか１項に記載の化合物、または請求項１３もしくは１４に記載の薬学的に許容される組成物を含む、経口剤形。An oral dosage form comprising a compound according to any one of claims 1 to 12 or a pharmaceutically acceptable composition according to claims 13 or 14. 脂質ベースのビヒクルをさらに含む、請求項１５に記載の経口剤形。16. The oral dosage form of claim 15, further comprising a lipid-based vehicle. 前記脂質ベースのビヒクルが、ゴマ油を含む、請求項１６に記載の経口剤形。17. The oral dosage form of claim 16, wherein the lipid-based vehicle comprises sesame oil. 前記脂質ベースのビヒクルが、実質的に非水性のビヒクルである、請求項１６または１７に記載の経口剤形。18. Oral dosage form according to claim 16 or 17, wherein the lipid-based vehicle is a substantially non-aqueous vehicle. 前記経口剤形が、自己乳化型薬物送達システム（ＳＥＤＤＳ）を含む、請求項１５に記載の経口剤形。16. The oral dosage form of claim 15, wherein the oral dosage form comprises a self-emulsifying drug delivery system (SEDDS). 前記ＳＥＤＤＳが、ゴマ油及び水溶性界面活性剤を含む、請求項１９に記載の経口剤形。20. The oral dosage form of claim 19, wherein the SEDDS comprises sesame oil and a water-soluble surfactant. 前記水溶性界面活性剤が、ポリオキシエチレンヒマシ油を含む、請求項２０に記載の経口剤形。21. The oral dosage form of claim 20, wherein the water-soluble surfactant comprises polyoxyethylene castor oil. 前記ポリオキシエチレンヒマシ油が、ポリオキシル４０水素添加ヒマシ油を含む、請求項２１に記載の経口剤形。22. The oral dosage form of claim 21, wherein the polyoxyethylene castor oil comprises polyoxyl 40 hydrogenated castor oil. 前記ＳＥＤＤＳが、８～４０個の炭素原子を有する脂肪酸鎖を有するグリセロールモノエステル及びジエステルをさらに含む、請求項１９～２２のいずれか１項に記載の経口剤形。Oral dosage form according to any one of claims 19 to 22, wherein the SEDDS further comprises glycerol monoesters and diesters with fatty acid chains having 8 to 40 carbon atoms. 前記ＳＥＤＤＳが、実質的に非水性である、請求項１９～２３のいずれか１項に記載の経口剤形。An oral dosage form according to any one of claims 19 to 23, wherein the SEDDS is substantially non-aqueous. 前記経口剤形が、カプセル剤である、請求項１５～２４のいずれか１項に記載の経口剤形。Oral dosage form according to any one of claims 15 to 24, wherein the oral dosage form is a capsule.
JP2022547958A 2020-02-05 2021-02-05 Lipid Prodrugs of Neurosteroids Pending JP2023514147A (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US202062970607P 2020-02-05 2020-02-05
US62/970,607 2020-02-05
US202063009533P 2020-04-14 2020-04-14
US63/009,533 2020-04-14
US202063070064P 2020-08-25 2020-08-25
US63/070,064 2020-08-25
PCT/US2021/016955 WO2021159021A1 (en) 2020-02-05 2021-02-05 Lipid prodrugs of neurosteroids

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JP2023514147A JP2023514147A (en) 2023-04-05
JPWO2021159021A5 true JPWO2021159021A5 (en) 2024-02-14

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EP (1) EP4100017A4 (en)
JP (1) JP2023514147A (en)
KR (1) KR20220149534A (en)
CN (1) CN115348864A (en)
AU (1) AU2021217172A1 (en)
CA (1) CA3166908A1 (en)
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