JPWO2019191119A5 - - Google Patents

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Publication number
JPWO2019191119A5
JPWO2019191119A5 JP2020551901A JP2020551901A JPWO2019191119A5 JP WO2019191119 A5 JPWO2019191119 A5 JP WO2019191119A5 JP 2020551901 A JP2020551901 A JP 2020551901A JP 2020551901 A JP2020551901 A JP 2020551901A JP WO2019191119 A5 JPWO2019191119 A5 JP WO2019191119A5
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JP
Japan
Prior art keywords
polysaccharide
acetylated
syndrome
subject
pharmaceutical preparation
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
JP2020551901A
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Japanese (ja)
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JP2021519367A (en
Publication date
Application filed filed Critical
Priority claimed from PCT/US2019/024104 external-priority patent/WO2019191119A1/en
Publication of JP2021519367A publication Critical patent/JP2021519367A/en
Publication of JPWO2019191119A5 publication Critical patent/JPWO2019191119A5/ja
Pending legal-status Critical Current

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Claims (30)

アセチル化多糖を作製する方法であって:
a)多糖を提供する工程と;
b)前記多糖を1~90質量%の純度まで精製する工程と;
c)アセチル化剤を提供する工程と;
d)触媒を提供する工程と;
e)前記アセチル化剤及び触媒を多糖と混合し、それによってアセチル化多糖を製造する工程であって、このアセチル化が工程a)における多糖のアセチル化を超える工程と;
f)前記アセチル化多糖を精製する工程と
を含む、方法。
A method for making acetylated polysaccharides:
a) With the process of providing polysaccharides;
b) A step of purifying the polysaccharide to a purity of 1 to 90% by mass;
c) With the process of providing an acetylating agent;
d) With the process of providing the catalyst;
e) A step of mixing the acetylating agent and the catalyst with a polysaccharide to produce an acetylated polysaccharide, wherein this acetylation exceeds the acetylation of the polysaccharide in step a);
f) A method comprising the step of purifying the acetylated polysaccharide.
前記多糖が、粉末配合物である、請求項1に記載の方法。 The method according to claim 1, wherein the polysaccharide is a powder formulation. 前記多糖が、グルコマンナン、グルコガラクトマンナン、ガラクトマンナン、マンナン及びそのアセチル化形態を含む、請求項1に記載の方法。 The method of claim 1, wherein the polysaccharide comprises glucomannan, glucogalactomannan, galactomannan, mannan and an acetylated form thereof. 前記多糖が、ヒドロキシル基を含み、前記ヒドロキシル基をアセチル基で置換することができる、請求項1に記載の方法。 The method of claim 1, wherein the polysaccharide comprises a hydroxyl group and the hydroxyl group can be replaced with an acetyl group. 前記多糖が、マンノース部分を含む、請求項1に記載の方法。 The method of claim 1, wherein the polysaccharide comprises a mannose moiety. 前記マンノース部分が、ヒドロキシル基を含み、前記ヒドロキシル基をアセチル化することができる、請求項5に記載の方法。 The method of claim 5, wherein the mannose moiety comprises a hydroxyl group and the hydroxyl group can be acetylated. 前記アセチル化多糖が、マンノース部分のマンノースの2位、3位及び/又は6位においてアセチル基を含む、請求項6に記載の方法。 The method of claim 6, wherein the acetylated polysaccharide comprises an acetyl group at the 2-, 3- and / or 6-positions of the mannose portion of the mannose moiety. 前記アセチル化剤が、無水酢酸(CH3CO)2O、塩化アセチル、及び酢酸である、請求項1に記載の方法。 The method of claim 1, wherein the acetylating agent is acetic anhydride (CH 3 CO) 2 O, acetyl chloride, and acetic acid. 前記触媒が、ピリジン、水酸化ナトリウム、水酸化カリウム、炭酸ナトリウム、又は炭酸カリウム及び溶媒である、請求項1に記載の方法。 The method of claim 1, wherein the catalyst is pyridine, sodium hydroxide, potassium hydroxide, sodium carbonate, or potassium carbonate and a solvent. 工程b)の精製工程が、エタノール沈殿により実施される、請求項1に記載の方法。 The method according to claim 1, wherein the purification step of step b) is carried out by ethanol precipitation. 工程f)の精製工程が、透析法により実施される、請求項1に記載の方法。 The method according to claim 1, wherein the purification step of step f) is carried out by a dialysis method. 請求項1から11のいずれか一項に記載の方法から製造されたアセチル化多糖。 Acetylated polysaccharide produced by the method according to any one of claims 1 to 11. 1つのマンノース基当たり、少なくとも1つ、2つ、又は3つのアセチル基を含む、請求項12に記載のアセチル化多糖。 12. The acetylated polysaccharide according to claim 12, which comprises at least one, two, or three acetyl groups per mannose group. マンノース基を含む、請求項12に記載のアセチル化多糖。 The acetylated polysaccharide according to claim 12, which comprises a mannose group. 前記多糖が、グルコマンナン、グルコガラクトマンナン、ガラクトマンナン、マンナン及び/又はそのアセチル化形態を含む、請求項12に記載のアセチル化多糖。 The acetylated polysaccharide according to claim 12, wherein the polysaccharide comprises glucomannan, glucogalactomannan, galactomannan, mannan and / or an acetylated form thereof. 約1~約70キロダルトンの範囲の分子量を有する、請求項12に記載のアセチル化多糖。 The acetylated polysaccharide according to claim 12, which has a molecular weight in the range of about 1 to about 70 kilodaltons. 約18キロダルトン又は約29キロダルトンの分子量を有する、請求項12に記載のアセチル化多糖。 The acetylated polysaccharide according to claim 12, which has a molecular weight of about 18 kilodaltons or about 29 kilodaltons. 請求項1から11のいずれか一項に記載の方法により製造されたアセチル化多糖;及び
薬学的に許容される賦形剤
を含む、医薬製剤。
A pharmaceutical preparation comprising an acetylated polysaccharide produced by the method according to any one of claims 1 to 11 ; and a pharmaceutically acceptable excipient.
湿潤剤、pH緩衝剤、及び吸収増強調製物等の無毒性補助物質を更に含む、請求項18に記載の医薬製剤。 The pharmaceutical preparation according to claim 18, further comprising a non-toxic auxiliary substance such as a wetting agent, a pH buffering agent, and an absorption-enhancing preparation. 丸剤、錠剤、グミ剤、カプセル剤、薬用ドロップ又は液体剤である、請求項19に記載の医薬製剤。 The pharmaceutical preparation according to claim 19, which is a pill, a tablet, a gummy candy, a capsule, a medicated drop or a liquid. 対象における炎症応答を処置し、軽快するか、又は予防する方法において使用するための、請求項18に記載の医薬製剤。 28. The pharmaceutical formulation of claim 18, for use in a method of treating, ameliorating or preventing an inflammatory response in a subject. 前記対象が、免疫異常を患っている、請求項21に記載の医薬製剤The pharmaceutical preparation according to claim 21, wherein the subject suffers from an immune abnormality. 前記免疫異常が、全身性ループス、強皮症、溶血性貧血、血管炎、I型糖尿病、グレーブス病、関節リウマチ、多発性硬化症、グッドパスチャー症候群、ミオパチー、重症複合免疫不全症、ディジョージ症候群、高免疫グロブリンE症候群、分類不能型免疫不全症、慢性肉芽腫症、ウィスコット-アルドリッチ症候群、自己免疫性リンパ増殖症候群、高免疫IgM症候群、白血球粘着不全症、NF-κB必須修飾因子(NEMO)変異、選択的免疫グロブリンA欠損症、X連鎖無ガンマグロブリン血症、X連鎖リンパ増殖性疾患又は毛細血管拡張性運動失調症である、請求項22に記載の医薬製剤The immunodeficiencies include systemic lupus, rhinitis, hemolytic anemia, vasculitis, type I diabetes, Graves disease, rheumatoid arthritis, multiple sclerosis, good pasture syndrome, myopathy, severe complex immunodeficiency, and DiGeorge syndrome. , Hyperimmunoglobulin E syndrome, unclassifiable immunodeficiency, chronic granulomatosis, Wiskott-Aldrich syndrome, autoimmune lymphoproliferative syndrome, hyperimmunoglobulin syndrome, leukocyte adhesion deficiency, NF-κB essential modifier (NEMO) ) The pharmaceutical preparation according to claim 22 , which is a mutation, selective immunoglobulin A deficiency, X-chain agammaglobulinemia, X-chain lymphoproliferative disorder or ataxia-telangiectosis. 対象における免疫異常を処置する方法において使用するための、請求項18に記載の医薬製剤。 The pharmaceutical formulation of claim 18, for use in a method of treating an immune disorder in a subject . 前記免疫異常が、全身性ループス、強皮症、溶血性貧血、血管炎、I型糖尿病、グレーブス病、関節リウマチ、多発性硬化症、グッドパスチャー症候群、ミオパチー、重症複合免疫不全症、ディジョージ症候群、高免疫グロブリンE症候群、分類不能型免疫不全症、慢性肉芽腫症、ウィスコット-アルドリッチ症候群、自己免疫性リンパ増殖症候群、高免疫IgM症候群、白血球粘着不全症、NF-κB必須修飾因子(NEMO)変異、選択的免疫グロブリンA欠損症、X連鎖無ガンマグロブリン血症、X連鎖リンパ増殖性疾患又は毛細血管拡張性運動失調症である、請求項24に記載の医薬製剤The immunodeficiencies include systemic lupus, rhinitis, hemolytic anemia, vasculitis, type I diabetes, Graves disease, rheumatoid arthritis, multiple sclerosis, good pasture syndrome, myopathy, severe complex immunodeficiency, and DiGeorge syndrome. , Hyperimmunoglobulin E syndrome, unclassifiable immunodeficiency, chronic granulomatosis, Wiskott-Aldrich syndrome, autoimmune lymphoproliferative syndrome, hyperimmunoglobulin syndrome, leukocyte adhesion deficiency, NF-κB essential modifier (NEMO) ) The pharmaceutical preparation according to claim 24 , which is a mutation, selective immunoglobulin A deficiency, X-chain agammaglobulinemia, X-chain lymphoproliferative disorder or ataxia-telangiectosis. 対象における抗炎症性IL-10(インターロイキン10)の発現を増加させる方法において使用するための、請求項18に記載の医薬製剤。 The pharmaceutical formulation according to claim 18, for use in a method of increasing the expression of anti-inflammatory IL-10 (interleukin 10) in a subject . 対象における抗炎症性サイトカインの発現を高める方法において使用するための、請求項18に記載の医薬製剤。 The pharmaceutical preparation according to claim 18, for use in a method for enhancing the expression of anti-inflammatory cytokines in a subject . 対象における腫瘍を処置する方法において使用するための、請求項18に記載の医薬製剤。 The pharmaceutical formulation of claim 18, for use in a method of treating a tumor in a subject . 前記対象が、がんを患っており、前記腫瘍が、肺がん、皮膚がん、肝がん、脳がん、腎がん、又は子宮がんからのものである、請求項28に記載の医薬製剤28. The apparatus of claim 28 , wherein the subject suffers from cancer and the tumor is from lung cancer, skin cancer, liver cancer, brain cancer, kidney cancer, or uterine cancer . Formulation . 対象におけるウイルス感染又は細菌感染を処置する方法において使用するための、請求項18に記載の医薬製剤。 The pharmaceutical preparation according to claim 18, for use in a method of treating a viral or bacterial infection in a subject .
JP2020551901A 2018-03-28 2019-03-26 Acetylation of polysaccharides Pending JP2021519367A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862649344P 2018-03-28 2018-03-28
US62/649,344 2018-03-28
PCT/US2019/024104 WO2019191119A1 (en) 2018-03-28 2019-03-26 Acetylation of polysaccharides

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JP2021519367A JP2021519367A (en) 2021-08-10
JPWO2019191119A5 true JPWO2019191119A5 (en) 2022-04-05

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US (1) US11547719B2 (en)
EP (1) EP3773612A4 (en)
JP (1) JP2021519367A (en)
CN (1) CN112533614A (en)
MX (1) MX2020010036A (en)
RU (1) RU2020135495A (en)
WO (1) WO2019191119A1 (en)

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