JP7425855B2 - エキセナチド類似体及びその用途 - Google Patents
エキセナチド類似体及びその用途 Download PDFInfo
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- JP7425855B2 JP7425855B2 JP2022509115A JP2022509115A JP7425855B2 JP 7425855 B2 JP7425855 B2 JP 7425855B2 JP 2022509115 A JP2022509115 A JP 2022509115A JP 2022509115 A JP2022509115 A JP 2022509115A JP 7425855 B2 JP7425855 B2 JP 7425855B2
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/22—Hormones
- A61K38/26—Glucagons
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/575—Hormones
- C07K14/605—Glucagons
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L29/00—Foods or foodstuffs containing additives; Preparation or treatment thereof
- A23L29/20—Foods or foodstuffs containing additives; Preparation or treatment thereof containing gelling or thickening agents
- A23L29/275—Foods or foodstuffs containing additives; Preparation or treatment thereof containing gelling or thickening agents of animal origin, e.g. chitin
- A23L29/281—Proteins, e.g. gelatin or collagen
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/17—Amino acids, peptides or proteins
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2319/00—Fusion polypeptide
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- General Health & Medical Sciences (AREA)
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Description
Claims (6)
- エキセナチドのアミノ酸配列のC末端の7~9個のアミノ酸が欠失し、カプリン酸が接合したエキセナチド類似体から形成される第1の単量体;及び
エキセナチドのアミノ酸配列のC末端の7~9個のアミノ酸が欠失し、カプリン酸が接合したエキセナチド類似体、又はグルカゴンから形成される第2の単量体;を含み、
前記第1の単量体及び前記第2の単量体が結合して二量体類似体を形成しており、
前記カプリン酸は、アミノ酸が欠失したエキセナチドのC末端にリジンリンカーを介して接合したものであり、
前記エキセナチドのアミノ酸配列は、
1)配列番号1のアミノ酸配列;
2)配列番号1のアミノ酸配列の17番目、24番目及び28番目の少なくとも1つがCysに置換されたアミノ酸配列;
3)配列番号1のアミノ酸配列の24番目及び28番目の少なくとも1つがCysに置換され、前記置換されたアミノ酸に11糖が結合したアミノ酸配列;又は
4)配列番号1のアミノ酸配列の28番目に11糖が結合したアミノ酸配列であり、
前記グルカゴンのアミノ酸配列は、
1)配列番号2のアミノ酸配列;
2)配列番号2のアミノ酸配列の16番目及び24番目の少なくとも1つがCys又はAsnに置換されたアミノ酸配列;又は
3)配列番号2のアミノ酸配列の16番目及び24番目の少なくとも1つがCys又はAsnに置換され、前記置換されたアミノ酸に11糖が結合したアミノ酸配列であり、
前記第2の単量体がエキセナチド類似体である場合に、前記第1の単量体及び前記第2の単量体の結合は、ジスルフィド結合により生成され、
前記第2の単量体がグルカゴンである場合に、前記第1の単量体及び前記第2の単量体の結合は、前記第1の単量体のC末端にLys残基を付加し、その側鎖にグルカゴンから形成される前記第2の単量体を結合することにより、又はジスルフィド結合により生成される、エキセナチド二量体類似体。 - 請求項1に記載のエキセナチド二量体類似体を含む、糖尿病の改善、予防又は治療用の薬剤学的組成物。
- 請求項1に記載のエキセナチド二量体類似体を含む、肥満の改善、予防又は治療用の薬剤学的組成物。
- 請求項1に記載のエキセナチド二量体類似体を含む、糖尿病の改善又は緩和用の食品組成物。
- 請求項1に記載のエキセナチド二量体類似体を含む、肥満の改善又は緩和用の食品組成物。
- 請求項1に記載のエキセナチド二量体類似体を含む、食欲抑制用の食品組成物。
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KR10-2019-0098911 | 2019-08-13 | ||
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KR1020200101087A KR102493143B1 (ko) | 2019-08-13 | 2020-08-12 | 당쇄화 엑세나타이드 유사체 및 이의 용도 |
KR1020200101088A KR102419566B1 (ko) | 2019-08-13 | 2020-08-12 | 엑세나타이드 이량 유사체 및 이의 용도 |
KR10-2020-0101088 | 2020-08-12 | ||
KR10-2020-0101087 | 2020-08-12 | ||
PCT/KR2020/010751 WO2021029698A1 (ko) | 2019-08-13 | 2020-08-13 | 엑세나타이드 유사체 및 이의 용도 |
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US (1) | US20220323548A1 (ja) |
EP (1) | EP4015528A4 (ja) |
JP (1) | JP7425855B2 (ja) |
CN (1) | CN115380043A (ja) |
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- 2020-08-13 CA CA3147770A patent/CA3147770A1/en active Pending
- 2020-08-13 CN CN202080057405.2A patent/CN115380043A/zh active Pending
- 2020-08-13 JP JP2022509115A patent/JP7425855B2/ja active Active
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EP4015528A1 (en) | 2022-06-22 |
CA3147770A1 (en) | 2021-02-18 |
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