WO2016108586A1 - 안정성이 증가된 글루카곤 유도체 - Google Patents
안정성이 증가된 글루카곤 유도체 Download PDFInfo
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- WO2016108586A1 WO2016108586A1 PCT/KR2015/014422 KR2015014422W WO2016108586A1 WO 2016108586 A1 WO2016108586 A1 WO 2016108586A1 KR 2015014422 W KR2015014422 W KR 2015014422W WO 2016108586 A1 WO2016108586 A1 WO 2016108586A1
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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
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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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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- 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
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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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- 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
Definitions
- overweight and obese increases blood pressure and cholesterol levels, causing the onset or worsening of various diseases such as heart disease, diabetes, arthritis, and the like.
- overweight and obesity have become a major factor in increasing the incidence of atherosclerosis, hypertension, hyperlipidemia or heart disease in adults as well as children and adolescents.
- Exendin-4 made from lizard venom with approximately 50% amino acid homology with GLP-1, is also known to activate the GLP-1 receptor to reduce hyperglycemia in diabetic patients.
- drugs for treating obesity including GLP-1 or exendin-4, exhibit problems that cause side effects of vomiting and nausea.
- X7 is threonine or valine
- X24 is valine, leucine, glutamine or arginine
- X27 is isoleucine or methionine
- the glucagon derivative comprising the amino acid sequence of Formula 1 is a substitution, addition deletion or post-translational modification of an amino acid in the sequence of natural glucagon set forth in SEQ ID NO: 1 (eg, methylation, Silicified, ubiquitated, intramolecular covalent bonds), which have an altered pI compared to natural glucagon while maintaining glucagon receptor activity, resulting in increased solubility with pH of the solution, thereby enhancing chemical stability in vivo Encompasses peptides.
- SEQ ID NO: 1 eg, methylation, Silicified, ubiquitated, intramolecular covalent bonds
- Such polymers are preferably water-soluble (amphiphilic or hydrophilic), non-toxic and pharmaceutically inert, preferably homo-polymers or co-polymers of PEG, PEG, monomethyl-substituted polymers of PEG (mPEG) Or poly-amino acids such as poly-lysine, poly-aspartic acid and poly-glutamic acid.
- the pharmaceutical composition of the present invention includes a glucagon derivative having a different pI, which is changed compared to natural glucagon, as an active ingredient, it exhibits improved solubility and high stability according to the pH of the solution, thereby providing stable glucagon for treating hypoglycemia or obesity. It can be usefully used in the preparation of the formulation.
- the present invention provides a method for preventing or treating hypoglycemia or obesity, comprising administering to a subject the glucagon derivative or a pharmaceutical composition comprising the same.
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- General Chemical & Material Sciences (AREA)
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- Obesity (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
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- Peptides Or Proteins (AREA)
Abstract
Description
서열번호 | 아미노산 서열 | 링 형성 |
서열번호: 1 | HSQGTFTSDYSKYLDSRRAQDFVQWLMNT | - |
서열번호: 2 | HSQGTFTSDYSKYLDCDRAQDFVQWLMNT | - |
서열번호: 3 | HSQGTFTSDYSKYLDCERAQDFVQWLMNT | - |
서열번호: 4 | HSQGTFTSDYSKYLDSCDAQDFVQWLMNT | - |
서열번호: 5 | HSQGTFTSDYSKYLDSCEAQDFVQWLMNT | - |
서열번호: 6 | HSQGTFTSDYSKYLDSCEADDFVQWLMNT | - |
서열번호: 7 | YSQGTFTSDYSKYLDSCEADDFVQWLMNT | - |
서열번호: 8 | YXQGTFTSDYSKYLDSCDAQDFVQWLINT | - |
서열번호: 9 | YXQGTFTSDYSKYLDSCDAQDFVVWLINT | - |
서열번호: 10 | YXQGTFTSDYSKYLDSCDADDFVVWLINT | - |
서열번호: 11 | YXQGTFTSDYSKYLDEKCAKEFVQWLMNT | - |
서열번호: 12 | YXQGTFTSDYSKYLDSRRAQDFVQWLMNT | - |
서열번호: 13 | YXQGTFTSDYSCYLDEKRAKEFVQWLMNT | - |
서열번호: 14 | YXQGTFTSDYSKYLDCKRAKEFVQWLMNT | - |
서열번호: 15 | YXQGTFTSDYSKYLCEKRAQDFVQWLMNT | - |
서열번호: 16 | YXQGTFTSDYSKYLDCRRAQVFVQWLMRT | - |
서열번호: 17 | YXQGTFTSDYSKYLDCVRAQDFVQWLMRT | - |
서열번호: 18 | YXQGTFTSDYSKYLDSRRACDFRLWLMNT | - |
서열번호: 19 | YXQGTFTSDYSKYLC E KRA K EFVQWLMNT | 링 형성 |
서열번호: 20 | YXQGTFTSDYSKYLD E CRA K EFVQWLMNT | 링 형성 |
서열번호: 21 | YXQGTFTSDYSKYLD E KCA K EFVQWLMNT | 링 형성 |
서열번호: 22 | YXQGTFTSDYSKYLD E KRC K EFVQWLMNT | 링 형성 |
서열번호: 23 | YXQGTFTSDYSKYCD E KRA K EFVQWLMNT | 링 형성 |
서열번호: 24 | YXQGTFTSDYSKCLD E KRA K EFVQWLMNT | 링 형성 |
서열번호: 25 | YXQGTFTSDYSKYLD E KRA K CFVQWLMNT | 링 형성 |
서열번호: 26 | WXQGTFTSDYSKYLD E CRA K DFVQWLMNT | 링 형성 |
서열번호: 27 | YXQGTFVSDYSKYLD E CRA K DFVQWLMNT | 링 형성 |
서열번호: 28 | WXQGTFVSDYSKYLD E CRA K DFVQWLMNT | 링 형성 |
서열번호: 29 | YXQGTFTSDYSKCLD E RRA K DFVQWLMNT | 링 형성 |
서열번호: 30 | WXQGTFTSDYSKCLD E RRA K DFVQWLMNT | 링 형성 |
서열번호: 31 | YXQGTFTSDYSKYLDC K RAK E FVQWLMNT | 링 형성 |
서열번호: 32 | -SQGTFTSDYSKYLD E CRA K EFVQWLMNT | 링 형성 |
서열번호: 33 | WXQGTFTSDYSKYCD E RRA K EFVQWLMNT | 링 형성 |
서열번호: 34 | YXQGTFTSDYSKYCD E RRA K EFVQWLMNT | 링 형성 |
펩티드 | pI |
서열번호: 1 | 6.8 |
서열번호: 2 | 4.56 |
서열번호: 3 | 4.66 |
서열번호: 4 | 4.13 |
서열번호: 5 | 4.22 |
서열번호: 6 | 4.03 |
서열번호: 7 | 3.71 |
서열번호: 8 | 3.77 |
서열번호: 9 | 3.77 |
서열번호: 10 | 3.66 |
서열번호: 11 | 4.78 |
서열번호: 12 | 6.04 |
서열번호: 13 | 4.78 |
서열번호: 14 | 8.12 |
서열번호: 15 | 6.11 |
서열번호: 16 | 9.11 |
서열번호: 17 | 6.03 |
서열번호: 18 | 8.15 |
서열번호: 19 | 8.12 |
서열번호: 20 | 4.78 |
서열번호: 21 | 4.78 |
서열번호: 22 | 6.20 |
서열번호: 23 | 6.20 |
서열번호: 24 | 6.21 |
서열번호: 25 | 8.12 |
서열번호: 26 | 4.68 |
서열번호: 27 | 4.68 |
서열번호: 28 | 4.68 |
서열번호: 29 | 6.15 |
서열번호: 30 | 4.44 |
서열번호: 31 | 8.12 |
서열번호: 32 | 4.78 |
서열번호: 33 | 6.21 |
서열번호: 34 | 6.21 |
Claims (15)
- 하기 일반식 1의 아미노산 서열을 포함하며, 천연형 글루카곤과 pI가 동일하지 않은 글루카곤 유도체:X1-X2-QGTF-X7-SDYS-X12-X13-X14-X15-X16-X17-X18-X19-X20-X21-F-X23-X24-W-L-X27-X28-T (일반식 1)상기 식에서,X1은 히스티딘, 데스아미노-히스티딘(desamino-histidine), 디메틸-히스티딘(N-dimethyl-histidine), 베타-히드록시 이미다조프로피온산(beta-hydroxyimidazopropionic acid), 4-이미다조아세트산(4-imidazoacetic acid), 베타-카르복시 이미다조프로피온산(beta-carboxyimidazopropionic acid), 트립토판, 티로신 혹은 부존재하고;X2는 알파-메틸-글루탐산(α-methyl-glutamic acid), Aib(aminoisobutyric acid), D-알라닌, 글리신, Sar(N-methylglycine), 세린 또는 D-세린이고;X7은 트레오닌 또는 발린이고;X12는 리신 또는 시스테인이고;X13은 티로신 또는 시스테인이고;X14는 류신 또는 시스테인이고;X15는 아스파르트산, 글루탐산 또는 시스테인이고;X16은 글루탐산, 아스파르트산, 세린, 알파-메틸-글루탐산 또는 시스테인이고;X17은 아스파르트산, 글루타민, 글루탐산, 리신, 아르기닌, 세린, 발린 또는 시스테인이고;X18은 아스파르트산, 글루타민, 글루탐산, 아르기닌 또는 시스테인이고;X19는 알라닌 또는 시스테인이고;X20은 리신, 글루탐산, 글루타민, 아스파르트산, 리신, 또는 시스테인이고;X21은 아스파르트산, 글루탐산, 발린 또는 시스테인이고;X23은 발린 또는 아르기닌이고;X24는 발린, 류신, 글루타민 또는 아르기닌이고;X27은 이소류신 또는 메티오닌이고;X28은 아르기닌 또는 아스파라긴임(단, 상기 일반식 1의 아미노산 서열이 서열번호: 1과 동일한 경우는 제외함).
- 제1항에 있어서, 일반식 1의 아미노산 서열에서X1이 히스티딘 또는 트립토판, 티로신 혹은 부존재하고;X2가 세린 또는 Aib(aminoisobutyric acid)이고;X7은 트레오닌 또는 발린이고;X12는 리신 또는 시스테인이고;X13은 티로신 또는 시스테인이고;X14는 류신 또는 시스테인이고;X15는 아스파르트산, 또는 시스테인이고;X16은 글루탐산, 아스파르트산, 세린, 또는 시스테인이고;X17은 아스파르트산, 글루탐산, 리신, 아르기닌, 발린 또는 시스테인이고;X18은 아스파르트산, 글루탐산, 아르기닌 또는 시스테인이고;X19는 알라닌 또는 시스테인이고;X20은 리신, 글루탐산, 글루타민, 아스파르트산, 리신, 또는 시스테인이고;X21은 아스파르트산, 글루탐산, 발린 또는 시스테인이고;X23은 발린 또는 아르기닌이고;X24는 발린, 류신 또는 글루타민이고;X27은 이소류신 또는 메티오닌이고;X28은 아르기닌 또는 아스파라긴(단, 상기 일반식 1의 아미노산 서열이 서열번호: 1과 동일한 경우는 제외함)인 글루카곤 유도체.
- 제1항에 있어서, 상기 글루카곤 유도체는 글루카곤 수용체 자극 활성이 있는 글루카곤 유도체.
- 제1항에 있어서, 상기 글루카곤 유도체가 서열번호: 2 내지 34의 아미노산 서열로 구성된 군으로부터 선택된 아미노산 서열을 포함하는 것인 글루카곤 유도체.
- 제1항 내지 제4항 중 어느 한 항의 글루카곤 유도체를 코딩하는 폴리뉴클레오티드.
- 제1항 내지 제4항 중 어느 한 항의 글루카곤 유도체를 유효성분으로 포함하는 저혈당의 예방 또는 치료용 약학적 조성물.
- 제1항 내지 제4항 중 어느 한 항의 글루카곤 유도체를 유효성분으로 포함하는 비만의 예방 또는 치료용 약학적 조성물.
- 제6항에 있어서, 약학적으로 허용가능한 담체를 추가로 포함하는 약학적 조성물.
- 제7항에 있어서, 약학적으로 허용가능한 담체를 추가로 포함하는 약학적 조성물.
- 제7항에 있어서, 상기 약학적 조성물이 단독 또는 다른 비만 예방 또는 치료효과를 나타내는 약학적 제제와 병용하여 투여되는 것인 약학적 조성물.
- 제7항에 있어서, 상기 약학적 조성물은 비만 예방 또는 치료효과를 나타내는 약학적 제제를 추가로 포함하는 약학적 조성물.
- 제10항에 있어서, 상기 비만 예방 또는 치료효과를 나타내는 약학적 제제를 GLP-1 수용체 작용제(agonist), GIP(glucose-dependent insulinotropic peptide) 수용체 길항제(antagonist), 렙틴(Leptin) 수용체 작용제, DPP-IV 저해제, Y5 수용체 길항제, MCH(Melanin-concentrating hormone) 수용체 길항제, Y2/3/4 수용체 작용제, MC3/4 수용체 작용제, 위/췌장 리파아제(gastric/pancreatic lipase) 저해제, 5HT2c 작용제, β3A 수용체 작용제, 아밀린(Amylin) 수용체 작용제, 그랠린(Ghrelin) 길항제 및 그랠린 수용체 길항제, FGF1, FGF21 수용체 작용제, CCK(Cholecystokinin) 수용체 작용제, PP(Pancreatic polypeptide) 수용체 작용제, 도파민 재흡수 억제제 및 이들의 조합으로 이루어진 군에서 선택하는 것인 약학적 조성물.
- 제11항에 있어서, 상기 비만 예방 또는 치료효과를 나타내는 약학적 제제를 GLP-1 수용체 작용제(agonist), GIP(glucose-dependent insulinotropic peptide) 수용체 길항제(antagonist), 렙틴(Leptin) 수용체 작용제, DPP-IV 저해제, Y5 수용체 길항제, MCH(Melanin-concentrating hormone) 수용체 길항제, Y2/3/4 수용체 작용제, MC3/4 수용체 작용제, 위/췌장 리파아제(gastric/pancreatic lipase) 저해제, 5HT2c 작용제, β3A 수용체 작용제, 아밀린(Amylin) 수용체 작용제, 그랠린(Ghrelin) 길항제 및 그랠린 수용체 길항제, FGF1, FGF21 수용체 작용제, CCK(Cholecystokinin) 수용체 작용제, PP(Pancreatic polypeptide) 수용체 작용제, 도파민 재흡수 억제제 및 이들의 조합으로 이루어진 군에서 선택하는 것인 약학적 조성물.
- 제1항 내지 제4항 중 어느 한 항의 글루카곤 유도체 또는 이를 포함하는 약학적 조성물을 개체에게 투여하는 단계를 포함하는, 저혈당 또는 비만의 예방 또는 치료 방법.
- 저혈당 또는 비만의 예방 또는 치료용 의약품의 제조에 있어서, 제1항 내지 제4항 중 어느 한 항의 글루카곤 유도체의 용도.
Priority Applications (24)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US15/540,729 US11135271B2 (en) | 2014-12-30 | 2015-12-30 | Glucagon derivatives with improved stability |
MYPI2017000967A MY185334A (en) | 2014-12-30 | 2015-12-30 | Glucagon derivatives with improved stability |
EP15875680.9A EP3241841A4 (en) | 2014-12-30 | 2015-12-30 | Glucagon derivative having improved stability |
JP2017535417A JP6797122B2 (ja) | 2014-12-30 | 2015-12-30 | 安定性が増加されたグルカゴン誘導体 |
MA40709A MA40709B1 (fr) | 2014-12-30 | 2015-12-30 | Dérivé du glucagon à stabilité améliorée |
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PE2022001996A PE20230304A1 (es) | 2014-12-30 | 2015-12-30 | Derivados de glucagon como agentes hipoglucemicos y antiobesidad |
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BR112017014205-8A BR112017014205B1 (pt) | 2014-12-30 | 2015-12-30 | Derivados de glucagon e seu uso, e uso de uma composição farmacêutica |
CN201580077186.3A CN107636009B (zh) | 2014-12-30 | 2015-12-30 | 具有改善的稳定性的胰高血糖素衍生物 |
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EA201791333A EA035527B1 (ru) | 2014-12-30 | 2015-12-30 | Производные глюкагона с улучшенной стабильностью |
CONC2017/0006308A CO2017006308A2 (es) | 2014-12-30 | 2017-06-27 | Derivados de glucagón |
IL253206A IL253206B (en) | 2014-12-30 | 2017-06-27 | Glucagon derivatives have improved stability |
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MA (1) | MA40709B1 (ko) |
MX (1) | MX2017008569A (ko) |
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PE (2) | PE20171154A1 (ko) |
PH (1) | PH12017501222A1 (ko) |
SG (1) | SG11201705376SA (ko) |
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UA (1) | UA126960C2 (ko) |
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WO2022216129A1 (ko) | 2021-04-09 | 2022-10-13 | 한미약품 주식회사 | 글루카곤 유도체를 포함하는 만성 신장 질환 예방 또는 치료용 약학 조성물 |
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