HRP20200332T1 - Modifikator eksenatida i njegova primjena - Google Patents
Modifikator eksenatida i njegova primjena Download PDFInfo
- Publication number
- HRP20200332T1 HRP20200332T1 HRP20200332TT HRP20200332T HRP20200332T1 HR P20200332 T1 HRP20200332 T1 HR P20200332T1 HR P20200332T T HRP20200332T T HR P20200332TT HR P20200332 T HRP20200332 T HR P20200332T HR P20200332 T1 HRP20200332 T1 HR P20200332T1
- Authority
- HR
- Croatia
- Prior art keywords
- exenatide
- modifier
- integer
- image
- pharmaceutically acceptable
- Prior art date
Links
- 108010011459 Exenatide Proteins 0.000 title claims 10
- 229960001519 exenatide Drugs 0.000 title claims 10
- HTQBXNHDCUEHJF-XWLPCZSASA-N Exenatide Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)CNC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 HTQBXNHDCUEHJF-XWLPCZSASA-N 0.000 title claims 9
- 239000003607 modifier Substances 0.000 title claims 9
- 150000003839 salts Chemical class 0.000 claims 6
- 208000004930 Fatty Liver Diseases 0.000 claims 2
- 206010019708 Hepatic steatosis Diseases 0.000 claims 2
- 230000023852 carbohydrate metabolic process Effects 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000010706 fatty liver disease Diseases 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 231100000240 steatosis hepatitis Toxicity 0.000 claims 2
- 208000024891 symptom Diseases 0.000 claims 2
- 230000004580 weight loss Effects 0.000 claims 2
- 229940089838 Glucagon-like peptide 1 receptor agonist Drugs 0.000 claims 1
- 125000001931 aliphatic group Chemical group 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- JUFFVKRROAPVBI-PVOYSMBESA-N chembl1210015 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)N[C@H]1[C@@H]([C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O)[C@@H](O)[C@@H](CO[C@]3(O[C@@H](C[C@H](O)[C@H](O)CO)[C@H](NC(C)=O)[C@@H](O)C3)C(O)=O)O2)O)[C@@H](CO)O1)NC(C)=O)C(=O)NCC(=O)NCC(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)CNC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 JUFFVKRROAPVBI-PVOYSMBESA-N 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001033 ether group Chemical group 0.000 claims 1
- 239000003877 glucagon like peptide 1 receptor agonist Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
Classifications
-
- 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
-
- 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
-
- 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
- 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
- A61K38/2278—Vasoactive intestinal peptide [VIP]; Related peptides (e.g. Exendin)
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- 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
-
- 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
-
- 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
- C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Organic Chemistry (AREA)
- Diabetes (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Endocrinology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Zoology (AREA)
- Gastroenterology & Hepatology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Hematology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Obesity (AREA)
- Toxicology (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Immunology (AREA)
- Emergency Medicine (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Child & Adolescent Psychology (AREA)
- Vascular Medicine (AREA)
- Dermatology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Medicinal Preparation (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Claims (7)
1. Modifikator eksenatida ili njegova farmaceutski prihvatljiva sol koji ima aktivnost agonista receptora GLP-1, kao što je prikazano u formuli (I):
(Ex-4)-L-Y (I)
pri čemu, Ex-4 je Eksendin-4; L je
[image]
za spajanje Ex-4 s Y; L’ je hidrofilni lanac koji sadrži skupinu etera; Y je alifatski lanac sa terminalnom karboksilnom skupinom, pri čemu modifikator eksenatida je:
[image]
k je bilo koji cijeli broj između 6-20.
2. Modifikator eksenatida ili njegova farmaceutski prihvatljiva sol prema patentnom zahtjevu 1, naznačen time što je L odabran od:
[image]
[image]
pri čemu, m je bilo koji cijeli broj između 2-20; n je bilo koji cijeli broj između 2-20; r je bilo koji cijeli broj između 1-6.
3. Modifikator eksenatida ili njegova farmaceutski prihvatljiva sol prema patentnom zahtjevu 1, naznačen time što modifikator eksenatida je:
[image]
[image]
pri čemu m je bilo koji cijeli broj između 2-20; n je bilo koji cijeli broj između 2-20; r je bilo koji cijeli broj između 1-6; k je bilo koji cijeli broj između 6-20.
4. Modifikator eksenatida ili njegova farmaceutski prihvatljiva sol prema patentnom zahtjevu 3, naznačen time što sadrži slijedeće spojeve:
[image]
[image]
5. Modifikator eksenatida ili njegova farmaceutski prihvatljiva sol prema patentnom zahtjevu 1 ili 2 naznačen time što je za uporabu za liječenje bolesti i/ili simptoma povezanih s glikometabolizmom,
ili za uporabu za liječenje dijabetesa,
ili za uporabu za liječenje masne jetre,
ili za uporabu u postupku gubljenja težine.
6. Farmaceutski pripravak naznačen time što sadrži modifikator eksenatida ili njegovu farmaceutski prihvatljivu sol prema patentnom zahtjevu 1 ili 2 i po izboru farmaceutski prihvatljive nosače.
7. Pripravak prema patentnom zahtjevu 6 naznačen time što je za uporabu za liječenje bolesti i/ili simptoma povezanih s glikometabolizmom,
ili za uporabu za liječenje dijabetesa,
ili za uporabu za liječenje masne jetre,
ili za uporabu u postupku gubljenja težine.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510619012.7A CN106554403B (zh) | 2015-09-25 | 2015-09-25 | 艾塞那肽修饰物及其用途 |
| PCT/CN2016/098844 WO2017050157A1 (zh) | 2015-09-25 | 2016-09-13 | 艾塞那肽修饰物及其用途 |
| EP16848039.0A EP3321279B1 (en) | 2015-09-25 | 2016-09-13 | Exenatide modifier and use thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20200332T1 true HRP20200332T1 (hr) | 2020-06-12 |
Family
ID=58385848
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20200332TT HRP20200332T1 (hr) | 2015-09-25 | 2020-02-27 | Modifikator eksenatida i njegova primjena |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US11179467B2 (hr) |
| EP (1) | EP3321279B1 (hr) |
| JP (1) | JP6647387B2 (hr) |
| KR (1) | KR102005294B1 (hr) |
| CN (1) | CN106554403B (hr) |
| AU (1) | AU2016328015B9 (hr) |
| CA (1) | CA2995613C (hr) |
| CY (1) | CY1122760T1 (hr) |
| DK (1) | DK3321279T3 (hr) |
| ES (1) | ES2775185T3 (hr) |
| HR (1) | HRP20200332T1 (hr) |
| HU (1) | HUE048411T2 (hr) |
| LT (1) | LT3321279T (hr) |
| PL (1) | PL3321279T3 (hr) |
| PT (1) | PT3321279T (hr) |
| RS (1) | RS60053B1 (hr) |
| SI (1) | SI3321279T1 (hr) |
| WO (1) | WO2017050157A1 (hr) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111333714A (zh) * | 2020-03-05 | 2020-06-26 | 成都奥达生物科技有限公司 | 一种长效glp-1化合物 |
| CN112939771A (zh) * | 2021-01-28 | 2021-06-11 | 宁夏蓝博思化学技术有限公司 | 长链烷基二酸单叔丁酯的制备方法 |
| CN115124602B (zh) * | 2021-03-25 | 2024-01-26 | 博瑞生物医药（苏州）股份有限公司 | Gip和glp-1的双受体激动剂、药物组合物及用途 |
| WO2024061310A1 (zh) * | 2022-09-23 | 2024-03-28 | 博瑞生物医药（苏州）股份有限公司 | 一种glp-1和gip双受体激动剂药物组合物及其用途 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU3247799A (en) | 1998-02-27 | 1999-09-15 | Novo Nordisk A/S | Glp-1 derivatives of glp-1 and exendin with protracted profile of action |
| ES2244416T5 (es) | 1999-01-14 | 2020-01-03 | Amylin Pharmaceuticals Llc | Formulaciones novedosas de agonistas de la exendina y métodos de administración de los mismos |
| EP1667724A2 (en) * | 2003-09-19 | 2006-06-14 | Novo Nordisk A/S | Albumin-binding derivatives of therapeutic peptides |
| TWI372629B (en) * | 2005-03-18 | 2012-09-21 | Novo Nordisk As | Acylated glp-1 compounds |
| WO2006097538A1 (en) | 2005-03-18 | 2006-09-21 | Novo Nordisk A/S | Extended glp-1 compounds |
| CN102827284B (zh) | 2006-11-14 | 2015-07-29 | 上海仁会生物制药股份有限公司 | 带有聚乙二醇基团的Exendin或其类似物及其制剂和用途 |
| CN101215324B (zh) | 2007-12-26 | 2010-11-24 | 吉林大学 | 艾塞那肽短肽模拟肽及其在制备糖尿病治疗药物中的应用 |
| BRPI0906643A2 (pt) * | 2008-02-01 | 2019-09-10 | Ascendis Pharma As | profármaco compreendendo um conjugado fármaco-ligante |
| US20110171164A1 (en) * | 2008-09-19 | 2011-07-14 | Nektar Therapeutics | Polymer conjugates of glp-2-like peptides |
| CN101870728A (zh) | 2009-04-23 | 2010-10-27 | 派格生物医药(苏州)有限公司 | 新型Exendin变体及其缀合物 |
| CN102397558B (zh) | 2010-09-09 | 2013-08-14 | 中国人民解放军军事医学科学院毒物药物研究所 | Exendin-4类似物的定位聚乙二醇化修饰物及其用途 |
| EP2438930A1 (en) | 2010-09-17 | 2012-04-11 | Sanofi-Aventis Deutschland GmbH | Prodrugs comprising an exendin linker conjugate |
| WO2013059323A1 (en) | 2011-10-18 | 2013-04-25 | Prolynx Llc | Peg conjugates of exenatide |
| CN102532303A (zh) | 2011-12-22 | 2012-07-04 | 江苏弘和药物研发有限公司 | 聚乙二醇缀合的艾塞那肽的合成及应用 |
| CN102827270A (zh) | 2012-09-13 | 2012-12-19 | 无锡和邦生物科技有限公司 | 一种聚乙二醇化艾塞那肽衍生物及其用途 |
| CN103405753B (zh) * | 2013-08-13 | 2016-05-11 | 上海仁会生物制药股份有限公司 | 稳定的促胰岛素分泌肽水针药物组合物 |
| KR101768446B1 (ko) * | 2014-03-21 | 2017-08-17 | 애니젠 주식회사 | 신규한 엑세나타이드 유사체 및 그의 용도 |
-
2015
- 2015-09-25 CN CN201510619012.7A patent/CN106554403B/zh active Active
-
2016
- 2016-09-13 PL PL16848039T patent/PL3321279T3/pl unknown
- 2016-09-13 US US15/752,838 patent/US11179467B2/en active Active
- 2016-09-13 JP JP2018506893A patent/JP6647387B2/ja active Active
- 2016-09-13 AU AU2016328015A patent/AU2016328015B9/en active Active
- 2016-09-13 ES ES16848039T patent/ES2775185T3/es active Active
- 2016-09-13 LT LTEP16848039.0T patent/LT3321279T/lt unknown
- 2016-09-13 KR KR1020187005100A patent/KR102005294B1/ko active IP Right Grant
- 2016-09-13 WO PCT/CN2016/098844 patent/WO2017050157A1/zh active Application Filing
- 2016-09-13 DK DK16848039.0T patent/DK3321279T3/da active
- 2016-09-13 CA CA2995613A patent/CA2995613C/en active Active
- 2016-09-13 RS RS20200228A patent/RS60053B1/sr unknown
- 2016-09-13 HU HUE16848039A patent/HUE048411T2/hu unknown
- 2016-09-13 PT PT168480390T patent/PT3321279T/pt unknown
- 2016-09-13 SI SI201630653T patent/SI3321279T1/sl unknown
- 2016-09-13 EP EP16848039.0A patent/EP3321279B1/en active Active
-
2020
- 2020-02-27 HR HRP20200332TT patent/HRP20200332T1/hr unknown
- 2020-02-28 CY CY20201100184T patent/CY1122760T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2017050157A1 (zh) | 2017-03-30 |
| JP2018531217A (ja) | 2018-10-25 |
| KR20180031740A (ko) | 2018-03-28 |
| HUE048411T2 (hu) | 2020-07-28 |
| ES2775185T3 (es) | 2020-07-24 |
| AU2016328015A1 (en) | 2018-03-01 |
| EP3321279A4 (en) | 2018-05-16 |
| PT3321279T (pt) | 2020-03-05 |
| CA2995613A1 (en) | 2017-03-30 |
| PL3321279T3 (pl) | 2020-10-19 |
| RS60053B1 (sr) | 2020-04-30 |
| JP6647387B2 (ja) | 2020-02-14 |
| CN106554403A (zh) | 2017-04-05 |
| CY1122760T1 (el) | 2021-03-12 |
| CA2995613C (en) | 2021-07-20 |
| KR102005294B1 (ko) | 2019-07-30 |
| SI3321279T1 (sl) | 2020-07-31 |
| EP3321279B1 (en) | 2020-02-12 |
| AU2016328015A9 (en) | 2018-11-01 |
| DK3321279T3 (da) | 2020-03-09 |
| LT3321279T (lt) | 2020-04-10 |
| AU2016328015B9 (en) | 2018-12-06 |
| AU2016328015B2 (en) | 2018-10-25 |
| CN106554403B (zh) | 2021-08-31 |
| US20200101162A1 (en) | 2020-04-02 |
| US11179467B2 (en) | 2021-11-23 |
| EP3321279A1 (en) | 2018-05-16 |
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