HRP20230820T1 - Heparan-sulfat, s visokom stopom 3-o-sulfatiranja u glukozaminskim ostacima - Google Patents
Heparan-sulfat, s visokom stopom 3-o-sulfatiranja u glukozaminskim ostacima Download PDFInfo
- Publication number
- HRP20230820T1 HRP20230820T1 HRP20230820TT HRP20230820T HRP20230820T1 HR P20230820 T1 HRP20230820 T1 HR P20230820T1 HR P20230820T T HRP20230820T T HR P20230820TT HR P20230820 T HRP20230820 T HR P20230820T HR P20230820 T1 HRP20230820 T1 HR P20230820T1
- Authority
- HR
- Croatia
- Prior art keywords
- sulfate group
- glcn
- polysaccharide
- polysaccharide according
- share
- Prior art date
Links
- 229920002971 Heparan sulfate Polymers 0.000 title 1
- MSWZFWKMSRAUBD-IVMDWMLBSA-N glucosamine group Chemical group OC1[C@H](N)[C@@H](O)[C@H](O)[C@H](O1)CO MSWZFWKMSRAUBD-IVMDWMLBSA-N 0.000 title 1
- 238000005670 sulfation reaction Methods 0.000 title 1
- 150000004676 glycans Chemical class 0.000 claims 13
- 229920001282 polysaccharide Polymers 0.000 claims 13
- 239000005017 polysaccharide Substances 0.000 claims 13
- QAOWNCQODCNURD-UHFFFAOYSA-L sulfate group Chemical group S(=O)(=O)([O-])[O-] QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 10
- 230000023555 blood coagulation Effects 0.000 claims 4
- AEMOLEFTQBMNLQ-HNFCZKTMSA-N L-idopyranuronic acid Chemical compound OC1O[C@@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O AEMOLEFTQBMNLQ-HNFCZKTMSA-N 0.000 claims 3
- 125000000600 disaccharide group Chemical group 0.000 claims 3
- AEMOLEFTQBMNLQ-AQKNRBDQSA-N D-glucopyranuronic acid Chemical group OC1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O AEMOLEFTQBMNLQ-AQKNRBDQSA-N 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 238000002360 preparation method Methods 0.000 claims 2
- 208000024891 symptom Diseases 0.000 claims 2
- 208000005189 Embolism Diseases 0.000 claims 1
- 108010029144 Factor IIa Proteins 0.000 claims 1
- 108010074860 Factor Xa Proteins 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 229920001218 Pullulan Polymers 0.000 claims 1
- 239000004373 Pullulan Substances 0.000 claims 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 1
- AEMOLEFTQBMNLQ-UHFFFAOYSA-N beta-D-galactopyranuronic acid Natural products OC1OC(C(O)=O)C(O)C(O)C1O AEMOLEFTQBMNLQ-UHFFFAOYSA-N 0.000 claims 1
- 238000000502 dialysis Methods 0.000 claims 1
- 238000005227 gel permeation chromatography Methods 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 230000000116 mitigating effect Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 230000014508 negative regulation of coagulation Effects 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 235000019423 pullulan Nutrition 0.000 claims 1
- 230000003252 repetitive effect Effects 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 230000001732 thrombotic effect Effects 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08B—POLYSACCHARIDES; DERIVATIVES THEREOF
- C08B37/00—Preparation of polysaccharides not provided for in groups C08B1/00 - C08B35/00; Derivatives thereof
- C08B37/006—Heteroglycans, i.e. polysaccharides having more than one sugar residue in the main chain in either alternating or less regular sequence; Gellans; Succinoglycans; Arabinogalactans; Tragacanth or gum tragacanth or traganth from Astragalus; Gum Karaya from Sterculia urens; Gum Ghatti from Anogeissus latifolia; Derivatives thereof
- C08B37/0063—Glycosaminoglycans or mucopolysaccharides, e.g. keratan sulfate; Derivatives thereof, e.g. fucoidan
- C08B37/0075—Heparin; Heparan sulfate; Derivatives thereof, e.g. heparosan; Purification or extraction methods thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
- A61K31/726—Glycosaminoglycans, i.e. mucopolysaccharides
- A61K31/727—Heparin; Heparan
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
- C12P19/00—Preparation of compounds containing saccharide radicals
- C12P19/04—Polysaccharides, i.e. compounds containing more than five saccharide radicals attached to each other by glycosidic bonds
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
- C12N15/09—Recombinant DNA-technology
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Zoology (AREA)
- Wood Science & Technology (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biotechnology (AREA)
- Microbiology (AREA)
- General Engineering & Computer Science (AREA)
- Genetics & Genomics (AREA)
- Materials Engineering (AREA)
- Polymers & Plastics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Polysaccharides And Polysaccharide Derivatives (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Enzymes And Modification Thereof (AREA)
- Saccharide Compounds (AREA)
Claims (13)
1. Polisaharid koji ima aktivnost antikoagulansa, u kojem je omjer između aktivnosti protiv čimbenika Xa i aktivnosti protiv čimbenika IIa 1,5 ili veći, čineći repetitivnu strukturu disaharidne jedinice prikazanu u sljedećoj općoj formuli (I):
[image]
,
naznačen time što
R1 do R5 ispunjavaju sljedeće uvjete;
svaki od R1, R2, R4 i R5 neovisno predstavlja vodik ili sulfatnu skupinu;
R3 predstavlja vodik, sulfatnu skupinu ili acetilnu skupinu;
udio sulfatne skupine u R2 u ostacima glukuronske kiseline je manji od 15%;
u najmanju ruku dio R3 je sulfatna skupina;
udio sulfatne skupine u R4 je 13% ili više; i
udio sulfatne skupine u R5 je 50% ili više,
gdje se 50% ili više šećernih lanaca u ukupnom broju šećernih lanaca koji čine navedeni polisaharid sastoji od strukture prikazane u sljedećoj općoj formuli (II):
[image]
,
gdje
R1 do R5 su isti kao R1 do R5 u navedenoj općoj formuli (I);
i
n je 3 do 30 kao prosječna vrijednost,
gdje je brojčano prosječna molekulska težina izmjerena gel permeacijskom kromatografijom uz upotrebu pululana kao standarda 12000 do 40000.
2. Polisaharid u skladu s patentnim zahtjevom 1, naznačen time što je udio sadržaja navedene disaharidne jedinice 90% ili više.
3. Polisaharid u skladu s patentnim zahtjevom 1 ili 2, naznačen time što se 50% ili više šećernih lanaca u ukupnom broju šećernih lanaca koji čine navedeni polisaharid sastoji od strukture prikazane u sljedećoj općoj formuli (II):
[image]
,
gdje
R1 do R5 su isti kao R1 do R5 u navedenoj općoj formuli (I);
i
n je 3 do 15 kao prosječna vrijednost.
4. Polisaharid u skladu s bilo kojim od patentnih zahtjeva 1 do 3, naznačen time što je prosječan broj vezanih šećernih ostataka 6 do 60.
5. Polisaharid u skladu s bilo kojim od patentnih zahtjeva 1 do 4, naznačen time što je udio sulfatne skupine u R1 0% do 80%.
6. Polisaharid u skladu s bilo kojim od patentnih zahtjeva 1 do 5, naznačen time što je udio sulfatne skupine u R3 70% do 100%.
7. Polisaharid u skladu s bilo kojim od patentnih zahtjeva 1 do 6, naznačen time što je udio sulfatne skupine u R4 45% ili manje.
8. Polisaharid u skladu s bilo kojim od patentnih zahtjeva 1 do 7, naznačen time što je udio sulfatne skupine u R5 70% do 100%.
9. Polisaharid u skladu s bilo kojim od patentnih zahtjeva 1 do 8, naznačen time što sadrži jednu ili više disaharidnih jedinica, koje se bira između GlcA-GlcN(NS3S6S), GlcA(2S)-GlcN(NS6S), IdoA(2S)-GlcN(NS6S), GlcA-GlcN(NS6S), IdoA(2S)-GlcN(NS), IdoA(2S)-GlcN(NS3S), IdoA-GlcN(NS6S), te GlcA-GlcN(NS), pri udjelu u ukupnom sadržaju od 50% ili više.
10. Polisaharid u skladu s bilo kojim od patentnih zahtjeva 1 do 9, naznačen time što je slobodni oblik, ili farmakološki prihvatljiva sol, ili njihova smjesa.
11. Farmaceutski pripravak, naznačen time što sadrži polisaharid u skladu s bilo kojim od patentnih zahtjeva 1 do 10.
12. Pripravak u skladu s patentnim zahtjevom 11, naznačen time što ga se upotrebljava u sprječavanju, ublažavanju i/ili liječenju simptoma kojeg se pripisuje zgrušavanju krvi.
13. Pripravak u skladu s patentnim zahtjevom 12, naznačen time što je navedeni simptom sindrom diseminiranog intravaskularnog zgrušavanja krvi, trombotička embolija, zgrušavanje krvi kod umjetne dijalize ili zgrušavanje krvi u izvantjelesnom krvotoku.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2015257022 | 2015-12-28 | ||
| EP16881651.0A EP3399045B9 (en) | 2015-12-28 | 2016-12-16 | Heparan sulfate having high 3-o-sulfation rate of glucosamine residues |
| PCT/JP2016/087689 WO2017115675A1 (ja) | 2015-12-28 | 2016-12-16 | グルコサミン残基の３－ｏ－硫酸化率が高いヘパラン硫酸 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20230820T1 true HRP20230820T1 (hr) | 2023-11-10 |
Family
ID=59225733
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20230820TT HRP20230820T1 (hr) | 2015-12-28 | 2016-12-16 | Heparan-sulfat, s visokom stopom 3-o-sulfatiranja u glukozaminskim ostacima |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US10889656B2 (hr) |
| EP (1) | EP3399045B9 (hr) |
| JP (2) | JP7006275B2 (hr) |
| CN (1) | CN108699580B (hr) |
| ES (1) | ES2947291T3 (hr) |
| HR (1) | HRP20230820T1 (hr) |
| HU (1) | HUE062293T2 (hr) |
| WO (1) | WO2017115675A1 (hr) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111065740B (zh) * | 2017-09-05 | 2024-06-25 | 味之素株式会社 | 2-o-硫酸化酶突变体和3-o-硫酸化酶突变体及其使用方法 |
| EP3816279A4 (en) | 2018-06-27 | 2022-04-20 | Ajinomoto Co., Inc. | STEM CELL CULTURE ADDITIVE, CULTURE MEDIUM, AND CULTURE METHOD |
| CN109321508B (zh) * | 2018-10-12 | 2022-12-27 | 北京化工大学 | 产heparosan的基因工程菌及其应用 |
| JP7540168B2 (ja) | 2019-04-16 | 2024-08-27 | 東ソー株式会社 | 強酸性陽イオン交換体及びその製造方法 |
| CN116103275B (zh) * | 2022-12-01 | 2024-03-08 | 上海兴糖生物技术有限公司 | 一种葡萄糖醛酸c5-差向异构酶、其核苷酸序列、表达载体、细胞株及其构建方法 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4396762A (en) * | 1981-08-24 | 1983-08-02 | Massachusetts Institute Of Technology | Heparinase derived anticoagulants |
| US8227449B2 (en) * | 2000-03-30 | 2012-07-24 | Glycores 2000 S.R.L. | Glycosaminoglycans derived from K5 polysaccharide having high anticoagulant and antithrombotic activities and process for their preparation |
| US20050027117A1 (en) * | 2000-12-18 | 2005-02-03 | Pasqua Oreste | Anticoagulant and antithrombotic LMW-glycosaminoglycans derived from K5 polysaccharide and process for their preparation |
| ITMI20032498A1 (it) * | 2003-12-17 | 2005-06-18 | Pasqua Anna Oreste | Polisaccaridi antitrombotici a basso peso molecolare e |
| AU2003293122A1 (en) * | 2002-11-27 | 2004-06-23 | Massachusetts Institute Of Technology | Methods for synthesizing polysaccharides |
| IN2014DN02837A (hr) | 2005-05-12 | 2015-07-10 | Univ North Carolina | |
| CN101531723A (zh) | 2009-02-27 | 2009-09-16 | 江南大学 | 一种用生物酶对肝素进行选择性结构修饰制备肝素衍生物的方法 |
| US8420790B2 (en) | 2009-10-30 | 2013-04-16 | Reliable Biopharmaceutical Corporation | Efficient and scalable process for the manufacture of Fondaparinux sodium |
| US11203772B2 (en) * | 2010-12-23 | 2021-12-21 | The University Of North Carolina At Chapel Hill | Chemoenzymatic synthesis of structurally homogeneous ultra-low molecular weight heparins |
| EP3054005B1 (en) * | 2013-10-02 | 2019-11-20 | Ajinomoto Co., Inc. | Heparosan-producing bacterium and heparosan manufacturing method |
-
2016
- 2016-12-16 JP JP2017558935A patent/JP7006275B2/ja active Active
- 2016-12-16 ES ES16881651T patent/ES2947291T3/es active Active
- 2016-12-16 WO PCT/JP2016/087689 patent/WO2017115675A1/ja active Application Filing
- 2016-12-16 HU HUE16881651A patent/HUE062293T2/hu unknown
- 2016-12-16 EP EP16881651.0A patent/EP3399045B9/en active Active
- 2016-12-16 HR HRP20230820TT patent/HRP20230820T1/hr unknown
- 2016-12-16 CN CN201680082662.5A patent/CN108699580B/zh active Active
-
2018
- 2018-06-26 US US16/018,487 patent/US10889656B2/en active Active
-
2021
- 2021-09-29 JP JP2021159986A patent/JP2022003136A/ja not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| JP2022003136A (ja) | 2022-01-11 |
| EP3399045A4 (en) | 2019-08-28 |
| US10889656B2 (en) | 2021-01-12 |
| JPWO2017115675A1 (ja) | 2018-10-18 |
| JP7006275B2 (ja) | 2022-02-10 |
| US20180298117A1 (en) | 2018-10-18 |
| CN108699580A (zh) | 2018-10-23 |
| HUE062293T2 (hu) | 2023-10-28 |
| EP3399045A1 (en) | 2018-11-07 |
| CN108699580B (zh) | 2022-09-23 |
| ES2947291T3 (es) | 2023-08-04 |
| EP3399045B1 (en) | 2023-06-07 |
| EP3399045C0 (en) | 2023-06-07 |
| EP3399045B9 (en) | 2023-10-04 |
| WO2017115675A1 (ja) | 2017-07-06 |
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