HRP20220166T1 - Konjugati stanozolola i hialuronske kiseline - Google Patents
Konjugati stanozolola i hialuronske kiseline Download PDFInfo
- Publication number
- HRP20220166T1 HRP20220166T1 HRP20220166TT HRP20220166T HRP20220166T1 HR P20220166 T1 HRP20220166 T1 HR P20220166T1 HR P20220166T T HRP20220166T T HR P20220166TT HR P20220166 T HRP20220166 T HR P20220166T HR P20220166 T1 HRP20220166 T1 HR P20220166T1
- Authority
- HR
- Croatia
- Prior art keywords
- hyaluronic acid
- salt
- group
- stanozolol
- conjugates
- Prior art date
Links
- KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 title claims 10
- 229920002674 hyaluronan Polymers 0.000 title claims 10
- 229960003160 hyaluronic acid Drugs 0.000 title claims 10
- LKAJKIOFIWVMDJ-IYRCEVNGSA-N Stanazolol Chemical compound C([C@@H]1CC[C@H]2[C@@H]3CC[C@@]([C@]3(CC[C@@H]2[C@@]1(C)C1)C)(O)C)C2=C1C=NN2 LKAJKIOFIWVMDJ-IYRCEVNGSA-N 0.000 title claims 4
- 229960000912 stanozolol Drugs 0.000 title claims 4
- 150000003839 salts Chemical class 0.000 claims 5
- 239000000017 hydrogel Substances 0.000 claims 3
- 230000003902 lesion Effects 0.000 claims 3
- 208000028185 Angioedema Diseases 0.000 claims 2
- 208000027418 Wounds and injury Diseases 0.000 claims 2
- 229910052783 alkali metal Inorganic materials 0.000 claims 2
- 150000001340 alkali metals Chemical class 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 238000002360 preparation method Methods 0.000 claims 2
- 208000009043 Chemical Burns Diseases 0.000 claims 1
- 206010011686 Cutaneous vasculitis Diseases 0.000 claims 1
- 206010052428 Wound Diseases 0.000 claims 1
- 239000007864 aqueous solution Substances 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 150000001768 cations Chemical class 0.000 claims 1
- 230000021615 conjugation Effects 0.000 claims 1
- 210000002808 connective tissue Anatomy 0.000 claims 1
- 239000006071 cream Substances 0.000 claims 1
- 230000006378 damage Effects 0.000 claims 1
- 230000003412 degenerative effect Effects 0.000 claims 1
- 239000000539 dimer Substances 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000000839 emulsion Substances 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 239000003889 eye drop Substances 0.000 claims 1
- 229940012356 eye drops Drugs 0.000 claims 1
- 239000006260 foam Substances 0.000 claims 1
- 239000001963 growth medium Substances 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 208000014674 injury Diseases 0.000 claims 1
- 210000003041 ligament Anatomy 0.000 claims 1
- 239000006210 lotion Substances 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 208000013441 ocular lesion Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 210000002435 tendon Anatomy 0.000 claims 1
- 201000005060 thrombophlebitis Diseases 0.000 claims 1
- 210000001519 tissue Anatomy 0.000 claims 1
- 230000000699 topical effect Effects 0.000 claims 1
- 230000000472 traumatic 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
- C08B37/0072—Hyaluronic acid, i.e. HA or hyaluronan; Derivatives thereof, e.g. crosslinked hyaluronic acid (hylan) or hyaluronates
-
- 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
- A61K47/56—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
- A61K47/61—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule the organic macromolecular compound being a polysaccharide or a derivative thereof
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
-
- 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
- A61K47/69—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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
- A61K47/6903—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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being semi-solid, e.g. an ointment, a gel, a hydrogel or a solidifying gel
-
- 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
- A61K9/0048—Eye, e.g. artificial tears
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
- A61L27/00—Materials for grafts or prostheses or for coating grafts or prostheses
- A61L27/14—Macromolecular materials
- A61L27/20—Polysaccharides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
- A61L27/00—Materials for grafts or prostheses or for coating grafts or prostheses
- A61L27/50—Materials characterised by their function or physical properties, e.g. injectable or lubricating compositions, shape-memory materials, surface modified materials
- A61L27/54—Biologically active materials, e.g. therapeutic substances
-
- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
- C08L5/00—Compositions of polysaccharides or of their derivatives not provided for in groups C08L1/00 or C08L3/00
- C08L5/08—Chitin; Chondroitin sulfate; Hyaluronic acid; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
- A61L2300/00—Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices
- A61L2300/40—Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices characterised by a specific therapeutic activity or mode of action
- A61L2300/43—Hormones, e.g. dexamethasone
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oral & Maxillofacial Surgery (AREA)
- Transplantation (AREA)
- Dermatology (AREA)
- Molecular Biology (AREA)
- Organic Chemistry (AREA)
- Polymers & Plastics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Ophthalmology & Optometry (AREA)
- Biochemistry (AREA)
- Materials Engineering (AREA)
- Biomedical Technology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Polysaccharides And Polysaccharide Derivatives (AREA)
- Cosmetics (AREA)
- Materials For Medical Uses (AREA)
Claims (8)
1. Konjugat između stanozolola i hialuronske kiseline ili soli hialuronske kiseline, naznačen time da stanozolol jest konjugiran s karboksilnom skupinom hialuronske kiseline ili soli hialuronske kiseline preko poveznice koju tvori esterska veza s hidroksilnom skupinom stanozolola te esterska ili amidna veza s karboksilnom skupinom hialuronske kiseline ili soli hialuronske kiseline.
2. Konjugat prema patentom zahtjevu 1, naznačen time da je stupanj konjugacije hialuronske kiseline u rasponu između 1 i 90% mol/mol s obzirom na broj ponavljajućih dimernih jedinica hialuronske kiseline ili njene soli.
3. Konjugat prema patentnim zahtjevima 1-2, prema formuli (I)
[image]
u kojoj:
n= 1-12,
X jest dvovalentna skupina odabrana od -O- i -NH-,
M+ je alkalni metal, proton ili kation,
skupina
[image]
je ponavljajuća jedinica hialuronske kiseline ili njene soli s alkallijskim metalom, gdje simbol * pokazuje ugljikov atom spomenute ponavljajuće jedinice vezan na skupinu X.
4. Konjugat prema patentom zahtjevu 3, naznačen time da X jest skupina -O-.
5. Farmaceutski i veterinarski pripravci koji sadrže konjugate iz patentnih zahtjeva 1-3 u smjesi s najmanje jednim nosačem ili ekscipijensom.
6. Pripravak prema patentom zahtjevu 5, u obliku hidrogelova, hidrogelova koji se mogu injektirati, hidrogelova za vanjsku upotrebu, krema, losiona, pjena, vodenih otopina za intraartikularnu upotrebu, emulzije za oftalmološku upotrebu ili očne kapi.
7. Matrice za uzgoj stanica, umjetna tkiva i mediji za kultiviranje sadrže konjugate iz patentnih zahtjeva 1-3.
8. Konjugati iz patentnih zahtjeva 1-3 za uporabu u topičkom liječenju osteohondralnih poremećaja i lezija, lezija tetive i ligamenta, degenerativnih procesa na vezivnim tkivima, ozljeda, rana, okularnih lezija, fizičkih i kemijskih opeklina, traumatskih lezija, angiodema ili Quinckeovog edema, kutanog vaskulitisa i tromboflebitisa.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IT102018000003841A IT201800003841A1 (it) | 2018-03-21 | 2018-03-21 | Coniugati di stanozololo e acido ialuronico |
| EP19721024.8A EP3768729B1 (en) | 2018-03-21 | 2019-03-13 | Conjugates of stanozolol and hyaluronic acid |
| PCT/IB2019/052034 WO2019180548A1 (en) | 2018-03-21 | 2019-03-13 | Conjugates of stanozolol and hyaluronic acid |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20220166T1 true HRP20220166T1 (hr) | 2022-04-29 |
Family
ID=62597894
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20220166TT HRP20220166T1 (hr) | 2018-03-21 | 2019-03-13 | Konjugati stanozolola i hialuronske kiseline |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US11013813B2 (hr) |
| EP (1) | EP3768729B1 (hr) |
| JP (1) | JP7301392B2 (hr) |
| KR (1) | KR20200135824A (hr) |
| CN (1) | CN111868097B (hr) |
| AU (1) | AU2019240175B2 (hr) |
| CA (1) | CA3094277A1 (hr) |
| CY (1) | CY1124939T1 (hr) |
| DK (1) | DK3768729T3 (hr) |
| ES (1) | ES2908887T3 (hr) |
| HR (1) | HRP20220166T1 (hr) |
| HU (1) | HUE058230T2 (hr) |
| IL (1) | IL277319B2 (hr) |
| IT (1) | IT201800003841A1 (hr) |
| LT (1) | LT3768729T (hr) |
| MX (1) | MX2020009680A (hr) |
| PL (1) | PL3768729T3 (hr) |
| PT (1) | PT3768729T (hr) |
| RS (1) | RS63033B1 (hr) |
| SI (1) | SI3768729T1 (hr) |
| WO (1) | WO2019180548A1 (hr) |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6107289A (en) * | 1992-04-21 | 2000-08-22 | The Schepens Eye Research Institute, Inc. | Ocular therapy in keratoconjunctivitis sicca using topically applied androgens or TGF-β |
| KR101234476B1 (ko) * | 2004-03-05 | 2013-02-18 | 덴끼 가가꾸 고교 가부시키가이샤 | 히알루론산/메토트렉세이트 화합물 |
| ITMI20061609A1 (it) * | 2006-08-10 | 2008-02-11 | Acme Drugs Srl | Formulazioni intrasinoviali di stanozololo |
| US20090202645A1 (en) | 2008-02-08 | 2009-08-13 | Acme Drugs S.R.L. | Intrasynovial formulations of stanozolol |
| CA2884142C (en) * | 2012-09-05 | 2020-11-10 | Chugai Seiyaku Kabushiki Kaisha | Hyaluronic acid derivative having amino acid and steryl group introduced thereinto |
-
2018
- 2018-03-21 IT IT102018000003841A patent/IT201800003841A1/it unknown
-
2019
- 2019-03-13 MX MX2020009680A patent/MX2020009680A/es unknown
- 2019-03-13 ES ES19721024T patent/ES2908887T3/es active Active
- 2019-03-13 AU AU2019240175A patent/AU2019240175B2/en active Active
- 2019-03-13 CA CA3094277A patent/CA3094277A1/en active Pending
- 2019-03-13 JP JP2020550101A patent/JP7301392B2/ja active Active
- 2019-03-13 HU HUE19721024A patent/HUE058230T2/hu unknown
- 2019-03-13 DK DK19721024.8T patent/DK3768729T3/da active
- 2019-03-13 SI SI201930172T patent/SI3768729T1/sl unknown
- 2019-03-13 LT LTEPPCT/IB2019/052034T patent/LT3768729T/lt unknown
- 2019-03-13 EP EP19721024.8A patent/EP3768729B1/en active Active
- 2019-03-13 KR KR1020207030033A patent/KR20200135824A/ko not_active Application Discontinuation
- 2019-03-13 PL PL19721024T patent/PL3768729T3/pl unknown
- 2019-03-13 PT PT197210248T patent/PT3768729T/pt unknown
- 2019-03-13 IL IL277319A patent/IL277319B2/en unknown
- 2019-03-13 CN CN201980020203.8A patent/CN111868097B/zh active Active
- 2019-03-13 US US16/981,810 patent/US11013813B2/en active Active
- 2019-03-13 WO PCT/IB2019/052034 patent/WO2019180548A1/en unknown
- 2019-03-13 RS RS20220225A patent/RS63033B1/sr unknown
- 2019-03-13 HR HRP20220166TT patent/HRP20220166T1/hr unknown
-
2022
- 2022-02-03 CY CY20221100093T patent/CY1124939T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2019240175A1 (en) | 2020-11-12 |
| KR20200135824A (ko) | 2020-12-03 |
| AU2019240175B2 (en) | 2024-05-02 |
| PT3768729T (pt) | 2022-03-11 |
| JP7301392B2 (ja) | 2023-07-03 |
| RS63033B1 (sr) | 2022-04-29 |
| WO2019180548A1 (en) | 2019-09-26 |
| SI3768729T1 (sl) | 2022-04-29 |
| ES2908887T3 (es) | 2022-05-04 |
| US11013813B2 (en) | 2021-05-25 |
| JP2021518378A (ja) | 2021-08-02 |
| IL277319A (en) | 2020-10-29 |
| PL3768729T3 (pl) | 2022-05-02 |
| CY1124939T1 (el) | 2023-01-05 |
| LT3768729T (lt) | 2022-05-25 |
| IT201800003841A1 (it) | 2019-09-21 |
| IL277319B2 (en) | 2024-02-01 |
| DK3768729T3 (da) | 2022-02-07 |
| CN111868097A (zh) | 2020-10-30 |
| IL277319B1 (en) | 2023-10-01 |
| EP3768729A1 (en) | 2021-01-27 |
| MX2020009680A (es) | 2020-10-12 |
| EP3768729B1 (en) | 2022-01-26 |
| HUE058230T2 (hu) | 2022-07-28 |
| US20210038735A1 (en) | 2021-02-11 |
| CN111868097B (zh) | 2023-06-06 |
| CA3094277A1 (en) | 2019-09-26 |
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