TR201808818T4 - Gip reseptör aktivitesi sergileyen glukagon analogları. - Google Patents
Gip reseptör aktivitesi sergileyen glukagon analogları. Download PDFInfo
- Publication number
- TR201808818T4 TR201808818T4 TR2018/08818T TR201808818T TR201808818T4 TR 201808818 T4 TR201808818 T4 TR 201808818T4 TR 2018/08818 T TR2018/08818 T TR 2018/08818T TR 201808818 T TR201808818 T TR 201808818T TR 201808818 T4 TR201808818 T4 TR 201808818T4
- Authority
- TR
- Turkey
- Prior art keywords
- amino acid
- peptide
- ala
- seq
- acetyl
- Prior art date
Links
- MASNOZXLGMXCHN-ZLPAWPGGSA-N glucagon Chemical class C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=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](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)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(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 MASNOZXLGMXCHN-ZLPAWPGGSA-N 0.000 title claims abstract 6
- 230000000694 effects Effects 0.000 title claims abstract 4
- 108020003175 receptors Proteins 0.000 title claims 3
- 102000005962 receptors Human genes 0.000 title claims 3
- 230000001747 exhibiting effect Effects 0.000 title 1
- 108010036598 gastric inhibitory polypeptide receptor Proteins 0.000 claims abstract 4
- 206010012601 diabetes mellitus Diseases 0.000 claims abstract 2
- 108090000765 processed proteins & peptides Proteins 0.000 claims 31
- 150000001413 amino acids Chemical class 0.000 claims 30
- -1 Acetyl D-His Chemical compound 0.000 claims 15
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 238000012986 modification Methods 0.000 claims 6
- 230000004048 modification Effects 0.000 claims 6
- 230000002378 acidificating effect Effects 0.000 claims 5
- 239000000539 dimer Substances 0.000 claims 5
- 101001015516 Homo sapiens Glucagon-like peptide 1 receptor Proteins 0.000 claims 4
- 125000003892 C18 acyl group Chemical group 0.000 claims 3
- HNDVDQJCIGZPNO-RXMQYKEDSA-N D-histidine Chemical compound OC(=O)[C@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-RXMQYKEDSA-N 0.000 claims 2
- 102000051325 Glucagon Human genes 0.000 claims 2
- 108060003199 Glucagon Proteins 0.000 claims 2
- 101000886868 Homo sapiens Gastric inhibitory polypeptide Proteins 0.000 claims 2
- 239000000556 agonist Substances 0.000 claims 2
- 229960004666 glucagon Drugs 0.000 claims 2
- 102000050325 human granulocyte inhibitory Human genes 0.000 claims 2
- FSYKKLYZXJSNPZ-UHFFFAOYSA-N sarcosine Chemical compound C[NH2+]CC([O-])=O FSYKKLYZXJSNPZ-UHFFFAOYSA-N 0.000 claims 2
- 230000004584 weight gain Effects 0.000 claims 2
- 235000019786 weight gain Nutrition 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- UKAUYVFTDYCKQA-UHFFFAOYSA-N -2-Amino-4-hydroxybutanoic acid Natural products OC(=O)C(N)CCO UKAUYVFTDYCKQA-UHFFFAOYSA-N 0.000 claims 1
- SCOZOHWKTFBYNS-UHFFFAOYSA-N 2,2-diamino-3-methyl-4-oxopentanoic acid Chemical compound CC(=O)C(C)C(N)(N)C(O)=O SCOZOHWKTFBYNS-UHFFFAOYSA-N 0.000 claims 1
- 125000001433 C-terminal amino-acid group Chemical group 0.000 claims 1
- 101100294115 Caenorhabditis elegans nhr-4 gene Proteins 0.000 claims 1
- OUYCCCASQSFEME-MRVPVSSYSA-N D-tyrosine Chemical compound OC(=O)[C@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-MRVPVSSYSA-N 0.000 claims 1
- 101001040075 Homo sapiens Glucagon receptor Proteins 0.000 claims 1
- UKAUYVFTDYCKQA-VKHMYHEASA-N L-homoserine Chemical compound OC(=O)[C@@H](N)CCO UKAUYVFTDYCKQA-VKHMYHEASA-N 0.000 claims 1
- QEFRNWWLZKMPFJ-ZXPFJRLXSA-N L-methionine (R)-S-oxide Chemical compound C[S@@](=O)CC[C@H]([NH3+])C([O-])=O QEFRNWWLZKMPFJ-ZXPFJRLXSA-N 0.000 claims 1
- UCUNFLYVYCGDHP-BYPYZUCNSA-N L-methionine sulfone Chemical compound CS(=O)(=O)CC[C@H](N)C(O)=O UCUNFLYVYCGDHP-BYPYZUCNSA-N 0.000 claims 1
- QEFRNWWLZKMPFJ-UHFFFAOYSA-N L-methionine sulphoxide Natural products CS(=O)CCC(N)C(O)=O QEFRNWWLZKMPFJ-UHFFFAOYSA-N 0.000 claims 1
- SNDPXSYFESPGGJ-UHFFFAOYSA-N L-norVal-OH Natural products CCCC(N)C(O)=O SNDPXSYFESPGGJ-UHFFFAOYSA-N 0.000 claims 1
- UEQUQVLFIPOEMF-UHFFFAOYSA-N Mianserin Chemical compound C1C2=CC=CC=C2N2CCN(C)CC2C2=CC=CC=C21 UEQUQVLFIPOEMF-UHFFFAOYSA-N 0.000 claims 1
- 108010077895 Sarcosine Proteins 0.000 claims 1
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 claims 1
- 125000001931 aliphatic group Chemical group 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000002209 hydrophobic effect Effects 0.000 claims 1
- 230000001939 inductive effect Effects 0.000 claims 1
- 125000002347 octyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 102000004196 processed proteins & peptides Human genes 0.000 claims 1
- 229940043230 sarcosine Drugs 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 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
- 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
- A61K38/26—Glucagons
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
-
- 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
- A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
-
- 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)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Zoology (AREA)
- Gastroenterology & Hepatology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Toxicology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Measuring Pulse, Heart Rate, Blood Pressure Or Blood Flow (AREA)
- Measurement And Recording Of Electrical Phenomena And Electrical Characteristics Of The Living Body (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261662874P | 2012-06-21 | 2012-06-21 | |
| US201361787973P | 2013-03-15 | 2013-03-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TR201808818T4 true TR201808818T4 (tr) | 2018-07-23 |
Family
ID=48692696
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TR2018/08818T TR201808818T4 (tr) | 2012-06-21 | 2013-06-18 | Gip reseptör aktivitesi sergileyen glukagon analogları. |
Country Status (30)
Families Citing this family (45)
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| ES2640916T3 (es) | 2012-04-26 | 2017-11-07 | Bristol-Myers Squibb Company | Derivados de imidazotiadiazol e imidazopirazina como inhibidores del receptor 4 activados por proteasa (PAR4) para tratar agregación plaquetaria |
| SI2864350T1 (en) * | 2012-06-21 | 2018-08-31 | Indiana University Research And Technology Corporation | GLUCAGON ANALOGUE ANALOGUE WITH ACTIVITY OF GIP RECEPTOR |
| UA116217C2 (uk) | 2012-10-09 | 2018-02-26 | Санофі | Пептидна сполука як подвійний агоніст рецепторів glp1-1 та глюкагону |
| HUE035803T2 (en) | 2012-12-21 | 2018-05-28 | Sanofi Sa | Dual GLP1 / GIP or trigonal GLP1 / GIP / glucagon agonists |
| DK3004155T3 (da) | 2013-05-28 | 2022-01-03 | Takeda Pharmaceuticals Co | Peptidforbindelse |
| WO2015086730A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Non-acylated exendin-4 peptide analogues |
| TW201609797A (zh) | 2013-12-13 | 2016-03-16 | 賽諾菲公司 | 雙重ｇｌｐ－１／升糖素受體促效劑 |
| WO2015086728A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Exendin-4 peptide analogues as dual glp-1/gip receptor agonists |
| EP3080154B1 (en) | 2013-12-13 | 2018-02-07 | Sanofi | Dual glp-1/gip receptor agonists |
| US10137170B2 (en) | 2013-12-20 | 2018-11-27 | Indiana University Research And Technology Corporation | Lipidated incretin receptor ligand human immunoglobulin Fc-region fusion polypeptides |
| TW201625669A (zh) * | 2014-04-07 | 2016-07-16 | 賽諾菲公司 | 衍生自艾塞那肽－４（Ｅｘｅｎｄｉｎ－４）之肽類雙重ＧＬＰ－１／升糖素受體促效劑 |
| TW201625670A (zh) * | 2014-04-07 | 2016-07-16 | 賽諾菲公司 | 衍生自ｅｘｅｎｄｉｎ－４之雙重ｇｌｐ－１／升糖素受體促效劑 |
| TW201625668A (zh) | 2014-04-07 | 2016-07-16 | 賽諾菲公司 | 作為胜肽性雙重ｇｌｐ－１／昇糖素受體激動劑之艾塞那肽－４衍生物 |
| US9932381B2 (en) | 2014-06-18 | 2018-04-03 | Sanofi | Exendin-4 derivatives as selective glucagon receptor agonists |
| JP6581656B2 (ja) | 2014-10-24 | 2019-09-25 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | グルカゴンおよびｇｌｐ−１受容体のコアゴニスト |
| KR102291020B1 (ko) | 2014-12-30 | 2021-08-20 | 한미약품 주식회사 | 안정성이 증가된 글루카곤 유도체 |
| AR105319A1 (es) | 2015-06-05 | 2017-09-27 | Sanofi Sa | Profármacos que comprenden un conjugado agonista dual de glp-1 / glucagón conector ácido hialurónico |
| FI3322437T3 (fi) | 2015-06-30 | 2024-02-20 | Hanmi Pharmaceutical Co Ltd | Glukagonijohdannainen ja sen pitkävaikutteisen konjugaatin käsittävä koostumus |
| TW201706291A (zh) | 2015-07-10 | 2017-02-16 | 賽諾菲公司 | 作為選擇性肽雙重ｇｌｐ－１／升糖素受體促效劑之新毒蜥外泌肽（ｅｘｅｎｄｉｎ－４）衍生物 |
| TWI622596B (zh) | 2015-10-26 | 2018-05-01 | 美國禮來大藥廠 | 升糖素受體促效劑 |
| AU2016379403B2 (en) | 2015-12-23 | 2020-03-12 | The Johns Hopkins University | Long-acting GLP-1r agonist as a therapy of neurological and neurodegenerative conditions |
| JP6712323B2 (ja) * | 2015-12-31 | 2020-06-17 | ハンミ ファーマシューティカル カンパニー リミテッド | グルカゴン、ｇｌｐ−１及びｇｉｐ受容体のすべてに活性を有する三重活性体 |
| EP3467106B1 (en) | 2016-05-24 | 2025-07-09 | Takeda Pharmaceutical Company Limited | Peptide compound |
| CN122440793A (zh) | 2016-06-29 | 2026-07-24 | 韩美药品株式会社 | 胰高血糖素衍生物、其缀合物、包含其的组合物、和其治疗用途 |
| AR110300A1 (es) | 2016-12-02 | 2019-03-13 | Sanofi Sa | Compuestos como agonistas peptídicos trigonales de los receptores de glp1 / glucagón / gip |
| AR110301A1 (es) | 2016-12-02 | 2019-03-13 | Sanofi Sa | Compuestos como agonistas peptídicos de receptores de glp1 / glucagón / gip |
| JOP20190211A1 (ar) | 2017-03-31 | 2019-09-15 | Takeda Pharmaceuticals Co | ببتيد منشط لمستقبل gip |
| CN115304666B (zh) * | 2017-11-24 | 2025-09-19 | 浙江道尔生物科技有限公司 | 一种治疗代谢疾病的胰高血糖素类似物 |
| MX2020010716A (es) | 2018-04-10 | 2021-03-09 | Sanofi Aventis Deutschland | Metodo para escindir de la fase solida peptidos unidos a una fase solida. |
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| PE20210473A1 (es) * | 2018-05-04 | 2021-03-08 | Novo Nordisk As | Derivados de gip y usos de estos |
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| ES3068975T3 (en) * | 2018-07-23 | 2026-06-03 | Lilly Co Eli | Gip/glp1 co-agonist compounds |
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| CN113493503B (zh) * | 2020-04-08 | 2022-08-05 | 浙江道尔生物科技有限公司 | 一种肠促胰岛素类似物及其制备方法和用途 |
| AU2021312323A1 (en) | 2020-07-22 | 2023-02-02 | Novo Nordisk A/S | Co-agonists at GLP-1 and GIP receptors suitable for oral delivery |
| CN114621327B (zh) * | 2020-12-10 | 2023-08-18 | 江苏中新医药有限公司 | GLP-1、GIP和Gcg多重受体激动蛋白质 |
| US20240059752A1 (en) | 2020-12-23 | 2024-02-22 | Zhejiang Doer Biologics Co., Ltd. | Long-acting glucagon derivative |
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| WO2010148089A1 (en) * | 2009-06-16 | 2010-12-23 | Indiana University Research And Technology Corporation | Gip receptor-active glucagon compounds |
| KR20120123443A (ko) | 2010-01-27 | 2012-11-08 | 인디애나 유니버시티 리서치 앤드 테크놀로지 코퍼레이션 | 대사 장애 및 비만 치료용 글루카곤 길항제-ｇｉｐ 항진제 콘쥬게이트 |
| ES2661228T3 (es) * | 2010-05-13 | 2018-03-28 | Indiana University Research And Technology Corporation | Péptidos de la superfamilia de glucagón que muestran actividad de receptor nuclear de hormona |
| US8778872B2 (en) * | 2010-06-24 | 2014-07-15 | Indiana University Research And Technology Corporation | Amide based glucagon superfamily peptide prodrugs |
| CN103857408B (zh) * | 2011-06-22 | 2017-04-12 | 印第安那大学科技研究公司 | 胰高血糖素/glp‑1受体协同激动剂 |
| JP6184404B2 (ja) * | 2011-06-22 | 2017-08-23 | インディアナ ユニヴァーシティ リサーチ アンド テクノロジー コーポレイション | グルカゴン／ｇｌｐ−１レセプターコアゴニスト |
| SI2864350T1 (en) * | 2012-06-21 | 2018-08-31 | Indiana University Research And Technology Corporation | GLUCAGON ANALOGUE ANALOGUE WITH ACTIVITY OF GIP RECEPTOR |
| CN108271356A (zh) * | 2014-09-24 | 2018-07-10 | 印第安纳大学研究及科技有限公司 | 肠降血糖素-胰岛素缀合物 |
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2013
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- 2013-06-18 KR KR20157001447A patent/KR20150039748A/ko not_active Abandoned
- 2013-06-18 BR BR112014031671A patent/BR112014031671A2/pt not_active Application Discontinuation
- 2013-06-18 ES ES13731246.8T patent/ES2674946T3/es active Active
- 2013-06-18 US US14/408,813 patent/US9868772B2/en not_active Expired - Fee Related
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- 2013-06-18 CA CA2877127A patent/CA2877127A1/en not_active Abandoned
- 2013-06-18 WO PCT/US2013/046229 patent/WO2013192130A1/en not_active Ceased
- 2013-06-18 RS RS20180728A patent/RS57347B1/sr unknown
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- 2013-06-18 DK DK13731246.8T patent/DK2864350T3/en active
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- 2013-06-18 AU AU2013277372A patent/AU2013277372B2/en not_active Ceased
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- 2013-06-18 MY MYPI2014003510A patent/MY185217A/en unknown
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- 2013-06-18 CN CN201380043984.5A patent/CN104583233B/zh not_active Expired - Fee Related
- 2013-06-18 EP EP13731246.8A patent/EP2864350B1/en not_active Not-in-force
- 2013-06-18 EA EA201590065A patent/EA029025B1/ru not_active IP Right Cessation
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2015
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