EA201591738A1 - Пиридиновые производные в качестве ингибиторов реаранжированной в процессе трансфекции (ret) киназы - Google Patents
Пиридиновые производные в качестве ингибиторов реаранжированной в процессе трансфекции (ret) киназыInfo
- Publication number
- EA201591738A1 EA201591738A1 EA201591738A EA201591738A EA201591738A1 EA 201591738 A1 EA201591738 A1 EA 201591738A1 EA 201591738 A EA201591738 A EA 201591738A EA 201591738 A EA201591738 A EA 201591738A EA 201591738 A1 EA201591738 A1 EA 201591738A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- cancer
- functional
- ret
- disorders
- constipation
- Prior art date
Links
Classifications
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- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/62—Oxygen or sulfur atoms
- C07D213/69—Two or more oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Peptides Or Proteins (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Abstract
Настоящее изобретение относится к новым соединениям, которые являются ингибиторами реаранжированной в процессе трансфекции (RET) киназы, к содержащим их фармацвтическим композициям, к способам их получения и к их применению в терапии, отдельно или в комбинации, для нормализации чувствительности, подвижности и/или секреции желудочно-кишечного тракта или и/или расстройств или заболеваний брюшной полости и/или лечения заболеваний, связанных с дисфункцией RET, или где модуляция RET активности может иметь терапевтический эффект, включая, но не ограничиваясь этим, все классификации синдрома раздраженной толстой кишки (IBS), включая тип дефекации с преобладанием диареи, с преобладанием запора или чередующийся тип, функциональное вздутие живота, функциональный запор, функциональную диарею, неопределенное функциональное расстройство кишечника, функциональный абдоминальный болевой синдром, хронический идиопатический запор, функциональные расстройства пищевода, функциональные гастродуоденальные расстройства, функциональную аноректальную боль, воспалительное заболевание кишечника, пролиферативные заболевания, такие как немелкоклеточный рак легкого, гепатоцеллюлярная карцинома, рак прямой кишки, медуллярный рак щитовидной железы, фолликулярный рак щитовидной железы, анапластический рак щитовидной железы, папиллярный рак щитовидной железы, опухоли головного мозга, рак брюшной полости, солидные опухоли, другие виды рака легких, рак головы и шеи, глиомы, нейробластомы, синдром Фон Гиппеля-Линдау и злокачественные опухоли почек, рак молочной железы, рак фаллопиевых труб, рак яичников, переходно-клеточный рак, рак предстательной
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013072683 | 2013-03-15 | ||
| CN2013090059 | 2013-12-20 | ||
| CN2014072449 | 2014-02-24 | ||
| PCT/IB2014/059817 WO2014141187A1 (en) | 2013-03-15 | 2014-03-14 | Pyridine derivatives as rearranged during transfection (ret) kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201591738A1 true EA201591738A1 (ru) | 2016-01-29 |
| EA029296B1 EA029296B1 (ru) | 2018-03-30 |
Family
ID=50390154
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201591738A EA029296B1 (ru) | 2013-03-15 | 2014-03-14 | Пиридиновые производные в качестве ингибиторов реаранжированной в процессе трансфекции (ret) киназы |
Country Status (33)
| Country | Link |
|---|---|
| US (2) | US9382238B2 (ru) |
| EP (1) | EP2970191B1 (ru) |
| JP (1) | JP2016516026A (ru) |
| CN (1) | CN105051027A (ru) |
| AU (1) | AU2014229233B2 (ru) |
| BR (1) | BR112015023618A2 (ru) |
| CA (1) | CA2905627A1 (ru) |
| CL (1) | CL2015002514A1 (ru) |
| CR (1) | CR20150490A (ru) |
| CY (1) | CY1118730T1 (ru) |
| DK (1) | DK2970191T3 (ru) |
| DO (1) | DOP2015000244A (ru) |
| EA (1) | EA029296B1 (ru) |
| ES (1) | ES2616655T3 (ru) |
| HR (1) | HRP20170363T1 (ru) |
| HU (1) | HUE033423T2 (ru) |
| IL (1) | IL241161A0 (ru) |
| LT (1) | LT2970191T (ru) |
| ME (1) | ME02664B (ru) |
| MX (1) | MX2015012286A (ru) |
| NZ (1) | NZ628388A (ru) |
| PE (1) | PE20151538A1 (ru) |
| PH (1) | PH12015502044A1 (ru) |
| PL (1) | PL2970191T3 (ru) |
| PT (1) | PT2970191T (ru) |
| RS (1) | RS55710B1 (ru) |
| SG (1) | SG11201506695UA (ru) |
| SI (1) | SI2970191T1 (ru) |
| SM (1) | SMT201700152T1 (ru) |
| TW (1) | TW201524958A (ru) |
| UA (1) | UA115264C2 (ru) |
| UY (1) | UY35465A (ru) |
| WO (1) | WO2014141187A1 (ru) |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2628418T3 (es) | 2010-05-20 | 2017-08-02 | Array Biopharma, Inc. | Compuestos macrocíclicos como inhibidores de la TRK cinasa |
| EP3191480A1 (en) * | 2014-09-08 | 2017-07-19 | GlaxoSmithKline Intellectual Property Development Limited | Crystalline forms of 2-(4-(4-ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fluorophenyl)-n-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)acetamide |
| JP6538153B2 (ja) | 2014-09-10 | 2019-07-03 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ | Ｒｅａｒｒａｎｇｅｄ ｄｕｒｉｎｇ ｔｒａｎｓｆｅｃｔｉｏｎ（ｒｅｔ）阻害剤としての新規な化合物 |
| SI3191450T1 (sl) | 2014-09-10 | 2019-07-31 | Glaxosmithkline Intellectual Property Development Limited | Piridonski derivati kot preurejeni med transfekcijo (RET) inhibitorjev kinaze |
| WO2016127074A1 (en) | 2015-02-06 | 2016-08-11 | Blueprint Medicines Corporation | 2-(pyridin-3-yl)-pyrimidine derivatives as ret inhibitors |
| KR20180041135A (ko) | 2015-07-16 | 2018-04-23 | 어레이 바이오파마 인크. | Ret 키나아제 억제제로서 치환된 피라졸로[1,5-a]피리딘 화합물 |
| WO2017019804A2 (en) | 2015-07-28 | 2017-02-02 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| HUE064659T2 (hu) * | 2015-11-02 | 2024-04-28 | Blueprint Medicines Corp | RET inhibitorai |
| WO2017145050A1 (en) | 2016-02-23 | 2017-08-31 | Glaxosmithkline Intellectual Property Development Limited | Pyridylpyridone derivative useful as a ret kinase inhibitor in the treatment of ibs and cancer |
| EP3430005B1 (en) * | 2016-03-16 | 2021-12-08 | Plexxikon Inc. | Compounds and methods for kinase modulation and indications therefore |
| TW201738228A (zh) | 2016-03-17 | 2017-11-01 | 藍圖醫藥公司 | Ｒｅｔ之抑制劑 |
| BR112018073300A2 (pt) | 2016-05-13 | 2019-03-26 | Instituto De Medicina Molecular | métodos para tratamento de doenças associadas com as células ilc3 |
| WO2018017983A1 (en) | 2016-07-22 | 2018-01-25 | Blueprint Medicines Corporation | Compounds useful for treating disorders related to ret |
| JP2018052878A (ja) | 2016-09-29 | 2018-04-05 | 第一三共株式会社 | ピリジン化合物 |
| JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| JP6888101B2 (ja) | 2017-01-18 | 2021-06-16 | アレイ バイオファーマ インコーポレイテッド | ＲＥＴキナーゼ阻害剤としての置換ピラゾロ［１，５−ａ］ピラジン化合物 |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| WO2018213329A1 (en) | 2017-05-15 | 2018-11-22 | Blueprint Medicines Corporation | Combinations of ret inhibitors and mtorc1 inhibitors and uses thereof for the treatment of cancer mediated by aberrant ret activity |
| US10093648B1 (en) * | 2017-09-22 | 2018-10-09 | Celgene Corporation | Crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione hemihydrate, compositions and methods of use thereof |
| TW202410896A (zh) * | 2017-10-10 | 2024-03-16 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
| TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
| TWI802635B (zh) | 2018-01-18 | 2023-05-21 | 美商亞雷生物製藥股份有限公司 | 作為ｒｅｔ激酶抑制劑之經取代吡咯并[2,3-d]嘧啶化合物 |
| JP6997876B2 (ja) | 2018-01-18 | 2022-02-04 | アレイ バイオファーマ インコーポレイテッド | Ｒｅｔキナーゼ阻害剤としての置換ピラゾリル［４，３－ｃ］ピリジン化合物 |
| TW201938169A (zh) | 2018-01-18 | 2019-10-01 | 美商亞雷生物製藥股份有限公司 | 作為RET激酶抑制劑之經取代吡唑并[3,4-d]嘧啶化合物 |
| EP4353317A3 (en) | 2018-04-03 | 2024-05-08 | Blueprint Medicines Corporation | Ret inhibitor for use in treating cancer having a ret alteration |
| CN109096264B (zh) * | 2018-08-28 | 2019-08-23 | 山东理工职业学院 | Ret抑制剂及其制备方法、组合物和用途 |
| CN112996794A (zh) | 2018-09-10 | 2021-06-18 | 阿雷生物药品公司 | 作为ret激酶抑制剂的稠合杂环化合物 |
| CA3137152A1 (en) | 2019-04-18 | 2020-10-22 | The Johns Hopkins University | Substituted 2-amino-pyrazolyl-[1,2,4]triazolo[1,5a] pyridine derivatives and use thereof |
| WO2021164742A1 (zh) * | 2020-02-20 | 2021-08-26 | 广州白云山医药集团股份有限公司白云山制药总厂 | 喹啉类化合物 |
| TWI777509B (zh) | 2020-04-27 | 2022-09-11 | 美商美國禮來大藥廠 | 用於抑制ret激酶之化合物 |
| WO2022017524A1 (zh) * | 2020-07-23 | 2022-01-27 | 深圳晶泰科技有限公司 | 吡啶酮类化合物及其制备方法和应用 |
| MX2023005289A (es) | 2020-11-06 | 2023-07-26 | Lilly Co Eli | Derivados de pirazol como inhibidores de la ret-cinasa. |
| WO2022254255A1 (en) | 2021-06-03 | 2022-12-08 | Fundacao D. Anna De Sommerchampalimaud E Dr. | Neuro-mesenchyme units control ilc2 and obesity via a brain-adipose circuit |
| CN115626880B (zh) * | 2022-11-15 | 2023-11-14 | 常州大学 | 3-硝基-5-氰基三氟甲苯的合成方法 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CZ2002422A3 (cs) | 1999-08-12 | 2002-11-13 | Pharmacia Italia S. P. A. | 3(5)-Aminopyrazolové deriváty, způsob jejich přípravy a jejich pouľití jako protinádorová činidla |
| MXPA03004644A (es) * | 2000-11-27 | 2003-09-05 | Pharmacia Italia Spa | Derivados de fenilacetamdia-pirazol y su uso como agentes antitumorales. |
| DE10201764A1 (de) | 2002-01-18 | 2003-07-31 | Bayer Cropscience Ag | Substituierte 4-Aminopyridin-Derivate |
| US7968574B2 (en) | 2004-12-28 | 2011-06-28 | Kinex Pharmaceuticals, Llc | Biaryl compositions and methods for modulating a kinase cascade |
| KR20090064602A (ko) * | 2006-10-16 | 2009-06-19 | 노파르티스 아게 | 단백질 키나제 억제제로서 유용한 페닐아세트아미드 |
| EP3048099A3 (en) * | 2006-11-15 | 2016-09-21 | YM BioSciences Australia Pty Ltd | Inhibitors of kinase activity |
| KR20120059558A (ko) | 2009-08-19 | 2012-06-08 | 암비트 바이오사이언시즈 코포레이션 | 바이아릴 화합물 및 이의 사용 방법 |
| EP2651930B1 (en) | 2010-12-16 | 2015-10-28 | Boehringer Ingelheim International GmbH | Biarylamide inhibitors of leukotriene production |
| US8937071B2 (en) | 2013-03-15 | 2015-01-20 | Glaxosmithkline Intellectual Property Development Limited | Compounds as rearranged during transfection (RET) inhibitors |
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2014
- 2014-03-14 TW TW103109315A patent/TW201524958A/zh unknown
- 2014-03-14 CA CA2905627A patent/CA2905627A1/en not_active Abandoned
- 2014-03-14 HU HUE14713598A patent/HUE033423T2/en unknown
- 2014-03-14 JP JP2015562529A patent/JP2016516026A/ja active Pending
- 2014-03-14 ES ES14713598.2T patent/ES2616655T3/es active Active
- 2014-03-14 PE PE2015001878A patent/PE20151538A1/es not_active Application Discontinuation
- 2014-03-14 UY UY0001035465A patent/UY35465A/es unknown
- 2014-03-14 BR BR112015023618A patent/BR112015023618A2/pt not_active IP Right Cessation
- 2014-03-14 PL PL14713598T patent/PL2970191T3/pl unknown
- 2014-03-14 NZ NZ628388A patent/NZ628388A/en not_active IP Right Cessation
- 2014-03-14 WO PCT/IB2014/059817 patent/WO2014141187A1/en active Application Filing
- 2014-03-14 UA UAA201510041A patent/UA115264C2/uk unknown
- 2014-03-14 PT PT147135982T patent/PT2970191T/pt unknown
- 2014-03-14 SG SG11201506695UA patent/SG11201506695UA/en unknown
- 2014-03-14 EP EP14713598.2A patent/EP2970191B1/en active Active
- 2014-03-14 ME MEP-2017-60A patent/ME02664B/me unknown
- 2014-03-14 MX MX2015012286A patent/MX2015012286A/es unknown
- 2014-03-14 LT LTEP14713598.2T patent/LT2970191T/lt unknown
- 2014-03-14 SI SI201430170A patent/SI2970191T1/sl unknown
- 2014-03-14 SM SM20170152T patent/SMT201700152T1/it unknown
- 2014-03-14 RS RS20170177A patent/RS55710B1/sr unknown
- 2014-03-14 CN CN201480015907.3A patent/CN105051027A/zh active Pending
- 2014-03-14 US US14/775,772 patent/US9382238B2/en not_active Expired - Fee Related
- 2014-03-14 EA EA201591738A patent/EA029296B1/ru not_active IP Right Cessation
- 2014-03-14 AU AU2014229233A patent/AU2014229233B2/en not_active Ceased
- 2014-03-14 DK DK14713598.2T patent/DK2970191T3/en active
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2015
- 2015-09-03 IL IL241161A patent/IL241161A0/en unknown
- 2015-09-08 CL CL2015002514A patent/CL2015002514A1/es unknown
- 2015-09-10 PH PH12015502044A patent/PH12015502044A1/en unknown
- 2015-09-14 CR CR20150490A patent/CR20150490A/es unknown
- 2015-09-15 DO DO2015000244A patent/DOP2015000244A/es unknown
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2016
- 2016-06-02 US US15/171,229 patent/US9789100B2/en not_active Expired - Fee Related
-
2017
- 2017-03-06 HR HRP20170363TT patent/HRP20170363T1/hr unknown
- 2017-03-14 CY CY20171100319T patent/CY1118730T1/el unknown
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| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG TJ TM RU |