UA110838C2 - 4-(8-МЕТОКСИ-1-(1-МЕТОКСИПРОПАН-2-ІЛ)-2-(ТЕТРАГІДРО-2H-ПІРАН-4-ІЛ)-1H-ІМІДАЗО[4,5-c]ХІНОЛІН-7-ІЛ)-3,5-ДИМЕТИЛІЗОКСАЗОЛ ТА ЙОГО ЗАСТОСУВАННЯ ЯК ІНГІБІТОРА БРОМОДОМЕНУ - Google Patents
4-(8-МЕТОКСИ-1-(1-МЕТОКСИПРОПАН-2-ІЛ)-2-(ТЕТРАГІДРО-2H-ПІРАН-4-ІЛ)-1H-ІМІДАЗО[4,5-c]ХІНОЛІН-7-ІЛ)-3,5-ДИМЕТИЛІЗОКСАЗОЛ ТА ЙОГО ЗАСТОСУВАННЯ ЯК ІНГІБІТОРА БРОМОДОМЕНУInfo
- Publication number
- UA110838C2 UA110838C2 UAA201400590A UAA201400590A UA110838C2 UA 110838 C2 UA110838 C2 UA 110838C2 UA A201400590 A UAA201400590 A UA A201400590A UA A201400590 A UAA201400590 A UA A201400590A UA 110838 C2 UA110838 C2 UA 110838C2
- Authority
- UA
- Ukraine
- Prior art keywords
- methoxy
- tssch
- dymetylizoksazol
- bromodomenu
- imidazo
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1114103.3A GB201114103D0 (en) | 2011-08-17 | 2011-08-17 | Novel compounds |
| PCT/EP2012/065918 WO2013024104A1 (en) | 2011-08-17 | 2012-08-15 | 4-(8-methoxy-1-((1-methoxypropan-2-yl)-2-(tetrahydro-2h-pyran-4-yl)-1 h-imidazo[4,5-c]quinolin-7-yl)-3,5-dimethylisoxazole and its use as bromodomain inhibitor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| UA110838C2 true UA110838C2 (uk) | 2016-02-25 |
Family
ID=44764570
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| UAA201400590A UA110838C2 (uk) | 2011-08-17 | 2012-08-15 | 4-(8-МЕТОКСИ-1-(1-МЕТОКСИПРОПАН-2-ІЛ)-2-(ТЕТРАГІДРО-2H-ПІРАН-4-ІЛ)-1H-ІМІДАЗО[4,5-c]ХІНОЛІН-7-ІЛ)-3,5-ДИМЕТИЛІЗОКСАЗОЛ ТА ЙОГО ЗАСТОСУВАННЯ ЯК ІНГІБІТОРА БРОМОДОМЕНУ |
Country Status (38)
Families Citing this family (56)
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| US9249161B2 (en) | 2010-12-02 | 2016-02-02 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| AR084070A1 (es) | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
| WO2012151512A2 (en) | 2011-05-04 | 2012-11-08 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| EP2721031B1 (en) | 2011-06-17 | 2016-01-20 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| GB201114103D0 (en) | 2011-08-17 | 2011-09-28 | Glaxosmithkline Llc | Novel compounds |
| TWI602820B (zh) | 2012-06-06 | 2017-10-21 | 星宿藥物公司 | 溴域抑制劑及其用途 |
| US9624244B2 (en) | 2012-06-06 | 2017-04-18 | Constellation Pharmaceuticals, Inc. | Benzo [B] isoxazoloazepine bromodomain inhibitors and uses thereof |
| US9073878B2 (en) | 2012-11-21 | 2015-07-07 | Zenith Epigenetics Corp. | Cyclic amines as bromodomain inhibitors |
| WO2014080291A2 (en) | 2012-11-21 | 2014-05-30 | Rvx Therapeutics Inc. | Biaryl derivatives as bromodomain inhibitors |
| AU2013365926B9 (en) | 2012-12-21 | 2019-01-17 | Zenith Epigenetics Ltd. | Novel heterocyclic compounds as bromodomain inhibitors |
| WO2014164771A1 (en) * | 2013-03-11 | 2014-10-09 | Abbvie Inc. | Bromodomain inhibitors |
| AU2014249192B2 (en) | 2013-03-11 | 2017-12-21 | The Regents Of The University Of Michigan | BET bromodomain inhibitors and therapeutic methods using the same |
| AU2014249034A1 (en) | 2013-03-11 | 2015-09-24 | Abbvie Inc. | Fused tetracyclic bromodomain inhibitors |
| UA119848C2 (uk) | 2013-03-15 | 2019-08-27 | Інсайт Холдинґс Корпорейшн | Трициклічні гетероцикли як інгібітори білків бет |
| TWI530499B (zh) * | 2013-03-28 | 2016-04-21 | 吉李德科學股份有限公司 | 作為溴結構域（ｂｒｏｍｏｄｏｍａｉｎ）抑制劑之苯並咪唑酮衍生物類 |
| KR102307566B1 (ko) | 2013-06-21 | 2021-10-05 | 제니쓰 에피제네틱스 리미티드 | 신규한 바이사이클릭 브로모도메인 억제제 |
| CA2915622C (en) | 2013-06-21 | 2020-08-18 | Zenith Epigenetics Corp. | Novel substituted bicyclic compounds as bromodomain inhibitors |
| JP2016523964A (ja) | 2013-07-08 | 2016-08-12 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｂｅｔタンパク質阻害剤としての三環式複素環 |
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| WO2015049629A1 (en) * | 2013-10-01 | 2015-04-09 | Piramal Enterprises Limited | Imidazoquinoline compounds as bromodomain inhibitors |
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| US9315501B2 (en) | 2013-11-26 | 2016-04-19 | Incyte Corporation | Bicyclic heterocycles as BET protein inhibitors |
| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| CN107074861A (zh) | 2014-02-28 | 2017-08-18 | 密执安大学评议会 | 作为bet溴结构域抑制剂的9h嘧啶并[4，5‑b]吲哚和相关类似物 |
| AU2015249810B2 (en) | 2014-04-23 | 2019-04-18 | Incyte Holdings Corporation | 1H-pyrrolo[2,3-c]pyridin-7(6H)-ones and pyrazolo[3,4-c]pyridin-7(6H)-ones as inhibitors of BET proteins |
| PT3157928T (pt) | 2014-06-20 | 2019-05-30 | Constellation Pharmaceuticals Inc | Formas cristalinas de 2-((4s)-6-(4-clorofenil)-1-metil-4h-benzo[c] isoxazolo[4,5-e]azepin-4-il)acetamida |
| ES2855225T3 (es) | 2014-09-15 | 2021-09-23 | Incyte Corp | Heterociclos tricíclicos para su uso como inhibidores de proteínas BET |
| HK1246273B (en) | 2014-12-01 | 2019-12-06 | 恒翼生物医药(上海)股份有限公司 | Substituted pyridines as bromodomain inhibitors |
| CA2966298A1 (en) | 2014-12-01 | 2016-06-09 | Zenith Epigenetics Ltd. | Substituted pyridinones as bromodomain inhibitors |
| JP2017537946A (ja) | 2014-12-11 | 2017-12-21 | ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． | ブロモドメイン阻害剤としての置換複素環 |
| JP2017538721A (ja) | 2014-12-17 | 2017-12-28 | ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． | ブロモドメインの阻害剤 |
| EP3253756B1 (en) * | 2015-02-03 | 2021-09-22 | Trillium Therapeutics Inc. | Fluorinated imidazo[4,5-c]quinoline derivatives as inhibitors of bromodomain containing proteins |
| WO2016138332A1 (en) | 2015-02-27 | 2016-09-01 | The Regents Of The University Of Michigan | 9h-pyrimido [4,5-b] indoles as bet bromodomain inhibitors |
| GB201504694D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Covalent conjugates |
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| WO2016196065A1 (en) | 2015-05-29 | 2016-12-08 | Genentech, Inc. | Methods and compositions for assessing responsiveness of cancers to bet inhibitors |
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| WO2017024406A1 (en) | 2015-08-11 | 2017-02-16 | Neomed Institute | N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals |
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| EP3416969B1 (en) | 2016-02-15 | 2021-05-05 | The Regents of The University of Michigan | Fused 1,4-oxazepines and related analogs as bet bromodomain inhibitors |
| JP7037500B2 (ja) | 2016-04-06 | 2022-03-16 | ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン | Ｍｄｍ２タンパク質分解剤 |
| EP3440082A1 (en) | 2016-04-06 | 2019-02-13 | The Regents of The University of Michigan | Monofunctional intermediates for ligand-dependent target protein degradation |
| SG11201808729WA (en) | 2016-04-12 | 2018-11-29 | Univ Michigan Regents | Bet protein degraders |
| SG11201811416VA (en) | 2016-06-20 | 2019-01-30 | Incyte Corp | Crystalline solid forms of a bet inhibitor |
| JP7035027B2 (ja) | 2016-09-13 | 2022-03-14 | ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン | Ｂｅｔタンパク質分解物質としての縮合１，４－ジアゼピン |
| US11466028B2 (en) | 2016-09-13 | 2022-10-11 | The Regents Of The University Of Michigan | Fused 1,4-oxazepines as BET protein degraders |
| US11046709B2 (en) | 2017-02-03 | 2021-06-29 | The Regents Of The University Of Michigan | Fused 1,4-diazepines as BET bromodomain inhibitors |
| WO2019055444A1 (en) | 2017-09-13 | 2019-03-21 | The Regents Of The University Of Michigan | DEGRADATION AGENTS OF BROMODOMAIN BET PROTEIN WITH CLEAR BINDERS |
| CN108033957A (zh) * | 2018-01-09 | 2018-05-15 | 中国药科大学 | 一种喹啉类BET bromodomain抑制剂及其制备方法和用途 |
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| WO2022132049A1 (en) * | 2020-12-17 | 2022-06-23 | National University Of Singapore | Treating cancers using bet inhibitors |
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| GB0211649D0 (en) | 2002-05-21 | 2002-07-03 | Novartis Ag | Organic compounds |
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| WO2007075468A1 (en) | 2005-12-16 | 2007-07-05 | Coley Pharmaceutical Group, Inc. | Substituted imidazoquinolines, imidazonaphthyridines, and imidazopyridines, compositions, and methods |
| JP2008156311A (ja) | 2006-12-26 | 2008-07-10 | Institute Of Physical & Chemical Research | Ｂｒｄ２ブロモドメイン結合剤 |
| JP5478262B2 (ja) | 2007-12-28 | 2014-04-23 | 田辺三菱製薬株式会社 | 抗癌剤 |
| GB0919432D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Use |
| GB0919434D0 (en) * | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| MX341212B (es) * | 2009-11-05 | 2016-08-11 | Glaxosmithkline Llc * | Inhibidor de bromodominio de benzodiazepina. |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB201106799D0 (en) | 2011-04-21 | 2011-06-01 | Glaxosmithkline Llc | Novel compounds |
| GB201114103D0 (en) | 2011-08-17 | 2011-09-28 | Glaxosmithkline Llc | Novel compounds |
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2011
- 2011-08-17 GB GBGB1114103.3A patent/GB201114103D0/en not_active Ceased
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2012
- 2012-08-15 AR ARP120102987A patent/AR087545A1/es unknown
- 2012-08-15 PH PH1/2014/500379A patent/PH12014500379A1/en unknown
- 2012-08-15 SI SI201230818A patent/SI2744809T1/sl unknown
- 2012-08-15 US US14/237,905 patent/US9067936B2/en not_active Expired - Fee Related
- 2012-08-15 SM SM20170005T patent/SMT201700005T1/it unknown
- 2012-08-15 KR KR1020147007082A patent/KR20140064878A/ko not_active Ceased
- 2012-08-15 RS RS20170014A patent/RS55560B1/sr unknown
- 2012-08-15 ES ES12748028.3T patent/ES2609857T3/es active Active
- 2012-08-15 MX MX2014001834A patent/MX350597B/es active IP Right Grant
- 2012-08-15 WO PCT/EP2012/065918 patent/WO2013024104A1/en not_active Ceased
- 2012-08-15 DK DK12748028.3T patent/DK2744809T3/en active
- 2012-08-15 CA CA2843537A patent/CA2843537A1/en not_active Abandoned
- 2012-08-15 AU AU2012296914A patent/AU2012296914B2/en not_active Ceased
- 2012-08-15 IN IN568CHN2014 patent/IN2014CN00568A/en unknown
- 2012-08-15 PL PL12748028T patent/PL2744809T3/pl unknown
- 2012-08-15 PT PT127480283T patent/PT2744809T/pt unknown
- 2012-08-15 UY UY0001034264A patent/UY34264A/es not_active Application Discontinuation
- 2012-08-15 HR HRP20161674TT patent/HRP20161674T1/hr unknown
- 2012-08-15 HU HUE12748028A patent/HUE030106T2/en unknown
- 2012-08-15 TW TW101129613A patent/TWI558704B/zh not_active IP Right Cessation
- 2012-08-15 UA UAA201400590A patent/UA110838C2/uk unknown
- 2012-08-15 MY MYPI2014700328A patent/MY170729A/en unknown
- 2012-08-15 CN CN201280040092.5A patent/CN103889984B/zh not_active Expired - Fee Related
- 2012-08-15 EP EP16192662.1A patent/EP3150601A1/en not_active Withdrawn
- 2012-08-15 BR BR112014003681A patent/BR112014003681A8/pt not_active Application Discontinuation
- 2012-08-15 JO JOP/2012/0229A patent/JO3187B1/ar active
- 2012-08-15 LT LTEP12748028.3T patent/LT2744809T/lt unknown
- 2012-08-15 EA EA201490200A patent/EA023374B1/ru not_active IP Right Cessation
- 2012-08-15 JP JP2014525437A patent/JP6059723B2/ja not_active Expired - Fee Related
- 2012-08-15 PE PE2014000167A patent/PE20141406A1/es not_active Application Discontinuation
- 2012-08-15 EP EP12748028.3A patent/EP2744809B1/en active Active
- 2012-08-15 ME MEP-2016-288A patent/ME02589B/me unknown
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2014
- 2014-01-16 IL IL230489A patent/IL230489A/en active IP Right Grant
- 2014-01-21 CO CO14011125A patent/CO6862151A2/es not_active Application Discontinuation
- 2014-02-13 CL CL2014000365A patent/CL2014000365A1/es unknown
- 2014-02-17 DO DO2014000031A patent/DOP2014000031A/es unknown
- 2014-02-17 CR CR20140076A patent/CR20140076A/es unknown
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2015
- 2015-05-28 US US14/723,556 patent/US9416130B2/en not_active Expired - Fee Related
-
2016
- 2016-07-08 US US15/205,372 patent/US9610284B2/en not_active Expired - Fee Related
- 2016-12-16 CY CY20161101310T patent/CY1118370T1/el unknown
-
2017
- 2017-01-04 SM SM201700005T patent/SMT201700005B/it unknown
- 2017-02-17 US US15/435,697 patent/US9861627B2/en not_active Expired - Fee Related
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