BR112017006093A2 - moduladores alostéricos negativos de n-alquilaril-5-oxiaril-octa-hidro-ciclopenta[c] pirrol de nr2b - Google Patents
moduladores alostéricos negativos de n-alquilaril-5-oxiaril-octa-hidro-ciclopenta[c] pirrol de nr2bInfo
- Publication number
- BR112017006093A2 BR112017006093A2 BR112017006093A BR112017006093A BR112017006093A2 BR 112017006093 A2 BR112017006093 A2 BR 112017006093A2 BR 112017006093 A BR112017006093 A BR 112017006093A BR 112017006093 A BR112017006093 A BR 112017006093A BR 112017006093 A2 BR112017006093 A2 BR 112017006093A2
- Authority
- BR
- Brazil
- Prior art keywords
- oxyaryl
- alkylaryl
- nr2b
- allosteric modulators
- negative allosteric
- Prior art date
Links
- 229940126662 negative allosteric modulator Drugs 0.000 title abstract 2
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 abstract 2
- 101100240516 Caenorhabditis elegans nhr-10 gene Proteins 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 229910052757 nitrogen Chemical group 0.000 abstract 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/52—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
-
- 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
- C07D401/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
-
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Indole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyrrole Compounds (AREA)
Abstract
a presente invenção refere-se a moduladores alostéricos negativos de n-alquilaril-5-oxiaril-octadi-hidrociclopent[c]pirrol de receptores de nr2b úteis no tratamento de doenças neurológicas tendo a fórmula i onde r1, r2, l1, l2, x, y, e y? são descritos aqui. em um aspecto, compostos da fórmula i são descritos e sais farmaceuticamente aceitáveis, profármacos, solvatos, hidratos, tautômeros ou este-reoisômeros dos mesmos, em que: l1 é c1-c5 alquila linear ou ramifi-cada substituída com um ou mais substituintes selecionados a partir do grupo consistindo em oh, or10, nh2, nhr10 e n(r10)(r10?) contanto que não mais do que um oxigênio ou nitrogênio seja ligado a qualquer carbo-no.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462056284P | 2014-09-26 | 2014-09-26 | |
| US62/056,284 | 2014-09-26 | ||
| PCT/US2015/051694 WO2016049165A1 (en) | 2014-09-26 | 2015-09-23 | N-alkylaryl-5-oxyaryl-octahydro-cyclopenta[c]pyrrole negative allosteric modulators of nr2b |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| BR112017006093A2 true BR112017006093A2 (pt) | 2017-12-19 |
| BR112017006093B1 BR112017006093B1 (pt) | 2023-03-21 |
Family
ID=55581945
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112017006093-0A BR112017006093B1 (pt) | 2014-09-26 | 2015-09-23 | Moduladores alostéricos negativos de n-alquilaril-5-oxiaril-octa- hidro-ciclopenta[c]pirrol de nr2b |
Country Status (40)
| Country | Link |
|---|---|
| US (3) | US10239835B2 (pt) |
| EP (4) | EP3683207B1 (pt) |
| JP (4) | JP6473227B2 (pt) |
| KR (1) | KR102479356B1 (pt) |
| CN (1) | CN106795111B (pt) |
| AP (1) | AP2017009832A0 (pt) |
| AR (1) | AR103199A1 (pt) |
| AU (1) | AU2015320721B2 (pt) |
| BR (1) | BR112017006093B1 (pt) |
| CA (1) | CA2962569C (pt) |
| CL (1) | CL2017000474A1 (pt) |
| CO (1) | CO2017002494A2 (pt) |
| CR (1) | CR20170114A (pt) |
| CU (1) | CU24482B1 (pt) |
| CY (1) | CY1123533T1 (pt) |
| DK (1) | DK3197868T3 (pt) |
| EA (1) | EA034937B1 (pt) |
| EC (1) | ECSP17025302A (pt) |
| ES (3) | ES2791327T3 (pt) |
| GT (1) | GT201700062A (pt) |
| HR (1) | HRP20200959T1 (pt) |
| HU (1) | HUE049698T2 (pt) |
| IL (1) | IL250909B (pt) |
| JO (1) | JO3579B1 (pt) |
| LT (1) | LT3197868T (pt) |
| MX (1) | MX2017003940A (pt) |
| MY (1) | MY182342A (pt) |
| NZ (1) | NZ729569A (pt) |
| PE (1) | PE20170893A1 (pt) |
| PH (1) | PH12017500513A1 (pt) |
| PL (1) | PL3197868T3 (pt) |
| PT (1) | PT3197868T (pt) |
| RS (1) | RS60497B1 (pt) |
| SG (1) | SG11201702023QA (pt) |
| SI (1) | SI3197868T1 (pt) |
| TN (1) | TN2017000076A1 (pt) |
| TW (1) | TWI687407B (pt) |
| UY (1) | UY36326A (pt) |
| WO (1) | WO2016049165A1 (pt) |
| ZA (1) | ZA201701061B (pt) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| JO3579B1 (ar) * | 2014-09-26 | 2020-07-05 | Luc Therapeutics Inc | مُعدِلات تفاغرية سالبة لمستقبل nr2b من المركب n-ألكيل أريل-5-أوكسي أريل-ثامن هيدرو-خماسي الحلقة [c] بيرول |
| IL273924B2 (en) | 2017-10-20 | 2024-07-01 | Univ Vanderbilt | Muscarinic acetylcholine M4 receptor antagonists |
| AU2018360581A1 (en) | 2017-10-31 | 2020-06-11 | Vanderbilt University | Antagonists of the muscarinic acetylcholine receptor M4 |
| US11414406B2 (en) | 2018-02-02 | 2022-08-16 | Vanderbilt University | Antagonists of the muscarinic acetylcholine receptor M4 |
| EP3761992A4 (en) | 2018-03-05 | 2021-11-24 | Arcus Biosciences, Inc. | ARGINASE INHIBITORS |
| TW202112378A (zh) | 2019-06-04 | 2021-04-01 | 德商百靈佳殷格翰國際股份有限公司 | 嘌呤衍生物及其作為藥物之用途 |
| CN111481543A (zh) * | 2020-05-21 | 2020-08-04 | 苏州健雄职业技术学院 | Nr2b负变构调节剂联合gaba受体调节剂在制备治疗阿尔兹海默症的药物中的用途 |
| IL303357A (en) | 2020-12-04 | 2023-08-01 | Novartis Ag | Dosing regimen for the NR2B-NMDA RECEPTOR NAM for the treatment of depression |
| JP2021058765A (ja) * | 2021-01-19 | 2021-04-15 | 株式会社藤商事 | 遊技機 |
| US20240208953A1 (en) | 2021-03-26 | 2024-06-27 | Novartis Ag | "Cyclopenta[c]pyrrol Negative Allosteric Modulators of NR2B" |
| EP4313042A1 (en) * | 2021-03-26 | 2024-02-07 | Novartis AG | Novel cyclopenta[c]pyrrol negative allosteric modulators of nr2b |
| TW202402271A (zh) | 2022-06-02 | 2024-01-16 | 瑞士商諾華公司 | Ｎｒ２ｂ—ｎｍｄａ受體ｎａｍ用於憂鬱障礙的劑量 |
| WO2024150146A1 (en) | 2023-01-12 | 2024-07-18 | Novartis Ag | Engineered ketoreductase polypeptides |
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| US5532243A (en) | 1992-02-14 | 1996-07-02 | The Dupont Merck Pharmaceutical Company | Antipsychotic nitrogen-containing bicyclic compounds |
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| DE4341403A1 (de) * | 1993-12-04 | 1995-06-08 | Basf Ag | N-substituierte 3-Azabicycloalkan-Derivate, ihre Herstellung und Verwendung |
| US5726172A (en) | 1996-01-16 | 1998-03-10 | Merck & Co., Inc. | Tocolytic oxytocin receptor antagonists |
| US6369076B1 (en) | 1999-10-29 | 2002-04-09 | Merck & Co. Inc. | 5-benzyl-octahydroindole and 6-benzyl-decahydroquinoline NMDA/NR2B antagonists |
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| US7696241B2 (en) | 2004-03-04 | 2010-04-13 | Bristol-Myers Squibb Company | Bicyclic compounds as modulators of androgen receptor function and method |
| CN101001860A (zh) * | 2004-06-09 | 2007-07-18 | 霍夫曼-拉罗奇有限公司 | 杂环抗病毒化合物 |
| EP1778688A1 (en) | 2004-07-22 | 2007-05-02 | Glaxo Group Limited | Antibacterial agents |
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| CA2640806A1 (en) | 2006-04-28 | 2007-11-15 | Laboratorios Del Dr. Esteve, S.A. | Bicyclic tetrahydropyrrole compounds |
| EP1849772A1 (en) | 2006-04-28 | 2007-10-31 | Laboratorios Del Dr. Esteve, S.A. | Bicyclic tetrahydropyrrole compounds |
| TW200845977A (en) | 2007-03-30 | 2008-12-01 | Targacept Inc | Sub-type selective azabicycloalkane derivatives |
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| US8211933B2 (en) | 2008-12-12 | 2012-07-03 | Vanderbilt University | 3.3.0 bicyclic GlyT1 inhibitors and methods of making and using same |
| FR2945533B1 (fr) | 2009-05-12 | 2011-05-27 | Sanofi Aventis | Derives de cyclopenta°c!pyrrolyl-alkylcarbamates d'heterocycles a 5 chainons, leur preparation et leur application en therapeutique |
| FR2945534B1 (fr) | 2009-05-12 | 2012-11-16 | Sanofi Aventis | DERIVES DE CYCLOPENTAL[c]PYRROLE-2-CARBOXYLATES, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE |
| BR112012016733A2 (pt) | 2010-01-07 | 2015-09-01 | Du Pont | "composto, composição fungicida e método" |
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| CN102432598A (zh) * | 2010-09-29 | 2012-05-02 | 江苏恒瑞医药股份有限公司 | 三环化合物、其制备方法及其在医药上的应用 |
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| JO3611B1 (ar) | 2011-08-10 | 2020-08-27 | Janssen Sciences Ireland Uc | سايكلو بنتا (سي (بيرول 4,3 ثاني هيدرو 1 hمستبدله [8,1] نافثيريدينونات مضادة للجراثيم |
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| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
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| AR097794A1 (es) * | 2013-09-26 | 2016-04-13 | Mnemosyne Pharmaceuticals Inc | Moduladores octahidro-ciclopenta[c]pirrol negativos de nr2b |
| EA037928B1 (ru) | 2014-03-26 | 2021-06-08 | Ф. Хоффманн-Ля Рош Аг | Бициклические соединения в качестве ингибиторов продукции аутотаксина (atx) и лизофосфатидиловой кислоты (lpa) |
| JO3579B1 (ar) * | 2014-09-26 | 2020-07-05 | Luc Therapeutics Inc | مُعدِلات تفاغرية سالبة لمستقبل nr2b من المركب n-ألكيل أريل-5-أوكسي أريل-ثامن هيدرو-خماسي الحلقة [c] بيرول |
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2015
- 2015-09-22 JO JOP/2015/0237A patent/JO3579B1/ar active
- 2015-09-23 MY MYPI2017700652A patent/MY182342A/en unknown
- 2015-09-23 DK DK15844057.8T patent/DK3197868T3/da active
- 2015-09-23 US US15/506,592 patent/US10239835B2/en active Active
- 2015-09-23 KR KR1020177007813A patent/KR102479356B1/ko active IP Right Grant
- 2015-09-23 SG SG11201702023QA patent/SG11201702023QA/en unknown
- 2015-09-23 EP EP20159713.5A patent/EP3683207B1/en active Active
- 2015-09-23 EP EP23185898.6A patent/EP4282412A3/en active Pending
- 2015-09-23 PT PT158440578T patent/PT3197868T/pt unknown
- 2015-09-23 AP AP2017009832A patent/AP2017009832A0/en unknown
- 2015-09-23 EA EA201790713A patent/EA034937B1/ru not_active IP Right Cessation
- 2015-09-23 EP EP15844057.8A patent/EP3197868B1/en active Active
- 2015-09-23 PE PE2017000506A patent/PE20170893A1/es unknown
- 2015-09-23 HU HUE15844057A patent/HUE049698T2/hu unknown
- 2015-09-23 AU AU2015320721A patent/AU2015320721B2/en active Active
- 2015-09-23 CU CU2017000037A patent/CU24482B1/es unknown
- 2015-09-23 RS RS20200721A patent/RS60497B1/sr unknown
- 2015-09-23 ES ES15844057T patent/ES2791327T3/es active Active
- 2015-09-23 EP EP21202255.2A patent/EP3974420B1/en active Active
- 2015-09-23 SI SI201531255T patent/SI3197868T1/sl unknown
- 2015-09-23 NZ NZ729569A patent/NZ729569A/en unknown
- 2015-09-23 LT LTEP15844057.8T patent/LT3197868T/lt unknown
- 2015-09-23 CA CA2962569A patent/CA2962569C/en active Active
- 2015-09-23 CN CN201580051671.3A patent/CN106795111B/zh active Active
- 2015-09-23 PL PL15844057T patent/PL3197868T3/pl unknown
- 2015-09-23 WO PCT/US2015/051694 patent/WO2016049165A1/en active Application Filing
- 2015-09-23 BR BR112017006093-0A patent/BR112017006093B1/pt active IP Right Grant
- 2015-09-23 ES ES21202255T patent/ES2956546T3/es active Active
- 2015-09-23 JP JP2017516358A patent/JP6473227B2/ja active Active
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