PE20170893A1 - N-alquilaril-5-oxiaril-octahidro ciclopenta[c]pirrol moduladores alostericos negativos de nr2b - Google Patents
N-alquilaril-5-oxiaril-octahidro ciclopenta[c]pirrol moduladores alostericos negativos de nr2bInfo
- Publication number
- PE20170893A1 PE20170893A1 PE2017000506A PE2017000506A PE20170893A1 PE 20170893 A1 PE20170893 A1 PE 20170893A1 PE 2017000506 A PE2017000506 A PE 2017000506A PE 2017000506 A PE2017000506 A PE 2017000506A PE 20170893 A1 PE20170893 A1 PE 20170893A1
- Authority
- PE
- Peru
- Prior art keywords
- alkylaryl
- oxyaril
- pirrol
- negative allosteric
- octahydro cyclopenta
- Prior art date
Links
- 102000034527 Retinoid X Receptors Human genes 0.000 title abstract 2
- 108010038912 Retinoid X Receptors Proteins 0.000 title abstract 2
- 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 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 208000020925 Bipolar disease Diseases 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000005346 substituted cycloalkyl 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)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Indole Compounds (AREA)
- Pyrrole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Se refiere al N-alquilaril-5-oxiaril-octahidro ciclopenta[c]pirrol de formula general (I), donde L1 es -C(O)-, -C(O)-C1-C3alquilenilo, entre otros; R1 es cicloalquilo, arilo o heteroarilo opcionalmente sustituido; X es O, S, entre otros; Y e Y´ son H, halogeno, entre otros; L2 es un enlace, -(CH2)n-, entre otros; R2 es fenilo, naftilo, entre otros; n es 1, 2 o 3. Es un compuesto seleccionado: 2-((3aR, 5s, 6aS)-5-(3, 4-difluorofenoxi)hexahidrociclopenta[c]pirrol-2(1H)-il)-1-(4-hidroxifenil)etanona. Tambien se refiere a una composicion y una combinacion. Dicho compuesto es un modulador alosterico negativo de NR2B, siendo util en el tratamiento de trastorno bipolar, trastorno obsesivo, entre otros
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462056284P | 2014-09-26 | 2014-09-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20170893A1 true PE20170893A1 (es) | 2017-07-12 |
Family
ID=55581945
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2017000506A PE20170893A1 (es) | 2014-09-26 | 2015-09-23 | N-alquilaril-5-oxiaril-octahidro ciclopenta[c]pirrol moduladores alostericos negativos de nr2b |
Country Status (40)
| Country | Link |
|---|---|
| US (4) | US10239835B2 (es) |
| EP (4) | EP4282412A3 (es) |
| JP (4) | JP6473227B2 (es) |
| KR (1) | KR102479356B1 (es) |
| CN (1) | CN106795111B (es) |
| AP (1) | AP2017009832A0 (es) |
| AR (1) | AR103199A1 (es) |
| AU (1) | AU2015320721B2 (es) |
| BR (1) | BR112017006093B1 (es) |
| CA (1) | CA2962569C (es) |
| CL (1) | CL2017000474A1 (es) |
| CO (1) | CO2017002494A2 (es) |
| CR (1) | CR20170114A (es) |
| CU (1) | CU24482B1 (es) |
| CY (1) | CY1123533T1 (es) |
| DK (1) | DK3197868T3 (es) |
| EA (1) | EA034937B1 (es) |
| EC (1) | ECSP17025302A (es) |
| ES (3) | ES2956546T3 (es) |
| GT (1) | GT201700062A (es) |
| HR (1) | HRP20200959T1 (es) |
| HU (1) | HUE049698T2 (es) |
| IL (1) | IL250909B (es) |
| JO (1) | JO3579B1 (es) |
| LT (1) | LT3197868T (es) |
| MX (1) | MX2017003940A (es) |
| MY (1) | MY182342A (es) |
| NZ (1) | NZ729569A (es) |
| PE (1) | PE20170893A1 (es) |
| PH (1) | PH12017500513A1 (es) |
| PL (1) | PL3197868T3 (es) |
| PT (1) | PT3197868T (es) |
| RS (1) | RS60497B1 (es) |
| SG (1) | SG11201702023QA (es) |
| SI (1) | SI3197868T1 (es) |
| TN (1) | TN2017000076A1 (es) |
| TW (1) | TWI687407B (es) |
| UY (1) | UY36326A (es) |
| WO (1) | WO2016049165A1 (es) |
| ZA (1) | ZA201701061B (es) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| CN111491920B (zh) | 2017-10-20 | 2024-01-30 | 范德比尔特大学 | 毒蕈碱性乙酰胆碱受体m4的拮抗剂 |
| CA3081324A1 (en) | 2017-10-31 | 2019-05-09 | Vanderbilt University | Antagonists of the muscarinic acetylcholine receptor m4 |
| AU2019216492A1 (en) | 2018-02-02 | 2020-08-20 | Vanderbilt University | Antagonists of the muscarinic acetylcholine receptor M4 |
| WO2020245136A1 (en) * | 2019-06-04 | 2020-12-10 | Boehringer Ingelheim International Gmbh | Purine derivatives, as nr2b negative modulators and the use thereof as medicament, in particular for treating depressive disorders |
| 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 |
| EP4255419A1 (en) | 2020-12-04 | 2023-10-11 | Novartis AG | Dosage regimen for a 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 |
| WO2022204337A1 (en) * | 2021-03-26 | 2022-09-29 | Novartis Ag | Novel cyclopenta[c]pyrrol negative allosteric modulators of nr2b |
| EP4313041A1 (en) * | 2021-03-26 | 2024-02-07 | Novartis AG | Novel cyclopental[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 |
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| US5262564A (en) | 1992-10-30 | 1993-11-16 | Octamer, Inc. | Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents |
| 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 |
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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 |
| DE602005004144T2 (de) * | 2004-06-09 | 2009-01-29 | F. Hoffmann-La Roche Ag | Octahydropyrroloä3,4-cüpyrrolderivate und deren verwendung als antivirale mittel |
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| JP2011500727A (ja) | 2007-10-22 | 2011-01-06 | シェーリング コーポレイション | Ｇｐｒ１１９の活性のモジュレーターとしての二環式ヘテロ環誘導体およびその使用 |
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| 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 |
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| WO2011149993A2 (en) | 2010-05-25 | 2011-12-01 | Abbott Laboratories | SUBSTITUTED OCTAHYDROCYCLOPENTA[c]PYRROLES AS CALCIUM CHANNEL MODULATORS |
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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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| MX368615B (es) * | 2012-09-25 | 2019-10-09 | Hoffmann La Roche | Derivados bicíclicos como inhibidores de la autotaxina (atx) que son inhibidores de la producción de ácido lisofosfatídico (lpa) y el uso de los mismos. |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| US9418332B2 (en) | 2013-08-16 | 2016-08-16 | Qualcomm Incorporated | Post ghost plasticity |
| US9540324B2 (en) | 2013-09-26 | 2017-01-10 | Luc Therapeutics, Inc. | Selective octahydro-cyclopenta[C] pyrrole negative modulators of NR2B |
| MA39792B1 (fr) | 2014-03-26 | 2019-12-31 | Hoffmann La Roche | Composés bicycliques en tant qu'inhibiteurs de production d'autotaxine (atx) et d'acide lysophosphatidique (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 CU CU2017000037A patent/CU24482B1/es unknown
- 2015-09-23 US US15/506,592 patent/US10239835B2/en active Active
- 2015-09-23 LT LTEP15844057.8T patent/LT3197868T/lt unknown
- 2015-09-23 EP EP23185898.6A patent/EP4282412A3/en active Pending
- 2015-09-23 BR BR112017006093-0A patent/BR112017006093B1/pt active IP Right Grant
- 2015-09-23 CA CA2962569A patent/CA2962569C/en active Active
- 2015-09-23 EP EP20159713.5A patent/EP3683207B1/en active Active
- 2015-09-23 PE PE2017000506A patent/PE20170893A1/es unknown
- 2015-09-23 MX MX2017003940A patent/MX2017003940A/es active IP Right Grant
- 2015-09-23 KR KR1020177007813A patent/KR102479356B1/ko active IP Right Grant
- 2015-09-23 ES ES21202255T patent/ES2956546T3/es active Active
- 2015-09-23 AU AU2015320721A patent/AU2015320721B2/en active Active
- 2015-09-23 AP AP2017009832A patent/AP2017009832A0/en unknown
- 2015-09-23 MY MYPI2017700652A patent/MY182342A/en unknown
- 2015-09-23 NZ NZ729569A patent/NZ729569A/en unknown
- 2015-09-23 DK DK15844057.8T patent/DK3197868T3/da active
- 2015-09-23 EP EP15844057.8A patent/EP3197868B1/en active Active
- 2015-09-23 ES ES15844057T patent/ES2791327T3/es active Active
- 2015-09-23 CR CR20170114A patent/CR20170114A/es unknown
- 2015-09-23 HU HUE15844057A patent/HUE049698T2/hu unknown
- 2015-09-23 PT PT158440578T patent/PT3197868T/pt unknown
- 2015-09-23 WO PCT/US2015/051694 patent/WO2016049165A1/en active Application Filing
- 2015-09-23 JP JP2017516358A patent/JP6473227B2/ja active Active
- 2015-09-23 RS RS20200721A patent/RS60497B1/sr unknown
- 2015-09-23 CN CN201580051671.3A patent/CN106795111B/zh active Active
- 2015-09-23 TN TN2017000076A patent/TN2017000076A1/en unknown
- 2015-09-23 ES ES20159713T patent/ES2911004T3/es active Active
- 2015-09-23 SI SI201531255T patent/SI3197868T1/sl unknown
- 2015-09-23 PL PL15844057T patent/PL3197868T3/pl unknown
- 2015-09-23 SG SG11201702023QA patent/SG11201702023QA/en unknown
- 2015-09-23 EA EA201790713A patent/EA034937B1/ru not_active IP Right Cessation
- 2015-09-23 EP EP21202255.2A patent/EP3974420B1/en active Active
- 2015-09-25 UY UY0001036326A patent/UY36326A/es active IP Right Grant
- 2015-09-25 TW TW104131936A patent/TWI687407B/zh active
- 2015-09-25 AR ARP150103084A patent/AR103199A1/es active IP Right Grant
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2017
- 2017-02-13 ZA ZA2017/01061A patent/ZA201701061B/en unknown
- 2017-02-28 CL CL2017000474A patent/CL2017000474A1/es unknown
- 2017-03-02 IL IL250909A patent/IL250909B/en active IP Right Grant
- 2017-03-15 CO CONC2017/0002494A patent/CO2017002494A2/es unknown
- 2017-03-17 PH PH12017500513A patent/PH12017500513A1/en unknown
- 2017-03-24 GT GT201700062A patent/GT201700062A/es unknown
- 2017-04-24 EC ECIEPI201725302A patent/ECSP17025302A/es unknown
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2019
- 2019-01-23 JP JP2019008873A patent/JP6772307B2/ja active Active
- 2019-01-23 US US16/255,500 patent/US10781174B2/en active Active
-
2020
- 2020-06-15 CY CY20201100542T patent/CY1123533T1/el unknown
- 2020-06-17 HR HRP20200959TT patent/HRP20200959T1/hr unknown
- 2020-08-12 US US16/991,684 patent/US20200369610A1/en not_active Abandoned
- 2020-09-30 JP JP2020166129A patent/JP7216060B2/ja active Active
-
2022
- 2022-05-03 US US17/735,386 patent/US20220274925A1/en active Pending
-
2023
- 2023-01-19 JP JP2023006525A patent/JP2023052515A/ja active Pending
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