AR108610A1 - Derivados de imidazolona inhibidores de la elastasa de neutrófilos humana - Google Patents
Derivados de imidazolona inhibidores de la elastasa de neutrófilos humanaInfo
- Publication number
- AR108610A1 AR108610A1 ARP170101444A ARP170101444A AR108610A1 AR 108610 A1 AR108610 A1 AR 108610A1 AR P170101444 A ARP170101444 A AR P170101444A AR P170101444 A ARP170101444 A AR P170101444A AR 108610 A1 AR108610 A1 AR 108610A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkylene
- group
- alkyl
- rarbrc
- nrdre
- Prior art date
Links
Classifications
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- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
-
- 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
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
- A61P37/08—Antiallergic 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/01—Sulfonic acids
- C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
-
- 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
- C07D403/14—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 three or more hetero rings
-
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
- C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
-
- 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
Abstract
Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1), o una sal farmacéuticamente aceptable del mismo, donde A se selecciona entre el grupo que consiste en los restos del grupo de fórmulas (2), donde el átomo de nitrógeno designado con el asterisco * está unido al grupo 4-cianofenilo y el átomo de carbono designado con # está unido al átomo de carbono del anillo 2-oxo-2,3-dihidroimidazol; X se selecciona entre el grupo que consiste en los restos del grupo de fórmulas (3), o se selecciona entre el grupo que consiste en los compuestos de fórmula (4) y (5); R¹ se selecciona entre el grupo que consiste en los restos del grupo de fórmulas (6); n es un entero entre 1 y 4; m es 0 o un entero entre 1 y 4; t es 0 o un entero entre 1 y 4; y es un entero entre 1 y 4; w es un entero entre 1 y 4; z es 0 ó 1; l es 0 ó 1; R² es -H o -C₁₋₄ alquilo lineal o ramificado; R³ es -C₁₋₄ alquilo lineal o ramificado o R² y R³ pueden formar juntos un cicloalquilo; R⁴ se selecciona entre el grupo que consiste en -arilen-C₁₋₄ alquilen-NRᵈRᵉ, -arilen-C₁₋₄ alquilen-N⁺RᵃRᵇRᶜ, -heteroarilen-C₁₋₄ alquilen-NRᵈRᵉ, -heteroarilen-C₁₋₄ alquilen-N⁺RᵃRᵇRᶜ y heteroarilo, donde cualquiera de dichos arilen-C₁₋₄ alquilen-NRᵈRᵉ, -arilen-C₁₋₄ alquilen-N⁺RᵃRᵇRᶜ, -heteroarilen-C₁₋₄ alquilen-NRᵈRᵉ, -heteroarilen-C₁₋₄ alquilen-N⁺RᵃRᵇRᶜ y heteroarilo puede estar opcionalmente sustituido con uno o más -C₁₋₄ alquilo o R⁴ se selecciona entre el grupo que consiste en los restos del grupo de fórmulas (7); R⁵ se selecciona entre el grupo que consiste en aril-C₁₋₄ alquilenoxi-, C₁₋₄ alquil-OC(O)-NH- lineal o ramificado, -(CH₂)ₜ-N⁺RᵃRᵇRᶜ, -C(O)-N(R¹⁰)C₁₋₄ alquilen-NRᵈRᵉ, -C(O)N(R¹⁰)C₁₋₄ alquilen-N⁺RᵃRᵇRᶜ, -C(O)OC₁₋₄ alquilen-NRᵈRᵉ, -C(O)OC₁₋₄ alquilen-N⁺RᵃRᵇRᶜ, -(CH₂)ₜNHC(O)-C₁₋₄ alquilen-NRᵈRᵉ, -(CH₂)ₜNHC(O)-C₁₋₄ alquilen-N⁺RᵃRᵇRᶜ, o se selecciona entre el grupo que consiste en los compuestos del grupo de fórmulas (8); R⁶ se selecciona entre el grupo que consiste en aril-C₁₋₄ alquilen-OCO-, CF₃C(O)-, aril-C₁₋₄ alquileno, C₁₋₄ alquil-OC(O)- lineal o ramificado, -C(O)-C₁₋₄ alquilen-NRᵈRᵉ, -C(O)-C₁₋₄ alquilen-N⁺RᵃRᵇRᶜ, -C(O)O-C₁₋₄ alquilen-NRᵈRᵉ, -C(O)O-C₁₋₄ alquilen-N⁺RᵃRᵇRᶜ, -C(O)-N(R¹⁰)C₁₋₄ alquilen-NRᵈRᵉ, -C(O)N(R¹⁰)C₁₋₄ alquilen-N⁺RᵃRᵇRᶜ; Rᵃ es -C₁₋₄ alquilo; Rᵇ es -C₁₋₄ alquilo; Rᶜ se selecciona entre -C₁₋₄ alquilo, aril-C₁₋₄ alquileno y heteroaril-C₁₋₄ alquileno, donde dicho heteroaril-C₁₋₄ alquileno puede estar opcionalmente sustituido con uno o más grupos -C₁₋₄ alquilo; Rᵈ es -H o -C₁₋₄ alquilo; Rᵉ es -H o -C₁₋₄ alquilo; R⁷ es -H o -C₁₋₄ alquilo; R⁸ es -H o -C₁₋₄ alquilo; R⁹ se selecciona entre el grupo que consiste en heterocicloalquilo, heterocicloalquil-C₁₋₄ alquileno-, C₁₋₄ alquilen-NRᵈRᵉ y C₁₋₄ alquilen-N⁺RᵃRᵇRᶜ; R¹⁰ es -H o -C₁₋₄ alquilo; donde cualquiera de dichos heterocicloalquilo, arilo, heteroarilo y aril-C₁₋₄ alquileno puede estar opcionalmente sustituido con uno o más grupos seleccionados en forma independiente entre C₁₋₄ alquilo y OR⁷ y donde el átomo de nitrógeno en los grupos heterocicloalquilo y heteroarilo puede estar cuaternizado.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP16172196 | 2016-05-31 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR108610A1 true AR108610A1 (es) | 2018-09-05 |
Family
ID=56096538
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP170101444A AR108610A1 (es) | 2016-05-31 | 2017-05-26 | Derivados de imidazolona inhibidores de la elastasa de neutrófilos humana |
Country Status (25)
Country | Link |
---|---|
US (2) | US9802919B1 (es) |
EP (1) | EP3464273B9 (es) |
JP (1) | JP6990663B2 (es) |
KR (1) | KR102404031B1 (es) |
CN (1) | CN109311850B (es) |
AR (1) | AR108610A1 (es) |
AU (1) | AU2017272405C1 (es) |
BR (1) | BR112018074608B1 (es) |
CA (1) | CA3020435A1 (es) |
CL (1) | CL2018003417A1 (es) |
CO (1) | CO2018012479A2 (es) |
EA (1) | EA036456B1 (es) |
GE (1) | GEP20207130B (es) |
IL (1) | IL263089B (es) |
MX (1) | MX2018014145A (es) |
MY (1) | MY195210A (es) |
NZ (1) | NZ747313A (es) |
PE (1) | PE20190176A1 (es) |
PH (1) | PH12018502242A1 (es) |
SA (1) | SA518400429B1 (es) |
SG (2) | SG10201912143UA (es) |
TW (1) | TWI738786B (es) |
UA (1) | UA123109C2 (es) |
WO (1) | WO2017207430A1 (es) |
ZA (1) | ZA201806743B (es) |
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP3976194A2 (en) | 2019-05-31 | 2022-04-06 | Ikena Oncology, Inc. | Tead inhibitors and uses thereof |
SG11202113154YA (en) | 2019-05-31 | 2021-12-30 | Ikena Oncology Inc | Tead inhibitors and uses thereof |
CN114650819A (zh) | 2019-09-17 | 2022-06-21 | 美莱奥生物制药第四有限公司 | 用于治疗移植物排斥、闭塞性细支气管炎综合征和移植物抗宿主病的阿维来司他 |
PT4106757T (pt) | 2020-04-16 | 2023-11-17 | Mereo Biopharma 5 Inc | Métodos que envolvem o inibidor da elastase neutrofílica alvelestat para o tratamento de doenças respiratórias mediadas pela deficiência de alfa 1 antitripsina |
TW202325294A (zh) | 2021-10-20 | 2023-07-01 | 英商梅瑞奧生物製藥4有限公司 | 用於治療纖維化之嗜中性球彈性蛋白酶抑制劑 |
WO2023115043A1 (en) * | 2021-12-16 | 2023-06-22 | Orixa Therapeutics Llc | Small molecule inhibitors of pr3 and hne and uses thereof |
Family Cites Families (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU650953B2 (en) | 1991-03-21 | 1994-07-07 | Novartis Ag | Inhaler |
EP1435353A4 (en) | 2001-10-03 | 2006-01-04 | Nippon Soda Co | NEW HETEROCYCLIC COMPOUND AND ANTI-INFLAMMATORY AGENT |
GB0605469D0 (en) * | 2006-03-17 | 2006-04-26 | Argenta Discovery Ltd | Multimers of heterocyclic compounds and their use |
TW200808771A (en) * | 2006-05-08 | 2008-02-16 | Astrazeneca Ab | Novel compounds II |
DE102009043260A1 (de) | 2009-09-28 | 2011-04-28 | Merck Patent Gmbh | Pyridinyl-imidazolonderivate |
BR112012007322A2 (pt) | 2009-10-02 | 2017-06-06 | Astrazeneca Ab | composto de 2-piridona usados como inibidores de neutrófilo elastase |
GB201004179D0 (en) | 2010-03-12 | 2010-04-28 | Pulmagen Therapeutics Inflamma | Enzyme inhibitors |
GB201004178D0 (en) | 2010-03-12 | 2010-04-28 | Pulmagen Therapeutics Inflamma | Enzyme inhibitors |
JP2013177318A (ja) | 2010-06-30 | 2013-09-09 | Dainippon Sumitomo Pharma Co Ltd | ジヒドロピリミジノン誘導体およびその医薬用途 |
RU2638537C2 (ru) * | 2012-07-12 | 2017-12-14 | КЬЕЗИ ФАРМАЧЕУТИЧИ С.п.А. | Ингибирование ферментов |
UA118021C2 (uk) | 2012-12-18 | 2018-11-12 | К'Єзі Фармачеутічі С.П.А. | Гетероциклічні сполуки, фармацевтична композиція, яка містить їх, і їх застосування в лікуванні захворювання або стану, в якому бере участь hne |
JP5799117B2 (ja) * | 2013-02-05 | 2015-10-21 | 大日本住友製薬株式会社 | ウラシル誘導体からなる医薬 |
KR20160097227A (ko) | 2013-12-16 | 2016-08-17 | 키에시 파르마슈티시 엣스. 피. 에이. | 인간 호중구 엘라스타제 억제제로서 테트라하이드로트리아졸로피리미딘 유도체 |
US9409870B2 (en) * | 2014-12-15 | 2016-08-09 | Chiesi Farmaceutici S.P.A. | Compounds |
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2017
- 2017-05-26 AU AU2017272405A patent/AU2017272405C1/en active Active
- 2017-05-26 CN CN201780031575.1A patent/CN109311850B/zh active Active
- 2017-05-26 PE PE2018002811A patent/PE20190176A1/es unknown
- 2017-05-26 KR KR1020187033435A patent/KR102404031B1/ko active IP Right Grant
- 2017-05-26 SG SG10201912143UA patent/SG10201912143UA/en unknown
- 2017-05-26 BR BR112018074608-8A patent/BR112018074608B1/pt active IP Right Grant
- 2017-05-26 AR ARP170101444A patent/AR108610A1/es unknown
- 2017-05-26 TW TW106117595A patent/TWI738786B/zh active
- 2017-05-26 EP EP17728091.4A patent/EP3464273B9/en active Active
- 2017-05-26 US US15/606,313 patent/US9802919B1/en active Active
- 2017-05-26 UA UAA201810656A patent/UA123109C2/uk unknown
- 2017-05-26 EA EA201892714A patent/EA036456B1/ru unknown
- 2017-05-26 MX MX2018014145A patent/MX2018014145A/es unknown
- 2017-05-26 SG SG11201809671PA patent/SG11201809671PA/en unknown
- 2017-05-26 CA CA3020435A patent/CA3020435A1/en active Pending
- 2017-05-26 JP JP2018555572A patent/JP6990663B2/ja active Active
- 2017-05-26 GE GEAP201714924A patent/GEP20207130B/en unknown
- 2017-05-26 NZ NZ747313A patent/NZ747313A/en unknown
- 2017-05-26 MY MYPI2018001793A patent/MY195210A/en unknown
- 2017-05-26 WO PCT/EP2017/062754 patent/WO2017207430A1/en unknown
- 2017-09-22 US US15/712,366 patent/US10023558B2/en active Active
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2018
- 2018-10-10 ZA ZA2018/06743A patent/ZA201806743B/en unknown
- 2018-10-19 PH PH12018502242A patent/PH12018502242A1/en unknown
- 2018-11-13 SA SA518400429A patent/SA518400429B1/ar unknown
- 2018-11-18 IL IL263089A patent/IL263089B/en unknown
- 2018-11-21 CO CONC2018/0012479A patent/CO2018012479A2/es unknown
- 2018-11-30 CL CL2018003417A patent/CL2018003417A1/es unknown
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