PE20190176A1 - Compuestos de imidazolona como inhibidores de la elastasa de neutrofilos humana - Google Patents
Compuestos de imidazolona como inhibidores de la elastasa de neutrofilos humanaInfo
- Publication number
- PE20190176A1 PE20190176A1 PE2018002811A PE2018002811A PE20190176A1 PE 20190176 A1 PE20190176 A1 PE 20190176A1 PE 2018002811 A PE2018002811 A PE 2018002811A PE 2018002811 A PE2018002811 A PE 2018002811A PE 20190176 A1 PE20190176 A1 PE 20190176A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- inhibitors
- imidazolone
- alkylene
- aryl
- Prior art date
Links
- WZELXJBMMZFDDU-UHFFFAOYSA-N Imidazol-2-one Chemical class O=C1N=CC=N1 WZELXJBMMZFDDU-UHFFFAOYSA-N 0.000 title 1
- 102000016387 Pancreatic elastase Human genes 0.000 title 1
- 108010067372 Pancreatic elastase Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 101000851058 Homo sapiens Neutrophil elastase Proteins 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 102000052502 human ELANE Human genes 0.000 abstract 2
- CAAMSDWKXXPUJR-UHFFFAOYSA-N 3,5-dihydro-4H-imidazol-4-one Chemical compound O=C1CNC=N1 CAAMSDWKXXPUJR-UHFFFAOYSA-N 0.000 abstract 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000005529 alkyleneoxy group Chemical group 0.000 abstract 1
- 201000009267 bronchiectasis Diseases 0.000 abstract 1
- 206010006451 bronchitis Diseases 0.000 abstract 1
- 230000006806 disease prevention Effects 0.000 abstract 1
- 125000002883 imidazolyl group Chemical group 0.000 abstract 1
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001425 triazolyl group Chemical group 0.000 abstract 1
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
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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
- A61K31/41—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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Otolaryngology (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Abstract
Se refiere a un compuesto derivado de imidazolona de formula I o una sal farmaceuticamente aceptable del mismo, donde A se selecciona de pirazolilo, imidazolilo o triazolilo; X es un grupo (a), (b), (c), entre otros; y, w y n son un entero entre 1 y 4; m y t son 0 o un numero entero entre 1 y 4; Z y l son 0 o 1; R2 es -H o (C1-C4)alquilo lineal o ramificado; R3 es -(C1-C4)alquilo lineal o ramificado; R4 es -arilen-(C1-C4)alquilen-NRdRe, entre otros; R5 es aril-(C1-C4)alquilenoxi, (C1-C4)alquil-OC(O)-NH, entre otros; R6 es CF3C(O), aril-(C1-C4)alquileno, entre otros; Ra y Rb son alquilo C1-C4; Rd es H o alquilo C1-C4. Dicho compuesto es util en el tratamiento o prevencion de enfermedades tales como enfermedad pulmonar obstructiva cronica, bronquiectasia, bronquitis, entre otras, en la que esta involucrada la elastasa de neutrofilos humana (HNE)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16172196 | 2016-05-31 | ||
| PCT/EP2017/062754 WO2017207430A1 (en) | 2016-05-31 | 2017-05-26 | Imidazolone compounds as human neutrophil elastase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20190176A1 true PE20190176A1 (es) | 2019-02-01 |
Family
ID=56096538
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2018002811A PE20190176A1 (es) | 2016-05-31 | 2017-05-26 | Compuestos de imidazolona como inhibidores de la elastasa de neutrofilos 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) | MX381423B (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 |
|---|---|---|---|---|
| KR20220034739A (ko) | 2019-05-31 | 2022-03-18 | 이케나 온콜로지, 인코포레이티드 | Tead 억제제 및 이의 용도 |
| KR20220030222A (ko) | 2019-05-31 | 2022-03-10 | 이케나 온콜로지, 인코포레이티드 | Tead 억제제 및 이의 용도 |
| WO2021053058A1 (en) | 2019-09-17 | 2021-03-25 | Mereo Biopharma 4 Limited | Alvelestat for use in the treatment of graft rejection, bronchiolitis obliterans syndrome and graft versus host disease |
| DK4106757T3 (da) | 2020-04-16 | 2023-10-23 | Mereo Biopharma 4 Ltd | Fremgangsmåder der involverer neutrofil elastase-inhibitor alvelestat til behandling af luftvejssygdom medieret af alpha-1-antitrypsin-mangel |
| AU2022373971A1 (en) | 2021-10-20 | 2024-04-04 | Mereo Biopharma 4 Limited | Neutrophil elastase inhibitors for use in the treatment of fibrosis |
| 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 |
| WO2003031414A1 (en) * | 2001-10-03 | 2003-04-17 | Nippon Soda Co.,Ltd. | Novel 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 |
| MX2012003644A (es) * | 2009-10-02 | 2012-04-30 | Astrazeneca Ab | Compuestos de 2-piridona empleados como inhibidores de la elastasa neutrofila. |
| 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 |
| WO2014009425A1 (en) | 2012-07-12 | 2014-01-16 | Chiesi Farmaceutici S.P.A. | Inhibition of enzymes |
| JP6390919B2 (ja) | 2012-12-18 | 2018-09-19 | チエシ ファルマスティスィ エス．ピー．エー． | 新規な化合物 |
| 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 |
| EP3083626B1 (en) | 2013-12-16 | 2017-10-25 | CHIESI FARMACEUTICI S.p.A. | Tetrahydrotriazolopyrimidine derivatives as human neutrophil elastase inhibitors |
| US9409870B2 (en) * | 2014-12-15 | 2016-08-09 | Chiesi Farmaceutici S.P.A. | Compounds |
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2017
- 2017-05-26 JP JP2018555572A patent/JP6990663B2/ja active Active
- 2017-05-26 CA CA3020435A patent/CA3020435A1/en active Pending
- 2017-05-26 BR BR112018074608-8A patent/BR112018074608B1/pt active IP Right Grant
- 2017-05-26 AR ARP170101444A patent/AR108610A1/es active IP Right Grant
- 2017-05-26 NZ NZ747313A patent/NZ747313A/en unknown
- 2017-05-26 MX MX2018014145A patent/MX381423B/es unknown
- 2017-05-26 MY MYPI2018001793A patent/MY195210A/en unknown
- 2017-05-26 AU AU2017272405A patent/AU2017272405C1/en active Active
- 2017-05-26 UA UAA201810656A patent/UA123109C2/uk unknown
- 2017-05-26 US US15/606,313 patent/US9802919B1/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 SG SG10201912143UA patent/SG10201912143UA/en unknown
- 2017-05-26 GE GEAP201714924A patent/GEP20207130B/en unknown
- 2017-05-26 SG SG11201809671PA patent/SG11201809671PA/en unknown
- 2017-05-26 KR KR1020187033435A patent/KR102404031B1/ko active Active
- 2017-05-26 WO PCT/EP2017/062754 patent/WO2017207430A1/en not_active Ceased
- 2017-05-26 TW TW106117595A patent/TWI738786B/zh active
- 2017-05-26 EA EA201892714A patent/EA036456B1/ru unknown
- 2017-05-26 EP EP17728091.4A patent/EP3464273B9/en active Active
- 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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