CO2018011105A2 - 6-hidroxi-4-oxo-1,4-dihidropirimidin-5-carboxamidas como agonistas del receptor de apelina (apj) - Google Patents
6-hidroxi-4-oxo-1,4-dihidropirimidin-5-carboxamidas como agonistas del receptor de apelina (apj)Info
- Publication number
- CO2018011105A2 CO2018011105A2 CONC2018/0011105A CO2018011105A CO2018011105A2 CO 2018011105 A2 CO2018011105 A2 CO 2018011105A2 CO 2018011105 A CO2018011105 A CO 2018011105A CO 2018011105 A2 CO2018011105 A2 CO 2018011105A2
- Authority
- CO
- Colombia
- Prior art keywords
- apj
- dihydropyrimidin
- carboxamides
- oxo
- hydroxy
- Prior art date
Links
- RVVVQQNYGKCVMV-UHFFFAOYSA-N 4-hydroxy-6-oxo-1h-pyrimidine-5-carboxamide Chemical class NC(=O)C1=C(O)N=CNC1=O RVVVQQNYGKCVMV-UHFFFAOYSA-N 0.000 title 1
- 108091008803 APLNR Proteins 0.000 title 1
- 102000016555 Apelin receptors Human genes 0.000 title 1
- 239000000018 receptor agonist Substances 0.000 title 1
- 229940044601 receptor agonist Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 239000000556 agonist Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 238000002483 medication Methods 0.000 abstract 1
- 239000000203 mixture Substances 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
- C07D403/06—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
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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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/52—Two oxygen atoms
- C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/52—Two oxygen atoms
- C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
- C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/52—Two oxygen atoms
- C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
- C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/557—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms, e.g. orotic acid
-
- 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
- C07D401/14—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
-
- 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
- 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
- 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)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Emergency Medicine (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662312780P | 2016-03-24 | 2016-03-24 | |
| PCT/US2017/023801 WO2017165640A1 (en) | 2016-03-24 | 2017-03-23 | 6-hydroxy-4-oxo-1,4-dihydropyrimidine-5-carboxamides as apj agonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO2018011105A2 true CO2018011105A2 (es) | 2018-10-22 |
Family
ID=58464691
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CONC2018/0011105A CO2018011105A2 (es) | 2016-03-24 | 2018-10-17 | 6-hidroxi-4-oxo-1,4-dihidropirimidin-5-carboxamidas como agonistas del receptor de apelina (apj) |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US10106528B2 (https=) |
| EP (1) | EP3433247B1 (https=) |
| JP (1) | JP6716711B2 (https=) |
| KR (1) | KR102433280B1 (https=) |
| CN (1) | CN109195963B (https=) |
| AR (1) | AR107973A1 (https=) |
| AU (1) | AU2017238504B2 (https=) |
| BR (1) | BR112018068341A2 (https=) |
| CA (1) | CA3018346A1 (https=) |
| CL (1) | CL2018002671A1 (https=) |
| CO (1) | CO2018011105A2 (https=) |
| EA (1) | EA037162B1 (https=) |
| ES (1) | ES2895124T3 (https=) |
| IL (1) | IL261904B (https=) |
| MA (1) | MA43761A (https=) |
| MX (1) | MX379088B (https=) |
| MY (1) | MY189454A (https=) |
| SG (1) | SG11201808163WA (https=) |
| TW (1) | TWI744301B (https=) |
| UY (1) | UY37169A (https=) |
| WO (1) | WO2017165640A1 (https=) |
| ZA (1) | ZA201806356B (https=) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016196771A1 (en) | 2015-06-03 | 2016-12-08 | Bristol-Myers Squibb Company | 4-hydroxy-3-(heteroaryl)pyridine-2-one apj agonists for use in the treatment of cardiovascular disorders |
| KR102707502B1 (ko) | 2015-10-14 | 2024-09-13 | 브리스톨-마이어스 스큅 컴퍼니 | Apj 효능제로서의 2,4-디히드록시-니코틴아미드 |
| UY37005A (es) | 2015-12-04 | 2017-06-30 | Bristol-Myers Squibb Company Una Corporacion Del Estado De Delaware | Hidroxipirimidinonas sustituidas como agonistas del receptor de apelina y sus usos |
| BR112018012112A2 (pt) | 2015-12-16 | 2018-12-04 | Bristol-Myers Squibb Company | heteroaril-hidroxipirimidinonas como agonistas do receptor apj |
| TWI744301B (zh) * | 2016-03-24 | 2021-11-01 | 美商必治妥美雅史谷比公司 | 做為apj促效劑之6-羥基-4-側氧-1,4-二氫嘧啶-5-甲醯胺 |
| WO2017192485A1 (en) | 2016-05-03 | 2017-11-09 | Amgen Inc. | Heterocyclic triazole compounds as agonists of the apj receptor |
| KR102384668B1 (ko) * | 2016-06-14 | 2022-04-07 | 브리스톨-마이어스 스큅 컴퍼니 | Apj 효능제로서의 6-히드록시-5-(페닐/헤테로아릴술포닐)피리미딘-4(1h)-온 |
| JP6962941B2 (ja) | 2016-06-14 | 2021-11-05 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | Ａｐｊ受容体アゴニストとしての４−ヒドロキシ−３−スルホニルピリジン−２（１ｈ）−オン |
| JP7037558B2 (ja) | 2016-10-14 | 2022-03-16 | ブリストル－マイヤーズ スクイブ カンパニー | ３－スルホニル－５－アミノピリジン－２，４－ジオール ａｐｊアゴニスト |
| EP3541803B1 (en) | 2016-11-16 | 2020-12-23 | Amgen Inc. | Triazole pyridyl compounds as agonists of the apj receptor |
| US11046680B1 (en) | 2016-11-16 | 2021-06-29 | Amgen Inc. | Heteroaryl-substituted triazoles as APJ receptor agonists |
| WO2018093579A1 (en) | 2016-11-16 | 2018-05-24 | Amgen Inc. | Triazole phenyl compounds as agonists of the apj receptor |
| EP3541792B1 (en) | 2016-11-16 | 2020-12-23 | Amgen Inc. | Triazole furan compounds as agonists of the apj receptor |
| US11020395B2 (en) | 2016-11-16 | 2021-06-01 | Amgen Inc. | Cycloalkyl substituted triazole compounds as agonists of the APJ receptor |
| WO2018093576A1 (en) | 2016-11-16 | 2018-05-24 | Amgen Inc. | Alkyl substituted triazole compounds as agonists of the apj receptor |
| US11149040B2 (en) | 2017-11-03 | 2021-10-19 | Amgen Inc. | Fused triazole agonists of the APJ receptor |
| WO2019213006A1 (en) | 2018-05-01 | 2019-11-07 | Amgen Inc. | Substituted pyrimidinones as agonists of the apj receptor |
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| WO2016196771A1 (en) * | 2015-06-03 | 2016-12-08 | Bristol-Myers Squibb Company | 4-hydroxy-3-(heteroaryl)pyridine-2-one apj agonists for use in the treatment of cardiovascular disorders |
| KR101711744B1 (ko) | 2015-07-16 | 2017-03-02 | 경희대학교 산학협력단 | 옥사디아졸 유도체, 이의 제조방법 및 이를 포함하는 전자수송층 |
| KR102707502B1 (ko) | 2015-10-14 | 2024-09-13 | 브리스톨-마이어스 스큅 컴퍼니 | Apj 효능제로서의 2,4-디히드록시-니코틴아미드 |
| WO2017091513A1 (en) | 2015-11-24 | 2017-06-01 | Daiichi Sankyo Company, Limited | Novel azole derivatives as apelin receptor agonist |
| UY37005A (es) | 2015-12-04 | 2017-06-30 | Bristol-Myers Squibb Company Una Corporacion Del Estado De Delaware | Hidroxipirimidinonas sustituidas como agonistas del receptor de apelina y sus usos |
| BR112018012112A2 (pt) | 2015-12-16 | 2018-12-04 | Bristol-Myers Squibb Company | heteroaril-hidroxipirimidinonas como agonistas do receptor apj |
| TWI744301B (zh) * | 2016-03-24 | 2021-11-01 | 美商必治妥美雅史谷比公司 | 做為apj促效劑之6-羥基-4-側氧-1,4-二氫嘧啶-5-甲醯胺 |
| JP6962941B2 (ja) | 2016-06-14 | 2021-11-05 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | Ａｐｊ受容体アゴニストとしての４−ヒドロキシ−３−スルホニルピリジン−２（１ｈ）−オン |
| KR102384668B1 (ko) | 2016-06-14 | 2022-04-07 | 브리스톨-마이어스 스큅 컴퍼니 | Apj 효능제로서의 6-히드록시-5-(페닐/헤테로아릴술포닐)피리미딘-4(1h)-온 |
-
2017
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- 2017-03-23 WO PCT/US2017/023801 patent/WO2017165640A1/en not_active Ceased
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- 2017-03-23 AU AU2017238504A patent/AU2017238504B2/en not_active Ceased
- 2017-03-23 EP EP17715361.6A patent/EP3433247B1/en active Active
- 2017-03-23 KR KR1020187030255A patent/KR102433280B1/ko active Active
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- 2018-09-21 ZA ZA2018/06356A patent/ZA201806356B/en unknown
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Also Published As
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|---|---|
| UY37169A (es) | 2017-09-29 |
| EP3433247A1 (en) | 2019-01-30 |
| EA201892123A1 (ru) | 2019-02-28 |
| JP2019509319A (ja) | 2019-04-04 |
| TW201736362A (zh) | 2017-10-16 |
| IL261904B (en) | 2020-09-30 |
| BR112018068341A2 (pt) | 2019-01-15 |
| TWI744301B (zh) | 2021-11-01 |
| CL2018002671A1 (es) | 2019-01-25 |
| US20190002441A1 (en) | 2019-01-03 |
| CN109195963B (zh) | 2021-04-23 |
| MY189454A (en) | 2022-02-14 |
| CN109195963A (zh) | 2019-01-11 |
| ZA201806356B (en) | 2021-05-26 |
| US20170275272A1 (en) | 2017-09-28 |
| IL261904A (en) | 2018-10-31 |
| WO2017165640A1 (en) | 2017-09-28 |
| AR107973A1 (es) | 2018-07-04 |
| US10106528B2 (en) | 2018-10-23 |
| MX2018011194A (es) | 2019-01-10 |
| MA43761A (fr) | 2021-05-05 |
| KR102433280B1 (ko) | 2022-08-17 |
| JP6716711B2 (ja) | 2020-07-01 |
| AU2017238504A1 (en) | 2018-11-15 |
| SG11201808163WA (en) | 2018-10-30 |
| ES2895124T3 (es) | 2022-02-17 |
| EA037162B1 (ru) | 2021-02-12 |
| KR20180129836A (ko) | 2018-12-05 |
| MX379088B (es) | 2025-03-10 |
| EP3433247B1 (en) | 2021-09-08 |
| US10590113B2 (en) | 2020-03-17 |
| AU2017238504B2 (en) | 2021-05-27 |
| CA3018346A1 (en) | 2017-09-28 |
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