BR112018015419A2 - degradantes seletivos de receptor de estrogênio e os usos dos mesmos - Google Patents
degradantes seletivos de receptor de estrogênio e os usos dos mesmosInfo
- Publication number
- BR112018015419A2 BR112018015419A2 BR112018015419A BR112018015419A BR112018015419A2 BR 112018015419 A2 BR112018015419 A2 BR 112018015419A2 BR 112018015419 A BR112018015419 A BR 112018015419A BR 112018015419 A BR112018015419 A BR 112018015419A BR 112018015419 A2 BR112018015419 A2 BR 112018015419A2
- Authority
- BR
- Brazil
- Prior art keywords
- estrogen receptor
- selective estrogen
- degradants
- present
- receptor degradants
- Prior art date
Links
- 239000008380 degradant Substances 0.000 title 1
- 102000015694 estrogen receptors Human genes 0.000 title 1
- 108010038795 estrogen receptors Proteins 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002062 proliferating effect Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4355—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/436—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4365—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/473—Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- 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
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/32—Antioestrogens
-
- 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
-
- 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
- C07D471/12—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 three hetero rings
- C07D471/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
- C07D491/14—Ortho-condensed systems
- C07D491/147—Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D495/14—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201662291921P | 2016-02-05 | 2016-02-05 | |
US62/291,921 | 2016-02-05 | ||
PCT/US2017/016452 WO2017136688A1 (en) | 2016-02-05 | 2017-02-03 | Selective estrogen receptor degraders and uses thereof |
Publications (2)
Publication Number | Publication Date |
---|---|
BR112018015419A2 true BR112018015419A2 (pt) | 2018-12-18 |
BR112018015419B1 BR112018015419B1 (pt) | 2024-01-30 |
Family
ID=59501091
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112018015419-9A BR112018015419B1 (pt) | 2016-02-05 | 2017-02-03 | Degradantes seletivos de receptor de estrogênio, seus usos, e composição farmacêutica |
Country Status (15)
Country | Link |
---|---|
US (4) | US10647724B2 (pt) |
EP (1) | EP3411034B1 (pt) |
JP (1) | JP6905539B2 (pt) |
KR (1) | KR102479822B1 (pt) |
CN (2) | CN113004273A (pt) |
AU (1) | AU2017213614B2 (pt) |
BR (1) | BR112018015419B1 (pt) |
CA (1) | CA3012078C (pt) |
DK (1) | DK3411034T3 (pt) |
ES (1) | ES2842579T3 (pt) |
IL (1) | IL260789B (pt) |
MX (1) | MX2018009496A (pt) |
RU (1) | RU2734501C2 (pt) |
WO (1) | WO2017136688A1 (pt) |
ZA (1) | ZA201805573B (pt) |
Families Citing this family (18)
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TWI784255B (zh) | 2014-12-18 | 2022-11-21 | 瑞士商赫孚孟拉羅股份公司 | 四氫-吡啶并[3,4-b]吲哚雌激素受體調節劑及其用途 |
CN107428758B (zh) * | 2015-11-12 | 2020-08-04 | 浙江海正药业股份有限公司 | 丙烯酸类衍生物、其制备方法及其在医药上的用途 |
CN113004273A (zh) * | 2016-02-05 | 2021-06-22 | 益方生物科技(上海)股份有限公司 | 选择性雌激素受体降解物及其用途 |
CN108699514B (zh) * | 2016-02-26 | 2023-07-07 | 隆萨沃克斯维尔股份有限公司 | 汇集肝细胞的方法 |
RU2738646C2 (ru) | 2016-04-01 | 2020-12-15 | РЕКЬЮРИУМ АйПи ХОЛДИНГС, ЛЛС | Модуляторы эстрогеновых рецепторов |
CN109311876B (zh) * | 2016-06-16 | 2022-05-03 | 豪夫迈·罗氏有限公司 | 杂芳基雌激素受体调节剂及其用途 |
CN107814798B (zh) * | 2016-09-14 | 2020-11-03 | 四川科伦博泰生物医药股份有限公司 | 3-取代丙烯酸类化合物及其制备方法和用途 |
WO2018130124A1 (zh) * | 2017-01-11 | 2018-07-19 | 南京圣和药业股份有限公司 | 作为选择性雌激素受体下调剂的三环类化合物及其应用 |
US11098040B2 (en) | 2018-02-28 | 2021-08-24 | Ferro Therapeutics, Inc. | Compounds and methods of use |
WO2019192533A1 (zh) * | 2018-04-04 | 2019-10-10 | 深圳福沃药业有限公司 | 用于治疗乳腺癌的雌激素受体降解剂 |
LT3810283T (lt) | 2018-06-21 | 2023-08-25 | F. Hoffmann-La Roche Ag | 3-((1r,3r)-1-(2,6-difluor-4-((1-(3-fluorpropil)azetidin-3- il)amino) fenil)-3-metil-1,3,4,9-tetrahidro-2h-pirido[3,4-b]indol-2-il)- 2,2- difluorpropan-1-olio tartrato druskos kietosios formos, jų paruošimo procesas ir jų naudojimo būdai vėžiui gydyti |
JP7571006B2 (ja) | 2018-08-17 | 2024-10-22 | ジェネンテック, インコーポレイテッド | 乳がんの処置のための診断的および治療的方法 |
CN113164467B (zh) * | 2018-12-24 | 2023-12-26 | 益方生物科技(上海)股份有限公司 | 选择性雌激素受体降解剂的新型盐 |
US11040964B2 (en) | 2019-02-27 | 2021-06-22 | Ferro Therapeutics, Inc. | Compounds and methods of use |
CN114929696A (zh) * | 2019-05-24 | 2022-08-19 | 浙江海正药业股份有限公司 | 丙烯酸类衍生物的晶型及其制备方法和用途 |
US11278532B2 (en) | 2019-08-06 | 2022-03-22 | Recurium Ip Holdings, Llc | Estrogen receptor modulators for treating mutants |
WO2021253380A1 (en) * | 2020-06-19 | 2021-12-23 | InventisBio Co., Ltd. | Oral formulations and uses thereof |
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WO2018019793A1 (en) | 2016-07-25 | 2018-02-01 | Astrazeneca Ab | N-(2-(4-((1r,3r)-3-methyl-2,3,4,9-tetrahydro-1h-pyrido[3,4-b]indol-1-yl)phenoxy)ethyl)propan-1-amine derivatives and related compounds as selective down-regulators of the estrogen receptor for treating cancer |
CN110139863B (zh) | 2016-10-28 | 2022-02-18 | 罗欣健康科技发展(北京)有限公司 | 作为雌激素受体降解剂的吲哚并取代哌啶类化合物 |
WO2018130124A1 (zh) | 2017-01-11 | 2018-07-19 | 南京圣和药业股份有限公司 | 作为选择性雌激素受体下调剂的三环类化合物及其应用 |
KR102246668B1 (ko) | 2017-01-30 | 2021-04-29 | 아스트라제네카 아베 | 에스트로겐 수용체 조절인자 |
CN113164467B (zh) * | 2018-12-24 | 2023-12-26 | 益方生物科技(上海)股份有限公司 | 选择性雌激素受体降解剂的新型盐 |
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2017
- 2017-02-03 CN CN202110236070.7A patent/CN113004273A/zh active Pending
- 2017-02-03 WO PCT/US2017/016452 patent/WO2017136688A1/en active Application Filing
- 2017-02-03 JP JP2018560447A patent/JP6905539B2/ja active Active
- 2017-02-03 CA CA3012078A patent/CA3012078C/en active Active
- 2017-02-03 DK DK17748247.8T patent/DK3411034T3/da active
- 2017-02-03 KR KR1020187025594A patent/KR102479822B1/ko active IP Right Grant
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- 2017-02-03 ES ES17748247T patent/ES2842579T3/es active Active
- 2017-02-03 AU AU2017213614A patent/AU2017213614B2/en active Active
- 2017-02-03 BR BR112018015419-9A patent/BR112018015419B1/pt active IP Right Grant
- 2017-02-03 MX MX2018009496A patent/MX2018009496A/es unknown
- 2017-02-03 CN CN201780008535.5A patent/CN109362222B/zh active Active
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2018
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DK3411034T3 (da) | 2021-01-11 |
AU2017213614B2 (en) | 2022-09-01 |
AU2017213614A1 (en) | 2018-08-09 |
CN109362222B (zh) | 2021-03-19 |
KR102479822B1 (ko) | 2022-12-21 |
US20210253592A1 (en) | 2021-08-19 |
KR20180104161A (ko) | 2018-09-19 |
RU2734501C2 (ru) | 2020-10-19 |
RU2018128318A (ru) | 2020-03-05 |
ZA201805573B (en) | 2020-12-23 |
JP2019504890A (ja) | 2019-02-21 |
CA3012078C (en) | 2024-01-30 |
US10647724B2 (en) | 2020-05-12 |
MX2018009496A (es) | 2018-12-11 |
US11014936B2 (en) | 2021-05-25 |
EP3411034B1 (en) | 2020-11-25 |
WO2017136688A1 (en) | 2017-08-10 |
US20240043442A1 (en) | 2024-02-08 |
JP6905539B2 (ja) | 2021-07-21 |
CN109362222A (zh) | 2019-02-19 |
US20200048250A1 (en) | 2020-02-13 |
CN113004273A (zh) | 2021-06-22 |
BR112018015419B1 (pt) | 2024-01-30 |
IL260789B (en) | 2021-03-25 |
NZ744516A (en) | 2024-05-31 |
US20200040001A1 (en) | 2020-02-06 |
EP3411034A4 (en) | 2019-08-28 |
CA3012078A1 (en) | 2017-08-10 |
ES2842579T3 (es) | 2021-07-14 |
EP3411034A1 (en) | 2018-12-12 |
RU2018128318A3 (pt) | 2020-04-02 |
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