UA122882C2 - Синтез індазолів - Google Patents

Синтез індазолів

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Publication number
UA122882C2
UA122882C2 UAA201811328A UAA201811328A UA122882C2 UA 122882 C2 UA122882 C2 UA 122882C2 UA A201811328 A UAA201811328 A UA A201811328A UA A201811328 A UAA201811328 A UA A201811328A UA 122882 C2 UA122882 C2 UA 122882C2
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UA
Ukraine
Prior art keywords
indazoles
synthesis
intermediate compounds
substituted indazole
novel
Prior art date
Application number
UAA201811328A
Other languages
English (en)
Inventor
Тобіас Талер
Тобиас Талер
Йоганнес Платцек
Ніколя Гімон
Николя Гимон
Original Assignee
Байєр Фарма Акцієнгезелльшафт
Байер Фарма Акциенгезелльшафт
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Байєр Фарма Акцієнгезелльшафт, Байер Фарма Акциенгезелльшафт filed Critical Байєр Фарма Акцієнгезелльшафт
Publication of UA122882C2 publication Critical patent/UA122882C2/uk

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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
    • C07D401/02—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
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
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    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • 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
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • A61P37/02—Immunomodulators
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Reproductive Health (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Transplantation (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Даний винахід належить до нового способу одержання 2-заміщеного індазолу формули (І) , (І) до нових проміжних сполук, і до застосування проміжних сполук для одержання зазначеного 2-заміщеного індазолу.
UAA201811328A 2016-04-29 2017-04-25 Синтез індазолів UA122882C2 (uk)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP16167650 2016-04-29
EP16167649 2016-04-29
PCT/EP2017/059748 WO2017186693A1 (en) 2016-04-29 2017-04-25 Synthesis of indazoles

Publications (1)

Publication Number Publication Date
UA122882C2 true UA122882C2 (uk) 2021-01-13

Family

ID=58579196

Family Applications (2)

Application Number Title Priority Date Filing Date
UAA201811328A UA122882C2 (uk) 2016-04-29 2017-04-25 Синтез індазолів
UAA201811327A UA123550C2 (uk) 2016-04-29 2017-04-25 Кристалічні форми n-[2-(3-гідрокси-3-метилбутил)-6-(2-гідроксипропан-2-іл)-2н-індазол-5-іл]-6-(трифторметил)піридин-2-карбоксаміду

Family Applications After (1)

Application Number Title Priority Date Filing Date
UAA201811327A UA123550C2 (uk) 2016-04-29 2017-04-25 Кристалічні форми n-[2-(3-гідрокси-3-метилбутил)-6-(2-гідроксипропан-2-іл)-2н-індазол-5-іл]-6-(трифторметил)піридин-2-карбоксаміду

Country Status (37)

Country Link
US (2) US10633365B2 (uk)
EP (2) EP3448847A1 (uk)
JP (2) JP6916207B2 (uk)
KR (2) KR102409105B1 (uk)
CN (3) CN109071491B (uk)
AU (2) AU2017257208B2 (uk)
BR (1) BR112018072247A2 (uk)
CA (2) CA3022329A1 (uk)
CL (2) CL2018003085A1 (uk)
CO (2) CO2018011607A2 (uk)
CU (1) CU24593B1 (uk)
DK (1) DK3448849T3 (uk)
DO (1) DOP2018000236A (uk)
EA (1) EA038103B1 (uk)
EC (1) ECSP18081451A (uk)
ES (1) ES2801800T3 (uk)
GE (1) GEP20217230B (uk)
HU (1) HUE049331T2 (uk)
IL (2) IL262391B (uk)
JO (2) JOP20170102B1 (uk)
LT (1) LT3448849T (uk)
MA (1) MA44758A (uk)
MX (2) MX2018013227A (uk)
NI (1) NI201800111A (uk)
PE (2) PE20190172A1 (uk)
PH (1) PH12018502288A1 (uk)
PL (1) PL3448849T3 (uk)
PT (1) PT3448849T (uk)
RS (1) RS60419B1 (uk)
SG (2) SG11201808686VA (uk)
SI (1) SI3448849T1 (uk)
SV (1) SV2018005776A (uk)
TN (1) TN2018000359A1 (uk)
TW (3) TWI671291B (uk)
UA (2) UA122882C2 (uk)
UY (2) UY37214A (uk)
WO (2) WO2017186700A1 (uk)

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US10435396B2 (en) 2016-03-03 2019-10-08 Bayer Pharma Aktiegesellschaft 2-substituted indazoles, methods for producing same, pharmaceutical preparations that contain same, and use of same to produce drugs
TN2018000359A1 (en) 2016-04-29 2020-06-15 Bayer Pharma AG Crystalline forms of n-[2-(3-hydroxy-3-methylbutyl)-6-(2-hydroxypropan-2-yl)-2h-indazol-5-yl]-6-(trifluoromethyl)pyridine-2-carboxamide.
RS64928B1 (sr) 2016-04-29 2023-12-29 Bayer Pharma AG Polimorfni oblik n-{6-(2-hidroksipropan-2-il)-2-[2-(metilsulfonil)etil]-2h-indazol-5-il}-6-(trifluorometil)piridin-2-karboksamida
SG10202011653WA (en) 2016-06-01 2020-12-30 Bayer Pharma AG Use of 2-substituted indazoles for the treatment and prophylaxis of autoimmune diseases
CA3025847A1 (en) * 2016-06-01 2017-12-07 Bayer Animal Health Gmbh Substituted indazoles ueful in the treatment of allergic dermatitis in animals
BR112020026507A8 (pt) 2018-06-25 2023-01-31 Chia Tai Tianqing Pharmaceutical Group Co Ltd Composto de isotiazolo[5,4-d]pirimidinas como inibidor de irak4
KR102392788B1 (ko) 2019-01-08 2022-04-28 주식회사 엘지에너지솔루션 폴더블 사이드 플레이트를 구비하는 배터리 모듈 및 그 제조 방법
CN111499612B (zh) * 2019-01-30 2022-12-30 上海美悦生物科技发展有限公司 一种作为irak抑制剂的化合物及其制备方法和用途
CN113521079A (zh) * 2020-04-20 2021-10-22 上海领泰生物医药科技有限公司 Irak4抑制剂在治疗ali/ards中的应用

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JO3705B1 (ar) * 2014-11-26 2021-01-31 Bayer Pharma AG إندازولات مستبدلة جديدة، عمليات لتحضيرها، مستحضرات دوائية تحتوي عليها واستخدامها في إنتاج أدوية
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US10435396B2 (en) 2016-03-03 2019-10-08 Bayer Pharma Aktiegesellschaft 2-substituted indazoles, methods for producing same, pharmaceutical preparations that contain same, and use of same to produce drugs
EP3219329A1 (en) * 2016-03-17 2017-09-20 Bayer Pharma Aktiengesellschaft Combinations of copanlisib
RS64928B1 (sr) 2016-04-29 2023-12-29 Bayer Pharma AG Polimorfni oblik n-{6-(2-hidroksipropan-2-il)-2-[2-(metilsulfonil)etil]-2h-indazol-5-il}-6-(trifluorometil)piridin-2-karboksamida
TN2018000359A1 (en) 2016-04-29 2020-06-15 Bayer Pharma AG Crystalline forms of n-[2-(3-hydroxy-3-methylbutyl)-6-(2-hydroxypropan-2-yl)-2h-indazol-5-yl]-6-(trifluoromethyl)pyridine-2-carboxamide.
SG10202011653WA (en) 2016-06-01 2020-12-30 Bayer Pharma AG Use of 2-substituted indazoles for the treatment and prophylaxis of autoimmune diseases
CA3025847A1 (en) 2016-06-01 2017-12-07 Bayer Animal Health Gmbh Substituted indazoles ueful in the treatment of allergic dermatitis in animals

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RS60419B1 (sr) 2020-07-31
EP3448849A1 (en) 2019-03-06
CL2018003097A1 (es) 2019-02-15
UA123550C2 (uk) 2021-04-21
TW201738233A (zh) 2017-11-01
AU2017256659B2 (en) 2021-05-27
BR112018072247A2 (pt) 2019-02-12
PT3448849T (pt) 2020-06-30
ECSP18081451A (es) 2018-11-30
TW201936599A (zh) 2019-09-16
HUE049331T2 (hu) 2020-09-28
WO2017186700A1 (en) 2017-11-02
UY37217A (es) 2017-11-30
CU24593B1 (es) 2022-05-11
JP2019514924A (ja) 2019-06-06
AU2017257208B2 (en) 2022-01-20
PL3448849T3 (pl) 2020-12-14
JOP20170101B1 (ar) 2022-03-14
US20190152944A1 (en) 2019-05-23
IL262413B (en) 2021-05-31
TWI671291B (zh) 2019-09-11
MA44758A (fr) 2019-03-06
US10633365B2 (en) 2020-04-28
MX2018013227A (es) 2019-02-13
JOP20170102B1 (ar) 2023-09-17
TWI651316B (zh) 2019-02-21
GEP20217230B (en) 2021-03-10
KR20190002468A (ko) 2019-01-08
CN109071491B (zh) 2020-08-21
UY37214A (es) 2017-11-30
CA3022327A1 (en) 2017-11-02
AU2017256659A1 (en) 2018-10-25
IL262391B (en) 2022-03-01
CA3022329A1 (en) 2017-11-02
CN109071491A (zh) 2018-12-21
SG11201809172WA (en) 2018-11-29
US10501437B2 (en) 2019-12-10
EA038103B1 (ru) 2021-07-06
DK3448849T3 (da) 2020-06-29
JP2019514921A (ja) 2019-06-06
NI201800111A (es) 2019-08-29
SG11201808686VA (en) 2018-11-29
TW201738231A (zh) 2017-11-01
DOP2018000236A (es) 2019-01-15
KR20180137498A (ko) 2018-12-27
EP3448849B1 (en) 2020-05-13
CO2018011655A2 (es) 2018-11-13
CU20180130A7 (es) 2019-06-04
LT3448849T (lt) 2020-09-25
PE20240651A1 (es) 2024-04-04
SV2018005776A (es) 2019-03-18
CO2018011607A2 (es) 2018-11-22
PE20190172A1 (es) 2019-02-01
EA201892407A1 (ru) 2019-05-31
PH12018502288A1 (en) 2019-07-15
CL2018003085A1 (es) 2019-02-15
KR102379948B1 (ko) 2022-03-31
ES2801800T3 (es) 2021-01-13
MX2018013232A (es) 2019-02-13
IL262391A (en) 2018-12-31
TN2018000359A1 (en) 2020-06-15
AU2017257208A1 (en) 2018-11-01
KR102409105B1 (ko) 2022-06-16
US20190144420A1 (en) 2019-05-16
WO2017186693A1 (en) 2017-11-02
EP3448847A1 (en) 2019-03-06
CN109415339A (zh) 2019-03-01
JP6821701B2 (ja) 2021-01-27
JP6916207B2 (ja) 2021-08-11
IL262413A (en) 2018-12-31
CN112898269A (zh) 2021-06-04
SI3448849T1 (sl) 2020-07-31
BR112018072213A2 (pt) 2019-02-12

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