JP2019520379A - ピリミジン系の抗増殖剤 - Google Patents
ピリミジン系の抗増殖剤 Download PDFInfo
- Publication number
- JP2019520379A JP2019520379A JP2018569079A JP2018569079A JP2019520379A JP 2019520379 A JP2019520379 A JP 2019520379A JP 2018569079 A JP2018569079 A JP 2018569079A JP 2018569079 A JP2018569079 A JP 2018569079A JP 2019520379 A JP2019520379 A JP 2019520379A
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- JP
- Japan
- Prior art keywords
- formula
- alkylene
- pharmaceutically acceptable
- alkyl
- compound
- Prior art date
- Legal status (The legal status 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 status listed.)
- Pending
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- 0 C*Nc1ncc(cc(C)[n]2CC(C)(C)P)c2n1 Chemical compound C*Nc1ncc(cc(C)[n]2CC(C)(C)P)c2n1 0.000 description 29
- XDTMQSROBMDMFD-UHFFFAOYSA-N C1CCCCC1 Chemical compound C1CCCCC1 XDTMQSROBMDMFD-UHFFFAOYSA-N 0.000 description 1
- UDBDJLBGLSKZBU-UHFFFAOYSA-N C=[I](C=C(C=C1)[I]2CCCCC2)=C1N Chemical compound C=[I](C=C(C=C1)[I]2CCCCC2)=C1N UDBDJLBGLSKZBU-UHFFFAOYSA-N 0.000 description 1
- SKAGMIKIHFHLJW-UHFFFAOYSA-N CN(CC1)CCC1N1CCOCC1 Chemical compound CN(CC1)CCC1N1CCOCC1 SKAGMIKIHFHLJW-UHFFFAOYSA-N 0.000 description 1
- XAAVYZGZIOQPNQ-UHFFFAOYSA-N CN(CC1)CCN1c1ccc(C=C)nc1 Chemical compound CN(CC1)CCN1c1ccc(C=C)nc1 XAAVYZGZIOQPNQ-UHFFFAOYSA-N 0.000 description 1
- YNDFLLLXYYFZPL-UHFFFAOYSA-N CN1CCN(CS)CC1 Chemical compound CN1CCN(CS)CC1 YNDFLLLXYYFZPL-UHFFFAOYSA-N 0.000 description 1
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Classifications
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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
- C07D471/12—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
- C07D473/00—Heterocyclic compounds containing purine ring 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
- A61K31/495—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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
-
- 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
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- 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
-
- 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
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
- C07D487/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
- C07D487/20—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/22—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains four or more hetero rings
-
- 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
- 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
- C07D491/22—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 four or more hetero rings
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662357630P | 2016-07-01 | 2016-07-01 | |
| US62/357,630 | 2016-07-01 | ||
| PCT/US2017/040093 WO2018005860A1 (en) | 2016-07-01 | 2017-06-29 | Pyrimidine-based antiproliferative agents |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019520379A true JP2019520379A (ja) | 2019-07-18 |
| JP2019520379A5 JP2019520379A5 (https=) | 2021-03-11 |
Family
ID=60787753
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018569079A Pending JP2019520379A (ja) | 2016-07-01 | 2017-06-29 | ピリミジン系の抗増殖剤 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US10829490B2 (https=) |
| EP (2) | EP3478294A4 (https=) |
| JP (1) | JP2019520379A (https=) |
| KR (1) | KR20190025943A (https=) |
| CN (1) | CN109789143A (https=) |
| AU (1) | AU2017290748A1 (https=) |
| BR (1) | BR112018077136A2 (https=) |
| CA (1) | CA3028751A1 (https=) |
| EA (1) | EA201990187A1 (https=) |
| IL (1) | IL263910A (https=) |
| MX (1) | MX2019000200A (https=) |
| RU (1) | RU2019102647A (https=) |
| WO (1) | WO2018005860A1 (https=) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2023528257A (ja) * | 2020-05-19 | 2023-07-04 | ジー1 セラピューティクス, インコーポレイテッド | 医学的障害を治療するためのサイクリン依存性キナーゼ阻害化合物 |
| JP2023538521A (ja) * | 2020-08-07 | 2023-09-08 | エイビーエム セラピューティックス コーポレイション | キナーゼ阻害剤およびその使用 |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018005863A1 (en) * | 2016-07-01 | 2018-01-04 | G1 Therapeutics, Inc. | Pyrimidine-based compounds for the treatment of cancer |
| RU2019102647A (ru) * | 2016-07-01 | 2020-08-03 | Г1 Терапьютикс, Инк. | Антипролиферационные средства на основе пиримидина |
| JOP20170169A1 (ar) | 2016-08-29 | 2019-01-30 | Novartis Ag | مركبات بيريدازين ثلاثية الحلقة مندمجة تفيد في علاج العدوى بفيروس أورثوميكسو |
| KR20190092478A (ko) | 2016-12-05 | 2019-08-07 | 쥐원 쎄라퓨틱스, 인크. | 화학요법 레지멘 동안의 면역 반응의 보존 |
| MX2019008158A (es) | 2017-01-06 | 2019-12-09 | G1 Therapeutics Inc | Terapia de combinacion para el tratamiento del cancer. |
| CN111163780A (zh) | 2017-07-18 | 2020-05-15 | 诺维逊生物股份有限公司 | 作为腺苷拮抗剂的杂环化合物 |
| CA3070073A1 (en) | 2017-07-18 | 2019-01-24 | Nuvation Bio Inc. | 1,8-naphthyridinone compounds and uses thereof |
| JP2021514359A (ja) | 2018-02-15 | 2021-06-10 | ニューベイション・バイオ・インコーポレイテッドNuvation Bio Inc. | キナーゼ阻害剤としての複素環式化合物 |
| CN118878544A (zh) | 2018-02-28 | 2024-11-01 | 诺华股份有限公司 | 作为正粘病毒复制抑制剂用于治疗流感的化合物 |
| WO2019222521A1 (en) * | 2018-05-16 | 2019-11-21 | G1 Therapeutics, Inc. | Cdk inhibitors for the treatment of neoplastic disorders |
| CN109836400B (zh) * | 2018-09-17 | 2022-12-09 | 南通华祥医药科技有限公司 | 杂环化合物及其盐的制备方法 |
| US11066404B2 (en) | 2018-10-11 | 2021-07-20 | Incyte Corporation | Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors |
| WO2020140054A1 (en) | 2018-12-28 | 2020-07-02 | Spv Therapeutics Inc. | Cyclin-dependent kinase inhibitors |
| CN111377921A (zh) * | 2018-12-29 | 2020-07-07 | 武汉光谷通用名药物研究院有限公司 | Cdk4-flt3抑制剂及其用途 |
| AU2020208644A1 (en) | 2019-01-18 | 2021-08-26 | Nuvation Bio Inc. | Heterocyclic compounds as adenosine antagonists |
| WO2020150676A1 (en) | 2019-01-18 | 2020-07-23 | Nuvation Bio Inc. | 1,8-naphthyridinone compounds and uses thereof |
| US11384083B2 (en) | 2019-02-15 | 2022-07-12 | Incyte Corporation | Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors |
| TW202100520A (zh) | 2019-03-05 | 2021-01-01 | 美商英塞特公司 | 作為cdk2 抑制劑之吡唑基嘧啶基胺化合物 |
| WO2020205560A1 (en) | 2019-03-29 | 2020-10-08 | Incyte Corporation | Sulfonylamide compounds as cdk2 inhibitors |
| WO2020206034A1 (en) * | 2019-04-01 | 2020-10-08 | G1 Therapeutics, Inc. | Cell cycle inhibiting compounds for the treatment of medical disorders |
| WO2020223469A1 (en) | 2019-05-01 | 2020-11-05 | Incyte Corporation | N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer |
| US11447494B2 (en) | 2019-05-01 | 2022-09-20 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| WO2020260252A1 (en) | 2019-06-24 | 2020-12-30 | Boehringer Ingelheim International Gmbh | New macrocyclic compounds and derivatives as egfr inhibitors |
| CA3150681A1 (en) | 2019-08-14 | 2021-02-18 | Incyte Corporation | Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors |
| US12570660B2 (en) | 2019-08-16 | 2026-03-10 | Cyclacel Pharmaceuticals, Inc | Process for the preparation of a pyrimidino-diazepine derivative |
| US11851426B2 (en) | 2019-10-11 | 2023-12-26 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| US10988479B1 (en) | 2020-06-15 | 2021-04-27 | G1 Therapeutics, Inc. | Morphic forms of trilaciclib and methods of manufacture thereof |
| US20240000782A1 (en) * | 2020-12-02 | 2024-01-04 | Telios Pharma, Inc. | Methods and compositions for treating an ophthalmic condition |
| IL308318A (en) * | 2021-05-11 | 2024-01-01 | Abbvie Inc | Dosage regimens of VENETOCLAX for use in the treatment of MYELODYSPLASTIC syndromes in combination with a CYP3A inhibitor and AZACITIDINE |
| US11981671B2 (en) | 2021-06-21 | 2024-05-14 | Incyte Corporation | Bicyclic pyrazolyl amines as CDK2 inhibitors |
| CN113788837B (zh) * | 2021-08-02 | 2022-08-26 | 深圳湾实验室坪山生物医药研发转化中心 | Trilaciclib的合成方法 |
| CN113786491B (zh) * | 2021-10-08 | 2023-03-28 | 中国医学科学院医药生物技术研究所 | 一种含汉防己甲素、二氢槲皮素或槲皮素的抗肿瘤联用制剂 |
| US11976073B2 (en) | 2021-12-10 | 2024-05-07 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| IL317242A (en) * | 2022-06-20 | 2025-01-01 | Incyclix Bio Llc | Cyclin-dependent kinase 2 inhibitors for medical treatment |
| IT202300001971A1 (it) * | 2023-02-07 | 2024-08-07 | Olon Spa | Processo per la preparazione di trilaciclib o un suo sale. |
| WO2025238662A1 (en) * | 2024-05-15 | 2025-11-20 | Msn Laboratories Private Limited, R&D Center | Improved process for the preparation of 4-amino-n-[(1s)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinecarboxamide and its salts |
Citations (8)
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| JP2006516561A (ja) * | 2003-01-17 | 2006-07-06 | ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー | 細胞増殖の阻害剤としての2−アミノピリジン置換ヘテロ環類 |
| JP2012500785A (ja) * | 2008-08-22 | 2012-01-12 | ノバルティス アーゲー | Cdk阻害剤としてのピロロピリミジン化合物 |
| JP2013543845A (ja) * | 2010-10-25 | 2013-12-09 | ジー1、セラピューティクス、インコーポレイテッド | Cdk阻害剤 |
| US20140274896A1 (en) * | 2013-03-15 | 2014-09-18 | G1 Therapeutics, Inc. | Transient Protection of Hematopoietic Stem and Progenitor Cells Against Ionizing Radiation |
| WO2016040858A1 (en) * | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Combinations and dosing regimes to treat rb-positive tumors |
| JP2016514689A (ja) * | 2013-03-15 | 2016-05-23 | ジー1、セラピューティクス、インコーポレイテッドG1 Therapeutics, Inc. | Rbポジティブ異常細胞増殖に対するhspc温存治療 |
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| JP2023538521A (ja) * | 2020-08-07 | 2023-09-08 | エイビーエム セラピューティックス コーポレイション | キナーゼ阻害剤およびその使用 |
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| RU2019102647A3 (https=) | 2020-08-03 |
| IL263910A (en) | 2019-01-31 |
| US20210047328A1 (en) | 2021-02-18 |
| BR112018077136A2 (pt) | 2019-04-30 |
| MX2019000200A (es) | 2019-09-26 |
| US20190135811A1 (en) | 2019-05-09 |
| RU2019102647A (ru) | 2020-08-03 |
| US10829490B2 (en) | 2020-11-10 |
| EA201990187A1 (ru) | 2019-07-31 |
| AU2017290748A1 (en) | 2019-01-17 |
| EP3478294A4 (en) | 2020-06-10 |
| CN109789143A (zh) | 2019-05-21 |
| EP3858835A1 (en) | 2021-08-04 |
| CA3028751A1 (en) | 2018-01-04 |
| KR20190025943A (ko) | 2019-03-12 |
| EP3478294A1 (en) | 2019-05-08 |
| WO2018005860A1 (en) | 2018-01-04 |
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