RU2018145776A - Комбинированные терапии модуляторами фарензоидного х-рецептора (fxr) - Google Patents
Комбинированные терапии модуляторами фарензоидного х-рецептора (fxr) Download PDFInfo
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- RU2018145776A RU2018145776A RU2018145776A RU2018145776A RU2018145776A RU 2018145776 A RU2018145776 A RU 2018145776A RU 2018145776 A RU2018145776 A RU 2018145776A RU 2018145776 A RU2018145776 A RU 2018145776A RU 2018145776 A RU2018145776 A RU 2018145776A
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- Prior art keywords
- optionally substituted
- heteroaryl
- alkylene
- aryl
- group
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- 238000002560 therapeutic procedure Methods 0.000 title 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 69
- -1 substituted Chemical class 0.000 claims 67
- 125000002947 alkylene group Chemical group 0.000 claims 62
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 54
- 229910052739 hydrogen Inorganic materials 0.000 claims 42
- 239000001257 hydrogen Substances 0.000 claims 42
- 150000002431 hydrogen Chemical class 0.000 claims 38
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 37
- 125000003118 aryl group Chemical group 0.000 claims 33
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 29
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 29
- 125000003107 substituted aryl group Chemical group 0.000 claims 29
- 239000000126 substance Substances 0.000 claims 28
- 229910052736 halogen Inorganic materials 0.000 claims 19
- 150000002367 halogens Chemical class 0.000 claims 19
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 12
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 12
- 229910052757 nitrogen Inorganic materials 0.000 claims 11
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 11
- 239000012453 solvate Substances 0.000 claims 11
- 150000001875 compounds Chemical class 0.000 claims 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 10
- 230000003143 atherosclerotic effect Effects 0.000 claims 8
- 201000010099 disease Diseases 0.000 claims 8
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- 201000001320 Atherosclerosis Diseases 0.000 claims 6
- 208000024172 Cardiovascular disease Diseases 0.000 claims 6
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- 125000004432 carbon atom Chemical group C* 0.000 claims 5
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- PNDKCRDVVKJPKG-WHERJAGFSA-N cenicriviroc Chemical compound C1=CC(OCCOCCCC)=CC=C1C1=CC=C(N(CC(C)C)CCC\C(=C/2)C(=O)NC=3C=CC(=CC=3)[S@@](=O)CC=3N(C=NC=3)CCC)C\2=C1 PNDKCRDVVKJPKG-WHERJAGFSA-N 0.000 claims 4
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- UFJGFNHRMPMALC-UHFFFAOYSA-N ethyl 2,7-dioxo-2,7-dihydro-3h-naphtho[1,2,3-de]quinoline-1-carboxylate Chemical compound C12=CC=CC=C2C(=O)C2=CC=CC3=C2C1=C(C(=O)OCC)C(=O)N3 UFJGFNHRMPMALC-UHFFFAOYSA-N 0.000 claims 4
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- XUKGFHHTSUKORV-UHFFFAOYSA-N n-[5-(cyclopropylamino)-7-(trifluoromethyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl]pyridine-3-carboxamide Chemical compound N12N=C(NC(=O)C=3C=NC=CC=3)N=C2C=C(C(F)(F)F)C=C1NC1CC1 XUKGFHHTSUKORV-UHFFFAOYSA-N 0.000 claims 4
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- CNPVJJQCETWNEU-CYFREDJKSA-N (4,6-dimethyl-5-pyrimidinyl)-[4-[(3S)-4-[(1R)-2-methoxy-1-[4-(trifluoromethyl)phenyl]ethyl]-3-methyl-1-piperazinyl]-4-methyl-1-piperidinyl]methanone Chemical compound N([C@@H](COC)C=1C=CC(=CC=1)C(F)(F)F)([C@H](C1)C)CCN1C(CC1)(C)CCN1C(=O)C1=C(C)N=CN=C1C CNPVJJQCETWNEU-CYFREDJKSA-N 0.000 claims 2
- ZMZRKOASUWINDA-VEABSNGSSA-N (4s)-4-[[(2s)-2-amino-3-carboxypropanoyl]amino]-5-[[(2s)-1-[[(2s)-1-carboxy-3-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-oxopentanoic acid Chemical compound OC(=O)C[C@@H](C=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@@H](N)CC(O)=O ZMZRKOASUWINDA-VEABSNGSSA-N 0.000 claims 2
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- GWNOTCOIYUNTQP-FQLXRVMXSA-N 4-[4-[[(3r)-1-butyl-3-[(r)-cyclohexyl(hydroxy)methyl]-2,5-dioxo-1,4,9-triazaspiro[5.5]undecan-9-yl]methyl]phenoxy]benzoic acid Chemical compound N([C@@H](C(=O)N1CCCC)[C@H](O)C2CCCCC2)C(=O)C1(CC1)CCN1CC(C=C1)=CC=C1OC1=CC=C(C(O)=O)C=C1 GWNOTCOIYUNTQP-FQLXRVMXSA-N 0.000 claims 2
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- 229960004034 sitagliptin Drugs 0.000 claims 2
- MFFMDFFZMYYVKS-SECBINFHSA-N sitagliptin Chemical compound C([C@H](CC(=O)N1CC=2N(C(=NN=2)C(F)(F)F)CC1)N)C1=CC(F)=C(F)C=C1F MFFMDFFZMYYVKS-SECBINFHSA-N 0.000 claims 2
- 229910052708 sodium Inorganic materials 0.000 claims 2
- 239000011734 sodium Substances 0.000 claims 2
- 229950007151 taspoglutide Drugs 0.000 claims 2
- 108010048573 taspoglutide Proteins 0.000 claims 2
- WRGVLTAWMNZWGT-VQSPYGJZSA-N taspoglutide Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 WRGVLTAWMNZWGT-VQSPYGJZSA-N 0.000 claims 2
- WGRQANOPCQRCME-PMACEKPBSA-N teneligliptin Chemical compound O=C([C@H]1NC[C@H](C1)N1CCN(CC1)C1=CC(=NN1C=1C=CC=CC=1)C)N1CCSC1 WGRQANOPCQRCME-PMACEKPBSA-N 0.000 claims 2
- 229950000034 teneligliptin Drugs 0.000 claims 2
- IWYJYHUNXVAVAA-OAHLLOKOSA-N trelagliptin Chemical compound C=1C(F)=CC=C(C#N)C=1CN1C(=O)N(C)C(=O)C=C1N1CCC[C@@H](N)C1 IWYJYHUNXVAVAA-OAHLLOKOSA-N 0.000 claims 2
- 229950010728 trelagliptin Drugs 0.000 claims 2
- 229950009860 vicriviroc Drugs 0.000 claims 2
- 229960001254 vildagliptin Drugs 0.000 claims 2
- SYOKIDBDQMKNDQ-XWTIBIIYSA-N vildagliptin Chemical compound C1C(O)(C2)CC(C3)CC1CC32NCC(=O)N1CCC[C@H]1C#N SYOKIDBDQMKNDQ-XWTIBIIYSA-N 0.000 claims 2
- SCVHJVCATBPIHN-SJCJKPOMSA-N (3s)-3-[[(2s)-2-[[2-(2-tert-butylanilino)-2-oxoacetyl]amino]propanoyl]amino]-4-oxo-5-(2,3,5,6-tetrafluorophenoxy)pentanoic acid Chemical compound N([C@@H](C)C(=O)N[C@@H](CC(O)=O)C(=O)COC=1C(=C(F)C=C(F)C=1F)F)C(=O)C(=O)NC1=CC=CC=C1C(C)(C)C SCVHJVCATBPIHN-SJCJKPOMSA-N 0.000 claims 1
- DIKVGBMQYOULPY-UHFFFAOYSA-N 6-(3,4-difluorobenzoyl)-4,4-dimethyl-N-propan-2-yl-3-(trifluoromethyl)-2,5-dihydropyrazolo[3,4-d]azepine-8-carboxamide Chemical compound CC(C)NC(=O)C1=CN(CC(C)(C)C2=C1NN=C2C(F)(F)F)C(=O)C1=CC(F)=C(F)C=C1 DIKVGBMQYOULPY-UHFFFAOYSA-N 0.000 claims 1
- 206010003827 Autoimmune hepatitis Diseases 0.000 claims 1
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims 1
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims 1
- 206010008609 Cholangitis sclerosing Diseases 0.000 claims 1
- 206010008631 Cholera Diseases 0.000 claims 1
- 206010010317 Congenital absence of bile ducts Diseases 0.000 claims 1
- 206010012735 Diarrhoea Diseases 0.000 claims 1
- 208000018522 Gastrointestinal disease Diseases 0.000 claims 1
- 206010019799 Hepatitis viral Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims 1
- 206010000059 abdominal discomfort Diseases 0.000 claims 1
- 201000005271 biliary atresia Diseases 0.000 claims 1
- 229960001713 canagliflozin Drugs 0.000 claims 1
- VHOFTEAWFCUTOS-TUGBYPPCSA-N canagliflozin hydrate Chemical compound O.CC1=CC=C([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)C=C1CC(S1)=CC=C1C1=CC=C(F)C=C1.CC1=CC=C([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)C=C1CC(S1)=CC=C1C1=CC=C(F)C=C1 VHOFTEAWFCUTOS-TUGBYPPCSA-N 0.000 claims 1
- 201000001883 cholelithiasis Diseases 0.000 claims 1
- 235000012000 cholesterol Nutrition 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 229940125904 compound 1 Drugs 0.000 claims 1
- 229940125782 compound 2 Drugs 0.000 claims 1
- 229940126214 compound 3 Drugs 0.000 claims 1
- 208000010643 digestive system disease Diseases 0.000 claims 1
- 229950000234 emricasan Drugs 0.000 claims 1
- 201000005206 focal segmental glomerulosclerosis Diseases 0.000 claims 1
- 231100000854 focal segmental glomerulosclerosis Toxicity 0.000 claims 1
- 208000018685 gastrointestinal system disease Diseases 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 201000006370 kidney failure Diseases 0.000 claims 1
- 208000007232 portal hypertension Diseases 0.000 claims 1
- 201000000742 primary sclerosing cholangitis Diseases 0.000 claims 1
- 201000002793 renal fibrosis Diseases 0.000 claims 1
- 208000010157 sclerosing cholangitis Diseases 0.000 claims 1
- 201000001862 viral hepatitis Diseases 0.000 claims 1
Classifications
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Gastroenterology & Hepatology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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| US201662341487P | 2016-05-25 | 2016-05-25 | |
| US201662341482P | 2016-05-25 | 2016-05-25 | |
| US62/341,487 | 2016-05-25 | ||
| US62/341,482 | 2016-05-25 | ||
| PCT/US2017/034564 WO2017205684A1 (en) | 2016-05-25 | 2017-05-25 | Combination therapies with farnesoid x receptor (fxr) modulators |
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| RU2018145776A true RU2018145776A (ru) | 2020-06-26 |
| RU2018145776A3 RU2018145776A3 (https=) | 2021-03-01 |
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| EP (1) | EP3463373A4 (https=) |
| JP (1) | JP2019517478A (https=) |
| KR (1) | KR20190040936A (https=) |
| CN (1) | CN109843298A (https=) |
| AU (1) | AU2017270221A1 (https=) |
| BR (1) | BR112018073460A2 (https=) |
| CA (1) | CA3025007A1 (https=) |
| IL (1) | IL263179A (https=) |
| MX (1) | MX2018014024A (https=) |
| RU (1) | RU2018145776A (https=) |
| SG (2) | SG10202011660RA (https=) |
| WO (1) | WO2017205684A1 (https=) |
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| RU2019144064A (ru) * | 2017-06-02 | 2021-07-13 | Акарна Терапьютикс, Лтд. | Конденсированные бициклические соединения |
| US11590161B2 (en) | 2018-08-13 | 2023-02-28 | Viscera Labs, Inc. | Therapeutic composition and methods |
| US11524029B2 (en) | 2018-08-13 | 2022-12-13 | Viscera Labs, Inc. | Therapeutic composition and methods |
| JP2022514731A (ja) * | 2018-08-14 | 2022-02-15 | アヴォリント | 原発性硬化性胆管炎の処置方法 |
| US20210393662A1 (en) * | 2018-10-18 | 2021-12-23 | Avolynt | Use of sglt2 inhibitors to treat primary sclerosing cholangitis |
| CN111320609A (zh) | 2018-12-13 | 2020-06-23 | 拓臻股份有限公司 | 一种THRβ受体激动剂化合物及其制备方法和用途 |
| CN111825653A (zh) * | 2019-04-19 | 2020-10-27 | 安道麦马克西姆有限公司 | 取代吡唑类化合物的制备及其作为邻氨基苯甲酰胺前体的用途 |
| AU2020336272A1 (en) | 2019-08-23 | 2022-04-14 | Terns Pharmaceuticals, Inc. | Thyroid hormone receptor beta agonist compounds |
| WO2021050945A1 (en) | 2019-09-12 | 2021-03-18 | Terns, Inc. | Thyroid hormone receptor beta agonist compounds |
| CN114929214A (zh) * | 2019-11-22 | 2022-08-19 | 阿沃林特有限公司 | Sglt2抑制剂治疗原发性胆汁性胆管炎的用途 |
| CA3168474A1 (en) * | 2020-03-11 | 2021-09-16 | Mi-Kyung Kim | Pharmaceutical composition for prevention or treatment of nonalcoholic steatohepatitis |
| US11478533B2 (en) | 2020-04-27 | 2022-10-25 | Novo Nordisk A/S | Semaglutide for use in medicine |
| US20220034871A1 (en) * | 2020-07-31 | 2022-02-03 | Daiichi Sankyo Company, Limited | Methods for administering pexidartinib |
| CA3193057A1 (en) | 2020-08-25 | 2022-03-03 | Eli Lilly And Company | Polymorphs of an ssao inhibitor |
| US20240319210A1 (en) * | 2020-12-18 | 2024-09-26 | Human Metabolomics Institute, Inc. | Application of neonatal biliary atresia biomarker and detection method for same |
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| US8466143B2 (en) * | 2003-07-23 | 2013-06-18 | Exelixis, Inc. | Azepine derivatives as pharmaceutical agents |
| JP5081161B2 (ja) * | 2005-12-19 | 2012-11-21 | スミスクライン ビーチャム コーポレーション | ファルネソイドｘ受容体アゴニスト |
| ES2552657T3 (es) * | 2010-05-26 | 2015-12-01 | Satiogen Pharmaceuticals, Inc. | Inhibidores del reciclado de ácidos biliares y saciógenos para el tratamiento de diabetes, obesidad, y afecciones gastrointestinales inflamatorias |
| EP3777863A1 (en) * | 2014-09-12 | 2021-02-17 | Tobira Therapeutics, Inc. | Cenicriviroc combination therapy for the treatment of fibrosis |
| CN111662297A (zh) * | 2014-11-21 | 2020-09-15 | 阿卡纳治疗学有限公司 | 用于治疗疾病的稠合双环化合物 |
| EP3715348A1 (en) * | 2015-03-26 | 2020-09-30 | Akarna Therapeutics, Ltd. | Fused bicyclic compounds for the treatment of disease |
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2017
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- 2017-05-25 SG SG10202011660RA patent/SG10202011660RA/en unknown
- 2017-05-25 EP EP17803627.3A patent/EP3463373A4/en not_active Withdrawn
- 2017-05-25 CN CN201780045766.3A patent/CN109843298A/zh active Pending
- 2017-05-25 CA CA3025007A patent/CA3025007A1/en not_active Abandoned
- 2017-05-25 WO PCT/US2017/034564 patent/WO2017205684A1/en not_active Ceased
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- 2017-05-25 MX MX2018014024A patent/MX2018014024A/es unknown
- 2017-05-25 US US16/303,741 patent/US20200397798A1/en not_active Abandoned
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- 2017-05-25 RU RU2018145776A patent/RU2018145776A/ru not_active Application Discontinuation
- 2017-05-25 AU AU2017270221A patent/AU2017270221A1/en not_active Abandoned
- 2017-05-25 SG SG11201810290WA patent/SG11201810290WA/en unknown
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2018
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Also Published As
| Publication number | Publication date |
|---|---|
| WO2017205684A1 (en) | 2017-11-30 |
| SG10202011660RA (en) | 2020-12-30 |
| RU2018145776A3 (https=) | 2021-03-01 |
| EP3463373A4 (en) | 2020-04-22 |
| SG11201810290WA (en) | 2018-12-28 |
| CA3025007A1 (en) | 2017-11-30 |
| AU2017270221A1 (en) | 2018-12-20 |
| BR112018073460A2 (pt) | 2019-07-09 |
| IL263179A (en) | 2018-12-31 |
| CN109843298A (zh) | 2019-06-04 |
| US20200397798A1 (en) | 2020-12-24 |
| MX2018014024A (es) | 2019-08-29 |
| EP3463373A1 (en) | 2019-04-10 |
| JP2019517478A (ja) | 2019-06-24 |
| KR20190040936A (ko) | 2019-04-19 |
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| Date | Code | Title | Description |
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| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20210820 |