RU2018121946A - Модуляторы ror-гамма - Google Patents
Модуляторы ror-гамма Download PDFInfo
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- RU2018121946A RU2018121946A RU2018121946A RU2018121946A RU2018121946A RU 2018121946 A RU2018121946 A RU 2018121946A RU 2018121946 A RU2018121946 A RU 2018121946A RU 2018121946 A RU2018121946 A RU 2018121946A RU 2018121946 A RU2018121946 A RU 2018121946A
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- Russia
- Prior art keywords
- compound according
- paragraphs
- alkyl
- compound
- pharmaceutically acceptable
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- 150000001875 compounds Chemical class 0.000 claims 56
- 150000003839 salts Chemical class 0.000 claims 20
- 229910052736 halogen Inorganic materials 0.000 claims 17
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 13
- 150000002367 halogens Chemical class 0.000 claims 13
- 229910052739 hydrogen Inorganic materials 0.000 claims 11
- 239000001257 hydrogen Substances 0.000 claims 11
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 9
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical group [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- 125000004093 cyano group Chemical group *C#N 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 125000000623 heterocyclic group Chemical group 0.000 claims 7
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 4
- 208000011231 Crohn disease Diseases 0.000 claims 4
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 4
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 4
- 208000006673 asthma Diseases 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 4
- 201000004681 Psoriasis Diseases 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 2
- 208000002874 Acne Vulgaris Diseases 0.000 claims 2
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 2
- 208000009137 Behcet syndrome Diseases 0.000 claims 2
- 125000004399 C1-C4 alkenyl group Chemical group 0.000 claims 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims 2
- 206010012438 Dermatitis atopic Diseases 0.000 claims 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 2
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 2
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 2
- 206010039710 Scleroderma Diseases 0.000 claims 2
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 2
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 2
- 206010046851 Uveitis Diseases 0.000 claims 2
- 206010000496 acne Diseases 0.000 claims 2
- 201000008937 atopic dermatitis Diseases 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 201000001981 dermatomyositis Diseases 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 201000002215 juvenile rheumatoid arthritis Diseases 0.000 claims 2
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 2
- 208000001797 obstructive sleep apnea Diseases 0.000 claims 2
- 201000008482 osteoarthritis Diseases 0.000 claims 2
- 125000004430 oxygen atom Chemical group O* 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 201000002859 sleep apnea Diseases 0.000 claims 2
- 150000003431 steroids Chemical class 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- 125000006536 (C1-C2)alkoxy group Chemical group 0.000 claims 1
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010003805 Autism Diseases 0.000 claims 1
- 208000020706 Autistic disease Diseases 0.000 claims 1
- 208000031212 Autoimmune polyendocrinopathy Diseases 0.000 claims 1
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims 1
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims 1
- 208000020925 Bipolar disease Diseases 0.000 claims 1
- 206010008609 Cholangitis sclerosing Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 208000015943 Coeliac disease Diseases 0.000 claims 1
- 206010011668 Cutaneous leishmaniasis Diseases 0.000 claims 1
- 201000003883 Cystic fibrosis Diseases 0.000 claims 1
- 206010012442 Dermatitis contact Diseases 0.000 claims 1
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 1
- 206010013774 Dry eye Diseases 0.000 claims 1
- 201000009273 Endometriosis Diseases 0.000 claims 1
- 208000003807 Graves Disease Diseases 0.000 claims 1
- 208000015023 Graves' disease Diseases 0.000 claims 1
- 208000035895 Guillain-Barré syndrome Diseases 0.000 claims 1
- 208000001204 Hashimoto Disease Diseases 0.000 claims 1
- 208000030836 Hashimoto thyroiditis Diseases 0.000 claims 1
- 241001163602 Hiodon tergisus Species 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 206010049567 Miller Fisher syndrome Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010029240 Neuritis Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims 1
- 206010039085 Rhinitis allergic Diseases 0.000 claims 1
- 206010039705 Scleritis Diseases 0.000 claims 1
- 201000009594 Systemic Scleroderma Diseases 0.000 claims 1
- 206010042953 Systemic sclerosis Diseases 0.000 claims 1
- 210000000577 adipose tissue Anatomy 0.000 claims 1
- 206010064930 age-related macular degeneration Diseases 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 201000010105 allergic rhinitis Diseases 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- 201000011385 autoimmune polyendocrine syndrome Diseases 0.000 claims 1
- 208000010928 autoimmune thyroid disease Diseases 0.000 claims 1
- 206010006451 bronchitis Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 208000015114 central nervous system disease Diseases 0.000 claims 1
- 208000019069 chronic childhood arthritis Diseases 0.000 claims 1
- 230000027288 circadian rhythm Effects 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 208000010247 contact dermatitis Diseases 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 208000030533 eye disease Diseases 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 208000002780 macular degeneration Diseases 0.000 claims 1
- 208000024714 major depressive disease Diseases 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 230000003287 optical effect Effects 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 208000005987 polymyositis Diseases 0.000 claims 1
- 208000015768 polyposis Diseases 0.000 claims 1
- 208000028173 post-traumatic stress disease Diseases 0.000 claims 1
- 201000000742 primary sclerosing cholangitis Diseases 0.000 claims 1
- 208000002815 pulmonary hypertension Diseases 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- -1 quinolin-2 (1H) -on-4-ylmethyl Chemical group 0.000 claims 1
- 230000033764 rhythmic process Effects 0.000 claims 1
- 201000000306 sarcoidosis Diseases 0.000 claims 1
- 208000010157 sclerosing cholangitis Diseases 0.000 claims 1
- 208000012672 seasonal affective disease Diseases 0.000 claims 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
Classifications
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
- C07D217/24—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
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- 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
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
- C07D217/04—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/12—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
- C07D217/14—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals
- C07D217/16—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals substituted by oxygen atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
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- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/88—Oxygen atoms
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- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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| US9663515B2 (en) | 2014-11-05 | 2017-05-30 | Vitae Pharmaceuticals, Inc. | Dihydropyrrolopyridine inhibitors of ROR-gamma |
| MX394388B (es) | 2015-05-15 | 2025-03-21 | Aurigene Discovery Tech Ltd | Compuestos de tetrahidroquinolinona sustituidos como moduladores de ror gamma |
| WO2017024018A1 (en) | 2015-08-05 | 2017-02-09 | Vitae Pharmaceuticals, Inc. | Modulators of ror-gamma |
| KR20180086221A (ko) | 2015-11-20 | 2018-07-30 | 비타이 파마슈티컬즈, 인코포레이티드 | Ror-감마의 조절물질 |
| TW202220968A (zh) | 2016-01-29 | 2022-06-01 | 美商維它藥物有限責任公司 | ROR-γ調節劑 |
| BR112019000603A2 (pt) | 2016-07-14 | 2019-04-30 | Cadila Healthcare Limited | composto, composição farmacêutica, método para o tratamento de doenças e uso do composto |
| TW201815388A (zh) | 2016-07-14 | 2018-05-01 | 印度商卡迪拉保健有限公司 | 作為RORγ調節劑之新穎化合物 |
| WO2018116285A1 (en) * | 2016-12-23 | 2018-06-28 | Glenmark Pharmaceuticals S.A. | Substituted morpholine derivatives as ror gamma modulators |
| WO2019018975A1 (en) | 2017-07-24 | 2019-01-31 | Vitae Pharmaceuticals, Inc. | INHIBITORS OF ROR GAMMA |
| MA49685A (fr) | 2017-07-24 | 2021-04-14 | Vitae Pharmaceuticals Llc | INHIBITEURS DE ROR gamma |
| CN109593068B (zh) * | 2017-09-30 | 2022-12-27 | 广东东阳光药业有限公司 | 一种RORγ抑制剂的中间体及其制备方法 |
| JPWO2019088057A1 (ja) * | 2017-10-31 | 2020-09-24 | 東レ株式会社 | アニリド誘導体及びその医薬用途 |
| WO2019157417A1 (en) * | 2018-02-09 | 2019-08-15 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Heterocyclic p2y14 receptor antagonists |
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| WO2020082921A1 (zh) * | 2018-10-24 | 2020-04-30 | 上海和誉生物医药科技有限公司 | 一种氮杂芳基酰胺衍生物及其制备方法和应用 |
| AU2019375983A1 (en) | 2018-11-09 | 2021-06-10 | Vivace Therapeutics, Inc. | Bicyclic compounds |
| CN117800904A (zh) * | 2018-11-27 | 2024-04-02 | 正大天晴药业集团股份有限公司 | 含有磺酰基结构的RORγ抑制剂 |
| CN111484505B (zh) * | 2019-01-28 | 2022-11-15 | 正大天晴药业集团股份有限公司 | 一种双环RORγ抑制剂的盐酸盐结晶型 |
| HUE070525T2 (hu) * | 2019-04-16 | 2025-06-28 | Vivace Therapeutics Inc | Biciklusos vegyületek |
| JP2022535980A (ja) * | 2019-06-12 | 2022-08-10 | ティーエムイーエム16エー リミテッド | 呼吸器疾患を処置するための化合物 |
| WO2021047406A1 (zh) * | 2019-09-10 | 2021-03-18 | 四川科伦博泰生物医药股份有限公司 | 一种三并环类化合物,包含其的药物组合物,其制备方法及其用途 |
| CN112745268B (zh) * | 2019-10-31 | 2022-09-16 | 江苏恒瑞医药股份有限公司 | 苯并咪唑衍生物的晶型及制备方法 |
| TW202136238A (zh) * | 2020-01-06 | 2021-10-01 | 大陸商廣東東陽光藥業有限公司 | RORγt抑制劑及其製備方法和用途 |
| CN115297861B (zh) * | 2020-01-29 | 2024-07-12 | 福宏治疗公司 | 化合物及其用途 |
| WO2025223511A1 (zh) * | 2024-04-25 | 2025-10-30 | 上海翊石医药科技有限公司 | 一类苯甲酰基甘氨酸衍生物及其制备方法和应用 |
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| MA49685A (fr) | 2017-07-24 | 2021-04-14 | Vitae Pharmaceuticals Llc | INHIBITEURS DE ROR gamma |
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-
2016
- 2016-11-17 KR KR1020187017452A patent/KR20180086221A/ko not_active Withdrawn
- 2016-11-17 EP EP21163201.3A patent/EP3868750A1/en not_active Withdrawn
- 2016-11-17 WO PCT/US2016/062422 patent/WO2017087608A1/en not_active Ceased
- 2016-11-17 CA CA3005658A patent/CA3005658A1/en not_active Abandoned
- 2016-11-17 MA MA053943A patent/MA53943A/fr unknown
- 2016-11-17 US US15/776,836 patent/US11008340B2/en active Active
- 2016-11-17 MX MX2018006223A patent/MX385332B/es unknown
- 2016-11-17 AU AU2016355710A patent/AU2016355710B2/en not_active Ceased
- 2016-11-17 JP JP2018526160A patent/JP6914257B2/ja not_active Expired - Fee Related
- 2016-11-17 EP EP16816023.2A patent/EP3377482B1/en active Active
- 2016-11-17 BR BR112018010018A patent/BR112018010018A2/pt not_active IP Right Cessation
- 2016-11-17 RU RU2018121946A patent/RU2018121946A/ru unknown
- 2016-11-17 CN CN201680078466.0A patent/CN108463458B/zh not_active Expired - Fee Related
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2018
- 2018-05-16 IL IL259421A patent/IL259421B/en active IP Right Grant
- 2018-05-18 MX MX2021009673A patent/MX2021009673A/es unknown
- 2018-05-20 SA SA518391624A patent/SA518391624B1/ar unknown
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2021
- 2021-05-31 IL IL283582A patent/IL283582A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20190322687A1 (en) | 2019-10-24 |
| MX2018006223A (es) | 2018-12-19 |
| JP6914257B2 (ja) | 2021-08-04 |
| IL283582A (en) | 2021-07-29 |
| MX2021009673A (es) | 2021-09-08 |
| CN108463458A (zh) | 2018-08-28 |
| KR20180086221A (ko) | 2018-07-30 |
| EP3868750A1 (en) | 2021-08-25 |
| SA518391624B1 (ar) | 2021-06-13 |
| CA3005658A1 (en) | 2017-05-26 |
| AU2016355710A1 (en) | 2018-05-31 |
| RU2018121946A3 (enExample) | 2020-04-16 |
| BR112018010018A2 (pt) | 2018-11-21 |
| WO2017087608A1 (en) | 2017-05-26 |
| MX385332B (es) | 2025-03-18 |
| EP3377482B1 (en) | 2021-05-12 |
| AU2016355710B2 (en) | 2021-03-25 |
| US11008340B2 (en) | 2021-05-18 |
| JP2018534326A (ja) | 2018-11-22 |
| IL259421A (en) | 2018-07-31 |
| WO2017087608A8 (en) | 2017-07-06 |
| IL259421B (en) | 2021-06-30 |
| EP3377482A1 (en) | 2018-09-26 |
| MA53943A (fr) | 2021-08-25 |
| CN108463458B (zh) | 2022-02-01 |
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