JP2020531432A5 - - Google Patents
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- JP2020531432A5 JP2020531432A5 JP2020508455A JP2020508455A JP2020531432A5 JP 2020531432 A5 JP2020531432 A5 JP 2020531432A5 JP 2020508455 A JP2020508455 A JP 2020508455A JP 2020508455 A JP2020508455 A JP 2020508455A JP 2020531432 A5 JP2020531432 A5 JP 2020531432A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- alkyl
- protecting group
- formula
- cycloalkyl
- 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.)
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- 229910052739 hydrogen Inorganic materials 0.000 claims description 90
- 239000001257 hydrogen Substances 0.000 claims description 90
- 125000000217 alkyl group Chemical group 0.000 claims description 85
- -1 substituted Chemical class 0.000 claims description 79
- 150000002431 hydrogen Chemical group 0.000 claims description 72
- 150000001875 compounds Chemical class 0.000 claims description 56
- 238000000034 method Methods 0.000 claims description 53
- 125000000623 heterocyclic group Chemical group 0.000 claims description 46
- 125000001072 heteroaryl group Chemical group 0.000 claims description 34
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 34
- 150000003839 salts Chemical class 0.000 claims description 34
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 29
- 229910052736 halogen Inorganic materials 0.000 claims description 24
- 150000002367 halogens Chemical class 0.000 claims description 24
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 22
- 125000004432 carbon atom Chemical group C* 0.000 claims description 22
- 125000003118 aryl group Chemical group 0.000 claims description 20
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 20
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 18
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 18
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 18
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 16
- 125000005017 substituted alkenyl group Chemical group 0.000 claims description 14
- 125000004426 substituted alkynyl group Chemical group 0.000 claims description 14
- 125000003107 substituted aryl group Chemical group 0.000 claims description 14
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 12
- 125000005843 halogen group Chemical group 0.000 claims description 12
- 201000010099 disease Diseases 0.000 claims description 10
- 125000002947 alkylene group Chemical group 0.000 claims description 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 8
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims description 6
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims description 6
- 206010012601 diabetes mellitus Diseases 0.000 claims description 6
- 208000033679 diabetic kidney disease Diseases 0.000 claims description 6
- 125000003342 alkenyl group Chemical group 0.000 claims description 5
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims description 4
- 208000005692 Bloom Syndrome Diseases 0.000 claims description 4
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims description 4
- 125000004103 aminoalkyl group Chemical group 0.000 claims description 4
- 125000004429 atom Chemical group 0.000 claims description 4
- 229910052799 carbon Inorganic materials 0.000 claims description 4
- 208000029078 coronary artery disease Diseases 0.000 claims description 4
- 230000008878 coupling Effects 0.000 claims description 4
- 238000010168 coupling process Methods 0.000 claims description 4
- 238000005859 coupling reaction Methods 0.000 claims description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 4
- 125000002950 monocyclic group Chemical group 0.000 claims description 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 2
- 125000006708 (C5-C14) heteroaryl group Chemical group 0.000 claims description 2
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 2
- 201000001320 Atherosclerosis Diseases 0.000 claims description 2
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims description 2
- 206010028980 Neoplasm Diseases 0.000 claims description 2
- 208000008589 Obesity Diseases 0.000 claims description 2
- 208000031481 Pathologic Constriction Diseases 0.000 claims description 2
- 102000013009 Pyruvate Kinase Human genes 0.000 claims description 2
- 108020005115 Pyruvate Kinase Proteins 0.000 claims description 2
- 230000002159 abnormal effect Effects 0.000 claims description 2
- 230000004913 activation Effects 0.000 claims description 2
- 125000000304 alkynyl group Chemical group 0.000 claims description 2
- 230000008901 benefit Effects 0.000 claims description 2
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- 150000001721 carbon Chemical group 0.000 claims description 2
- 230000004663 cell proliferation Effects 0.000 claims description 2
- 208000035475 disorder Diseases 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 239000008103 glucose Substances 0.000 claims description 2
- 125000001188 haloalkyl group Chemical group 0.000 claims description 2
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 2
- 201000001421 hyperglycemia Diseases 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 125000001624 naphthyl group Chemical group 0.000 claims description 2
- 235000020824 obesity Nutrition 0.000 claims description 2
- 229910052760 oxygen Inorganic materials 0.000 claims description 2
- 230000002062 proliferating effect Effects 0.000 claims description 2
- 125000006239 protecting group Chemical group 0.000 claims description 2
- 208000037804 stenosis Diseases 0.000 claims description 2
- 125000005415 substituted alkoxy group Chemical group 0.000 claims description 2
- 229910052717 sulfur Inorganic materials 0.000 claims description 2
- 239000011593 sulfur Substances 0.000 claims description 2
- 0 *C(*=I)(N(C1=O)N=Cc2c1[n](*)c1c2[s]c(I*)n1)[Ru] Chemical compound *C(*=I)(N(C1=O)N=Cc2c1[n](*)c1c2[s]c(I*)n1)[Ru] 0.000 description 26
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 9
- 125000003545 alkoxy group Chemical group 0.000 description 5
- 239000011541 reaction mixture Substances 0.000 description 4
- 238000003556 assay Methods 0.000 description 2
- 238000006243 chemical reaction Methods 0.000 description 2
- 239000012895 dilution Substances 0.000 description 2
- 238000010790 dilution Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 239000011535 reaction buffer Substances 0.000 description 2
- 230000001105 regulatory effect Effects 0.000 description 2
- 208000023275 Autoimmune disease Diseases 0.000 description 1
- SCIOVXDURPOXPM-UTCJRWHESA-N CC(C(N(C)/C=N\N[RnH])=O)[RnH] Chemical compound CC(C(N(C)/C=N\N[RnH])=O)[RnH] SCIOVXDURPOXPM-UTCJRWHESA-N 0.000 description 1
- JQKCGRMCAXRDNC-GQCTYLIASA-N CCN/C=N\C=C(/C)\[Rn]=N Chemical compound CCN/C=N\C=C(/C)\[Rn]=N JQKCGRMCAXRDNC-GQCTYLIASA-N 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 239000007983 Tris buffer Substances 0.000 description 1
- 238000002835 absorbance Methods 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 229930027945 nicotinamide-adenine dinucleotide Natural products 0.000 description 1
- BOPGDPNILDQYTO-NNYOXOHSSA-N nicotinamide-adenine dinucleotide Chemical compound C1=CCC(C(=O)N)=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](COP(O)(=O)OP(O)(=O)OC[C@@H]2[C@H]([C@@H](O)[C@@H](O2)N2C3=NC=NC(N)=C3N=C2)O)O1 BOPGDPNILDQYTO-NNYOXOHSSA-N 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 239000011550 stock solution Substances 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022199462A JP2023027276A (ja) | 2017-08-15 | 2022-12-14 | ピルビン酸キナーゼ調節因子およびその使用 |
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2017097496 | 2017-08-15 | ||
| CNPCT/CN2017/097496 | 2017-08-15 | ||
| US201862673526P | 2018-05-18 | 2018-05-18 | |
| US201862673533P | 2018-05-18 | 2018-05-18 | |
| US62/673,533 | 2018-05-18 | ||
| US62/673,526 | 2018-05-18 | ||
| PCT/US2018/000129 WO2019035865A1 (en) | 2017-08-15 | 2018-08-15 | MODULATORS OF PYRUVATE KINASE AND THEIR USE |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022199462A Division JP2023027276A (ja) | 2017-08-15 | 2022-12-14 | ピルビン酸キナーゼ調節因子およびその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020531432A JP2020531432A (ja) | 2020-11-05 |
| JP2020531432A5 true JP2020531432A5 (cg-RX-API-DMAC10.html) | 2021-09-30 |
| JP7301040B2 JP7301040B2 (ja) | 2023-06-30 |
Family
ID=63524352
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020508455A Active JP7301040B2 (ja) | 2017-08-15 | 2018-08-15 | ピルビン酸キナーゼ調節因子およびその使用 |
| JP2020508498A Active JP7275107B2 (ja) | 2017-08-15 | 2018-08-15 | 血液障害の治療に使用するためのピルビン酸キナーゼ活性化因子 |
| JP2022199462A Pending JP2023027276A (ja) | 2017-08-15 | 2022-12-14 | ピルビン酸キナーゼ調節因子およびその使用 |
| JP2023005925A Active JP7530453B2 (ja) | 2017-08-15 | 2023-01-18 | 血液障害の治療に使用するためのピルビン酸キナーゼ活性化因子 |
| JP2024121066A Pending JP2024147805A (ja) | 2017-08-15 | 2024-07-26 | 血液障害の治療に使用するためのピルビン酸キナーゼ活性化因子 |
Family Applications After (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020508498A Active JP7275107B2 (ja) | 2017-08-15 | 2018-08-15 | 血液障害の治療に使用するためのピルビン酸キナーゼ活性化因子 |
| JP2022199462A Pending JP2023027276A (ja) | 2017-08-15 | 2022-12-14 | ピルビン酸キナーゼ調節因子およびその使用 |
| JP2023005925A Active JP7530453B2 (ja) | 2017-08-15 | 2023-01-18 | 血液障害の治療に使用するためのピルビン酸キナーゼ活性化因子 |
| JP2024121066A Pending JP2024147805A (ja) | 2017-08-15 | 2024-07-26 | 血液障害の治療に使用するためのピルビン酸キナーゼ活性化因子 |
Country Status (34)
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
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| AR111295A1 (es) | 2017-03-20 | 2019-06-26 | Forma Therapeutics Inc | Composiciones de pirrolopirrol como activadores de piruvato quinasa (pkr) |
| EP3668513B1 (en) | 2017-08-15 | 2021-11-10 | Agios Pharmaceuticals, Inc. | Pyruvate kinase activators for use in treating blood disorders |
| US12233063B2 (en) | 2017-10-20 | 2025-02-25 | The Regents Of The University Of Michigan | Compositions and methods for treating eye disorders |
| US20200129485A1 (en) | 2018-09-19 | 2020-04-30 | Forma Therapeutics, Inc. | Treating sickle cell disease with a pyruvate kinase r activating compound |
| WO2020061255A1 (en) | 2018-09-19 | 2020-03-26 | Forma Therapeutics, Inc. | Activating pyruvate kinase r |
| US20220127267A1 (en) * | 2019-02-13 | 2022-04-28 | Agios Pharmaceuticals, Inc. | Thieno[3,2-b] pyrrole[3,2-d]pyridazinone derivatives and their use as pkm2 derivatives for the treatment of cancer, obesity and diabetes related disorders |
| KR102794329B1 (ko) * | 2019-06-26 | 2025-04-14 | 닛산 가가쿠 가부시키가이샤 | 전하 수송성 바니시 |
| MX2022003025A (es) | 2019-09-19 | 2022-04-07 | Forma Therapeutics Inc | Activacion de la piruvato cinasa r. |
| CA3183980A1 (en) * | 2020-07-21 | 2022-01-27 | The Regents Of The University Of Michigan | Compositions and methods for activating pyruvate kinase |
| CN112490502B (zh) * | 2020-12-04 | 2022-01-21 | 广州天赐高新材料股份有限公司 | 一种电解液及锂二次电池 |
| WO2022170200A1 (en) | 2021-02-08 | 2022-08-11 | Global Blood Therapeutics, Inc. | 1-(2-sulfonyl-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4h)-yl]-ethanone derivatives as pyruvate kinase (pkr) and pkm2 activators for the treatment of sickle cell disease |
| US12128035B2 (en) | 2021-03-19 | 2024-10-29 | Novo Nordisk Health Care Ag | Activating pyruvate kinase R |
| WO2023052783A1 (en) * | 2021-09-30 | 2023-04-06 | Sitryx Therapeutics Limited | Novel compounds |
| KR20240107326A (ko) * | 2021-11-16 | 2024-07-09 | 아지오스 파마슈티컬스 아이엔씨. | Mds 관련 빈혈 및 기타 상태를 치료하기 위한 화합물 |
| CN116159061A (zh) * | 2023-03-09 | 2023-05-26 | 上海市第十人民医院 | 丙酮酸激酶m2激活剂在制备预防或治疗心力衰竭的药物中的应用 |
| EP4671102A1 (en) | 2023-03-28 | 2025-12-31 | Honda Motor Co., Ltd. | METHOD FOR PROVIDING INFORMATION, PROGRAM FOR PROVIDING INFORMATION, STORAGE MEDIA AND INFORMATION PROCESSING APPARATUS |
| WO2024238659A1 (en) | 2023-05-15 | 2024-11-21 | Agios Pharmaceuticals, Inc. | Crystalline salts or amorphous forms of 2-((1h-pyrazol-3-yl)methyl)-6-((6-aminopyridin-2-yl)methyl)-4-methyl-4,6-dihydro -5h-thiazolo[5',4':4,5]pyrrolo[2,3-d]pyridazin-5-one |
| CN121443584A (zh) * | 2023-07-05 | 2026-01-30 | 安吉奥斯医药品有限公司 | 丙酮酸激酶活化剂的合成 |
| WO2025207563A1 (en) | 2024-03-27 | 2025-10-02 | Agios Pharmaceuticals, Inc. | Use of a pk activator in the treatment of sickle cell disease |
| WO2026076363A1 (en) | 2024-10-04 | 2026-04-09 | Agios Pharmaceuticals, Inc. | Compounds for treating mds-associated anemias and other conditions |
| WO2026096368A1 (en) | 2024-10-28 | 2026-05-07 | Agios Pharmaceuticals, Inc. | Use of the pyruvate kinase activator tebapivat in the treatment of renal fibrosis and other renal diseases |
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| US4883914A (en) | 1987-08-17 | 1989-11-28 | American Cyanamid Company | Benzenesulfonyl carboxamide compounds useful as herbicidal agents |
| BR0012896A (pt) | 1999-07-30 | 2002-06-18 | Abbott Gmbh & Co Kg | 2-pirazolin-5-onas |
| CZ2002773A3 (cs) | 1999-09-04 | 2002-06-12 | Astrazeneca Ab | Substituované deriváty N-fenyl-2-hydroxy-2-methyl-3,3,3-trifluorpropanamidu, které zvyąují aktivitu pyruvátdehydrogenázy |
| EP1972629A1 (en) * | 2007-03-23 | 2008-09-24 | Mutabilis SA | New imidazolo-heteroaryl derivatives with antibacterial properties |
| FR2933983B1 (fr) * | 2008-07-15 | 2010-08-27 | Servier Lab | Nouveaux derives tricycliques,leur procede de preparation et les compositions pharmaceutiques qui les contiennent. |
| CA2731432A1 (en) * | 2008-07-23 | 2010-01-28 | Vertex Pharmaceuticals Incorporated | Tri-cyclic pyrazolopyridine kinase inhibitors |
| WO2010025202A1 (en) * | 2008-08-29 | 2010-03-04 | Amgen Inc. | PYRIDO[3,2-d]PYRIDAZINE-2(1H)-ONE COMPOUNDS AS P38 MODULATORS AND METHODS OF USE THEREOF |
| ES2620634T3 (es) * | 2008-10-09 | 2017-06-29 | The U.S.A. As Represented By The Secretary, Department Of Health And Human Services | Activadores de piruvato quinasa humana |
| JP5756457B2 (ja) * | 2009-04-06 | 2015-07-29 | アジオス ファーマシューティカルズ， インコーポレイテッド | ピルビン酸キナーゼｍ２調節剤、治療組成物および関連する使用方法 |
| PE20120693A1 (es) | 2009-06-29 | 2012-07-04 | Agios Pharmaceuticals Inc | Compuestos heterociclos como moduladores de la piruvato cinasa m2 (pkm2) |
| US20130109672A1 (en) | 2010-04-29 | 2013-05-02 | The United States Of America,As Represented By The Secretary, Department Of Health And Human Service | Activators of human pyruvate kinase |
| US8637536B2 (en) | 2010-12-06 | 2014-01-28 | Glaxo Group Limited | Pyrimidinone compounds for use in the treatment of diseases or conditions mediated by Lp-PLA2 |
| TWI549947B (zh) | 2010-12-29 | 2016-09-21 | 阿吉歐斯製藥公司 | 治療化合物及組成物 |
| PT3406251T (pt) | 2011-05-03 | 2024-01-24 | Agios Pharmaceuticals Inc | Ativadores da piruvato-cinase para utilização em terapia |
| US9388164B2 (en) | 2011-05-03 | 2016-07-12 | Agios Pharmaceuticals, Inc | Methods of using pyruvate kinase activators |
| EP2704719B1 (en) * | 2011-05-03 | 2018-02-21 | Agios Pharmaceuticals, Inc. | Pyruvate kinase activators for use for increasing lifetime of the red blood cells and treating anemia |
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| EP3668513B1 (en) * | 2017-08-15 | 2021-11-10 | Agios Pharmaceuticals, Inc. | Pyruvate kinase activators for use in treating blood disorders |
| US20220127267A1 (en) * | 2019-02-13 | 2022-04-28 | Agios Pharmaceuticals, Inc. | Thieno[3,2-b] pyrrole[3,2-d]pyridazinone derivatives and their use as pkm2 derivatives for the treatment of cancer, obesity and diabetes related disorders |
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2018
- 2018-08-15 EP EP18779068.8A patent/EP3668513B1/en active Active
- 2018-08-15 WO PCT/US2018/000127 patent/WO2019035863A1/en not_active Ceased
- 2018-08-15 MX MX2020001833A patent/MX2020001833A/es unknown
- 2018-08-15 FI FIEP18766400.8T patent/FI3668512T3/fi active
- 2018-08-15 BR BR112020003254-9A patent/BR112020003254A2/pt not_active Application Discontinuation
- 2018-08-15 KR KR1020207007346A patent/KR102642408B1/ko active Active
- 2018-08-15 US US16/639,086 patent/US11464775B2/en active Active
- 2018-08-15 SG SG11202001353PA patent/SG11202001353PA/en unknown
- 2018-08-15 PL PL18766400.8T patent/PL3668512T3/pl unknown
- 2018-08-15 SM SM20220023T patent/SMT202200023T1/it unknown
- 2018-08-15 WO PCT/US2018/000128 patent/WO2019035864A1/en not_active Ceased
- 2018-08-15 MD MDE20200663T patent/MD3668513T2/ro unknown
- 2018-08-15 HR HRP20230452TT patent/HRP20230452T1/hr unknown
- 2018-08-15 ES ES18766063T patent/ES2966825T3/es active Active
- 2018-08-15 EP EP18766063.4A patent/EP3668881B1/en active Active
- 2018-08-15 JP JP2020508455A patent/JP7301040B2/ja active Active
- 2018-08-15 ES ES18779068T patent/ES2905100T3/es active Active
- 2018-08-15 UA UAA202001747A patent/UA126292C2/uk unknown
- 2018-08-15 CN CN202310962497.4A patent/CN117186119B/zh active Active
- 2018-08-15 CA CA3072455A patent/CA3072455A1/en active Pending
- 2018-08-15 US US16/639,081 patent/US11590132B2/en active Active
- 2018-08-15 TW TW107128429A patent/TWI790271B/zh active
- 2018-08-15 AU AU2018316587A patent/AU2018316587B2/en active Active
- 2018-08-15 MY MYPI2020000757A patent/MY204421A/en unknown
- 2018-08-15 CR CR20200123A patent/CR20200123A/es unknown
- 2018-08-15 CN CN201880053315.9A patent/CN111032045B/zh active Active
- 2018-08-15 RS RS20220003A patent/RS62871B1/sr unknown
- 2018-08-15 CN CN201880053325.2A patent/CN111032046B/zh active Active
- 2018-08-15 SG SG11202001262QA patent/SG11202001262QA/en unknown
- 2018-08-15 US US16/639,075 patent/US11364240B2/en active Active
- 2018-08-15 KR KR1020207007344A patent/KR102717594B1/ko active Active
- 2018-08-15 IL IL272599A patent/IL272599B/en unknown
- 2018-08-15 PT PT187664008T patent/PT3668512T/pt unknown
- 2018-08-15 LT LTEPPCT/US2018/000129T patent/LT3668512T/lt unknown
- 2018-08-15 PT PT187790688T patent/PT3668513T/pt unknown
- 2018-08-15 DK DK18779068.8T patent/DK3668513T3/da active
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