JP2018530559A5 - - Google Patents
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- JP2018530559A5 JP2018530559A5 JP2018517509A JP2018517509A JP2018530559A5 JP 2018530559 A5 JP2018530559 A5 JP 2018530559A5 JP 2018517509 A JP2018517509 A JP 2018517509A JP 2018517509 A JP2018517509 A JP 2018517509A JP 2018530559 A5 JP2018530559 A5 JP 2018530559A5
- Authority
- JP
- Japan
- Prior art keywords
- halogen
- oso
- compound according
- carbon atom
- oxo
- 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.)
- Granted
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- 229910052736 halogen Inorganic materials 0.000 claims description 136
- -1 5-oxo-1,2,4-oxadiazolyl Chemical group 0.000 claims description 126
- 150000001875 compounds Chemical class 0.000 claims description 102
- 150000002367 halogens Chemical class 0.000 claims description 84
- 229910052799 carbon Inorganic materials 0.000 claims description 76
- 125000004432 carbon atom Chemical group C* 0.000 claims description 62
- 125000005843 halogen group Chemical group 0.000 claims description 52
- 125000000217 alkyl group Chemical group 0.000 claims description 49
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 34
- 125000005842 heteroatom Chemical group 0.000 claims description 28
- 229910052760 oxygen Inorganic materials 0.000 claims description 28
- 229910052717 sulfur Inorganic materials 0.000 claims description 28
- 150000003839 salts Chemical class 0.000 claims description 26
- 150000001413 amino acids Chemical class 0.000 claims description 24
- 239000012453 solvate Substances 0.000 claims description 24
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 22
- 125000003545 alkoxy group Chemical group 0.000 claims description 20
- 201000010099 disease Diseases 0.000 claims description 20
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 16
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 16
- 125000001113 thiadiazolyl group Chemical group 0.000 claims description 16
- 125000003342 alkenyl group Chemical group 0.000 claims description 14
- 125000000304 alkynyl group Chemical group 0.000 claims description 14
- 125000000623 heterocyclic group Chemical group 0.000 claims description 14
- 229910052739 hydrogen Inorganic materials 0.000 claims description 14
- 125000004043 oxo group Chemical group O=* 0.000 claims description 12
- 206010008635 Cholestasis Diseases 0.000 claims description 6
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims description 6
- 206010028980 Neoplasm Diseases 0.000 claims description 6
- 201000011510 cancer Diseases 0.000 claims description 6
- 230000007870 cholestasis Effects 0.000 claims description 6
- 231100000359 cholestasis Toxicity 0.000 claims description 6
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims description 6
- 208000018522 Gastrointestinal disease Diseases 0.000 claims description 5
- 208000010643 digestive system disease Diseases 0.000 claims description 5
- 208000018685 gastrointestinal system disease Diseases 0.000 claims description 5
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims description 4
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims description 4
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 4
- 208000031226 Hyperlipidaemia Diseases 0.000 claims description 4
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims description 4
- 230000001580 bacterial effect Effects 0.000 claims description 4
- 230000001684 chronic effect Effects 0.000 claims description 4
- 206010012601 diabetes mellitus Diseases 0.000 claims description 4
- 208000016097 disease of metabolism Diseases 0.000 claims description 4
- 201000005206 focal segmental glomerulosclerosis Diseases 0.000 claims description 4
- 231100000854 focal segmental glomerulosclerosis Toxicity 0.000 claims description 4
- 208000002551 irritable bowel syndrome Diseases 0.000 claims description 4
- 208000017169 kidney disease Diseases 0.000 claims description 4
- 210000004185 liver Anatomy 0.000 claims description 4
- 208000019423 liver disease Diseases 0.000 claims description 4
- 208000030159 metabolic disease Diseases 0.000 claims description 4
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims description 4
- 238000002054 transplantation Methods 0.000 claims description 4
- 208000008589 Obesity Diseases 0.000 claims description 3
- 208000012868 Overgrowth Diseases 0.000 claims description 3
- 235000020824 obesity Nutrition 0.000 claims description 3
- 208000022309 Alcoholic Liver disease Diseases 0.000 claims description 2
- 206010003210 Arteriosclerosis Diseases 0.000 claims description 2
- 201000001320 Atherosclerosis Diseases 0.000 claims description 2
- 206010003827 Autoimmune hepatitis Diseases 0.000 claims description 2
- 206010004637 Bile duct stone Diseases 0.000 claims description 2
- 206010005003 Bladder cancer Diseases 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 2
- 201000009331 Choledocholithiasis Diseases 0.000 claims description 2
- 206010063209 Chronic allograft nephropathy Diseases 0.000 claims description 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 2
- 206010010356 Congenital anomaly Diseases 0.000 claims description 2
- 102000012437 Copper-Transporting ATPases Human genes 0.000 claims description 2
- 208000011231 Crohn disease Diseases 0.000 claims description 2
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims description 2
- 208000032928 Dyslipidaemia Diseases 0.000 claims description 2
- 208000015872 Gaucher disease Diseases 0.000 claims description 2
- 206010018367 Glomerulonephritis chronic Diseases 0.000 claims description 2
- 208000009329 Graft vs Host Disease Diseases 0.000 claims description 2
- 208000024815 Granulomatous liver disease Diseases 0.000 claims description 2
- 208000018565 Hemochromatosis Diseases 0.000 claims description 2
- 206010019799 Hepatitis viral Diseases 0.000 claims description 2
- 208000002972 Hepatolenticular Degeneration Diseases 0.000 claims description 2
- 208000035150 Hypercholesterolemia Diseases 0.000 claims description 2
- 206010020772 Hypertension Diseases 0.000 claims description 2
- 206010022489 Insulin Resistance Diseases 0.000 claims description 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 2
- 208000017170 Lipid metabolism disease Diseases 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 206010025476 Malabsorption Diseases 0.000 claims description 2
- 208000004155 Malabsorption Syndromes Diseases 0.000 claims description 2
- 208000012902 Nervous system disease Diseases 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 206010038389 Renal cancer Diseases 0.000 claims description 2
- 208000004337 Salivary Gland Neoplasms Diseases 0.000 claims description 2
- 206010061934 Salivary gland cancer Diseases 0.000 claims description 2
- 206010040047 Sepsis Diseases 0.000 claims description 2
- 208000021386 Sjogren Syndrome Diseases 0.000 claims description 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 2
- 206010048302 Tubulointerstitial nephritis Diseases 0.000 claims description 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims description 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 2
- 208000018839 Wilson disease Diseases 0.000 claims description 2
- 206010048215 Xanthomatosis Diseases 0.000 claims description 2
- 239000000654 additive Substances 0.000 claims description 2
- 230000000996 additive effect Effects 0.000 claims description 2
- 201000005188 adrenal gland cancer Diseases 0.000 claims description 2
- 208000024447 adrenal gland neoplasm Diseases 0.000 claims description 2
- 208000011775 arteriosclerosis disease Diseases 0.000 claims description 2
- 230000002490 cerebral effect Effects 0.000 claims description 2
- 231100000850 chronic interstitial nephritis Toxicity 0.000 claims description 2
- 208000019425 cirrhosis of liver Diseases 0.000 claims description 2
- 206010009887 colitis Diseases 0.000 claims description 2
- 208000033679 diabetic kidney disease Diseases 0.000 claims description 2
- 208000035475 disorder Diseases 0.000 claims description 2
- 229940079593 drug Drugs 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 206010017758 gastric cancer Diseases 0.000 claims description 2
- 208000024908 graft versus host disease Diseases 0.000 claims description 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 2
- 201000001421 hyperglycemia Diseases 0.000 claims description 2
- 208000020346 hyperlipoproteinemia Diseases 0.000 claims description 2
- 230000001631 hypertensive effect Effects 0.000 claims description 2
- 208000006575 hypertriglyceridemia Diseases 0.000 claims description 2
- 208000001024 intrahepatic cholestasis Diseases 0.000 claims description 2
- 230000007872 intrahepatic cholestasis Effects 0.000 claims description 2
- 201000010982 kidney cancer Diseases 0.000 claims description 2
- 150000002632 lipids Chemical class 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 230000036210 malignancy Effects 0.000 claims description 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 208000008275 microscopic colitis Diseases 0.000 claims description 2
- 201000009925 nephrosclerosis Diseases 0.000 claims description 2
- 201000004228 ovarian endometrial cancer Diseases 0.000 claims description 2
- 201000002528 pancreatic cancer Diseases 0.000 claims description 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
- 235000016236 parenteral nutrition Nutrition 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 208000030761 polycystic kidney disease Diseases 0.000 claims description 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 2
- 230000008929 regeneration Effects 0.000 claims description 2
- 238000011069 regeneration method Methods 0.000 claims description 2
- 201000000306 sarcoidosis Diseases 0.000 claims description 2
- 208000010157 sclerosing cholangitis Diseases 0.000 claims description 2
- 201000011549 stomach cancer Diseases 0.000 claims description 2
- 210000002435 tendon Anatomy 0.000 claims description 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 2
- 201000001862 viral hepatitis Diseases 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 13
- 230000007812 deficiency Effects 0.000 claims 1
- 239000002753 trypsin inhibitor Substances 0.000 claims 1
- 238000000034 method Methods 0.000 description 11
- 208000006682 alpha 1-Antitrypsin Deficiency Diseases 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562238246P | 2015-10-07 | 2015-10-07 | |
| US62/238,246 | 2015-10-07 | ||
| PCT/US2016/055980 WO2017062763A1 (en) | 2015-10-07 | 2016-10-07 | Farnesoid x receptor modulators |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019171488A Division JP2019210297A (ja) | 2015-10-07 | 2019-09-20 | ファルネソイドｘ受容体調節剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018530559A JP2018530559A (ja) | 2018-10-18 |
| JP2018530559A5 true JP2018530559A5 (cg-RX-API-DMAC7.html) | 2019-11-07 |
| JP7021080B2 JP7021080B2 (ja) | 2022-02-16 |
Family
ID=58488545
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018517509A Active JP7021080B2 (ja) | 2015-10-07 | 2016-10-07 | ファルネソイドｘ受容体調節剤 |
| JP2019171488A Pending JP2019210297A (ja) | 2015-10-07 | 2019-09-20 | ファルネソイドｘ受容体調節剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019171488A Pending JP2019210297A (ja) | 2015-10-07 | 2019-09-20 | ファルネソイドｘ受容体調節剤 |
Country Status (26)
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20170094184A (ko) | 2014-11-06 | 2017-08-17 | 이난타 파마슈티칼스, 인코포레이티드 | Fxr/tgr5 작용제로서의 담즙산 유사체 및 이의 이용 방법 |
| US10208081B2 (en) | 2014-11-26 | 2019-02-19 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof |
| KR20170099909A (ko) | 2014-11-26 | 2017-09-01 | 이난타 파마슈티칼스, 인코포레이티드 | Fxr/tgr5 작용제로서의 담즙산 유사체 및 이의 이용 방법 |
| WO2016086115A1 (en) | 2014-11-26 | 2016-06-02 | Enanta Pharmaceuticals, Inc. | Tetrazole derivatives of bile acids as fxr/tgr5 agonists and methods of use thereof |
| SG11201706089RA (en) | 2015-02-11 | 2017-09-28 | Enanta Pharm Inc | Bile acid analogs as fxr/tgr5 agonists and methods of use thereof |
| PT3277286T (pt) | 2015-03-31 | 2021-07-01 | Enanta Pharm Inc | Derivados de ácidos biliares como agonistas de fxr/tgr5 e métodos de utilização destes |
| EP3359160B1 (en) | 2015-10-07 | 2021-08-25 | Intercept Pharmaceuticals, Inc. | Farnesoid x receptor modulators |
| WO2017147174A1 (en) | 2016-02-23 | 2017-08-31 | Enanta Pharmaceuticals, Inc. | Heteroaryl containing bile acid analogs as fxr/tgr5 agonists and methods of use thereof |
| US10364267B2 (en) | 2016-02-23 | 2019-07-30 | Enanta Pharmaceuticals, Inc. | Deuterated bile acid derivatives as FXR/TGR5 agonists and methods of use thereof |
| WO2017147137A1 (en) | 2016-02-23 | 2017-08-31 | Enanta Pharmaceuticals, Inc. | Benzoic acid derivatives of bile acid as fxr/tgr5 agonists and methods of use thereof |
| WO2018102418A1 (en) | 2016-11-29 | 2018-06-07 | Enanta Pharmaceuticals, Inc. | Process for preparation of sulfonylurea bile acid derivatives |
| US10472386B2 (en) | 2017-02-14 | 2019-11-12 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as FXR agonists and methods of use thereof |
| WO2018187804A1 (en) | 2017-04-07 | 2018-10-11 | Enanta Pharmaceuticals, Inc. | Process for preparation of sulfonyl carbamate bile acid derivatives |
| KR20250109791A (ko) | 2017-06-23 | 2025-07-17 | 인터셉트 파마슈티컬즈, 인크. | 담즙산 유도체 제조를 위한 방법 및 중간체 |
| CN111050772A (zh) | 2017-07-24 | 2020-04-21 | 英特塞普特医药品公司 | 同位素标记的胆汁酸衍生物 |
| ES2999311T3 (en) * | 2017-12-19 | 2025-02-25 | Xian Biocare Pharma Ltd | Compound for treating metabolic diseases and preparation method and use thereof |
| GB201812382D0 (en) | 2018-07-30 | 2018-09-12 | Nzp Uk Ltd | Compounds |
| WO2020243590A1 (en) | 2019-05-30 | 2020-12-03 | Intercept Pharmaceuticals, Inc. | Pharmaceutical compositions comprising a fxr agonist and a fibrate for use in the treatment of cholestatic liver disease |
| WO2023288123A1 (en) | 2021-07-16 | 2023-01-19 | Interecept Pharmaceuticals, Inc. | Methods and intermediates for the preparation of 3.alpha.,7.alpha.,11.beta.-trihydroxy-6.alpha.-ethyl-5.beta.-cholan-24-oic acid |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2599481A (en) | 1948-09-28 | 1952-06-03 | Ciba Pharm Prod Inc | Reduction of steroid epoxides |
| EP0101554B1 (en) * | 1982-07-29 | 1986-10-15 | Lehner A.G. | New derivatives of biliary acids, process for the production thereof and pharmaceutical compositions containing the same |
| IT1223313B (it) | 1987-10-20 | 1990-09-19 | Gipharmex Spa | Derivati di acidi biliari loro preparazione e composizioni farmaceutiche che li contengono |
| DE10113257C1 (de) | 2001-03-19 | 2002-11-14 | Inst Mikrotechnik Mainz Gmbh | Elektrophoresevorrichtung und ihre Verwendung |
| US20070197484A1 (en) * | 2001-05-03 | 2007-08-23 | Ching Song | Method of treating disorder related to high cholesterol concentration |
| ES2523591T3 (es) * | 2006-06-27 | 2014-11-27 | Intercept Pharmaceuticals Inc. | Derivados de ácidos biliares como ligandos de FXR para la prevención o el tratamiento de enfermedades o estados mediados por FXR |
| DK2376519T3 (da) * | 2008-11-19 | 2014-02-03 | Intercept Pharmaceuticals Inc | TGR5-modulatorer og fremgangsmåde til anvendelse deraf |
| EA201990211A1 (ru) | 2012-06-19 | 2019-06-28 | Интерсепт Фармасьютикалз, Инк. | Получение, применение и твердые формы обетихолевой кислоты |
| KR102106186B1 (ko) * | 2012-11-28 | 2020-05-04 | 인터셉트 파마슈티컬즈, 인크. | 폐 질환의 치료 |
| ES2847002T3 (es) | 2013-05-14 | 2021-07-30 | Intercept Pharmaceuticals Inc | Derivados 11-hidroxil-6-sustituidos de ácidos biliares y conjugados de aminoácido de los mismos como moduladores del receptor X farnesoide |
| US9351083B2 (en) | 2013-10-17 | 2016-05-24 | Turtle Beach Corporation | Transparent parametric emitter |
| KR20170099909A (ko) * | 2014-11-26 | 2017-09-01 | 이난타 파마슈티칼스, 인코포레이티드 | Fxr/tgr5 작용제로서의 담즙산 유사체 및 이의 이용 방법 |
| WO2016086115A1 (en) * | 2014-11-26 | 2016-06-02 | Enanta Pharmaceuticals, Inc. | Tetrazole derivatives of bile acids as fxr/tgr5 agonists and methods of use thereof |
| EP3359160B1 (en) | 2015-10-07 | 2021-08-25 | Intercept Pharmaceuticals, Inc. | Farnesoid x receptor modulators |
| MX2018003914A (es) | 2015-10-07 | 2018-05-23 | Stoller Ets | Manejo de etileno en plantas mediante el uso de una formula agricola sinergica que comprende diacil o diarilurea y al menos un complejo de metales. |
| SG11201807784SA (en) | 2016-03-11 | 2018-10-30 | Intercept Pharmaceuticals Inc | 3-desoxy derivative and pharmaceutical compositions thereof |
| KR20250109791A (ko) * | 2017-06-23 | 2025-07-17 | 인터셉트 파마슈티컬즈, 인크. | 담즙산 유도체 제조를 위한 방법 및 중간체 |
| WO2020243590A1 (en) | 2019-05-30 | 2020-12-03 | Intercept Pharmaceuticals, Inc. | Pharmaceutical compositions comprising a fxr agonist and a fibrate for use in the treatment of cholestatic liver disease |
-
2016
- 2016-10-07 EP EP16854420.3A patent/EP3359160B1/en active Active
- 2016-10-07 AR ARP160103074A patent/AR106293A1/es unknown
- 2016-10-07 TW TW105132613A patent/TW201718621A/zh unknown
- 2016-10-07 CA CA3000881A patent/CA3000881C/en active Active
- 2016-10-07 KR KR1020187012652A patent/KR20180061351A/ko not_active Ceased
- 2016-10-07 MA MA42339A patent/MA42339A1/fr unknown
- 2016-10-07 CN CN201680063616.0A patent/CN108348530B/zh active Active
- 2016-10-07 EP EP21192609.2A patent/EP3981779A1/en not_active Withdrawn
- 2016-10-07 DK DK16854420.3T patent/DK3359160T3/da active
- 2016-10-07 JP JP2018517509A patent/JP7021080B2/ja active Active
- 2016-10-07 MX MX2018004186A patent/MX387172B/es unknown
- 2016-10-07 WO PCT/US2016/055980 patent/WO2017062763A1/en not_active Ceased
- 2016-10-07 CR CR20180201A patent/CR20180201A/es unknown
- 2016-10-07 EA EA201890899A patent/EA038665B1/ru unknown
- 2016-10-07 AU AU2016335765A patent/AU2016335765B2/en active Active
- 2016-10-07 IL IL258359A patent/IL258359B2/en unknown
- 2016-10-07 ES ES16854420T patent/ES2898705T3/es active Active
- 2016-10-07 MA MA045761A patent/MA45761A/fr unknown
- 2016-10-07 KR KR1020257025658A patent/KR20250120445A/ko active Pending
- 2016-10-07 TN TNP/2018/000106A patent/TN2018000106A1/en unknown
- 2016-10-07 UA UAA201804942A patent/UA123948C2/uk unknown
- 2016-10-07 BR BR112018006892-6A patent/BR112018006892B1/pt active IP Right Grant
- 2016-10-07 US US15/288,390 patent/US11034717B2/en active Active
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2018
- 2018-04-05 CL CL2018000883A patent/CL2018000883A1/es unknown
- 2018-04-05 SV SV2018005662A patent/SV2018005662A/es unknown
- 2018-04-06 CO CONC2018/0003728A patent/CO2018003728A2/es unknown
- 2018-04-10 PH PH12018500777A patent/PH12018500777A1/en unknown
- 2018-04-19 EC ECIEPI201830284A patent/ECSP18030284A/es unknown
- 2018-05-03 ZA ZA2018/02901A patent/ZA201802901B/en unknown
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2019
- 2019-09-20 JP JP2019171488A patent/JP2019210297A/ja active Pending
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2021
- 2021-05-14 US US17/320,286 patent/US12291549B2/en active Active
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2025
- 2025-05-05 US US19/198,431 patent/US20250376488A1/en active Pending