JP6855477B2 - 血漿カリクレイン阻害薬としてのヘテロアリールカルボキサミド誘導体 - Google Patents
血漿カリクレイン阻害薬としてのヘテロアリールカルボキサミド誘導体 Download PDFInfo
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- JP6855477B2 JP6855477B2 JP2018521608A JP2018521608A JP6855477B2 JP 6855477 B2 JP6855477 B2 JP 6855477B2 JP 2018521608 A JP2018521608 A JP 2018521608A JP 2018521608 A JP2018521608 A JP 2018521608A JP 6855477 B2 JP6855477 B2 JP 6855477B2
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- 0 C*C(*)(*)N(*)*C(**)C(C)=O Chemical compound C*C(*)(*)N(*)*C(**)C(C)=O 0.000 description 10
- UYZFHZFCIOYIDB-UHFFFAOYSA-N CCOC(c1c[n](C(C)c(cn2)ccc2Cl)nc1)=O Chemical compound CCOC(c1c[n](C(C)c(cn2)ccc2Cl)nc1)=O UYZFHZFCIOYIDB-UHFFFAOYSA-N 0.000 description 2
- JBBZGFVYKHNTAA-UHFFFAOYSA-N C=Nc1ccc(C(CC2)NC(c3c[n](Cc(cc4)ccc4N(CC4N5CCC4)C5=O)nn3)=O)c2n1 Chemical compound C=Nc1ccc(C(CC2)NC(c3c[n](Cc(cc4)ccc4N(CC4N5CCC4)C5=O)nn3)=O)c2n1 JBBZGFVYKHNTAA-UHFFFAOYSA-N 0.000 description 1
- RDMFVAFQYXUCNX-UHFFFAOYSA-N CC(c(cc1)cnc1Cl)[ClH]C Chemical compound CC(c(cc1)cnc1Cl)[ClH]C RDMFVAFQYXUCNX-UHFFFAOYSA-N 0.000 description 1
- BFZGBMAIGRAQJH-UHFFFAOYSA-M CC(c1ccc(N2CC(C3)C3C2)nc1)[n]1ncc(C([O-])=O)c1 Chemical compound CC(c1ccc(N2CC(C3)C3C2)nc1)[n]1ncc(C([O-])=O)c1 BFZGBMAIGRAQJH-UHFFFAOYSA-M 0.000 description 1
- UZMMJOGGOPCLBN-UHFFFAOYSA-N CCCC1=C(CCC)NCC1C(C)=N Chemical compound CCCC1=C(CCC)NCC1C(C)=N UZMMJOGGOPCLBN-UHFFFAOYSA-N 0.000 description 1
- KACZQOKEFKFNDB-UHFFFAOYSA-N CCOC(c1c[nH]nc1)=O Chemical compound CCOC(c1c[nH]nc1)=O KACZQOKEFKFNDB-UHFFFAOYSA-N 0.000 description 1
- NNLRPWCTZMXGGC-UHFFFAOYSA-N CCOC(c1c[n](Cc2cc(N(CCN3C4CCCC3)C4=O)ccc2)nn1)=O Chemical compound CCOC(c1c[n](Cc2cc(N(CCN3C4CCCC3)C4=O)ccc2)nn1)=O NNLRPWCTZMXGGC-UHFFFAOYSA-N 0.000 description 1
- NYCINFNSECJDFM-UHFFFAOYSA-N CCOC(c1c[n](Cc2ccc(CCl)cc2)nc1)=O Chemical compound CCOC(c1c[n](Cc2ccc(CCl)cc2)nc1)=O NYCINFNSECJDFM-UHFFFAOYSA-N 0.000 description 1
- ZTDXOVAPGGNGSD-UHFFFAOYSA-N COC(c1ccc(CBr)cc1Br)=O Chemical compound COC(c1ccc(CBr)cc1Br)=O ZTDXOVAPGGNGSD-UHFFFAOYSA-N 0.000 description 1
- MTPPWWGDYBCMCL-UHFFFAOYSA-N COC(c1ccc(CN(CC2C3C2)C3=O)cc1Br)=O Chemical compound COC(c1ccc(CN(CC2C3C2)C3=O)cc1Br)=O MTPPWWGDYBCMCL-UHFFFAOYSA-N 0.000 description 1
- TYMBXXFYOJPBDM-UHFFFAOYSA-N Cc1c(CBr)ccc(C(OC)=O)c1 Chemical compound Cc1c(CBr)ccc(C(OC)=O)c1 TYMBXXFYOJPBDM-UHFFFAOYSA-N 0.000 description 1
- GPGKTIZFVDEARF-UHFFFAOYSA-N Cc1c(CO)ccc(C(OC)=O)c1 Chemical compound Cc1c(CO)ccc(C(OC)=O)c1 GPGKTIZFVDEARF-UHFFFAOYSA-N 0.000 description 1
- ZZHIDJWUJRKHGX-UHFFFAOYSA-N ClCc1ccc(CCl)cc1 Chemical compound ClCc1ccc(CCl)cc1 ZZHIDJWUJRKHGX-UHFFFAOYSA-N 0.000 description 1
- OQZPWQZTUHATOH-UHFFFAOYSA-N NC1(CC1)c(cn1)ccc1Cl Chemical compound NC1(CC1)c(cn1)ccc1Cl OQZPWQZTUHATOH-UHFFFAOYSA-N 0.000 description 1
- WAEVDUPZHCACBO-UHFFFAOYSA-N NNC1(CC1)c(cc1)cnc1N1CC(C2)C2C1 Chemical compound NNC1(CC1)c(cc1)cnc1N1CC(C2)C2C1 WAEVDUPZHCACBO-UHFFFAOYSA-N 0.000 description 1
- JBCGZNZODRVLCA-ALLBUHFWSA-N Nc1c(CC[C@H]2NC(c3c[n](Cc4ccc(N5CC(C6)C6C5)nc4)nc3)=O)c2ccn1 Chemical compound Nc1c(CC[C@H]2NC(c3c[n](Cc4ccc(N5CC(C6)C6C5)nc4)nc3)=O)c2ccn1 JBCGZNZODRVLCA-ALLBUHFWSA-N 0.000 description 1
- AAADVWQOGINTHS-UHFFFAOYSA-N OC(c1c[n](Cc(cc2)ccc2N(CC2N3CCC2)C3=O)nn1)=O Chemical compound OC(c1c[n](Cc(cc2)ccc2N(CC2N3CCC2)C3=O)nn1)=O AAADVWQOGINTHS-UHFFFAOYSA-N 0.000 description 1
- XKVGJEQSDYCLCI-UHFFFAOYSA-M [O-]C(c1c[n](Cc2ccc(N3CC(C4)C4C3)nc2)nc1)=O Chemical compound [O-]C(c1c[n](Cc2ccc(N3CC(C4)C4C3)nc2)nc1)=O XKVGJEQSDYCLCI-UHFFFAOYSA-M 0.000 description 1
Classifications
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—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
- C07D405/14—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 three or more hetero rings
-
- 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
- C07D471/02—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 two hetero rings
- C07D471/04—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
- C07D487/02—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 two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- C07D491/02—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 two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
-
- 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
- C07D498/02—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 two hetero rings
- C07D498/04—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
- C07D498/02—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 two hetero rings
- C07D498/10—Spiro-condensed systems
-
- 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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Emergency Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Endocrinology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15191759 | 2015-10-27 | ||
| EP15191759.8 | 2015-10-27 | ||
| PCT/EP2016/075222 WO2017072021A1 (en) | 2015-10-27 | 2016-10-20 | Heteroarylcarboxamide derivatives as plasma kallikrein inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018535963A JP2018535963A (ja) | 2018-12-06 |
| JP2018535963A5 JP2018535963A5 (2) | 2019-12-05 |
| JP6855477B2 true JP6855477B2 (ja) | 2021-04-07 |
Family
ID=54360328
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018521608A Active JP6855477B2 (ja) | 2015-10-27 | 2016-10-20 | 血漿カリクレイン阻害薬としてのヘテロアリールカルボキサミド誘導体 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US10640486B2 (2) |
| EP (1) | EP3368524B1 (2) |
| JP (1) | JP6855477B2 (2) |
| WO (1) | WO2017072021A1 (2) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI636047B (zh) | 2013-08-14 | 2018-09-21 | 英商卡爾維斯塔製藥有限公司 | 雜環衍生物 |
| GB201421085D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | New enzyme inhibitors |
| GB201421083D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | Enzyme inhibitors |
| EP3368524B1 (en) | 2015-10-27 | 2021-08-18 | Boehringer Ingelheim International GmbH | Heteroarylcarboxamide derivatives as plasma kallikrein inhibitors |
| DK3464271T3 (da) | 2016-05-31 | 2020-06-15 | Kalvista Pharmaceuticals Ltd | Pyrazolderivater som plasma-kallikreininhibitorer |
| GB201609603D0 (en) | 2016-06-01 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)Methyl]-3-(methoxymethyl)-1-({4-[(2-ox opyridin-1-YL)Methyl]phenyl}methyl)pyrazole-4-carboxamide |
| GB201609607D0 (en) | 2016-06-01 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of N-(3-Fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-({4-((2-oxopy ridin-1-yl)methyl)phenyl}methyl)pyrazole-4-carboxamide and salts |
| US10501440B2 (en) | 2017-04-21 | 2019-12-10 | Boehringer Ingelheim International Gmbh | Heteroarylcarboxamide derivatives as plasma kallikrein inhibitors |
| PT3716952T (pt) | 2017-11-29 | 2022-04-14 | Kalvista Pharmaceuticals Ltd | Formas de administração que incluem um inibidor de calicreína plasmática |
| GB201719881D0 (en) | 2017-11-29 | 2018-01-10 | Kalvista Pharmaceuticals Ltd | Solid forms of plasma kallikrein inhibitor and salts thereof |
| JP6828191B2 (ja) | 2018-08-16 | 2021-02-10 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 血漿カリクレイン阻害剤としての複素芳香族カルボキサミド誘導体 |
| CN112839711A (zh) | 2018-10-10 | 2021-05-25 | 勃林格殷格翰国际有限公司 | 作为血浆激肽释放酶抑制剂的苯基四唑衍生物 |
| CN109232416B (zh) * | 2018-10-24 | 2021-09-24 | 福州大学 | 一种合成4-三氟甲基-2-吡喃酮/吡啶酮化合物的方法 |
| EP4010333A1 (en) | 2019-08-09 | 2022-06-15 | Kalvista Pharmaceuticals Limited | Plasma kallikrein inhibitors |
| CN113004283B (zh) * | 2019-12-20 | 2022-08-12 | 成都康弘药业集团股份有限公司 | 作为血浆激肽释放酶抑制剂的四环类化合物及其用途 |
| CN113004284B (zh) * | 2019-12-20 | 2022-08-12 | 成都康弘药业集团股份有限公司 | 作为血浆激肽释放酶抑制剂的四环类化合物及其用途 |
| CN113004286B (zh) * | 2019-12-20 | 2022-08-12 | 成都康弘药业集团股份有限公司 | 作为血浆激肽释放酶抑制剂的三环类化合物及其用途 |
| TWI873290B (zh) * | 2020-02-13 | 2025-02-21 | 德商百靈佳殷格翰國際股份有限公司 | 作為血漿激肽釋放酶抑制劑之雜芳族甲醯胺衍生物 |
| TW202144331A (zh) | 2020-02-13 | 2021-12-01 | 德商百靈佳殷格翰國際股份有限公司 | 作為血漿激肽釋放酶抑制劑之雜芳族甲醯胺衍生物 |
| WO2021198534A1 (en) | 2020-04-04 | 2021-10-07 | Oxurion NV | Plasma kallikrein inhibitors for use in the treatment of coronaviral disease |
| CN115989224B (zh) * | 2020-06-16 | 2025-02-25 | 默沙东有限责任公司 | 血浆激肽释放酶抑制剂 |
| KR20230038526A (ko) * | 2020-07-10 | 2023-03-20 | 머크 샤프 앤드 돔 엘엘씨 | 혈장 칼리크레인 억제제 |
| WO2023144030A1 (en) | 2022-01-31 | 2023-08-03 | Oxurion NV | Plasma kallikrein inhibitor therapy for anti-vegf sensitization |
| WO2023148016A1 (en) | 2022-02-04 | 2023-08-10 | Oxurion NV | Biomarker for plasma kallikrein inhibitor therapy response |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI243164B (en) * | 2001-02-13 | 2005-11-11 | Aventis Pharma Gmbh | Acylated indanyl amines and their use as pharmaceuticals |
| US20050090529A1 (en) * | 2003-07-31 | 2005-04-28 | Pfizer Inc | 3,5 Disubstituted indazole compounds with nitrogen-bearing 5-membered heterocycles, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation |
| EP2259679A4 (en) | 2008-01-31 | 2011-09-14 | Joslin Diabetes Ct | METHODS OF TREATING KALLIKREIN RELATED DISORDERS |
| US9290485B2 (en) * | 2010-08-04 | 2016-03-22 | Novartis Ag | N-((6-amino-pyridin-3-yl)methyl)-heteroaryl-carboxamides |
| US20140378474A1 (en) * | 2012-01-27 | 2014-12-25 | Novartis Ag | 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors |
| EP2807156A1 (en) * | 2012-01-27 | 2014-12-03 | Novartis AG | Aminopyridine derivatives as plasma kallikrein inhibitors |
| EP2999697B1 (en) * | 2013-05-23 | 2017-04-19 | Kalvista Pharmaceuticals Limited | Heterocyclic derivates |
| WO2017072020A1 (en) | 2015-10-27 | 2017-05-04 | Boehringer Ingelheim International Gmbh | Heteroarylcarboxamide derivatives as plasma kallikrein inhibitors |
| EP3368524B1 (en) | 2015-10-27 | 2021-08-18 | Boehringer Ingelheim International GmbH | Heteroarylcarboxamide derivatives as plasma kallikrein inhibitors |
-
2016
- 2016-10-20 EP EP16784892.8A patent/EP3368524B1/en active Active
- 2016-10-20 US US15/770,763 patent/US10640486B2/en active Active
- 2016-10-20 JP JP2018521608A patent/JP6855477B2/ja active Active
- 2016-10-20 WO PCT/EP2016/075222 patent/WO2017072021A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| WO2017072021A1 (en) | 2017-05-04 |
| JP2018535963A (ja) | 2018-12-06 |
| US20180319771A1 (en) | 2018-11-08 |
| US10640486B2 (en) | 2020-05-05 |
| EP3368524B1 (en) | 2021-08-18 |
| EP3368524A1 (en) | 2018-09-05 |
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