JP2021502372A5 - - Google Patents
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- JP2021502372A5 JP2021502372A5 JP2020525911A JP2020525911A JP2021502372A5 JP 2021502372 A5 JP2021502372 A5 JP 2021502372A5 JP 2020525911 A JP2020525911 A JP 2020525911A JP 2020525911 A JP2020525911 A JP 2020525911A JP 2021502372 A5 JP2021502372 A5 JP 2021502372A5
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- JP
- Japan
- Prior art keywords
- nhch
- cooh
- formula
- linker
- gamma
- 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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- -1 diboron compound Chemical class 0.000 claims 39
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims 34
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 18
- 239000004471 Glycine Substances 0.000 claims 17
- 239000008186 active pharmaceutical agent Substances 0.000 claims 7
- 229940088679 drug related substance Drugs 0.000 claims 7
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 6
- ZOCHARZZJNPSEU-UHFFFAOYSA-N diboron Chemical compound B#B ZOCHARZZJNPSEU-UHFFFAOYSA-N 0.000 claims 6
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 6
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 6
- 239000005711 Benzoic acid Substances 0.000 claims 3
- 150000008575 L-amino acids Chemical group 0.000 claims 3
- 235000010233 benzoic acid Nutrition 0.000 claims 3
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- DUWWHGPELOTTOE-UHFFFAOYSA-N n-(5-chloro-2,4-dimethoxyphenyl)-3-oxobutanamide Chemical compound COC1=CC(OC)=C(NC(=O)CC(C)=O)C=C1Cl DUWWHGPELOTTOE-UHFFFAOYSA-N 0.000 claims 3
- 235000019260 propionic acid Nutrition 0.000 claims 3
- WCOQAGPRGRKKLM-UHFFFAOYSA-N pyrrolidine-3,4-diamine Chemical compound NC1CNCC1N WCOQAGPRGRKKLM-UHFFFAOYSA-N 0.000 claims 3
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 2
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 claims 2
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- AHUCXBQJEJTERU-UHFFFAOYSA-N (4-carbamoyl-2-fluorophenyl)boronic acid Chemical compound NC(=O)C1=CC=C(B(O)O)C(F)=C1 AHUCXBQJEJTERU-UHFFFAOYSA-N 0.000 claims 1
- LKXXEWDYAWOZRW-UHFFFAOYSA-N (4-carbamoyl-3-fluorophenyl)boronic acid Chemical compound NC(=O)C1=CC=C(B(O)O)C=C1F LKXXEWDYAWOZRW-UHFFFAOYSA-N 0.000 claims 1
- DMHQMKRFJWBZLV-UHFFFAOYSA-N 3-borono-5-(3-borono-4-fluorophenyl)sulfonyl-4-fluorobenzoic acid Chemical compound B(O)(O)C=1C=C(C(=O)O)C=C(C=1F)S(=O)(=O)C1=CC(=C(C=C1)F)B(O)O DMHQMKRFJWBZLV-UHFFFAOYSA-N 0.000 claims 1
- MRGFTTLPAZFITK-UHFFFAOYSA-N 3-borono-5-(3-borono-5-fluorobenzoyl)benzoic acid Chemical compound B(O)(O)C=1C=C(C(=O)O)C=C(C=1)C(C1=CC(=CC(=C1)F)B(O)O)=O MRGFTTLPAZFITK-UHFFFAOYSA-N 0.000 claims 1
- YHAQWGCPUZAMBH-UHFFFAOYSA-N 3-borono-5-(5-borono-2,4-difluorobenzoyl)benzoic acid Chemical compound B(O)(O)C=1C=C(C(=O)O)C=C(C=1)C(C1=C(C=C(C(=C1)B(O)O)F)F)=O YHAQWGCPUZAMBH-UHFFFAOYSA-N 0.000 claims 1
- UIUJIQZEACWQSV-UHFFFAOYSA-N 4-Oxobutanoic acid Natural products OC(=O)CCC=O UIUJIQZEACWQSV-UHFFFAOYSA-N 0.000 claims 1
- FSBSTRDJNASFCP-UHFFFAOYSA-N 4-borono-2-[3-borono-5-(trifluoromethyl)phenyl]sulfonyl-6-(trifluoromethyl)benzoic acid Chemical compound OB(O)C1=CC(=CC(=C1)S(=O)(=O)C1=C(C(O)=O)C(=CC(=C1)B(O)O)C(F)(F)F)C(F)(F)F FSBSTRDJNASFCP-UHFFFAOYSA-N 0.000 claims 1
- 239000004472 Lysine Substances 0.000 claims 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 1
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims 1
- 150000001732 carboxylic acid derivatives Chemical group 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 238000001212 derivatisation Methods 0.000 claims 1
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- QLNJFJADRCOGBJ-UHFFFAOYSA-N propionamide Chemical compound CCC(N)=O QLNJFJADRCOGBJ-UHFFFAOYSA-N 0.000 claims 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 1
- 0 CC(NCCN(*)C(C)=O)=O Chemical compound CC(NCCN(*)C(C)=O)=O 0.000 description 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023051919A JP7622123B2 (ja) | 2017-11-09 | 2023-03-28 | ジボロン化合物および糖尿病関連ペプチドまたはタンパク質を含むジボロンコンジュゲートならびに１－ヒドロキシ－４－（トリフルオロメチル）－１，３－ジヒドロベンゾ［ｃ］［１，２］オキサボロール－６－カルボン酸 |
| JP2025005534A JP2025061325A (ja) | 2017-11-09 | 2025-01-15 | グルコース感受性アルブミン結合誘導体 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP17200734 | 2017-11-09 | ||
| EP17200734.6 | 2017-11-09 | ||
| EP18178294 | 2018-06-18 | ||
| EP18178294.7 | 2018-06-18 | ||
| PCT/EP2018/080650 WO2019092125A1 (en) | 2017-11-09 | 2018-11-08 | Glucose-sensitive albumin-binding derivatives |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023051919A Division JP7622123B2 (ja) | 2017-11-09 | 2023-03-28 | ジボロン化合物および糖尿病関連ペプチドまたはタンパク質を含むジボロンコンジュゲートならびに１－ヒドロキシ－４－（トリフルオロメチル）－１，３－ジヒドロベンゾ［ｃ］［１，２］オキサボロール－６－カルボン酸 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021502372A JP2021502372A (ja) | 2021-01-28 |
| JP2021502372A5 true JP2021502372A5 (https=) | 2021-11-18 |
| JP7254792B2 JP7254792B2 (ja) | 2023-04-10 |
Family
ID=64049277
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020525911A Active JP7254792B2 (ja) | 2017-11-09 | 2018-11-08 | グルコース感受性アルブミン結合誘導体 |
| JP2023051919A Active JP7622123B2 (ja) | 2017-11-09 | 2023-03-28 | ジボロン化合物および糖尿病関連ペプチドまたはタンパク質を含むジボロンコンジュゲートならびに１－ヒドロキシ－４－（トリフルオロメチル）－１，３－ジヒドロベンゾ［ｃ］［１，２］オキサボロール－６－カルボン酸 |
| JP2025005534A Pending JP2025061325A (ja) | 2017-11-09 | 2025-01-15 | グルコース感受性アルブミン結合誘導体 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023051919A Active JP7622123B2 (ja) | 2017-11-09 | 2023-03-28 | ジボロン化合物および糖尿病関連ペプチドまたはタンパク質を含むジボロンコンジュゲートならびに１－ヒドロキシ－４－（トリフルオロメチル）－１，３－ジヒドロベンゾ［ｃ］［１，２］オキサボロール－６－カルボン酸 |
| JP2025005534A Pending JP2025061325A (ja) | 2017-11-09 | 2025-01-15 | グルコース感受性アルブミン結合誘導体 |
Country Status (7)
| Country | Link |
|---|---|
| US (4) | US11186595B2 (https=) |
| EP (2) | EP4227313B1 (https=) |
| JP (3) | JP7254792B2 (https=) |
| CN (2) | CN111315751B (https=) |
| ES (2) | ES3056386T3 (https=) |
| MA (2) | MA71363A (https=) |
| WO (1) | WO2019092125A1 (https=) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016179568A1 (en) | 2015-05-06 | 2016-11-10 | Protomer Technologies, Inc. | Glucose responsive insulins |
| WO2019092125A1 (en) * | 2017-11-09 | 2019-05-16 | Novo Nordisk A/S | Glucose-sensitive albumin-binding derivatives |
| EP3946363A2 (en) * | 2019-03-29 | 2022-02-09 | Novo Nordisk A/S | Glucose sensitive insulin derivatives |
| CN112174989B (zh) * | 2019-07-02 | 2023-06-20 | 江西同和药业股份有限公司 | 一种克立硼罗的制备方法 |
| JP7834341B2 (ja) * | 2019-07-31 | 2026-03-24 | シーエス ファーマシューティカルズ エルエルシー | グルコース調節型立体配座スイッチを有するインスリン類似体 |
| EP4126058A1 (en) * | 2020-03-31 | 2023-02-08 | Protomer Technologies Inc. | Conjugates for selective responsiveness to vicinal diols |
| JP2024500284A (ja) * | 2020-11-19 | 2024-01-09 | プロトマー・テクノロジーズ・インコーポレイテッド | 芳香族ホウ素含有化合物及びインスリン類似体 |
| EP4255468A4 (en) * | 2020-12-02 | 2024-06-05 | The Regents of University of California | INJECTABLE BIODEGRADABLE POLYMER COMPLEX FOR GLUCOSE-DEPENDENT INSULIN DELIVERY |
| WO2022235691A1 (en) * | 2021-05-03 | 2022-11-10 | The Trustees Of Indiana University | Molecular design of glucose sensors in glucose-responsive insulin analogues |
| CN114478597B (zh) * | 2021-12-29 | 2023-08-29 | 宁波大学 | 一种快速识别葡萄糖手性的试剂及其制备方法和应用 |
| WO2023225534A1 (en) | 2022-05-18 | 2023-11-23 | Protomer Technologies Inc. | Aromatic boron-containing compounds and related insulin analogs |
| AU2024251658A1 (en) * | 2023-04-11 | 2025-09-18 | Protomer Technologies, Inc. | Compounds containing one or more diboronates and related insulin analogs |
| AU2024295902A1 (en) | 2023-07-18 | 2026-01-15 | Novo Nordisk A/S | Pharmaceutical compositions of insulin derivatives |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU628674B2 (en) | 1989-10-19 | 1992-09-17 | Nippon Oil And Fats Company, Limited | Polymer complexes of a sugar response type |
| AU2001263775A1 (en) | 2000-06-02 | 2001-12-11 | Novo-Nordisk A/S | Glucose dependent release of insulin from glucose sensing insulin derivatives |
| US7316999B2 (en) * | 2000-06-02 | 2008-01-08 | Novo Nordisk A/S | Glucose dependent release of insulin from glucose sensing insulin derivatives |
| EP1453860A2 (en) | 2001-12-02 | 2004-09-08 | Novo Nordisk A/S | Novel glucose-dependant insulins |
| US7317000B2 (en) | 2001-12-02 | 2008-01-08 | Novo Nordisk A/S | Glucose-dependent insulins |
| AU2003223930A1 (en) | 2002-06-14 | 2003-12-31 | Novo Nordisk A/S | Pharmaceutical use of boronic acids and esters thereof |
| WO2009112583A2 (en) | 2008-03-14 | 2009-09-17 | Novo Nordisk A/S | Protease-stabilized insulin analogues |
| DE102008052314A1 (de) * | 2008-10-15 | 2010-04-22 | Syntatec Chemicals Gmbh | Aromatische und heteroaromatische Poly-trifluoroborate und Verfahren zur Herstellung |
| WO2011000823A1 (en) | 2009-06-30 | 2011-01-06 | Novo Nordisk A/S | Insulin derivatives |
| TWI458732B (zh) * | 2012-06-27 | 2014-11-01 | 國立交通大學 | 具硼酸基團連接子及含有其之生物感測元件 |
| WO2014093696A2 (en) | 2012-12-12 | 2014-06-19 | Massachusetts Institute Of Technology | Insulin derivatives for diabetes treatment |
| WO2015097276A1 (en) * | 2013-12-23 | 2015-07-02 | Syngenta Participations Ag | Benzoxaborole fungicides |
| WO2015106292A1 (en) * | 2014-01-13 | 2015-07-16 | Coferon, Inc. | Bcr-abl tyrosine-kinase ligands capable of dimerizing in an aqueous solution, and methods of using same |
| AR103397A1 (es) * | 2015-01-13 | 2017-05-10 | Syngenta Participations Ag | Oxoborazoles microbicidas |
| JP6914844B2 (ja) | 2015-03-13 | 2021-08-04 | ケース ウェスタン リザーブ ユニバーシティＣａｓｅ Ｗｅｓｔｅｒｎ Ｒｅｓｅｒｖｅ Ｕｎｉｖｅｒｓｉｔｙ | グルコース制御立体配座スイッチを含むインスリン類似体 |
| WO2016179568A1 (en) | 2015-05-06 | 2016-11-10 | Protomer Technologies, Inc. | Glucose responsive insulins |
| UA121354C2 (uk) * | 2016-05-12 | 2020-05-12 | Анакор Фармасутікалз, Інк. | Нові сполуки для лікування паразитарних захворювань |
| US10690675B2 (en) * | 2017-04-14 | 2020-06-23 | Georgia Tech Research Corporation | Methods for enriching glycopeptides for global analysis of glycoproteins |
| WO2019092125A1 (en) * | 2017-11-09 | 2019-05-16 | Novo Nordisk A/S | Glucose-sensitive albumin-binding derivatives |
| EP3781147A4 (en) | 2018-04-16 | 2022-04-20 | University of Utah Research Foundation | Glucose-responsive insulin |
-
2018
- 2018-11-08 WO PCT/EP2018/080650 patent/WO2019092125A1/en not_active Ceased
- 2018-11-08 MA MA71363A patent/MA71363A/fr unknown
- 2018-11-08 MA MA050552A patent/MA50552A/fr unknown
- 2018-11-08 JP JP2020525911A patent/JP7254792B2/ja active Active
- 2018-11-08 US US16/759,378 patent/US11186595B2/en active Active
- 2018-11-08 EP EP23172873.4A patent/EP4227313B1/en active Active
- 2018-11-08 EP EP18795692.5A patent/EP3707145B1/en active Active
- 2018-11-08 ES ES23172873T patent/ES3056386T3/es active Active
- 2018-11-08 ES ES18795692T patent/ES2956032T3/es active Active
- 2018-11-08 CN CN201880072571.2A patent/CN111315751B/zh active Active
- 2018-11-08 CN CN202311566982.6A patent/CN117624207A/zh active Pending
-
2021
- 2021-10-13 US US17/500,242 patent/US11767332B2/en active Active
-
2023
- 2023-03-28 JP JP2023051919A patent/JP7622123B2/ja active Active
- 2023-06-16 US US18/210,763 patent/US12227528B2/en active Active
-
2024
- 2024-12-18 US US18/985,160 patent/US20250122226A1/en active Pending
-
2025
- 2025-01-15 JP JP2025005534A patent/JP2025061325A/ja active Pending
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