JP2021502372A5 - - Google Patents
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- Publication number
- 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
- Authority
- 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 |
|---|---|---|---|
| EP17200734.6 | 2017-11-09 | ||
| EP17200734 | 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 (enExample) | 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 (enExample) |
| EP (2) | EP3707145B1 (enExample) |
| JP (3) | JP7254792B2 (enExample) |
| CN (2) | CN111315751B (enExample) |
| ES (1) | ES2956032T3 (enExample) |
| MA (2) | MA50552A (enExample) |
| WO (1) | WO2019092125A1 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3291828A4 (en) | 2015-05-06 | 2018-10-03 | Alborz Mahdavi | Glucose responsive insulins |
| CN111315751B (zh) * | 2017-11-09 | 2023-12-12 | 诺和诺德股份有限公司 | 葡萄糖敏感性白蛋白结合衍生物 |
| TW202112397A (zh) * | 2019-03-29 | 2021-04-01 | 丹麥商諾佛．儂迪克股份有限公司 | 葡萄糖敏感型胰島素衍生物 |
| 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 |
| JP2022543586A (ja) * | 2019-07-31 | 2022-10-13 | サーマリン インコーポレイテッド | 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 |
| MX2022012208A (es) * | 2020-03-31 | 2022-12-15 | Protomer Tech Inc | Conjugados para reactividad selectiva a dioles vecinales. |
| US20240374735A1 (en) * | 2020-11-19 | 2024-11-14 | Protomer Technologies Inc. | Aromatic boron-containing compounds and insulin analogs |
| EP4255468A4 (en) * | 2020-12-02 | 2024-06-05 | The Regents of University of California | Injectable biodegradable polymeric complex for glucose-responsive 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 |
| US12139502B2 (en) | 2022-05-18 | 2024-11-12 | Protomer Technologies Inc. | Aromatic boron-containing compounds and related insulin analogs |
| KR20250165660A (ko) * | 2023-04-11 | 2025-11-26 | 프로토머 테크놀로지스 인크. | 1개 이상의 디보로네이트를 함유하는 화합물 및 관련 인슐린 유사체 |
| KR20250015926A (ko) | 2023-07-18 | 2025-02-03 | 노보 노르디스크 에이/에스 | 인슐린 유도체의 약학적 조성물 |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR930001305B1 (ko) | 1989-10-19 | 1993-02-25 | 니뽕 유우시 가부시끼가이샤 | 당 응답형 고분자 복합체(Polymer Complexes of Sugar Response Type) |
| US7316999B2 (en) * | 2000-06-02 | 2008-01-08 | Novo Nordisk A/S | Glucose dependent release of insulin from glucose sensing insulin derivatives |
| EP1290024A1 (en) * | 2000-06-02 | 2003-03-12 | Novo Nordisk A/S | Glucose dependent release of insulin from glucose sensing insulin derivatives |
| AU2002349295A1 (en) | 2001-12-02 | 2003-06-17 | Novo Nordisk A/S | Glucose dependant release of insulin from glucose sensing insulin derivatives |
| US7317000B2 (en) | 2001-12-02 | 2008-01-08 | Novo Nordisk A/S | Glucose-dependent insulins |
| WO2003105860A1 (en) | 2002-06-14 | 2003-12-24 | Novo Nordisk A/S | Pharmaceutical use of boronic acids and esters thereof |
| CN101970477B (zh) | 2008-03-14 | 2014-12-31 | 诺沃-诺迪斯克有限公司 | 蛋白酶稳定的胰岛素类似物 |
| DE102008052314A1 (de) * | 2008-10-15 | 2010-04-22 | Syntatec Chemicals Gmbh | Aromatische und heteroaromatische Poly-trifluoroborate und Verfahren zur Herstellung |
| ES2611040T3 (es) | 2009-06-30 | 2017-05-04 | Novo Nordisk A/S | Derivados de insulina |
| TWI458732B (zh) * | 2012-06-27 | 2014-11-01 | Univ Nat Chiao Tung | 具硼酸基團連接子及含有其之生物感測元件 |
| US9867869B2 (en) | 2012-12-12 | 2018-01-16 | 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 |
| EP3270949B1 (en) | 2015-03-13 | 2025-01-29 | Case Western Reserve University | Insulin analogues containing a glucose-regulated conformational switch |
| EP3291828A4 (en) | 2015-05-06 | 2018-10-03 | Alborz Mahdavi | 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 |
| CN111315751B (zh) | 2017-11-09 | 2023-12-12 | 诺和诺德股份有限公司 | 葡萄糖敏感性白蛋白结合衍生物 |
| EP3781147A4 (en) | 2018-04-16 | 2022-04-20 | University of Utah Research Foundation | Glucose-responsive insulin |
-
2018
- 2018-11-08 CN CN201880072571.2A patent/CN111315751B/zh active Active
- 2018-11-08 CN CN202311566982.6A patent/CN117624207A/zh active Pending
- 2018-11-08 MA MA050552A patent/MA50552A/fr unknown
- 2018-11-08 MA MA71363A patent/MA71363A/fr unknown
- 2018-11-08 ES ES18795692T patent/ES2956032T3/es active Active
- 2018-11-08 WO PCT/EP2018/080650 patent/WO2019092125A1/en not_active Ceased
- 2018-11-08 JP JP2020525911A patent/JP7254792B2/ja active Active
- 2018-11-08 EP EP18795692.5A patent/EP3707145B1/en 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
-
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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