JP2012512898A5 - - Google Patents
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- Publication number
- JP2012512898A5 JP2012512898A5 JP2011542481A JP2011542481A JP2012512898A5 JP 2012512898 A5 JP2012512898 A5 JP 2012512898A5 JP 2011542481 A JP2011542481 A JP 2011542481A JP 2011542481 A JP2011542481 A JP 2011542481A JP 2012512898 A5 JP2012512898 A5 JP 2012512898A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- hydrogen
- group
- aryl
- atoms
- 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.)
- Withdrawn
Links
- 125000000217 alkyl group Chemical group 0.000 claims 101
- 229910052739 hydrogen Inorganic materials 0.000 claims 73
- 239000001257 hydrogen Substances 0.000 claims 57
- 150000002431 hydrogen Chemical class 0.000 claims 30
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 27
- 125000003118 aryl group Chemical group 0.000 claims 24
- 125000004429 atom Chemical group 0.000 claims 24
- 125000000623 heterocyclic group Chemical group 0.000 claims 19
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 17
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 16
- 125000003342 alkenyl group Chemical group 0.000 claims 14
- 229910052799 carbon Inorganic materials 0.000 claims 14
- 150000001413 amino acids Chemical class 0.000 claims 13
- 239000000651 prodrug Substances 0.000 claims 13
- 229940002612 prodrug Drugs 0.000 claims 13
- 125000005843 halogen group Chemical group 0.000 claims 12
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 7
- 239000003795 chemical substances by application Substances 0.000 claims 7
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 229920000642 polymer Polymers 0.000 claims 6
- 238000003776 cleavage reaction Methods 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 230000007017 scission Effects 0.000 claims 4
- 125000002252 acyl group Chemical group 0.000 claims 3
- 150000001412 amines Chemical class 0.000 claims 3
- 230000004962 physiological condition Effects 0.000 claims 3
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 2
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Chemical compound OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 claims 2
- 239000002202 Polyethylene glycol Substances 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 125000003277 amino group Chemical group 0.000 claims 2
- 230000000975 bioactive effect Effects 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 229920001223 polyethylene glycol Polymers 0.000 claims 2
- 108090000765 processed proteins & peptides Proteins 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- XUIIKFGFIJCVMT-UHFFFAOYSA-N thyroxine-binding globulin Natural products IC1=CC(CC([NH3+])C([O-])=O)=CC(I)=C1OC1=CC(I)=C(O)C(I)=C1 XUIIKFGFIJCVMT-UHFFFAOYSA-N 0.000 claims 2
- HZCBWYNLGPIQRK-LBPRGKRZSA-N 3,3',5'-triiodo-L-thyronine Chemical compound IC1=CC(C[C@H]([NH3+])C([O-])=O)=CC=C1OC1=CC(I)=C(O)C(I)=C1 HZCBWYNLGPIQRK-LBPRGKRZSA-N 0.000 claims 1
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 claims 1
- 125000003892 C18 acyl group Chemical group 0.000 claims 1
- XUIIKFGFIJCVMT-GFCCVEGCSA-N D-thyroxine Chemical compound IC1=CC(C[C@@H](N)C(O)=O)=CC(I)=C1OC1=CC(I)=C(O)C(I)=C1 XUIIKFGFIJCVMT-GFCCVEGCSA-N 0.000 claims 1
- 229920002307 Dextran Polymers 0.000 claims 1
- 108010016626 Dipeptides Proteins 0.000 claims 1
- XUIIKFGFIJCVMT-LBPRGKRZSA-N L-thyroxine Chemical compound IC1=CC(C[C@H]([NH3+])C([O-])=O)=CC(I)=C1OC1=CC(I)=C(O)C(I)=C1 XUIIKFGFIJCVMT-LBPRGKRZSA-N 0.000 claims 1
- 229920000954 Polyglycolide Polymers 0.000 claims 1
- AUYYCJSJGJYCDS-LBPRGKRZSA-N Thyrolar Chemical compound IC1=CC(C[C@H](N)C(O)=O)=CC(I)=C1OC1=CC=C(O)C(I)=C1 AUYYCJSJGJYCDS-LBPRGKRZSA-N 0.000 claims 1
- -1 aliphatic amino acid Chemical group 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 229920001577 copolymer Polymers 0.000 claims 1
- 230000008021 deposition Effects 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 230000002255 enzymatic effect Effects 0.000 claims 1
- 229910052740 iodine Inorganic materials 0.000 claims 1
- 239000011630 iodine Substances 0.000 claims 1
- 235000014655 lactic acid Nutrition 0.000 claims 1
- 239000004310 lactic acid Substances 0.000 claims 1
- 125000005647 linker group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 229920000747 poly(lactic acid) Polymers 0.000 claims 1
- 239000004633 polyglycolic acid Substances 0.000 claims 1
- 239000004626 polylactic acid Substances 0.000 claims 1
- 210000002966 serum Anatomy 0.000 claims 1
- 229940034208 thyroxine Drugs 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US13922708P | 2008-12-19 | 2008-12-19 | |
| US61/139,227 | 2008-12-19 | ||
| PCT/US2009/068711 WO2010080605A1 (en) | 2008-12-19 | 2009-12-18 | Dipeptide linked medicinal agents |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015181062A Division JP2016028082A (ja) | 2008-12-19 | 2015-09-14 | ジペプチド結合薬用剤 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012512898A JP2012512898A (ja) | 2012-06-07 |
| JP2012512898A5 true JP2012512898A5 (enExample) | 2013-02-14 |
Family
ID=42316744
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011542481A Withdrawn JP2012512898A (ja) | 2008-12-19 | 2009-12-18 | ジペプチド結合薬用剤 |
| JP2015181062A Pending JP2016028082A (ja) | 2008-12-19 | 2015-09-14 | ジペプチド結合薬用剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015181062A Pending JP2016028082A (ja) | 2008-12-19 | 2015-09-14 | ジペプチド結合薬用剤 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20110237493A1 (enExample) |
| EP (1) | EP2376098A4 (enExample) |
| JP (2) | JP2012512898A (enExample) |
| KR (1) | KR20110114568A (enExample) |
| CN (1) | CN102300580A (enExample) |
| AU (1) | AU2009335711A1 (enExample) |
| CA (1) | CA2747195A1 (enExample) |
| IL (1) | IL213341A0 (enExample) |
| MX (1) | MX2011006527A (enExample) |
| PE (1) | PE20120331A1 (enExample) |
| RU (1) | RU2578591C2 (enExample) |
| SG (1) | SG172290A1 (enExample) |
| WO (1) | WO2010080605A1 (enExample) |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2628241C (en) | 2005-11-07 | 2016-02-02 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting physiological solubility and stability |
| CN101578102B (zh) | 2007-01-05 | 2013-07-17 | 印第安纳大学研究及科技有限公司 | 在生理性pH缓冲液中显示增强的溶解性的胰高血糖素类似物 |
| MX2009008241A (es) | 2007-02-15 | 2009-10-08 | Univ Indiana Res & Tech Corp | Co-agonistas de receptor de glucagon/glp-1. |
| JP5771005B2 (ja) | 2007-10-30 | 2015-08-26 | インディアナ ユニバーシティー リサーチ アンド テクノロジー コーポレーションＩｎｄｉａｎａ Ｕｎｉｖｅｒｓｉｔｙ Ｒｅｓｅａｒｃｈ Ａｎｄ Ｔｅｃｈｎｏｌｏｇｙ Ｃｏｒｐｏｒａｔｉｏｎ | グルカゴンアンタゴニスト及びｇｌｐ−１アゴニスト活性を示す化合物 |
| CA2707861A1 (en) | 2007-10-30 | 2009-05-07 | Indiana University Research And Technology Corporation | Glucagon antagonists |
| WO2009099763A1 (en) | 2008-01-30 | 2009-08-13 | Indiana University Research And Technology Corporation | Ester-based peptide prodrugs |
| TWI474835B (zh) | 2008-06-17 | 2015-03-01 | Univ Indiana Res & Tech Corp | 用於治療代謝病症及肥胖症之基於ｇｉｐ之混合激動劑 |
| TWI541023B (zh) | 2008-06-17 | 2016-07-11 | 印第安納大學科技研究公司 | 在生理ｐｈ緩衝液中呈現增強之溶解度及穩定性之升糖激素類似物 |
| EP2300037B1 (en) | 2008-06-17 | 2016-03-30 | Indiana University Research and Technology Corporation | Glucagon/glp-1 receptor co-agonists |
| JP5789515B2 (ja) | 2008-12-19 | 2015-10-07 | インディアナ ユニバーシティー リサーチ アンド テクノロジー コーポレーションＩｎｄｉａｎａ Ｕｎｉｖｅｒｓｉｔｙ Ｒｅｓｅａｒｃｈ Ａｎｄ Ｔｅｃｈｎｏｌｏｇｙ Ｃｏｒｐｏｒａｔｉｏｎ | インスリン類似体 |
| CN102245624B (zh) | 2008-12-19 | 2016-08-10 | 印第安纳大学研究及科技有限公司 | 基于酰胺的胰岛素前药 |
| RU2550696C2 (ru) | 2008-12-19 | 2015-05-10 | Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн | Основанные на амидах пролекарства пептидов глюкагонового надсемейства |
| WO2010148089A1 (en) | 2009-06-16 | 2010-12-23 | Indiana University Research And Technology Corporation | Gip receptor-active glucagon compounds |
| US8703701B2 (en) | 2009-12-18 | 2014-04-22 | Indiana University Research And Technology Corporation | Glucagon/GLP-1 receptor co-agonists |
| EP2528618A4 (en) | 2010-01-27 | 2015-05-27 | Univ Indiana Res & Tech Corp | GLUCAGON ANTAGONISTE AND GIP AGONISTS CONJUGATES AND COMPOSITIONS FOR THE TREATMENT OF METABOLISM DISEASES AND ADIPOSITAS |
| WO2011143208A1 (en) | 2010-05-13 | 2011-11-17 | Indiana University Research And Technology Corporation | Glucagon superfamily peptides exhibiting g protein-coupled receptor activity |
| CA2797095A1 (en) | 2010-05-13 | 2011-11-17 | Indiana University Research And Technology Corporation | Glucagon superfamily peptides exhibiting nuclear hormone receptor activity |
| EP2582719B1 (en) | 2010-06-16 | 2016-08-10 | Indiana University Research and Technology Corporation | Single chain insulin agonists exhibiting high activity at the insulin receptor |
| MX2012014576A (es) | 2010-06-24 | 2013-02-21 | Univ Indiana Res & Tech Corp | Profarmacos de peptido de la superfamilia de glucagon basado en amida. |
| US20130137849A1 (en) * | 2010-06-24 | 2013-05-30 | Indiana University Research And Technology Corporation | Dipeptide linked medicinal agents |
| CA2803164C (en) | 2010-06-24 | 2018-08-21 | Indiana University Research And Technology Corporation | Amide-based insulin prodrugs |
| WO2012088116A2 (en) | 2010-12-22 | 2012-06-28 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting gip receptor activity |
| MX2013015168A (es) | 2011-06-22 | 2014-03-31 | Univ Indiana Res & Tech Corp | Co-agonista del receptor de glucagon/glp-1. |
| CN103857408B (zh) | 2011-06-22 | 2017-04-12 | 印第安那大学科技研究公司 | 胰高血糖素/glp‑1受体协同激动剂 |
| HK1198810A1 (en) | 2011-11-17 | 2015-06-12 | Indiana University Research And Technology Corporation | Glucagon superfamily peptides exhibiting glucocorticoid receptor activity |
| CN104114183A (zh) | 2011-12-20 | 2014-10-22 | 印第安纳大学研究及科技有限公司 | 用于治疗糖尿病的基于ctp的胰岛素类似物 |
| CN103172726B (zh) * | 2011-12-22 | 2017-06-13 | 杭州淳泰科技有限公司 | 胰泌素类似物及其制备方法和用途 |
| EP2820038B1 (en) | 2012-03-01 | 2020-06-17 | Novo Nordisk A/S | Glp-1 prodrugs |
| US9340600B2 (en) | 2012-06-21 | 2016-05-17 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting GIP receptor activity |
| CN108383902A (zh) | 2012-09-26 | 2018-08-10 | 印第安纳大学研究及科技有限公司 | 胰岛素类似物二聚体 |
| JP6538645B2 (ja) | 2013-03-14 | 2019-07-03 | インディアナ ユニバーシティー リサーチ アンド テクノロジー コーポレーションＩｎｄｉａｎａ Ｕｎｉｖｅｒｓｉｔｙ Ｒｅｓｅａｒｃｈ Ａｎｄ Ｔｅｃｈｎｏｌｏｇｙ Ｃｏｒｐｏｒａｔｉｏｎ | インスリン‐インクレチン複合物 |
| CN112043835B (zh) | 2013-12-06 | 2022-10-21 | 韩捷 | 用于含氮和羟基的药物的生物可逆引入基团 |
| US10232020B2 (en) | 2014-09-24 | 2019-03-19 | Indiana University Research And Technology Corporation | Incretin-insulin conjugates |
| CN107001441A (zh) | 2014-09-24 | 2017-08-01 | 印第安纳大学研究及科技有限公司 | 脂质化的基于酰胺的胰岛素前药 |
| HRP20220479T1 (hr) | 2016-06-01 | 2022-05-27 | Athira Pharma, Inc. | Spojevi |
| BR112022024058A2 (pt) * | 2020-05-26 | 2022-12-20 | Univ Indiana Res & Tech Corp | Análogos de pth para o tratamento de hipoparatireoidismo |
| AU2021312323A1 (en) | 2020-07-22 | 2023-02-02 | Novo Nordisk A/S | Co-agonists at GLP-1 and GIP receptors suitable for oral delivery |
| EP4240420A1 (en) | 2020-11-06 | 2023-09-13 | Novo Nordisk A/S | Glp-1 prodrugs and uses hereof |
| WO2023012263A1 (en) | 2021-08-04 | 2023-02-09 | Novo Nordisk A/S | Solid oral peptide formulations |
| TW202330584A (zh) | 2022-01-20 | 2023-08-01 | 丹麥商諾佛 儂迪克股份有限公司 | 前藥及其用途 |
| CN119173275A (zh) | 2022-05-10 | 2024-12-20 | 诺和诺德股份有限公司 | Glp-1多肽的前药及其用途 |
| TW202421645A (zh) | 2022-11-25 | 2024-06-01 | 丹麥商諾佛 儂迪克股份有限公司 | 如ｇｌｐ—１之肽治療劑的口服投與 |
Family Cites Families (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3740385A (en) * | 1970-05-07 | 1973-06-19 | M Ondetti | N-terminal derivatives of secretin |
| DK119785D0 (da) * | 1985-03-15 | 1985-03-15 | Nordisk Gentofte | Insulinpraeparat |
| US4741897A (en) * | 1986-07-08 | 1988-05-03 | Baxter Travenol | Thyroxine analogs and reagents for thyroid hormone assays |
| US5545618A (en) * | 1990-01-24 | 1996-08-13 | Buckley; Douglas I. | GLP-1 analogs useful for diabetes treatment |
| DE19828113A1 (de) * | 1998-06-24 | 2000-01-05 | Probiodrug Ges Fuer Arzneim | Prodrugs von Inhibitoren der Dipeptidyl Peptidase IV |
| US20030236190A1 (en) * | 1998-09-02 | 2003-12-25 | Renuka Pillutla | Isulin and IGF-1 receptor agonists and antagonists |
| DE60012721T4 (de) * | 1999-03-29 | 2010-09-09 | Uutech Ltd., Coleraine | Analoge des magensaft inhibierenden peptides und ihre verwendung für die behandlung von diabetes |
| AUPQ661800A0 (en) * | 2000-03-31 | 2000-05-04 | Metabolic Pharmaceuticals Limited | Insulin-potentiating compounds |
| AU2001284697A1 (en) * | 2000-08-04 | 2002-02-18 | Dmi Biosciences, Inc. | Method of synthesizing diketopiperazines |
| ATE516820T1 (de) * | 2000-09-29 | 2011-08-15 | Schering Corp | Pegyliertes interleukin 10 |
| EP1243276A1 (en) * | 2001-03-23 | 2002-09-25 | Franciscus Marinus Hendrikus De Groot | Elongated and multiple spacers containing activatible prodrugs |
| IL158418A0 (en) * | 2001-04-19 | 2004-05-12 | Scripps Research Inst | In vivo incorporation of unnatural amino acids |
| CA2452044A1 (en) * | 2001-08-28 | 2003-03-13 | Eli Lilly And Company | Pre-mixes of glp-1 and basal insulin |
| US7238656B2 (en) * | 2001-08-29 | 2007-07-03 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | Protective factors against inflammation, burns and noxious stimuli |
| CZ2004710A3 (cs) * | 2001-12-20 | 2005-02-16 | Eli Lilly And Company | Inzulínová sloučenina s protrahovaným účinkem |
| FR2842209B1 (fr) * | 2002-07-09 | 2007-11-23 | Nouvelle protease aspartique dite saspase et son utilisation dans le domaine cosmetique et therapeutique | |
| AU2004231461B2 (en) * | 2003-03-19 | 2009-11-12 | Eli Lilly And Company | Polyethelene glycol linked GLP-1 compounds |
| CA2521784C (en) * | 2003-04-08 | 2012-03-27 | Yeda Research And Development Co. Ltd. | Reversible pegylated drugs |
| GB0310593D0 (en) * | 2003-05-08 | 2003-06-11 | Leuven K U Res & Dev | Peptidic prodrugs |
| KR101241862B1 (ko) * | 2003-09-19 | 2013-03-13 | 노보 노르디스크 에이/에스 | 신규 ｇｌｐ-1 유도체 |
| WO2005035003A2 (en) * | 2003-09-22 | 2005-04-21 | Dihedron Corporation | Compositions and methods for increasing drug efficiency |
| US8263545B2 (en) * | 2005-02-11 | 2012-09-11 | Amylin Pharmaceuticals, Inc. | GIP analog and hybrid polypeptides with selectable properties |
| JP2009507847A (ja) * | 2005-09-08 | 2009-02-26 | シャイア エルエルシー | 生体利用性を増強したｔ３及びｔ４のプロドラッグ |
| EP2004238A2 (en) * | 2006-03-21 | 2008-12-24 | Amylin Pharmaceuticals, Inc. | Peptide-peptidase inhibitor conjugates and methods of using same |
| WO2008030558A2 (en) * | 2006-09-08 | 2008-03-13 | Ambrx, Inc. | Modified human plasma polypeptide or fc scaffolds and their uses |
| DE102006052755A1 (de) * | 2006-11-08 | 2008-05-15 | N-Zyme Biotec Gmbh | Michaelsysteme als Transglutaminaseinhibitoren |
| MX2009008241A (es) * | 2007-02-15 | 2009-10-08 | Univ Indiana Res & Tech Corp | Co-agonistas de receptor de glucagon/glp-1. |
| WO2009099763A1 (en) * | 2008-01-30 | 2009-08-13 | Indiana University Research And Technology Corporation | Ester-based peptide prodrugs |
| RU2550696C2 (ru) * | 2008-12-19 | 2015-05-10 | Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн | Основанные на амидах пролекарства пептидов глюкагонового надсемейства |
-
2009
- 2009-12-18 KR KR1020117016192A patent/KR20110114568A/ko not_active Ceased
- 2009-12-18 PE PE2011001237A patent/PE20120331A1/es not_active Application Discontinuation
- 2009-12-18 MX MX2011006527A patent/MX2011006527A/es active IP Right Grant
- 2009-12-18 SG SG2011045275A patent/SG172290A1/en unknown
- 2009-12-18 EP EP09837981.1A patent/EP2376098A4/en not_active Withdrawn
- 2009-12-18 CN CN2009801518123A patent/CN102300580A/zh active Pending
- 2009-12-18 RU RU2011129764/04A patent/RU2578591C2/ru not_active IP Right Cessation
- 2009-12-18 CA CA2747195A patent/CA2747195A1/en not_active Abandoned
- 2009-12-18 JP JP2011542481A patent/JP2012512898A/ja not_active Withdrawn
- 2009-12-18 WO PCT/US2009/068711 patent/WO2010080605A1/en not_active Ceased
- 2009-12-18 US US13/130,963 patent/US20110237493A1/en not_active Abandoned
- 2009-12-18 AU AU2009335711A patent/AU2009335711A1/en not_active Abandoned
-
2011
- 2011-06-02 IL IL213341A patent/IL213341A0/en unknown
-
2015
- 2015-09-14 JP JP2015181062A patent/JP2016028082A/ja active Pending
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