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- Withdrawn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 (https=) | 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 (https=) |
| EP (1) | EP2376098A4 (https=) |
| JP (2) | JP2012512898A (https=) |
| KR (1) | KR20110114568A (https=) |
| CN (1) | CN102300580A (https=) |
| AU (1) | AU2009335711A1 (https=) |
| CA (1) | CA2747195A1 (https=) |
| IL (1) | IL213341A0 (https=) |
| MX (1) | MX2011006527A (https=) |
| PE (1) | PE20120331A1 (https=) |
| RU (1) | RU2578591C2 (https=) |
| SG (1) | SG172290A1 (https=) |
| WO (1) | WO2010080605A1 (https=) |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2570133B1 (en) | 2005-11-07 | 2016-03-23 | Indiana University Research and Technology Corporation | Glucagon analogs exhibiting physiological solubility and stability |
| RU2477286C2 (ru) | 2007-01-05 | 2013-03-10 | Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн | АНАЛОГИ ГЛЮКАГОНА, ОБЛАДАЮЩИЕ ПОВЫШЕННОЙ РАСТВОРИМОСТЬЮ В БУФЕРАХ С ФИЗИОЛОГИЧЕСКИМ ЗНАЧЕНИЕМ pH |
| AU2008216265B2 (en) | 2007-02-15 | 2014-04-03 | Indiana University Research And Technology Corporation | Glucagon/GLP-1 receptor co-agonists |
| WO2009058662A2 (en) | 2007-10-30 | 2009-05-07 | Indiana University Research And Technology Corporation | Glucagon antagonists |
| US8980830B2 (en) | 2007-10-30 | 2015-03-17 | Indiana University Research And Technology Corporation | Peptide compounds exhibiting glucagon antagonist and GLP-1 agonist activity |
| AU2009210570B2 (en) | 2008-01-30 | 2014-11-20 | Indiana University Research And Technology Corporation | Ester-based insulin prodrugs |
| WO2009155257A1 (en) | 2008-06-17 | 2009-12-23 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting enhanced solubility and stability physiological ph buffers |
| DK2300035T3 (en) | 2008-06-17 | 2015-11-16 | Univ Indiana Res & Tech Corp | Mixed GIP-based agonists for the treatment of metabolic diseases and obesity |
| EP2300037B1 (en) | 2008-06-17 | 2016-03-30 | Indiana University Research and Technology Corporation | Glucagon/glp-1 receptor co-agonists |
| CN102325539A (zh) | 2008-12-19 | 2012-01-18 | 印第安纳大学研究及科技有限公司 | 基于酰胺的胰高血糖素超家族肽前药 |
| WO2010080609A1 (en) | 2008-12-19 | 2010-07-15 | Indiana University Research And Technology Corporation | Amide-based insulin prodrugs |
| WO2010080606A1 (en) | 2008-12-19 | 2010-07-15 | Indiana University Research And Technology Corporation | Insulin analogs |
| 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 |
| EP2588127A4 (en) * | 2010-06-24 | 2014-06-11 | Univ Indiana Res & Tech Corp | DIPEPTIDE-NETWORKED MEDICAL ACTIVE SUBSTANCES |
| RU2580317C2 (ru) | 2010-06-24 | 2016-04-10 | Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн | Пептидные пролекарства, принадлежащие к суперсемейству амид-содержащих глюкагонов |
| JP5912112B2 (ja) | 2010-06-24 | 2016-04-27 | 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 | アミド系インスリンプロドラッグ |
| US8507428B2 (en) | 2010-12-22 | 2013-08-13 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting GIP receptor activity |
| RS56173B1 (sr) | 2011-06-22 | 2017-11-30 | Univ Indiana Res & Tech Corp | Koagonisti receptora za glukagon/glp-1 receptora |
| BR112013032717A2 (pt) | 2011-06-22 | 2017-01-24 | Univ Indiana Res & Tech Corp | coagonistas do receptor de glucagon/glp-1 |
| RU2014117678A (ru) * | 2011-11-17 | 2015-12-27 | Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн | Пептиды глюкагонового суперсемейства, обладающие глюкокортикоидной рецепторной активностью |
| US9573987B2 (en) | 2011-12-20 | 2017-02-21 | Indiana University Research And Technology Corporation | CTP-based insulin analogs for treatment of diabetes |
| 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 |
| ES2810153T3 (es) | 2012-03-01 | 2021-03-08 | Novo Nordisk As | Profármacos de GLP-1 |
| CA2877358A1 (en) | 2012-06-21 | 2013-12-27 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting gip receptor activity |
| AU2013323669B2 (en) | 2012-09-26 | 2018-03-01 | Indiana University Research And Technology Corporation | Insulin analog dimers |
| WO2014158900A1 (en) | 2013-03-14 | 2014-10-02 | Indiana University Research And Technology Corporation | Insulin-incretin conjugates |
| 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 |
| WO2016049174A1 (en) | 2014-09-24 | 2016-03-31 | Indiana University Research And Technology Corporation | Lipidated amide-based insulin prodrugs |
| ES2822994T3 (es) | 2014-09-24 | 2021-05-05 | Univ Indiana Res & Tech Corp | Conjugados de incretina-insulina |
| EP4067368A1 (en) | 2016-06-01 | 2022-10-05 | Athira Pharma, Inc. | Compounds |
| MX2022014907A (es) * | 2020-05-26 | 2023-01-04 | Univ Indiana Res & Tech Corp | Analogos de la hormona paratiroidea para el tratamiento del hipoparatiroidismo. |
| MX2023000303A (es) | 2020-07-22 | 2023-02-09 | Novo Nordisk As | Coagonistas de los receptores del peptido 1 similar al glucagon (glp-1) y del polipeptido insulinotropico dependiente de glucosa (gip) adecuados para el suministro oral. |
| MY206918A (en) | 2020-11-06 | 2025-01-17 | Novo Nordisk As | 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 |
| JP2025517672A (ja) | 2022-05-10 | 2025-06-10 | ノヴォ ノルディスク アー／エス | プロドラッグおよびその使用 |
| 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 |
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| 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 |
| PT1171465E (pt) * | 1999-03-29 | 2004-12-31 | Uutech Ltd | Analogos de petido inibidor gastrico e sua utilizacao para o tratamento de diabetes |
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| US7052686B2 (en) * | 2000-09-29 | 2006-05-30 | Schering Corporation | Pegylated interleukin-10 |
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| 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 |
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| FR2842209B1 (fr) * | 2002-07-09 | 2007-11-23 | Nouvelle protease aspartique dite saspase et son utilisation dans le domaine cosmetique et therapeutique | |
| EP1605897B1 (en) * | 2003-03-19 | 2012-07-25 | Eli Lilly And Company | Polyethelene glycol link 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 |
| US20050187147A1 (en) * | 2003-09-22 | 2005-08-25 | Newman Michael J. | 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 |
| EP1929030A2 (en) * | 2005-09-08 | 2008-06-11 | Shire LLC | Prodrugs of t3 and t4 with enhanced bioavailability |
| WO2007109354A2 (en) * | 2006-03-21 | 2007-09-27 | Amylin Pharmaceuticals, Inc. | Peptide-peptidase inhibitor conjugates and methods of using same |
| CN106008699A (zh) * | 2006-09-08 | 2016-10-12 | Ambrx公司 | 经修饰的人类血浆多肽或Fc骨架和其用途 |
| DE102006052755A1 (de) * | 2006-11-08 | 2008-05-15 | N-Zyme Biotec Gmbh | Michaelsysteme als Transglutaminaseinhibitoren |
| AU2008216265B2 (en) * | 2007-02-15 | 2014-04-03 | Indiana University Research And Technology Corporation | Glucagon/GLP-1 receptor co-agonists |
| AU2009210570B2 (en) * | 2008-01-30 | 2014-11-20 | Indiana University Research And Technology Corporation | Ester-based insulin prodrugs |
| CN102325539A (zh) * | 2008-12-19 | 2012-01-18 | 印第安纳大学研究及科技有限公司 | 基于酰胺的胰高血糖素超家族肽前药 |
-
2009
- 2009-12-18 CN CN2009801518123A patent/CN102300580A/zh active Pending
- 2009-12-18 PE PE2011001237A patent/PE20120331A1/es not_active Application Discontinuation
- 2009-12-18 EP EP09837981.1A patent/EP2376098A4/en not_active Withdrawn
- 2009-12-18 RU RU2011129764/04A patent/RU2578591C2/ru not_active IP Right Cessation
- 2009-12-18 US US13/130,963 patent/US20110237493A1/en not_active Abandoned
- 2009-12-18 KR KR1020117016192A patent/KR20110114568A/ko not_active Ceased
- 2009-12-18 SG SG2011045275A patent/SG172290A1/en unknown
- 2009-12-18 AU AU2009335711A patent/AU2009335711A1/en not_active Abandoned
- 2009-12-18 CA CA2747195A patent/CA2747195A1/en not_active Abandoned
- 2009-12-18 MX MX2011006527A patent/MX2011006527A/es active IP Right Grant
- 2009-12-18 WO PCT/US2009/068711 patent/WO2010080605A1/en not_active Ceased
- 2009-12-18 JP JP2011542481A patent/JP2012512898A/ja not_active Withdrawn
-
2011
- 2011-06-02 IL IL213341A patent/IL213341A0/en unknown
-
2015
- 2015-09-14 JP JP2015181062A patent/JP2016028082A/ja active Pending