JP2013531659A5 - - Google Patents
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- Publication number
- JP2013531659A5 JP2013531659A5 JP2013516595A JP2013516595A JP2013531659A5 JP 2013531659 A5 JP2013531659 A5 JP 2013531659A5 JP 2013516595 A JP2013516595 A JP 2013516595A JP 2013516595 A JP2013516595 A JP 2013516595A JP 2013531659 A5 JP2013531659 A5 JP 2013531659A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- hydrogen
- prodrug
- gly
- 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
Links
- 229910052739 hydrogen Inorganic materials 0.000 claims description 74
- 239000001257 hydrogen Substances 0.000 claims description 70
- 125000000217 alkyl group Chemical group 0.000 claims description 65
- 150000001412 amines Chemical class 0.000 claims description 6
- 230000004962 physiological condition Effects 0.000 claims description 3
- 239000008177 pharmaceutical agent Substances 0.000 claims description 2
- 229940002612 prodrug Drugs 0.000 claims 13
- 239000000651 prodrug Substances 0.000 claims 13
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims 12
- 239000004471 Glycine Substances 0.000 claims 6
- 125000002252 acyl group Chemical group 0.000 claims 4
- 125000001931 aliphatic group Chemical group 0.000 claims 4
- 125000003277 amino group Chemical group 0.000 claims 4
- 239000002202 Polyethylene glycol Substances 0.000 claims 3
- 229920001223 polyethylene glycol Polymers 0.000 claims 3
- FUOOLUPWFVMBKG-UHFFFAOYSA-N 2-Aminoisobutyric acid Chemical compound CC(C)(N)C(O)=O FUOOLUPWFVMBKG-UHFFFAOYSA-N 0.000 claims 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 2
- 125000006850 spacer group Chemical group 0.000 claims 2
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-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
- 125000001429 N-terminal alpha-amino-acid group Chemical group 0.000 claims 1
- 235000004279 alanine Nutrition 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 description 39
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 29
- 125000003118 aryl group Chemical group 0.000 description 20
- 125000004429 atom Chemical group 0.000 description 13
- 125000000623 heterocyclic group Chemical group 0.000 description 9
- 125000003342 alkenyl group Chemical group 0.000 description 4
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 description 4
- 125000005843 halogen group Chemical group 0.000 description 4
- 125000000896 monocarboxylic acid group Chemical group 0.000 description 4
- 108010016626 Dipeptides Proteins 0.000 description 2
- 0 CC*C(*)(*)C(N(*)C(C)(*)C(C)=*)=O Chemical compound CC*C(*)(*)C(N(*)C(C)(*)C(C)=*)=O 0.000 description 1
- 125000001424 substituent group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US35819410P | 2010-06-24 | 2010-06-24 | |
| US61/358,194 | 2010-06-24 | ||
| PCT/US2011/039755 WO2011162968A1 (en) | 2010-06-24 | 2011-06-09 | Dipeptide linked medicinal agents |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013531659A JP2013531659A (ja) | 2013-08-08 |
| JP2013531659A5 true JP2013531659A5 (enExample) | 2017-02-09 |
| JP6101202B2 JP6101202B2 (ja) | 2017-03-22 |
Family
ID=45371760
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013516595A Active JP6101202B2 (ja) | 2010-06-24 | 2011-06-09 | ジペプチド結合医薬剤 |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US20130137849A1 (enExample) |
| EP (1) | EP2588127A4 (enExample) |
| JP (1) | JP6101202B2 (enExample) |
| KR (1) | KR20130083843A (enExample) |
| CN (1) | CN102958533B (enExample) |
| AR (1) | AR081984A1 (enExample) |
| CA (1) | CA2796879A1 (enExample) |
| MX (1) | MX2012014573A (enExample) |
| RU (1) | RU2013102991A (enExample) |
| TW (1) | TW201204392A (enExample) |
| WO (1) | WO2011162968A1 (enExample) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5631201B2 (ja) | 2007-03-28 | 2014-11-26 | プレジデント アンド フェローズ オブ ハーバード カレッジ | ステッチングされたポリペプチド |
| EP2300037B1 (en) | 2008-06-17 | 2016-03-30 | Indiana University Research and Technology Corporation | Glucagon/glp-1 receptor co-agonists |
| WO2010148089A1 (en) | 2009-06-16 | 2010-12-23 | Indiana University Research And Technology Corporation | Gip receptor-active glucagon compounds |
| KR102104762B1 (ko) | 2010-08-13 | 2020-04-24 | 에일러론 테라퓨틱스 인코포레이티드 | 펩티도미메틱 거대고리 |
| 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 |
| EP2768518A4 (en) | 2011-10-18 | 2015-05-27 | Aileron Therapeutics Inc | PEPTIDOMIMETIC MACROCYCLES |
| CA2864120A1 (en) | 2012-02-15 | 2013-08-22 | Aileron Therapeutics, Inc. | Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles |
| RU2642299C2 (ru) | 2012-02-15 | 2018-01-24 | Эйлерон Терапьютикс, Инк. | P53 пептидомиметические макроциклы |
| BR112015009470A2 (pt) | 2012-11-01 | 2019-12-17 | Aileron Therapeutics Inc | aminoácidos dissubstituídos e seus métodos de preparação e uso |
| EP3197478A4 (en) | 2014-09-24 | 2018-05-30 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| JP2018516844A (ja) | 2015-03-20 | 2018-06-28 | エルロン・セラピューティクス・インコーポレイテッドＡｉｌｅｒｏｎ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． | ペプチド模倣大環状分子およびその使用 |
| CA3070241A1 (en) | 2017-07-17 | 2019-01-24 | Keith Roizman | Topical delivery of therapeutic agents comprising cell-penetrating peptides for use for the treatment of age-related macular degeneration and other eye diseases |
| AU2021312323A1 (en) | 2020-07-22 | 2023-02-02 | Novo Nordisk A/S | Co-agonists at GLP-1 and GIP receptors suitable for oral delivery |
| 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 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5786335A (en) * | 1995-11-06 | 1998-07-28 | Warner-Lambert Company | Sulfhydryl containing peptides for treating vascular disease |
| EP1243276A1 (en) * | 2001-03-23 | 2002-09-25 | Franciscus Marinus Hendrikus De Groot | Elongated and multiple spacers containing activatible prodrugs |
| 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 |
| ES2632504T3 (es) * | 2007-11-20 | 2017-09-13 | Ambrx, Inc. | Polipéptidos de insulina modificados y sus usos |
| WO2009099763A1 (en) * | 2008-01-30 | 2009-08-13 | Indiana University Research And Technology Corporation | Ester-based peptide prodrugs |
| KR20110114568A (ko) * | 2008-12-19 | 2011-10-19 | 인디애나 유니버시티 리서치 앤드 테크놀로지 코퍼레이션 | 디펩티드 링크된 약효 물질 |
| RU2550696C2 (ru) * | 2008-12-19 | 2015-05-10 | Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн | Основанные на амидах пролекарства пептидов глюкагонового надсемейства |
| 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 |
-
2011
- 2011-06-09 US US13/697,050 patent/US20130137849A1/en not_active Abandoned
- 2011-06-09 CN CN201180031396.0A patent/CN102958533B/zh not_active Expired - Fee Related
- 2011-06-09 JP JP2013516595A patent/JP6101202B2/ja active Active
- 2011-06-09 CA CA2796879A patent/CA2796879A1/en not_active Abandoned
- 2011-06-09 EP EP11798607.5A patent/EP2588127A4/en not_active Withdrawn
- 2011-06-09 KR KR1020127033201A patent/KR20130083843A/ko not_active Withdrawn
- 2011-06-09 MX MX2012014573A patent/MX2012014573A/es not_active Application Discontinuation
- 2011-06-09 WO PCT/US2011/039755 patent/WO2011162968A1/en not_active Ceased
- 2011-06-09 RU RU2013102991/04A patent/RU2013102991A/ru not_active Application Discontinuation
- 2011-06-23 TW TW100121932A patent/TW201204392A/zh unknown
- 2011-06-23 AR ARP110102185A patent/AR081984A1/es unknown
-
2016
- 2016-02-05 US US15/016,959 patent/US20160158375A1/en not_active Abandoned
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