JP2015502971A5 - - Google Patents
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- Publication number
- JP2015502971A5 JP2015502971A5 JP2014548070A JP2014548070A JP2015502971A5 JP 2015502971 A5 JP2015502971 A5 JP 2015502971A5 JP 2014548070 A JP2014548070 A JP 2014548070A JP 2014548070 A JP2014548070 A JP 2014548070A JP 2015502971 A5 JP2015502971 A5 JP 2015502971A5
- Authority
- JP
- Japan
- Prior art keywords
- insulin
- terminally modified
- modified insulin
- terminal
- human insulin
- 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- Withdrawn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
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical group N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 19
- 101000976075 Homo sapiens Insulin Proteins 0.000 claims 12
- PBGKTOXHQIOBKM-FHFVDXKLSA-N insulin (human) Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CSSC[C@H]2C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@H](C(N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=3C=CC(O)=CC=3)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=3C=CC(O)=CC=3)C(=O)N[C@@H](CSSC[C@H](NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=3C=CC(O)=CC=3)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=3NC=NC=3)NC(=O)[C@H](CO)NC(=O)CNC1=O)C(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(=O)N[C@@H](CC(N)=O)C(O)=O)=O)CSSC[C@@H](C(N2)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](NC(=O)CN)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](N)CC=1C=CC=CC=1)C(C)C)C1=CN=CN1 PBGKTOXHQIOBKM-FHFVDXKLSA-N 0.000 claims 12
- 108090000765 processed proteins & peptides Proteins 0.000 claims 10
- 102200127556 rs34159654 Human genes 0.000 claims 9
- 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 claims 5
- 102000009027 Albumins Human genes 0.000 claims 4
- 108010088751 Albumins Proteins 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 235000018417 cysteine Nutrition 0.000 claims 4
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 4
- 238000006467 substitution reaction Methods 0.000 claims 4
- -1 N-dimethyl Inorganic materials 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 108090001061 Insulin Proteins 0.000 claims 2
- 125000000539 amino acid group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 230000007935 neutral effect Effects 0.000 claims 2
- 102000004877 Insulin Human genes 0.000 claims 1
- 102000003746 Insulin Receptor Human genes 0.000 claims 1
- 108010001127 Insulin Receptor Proteins 0.000 claims 1
- 125000001429 N-terminal alpha-amino-acid group Chemical group 0.000 claims 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 1
- 230000002378 acidificating effect Effects 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 235000001014 amino acid Nutrition 0.000 claims 1
- 150000001413 amino acids Chemical class 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 125000004063 butyryl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 235000014113 dietary fatty acids Nutrition 0.000 claims 1
- RUHSSBIALTWUSD-UHFFFAOYSA-N diethylamino-[(dimethylamino)methyl]-(dipropylamino)-methylazanium Chemical compound CN(C)C[N+](C)(N(CCC)CCC)N(CC)CC RUHSSBIALTWUSD-UHFFFAOYSA-N 0.000 claims 1
- HPNMFZURTQLUMO-UHFFFAOYSA-O diethylammonium Chemical group CC[NH2+]CC HPNMFZURTQLUMO-UHFFFAOYSA-O 0.000 claims 1
- WEHWNAOGRSTTBQ-UHFFFAOYSA-O dipropylazanium Chemical group CCC[NH2+]CCC WEHWNAOGRSTTBQ-UHFFFAOYSA-O 0.000 claims 1
- LYCAIKOWRPUZTN-UHFFFAOYSA-N ethylene glycol Natural products OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims 1
- 229930195729 fatty acid Natural products 0.000 claims 1
- 239000000194 fatty acid Substances 0.000 claims 1
- 150000004665 fatty acids Chemical class 0.000 claims 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 1
- 125000003630 glycyl group Chemical group [H]N([H])C([H])([H])C(*)=O 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims 1
- 229940125396 insulin Drugs 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000001501 propionyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 238000011191 terminal modification Methods 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11194898.0 | 2011-12-21 | ||
| EP11194898 | 2011-12-21 | ||
| US201261593636P | 2012-02-01 | 2012-02-01 | |
| US61/593,636 | 2012-02-01 | ||
| PCT/EP2012/076650 WO2013093009A1 (en) | 2011-12-21 | 2012-12-21 | N -terminally modified insulin derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015502971A JP2015502971A (ja) | 2015-01-29 |
| JP2015502971A5 true JP2015502971A5 (https=) | 2016-02-18 |
Family
ID=48667766
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014548070A Withdrawn JP2015502971A (ja) | 2011-12-21 | 2012-12-21 | Ｎ末端修飾インスリン誘導体 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20140357838A1 (https=) |
| EP (1) | EP2794648A1 (https=) |
| JP (1) | JP2015502971A (https=) |
| CN (1) | CN104364262A (https=) |
| WO (1) | WO2013093009A1 (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2015292822B2 (en) * | 2014-07-21 | 2021-11-25 | Unchained Labs | Determination of protein aggregation from the concentration dependence of delta G |
| US20180000742A1 (en) * | 2015-01-29 | 2018-01-04 | Novo Nordisk A/S | Pharmaceutical Composition for Oral Insulin Administration Comprising a Tablet Core and a Polyvinyl Alcohol Coating |
| US10822385B2 (en) * | 2016-01-13 | 2020-11-03 | Novo Nordisk A/S | EGF(A) analogues with fatty acid substituents |
| EP3655427A1 (en) | 2017-07-19 | 2020-05-27 | Novo Nordisk A/S | Bifunctional compounds |
| CN111032685A (zh) | 2017-08-17 | 2020-04-17 | 诺沃挪第克公司 | 新型酰化胰岛素类似物及其用途 |
| SG11202106167XA (en) | 2018-12-11 | 2021-07-29 | Sanofi Sa | Insulin conjugates |
| CN116621944A (zh) * | 2022-02-10 | 2023-08-22 | 成都奥达生物科技有限公司 | 一种长效肝炎病毒进入抑制剂 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2003903124A0 (en) * | 2003-06-20 | 2003-07-10 | Mark Del Borgo | Analogues of heteromeric proteins |
| MXPA06001283A (es) | 2003-08-05 | 2006-04-11 | Novo Nordisk As | Derivados de insulina novedosos. |
| EP1846447B1 (en) * | 2005-02-02 | 2013-08-21 | Novo Nordisk A/S | Insulin derivatives |
| US8097584B2 (en) | 2005-05-25 | 2012-01-17 | Novo Nordisk A/S | Stabilized formulations of insulin that comprise ethylenediamine |
| CN101437849B (zh) * | 2006-05-09 | 2015-09-30 | 诺沃-诺迪斯克有限公司 | 胰岛素衍生物 |
| WO2008145721A2 (en) | 2007-06-01 | 2008-12-04 | Novo Nordisk A/S | N-terminal modification of polypeptides for protection against degradation by aminopeptidases |
| US20110144010A1 (en) | 2007-06-01 | 2011-06-16 | Novo Nordisk A/S | Spontaneously Dispersible Preconcentrates Including a Peptide Drug in a Solid or Semisolid Carrier |
| CN102037008B (zh) | 2008-03-18 | 2016-08-31 | 诺沃-诺迪斯克有限公司 | 蛋白酶稳定化的、酰化胰岛素类似物 |
| WO2010033220A2 (en) | 2008-09-19 | 2010-03-25 | Nektar Therapeutics | Modified therapeutics peptides, methods of their preparation and use |
| WO2010060667A1 (en) | 2008-11-28 | 2010-06-03 | Novo Nordisk A/S | Pharmaceutical compositions suitable for oral administration of derivatized insulin peptides |
| CA2786953A1 (en) | 2010-01-12 | 2011-07-21 | Florian Anders Foeger | Pharmaceutical compositions for oral administration of insulin peptides |
| RU2598273C2 (ru) * | 2010-06-23 | 2016-09-20 | Ново Нордиск А/С | Производные инсулина, содержащие дополнительные дисульфидные связи |
| EP2585484A1 (en) * | 2010-06-23 | 2013-05-01 | Novo Nordisk A/S | Insulin analogues containing additional disulfide bonds |
| CN102933599A (zh) * | 2010-06-23 | 2013-02-13 | 诺沃—诺迪斯克有限公司 | 包含额外的二硫键的人胰岛素 |
-
2012
- 2012-12-21 US US14/366,987 patent/US20140357838A1/en not_active Abandoned
- 2012-12-21 CN CN201280063236.9A patent/CN104364262A/zh not_active Withdrawn
- 2012-12-21 EP EP12815698.1A patent/EP2794648A1/en not_active Withdrawn
- 2012-12-21 JP JP2014548070A patent/JP2015502971A/ja not_active Withdrawn
- 2012-12-21 WO PCT/EP2012/076650 patent/WO2013093009A1/en not_active Ceased
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