JP2015502971A5 - - Google Patents

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Publication number: JP2015502971A5
Authority: JP; Japan
Prior art keywords: insulin; terminally modified; modified insulin; terminal; human insulin
Prior art date: 2012-12-21
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 Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.): Withdrawn

Application number

JP2014548070A

Other languages

English (en)

Japanese (ja)

Other versions

JP2015502971A (ja

Filing date

2012-12-21

Publication date

2016-02-18

2012-12-21 Application filed filed Critical

2012-12-21 Priority claimed from PCT/EP2012/076650 external-priority patent/WO2013093009A1/en

2015-01-29 Publication of JP2015502971A publication Critical patent/JP2015502971A/ja

2016-02-18 Publication of JP2015502971A5 publication Critical patent/JP2015502971A5/ja

Status Withdrawn legal-status Critical Current

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

JP2014548070A 2011-12-21 2012-12-21 Ｎ末端修飾インスリン誘導体 Withdrawn JP2015502971A (ja)

Applications Claiming Priority (5)

Application Number	Priority Date	Filing Date	Title
EP11194898		2011-12-21
EP11194898.0		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 (2)	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 (2)
EP (1)	EP2794648A1 (2)
JP (1)	JP2015502971A (2)
CN (1)	CN104364262A (2)
WO (1)	WO2013093009A1 (2)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
EP3194977B1 (en) *	2014-07-21	2019-10-02	Unchained Labs	Determination of protein aggregation from the concentration dependence of delta g
WO2016119854A1 (en) *	2015-01-29	2016-08-04	Novo Nordisk A/S	Pharmaceutical composition for oral insulin administration comprising a tablet core and a polyvinyl alcohol coating
SI3402811T1 (sl) *	2016-01-13	2022-06-30	Novo Nordisk A/S	Analogi EGF(A) z maščobnokislinskimi substituenti
CA3068956A1 (en)	2017-07-19	2019-01-24	Novo Nordisk A/S	Bifunctional compounds
US10919949B2 (en)	2017-08-17	2021-02-16	Novo Nordisk A/S	Acylated insulin analogues and uses thereof
KR20210102347A (ko)	2018-12-11	2021-08-19	사노피	인슐린 수용체 결합 친화성이 감소된 인슐린 유사체
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

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AU2003903124A0 (en) *	2003-06-20	2003-07-10	Mark Del Borgo	Analogues of heteromeric proteins
CA2531988C (en)	2003-08-05	2016-06-28	Novo Nordisk A/S	Novel insulin derivatives
US20080171695A1 (en) *	2005-02-02	2008-07-17	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
HUE032284T2 (en)	2008-03-18	2017-09-28	Novo Nordisk As	Protease-stabilized, acylated insulin analogues
EP2344200A2 (en)	2008-09-19	2011-07-20	Nektar Therapeutics	Modified therapeutics peptides, methods of their preparation and use
EP2370059A1 (en)	2008-11-28	2011-10-05	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
WO2011161083A1 (en) *	2010-06-23	2011-12-29	Novo Nordisk A/S	Human insulin containing additional disulfide bonds
KR20130036290A (ko) *	2010-06-23	2013-04-11	노보 노르디스크 에이/에스	추가 이황화 결합을 함유하는 인슐린 유도체
JP5973427B2 (ja) *	2010-06-23	2016-08-23	ノヴォノルディスクアー／エス	追加のジスルフィド結合を含有するインスリン類似体

2012
- 2012-12-21 US US14/366,987 patent/US20140357838A1/en not_active Abandoned
- 2012-12-21 WO PCT/EP2012/076650 patent/WO2013093009A1/en not_active Ceased
- 2012-12-21 EP EP12815698.1A patent/EP2794648A1/en not_active Withdrawn
- 2012-12-21 CN CN201280063236.9A patent/CN104364262A/zh not_active Withdrawn
- 2012-12-21 JP JP2014548070A patent/JP2015502971A/ja not_active Withdrawn

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