JP2020521784A5 - - Google Patents
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- JP2020521784A5 JP2020521784A5 JP2019565921A JP2019565921A JP2020521784A5 JP 2020521784 A5 JP2020521784 A5 JP 2020521784A5 JP 2019565921 A JP2019565921 A JP 2019565921A JP 2019565921 A JP2019565921 A JP 2019565921A JP 2020521784 A5 JP2020521784 A5 JP 2020521784A5
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- JP
- Japan
- Prior art keywords
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- amino acid
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- functional variant
- Prior art date
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- FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical compound C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 claims 57
- 125000003275 alpha amino acid group Chemical group 0.000 claims 53
- 238000006467 substitution reaction Methods 0.000 claims 31
- 235000014113 dietary fatty acids Nutrition 0.000 claims 28
- 229930195729 fatty acid Natural products 0.000 claims 28
- 239000000194 fatty acid Substances 0.000 claims 28
- 150000004665 fatty acids Chemical class 0.000 claims 28
- 108090000765 processed proteins & peptides Proteins 0.000 claims 26
- 125000000539 amino acid group Chemical group 0.000 claims 23
- 150000001413 amino acids Chemical class 0.000 claims 13
- 244000137850 Marrubium vulgare Species 0.000 claims 12
- 125000003277 amino group Chemical group 0.000 claims 12
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 5
- LRQKBLKVPFOOQJ-YFKPBYRVSA-N L-norleucine Chemical compound CCCC[C@H]([NH3+])C([O-])=O LRQKBLKVPFOOQJ-YFKPBYRVSA-N 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 108010016626 Dipeptides Proteins 0.000 claims 3
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 3
- 125000002252 acyl group Chemical group 0.000 claims 3
- 210000004369 blood Anatomy 0.000 claims 3
- 239000008280 blood Substances 0.000 claims 3
- 239000008103 glucose Substances 0.000 claims 3
- 125000006850 spacer group Chemical group 0.000 claims 3
- 108010010234 HDL Lipoproteins Proteins 0.000 claims 2
- 102000015779 HDL Lipoproteins Human genes 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 230000028327 secretion Effects 0.000 claims 2
- 210000002966 serum Anatomy 0.000 claims 2
- -1 with L Chemical class 0.000 claims 2
- OGNSCSPNOLGXSM-UHFFFAOYSA-N (+/-)-DABA Natural products NCCC(N)C(O)=O OGNSCSPNOLGXSM-UHFFFAOYSA-N 0.000 claims 1
- RIFRYROLBMMDGQ-UHFFFAOYSA-N 5-amino-2-(2-aminoethyl)-3-oxohexanoic acid Chemical compound NC(CC(=O)C(C(=O)O)CCN)C RIFRYROLBMMDGQ-UHFFFAOYSA-N 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000006386 Bone Resorption Diseases 0.000 claims 1
- 125000001433 C-terminal amino-acid group Chemical group 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 108010004460 Gastric Inhibitory Polypeptide Proteins 0.000 claims 1
- 102100039997 Gastric inhibitory polypeptide receptor Human genes 0.000 claims 1
- 102000051325 Glucagon Human genes 0.000 claims 1
- 108060003199 Glucagon Proteins 0.000 claims 1
- 206010018429 Glucose tolerance impaired Diseases 0.000 claims 1
- IKAIKUBBJHFNBZ-LURJTMIESA-N Gly-Lys Chemical compound NCCCC[C@@H](C(O)=O)NC(=O)CN IKAIKUBBJHFNBZ-LURJTMIESA-N 0.000 claims 1
- 101000886866 Homo sapiens Gastric inhibitory polypeptide receptor Proteins 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- OFOBLEOULBTSOW-UHFFFAOYSA-N Malonic acid Chemical compound OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 125000000729 N-terminal amino-acid group Chemical group 0.000 claims 1
- 206010033307 Overweight Diseases 0.000 claims 1
- 208000001280 Prediabetic State Diseases 0.000 claims 1
- 102000005157 Somatostatin Human genes 0.000 claims 1
- 108010056088 Somatostatin Proteins 0.000 claims 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 230000024279 bone resorption Effects 0.000 claims 1
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 claims 1
- 210000004899 c-terminal region Anatomy 0.000 claims 1
- 230000003247 decreasing effect Effects 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 230000004129 fatty acid metabolism Effects 0.000 claims 1
- 230000004136 fatty acid synthesis Effects 0.000 claims 1
- 235000021588 free fatty acids Nutrition 0.000 claims 1
- 229960003692 gamma aminobutyric acid Drugs 0.000 claims 1
- 125000002642 gamma-glutamyl group Chemical group 0.000 claims 1
- MASNOZXLGMXCHN-ZLPAWPGGSA-N glucagon Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 MASNOZXLGMXCHN-ZLPAWPGGSA-N 0.000 claims 1
- 229960004666 glucagon Drugs 0.000 claims 1
- 230000004190 glucose uptake Effects 0.000 claims 1
- 239000004220 glutamic acid Substances 0.000 claims 1
- 125000003630 glycyl group Chemical group [H]N([H])C([H])([H])C(*)=O 0.000 claims 1
- 108010015792 glycyllysine Proteins 0.000 claims 1
- 201000001421 hyperglycemia Diseases 0.000 claims 1
- 230000001771 impaired effect Effects 0.000 claims 1
- 230000003914 insulin secretion Effects 0.000 claims 1
- 230000002473 insulinotropic effect Effects 0.000 claims 1
- 235000020825 overweight Nutrition 0.000 claims 1
- 230000000291 postprandial effect Effects 0.000 claims 1
- 201000009104 prediabetes syndrome Diseases 0.000 claims 1
- 102000005962 receptors Human genes 0.000 claims 1
- 108020003175 receptors Proteins 0.000 claims 1
- 230000009467 reduction Effects 0.000 claims 1
- NHXLMOGPVYXJNR-ATOGVRKGSA-N somatostatin Chemical compound C([C@H]1C(=O)N[C@H](C(N[C@@H](CO)C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N1)[C@@H](C)O)NC(=O)CNC(=O)[C@H](C)N)C(O)=O)=O)[C@H](O)C)C1=CC=CC=C1 NHXLMOGPVYXJNR-ATOGVRKGSA-N 0.000 claims 1
- 229960000553 somatostatin Drugs 0.000 claims 1
- 150000003626 triacylglycerols Chemical class 0.000 claims 1
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 108010002139 very low density lipoprotein triglyceride Proteins 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP17173628.3 | 2017-05-31 | ||
| EP17173628 | 2017-05-31 | ||
| PCT/EP2018/064355 WO2018220123A1 (en) | 2017-05-31 | 2018-05-31 | Long-acting gip peptide analogues |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020521784A JP2020521784A (ja) | 2020-07-27 |
| JP2020521784A5 true JP2020521784A5 (enExample) | 2021-07-26 |
Family
ID=59021262
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019565921A Pending JP2020521784A (ja) | 2017-05-31 | 2018-05-31 | 長時間作用性ｇｉｐペプチド類似体 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US11572399B2 (enExample) |
| EP (2) | EP3630806B1 (enExample) |
| JP (1) | JP2020521784A (enExample) |
| KR (1) | KR102743887B1 (enExample) |
| CN (1) | CN110691788B (enExample) |
| AU (1) | AU2018276434B2 (enExample) |
| BR (1) | BR112019025195A8 (enExample) |
| CA (1) | CA3064510A1 (enExample) |
| ES (1) | ES2972848T3 (enExample) |
| PL (1) | PL3630806T3 (enExample) |
| WO (1) | WO2018220123A1 (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10968266B2 (en) | 2014-09-05 | 2021-04-06 | University Of Copenhagen | GIP peptide analogues |
| CN110691788B (zh) | 2017-05-31 | 2024-05-31 | 哥本哈根大学 | 长效gip肽类似物 |
| CN112074531B (zh) * | 2018-05-04 | 2025-04-15 | 诺和诺德股份有限公司 | Gip衍生物及其用途 |
| KR20210102911A (ko) | 2018-12-03 | 2021-08-20 | 안타그 테라퓨틱스 에이피에스 | 변형된 gip 펩티드 유사체 |
| WO2023139106A2 (en) | 2022-01-18 | 2023-07-27 | Novo Nordisk A/S | Long-acting gipr antagonists |
Family Cites Families (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5869602A (en) | 1995-03-17 | 1999-02-09 | Novo Nordisk A/S | Peptide derivatives |
| US6458924B2 (en) | 1996-08-30 | 2002-10-01 | Novo Nordisk A/S | Derivatives of GLP-1 analogs |
| ES2283025T3 (es) | 1996-08-30 | 2007-10-16 | Novo Nordisk A/S | Derivados de glp-1.1. |
| US6268343B1 (en) | 1996-08-30 | 2001-07-31 | Novo Nordisk A/S | Derivatives of GLP-1 analogs |
| US6384016B1 (en) | 1998-03-13 | 2002-05-07 | Novo Nordisk A/S | Stabilized aqueous peptide solutions |
| AU5518798A (en) | 1996-12-03 | 1998-06-29 | Trustees Of Boston University | Specific antagonists for glucose-dependent insulinotropic polypeptide (gip) |
| UA56256C2 (uk) | 1998-01-30 | 2003-05-15 | Ново Нордіск А/С | Шприц для ін'єкцій |
| WO1999043708A1 (en) | 1998-02-27 | 1999-09-02 | Novo Nordisk A/S | Glp-1 derivatives of glp-1 and exendin with protracted profile of action |
| AU6294899A (en) | 1998-10-07 | 2000-04-26 | Medical College Of Georgia Research Institute, Inc. | Glucose-dependent insulinotropic peptide for use as an osteotropic hormone |
| SG125915A1 (en) | 1998-12-07 | 2006-10-30 | Sod Conseils Rech Applic | Analogues of glp-1 |
| PT1171465E (pt) | 1999-03-29 | 2004-12-31 | Uutech Ltd | Analogos de petido inibidor gastrico e sua utilizacao para o tratamento de diabetes |
| GB0404124D0 (en) * | 2004-02-25 | 2004-03-31 | Univ Ulster | Antagonists of GIP |
| US20050272652A1 (en) | 1999-03-29 | 2005-12-08 | Gault Victor A | Peptide analogues of GIP for treatment of diabetes, insulin resistance and obesity |
| DK1355942T3 (da) | 2000-12-07 | 2008-11-17 | Lilly Co Eli | GLP-1-fusionsproteiner |
| US20030232761A1 (en) | 2002-03-28 | 2003-12-18 | Hinke Simon A. | Novel analogues of glucose-dependent insulinotropic polypeptide |
| US20050059605A1 (en) | 2003-01-31 | 2005-03-17 | Krishna Peri | Chemically modified metabolites of regulatory peptides and methods of producing and using same |
| WO2006086769A2 (en) | 2005-02-11 | 2006-08-17 | Amylin Pharmaceuticals, Inc. | Gip analog and hybrid polypeptides with selectable properties |
| US8263545B2 (en) | 2005-02-11 | 2012-09-11 | Amylin Pharmaceuticals, Inc. | GIP analog and hybrid polypeptides with selectable properties |
| TWI372629B (en) | 2005-03-18 | 2012-09-21 | Novo Nordisk As | Acylated glp-1 compounds |
| EP2004238A2 (en) | 2006-03-21 | 2008-12-24 | Amylin Pharmaceuticals, Inc. | Peptide-peptidase inhibitor conjugates and methods of using same |
| CA2660835A1 (en) | 2006-08-17 | 2008-02-21 | Amylin Pharmaceuticals, Inc. | Dpp-iv resistant gip hybrid polypeptides with selectable propperties |
| WO2010016936A1 (en) | 2008-08-07 | 2010-02-11 | Ipsen Pharma S.A.S. | Pharmaceutical compositions of analogues of glucose-dependent insulinotropic polypeptide |
| EP2318433A4 (en) | 2008-08-07 | 2012-08-08 | Ipsen Pharma Sas | GLUCOSE-DEPENDENT INSULINOTROPIC POLYPEPTIDE ANALOGUES (GIP) MODIFIED AT THE N-TERMINAL END |
| US9074014B2 (en) | 2008-08-07 | 2015-07-07 | Ipsen Pharma S.A.S. | Analogues of glucose-dependent insulinotropic polypeptide |
| MX2011001030A (es) | 2008-08-07 | 2011-04-26 | Ipsen Pharma Sas | Analogos de polipeptidos insulinotropicos dependientes de glucosa. |
| EP2320923B1 (en) | 2008-08-07 | 2014-12-24 | Ipsen Pharma S.A.S. | Truncated analogues of glucose-dependent insulinotropic polypeptide |
| 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 |
| US9023986B2 (en) | 2010-10-25 | 2015-05-05 | Hoffmann-La Roche Inc. | Glucose-dependent insulinotropic peptide analogs |
| AR084558A1 (es) * | 2010-12-22 | 2013-05-22 | Marcadia Biotech | Metodos para tratar trastornos metabolicos y obesidad con peptidos basados en glucagon activos para el receptor de peptido insulinotropico dependiente de glucosa (gip)/peptido-1 similar al glucagon (glp-1) |
| EP2718317B1 (en) * | 2011-06-10 | 2018-11-14 | Beijing Hanmi Pharmaceutical Co., Ltd. | Glucose dependent insulinotropic polypeptide analogs, pharmaceutical compositions and use thereof |
| US20140377171A1 (en) * | 2011-06-10 | 2014-12-25 | Jean Claude Reubi | Imaging and Treatment of Neuroendocrine Tumors with Glucose - Dependent Insulinotropic Polypeptide or Analogues or Antagonists Thereof |
| CN105324125A (zh) | 2013-03-15 | 2016-02-10 | 印第安纳大学研究及科技有限公司 | 具有长效的前体药物 |
| US10968266B2 (en) * | 2014-09-05 | 2021-04-06 | University Of Copenhagen | GIP peptide analogues |
| ES2883345T3 (es) | 2014-10-29 | 2021-12-07 | Zealand Pharma As | Compuestos agonistas del GIP y métodos |
| US20190000928A1 (en) | 2015-06-17 | 2019-01-03 | The California Institute For Biomedical Research | Modified therapeutic agents and compositions thereof |
| EP3526242A1 (en) * | 2016-10-12 | 2019-08-21 | University of Copenhagen | Peptide dual agonists of gipr and glp2r |
| CN110099694A (zh) | 2016-12-26 | 2019-08-06 | 花王株式会社 | 低体温改善剂 |
| JP7165496B2 (ja) | 2016-12-26 | 2022-11-04 | 花王株式会社 | 認知機能改善剤 |
| US11319369B2 (en) | 2016-12-26 | 2022-05-03 | Kao Corporation | Motor control function improving agent |
| CN110691788B (zh) | 2017-05-31 | 2024-05-31 | 哥本哈根大学 | 长效gip肽类似物 |
-
2018
- 2018-05-31 CN CN201880036341.0A patent/CN110691788B/zh active Active
- 2018-05-31 WO PCT/EP2018/064355 patent/WO2018220123A1/en not_active Ceased
- 2018-05-31 AU AU2018276434A patent/AU2018276434B2/en active Active
- 2018-05-31 PL PL18728872.5T patent/PL3630806T3/pl unknown
- 2018-05-31 BR BR112019025195A patent/BR112019025195A8/pt unknown
- 2018-05-31 EP EP18728872.5A patent/EP3630806B1/en active Active
- 2018-05-31 US US16/617,698 patent/US11572399B2/en active Active
- 2018-05-31 ES ES18728872T patent/ES2972848T3/es active Active
- 2018-05-31 JP JP2019565921A patent/JP2020521784A/ja active Pending
- 2018-05-31 CA CA3064510A patent/CA3064510A1/en active Pending
- 2018-05-31 EP EP24150677.3A patent/EP4361173A3/en active Pending
- 2018-05-31 KR KR1020197034279A patent/KR102743887B1/ko active Active
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