JP2014524908A5 - - Google Patents
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- JP2014524908A5 JP2014524908A5 JP2014517015A JP2014517015A JP2014524908A5 JP 2014524908 A5 JP2014524908 A5 JP 2014524908A5 JP 2014517015 A JP2014517015 A JP 2014517015A JP 2014517015 A JP2014517015 A JP 2014517015A JP 2014524908 A5 JP2014524908 A5 JP 2014524908A5
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- Prior art keywords
- amino acid
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- acid sequence
- Prior art date
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- 108090000765 processed proteins & peptides Proteins 0.000 claims 48
- 150000001413 amino acids Chemical group 0.000 claims 38
- 102000051325 Glucagon Human genes 0.000 claims 4
- 108060003199 Glucagon Proteins 0.000 claims 4
- 108010086246 Glucagon-Like Peptide-1 Receptor Proteins 0.000 claims 4
- 102100032882 Glucagon-like peptide 1 receptor Human genes 0.000 claims 4
- 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 4
- 229960004666 glucagon Drugs 0.000 claims 4
- 108010063919 Glucagon Receptors Proteins 0.000 claims 3
- 102100040890 Glucagon receptor Human genes 0.000 claims 3
- 101001015516 Homo sapiens Glucagon-like peptide 1 receptor Proteins 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 210000004899 c-terminal region Anatomy 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 230000001747 exhibiting effect Effects 0.000 claims 3
- 108010036598 gastric inhibitory polypeptide receptor Proteins 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000006850 spacer group Chemical group 0.000 claims 3
- 125000001433 C-terminal amino-acid group Chemical group 0.000 claims 2
- 101710198884 GATA-type zinc finger protein 1 Proteins 0.000 claims 2
- DTHNMHAUYICORS-KTKZVXAJSA-N Glucagon-like peptide 1 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](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(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 claims 2
- 102100040918 Pro-glucagon Human genes 0.000 claims 2
- 239000000539 dimer Substances 0.000 claims 2
- 229920001223 polyethylene glycol Polymers 0.000 claims 2
- 102000004196 processed proteins & peptides Human genes 0.000 claims 2
- 108010016626 Dipeptides Proteins 0.000 claims 1
- IEFJWDNGDZAYNZ-BYPYZUCNSA-N Gly-Glu Chemical compound NCC(=O)N[C@H](C(O)=O)CCC(O)=O IEFJWDNGDZAYNZ-BYPYZUCNSA-N 0.000 claims 1
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims 1
- 206010019708 Hepatic steatosis Diseases 0.000 claims 1
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 claims 1
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims 1
- FFFHZYDWPBMWHY-VKHMYHEASA-N L-homocysteine Chemical compound OC(=O)[C@@H](N)CCS FFFHZYDWPBMWHY-VKHMYHEASA-N 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 108010002311 N-glycylglutamic acid Proteins 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 239000002202 Polyethylene glycol Substances 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 230000002378 acidificating effect Effects 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 150000001408 amides Chemical group 0.000 claims 1
- 150000007942 carboxylates Chemical class 0.000 claims 1
- 108091006116 chimeric peptides Proteins 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 229940039227 diagnostic agent Drugs 0.000 claims 1
- 239000000032 diagnostic agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 239000012634 fragment Substances 0.000 claims 1
- 230000004927 fusion Effects 0.000 claims 1
- YMAWOPBAYDPSLA-UHFFFAOYSA-N glycylglycine Chemical compound [NH3+]CC(=O)NCC([O-])=O YMAWOPBAYDPSLA-UHFFFAOYSA-N 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 102000039446 nucleic acids Human genes 0.000 claims 1
- 108020004707 nucleic acids Proteins 0.000 claims 1
- 150000007523 nucleic acids Chemical class 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 229920000642 polymer Polymers 0.000 claims 1
- 229920001184 polypeptide Polymers 0.000 claims 1
- 239000002096 quantum dot Substances 0.000 claims 1
- 150000003384 small molecules Chemical class 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 239000003053 toxin Substances 0.000 claims 1
- 231100000765 toxin Toxicity 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161500025P | 2011-06-22 | 2011-06-22 | |
| US61/500,025 | 2011-06-22 | ||
| PCT/US2012/042085 WO2012177444A2 (en) | 2011-06-22 | 2012-06-12 | Glucagon/glp-1 receptor co-agonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014524908A JP2014524908A (ja) | 2014-09-25 |
| JP2014524908A5 true JP2014524908A5 (enExample) | 2015-07-30 |
| JP6184404B2 JP6184404B2 (ja) | 2017-08-23 |
Family
ID=47362407
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014517015A Expired - Fee Related JP6184404B2 (ja) | 2011-06-22 | 2012-06-12 | グルカゴン/glp−1レセプターコアゴニスト |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US8729017B2 (enExample) |
| EP (1) | EP2723766A4 (enExample) |
| JP (1) | JP6184404B2 (enExample) |
| KR (1) | KR20140043793A (enExample) |
| CN (1) | CN103748109A (enExample) |
| AU (1) | AU2012273365A1 (enExample) |
| BR (1) | BR112013032717A2 (enExample) |
| CA (1) | CA2839867A1 (enExample) |
| MX (1) | MX2013015168A (enExample) |
| RU (1) | RU2014101697A (enExample) |
| WO (1) | WO2012177444A2 (enExample) |
Families Citing this family (66)
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| WO2007049941A1 (en) * | 2005-10-27 | 2007-05-03 | Peptron Co., Ltd | Bioactive substance carrier for in vivo stable delivery tehreof, conjugate containing the same, and method of in vivo stable delivery of the bioactive substance |
| AU2009260302B2 (en) | 2008-06-17 | 2014-10-23 | Indiana University Research And Technology Corporation | Glucagon/GLP-1 receptor co-agonists |
| US9150632B2 (en) | 2009-06-16 | 2015-10-06 | Indiana University Research And Technology Corporation | GIP receptor-active glucagon compounds |
| HRP20181591T1 (hr) | 2011-06-10 | 2018-11-30 | Hanmi Science Co., Ltd. | Novi derivati oksintomodulina i farmaceutski pripravci za liječenje pretilosti koji ih sadrže |
| AU2012270366C1 (en) | 2011-06-17 | 2017-07-13 | Hanmi Science Co., Ltd. | A conjugate comprising oxyntomodulin and an immunoglobulin fragment, and use thereof |
| EA031230B1 (ru) | 2011-06-22 | 2018-12-28 | Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн | Агонисты глюкагонового рецептора/glp-1-рецептора |
| JP6352806B2 (ja) | 2011-09-23 | 2018-07-04 | ノヴォ ノルディスク アー/エス | 新規のグルカゴン類似体 |
| JP6300239B2 (ja) * | 2012-06-21 | 2018-03-28 | 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 | Gip受容体活性を示すグルカゴンアナローグ |
| KR101968344B1 (ko) | 2012-07-25 | 2019-04-12 | 한미약품 주식회사 | 옥신토모듈린 유도체를 포함하는 고지혈증 치료용 조성물 |
| UA116217C2 (uk) | 2012-10-09 | 2018-02-26 | Санофі | Пептидна сполука як подвійний агоніст рецепторів glp1-1 та глюкагону |
| KR101993393B1 (ko) | 2012-11-06 | 2019-10-01 | 한미약품 주식회사 | 옥신토모듈린 유도체를 포함하는 당뇨병 또는 비만성 당뇨병 치료용 조성물 |
| NZ739063A (en) * | 2012-11-06 | 2019-11-29 | Hanmi Pharm Ind Co Ltd | Liquid formulation of protein conjugate comprising the oxyntomodulin and an immunoglobulin fragment |
| SG10201705097PA (en) | 2012-12-21 | 2017-07-28 | Sanofi Sa | Functionalized exendin-4 derivatives |
| CA2902352A1 (en) * | 2013-03-14 | 2014-09-18 | Medimmune Limited | Pegylated glucagon and glp-1 co-agonists for the treatment of obesity |
| PL2986313T3 (pl) * | 2013-04-18 | 2019-12-31 | Novo Nordisk A/S | Stabilni, dłużej działający współagoniści receptora glp-1/glukagonu do zastosowań medycznych |
| TW201609795A (zh) | 2013-12-13 | 2016-03-16 | 賽諾菲公司 | 作為雙重glp-1/gip受體促效劑的艾塞那肽-4(exendin-4)胜肽類似物 |
| EP3080149A1 (en) | 2013-12-13 | 2016-10-19 | Sanofi | Dual glp-1/glucagon receptor agonists |
| WO2015086730A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Non-acylated exendin-4 peptide analogues |
| WO2015086729A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Dual glp-1/gip receptor agonists |
| AR098614A1 (es) | 2013-12-18 | 2016-06-01 | Lilly Co Eli | Compuesto para el tratamiento de hipoglicemia severa |
| TW201625668A (zh) | 2014-04-07 | 2016-07-16 | 賽諾菲公司 | 作為胜肽性雙重glp-1/昇糖素受體激動劑之艾塞那肽-4衍生物 |
| TW201625669A (zh) | 2014-04-07 | 2016-07-16 | 賽諾菲公司 | 衍生自艾塞那肽-4(Exendin-4)之肽類雙重GLP-1/升糖素受體促效劑 |
| TW201625670A (zh) | 2014-04-07 | 2016-07-16 | 賽諾菲公司 | 衍生自exendin-4之雙重glp-1/升糖素受體促效劑 |
| EP3151852A1 (en) | 2014-06-04 | 2017-04-12 | Novo Nordisk A/S | Glp-1/glucagon receptor co-agonists for medical use |
| US9932381B2 (en) | 2014-06-18 | 2018-04-03 | Sanofi | Exendin-4 derivatives as selective glucagon receptor agonists |
| TWI772252B (zh) | 2014-09-16 | 2022-08-01 | 南韓商韓美藥品股份有限公司 | 長效glp-1/高血糖素受體雙促效劑治療非酒精性脂肝疾病之用途 |
| CN107108715A (zh) * | 2014-10-24 | 2017-08-29 | 默沙东公司 | 胰高血糖素和glp‑1受体的共激动剂 |
| US20160151511A1 (en) | 2014-12-02 | 2016-06-02 | Antriabio, Inc. | Proteins and protein conjugates with increased hydrophobicity |
| WO2016098275A1 (ja) * | 2014-12-15 | 2016-06-23 | 日本電気株式会社 | 通信方法 |
| KR102418477B1 (ko) | 2014-12-30 | 2022-07-08 | 한미약품 주식회사 | 글루카곤 유도체 |
| MA52253A (fr) | 2015-02-17 | 2021-02-17 | Lilly Co Eli | Formulation de poudre nasale pour le traitement de l'hypoglycémie |
| CN107708679A (zh) | 2015-06-04 | 2018-02-16 | 安特里阿比奥有限公司 | 用于制备位点特异性蛋白质偶联物的胺聚乙二醇化方法 |
| AR105319A1 (es) | 2015-06-05 | 2017-09-27 | Sanofi Sa | Profármacos que comprenden un conjugado agonista dual de glp-1 / glucagón conector ácido hialurónico |
| WO2016198628A1 (en) | 2015-06-12 | 2016-12-15 | Sanofi | Non-acylated exendin-4 derivatives as dual glp-1/glucagon receptor agonists |
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| TWI669309B (zh) | 2015-06-22 | 2019-08-21 | 美商美國禮來大藥廠 | 升糖素及glp-1共激動劑化合物 |
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| EP3359191A4 (en) | 2015-10-05 | 2019-05-29 | Merck Sharp & Dohme Corp. | ANTIBODY PEPTIDE CONJUGATES WITH AGONISTEACTIVITY ON GLUCAGON RECEPTORS AND GLUCAGON-LIKE PEPTIDE-1 |
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| EP3394091A4 (en) | 2015-12-09 | 2019-12-18 | Merck Sharp & Dohme Corp. | CO-AGONISTS OF GLUCAGON AND GLP-1 RECEPTORS |
| PL3393496T3 (pl) | 2015-12-23 | 2024-04-22 | The Johns Hopkins University | Długo działający agonista glp-1r jako terapia stanów neurologicznych i neurodegeneracyjnych |
| CN113456802A (zh) * | 2015-12-29 | 2021-10-01 | 派格生物医药(苏州)股份有限公司 | 包含glp-1受体激动剂和胰高血糖素受体激动剂的组合物及其用途 |
| PH12018501409B1 (en) * | 2015-12-31 | 2023-03-10 | Hanmi Pharmaceutical Co Ltd | Triple glucagon/glp-1/gip receptor agonist |
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| KR102505628B1 (ko) | 2017-09-25 | 2023-03-02 | 머크 샤프 앤드 돔 엘엘씨 | 글루카곤 및 glp-1 수용체의 장기-작용성 공-효능제 |
| JP7503492B2 (ja) * | 2017-11-08 | 2024-06-20 | アイオニス・ファーマシューティカルズ・インコーポレイテッド | Glp-1受容体リガンド部分コンジュゲート化オリゴヌクレオチド及びその使用 |
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| AU2019340465B2 (en) * | 2018-09-11 | 2025-08-14 | Anbition S.R.L. | Peptides and medical uses thereof |
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| EP3842061A1 (en) | 2019-12-23 | 2021-06-30 | Merck Sharp & Dohme Corp. | Stapled triazole co-agonists of the glucagon and glp-1 receptors |
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| WO2021169512A1 (zh) * | 2020-02-24 | 2021-09-02 | 中山大学 | 多肽化合物及其在预防或治疗糖尿病或糖尿病并发症中的应用 |
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| CN117586373A (zh) * | 2022-08-10 | 2024-02-23 | 成都奥达生物科技有限公司 | 一种长效双激动剂化合物 |
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| KR20260022948A (ko) | 2023-06-09 | 2026-02-20 | 썬 파마슈티컬 인더스트리스 리미티드 | Glp-1/gip 이중 수용체 작용제, glp-1/gcg 이중 수용체 작용제, 및 glp-1/gip/gcg 삼중 수용체 작용제 |
| US12303604B1 (en) | 2024-10-16 | 2025-05-20 | Currax Pharmaceuticals Llc | Pharmaceutical formulations comprising naltrexone and/or bupropion |
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-
2012
- 2012-06-12 BR BR112013032717A patent/BR112013032717A2/pt not_active IP Right Cessation
- 2012-06-12 US US13/494,480 patent/US8729017B2/en not_active Expired - Fee Related
- 2012-06-12 CA CA2839867A patent/CA2839867A1/en not_active Abandoned
- 2012-06-12 MX MX2013015168A patent/MX2013015168A/es not_active Application Discontinuation
- 2012-06-12 CN CN201280040883.8A patent/CN103748109A/zh active Pending
- 2012-06-12 EP EP12803439.4A patent/EP2723766A4/en not_active Withdrawn
- 2012-06-12 AU AU2012273365A patent/AU2012273365A1/en not_active Abandoned
- 2012-06-12 JP JP2014517015A patent/JP6184404B2/ja not_active Expired - Fee Related
- 2012-06-12 KR KR1020147001710A patent/KR20140043793A/ko not_active Withdrawn
- 2012-06-12 US US14/127,469 patent/US9309301B2/en not_active Expired - Fee Related
- 2012-06-12 RU RU2014101697/10A patent/RU2014101697A/ru not_active Application Discontinuation
- 2012-06-12 WO PCT/US2012/042085 patent/WO2012177444A2/en not_active Ceased
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