JP2015503554A5 - - Google Patents
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- Publication number
- JP2015503554A5 JP2015503554A5 JP2014550024A JP2014550024A JP2015503554A5 JP 2015503554 A5 JP2015503554 A5 JP 2015503554A5 JP 2014550024 A JP2014550024 A JP 2014550024A JP 2014550024 A JP2014550024 A JP 2014550024A JP 2015503554 A5 JP2015503554 A5 JP 2015503554A5
- Authority
- JP
- Japan
- Prior art keywords
- glp
- group
- derivative
- immunoglobulin
- fragment
- 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
- TWSALRJGPBVBQU-PKQQPRCHSA-N glucagon-like peptide 2 Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CC(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]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(O)=O)C(O)=O)[C@@H](C)CC)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)CC)C1=CC=CC=C1 TWSALRJGPBVBQU-PKQQPRCHSA-N 0.000 claims 43
- 101800000221 Glucagon-like peptide 2 Proteins 0.000 claims 39
- 102100040918 Pro-glucagon Human genes 0.000 claims 38
- 102000018071 Immunoglobulin Fc Fragments Human genes 0.000 claims 14
- 108010091135 Immunoglobulin Fc Fragments Proteins 0.000 claims 14
- 229920000642 polymer Polymers 0.000 claims 14
- 108090000765 processed proteins & peptides Proteins 0.000 claims 13
- 125000003277 amino group Chemical group 0.000 claims 9
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 8
- 108060003951 Immunoglobulin Proteins 0.000 claims 3
- 102000018358 immunoglobulin Human genes 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- KZNICNPSHKQLFF-UHFFFAOYSA-N succinimide Chemical class O=C1CCC(=O)N1 KZNICNPSHKQLFF-UHFFFAOYSA-N 0.000 claims 3
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 2
- 125000003172 aldehyde group Chemical group 0.000 claims 2
- 125000005439 maleimidyl group Chemical group C1(C=CC(N1*)=O)=O 0.000 claims 2
- 239000011541 reaction mixture Substances 0.000 claims 2
- -1 succinimidyl carboxymethyl Chemical group 0.000 claims 2
- ZJIFDEVVTPEXDL-UHFFFAOYSA-N (2,5-dioxopyrrolidin-1-yl) hydrogen carbonate Chemical compound OC(=O)ON1C(=O)CCC1=O ZJIFDEVVTPEXDL-UHFFFAOYSA-N 0.000 claims 1
- AASBXERNXVFUEJ-UHFFFAOYSA-N (2,5-dioxopyrrolidin-1-yl) propanoate Chemical compound CCC(=O)ON1C(=O)CCC1=O AASBXERNXVFUEJ-UHFFFAOYSA-N 0.000 claims 1
- KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 claims 1
- ZTQSAGDEMFDKMZ-UHFFFAOYSA-N Butyraldehyde Chemical group CCCC=O ZTQSAGDEMFDKMZ-UHFFFAOYSA-N 0.000 claims 1
- 229920002101 Chitin Polymers 0.000 claims 1
- 229920002307 Dextran Polymers 0.000 claims 1
- 208000018522 Gastrointestinal disease Diseases 0.000 claims 1
- 102000015626 Glucagon-Like Peptide-2 Receptor Human genes 0.000 claims 1
- 108010024044 Glucagon-Like Peptide-2 Receptor Proteins 0.000 claims 1
- PEEHTFAAVSWFBL-UHFFFAOYSA-N Maleimide Chemical compound O=C1NC(=O)C=C1 PEEHTFAAVSWFBL-UHFFFAOYSA-N 0.000 claims 1
- 239000002202 Polyethylene glycol Substances 0.000 claims 1
- 239000004372 Polyvinyl alcohol Substances 0.000 claims 1
- NBBJYMSMWIIQGU-UHFFFAOYSA-N Propionic aldehyde Chemical group CCC=O NBBJYMSMWIIQGU-UHFFFAOYSA-N 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 150000001299 aldehydes Chemical class 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 235000001014 amino acid Nutrition 0.000 claims 1
- 125000000539 amino acid group Chemical group 0.000 claims 1
- 150000001413 amino acids Chemical class 0.000 claims 1
- 229940053198 antiepileptics succinimide derivative Drugs 0.000 claims 1
- 229920002988 biodegradable polymer Polymers 0.000 claims 1
- 239000004621 biodegradable polymer Substances 0.000 claims 1
- 210000004899 c-terminal region Anatomy 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 229920001577 copolymer Polymers 0.000 claims 1
- 230000008878 coupling Effects 0.000 claims 1
- 238000010168 coupling process Methods 0.000 claims 1
- 238000005859 coupling reaction Methods 0.000 claims 1
- 235000018417 cysteine Nutrition 0.000 claims 1
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 1
- 239000000539 dimer Substances 0.000 claims 1
- 125000000118 dimethyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 150000004676 glycans Chemical class 0.000 claims 1
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 claims 1
- 229920002674 hyaluronan Polymers 0.000 claims 1
- 229960003160 hyaluronic acid Drugs 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 229940072221 immunoglobulins Drugs 0.000 claims 1
- 208000028774 intestinal disease Diseases 0.000 claims 1
- 230000000968 intestinal effect Effects 0.000 claims 1
- FZWBNHMXJMCXLU-BLAUPYHCSA-N isomaltotriose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1OC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)[C@@H](OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C=O)O1 FZWBNHMXJMCXLU-BLAUPYHCSA-N 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000004048 modification Effects 0.000 claims 1
- 238000012986 modification Methods 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 229920001583 poly(oxyethylated polyols) Polymers 0.000 claims 1
- 229920001223 polyethylene glycol Polymers 0.000 claims 1
- 229920001451 polypropylene glycol Polymers 0.000 claims 1
- 229920001282 polysaccharide Polymers 0.000 claims 1
- 239000005017 polysaccharide Substances 0.000 claims 1
- 229920002451 polyvinyl alcohol Polymers 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 229920002554 vinyl polymer Polymers 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR10-2011-0147684 | 2011-12-30 | ||
| KR1020110147684A KR101895047B1 (ko) | 2011-12-30 | 2011-12-30 | 면역글로불린 단편을 이용한 위치 특이적 글루카곤 유사 펩타이드-2 약물 결합체 |
| PCT/KR2012/011748 WO2013100704A1 (en) | 2011-12-30 | 2012-12-28 | A site-specific glp-2 conjugate using an immunoglobulin fragment |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015503554A JP2015503554A (ja) | 2015-02-02 |
| JP2015503554A5 true JP2015503554A5 (https=) | 2016-01-28 |
| JP6131490B2 JP6131490B2 (ja) | 2017-05-24 |
Family
ID=48698036
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014550024A Active JP6131490B2 (ja) | 2011-12-30 | 2012-12-28 | 免疫グロブリンフラグメントを用いた部位特異的ｇｌｐ−２薬物結合体 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US9504757B2 (https=) |
| EP (1) | EP2797621B1 (https=) |
| JP (1) | JP6131490B2 (https=) |
| KR (1) | KR101895047B1 (https=) |
| CN (2) | CN109810198B (https=) |
| AR (1) | AR089506A1 (https=) |
| ES (1) | ES2725805T3 (https=) |
| TW (1) | TWI666219B (https=) |
| WO (1) | WO2013100704A1 (https=) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20130049671A (ko) | 2011-11-04 | 2013-05-14 | 한미사이언스 주식회사 | 생리활성 폴리펩타이드 결합체 제조 방법 |
| AR090281A1 (es) * | 2012-03-08 | 2014-10-29 | Hanmi Science Co Ltd | Proceso mejorado para la preparacion de un complejo polipeptidico fisiologicamente activo |
| US9949927B2 (en) | 2012-04-10 | 2018-04-24 | The Regents Of The University Of California | Bis-polymer lipid-peptide conjugates and nanoparticles thereof |
| WO2015042252A1 (en) * | 2013-09-19 | 2015-03-26 | The Regents Of The University Of California | Methods of treatment using bis-polymer lipid-peptide conjugates and nanoparticles thereof |
| US9994616B2 (en) | 2013-10-15 | 2018-06-12 | The University Of Tokyo | c-Met protein agonist |
| AU2014364589B2 (en) * | 2013-12-18 | 2020-02-27 | The California Institute For Biomedical Research | Modified therapeutic agents, stapled peptide lipid conjugates, and compositions thereof |
| AU2015242657B2 (en) * | 2014-03-31 | 2020-05-21 | Hanmi Pharm. Co., Ltd. | Method for improving solubility of protein and peptide by using immunoglobulin Fc fragment linkage |
| KR101825048B1 (ko) * | 2014-12-31 | 2018-02-05 | 주식회사 제넥신 | GLP 및 면역글로불린 하이브리드 Fc 융합 폴리펩타이드 및 이의 용도 |
| MY206271A (en) | 2016-07-11 | 2024-12-06 | Opko Biologics Ltd | Long-acting coagulation factor vii and methods of producing same |
| CN107987170B (zh) * | 2016-10-27 | 2018-12-18 | 浙江道尔生物科技有限公司 | 一种用于治疗肠道疾病的融合蛋白 |
| US10925930B2 (en) | 2017-02-27 | 2021-02-23 | Urigen N.A. | Treatment of lower urinary tract epithelium with glucagon like peptide 2 |
| KR102174436B1 (ko) * | 2017-08-17 | 2020-11-04 | 주식회사 엘지화학 | 불용성 안료 화합물의 정성분석방법 |
| US20200199192A1 (en) | 2017-08-22 | 2020-06-25 | Shire-Nps Pharmaceuticals, Inc. | Glp-2 fusion polypeptides and uses for treating and preventing gastrointestinal conditions |
| CA3084326A1 (en) * | 2017-09-28 | 2019-04-04 | Jaehyuk Choi | Long-acting conjugates of glp-2 derivatives |
| US11660328B2 (en) * | 2017-11-06 | 2023-05-30 | Takeda Pharmaceutical Company Limited | GLP-2 analogs and peptibodies for administration before, during or after surgery |
| JP2022512688A (ja) * | 2018-10-24 | 2022-02-07 | シャイア－エヌピーエス ファーマシューティカルズ インコーポレイテッド | Ｇｌｐ－２融合ポリペプチドならびに消化管の状態の処置および予防のための使用 |
| EP3924369A1 (en) * | 2019-02-11 | 2021-12-22 | OPKO Biologics Ltd. | Long-acting glp-2 analogs |
| WO2020198604A1 (en) * | 2019-03-28 | 2020-10-01 | United States Government As Represented By The Department Of Veterans Affairs | Compositions and methods of treating and preventing systemic complications of acute illness |
| AU2020397917A1 (en) | 2019-12-04 | 2022-06-23 | The Scripps Research Institute | GLP2 receptor agonists and methods of use |
| JP7846622B2 (ja) * | 2019-12-24 | 2026-04-15 | ハンミ ファーマシューティカル カンパニー リミテッド | Ｇｌｐ－２又はその結合体を含む、代謝性骨疾患の予防又は治療用薬学的組成物 |
| EP4144361A4 (en) * | 2020-04-03 | 2024-05-22 | Hanmi Pharm. Co., Ltd. | PHARMACEUTICAL COMPOSITION FOR THE PREVENTION OR TREATMENT OF MUCOSITIS INDUCED BY RADIOTHERAPY, CHEMOTHERAPY OR A COMBINATION THEREOF, WITH GLP-2 DERIVATIVES OR LONG-ACTING CONJUGATE THEREOF |
| EP4154869A4 (en) * | 2020-05-22 | 2025-01-22 | Hanmi Pharm. Co., Ltd. | Liquid formulation of long-acting conjugate of glp-2 |
| CN111560062A (zh) * | 2020-05-26 | 2020-08-21 | 成都圣诺生物制药有限公司 | 一种Elisiglutide的制备方法 |
| WO2022159555A1 (en) * | 2021-01-20 | 2022-07-28 | The Trustees Of Columbia University In The City Of New York | Methods for treating graft-versus-host disease using glp-2 agonists and analogues thereof |
| MX2023014771A (es) | 2021-06-09 | 2024-03-19 | Scripps Research Inst | Conjugados peptidicos duales gip/glp-1 de accion prolongada y metodos de uso. |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4179337A (en) | 1973-07-20 | 1979-12-18 | Davis Frank F | Non-immunogenic polypeptides |
| US6096871A (en) | 1995-04-14 | 2000-08-01 | Genentech, Inc. | Polypeptides altered to contain an epitope from the Fc region of an IgG molecule for increased half-life |
| JP4046354B2 (ja) | 1996-03-18 | 2008-02-13 | ボード オブ リージェンツ，ザ ユニバーシティ オブ テキサス システム | 増大した半減期を有する免疫グロブリン様ドメイン |
| US6924264B1 (en) | 1999-04-30 | 2005-08-02 | Amylin Pharmaceuticals, Inc. | Modified exendins and exendin agonists |
| US6756480B2 (en) | 2000-04-27 | 2004-06-29 | Amgen Inc. | Modulators of receptors for parathyroid hormone and parathyroid hormone-related protein |
| BR0116024A (pt) * | 2000-12-07 | 2005-12-13 | Lilly Co Eli | Proteìna de fusão heteróloga e uso da mesma |
| ATE396202T1 (de) | 2001-02-16 | 2008-06-15 | Conjuchem Biotechnologies Inc | Lang wirkendes glucagon-ähnliches peptid-2 für die behandlung von gastrointestinalen krankheiten und störungen |
| CN1705681A (zh) * | 2002-10-14 | 2005-12-07 | 诺沃挪第克公司 | Glp－2化合物、制剂及其用途 |
| US20070060512A1 (en) * | 2003-03-04 | 2007-03-15 | Homayoun Sadeghi | Dipeptidyl-peptidase protected protein |
| ATE555133T1 (de) | 2003-11-13 | 2012-05-15 | Hanmi Holdings Co Ltd | Igg fc fragment für einen arzneimittelträger und verfahren zu dessen herstellung |
| WO2005067368A2 (en) | 2003-11-21 | 2005-07-28 | Nps Allelix Corp. | Production of glucagon like peptide 2 and analogs |
| WO2006076471A2 (en) | 2005-01-12 | 2006-07-20 | Nobex Corporation | Bnp conjugates and methods of use |
| DE602006020123D1 (de) | 2005-05-04 | 2011-03-31 | Zealand Pharma As | Glucagon-like-peptide-2- (glp-2-) analoga |
| WO2007067828A2 (en) * | 2005-10-24 | 2007-06-14 | Centocor, Inc. | Glp-2 mimetibodies, polypeptides, compositions, methods and uses |
| JP2008169195A (ja) * | 2007-01-05 | 2008-07-24 | Hanmi Pharmaceutical Co Ltd | キャリア物質を用いたインスリン分泌ペプチド薬物結合体 |
| BRPI1013626B8 (pt) | 2009-03-20 | 2021-05-25 | Hanmi Holdings Co Ltd | método para preparar conjugado de polipeptídeo fisiologicamente ativo em sítio específico |
| EP2408814B1 (en) * | 2009-03-20 | 2018-11-21 | Amgen Inc. | Carrier immunoglobulins and uses thereof |
| KR101746686B1 (ko) * | 2010-10-26 | 2017-06-15 | 한미사이언스 주식회사 | 면역글로불린 단편을 이용한 글루카곤 유사 펩타이드―２（ｇｌｐ―２）약물 결합체 |
-
2011
- 2011-12-30 KR KR1020110147684A patent/KR101895047B1/ko active Active
-
2012
- 2012-12-27 AR ARP120105030A patent/AR089506A1/es unknown
- 2012-12-28 JP JP2014550024A patent/JP6131490B2/ja active Active
- 2012-12-28 EP EP12861579.6A patent/EP2797621B1/en active Active
- 2012-12-28 CN CN201910158317.0A patent/CN109810198B/zh active Active
- 2012-12-28 TW TW101150930A patent/TWI666219B/zh active
- 2012-12-28 ES ES12861579T patent/ES2725805T3/es active Active
- 2012-12-28 WO PCT/KR2012/011748 patent/WO2013100704A1/en not_active Ceased
- 2012-12-28 US US14/369,436 patent/US9504757B2/en active Active
- 2012-12-28 CN CN201280071002.9A patent/CN104144697A/zh active Pending
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