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 |
|---|---|---|---|
| KR1020110147684A KR101895047B1 (ko) | 2011-12-30 | 2011-12-30 | 면역글로불린 단편을 이용한 위치 특이적 글루카곤 유사 펩타이드-2 약물 결합체 |
| KR10-2011-0147684 | 2011-12-30 | ||
| 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 (enExample) | 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 (enExample) |
| EP (1) | EP2797621B1 (enExample) |
| JP (1) | JP6131490B2 (enExample) |
| KR (1) | KR101895047B1 (enExample) |
| CN (2) | CN104144697A (enExample) |
| AR (1) | AR089506A1 (enExample) |
| ES (1) | ES2725805T3 (enExample) |
| TW (1) | TWI666219B (enExample) |
| WO (1) | WO2013100704A1 (enExample) |
Families Citing this family (24)
| 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 |
| WO2015056713A1 (ja) * | 2013-10-15 | 2015-04-23 | 国立大学法人東京大学 | ｃ－Ｍｅｔタンパク質アゴニスト |
| AU2014364589B2 (en) | 2013-12-18 | 2020-02-27 | The California Institute For Biomedical Research | Modified therapeutic agents, stapled peptide lipid conjugates, and compositions thereof |
| DK3127923T3 (da) * | 2014-03-31 | 2021-11-22 | Hanmi Pharm Ind Co Ltd | Fremgangsmåde til forbedring af oppløselighed af protein og peptid ved hjælp af immunoglobulin-fc-fragment-binding |
| KR101825048B1 (ko) * | 2014-12-31 | 2018-02-05 | 주식회사 제넥신 | GLP 및 면역글로불린 하이브리드 Fc 융합 폴리펩타이드 및 이의 용도 |
| TW202444744A (zh) | 2016-07-11 | 2024-11-16 | 以色列商歐科生物製品有限公司 | 長效型凝血因子及其生產方法 |
| 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 |
| WO2018157131A1 (en) | 2017-02-27 | 2018-08-30 | 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 |
| JP7249492B2 (ja) * | 2017-08-22 | 2023-03-31 | タケダ ファーマシューティカルズ ユーエスエー 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を処置および予防するための使用 |
| CA3084326A1 (en) * | 2017-09-28 | 2019-04-04 | Jaehyuk Choi | Long-acting conjugates of glp-2 derivatives |
| KR102825098B1 (ko) * | 2017-11-06 | 2025-06-26 | 다케다 야쿠힌 고교 가부시키가이샤 | 수술전, 수술동안 또는 수술후 투여용 glp-2 유사체 및 펩티바디 |
| US20210355187A1 (en) * | 2018-10-24 | 2021-11-18 | Shire-Nps Pharmaceuticals, Inc. | Glp-2 fusion polypeptides and uses for treating and preventing gastrointestinal conditions |
| WO2020165900A1 (en) * | 2019-02-11 | 2020-08-20 | Opko Biologics Ltd. | Long-acting glp-2 analogs |
| US20220257722A1 (en) * | 2019-03-28 | 2022-08-18 | United States Government As Represented By The Department Of Veterans Affairs | Compositions and methods of treating and preventing systemic complications of acute illness |
| WO2021133087A1 (ko) * | 2019-12-24 | 2021-07-01 | 한미약품 주식회사 | Glp-2 또는 이의 결합체를 포함하는 골 대사성 질환에 대한 예방 또는 치료용 약학적 조성물 |
| CA3173353A1 (en) * | 2020-04-03 | 2021-10-07 | Jin Bong Lee | Pharmaceutical composition for preventing or treating mucositis induced by radiotherapy, chemotherapy, or combination thereof, comprising glp-2 derivatives or long-acting conjugate of same |
| US20230285584A1 (en) * | 2020-05-22 | 2023-09-14 | 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 |
| AU2022289610A1 (en) | 2021-06-09 | 2024-01-25 | The Scripps Research Institute | Long-acting dual gip/glp-1 peptide conjugates and methods of use |
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 |
| WO1997034631A1 (en) | 1996-03-18 | 1997-09-25 | Board Of Regents, The University Of Texas System | Immunoglobin-like domains with increased half lives |
| 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 |
| DK1355942T3 (da) | 2000-12-07 | 2008-11-17 | Lilly Co Eli | GLP-1-fusionsproteiner |
| WO2002066511A2 (en) * | 2001-02-16 | 2002-08-29 | Conjuchem Inc. | Long lasting glucagon-like peptide 2 (glp-2) for the treatment of gastrointestinal diseases and disorders |
| 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 |
| BRPI0406606A (pt) * | 2003-11-13 | 2005-12-06 | Hanmi Pharm Ind Co Ltd | Composição farmacêutica compreendendo uma região fc de imunoglobulina como um veìculo |
| DK1704234T3 (da) | 2003-11-21 | 2012-05-07 | Nps Pharma Inc | Fremstilling af glucagon-lignende peptid 2 og analoger |
| WO2006076471A2 (en) | 2005-01-12 | 2006-07-20 | Nobex Corporation | Bnp conjugates and methods of use |
| CN101171262B (zh) | 2005-05-04 | 2012-06-27 | 西兰制药公司 | 胰高血糖素样肽-2(glp-2)类似物 |
| 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 |
| AU2010225523B2 (en) * | 2009-03-20 | 2012-05-24 | Hanmi Science Co., Ltd. | Method for preparing a site-specific physiologically active polypeptide conjugate |
| CA2755133A1 (en) * | 2009-03-20 | 2010-09-23 | Amgen Inc. | Selective and potent peptide inhibitors of kv1.3 |
| 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 EP EP12861579.6A patent/EP2797621B1/en active Active
- 2012-12-28 CN CN201280071002.9A patent/CN104144697A/zh active Pending
- 2012-12-28 CN CN201910158317.0A patent/CN109810198B/zh active Active
- 2012-12-28 ES ES12861579T patent/ES2725805T3/es active Active
- 2012-12-28 JP JP2014550024A patent/JP6131490B2/ja active Active
- 2012-12-28 WO PCT/KR2012/011748 patent/WO2013100704A1/en not_active Ceased
- 2012-12-28 TW TW101150930A patent/TWI666219B/zh active
- 2012-12-28 US US14/369,436 patent/US9504757B2/en active Active
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