JP2018505146A5 - - Google Patents
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- JP2018505146A5 JP2018505146A5 JP2017533789A JP2017533789A JP2018505146A5 JP 2018505146 A5 JP2018505146 A5 JP 2018505146A5 JP 2017533789 A JP2017533789 A JP 2017533789A JP 2017533789 A JP2017533789 A JP 2017533789A JP 2018505146 A5 JP2018505146 A5 JP 2018505146A5
- Authority
- JP
- Japan
- Prior art keywords
- amino
- ethoxy
- chem
- acetyl
- carboxy
- 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
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- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 48
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 36
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 claims 24
- 108090000376 Fibroblast growth factor 21 Proteins 0.000 claims 15
- 102000003973 Fibroblast growth factor 21 Human genes 0.000 claims 15
- -1 11-carboxyun Decanoyl-amino Chemical group 0.000 claims 12
- 125000004063 butyryl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 12
- 101000846529 Homo sapiens Fibroblast growth factor 21 Proteins 0.000 claims 6
- 102000056713 human FGF21 Human genes 0.000 claims 6
- 102000004169 proteins and genes Human genes 0.000 claims 5
- 108090000623 proteins and genes Proteins 0.000 claims 5
- 150000001875 compounds Chemical class 0.000 claims 3
- 150000001413 amino acids Chemical class 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- AOSZTAHDEDLTLQ-AZKQZHLXSA-N (1S,2S,4R,8S,9S,11S,12R,13S,19S)-6-[(3-chlorophenyl)methyl]-12,19-difluoro-11-hydroxy-8-(2-hydroxyacetyl)-9,13-dimethyl-6-azapentacyclo[10.8.0.02,9.04,8.013,18]icosa-14,17-dien-16-one Chemical compound C([C@@H]1C[C@H]2[C@H]3[C@]([C@]4(C=CC(=O)C=C4[C@@H](F)C3)C)(F)[C@@H](O)C[C@@]2([C@@]1(C1)C(=O)CO)C)N1CC1=CC=CC(Cl)=C1 AOSZTAHDEDLTLQ-AZKQZHLXSA-N 0.000 claims 1
- GLGNXYJARSMNGJ-VKTIVEEGSA-N (1s,2s,3r,4r)-3-[[5-chloro-2-[(1-ethyl-6-methoxy-2-oxo-4,5-dihydro-3h-1-benzazepin-7-yl)amino]pyrimidin-4-yl]amino]bicyclo[2.2.1]hept-5-ene-2-carboxamide Chemical compound CCN1C(=O)CCCC2=C(OC)C(NC=3N=C(C(=CN=3)Cl)N[C@H]3[C@H]([C@@]4([H])C[C@@]3(C=C4)[H])C(N)=O)=CC=C21 GLGNXYJARSMNGJ-VKTIVEEGSA-N 0.000 claims 1
- SZUVGFMDDVSKSI-WIFOCOSTSA-N (1s,2s,3s,5r)-1-(carboxymethyl)-3,5-bis[(4-phenoxyphenyl)methyl-propylcarbamoyl]cyclopentane-1,2-dicarboxylic acid Chemical compound O=C([C@@H]1[C@@H]([C@](CC(O)=O)([C@H](C(=O)N(CCC)CC=2C=CC(OC=3C=CC=CC=3)=CC=2)C1)C(O)=O)C(O)=O)N(CCC)CC(C=C1)=CC=C1OC1=CC=CC=C1 SZUVGFMDDVSKSI-WIFOCOSTSA-N 0.000 claims 1
- WWTBZEKOSBFBEM-SPWPXUSOSA-N (2s)-2-[[2-benzyl-3-[hydroxy-[(1r)-2-phenyl-1-(phenylmethoxycarbonylamino)ethyl]phosphoryl]propanoyl]amino]-3-(1h-indol-3-yl)propanoic acid Chemical compound N([C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)O)C(=O)C(CP(O)(=O)[C@H](CC=1C=CC=CC=1)NC(=O)OCC=1C=CC=CC=1)CC1=CC=CC=C1 WWTBZEKOSBFBEM-SPWPXUSOSA-N 0.000 claims 1
- IWZSHWBGHQBIML-ZGGLMWTQSA-N (3S,8S,10R,13S,14S,17S)-17-isoquinolin-7-yl-N,N,10,13-tetramethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-amine Chemical compound CN(C)[C@H]1CC[C@]2(C)C3CC[C@@]4(C)[C@@H](CC[C@@H]4c4ccc5ccncc5c4)[C@@H]3CC=C2C1 IWZSHWBGHQBIML-ZGGLMWTQSA-N 0.000 claims 1
- ONBQEOIKXPHGMB-VBSBHUPXSA-N 1-[2-[(2s,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]oxy-4,6-dihydroxyphenyl]-3-(4-hydroxyphenyl)propan-1-one Chemical compound O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1OC1=CC(O)=CC(O)=C1C(=O)CCC1=CC=C(O)C=C1 ONBQEOIKXPHGMB-VBSBHUPXSA-N 0.000 claims 1
- UNILWMWFPHPYOR-KXEYIPSPSA-M 1-[6-[2-[3-[3-[3-[2-[2-[3-[[2-[2-[[(2r)-1-[[2-[[(2r)-1-[3-[2-[2-[3-[[2-(2-amino-2-oxoethoxy)acetyl]amino]propoxy]ethoxy]ethoxy]propylamino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-[(2r)-2,3-di(hexadecanoyloxy)propyl]sulfanyl-1-oxopropan-2-yl Chemical compound O=C1C(SCCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CSC[C@@H](COC(=O)CCCCCCCCCCCCCCC)OC(=O)CCCCCCCCCCCCCCC)C(=O)NCC(=O)N[C@H](CO)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O)CC(=O)N1CCNC(=O)CCCCCN\1C2=CC=C(S([O-])(=O)=O)C=C2CC/1=C/C=C/C=C/C1=[N+](CC)C2=CC=C(S([O-])(=O)=O)C=C2C1 UNILWMWFPHPYOR-KXEYIPSPSA-M 0.000 claims 1
- KCBAMQOKOLXLOX-BSZYMOERSA-N CC1=C(SC=N1)C2=CC=C(C=C2)[C@H](C)NC(=O)[C@@H]3C[C@H](CN3C(=O)[C@H](C(C)(C)C)NC(=O)CCCCCCCCCCNCCCONC(=O)C4=C(C(=C(C=C4)F)F)NC5=C(C=C(C=C5)I)F)O Chemical compound CC1=C(SC=N1)C2=CC=C(C=C2)[C@H](C)NC(=O)[C@@H]3C[C@H](CN3C(=O)[C@H](C(C)(C)C)NC(=O)CCCCCCCCCCNCCCONC(=O)C4=C(C(=C(C=C4)F)F)NC5=C(C=C(C=C5)I)F)O KCBAMQOKOLXLOX-BSZYMOERSA-N 0.000 claims 1
- 229940126657 Compound 17 Drugs 0.000 claims 1
- OPFJDXRVMFKJJO-ZHHKINOHSA-N N-{[3-(2-benzamido-4-methyl-1,3-thiazol-5-yl)-pyrazol-5-yl]carbonyl}-G-dR-G-dD-dD-dD-NH2 Chemical compound S1C(C=2NN=C(C=2)C(=O)NCC(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(=O)N[C@H](CC(O)=O)C(=O)N[C@H](CC(O)=O)C(=O)N[C@H](CC(O)=O)C(N)=O)=C(C)N=C1NC(=O)C1=CC=CC=C1 OPFJDXRVMFKJJO-ZHHKINOHSA-N 0.000 claims 1
- LNUFLCYMSVYYNW-ZPJMAFJPSA-N [(2r,3r,4s,5r,6r)-2-[(2r,3r,4s,5r,6r)-6-[(2r,3r,4s,5r,6r)-6-[(2r,3r,4s,5r,6r)-6-[[(3s,5s,8r,9s,10s,13r,14s,17r)-10,13-dimethyl-17-[(2r)-6-methylheptan-2-yl]-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-3-yl]oxy]-4,5-disulfo Chemical compound O([C@@H]1[C@@H](COS(O)(=O)=O)O[C@@H]([C@@H]([C@H]1OS(O)(=O)=O)OS(O)(=O)=O)O[C@@H]1[C@@H](COS(O)(=O)=O)O[C@@H]([C@@H]([C@H]1OS(O)(=O)=O)OS(O)(=O)=O)O[C@@H]1[C@@H](COS(O)(=O)=O)O[C@H]([C@@H]([C@H]1OS(O)(=O)=O)OS(O)(=O)=O)O[C@@H]1C[C@@H]2CC[C@H]3[C@@H]4CC[C@@H]([C@]4(CC[C@@H]3[C@@]2(C)CC1)C)[C@H](C)CCCC(C)C)[C@H]1O[C@H](COS(O)(=O)=O)[C@@H](OS(O)(=O)=O)[C@H](OS(O)(=O)=O)[C@H]1OS(O)(=O)=O LNUFLCYMSVYYNW-ZPJMAFJPSA-N 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- XRWSZZJLZRKHHD-WVWIJVSJSA-N asunaprevir Chemical compound O=C([C@@H]1C[C@H](CN1C(=O)[C@@H](NC(=O)OC(C)(C)C)C(C)(C)C)OC1=NC=C(C2=CC=C(Cl)C=C21)OC)N[C@]1(C(=O)NS(=O)(=O)C2CC2)C[C@H]1C=C XRWSZZJLZRKHHD-WVWIJVSJSA-N 0.000 claims 1
- 210000000227 basophil cell of anterior lobe of hypophysis Anatomy 0.000 claims 1
- 229940126543 compound 14 Drugs 0.000 claims 1
- 229940125758 compound 15 Drugs 0.000 claims 1
- 229940126142 compound 16 Drugs 0.000 claims 1
- 229940125810 compound 20 Drugs 0.000 claims 1
- 229940126086 compound 21 Drugs 0.000 claims 1
- 229940126208 compound 22 Drugs 0.000 claims 1
- 229940125833 compound 23 Drugs 0.000 claims 1
- 229940125961 compound 24 Drugs 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 208000010706 fatty liver disease Diseases 0.000 claims 1
- JAXFJECJQZDFJS-XHEPKHHKSA-N gtpl8555 Chemical compound OC(=O)C[C@H](N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@H](B1O[C@@]2(C)[C@H]3C[C@H](C3(C)C)C[C@H]2O1)CCC1=CC=C(F)C=C1 JAXFJECJQZDFJS-XHEPKHHKSA-N 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 231100000240 steatosis hepatitis Toxicity 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000004434 sulfur atom Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14199935 | 2014-12-23 | ||
| EP14199935.9 | 2014-12-23 | ||
| PCT/EP2015/080969 WO2016102562A1 (en) | 2014-12-23 | 2015-12-22 | Fgf21 derivatives and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018505146A JP2018505146A (ja) | 2018-02-22 |
| JP2018505146A5 true JP2018505146A5 (2) | 2018-11-29 |
| JP6727210B2 JP6727210B2 (ja) | 2020-07-22 |
Family
ID=52130150
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017533789A Active JP6727210B2 (ja) | 2014-12-23 | 2015-12-22 | Ｆｇｆ２１誘導体及びその使用 |
Country Status (24)
| Country | Link |
|---|---|
| US (3) | US9744213B2 (2) |
| EP (1) | EP3236991B1 (2) |
| JP (1) | JP6727210B2 (2) |
| KR (1) | KR102427527B1 (2) |
| CN (1) | CN107108709B (2) |
| AR (1) | AR103246A1 (2) |
| AU (1) | AU2015371056B2 (2) |
| DK (1) | DK3236991T3 (2) |
| ES (1) | ES2742503T3 (2) |
| HK (1) | HK1246156B (2) |
| HR (1) | HRP20191292T1 (2) |
| HU (1) | HUE044783T2 (2) |
| IL (1) | IL252438B (2) |
| MX (1) | MX377044B (2) |
| MY (1) | MY181181A (2) |
| PL (1) | PL3236991T3 (2) |
| PT (1) | PT3236991T (2) |
| RS (1) | RS59154B1 (2) |
| RU (1) | RU2729011C2 (2) |
| SA (1) | SA517381673B1 (2) |
| SI (1) | SI3236991T1 (2) |
| TW (2) | TWI681966B (2) |
| WO (1) | WO2016102562A1 (2) |
| ZA (1) | ZA201703768B (2) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102433503B1 (ko) | 2016-05-24 | 2022-08-18 | 노보 노르디스크 에이/에스 | Mic-1 화합물 및 이것의 사용 |
| CN106421753A (zh) * | 2016-10-19 | 2017-02-22 | 哈尔滨医科大学 | 重组人成纤维细胞生长因子‑21在制备预防和治疗缺血性心律失常药物中的应用 |
| TWI710377B (zh) * | 2017-05-23 | 2020-11-21 | 丹麥商諾佛 儂迪克股份有限公司 | Ｍｉｃ－１化合物及其用途 |
| IL272987B (en) | 2017-09-04 | 2022-08-01 | 89Bio Ltd | fgf-21 mutant peptide conjugates and uses thereof |
| KR20210027426A (ko) | 2018-07-03 | 2021-03-10 | 브리스톨-마이어스 스큅 컴퍼니 | Fgf21 제제 |
| US11427623B1 (en) | 2019-05-28 | 2022-08-30 | 89Bio Ltd. | Methods of treatment using mutant FGF-21 peptide conjugates |
| CN113728013B (zh) | 2020-01-11 | 2022-06-14 | 北京质肽生物医药科技有限公司 | Glp-1和fgf21的融合蛋白的缀合物 |
| WO2022238510A1 (en) | 2021-05-11 | 2022-11-17 | Cytoki Pharma Aps | Therapeutic derivatives of interleukin-22 |
| EP4089108A1 (en) | 2021-05-11 | 2022-11-16 | CytoKi Pharma ApS | Therapeutic derivatives of interleukin-22 |
| KR102631925B1 (ko) * | 2021-06-10 | 2024-02-01 | 토드제약 주식회사 | 신규 fgf21 변이체 개발 및 이의 생산기법과 용도 |
| WO2023284822A1 (en) | 2021-07-14 | 2023-01-19 | Beijing Ql Biopharmaceutical Co., Ltd. | Fusion polypeptides for metabolic disorders |
| WO2023035817A1 (zh) * | 2021-09-08 | 2023-03-16 | 北京志道生物科技有限公司 | 一种fgf21突变蛋白及其应用 |
| IL317317A (en) | 2022-07-08 | 2025-01-01 | Novo Nordisk As | Highly potent ISVD compounds capable of replacing FVIII(A) |
| US12098400B2 (en) | 2022-07-08 | 2024-09-24 | Novo Nordisk A/S | Highly potent ISVD compounds capable of substituting for FVIII(A) |
| KR20250167609A (ko) | 2023-03-30 | 2025-12-01 | 노보 노르디스크 에이/에스 | 융합 화합물 및 그 용도 |
| JP7823234B2 (ja) * | 2023-05-12 | 2026-03-03 | ノヴォ ノルディスク アー／エス | 長時間作用型成長ホルモン受容体拮抗薬およびその使用 |
| WO2025056575A1 (en) | 2023-09-11 | 2025-03-20 | Novo Nordisk A/S | Anti il-6 domain antibodies |
| CN118307684B (zh) * | 2024-06-11 | 2024-10-18 | 北京志道生物科技有限公司 | 一种经脂肪酸链修饰的glp-1-fgf21融合蛋白及其制备方法和应用 |
| WO2026012311A1 (zh) * | 2024-07-08 | 2026-01-15 | 浙江道尔生物科技有限公司 | Fgf21衍生物及其用途 |
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| US5424286A (en) | 1993-05-24 | 1995-06-13 | Eng; John | Exendin-3 and exendin-4 polypeptides, and pharmaceutical compositions comprising same |
| IL128332A0 (en) | 1996-08-30 | 2000-01-31 | Novo Nordisk As | GLP-1 derivatives |
| US20040259780A1 (en) | 2001-07-30 | 2004-12-23 | Glasebrook Andrew Lawrence | Method for treating diabetes and obesity |
| EP1329227A1 (en) | 2002-01-22 | 2003-07-23 | Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts | Diagnostic conjugate useful for intercellular imaging and for differentiating between tumor- and non-tumor cells |
| DK1641823T3 (da) | 2003-06-12 | 2011-12-12 | Lilly Co Eli | GLP-1-analog fusionsproteiner |
| EP1667724A2 (en) | 2003-09-19 | 2006-06-14 | Novo Nordisk A/S | Albumin-binding derivatives of therapeutic peptides |
| BR122019021416A2 (2) | 2003-09-19 | 2019-12-21 | ||
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| EP1696962A2 (en) | 2003-12-18 | 2006-09-06 | Novo Nordisk A/S | Novel glp-1 analogues linked to albumin-like agents |
| JP2007531715A (ja) | 2004-03-17 | 2007-11-08 | イーライ リリー アンド カンパニー | グリコール結合ｆｇｆ−２１化合物 |
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| GB0412181D0 (en) | 2004-06-01 | 2004-06-30 | Celltech R&D Ltd | Biological products |
| CA2572770A1 (en) * | 2004-07-08 | 2006-01-19 | Novo-Nordisk A/S | Polypeptide protracting tags comprising a tetrazole moiety |
| KR100854198B1 (ko) | 2004-09-02 | 2008-08-26 | 일라이 릴리 앤드 캄파니 | 섬유아세포 성장 인자 21의 뮤테인 |
| US7622445B2 (en) | 2004-09-02 | 2009-11-24 | Eli Lilly And Company | Muteins of fibroblast growth factor 21 |
| WO2006050247A2 (en) | 2004-10-29 | 2006-05-11 | Neose Technologies, Inc. | Remodeling and glycopegylation of fibroblast growth factor (fgf) |
| US7655627B2 (en) | 2004-12-14 | 2010-02-02 | Eli Lilly And Company | Muteins of fibroblast growth factor 21 |
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| US20100022446A1 (en) | 2007-01-18 | 2010-01-28 | Novo Nordisk A/S | Use of Peptides in Combination with Surgical Intervention for the Treatment of Obesity |
| SI2068909T1 (sl) | 2007-03-30 | 2012-09-28 | Ambrx Inc | Modificirani fgf-21 polipeptidi in njihova uporaba |
| CN107501407B (zh) | 2007-03-30 | 2022-03-18 | Ambrx公司 | 经修饰fgf-21多肽和其用途 |
| US20110034373A1 (en) | 2007-08-03 | 2011-02-10 | Eli Lilly And Company | Use of an fgf-21 compound and a glp-1 compound for the treatment of obesity |
| WO2009030771A1 (en) | 2007-09-05 | 2009-03-12 | Novo Nordisk A/S | Peptides derivatized with a-b-c-d- and their therapeutical use |
| US20100317057A1 (en) | 2007-12-28 | 2010-12-16 | Novo Nordisk A/S | Semi-recombinant preparation of glp-1 analogues |
| CN100587073C (zh) | 2008-03-24 | 2010-02-03 | 吉林农大生物反应器工程有限公司 | 人成纤维细胞生长因子-21的重组表达 |
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| US20120035099A1 (en) * | 2009-06-11 | 2012-02-09 | Novo Nordisk A/S | Fgf21 analogues and derivatives |
| CN103415300B (zh) * | 2010-07-20 | 2018-02-23 | 诺沃—诺迪斯克有限公司 | N‑末端修饰的fgf21化合物 |
| MX2014002260A (es) * | 2011-08-31 | 2014-08-18 | Amgen Inc | Factor de crecimiento de fibroblasto 21 para usar en el tratamiento de diabetes tipo 1. |
| JP2015533483A (ja) * | 2012-09-07 | 2015-11-26 | サノフイ | メタボリックシンドロームを治療するための融合タンパク質 |
| ES2915851T3 (es) * | 2012-12-27 | 2022-06-27 | Ngm Biopharmaceuticals Inc | Péptidos quiméricos de FGF19 para usar en el tratamiento de trastornos de ácidos biliares |
-
2015
- 2015-12-22 AR ARP150104256A patent/AR103246A1/es active IP Right Grant
- 2015-12-22 TW TW104143111A patent/TWI681966B/zh active
- 2015-12-22 ES ES15817847T patent/ES2742503T3/es active Active
- 2015-12-22 WO PCT/EP2015/080969 patent/WO2016102562A1/en not_active Ceased
- 2015-12-22 EP EP15817847.5A patent/EP3236991B1/en active Active
- 2015-12-22 RS RSP20191106 patent/RS59154B1/sr unknown
- 2015-12-22 PT PT15817847T patent/PT3236991T/pt unknown
- 2015-12-22 MY MYPI2017701848A patent/MY181181A/en unknown
- 2015-12-22 DK DK15817847.5T patent/DK3236991T3/da active
- 2015-12-22 CN CN201580069436.9A patent/CN107108709B/zh active Active
- 2015-12-22 HK HK18105587.8A patent/HK1246156B/en unknown
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