JP2016512213A5 - - Google Patents
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- Publication number
- JP2016512213A5 JP2016512213A5 JP2015562166A JP2015562166A JP2016512213A5 JP 2016512213 A5 JP2016512213 A5 JP 2016512213A5 JP 2015562166 A JP2015562166 A JP 2015562166A JP 2015562166 A JP2015562166 A JP 2015562166A JP 2016512213 A5 JP2016512213 A5 JP 2016512213A5
- Authority
- JP
- Japan
- Prior art keywords
- less
- peptide
- peg
- receptor
- glp
- 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.)
- Pending
Links
- 108090000765 processed proteins & peptides Proteins 0.000 claims 50
- 238000000034 method Methods 0.000 claims 14
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 7
- 239000004472 Lysine Substances 0.000 claims 7
- 230000000694 effects Effects 0.000 claims 7
- FUOOLUPWFVMBKG-UHFFFAOYSA-N 2-Aminoisobutyric acid Chemical compound CC(C)(N)C(O)=O FUOOLUPWFVMBKG-UHFFFAOYSA-N 0.000 claims 6
- 108010063919 Glucagon Receptors Proteins 0.000 claims 6
- 102100040890 Glucagon receptor Human genes 0.000 claims 6
- 108010086246 Glucagon-Like Peptide-1 Receptor Proteins 0.000 claims 6
- 102100032882 Glucagon-like peptide 1 receptor Human genes 0.000 claims 6
- 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 5
- 150000001413 amino acids Chemical group 0.000 claims 5
- 102100040918 Pro-glucagon Human genes 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 101710198884 GATA-type zinc finger protein 1 Proteins 0.000 claims 3
- 102000051325 Glucagon Human genes 0.000 claims 3
- 108060003199 Glucagon Proteins 0.000 claims 3
- 102000008100 Human Serum Albumin Human genes 0.000 claims 3
- 108091006905 Human Serum Albumin Proteins 0.000 claims 3
- 239000000556 agonist Substances 0.000 claims 3
- 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 3
- 229960004666 glucagon Drugs 0.000 claims 3
- 125000003588 lysine group Chemical group [H]N([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])(N([H])[H])C(*)=O 0.000 claims 3
- 102000004196 processed proteins & peptides Human genes 0.000 claims 3
- YBJHBAHKTGYVGT-ZKWXMUAHSA-N (+)-Biotin Chemical compound N1C(=O)N[C@@H]2[C@H](CCCCC(=O)O)SC[C@@H]21 YBJHBAHKTGYVGT-ZKWXMUAHSA-N 0.000 claims 2
- 101001040075 Homo sapiens Glucagon receptor Proteins 0.000 claims 2
- 101001015516 Homo sapiens Glucagon-like peptide 1 receptor Proteins 0.000 claims 2
- 238000013262 cAMP assay Methods 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 238000002347 injection Methods 0.000 claims 2
- 239000007924 injection Substances 0.000 claims 2
- 239000003446 ligand Substances 0.000 claims 2
- 125000001312 palmitoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 229920001184 polypeptide Polymers 0.000 claims 2
- GUOSQNAUYHMCRU-UHFFFAOYSA-N 11-Aminoundecanoic acid Chemical group NCCCCCCCCCCC(O)=O GUOSQNAUYHMCRU-UHFFFAOYSA-N 0.000 claims 1
- KXSKAZFMTGADIV-UHFFFAOYSA-N 2-[3-(2-hydroxyethoxy)propoxy]ethanol Chemical compound OCCOCCCOCCO KXSKAZFMTGADIV-UHFFFAOYSA-N 0.000 claims 1
- SLXKOJJOQWFEFD-UHFFFAOYSA-N 6-aminohexanoic acid Chemical group NCCCCCC(O)=O SLXKOJJOQWFEFD-UHFFFAOYSA-N 0.000 claims 1
- 102000009027 Albumins Human genes 0.000 claims 1
- 108010088751 Albumins Proteins 0.000 claims 1
- 125000001433 C-terminal amino-acid group Chemical group 0.000 claims 1
- 102000004127 Cytokines Human genes 0.000 claims 1
- 108090000695 Cytokines Proteins 0.000 claims 1
- 102000004190 Enzymes Human genes 0.000 claims 1
- 108090000790 Enzymes Proteins 0.000 claims 1
- 108091016366 Histone-lysine N-methyltransferase EHMT1 Proteins 0.000 claims 1
- 101000693243 Homo sapiens Paternally-expressed gene 3 protein Proteins 0.000 claims 1
- 102100026120 IgG receptor FcRn large subunit p51 Human genes 0.000 claims 1
- 101710177940 IgG receptor FcRn large subunit p51 Proteins 0.000 claims 1
- 102000008394 Immunoglobulin Fragments Human genes 0.000 claims 1
- 108010021625 Immunoglobulin Fragments Proteins 0.000 claims 1
- 101001040082 Mus musculus Glucagon receptor Proteins 0.000 claims 1
- 101001015515 Mus musculus Glucagon-like peptide 1 receptor Proteins 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010033307 Overweight Diseases 0.000 claims 1
- 102100025757 Paternally-expressed gene 3 protein Human genes 0.000 claims 1
- 239000002202 Polyethylene glycol Substances 0.000 claims 1
- 229960002684 aminocaproic acid Drugs 0.000 claims 1
- 229960002685 biotin Drugs 0.000 claims 1
- 235000020958 biotin Nutrition 0.000 claims 1
- 239000011616 biotin Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229920000592 inorganic polymer Polymers 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 229920000620 organic polymer Polymers 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 229920001223 polyethylene glycol Polymers 0.000 claims 1
- 229920000642 polymer Polymers 0.000 claims 1
- 108020001580 protein domains Proteins 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 102000005962 receptors Human genes 0.000 claims 1
- 108020003175 receptors Proteins 0.000 claims 1
- 210000002966 serum Anatomy 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361783675P | 2013-03-14 | 2013-03-14 | |
| US61/783,675 | 2013-03-14 | ||
| PCT/EP2014/055034 WO2014140222A1 (en) | 2013-03-14 | 2014-03-13 | Pegylated glucagon and glp-1 co-agonists for the treatment of obesity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016512213A JP2016512213A (ja) | 2016-04-25 |
| JP2016512213A5 true JP2016512213A5 (https=) | 2017-04-13 |
Family
ID=50272654
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015562166A Pending JP2016512213A (ja) | 2013-03-14 | 2014-03-13 | 肥満の治療のためのペグ化グルカゴン及びｇｌｐ−１コアゴニスト |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US9714277B2 (https=) |
| EP (2) | EP2968581A1 (https=) |
| JP (1) | JP2016512213A (https=) |
| AU (1) | AU2014230472A1 (https=) |
| CA (1) | CA2902352A1 (https=) |
| HK (1) | HK1220383A1 (https=) |
| WO (1) | WO2014140222A1 (https=) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA116217C2 (uk) | 2012-10-09 | 2018-02-26 | Санофі | Пептидна сполука як подвійний агоніст рецепторів glp1-1 та глюкагону |
| AU2013366692B2 (en) | 2012-12-21 | 2017-11-23 | Sanofi | Dual GLP1/GIP or trigonal GLP1/GIP/Glucagon agonists |
| SI3004155T1 (sl) | 2013-05-28 | 2022-02-28 | Takeda Pharmaceutical Company Limited | Peptidna spojina |
| CN105829339B (zh) * | 2013-11-06 | 2021-03-12 | 西兰制药公司 | 胰高血糖素-glp-1-gip三重激动剂化合物 |
| WO2015086733A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Dual glp-1/glucagon receptor agonists |
| EP3080152A1 (en) | 2013-12-13 | 2016-10-19 | Sanofi | Non-acylated exendin-4 peptide analogues |
| EP3080154B1 (en) | 2013-12-13 | 2018-02-07 | Sanofi | Dual glp-1/gip receptor agonists |
| WO2015086728A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Exendin-4 peptide analogues as dual glp-1/gip receptor agonists |
| 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 |
| 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 |
| US9932381B2 (en) | 2014-06-18 | 2018-04-03 | Sanofi | Exendin-4 derivatives as selective glucagon receptor agonists |
| AR105319A1 (es) | 2015-06-05 | 2017-09-27 | Sanofi Sa | Profármacos que comprenden un conjugado agonista dual de glp-1 / glucagón conector ácido hialurónico |
| TWI726889B (zh) * | 2015-06-10 | 2021-05-11 | 英商梅迪繆思有限公司 | 蛋白酶抗性之脂化肽 |
| WO2016198624A1 (en) | 2015-06-12 | 2016-12-15 | Sanofi | Exendin-4 derivatives as trigonal glp-1/glucagon/gip receptor agonists |
| WO2016198628A1 (en) | 2015-06-12 | 2016-12-15 | Sanofi | Non-acylated exendin-4 derivatives as dual glp-1/glucagon receptor agonists |
| TW201706291A (zh) | 2015-07-10 | 2017-02-16 | 賽諾菲公司 | 作為選擇性肽雙重ｇｌｐ－１／升糖素受體促效劑之新毒蜥外泌肽（ｅｘｅｎｄｉｎ－４）衍生物 |
| JP6995042B2 (ja) * | 2016-05-24 | 2022-02-04 | 武田薬品工業株式会社 | ペプチド化合物 |
| RU2670983C1 (ru) * | 2017-10-11 | 2018-10-29 | Федеральное государственное бюджетное учреждение "Государственный научно-исследовательский институт генетики и селекции промышленных микроорганизмов Национального исследовательского центра "Курчатовский институт" (НИЦ "Курчатовский институт" - ГосНИИгенетика) | Применение полипептида, полученного на основе глюкагоноподобного пептида 1 человека, в качестве средства для контроля за весом тела |
| TWI770085B (zh) * | 2017-11-21 | 2022-07-11 | 日商武田藥品工業股份有限公司 | 胜肽化合物 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3572982D1 (en) | 1984-03-06 | 1989-10-19 | Takeda Chemical Industries Ltd | Chemically modified lymphokine and production thereof |
| WO1990006952A1 (fr) | 1988-12-22 | 1990-06-28 | Kirin-Amgen, Inc. | Facteur de stimulation de colonies de granulocytes modifies chimiquement |
| US6440175B1 (en) | 2001-06-28 | 2002-08-27 | Stanley, Iii Virgil E. | Hair coloring kit |
| JP2006501820A (ja) * | 2002-09-06 | 2006-01-19 | バイエル・フアーマシユーチカルズ・コーポレーシヨン | 修飾ｇｌｐ−１受容体アゴニストおよびそれらの薬理学的使用法 |
| US20090202497A1 (en) * | 2005-08-23 | 2009-08-13 | The General Hospital Corporation | Use of glp-1, glp-1 derivatives or glp-1 fragments for skin regeneration, stimulation of hair growth, or treatment of diabetes |
| SI2173890T1 (sl) | 2007-06-21 | 2011-06-30 | Univ Muenchen Tech | Biološko aktivni proteini, ki imajo povečano in vivo in/ali in vitro stabilnost |
| AR072160A1 (es) * | 2008-06-17 | 2010-08-11 | Univ Indiana Res & Tech Corp | Co-agonistas del receptor de glucagon/glp-1 |
| EP2443146B1 (en) * | 2009-06-16 | 2016-10-05 | Indiana University Research And Technology Corporation | Gip receptor-active glucagon compounds |
| AU2010272944B2 (en) * | 2009-07-13 | 2015-11-19 | Zealand Pharma A/S | Acylated glucagon analogues |
| MX2012013001A (es) | 2010-05-13 | 2013-02-26 | Univ Indiana Res & Tech Corp | Peptidos de la superfamilia de glucagon que presentan actividad del receptor nuclear de hormonas. |
| WO2012054822A1 (en) * | 2010-10-22 | 2012-04-26 | Nektar Therapeutics | Pharmacologically active polymer-glp-1 conjugates |
| US8507428B2 (en) * | 2010-12-22 | 2013-08-13 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting GIP receptor activity |
| WO2012150503A2 (en) * | 2011-05-03 | 2012-11-08 | Zealand Pharma A/S | Glu-glp-1 dual agonist signaling-selective compounds |
| KR20140043793A (ko) * | 2011-06-22 | 2014-04-10 | 인디애나 유니버시티 리서치 앤드 테크놀로지 코퍼레이션 | 글루카곤/glp-1 수용체 공동-작용물질 |
| TWI617574B (zh) * | 2012-12-11 | 2018-03-11 | 梅迪繆思有限公司 | 用於治療肥胖之升糖素與ｇｌｐ－１共促效劑 |
-
2014
- 2014-03-13 CA CA2902352A patent/CA2902352A1/en not_active Abandoned
- 2014-03-13 AU AU2014230472A patent/AU2014230472A1/en not_active Abandoned
- 2014-03-13 US US14/775,074 patent/US9714277B2/en not_active Expired - Fee Related
- 2014-03-13 WO PCT/EP2014/055034 patent/WO2014140222A1/en not_active Ceased
- 2014-03-13 EP EP14709713.3A patent/EP2968581A1/en not_active Withdrawn
- 2014-03-13 JP JP2015562166A patent/JP2016512213A/ja active Pending
- 2014-03-13 HK HK16108513.3A patent/HK1220383A1/zh unknown
- 2014-03-13 EP EP17174372.7A patent/EP3238734A1/en not_active Withdrawn
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