JP2014516993A5 - - Google Patents
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- Publication number
- JP2014516993A5 JP2014516993A5 JP2014513790A JP2014513790A JP2014516993A5 JP 2014516993 A5 JP2014516993 A5 JP 2014516993A5 JP 2014513790 A JP2014513790 A JP 2014513790A JP 2014513790 A JP2014513790 A JP 2014513790A JP 2014516993 A5 JP2014516993 A5 JP 2014516993A5
- Authority
- JP
- Japan
- Prior art keywords
- peg
- conjugate
- fmoc
- mal
- fms
- 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
- 239000002202 Polyethylene glycol Substances 0.000 claims 30
- 229920001223 polyethylene glycol Polymers 0.000 claims 30
- 101800001388 Oxyntomodulin Proteins 0.000 claims 29
- 102400000319 Oxyntomodulin Human genes 0.000 claims 29
- 108010086246 Glucagon-Like Peptide-1 Receptor Proteins 0.000 claims 22
- 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 22
- 102100040918 Pro-glucagon Human genes 0.000 claims 22
- 230000009977 dual effect Effects 0.000 claims 22
- 229940123232 Glucagon receptor agonist Drugs 0.000 claims 20
- PXZWGQLGAKCNKD-DPNMSELWSA-N molport-023-276-326 Chemical group 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(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(O)=O)[C@@H](C)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 PXZWGQLGAKCNKD-DPNMSELWSA-N 0.000 claims 19
- 125000005647 linker group Chemical group 0.000 claims 17
- 239000008177 pharmaceutical agent Substances 0.000 claims 9
- 125000003088 (fluoren-9-ylmethoxy)carbonyl group Chemical group 0.000 claims 7
- -1 9-fluorenylmethoxycarbonyl (Fmoc) Chemical class 0.000 claims 7
- 125000003277 amino group Chemical group 0.000 claims 7
- 238000000034 method Methods 0.000 claims 7
- JLPNPVIABCLANH-UHFFFAOYSA-N 9-[(2,5-dioxopyrrolidin-1-yl)oxycarbonyloxymethyl]-7-[3-(2,5-dioxopyrrol-1-yl)propanoylamino]-9h-fluorene-2-sulfonic acid Chemical compound C=1C(S(=O)(=O)O)=CC=C(C2=CC=C(NC(=O)CCN3C(C=CC3=O)=O)C=C22)C=1C2COC(=O)ON1C(=O)CCC1=O JLPNPVIABCLANH-UHFFFAOYSA-N 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 4
- 101500028776 Homo sapiens Oxyntomodulin Proteins 0.000 claims 3
- 125000003983 fluorenyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3CC12)* 0.000 claims 3
- 108010063919 Glucagon Receptors Proteins 0.000 claims 2
- 102100040890 Glucagon receptor Human genes 0.000 claims 2
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 206010022489 Insulin Resistance Diseases 0.000 claims 2
- 239000000556 agonist Substances 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 150000001412 amines Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 230000008878 coupling Effects 0.000 claims 2
- 238000010168 coupling process Methods 0.000 claims 2
- 238000005859 coupling reaction Methods 0.000 claims 2
- 239000008103 glucose Substances 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 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 2
- 239000000376 reactant Substances 0.000 claims 2
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000002877 alkyl aryl group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000003275 alpha amino acid group Chemical group 0.000 claims 1
- 125000000539 amino acid group Chemical group 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 230000004071 biological effect Effects 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 230000037396 body weight Effects 0.000 claims 1
- 150000001720 carbohydrates Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000037406 food intake Effects 0.000 claims 1
- 235000012631 food intake Nutrition 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 238000005580 one pot reaction Methods 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims 1
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 108090000765 processed proteins & peptides Proteins 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161492448P | 2011-06-02 | 2011-06-02 | |
| US61/492,448 | 2011-06-02 | ||
| US201261624589P | 2012-04-16 | 2012-04-16 | |
| US61/624,589 | 2012-04-16 | ||
| PCT/US2012/040744 WO2012167251A1 (en) | 2011-06-02 | 2012-06-04 | Long-acting glp-1/glucagon receptor agonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014516993A JP2014516993A (ja) | 2014-07-17 |
| JP2014516993A5 true JP2014516993A5 (OSRAM) | 2015-07-23 |
| JP6182134B2 JP6182134B2 (ja) | 2017-08-16 |
Family
ID=47259955
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014513790A Active JP6182134B2 (ja) | 2011-06-02 | 2012-06-04 | 長時間作用型ｇｌｐ−１／グルカゴン受容体アゴニスト |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US20140349922A1 (OSRAM) |
| EP (1) | EP2714070B1 (OSRAM) |
| JP (1) | JP6182134B2 (OSRAM) |
| KR (1) | KR102092206B1 (OSRAM) |
| CN (1) | CN104023739A (OSRAM) |
| AU (1) | AU2012261869B2 (OSRAM) |
| BR (1) | BR112013030933A2 (OSRAM) |
| CA (1) | CA2837710C (OSRAM) |
| CL (1) | CL2013003450A1 (OSRAM) |
| CO (1) | CO6980619A2 (OSRAM) |
| EA (1) | EA201391764A1 (OSRAM) |
| ES (1) | ES2981891T3 (OSRAM) |
| HK (1) | HK1201478A1 (OSRAM) |
| IL (1) | IL229732B (OSRAM) |
| MX (2) | MX346957B (OSRAM) |
| SG (1) | SG10201606243YA (OSRAM) |
| WO (1) | WO2012167251A1 (OSRAM) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10351615B2 (en) | 2006-02-03 | 2019-07-16 | Opko Biologics Ltd. | Methods of treatment with long-acting growth hormone |
| US20150038413A1 (en) | 2006-02-03 | 2015-02-05 | Opko Biologics Ltd. | Long-acting polypeptides and methods of producing and administering same |
| US10221228B2 (en) | 2006-02-03 | 2019-03-05 | Opko Biologics Ltd. | Long-acting polypeptides and methods of producing and administering same |
| US20140113860A1 (en) | 2006-02-03 | 2014-04-24 | Prolor Biotech Ltd. | Long-acting polypeptides and methods of producing and administering same |
| US9458444B2 (en) | 2006-02-03 | 2016-10-04 | Opko Biologics Ltd. | Long-acting coagulation factors and methods of producing same |
| US8946155B2 (en) | 2006-02-03 | 2015-02-03 | Opko Biologics Ltd. | Long-acting polypeptides and methods of producing and administering same |
| US9249407B2 (en) | 2006-02-03 | 2016-02-02 | Opko Biologics Ltd. | Long-acting coagulation factors and methods of producing same |
| US8048849B2 (en) | 2006-02-03 | 2011-11-01 | Modigene, Inc. | Long-acting polypeptides and methods of producing same |
| US9663778B2 (en) | 2009-07-09 | 2017-05-30 | OPKO Biologies Ltd. | Long-acting coagulation factors and methods of producing same |
| US12203113B2 (en) | 2009-07-09 | 2025-01-21 | Opko Biologics Ltd. | Long-acting coagulation factors and methods of producing same |
| US10166295B2 (en) | 2011-06-02 | 2019-01-01 | Opko Biologics Ltd. | Pegylated OXM variants |
| SG11201406671RA (en) | 2012-04-19 | 2014-11-27 | Opko Biolog Ltd | Long-acting oxyntomodulin variants and methods of producing same |
| PE20150181A1 (es) | 2012-06-04 | 2015-02-28 | Opko Biolog Ltd | Variantes de oxm pegilada |
| CN112661863A (zh) | 2012-11-20 | 2021-04-16 | 奥普科生物制品有限公司 | 通过连接至促性腺激素羧基端肽来增加多肽的流体动力学体积的方法 |
| US20150158926A1 (en) | 2013-10-21 | 2015-06-11 | Opko Biologics, Ltd. | Long-acting polypeptides and methods of producing and administering same |
| PE20161153A1 (es) | 2014-01-20 | 2016-10-27 | Hanmi Pharm Ind Co Ltd | Insulina de accion prolongada y uso de la misma |
| AR100639A1 (es) | 2014-05-29 | 2016-10-19 | Hanmi Pharm Ind Co Ltd | Composición para tratar diabetes que comprende conjugados de análogos de insulina de acción prolongada y conjugados de péptidos insulinotrópicos de acción prolongada |
| TWI684458B (zh) * | 2014-05-30 | 2020-02-11 | 南韓商韓美藥品股份有限公司 | 包含胰島素及ｇｌｐ-１/昇糖素雙重促效劑之治療糖尿病之組成物 |
| TWI746427B (zh) | 2014-12-10 | 2021-11-21 | 以色列商歐科生物製品有限公司 | 製造長效ｃｔｐ修飾的多肽之方法 |
| KR20180014754A (ko) * | 2015-05-29 | 2018-02-09 | 옵코 바이오로직스 리미티드 | 페길화된 옥신토모둘린 변이체 |
| EP3310347B1 (en) | 2015-06-19 | 2021-08-04 | OPKO Biologics Ltd. | Long-acting coagulation factors and methods of producing same |
| AR105284A1 (es) * | 2015-07-10 | 2017-09-20 | Sanofi Sa | Derivados de exendina-4 como agonistas peptídicos duales específicos de los receptores de glp-1 / glucagón |
| UY36870A (es) | 2015-08-28 | 2017-03-31 | Hanmi Pharm Ind Co Ltd | Análogos de insulina novedosos |
| EP3368693A4 (en) * | 2015-10-30 | 2019-03-27 | The Research Foundation For The State University Of New York University at Buffalo | OXYNTOMODULINANALOGA AND METHOD FOR THE PRODUCTION AND USE THEREOF |
| CN106938050B (zh) * | 2015-12-29 | 2021-08-24 | 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 |
| EP3468610A1 (en) * | 2016-06-09 | 2019-04-17 | OPKO Biologics Ltd. | Long-acting oxyntomodulin formulation and methods of producing and administering same |
| ES2963725T3 (es) | 2016-07-11 | 2024-04-01 | Opko Biologics Ltd | Factor VII de coagulación de acción prolongada y métodos para producir el mismo |
| RU2764197C1 (ru) | 2016-09-23 | 2022-01-14 | Ханми Фарм. Ко., Лтд. | Аналоги инсулина с пониженной аффинностью к рецептору инсулина и их применение |
| WO2018174668A2 (ko) | 2017-03-23 | 2018-09-27 | 한미약품 주식회사 | 인슐린 수용체와의 결합력이 감소된 인슐린 아날로그의 결합체 및 이의 용도 |
| EP3713993B1 (en) | 2017-11-23 | 2024-07-10 | Sentigel Ab | Hydrogel composition and its uses |
| US12441776B2 (en) | 2018-11-30 | 2025-10-14 | Eirgen Pharma Ltd. | Oxyntomodulin peptide analog formulations |
| US20200254065A1 (en) | 2019-02-11 | 2020-08-13 | Opko Biologics Ltd. | Long-acting glp-2 analogs |
| 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 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL119029A0 (en) | 1996-08-07 | 1996-11-14 | Yeda Res & Dev | Long-acting drugs and pharamaceutical compositions comprising them |
| PL1620118T3 (pl) | 2003-04-08 | 2014-11-28 | Yeda Res & Dev | Leki odwracalnie pegylowane |
| WO2007100535A2 (en) * | 2006-02-22 | 2007-09-07 | Merck & Co., Inc. | Oxyntomodulin derivatives |
| EP2898900B1 (en) * | 2008-09-19 | 2017-11-15 | Nektar Therapeutics | Polymer conjugates of ziconotide |
| DK2408800T3 (en) * | 2009-03-20 | 2016-08-29 | Hanmi Science Co Ltd | A process for the preparation of a site-specific conjugate of a physiologically active polypeptide |
| AR079344A1 (es) * | 2009-12-22 | 2012-01-18 | Lilly Co Eli | Analogo peptidico de oxintomodulina, composicion farmaceutica que lo comprende y uso para preparar un medicamento util para tratar diabetes no insulinodependiente y/u obesidad |
-
2012
- 2012-06-04 US US14/123,106 patent/US20140349922A1/en active Pending
- 2012-06-04 JP JP2014513790A patent/JP6182134B2/ja active Active
- 2012-06-04 CA CA2837710A patent/CA2837710C/en active Active
- 2012-06-04 MX MX2013014069A patent/MX346957B/es active IP Right Grant
- 2012-06-04 EP EP12793107.9A patent/EP2714070B1/en active Active
- 2012-06-04 KR KR1020137035156A patent/KR102092206B1/ko active Active
- 2012-06-04 HK HK15102153.2A patent/HK1201478A1/xx unknown
- 2012-06-04 ES ES12793107T patent/ES2981891T3/es active Active
- 2012-06-04 CN CN201280038726.3A patent/CN104023739A/zh active Pending
- 2012-06-04 MX MX2015011960A patent/MX386803B/es unknown
- 2012-06-04 SG SG10201606243YA patent/SG10201606243YA/en unknown
- 2012-06-04 EA EA201391764A patent/EA201391764A1/ru unknown
- 2012-06-04 WO PCT/US2012/040744 patent/WO2012167251A1/en not_active Ceased
- 2012-06-04 AU AU2012261869A patent/AU2012261869B2/en active Active
- 2012-06-04 BR BR112013030933A patent/BR112013030933A2/pt not_active IP Right Cessation
-
2013
- 2013-11-28 IL IL229732A patent/IL229732B/en unknown
- 2013-12-02 CL CL2013003450A patent/CL2013003450A1/es unknown
- 2013-12-27 CO CO13301132A patent/CO6980619A2/es unknown
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