JP2014520798A5 - - Google Patents
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- Publication number
- JP2014520798A5 JP2014520798A5 JP2014518803A JP2014518803A JP2014520798A5 JP 2014520798 A5 JP2014520798 A5 JP 2014520798A5 JP 2014518803 A JP2014518803 A JP 2014518803A JP 2014518803 A JP2014518803 A JP 2014518803A JP 2014520798 A5 JP2014520798 A5 JP 2014520798A5
- Authority
- JP
- Japan
- Prior art keywords
- polyethylene glycol
- exendin
- composition
- derivative
- analog
- 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 description 53
- 229920001223 polyethylene glycol Polymers 0.000 claims description 53
- JUFFVKRROAPVBI-PVOYSMBESA-N chembl1210015 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=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](CCCCN)C(=O)N[C@@H](CC(=O)N[C@H]1[C@@H]([C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O)[C@@H](O)[C@@H](CO[C@]3(O[C@@H](C[C@H](O)[C@H](O)CO)[C@H](NC(C)=O)[C@@H](O)C3)C(O)=O)O2)O)[C@@H](CO)O1)NC(C)=O)C(=O)NCC(=O)NCC(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)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)CNC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 JUFFVKRROAPVBI-PVOYSMBESA-N 0.000 claims description 28
- 239000000203 mixture Substances 0.000 claims description 19
- 238000000034 method Methods 0.000 claims description 15
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 15
- PEEHTFAAVSWFBL-UHFFFAOYSA-N Maleimide Chemical compound O=C1NC(=O)C=C1 PEEHTFAAVSWFBL-UHFFFAOYSA-N 0.000 claims description 11
- 235000018417 cysteine Nutrition 0.000 claims description 11
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims description 11
- 150000002334 glycols Chemical class 0.000 claims description 9
- 239000013638 trimer Substances 0.000 claims description 9
- 108010011459 Exenatide Proteins 0.000 claims description 5
- 239000000539 dimer Substances 0.000 claims description 5
- 229960001519 exenatide Drugs 0.000 claims description 5
- LOKCTEFSRHRXRJ-UHFFFAOYSA-I dipotassium trisodium dihydrogen phosphate hydrogen phosphate dichloride Chemical compound P(=O)(O)(O)[O-].[K+].P(=O)(O)([O-])[O-].[Na+].[Na+].[Cl-].[K+].[Cl-].[Na+] LOKCTEFSRHRXRJ-UHFFFAOYSA-I 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 239000002953 phosphate buffered saline Substances 0.000 claims description 4
- AASBXERNXVFUEJ-UHFFFAOYSA-N (2,5-dioxopyrrolidin-1-yl) propanoate Chemical compound CCC(=O)ON1C(=O)CCC1=O AASBXERNXVFUEJ-UHFFFAOYSA-N 0.000 claims description 3
- NQTADLQHYWFPDB-UHFFFAOYSA-N N-Hydroxysuccinimide Chemical compound ON1C(=O)CCC1=O NQTADLQHYWFPDB-UHFFFAOYSA-N 0.000 claims description 3
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims description 3
- 210000004899 c-terminal region Anatomy 0.000 claims description 3
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 3
- 239000004480 active ingredient Substances 0.000 claims description 2
- 239000000243 solution Substances 0.000 claims description 2
- 125000006850 spacer group Chemical group 0.000 claims 7
- 235000001014 amino acid Nutrition 0.000 claims 3
- 150000001413 amino acids Chemical class 0.000 claims 3
- NBBJYMSMWIIQGU-UHFFFAOYSA-N Propionic aldehyde Chemical compound CCC=O NBBJYMSMWIIQGU-UHFFFAOYSA-N 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- ZTQSAGDEMFDKMZ-UHFFFAOYSA-N butyric aldehyde Natural products CCCC=O ZTQSAGDEMFDKMZ-UHFFFAOYSA-N 0.000 claims 1
- 239000000839 emulsion Substances 0.000 claims 1
- 239000008187 granular material Substances 0.000 claims 1
- 239000007902 hard capsule Substances 0.000 claims 1
- 238000002347 injection Methods 0.000 claims 1
- 239000007924 injection Substances 0.000 claims 1
- 125000005439 maleimidyl group Chemical group C1(C=CC(N1*)=O)=O 0.000 claims 1
- 239000008188 pellet Substances 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 239000007901 soft capsule Substances 0.000 claims 1
- 239000000725 suspension Substances 0.000 claims 1
- 239000006188 syrup Substances 0.000 claims 1
- 235000020357 syrup Nutrition 0.000 claims 1
- 239000003826 tablet Substances 0.000 claims 1
- 230000003442 weekly effect Effects 0.000 claims 1
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 description 6
- 102000004877 Insulin Human genes 0.000 description 3
- 108090001061 Insulin Proteins 0.000 description 3
- 201000010099 disease Diseases 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 229940125396 insulin Drugs 0.000 description 3
- 208000002249 Diabetes Complications Diseases 0.000 description 1
- 206010012655 Diabetic complications Diseases 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 230000006320 pegylation Effects 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR1020110062858A KR101357117B1 (ko) | 2011-06-28 | 2011-06-28 | 폴리에틸렌글라이콜 또는 이의 유도체로 페길화된 엑센딘-4 유사체, 이의 제조방법 및 이를 유효성분으로 함유하는 당뇨병 예방 또는 치료용 약학적 조성물 |
| KR10-2011-0062858 | 2011-06-28 | ||
| PCT/KR2012/005137 WO2013002580A2 (ko) | 2011-06-28 | 2012-06-28 | 폴리에틸렌글라이콜 또는 이의 유도체로 페길화된 엑센딘-4 유사체, 이의 제조방법 및 이를 유효성분으로 함유하는 당뇨병 예방 또는 치료용 약학적 조성물 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014520798A JP2014520798A (ja) | 2014-08-25 |
| JP2014520798A5 true JP2014520798A5 (cg-RX-API-DMAC7.html) | 2015-08-20 |
| JP6084215B2 JP6084215B2 (ja) | 2017-02-22 |
Family
ID=47424684
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014518803A Active JP6084215B2 (ja) | 2011-06-28 | 2012-06-28 | ポリエチレングリコールまたはその誘導体でｐｅｇ化されたエキセンジン−４類似体、その調製法、および活性成分としてこれを含有する、糖尿病を予防または処置するための薬学的組成物 |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US20130217622A1 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2727605B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP6084215B2 (cg-RX-API-DMAC7.html) |
| KR (1) | KR101357117B1 (cg-RX-API-DMAC7.html) |
| CN (1) | CN103338790B (cg-RX-API-DMAC7.html) |
| AU (1) | AU2012276478B2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2839410C (cg-RX-API-DMAC7.html) |
| DK (1) | DK2727605T3 (cg-RX-API-DMAC7.html) |
| ES (1) | ES2674581T3 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2013002580A2 (cg-RX-API-DMAC7.html) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112142855A (zh) | 2012-05-18 | 2020-12-29 | 爱德迪安（北京）生物技术有限公司 | 用于糖尿病治疗的蛋白、蛋白缀合物及其应用 |
| UA116217C2 (uk) | 2012-10-09 | 2018-02-26 | Санофі | Пептидна сполука як подвійний агоніст рецепторів glp1-1 та глюкагону |
| CA2895875A1 (en) | 2012-12-21 | 2014-06-26 | Sanofi | Exendin-4 derivatives |
| AU2014359894B2 (en) | 2013-12-06 | 2020-09-17 | Baikang (Suzhou) Co., Ltd | Bioreversable promoieties for nitrogen-containing and hydroxyl-containing drugs |
| EP3080150B1 (en) | 2013-12-13 | 2018-08-01 | Sanofi | Exendin-4 peptide analogues as dual glp-1/gip receptor agonists |
| WO2015086733A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Dual glp-1/glucagon receptor agonists |
| WO2015086730A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Non-acylated exendin-4 peptide analogues |
| EP3080154B1 (en) | 2013-12-13 | 2018-02-07 | Sanofi | 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 |
| 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 |
| 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 |
| US9932381B2 (en) | 2014-06-18 | 2018-04-03 | Sanofi | Exendin-4 derivatives as selective glucagon receptor agonists |
| CN105985425B (zh) * | 2014-12-11 | 2019-12-17 | 浙江海昶生物医药技术有限公司 | 一种聚乙二醇修饰的exendin类似物及其制备方法和应用 |
| AR105319A1 (es) | 2015-06-05 | 2017-09-27 | Sanofi Sa | Profármacos que comprenden un conjugado agonista dual de glp-1 / glucagón conector ácido hialurónico |
| 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 |
| EP3331557B1 (en) | 2015-08-04 | 2021-04-07 | Duke University | Genetically encoded intrinsically disordered stealth polymers for delivery and methods of using same |
| US11752213B2 (en) | 2015-12-21 | 2023-09-12 | Duke University | Surfaces having reduced non-specific binding and antigenicity |
| EA201891469A1 (ru) | 2015-12-23 | 2018-12-28 | Дзе Джонс Хопкинс Юниверсити | Агонист длительного действия glp-1r как терапия для лечения неврологических и нейродегенеративных патологических состояний |
| CN113546159B (zh) * | 2015-12-29 | 2023-09-08 | 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 |
| US11467156B2 (en) | 2016-06-01 | 2022-10-11 | Duke University | Nonfouling biosensors |
| WO2018057847A1 (en) | 2016-09-23 | 2018-03-29 | Duke University | Unstructured non-repetitive polypeptides having lcst behavior |
| US11648200B2 (en) | 2017-01-12 | 2023-05-16 | Duke University | Genetically encoded lipid-polypeptide hybrid biomaterials that exhibit temperature triggered hierarchical self-assembly |
| US11554097B2 (en) | 2017-05-15 | 2023-01-17 | Duke University | Recombinant production of hybrid lipid-biopolymer materials that self-assemble and encapsulate agents |
| WO2019147954A1 (en) | 2018-01-26 | 2019-08-01 | Duke University | Albumin binding peptide-drug (aibiped) conjugates and methods of making and using same |
| EP3788343B1 (en) | 2018-04-30 | 2024-03-27 | Duke University | Stimuli-responsive peg-like polymer-based drug delivery platform |
| KR20200135618A (ko) * | 2019-05-23 | 2020-12-03 | ㈜ 디앤디파마텍 | 폴리펩티드를 포함하는 비알코올성 지방간 질환의 예방 또는 치료용 약학 조성물 |
| EP3829622A4 (en) | 2018-08-02 | 2022-05-11 | Duke University | DOUBLE AGONIST FUSION PROTEINS |
| US11512314B2 (en) | 2019-07-12 | 2022-11-29 | Duke University | Amphiphilic polynucleotides |
| KR102193211B1 (ko) * | 2019-11-27 | 2020-12-18 | (주)디앤디파마텍 | 비오틴 모이어티가 결합된 폴리펩티드 및 이를 포함하는 경구 투여용 약학적 조성물 |
| EP4313158A1 (en) * | 2021-04-01 | 2024-02-07 | Duke University | Poegma copolymer conjugates and methods of treating diseases |
| US20240374691A1 (en) | 2021-08-25 | 2024-11-14 | Neuraly, Inc. | Glp-1r agonists for use in a treatment of neurologial impairment associated with viral infection |
| KR20240155737A (ko) | 2023-04-20 | 2024-10-29 | 전북대학교산학협력단 | 폴리에틸렌글리콜을 이용한 분자 전달 방법 |
| WO2024229006A1 (en) * | 2023-05-01 | 2024-11-07 | Neuraly, Inc. | Glucagon-like peptide-1 receptor agonist variants and methods thereof |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1143989B1 (en) * | 1999-01-14 | 2006-12-13 | Amylin Pharmaceuticals, Inc. | Exendins for glucagon suppression |
| DE60006100T2 (de) * | 1999-05-17 | 2004-07-01 | Conjuchem, Inc., Montreal | Lang wirkende insulinotrope peptide |
| EP1539210A4 (en) * | 2002-09-06 | 2006-06-07 | Bayer Pharmaceuticals Corp | GLP-1 RECEPTOR MODIFIED AGONISTS AND THEIR PHARMACOLOGICAL METHODS OF USE |
| AU2004220325B2 (en) * | 2003-06-30 | 2011-05-12 | Domantis Limited | Polypeptides |
| US20080182783A1 (en) * | 2004-10-18 | 2008-07-31 | Novo Nordisk A/S | Growth Hormone Conjugates |
| WO2007075534A2 (en) * | 2005-12-16 | 2007-07-05 | Nektar Therapeutics Al, Corporation | Polymer conjugates of glp-1 |
| KR100890989B1 (ko) * | 2006-06-01 | 2009-03-31 | 이강춘 | 폴리에틸렌글리콜 또는 이의 유도체로 단일 수식된 엑센딘,이의 제조방법 및 이의 용도 |
| US8420598B2 (en) * | 2007-04-20 | 2013-04-16 | B & L Delipharm Corp. | Mono modified exendin with polyethylene glycol or its derivatives and uses thereof |
| CN101870728A (zh) * | 2009-04-23 | 2010-10-27 | 派格生物医药(苏州)有限公司 | 新型Exendin变体及其缀合物 |
| KR101112578B1 (ko) * | 2009-07-16 | 2012-02-16 | 성균관대학교산학협력단 | 엑센딘의 비강투여용 약제학적 조성물 및 이의 제조방법 |
-
2011
- 2011-06-28 KR KR1020110062858A patent/KR101357117B1/ko active Active
-
2012
- 2012-06-28 CN CN201280003243.XA patent/CN103338790B/zh active Active
- 2012-06-28 WO PCT/KR2012/005137 patent/WO2013002580A2/ko not_active Ceased
- 2012-06-28 AU AU2012276478A patent/AU2012276478B2/en active Active
- 2012-06-28 US US13/882,361 patent/US20130217622A1/en not_active Abandoned
- 2012-06-28 EP EP12804683.6A patent/EP2727605B1/en active Active
- 2012-06-28 CA CA2839410A patent/CA2839410C/en active Active
- 2012-06-28 ES ES12804683.6T patent/ES2674581T3/es active Active
- 2012-06-28 DK DK12804683.6T patent/DK2727605T3/en active
- 2012-06-28 JP JP2014518803A patent/JP6084215B2/ja active Active
-
2017
- 2017-01-23 US US15/413,029 patent/US10406230B2/en active Active
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