AU2009335715B2 - Amide-based insulin prodrugs - Google Patents
Amide-based insulin prodrugs Download PDFInfo
- Publication number
- AU2009335715B2 AU2009335715B2 AU2009335715A AU2009335715A AU2009335715B2 AU 2009335715 B2 AU2009335715 B2 AU 2009335715B2 AU 2009335715 A AU2009335715 A AU 2009335715A AU 2009335715 A AU2009335715 A AU 2009335715A AU 2009335715 B2 AU2009335715 B2 AU 2009335715B2
- Authority
- AU
- Australia
- Prior art keywords
- alkyl
- group
- seq
- insulin
- chain
- 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.)
- Ceased
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- 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 title claims abstract description 456
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- XMVJITFPVVRMHC-UHFFFAOYSA-N roxarsone Chemical group OC1=CC=C([As](O)(O)=O)C=C1[N+]([O-])=O XMVJITFPVVRMHC-UHFFFAOYSA-N 0.000 description 1
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- MFFMDFFZMYYVKS-SECBINFHSA-N sitagliptin Chemical compound C([C@H](CC(=O)N1CC=2N(C(=NN=2)C(F)(F)F)CC1)N)C1=CC(F)=C(F)C=C1F MFFMDFFZMYYVKS-SECBINFHSA-N 0.000 description 1
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/575—Hormones
- C07K14/62—Insulins
- C07K14/622—Insulins at least 1 amino acid in D-form
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/22—Hormones
- A61K38/28—Insulins
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/575—Hormones
- C07K14/62—Insulins
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
- A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/575—Hormones
- C07K14/62—Insulins
- C07K14/625—Extraction from natural sources
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Diabetes (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Endocrinology (AREA)
- Zoology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Gastroenterology & Hepatology (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Toxicology (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Immunology (AREA)
- Emergency Medicine (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US13921808P | 2008-12-19 | 2008-12-19 | |
| US61/139,218 | 2008-12-19 | ||
| PCT/US2009/068716 WO2010080609A1 (en) | 2008-12-19 | 2009-12-18 | Amide-based insulin prodrugs |
Publications (2)
| Publication Number | Publication Date |
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| AU2009335715A1 AU2009335715A1 (en) | 2010-07-15 |
| AU2009335715B2 true AU2009335715B2 (en) | 2016-09-15 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2009335715A Ceased AU2009335715B2 (en) | 2008-12-19 | 2009-12-18 | Amide-based insulin prodrugs |
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| Country | Link |
|---|---|
| US (1) | US8697632B2 (enExample) |
| EP (1) | EP2376521B1 (enExample) |
| JP (1) | JP5755566B2 (enExample) |
| CN (1) | CN102245624B (enExample) |
| AU (1) | AU2009335715B2 (enExample) |
| CA (1) | CA2744558A1 (enExample) |
| WO (1) | WO2010080609A1 (enExample) |
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| JP2011511778A (ja) | 2008-01-30 | 2011-04-14 | インディアナ ユニバーシティー リサーチ アンド テクノロジー コーポレーション | エステルに基づいたペプチドプロドラッグ |
| PA8830501A1 (es) | 2008-06-17 | 2010-07-27 | Univ Indiana Res & Tech Corp | Co-agonistas del receptor de glucagon/glp-1 |
| ES2439499T3 (es) | 2008-12-15 | 2014-01-23 | Zealand Pharma A/S | Análogos de glucagón |
| JP5635530B2 (ja) | 2008-12-15 | 2014-12-03 | ジーランド ファーマ アクティーゼルスカブ | グルカゴン類似体 |
| KR20150116912A (ko) | 2008-12-15 | 2015-10-16 | 질랜드 파마 에이/에스 | 글루카곤 유사체 |
| US8680049B2 (en) | 2008-12-15 | 2014-03-25 | Zealand Pharma A/S | Glucagon analogues |
| CN102325539A (zh) | 2008-12-19 | 2012-01-18 | 印第安纳大学研究及科技有限公司 | 基于酰胺的胰高血糖素超家族肽前药 |
| CN102459325B (zh) | 2009-06-16 | 2015-03-25 | 印第安纳大学科技研究有限公司 | 胃抑胜肽受体活化的胰高血糖素化合物 |
| PT2454282E (pt) | 2009-07-13 | 2015-06-23 | Zealand Pharma As | Análogos de glucagão acilados |
| AR081975A1 (es) | 2010-06-23 | 2012-10-31 | Zealand Pharma As | Analogos de glucagon |
| WO2011162968A1 (en) * | 2010-06-24 | 2011-12-29 | Indiana University Research And Technology Corporation | Dipeptide linked medicinal agents |
| MA34383B1 (fr) | 2010-06-24 | 2013-07-03 | Zealand Pharma As | Analogues de glucagon |
| US8946147B2 (en) | 2010-06-24 | 2015-02-03 | Indiana University Research And Technology Corporation | Amide-based insulin prodrugs |
| MX2013008005A (es) | 2011-01-20 | 2013-08-21 | Zealand Pharma As | Combinacion de analogos de glucagon acilados con analogos de insulina. |
| EP2686003A2 (en) * | 2011-03-15 | 2014-01-22 | Novo Nordisk A/S | Human insulin analogues and derivatives comprising cysteine substitutions |
| JP6058646B2 (ja) * | 2011-06-15 | 2017-01-11 | ノヴォ ノルディスク アー／エス | 多置換インスリン |
| PE20140724A1 (es) | 2011-06-22 | 2014-07-10 | Univ Indiana Res & Tech Corp | Coagonistas del receptor de glucagon/glp-1 |
| BR112014015156A2 (pt) * | 2011-12-20 | 2020-10-27 | Indiana University Research And Technology Corporation | análogos de insulina à base de ctp, seus métodos de produção e uso no tratamento de hiperglicemia, bem como sequência de ácido nucleico e célula hospedeira |
| AR090937A1 (es) | 2012-05-03 | 2014-12-17 | Zealand Pharma As | Compuestos agonista duales de gip-glp-1 y metodos para usarlos |
| BR112015001451B1 (pt) | 2012-07-23 | 2022-03-29 | Zealand Pharma A/S | Composto, construção de ácido nucleico, vetor de expressão, célula hospedeira, composição farmacêutica, utilização de um composto ou de seu sal ou solvato farmaceuticamente aceitável |
| TWI608013B (zh) | 2012-09-17 | 2017-12-11 | 西蘭製藥公司 | 升糖素類似物 |
| CN108383902A (zh) | 2012-09-26 | 2018-08-10 | 印第安纳大学研究及科技有限公司 | 胰岛素类似物二聚体 |
| US9707276B2 (en) | 2012-12-03 | 2017-07-18 | Merck Sharp & Dohme Corp. | O-glycosylated carboxy terminal portion (CTP) peptide-based insulin and insulin analogues |
| US10421795B2 (en) | 2012-12-17 | 2019-09-24 | Merck Sharp & Dohme Corp. | Process for purifying insulin and analogues thereof |
| WO2014158900A1 (en) | 2013-03-14 | 2014-10-02 | Indiana University Research And Technology Corporation | Insulin-incretin conjugates |
| TW201605470A (zh) | 2013-10-04 | 2016-02-16 | 默沙東藥廠 | 葡萄糖反應性胰島素結合物 |
| US9988429B2 (en) | 2013-10-17 | 2018-06-05 | Zealand Pharma A/S | Glucagon analogues |
| MX368436B (es) | 2013-10-17 | 2019-10-03 | Zealand Pharma As | Analogos de glucagon acilados. |
| KR102310392B1 (ko) | 2013-11-06 | 2021-10-13 | 질랜드 파마 에이/에스 | 글루카곤-ｇｌｐ-1-ｇｉｐ 삼원 효능제 화합물 |
| CA2929459C (en) | 2013-11-06 | 2022-05-03 | Zealand Pharma A/S | Gip-glp-1 dual agonist compounds and methods |
| US9822158B2 (en) | 2013-12-04 | 2017-11-21 | Merck Sharp & Dohme Corp. | Method for preparing crystalline insulin |
| US10626156B2 (en) | 2013-12-06 | 2020-04-21 | Jie Han | Bioreversable promoieties for nitrogen-containing and hydroxyl-containing drugs |
| MX369656B (es) | 2014-01-20 | 2019-11-15 | Hanmi Pharm Ind Co Ltd | Insulina de accion prolongada y uso de la misma. |
| AR099569A1 (es) | 2014-02-28 | 2016-08-03 | Novo Nordisk As | Derivados de insulina y los usos médicos de estos |
| WO2015138548A1 (en) | 2014-03-14 | 2015-09-17 | Merck Sharp & Dohme Corp. | Purifying insulin using cation exchange and reverse phase chromatography in the presence of an organic modifier and elevated temperature |
| 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 |
| WO2016014325A1 (en) | 2014-07-21 | 2016-01-28 | Merck Sharp & Dohme Corp. | Chromatography process for purification of inlsulin and insulin analogs |
| ES2947409T3 (es) | 2014-09-24 | 2023-08-08 | Univ Indiana Res & Tech Corp | Profármacos de insulina a base de amida lipídica |
| JP6657230B2 (ja) | 2014-09-24 | 2020-03-04 | インディアナ ユニヴァーシティ リサーチ アンド テクノロジー コーポレイション | インクレチン−インスリンコンジュゲート |
| ES2883345T3 (es) | 2014-10-29 | 2021-12-07 | Zealand Pharma As | Compuestos agonistas del GIP y métodos |
| AU2015349890B2 (en) | 2014-11-21 | 2018-08-30 | Merck Sharp & Dohme Llc | Insulin receptor partial agonists |
| US10562951B2 (en) | 2015-03-10 | 2020-02-18 | Merck Sharp & Dohme Corp. | Process for preparing recombinant insulin using microfiltration |
| PL3283507T3 (pl) | 2015-04-16 | 2020-05-18 | Zealand Pharma A/S | Acylowany analog glukagonu |
| UY36870A (es) | 2015-08-28 | 2017-03-31 | Hanmi Pharm Ind Co Ltd | Análogos de insulina novedosos |
| EP3344651B1 (en) | 2015-09-02 | 2022-03-02 | Merck Sharp & Dohme Corp. | A process for obtaining insulin with correctly formed disulfide bonds |
| US20190142963A1 (en) | 2016-04-15 | 2019-05-16 | Richard D. DiMarchi | Fgf21 c-terminal peptide optimization |
| WO2017189342A1 (en) | 2016-04-26 | 2017-11-02 | Merck Sharp & Dohme Corp. | Insulin dimer-incretin conjugates |
| US10953076B2 (en) | 2016-05-24 | 2021-03-23 | Merck Sharp & Dohme Corp. | Insulin receptor partial agonists and GLP-1 analogues |
| US10689430B2 (en) | 2016-05-25 | 2020-06-23 | Merck Sharp & Dohme Corp. | Insulin receptor partial agonists |
| AU2017273857B2 (en) | 2016-06-01 | 2021-08-19 | Athira Pharma, Inc. | Compounds |
| WO2017210168A1 (en) * | 2016-06-02 | 2017-12-07 | Indiana University Research And Technology Corporation | Aqueously soluble and chemically stable depsi glucagon agonists |
| AU2017300590A1 (en) | 2016-07-18 | 2019-01-24 | Eth Zurich | B-cell-mimetic cells |
| EP3272877A1 (en) | 2016-07-18 | 2018-01-24 | ETH Zurich | B-cell-mimetic cells |
| AU2017332408B2 (en) | 2016-09-23 | 2022-02-10 | Hanmi Pharm. Co., Ltd. | Insulin analogs with reduced affinity to insulin receptor and use thereof |
| US11174303B2 (en) | 2017-03-07 | 2021-11-16 | Case Western Reserve University | Single-chain insulin analogues stabilized by a fourth disulfide bridge |
| AU2018239037B2 (en) | 2017-03-23 | 2022-05-26 | Hanmi Pharm. Co., Ltd. | Insulin analog complex with reduced affinity for insulin receptor and use thereof |
| US11041009B2 (en) | 2017-03-23 | 2021-06-22 | Merck Sharp & Dohme Corp. | Glucose responsive insulin comprising a tri-valent sugar cluster for treatment of diabetes |
| EP3624828B1 (en) | 2017-05-18 | 2024-08-07 | Merck Sharp & Dohme LLC | Pharmaceutical formulation comprising incretin-insulin conjugates |
| BR112020002364A2 (pt) | 2017-08-17 | 2020-09-01 | Novo Nordisk A/S | derivado de insulina, produto intermediário, uso de um derivado de insulina, e, métodos para o tratamento ou prevenção de diabetes, diabetes do tipo 1, diabetes do tipo 2, tolerância à glicose comprometida, hiperglicemia, dislipidemia, obesidade, síndrome metabólica, hipertensão, distúrbios cognitivos, aterosclerose, infarto do miocárdio, acidente vascular cerebral, distúrbios cardiovasculares, doença cardíaca coronariana, síndrome intestinal inflamatória, dispepsia, hipotensão ou úlceras gástricas, e para determinar a seletividade de um composto de insulina |
| CA3122636A1 (en) | 2018-12-11 | 2020-06-18 | Sanofi | Insulin analogs having reduced insulin receptor binding affinity |
| EP3980052A4 (en) | 2019-06-06 | 2023-08-23 | Merck Sharp & Dohme LLC | GLUCOSE-RESPONDING INSULIN CONJUGATES |
| BR112022024058A2 (pt) * | 2020-05-26 | 2022-12-20 | Univ Indiana Res & Tech Corp | Análogos de pth para o tratamento de hipoparatireoidismo |
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| US20060024053A1 (en) * | 2002-05-30 | 2006-02-02 | Medivance Instruments Limited | Apparatus for determining replenishment of chemicals |
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Also Published As
| Publication number | Publication date |
|---|---|
| US20110257076A1 (en) | 2011-10-20 |
| CN102245624B (zh) | 2016-08-10 |
| CA2744558A1 (en) | 2010-07-15 |
| AU2009335715A1 (en) | 2010-07-15 |
| JP2012512901A (ja) | 2012-06-07 |
| EP2376521A1 (en) | 2011-10-19 |
| EP2376521A4 (en) | 2014-06-25 |
| CN102245624A (zh) | 2011-11-16 |
| JP5755566B2 (ja) | 2015-07-29 |
| EP2376521B1 (en) | 2016-04-13 |
| US8697632B2 (en) | 2014-04-15 |
| WO2010080609A1 (en) | 2010-07-15 |
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