AU2017234680A1 - Extended release conjugates of exenatide analogs - Google Patents
Extended release conjugates of exenatide analogs Download PDFInfo
- Publication number
- AU2017234680A1 AU2017234680A1 AU2017234680A AU2017234680A AU2017234680A1 AU 2017234680 A1 AU2017234680 A1 AU 2017234680A1 AU 2017234680 A AU2017234680 A AU 2017234680A AU 2017234680 A AU2017234680 A AU 2017234680A AU 2017234680 A1 AU2017234680 A1 AU 2017234680A1
- Authority
- AU
- Australia
- Prior art keywords
- optionally substituted
- pct
- alkyl
- peptide
- heteroaryl
- 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.)
- Abandoned
Links
- 238000013265 extended release Methods 0.000 title claims abstract description 25
- HTQBXNHDCUEHJF-XWLPCZSASA-N Exenatide Chemical class 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(N)=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 HTQBXNHDCUEHJF-XWLPCZSASA-N 0.000 title claims description 134
- 239000000556 agonist Substances 0.000 claims abstract description 24
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- 125000001072 heteroaryl group Chemical group 0.000 claims description 36
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 34
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 34
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 31
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- 125000000217 alkyl group Chemical group 0.000 claims description 22
- 238000006731 degradation reaction Methods 0.000 claims description 19
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- 230000015556 catabolic process Effects 0.000 claims description 17
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- 125000003107 substituted aryl group Chemical group 0.000 claims description 12
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- 125000000468 ketone group Chemical group 0.000 claims description 4
- LLVWLCAZSOLOTF-UHFFFAOYSA-N 1-methyl-4-[1,4,4-tris(4-methylphenyl)buta-1,3-dienyl]benzene Chemical compound C1=CC(C)=CC=C1C(C=1C=CC(C)=CC=1)=CC=C(C=1C=CC(C)=CC=1)C1=CC=C(C)C=C1 LLVWLCAZSOLOTF-UHFFFAOYSA-N 0.000 claims description 3
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- 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
- A61K47/56—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 an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
- A61K47/59—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 an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
- A61K47/60—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 an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- 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
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- 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
- A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
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- A—HUMAN NECESSITIES
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- 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
- A61K47/69—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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
- A61K47/6903—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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being semi-solid, e.g. an ointment, a gel, a hydrogel or a solidifying gel
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
- A61K9/0004—Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas
-
- 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
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- A—HUMAN NECESSITIES
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- 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
-
- 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
- C07K14/605—Glucagons
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
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- Zoology (AREA)
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- Molecular Biology (AREA)
- Emergency Medicine (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
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| PCT/US2017/022791 WO2017161174A1 (en) | 2016-03-16 | 2017-03-16 | Extended release conjugates of exenatide analogs |
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| US10745456B2 (en) * | 2015-04-01 | 2020-08-18 | The Scripps Research Institute | Methods and compositions related to GPCR agonist polypeptides |
| JOP20190245A1 (ar) | 2017-04-20 | 2019-10-15 | Novartis Ag | أنظمة توصيل إطلاق مستدام تتضمن روابط بلا أثر لنقطة الربط |
| AR116566A1 (es) | 2018-10-03 | 2021-05-19 | Novartis Ag | Administración sostenida de polipéptidos similares a la angiopoyetina 3 |
| WO2020206358A1 (en) | 2019-04-05 | 2020-10-08 | Prolynx Llc | Improved conjugation linkers |
| EP4010041A4 (en) * | 2019-08-07 | 2024-12-11 | Prolynx LLC | Steam sterilization of hydrogels crosslinked by beta-eliminative linkers |
| WO2022115563A1 (en) * | 2020-11-25 | 2022-06-02 | Prolynx Llc | Extended release hydrogel conjugates of c-natriuretic peptides |
| US12576400B2 (en) | 2021-01-08 | 2026-03-17 | Cellanome, Inc. | Methods for incubating and analyzing a cell in a compartment of a fluidic device |
| JP2024502618A (ja) | 2021-01-08 | 2024-01-22 | セラノーム， インコーポレイテッド | 生体試料を分析するためのデバイスおよび方法 |
| WO2025128916A1 (en) * | 2023-12-13 | 2025-06-19 | Cellanome, Inc. | Devices and methods for analyzing biological samples |
| KR102716759B1 (ko) | 2023-12-20 | 2024-10-15 | (주)인벤티지랩 | 엑세나타이드를 포함하는 서방형 주사제 조성물 및 이의 제조 방법 |
| WO2026020143A1 (en) * | 2024-07-19 | 2026-01-22 | Prolynx Llc | Extended-release conjugates of lipidated peptides, and uses thereof |
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| DK1143989T3 (da) * | 1999-01-14 | 2007-04-16 | Amylin Pharmaceuticals Inc | Exendiner til glucagonundertrykkelse |
| 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 |
| AU2003268621B2 (en) | 2002-10-02 | 2009-01-15 | Zealand Pharma A/S | Stabilized exendin-4 compounds |
| CA2603630C (en) * | 2005-01-14 | 2015-06-09 | Wuxi Grandchamp Pharmaceutical Technology Co., Ltd. | Modified exendins and uses thereof |
| GB2427360A (en) | 2005-06-22 | 2006-12-27 | Complex Biosystems Gmbh | Aliphatic prodrug linker |
| CN101125207B (zh) * | 2006-11-14 | 2012-09-05 | 上海华谊生物技术有限公司 | 带有聚乙二醇基团的艾塞丁或其类似物及其制剂和用途 |
| WO2008116294A1 (en) | 2007-03-23 | 2008-10-02 | Matregen Corp. | Exendin analogs |
| WO2009158668A1 (en) | 2008-06-26 | 2009-12-30 | Prolynx Llc | Prodrugs and drug-macromolecule conjugates having controlled drug release rates |
| WO2010017215A2 (en) * | 2008-08-04 | 2010-02-11 | The Regents Of The University Of California | Biodegradable microspheres and methods of use thereof |
| NZ599847A (en) * | 2009-11-13 | 2013-09-27 | Sanofi Aventis Deutschland | Pharmaceutical composition comprising a glp-1 agonist and methionine |
| EP2566334B1 (en) * | 2010-05-05 | 2018-04-18 | Prolynx, LLC | Controlled drug release from solid supports |
| EP2566335B1 (en) * | 2010-05-05 | 2016-06-29 | Prolynx Llc | Controlled release of active compounds from macromolecular conjugates |
| US8703907B2 (en) | 2010-05-05 | 2014-04-22 | Prolynx Llc | Controlled drug release from dendrimers |
| WO2011156407A2 (en) * | 2010-06-09 | 2011-12-15 | Amylin Pharmaceuticals, Inc. | Glp-1 receptor agonists to treat pancre-atitis |
| KR102109067B1 (ko) | 2011-09-07 | 2020-05-13 | 프로린크스 엘엘시 | 생분해성 교차결합을 가지는 하이드로젤 |
| US20140256626A1 (en) * | 2011-10-18 | 2014-09-11 | Prolynx Llc | Peg conjugates of exenatide |
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2017
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- 2017-03-16 JP JP2018548652A patent/JP7017248B2/ja not_active Expired - Fee Related
- 2017-03-16 SG SG11201807832VA patent/SG11201807832VA/en unknown
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2018
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2021
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Also Published As
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| RU2018136200A3 (https=) | 2020-12-25 |
| ZA201905787B (en) | 2021-03-31 |
| JP7017248B2 (ja) | 2022-02-08 |
| AU2017234680A2 (en) | 2018-12-13 |
| CA3016814A1 (en) | 2017-09-21 |
| WO2017161174A1 (en) | 2017-09-21 |
| MX2018011149A (es) | 2019-05-30 |
| JP2019511497A (ja) | 2019-04-25 |
| EP3429608A4 (en) | 2019-12-11 |
| RU2018136200A (ru) | 2020-04-16 |
| AU2021232810A1 (en) | 2021-10-14 |
| RU2764547C2 (ru) | 2022-01-18 |
| US20200164083A1 (en) | 2020-05-28 |
| KR20180129825A (ko) | 2018-12-05 |
| ZA201805953B (en) | 2019-11-27 |
| EP3429608A1 (en) | 2019-01-23 |
| BR112018068639A2 (pt) | 2019-07-30 |
| EP3922269A1 (en) | 2021-12-15 |
| SG11201807832VA (en) | 2018-10-30 |
| CN109414469A (zh) | 2019-03-01 |
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