CA2933701C - Modified therapeutic agents, stapled peptide lipid conjugates, and compositions thereof - Google Patents

Modified therapeutic agents, stapled peptide lipid conjugates, and compositions thereof Download PDF

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Publication number
CA2933701C
CA2933701C CA2933701A CA2933701A CA2933701C CA 2933701 C CA2933701 C CA 2933701C CA 2933701 A CA2933701 A CA 2933701A CA 2933701 A CA2933701 A CA 2933701A CA 2933701 C CA2933701 C CA 2933701C
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Prior art keywords
amino acid
peptide
mta
residues
disease
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CA2933701A
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English (en)
French (fr)
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CA2933701A1 (en
Inventor
Weijun Shen
Pengyu YANG
Huafei ZOU
Peter G. Schultz
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Scripps Research Institute
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Scripps Research Institute
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22Hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22Hormones
    • A61K38/2278Vasoactive intestinal peptide [VIP]; Related peptides (e.g. Exendin)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22Hormones
    • A61K38/26Glucagons
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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 compound
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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 compound
    • A61K47/542Carboxylic acids, e.g. a fatty acid or an amino acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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 compound
    • A61K47/543Lipids, e.g. triglycerides; Polyamines, e.g. spermine or spermidine
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K47/50Medicinal 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
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    • A61K47/54Medicinal 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 compound
    • A61K47/554Medicinal 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 compound the modifying agent being a steroid plant sterol, glycyrrhetic acid, enoxolone or bile acid
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    • A61K47/59Medicinal 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
    • A61K47/60Medicinal 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
    • AHUMAN NECESSITIES
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    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A61K9/0021Intradermal administration, e.g. through microneedle arrays, needleless injectors
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    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
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    • A61K9/70Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • A61K9/703Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Botany (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Psychology (AREA)
  • Hematology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
CA2933701A 2013-12-18 2014-12-17 Modified therapeutic agents, stapled peptide lipid conjugates, and compositions thereof Active CA2933701C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361917816P 2013-12-18 2013-12-18
US61/917,816 2013-12-18
PCT/US2014/070977 WO2015095406A1 (en) 2013-12-18 2014-12-17 Modified therapeutic agents, stapled peptide lipid conjugates, and compositions thereof

Publications (2)

Publication Number Publication Date
CA2933701A1 CA2933701A1 (en) 2015-06-25
CA2933701C true CA2933701C (en) 2022-05-31

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CA2933701A Active CA2933701C (en) 2013-12-18 2014-12-17 Modified therapeutic agents, stapled peptide lipid conjugates, and compositions thereof

Country Status (8)

Country Link
US (5) US10039809B2 (cg-RX-API-DMAC7.html)
EP (2) EP4212180A1 (cg-RX-API-DMAC7.html)
JP (1) JP6572497B2 (cg-RX-API-DMAC7.html)
KR (1) KR102455171B1 (cg-RX-API-DMAC7.html)
CN (1) CN106456589B (cg-RX-API-DMAC7.html)
AU (1) AU2014364589B2 (cg-RX-API-DMAC7.html)
CA (1) CA2933701C (cg-RX-API-DMAC7.html)
WO (1) WO2015095406A1 (cg-RX-API-DMAC7.html)

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JP6822839B2 (ja) 2013-09-13 2021-01-27 ザ・スクリップス・リサーチ・インスティテュート 修飾された治療剤、及びその組成物
CA2933701C (en) 2013-12-18 2022-05-31 The California Institute For Biomedical Research Modified therapeutic agents, stapled peptide lipid conjugates, and compositions thereof
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EP3310376A4 (en) * 2015-06-17 2019-01-23 The California Institute for Biomedical Research MODIFIED THERAPEUTIC AGENTS AND COMPOSITIONS THEREOF
TWI713541B (zh) 2015-06-30 2020-12-21 南韓商韓美藥品股份有限公司 升糖素衍生物及包含該衍生物之長效接合物之組成物
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
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
HUE059737T2 (hu) 2015-12-31 2022-12-28 Hanmi Pharm Ind Co Ltd Glükagon, GLP-1 és GIP receptor aktiváló tripla aktivátor
CN106046145B (zh) 2016-04-22 2022-11-04 深圳市图微安创科技开发有限公司 Glp-1r/gcgr双靶点激动剂多肽治疗脂肪肝病、高脂血症和动脉硬化
PE20190355A1 (es) 2016-06-29 2019-03-07 Hanmi Pharm Ind Co Ltd Derivado de glucagon, conjugado del mismo, composicion que comprende el mismo y uso terapeutico del mismo
US10864279B2 (en) * 2016-12-16 2020-12-15 Industrial Technology Research Institute Linker-drug and antibody-drug conjugate (ADC) employing the same
SG11201907209QA (en) 2017-02-08 2019-09-27 Bristol Myers Squibb Co Modified relaxin polypeptides comprising a pharmacokinetic enhancer and uses thereof
AU2018237139A1 (en) * 2017-03-22 2019-10-17 The Regents Of The University Of California Modified oligonucleotides and therapeutic uses thereof
US20200164078A1 (en) * 2017-07-17 2020-05-28 Technische Universiteit Eindhoven Applicable chemical composition comprising an agent conjugated to a hydrophobic moiety and a carrier
US11274158B2 (en) * 2018-01-30 2022-03-15 Flagship Pioneering Innovations V, Inc. Methods and compositions for treating inflammatory or autoimmune diseases or conditions using calcitonin receptor activators
CA3110082A1 (en) 2018-08-20 2020-02-27 Fog Pharmaceuticals, Inc. Collections of peptides, peptide agents, and methods of use thereof
US12441776B2 (en) 2018-11-30 2025-10-14 Eirgen Pharma Ltd. Oxyntomodulin peptide analog formulations
US12073515B2 (en) * 2019-03-28 2024-08-27 Nec Corporation Information processing apparatus, display system, display method, and non-transitory computer readable medium storing program
AU2020397917A1 (en) * 2019-12-04 2022-06-23 The Scripps Research Institute GLP2 receptor agonists and methods of use
EP3842449A1 (en) * 2019-12-23 2021-06-30 Merck Sharp & Dohme Corp. Stapled olefin co-agonists of the glucagon and glp-1 receptors
CN113024635B (zh) * 2019-12-25 2023-12-19 中国医学科学院药物研究所 一类订书肽化合物及其药物组合物的用途
CA3196989A1 (en) * 2020-12-16 2022-06-23 Zealand Pharma A/S Pharmaceutical composition of glp-1/glp-2 dual agonists
CN117120462A (zh) * 2021-01-22 2023-11-24 深圳市图微安创科技开发有限公司 多肽化合物在预防或治疗炎症性肠病及其相关的肠纤维化中的应用
KR20240068586A (ko) * 2021-04-30 2024-05-17 리간달 인코포레이티드 대규모 접합가능한 중합체 및 단백질 합성을 위한 방법 및 조성물
CA3219056A1 (en) * 2021-05-05 2022-11-10 Arcturus Therapeutics, Inc. Peptide-lipid conjugates
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US20250326815A1 (en) * 2021-11-19 2025-10-23 Soter Biopharma Pte. Ltd. Staple-containing polypeptides and application thereof
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