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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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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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    • A61K9/0019Injectable 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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    • 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)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Zoology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Botany (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Psychology (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (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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Family Applications (1)

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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 (enExample)
EP (2) EP4212180A1 (enExample)
JP (1) JP6572497B2 (enExample)
KR (1) KR102455171B1 (enExample)
CN (1) CN106456589B (enExample)
AU (1) AU2014364589B2 (enExample)
CA (1) CA2933701C (enExample)
WO (1) WO2015095406A1 (enExample)

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US10286078B2 (en) 2013-09-13 2019-05-14 The California Institute For Biomedical Research Modified therapeutic agents and compositions thereof
EP4212180A1 (en) 2013-12-18 2023-07-19 The Scripps Research Institute Modified therapeutic agents, stapled peptide lipid conjugates, and compositions thereof
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AU2016270302B2 (en) 2015-06-04 2020-09-17 Rezolute, Inc. Amine pegylation methods for the preparation of site-specific protein conjugates
EP3310376A4 (en) * 2015-06-17 2019-01-23 The California Institute for Biomedical Research MODIFIED THERAPEUTIC AGENTS AND COMPOSITIONS THEREOF
TN2017000555A1 (en) 2015-06-30 2019-04-12 Hanmi Pharm Ind Co Ltd Glucagon derivative and a composition comprising a long acting conjugate of the same
CN108602894A (zh) * 2015-10-30 2018-09-28 纽约州立大学研究基金会 胃泌酸调节素类似物及其制备和使用方法
WO2017112889A1 (en) 2015-12-23 2017-06-29 The Johns Hopkins University Long-acting glp-1r agonist as a therapy of neurological and neurodegenerative conditions
KR20170080521A (ko) 2015-12-31 2017-07-10 한미약품 주식회사 글루카곤, glp-1 및 gip 수용체 모두에 활성을 갖는 삼중 활성체
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
JP7208020B2 (ja) 2016-06-29 2023-01-18 ハンミ ファーマシューティカル カンパニー リミテッド グルカゴン誘導体、その結合体、及びそれを含む組成物、並びにその治療的用途
US10864279B2 (en) 2016-12-16 2020-12-15 Industrial Technology Research Institute Linker-drug and antibody-drug conjugate (ADC) employing the same
US10266578B2 (en) 2017-02-08 2019-04-23 Bristol-Myers Squibb Company Modified relaxin polypeptides comprising a pharmacokinetic enhancer and uses thereof
WO2018175592A1 (en) * 2017-03-22 2018-09-27 The Regents Of The University Of California Modified oligonucleotides and therapeutic uses thereof
WO2019016208A1 (en) * 2017-07-17 2019-01-24 Technische Universiteit Eindhoven APPLICABLE CHEMICAL COMPOSITION COMPRISING AN AGENT CONJUGATED TO A HYDROPHOBIC PART AND A SUPPORT
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
CN113039195A (zh) 2018-08-20 2021-06-25 弗格制药有限公司 肽集合、肽试剂及其使用方法
US12441776B2 (en) 2018-11-30 2025-10-14 Eirgen Pharma Ltd. Oxyntomodulin peptide analog formulations
JP7160183B2 (ja) * 2019-03-28 2022-10-25 日本電気株式会社 情報処理装置、表示システム、表示方法、及びプログラム
WO2021113535A1 (en) * 2019-12-04 2021-06-10 The Scripps Research Institute Peptide conjugates 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
US20230405088A1 (en) * 2020-12-16 2023-12-21 Zealand Pharma A/S Pharmaceutical Composition of GLP-1/GLP-2 Dual Agonists
WO2022156189A1 (zh) * 2021-01-22 2022-07-28 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
US20220378702A1 (en) * 2021-05-05 2022-12-01 Arcturus Therapeutics, Inc. Peptide-lipid conjugates
IL309067A (en) 2021-06-09 2024-02-01 Scripps Research Inst Long-acting dual gip/glp-1 peptide conjugates and methods of use
KR20240103040A (ko) * 2021-11-19 2024-07-03 소테르 바이오파마 피티이. 리미티드 스테이플-함유 폴리펩티드 및 이의 적용
WO2023159052A2 (en) * 2022-02-15 2023-08-24 Transira Therapeutics, Llc Stapled peptides, methods of making same, and uses thereof

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