EA033912B1 - ИНГИБИТОРЫ MetAP2 И СПОСОБЫ ЛЕЧЕНИЯ ОЖИРЕНИЯ - Google Patents

ИНГИБИТОРЫ MetAP2 И СПОСОБЫ ЛЕЧЕНИЯ ОЖИРЕНИЯ Download PDF

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Publication number
EA033912B1
EA033912B1 EA201591943A EA201591943A EA033912B1 EA 033912 B1 EA033912 B1 EA 033912B1 EA 201591943 A EA201591943 A EA 201591943A EA 201591943 A EA201591943 A EA 201591943A EA 033912 B1 EA033912 B1 EA 033912B1
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EA
Eurasian Patent Office
Prior art keywords
glycine
bond
compound
phenylalanine
leucine
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Application number
EA201591943A
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English (en)
Russian (ru)
Other versions
EA201591943A1 (ru
Inventor
Джон С. Петерсен
Джеймс Шанахан
Original Assignee
Синдевркс, Инк.
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Publication of EA201591943A1 publication Critical patent/EA201591943A1/ru
Publication of EA033912B1 publication Critical patent/EA033912B1/ru

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/336—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/74—Synthetic polymeric materials
    • A61K31/765—Polymers containing oxygen
    • A61K31/77—Polymers containing oxygen of oxiranes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06—Tripeptides
    • 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
    • A61K47/54—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 compound
    • A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
    • 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
    • A61K47/56—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
    • A61K47/58—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 by reactions only involving carbon-to-carbon unsaturated bonds, e.g. poly[meth]acrylate, polyacrylamide, polystyrene, polyvinylpyrrolidone, polyvinylalcohol or polystyrene sulfonic acid resin
    • 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
    • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Diabetes (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
EA201591943A 2013-04-10 2014-04-09 ИНГИБИТОРЫ MetAP2 И СПОСОБЫ ЛЕЧЕНИЯ ОЖИРЕНИЯ EA033912B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361810468P 2013-04-10 2013-04-10
US201461925918P 2014-01-10 2014-01-10
PCT/US2014/033476 WO2014169026A1 (en) 2013-04-10 2014-04-09 Metap2 inhibitors and methods of treating obesity

Publications (2)

Publication Number Publication Date
EA201591943A1 EA201591943A1 (ru) 2016-07-29
EA033912B1 true EA033912B1 (ru) 2019-12-09

Family

ID=51686946

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201591943A EA033912B1 (ru) 2013-04-10 2014-04-09 ИНГИБИТОРЫ MetAP2 И СПОСОБЫ ЛЕЧЕНИЯ ОЖИРЕНИЯ

Country Status (12)

Country Link
US (9) US9173956B2 (https=)
EP (2) EP2984085B1 (https=)
JP (5) JP6420314B2 (https=)
CN (2) CN105431426A (https=)
AU (1) AU2014250983B2 (https=)
BR (1) BR112015025892A2 (https=)
CA (1) CA2908993C (https=)
DK (2) DK3574922T3 (https=)
EA (1) EA033912B1 (https=)
ES (2) ES2902082T3 (https=)
MX (2) MX386958B (https=)
WO (1) WO2014169026A1 (https=)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2576638T3 (da) 2010-05-25 2021-03-15 Syndevrx Inc Polymerkonjugerede metap2-inhibitorer og terapeutiske fremgangsmåder til anvendelse deraf
US9895449B2 (en) 2010-05-25 2018-02-20 Syndevrx, Inc. Polymer-conjugated MetAP2 inhibitors, and therapeutic methods of use thereof
CN105431426A (zh) 2013-04-10 2016-03-23 新德发制药有限公司 Metap2抑制剂和治疗肥胖症的方法
CN106432255A (zh) * 2015-08-11 2017-02-22 扎夫根公司 烟曲霉素醇螺环化合物和制备和使用其的方法
US9969722B2 (en) 2015-12-10 2018-05-15 Syndevrx, Inc. Fumagillol derivatives and polymorphs thereof
CN108697807B (zh) * 2016-01-11 2021-11-26 辛德弗雷克斯公司 代谢功能障碍引起的肿瘤的治疗
CN113453721B (zh) 2018-10-26 2025-09-16 辛德弗雷克斯公司 Metap2抑制剂的生物标志物及其应用
CN114573476B (zh) * 2020-09-14 2024-06-11 广州药本君安医药科技股份有限公司 线性头尾二胺桥连化合物及在制备治疗糖代谢紊乱疾病药物中的应用
CN118871428A (zh) * 2022-02-16 2024-10-29 耶路撒冷希伯来大学伊森姆研究发展有限公司 Metap2抑制剂及其用途

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CA1305053C (en) * 1985-01-04 1992-07-14 Jindrich Kopecek Synthetic polymeric drugs
US5037957A (en) * 1987-06-18 1991-08-06 Anders Grubb Cysteine proteinase inhibitor
EP0673258B1 (en) * 1993-10-08 2003-05-07 Pharmacia Italia S.p.A. Polymer-bound camptothecin derivatives
US20050036948A1 (en) * 1994-01-24 2005-02-17 Neorx Corporation Radiolabeled annexins
US20020076442A1 (en) * 1997-09-02 2002-06-20 Martin Burke Vitamin d3 analog loaded polymer formulations for cancer and neurodegenerative disorders
WO2004110358A2 (en) * 2003-05-15 2004-12-23 Vectramed, Inc. Polymeric conjugates for tissue activated drug delivery
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Publication number Publication date
ES2749746T3 (es) 2020-03-23
JP2021091738A (ja) 2021-06-17
JP6420314B2 (ja) 2018-11-07
MX2015014329A (es) 2016-06-21
US20170028014A1 (en) 2017-02-02
JP2016519106A (ja) 2016-06-30
WO2014169026A1 (en) 2014-10-16
ES2902082T3 (es) 2022-03-24
DK2984085T3 (da) 2019-10-21
US10588904B2 (en) 2020-03-17
JP2025109807A (ja) 2025-07-25
US20180271856A1 (en) 2018-09-27
DK3574922T3 (da) 2021-12-06
AU2014250983B2 (en) 2019-04-11
US20260076960A1 (en) 2026-03-19
US11304944B2 (en) 2022-04-19
US20230048989A1 (en) 2023-02-16
EP3574922B1 (en) 2021-09-15
CA2908993C (en) 2023-05-23
US20140308235A1 (en) 2014-10-16
CN105431426A (zh) 2016-03-23
EP3574922A1 (en) 2019-12-04
EA201591943A1 (ru) 2016-07-29
JP2023082195A (ja) 2023-06-13
BR112015025892A2 (pt) 2017-07-25
HK1216313A1 (en) 2016-11-04
US20170326135A1 (en) 2017-11-16
CN112494476A (zh) 2021-03-16
US9750737B2 (en) 2017-09-05
CA2908993A1 (en) 2014-10-16
MX371095B (es) 2020-01-16
EP2984085A1 (en) 2016-02-17
MX386958B (es) 2025-03-19
US9757373B2 (en) 2017-09-12
EP2984085A4 (en) 2016-12-07
US20160346244A1 (en) 2016-12-01
US9173956B2 (en) 2015-11-03
AU2014250983A1 (en) 2015-10-29
EP2984085B1 (en) 2019-07-17
US20200155545A1 (en) 2020-05-21
US10010544B2 (en) 2018-07-03
JP7681054B2 (ja) 2025-05-21
JP2019023219A (ja) 2019-02-14
US9433600B2 (en) 2016-09-06
US20150374657A1 (en) 2015-12-31

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