JP6420314B2 - Metap2阻害剤及び肥満症の治療方法 - Google Patents

Metap2阻害剤及び肥満症の治療方法 Download PDF

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JP6420314B2
JP6420314B2 JP2016507631A JP2016507631A JP6420314B2 JP 6420314 B2 JP6420314 B2 JP 6420314B2 JP 2016507631 A JP2016507631 A JP 2016507631A JP 2016507631 A JP2016507631 A JP 2016507631A JP 6420314 B2 JP6420314 B2 JP 6420314B2
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glycine
pharmaceutical composition
compound
certain embodiments
obesity
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JP2016519106A5 (cg-RX-API-DMAC7.html
JP2016519106A (ja
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エス.ピーターソン ジョン
エス.ピーターソン ジョン
シャナハン ジェイムズ
シャナハン ジェイムズ
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シンデブルックス,インコーポレイティド
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/485Morphinan derivatives, e.g. morphine, codeine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/336Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/74Synthetic polymeric materials
    • A61K31/765Polymers containing oxygen
    • A61K31/77Polymers containing oxygen of oxiranes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06Tripeptides
    • AHUMAN NECESSITIES
    • 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
    • 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
    • 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
    • A61K47/56Medicinal 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
    • A61K47/58Medicinal 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
    • AHUMAN NECESSITIES
    • 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
    • A61K47/62Medicinal 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
    • A61K47/65Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Diabetes (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Child & Adolescent Psychology (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (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)
JP2016507631A 2013-04-10 2014-04-09 Metap2阻害剤及び肥満症の治療方法 Active JP6420314B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361810468P 2013-04-10 2013-04-10
US61/810,468 2013-04-10
US201461925918P 2014-01-10 2014-01-10
US61/925,918 2014-01-10
PCT/US2014/033476 WO2014169026A1 (en) 2013-04-10 2014-04-09 Metap2 inhibitors and methods of treating obesity

Related Child Applications (1)

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JP2018192578A Division JP2019023219A (ja) 2013-04-10 2018-10-11 Metap2阻害剤及び肥満症の治療方法

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JP2016519106A JP2016519106A (ja) 2016-06-30
JP2016519106A5 JP2016519106A5 (cg-RX-API-DMAC7.html) 2017-04-13
JP6420314B2 true JP6420314B2 (ja) 2018-11-07

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JP2016507631A Active JP6420314B2 (ja) 2013-04-10 2014-04-09 Metap2阻害剤及び肥満症の治療方法
JP2018192578A Pending JP2019023219A (ja) 2013-04-10 2018-10-11 Metap2阻害剤及び肥満症の治療方法
JP2021043481A Pending JP2021091738A (ja) 2013-04-10 2021-03-17 Metap2阻害剤及び肥満症の治療方法
JP2023061783A Active JP7681054B2 (ja) 2013-04-10 2023-04-05 Metap2阻害剤及び肥満症の治療方法
JP2025078682A Pending JP2025109807A (ja) 2013-04-10 2025-05-09 Metap2阻害剤及び肥満症の治療方法

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JP2021043481A Pending JP2021091738A (ja) 2013-04-10 2021-03-17 Metap2阻害剤及び肥満症の治療方法
JP2023061783A Active JP7681054B2 (ja) 2013-04-10 2023-04-05 Metap2阻害剤及び肥満症の治療方法
JP2025078682A Pending JP2025109807A (ja) 2013-04-10 2025-05-09 Metap2阻害剤及び肥満症の治療方法

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US (8) US9173956B2 (cg-RX-API-DMAC7.html)
EP (2) EP2984085B1 (cg-RX-API-DMAC7.html)
JP (5) JP6420314B2 (cg-RX-API-DMAC7.html)
CN (2) CN105431426A (cg-RX-API-DMAC7.html)
AU (1) AU2014250983B2 (cg-RX-API-DMAC7.html)
BR (1) BR112015025892A2 (cg-RX-API-DMAC7.html)
CA (1) CA2908993C (cg-RX-API-DMAC7.html)
DK (2) DK3574922T3 (cg-RX-API-DMAC7.html)
EA (1) EA033912B1 (cg-RX-API-DMAC7.html)
ES (2) ES2902082T3 (cg-RX-API-DMAC7.html)
MX (2) MX386958B (cg-RX-API-DMAC7.html)
WO (1) WO2014169026A1 (cg-RX-API-DMAC7.html)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103140512B (zh) * 2010-05-25 2017-03-01 辛德弗雷克斯公司 聚合物缀合的MetAP2抑制剂及其应用的治疗方法
US9895449B2 (en) 2010-05-25 2018-02-20 Syndevrx, Inc. Polymer-conjugated MetAP2 inhibitors, and therapeutic methods of use thereof
MX386958B (es) * 2013-04-10 2025-03-19 Syndevrx Inc Inhibidores de metionina aminopeptidasa-2 y métodos de tratamiento de la obesidad.
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
MX2018006904A (es) 2015-12-10 2018-08-24 Syndevrx Inc Derivados de fumagilol y polimorfos de los mismos.
MX2018008321A (es) * 2016-01-11 2018-09-21 Syndevrx Inc Tratamiento de tumores ocasionados por disfuncion metabolica.
AU2019366819C1 (en) 2018-10-26 2025-12-18 Syndevrx Inc. Biomarkers of MetAP2 inhibitors and applications thereof
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
WO2023156996A1 (en) * 2022-02-16 2023-08-24 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Metap2 inhibitors and uses thereof

Family Cites Families (61)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2803586A (en) 1953-06-29 1957-08-20 Abbott Lab ph control in production of fumagillin
GB8500209D0 (en) * 1985-01-04 1985-02-13 Ceskoslovenska Akademie Ved Synthetic polymeric drugs
SE8702550D0 (sv) * 1987-06-18 1987-06-18 Anders Grubb Cysteinproteashemmare
US5166172A (en) 1988-09-01 1992-11-24 Takeda Chemical Industries, Ltd. Fumagillol derivatives and pharmaceutical compositions thereof
US4997878A (en) 1988-12-29 1991-03-05 Exxon Research And Engineering Company Hydrophobically associating polymers containing dimethyl acrylamide functionality
US5258453A (en) 1992-01-21 1993-11-02 University Of Utah Drug delivery system for the simultaneous delivery of drugs activatable by enzymes and light
GB9320781D0 (en) 1993-10-08 1993-12-01 Erba Carlo Spa Polymer-bound camptothecin derivatives
US20030220233A1 (en) * 1994-01-24 2003-11-27 Neorx Corporation Radiolabeled annexins
TW409058B (en) 1996-06-06 2000-10-21 Daiichi Seiyaku Co Method for preparation of a drug complex
TW527183B (en) 1996-06-06 2003-04-11 Daiichi Seiyaku Co Drug complex
US6759509B1 (en) 1996-11-05 2004-07-06 Bristol-Myers Squibb Company Branched peptide linkers
AU9376998A (en) * 1997-09-02 1999-03-22 Johns Hopkins University School Of Medicine, The Vitamin d3 analog loaded polymer formulations for cancer and neurodegenerative disorders
CA2307792C (en) 1997-10-31 2007-06-26 Children's Medical Center Corporation Method for regulating size and growth of vascularized normal tissue
US6242494B1 (en) 1998-05-01 2001-06-05 Abbott Laboratories Substituted β-amino acid inhibitors of methionine aminopeptidase-2
KR100357542B1 (ko) 1998-05-15 2002-10-18 주식회사종근당 푸마질롤 유도체 및 그 제조방법
TWI253935B (en) 1998-05-22 2006-05-01 Daiichi Seiyaku Co Drug complex
US6464850B1 (en) 1998-07-31 2002-10-15 Biowhittaker Molecular Applications, Inc. Method for producing hydrophilic monomers and uses thereof
EP1619210A1 (en) 1998-10-30 2006-01-25 Daiichi Pharmaceutical Co., Ltd. DDS compounds and method for assaying the same
JP4883515B2 (ja) 1999-09-08 2012-02-22 ポリセリックス リミテッド 均一分子量ポリマー
US6811788B2 (en) 2000-01-19 2004-11-02 Baofa Yu Combinations and methods for treating neoplasms
US20020002152A1 (en) 2000-04-14 2002-01-03 Craig Richard A. Hydrazide and alkoxyamide angiogenesis inhibitors
US20070161570A1 (en) * 2000-11-01 2007-07-12 Praecis Pharmaceuticals, Inc. Methionine aminopeptidase-2 inhibitors and methods of use thereof
US6548477B1 (en) 2000-11-01 2003-04-15 Praecis Pharmaceuticals Inc. Therapeutic agents and methods of use thereof for the modulation of angiogenesis
EP1243276A1 (en) 2001-03-23 2002-09-25 Franciscus Marinus Hendrikus De Groot Elongated and multiple spacers containing activatible prodrugs
US7091186B2 (en) 2001-09-24 2006-08-15 Seattle Genetics, Inc. p-Amidobenzylethers in drug delivery agents
US7087768B2 (en) 2001-09-27 2006-08-08 Equispharm Co., Ltd. Fumagillol derivatives and preparing method thereof
WO2003070173A2 (en) 2002-02-15 2003-08-28 Sympore Gmbh Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof
EP1494662B1 (en) 2002-04-11 2012-11-28 Children's Medical Center Corporation Tnp-470-hpma-methacrylic acid copolymer conjugates and use thereof
US20040001801A1 (en) 2002-05-23 2004-01-01 Corvas International, Inc. Conjugates activated by cell surface proteases and therapeutic uses thereof
US7030262B2 (en) 2002-08-06 2006-04-18 Abbott Laboratories 3-Amino-2-hydroxyalkanoic acids and their prodrugs
US20040116348A1 (en) 2002-09-23 2004-06-17 Ying Chau Polymer-linker-drug conjugates for targeted drug delivery
US7491718B2 (en) 2002-10-08 2009-02-17 Abbott Laboratories Sulfonamides having antiangiogenic and anticancer activity
US20040228831A1 (en) * 2003-05-15 2004-11-18 Belinka Benjamin A. Polymeric conjugates for tissue activated drug delivery
EP2395112B1 (en) 2003-12-31 2017-02-15 The Penn State Research Foundation Methods for predicting and overcoming resistance to chemotherapy in ovarian cancer and for predicting colon cancer occurrence
US20070287680A1 (en) 2004-05-10 2007-12-13 University Of Utah Research Foundation Combined Active and Passive Targeting of Biologically Active Agents
US7214664B2 (en) 2004-12-03 2007-05-08 The Curators Of The University Of Missouri Peptidyl prodrugs that resist P-glycoprotein mediated drug efflux
US20100056623A1 (en) * 2005-01-26 2010-03-04 Chong Kun Dang Pharmaceutical Corp. Fumagillol derivatives or method for preparation of fumagillol derivatives, and pharmaceutical compositions comprising the same
WO2006084054A2 (en) 2005-02-02 2006-08-10 Children's Medical Center Corporation Method of treating angiogenic diseases
US7629315B2 (en) * 2005-03-09 2009-12-08 University Of Pittsburgh Of The Commonwealth System Of Higher Education Compositions for blocking the inhibitory effect of human CRP on human leptin
WO2006124711A1 (en) 2005-05-16 2006-11-23 The Board Of Trustees Of The University Of Illinois Composition and method for providing localized delivery of a therapeutic agent
JP2010531896A (ja) 2007-06-26 2010-09-30 チルドレンズ メディカル センター コーポレーション 治療的投与のためのMetAP−2阻害剤ポリマーソーム
WO2009036108A1 (en) * 2007-09-13 2009-03-19 Children's Medical Center Corporation Methods and compositions for inhibiting vascular leakage
US20090104210A1 (en) 2007-10-17 2009-04-23 Tota Michael R Peptide compounds for treating obesity and insulin resistance
AU2008331516B2 (en) 2007-11-28 2014-01-09 Mersana Therapeutics, Inc. Biocompatible biodegradable fumagillin analog conjugates
US8586019B2 (en) 2008-05-22 2013-11-19 Ramot At Tel-Aviv University Ltd. Conjugates of polymers having a therapeutically active agent and an angiogenesis targeting moiety attached thereto and uses thereof in the treatment of angiogenesis related diseases
DE102008027574A1 (de) 2008-06-10 2009-12-17 Merck Patent Gmbh Neue Pyrrolidinderivate als MetAP-2 Inhibitoren
US8642650B2 (en) 2008-12-04 2014-02-04 Zafgen, Inc. Methods of treating an overweight or obese subject
US20120004162A1 (en) * 2008-12-04 2012-01-05 Vath James E Methods of Treating an Overweight or Obese Subject
TWI373345B (en) 2009-02-19 2012-10-01 Academia Sinica Breast cancer-targeting peptides and use thereof
EP2493497A4 (en) 2009-11-01 2013-07-24 Brigham & Womens Hospital NOTCH INHIBITION IN THE TREATMENT AND PROPHYLAXIS OF ADIPOSITAS AND METABOLISM SYNDROME
WO2011127304A2 (en) * 2010-04-07 2011-10-13 Zafgen Corporation Methods of treating an overweight subject
US9895449B2 (en) 2010-05-25 2018-02-20 Syndevrx, Inc. Polymer-conjugated MetAP2 inhibitors, and therapeutic methods of use thereof
CN103140512B (zh) 2010-05-25 2017-03-01 辛德弗雷克斯公司 聚合物缀合的MetAP2抑制剂及其应用的治疗方法
WO2011150088A1 (en) 2010-05-25 2011-12-01 SynDevRX Optimized drug conjugates
PH12013500934A1 (en) 2010-11-09 2022-10-24 Zafgen Inc Crystalline solids of a metap-2 inhibitor and methods of making and using same
JP2013543899A (ja) * 2010-11-29 2013-12-09 ザフゲン,インコーポレイテッド 6−o−(4−ジメチルアミノエトキシ)シンナモイルフマギロールの非連日投与を用いた肥満の治療
CN103534244B (zh) * 2011-03-08 2016-10-12 扎夫根股份有限公司 氧杂螺[2.5]辛烷衍生物及类似物
MX386958B (es) 2013-04-10 2025-03-19 Syndevrx Inc Inhibidores de metionina aminopeptidasa-2 y métodos de tratamiento de la obesidad.
JP2018505152A (ja) 2014-12-23 2018-02-22 アン ブリンブル マーガレット アミノ酸複合体及びペプチド複合体ならびにそれらの使用
MX2018006904A (es) 2015-12-10 2018-08-24 Syndevrx Inc Derivados de fumagilol y polimorfos de los mismos.
MX2018008321A (es) 2016-01-11 2018-09-21 Syndevrx Inc Tratamiento de tumores ocasionados por disfuncion metabolica.

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EP3574922B1 (en) 2021-09-15
US20230048989A1 (en) 2023-02-16
DK2984085T3 (da) 2019-10-21
US20140308235A1 (en) 2014-10-16
MX386958B (es) 2025-03-19
JP7681054B2 (ja) 2025-05-21
US20150374657A1 (en) 2015-12-31
EP3574922A1 (en) 2019-12-04
US11304944B2 (en) 2022-04-19
US9433600B2 (en) 2016-09-06
EA033912B1 (ru) 2019-12-09
WO2014169026A1 (en) 2014-10-16
US20170028014A1 (en) 2017-02-02
US20160346244A1 (en) 2016-12-01
CN112494476A (zh) 2021-03-16
US10010544B2 (en) 2018-07-03
CA2908993C (en) 2023-05-23
HK1216313A1 (en) 2016-11-04
CN105431426A (zh) 2016-03-23
US20170326135A1 (en) 2017-11-16
BR112015025892A2 (pt) 2017-07-25
DK3574922T3 (da) 2021-12-06
MX2015014329A (es) 2016-06-21
MX371095B (es) 2020-01-16
US20180271856A1 (en) 2018-09-27
EA201591943A1 (ru) 2016-07-29
ES2902082T3 (es) 2022-03-24
US9757373B2 (en) 2017-09-12
US9173956B2 (en) 2015-11-03
US20200155545A1 (en) 2020-05-21
US10588904B2 (en) 2020-03-17
JP2023082195A (ja) 2023-06-13
EP2984085A4 (en) 2016-12-07
AU2014250983B2 (en) 2019-04-11
JP2016519106A (ja) 2016-06-30
JP2021091738A (ja) 2021-06-17
US9750737B2 (en) 2017-09-05
ES2749746T3 (es) 2020-03-23
CA2908993A1 (en) 2014-10-16
JP2025109807A (ja) 2025-07-25
EP2984085B1 (en) 2019-07-17
AU2014250983A1 (en) 2015-10-29
EP2984085A1 (en) 2016-02-17
JP2019023219A (ja) 2019-02-14

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