JP2019515880A - 炭酸無水酵素ix阻害剤抱合体およびその使用 - Google Patents

炭酸無水酵素ix阻害剤抱合体およびその使用 Download PDF

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JP2019515880A
JP2019515880A JP2018549266A JP2018549266A JP2019515880A JP 2019515880 A JP2019515880 A JP 2019515880A JP 2018549266 A JP2018549266 A JP 2018549266A JP 2018549266 A JP2018549266 A JP 2018549266A JP 2019515880 A JP2019515880 A JP 2019515880A
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alkyl
alkenyl
alkynyl
conjugate
pharmaceutically acceptable
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JP2019515880A5 (https=
Inventor
クリストファー・ピー・リーモン
イオンチョ・アール・ヴラホフ
ジョナサン・エム・シリングフォード
ポール・ジェイ・クラインドル
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Endocyte Inc
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Endocyte Inc
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    • 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
    • A61K47/545Heterocyclic compounds
    • 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
    • A61K38/07Tetrapeptides
    • 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
    • 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
    • A61P35/00Antineoplastic agents
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    • C12Q1/00Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/527Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving lyase
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5091Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing the pathological state of an organism
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/575Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/58Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving labelled substances
    • G01N33/582Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving labelled substances with fluorescent label
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    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06043Leu-amino acid
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    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06104Dipeptides with the first amino acid being acidic
    • C07K5/06113Asp- or Asn-amino acid
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    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • C07K5/06165Dipeptides with the first amino acid being heterocyclic and Pro-amino acid; Derivatives thereof
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    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0819Tripeptides with the first amino acid being acidic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10Tetrapeptides
    • C07K5/1021Tetrapeptides with the first amino acid being acidic
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00Detection or diagnosis of diseases
    • G01N2800/70Mechanisms involved in disease identification
    • G01N2800/7023(Hyper)proliferation
    • G01N2800/7028Cancer

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  • Chemical & Material Sciences (AREA)
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  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Immunology (AREA)
  • Biochemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
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  • Genetics & Genomics (AREA)
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  • Urology & Nephrology (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Analytical Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • General Physics & Mathematics (AREA)
  • Cell Biology (AREA)
  • Food Science & Technology (AREA)
  • Pathology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Wood Science & Technology (AREA)
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  • Gastroenterology & Hepatology (AREA)
  • General Engineering & Computer Science (AREA)
  • Tropical Medicine & Parasitology (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP2018549266A 2016-03-16 2017-03-16 炭酸無水酵素ix阻害剤抱合体およびその使用 Pending JP2019515880A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662309271P 2016-03-16 2016-03-16
US62/309,271 2016-03-16
PCT/US2017/022755 WO2017161144A1 (en) 2016-03-16 2017-03-16 Carbonic anhydrase ix inhibitor conjugates and uses thereof

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JP2019515880A true JP2019515880A (ja) 2019-06-13
JP2019515880A5 JP2019515880A5 (https=) 2020-04-23

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US (1) US10857234B2 (https=)
EP (1) EP3429637A4 (https=)
JP (1) JP2019515880A (https=)
CA (1) CA3017211A1 (https=)
WO (1) WO2017161144A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019512511A (ja) * 2016-03-16 2019-05-16 パーデュー・リサーチ・ファウンデイションPurdue Research Foundation 炭酸無水酵素ixを標的とする薬剤および方法

Families Citing this family (4)

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Publication number Priority date Publication date Assignee Title
CN112312901B (zh) 2018-05-10 2024-05-14 路易斯维尔大学研究基金会有限公司 Ras癌蛋白抑制剂及其制备方法和使用方法
KR20240069480A (ko) * 2022-11-11 2024-05-20 울산과학기술원 자가조립 가능한 펩타이드 분자를 포함하는 양친매성 접합체 및 이의 용도
EP4619037A1 (en) * 2022-11-17 2025-09-24 Hans-Georg Lerchen Small molecule-drug-conjugates cleavable in a tumor microenvironment
WO2025044924A1 (zh) * 2023-08-25 2025-03-06 无锡诺宇医药科技有限公司 靶向碳酸酐酶放射性药物

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008101231A2 (en) * 2007-02-16 2008-08-21 Endocyte, Inc. Methods and compositions for treating and diagnosing kidney disease
JP2014520076A (ja) * 2011-05-09 2014-08-21 ビセン メディカル, インコーポレイテッド 炭酸脱水酵素標的化剤およびそれの使用方法
WO2014134543A1 (en) * 2013-03-01 2014-09-04 Endocyte, Inc. Processes for preparing tubulysins

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2260875T3 (da) 2002-05-06 2014-06-30 Endocyte Inc Folatreceptor-targetede billeddannelsesmidler
AU2006279304A1 (en) * 2005-08-19 2007-02-22 Endocyte, Inc. Multi-drug ligand conjugates
US20090043099A1 (en) 2006-03-17 2009-02-12 The Burnham Institute Methods and compositions for derepression of IAP-inhibited caspase
BRPI0812970A2 (pt) 2007-06-25 2019-09-24 Endocyte Inc conjugados contendo espaçadores hidrofílicos
EP4464384A3 (en) 2007-08-17 2025-01-08 Purdue Research Foundation Psma binding ligand-linker conjugates and methods for using
CA2711678A1 (en) * 2008-01-09 2009-07-16 Molecular Insight Pharmaceuticals, Inc. Inhibitors of carbonic anhydrase ix
WO2010087994A2 (en) 2009-01-30 2010-08-05 Whitehead Institute For Biomedical Research Methods for ligation and uses thereof
CN101596433B (zh) 2009-07-15 2011-07-06 中国科学院工程热物理研究所 U形返料器的冷却式隔板
FR2951449B1 (fr) 2009-10-15 2011-11-25 Commissariat Energie Atomique Procede de fonctionnalisation de molecules biologiques
US8547533B2 (en) 2009-12-28 2013-10-01 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Composite probes and use thereof in super resolution methods
US20130053392A1 (en) 2010-02-12 2013-02-28 Peter Ebbesen Carbonic anhydrase inhibitors
JP5544239B2 (ja) 2010-07-29 2014-07-09 富士フイルム株式会社 重合性組成物
AU2012296937B2 (en) 2011-08-17 2017-10-12 Merck & Cie Folate conjugates of albumin-binding entities
WO2015113760A1 (en) 2014-01-28 2015-08-06 Tube Pharmaceuticals Gmbh Cytotoxic tubulysin compounds for conjugation
US9771380B2 (en) 2014-06-09 2017-09-26 University Of Oregon Gold nanoparticles and methods of making and using gold nanoparticles
CA3017214A1 (en) * 2016-03-16 2017-09-21 Purdue Research Foundation Carbonic anhydrase ix targeting agents and methods
JP7282521B2 (ja) * 2016-04-08 2023-05-29 パーデュー・リサーチ・ファウンデイション Car t細胞療法のための方法および組成物

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008101231A2 (en) * 2007-02-16 2008-08-21 Endocyte, Inc. Methods and compositions for treating and diagnosing kidney disease
JP2014520076A (ja) * 2011-05-09 2014-08-21 ビセン メディカル, インコーポレイテッド 炭酸脱水酵素標的化剤およびそれの使用方法
WO2014134543A1 (en) * 2013-03-01 2014-09-04 Endocyte, Inc. Processes for preparing tubulysins

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
AHLSKOG, JULIA K. J. ET AL.: "In vivo targeting of tumor-associated carbonic anhydrases using acetazolamide derivatives", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 19(16),, JPN6021006782, 2009, pages 4851 - 4856, ISSN: 0004454107 *
CECCHI, ALESSANDRO ET AL.: "Carbonic Anhydrase Inhibitors. Design of Fluorescent Sulfonamides as Probes of Tumor-Associated Carb", JOURNAL OF MEDICINAL CHEMISTRY, vol. 48(15),, JPN6021006781, 2005, pages 4834 - 4841, ISSN: 0004454106 *
CECCHI, ALESSANDRO ET AL.: "Carbonic anhydrase inhibitors: synthesis and inhibition ofcytosolic/tumor-associated carbonic anhydr", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 14(23),, JPN6021006784, 2004, pages 5775 - 5780, ISSN: 0004454108 *
KRALL, NIKOLAUS ET AL.: "A small-molecule drug conjugate for the treatment of carbonic anhydrase IX expressing tumors", ANGEWANDTE CHEMIE, INTERNATIONAL EDITION, vol. 53(16),, JPN6021006777, 2014, pages 4231 - 4235, ISSN: 0004607945 *
RAMI, MAROUAN ET AL.: "Carbonic anhydrase inhibitors: Copper(II) complexes ofpolyamino-polycarboxylamido aromatic/heterocyc", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 18(2),, JPN6021006779, 2008, pages 836 - 841, ISSN: 0004607946 *
WICHERT, MORENO ET AL.: "Dual-display of small molecules enables the discovery of ligand pairs and facilitates affinity matur", NATURE CHEMISTRY, vol. 7(3),, JPN6021006780, 2015, pages 241 - 249, ISSN: 0004607947 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019512511A (ja) * 2016-03-16 2019-05-16 パーデュー・リサーチ・ファウンデイションPurdue Research Foundation 炭酸無水酵素ixを標的とする薬剤および方法
JP7027325B2 (ja) 2016-03-16 2022-03-01 パーデュー・リサーチ・ファウンデイション 炭酸無水酵素ixを標的とする薬剤および方法

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EP3429637A4 (en) 2020-03-11
US10857234B2 (en) 2020-12-08
WO2017161144A1 (en) 2017-09-21
EP3429637A1 (en) 2019-01-23
US20190083631A1 (en) 2019-03-21
CA3017211A1 (en) 2017-09-21

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