AU2019216531A1 - Small molecule drug conjugates of gemcitabine monophosphate - Google Patents

Small molecule drug conjugates of gemcitabine monophosphate Download PDF

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Publication number
AU2019216531A1
AU2019216531A1 AU2019216531A AU2019216531A AU2019216531A1 AU 2019216531 A1 AU2019216531 A1 AU 2019216531A1 AU 2019216531 A AU2019216531 A AU 2019216531A AU 2019216531 A AU2019216531 A AU 2019216531A AU 2019216531 A1 AU2019216531 A1 AU 2019216531A1
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AU
Australia
Prior art keywords
compound
int
halo
ester
pharmaceutically acceptable
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
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AU2019216531A
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English (en)
Inventor
Craig Alan Coburn
Steven Albert Everett
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Maverix Oncology Inc
Original Assignee
Maverix Oncology Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Maverix Oncology Inc filed Critical Maverix Oncology Inc
Publication of AU2019216531A1 publication Critical patent/AU2019216531A1/en
Abandoned legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06Pyrimidine radicals
    • C07H19/10Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic 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
    • A61K47/54Medicinal 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • G01N33/5758Immunoassay; Biospecific binding assay; Materials therefor for cancer involving compounds serving as markers for tumours, cancers or neoplasias, e.g. cellular determinants, receptors, heat shock/stress proteins, A-protein, oligosaccharides or metabolites
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/90Enzymes; Proenzymes
    • G01N2333/902Oxidoreductases (1.)
    • G01N2333/90245Oxidoreductases (1.) acting on paired donors with incorporation of molecular oxygen (1.14)
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2440/00Post-translational modifications [PTMs] in chemical analysis of biological material
    • G01N2440/24Post-translational modifications [PTMs] in chemical analysis of biological material hydroxylation

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Genetics & Genomics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cell Biology (AREA)
  • Food Science & Technology (AREA)
  • Pathology (AREA)
  • Physics & Mathematics (AREA)
  • Microbiology (AREA)
  • Analytical Chemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
AU2019216531A 2018-02-02 2019-02-04 Small molecule drug conjugates of gemcitabine monophosphate Abandoned AU2019216531A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862625820P 2018-02-02 2018-02-02
US62/625,820 2018-02-02
PCT/US2019/016557 WO2019152955A1 (en) 2018-02-02 2019-02-04 Small molecule drug conjugates of gemcitabine monophosphate

Publications (1)

Publication Number Publication Date
AU2019216531A1 true AU2019216531A1 (en) 2020-09-24

Family

ID=65494554

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2019216531A Abandoned AU2019216531A1 (en) 2018-02-02 2019-02-04 Small molecule drug conjugates of gemcitabine monophosphate

Country Status (17)

Country Link
US (1) US11760773B2 (https=)
EP (1) EP3746134A1 (https=)
JP (2) JP2021512953A (https=)
KR (1) KR20200118827A (https=)
CN (1) CN112135634A (https=)
AU (1) AU2019216531A1 (https=)
BR (1) BR112020015745A2 (https=)
CA (1) CA3091027A1 (https=)
CL (1) CL2020002022A1 (https=)
CO (1) CO2020010970A2 (https=)
EA (1) EA202091856A1 (https=)
IL (1) IL276436A (https=)
MX (1) MX2020008188A (https=)
PE (1) PE20210367A1 (https=)
PH (1) PH12020551182A1 (https=)
SG (1) SG11202007386RA (https=)
WO (1) WO2019152955A1 (https=)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2019216531A1 (en) * 2018-02-02 2020-09-24 Maverix Oncology, Inc. Small molecule drug conjugates of gemcitabine monophosphate

Family Cites Families (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SU389090A1 (ru) 1971-05-17 1973-07-05 Ташкентский государственный медицинский институт Библиотека
US4526988A (en) 1983-03-10 1985-07-02 Eli Lilly And Company Difluoro antivirals and intermediate therefor
US5229272A (en) 1989-04-25 1993-07-20 Igen, Inc. Catalytic antibody components
EP0184365B1 (en) 1984-12-04 1993-08-04 Eli Lilly And Company Improvements in the treatment of tumors in mammals
ZA859008B (en) 1984-12-04 1987-07-29 Lilly Co Eli The treatment of tumors in mammals
DE3786834T2 (de) 1986-04-30 1994-03-03 Otsuka Pharma Co Ltd 5-Fluoro-Uracil-Derivate.
US6702705B1 (en) 1988-05-04 2004-03-09 Igen International, Inc. Prodrugs activated by targeted catalytic proteins
JPH04501253A (ja) 1988-05-25 1992-03-05 リサーチ コーポレーシヨン テクノロジーズ インコーポレーテツド 抗腫瘍剤として有用なホスホラミド
DE3834861A1 (de) 1988-10-13 1990-04-19 Basf Ag Arylalkoxycumarine, verfahren zu ihrer herstellung und diese enthaltende therapeutische mittel
DE3834860A1 (de) 1988-10-13 1990-04-19 Basf Ag Heterocyclisch substituierte alkoxycumarine, verfahren zu ihrer herstellung und diese enthaltende therapeutische mittel
US6258360B1 (en) 1989-05-04 2001-07-10 Igen International, Inc. Prodrugs activated by targeted catalytic proteins
US6060592A (en) 1990-01-11 2000-05-09 Isis Pharmaceuticals, Inc. Pyrimidine nucleoside compounds and oligonucleoside compounds containing same
US5401838A (en) 1992-06-22 1995-03-28 Eli Lilly And Company Stereoselective fusion glycosylation process for preparing 2'-deoxy-2',2'-difluoronucleosides and 2'-deoxy-2'-fluoronucleosides
HU217779B (hu) 1993-06-08 2000-04-28 Cancer Research Campaign Technology Limited O6-Helyettesített guaninszármazékok, ezeket tartalmazó gyógyászati készítmények, valamint eljárás e vegyületek előállítására
EP0795334B1 (de) 1996-03-12 2006-02-01 Sanofi-Aventis Deutschland GmbH Neuartige Prodrugs für die Therapie von Tumoren und entzündlichen Erkrankungen
WO1998011484A1 (fr) 1996-09-13 1998-03-19 Hitachi, Ltd. Processeur de commande a memoire d'historique
CA2278056C (en) 1997-01-24 2006-12-12 Norsk Hydro Asa Gemcitabine derivatives
NZ330360A (en) 1997-06-02 1999-03-29 Hoffmann La Roche 5'-deoxy-cytidine derivatives, their manufacture and use as antitumoral agents
TW434252B (en) 1997-07-23 2001-05-16 Univ Georgia Res Found Process for the preparation of 2'-fluoro-5-methyl-β-L-arabino-furanosyluridine
JP4642226B2 (ja) 1998-02-06 2011-03-02 デ モントフォート ユニヴァーシティ ヒドロキシル化により活性化されたプロドラッグ
WO1999040944A2 (en) 1998-02-12 1999-08-19 De Montfort University Hydroxylation activated drug release
DE19834751A1 (de) 1998-08-01 2000-02-03 Boehringer Ingelheim Pharma Disubstituierte bicyclische Heterocyclen, ihre Herstellung und ihre Verwendung als Arzneimittel
US6175001B1 (en) 1998-10-16 2001-01-16 The Scripps Research Institute Functionalized pyrimidine nucleosides and nucleotides and DNA's incorporating same
KR100523119B1 (ko) 2000-03-16 2005-10-20 에프. 호프만-라 로슈 아게 Ip 길항제로서의 카복실산 유도체
GB0007401D0 (en) 2000-03-27 2000-05-17 Cancer Res Campaign Tech Substituted chalcones as therapeeutic compounds
US6875751B2 (en) 2000-06-15 2005-04-05 Idenix Pharmaceuticals, Inc. 3′-prodrugs of 2′-deoxy-β-L-nucleosides
US7115585B2 (en) 2000-08-21 2006-10-03 Inspire Pharmaceuticals, Inc. Compositions for treating epithelial and retinal tissue diseases
JP3692927B2 (ja) 2000-11-07 2005-09-07 日本電気株式会社 ファクシミリ装置
UA74852C2 (en) 2000-12-08 2006-02-15 3M Innovative Properties Co Urea-substituted imidazoquinoline ethers
CA2438737A1 (en) 2001-03-02 2002-09-12 F. Hoffmann-La Roche Ag Alkoxycarbonylamino benzoic acid or alkoxycarbonylamino tetrazolyl phenyl derivatives as ip antagonists
ATE302898T1 (de) 2001-05-18 2005-09-15 Hess Eng Inc Verfahren und vorrichtung zur herstellung eines katalysators
US6780859B2 (en) 2001-09-14 2004-08-24 Bayer Pharmaceuticals Corporation Benzofuran and dihydrobenzofuran derivatives useful as beta-3 adrenoreceptor agonists
EP1300403A1 (en) 2001-10-02 2003-04-09 Aventis Pharma S.A. Process for the manufacture of hypoxyxylerone derivatives
GB0123780D0 (en) 2001-10-03 2001-11-21 Cancer Res Ventures Ltd Substituted chalcones as therapeutic agents
GB0123777D0 (en) 2001-10-03 2001-11-21 Cancer Res Ventures Ltd Substituted chalcones as therapeutic agents
WO2004041203A2 (en) 2002-11-04 2004-05-21 Xenoport, Inc. Gemcitabine prodrugs, pharmaceutical compositions and uses thereof
CN102174038A (zh) 2003-02-19 2011-09-07 耶鲁大学 用于治疗病毒感染的抗病毒核苷
US7148226B2 (en) 2003-02-21 2006-12-12 Agouron Pharmaceuticals, Inc. Inhibitors of hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments using the same
ZA200507752B (en) 2003-03-28 2007-01-31 Threshold Pharmaceuticals Inc Compositions and methods for treating cancer
GB0317009D0 (en) 2003-07-21 2003-08-27 Univ Cardiff Chemical compounds
CA2548513A1 (en) 2003-12-04 2005-07-07 Wyeth Biaryl sulfonamides and methods for using same
CA2550299C (en) 2003-12-22 2010-03-30 Christopher R. Roberts Process for fluorocytidine derivatives
WO2005072061A2 (en) 2004-02-02 2005-08-11 Biosight Ltd. Conjugates for cancer therapy and diagnosis
US8026366B2 (en) 2004-06-18 2011-09-27 3M Innovative Properties Company Aryloxy and arylalkyleneoxy substituted thiazoloquinolines and thiazolonaphthyridines
GB0421294D0 (en) 2004-09-24 2004-10-27 Angiogene Pharm Ltd Bioreductively-activated prodrugs
CA2589850C (en) 2004-12-17 2012-05-01 Eli Lilly And Company Amide prodrug of gemcitabine, compositions and use thereof
EP1676834A1 (en) 2004-12-30 2006-07-05 Sanofi-Aventis Deutschland GmbH Fused bicyclic carboxamide derivates for use as CXCR2 inhibitors in the treatment of inflammation
NO322682B1 (no) 2005-03-18 2006-11-27 Clavis Pharma Asa Anvendelse av gemcitabinderivater for fremstilling av orale doseringsformer ved kreftbehandling, samt slike orale doseringsformer
EP1937658A1 (en) 2005-10-06 2008-07-02 Sanofi-Aventis 4-oxy-n-[1 ,3,4]-thiadiazol-2-yl-benzene sulfonamides, processes for their preparation and their use as pharmaceuticals
US20090069557A1 (en) 2006-02-06 2009-03-12 Dr. Reddy's Laboratories Ltd. Preparation of gemcitabine
US20080004237A1 (en) 2006-02-23 2008-01-03 Tam Joemy C Polysacchocride prodrug of 5-fluorouracil (5-FU) with enhanced target specificity for galectin-3 expressing cancers
US20070225248A1 (en) 2006-03-21 2007-09-27 Clavis Pharma As Oral dosage forms of gemcitabine derivatives
GB0722769D0 (en) 2007-11-21 2008-01-02 Biolipox Ab New compounds
EP2136626A4 (en) 2007-03-19 2011-02-23 Oregon State Mannich base n-oxide drugs
CN100475832C (zh) 2007-05-31 2009-04-08 南京卡文迪许生物工程技术有限公司 一种新颖的高立体选择性合成吉西他滨工艺及中间体
JO2778B1 (en) 2007-10-16 2014-03-15 ايساي انك Certain Compounds, Compositions and Methods
KR20100102107A (ko) 2007-11-06 2010-09-20 파마이센시아 코퍼레이션 β-뉴클레오시드의 새로운 합성 방법
GB0907551D0 (en) 2009-05-01 2009-06-10 Univ Dundee Treatment or prophylaxis of proliferative conditions
WO2011017297A2 (en) * 2009-08-03 2011-02-10 The University Of North Carolina At Chapel Hill Biodegradable delivery system complexes for the delivery of bioactive compounds
US20130131008A1 (en) 2011-10-25 2013-05-23 Board Of Regents, The University Of Texas System Lipophilic monophosphorylated derivatives and nanoparticles
CN104955458A (zh) 2012-11-07 2015-09-30 Z·索 取代的吉西他滨芳基酰胺类似物和使用所述类似物的治疗方法
WO2014145207A1 (en) * 2013-03-15 2014-09-18 Ohio State Innovation Foundation Substituted gemcitabine bicyclic amide analogs and treatment methods using same
CN106459130A (zh) * 2014-03-03 2017-02-22 纽科利制药公司 吉西他滨类似物
CN105001291B (zh) 2014-04-15 2018-12-04 上海知萌生物医药科技有限公司 吉西他滨化学传递前药及其制备方法和应用
CN105001191A (zh) * 2015-07-23 2015-10-28 广西师范学院 具有5,2’-二羟基-4’-甲氧基-3-香叶基黄酮骨架的衍生物及其制备方法和用途
CA3090272A1 (en) * 2018-02-02 2019-08-08 Maverix Oncology, Inc. Novel small molecule drug conjugates of gemcitabine derivatives
AU2019216531A1 (en) * 2018-02-02 2020-09-24 Maverix Oncology, Inc. Small molecule drug conjugates of gemcitabine monophosphate

Also Published As

Publication number Publication date
CN112135634A (zh) 2020-12-25
SG11202007386RA (en) 2020-08-28
BR112020015745A2 (pt) 2020-12-08
PE20210367A1 (es) 2021-02-26
PH12020551182A1 (en) 2021-05-10
MX2020008188A (es) 2020-11-18
US20210040136A1 (en) 2021-02-11
EA202091856A1 (ru) 2020-12-07
CO2020010970A2 (es) 2020-11-20
JP2021512953A (ja) 2021-05-20
EP3746134A1 (en) 2020-12-09
US11760773B2 (en) 2023-09-19
CL2020002022A1 (es) 2021-02-12
IL276436A (en) 2020-09-30
WO2019152955A9 (en) 2020-08-13
WO2019152955A1 (en) 2019-08-08
JP2024054873A (ja) 2024-04-17
CA3091027A1 (en) 2019-08-08
KR20200118827A (ko) 2020-10-16

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