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
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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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds 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
    • A61K31/7064—Compounds 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
    • A61K31/7068—Compounds 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
    • 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
    • A61K47/545—Heterocyclic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/575—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/5758—Immunoassay; 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
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/90—Enzymes; Proenzymes
    • G01N2333/902—Oxidoreductases (1.)
    • G01N2333/90245—Oxidoreductases (1.) acting on paired donors with incorporation of molecular oxygen (1.14)
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2440/00—Post-translational modifications [PTMs] in chemical analysis of biological material
    • G01N2440/24—Post-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
PE20210367A1 (es) * 2018-02-02 2021-02-26 Maverix Oncology Inc Conjugados de farmacos de molecula pequena de monofosfato de gemcitabina

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
ZA859008B (en) 1984-12-04 1987-07-29 Lilly Co Eli The treatment of tumors in mammals
ATE92499T1 (de) 1984-12-04 1993-08-15 Lilly Co Eli Tumorbehandlung bei saeugetieren.
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
EP0418292A4 (en) 1988-05-25 1991-09-25 Research Corporation Technologies, Inc Phosphoramides useful as antitumor agents
DE3834860A1 (de) 1988-10-13 1990-04-19 Basf Ag Heterocyclisch substituierte alkoxycumarine, verfahren zu ihrer herstellung und diese enthaltende therapeutische mittel
DE3834861A1 (de) 1988-10-13 1990-04-19 Basf Ag Arylalkoxycumarine, 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
DK0702683T3 (da) 1993-06-08 2004-02-02 Cancer Rec Tech Ltd 06-substituerede guaninderivater, fremgangsmåde til fremstilling deraf og anvendelse deraf i behandling af tumorceller
DK0795334T3 (da) 1996-03-12 2006-06-06 Sanofi Aventis Deutschland Nye prodrugs til behandling af tumorer og betændelsessygdomme
WO1998011484A1 (fr) 1996-09-13 1998-03-19 Hitachi, Ltd. Processeur de commande a memoire d'historique
ATE236188T1 (de) 1997-01-24 2003-04-15 Conpharma As Gemcitabin-derivate
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
EP1051383B1 (en) 1998-02-06 2004-07-28 De Montfort University Hydroxylation activated prodrugs
AU2531599A (en) 1998-02-12 1999-08-30 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
YU68102A (sh) 2000-03-16 2006-01-16 F. Hoffmann-La Roche Ag. Derivati karboksilne kiseline kao ip antagonisti
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
UA75622C2 (en) 2000-12-08 2006-05-15 3M Innovative Properties Co Aryl ether substituted imidazoquinolines, pharmaceutical composition based thereon
BR0207795A (pt) 2001-03-02 2004-03-23 Hoffmann La Roche Derivados de ácido alcoxicarbonilamino benzóico ou alcoxicarbonilamino tetrazolil fenila como antagonistas de ip
CN1274948C (zh) 2001-05-18 2006-09-13 赫斯工程股份有限公司 用于制造催化式排气净化器的方法和装置
CA2459454A1 (en) 2001-09-14 2003-03-27 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
GB0123777D0 (en) 2001-10-03 2001-11-21 Cancer Res Ventures Ltd Substituted chalcones as therapeutic agents
GB0123780D0 (en) 2001-10-03 2001-11-21 Cancer Res Ventures Ltd Substituted chalcones as therapeutic agents
US7265096B2 (en) 2002-11-04 2007-09-04 Xenoport, Inc. Gemcitabine prodrugs, pharmaceutical compositions and uses thereof
EA012844B1 (ru) 2003-02-19 2009-12-30 Йельский Университет Аналоги противовирусных нуклеозидов и способы лечения вирусных инфекций, в частности вич-инфекций
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
WO2005061459A1 (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
EP3075247B1 (en) 2004-02-02 2022-10-12 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
KR100874052B1 (ko) 2004-12-17 2008-12-12 일라이 릴리 앤드 캄파니 젬시타빈의 아미드 전구약, 그의 조성물 및 그의 용도
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
CA2624726A1 (en) 2005-10-06 2007-04-12 Sanofi-Aventis 4-oxy-n-[1 ,3,4]-thiadiazol-2-yl-benzene sulfonamides, processes for their preparation and their use as pharmaceuticals
WO2007117760A2 (en) 2006-02-06 2007-10-18 Dr. Reddy's Laboratories Ltd. Preparation of gemcitabine
US20080182816A1 (en) 2006-02-23 2008-07-31 Tam Joemy C Methods for preparing a novel family of polysaccharride prodrugs for colonic delivery
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
TWI415858B (zh) 2007-11-06 2013-11-21 Pharmaessentia Corp β－核苷之新穎合成技術
GB0907551D0 (en) 2009-05-01 2009-06-10 Univ Dundee Treatment or prophylaxis of proliferative conditions
US9937128B2 (en) * 2009-08-03 2018-04-10 The University Of North Carolina At Chapel Hill Liposomes comprising a calcium phosphate-containing precipitate
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
US10000521B2 (en) * 2013-03-15 2018-06-19 Nucorion Pharmaceuticals, Inc. Substituted gemcitabine bicyclic amide analogs and treatment methods using same
WO2015134334A1 (en) * 2014-03-03 2015-09-11 Suo Zucai Gemcitabine analogs
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
US20210380626A1 (en) * 2018-02-02 2021-12-09 Maverix Oncology, Inc. Novel small molecule drug conjugates of gemcitabine derivatives
PE20210367A1 (es) * 2018-02-02 2021-02-26 Maverix Oncology Inc Conjugados de farmacos de molecula pequena de monofosfato de gemcitabina

Also Published As

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

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