IN2014DN08886A - - Google Patents

Info

Publication number
IN2014DN08886A
IN2014DN08886A IN8886DEN2014A IN2014DN08886A IN 2014DN08886 A IN2014DN08886 A IN 2014DN08886A IN 8886DEN2014 A IN8886DEN2014 A IN 8886DEN2014A IN 2014DN08886 A IN2014DN08886 A IN 2014DN08886A
Authority
IN
India
Prior art keywords
compound
pyridyn
pfkfb3
quinolin
prop
Prior art date
Application number
Inventor
Pooran Chand
Gilles H Tapolsky
Original Assignee
Advanced Cancer Therapeutics Llc
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 Advanced Cancer Therapeutics Llc filed Critical Advanced Cancer Therapeutics Llc
Publication of IN2014DN08886A publication Critical patent/IN2014DN08886A/en

Links

Classifications

    • 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
    • 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
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/40—Cyclodextrins; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Inorganic Chemistry (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

A novel compound, (E)- 1 -(pyridyn-4-yl)-3-(7-(trifluoromethyl)quinolin-2-y1)- 5 prop-2-en- 1 -one, is provided herein: 0 (E)- 1 -(pyridyn-4-y1)-3 -(7-(trifluoromethyl)quinolin-2-1-prop-en- 1 -one is an inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-biphosphata3se ( PFKFB3) with surprisingly superior efficacy and pharmacodynamic properties in vitro and in vivo. Also provided 10 are pharmaceutical compositions including the compound and methods of use of the compound in treating cancer and tumors in vivo, as well as inhibiting glycolytic flux and PFKFB3 enzymatic activity in cells.
IN8886DEN2014 2012-03-29 2013-03-14 IN2014DN08886A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261617073P 2012-03-29 2012-03-29
PCT/US2013/031159 WO2013148228A1 (en) 2012-03-29 2013-03-14 Pfkfb3 inhibitor and methods of use as an anti-cancer therapeutic

Publications (1)

Publication Number Publication Date
IN2014DN08886A true IN2014DN08886A (en) 2015-05-22

Family

ID=49261041

Family Applications (1)

Application Number Title Priority Date Filing Date
IN8886DEN2014 IN2014DN08886A (en) 2012-03-29 2013-03-14

Country Status (9)

Country Link
US (2) US9649305B2 (en)
EP (1) EP2831047B1 (en)
JP (1) JP6075903B2 (en)
CN (2) CN104520274B (en)
AU (1) AU2013240340B2 (en)
CA (1) CA2868787A1 (en)
ES (1) ES2629932T3 (en)
IN (1) IN2014DN08886A (en)
WO (1) WO2013148228A1 (en)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MA41044A (en) 2014-10-08 2017-08-15 Novartis Ag COMPOSITIONS AND METHODS OF USE FOR INCREASED IMMUNE RESPONSE AND CANCER TREATMENT
EP4245376A3 (en) 2014-10-14 2023-12-13 Novartis AG Antibody molecules to pd-l1 and uses thereof
US20180148429A1 (en) * 2015-05-13 2018-05-31 Selvita S.A. Substituted quinoxaline derivatives
WO2016191660A1 (en) * 2015-05-28 2016-12-01 University Of Louisville Research Foundation, Inc. Combinations of pfkfb3 inhibitors and immune checkpoint inhibitors to treat cancer
EP3328418A1 (en) 2015-07-29 2018-06-06 Novartis AG Combination therapies comprising antibody molecules to pd-1
LT3317301T (en) 2015-07-29 2021-07-26 Novartis Ag Combination therapies comprising antibody molecules to lag-3
US20180207273A1 (en) 2015-07-29 2018-07-26 Novartis Ag Combination therapies comprising antibody molecules to tim-3
MX2018007423A (en) 2015-12-17 2018-11-09 Novartis Ag Antibody molecules to pd-1 and uses thereof.
AU2017357488A1 (en) * 2016-11-08 2019-06-20 Merck Patent Gmbh Substituted quinoxaline derivatives as inhibitors of PFKFB
CN109136206B (en) * 2017-06-15 2021-07-23 厦门大学 Phosphorylation of 194 th tyrosine of PFKFB3 protein and application thereof
CN109134434B (en) * 2017-11-06 2021-02-19 北京大学深圳研究生院 Quinoline or quinazoline compound and preparation method and application thereof
JP2022544098A (en) * 2019-08-06 2022-10-17 ザ ユニバーシティ オブ ノース カロライナ アット チャペル ヒル RNA-targeting ligands, compositions thereof, and methods of making and using the same
CN111228265A (en) * 2020-02-10 2020-06-05 中山大学肿瘤防治中心（中山大学附属肿瘤医院、中山大学肿瘤研究所） Application of p38 gamma inhibitor in preparation of medicine for treating pancreatic cancer
KR102344676B1 (en) * 2020-02-12 2021-12-30 한국과학기술연구원 Novel compounds useful as near infrared fluorescent probes selectively binding to tau aggregates and preparation method thereof
CN111996247B (en) * 2020-08-27 2021-09-10 北京大学人民医院 Glycolysis inhibitor and application thereof in repairing endothelial cell injury
CN114617884B (en) * 2020-12-10 2023-06-02 中国科学院大连化学物理研究所 Application of PFK-158 in preparation of anti-coronavirus medicament and medicament
WO2023147161A2 (en) * 2022-01-31 2023-08-03 New Frontier Bio, Inc. Nicotinate and nicotinamide riboside-based compounds and derivatives thereof

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7034013B2 (en) * 2001-03-20 2006-04-25 Cydex, Inc. Formulations containing propofol and a sulfoalkyl ether cyclodextrin
CN1182846C (en) * 2003-03-14 2005-01-05 南开大学 Water soluble anticancer medicine taxol composite and its prepn
CN1554336A (en) * 2003-12-23 2004-12-15 广州国桥医药研究有限公司 Process for preparing water soluble arteannuin preparation
KR100825492B1 (en) * 2004-04-12 2008-04-28 토렌트 파마슈티칼스 리미티드 2-propene-1-ones as hsp 70 inducers
CN101020060A (en) * 2007-03-10 2007-08-22 杨喜鸿 Cyclodextrin clathrate of entecavir and its prepn proces and medicinal application
WO2008156783A2 (en) * 2007-06-18 2008-12-24 University Of Louisville Research Foundation, Inc. Family of pfkfb3 inhibitors with anti-neoplastic activities
US8916711B2 (en) * 2009-10-13 2014-12-23 Council Of Scientific And Industrial Research Imidazothiazole-chalcone derivatives as potential anticancer agents and process for the preparation thereof
CN102000080A (en) * 2010-09-21 2011-04-06 江苏先声药物研究有限公司 Method for solubilizing camptothecin compound

Also Published As

Publication number Publication date
AU2013240340B2 (en) 2016-11-10
CN104520274A (en) 2015-04-15
AU2013240340A1 (en) 2014-10-23
WO2013148228A1 (en) 2013-10-03
CN106074368B (en) 2019-01-22
EP2831047A4 (en) 2015-09-02
JP6075903B2 (en) 2017-02-08
CN106074368A (en) 2016-11-09
US10010542B2 (en) 2018-07-03
CN104520274B (en) 2016-08-24
US20170258783A1 (en) 2017-09-14
EP2831047A1 (en) 2015-02-04
JP2015512398A (en) 2015-04-27
EP2831047B1 (en) 2017-05-03
CA2868787A1 (en) 2013-10-03
US20150064175A1 (en) 2015-03-05
US9649305B2 (en) 2017-05-16
ES2629932T3 (en) 2017-08-16

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