MX2016014574A - El uso de compuestos de tienotriazolodiazepina para el tratamiento de cancer de mama triple-negativo. - Google Patents

El uso de compuestos de tienotriazolodiazepina para el tratamiento de cancer de mama triple-negativo.

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Publication number
MX2016014574A
MX2016014574A MX2016014574A MX2016014574A MX2016014574A MX 2016014574 A MX2016014574 A MX 2016014574A MX 2016014574 A MX2016014574 A MX 2016014574A MX 2016014574 A MX2016014574 A MX 2016014574A MX 2016014574 A MX2016014574 A MX 2016014574A
Authority
MX
Mexico
Prior art keywords
carbon number
alkyl
halogen atom
optionally substituted
integer
Prior art date
Application number
MX2016014574A
Other languages
English (en)
Inventor
Maurizio D'incalci
Noel Kay
Original Assignee
Oncoethix Gmbh
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 Oncoethix Gmbh filed Critical Oncoethix Gmbh
Publication of MX2016014574A publication Critical patent/MX2016014574A/es

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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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • 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
    • A61K31/337Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/55171,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1652Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4866Organic macromolecular compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/26Cyanate or isocyanate esters; Thiocyanate or isothiocyanate esters
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Un método de tratamiento de cáncer de mama triple negativo en un mamífero que comprende el paso de: administrar a un paciente una cantidad farmacéuticamente aceptable de un compuesto siendo un compuesto de tienotriazolodiazepina de la fórmula (1) (ver Fórmula) en donde R1 es alquilo que tiene un número de carbonos de 1 a 4, R2 es un átomo de hidrógeno; un átomo de halógeno; o alquilo que tiene un número de carbonos de 1 a 4 opcionalmente sustituido por un átomo de halógeno o un grupo hidroxilo, R3 es un átomo de halógeno; fenilo opcionalmente sustituido por un átomo de halógeno, alquilo que tiene un número de carbonos de 1 a 4, alcoxi que tiene un número de carbonos de 1 a 4 o ciano; -NR5- (CH2)m-R6, en donde R5 es un átomo de hidrógeno o alquilo que tiene un número de carbonos de 1 a 4, m es un número entero de 0-4, y R6 es fenilo o piridilo opcionalmente sustituido por un átomo de halógeno; o -NR7-CO- (CH2)n-R8 en donde R7 es un átomo de hidrógeno o alquilo que tiene un número de carbonos de 1 a 4, n es un número entero de 0 a 2, y R8 es fenilo o piridilo opcionalmente sustituido por un átomo de halógeno y R4 es (CH2)a-CO-NH-R9 en donde a es un número entero de 1-4, y R9 es alquilo que tiene un número de carbonos de 1 a 4; hidroxialquilo que tiene un número de carbonos de 1 a 4; alcoxi que tiene un número de carbonos de 1 a 4; o fenilo o piridilo opcionalmente sustituido con alquilo que tiene un número de carbonos de 1 a 4, alcoxi que tiene un número de carbonos de 1 a 4, amino o un grupo hidroxilo o -(CH2)b-COOR10, en donde b es un número entero de 1 a 4, y R10 es alquilo que tiene un número de carbonos de 1 a 4, o una sal farmacéuticamente aceptable del mismo o un hidrato o solvato del mismo, en combinación con uno o más fármacos de quimioterapia seleccionados del grupo que consiste en inhibidores de m-TOR e inhibidores de la mitosis.
MX2016014574A 2014-05-08 2015-05-08 El uso de compuestos de tienotriazolodiazepina para el tratamiento de cancer de mama triple-negativo. MX2016014574A (es)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201461990457P 2014-05-08 2014-05-08
US201462012048P 2014-06-13 2014-06-13
US201462080751P 2014-11-17 2014-11-17
US201462086400P 2014-12-02 2014-12-02
US201562150044P 2015-04-20 2015-04-20
PCT/EP2015/060200 WO2015169951A1 (en) 2014-05-08 2015-05-08 Method of treating triple-negative breast cancer using thienotriazolodiazepine compounds

Publications (1)

Publication Number Publication Date
MX2016014574A true MX2016014574A (es) 2017-02-23

Family

ID=53191652

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2016014574A MX2016014574A (es) 2014-05-08 2015-05-08 El uso de compuestos de tienotriazolodiazepina para el tratamiento de cancer de mama triple-negativo.

Country Status (11)

Country Link
US (1) US9968619B2 (es)
EP (1) EP3139959A1 (es)
JP (1) JP2017519727A (es)
KR (1) KR20170002610A (es)
CN (1) CN106852120A (es)
AU (1) AU2015257658A1 (es)
BR (1) BR112016026046A8 (es)
CA (1) CA2947970A1 (es)
MX (1) MX2016014574A (es)
RU (1) RU2016147946A (es)
WO (1) WO2015169951A1 (es)

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MX366703B (es) 2013-03-15 2019-07-22 Incyte Holdings Corp Heterociclos tricíclicos como inhibidores de la proteína bet.
WO2015006193A1 (en) 2013-07-08 2015-01-15 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
WO2015081203A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
UA119870C2 (uk) 2014-04-23 2019-08-27 Інсайт Корпорейшн 1H-ПІРОЛО[2,3-c]ПІРИДИН-7(6H)-ОНИ ТА ПІРАЗОЛО[3,4-c]ПІРИДИН-7(6H)-ОНИ ЯК ІНГІБІТОРИ БІЛКІВ BET
ES2855225T3 (es) 2014-09-15 2021-09-23 Incyte Corp Heterociclos tricíclicos para su uso como inhibidores de proteínas BET
TW201722966A (zh) 2015-10-29 2017-07-01 英塞特公司 Bet蛋白質抑制劑之非晶固體形式
AU2017281286B2 (en) 2016-06-20 2021-05-20 Incyte Corporation Crystalline solid forms of a bet inhibitor
EP4118431A1 (de) * 2020-03-12 2023-01-18 Heinrich-Heine-Universität Düsseldorf Inhibition von fkbp1a zur therapie des triple-negativen mammakarzinoms
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
AU2022289869A1 (en) 2021-06-08 2023-12-21 Poseidon Innovation, Llc Anticancer compounds

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EP2239264A4 (en) * 2007-12-28 2012-01-11 Mitsubishi Tanabe Pharma Corp ANTITUMORAL MEDIUM
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WO2012120151A1 (en) * 2011-03-10 2012-09-13 Institut National De La Sante Et De La Recherche Medicale (Inserm) Atip3 and biologically active fragments thereof for use in the treatment of cancer
MX2014015986A (es) 2012-06-25 2016-02-11 Oncoethix Gmbh Metodo para tratar linfoma utilizando compuestos de tienotriazolodiazepina.
AU2013284457A1 (en) * 2012-06-27 2015-01-22 The Curators Of The University Of Missouri Induction of estrogen receptor beta by cholesterol biosynthesis inhibitors and methods of treatment of cancer
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Also Published As

Publication number Publication date
CN106852120A (zh) 2017-06-13
RU2016147946A (ru) 2018-06-08
WO2015169951A1 (en) 2015-11-12
EP3139959A1 (en) 2017-03-15
AU2015257658A1 (en) 2016-11-10
CA2947970A1 (en) 2015-11-12
US20170065607A1 (en) 2017-03-09
BR112016026046A2 (pt) 2017-08-15
BR112016026046A8 (pt) 2021-07-20
US9968619B2 (en) 2018-05-15
JP2017519727A (ja) 2017-07-20
RU2016147946A3 (es) 2018-12-26
KR20170002610A (ko) 2017-01-06

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