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.

Info

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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    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic 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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic 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
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436—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 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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic 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
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • A61K9/141—Intimate 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
    • A61K9/146—Intimate 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
    • 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
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/26—Cyanate or isocyanate esters; Thiocyanate or isothiocyanate esters
    • 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
    • A61K31/55—Heterocyclic 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)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Nutrition Science (AREA)
  • Physiology (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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EP2970282B1 (en) 2013-03-15 2019-08-21 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
ES2635560T3 (es) 2013-07-08 2017-10-04 Incyte Holdings Corporation Heterociclos tricíclicos como inhibidores de la proteína NET
US9399640B2 (en) 2013-11-26 2016-07-26 Incyte Corporation Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors
WO2015081189A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
CN106414442B (zh) 2014-04-23 2019-03-15 因赛特公司 作为BET蛋白抑制剂的1H-吡咯并[2,3-c]吡啶-7(6H)-酮和吡唑并[3,4-c]吡啶-7(6H)-酮
TWI712603B (zh) 2014-09-15 2020-12-11 美商英塞特公司 作為ｂｅｔ蛋白抑制劑之三環雜環
AR106520A1 (es) 2015-10-29 2018-01-24 Incyte Corp Forma sólida amorfa de un inhibidor de proteína bet
PE20190623A1 (es) 2016-06-20 2019-04-26 Incyte Corp Formas solidas cristalinas de un inhibidor de bet
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

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EP1297836A4 (en) 2000-06-16 2007-06-13 Mitsubishi Pharma Corp COMPOSITIONS FOR CHECKING RELEASE, PH AREA AND / OR SPEED
CA2710740C (en) * 2007-12-28 2016-07-19 Shinji Miyoshi Thienotriazolodiazepine compound as antitumor agent
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WO2012075456A1 (en) 2010-12-02 2012-06-07 Constellation Pharmaceuticals Bromodomain inhibitors and uses thereof
EP2683734A1 (en) * 2011-03-10 2014-01-15 Institut National de la Sante et de la Recherche Medicale (INSERM) Atip3 and biologically active fragments thereof for use in the treatment of cancer
CN105050605A (zh) 2012-06-25 2015-11-11 翁科埃蒂克斯股份公司 使用噻吩并三唑并二氮杂*化合物治疗淋巴瘤的方法
WO2014004854A1 (en) * 2012-06-27 2014-01-03 The Curators Of The University Of Missouri Induction of estrogen receptor beta by cholesterol biosynthesis inhibitors and methods of treatment of cancer
BR112015006537A2 (pt) 2012-09-28 2017-07-04 Oncoethix Sa dispersão sólida, formulação farmacêutica, cápsula farmacêutica, e, tablete farmacêutico
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WO2015018523A1 (en) * 2013-08-06 2015-02-12 Oncoethix Sa A novel bet-brd inhibitor for treatment of solid tumors

Also Published As

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

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