AR107500A1 - Terapia de combinación de inhibidores de bromodominio y moduladores inmunitarios - Google Patents

Terapia de combinación de inhibidores de bromodominio y moduladores inmunitarios

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Publication number
AR107500A1
AR107500A1 ARP160103015A ARP160103015A AR107500A1 AR 107500 A1 AR107500 A1 AR 107500A1 AR P160103015 A ARP160103015 A AR P160103015A AR P160103015 A ARP160103015 A AR P160103015A AR 107500 A1 AR107500 A1 AR 107500A1
Authority
AR
Argentina
Prior art keywords
inhibitor
bromodomain inhibitor
immune
tautomer
stereoisomer
Prior art date
Application number
ARP160103015A
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English (en)
Original Assignee
Dana Farber Cancer Inst Inc
Peter Maccallum Cancer Inst
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 Dana Farber Cancer Inst Inc, Peter Maccallum Cancer Inst filed Critical Dana Farber Cancer Inst Inc
Publication of AR107500A1 publication Critical patent/AR107500A1/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
    • A61K31/435Heterocyclic 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
    • A61K31/437Heterocyclic 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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • 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
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K39/395Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
    • C07K16/2827Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against B7 molecules, e.g. CD80, CD86
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2878Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the NGF-receptor/TNF-receptor superfamily, e.g. CD27, CD30, CD40, CD95
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K2039/505Medicinal preparations containing antigens or antibodies comprising antibodies
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/20Immunoglobulins specific features characterized by taxonomic origin
    • C07K2317/24Immunoglobulins specific features characterized by taxonomic origin containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered

Abstract

La presente divulga un método para tratar el cáncer en un sujeto que necesita el mismo, comprendiendo el método administrar al sujeto una cantidad terapéuticamente eficaz de un inhibidor de bromodominio; y, un modulador inmunitario. Reivindicación 11: El método de la reivindicación 9 ó 10, donde el inhibidor de bromodominio es JQ1 de fórmula (1), o una sal, solvato, hidrato, polimorfo, co-cristal, tautómero, estereoisómero, derivado marcado con isótopos o profármaco farmacéuticamente aceptable del mismo. Reivindicación 12: El método de la reivindicación 9 ó 10, donde el inhibidor de bromodominio es Y803 de fórmula (2), o una sal, solvato, hidrato, polimorfo, co-cristal, tautómero, estereoisómero, derivado marcado con isótopos o profármaco farmacéuticamente aceptable del mismo. Reivindicación 13: El método de la reivindicación 9 ó 10, donde el inhibidor de bromodominio es CPI-203 de fórmula (3), o una sal, solvato, hidrato, polimorfo, co-cristal, tautómero, estereoisómero, derivado marcado con isótopos o profármaco farmacéuticamente aceptable del mismo. Reivindicación 14: El método de una cualquiera de las reivindicaciones 1 a 8, donde el inhibidor de bromodominio es dBET1 de fórmula (4) o una sal, solvato, hidrato, polimorfo, co-cristal, tautómero, estereoisómero, derivado marcado con isótopos o profármaco farmacéuticamente aceptable del mismo. Reivindicación 17: El método de la reivindicación 15 ó 16, donde el inhibidor de bromodominio es IBET-151 de fórmula (5), o una sal, solvato, hidrato, polimorfo, co-cristal, tautómero, estereoisómero, derivado marcado con isótopos o profármaco farmacéuticamente aceptable del mismo. Reivindicación 20: El método de la reivindicación 18 ó 19, donde el inhibidor de bromodominio es IBET-762 de fórmula (6), o una sal, solvato, hidrato, polimorfo, co-cristal, tautómero, estereoisómero, derivado marcado con isótopos o profármaco farmacéuticamente aceptable del mismo. Reivindicación 23: El método de la reivindicación 21 ó 22, donde el inhibidor de bromodominio es RVX-208 de fórmula (7), o una sal, solvato, hidrato polimorfo, co-cristal, tautómero, estereoisómero, derivado marcado con isótopos o profármaco farmacéuticamente aceptable del mismo. Reivindicación 37: El método de la reivindicación 36, donde la molécula inmunitaria estimuladora se selecciona entre el grupo que consiste en 4-1BB (CD137), CD137L, OX40, OX40L, ICOS, CD40, CD40L, CD70, CD27, CD28, CD80, CD86, B7RP1 y HVEM. Reivindicación 38: El método de una cualquiera de las reivindicaciones 1 a 35, donde el modulador inmunitario es un inhibidor de puntos de control inmunitarios. Reivindicación 39: El método de la reivindicación 39, donde el inhibidor de puntos de control inmunitarios es un inhibidor de una proteína de puntos de control inmunitarios seleccionada entre el grupo que consiste en: CTLA-4, PD-1, PDL-1, TIM3, LAG3, B7-H3, B7-H4, BTLA, GAL9 y A2aR. Reivindicación 49: El método de la reivindicación 39, donde el inhibidor de puntos de control inmunitarios es un inhibidor de A2aR. Reivindicación 50: El método de la reivindicación 49, donde el modulador inmunitario es un péptido, anticuerpo, ARN de interferencia, o molécula pequeña. Reivindicación 51: El método de la reivindicación 50, donde el modulador inmunitario es un anticuerpo monoclonal, o una proteína de fusión de Ig. Reivindicación 52: El método de la reivindicación 51, donde el modulador inmunitario es un anticuerpo anti-4-1BB. Reivindicación 53: El método de la reivindicación 51, donde el modulador inmunitario es un anticuerpo anti-PD-1. Reivindicación 54: El método de una cualquiera de las reivindicaciones 1 a 53, donde el inhibidor de bromodominio y el modulador inmunitario se administran al sujeto simultáneamente como una única composición. Reivindicación 60: El método de una cualquiera de las reivindicaciones 1 a 59, donde el inhibidor de bromodominio y el modulador inmunitario son sinérgicos en el tratamiento del cáncer, en comparación con el inhibidor de bromodominio en solitario o el modulador inmunitario en solitario.
ARP160103015A 2015-10-02 2016-09-30 Terapia de combinación de inhibidores de bromodominio y moduladores inmunitarios AR107500A1 (es)

Applications Claiming Priority (1)

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US201562236280P 2015-10-02 2015-10-02

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AR107500A1 true AR107500A1 (es) 2018-05-09

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US (1) US20190192532A1 (es)
EP (1) EP3355922A2 (es)
JP (1) JP2018530554A (es)
KR (1) KR20180081507A (es)
CN (1) CN108289957A (es)
AR (1) AR107500A1 (es)
AU (1) AU2016331190A1 (es)
BR (1) BR112018006689A2 (es)
CA (1) CA2999523A1 (es)
CL (1) CL2018000853A1 (es)
HK (1) HK1256269A1 (es)
IL (1) IL258212A (es)
MA (1) MA43037A (es)
MX (1) MX2018003824A (es)
PE (1) PE20181068A1 (es)
WO (1) WO2017059319A2 (es)

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CN108289957A (zh) 2018-07-17
CA2999523A1 (en) 2017-04-06
EP3355922A2 (en) 2018-08-08
CL2018000853A1 (es) 2018-08-31
JP2018530554A (ja) 2018-10-18
MA43037A (fr) 2018-08-08
KR20180081507A (ko) 2018-07-16
MX2018003824A (es) 2019-04-01
WO2017059319A2 (en) 2017-04-06
BR112018006689A2 (pt) 2018-10-09
WO2017059319A3 (en) 2017-10-12
PE20181068A1 (es) 2018-07-04
IL258212A (en) 2018-05-31
AU2016331190A1 (en) 2018-04-12
US20190192532A1 (en) 2019-06-27
HK1256269A1 (zh) 2019-09-20

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