BR112017016776A2 - combinações de moduladores duplos de irs/stat3 e agentes anticâncer para o tratamento de câncer - Google Patents

combinações de moduladores duplos de irs/stat3 e agentes anticâncer para o tratamento de câncer

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Publication number
BR112017016776A2
BR112017016776A2 BR112017016776A BR112017016776A BR112017016776A2 BR 112017016776 A2 BR112017016776 A2 BR 112017016776A2 BR 112017016776 A BR112017016776 A BR 112017016776A BR 112017016776 A BR112017016776 A BR 112017016776A BR 112017016776 A2 BR112017016776 A2 BR 112017016776A2
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Brazil
Prior art keywords
inhibitor
combination
tumor
irs
treatment
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BR112017016776A
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English (en)
Other versions
BR112017016776B1 (pt
Inventor
Reuveni Hadas
Haviv Izhak
Kupershmidt Lana
Original Assignee
Tyrnovo Ltd
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Publication date
Application filed by Tyrnovo Ltd filed Critical Tyrnovo Ltd
Publication of BR112017016776A2 publication Critical patent/BR112017016776A2/pt
Publication of BR112017016776B1 publication Critical patent/BR112017016776B1/pt

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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
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/145Amines having sulfur, e.g. thiurams (>N—C(S)—S—C(S)—N< and >N—C(S)—S—S—C(S)—N<), Sulfinylamines (—N=SO), Sulfonylamines (—N=SO2)
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/435Heterocyclic 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
    • A61K31/4375Heterocyclic 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 nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • AHUMAN NECESSITIES
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    • A61K31/00Medicinal preparations containing organic active ingredients
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    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
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    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
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    • 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
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    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • 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
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
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    • 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
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/5415Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
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    • A61K39/00Medicinal preparations containing antigens or antibodies
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    • A61K39/39533Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/39558Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against tumor tissues, cells, antigens
    • AHUMAN NECESSITIES
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    • 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
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    • A61P35/00Antineoplastic agents
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    • C07K16/28Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2863Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against receptors for growth factors, growth regulators
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    • C07K2317/76Antagonist effect on antigen, e.g. neutralization or inhibition of binding

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Abstract

a presente invenção se refere ao tratamento de câncer usando terapia de combinação compreendendo um modulador duplo de substrato de receptor de insulina (irs) e transdutor de sinal e ativador da transcrição 3 (stat3), em combinação com (i) um modulador de uma proteína quinase (pk) selecionada dentre um inibidor do fator de crescimento epidérmico (inibidor de egfr) e anticorpo egfr; (ii) um inibidor do alvo de mamíferos da rapamicina (mtor); (iii) um inibidor da proteína quinase ativada por mitógeno (mek); (iv) um inibidor de b-raf mutado; (v) um agente quimioterápico como gemcitabina, 5-fu, irinotecan e oxaliplatina; e (vi) certas combinações dos mesmos. a combinação pode ser usada para tratar um tumor que tenha desenvolvido resistência a um inibidor de egfr, anticorpo egfr, inibidor de mtor, inibidor de mek, inibidor de b-raf mutado, agentes quimioterápicos, e certas combinações dos mesmos, ou para prevenir a resistência adquirida de um tumor a qualquer um de ditos inibidores ou agentes, ou para prevenir a recorrência do tumor após o cessar do tratamento com qualquer um de ditos inibidores ou agentes ou uma combinação dos mesmos. a combinação provê um efeito terapêutico que é pelo menos aditivo e é preferencialmente sinérgico. a presente invenção se refere adicionalmente ao tratamento de câncer usando terapia de combinação compreendendo um modulador duplo de irs e stat3 em combinação com um agente de imunoterapia. a combinação pode ser usada para sensibilizar um tumor à imunoterapia.
BR112017016776-0A 2015-02-05 2016-02-04 Composição e combinação farmacêutica compreendendo um composto d, um inibidor de egfr e/ou um anticorpo egfr BR112017016776B1 (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201562112257P 2015-02-05 2015-02-05
US62/112,257 2015-02-05
US201562136530P 2015-03-22 2015-03-22
US62/136,530 2015-03-22
PCT/IL2016/050134 WO2016125169A1 (en) 2015-02-05 2016-02-04 Combinations of irs/stat3 dual modulators and anti-cancer agents for treating cancer

Publications (2)

Publication Number Publication Date
BR112017016776A2 true BR112017016776A2 (pt) 2018-04-17
BR112017016776B1 BR112017016776B1 (pt) 2023-09-19

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Publication number Publication date
WO2016125169A1 (en) 2016-08-11
EP3253733B1 (en) 2020-04-29
EP3253733A1 (en) 2017-12-13
IL280378A (en) 2021-03-01
AU2020250235A1 (en) 2020-11-05
US10912745B2 (en) 2021-02-09
JP2018504418A (ja) 2018-02-15
IL253797B (en) 2021-02-28
CN112494653A (zh) 2021-03-16
JP2021073254A (ja) 2021-05-13
IL280378B (en) 2022-03-01
AU2016213972B2 (en) 2020-07-09
EP3253733A4 (en) 2018-10-31
CN112353938A (zh) 2021-02-12
AU2016213972A1 (en) 2017-08-24
JP2023062187A (ja) 2023-05-02
EP3750530A1 (en) 2020-12-16
IL253797A0 (en) 2017-09-28
CA2975673A1 (en) 2016-08-11
US20210220297A1 (en) 2021-07-22
CN107250108B (zh) 2020-11-27
KR20170109589A (ko) 2017-09-29
CN107250108A (zh) 2017-10-13
US20180028475A1 (en) 2018-02-01
ES2808781T3 (es) 2021-03-01

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