AR095197A1 - COMBINATION OF AN EGFR T790M INHIBITOR AND EGFR INHIBITOR FOR THE TREATMENT OF PULMONARY CANCER OF NON-SMALL CELLS - Google Patents

COMBINATION OF AN EGFR T790M INHIBITOR AND EGFR INHIBITOR FOR THE TREATMENT OF PULMONARY CANCER OF NON-SMALL CELLS

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Publication number
AR095197A1
AR095197A1 ARP140100804A ARP140100804A AR095197A1 AR 095197 A1 AR095197 A1 AR 095197A1 AR P140100804 A ARP140100804 A AR P140100804A AR P140100804 A ARP140100804 A AR P140100804A AR 095197 A1 AR095197 A1 AR 095197A1
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AR
Argentina
Prior art keywords
inhibitor
egfr
combination
treatment
salt
Prior art date
Application number
ARP140100804A
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Spanish (es)
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Pfizer
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Publication date
Application filed by Pfizer filed Critical Pfizer
Publication of AR095197A1 publication Critical patent/AR095197A1/en

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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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • A61K31/66—Phosphorus compounds
    • 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
    • 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

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

Abstract

Un método para el tratamiento del cáncer pulmonar de células no pequeñas mediante la administración de una combinación de un inhibidor de EGFR T790M en combinación con una cantidad de dosis baja de un inhibidor de panHER. También se refiere a un método para el tratamiento del cáncer pulmonar de células no pequeñas mediante la administración de una combinación de un inhibidor irreversible de EGFR T790M en combinación con un inhibidor de EGFR. Reivindicación 1: Un método para el tratamiento del cáncer pulmonar de células no pequeñas, que comprende administrar a un paciente que lo necesita una cantidad eficaz de un inhibidor irreversible de EGFR T790M en combinación con una cantidad eficaz de un inhibidor de EGFR. Reivindicación 2: El método de acuerdo con la reivindicación 1, en donde el inhibidor irreversible de EGFR T790M es 1-{(3R,4R)-3-[({5-cloro-2-[(1-metil-1H-pirazol-4-il)amino]-7H-pirrolo[2,3-d]pirimidin-4-il}oxi)metil]-4-metoxipirrolidin-1-iI}prop-2-en-1-ona o una sal de esta aceptable desde el punto de vista farmacéutico. Reivindicación 3: El método de acuerdo con las reivindicaciones 1 ó 2, en donde el inhibidor de EGFR se selecciona del grupo que consiste en gefitinib, erlotinib, icotinib, vandetanib, lapatinib, neratinib, afatinib, pelitinib, dacomitinib, canertinib, cetuximab y panitumumab, o una sal de estos aceptable desde el punto de vista farmacéutico. Reivindicación 13: El método de acuerdo con cualquiera de las reivindicaciones 7 - 10, en donde el inhibidor de panHER se selecciona del grupo que consiste en lapatinib, neratinib, afatinib, pelitinib, dacomitinib y canertinib, o una sal de estos aceptable desde el punto de vista farmacéutico. Reivindicación 17: El método de acuerdo con la reivindicación 16, en donde el inhibidor de EGFR T790M se selecciona del grupo que consiste en Go6976, PKC412, AP26113, HM61713, WZ4002, CO-1686 y TAS-2913, o una sal de estos aceptable desde el punto de vista farmacéutico. Reivindicación 22: Una combinación sinérgica de: (a) un inhibidor de EGFR T790M; y (b) un inhibidor de EGFR, en donde el componente (a) y el componente (b) son sinérgicos.A method for treating non-small cell lung cancer by administering a combination of an EGFR T790M inhibitor in combination with a low dose amount of a panHER inhibitor. It also refers to a method for the treatment of non-small cell lung cancer by administering a combination of an irreversible EGFR T790M inhibitor in combination with an EGFR inhibitor. Claim 1: A method for the treatment of non-small cell lung cancer, which comprises administering to an in need patient an effective amount of an irreversible EGFR T790M inhibitor in combination with an effective amount of an EGFR inhibitor. Claim 2: The method according to claim 1, wherein the irreversible EGFR T790M inhibitor is 1 - {(3R, 4R) -3 - [({5-chloro-2 - [(1-methyl-1H-pyrazole) -4-yl) amino] -7H-pyrrolo [2,3-d] pyrimidin-4-yl} oxy) methyl] -4-methoxypyrrolidin-1-iI} prop-2-en-1-one or a salt of It is pharmaceutically acceptable. Claim 3: The method according to claims 1 or 2, wherein the EGFR inhibitor is selected from the group consisting of gefitinib, erlotinib, icotinib, vandetanib, lapatinib, neratinib, afatinib, pelitinib, dacomitinib, canertinib, cetuximab and panitumumab , or a salt thereof pharmaceutically acceptable. Claim 13: The method according to any of claims 7-10, wherein the panHER inhibitor is selected from the group consisting of lapatinib, neratinib, afatinib, pelitinib, dacomitinib and canertinib, or a salt thereof acceptable from the point Pharmaceutical view. Claim 17: The method according to claim 16, wherein the EGFR T790M inhibitor is selected from the group consisting of Go6976, PKC412, AP26113, HM61713, WZ4002, CO-1686 and TAS-2913, or an acceptable salt thereof from the pharmaceutical point of view. Claim 22: A synergistic combination of: (a) a T790M EGFR inhibitor; and (b) an EGFR inhibitor, wherein component (a) and component (b) are synergistic.

ARP140100804A 2013-03-14 2014-03-10 COMBINATION OF AN EGFR T790M INHIBITOR AND EGFR INHIBITOR FOR THE TREATMENT OF PULMONARY CANCER OF NON-SMALL CELLS AR095197A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201361786130P 2013-03-14 2013-03-14

Publications (1)

Publication Number Publication Date
AR095197A1 true AR095197A1 (en) 2015-09-30

Family

ID=50288209

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP140100804A AR095197A1 (en) 2013-03-14 2014-03-10 COMBINATION OF AN EGFR T790M INHIBITOR AND EGFR INHIBITOR FOR THE TREATMENT OF PULMONARY CANCER OF NON-SMALL CELLS

Country Status (14)

Country Link
EP (1) EP2968336A2 (en)
JP (1) JP2014177456A (en)
KR (1) KR20150119210A (en)
CN (1) CN105073116A (en)
AR (1) AR095197A1 (en)
AU (1) AU2014229468A1 (en)
BR (1) BR112015023020A2 (en)
CA (1) CA2904797A1 (en)
IL (1) IL240730A0 (en)
MX (1) MX2015012106A (en)
RU (1) RU2015137596A (en)
SG (1) SG11201506531WA (en)
TW (1) TW201446248A (en)
WO (1) WO2014140989A2 (en)

Families Citing this family (17)

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MD20140023A2 (en) 2011-09-22 2014-06-30 Pfizer Inc. Pyrrolopyrimidine and purine derivatives
US9840517B2 (en) 2013-09-18 2017-12-12 Beijing Hanmi Pharmaceutical Co., Ltd. Compound inhibiting activities of BTK and/or JAK3 kinases
UA115388C2 (en) 2013-11-21 2017-10-25 Пфайзер Інк. 2,6-substituted purine derivatives and their use in the treatment of proliferative disorders
TW201622744A (en) 2014-03-04 2016-07-01 美國禮來大藥廠 Combination therapy for cancer
EP3201190A4 (en) 2014-10-01 2018-03-14 Sun Pharmaceutical Industries Ltd Crystalline form of afatinib dimaleate
CN114224894A (en) * 2014-12-03 2022-03-25 奥克兰联合服务有限公司 Kinase inhibitor prodrugs for the treatment of cancer
US10538518B2 (en) * 2015-08-11 2020-01-21 Principia Biopharma, Inc. Processes for preparing an FGFR inhibitor
US10583142B2 (en) 2016-03-25 2020-03-10 OSI Pharmaceuticals, LLC Pulse dosing regimen and methods of treatment
WO2017164887A1 (en) * 2016-03-25 2017-09-28 OSI Pharmaceuticals, LLC Pulse dosing regimen and methods for treatment
WO2017176565A1 (en) 2016-04-07 2017-10-12 Eli Lilly And Company Combinations of an anti-b7-h1 antibody and a cxcr4 peptide antagonist for treating a solid tumor
US10813933B2 (en) 2016-05-17 2020-10-27 Japanese Foundation For Cancer Research Therapeutic agent for lung cancer that has acquired EGFR-TKI resistance
US20190125751A1 (en) * 2016-05-18 2019-05-02 Boehringer Ingelheim International Gmbh Anticancer combination therapy
TWI808958B (en) * 2017-01-25 2023-07-21 美商特普醫葯公司 Combination therapy involving diaryl macrocyclic compounds
US11395821B2 (en) 2017-01-30 2022-07-26 G1 Therapeutics, Inc. Treatment of EGFR-driven cancer with fewer side effects
EP3592338A1 (en) * 2017-03-08 2020-01-15 ARIAD Pharmaceuticals, Inc. Pharmaceutical formulations comprising 5-chloro-n4
WO2019112269A1 (en) * 2017-12-05 2019-06-13 주식회사 오스코텍 Pyrrolo(pyrazolo)pyrimidine derivative as lrrk2 inhibitor
WO2024026056A2 (en) * 2022-07-29 2024-02-01 Accutar Biotechnology, Inc. Heteroaryl compounds as egfr inhibitors and their uses

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102146059A (en) * 2010-02-08 2011-08-10 上海艾力斯医药科技有限公司 Quinazoline derivatives and preparation method and application thereof
MD20140023A2 (en) * 2011-09-22 2014-06-30 Pfizer Inc. Pyrrolopyrimidine and purine derivatives

Also Published As

Publication number Publication date
AU2014229468A1 (en) 2015-09-03
TW201446248A (en) 2014-12-16
EP2968336A2 (en) 2016-01-20
MX2015012106A (en) 2016-01-12
WO2014140989A3 (en) 2014-12-04
BR112015023020A2 (en) 2017-07-18
RU2015137596A (en) 2017-04-17
JP2014177456A (en) 2014-09-25
WO2014140989A2 (en) 2014-09-18
CA2904797A1 (en) 2014-09-18
SG11201506531WA (en) 2015-09-29
IL240730A0 (en) 2015-10-29
KR20150119210A (en) 2015-10-23
CN105073116A (en) 2015-11-18

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