JP6147246B2 - Ａｋｔ及びｍｅｋ阻害剤化合物の組み合わせ、及び使用方法 - Google Patents

Ａｋｔ及びｍｅｋ阻害剤化合物の組み合わせ、及び使用方法 Download PDF

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JP6147246B2
JP6147246B2 JP2014502884A JP2014502884A JP6147246B2 JP 6147246 B2 JP6147246 B2 JP 6147246B2 JP 2014502884 A JP2014502884 A JP 2014502884A JP 2014502884 A JP2014502884 A JP 2014502884A JP 6147246 B2 JP6147246 B2 JP 6147246B2
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pharmaceutically acceptable
acceptable salt
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compound
formula
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JP2014512355A5 (OSRAM
JP2014512355A (ja
Inventor
ブライアン リー，
ブライアン リー，
クイ リン，
クイ リン，
ミシェル ナンニーニ，
ミシェル ナンニーニ，
エリザベス パンヌース，
エリザベス パンヌース，
ディーパク サンパス，
ディーパク サンパス，
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Genentech Inc
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Genentech Inc
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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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61K31/517—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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4402—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2014502884A 2011-04-01 2012-03-30 Ａｋｔ及びｍｅｋ阻害剤化合物の組み合わせ、及び使用方法 Active JP6147246B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161471038P 2011-04-01 2011-04-01
US61/471,038 2011-04-01
PCT/US2012/031716 WO2012135779A1 (en) 2011-04-01 2012-03-30 Combinations of akt and mek inhibitor compounds, and methods of use

Publications (3)

Publication Number Publication Date
JP2014512355A JP2014512355A (ja) 2014-05-22
JP2014512355A5 JP2014512355A5 (OSRAM) 2015-05-21
JP6147246B2 true JP6147246B2 (ja) 2017-06-14

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Country Status (16)

Country Link
US (1) US9682082B2 (OSRAM)
EP (1) EP2694073B1 (OSRAM)
JP (1) JP6147246B2 (OSRAM)
KR (1) KR20140022053A (OSRAM)
CN (2) CN103841976A (OSRAM)
AU (1) AU2012236164A1 (OSRAM)
BR (1) BR112013025397A2 (OSRAM)
CA (1) CA2831932A1 (OSRAM)
ES (1) ES2688809T3 (OSRAM)
IL (1) IL228643A0 (OSRAM)
MX (1) MX2013011333A (OSRAM)
PL (1) PL2694073T3 (OSRAM)
RU (1) RU2013148817A (OSRAM)
SG (1) SG194047A1 (OSRAM)
TR (1) TR201815685T4 (OSRAM)
WO (1) WO2012135779A1 (OSRAM)

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PE20121816A1 (es) * 2009-10-12 2013-01-02 Hoffmann La Roche Combinaciones de un inhibidor de pi3k y un inhibidor de mek
US9566334B2 (en) * 2012-12-07 2017-02-14 The General Hospital Corporation Combinations of a PI3K/AKT inhibitor compound with an HER3/EGFR inhibitor compound and use thereof in the treatment of a hyperproliferative disorder
JP6669500B2 (ja) * 2013-02-25 2020-03-18 ジェネンテック， インコーポレイテッド 薬物耐性ａｋｔ変異体を検出し治療するための方法及び組成物
WO2015035146A2 (en) * 2013-09-05 2015-03-12 Memorial Sloan-Kettering Cancer Center Ddx43 as a biomarker of resistance to mek1/2 inhibitors
CN113194941A (zh) 2018-12-19 2021-07-30 基因泰克公司 使用包括akt抑制剂、紫杉烷和pd-l1抑制剂的组合疗法治疗乳腺癌
AU2021246141A1 (en) * 2020-04-03 2022-12-01 Beigene, Ltd. Co-administration of mirdametinib and lifirafenib for use in treating cancers
US11084780B1 (en) * 2021-02-17 2021-08-10 Springworks Therapeutics, Inc. Crystalline solids of MEK inhibitor N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide and uses thereof
US11066358B1 (en) * 2021-02-17 2021-07-20 Warner-Lambert Company Llc Compositions of essentially pure form IV of N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide and uses thereof
WO2024255830A1 (zh) * 2023-06-14 2024-12-19 南京正大天晴制药有限公司 Akt抑制剂在制备预防或治疗卵巢癌药物中的用途

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CA2831932A1 (en) 2012-10-04
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US20140155372A1 (en) 2014-06-05
AU2012236164A1 (en) 2013-11-21
RU2013148817A (ru) 2015-05-10
MX2013011333A (es) 2014-04-16
BR112013025397A2 (pt) 2019-09-24
PL2694073T3 (pl) 2019-06-28
EP2694073A1 (en) 2014-02-12
ES2688809T3 (es) 2018-11-07
KR20140022053A (ko) 2014-02-21
SG194047A1 (en) 2013-11-29
EP2694073B1 (en) 2018-08-08
CN110433165A (zh) 2019-11-12
IL228643A0 (en) 2013-12-31
CN103841976A (zh) 2014-06-04
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US9682082B2 (en) 2017-06-20

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