CN103764144B - Pi3k抑制剂与mek抑制剂的协同组合 - Google Patents

Pi3k抑制剂与mek抑制剂的协同组合 Download PDF

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Publication number
CN103764144B
CN103764144B CN201280041783.7A CN201280041783A CN103764144B CN 103764144 B CN103764144 B CN 103764144B CN 201280041783 A CN201280041783 A CN 201280041783A CN 103764144 B CN103764144 B CN 103764144B
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cancer
compound
combination
amide
pharmaceutically acceptable
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Expired - Fee Related
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CN201280041783.7A
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Chinese (zh)
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CN103764144A (zh
Inventor
C·弗里特什
X·黄
M·伯恩
托玛索 E·迪
E·迪托玛索
J·G·考瑟特
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Novartis AG
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Novartis AG
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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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4412Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2121/00Preparations for use in therapy

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  • 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)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Hematology (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)
CN201280041783.7A 2011-08-31 2012-08-30 Pi3k抑制剂与mek抑制剂的协同组合 Expired - Fee Related CN103764144B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201161529380P 2011-08-31 2011-08-31
US61/529,380 2011-08-31
US201161542463P 2011-10-03 2011-10-03
US61/542,463 2011-10-03
PCT/US2012/052955 WO2013066483A1 (en) 2011-08-31 2012-08-30 Synergistic combinations of pi3k- and mek-inhibitors

Publications (2)

Publication Number Publication Date
CN103764144A CN103764144A (zh) 2014-04-30
CN103764144B true CN103764144B (zh) 2016-07-20

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
CN201280041783.7A Expired - Fee Related CN103764144B (zh) 2011-08-31 2012-08-30 Pi3k抑制剂与mek抑制剂的协同组合

Country Status (11)

Country Link
US (1) US9675595B2 (https=)
EP (1) EP2750675A1 (https=)
JP (1) JP6058009B2 (https=)
KR (1) KR20140072028A (https=)
CN (1) CN103764144B (https=)
AU (1) AU2012333092B2 (https=)
BR (1) BR112014004587A2 (https=)
CA (1) CA2846454A1 (https=)
MX (1) MX2014002471A (https=)
RU (1) RU2607944C2 (https=)
WO (1) WO2013066483A1 (https=)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3613743B1 (en) 2008-01-04 2022-03-16 Intellikine, LLC Processes for the preparation of 1h-pyrazolo[3,4-d]pyrimidin-4-amine derivatives
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
TWI674262B (zh) 2011-01-10 2019-10-11 美商英菲尼提製藥股份有限公司 製備異喹啉酮之方法及異喹啉酮之固體形式
US8828998B2 (en) 2012-06-25 2014-09-09 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
EP2914296B2 (en) 2012-11-01 2021-09-29 Infinity Pharmaceuticals, Inc. Treatment of cancers using pi3 kinase isoform modulators
RU2015156221A (ru) * 2013-06-11 2017-07-17 Новартис Аг Фармацевтические комбинация ингибитора pi3k и средства, дестабилизирующего микротрубочки
KR20160020502A (ko) * 2013-06-18 2016-02-23 노파르티스 아게 제약 조합물
BR112016012141A2 (pt) * 2014-01-15 2017-08-08 Novartis Ag "combinações farmacêuticas, uso das mesmas, e embalagem comercial"
WO2015160975A2 (en) 2014-04-16 2015-10-22 Infinity Pharmaceuticals, Inc. Combination therapies
US20150320754A1 (en) * 2014-04-16 2015-11-12 Infinity Pharmaceuticals, Inc. Combination therapies
AU2016349279A1 (en) * 2015-11-03 2018-05-10 Board Of Regents, The University Of Texas System Combination of Bcl-2 inhibitor and MEK inhibitor for the treatment of cancer
RU2754507C2 (ru) 2016-06-24 2021-09-02 Инфинити Фармасьютикалз, Инк. Комбинированная терапия
WO2020053125A1 (en) * 2018-09-10 2020-03-19 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of neurofibromatosis

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1874768A (zh) * 2003-08-29 2006-12-06 阵列生物制药公司 作为mek抑制剂的n3烷基化苯并咪唑衍生物
WO2011054620A1 (en) * 2009-10-12 2011-05-12 F. Hoffmann-La Roche Ag Combinations of a pi3k inhibitor and a mek inhibitor
CN102149711A (zh) * 2008-09-10 2011-08-10 诺瓦提斯公司 有机化合物

Family Cites Families (12)

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DZ3401A1 (fr) 2000-07-19 2002-01-24 Warner Lambert Co Esters oxygenes d'acides 4-iodophenylamino benzhydroxamiques
RU2192861C1 (ru) 2001-06-29 2002-11-20 Новосибирский институт биоорганической химии СО РАН Композиция для антибластической терапии
SG2013013339A (en) * 2002-03-13 2014-12-30 Array Biopharma Inc N3 alkylated benzimidazole derivatives as mek inhibitors
US7378423B2 (en) 2004-06-11 2008-05-27 Japan Tobacco Inc. Pyrimidine compound and medical use thereof
AU2005252110B2 (en) 2004-06-11 2008-09-04 Shionogi & Co., Ltd. 5-amino-2,4,7-trioxo-3,4,7,8-tetrahydro-2H-pyrido[2,3-D] pyrimidine derivatives and related compounds for the treatment of cancer
RU2368602C2 (ru) * 2005-01-26 2009-09-27 Айрм Ллк Соединения и композиции в качестве ингибиторов протеинкиназ
SG177981A1 (en) 2005-05-18 2012-02-28 Array Biopharma Inc 4-(phenylamino)-6-oxo-1, 6-dihydropyridazine-3-carboxamide derivatives as mek inhibitors for the treatment of hyperproliferative diseases
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
PE20070335A1 (es) 2005-08-30 2007-04-21 Novartis Ag Benzimidazoles sustituidos y metodos para su preparacion
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
DK2074122T5 (da) 2006-09-15 2014-03-17 Pfizer Prod Inc Pyrido (2, 3-d) pyrimidin0n-forbindelser og anvendelse deraf som pi3 inhibitorer
KR20110028651A (ko) * 2008-07-11 2011-03-21 노파르티스 아게 (a) 포스포이노시타이드 3-키나제 억제제 및 (b) ras/raf/mek 경로의 조절제의 조합물

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1874768A (zh) * 2003-08-29 2006-12-06 阵列生物制药公司 作为mek抑制剂的n3烷基化苯并咪唑衍生物
CN102149711A (zh) * 2008-09-10 2011-08-10 诺瓦提斯公司 有机化合物
WO2011054620A1 (en) * 2009-10-12 2011-05-12 F. Hoffmann-La Roche Ag Combinations of a pi3k inhibitor and a mek inhibitor

Also Published As

Publication number Publication date
RU2607944C2 (ru) 2017-01-11
US20140179744A1 (en) 2014-06-26
AU2012333092B2 (en) 2016-04-21
AU2012333092A1 (en) 2014-03-06
CA2846454A1 (en) 2013-05-10
EP2750675A1 (en) 2014-07-09
MX2014002471A (es) 2014-03-27
US9675595B2 (en) 2017-06-13
WO2013066483A1 (en) 2013-05-10
CN103764144A (zh) 2014-04-30
JP2014525454A (ja) 2014-09-29
RU2014112198A (ru) 2015-10-10
BR112014004587A2 (pt) 2017-03-14
JP6058009B2 (ja) 2017-01-11
KR20140072028A (ko) 2014-06-12

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