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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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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    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2121/00—Preparations 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)

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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

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

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US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
DK2240451T3 (da) 2008-01-04 2017-11-20 Intellikine Llc Isoquinolinonderivater substitueret med en purin, der er anvendelig som pi3k-inhibitorer
DK2663309T3 (en) 2011-01-10 2017-06-19 Infinity Pharmaceuticals Inc METHODS FOR PRODUCING ISOQUINOLINONES AND SOLID FORMS OF ISOQUINOLINONES
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
KR102229478B1 (ko) 2012-11-01 2021-03-18 인피니티 파마슈티칼스, 인코포레이티드 Pi3 키나아제 동형단백질 조절인자를 사용하는 암의 치료
RU2015156221A (ru) * 2013-06-11 2017-07-17 Новартис Аг Фармацевтические комбинация ингибитора pi3k и средства, дестабилизирующего микротрубочки
WO2014203152A1 (en) * 2013-06-18 2014-12-24 Novartis Ag Pharmaceutical combinations
RU2016133285A (ru) * 2014-01-15 2018-02-20 Новартис Аг Фармацевтические комбинации
WO2015160986A2 (en) * 2014-04-16 2015-10-22 Infinity Pharmaceuticals, Inc. Combination therapies
US20150320755A1 (en) 2014-04-16 2015-11-12 Infinity Pharmaceuticals, Inc. Combination therapies
JP6724136B2 (ja) * 2015-11-03 2020-07-15 ジェネンテック， インコーポレイテッド がん治療のためのＢｃｌ−２阻害剤及びＭＥＫ阻害剤の組み合わせ
IL263680B2 (en) 2016-06-24 2025-10-01 Infinity Pharmaceuticals Inc PI3K inhibitors for use in combination with a second therapeutic agent for the treatment, management or prevention of cancer
EP3849545A1 (en) * 2018-09-10 2021-07-21 Institut National de la Santé et de la Recherche Médicale (INSERM) 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

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US6960614B2 (en) 2000-07-19 2005-11-01 Warner-Lambert Company Oxygenated esters of 4-lodo phenylamino benzhydroxamic acids
RU2192861C1 (ru) 2001-06-29 2002-11-20 Новосибирский институт биоорганической химии СО РАН Композиция для антибластической терапии
MXPA04008893A (es) * 2002-03-13 2005-06-20 Array Biopharma Inc Derivados de bencimidazol n3 alquilados como inhibidores de mek.
PL1761528T3 (pl) 2004-06-11 2008-05-30 Japan Tobacco Inc Pochodne 5-amino-2,4,7-triokso-3,4,7,8-tetrahydro-2H-pirydo[2,3-D]pirymidyny i związki pokrewne do leczenia raka
US7378423B2 (en) 2004-06-11 2008-05-27 Japan Tobacco Inc. Pyrimidine compound and medical use thereof
CN101106990B (zh) * 2005-01-26 2010-12-08 Irm责任有限公司 用作蛋白激酶抑制剂的化合物和组合物
NZ563707A (en) 2005-05-18 2011-01-28 Array Biopharma Inc Heterocyclic inhibitors of MEK and methods of use thereof
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
TWI387592B (zh) 2005-08-30 2013-03-01 Novartis Ag 經取代之苯并咪唑及其作為與腫瘤形成相關激酶之抑制劑之方法
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
HRP20110621T2 (hr) 2006-09-15 2013-12-06 Pfizer Products Inc. SPOJEVI PIRIDO[2,3-d]PIRIMIDINONA I NJIHOVA UPOTREBA KAO INHIBITORI PI3
JP2011527703A (ja) 2008-07-11 2011-11-04 ノバルティス アーゲー （ａ）ホスホイノシタイド３−キナーゼ阻害剤および（ｂ）Ｒａｓ／Ｒａｆ／Ｍｅｋ経路のモジュレーターの配合物

Patent Citations (3)

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

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