AU2012333092B2 - Synergistic combinations of PI3K- and MEK-inhibitors - Google Patents

Synergistic combinations of PI3K- and MEK-inhibitors Download PDF

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Publication number
AU2012333092B2
AU2012333092B2 AU2012333092A AU2012333092A AU2012333092B2 AU 2012333092 B2 AU2012333092 B2 AU 2012333092B2 AU 2012333092 A AU2012333092 A AU 2012333092A AU 2012333092 A AU2012333092 A AU 2012333092A AU 2012333092 B2 AU2012333092 B2 AU 2012333092B2
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AU
Australia
Prior art keywords
combination
mutation
compound
amide
pharmaceutically acceptable
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Ceased
Application number
AU2012333092A
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English (en)
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AU2012333092A1 (en
Inventor
Markus Boehm
Jan GCE COSAERT
Emmanuelle DI TOMASO
Christine Fritsch
Xizhong Huang
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Novartis AG
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Novartis AG
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Publication of AU2012333092A1 publication Critical patent/AU2012333092A1/en
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Publication of AU2012333092B2 publication Critical patent/AU2012333092B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • 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
    • A61K31/4427Non 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
    • A61K31/435Heterocyclic 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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2012333092A 2011-08-31 2012-08-30 Synergistic combinations of PI3K- and MEK-inhibitors Ceased AU2012333092B2 (en)

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
AU2012333092A1 AU2012333092A1 (en) 2014-03-06
AU2012333092B2 true AU2012333092B2 (en) 2016-04-21

Family

ID=47720713

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2012333092A Ceased AU2012333092B2 (en) 2011-08-31 2012-08-30 Synergistic combinations of PI3K- and MEK-inhibitors

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
MX2010007419A (es) 2008-01-04 2010-11-12 Intellikine Inc Ciertas entidades quimicas, composiciones y metodos.
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
ES2637113T3 (es) 2011-01-10 2017-10-10 Infinity Pharmaceuticals, Inc. Procedimientos para preparar isoquinolinonas y formas sólidas de isoquinolinonas
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
AU2013337717B2 (en) 2012-11-01 2018-10-25 Infinity Pharmaceuticals, Inc. Treatment of cancers using PI3 kinase isoform modulators
CA2912346A1 (en) * 2013-06-11 2014-12-18 Novartis Ag Pharmaceutical combinations of a pi3k inhibitor and a microtubule destabilizing agent
BR112015030578A2 (pt) * 2013-06-18 2017-07-25 Novartis Ag combinações farmacêuticas
BR112016012141A2 (pt) * 2014-01-15 2017-08-08 Novartis Ag "combinações farmacêuticas, uso das mesmas, e embalagem comercial"
US20150320754A1 (en) * 2014-04-16 2015-11-12 Infinity Pharmaceuticals, Inc. Combination therapies
WO2015160975A2 (en) 2014-04-16 2015-10-22 Infinity Pharmaceuticals, Inc. Combination therapies
KR102124715B1 (ko) * 2015-11-03 2020-06-18 제넨테크, 인크. 암의 치료를 위한 bcl-2 억제제 및 mek 억제제의 조합물
SG11201811237WA (en) 2016-06-24 2019-01-30 Infinity Pharmaceuticals Inc Combination therapies
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
WO2003077914A1 (en) * 2002-03-13 2003-09-25 Array Biopharma, Inc N3 alkylated benzimidazole derivatives as mek inhibitors
WO2007044084A2 (en) * 2005-05-18 2007-04-19 Array Biopharma Inc. Heterocyclic inhibitors of mek and methods of use thereof
WO2010029082A1 (en) * 2008-09-10 2010-03-18 Novartis Ag Organic compounds

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3811775B2 (ja) 2000-07-19 2006-08-23 ワーナー−ランバート カンパニー リミティド ライアビリティー カンパニー 4−ヨードフェニルアミノベンズヒドロキサム酸の酸素化エステル
RU2192861C1 (ru) 2001-06-29 2002-11-20 Новосибирский институт биоорганической химии СО РАН Композиция для антибластической терапии
US7235537B2 (en) * 2002-03-13 2007-06-26 Array Biopharma, Inc. N3 alkylated benzimidazole derivatives as MEK inhibitors
SI1761528T1 (sl) 2004-06-11 2008-06-30 Japan Tobacco Inc 5-amino-2,4,7-triokso-3,4,7,8-tetrahidro-2H-pirido(2,3-D)pirimidinski derivati in sorodne spojine za zdravljenje raka
US7378423B2 (en) 2004-06-11 2008-05-27 Japan Tobacco Inc. Pyrimidine compound and medical use thereof
WO2006081172A2 (en) * 2005-01-26 2006-08-03 Irm Llc Compounds and compositions as protein kinase inhibitors
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
PT2074122E (pt) 2006-09-15 2011-08-24 Pfizer Prod Inc Compostos de pirido(2,3-d)-pirimidinona e sua utilização como inibidores de pi3
US20110105521A1 (en) 2008-07-11 2011-05-05 Novartis Ag Combination of (a) a phosphoinositide 3-kinase inhibitor and (b) a modulator of ras/raf/mek pathway
CA2776944A1 (en) * 2009-10-12 2011-05-12 F. Hoffmann-La Roche Ag Combinations of a pi3k inhibitor and a mek inhibitor

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003077914A1 (en) * 2002-03-13 2003-09-25 Array Biopharma, Inc N3 alkylated benzimidazole derivatives as mek inhibitors
WO2007044084A2 (en) * 2005-05-18 2007-04-19 Array Biopharma Inc. Heterocyclic inhibitors of mek and methods of use thereof
WO2010029082A1 (en) * 2008-09-10 2010-03-18 Novartis Ag Organic compounds

Also Published As

Publication number Publication date
US20140179744A1 (en) 2014-06-26
RU2607944C2 (ru) 2017-01-11
CN103764144B (zh) 2016-07-20
WO2013066483A1 (en) 2013-05-10
RU2014112198A (ru) 2015-10-10
AU2012333092A1 (en) 2014-03-06
US9675595B2 (en) 2017-06-13
CN103764144A (zh) 2014-04-30
JP2014525454A (ja) 2014-09-29
CA2846454A1 (en) 2013-05-10
KR20140072028A (ko) 2014-06-12
EP2750675A1 (en) 2014-07-09
JP6058009B2 (ja) 2017-01-11
BR112014004587A2 (pt) 2017-03-14
MX2014002471A (es) 2014-03-27

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FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired