CN102740851B - Pi3k抑制剂和mek抑制剂的组合 - Google Patents

Pi3k抑制剂和mek抑制剂的组合 Download PDF

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Publication number
CN102740851B
CN102740851B CN2010800563069A CN201080056306A CN102740851B CN 102740851 B CN102740851 B CN 102740851B CN 2010800563069 A CN2010800563069 A CN 2010800563069A CN 201080056306 A CN201080056306 A CN 201080056306A CN 102740851 B CN102740851 B CN 102740851B
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gdc
patient
combination
compound
locally advanced
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Chinese (zh)
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CN102740851A (zh
Inventor
M.贝尔文
I.T.钱
L.弗里德曼
K.P.霍夫利科
J.普雷斯科特
J.沃林
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F Hoffmann La Roche AG
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F Hoffmann La Roche 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61K31/435—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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN2010800563069A 2009-10-12 2010-10-11 Pi3k抑制剂和mek抑制剂的组合 Expired - Fee Related CN102740851B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US25085209P 2009-10-12 2009-10-12
US61/250,852 2009-10-12
PCT/EP2010/065149 WO2011054620A1 (en) 2009-10-12 2010-10-11 Combinations of a pi3k inhibitor and a mek inhibitor

Publications (2)

Publication Number Publication Date
CN102740851A CN102740851A (zh) 2012-10-17
CN102740851B true CN102740851B (zh) 2013-12-18

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ID=43072663

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CN2010800563069A Expired - Fee Related CN102740851B (zh) 2009-10-12 2010-10-11 Pi3k抑制剂和mek抑制剂的组合

Country Status (24)

Country Link
US (1) US20110086837A1 (enExample)
EP (1) EP2488178B1 (enExample)
JP (2) JP2013507415A (enExample)
KR (1) KR101489045B1 (enExample)
CN (1) CN102740851B (enExample)
AR (1) AR078588A1 (enExample)
AU (1) AU2010314287A1 (enExample)
BR (1) BR112012008483A2 (enExample)
CA (1) CA2776944A1 (enExample)
CL (1) CL2012000913A1 (enExample)
CO (1) CO6531463A2 (enExample)
CR (1) CR20120173A (enExample)
EC (1) ECSP12011865A (enExample)
ES (1) ES2609767T3 (enExample)
IL (1) IL219105A0 (enExample)
MA (1) MA33974B1 (enExample)
MX (1) MX345155B (enExample)
NZ (1) NZ599939A (enExample)
PE (1) PE20121816A1 (enExample)
PH (1) PH12012500709A1 (enExample)
RU (1) RU2563193C2 (enExample)
TW (1) TWI428336B (enExample)
WO (1) WO2011054620A1 (enExample)
ZA (1) ZA201202618B (enExample)

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MX336723B (es) 2008-07-11 2016-01-28 Novartis Ag Combinacion de (a) un inhibidor de fosfoinositido 3-cinasa y (b) un modulador de la ruta de ras/raf/mek.
EA024252B1 (ru) 2009-01-08 2016-08-31 Кьюрис, Инк. Ингибиторы фосфоинозитид-3-киназ с цинксвязывающей группой
PH12012501361A1 (en) 2009-12-31 2012-10-22 Centro Nac De Investigaciones Oncologicas Cnio Tricyclic compounds for use as kinase inhibitors
WO2012098387A1 (en) 2011-01-18 2012-07-26 Centro Nacional De Investigaciones Oncológicas (Cnio) 6, 7-ring-fused triazolo [4, 3 - b] pyridazine derivatives as pim inhibitors
HUE028910T2 (en) 2011-04-01 2017-01-30 Curis Inc Phosphoinositide 3-kinase inhibitor with a zinc binding moiety
BR122022000334B1 (pt) * 2011-08-01 2023-03-21 Genentech, Inc Composição farmacêutica compreendendo um antagonista de ligação ao eixo pd-1 e um inibidor de mek
CA2846454A1 (en) * 2011-08-31 2013-05-10 Novartis Ag Synergistic combinations of pi3k- and mek-inhibitors
WO2013055996A1 (en) 2011-10-13 2013-04-18 Genentech, Inc. Treatment of pharmacological-induced hypochlorhydria
EP2776051A4 (en) * 2011-10-28 2015-06-17 Hoffmann La Roche THERAPEUTIC COMBINATIONS AND METHOD FOR THE TREATMENT OF MELANOMA
WO2013082511A1 (en) 2011-12-02 2013-06-06 Genentech, Inc. Methods for overcoming tumor resistance to vegf antagonists
AU2013243429A1 (en) * 2012-04-06 2014-10-23 Merck Patent Gmbh Methods for treating cancer using PI3K inhibitor and MEK inhibitor
WO2013157648A1 (ja) * 2012-04-19 2013-10-24 国立大学法人九州大学 医薬組成物
SG10201706196XA (en) 2012-06-08 2017-08-30 Hoffmann La Roche Mutant selectivity and combinations of a phosphoinositide 3 kinase inhibitor compound and chemotherapeutic agents for the treatment of cancer
KR20150039818A (ko) 2012-08-02 2015-04-13 제넨테크, 인크. 항-etbr 항체 및 면역접합체
KR20150032886A (ko) 2012-08-02 2015-03-30 제넨테크, 인크. 항-etbr 항체 및 면역접합체
HK1206605A1 (en) 2012-08-17 2016-01-15 霍夫曼-拉罗奇有限公司 Combination therapies for melanoma comprising administering cobimetinib and vemurafinib
EP2968540A2 (en) * 2013-03-14 2016-01-20 Genentech, Inc. Combinations of a mek inhibitor compound with an her3/egfr inhibitor compound and methods of use
US9532987B2 (en) 2013-09-05 2017-01-03 Genentech, Inc. Use of a combination of a MEK inhibitor and an ERK inhibitor for treatment of hyperproliferative diseases
WO2015120289A1 (en) 2014-02-07 2015-08-13 Verastem, Inc. Methods and compositions for treating abnormal cell growth
CA2954508A1 (en) 2014-07-15 2016-01-21 Genentech, Inc. Compositions for treating cancer using pd-1 axis binding antagonists and mek inhibitors
CN107073066B (zh) * 2014-09-11 2021-09-17 加利福尼亚大学董事会 mTORC1抑制剂
WO2020055840A1 (en) 2018-09-11 2020-03-19 Curis Inc. Combination therapy with a phosphoinositide 3-kinase inhibitor with a zinc binding moiety
CN110420330B (zh) * 2019-07-19 2020-05-29 南京医科大学 一种pi3k与mth1靶向药组合物的制药用途
WO2021047783A1 (en) 2019-09-13 2021-03-18 The Institute Of Cancer Research: Royal Cancer Hospital Vs-6063 in combination with ch5126766 for the treatment of cancer
US11873296B2 (en) 2022-06-07 2024-01-16 Verastem, Inc. Solid forms of a dual RAF/MEK inhibitor

Citations (3)

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WO2007044515A1 (en) * 2005-10-07 2007-04-19 Exelixis, Inc. Azetidines as mek inhibitors for the treatment of proliferative diseases
WO2007129161A2 (en) * 2006-04-26 2007-11-15 F. Hoffmann-La Roche Ag Thieno [3, 2-d] pyrimidine derivative useful as pi3k inhibitor
WO2008070740A1 (en) * 2006-12-07 2008-06-12 F.Hoffmann-La Roche Ag Phosphoinositide 3-kinase inhibitor compounds and methods of use

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BE754606A (fr) * 1969-08-08 1971-02-08 Thomae Gmbh Dr K Nouvelles 2-aminoalcoylamino-thieno(3,2-d)pyrimidines et leurs procedesde fabrication
BE759493A (fr) * 1969-11-26 1971-05-25 Thomae Gmbh Dr K Nouvelles 2-(5-nitro-2-furyl)-thieno(3,2-d) pyrimidines et procedes pour les fabriquer
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WO2007044515A1 (en) * 2005-10-07 2007-04-19 Exelixis, Inc. Azetidines as mek inhibitors for the treatment of proliferative diseases
WO2007129161A2 (en) * 2006-04-26 2007-11-15 F. Hoffmann-La Roche Ag Thieno [3, 2-d] pyrimidine derivative useful as pi3k inhibitor
WO2008070740A1 (en) * 2006-12-07 2008-06-12 F.Hoffmann-La Roche Ag Phosphoinositide 3-kinase inhibitor compounds and methods of use

Also Published As

Publication number Publication date
AU2010314287A1 (en) 2012-05-03
MX2012004286A (es) 2012-05-22
RU2563193C2 (ru) 2015-09-20
BR112012008483A2 (pt) 2019-09-24
MX345155B (es) 2017-01-18
KR20120064132A (ko) 2012-06-18
ECSP12011865A (es) 2012-06-29
HK1175125A1 (en) 2013-06-28
TWI428336B (zh) 2014-03-01
CA2776944A1 (en) 2011-05-12
PH12012500709A1 (en) 2012-10-29
MA33974B1 (fr) 2013-02-01
TW201118082A (en) 2011-06-01
AU2010314287A2 (en) 2012-07-12
ZA201202618B (en) 2014-10-29
RU2012118974A (ru) 2013-11-20
PE20121816A1 (es) 2013-01-02
KR101489045B1 (ko) 2015-02-02
CN102740851A (zh) 2012-10-17
CO6531463A2 (es) 2012-09-28
WO2011054620A1 (en) 2011-05-12
EP2488178B1 (en) 2016-11-16
CR20120173A (es) 2012-07-04
IL219105A0 (en) 2012-06-28
JP5745678B2 (ja) 2015-07-08
AR078588A1 (es) 2011-11-16
JP2015038110A (ja) 2015-02-26
EP2488178A1 (en) 2012-08-22
ES2609767T3 (es) 2017-04-24
CL2012000913A1 (es) 2012-09-14
JP2013507415A (ja) 2013-03-04
US20110086837A1 (en) 2011-04-14
NZ599939A (en) 2014-02-28

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