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
tumor
compound
formula
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Expired - Fee Related
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English (en)
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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (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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CN2010800563069A Expired - Fee Related CN102740851B (zh) 2009-10-12 2010-10-11 Pi3k抑制剂和mek抑制剂的组合

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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)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20110028651A (ko) 2008-07-11 2011-03-21 노파르티스 아게 (ａ) 포스포이노시타이드 3-키나제 억제제 및 (ｂ) ｒａｓ/ｒａｆ/ｍｅｋ 경로의 조절제의 조합물
PT2385832E (pt) 2009-01-08 2015-11-02 Curis Inc Inibidores de fosfoinoritide 3-quinase com uma fração de ligação ao zinco
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
PT3111938T (pt) 2011-04-01 2019-07-10 Curis Inc Inibidores de fosfoinoritide 3-quinase com uma fração de ligação ao zinco
BR112014002353B1 (pt) 2011-08-01 2022-09-27 Genentech, Inc Usos de antagonistas de ligação do eixo pd-1 e inibidores de mek, composições farmacêuticas, e kit
CN103764144B (zh) * 2011-08-31 2016-07-20 诺华股份有限公司 Pi3k抑制剂与mek抑制剂的协同组合
JP6062442B2 (ja) 2011-10-13 2017-01-18 ジェネンテック， インコーポレイテッド 薬剤誘発性低酸症の治療
KR20140097205A (ko) * 2011-10-28 2014-08-06 제넨테크, 인크. 흑색종을 치료하는 치료 조합물 및 방법
WO2013082511A1 (en) 2011-12-02 2013-06-06 Genentech, Inc. Methods for overcoming tumor resistance to vegf antagonists
CN104334192A (zh) * 2012-04-06 2015-02-04 赛诺菲 使用pi3k抑制剂和mek抑制剂治疗癌症的方法
WO2013157648A1 (ja) * 2012-04-19 2013-10-24 国立大学法人九州大学 医薬組成物
CN104379163A (zh) 2012-06-08 2015-02-25 霍夫曼-拉罗奇有限公司 用于治疗癌症的磷酸肌醇3激酶抑制剂化合物和化疗剂的突变选择性及组合
WO2014022680A1 (en) 2012-08-02 2014-02-06 Genentech, Inc. Anti-etbr antibodies and immunoconjugates
BR112015002193A2 (pt) 2012-08-02 2017-07-04 Genentech Inc anticorpos anti-etbr e imunoconjugados
DK2884979T3 (da) * 2012-08-17 2019-09-02 Hoffmann La Roche Kombinationsbehandlinger mod melanom omfattende indgivelse af cobimetinib og vemurafenib
WO2014152358A2 (en) * 2013-03-14 2014-09-25 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
ES2779975T3 (es) 2014-02-07 2020-08-21 Verastem Inc Métodos y composiciones para tratar el crecimiento celular anormal
BR112017000672A2 (pt) 2014-07-15 2017-11-14 Genentech Inc composições para tratamento de câncer utilizando antagonistas de ligação de eixo pd-1 e inibidores de mek
EP3193902A4 (en) * 2014-09-11 2018-03-28 The Regents of The University of California mTORC1 INHIBITORS
EP3849554B1 (en) 2018-09-11 2025-01-29 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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1470356A1 (de) * 1964-01-15 1970-04-30 Thomae Gmbh Dr K Neue Thieno[3,2-d]pyrimidine und Verfahren zu ihrer Herstellung
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
US3763156A (en) * 1970-01-28 1973-10-02 Boehringer Sohn Ingelheim 2-heterocyclic amino-4-morpholinothieno(3,2-d)pyrimidines
CH592668A5 (enExample) * 1973-10-02 1977-10-31 Delalande Sa
GB1570494A (en) * 1975-11-28 1980-07-02 Ici Ltd Thienopyrimidine derivatives and their use as pesticides
US4510139A (en) * 1984-01-06 1985-04-09 Sterling Drug Inc. Substituted aminobenzamides and their use as agents which inhibit lipoxygenase activity
AU685933B2 (en) * 1994-04-01 1998-01-29 Shionogi & Co., Ltd. Oxime derivative and bactericide containing the same as active ingredient
US6974878B2 (en) * 2001-03-21 2005-12-13 Symyx Technologies, Inc. Catalyst ligands, catalytic metal complexes and processes using same
US6608053B2 (en) * 2000-04-27 2003-08-19 Yamanouchi Pharmaceutical Co., Ltd. Fused heteroaryl derivatives
US7498304B2 (en) * 2000-06-16 2009-03-03 Curis, Inc. Angiogenesis-modulating compositions and uses
AU7349801A (en) * 2000-07-19 2002-01-30 Warner Lambert Co Oxygenated esters of 4-iodo phenylamino benzhydroxamic acids
US7235537B2 (en) * 2002-03-13 2007-06-26 Array Biopharma, Inc. N3 alkylated benzimidazole derivatives as MEK inhibitors
KR101099281B1 (ko) * 2003-03-03 2011-12-26 어레이 바이오파마 인크. ｐ38 억제제 및 그의 사용 방법
US20050049276A1 (en) * 2003-07-23 2005-03-03 Warner-Lambert Company, Llc Imidazopyridines and triazolopyridines
US7538120B2 (en) * 2003-09-03 2009-05-26 Array Biopharma Inc. Method of treating inflammatory diseases
US7144907B2 (en) * 2003-09-03 2006-12-05 Array Biopharma Inc. Heterocyclic inhibitors of MEK and methods of use thereof
JP4931419B2 (ja) * 2003-09-19 2012-05-16 中外製薬株式会社 新規４−フェニルアミノ−ベンズアルドオキシム誘導体並びにそのｍｅｋ阻害剤としての使用
US7517994B2 (en) * 2003-11-19 2009-04-14 Array Biopharma Inc. Heterocyclic inhibitors of MEK and methods of use thereof
GB0423653D0 (en) 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
CA2658725A1 (en) * 2006-08-16 2008-02-21 Exelixis, Inc. Using pi3k and mek modulators in treatments of cancer
BRPI0816769A2 (pt) * 2007-09-12 2016-11-29 Hoffmann La Roche combinações de compostos inibidores de fosfoinositida 3-cinase e agentes quimioterapêuticos, e métodos de uso
TR201815685T4 (tr) * 2011-04-01 2018-11-21 Genentech Inc Kanser tedavisi için akt ve mek inhibe edici bileşiklerin kombinasyonları.

Patent Citations (3)

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

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