JP6150813B2 - 増殖性疾患の治療方法 - Google Patents
増殖性疾患の治療方法 Download PDFInfo
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- JP6150813B2 JP6150813B2 JP2014541283A JP2014541283A JP6150813B2 JP 6150813 B2 JP6150813 B2 JP 6150813B2 JP 2014541283 A JP2014541283 A JP 2014541283A JP 2014541283 A JP2014541283 A JP 2014541283A JP 6150813 B2 JP6150813 B2 JP 6150813B2
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- Prior art keywords
- braf
- treatment
- inhibitor
- mutation
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Images
Classifications
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (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)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161558619P | 2011-11-11 | 2011-11-11 | |
| US61/558,619 | 2011-11-11 | ||
| PCT/US2012/064269 WO2013070996A1 (en) | 2011-11-11 | 2012-11-09 | Method of treating a proliferative disease |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014533272A JP2014533272A (ja) | 2014-12-11 |
| JP2014533272A5 JP2014533272A5 (enExample) | 2015-12-24 |
| JP6150813B2 true JP6150813B2 (ja) | 2017-06-21 |
Family
ID=47279036
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014541283A Active JP6150813B2 (ja) | 2011-11-11 | 2012-11-09 | 増殖性疾患の治療方法 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US11007194B2 (enExample) |
| EP (1) | EP2776037B1 (enExample) |
| JP (1) | JP6150813B2 (enExample) |
| CN (2) | CN103917236A (enExample) |
| AU (1) | AU2012335663B2 (enExample) |
| BR (1) | BR112014011223A8 (enExample) |
| CA (1) | CA2855243C (enExample) |
| MX (1) | MX354725B (enExample) |
| RU (1) | RU2622015C2 (enExample) |
| WO (1) | WO2013070996A1 (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR077975A1 (es) | 2009-08-28 | 2011-10-05 | Irm Llc | Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina |
| EP3574904A1 (en) * | 2012-08-07 | 2019-12-04 | Array Biopharma, Inc. | Pharmaceutical combinations comprising a b-raf inhibitor, an egfr inhibitor and optionally a pi3k-alpha inhibitor |
| CN109890386B (zh) | 2016-06-03 | 2022-05-24 | 阵列生物制药公司 | 药物组合 |
| WO2018107146A1 (en) * | 2016-12-11 | 2018-06-14 | Memorial Sloan Kettering Cancer Center | Methods and compositions for treatment of braf mutant cancers |
| WO2020011141A1 (zh) * | 2018-07-12 | 2020-01-16 | 深圳市塔吉瑞生物医药有限公司 | 一种二芳基吡唑化合物及包含该化合物的组合物及其用途 |
| TWI817018B (zh) | 2019-06-28 | 2023-10-01 | 美商艾瑞生藥股份有限公司 | 用於治療braf相關的疾病和失調症之化合物 |
| IL294484A (en) * | 2020-01-07 | 2022-09-01 | Revolution Medicines Inc | Shp2 inhibitor dosing and methods of treating cancer |
| PE20231651A1 (es) | 2020-06-09 | 2023-10-17 | Array Biopharma Inc | Compuestos para el tratamiento de enfermedades y trastornos asociados a braf |
| CA3257280A1 (en) | 2022-05-25 | 2023-11-30 | Msd International Gmbh | COMBINATION OF A BRAF INHIBITOR, AN EGFR INHIBITOR AND A PD-1 ANTAGONIST FOR THE TREATMENT OF COLORECTAL CANCER MSI-H/DMMR, WITH BRAF V600E MUTATION |
| ES3035530T3 (en) | 2023-03-09 | 2025-09-04 | Minneamrita Therapeutics Llc | Drug combination for the treatment of stomach cancer |
| WO2025003956A1 (en) | 2023-06-30 | 2025-01-02 | Pfizer Inc. | High drug loading formulations of encorafenib |
Family Cites Families (58)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6358932B1 (en) | 1994-05-31 | 2002-03-19 | Isis Pharmaceticals, Inc. | Antisense oligonucleotide inhibition of raf gene expression |
| US6391636B1 (en) | 1994-05-31 | 2002-05-21 | Isis Pharmaceuticals, Inc. | Antisense oligonucleotide modulation of raf gene expression |
| US6037136A (en) | 1994-10-24 | 2000-03-14 | Cold Spring Harbor Laboratory | Interactions between RaF proto-oncogenes and CDC25 phosphatases, and uses related thereto |
| US5717100A (en) | 1995-10-06 | 1998-02-10 | Merck & Co., Inc. | Substituted imidazoles having anti-cancer and cytokine inhibitory activity |
| AR012634A1 (es) | 1997-05-02 | 2000-11-08 | Sugen Inc | Compuesto basado en quinazolina, composicion famaceutica que lo comprende, metodo para sintetizarlo, su uso, metodos de modulacion de la funcion deserina/treonina proteinaquinasa con dicho compuesto y metodo in vitro para identificar compuestos que modulan dicha funcion |
| IL132991A (en) | 1997-05-22 | 2005-11-20 | Searle & Co | Substituted pyrazoles, pharmaceutical compositionscomprising them and their use as p38 inase inhibi tors |
| US6514977B1 (en) | 1997-05-22 | 2003-02-04 | G.D. Searle & Company | Substituted pyrazoles as p38 kinase inhibitors |
| GB9716557D0 (en) | 1997-08-06 | 1997-10-08 | Glaxo Group Ltd | Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity |
| US6022884A (en) | 1997-11-07 | 2000-02-08 | Amgen Inc. | Substituted pyridine compounds and methods of use |
| US6204467B1 (en) | 1998-03-24 | 2001-03-20 | Ford Global Technologies, Inc. | Method and apparatus for resistive welding |
| RU2319693C9 (ru) | 1999-01-13 | 2008-08-20 | Байер Копэрейшн | Производные мочевины (варианты), фармацевтическая композиция (варианты) и способ лечения заболевания, связанного с ростом раковых клеток (варианты) |
| US6316435B2 (en) | 1999-02-24 | 2001-11-13 | Supergen, Inc. | Combination therapy for lymphoproliferative diseases |
| PE20020354A1 (es) | 2000-09-01 | 2002-06-12 | Novartis Ag | Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda) |
| US20050043409A1 (en) | 2001-10-25 | 2005-02-24 | Chen Ying-Nan Pan | Combinations comprising a selective cyclooxygenase-2 inhibitor |
| ATE374753T1 (de) | 2001-12-21 | 2007-10-15 | Vernalis Cambridge Ltd | 3-(2,4)dihydroxyphenyl-4-phenylpyrazole und deren medizinische verwendung |
| BRPI0414698A (pt) | 2003-09-23 | 2006-11-28 | Novartis Ag | combinação de um inibidor receptor de vegf com um agente quimioterapêutico |
| CA2545942C (en) | 2003-11-14 | 2012-07-10 | Lorus Therapeutics Inc. | Aryl imidazoles and their use as anti-cancer agents |
| BRPI0506760A (pt) | 2004-01-09 | 2007-05-22 | Novartis Ag | derivados de fenil-[4-(3-fenil-1h-pirazol-4-il)-pirimidin-2-il]-amina como inibidores de igf-ir |
| RU2401265C2 (ru) | 2004-06-10 | 2010-10-10 | Айрм Ллк | Соединения и композиции в качестве ингибиторов протеинкиназы |
| KR20070113295A (ko) | 2005-03-17 | 2007-11-28 | 노파르티스 아게 | 티로신/트레오닌 키나제 억제제, 특히 b-raf 키나제억제제로서의n-[3-(1-아미노-5,6,7,8-테트라히드로-2,4,4b-트리아자플루오렌-9-일)-페닐]벤즈아미드 |
| US20070099856A1 (en) * | 2005-05-13 | 2007-05-03 | Gumerlock Paul H | Combined treatment with docetaxel and an epidermal growth factor receptor kinase inhibitor using an intermittent dosing regimen |
| AU2006279794B2 (en) | 2005-08-12 | 2011-04-07 | Synta Pharmaceuticals Corp. | Pyrazole compounds that modulate HSP90 activity |
| AU2006284053B2 (en) | 2005-08-22 | 2010-04-22 | Novartis Ag | Pharmaceutical compositions comprising a pH-dependent drug, a pH modifier and a retarding agent |
| US20080242667A1 (en) | 2005-08-26 | 2008-10-02 | Smithkline Beecham Corporation | Pyrimidinyl-Pyrazole Inhibitors of Aurora Kinases |
| 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 |
| JP2009530261A (ja) | 2006-03-16 | 2009-08-27 | ファイザー・プロダクツ・インク | ピラゾール化合物 |
| JP2009532497A (ja) | 2006-04-05 | 2009-09-10 | ノバルティス アクチエンゲゼルシャフト | 癌を処置するための治療剤の組合せ |
| WO2007123892A2 (en) | 2006-04-17 | 2007-11-01 | Arqule Inc. | Raf inhibitors and their uses |
| CA2663366C (en) | 2006-10-02 | 2012-02-07 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| AU2007308045A1 (en) | 2006-10-06 | 2008-04-17 | Irm Llc | Protein kinase inhibitors and methods for using thereof |
| WO2008100985A2 (en) | 2007-02-15 | 2008-08-21 | Novartis Ag | Combination of lbh589 with other therapeutic agents for treating cancer |
| US20090022789A1 (en) | 2007-07-18 | 2009-01-22 | Supernus Pharmaceuticals, Inc. | Enhanced formulations of lamotrigine |
| EA201000113A1 (ru) | 2007-08-01 | 2010-08-30 | Пфайзер Инк. | Пиразольные соединения |
| AU2008313622A1 (en) | 2007-10-19 | 2009-04-23 | Abbott Gmbh & Co. Kg | Solid dispersion product of N-aryl urea-based drugs |
| AU2008323287B2 (en) | 2007-11-14 | 2011-07-14 | Addex Pharma S.A. | Imidazo[1,2-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors |
| US8129394B2 (en) | 2008-03-21 | 2012-03-06 | Novartis Ag | Heteroaryl-substituted imidazole compounds and uses thereof |
| UA103319C2 (en) | 2008-05-06 | 2013-10-10 | Глаксосмитклайн Ллк | Thiazole- and oxazole-benzene sulfonamide compounds |
| BRPI0916356B1 (pt) | 2008-07-24 | 2022-08-23 | Nerviano Medical Sciences S.R.L | 3,4-diaril pirazois como inibidores da proteína quinase |
| MX2011001090A (es) | 2008-07-28 | 2011-03-15 | Gilead Sciences Inc | Compuestos de inhibidor de desacetilasa de histona de cicloalquilideno y heterocicloalquilideno. |
| US8778929B2 (en) | 2008-09-29 | 2014-07-15 | Boehringer Ingelheim International Gmbh | Substituted heteroaryl inhibitors of B-RAF |
| MY160340A (en) | 2008-10-07 | 2017-02-28 | Astrazeneca Uk Ltd | Pharmaceutical formulation 514 |
| US20110293750A1 (en) | 2008-11-11 | 2011-12-01 | Yale University | Activated wnt-beta-catenin signaling in melanoma |
| US8524707B2 (en) | 2008-12-19 | 2013-09-03 | Nerviano Medical Sciences S.R.L. | Bicyclic pyrazoles as protein kinase inhibitors |
| AR075180A1 (es) | 2009-01-29 | 2011-03-16 | Novartis Ag | Formulaciones orales solidas de una pirido-pirimidinona |
| RU2402602C1 (ru) | 2009-02-12 | 2010-10-27 | Государственное учреждение Российский онкологический научный центр им. Н.Н. Блохина РАМН | КЛЕТОЧНАЯ ЛИНИЯ МЕЛАНОМЫ ЧЕЛОВЕКА mel Rac, ИСПОЛЬЗУЕМАЯ ДЛЯ ПОЛУЧЕНИЯ ПРОТИВООПУХОЛЕВЫХ ВАКЦИН |
| WO2010100127A1 (en) | 2009-03-04 | 2010-09-10 | Novartis Ag | Disubstituted imidazole derivatives as modulators of raf kinase |
| TWI532484B (zh) | 2009-06-08 | 2016-05-11 | 艾伯維有限公司 | 包含凋亡促進劑之固態分散劑 |
| US8546413B2 (en) | 2009-06-15 | 2013-10-01 | Nerviano Medical Sciences S.R.L. | Substituted pyrimidinylpyrrolopyridinone derivatives, process for their preparation and their use as kinase inhibitors |
| KR101256018B1 (ko) | 2009-08-20 | 2013-04-18 | 한국과학기술연구원 | 단백질 키나아제 저해활성을 갖는 1,3,6-치환된 인돌 화합물 |
| AR077975A1 (es) | 2009-08-28 | 2011-10-05 | Irm Llc | Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina |
| US8242260B2 (en) | 2009-08-28 | 2012-08-14 | Novartis Ag | Compounds and compositions as protein kinase inhibitors |
| EA023942B1 (ru) | 2010-01-27 | 2016-07-29 | НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. | Сульфонамидные производные 3,4-диарилпиразолов в качестве ингибиторов протеинкиназы |
| RU2639876C2 (ru) | 2010-03-30 | 2017-12-25 | Версеон Корпорейшн | Мультизамещенные ароматические соединения в качестве ингибиторов тромбина |
| EP2601185B1 (en) | 2010-08-03 | 2015-10-07 | Nerviano Medical Sciences S.r.l. | Derivatives of pyrazolophenyl-benzenesulfonamide compounds and use thereof as antitumor agents |
| EP2688572B1 (en) | 2011-03-21 | 2017-05-03 | Valcuria AB | A pharmaceutical composition comprising a hdac inhibitor and a steroid and the use thereof. |
| CA2844407A1 (en) | 2011-06-14 | 2012-12-20 | Novartis Ag | Combination of panobinostat and ruxolitinib in the treatment of cancer such as a myeloproliferative neoplasm |
| KR102091295B1 (ko) | 2011-11-23 | 2020-03-19 | 어레이 바이오파마 인크. | 제약 제제 |
| CA2890663A1 (en) | 2012-11-08 | 2014-05-15 | Novartis Ag | Pharmaceutical combination comprising a b-raf inhibitor and a histone deacetylase inhibitor and their use in the treatment of proliferative diseases |
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| AU2012335663A1 (en) | 2014-05-29 |
| US20140275136A1 (en) | 2014-09-18 |
| JP2014533272A (ja) | 2014-12-11 |
| CA2855243A1 (en) | 2013-05-16 |
| CN103917236A (zh) | 2014-07-09 |
| US11007194B2 (en) | 2021-05-18 |
| CN108542906A (zh) | 2018-09-18 |
| RU2014117707A (ru) | 2015-12-20 |
| RU2622015C2 (ru) | 2017-06-08 |
| WO2013070996A1 (en) | 2013-05-16 |
| MX354725B (es) | 2018-03-16 |
| EP2776037B1 (en) | 2019-01-09 |
| EP2776037A1 (en) | 2014-09-17 |
| AU2012335663B2 (en) | 2015-12-24 |
| CA2855243C (en) | 2020-04-14 |
| HK1198920A1 (en) | 2015-06-19 |
| BR112014011223A2 (pt) | 2017-05-09 |
| MX2014005726A (es) | 2014-05-28 |
| BR112014011223A8 (pt) | 2023-01-31 |
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