CN108542906A - 治疗增生性疾病的方法 - Google Patents
治疗增生性疾病的方法 Download PDFInfo
- Publication number
- CN108542906A CN108542906A CN201810135736.8A CN201810135736A CN108542906A CN 108542906 A CN108542906 A CN 108542906A CN 201810135736 A CN201810135736 A CN 201810135736A CN 108542906 A CN108542906 A CN 108542906A
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- China
- Prior art keywords
- proliferative disease
- braf
- treating
- braf inhibitor
- cancer
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- Pending
Links
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims description 19
- 230000002062 proliferating effect Effects 0.000 title claims description 19
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- 229940079593 drug Drugs 0.000 claims description 7
- 201000001441 melanoma Diseases 0.000 claims description 7
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- 108010091528 Proto-Oncogene Proteins B-raf Proteins 0.000 claims description 5
- 102000018471 Proto-Oncogene Proteins B-raf Human genes 0.000 claims description 5
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 4
- 101000984753 Homo sapiens Serine/threonine-protein kinase B-raf Proteins 0.000 claims description 3
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- SYLABBNLHCTJEF-UHFFFAOYSA-N 2-pyridin-2-yloxy-1h-benzimidazole Chemical group N=1C2=CC=CC=C2NC=1OC1=CC=CC=N1 SYLABBNLHCTJEF-UHFFFAOYSA-N 0.000 description 1
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- OGEBRHQLRGFBNV-RZDIXWSQSA-N chembl2036808 Chemical group C12=NC(NCCCC)=NC=C2C(C=2C=CC(F)=CC=2)=NN1C[C@H]1CC[C@H](N)CC1 OGEBRHQLRGFBNV-RZDIXWSQSA-N 0.000 description 1
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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
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (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 | ||
| CN201280054663.0A CN103917236A (zh) | 2011-11-11 | 2012-11-09 | 治疗增生性疾病的方法 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280054663.0A Division CN103917236A (zh) | 2011-11-11 | 2012-11-09 | 治疗增生性疾病的方法 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN108542906A true CN108542906A (zh) | 2018-09-18 |
Family
ID=47279036
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201810135736.8A Pending CN108542906A (zh) | 2011-11-11 | 2012-11-09 | 治疗增生性疾病的方法 |
| CN201280054663.0A Pending CN103917236A (zh) | 2011-11-11 | 2012-11-09 | 治疗增生性疾病的方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280054663.0A Pending CN103917236A (zh) | 2011-11-11 | 2012-11-09 | 治疗增生性疾病的方法 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US11007194B2 (enExample) |
| EP (1) | EP2776037B1 (enExample) |
| JP (1) | JP6150813B2 (enExample) |
| CN (2) | CN108542906A (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 |
| JP6342396B2 (ja) * | 2012-08-07 | 2018-06-13 | ノバルティス アーゲー | Ｂ−Ｒａｆ阻害薬、ＥＧＦＲ阻害薬及び場合によってはＰＩ３Ｋ−α阻害薬を含む組合せ医薬 |
| BR112018074941A2 (pt) * | 2016-06-03 | 2019-03-12 | Caponigro Giordano | combinações farmacêuticas |
| US11590133B2 (en) * | 2016-12-11 | 2023-02-28 | Memorial Sloan Kettering Cancer Center | Methods and compositions for treatment of BRAF mutant cancers |
| CN110256408B (zh) * | 2018-07-12 | 2022-03-22 | 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 |
| CA3163703A1 (en) * | 2020-01-07 | 2021-07-15 | Steve Kelsey | Shp2 inhibitor dosing and methods of treating cancer |
| AU2021289163B2 (en) | 2020-06-09 | 2024-05-02 | Array Biopharma Inc. | 4-oxo-3,4-dihydroquinazolinon compounds for the treatment of BRAF-associated diseases and disorders |
| 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 |
| AU2024204522B1 (en) | 2023-03-09 | 2024-08-22 | Minneamrita Therapeutics Llc | Drug combination for treatment of gastric cancer |
| WO2025003956A1 (en) | 2023-06-30 | 2025-01-02 | Pfizer Inc. | High drug loading formulations of encorafenib |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011025927A1 (en) * | 2009-08-28 | 2011-03-03 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
Family Cites Families (57)
| 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 |
| US6514977B1 (en) | 1997-05-22 | 2003-02-04 | G.D. Searle & Company | Substituted pyrazoles as p38 kinase inhibitors |
| JP2002508754A (ja) | 1997-05-22 | 2002-03-19 | ジー ディ サール アンド カンパニ | ｐ３８キナーゼ阻害剤としての置換基を有するピラゾール類 |
| 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 |
| US7351834B1 (en) | 1999-01-13 | 2008-04-01 | Bayer Pharmaceuticals Corporation | ω-Carboxyaryl substituted diphenyl ureas as raf kinase inhibitors |
| 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) |
| DE60224299T2 (de) | 2001-10-25 | 2008-12-11 | Novartis Ag | Kombinationsmedikationen mit einem selektiven cyclooxygenase-2-inhibitor |
| EP1456180B1 (en) | 2001-12-21 | 2007-10-03 | Vernalis (Cambridge) Limited | 3-(2,4)dihydroxyphenyl-4-phenylpyrazoles and their medical use |
| US20080085902A1 (en) | 2003-09-23 | 2008-04-10 | Guido Bold | Combination Of A Vegf Receptor Inhibitor Or With A Chemotherapeutic Agent |
| DK1692113T3 (en) | 2003-11-14 | 2018-01-08 | Lorus Therapeutics Inc | ARYLIMIDAZOLES AND USE THEREOF AS ANTICANCES |
| EP1706400A1 (en) | 2004-01-09 | 2006-10-04 | Novartis AG | Phenyl- 4-(3-phenyl-1h-pyrazol-4-yl)-pyrimidin-2-yl -amine derivatives as igf-ir inhibitors |
| ES2396135T3 (es) | 2004-06-10 | 2013-02-19 | Irm Llc | Compuestos y composiciones como inhibidores de proteínas cinasas |
| CA2601766A1 (en) | 2005-03-17 | 2006-09-28 | Novartis Ag | N- [3- (1-amin0-5, 6, 7, 8-tetrahydro-2 , 4, 4b-triazafluoren-9-yl)-phenyl] benzamides as tyrosine/threonine kinase inhibitors, in particular b-raf kinase |
| 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 |
| US7608635B2 (en) | 2005-08-12 | 2009-10-27 | Synta Pharmaceuticals Corp. | Pyrazole compounds that modulate HSP90 activity |
| EP1919460A2 (en) | 2005-08-22 | 2008-05-14 | Novartis AG | Pharmaceutical compositions comprising a ph-dependent drug, a ph modifier and a retarding agent |
| EP1917258A2 (en) | 2005-08-26 | 2008-05-07 | SmithKline Beecham Corporation | Pyrimidinyl-pyrazole inhibitors of aurora kinases |
| TW200804345A (en) | 2005-08-30 | 2008-01-16 | Novartis Ag | Substituted benzimidazoles and methods of preparation |
| CA2643066A1 (en) | 2006-03-16 | 2007-09-20 | Pfizer Products Inc. | Pyrazole compounds |
| WO2007115286A2 (en) | 2006-04-05 | 2007-10-11 | Novartis Ag. | Combinations of therapeutic agents for treating cancer |
| WO2007123892A2 (en) | 2006-04-17 | 2007-11-01 | Arqule Inc. | Raf inhibitors and their uses |
| MX2009003456A (es) | 2006-10-02 | 2009-04-14 | Irm Llc | Compuestos y composiciones como inhibidores de proteina cinasa. |
| CN101522026A (zh) | 2006-10-06 | 2009-09-02 | Irm责任有限公司 | 蛋白激酶抑制剂及其应用方法 |
| EP2491923A3 (en) | 2007-02-15 | 2012-12-26 | Novartis AG | Combinations of therapeutic agents for treating cancer |
| US20090022789A1 (en) | 2007-07-18 | 2009-01-22 | Supernus Pharmaceuticals, Inc. | Enhanced formulations of lamotrigine |
| KR20100038119A (ko) | 2007-08-01 | 2010-04-12 | 화이자 인코포레이티드 | 피라졸 화합물 및 ｒａｆ 억제제로서 이의 용도 |
| UA100865C2 (ru) | 2007-10-19 | 2013-02-11 | Эбботт Гмбх Унд Ко. Кг | Твердый дисперсный продукт лекарственных средств на основе n-арилмочевины |
| EP2220083B1 (en) | 2007-11-14 | 2017-07-19 | Janssen Pharmaceuticals, Inc. | Imidazo[1,2-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors |
| BRPI0908906A2 (pt) | 2008-03-21 | 2019-09-24 | Novartis Ag | compostos heterocíclicos e usos dos mesmos |
| UA103319C2 (en) | 2008-05-06 | 2013-10-10 | Глаксосмитклайн Ллк | Thiazole- and oxazole-benzene sulfonamide compounds |
| PL2324008T3 (pl) | 2008-07-24 | 2012-09-28 | Nerviano Medical Sciences Srl | 3,4-diarylopirazole jako inhibitory kinazy białkowej |
| AU2009276699A1 (en) | 2008-07-28 | 2010-02-04 | Gilead Sciences, Inc. | Cycloalkylidene and heterocycloalkylidene histone deacetylase inhibitor compounds |
| JP5603869B2 (ja) | 2008-09-29 | 2014-10-08 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 新規化合物 |
| BR122021018683B1 (pt) | 2008-10-07 | 2022-11-16 | Kudos Pharmaceuticals Limited | Formulação farmacêutica de 4-[3-(4-ciclopropanocarbonil- piperazina-1-carbonil)-4-flúor- benzil]-2h-ftalazin-1-ona, uso de um polímero de matriz, forma de dosagem e método para produzir uma dispersão amorfa sólida |
| WO2010056662A1 (en) | 2008-11-11 | 2010-05-20 | University Of Washington | Activated wnt-beta-catenin signaling in melanoma |
| WO2010070060A1 (en) | 2008-12-19 | 2010-06-24 | 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 |
| WO2010145998A1 (en) | 2009-06-15 | 2010-12-23 | 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 |
| US8242260B2 (en) | 2009-08-28 | 2012-08-14 | Novartis Ag | Compounds and compositions as protein kinase inhibitors |
| CN104958294A (zh) | 2010-01-27 | 2015-10-07 | 内尔维安诺医学科学有限公司 | 作为蛋白激酶抑制剂的3,4-二芳基吡唑的亚磺酰氨基衍生物 |
| JP6155187B2 (ja) | 2010-03-30 | 2017-06-28 | ヴァーセオン コーポレイション | トロンビンの阻害剤としての多置換芳香族化合物 |
| JP5938038B2 (ja) | 2010-08-03 | 2016-06-22 | ネルヴィアーノ・メディカル・サイエンシズ・ソチエタ・ア・レスポンサビリタ・リミタータ | ピラゾロフェニル−ベンゼンスルホンアミド化合物の誘導体及びその抗腫瘍薬としての使用 |
| DK2688572T3 (en) | 2011-03-21 | 2017-06-12 | Valcuria Ab | PHARMACEUTICAL COMPOSITION WITH AN HDAC INHIBITOR AND A STEROID AND 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 |
| WO2013078264A1 (en) | 2011-11-23 | 2013-05-30 | Novartis Ag | Pharmaceutical formulations |
| RU2015121367A (ru) | 2012-11-08 | 2017-01-10 | Новартис Аг | Фармацевтическая комбинация, содержащая ингибитор b-raf и ингибитор деацетилазы гистонов, и ее применение при лечении пролиферативных заболеваний |
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| WO2011025927A1 (en) * | 2009-08-28 | 2011-03-03 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
Non-Patent Citations (2)
| Title |
|---|
| CRISTIAN TOMASETTI ，ET AL: "An elementary approach to modeling drug resistance in cancer", 《MATHEMATICAL BIOSCIENCES AND ENGINEERING : MBE》 * |
| PIZZOLATO, N. ET AL: "Stochastic dynamics of leukemic cells under an intermittent targeted therapy", 《THEORY IN BIOSCIENCES》 * |
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| US11007194B2 (en) | 2021-05-18 |
| MX354725B (es) | 2018-03-16 |
| RU2014117707A (ru) | 2015-12-20 |
| AU2012335663B2 (en) | 2015-12-24 |
| BR112014011223A2 (pt) | 2017-05-09 |
| CA2855243A1 (en) | 2013-05-16 |
| EP2776037B1 (en) | 2019-01-09 |
| MX2014005726A (es) | 2014-05-28 |
| CA2855243C (en) | 2020-04-14 |
| HK1198920A1 (en) | 2015-06-19 |
| BR112014011223A8 (pt) | 2023-01-31 |
| RU2622015C2 (ru) | 2017-06-08 |
| CN103917236A (zh) | 2014-07-09 |
| EP2776037A1 (en) | 2014-09-17 |
| JP6150813B2 (ja) | 2017-06-21 |
| AU2012335663A1 (en) | 2014-05-29 |
| US20140275136A1 (en) | 2014-09-18 |
| WO2013070996A1 (en) | 2013-05-16 |
| JP2014533272A (ja) | 2014-12-11 |
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