CN104507474B - CDK4/6抑制剂和B‑Raf抑制剂的药物组合 - Google Patents
CDK4/6抑制剂和B‑Raf抑制剂的药物组合 Download PDFInfo
- Publication number
- CN104507474B CN104507474B CN201380039725.5A CN201380039725A CN104507474B CN 104507474 B CN104507474 B CN 104507474B CN 201380039725 A CN201380039725 A CN 201380039725A CN 104507474 B CN104507474 B CN 104507474B
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- Prior art keywords
- combination
- compound
- raf
- inhibitor
- cancer
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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
- A61K31/495—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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/136—Amines having aromatic rings, e.g. ketamine, nortriptyline having the amino group directly attached to the aromatic ring, e.g. benzeneamine
-
- 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
- A61K31/41—Heterocyclic 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
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- A—HUMAN NECESSITIES
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- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
-
- 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
- A61K31/41—Heterocyclic 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
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- 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
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- 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
- A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
-
- A—HUMAN NECESSITIES
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- 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
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- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A—HUMAN NECESSITIES
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- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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- A—HUMAN NECESSITIES
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- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Gastroenterology & Hepatology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pulmonology (AREA)
- Urology & Nephrology (AREA)
- Dermatology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261676134P | 2012-07-26 | 2012-07-26 | |
| US61/676,134 | 2012-07-26 | ||
| US201361830911P | 2013-06-04 | 2013-06-04 | |
| US61/830,911 | 2013-06-04 | ||
| PCT/US2013/051990 WO2014018725A1 (en) | 2012-07-26 | 2013-07-25 | Pharmaceutical combinations of a cdk4/6 inhibitor and a b-raf inhibitor |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN104507474A CN104507474A (zh) | 2015-04-08 |
| CN104507474B true CN104507474B (zh) | 2018-01-02 |
Family
ID=48917729
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201380039725.5A Active CN104507474B (zh) | 2012-07-26 | 2013-07-25 | CDK4/6抑制剂和B‑Raf抑制剂的药物组合 |
Country Status (15)
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2934515B1 (en) * | 2012-12-20 | 2018-04-04 | Novartis AG | A pharmaceutical combination comprising binimetinib |
| JP2016516005A (ja) * | 2013-02-25 | 2016-06-02 | ノバルティス アーゲー | 新規のアンドロゲンレセプター変異 |
| CA2907704C (en) | 2013-03-21 | 2023-01-10 | Giordano Caponigro | Combination therapy for reversing b-raf inhibitor resistance comprising a second inhibitor based on genetic alterations |
| US20180263979A1 (en) * | 2014-12-23 | 2018-09-20 | Millennium Pharmaceuticals, Inc. | Combination of raf inhibitors and aurora kinase inhibitors |
| US10323035B2 (en) * | 2015-04-01 | 2019-06-18 | Crystal Pharmatech Co., Ltd. | Co-crystal of a CDK inhibitor and an MEK inhibitor and process of preparation thereof |
| CN105753869B (zh) * | 2015-04-01 | 2018-09-25 | 苏州晶云药物科技有限公司 | 一种cdk抑制剂和mek抑制剂的共晶及其制备方法 |
| US20190365741A1 (en) * | 2015-08-28 | 2019-12-05 | Novartis Ag | Combinations of the cdk4/6 inhibitor lee011 and the mek1/2 inhibitor trametinib, optionally further comprising the pi3k inhibitor byl719 to treat cancer |
| CN105732642B (zh) * | 2015-11-18 | 2018-09-25 | 苏州晶云药物科技有限公司 | 一种cdk抑制剂和mek抑制剂的共晶及其制备方法 |
| CR20190002A (es) * | 2016-06-03 | 2019-06-10 | Zhu Alexander Cao | Combinaciones farmacéuticas |
| AU2017315357B2 (en) * | 2016-08-23 | 2022-12-01 | Eisai R&D Management Co., Ltd. | Combination therapies for the treatment of hepatocellular carcinoma |
| JP7114575B2 (ja) | 2016-09-19 | 2022-08-08 | ノバルティス アーゲー | Raf阻害剤及びerk阻害剤を含む治療用組合せ |
| WO2018081211A1 (en) * | 2016-10-26 | 2018-05-03 | Li George Y | Deuterated 7-cyclopentyl-n, n-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7h-pyrrolo[2,3-d]pyrimdine-6-carboxamide |
| US11395821B2 (en) | 2017-01-30 | 2022-07-26 | G1 Therapeutics, Inc. | Treatment of EGFR-driven cancer with fewer side effects |
| IL311471A (en) * | 2017-05-02 | 2024-05-01 | Novartis Ag | Combination therapy |
| WO2018218633A1 (en) | 2017-06-02 | 2018-12-06 | Beijing Percans Oncology Co. Ltd. | Combination therapies for treating cancers |
| BR112020013915A2 (pt) | 2018-01-08 | 2020-12-01 | G1 Therapeutics, Inc. | regime de dosagem para liberação, e, método para tratar um câncer dependente de replicação de cdk4/6 em um humano |
| EP3752491A4 (en) | 2018-02-15 | 2021-12-01 | Nuvation Bio Inc. | HETEROCYCLIC COMPOUNDS USED AS KINASE INHIBITORS |
| WO2019195959A1 (en) * | 2018-04-08 | 2019-10-17 | Cothera Biosciences, Inc. | Combination therapy for cancers with braf mutation |
| WO2020010280A1 (en) * | 2018-07-06 | 2020-01-09 | Memorial Sloan Kettering Cancer Center | Combination therapy with mek inhibitor and cdk4/6 inhibitor to treat pancreatic cancer |
| BR112021011699A2 (pt) * | 2018-12-20 | 2021-09-08 | Novartis Ag | Terapia de combinação com um inibidor de raf e um inibidor de cdk4/6 para uso no tratamento contra câncer |
| EP4563150A3 (en) | 2019-05-13 | 2025-07-23 | Novartis AG | New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl) isonicotinamide as raf inhibitors for the treatment of cancer |
| TW202114667A (zh) * | 2019-09-11 | 2021-04-16 | 大陸商江蘇恒瑞醫藥股份有限公司 | Mek抑制劑與cdk4/6抑制劑聯合在製備治療腫瘤的藥物中的用途 |
| HRP20250418T1 (hr) | 2019-12-10 | 2025-06-06 | F. Hoffmann - La Roche Ag | Novi derivati metil-kinazolinona |
| JP2023525100A (ja) * | 2020-05-12 | 2023-06-14 | ノバルティス アーゲー | Craf阻害剤を含む治療的組み合わせ |
| WO2023230554A1 (en) | 2022-05-25 | 2023-11-30 | Pfizer Inc. | Combination of a braf inhibitor, an egfr inhibitor, and a pd-1 antagonist for the treatment of braf v600e-mutant, msi-h/dmmr colorectal cancer |
| WO2025003956A1 (en) | 2023-06-30 | 2025-01-02 | Pfizer Inc. | High drug loading formulations of encorafenib |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1874768A (zh) * | 2003-08-29 | 2006-12-06 | 阵列生物制药公司 | 作为mek抑制剂的n3烷基化苯并咪唑衍生物 |
| WO2011025927A1 (en) * | 2009-08-28 | 2011-03-03 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| CN102186856A (zh) * | 2008-08-22 | 2011-09-14 | 诺瓦提斯公司 | 作为cdk抑制剂的吡咯并嘧啶化合物 |
Family Cites Families (4)
| 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 |
| EP1740184A1 (en) * | 2004-03-30 | 2007-01-10 | Pfizer Products Incorporated | Combinations of signal transduction inhibitors |
| KR20110028651A (ko) | 2008-07-11 | 2011-03-21 | 노파르티스 아게 | (a) 포스포이노시타이드 3-키나제 억제제 및 (b) ras/raf/mek 경로의 조절제의 조합물 |
| ES2689177T3 (es) * | 2010-04-13 | 2018-11-08 | Novartis Ag | Combinación que comprende un inhibidor de cinasa 4 dependiente de ciclina o cinasa dependiente de ciclina (CDK4/6) y un inhibidor de mTOR para tratar cáncer |
-
2013
- 2013-07-24 AR ARP130102621A patent/AR091876A1/es not_active Application Discontinuation
- 2013-07-25 EP EP13745540.8A patent/EP2877174B1/en active Active
- 2013-07-25 TW TW102126726A patent/TWI599357B/zh active
- 2013-07-25 RU RU2015106524A patent/RU2685250C2/ru active
- 2013-07-25 WO PCT/US2013/051990 patent/WO2014018725A1/en not_active Ceased
- 2013-07-25 IN IN376DEN2015 patent/IN2015DN00376A/en unknown
- 2013-07-25 CN CN201380039725.5A patent/CN104507474B/zh active Active
- 2013-07-25 JO JOP/2013/0223A patent/JO3776B1/ar active
- 2013-07-25 CA CA2874860A patent/CA2874860C/en active Active
- 2013-07-25 US US14/414,998 patent/US9700557B2/en active Active
- 2013-07-25 KR KR1020157001594A patent/KR102113363B1/ko active Active
- 2013-07-25 AU AU2013295771A patent/AU2013295771B2/en active Active
- 2013-07-25 JP JP2015524444A patent/JP6320379B2/ja active Active
- 2013-07-25 ES ES13745540T patent/ES2778059T3/es active Active
- 2013-07-25 MX MX2015001122A patent/MX360045B/es active IP Right Grant
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1874768A (zh) * | 2003-08-29 | 2006-12-06 | 阵列生物制药公司 | 作为mek抑制剂的n3烷基化苯并咪唑衍生物 |
| CN102186856A (zh) * | 2008-08-22 | 2011-09-14 | 诺瓦提斯公司 | 作为cdk抑制剂的吡咯并嘧啶化合物 |
| WO2011025927A1 (en) * | 2009-08-28 | 2011-03-03 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
Also Published As
| Publication number | Publication date |
|---|---|
| US20150164897A1 (en) | 2015-06-18 |
| BR112014033118A2 (pt) | 2017-06-27 |
| TWI599357B (zh) | 2017-09-21 |
| JO3776B1 (ar) | 2021-01-31 |
| RU2015106524A (ru) | 2016-09-20 |
| US9700557B2 (en) | 2017-07-11 |
| RU2685250C2 (ru) | 2019-04-17 |
| ES2778059T3 (es) | 2020-08-07 |
| CN104507474A (zh) | 2015-04-08 |
| MX2015001122A (es) | 2015-04-08 |
| WO2014018725A1 (en) | 2014-01-30 |
| CA2874860C (en) | 2020-06-23 |
| TW201412316A (zh) | 2014-04-01 |
| AU2013295771B2 (en) | 2016-08-11 |
| BR112014033118A8 (pt) | 2023-01-31 |
| KR102113363B1 (ko) | 2020-05-21 |
| EP2877174B1 (en) | 2020-01-01 |
| MX360045B (es) | 2018-10-19 |
| IN2015DN00376A (cg-RX-API-DMAC10.html) | 2015-06-12 |
| AU2013295771A1 (en) | 2014-12-11 |
| JP2015523397A (ja) | 2015-08-13 |
| AR091876A1 (es) | 2015-03-04 |
| HK1210721A1 (en) | 2016-05-06 |
| JP6320379B2 (ja) | 2018-05-09 |
| EP2877174A1 (en) | 2015-06-03 |
| KR20150036146A (ko) | 2015-04-07 |
| CA2874860A1 (en) | 2014-01-30 |
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