JOP20130304B1 - مستحضر وصيغة تشتمل على مثبط mek - Google Patents

مستحضر وصيغة تشتمل على مثبط mek

Info

Publication number
JOP20130304B1
JOP20130304B1 JOP/2013/0304A JOP20130304A JOP20130304B1 JO P20130304 B1 JOP20130304 B1 JO P20130304B1 JO P20130304 A JOP20130304 A JO P20130304A JO P20130304 B1 JOP20130304 B1 JO P20130304B1
Authority
JO
Jordan
Prior art keywords
formulaton
preparation
mek inhibitor
hydroxyethyoxy
fluorophenylamino
Prior art date
Application number
JOP/2013/0304A
Other languages
Arabic (ar)
English (en)
Inventor
Andreas Niederer Daniel
Heinz Pachinger Werner
Wolf Marie-Christine
Zimmermann Daniel
Nichols Paul
Misun Marian
J Stengel Peter
Max Krell Christoph
Liu Weidong
Original Assignee
Array Biopharma Inc
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=50488781&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=JOP20130304(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Array Biopharma Inc, Novartis Ag filed Critical Array Biopharma Inc
Application granted granted Critical
Publication of JOP20130304B1 publication Critical patent/JOP20130304B1/ar

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2009Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/08Radicals containing only hydrogen and carbon atoms
    • CCHEMISTRY; METALLURGY
    • C30CRYSTAL GROWTH
    • C30BSINGLE-CRYSTAL GROWTH; UNIDIRECTIONAL SOLIDIFICATION OF EUTECTIC MATERIAL OR UNIDIRECTIONAL DEMIXING OF EUTECTOID MATERIAL; REFINING BY ZONE-MELTING OF MATERIAL; PRODUCTION OF A HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; SINGLE CRYSTALS OR HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; AFTER-TREATMENT OF SINGLE CRYSTALS OR A HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; APPARATUS THEREFOR
    • C30B29/00Single crystals or homogeneous polycrystalline material with defined structure characterised by the material or by their shape
    • C30B29/54Organic compounds
    • CCHEMISTRY; METALLURGY
    • C30CRYSTAL GROWTH
    • C30BSINGLE-CRYSTAL GROWTH; UNIDIRECTIONAL SOLIDIFICATION OF EUTECTIC MATERIAL OR UNIDIRECTIONAL DEMIXING OF EUTECTOID MATERIAL; REFINING BY ZONE-MELTING OF MATERIAL; PRODUCTION OF A HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; SINGLE CRYSTALS OR HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; AFTER-TREATMENT OF SINGLE CRYSTALS OR A HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; APPARATUS THEREFOR
    • C30B7/00Single-crystal growth from solutions using solvents which are liquid at normal temperature, e.g. aqueous solutions
    • C30B7/08Single-crystal growth from solutions using solvents which are liquid at normal temperature, e.g. aqueous solutions by cooling of the solution
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Biophysics (AREA)
  • Inorganic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Metallurgy (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Materials Engineering (AREA)
  • Biochemistry (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JOP/2013/0304A 2012-10-19 2013-10-20 مستحضر وصيغة تشتمل على مثبط mek JOP20130304B1 (ar)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201261716169P 2012-10-19 2012-10-19

Publications (1)

Publication Number Publication Date
JOP20130304B1 true JOP20130304B1 (ar) 2021-08-17

Family

ID=50488781

Family Applications (1)

Application Number Title Priority Date Filing Date
JOP/2013/0304A JOP20130304B1 (ar) 2012-10-19 2013-10-20 مستحضر وصيغة تشتمل على مثبط mek

Country Status (23)

Country Link
US (7) US9238627B2 (enExample)
EP (3) EP2909182B1 (enExample)
JP (3) JP6385939B2 (enExample)
CN (3) CN104870427B (enExample)
AR (1) AR099630A1 (enExample)
BR (1) BR112015008623B1 (enExample)
CA (2) CA2888474C (enExample)
CY (1) CY1122670T1 (enExample)
DK (2) DK2909182T3 (enExample)
ES (2) ES2971077T3 (enExample)
FI (1) FI3702351T3 (enExample)
HR (1) HRP20240033T1 (enExample)
HU (2) HUE047708T2 (enExample)
JO (1) JOP20130304B1 (enExample)
LT (1) LT3702351T (enExample)
PL (2) PL3702351T3 (enExample)
PT (2) PT2909182T (enExample)
RS (1) RS65117B1 (enExample)
RU (2) RU2018127873A (enExample)
SI (2) SI2909182T1 (enExample)
SM (1) SMT202400044T1 (enExample)
TW (1) TWI650316B (enExample)
WO (1) WO2014063024A1 (enExample)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR099630A1 (es) 2012-10-19 2016-08-10 Novartis Ag Preparación de un inhibidor de mek y formulación que lo comprende
CN105566225A (zh) * 2015-02-16 2016-05-11 苏州晶云药物科技有限公司 一种口服丝裂原活化蛋白激酶抑制剂的晶型及其制备方法
MX387795B (es) * 2016-06-03 2025-03-19 Array Biopharma Inc Combinaciones farmaceuticas.
CN109438362B (zh) 2017-11-14 2020-07-21 深圳市塔吉瑞生物医药有限公司 一种取代的苯并咪唑化合物及包含该化合物的组合物
TW201938165A (zh) 2017-12-18 2019-10-01 美商輝瑞股份有限公司 治療癌症的方法及組合療法
US11395823B2 (en) * 2018-01-09 2022-07-26 Duke University Topical administration of MEK inhibiting agents for the treatment of skin disorders
WO2020212832A1 (en) * 2019-04-16 2020-10-22 Alembic Pharmaceuticals Limited Process of preparation of benzimidazole compounds
WO2021116901A1 (en) * 2019-12-09 2021-06-17 Biocon Limited Forms of binimetinib and process for preparation thereof
EP4225307A1 (en) 2020-10-05 2023-08-16 Pierre Fabre Medicament Combination of encorafenib and binimetinib as adjuvant treatment for resected stage ii melanoma
CN112679438A (zh) * 2020-12-31 2021-04-20 武汉九州钰民医药科技有限公司 制备司美替尼的方法
WO2022251193A1 (en) 2021-05-27 2022-12-01 Mirati Therapeutics, Inc. Combination therapies
WO2023084489A1 (en) 2021-11-15 2023-05-19 Pfizer Inc. Methods of treating coronavirus disease 2019
EP4460303A4 (en) * 2022-01-06 2025-07-23 Msn Laboratories Private Ltd R&D Center IMPROVED PROCESS FOR THE PREPARATION OF 5-[(4-BROMO-2-FLUOROPHENYL)AMINO]-4-FLUORO-N-(2HYDROXYETHOXY)-1-METHYL-1H-BENZIMIDAZOLE-6-CARBOXAMIDE
WO2024003942A1 (en) * 2022-07-01 2024-01-04 Natco Pharma Limited An improved process for the preparation of selumetinib sulfate
TW202508595A (zh) 2023-05-04 2025-03-01 美商銳新醫藥公司 用於ras相關疾病或病症之組合療法
WO2025034702A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 for use in the treatment of ras protein-related disease or disorder
WO2025080946A2 (en) 2023-10-12 2025-04-17 Revolution Medicines, Inc. Ras inhibitors
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
FR3159741A1 (fr) 2024-03-04 2025-09-05 Pierre Fabre Medicament Formulation topique comprenant du binimetinib
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors

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IL144214A0 (en) * 1999-01-13 2002-05-23 Warner Lambert Co Benzoheterocycles and their use as mek inhibitors
CN1358094A (zh) * 1999-07-16 2002-07-10 沃尼尔·朗伯公司 用mek抑制剂治疗慢性疼痛的方法
US7235537B2 (en) * 2002-03-13 2007-06-26 Array Biopharma, Inc. N3 alkylated benzimidazole derivatives as MEK inhibitors
CA2478374C (en) * 2002-03-13 2009-01-06 Eli M. Wallace N3 alkylated benzimidazole derivatives as mek inhibitors
WO2005009975A2 (en) * 2003-07-24 2005-02-03 Warner-Lambert Company Llc Benzimidazole derivatives as mek inhibitors
WO2006030826A1 (ja) 2004-09-17 2006-03-23 Eisai R & D Management Co., Ltd. 医薬組成物
ES2567133T3 (es) 2005-06-23 2016-04-20 Array Biopharma, Inc. Proceso para preparar compuestos de benzoimidazol
BRPI0612306A2 (pt) 2005-06-23 2010-11-03 Array Biopharma Inc processo snar para preparar composto de benzimidazol
TWI405756B (zh) * 2005-12-21 2013-08-21 Array Biopharma Inc 新穎硫酸氫鹽
CN101341132A (zh) * 2005-12-21 2009-01-07 阿斯利康(瑞典)有限公司 作为mek抑制剂用于治疗癌症的6-(4-溴-2-氯-苯基氨基)-7-氟-n-(2-羟基乙氧基)-3-甲基-3h-苯并咪唑-5-甲酰胺的甲苯磺酸盐
KR20150091434A (ko) * 2007-07-30 2015-08-10 아디아 바이오사이언스즈 인크. 다형체를 포함하는, mek의 억제제로서의 n-(아릴아미노) 술폰아미드의 유도체 및 조성물, 사용 방법 및 이의 제조 방법
WO2009064675A1 (en) 2007-11-12 2009-05-22 Takeda Pharmaceutical Company Limited Mapk/erk kinase inhibitors
JP2012524114A (ja) * 2009-04-21 2012-10-11 ノバルティス アーゲー Mek阻害剤としてのヘテロ環式化合物
WO2012145503A1 (en) 2011-04-21 2012-10-26 Novartis Ag Pharmaceutical combinations
EP2750672A1 (en) 2011-09-01 2014-07-09 Novartis AG Use of organic compound for the treatment of noonan syndrome
AR099630A1 (es) 2012-10-19 2016-08-10 Novartis Ag Preparación de un inhibidor de mek y formulación que lo comprende

Also Published As

Publication number Publication date
HUE047708T2 (hu) 2020-05-28
US20180296533A1 (en) 2018-10-18
EP3702351A1 (en) 2020-09-02
HRP20240033T1 (hr) 2024-03-29
EP2909182A4 (en) 2016-07-06
EP2909182B1 (en) 2019-12-04
US20160168103A1 (en) 2016-06-16
CN109456272A (zh) 2019-03-12
US9562016B2 (en) 2017-02-07
PL3702351T3 (pl) 2024-04-02
CN109336824A (zh) 2019-02-15
CN104870427A (zh) 2015-08-26
TWI650316B (zh) 2019-02-11
JP6385939B2 (ja) 2018-09-05
EP3702351B1 (en) 2023-11-22
PT2909182T (pt) 2020-03-02
JP2016503391A (ja) 2016-02-04
RS65117B1 (sr) 2024-02-29
SI3702351T1 (sl) 2024-03-29
RU2669391C2 (ru) 2018-10-11
HUE065433T2 (hu) 2024-05-28
PT3702351T (pt) 2024-01-17
EP4306171A2 (en) 2024-01-17
CN109336824B (zh) 2022-11-11
JP6737838B2 (ja) 2020-08-12
US10398683B2 (en) 2019-09-03
JP2019194272A (ja) 2019-11-07
FI3702351T3 (fi) 2024-01-24
SMT202400044T1 (it) 2024-03-13
PL2909182T3 (pl) 2020-06-01
JP2018135399A (ja) 2018-08-30
AR099630A1 (es) 2016-08-10
CA2888474A1 (en) 2014-04-24
EP4306171A3 (en) 2024-04-03
HK1214254A1 (en) 2016-07-22
US20200171002A1 (en) 2020-06-04
DK2909182T3 (da) 2020-02-17
US20140128442A1 (en) 2014-05-08
CA3079071C (en) 2022-06-07
US9382212B1 (en) 2016-07-05
CY1122670T1 (el) 2021-03-12
ES2971077T3 (es) 2024-06-03
ES2772498T3 (es) 2020-07-07
BR112015008623A2 (pt) 2017-07-04
US9598376B2 (en) 2017-03-21
RU2015118572A (ru) 2016-12-20
RU2018127873A (ru) 2019-03-14
US20160168104A1 (en) 2016-06-16
CA2888474C (en) 2021-03-02
US10729678B2 (en) 2020-08-04
SI2909182T1 (sl) 2020-03-31
LT3702351T (lt) 2024-01-10
CA3079071A1 (en) 2014-04-24
TW201427956A (zh) 2014-07-16
US20170231963A1 (en) 2017-08-17
WO2014063024A1 (en) 2014-04-24
US9238627B2 (en) 2016-01-19
US9980944B2 (en) 2018-05-29
US20160168102A1 (en) 2016-06-16
EP2909182A1 (en) 2015-08-26
DK3702351T3 (da) 2024-01-29
BR112015008623B1 (pt) 2022-10-25
CN104870427B (zh) 2018-10-23

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