EA020624B1 - Кристаллическая полиморфная форма n-(-)-(3,4-дифтор-2-(2-фтор-4-йодфениламино)-6-метоксифенил)-l-(2,3-дигидроксипропил)циклопропан-1-сульфонамида и ее применение в качестве ингибитора mek - Google Patents

Кристаллическая полиморфная форма n-(-)-(3,4-дифтор-2-(2-фтор-4-йодфениламино)-6-метоксифенил)-l-(2,3-дигидроксипропил)циклопропан-1-сульфонамида и ее применение в качестве ингибитора mek Download PDF

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Publication number
EA020624B1
EA020624B1 EA201000268A EA201000268A EA020624B1 EA 020624 B1 EA020624 B1 EA 020624B1 EA 201000268 A EA201000268 A EA 201000268A EA 201000268 A EA201000268 A EA 201000268A EA 020624 B1 EA020624 B1 EA 020624B1
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Eurasian Patent Office
Prior art keywords
cancer
compound
day
administered
inhibitors
Prior art date
Application number
EA201000268A
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English (en)
Russian (ru)
Other versions
EA201000268A1 (ru
Inventor
Жан-Мишель Вернье
Колин Эдуард Роулингс
Жан-Люк Жирарде
Стьюарт Даймок
Барри Кварт
Джеффри Н. Майнер
Original Assignee
Арди Байосайенсиз, Инк.
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40304796&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA020624(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from US11/830,733 external-priority patent/US8101799B2/en
Application filed by Арди Байосайенсиз, Инк. filed Critical Арди Байосайенсиз, Инк.
Publication of EA201000268A1 publication Critical patent/EA201000268A1/ru
Publication of EA020624B1 publication Critical patent/EA020624B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/22Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
    • C07C311/28Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N41/00Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a sulfur atom bound to a hetero atom
    • A01N41/02Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a sulfur atom bound to a hetero atom containing a sulfur-to-oxygen double bond
    • A01N41/04Sulfonic acids; Derivatives thereof
    • A01N41/06Sulfonic acid amides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/18Sulfonamides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/02Systems containing only non-condensed rings with a three-membered ring

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Communicable Diseases (AREA)
  • Psychiatry (AREA)
  • Plant Pathology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Agronomy & Crop Science (AREA)
  • Pest Control & Pesticides (AREA)
  • Rheumatology (AREA)
  • Dentistry (AREA)
EA201000268A 2007-07-30 2008-07-28 Кристаллическая полиморфная форма n-(-)-(3,4-дифтор-2-(2-фтор-4-йодфениламино)-6-метоксифенил)-l-(2,3-дигидроксипропил)циклопропан-1-сульфонамида и ее применение в качестве ингибитора mek EA020624B1 (ru)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US11/830,733 US8101799B2 (en) 2005-07-21 2007-07-30 Derivatives of N-(arylamino) sulfonamides as inhibitors of MEK
US3446608P 2008-03-06 2008-03-06
US3446408P 2008-03-06 2008-03-06
US4488608P 2008-04-14 2008-04-14
PCT/US2008/071392 WO2009018233A1 (en) 2007-07-30 2008-07-28 Derivatives of n-(arylamino) sulfonamides including polymorphs as inhibitors of mek as well as compositions, methods of use and methods for preparing the same

Publications (2)

Publication Number Publication Date
EA201000268A1 EA201000268A1 (ru) 2010-08-30
EA020624B1 true EA020624B1 (ru) 2014-12-30

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Family Applications (2)

Application Number Title Priority Date Filing Date
EA201000268A EA020624B1 (ru) 2007-07-30 2008-07-28 Кристаллическая полиморфная форма n-(-)-(3,4-дифтор-2-(2-фтор-4-йодфениламино)-6-метоксифенил)-l-(2,3-дигидроксипропил)циклопропан-1-сульфонамида и ее применение в качестве ингибитора mek
EA201400552A EA032294B1 (ru) 2007-07-30 2008-07-28 Способ получения полиморфной формы производного n-(ариламино)сульфонамида, фармацевтическая композиция, содержащая указанное производное, и способ лечения с помощью указанного производного

Family Applications After (1)

Application Number Title Priority Date Filing Date
EA201400552A EA032294B1 (ru) 2007-07-30 2008-07-28 Способ получения полиморфной формы производного n-(ариламино)сульфонамида, фармацевтическая композиция, содержащая указанное производное, и способ лечения с помощью указанного производного

Country Status (22)

Country Link
EP (1) EP2184984A4 (https=)
JP (3) JP2010535232A (https=)
KR (3) KR20150091434A (https=)
CN (2) CN103479604B (https=)
AP (1) AP2817A (https=)
AU (2) AU2008282338B2 (https=)
BR (1) BRPI0815659A2 (https=)
CA (1) CA2693390C (https=)
CO (1) CO6470808A2 (https=)
CR (1) CR11244A (https=)
DO (1) DOP2010000045A (https=)
EA (2) EA020624B1 (https=)
EC (1) ECSP109910A (https=)
HN (1) HN2010000203A (https=)
IL (1) IL203296A (https=)
MA (1) MA31881B1 (https=)
MX (1) MX2010001244A (https=)
NZ (1) NZ582929A (https=)
PH (1) PH12015501914A1 (https=)
SV (1) SV2010003469A (https=)
TN (1) TN2010000049A1 (https=)
WO (1) WO2009018233A1 (https=)

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US20170027940A1 (en) 2014-04-10 2017-02-02 Stichting Het Nederlands Kanker Instituut Method for treating cancer
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Publication number Publication date
JP2015078199A (ja) 2015-04-23
EP2184984A1 (en) 2010-05-19
CN103479604A (zh) 2014-01-01
EA201400552A1 (ru) 2014-09-30
KR20100092424A (ko) 2010-08-20
EA201000268A1 (ru) 2010-08-30
SV2010003469A (es) 2010-04-30
JP6309880B2 (ja) 2018-04-11
JP2010535232A (ja) 2010-11-18
KR20150091434A (ko) 2015-08-10
CA2693390C (en) 2017-01-17
NZ582929A (en) 2012-03-30
CO6470808A2 (es) 2012-06-29
AU2008282338B2 (en) 2015-02-12
EP2184984A4 (en) 2013-07-24
HN2010000203A (es) 2012-11-19
HK1147396A1 (en) 2011-08-12
PH12015501914A1 (en) 2017-07-31
BRPI0815659A2 (pt) 2014-09-30
CA2693390A1 (en) 2009-02-05
CN103479604B (zh) 2016-08-10
AP2010005134A0 (en) 2010-02-28
EA032294B1 (ru) 2019-05-31
MA31881B1 (fr) 2010-12-01
CN101808516A (zh) 2010-08-18
AU2008282338A1 (en) 2009-02-05
ECSP109910A (es) 2010-04-30
WO2009018233A1 (en) 2009-02-05
CR11244A (es) 2010-05-20
TN2010000049A1 (en) 2011-09-26
JP2017125021A (ja) 2017-07-20
AU2015200390B2 (en) 2017-02-23
KR20140098185A (ko) 2014-08-07
CN101808516B (zh) 2013-08-28
AP2817A (en) 2013-12-31
IL203296A (en) 2017-06-29
DOP2010000045A (es) 2010-10-31
MX2010001244A (es) 2010-08-31

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