EA201401027A1 - НОВЫЕ КРИСТАЛЛИЧЕСКИЕ ПОЛИМОРФНЫЕ ФОРМЫ ГЕМИНАПАДИЗИЛАТА 5-(2-{[6-(2,2-ДИФТОР-2-ФЕНИЛЭТОКСИ)ГЕКСИЛ]АМИНО}-1-(R)-ГИДРОКСИЭТИЛ)-8-ГИДРОКСИХИНОЛИН-2(1H)-ОНА В КАЧЕСТВЕ АГОНИСТОВ βАДРЕНЕРГИЧЕСКОГО РЕЦЕПТОРА - Google Patents

НОВЫЕ КРИСТАЛЛИЧЕСКИЕ ПОЛИМОРФНЫЕ ФОРМЫ ГЕМИНАПАДИЗИЛАТА 5-(2-{[6-(2,2-ДИФТОР-2-ФЕНИЛЭТОКСИ)ГЕКСИЛ]АМИНО}-1-(R)-ГИДРОКСИЭТИЛ)-8-ГИДРОКСИХИНОЛИН-2(1H)-ОНА В КАЧЕСТВЕ АГОНИСТОВ βАДРЕНЕРГИЧЕСКОГО РЕЦЕПТОРА

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Publication number
EA201401027A1
EA201401027A1 EA201401027A EA201401027A EA201401027A1 EA 201401027 A1 EA201401027 A1 EA 201401027A1 EA 201401027 A EA201401027 A EA 201401027A EA 201401027 A EA201401027 A EA 201401027A EA 201401027 A1 EA201401027 A1 EA 201401027A1
Authority
EA
Eurasian Patent Office
Prior art keywords
hydroxyethyl
crystalline polymorphic
amino
polymorphic forms
adrenergic receptor
Prior art date
Application number
EA201401027A
Other languages
English (en)
Other versions
EA030015B1 (ru
Inventor
Местрес-Хемма Амат
Эльвира Балагуер-Ардануй
Франсеск Каррера-Каррера
Иоланда Маркуета-Эреу
Энрике Мойес-Вальс
Original Assignee
Альмираль, С.А.
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=45894403&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA201401027(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Альмираль, С.А. filed Critical Альмираль, С.А.
Publication of EA201401027A1 publication Critical patent/EA201401027A1/ru
Publication of EA030015B1 publication Critical patent/EA030015B1/ru

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/227—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/24—Oxygen atoms attached in position 8
    • C07D215/26—Alcohols; Ethers thereof
    • 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
    • A61K31/435—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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4704—2-Quinolinones, e.g. carbostyril
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pulmonology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Peptides Or Proteins (AREA)

Abstract

В заявке описаны новые кристаллические полиморфные формы геминападизилата 5-(2-{[6-(2,2-дифтор-2-фенилэтокси)гексил]амино}-1-(R)-гидроксиэтил)-8-гидроксихинолин-2(1Н)-она. В заявке также описаны фармацевтические композиции, содержащие указанные кристаллические полиморфные формы, способы их применения для лечения респираторных заболеваний, связанных с активностью β2 адренергического рецептора, и способ получения таких кристаллических полиморфных.
EA201401027A 2012-03-20 2013-03-15 НОВЫЕ КРИСТАЛЛИЧЕСКИЕ ПОЛИМОРФНЫЕ ФОРМЫ ГЕМИНАПАДИЗИЛАТА 5-(2-{[6-(2,2-ДИФТОР-2-ФЕНИЛЭТОКСИ)ГЕКСИЛ]АМИНО}-1-(R)-ГИДРОКСИЭТИЛ)-8-ГИДРОКСИХИНОЛИН-2(1H)-ОНА В КАЧЕСТВЕ АГОНИСТОВ β2 АДРЕНЕРГИЧЕСКОГО РЕЦЕПТОРА EA030015B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP12382101.9A EP2641900A1 (en) 2012-03-20 2012-03-20 Novel polymorphic Crystal forms of 5-(2-{[6-(2,2-difluoro-2-phenylethoxy) hexyl]amino}-1-(R)-hydroxyethyl)-8-hydroxyquinolin-2(1h)-one, heminapadisylate as agonist of the ß2 adrenergic receptor.
US201261622266P 2012-04-10 2012-04-10
PCT/EP2013/055488 WO2013139712A1 (en) 2012-03-20 2013-03-15 NOVEL POLYMORPHIC CRYSTAL FORMS OF 5-(2-{[6-(2,2-DIFLUORO-2-PHENYLETHOXY)HEXYL]AMINO}-1-(R)-HYDROXYETHYL)-8-HYDROXYQUINOLIN-2(1H)-ONE, HEMINAPADISYLATE AS AGONIST OF THE β2 ADRENERGIC RECEPTOR.

Publications (2)

Publication Number Publication Date
EA201401027A1 true EA201401027A1 (ru) 2015-03-31
EA030015B1 EA030015B1 (ru) 2018-06-29

Family

ID=45894403

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201401027A EA030015B1 (ru) 2012-03-20 2013-03-15 НОВЫЕ КРИСТАЛЛИЧЕСКИЕ ПОЛИМОРФНЫЕ ФОРМЫ ГЕМИНАПАДИЗИЛАТА 5-(2-{[6-(2,2-ДИФТОР-2-ФЕНИЛЭТОКСИ)ГЕКСИЛ]АМИНО}-1-(R)-ГИДРОКСИЭТИЛ)-8-ГИДРОКСИХИНОЛИН-2(1H)-ОНА В КАЧЕСТВЕ АГОНИСТОВ β2 АДРЕНЕРГИЧЕСКОГО РЕЦЕПТОРА

Country Status (29)

Country Link
US (1) US9346759B2 (ru)
EP (2) EP2641900A1 (ru)
JP (1) JP6134377B2 (ru)
KR (1) KR101856818B1 (ru)
CN (1) CN104203918B (ru)
AR (1) AR090448A1 (ru)
AU (1) AU2013234514B2 (ru)
CA (1) CA2862934C (ru)
CL (1) CL2014002440A1 (ru)
CO (1) CO7081154A2 (ru)
CR (1) CR20140433A (ru)
EA (1) EA030015B1 (ru)
ES (1) ES2646776T3 (ru)
HK (1) HK1201832A1 (ru)
HR (1) HRP20171982T1 (ru)
HU (1) HUE037364T2 (ru)
IL (1) IL234175B (ru)
MX (1) MX351293B (ru)
MY (1) MY172680A (ru)
NZ (1) NZ628697A (ru)
PE (1) PE20142336A1 (ru)
PH (1) PH12014502097A1 (ru)
PL (1) PL2828242T3 (ru)
RS (1) RS56794B1 (ru)
SG (2) SG10201607630WA (ru)
SI (1) SI2828242T1 (ru)
UY (1) UY34699A (ru)
WO (1) WO2013139712A1 (ru)
ZA (1) ZA201405480B (ru)

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Publication number Priority date Publication date Assignee Title
EP2578570A1 (en) 2011-10-07 2013-04-10 Almirall, S.A. Novel process for preparing 5-(2-{[6-(2,2-difluoro-2-phenylethoxy)hexyl]amino}-1(r)-hydroxyethyl)-8-hydroxyquinolin-2(1h)-one via novel intermediates of synthesis.
EP2641900A1 (en) 2012-03-20 2013-09-25 Almirall, S.A. Novel polymorphic Crystal forms of 5-(2-{[6-(2,2-difluoro-2-phenylethoxy) hexyl]amino}-1-(R)-hydroxyethyl)-8-hydroxyquinolin-2(1h)-one, heminapadisylate as agonist of the ß2 adrenergic receptor.
CA3025377A1 (en) 2016-06-02 2017-12-07 Abbvie Inc. Glucocorticoid receptor agonist and immunoconjugates thereof
EP3694839B1 (en) 2017-10-13 2022-07-27 Treeway TW001 B.V. Edaravone salt
PL3658192T3 (pl) 2017-12-01 2021-10-18 Abbvie Inc. Agonista receptora glukokortykoidowego i jego immunokoniugaty
CN111748010B (zh) * 2019-03-29 2023-12-08 天津药业研究院股份有限公司 一种醋丙甲泼尼龙无水晶型及其组合物

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IL234175B (en) 2018-10-31
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