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EA201100245A1 - Новый холиновый сокристалл эпалрестата - Google Patents

Новый холиновый сокристалл эпалрестата

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Publication number
EA201100245A1
EA201100245A1 EA201100245A EA201100245A EA201100245A1 EA 201100245 A1 EA201100245 A1 EA 201100245A1 EA 201100245 A EA201100245 A EA 201100245A EA 201100245 A EA201100245 A EA 201100245A EA 201100245 A1 EA201100245 A1 EA 201100245A1
Authority
EA
Eurasian Patent Office
Prior art keywords
new
epalrestat
treatment
sokristall
holin
Prior art date
Application number
EA201100245A
Other languages
English (en)
Other versions
EA016904B1 (ru
Inventor
Изабель Калофонос
Г. Патрик Стэнли
Вильям Мартин-Дойл
Димитрис Калофонос
Джефри С. Сталтс
Травис Л. Хьюстон
Original Assignee
Бионевия Фармасьютикалс, Инк.
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
Application filed by Бионевия Фармасьютикалс, Инк. filed Critical Бионевия Фармасьютикалс, Инк.
Publication of EA201100245A1 publication Critical patent/EA201100245A1/ru
Publication of EA016904B1 publication Critical patent/EA016904B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D277/36—Sulfur atoms
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • 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
    • A61K31/14—Quaternary ammonium compounds, e.g. edrophonium, choline
    • 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
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/12—Ophthalmic agents for cataracts
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C215/40—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton with quaternised nitrogen atoms bound to carbon atoms of the carbon skeleton
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Vascular Medicine (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Изобретение относится к области фармакологии, в частности к новому холиновому сокристаллу эпалрестата 5-[(1Z,2Е)-2-метил-3-фенилпропенилиден]-4-оксо-2-тиоксо-3-тиазолидинуксусной кислоты. Получают новый сокристалл холина в соответствии с различными вариантами изобретения. Изобретение относится также к фармацевтическим соединениям, содержащим новый сокристалл холина, и связано с терапевтическим применением нового сокристалла холина для лечения и/или профилактики различных заболеваний, включая лечение и/или профилактику осложнений диабета, лечение и/или профилактику гомоцистинурии, связанной с уменьшением уровней гомоцистеина в сыворотке крови, ингибирование альдозо-редуктазы, а также создание кардиопротекторного эффекта у пациентов без диабета.
EA201100245A 2008-09-06 2009-09-03 Новый холиновый сокристалл эпалрестата EA016904B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US9490408P 2008-09-06 2008-09-06
PCT/US2009/055868 WO2010028132A2 (en) 2008-09-06 2009-09-03 Novel choline cocrystal of epalrestat

Publications (2)

Publication Number Publication Date
EA201100245A1 true EA201100245A1 (ru) 2011-08-30
EA016904B1 EA016904B1 (ru) 2012-08-30

Family

ID=41797847

Family Applications (2)

Application Number Title Priority Date Filing Date
EA201200489A EA023435B1 (ru) 2008-09-06 2009-09-03 Фармацевтическая композиция, включающая новый холиновый сокристалл эпалрестата
EA201100245A EA016904B1 (ru) 2008-09-06 2009-09-03 Новый холиновый сокристалл эпалрестата

Family Applications Before (1)

Application Number Title Priority Date Filing Date
EA201200489A EA023435B1 (ru) 2008-09-06 2009-09-03 Фармацевтическая композиция, включающая новый холиновый сокристалл эпалрестата

Country Status (17)

Country Link
US (3) US8906948B2 (ru)
EP (1) EP2326632B8 (ru)
CN (1) CN102216281B (ru)
AU (1) AU2009288037B2 (ru)
CA (1) CA2738231C (ru)
CY (1) CY1119752T1 (ru)
DK (1) DK2326632T3 (ru)
EA (2) EA023435B1 (ru)
ES (1) ES2639019T3 (ru)
GB (1) GB2476202B (ru)
HU (1) HUE034456T2 (ru)
LT (1) LT2326632T (ru)
PL (1) PL2326632T3 (ru)
PT (1) PT2326632T (ru)
SI (1) SI2326632T1 (ru)
UA (1) UA106209C2 (ru)
WO (1) WO2010028132A2 (ru)

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PT2326632T (pt) 2008-09-06 2017-09-05 Bionevia Pharmaceuticals Inc Novo cocristal de colina de epalrestat
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HRP20151321T1 (hr) * 2011-01-20 2016-01-29 Bionevia Pharmaceuticals Inc. Epalrestat ili njegov derivat u oblicima s prilagođenim otpuštanjem te postupci uporabe istih
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Also Published As

Publication number Publication date
CY1119752T1 (el) 2018-06-27
WO2010028132A2 (en) 2010-03-11
CN102216281A (zh) 2011-10-12
US20170174643A1 (en) 2017-06-22
EP2326632B8 (en) 2017-08-09
GB2476202B (en) 2012-04-11
PT2326632T (pt) 2017-09-05
UA106209C2 (en) 2014-08-11
EP2326632A2 (en) 2011-06-01
EA201200489A1 (ru) 2013-01-30
ES2639019T3 (es) 2017-10-25
AU2009288037A1 (en) 2010-03-11
LT2326632T (lt) 2017-09-25
GB201105528D0 (en) 2011-05-18
CA2738231C (en) 2015-04-07
PL2326632T3 (pl) 2017-10-31
US20110275682A1 (en) 2011-11-10
CA2738231A1 (en) 2010-03-11
EA023435B1 (ru) 2016-06-30
DK2326632T3 (en) 2017-09-18
US9611234B2 (en) 2017-04-04
WO2010028132A3 (en) 2010-06-17
US8906948B2 (en) 2014-12-09
HUE034456T2 (en) 2018-02-28
CN102216281B (zh) 2014-11-05
US20150057319A1 (en) 2015-02-26
EP2326632B1 (en) 2017-05-31
EA016904B1 (ru) 2012-08-30
SI2326632T1 (sl) 2017-11-30
GB2476202A (en) 2011-06-15
EP2326632A4 (en) 2012-05-30
AU2009288037B2 (en) 2014-08-14
US10464912B2 (en) 2019-11-05

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