EA201200146A1 - Бензолсульфонат 2-[[[2-[(гидроксиацетил)амино]-4-пиридинил]метил]тио]-n-[4-(трифторметокси)фенил]-3-пиридинкарбоксамида, его кристаллы, его полиморфы и способы их получения - Google Patents

Бензолсульфонат 2-[[[2-[(гидроксиацетил)амино]-4-пиридинил]метил]тио]-n-[4-(трифторметокси)фенил]-3-пиридинкарбоксамида, его кристаллы, его полиморфы и способы их получения

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Publication number
EA201200146A1
EA201200146A1 EA201200146A EA201200146A EA201200146A1 EA 201200146 A1 EA201200146 A1 EA 201200146A1 EA 201200146 A EA201200146 A EA 201200146A EA 201200146 A EA201200146 A EA 201200146A EA 201200146 A1 EA201200146 A1 EA 201200146A1
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EA
Eurasian Patent Office
Prior art keywords
crystals
compound
pyridinecarboxamide
salt
difficult
Prior art date
Application number
EA201200146A
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English (en)
Other versions
EA019689B1 (ru
Inventor
Масаси Нива
Хироси Дегути
Original Assignee
Сантен Фармасьютикал Ко., Лтд.
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Application filed by Сантен Фармасьютикал Ко., Лтд. filed Critical Сантен Фармасьютикал Ко., Лтд.
Publication of EA201200146A1 publication Critical patent/EA201200146A1/ru
Publication of EA019689B1 publication Critical patent/EA019689B1/ru

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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
    • A61K31/435—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
    • A61K31/455—Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P7/10—Antioedematous agents; Diuretics
    • 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
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/32—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of salts of sulfonic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

При получении 2-[[[2-[(гидроксиацетил)амино]-4-пиридинил]метил]тио]-N-[4-(трифторметокси)фенил]-3-пиридинкарбоксамида (соединение А) возникает множество проблем: 1) соединение А или его соль трудно перекристаллизовывается, стабильность при хранении в значительной мере варьирует в зависимости от вида соли и очень трудно получить соль соединения А с хорошей стабильностью при хранении; 2) в процессе кристаллизации соединения А очень трудно контролировать кристаллический полиморф; и 3) соединение А (свободная форма) вызывает отложение минералов в желудке при его многократном пероральном введении. Для решения этих проблем авторы в процессе разработки сконцентрировали свое внимание на виде соли и обнаружили в результате, что 1) бензолсульфонат соединения А не разлагается под действием света, влаги и других внешних факторов, оцениваемых в рамках 1-недельного предварительного теста на стабильность (жесткий тест), и не создает проблем со стабильностью при хранении, 2) был разработан способ селективного получения двух видов кристаллических форм бензолсульфоната соединения А; и в этом случае 3) не наблюдается отложение минеральных соединений в желудке даже после 4-недельного многократного перорального введения.
EA201200146A 2009-07-17 2010-07-16 Бензолсульфонат 2-[[[2-[(гидроксиацетил)амино]-4-пиридинил]метил]тио]-n-[4-(трифторметокси)фенил]-3-пиридинкарбоксамида, его кристаллы, его полиморфы и способы их получения EA019689B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2009169130 2009-07-17
PCT/JP2010/062071 WO2011007870A1 (ja) 2009-07-17 2010-07-16 ２－［［［２－［（ヒドロキシアセチル）アミノ］－４－ピリジニル］メチル］チオ］－ｎ－［４－（トリフルオロメトキシ）フェニル］－３－ピリジンカルボキサミドのベンゼンスルホン酸塩、その結晶、その結晶多形およびそれらの製造方法

Publications (2)

Publication Number Publication Date
EA201200146A1 true EA201200146A1 (ru) 2012-06-29
EA019689B1 EA019689B1 (ru) 2014-05-30

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Family Applications (1)

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EA201200146A EA019689B1 (ru) 2009-07-17 2010-07-16 Бензолсульфонат 2-[[[2-[(гидроксиацетил)амино]-4-пиридинил]метил]тио]-n-[4-(трифторметокси)фенил]-3-пиридинкарбоксамида, его кристаллы, его полиморфы и способы их получения

Country Status (17)

Country Link
US (4) US9029398B2 (ru)
EP (1) EP2455368B1 (ru)
JP (1) JP5662719B2 (ru)
KR (1) KR101710740B1 (ru)
CN (1) CN102471273B (ru)
AU (1) AU2010271746B2 (ru)
BR (1) BR112012001159A2 (ru)
CA (1) CA2767992C (ru)
EA (1) EA019689B1 (ru)
ES (1) ES2554360T3 (ru)
HK (2) HK1167644A1 (ru)
IN (1) IN2012DN01152A (ru)
MX (1) MX2012000749A (ru)
MY (1) MY157122A (ru)
NZ (1) NZ597495A (ru)
SG (1) SG177576A1 (ru)
WO (1) WO2011007870A1 (ru)

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SG10201606271RA (en) 2012-01-31 2016-09-29 Santen Pharmaceutical Co Ltd Non-aqueous liquid composition
MY163236A (en) * 2013-09-20 2017-08-30 Santen Pharmaceutical Co Ltd Polyethylene glycol-containing composition
TW201609145A (zh) 2013-12-25 2016-03-16 參天製藥股份有限公司 注射劑及形成緩釋（ｄｅｐｏｔ）之方法
CA2979802C (en) * 2015-03-17 2023-06-27 Santen Pharmaceutical Co., Ltd. Pharmaceutical composition comprising polypeptide
CA2979971A1 (en) * 2015-03-18 2016-09-22 Santen Pharmaceutical Co., Ltd. Sustained-release pharmaceutical composition
WO2016148227A1 (ja) * 2015-03-18 2016-09-22 参天製薬株式会社 医薬組成物の安定保存
WO2016178900A1 (en) * 2015-05-01 2016-11-10 Odin Biotech Ocular implant for delivery of pyridinecarboxamide derivative

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4626353B2 (ja) * 2004-02-17 2011-02-09 参天製薬株式会社 置換又は無置換アミノ基を導入した４−ピリジルアルキルチオ基を有する新規環式化合物
PL1717229T3 (pl) * 2004-02-17 2011-11-30 Santen Pharmaceutical Co Ltd Nowy cykliczny związek mający grupę 4-pirydyloalkilotiolową z wprowadzoną do niej (nie)podstawioną grupą aminową
ES2368153T3 (es) 2004-02-17 2011-11-14 Santen Pharmaceutical Co., Ltd. Nuevo compuesto cíclico que presenta un grupo 4-piridilalquiltio que presenta amino (no) sustituido introducido en el mismo.
JP4834441B2 (ja) 2005-03-31 2011-12-14 参天製薬株式会社 ピリミジニルアルキルチオ基を有する新規環式化合物
ES2548729T3 (es) 2005-03-31 2015-10-20 Santen Pharmaceutical Co., Ltd. Nuevo compuesto cíclico que tiene grupo pirimidinilalquiltio

Also Published As

Publication number Publication date
US9359328B2 (en) 2016-06-07
JP2011037844A (ja) 2011-02-24
US9546140B2 (en) 2017-01-17
SG177576A1 (en) 2012-02-28
EP2455368B1 (en) 2015-09-16
US20150291560A1 (en) 2015-10-15
AU2010271746B2 (en) 2014-07-03
HK1167647A1 (en) 2012-12-07
CA2767992A1 (en) 2011-01-20
MX2012000749A (es) 2012-01-27
US20170081286A1 (en) 2017-03-23
JP5662719B2 (ja) 2015-02-04
AU2010271746A1 (en) 2012-02-02
US9902698B2 (en) 2018-02-27
ES2554360T3 (es) 2015-12-18
EA019689B1 (ru) 2014-05-30
HK1167644A1 (en) 2012-12-07
WO2011007870A1 (ja) 2011-01-20
MY157122A (en) 2016-05-13
US20160251314A1 (en) 2016-09-01
CN102471273B (zh) 2014-07-16
KR20130025857A (ko) 2013-03-12
EP2455368A1 (en) 2012-05-23
IN2012DN01152A (en) 2015-04-10
US9029398B2 (en) 2015-05-12
NZ597495A (en) 2013-08-30
US20120116088A1 (en) 2012-05-10
CA2767992C (en) 2017-03-21
CN102471273A (zh) 2012-05-23
BR112012001159A2 (pt) 2016-03-01
KR101710740B1 (ko) 2017-02-27
EP2455368A4 (en) 2013-01-09

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