EA201270639A1 - Способ получения метил{4,6-диамино-2-[1-(2-фторбензил)-1н-пиразоло[3,4-в]пиридин-3-ил]пиримидин-5-ил}карбамата и его очистка для его применения в качестве фармацевтического биологически активного вещества - Google Patents

Способ получения метил{4,6-диамино-2-[1-(2-фторбензил)-1н-пиразоло[3,4-в]пиридин-3-ил]пиримидин-5-ил}карбамата и его очистка для его применения в качестве фармацевтического биологически активного вещества

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EA201270639A1
EA201270639A1 EA201270639A EA201270639A EA201270639A1 EA 201270639 A1 EA201270639 A1 EA 201270639A1 EA 201270639 A EA201270639 A EA 201270639A EA 201270639 A EA201270639 A EA 201270639A EA 201270639 A1 EA201270639 A1 EA 201270639A1
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Eurasian Patent Office
Prior art keywords
pyrazolo
diamino
active substance
purification
carbamata
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EA201270639A
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English (en)
Inventor
Франц-Ёзеф Майс
Йоахим Резе
Винфрид Йонтген
Конрад Зигель
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Байер Интеллектуэль Проперти Гмбх
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Publication of EA201270639A1 publication Critical patent/EA201270639A1/ru

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
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    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

Настоящее изобретение касается способа получения метил{4,6-диамино-2-[1-(2-фторбензил)-1Н-пиразоло[3,4-b]пиридин-3-ил]пиримидин-5-ил}карбамата, т.е. соединения формулы (I)а также способа очистки исходного продукта формулы (I) для применения в качестве фармацевтически активного вещества, причем для очистки метил{4,6-диамино-2-[1-(2-фторбензил)-1H-пиразоло[3,4-b]пиридин-3-ил]пиримидин-5-ил}карбамат-сульфинилдиметан (1:2) формулы (II) выделяют как промежуточную ступень или получают как промежуточную ступень в данном способе очистки, при необходимости в смеси.
EA201270639A 2009-11-27 2010-11-22 Способ получения метил{4,6-диамино-2-[1-(2-фторбензил)-1н-пиразоло[3,4-в]пиридин-3-ил]пиримидин-5-ил}карбамата и его очистка для его применения в качестве фармацевтического биологически активного вещества EA201270639A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP09177369 2009-11-27
PCT/EP2010/067884 WO2011064156A2 (de) 2009-11-27 2010-11-22 Verfahren zur herstellung von methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamat und dessen aufreinigung für die verwendung als pharmazeutischer wirkstoff

Publications (1)

Publication Number Publication Date
EA201270639A1 true EA201270639A1 (ru) 2013-01-30

Family

ID=43568194

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201270639A EA201270639A1 (ru) 2009-11-27 2010-11-22 Способ получения метил{4,6-диамино-2-[1-(2-фторбензил)-1н-пиразоло[3,4-в]пиридин-3-ил]пиримидин-5-ил}карбамата и его очистка для его применения в качестве фармацевтического биологически активного вещества

Country Status (22)

Country Link
US (1) US8501945B2 (ru)
EP (1) EP2504335B1 (ru)
JP (1) JP2013512211A (ru)
KR (1) KR20120098815A (ru)
CN (1) CN102712637A (ru)
AR (1) AR079135A1 (ru)
AU (1) AU2010323297A1 (ru)
BR (1) BR112012012618A2 (ru)
CA (1) CA2781922A1 (ru)
CO (1) CO6551707A2 (ru)
CU (1) CU20120083A7 (ru)
DO (1) DOP2012000143A (ru)
EA (1) EA201270639A1 (ru)
EC (1) ECSP12011920A (ru)
ES (1) ES2433236T3 (ru)
IL (1) IL219861A0 (ru)
MA (1) MA33764B1 (ru)
MX (1) MX2012005942A (ru)
TN (1) TN2012000259A1 (ru)
TW (1) TW201200513A (ru)
UY (1) UY33041A (ru)
WO (1) WO2011064156A2 (ru)

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MY180184A (en) 2009-11-27 2020-11-24 Adverio Pharma Gmbh Method for producing methyl-{4,6-diamino-2-[1-(2-fluorobenyl)-1h-pyrazolo[3,4-b]pyridino-3-yl]pyrimidino-5-yl}methyl carbamate and its purification for use thereof as pharmaceutical substance
DE102010021637A1 (de) 2010-05-26 2011-12-01 Bayer Schering Pharma Aktiengesellschaft Substituierte 5-Fluor-1H-Pyrazolopyridine und ihre Verwendung
DE102010043379A1 (de) 2010-11-04 2012-05-10 Bayer Schering Pharma Aktiengesellschaft Substituierte 6-Fluor-1H-Pyrazolo[4,3-b]pyridine und ihre Verwendung
DE102010043380A1 (de) 2010-11-04 2012-05-10 Bayer Schering Pharma Aktiengesellschaft Benzyl-substituierte Carbamate und ihre Verwendung
DK2896617T3 (en) 2011-11-25 2016-12-12 Adverio Pharma Gmbh Method for preparing substituted (Z) -alpha-fluoro-beta-amino-ACRYLALDEHYDER
JP6386478B2 (ja) 2013-02-21 2018-09-05 アドヴェリオ・ファーマ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング メチル｛４，６−ジアミノ−２−［１−（２−フルオロベンジル）−１ｈ−ピラゾロ［３，４−ｂ］ピリジノ−３−イル］ピリミジノ−５−イル｝メチルカルバメートの形態
MX2018007152A (es) 2015-12-14 2018-08-15 Ironwood Pharmaceuticals Inc Uso de estimuladores de guanilato ciclasa soluble (sgc) para el tratamiento de la disfuncion del esfinter gastrointestinal.
CN108069960A (zh) * 2016-11-15 2018-05-25 江苏豪森药业集团有限公司 利奥西呱中间体的制备方法
US20190381039A1 (en) 2016-12-13 2019-12-19 Cyclerion Therapeutics, Inc. USE OF sGC STIMULATORS FOR THE TREATMENT OF ESOPHAGEAL MOTILITY DISORDERS
WO2020014504A1 (en) 2018-07-11 2020-01-16 Cyclerion Therapeutics, Inc. USE OF sGC STIMULATORS FOR THE TREATMENT OF MITOCHONRIAL DISORDERS
EP3925953A1 (en) * 2020-06-16 2021-12-22 Adverio Pharma GmbH Process for preparing methyl {4,6-diamino-2-[5-fluoro-1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate

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US8501945B2 (en) 2013-08-06
CO6551707A2 (es) 2012-10-31
AU2010323297A1 (en) 2012-06-14
US20110130411A1 (en) 2011-06-02
IL219861A0 (en) 2012-07-31
MX2012005942A (es) 2012-10-03
AR079135A1 (es) 2011-12-28
EP2504335A2 (de) 2012-10-03
WO2011064156A3 (de) 2011-10-20
TN2012000259A1 (en) 2013-12-12
CU20120083A7 (es) 2012-10-15
WO2011064156A2 (de) 2011-06-03
ECSP12011920A (es) 2012-07-31
ES2433236T3 (es) 2013-12-10
UY33041A (es) 2011-06-30
KR20120098815A (ko) 2012-09-05
BR112012012618A2 (pt) 2015-09-08
DOP2012000143A (es) 2013-01-31
CA2781922A1 (en) 2011-06-03
JP2013512211A (ja) 2013-04-11
EP2504335B1 (de) 2013-09-04
MA33764B1 (fr) 2012-11-01
TW201200513A (en) 2012-01-01
CN102712637A (zh) 2012-10-03

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