BR112012012618A2 - processo para preparação de metil {4, 6-diamino-2-[1-(2-fluorobenzil) - 1h-pirazolo [3, 4-b] piridin-3-il] pirimidin-5-il} carbamato e sua purificação para uso com substância ativa farmacêutica - Google Patents

processo para preparação de metil {4, 6-diamino-2-[1-(2-fluorobenzil) - 1h-pirazolo [3, 4-b] piridin-3-il] pirimidin-5-il} carbamato e sua purificação para uso com substância ativa farmacêutica

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Publication number
BR112012012618A2
BR112012012618A2 BR112012012618A BR112012012618A BR112012012618A2 BR 112012012618 A2 BR112012012618 A2 BR 112012012618A2 BR 112012012618 A BR112012012618 A BR 112012012618A BR 112012012618 A BR112012012618 A BR 112012012618A BR 112012012618 A2 BR112012012618 A2 BR 112012012618A2
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BR
Brazil
Prior art keywords
fluorobenzyl
pyrazolo
pyrimidin
diamino
pyridin
Prior art date
Application number
BR112012012618A
Other languages
English (en)
Inventor
Franz-Josef Mais
Joachim Rehse
Konrad Siegel
Winfried Joentgen
Original Assignee
Bayer Ip Gmbh
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 Bayer Ip Gmbh filed Critical Bayer Ip Gmbh
Publication of BR112012012618A2 publication Critical patent/BR112012012618A2/pt

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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
    • 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
    • A61K31/4353—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
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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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)
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Abstract

processo para preparação de metil{4,6-diamino-2-[1-(2-fluorobenzil)-1h-pirazolo[3,4-b]piridin-3-il]pirimidin-5-il}carbamato e sua purificação para uso como substância ativa farmacêutica. a presente invenção refere-se a um processo para preparação de metil-{4,6-diamino-2-[1-(2-fluorobenzil)-1h-pirazolo[3,4-b]piridin-3-il]pirimidin-5-il} carbamato, isto é, o cosposto da fómula (i), assim como a um processo para purificação do produto cru da fórmula (i) para emprego como matéria prima farmaceuticamente eficaz, sendo que, para purificação, é isolado metil-{4,6-diamino-2-[1-(2-fluorobenzil)-1h-pirazolo[3,4-b]piridin-3-il]pirimidin-5-il} carbamato-sulfinildimetano (1:2) da fórmula (ii) como etapa intermediária, ou é preparado como etapa intermediária neste processo de purificação, se apropriado presente em uma mistura.
BR112012012618A 2009-11-27 2010-11-22 processo para preparação de metil {4, 6-diamino-2-[1-(2-fluorobenzil) - 1h-pirazolo [3, 4-b] piridin-3-il] pirimidin-5-il} carbamato e sua purificação para uso com substância ativa farmacêutica BR112012012618A2 (pt)

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
BR112012012618A2 true BR112012012618A2 (pt) 2015-09-08

Family

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Family Applications (1)

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BR112012012618A BR112012012618A2 (pt) 2009-11-27 2010-11-22 processo para preparação de metil {4, 6-diamino-2-[1-(2-fluorobenzil) - 1h-pirazolo [3, 4-b] piridin-3-il] pirimidin-5-il} carbamato e sua purificação para uso com substância ativa farmacêutica

Country Status (22)

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

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SI2504334T1 (sl) 2009-11-27 2014-11-28 Bayer Intellectual Property Gmbh Postopek čiščenja (4,6-diamino-2-(1-(2-fluorobenzil)-1H-pirazolo-(3,4-b)piridin-3-il)piri midin-5-il)metilkarbamata
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
RS61609B1 (sr) * 2011-11-25 2021-04-29 Adverio Pharma Gmbh Supstituisani 5-fluor-1h-pirazolopiridin u kristalnom obliku
EP2958914B1 (en) 2013-02-21 2020-07-15 Adverio Pharma GmbH Forms of methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridino-3-yl]pyrimidino-5-yl}methyl carbamate
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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
WO2018111795A2 (en) 2016-12-13 2018-06-21 Ironwood Pharmaceuticals, 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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Also Published As

Publication number Publication date
UY33041A (es) 2011-06-30
JP2013512211A (ja) 2013-04-11
EP2504335B1 (de) 2013-09-04
CA2781922A1 (en) 2011-06-03
ES2433236T3 (es) 2013-12-10
AR079135A1 (es) 2011-12-28
KR20120098815A (ko) 2012-09-05
MA33764B1 (fr) 2012-11-01
US8501945B2 (en) 2013-08-06
EA201270639A1 (ru) 2013-01-30
US20110130411A1 (en) 2011-06-02
IL219861A0 (en) 2012-07-31
CO6551707A2 (es) 2012-10-31
AU2010323297A1 (en) 2012-06-14
TN2012000259A1 (en) 2013-12-12
CU20120083A7 (es) 2012-10-15
DOP2012000143A (es) 2013-01-31
WO2011064156A2 (de) 2011-06-03
CN102712637A (zh) 2012-10-03
ECSP12011920A (es) 2012-07-31
TW201200513A (en) 2012-01-01
WO2011064156A3 (de) 2011-10-20
MX2012005942A (es) 2012-10-03
EP2504335A2 (de) 2012-10-03

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