CU20120083A7 - Procedimiento para la preparación de {4,6-diamino-2-[1-(2-fluorobencil)-1h-pirazolo[3,4-b]piridin-3-il]pirimidin-5-il}carbamato de metilo y su purificación para el uso como principio activo farmacéutico - Google Patents

Procedimiento para la preparación de {4,6-diamino-2-[1-(2-fluorobencil)-1h-pirazolo[3,4-b]piridin-3-il]pirimidin-5-il}carbamato de metilo y su purificación para el uso como principio activo farmacéutico

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Publication number
CU20120083A7
CU20120083A7 CU2012000083A CU20120083A CU20120083A7 CU 20120083 A7 CU20120083 A7 CU 20120083A7 CU 2012000083 A CU2012000083 A CU 2012000083A CU 20120083 A CU20120083 A CU 20120083A CU 20120083 A7 CU20120083 A7 CU 20120083A7
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CU
Cuba
Prior art keywords
purification
diamino
preparation
procedure
mettilo
Prior art date
Application number
CU2012000083A
Other languages
English (en)
Inventor
Franz-Josef Mais
Joachim Rehse
Winfried Joentgen
Konrad Siegel
Original Assignee
Bayer Ip Gmbh
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Publication date
Application filed by Bayer Ip Gmbh filed Critical Bayer Ip Gmbh
Publication of CU20120083A7 publication Critical patent/CU20120083A7/es

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    • C—CHEMISTRY; METALLURGY
    • 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
    • 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
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/06—Antiarrhythmics
    • 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
    • A61P9/12—Antihypertensives
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Pulmonology (AREA)
  • Reproductive Health (AREA)
  • Ophthalmology & Optometry (AREA)
  • Vascular Medicine (AREA)
  • Gynecology & Obstetrics (AREA)
  • Hospice & Palliative Care (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

La presente invención se refiere a un procedimiento para la preparación de {4,6-diamino-2-[1-(2-fluorobencil)-1H-pirazolo[3,4-B]piridin-3-il]pirimidin-5-il}carbamato de metilo, es decir del compuesto de fórmula (I) ESPACIO PARA LA FÓRMULA así como a un procedimiento para la purificación del producto bruto de fórmula (I) para el uso como sustancia farmacéuticamente activa. Aislándose para la purificación se genera {4,6-diamino-2-[1-(2-fluorobencil)-1H-pirazolo[3,4-B]piridin-3-il]pirimidin-5-il}metilcarbamato de metilo-sulfinildimetano (1:2) de fórmula (II) como sustancia intermedia o se genera como sustancia intermedia en este procedimiento de purificación presentándose dado el caso en una mezcla.
CU2012000083A 2009-11-27 2012-05-24 Procedimiento para la preparación de {4,6-diamino-2-[1-(2-fluorobencil)-1h-pirazolo[3,4-b]piridin-3-il]pirimidin-5-il}carbamato de metilo y su purificación para el uso como principio activo farmacéutico CU20120083A7 (es)

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
CU20120083A7 true CU20120083A7 (es) 2012-10-15

Family

ID=43568194

Family Applications (1)

Application Number Title Priority Date Filing Date
CU2012000083A CU20120083A7 (es) 2009-11-27 2012-05-24 Procedimiento para la preparación de {4,6-diamino-2-[1-(2-fluorobencil)-1h-pirazolo[3,4-b]piridin-3-il]pirimidin-5-il}carbamato de metilo y su purificación para el uso como principio activo farmacéutico

Country Status (22)

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

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
AU2016371762A1 (en) 2015-12-14 2018-06-21 Cyclerion Therapeutics, Inc. Use of sGC stimulators for the treatment of gastrointestinal sphincter dysfunction
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
BR112012012618A2 (pt) 2015-09-08
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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