DOP2012000143A - Procedimiento para la preparacion de {4,6-diamino-2-[1-(2-fluorobencil)-1h-pirazolo [3,4-b]piridin-3-il]pirimidin-5-il}carbamato de metilo y su purificacion para el uso como principio activo farmaceutico - Google Patents

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

Info

Publication number
DOP2012000143A
DOP2012000143A DO2012000143A DO2012000143A DOP2012000143A DO P2012000143 A DOP2012000143 A DO P2012000143A DO 2012000143 A DO2012000143 A DO 2012000143A DO 2012000143 A DO2012000143 A DO 2012000143A DO P2012000143 A DOP2012000143 A DO P2012000143A
Authority
DO
Dominican Republic
Prior art keywords
purification
diamino
preparation
mettilo
fluorobencil
Prior art date
Application number
DO2012000143A
Other languages
English (en)
Inventor
Joachim Rehse
Franz-Josef Mais
Winfried Joentgen
Konrad Siegel
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 DOP2012000143A publication Critical patent/DOP2012000143A/es

Links

Classifications

    • 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

Abstract

La presente invención se refiere a un procedimiento para la preparación de {4,6-diamino-2-[1 -(2-fluorobencil)-1 H-pirazolo[3,4-b]piridin-3-il]pirìmidin-5- il}carbamato de metilo, es decir del compuesto de fórmula (l) así como a un procedimiento para la purifìcación del producto bruto de fórmula (l) para el uso como sustancia farmacéuticamente activa. Aislándose para la purificación se genera {4,6-diamino-2-[1-(2-fluorobencil)-1 H-pirazolo[3,4-b]piridin- 3-il]pirimidin-5-il}carbamato de metilo sulfinildimetano (1 :2) de fórmula (11) como sustancia intermedia o se genera como sustancia intermedia en este procedimiento de purificación presentándose dado el caso en una mezcla.
DO2012000143A 2009-11-27 2012-05-24 Procedimiento para la preparacion de {4,6-diamino-2-[1-(2-fluorobencil)-1h-pirazolo [3,4-b]piridin-3-il]pirimidin-5-il}carbamato de metilo y su purificacion para el uso como principio activo farmaceutico DOP2012000143A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09177369 2009-11-27

Publications (1)

Publication Number Publication Date
DOP2012000143A true DOP2012000143A (es) 2013-01-31

Family

ID=43568194

Family Applications (1)

Application Number Title Priority Date Filing Date
DO2012000143A DOP2012000143A (es) 2009-11-27 2012-05-24 Procedimiento para la preparacion de {4,6-diamino-2-[1-(2-fluorobencil)-1h-pirazolo [3,4-b]piridin-3-il]pirimidin-5-il}carbamato de metilo y su purificacion para el uso como principio activo farmaceutico

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
SI3415515T1 (sl) 2009-11-27 2020-03-31 Adverio Pharma Gmbh Postopek priprave metil-(4,6-diamino-2-(1-(2-fluorobenzil)-1H-pirazolo(3,4-b)piridin-3- il)pirimidin-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
MY168412A (en) * 2011-11-25 2018-11-09 Adverio Pharma Gmbh Method for producing substituted 5-fluoro-1h-pyrazolopyridines
SG11201506211RA (en) 2013-02-21 2015-09-29 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
CA3006764A1 (en) 2015-12-14 2017-06-22 Ironwood Pharmaceuticals, 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
AU2019301683A1 (en) 2018-07-11 2021-02-11 Tisento 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

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9013750D0 (en) 1990-06-20 1990-08-08 Pfizer Ltd Therapeutic agents
GB9311920D0 (en) 1993-06-09 1993-07-28 Pfizer Ltd Therapeutic agents
GB9401090D0 (en) 1994-01-21 1994-03-16 Glaxo Lab Sa Chemical compounds
DE19642255A1 (de) 1996-10-14 1998-04-16 Bayer Ag Verwendung von 1-Benzyl-3-(substituierten-hetaryl) -kondensierten Pyrazol-Derivaten
EP0934311B1 (de) 1996-10-14 2009-05-13 Bayer HealthCare AG Neue heterocyclylmethyl-substituierte pyrazolderivate und ihre verwendung in der behandlung von herz-kreislauf-erkrankungen
DE19649460A1 (de) 1996-11-26 1998-05-28 Bayer Ag Neue substituierte Pyrazolderivate
GB2346877B (en) 1997-11-12 2001-12-05 Bayer Ag 2-phenyl substituted imidazotriazinones as phosphodiesterase inhibitors
DE19834044A1 (de) 1998-07-29 2000-02-03 Bayer Ag Neue substituierte Pyrazolderivate
DE19834047A1 (de) 1998-07-29 2000-02-03 Bayer Ag Substituierte Pyrazolderivate
DE19834045A1 (de) 1998-07-29 2000-02-03 Bayer Ag (4-Amino-5-ethylpyrimidin-2-yl)-1-(2-fluorbenzyl)-1H-pyrazolo[3,4-b]pyridin
DE19846514A1 (de) 1998-10-09 2000-04-20 Bayer Ag Neue Heterocyclyl-methyl-substituierte Pyrazole
DE10057754A1 (de) * 2000-11-22 2002-05-23 Bayer Ag Neue Sulfonamid-substituierte Pyrazolopyridinderivate
DE10057751A1 (de) 2000-11-22 2002-05-23 Bayer Ag Neue Carbamat-substituierte Pyrazolopyridinderivate
US6903089B1 (en) * 2000-11-22 2005-06-07 Bayer Aktiengesellschaft Lactam-substituted pyrazolopyridine derivatives
AR031176A1 (es) 2000-11-22 2003-09-10 Bayer Ag Nuevos derivados de pirazolpiridina sustituidos con piridina
DE10122894A1 (de) * 2001-05-11 2002-11-14 Bayer Ag Neue Sulfonat-substituierte Pyrazolopyridinderivate
DE10132416A1 (de) * 2001-07-04 2003-01-16 Bayer Ag Neue Morpholin-überbrückte Pyrazolopyridinderivate
DE10220570A1 (de) 2002-05-08 2003-11-20 Bayer Ag Carbamat-substituierte Pyrazolopyridine
DE10222550A1 (de) * 2002-05-17 2003-11-27 Bayer Ag Substituierte Benzyl-pyrazolopyridine
DE10351903A1 (de) * 2003-11-06 2005-06-09 Bayer Healthcare Ag Neue Kombination
DE102006021733A1 (de) * 2006-05-09 2007-11-22 Bayer Healthcare Ag 3-Tetrazolylindazole und 3-Tetrazolylpyrazolopyridine sowie ihre Verwendung
DE102006043443A1 (de) * 2006-09-15 2008-03-27 Bayer Healthcare Ag Neue aza-bicyclische Verbindungen und ihre Verwendung
DE102009004245A1 (de) * 2009-01-09 2010-07-15 Bayer Schering Pharma Aktiengesellschaft Neue anellierte, Heteroatom-verbrückte Pyrazol- und Imidazol-Derivate und ihre Verwendung

Also Published As

Publication number Publication date
MX2012005942A (es) 2012-10-03
EP2504335B1 (de) 2013-09-04
EA201270639A1 (ru) 2013-01-30
IL219861A0 (en) 2012-07-31
BR112012012618A2 (pt) 2015-09-08
WO2011064156A3 (de) 2011-10-20
KR20120098815A (ko) 2012-09-05
CO6551707A2 (es) 2012-10-31
CN102712637A (zh) 2012-10-03
MA33764B1 (fr) 2012-11-01
AU2010323297A1 (en) 2012-06-14
AR079135A1 (es) 2011-12-28
US8501945B2 (en) 2013-08-06
CA2781922A1 (en) 2011-06-03
EP2504335A2 (de) 2012-10-03
WO2011064156A2 (de) 2011-06-03
CU20120083A7 (es) 2012-10-15
TW201200513A (en) 2012-01-01
ES2433236T3 (es) 2013-12-10
US20110130411A1 (en) 2011-06-02
UY33041A (es) 2011-06-30
JP2013512211A (ja) 2013-04-11
TN2012000259A1 (en) 2013-12-12
ECSP12011920A (es) 2012-07-31

Similar Documents

Publication Publication Date Title
ECSP18018453A (es) Procedimiento para la preparación de {4,6-diamino-2-[1-(2-fluorobencil)-1h-pirazolo[3,4-b]piridin-3-il]pirimidin-5-il}metilcarbamato de metilo y su purificación para su uso como principio activo farmacéutico
DOP2012000143A (es) Procedimiento para la preparacion de {4,6-diamino-2-[1-(2-fluorobencil)-1h-pirazolo [3,4-b]piridin-3-il]pirimidin-5-il}carbamato de metilo y su purificacion para el uso como principio activo farmaceutico
CR20130617A (es) Derivados de piridin-2(1h)-ona útiles como medicamentos para el tratamiento de trastornos mieloproliferativos, rechazo de trasplantes, enfermedades mediadas por el sistema inmune y enfermedades inflamatorias
GEP20156417B (en) Pyrrolo [2,3-d] pyrimidine derivatives as inhibitors of tropomyosin-related kinases
BR112013023876A2 (pt) derivados de pirroltriazinona como inibidores de pi3k
CR11641A (es) Derivados heterociclicos de urea y metodos de uso de los mismos-211
DOP2014000008A (es) 4-imidazopiridazina-1-il-benzamidas y 4-imidazotriazina-1-il-benzamidas como inhibidores de btk
GT201300137A (es) Derivados de imidazo [1,2-b] piridazina e imidazo [4,5-b] piridina como inhibidores de jak
MX2013008359A (es) Aminas de c-28 de derivados de acido betulinico modificado de c-3 como inhibidores de la maduracion del virus de inmunodeficiencia humana.
MX2012007175A (es) Derivados de imidazopiridina como inhibidores de jak.
ECSP109935A (es) Derivados de morfolino pirimidina utilizados en enfermedades relacionadas con mtor quinasa y/o pi3k
BR112015007231A2 (pt) derivados de pirroltriazinona como inibidores de pi3k
WO2013004995A8 (en) Pyrimidinone compounds and their use
BR112014002245A2 (pt) derivados de piridin-2(1h)-ona como inibidores de jak
ECSP12011923A (es) Nuevas formas polimorfas de {4,6-diamino-2-[1-(2-fluorobencil)-1h-pirazolo[3,4-b]piridin-3-il]pirimidin-5-il}carbamato de metilo
UY32674A (es) Derivados heterociclicos de la urea y sus metodos de empleo
CO6382176A2 (es) Derivados de urea heterociclicos y metodos de uso de los mismos-332
DOP2010000374A (es) Derivados heterociclicos de la urea y sus metodos de empleo
UY32694A (es) Derivados heterocíclicos de urea y métodos de uso de los mismos
BR112012018658A2 (pt) sais farmaceuticamente aceitáveis de derivados heterocíclicos nitrogenosos - pirrolo, processo de preração e seu uso médico
CU20100004A7 (es) Derivados de morfolino pirimidina utilizados en enfermedades relacionadas con mtor quinasa y/o pi3k