ECSP13012847A - Dimaleato de 9-[4-(3-cloro-2-fluoro-fenilamino)-7-metoxi-quinazolin-6-iloxi]-1,4-diaza-espiro[5.5]undecan-5-ona, su uso como medicamento y su preparación. - Google Patents

Dimaleato de 9-[4-(3-cloro-2-fluoro-fenilamino)-7-metoxi-quinazolin-6-iloxi]-1,4-diaza-espiro[5.5]undecan-5-ona, su uso como medicamento y su preparación.

Info

Publication number
ECSP13012847A
ECSP13012847A ECSP13012847A ECSP13012847A EC SP13012847 A ECSP13012847 A EC SP13012847A EC SP13012847 A ECSP13012847 A EC SP13012847A EC SP13012847 A ECSP13012847 A EC SP13012847A
Authority
EC
Ecuador
Prior art keywords
espiro
iloxi
metoxi
undecan
dimaleate
Prior art date
Application number
Other languages
English (en)
Inventor
Waldemar Pfrengle
Peter Sieger
Guenther Huchler
Markus Ostermeier
Original Assignee
Boehringer Ingelheim Int
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 Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of ECSP13012847A publication Critical patent/ECSP13012847A/es

Links

Classifications

    • 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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • 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
    • 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
    • A61P13/08—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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Un método para prevenir el ictus en un paciente que padece fibrilación auricular, en el que el paciente no tiene factores de riesgo para acontecimientos hemorrágicos mayores, comprendiendo el método administrar al paciente 150 mg b.i.d. de etexilato de dabigatrán, opcionalmente en forma de una sal farmacéuticamente aceptable del mismo.
ECSP13012847 2011-02-01 2013-08-21 Dimaleato de 9-[4-(3-cloro-2-fluoro-fenilamino)-7-metoxi-quinazolin-6-iloxi]-1,4-diaza-espiro[5.5]undecan-5-ona, su uso como medicamento y su preparación. ECSP13012847A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP11152895 2011-02-01

Publications (1)

Publication Number Publication Date
ECSP13012847A true ECSP13012847A (es) 2014-09-30

Family

ID=43896655

Family Applications (1)

Application Number Title Priority Date Filing Date
ECSP13012847 ECSP13012847A (es) 2011-02-01 2013-08-21 Dimaleato de 9-[4-(3-cloro-2-fluoro-fenilamino)-7-metoxi-quinazolin-6-iloxi]-1,4-diaza-espiro[5.5]undecan-5-ona, su uso como medicamento y su preparación.

Country Status (24)

Country Link
US (2) US8853225B2 (es)
EP (1) EP2670736B1 (es)
JP (1) JP2014504619A (es)
KR (1) KR20140011330A (es)
CN (1) CN103608336A (es)
AP (1) AP3531A (es)
AR (1) AR085056A1 (es)
AU (1) AU2012213556A1 (es)
BR (1) BR112013019416A2 (es)
CA (1) CA2826193A1 (es)
CL (1) CL2013002031A1 (es)
CO (1) CO6781555A2 (es)
EA (1) EA023573B1 (es)
EC (1) ECSP13012847A (es)
GE (1) GEP20156423B (es)
IL (1) IL227534A0 (es)
MA (1) MA34845B1 (es)
MX (1) MX2013008870A (es)
PE (1) PE20141012A1 (es)
PH (1) PH12013501599A1 (es)
SG (1) SG192216A1 (es)
TN (1) TN2013000323A1 (es)
UY (1) UY33889A (es)
WO (1) WO2012104206A1 (es)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2289881A1 (de) * 2009-08-06 2011-03-02 Boehringer Ingelheim International GmbH Verfahren zur stereoselektiven Synthese bicyclischer Heterocyclen
GEP20156423B (en) 2011-02-01 2016-01-11 Boehringer Ingelheim Int 9-[4-(3-chlor-2-fluorphenylamino)-7-methoxy- quinazolin-6-yloxy]-1,4-diaza-spiro[5.5]undecan-5-one dimaleate, usage thereas drug, and production thereof
JP6105631B2 (ja) 2012-02-09 2017-03-29 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 1,4−保護9−ヒドロキシ−5−オキソ−1,4−ジアザ−スピロ[5.5]ウンデカンの立体選択的合成方法
JP2015524400A (ja) 2012-07-19 2015-08-24 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 9−[4−(3−クロロ−2−フルオロ−フェニルアミノ)−7−メトキシ−キナゾリン−6−イルオキシ]−1,4−ジアザ−スピロ[5.5]ウンデカン−5−オンのフマル酸塩、その薬物としての使用及び調製
JP6342001B2 (ja) * 2013-12-12 2018-06-13 天津和美奥康医薬科技有限公司 キナゾリン誘導体
CN105017164A (zh) * 2015-08-25 2015-11-04 佛山市赛维斯医药科技有限公司 含新型苯并喹唑啉和邻位氯结构的酪氨酸激酶抑制剂及用途
CN105130913A (zh) * 2015-08-25 2015-12-09 佛山市赛维斯医药科技有限公司 一类多取代的苯并喹唑啉类酪氨酸激酶抑制剂及用途
CN109503579A (zh) * 2018-12-17 2019-03-22 天津药明康德新药开发有限公司 叔丁基-1-甲基-5-氧亚基三氮杂螺[5.5]十一烷-9-甲酸基酯的制备方法
CN109485648A (zh) * 2018-12-17 2019-03-19 无锡合全药业有限公司 叔丁基-1-甲基-5-氧亚基三氮杂螺[5.5]十一烷-8-甲酸基酯的制备方法
CN109608470A (zh) * 2018-12-17 2019-04-12 上海药明康德新药开发有限公司 叔丁基-9-氧亚基-2,5,8-三氮杂螺[3.5]壬烷-2-甲酸基酯的合成方法

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200813014A (en) 2002-03-28 2008-03-16 Astrazeneca Ab Quinazoline derivatives
NZ536114A (en) 2002-03-30 2007-11-30 Boehringer Ingelheim Pharma 4-(N-phenylamino)-quinazolines / quinolines as tyrosine kinase inhibitors
CA2581150A1 (en) 2004-09-17 2006-03-30 Osi Pharmaceuticals, Inc. (spirocyclylamido) aminothiophene compounds as c-kit proto- oncogene inhibitors
EP1966189A1 (de) 2005-12-12 2008-09-10 Boehringer Ingelheim International Gmbh Bicyclische heterocyclen, diese verbindungen enthaltende arzneimittel, deren verwendung und verfahren zu ihrer herstellung
TWI421070B (zh) 2007-10-26 2014-01-01 Japan Tobacco Inc 螺化合物及其醫藥用途
WO2009098061A1 (de) * 2008-02-07 2009-08-13 Boehringer Ingelheim International Gmbh Spirocyclische heterocyclen, diese verbindungen enthaltende arzneimittel, deren verwendung und verfahren zu ihrer herstellung
EP2346507A1 (en) * 2008-09-03 2011-07-27 Boehringer Ingelheim International GmbH Use of quinazoline derivatives for the treatment of viral diseases
EP2289881A1 (de) 2009-08-06 2011-03-02 Boehringer Ingelheim International GmbH Verfahren zur stereoselektiven Synthese bicyclischer Heterocyclen
GEP20156423B (en) 2011-02-01 2016-01-11 Boehringer Ingelheim Int 9-[4-(3-chlor-2-fluorphenylamino)-7-methoxy- quinazolin-6-yloxy]-1,4-diaza-spiro[5.5]undecan-5-one dimaleate, usage thereas drug, and production thereof

Also Published As

Publication number Publication date
CN103608336A (zh) 2014-02-26
US20130030003A1 (en) 2013-01-31
MX2013008870A (es) 2013-08-14
AP2013006989A0 (en) 2013-07-31
EP2670736A1 (de) 2013-12-11
US8906931B1 (en) 2014-12-09
KR20140011330A (ko) 2014-01-28
UY33889A (es) 2012-08-31
GEP20156423B (en) 2016-01-11
EA023573B1 (ru) 2016-06-30
MA34845B1 (fr) 2014-01-02
CL2013002031A1 (es) 2013-12-27
TN2013000323A1 (en) 2015-01-20
CO6781555A2 (es) 2013-10-31
AR085056A1 (es) 2013-08-07
JP2014504619A (ja) 2014-02-24
WO2012104206A1 (de) 2012-08-09
NZ613917A (en) 2015-08-28
AU2012213556A1 (en) 2013-08-22
AP3531A (en) 2016-01-13
PE20141012A1 (es) 2014-09-10
IL227534A0 (en) 2013-09-30
US20140371226A1 (en) 2014-12-18
PH12013501599A1 (en) 2019-03-22
WO2012104206A9 (de) 2013-11-21
BR112013019416A2 (pt) 2019-09-24
EA201300872A1 (ru) 2014-01-30
CA2826193A1 (en) 2012-08-09
US8853225B2 (en) 2014-10-07
EP2670736B1 (de) 2017-03-15
SG192216A1 (en) 2013-09-30

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