EA201200219A1 - Способ стереоселективного синтеза бициклических гетероциклов - Google Patents

Способ стереоселективного синтеза бициклических гетероциклов

Info

Publication number
EA201200219A1
EA201200219A1 EA201200219A EA201200219A EA201200219A1 EA 201200219 A1 EA201200219 A1 EA 201200219A1 EA 201200219 A EA201200219 A EA 201200219A EA 201200219 A EA201200219 A EA 201200219A EA 201200219 A1 EA201200219 A1 EA 201200219A1
Authority
EA
Eurasian Patent Office
Prior art keywords
primarily
diseases
stereoelective
synthesis
well
Prior art date
Application number
EA201200219A
Other languages
English (en)
Other versions
EA023562B1 (ru
Inventor
Маркус Остермайер
Юрген Дойблер
Гюнтер Хухлер
Штефан Клинг
Марко Сантагостино
Original Assignee
Бёрингер Ингельхайм Интернациональ Гмбх
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 Бёрингер Ингельхайм Интернациональ Гмбх filed Critical Бёрингер Ингельхайм Интернациональ Гмбх
Publication of EA201200219A1 publication Critical patent/EA201200219A1/ru
Publication of EA023562B1 publication Critical patent/EA023562B1/ru

Links

Classifications

    • 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
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • 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
    • 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
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Steroid Compounds (AREA)

Abstract

В заявке описан способ стереоселективного получения соединений формул (1А) и (1В)и их солей, прежде всего их физиологически совместимых солей с неорганическими или органическими кислотами и основаниями, обладающих ценными фармакологическими свойствами, прежде всего ингибирующим действием на опосредуемую тирозинкиназами трансдукцию сигналов, а также описано их применение для лечения различных заболеваний, прежде всего опухолевых заболеваний, а также доброкачественной гиперплазии простаты, заболеваний легких и дыхательных путей.
EA201200219A 2009-08-06 2010-07-30 Способ стереоселективного синтеза бициклических гетероциклов EA023562B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP09167393A EP2289881A1 (de) 2009-08-06 2009-08-06 Verfahren zur stereoselektiven Synthese bicyclischer Heterocyclen
PCT/EP2010/061096 WO2011015526A1 (de) 2009-08-06 2010-07-30 Verfahren zur stereoselektiven synthese bicyclischer heterocyclen

Publications (2)

Publication Number Publication Date
EA201200219A1 true EA201200219A1 (ru) 2012-11-30
EA023562B1 EA023562B1 (ru) 2016-06-30

Family

ID=41205591

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201200219A EA023562B1 (ru) 2009-08-06 2010-07-30 Способ стереоселективного синтеза бициклических гетероциклов

Country Status (21)

Country Link
US (2) US8658790B2 (ru)
EP (2) EP2289881A1 (ru)
JP (1) JP2013501025A (ru)
KR (1) KR20120049248A (ru)
CN (1) CN102471288B (ru)
AR (1) AR077797A1 (ru)
AU (1) AU2010280852B2 (ru)
BR (1) BR112012002104A2 (ru)
CA (1) CA2767963A1 (ru)
CL (1) CL2012000159A1 (ru)
DK (1) DK2462126T3 (ru)
EA (1) EA023562B1 (ru)
ES (1) ES2549770T3 (ru)
HU (1) HUE025400T2 (ru)
IL (1) IL216969A (ru)
MX (1) MX2012001089A (ru)
NZ (1) NZ597698A (ru)
PL (1) PL2462126T3 (ru)
TW (1) TW201120013A (ru)
UY (1) UY32830A (ru)
WO (1) WO2011015526A1 (ru)

Families Citing this family (5)

* 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
EP2670736B1 (de) * 2011-02-01 2017-03-15 Boehringer Ingelheim International GmbH 9-[4-(3-chlor-2-fluor-phenylamino)-7-methoxy-chinazolin-6- yloxy]-1,4-diaza-spiro[5.5]undecan-5-on dimaleat, dessen verwendung als arzneimittel und dessen herstellung
AU2013218119A1 (en) * 2012-02-09 2014-07-17 Boehringer Ingelheim International Gmbh Method for stereoselective synthesis of 1,4-protected 9-hydroxy-5-oxo-1,4-diaza-spiro [5.5] undecanes
EP2875020B1 (en) * 2012-07-19 2017-09-06 Boehringer Ingelheim International GmbH Process for the preparation of a fumaric acid salt of 9-[4-(3-chloro-2-fluoro-phenylamino)-7-methoxy- chinazolin-6-yloxy]-1,4-diaza-spiro[5.5]undecan-5-one
WO2021198188A1 (en) 2020-03-30 2021-10-07 Enyo Pharma Quinazolinone derivatives and uses thereof for treating a cancer

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI324597B (en) 2002-03-28 2010-05-11 Astrazeneca Ab Quinazoline derivatives
MX2009007610A (es) * 2007-02-06 2009-07-24 Boehringer Ingelheim Int Heterociclicos biciclicos, medicamentos que contienen estos compuestos, su utilizacion y procedimientos para su preparacion.
TWI421070B (zh) * 2007-10-26 2014-01-01 Japan Tobacco Inc 螺化合物及其醫藥用途
EP2245026B1 (de) * 2008-02-07 2012-08-01 Boehringer Ingelheim International GmbH Spirocyclische heterocyclen, diese verbindungen enthaltende arzneimittel, deren verwendung und verfahren zu ihrer herstellung
JP5611207B2 (ja) * 2008-08-08 2014-10-22 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 二環式複素環の立体選択的調製方法
EP2289881A1 (de) * 2009-08-06 2011-03-02 Boehringer Ingelheim International GmbH Verfahren zur stereoselektiven Synthese bicyclischer Heterocyclen
EP2670736B1 (de) 2011-02-01 2017-03-15 Boehringer Ingelheim International GmbH 9-[4-(3-chlor-2-fluor-phenylamino)-7-methoxy-chinazolin-6- yloxy]-1,4-diaza-spiro[5.5]undecan-5-on dimaleat, dessen verwendung als arzneimittel und dessen herstellung
AU2013218119A1 (en) * 2012-02-09 2014-07-17 Boehringer Ingelheim International Gmbh Method for stereoselective synthesis of 1,4-protected 9-hydroxy-5-oxo-1,4-diaza-spiro [5.5] undecanes

Also Published As

Publication number Publication date
WO2011015526A1 (de) 2011-02-10
UY32830A (es) 2011-03-31
IL216969A0 (en) 2012-02-29
US8993753B2 (en) 2015-03-31
PL2462126T3 (pl) 2015-11-30
IL216969A (en) 2015-06-30
CN102471288B (zh) 2014-10-22
ES2549770T3 (es) 2015-11-02
US8658790B2 (en) 2014-02-25
CA2767963A1 (en) 2011-02-10
AR077797A1 (es) 2011-09-21
HUE025400T2 (en) 2016-02-29
KR20120049248A (ko) 2012-05-16
CN102471288A (zh) 2012-05-23
EP2462126B1 (de) 2015-07-15
TW201120013A (en) 2011-06-16
AU2010280852B2 (en) 2015-04-02
US20110183987A1 (en) 2011-07-28
US20140135495A1 (en) 2014-05-15
NZ597698A (en) 2014-03-28
JP2013501025A (ja) 2013-01-10
MX2012001089A (es) 2012-02-28
EP2289881A1 (de) 2011-03-02
BR112012002104A2 (pt) 2015-09-15
EA023562B1 (ru) 2016-06-30
CL2012000159A1 (es) 2012-08-31
DK2462126T3 (en) 2015-09-07
EP2462126A1 (de) 2012-06-13
AU2010280852A1 (en) 2012-02-09

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Legal Events

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM RU