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EA201201662A1 - Дизамещенные тетрагидрофуранильные соединения в качестве антагонистов брадикининового рецептора в1 - Google Patents

Дизамещенные тетрагидрофуранильные соединения в качестве антагонистов брадикининового рецептора в1

Info

Publication number
EA201201662A1
EA201201662A1 EA201201662A EA201201662A EA201201662A1 EA 201201662 A1 EA201201662 A1 EA 201201662A1 EA 201201662 A EA201201662 A EA 201201662A EA 201201662 A EA201201662 A EA 201201662A EA 201201662 A1 EA201201662 A1 EA 201201662A1
Authority
EA
Eurasian Patent Office
Prior art keywords
tetrahydrofuranile
radique
antagonists
receptor
connections
Prior art date
Application number
EA201201662A
Other languages
English (en)
Other versions
EA022787B1 (ru
Inventor
Норберт Хауэль
Анджело Чечи
Хенри Додс
Биргит Юнг
Раймунд Кюльцер
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 EA201201662A1 publication Critical patent/EA201201662A1/ru
Publication of EA022787B1 publication Critical patent/EA022787B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom 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
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P17/04—Antipruritics
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/16—Emollients or protectives, e.g. against radiation
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • 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
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Biomedical Technology (AREA)
  • Toxicology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

В заявке описаны обладающие ценными свойствами дизамещенные тетрагидрофуранильные соединения общей формулы (I)в которой переменные R, Rи X имеют указанные в описании изобретения значения, их энантиомеры, их диастереомеры, их смеси и их соли, прежде всего их физиологически совместимые соли с органическими или неорганическими кислотами или основаниями, способ их получения, содержащие такие фармакологически активные соединения лекарственные средства, способ их приготовления и их применение.
EA201201662A 2010-08-20 2011-08-19 Дизамещенные тетрагидрофуранильные соединения в качестве антагонистов брадикининового рецептора в1 EA022787B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP10173489 2010-08-20
PCT/EP2011/064260 WO2012022795A1 (de) 2010-08-20 2011-08-19 Disubstituierte tetrahydofuranyl-verbindungen als antagonisten des bradykinin-b1-rezeptors

Publications (2)

Publication Number Publication Date
EA201201662A1 true EA201201662A1 (ru) 2013-07-30
EA022787B1 EA022787B1 (ru) 2016-03-31

Family

ID=44510978

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201201662A EA022787B1 (ru) 2010-08-20 2011-08-19 Дизамещенные тетрагидрофуранильные соединения в качестве антагонистов брадикининового рецептора в1

Country Status (36)

Country Link
US (1) US8937073B2 (ru)
EP (1) EP2606042B1 (ru)
JP (1) JP5727011B2 (ru)
KR (1) KR101822371B1 (ru)
CN (1) CN103068817B (ru)
AP (1) AP2012006630A0 (ru)
AR (1) AR082507A1 (ru)
AU (1) AU2011290727B2 (ru)
BR (1) BR112013003752A2 (ru)
CA (1) CA2807086A1 (ru)
CL (1) CL2013000310A1 (ru)
CO (1) CO6680689A2 (ru)
CY (1) CY1115933T1 (ru)
DK (1) DK2606042T3 (ru)
EA (1) EA022787B1 (ru)
EC (1) ECSP13012495A (ru)
ES (1) ES2525296T3 (ru)
GE (1) GEP20146196B (ru)
HR (1) HRP20141172T1 (ru)
IL (1) IL224039A (ru)
MA (1) MA34578B1 (ru)
ME (1) ME01899B (ru)
MX (1) MX352548B (ru)
MY (1) MY156233A (ru)
NZ (1) NZ607435A (ru)
PE (1) PE20130810A1 (ru)
PH (1) PH12013500330A1 (ru)
PL (1) PL2606042T3 (ru)
PT (1) PT2606042E (ru)
RS (1) RS53622B1 (ru)
SG (1) SG187835A1 (ru)
SI (1) SI2606042T1 (ru)
TW (1) TWI548632B (ru)
UA (1) UA108765C2 (ru)
UY (1) UY33565A (ru)
WO (1) WO2012022795A1 (ru)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
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DE102007034620A1 (de) * 2007-07-25 2009-01-29 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue B1-Antagonisten
TW200911761A (en) 2007-08-29 2009-03-16 Boehringer Ingelheim Int New B1-antagonists
US8937073B2 (en) 2010-08-20 2015-01-20 Boehringer Ingelheim International Gmbh Disubstituted tetrahydrofuranyl compounds and their use as B1-receptor antagonists
US10544117B2 (en) 2014-09-10 2020-01-28 Temple University—Of the Commonwealth System of Higher Education 5-hydroxytryptamine receptor 7 activity modulators and their method of use
US20180221365A1 (en) * 2015-05-12 2018-08-09 Temple University-Of The Commonwealth System Of Higher Education Novel sigma-2 receptor binders and their method of use
WO2021198534A1 (en) 2020-04-04 2021-10-07 Oxurion NV Plasma kallikrein inhibitors for use in the treatment of coronaviral disease
US11401303B2 (en) * 2020-06-15 2022-08-02 Taian City Qihang Biotechnology Co. Synthetic peptide BRAP and application in preparation of anti-inflammatory drug for COVID-19 thereof
WO2023148016A1 (en) 2022-02-04 2023-08-10 Oxurion NV Biomarker for plasma kallikrein inhibitor therapy response

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WO2003065789A2 (en) 2002-02-08 2003-08-14 Merck & Co., Inc. N-biphenylmethyl aminocycloalkanecarboxamide derivatives
US6919343B2 (en) 2002-02-08 2005-07-19 Merck & Co., Inc. N-biphenyl(substituted methyl) aminocycloalkane-carboxamide derivatives
RU2005108667A (ru) 2002-08-29 2005-08-27 Мерк энд Ко., Инк. (US) Производные n-биарилметиламиноциклоалканкарбоксамида
CA2534188A1 (en) 2003-08-07 2005-02-24 Merck & Co., Inc. Sulfonyl substituted n-(biarylmethyl) aminocyclopropanecarboxamides
CN1832922A (zh) * 2003-08-07 2006-09-13 默克公司 磺酰基取代的n－(联芳基甲基)氨基环丙烷甲酰胺类
AU2005219836A1 (en) * 2004-03-02 2005-09-15 Merck & Co., Inc. Amino cyclopropane carboxamide derivatives as bradykinin antagonists
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US7998980B2 (en) * 2006-09-15 2011-08-16 Hydra Biosciences, Inc. Compounds for modulating TRPV3 function
HUP0600809A3 (en) 2006-10-27 2008-09-29 Richter Gedeon Nyrt New phenylsulfamoyl-benzamide derivatives as bradykinin antagonists, process and intermediates for their preparation and pharmaceutical compositions containing them
DE102007034620A1 (de) 2007-07-25 2009-01-29 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue B1-Antagonisten
EP2025675A1 (de) 2007-08-14 2009-02-18 Boehringer Ingelheim International GmbH Arylsulfonamide mit analgetischer Wirkung
TW200911761A (en) 2007-08-29 2009-03-16 Boehringer Ingelheim Int New B1-antagonists
AR068509A1 (es) * 2007-09-19 2009-11-18 Jerini Ag Antagosnistas del receptor de bradiquinina b1
WO2010057899A1 (de) 2008-11-20 2010-05-27 Boehringer Ingelheim International Gmbh Cykloalkylaminocarbonylderivate als bradykinin-b1-rezeptor antagonisten
DK2401256T3 (da) * 2009-02-26 2013-06-03 Boehringer Ingelheim Int Forbindelser som bradykinin-B1-antagonister.
WO2010097374A1 (de) 2009-02-26 2010-09-02 Boehringer Ingelheim International Gmbh Verbindungen als bradykinin-b1-antagonisten
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US8586604B2 (en) 2010-08-20 2013-11-19 Boehringer Ingelheim International Gmbh Inhibitors of the microsomal prostaglandin E2 synthase-1
EP2606043B1 (de) * 2010-08-20 2014-07-09 Boehringer Ingelheim International GmbH Pyridazinderivative als bradykinin b1 rezeptor antagonsiten
US8937073B2 (en) 2010-08-20 2015-01-20 Boehringer Ingelheim International Gmbh Disubstituted tetrahydrofuranyl compounds and their use as B1-receptor antagonists
US8759537B2 (en) 2010-08-20 2014-06-24 Boehringer Ingelheim International Gmbh 3H-imidazo [4, 5-C] pyridine-6-carboxamides as anti-inflammatory agents
CA2808798C (en) 2010-08-20 2020-04-28 Allergan, Inc. Compounds act at multiple prostaglandin receptors giving a general anti-inflammatory response

Also Published As

Publication number Publication date
ECSP13012495A (es) 2013-04-30
JP5727011B2 (ja) 2015-06-03
AU2011290727A1 (en) 2013-03-14
PL2606042T3 (pl) 2015-03-31
US8937073B2 (en) 2015-01-20
DK2606042T3 (da) 2014-12-08
SG187835A1 (en) 2013-03-28
MY156233A (en) 2016-01-29
TWI548632B (zh) 2016-09-11
KR20130114082A (ko) 2013-10-16
EA022787B1 (ru) 2016-03-31
CN103068817B (zh) 2014-10-29
BR112013003752A2 (pt) 2016-05-31
TW201305145A (zh) 2013-02-01
UY33565A (es) 2012-03-30
MX352548B (es) 2017-11-29
MA34578B1 (fr) 2013-10-02
WO2012022795A1 (de) 2012-02-23
UA108765C2 (xx) 2015-06-10
MX2013001965A (es) 2013-05-09
GEP20146196B (en) 2014-11-10
HRP20141172T1 (hr) 2015-02-13
PE20130810A1 (es) 2013-07-25
US20120208823A1 (en) 2012-08-16
RS53622B1 (en) 2015-04-30
ES2525296T3 (es) 2014-12-19
AU2011290727B2 (en) 2015-07-16
EP2606042A1 (de) 2013-06-26
AP2012006630A0 (en) 2012-12-31
KR101822371B1 (ko) 2018-01-31
ME01899B (me) 2014-12-20
SI2606042T1 (sl) 2014-12-31
HK1178902A1 (en) 2013-09-19
CY1115933T1 (el) 2017-01-25
CO6680689A2 (es) 2013-05-31
AR082507A1 (es) 2012-12-12
PH12013500330A1 (en) 2021-06-02
CN103068817A (zh) 2013-04-24
PT2606042E (pt) 2014-10-15
JP2013534238A (ja) 2013-09-02
IL224039A (en) 2016-03-31
CA2807086A1 (en) 2012-02-23
NZ607435A (en) 2015-07-31
CL2013000310A1 (es) 2013-04-01
EP2606042B1 (de) 2014-09-03

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