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EA201390723A1 - Аминозамещенные производные бисфенилпентановой кислоты в качестве ингибиторов nep - Google Patents

Аминозамещенные производные бисфенилпентановой кислоты в качестве ингибиторов nep

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Publication number
EA201390723A1
EA201390723A1 EA201390723A EA201390723A EA201390723A1 EA 201390723 A1 EA201390723 A1 EA 201390723A1 EA 201390723 A EA201390723 A EA 201390723A EA 201390723 A EA201390723 A EA 201390723A EA 201390723 A1 EA201390723 A1 EA 201390723A1
Authority
EA
Eurasian Patent Office
Prior art keywords
bisfenyl
amine
nep inhibitors
pentane acid
substitutional
Prior art date
Application number
EA201390723A
Other languages
English (en)
Other versions
EA021537B1 (ru
Inventor
Гари Марк Коппола
Раджешри Ганеш Карки
Тосио Каванами
Original Assignee
Новартис Аг
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 Новартис Аг filed Critical Новартис Аг
Publication of EA201390723A1 publication Critical patent/EA201390723A1/ru
Publication of EA021537B1 publication Critical patent/EA021537B1/ru

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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/70Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/72Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms
    • C07C235/74Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of a saturated carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/70Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/192Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
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Abstract

Настоящее изобретение представляет соединение формулы Iили его фармацевтически приемлемую соль, где R, R, R, А, X, X, s и n определены в описании. Изобретение также касается способа получения соединений по изобретению и их терапевтического применения. Настоящее изобретение также представляет фармацевтическую композицию соединений изобретения и комбинацию фармакологически активных агентов и соединения по изобретению.
EA201390723A 2010-11-16 2011-11-14 Аминозамещенные производные бисфенилпентановой кислоты в качестве ингибиторов nep EA021537B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US41416310P 2010-11-16 2010-11-16
PCT/EP2011/070080 WO2012065956A1 (en) 2010-11-16 2011-11-14 Substituted amino bisphenyl pentanoic acid derivatives as nep inhibitors

Publications (2)

Publication Number Publication Date
EA201390723A1 true EA201390723A1 (ru) 2013-09-30
EA021537B1 EA021537B1 (ru) 2015-07-30

Family

ID=45093705

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EA201390723A EA021537B1 (ru) 2010-11-16 2011-11-14 Аминозамещенные производные бисфенилпентановой кислоты в качестве ингибиторов nep

Country Status (14)

Country Link
US (1) US8673974B2 (ru)
EP (1) EP2640690A1 (ru)
JP (1) JP5872575B2 (ru)
KR (1) KR101951492B1 (ru)
CN (1) CN103201257B (ru)
AR (1) AR083873A1 (ru)
AU (1) AU2011331294B2 (ru)
BR (1) BR112013011580A2 (ru)
CA (1) CA2817114A1 (ru)
EA (1) EA021537B1 (ru)
MX (1) MX2013005533A (ru)
TW (1) TW201305089A (ru)
UY (1) UY33731A (ru)
WO (1) WO2012065956A1 (ru)

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KR102640906B1 (ko) 2015-02-11 2024-02-27 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 네프릴리신 저해제로서 (2s,4r)-5-(5''-클로로-2''-플루오로비페닐-4-일)-4-(에톡시옥살릴아미노)-2-히드록시메틸-2-메틸펜타노익산
BR112017017783A2 (pt) 2015-02-19 2018-07-17 Theravance Biopharma R&D Ip, Llc Ácido (2r,4r)-5-(5'-cloro-2'-fluorbifenil-4-il)-2-hidróxi- 4-[(5-metiloxazol-2-carbonil)amino]pentanóico.
HUE055546T2 (hu) 2016-03-08 2021-12-28 Theravance Biopharma R&D Ip Llc Kristályos (2S,4R)-5-(5'-klór-2-fluor-[1,1'-bifenil]-4-il)-2-(etoximetil)-4-(3-hidroxi izoxazol-5-karboxamido)-2-metilpentánsav és alkalmazásaik
UY38072A (es) 2018-02-07 2019-10-01 Novartis Ag Compuestos derivados de éster butanoico sustituido con bisfenilo como inhibidores de nep, composiciones y combinaciones de los mismos
UY38485A (es) 2018-11-27 2020-06-30 Novartis Ag Compuestos tetrámeros cíclicos como inhibidores de proproteína convertasa subtilisina/kexina tipo 9 (pcsk9), método de tratamiento, uso y su preparación
US20230089867A1 (en) 2018-11-27 2023-03-23 Novartis Ag Cyclic pentamer compounds as proprotein convertase subtilisin/kexin type 9 (pcsk9) inhibitors for the treatment of metabolic disorder
CN113166204B (zh) 2018-11-27 2025-01-28 诺华股份有限公司 作为治疗代谢障碍的蛋白质原转换酶枯草杆菌蛋白酶/kexin 9型(PCSK9)抑制剂的环状肽
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AU2011331294A1 (en) 2013-05-02
AU2011331294B2 (en) 2015-11-05
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MX2013005533A (es) 2013-07-03
AR083873A1 (es) 2013-03-27
UY33731A (es) 2012-06-29
BR112013011580A2 (pt) 2016-08-09
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US8673974B2 (en) 2014-03-18
US20120122977A1 (en) 2012-05-17
JP5872575B2 (ja) 2016-03-01
TW201305089A (zh) 2013-02-01
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KR101951492B1 (ko) 2019-02-22
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