EA201390723A1 - Аминозамещенные производные бисфенилпентановой кислоты в качестве ингибиторов nep - Google Patents
Аминозамещенные производные бисфенилпентановой кислоты в качестве ингибиторов nepInfo
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/70—Carboxylic 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
- C07C235/72—Carboxylic 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
- C07C235/74—Carboxylic 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/70—Carboxylic 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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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
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- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
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- Health & Medical Sciences (AREA)
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- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
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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.
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
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
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) |
Families Citing this family (26)
Publication number | Priority date | Publication date | Assignee | Title |
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BRPI0815547B8 (pt) | 2007-08-17 | 2021-05-25 | Novartis Ag | composição farmacêutica compreendendo depsipeptídeos cíclicos, e seus usos |
BR112013014952A2 (pt) | 2010-12-15 | 2017-05-30 | Theravance Inc | inibidores de neprilisina |
PT2651896E (pt) | 2010-12-15 | 2015-11-03 | Theravance Biopharma R&D Ip Llc | Inibidores de neprilisina |
US8449890B2 (en) | 2011-02-17 | 2013-05-28 | Theravance, Inc. | Neprilysin inhibitors |
SG192815A1 (en) | 2011-02-17 | 2013-09-30 | Theravance Inc | Substituted aminobutyric derivatives as neprilysin inhibitors |
WO2012166389A1 (en) | 2011-05-31 | 2012-12-06 | Theravance, Inc. | Neprilysin inhibitors |
WO2012166387A1 (en) | 2011-05-31 | 2012-12-06 | Theravance, Inc. | Neprilysin inhibitors |
CA2835220A1 (en) | 2011-05-31 | 2012-12-06 | Theravance, Inc. | Neprilysin inhibitors |
TWI560172B (en) | 2011-11-02 | 2016-12-01 | Theravance Biopharma R&D Ip Llc | Neprilysin inhibitors |
WO2013181332A1 (en) | 2012-05-31 | 2013-12-05 | Theravance, Inc. | Nitric oxide donor neprilysin inhibitors |
JP6162229B2 (ja) | 2012-06-08 | 2017-07-12 | セラヴァンス バイオファーマ アール&ディー アイピー, エルエルシー | ネプリライシン阻害剤 |
SG10201703185VA (en) | 2012-06-08 | 2017-05-30 | Theravance Biopharma R&D Ip Llc | Neprilysin inhibitors |
CA2879697C (en) | 2012-08-08 | 2020-07-07 | Theravance Biopharma R&D Ip, Llc | Neprilysin inhibitors |
EP2964616B1 (en) | 2013-03-05 | 2017-05-03 | Theravance Biopharma R&D IP, LLC | Neprilysin inhibitors |
CA2934898A1 (en) | 2014-01-30 | 2015-08-06 | Theravance Biopharma R&D Ip, Llc | 5-biphenyl-4-heteroarylcarbonylamino-pentanoic acid derivatives as neprilysin inhibitors |
WO2015116786A1 (en) | 2014-01-30 | 2015-08-06 | Theravance Biopharma R&D Ip, Llc | Neprilysin inhibitors |
PH12017501029B1 (en) | 2014-12-24 | 2022-04-27 | Lg Chemical Ltd | Biaryl derivative as gpr120 agonist |
CN104557600B (zh) * | 2015-01-26 | 2016-05-04 | 苏州明锐医药科技有限公司 | 沙库比曲的制备方法 |
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 |
TW202333563A (zh) | 2021-11-12 | 2023-09-01 | 瑞士商諾華公司 | 用於治療疾病或障礙之二胺基環戊基吡啶衍生物 |
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-
2011
- 2011-11-11 US US13/294,262 patent/US8673974B2/en active Active
- 2011-11-14 KR KR1020137015361A patent/KR101951492B1/ko not_active Expired - Fee Related
- 2011-11-14 AU AU2011331294A patent/AU2011331294B2/en not_active Ceased
- 2011-11-14 AR ARP110104250A patent/AR083873A1/es not_active Application Discontinuation
- 2011-11-14 CN CN201180053783.4A patent/CN103201257B/zh not_active Expired - Fee Related
- 2011-11-14 MX MX2013005533A patent/MX2013005533A/es active IP Right Grant
- 2011-11-14 UY UY0001033731A patent/UY33731A/es not_active Application Discontinuation
- 2011-11-14 JP JP2013539219A patent/JP5872575B2/ja not_active Expired - Fee Related
- 2011-11-14 WO PCT/EP2011/070080 patent/WO2012065956A1/en active Application Filing
- 2011-11-14 CA CA2817114A patent/CA2817114A1/en not_active Abandoned
- 2011-11-14 BR BR112013011580A patent/BR112013011580A2/pt not_active Application Discontinuation
- 2011-11-14 EP EP11790902.8A patent/EP2640690A1/en not_active Withdrawn
- 2011-11-14 EA EA201390723A patent/EA021537B1/ru not_active IP Right Cessation
- 2011-11-15 TW TW100141702A patent/TW201305089A/zh unknown
Also Published As
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KR20130116288A (ko) | 2013-10-23 |
WO2012065956A1 (en) | 2012-05-24 |
CA2817114A1 (en) | 2012-05-24 |
JP2014501720A (ja) | 2014-01-23 |
AU2011331294A1 (en) | 2013-05-02 |
AU2011331294B2 (en) | 2015-11-05 |
CN103201257B (zh) | 2016-01-20 |
MX2013005533A (es) | 2013-07-03 |
AR083873A1 (es) | 2013-03-27 |
UY33731A (es) | 2012-06-29 |
BR112013011580A2 (pt) | 2016-08-09 |
EP2640690A1 (en) | 2013-09-25 |
US8673974B2 (en) | 2014-03-18 |
US20120122977A1 (en) | 2012-05-17 |
JP5872575B2 (ja) | 2016-03-01 |
TW201305089A (zh) | 2013-02-01 |
EA021537B1 (ru) | 2015-07-30 |
KR101951492B1 (ko) | 2019-02-22 |
CN103201257A (zh) | 2013-07-10 |
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