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CO2018005941A2 - Formas sólidas de éster etílico del ácido (2r,4s)-5-(bifenil-4-il)-4-[(3-carboxipropionil)amino]-2-metil-pentanoico, sus sales y un método de preparación - Google Patents

Formas sólidas de éster etílico del ácido (2r,4s)-5-(bifenil-4-il)-4-[(3-carboxipropionil)amino]-2-metil-pentanoico, sus sales y un método de preparación

Info

Publication number
CO2018005941A2
CO2018005941A2 CONC2018/0005941A CO2018005941A CO2018005941A2 CO 2018005941 A2 CO2018005941 A2 CO 2018005941A2 CO 2018005941 A CO2018005941 A CO 2018005941A CO 2018005941 A2 CO2018005941 A2 CO 2018005941A2
Authority
CO
Colombia
Prior art keywords
sacubitrile
formula
salts
salt
preparation
Prior art date
Application number
CONC2018/0005941A
Other languages
English (en)
Inventor
Ales Halama
Pavel Zvatora
Michal Voslar
Jan Stach
Michal Zapadlo
Ondrej Dammer
Lukas Krejcik
Lenka Dvorakova
Marketa Rezankova
Rostislav Vyslouzil
Original Assignee
Zentiva Ks
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=57614098&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CO2018005941(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from CZ2015-891A external-priority patent/CZ2015891A3/cs
Priority claimed from CZ2015-896A external-priority patent/CZ2015896A3/cs
Application filed by Zentiva Ks filed Critical Zentiva Ks
Publication of CO2018005941A2 publication Critical patent/CO2018005941A2/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/45—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/46—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/47—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
    • 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
    • A61K31/21—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Emergency Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La invención se refiere a formas sólidas del ácido libre de sacubitrilo de fórmula 1, especialmente una forma cristalina, incl. un método para eliminar impurezas químicas del ácido libre en bruto de sacubitrilo que se caracteriza por el uso de sales de sacubitrilo que cristalizan bien con las aminas de fórmula 9, donde R1, R2, R3 representan independientemente hidrógeno o un alquilo C1-C7, preferiblemente la sal con ciclohexilamina, terc-butilamina o iso-propilamina. La invención también se refiere a un sólido novedoso, forma cristalina de sacubitrilo (8) - hemisolvato de la sal de potasio de sacubitrilo, incl. métodos de preparación directos, altamente eficaces e industrialmente útiles de una forma sólida de ácido libre de sacubitrilo y sus sales farmacéuticamente aplicables, especialmente la sal de sodio cristalina de fórmula 5, sal de calcio de sacubitrilo de fórmula 6 y el hemisolvato de la sal de potasio de sacubitrilo de fórmula 8.
CONC2018/0005941A 2015-12-11 2018-06-12 Formas sólidas de éster etílico del ácido (2r,4s)-5-(bifenil-4-il)-4-[(3-carboxipropionil)amino]-2-metil-pentanoico, sus sales y un método de preparación CO2018005941A2 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CZ2015-891A CZ2015891A3 (cs) 2015-12-11 2015-12-11 Krystalická forma draselné soli ethylesteru (2R,4S)-5-(bifenyl-4-yl)-4-[(3-karboxypropionyl)amino]-2-methylpentanové kyseliny a průmyslově použitelný způsob její přípravy
CZ2015-896A CZ2015896A3 (cs) 2015-12-14 2015-12-14 Pevné formy ethyl esteru (2R,4S)-5-(bifenyl-4-yl)-4-[3-karboxypropionyl)amino]-2--methylpentanové kyseliny, její sole a způsob přípravy
PCT/CZ2016/000130 WO2017097275A1 (en) 2015-12-11 2016-12-12 Solid forms of (2r,4s)-5-(biphenyl-4-yl)-4-[(3-carboxypropionyl)amino]-2- -methylpentanoic acid ethyl ester, its salts and a preparation method

Publications (1)

Publication Number Publication Date
CO2018005941A2 true CO2018005941A2 (es) 2018-07-10

Family

ID=57614098

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2018/0005941A CO2018005941A2 (es) 2015-12-11 2018-06-12 Formas sólidas de éster etílico del ácido (2r,4s)-5-(bifenil-4-il)-4-[(3-carboxipropionil)amino]-2-metil-pentanoico, sus sales y un método de preparación

Country Status (6)

Country Link
EP (1) EP3386945A1 (es)
BR (1) BR112018011788A2 (es)
CO (1) CO2018005941A2 (es)
MX (1) MX2018007129A (es)
WO (1) WO2017097275A1 (es)
ZA (1) ZA201803749B (es)

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EP3511317A4 (en) * 2016-09-07 2020-04-15 Noratech Pharmaceuticals, Inc. New crystalline form of sacubitril sodium salt
US10857132B2 (en) 2016-10-10 2020-12-08 Laurus Labs Limited Stable amorphous form of sacubitril valsartan trisodium complex and processes for preparation thereof
BR112019008581A2 (pt) 2016-10-28 2019-09-17 Biocon Ltd sacubitril valsartana trissódica amorfa e processo para sua preparação
CN107311909A (zh) * 2017-06-22 2017-11-03 东南大学 一种lcz696杂质对照品的制备方法
MX391562B (es) * 2017-07-28 2025-03-21 Synthon Bv Composicion farmaceutica que comprende sacubitril y valsartan
CN109400493B (zh) * 2017-08-15 2021-07-09 成都博腾药业有限公司 沙库比曲及其中间体的制备方法
CN107602410A (zh) * 2017-09-13 2018-01-19 浙江三门恒康制药有限公司 沙库比曲钠盐的晶型ii及其制备方法
WO2019127994A1 (zh) * 2017-12-27 2019-07-04 浙江天宇药业股份有限公司 一种沙库比曲钠盐、沙库比曲游离酸与乙酸的共晶物、其晶型、晶型的制备方法及用途
CN108558693A (zh) * 2018-04-24 2018-09-21 南京双科医药开发有限公司 一种沙库巴曲游离酸及其金属盐在药物制备中应用的方法
GB201810326D0 (en) * 2018-06-22 2018-08-08 Johnson Matthey Plc Crystalline form of sacubitril, its preparation and use
CN109912486B (zh) * 2019-04-25 2022-09-27 东北制药集团股份有限公司 一种联苯甲基内酰胺化合物的制备方法
CN110878039A (zh) * 2019-12-18 2020-03-13 株洲千金药业股份有限公司 一种沙库巴曲缬沙坦钠杂质的制备方法
CN115677521B (zh) * 2022-11-16 2024-02-02 迪嘉药业集团股份有限公司 一种高纯度沙库巴曲钙的制备方法

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WO2007045663A2 (en) 2005-10-19 2007-04-26 Novartis Ag Combination of an ati receptor antagonist and a np inhibitor fro treating ia hypertension and heartfailure
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Also Published As

Publication number Publication date
WO2017097275A1 (en) 2017-06-15
ZA201803749B (en) 2019-04-24
BR112018011788A2 (pt) 2018-12-04
MX2018007129A (es) 2018-11-09
EP3386945A1 (en) 2018-10-17

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