BR112018011788A2 - formas sólidas de éster etílico de ácido (2r,4s)-5-(bifenil-4-il)-4-[(3-carboxipropionil)amino]-2-metil-pentanoico, seus sais e um método de preparação - Google Patents

formas sólidas de éster etílico de ácido (2r,4s)-5-(bifenil-4-il)-4-[(3-carboxipropionil)amino]-2-metil-pentanoico, seus sais e um método de preparação

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Publication number
BR112018011788A2
BR112018011788A2 BR112018011788A BR112018011788A BR112018011788A2 BR 112018011788 A2 BR112018011788 A2 BR 112018011788A2 BR 112018011788 A BR112018011788 A BR 112018011788A BR 112018011788 A BR112018011788 A BR 112018011788A BR 112018011788 A2 BR112018011788 A2 BR 112018011788A2
Authority
BR
Brazil
Prior art keywords
sacubitrile
formula
salts
salt
acid
Prior art date
Application number
BR112018011788A
Other languages
English (en)
Inventor
Halama Ales
Ondrej Dammer
Lenka Dvorakova
Stach Jan
Krejcik Lukas
Rezankova Marketa
Voslar Michal
Zapadlo Michal
Zvatora Pavel
Vyslouzil Rostislav
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=BR112018011788(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 BR112018011788A2 publication Critical patent/BR112018011788A2/pt

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

Abstract

a invenção se refere a formas sólidas do ácido livre de sacubitril da fórmula 1, especialmente, uma forma cristalina, incluindo um método de remoção de impurezas químicas do ácido livre bruto de sacubitril que é caracterizado pelo uso de sais de sacubitril com boa cristalização com as aminas da fórmula 9, em que r1, r2, r3 representam independentemente hidrogênio ou uma c1-c7 alquila, de preferência, o sal com ciclo-hexilamina, terc-butilamina ou iso-propilamina. a invenção se refere adicionalmente a uma forma cristalina sólida inovadora de sacubitril (8) - hemissolvato do sal de potássio de sacubitril, incluindo métodos de preparação direta e altamente eficientes e industrialmente úteis de uma forma sólida de ácido de sacubitril livre e seus sais farmaceuticamente aplicáveis, especialmente o sal cristalino de sódio da fórmula 5, o sal de cálcio de sacubitril da fórmula 6 e o hemissolvato do sal de potássio de sacubitril da fórmula 8.
BR112018011788A 2015-12-11 2016-12-12 formas sólidas de éster etílico de ácido (2r,4s)-5-(bifenil-4-il)-4-[(3-carboxipropionil)amino]-2-metil-pentanoico, seus sais e um método de preparação BR112018011788A2 (pt)

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
BR112018011788A2 true BR112018011788A2 (pt) 2018-12-04

Family

ID=57614098

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112018011788A BR112018011788A2 (pt) 2015-12-11 2016-12-12 formas sólidas de éster etílico de ácido (2r,4s)-5-(bifenil-4-il)-4-[(3-carboxipropionil)amino]-2-metil-pentanoico, seus sais e um método de preparação

Country Status (6)

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

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US10683260B2 (en) * 2016-09-07 2020-06-16 Nanjing Noratech Pharmaceuticals Co., Ltd. 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
RU2019115782A (ru) 2016-10-28 2020-11-30 Биокон Лимитед Аморфный тринатрий сакубитрил вальсартан и способ его получения
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
PL3658122T3 (pl) * 2017-07-28 2021-10-18 Synthon B.V. Kompozycja farmaceutyczna zawierająca sakubitryl i walsartan
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
CN108530371B (zh) * 2017-12-27 2020-09-01 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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CA2472399C (en) 2002-01-17 2012-02-21 Novartis Ag Pharmaceutical compositions comprising valsartan and nep inhibitors
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Also Published As

Publication number Publication date
MX2018007129A (es) 2018-11-09
WO2017097275A1 (en) 2017-06-15
CO2018005941A2 (es) 2018-07-10
EP3386945A1 (en) 2018-10-17
ZA201803749B (en) 2019-04-24

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Legal Events

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B11A Dismissal acc. art.33 of ipl - examination not requested within 36 months of filing
B11Y Definitive dismissal acc. article 33 of ipl - extension of time limit for request of examination expired