CZ2015896A3 - The solid forms of the ethyl ester of (2R,4S)-5-(biphenyl-4-yl)-4-[3-carboxy-propionyl)amino]-2—methylpentanoic acid, its salts and the method of its preparation - Google Patents

The solid forms of the ethyl ester of (2R,4S)-5-(biphenyl-4-yl)-4-[3-carboxy-propionyl)amino]-2—methylpentanoic acid, its salts and the method of its preparation Download PDF

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Publication number
CZ2015896A3
CZ2015896A3 CZ2015-896A CZ2015896A CZ2015896A3 CZ 2015896 A3 CZ2015896 A3 CZ 2015896A3 CZ 2015896 A CZ2015896 A CZ 2015896A CZ 2015896 A3 CZ2015896 A3 CZ 2015896A3
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CZ
Czechia
Prior art keywords
sacubitrile
salts
preparation
solid forms
propionyl
Prior art date
Application number
CZ2015-896A
Other languages
Czech (cs)
Inventor
Aleš Halama
Pavel Žvátora
Michal Voslař
Jan Stach
Michal Zapadlo
Ondřej Dammer
Lukáš Krejčík
Original Assignee
Zentiva, K.S.
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.)
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Publication date
Application filed by Zentiva, K.S. filed Critical Zentiva, K.S.
Priority to CZ2015-896A priority Critical patent/CZ2015896A3/en
Priority to PCT/CZ2016/000130 priority patent/WO2017097275A1/en
Priority to EP16818971.0A priority patent/EP3386945A1/en
Priority to MX2018007129A priority patent/MX2018007129A/en
Priority to BR112018011788A priority patent/BR112018011788A2/en
Publication of CZ2015896A3 publication Critical patent/CZ2015896A3/en
Priority to ZA2018/03749A priority patent/ZA201803749B/en
Priority to CONC2018/0005941A priority patent/CO2018005941A2/en

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Abstract

Předmětem řešení jsou pevné formy volné kyseliny sacubitrilu vzorce I, zejména forma krystalická, včetně způsobu odstranění chemických nečistot ze surové volné kyseliny sacubitrilu, který se vyznačuje použitím dobře krystalujících solí sacubitrilu s aminy vzorce 9, kde R.sub.1.n., R.sub.2.n., R.sub.3.n.nezávisle na sobě značí vodík nebo alkyl C1-C7, s výhodou sůl s cyklohexylaminem, tert.butylaminem nebo iso-propylaminem. Řešení se dále týká vysoce efektivních a průmyslově využitelných způsobu přípravy pevné formy volné kyseliny sacubitrilu a jejích farmaceuticky využitelných solí, zejména krystalické sodné vzorce 5 a vápenaté soli sacubitrilu vzorce 6.The subject matter of the invention is the solid forms of the free acid of the sacubitrile of the formula I, in particular the crystalline form, including the method of removing chemical impurities from the crude free acid of the sacubitrile, characterized by the use of the well crystallizing salts of the sacubitrile with amines of the formula 9, independently of one another is hydrogen or C1-C7 alkyl, preferably a salt with cyclohexylamine, tert-butylamine or isopropylamine. The invention further relates to highly efficient and industrially useful processes for the preparation of the solid form of the free acid of sacubitrile and its pharmaceutically usable salts, in particular the crystalline sodium 5 and the calcium salt of the sacubitrile of formula 6.

CZ2015-896A 2015-12-11 2015-12-14 The solid forms of the ethyl ester of (2R,4S)-5-(biphenyl-4-yl)-4-[3-carboxy-propionyl)amino]-2—methylpentanoic acid, its salts and the method of its preparation CZ2015896A3 (en)

Priority Applications (7)

Application Number Priority Date Filing Date Title
CZ2015-896A CZ2015896A3 (en) 2015-12-14 2015-12-14 The solid forms of the ethyl ester of (2R,4S)-5-(biphenyl-4-yl)-4-[3-carboxy-propionyl)amino]-2—methylpentanoic acid, its salts and the method of its preparation
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
EP16818971.0A EP3386945A1 (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
MX2018007129A MX2018007129A (en) 2015-12-11 2016-12-12 Solid forms of (2r,4s)-5-(biphenyl-4-yl)-4-[(3-carboxypropionyl)a mino]-2- -methylpentanoic acid ethyl ester, its salts and a preparation method.
BR112018011788A BR112018011788A2 (en) 2015-12-11 2016-12-12 (2r, 4s) -5- (biphenyl-4-yl) -4 - [(3-carboxypropionyl) amino] -2-methylpentanoic acid ethyl ester solid forms, their salts and a preparation method
ZA2018/03749A ZA201803749B (en) 2015-12-11 2018-06-06 Solid forms of (2r,4s)-5-(biphenyl-4-yl)-4-[(3-carboxypropionyl)amino]-2- -methylpentanoic acid ethyl ester, its salts and a preparation method
CONC2018/0005941A CO2018005941A2 (en) 2015-12-11 2018-06-12 Solid forms of (2r, 4s) -5- (biphenyl-4-yl) -4 - [(3-carboxypropionyl) amino] -2-methyl-pentanoic acid ethyl ester, its salts and a preparation method

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CZ2015-896A CZ2015896A3 (en) 2015-12-14 2015-12-14 The solid forms of the ethyl ester of (2R,4S)-5-(biphenyl-4-yl)-4-[3-carboxy-propionyl)amino]-2—methylpentanoic acid, its salts and the method of its preparation

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CZ2015896A3 true CZ2015896A3 (en) 2017-06-21

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CZ2015-896A CZ2015896A3 (en) 2015-12-11 2015-12-14 The solid forms of the ethyl ester of (2R,4S)-5-(biphenyl-4-yl)-4-[3-carboxy-propionyl)amino]-2—methylpentanoic acid, its salts and the method of its preparation

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3766484A1 (en) 2019-07-19 2021-01-20 Zentiva, K.S. Solid pharmaceutical dosage form comprising valsartan and sacubitril

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3766484A1 (en) 2019-07-19 2021-01-20 Zentiva, K.S. Solid pharmaceutical dosage form comprising valsartan and sacubitril

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