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)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
EA202090398A1 (ru) * 2017-07-28 2020-05-15 Синтон Б.В. Фармацевтическая композиция, включающая сакубитрил и валсартан
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

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5217996A (en) * 1992-01-22 1993-06-08 Ciba-Geigy Corporation Biaryl substituted 4-amino-butyric acid amides
BRPI0306907B8 (pt) 2002-01-17 2021-05-25 Novartis Ag composição farmacêutica, que compreende valsartan e inibidor de nep ou seus sais
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
AR057882A1 (es) 2005-11-09 2007-12-26 Novartis Ag Compuestos de accion doble de bloqueadores del receptor de angiotensina e inhibidores de endopeptidasa neutra
EP1903027A1 (en) 2006-09-13 2008-03-26 Novartis AG Process for preparing biaryl substituted 4-amino-butyric acid or derivatives thereof and their use in the production of NEP inhibitors
AR064842A1 (es) 2007-01-12 2009-04-29 Mazzucco Gavieiro Maria Belen Pirrolidin-2-onas, y su uso en la preparacion de inhibidores de nep
PE20091364A1 (es) 2008-01-17 2009-10-13 Novartis Ag Proceso para la preparacion de inhibidores de nep
RU2564024C2 (ru) 2010-01-22 2015-09-27 Новартис Аг Промежуточные продукты для получения ингибиторов нейтральной эндопептидазы и способ их получения
KR101476937B1 (ko) 2010-08-23 2014-12-24 노파르티스 아게 Ｎｅｐ 억제제의 제조를 위한 중간체의 제조 방법
BR112013004179A2 (pt) 2010-08-23 2016-05-10 Novartis Ag processo para a preparação de intermediários úteis para a fabricação de inibidores de nep
AR092278A1 (es) 2012-08-31 2015-04-08 Novartis Ag Proceso de obtencion de derivados n-acilicos de bifenil-alanina e intermediarios relacionados
US20160206597A1 (en) 2013-08-26 2016-07-21 Toni Lynne Bransford New Use
CN105622452A (zh) * 2014-08-27 2016-06-01 上海翰森生物医药科技有限公司 Ahu-377结晶型游离酸及其制备方法和应用
WO2016029828A1 (zh) * 2014-08-27 2016-03-03 上海翰森生物医药科技有限公司 AHU-377结晶型游离酸、半钙盐、α﹣苯乙胺盐及其制备方法和应用
CN105461587A (zh) * 2014-08-27 2016-04-06 上海翰森生物医药科技有限公司 Ahu-377半钙盐晶型及其制备方法和应用
WO2016074651A1 (en) * 2014-11-14 2016-05-19 Zentiva, K.S. A method for the preparation, isolation and purification of pharmaceutically applicable forms of ahu-377
CN105837464A (zh) * 2015-01-15 2016-08-10 四川海思科制药有限公司 沙库比曲钠的晶型及其制备方法和用途

Also Published As

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

Similar Documents

Publication Publication Date Title
CO2018005941A2 (es) 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
EA201992601A1 (ru) Конденсированное имидазопиперидиновое соединение, являющееся ингибитором jak
AR110381A2 (es) Inhibidores biarilo de tirosina cinasa de bruton
AR111304A1 (es) Métodos para sintetizar un inhibidor de mcl-1
PE20200604A1 (es) Derivados de indolina sustituidos como inhibidores de la replicacion virica de dengue
AR106141A1 (es) Métodos e intermediarios para la preparación de derivados de ácidos biliares
EA201890899A1 (ru) Модуляторы фарнезоидного x-рецептора
AR107547A1 (es) Maleato de agonista de tlr7, sus formas cristalinas c, d y e, sus procesos de preparación y su uso
GT201000211A (es) Procesos e intermediarios para la preparación de derivados de acido 5-bifenil-a-il-2-metilpentanoico
CU24671B1 (es) Compuesto de pirimidina inhibidor de las janocinasas, composición, forma cristalina y proceso de preparación
PE20142081A1 (es) Inhibidores de quinurenina-3-monooxigenasa, composiciones farmaceuticas y metodo de uso de los mismos
CO2018000795A2 (es) Método para preparar derivados de ácido 3-(2-anilino-1-ciclohexil-1h-bencimidazol-5-il)propanoico sustituido
AR111469A1 (es) Sal de un compuesto del derivado de aminopiridina, una forma cristalina de la misma, y un proceso para preparar la misma
PE20191103A1 (es) Inhibidores de dopamina-b-hidroxilasa
PE20171119A1 (es) Compuestos de dihidropirimidin-2-ona y sus usos medicos
AR081819A1 (es) Derivados de pirimidil-piperidinil-oxipiridinona, composiciones farmaceuticas que los contienen y uso de los mismos para tratar diabetes, dislipemias, obesidad y otras enfermedades
AU2015306910A8 (en) Crystallization process of aripiprazole derivatives in extended release formulations for treatment of schizophrenia
CL2016001927A1 (es) Formas solidas de 2-(ter-butilamino)-4-((1r,3r,4r)-3-hidroxi-4-metilciclohexilamino)pirimidin-5-carboxamida, composiciones de la misma y métodos para su uso.
PE20170212A1 (es) Composicion reactiva basada en bicarbonato de sodio y procedimiento para su produccion
PH12017501397A1 (en) (2s, 4r)-5-(5`-chloro-2`-fluorobiphenyl-4-yl)-4-(ethoxyoxalylamino)-2-hydroxymethyl-2-methylpentanoic acid as neprilysin inhibitor
BR112017018580A2 (pt) p-toluenossulfonato para inibidor de mek quinase, e forma cristalina do mesmo e método de preparação para tal
CO2021009309A2 (es) Formas de sal y cristalinas de un compuesto orgánico y composiciones farmacéuticas del mismo
BR112017012926A2 (pt) precursores de ácido n-acético de alanina, processo de preparação de precursores, uso de precursores, e processo de hidrólise dos precursores
EA201690467A1 (ru) Промышленный способ синтеза улипристала ацетата и его 4'-ацетильного аналога
AR077429A1 (es) Compuestos hidroxiasenapina sus derivados y composiciones farmaceuticas que comprenden los mismos