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 preparaçãoInfo
- 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
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.
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) |
Families Citing this family (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2018045505A1 (zh) * | 2016-09-07 | 2018-03-15 | 诺瑞特国际药业股份有限公司 | 沙库比曲钠盐新晶型 |
EP3522886A4 (en) | 2016-10-10 | 2020-02-19 | Laurus Labs Limited | STABLE AMORPHE FORM OF THE SACUBITRIL VALSARTAN TRINATRIUM COMPLEX AND METHOD FOR THE PRODUCTION 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)
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 |
CA2472399C (en) | 2002-01-17 | 2012-02-21 | Novartis Ag | Pharmaceutical compositions comprising valsartan and nep inhibitors |
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 |
MX2009007474A (es) | 2007-01-12 | 2009-10-08 | Novartis Ag | Proceso para la preparacion de acido 5-bifenil-4-amino-2-metil pentanoico. |
AR070176A1 (es) | 2008-01-17 | 2010-03-17 | Novartis Ag | Procesos de sintesis de inhibidores de nep, compuestos intermediarios y uso de los mismos en la sintesis |
CN104262228B (zh) | 2010-01-22 | 2017-01-18 | 诺华股份有限公司 | 中性内肽酶抑制剂中间体和其制备方法 |
KR101476937B1 (ko) | 2010-08-23 | 2014-12-24 | 노파르티스 아게 | Nep 억제제의 제조를 위한 중간체의 제조 방법 |
JP6002133B2 (ja) | 2010-08-23 | 2016-10-05 | ノバルティス アーゲー | Nep阻害剤の製造に有用な中間体の新規調製方法 |
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 |
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 |
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 |
PL3218351T3 (pl) * | 2014-11-14 | 2019-12-31 | Zentiva K.S. | Sposób wytwarzania, wyodrębniania i oczyszczania farmaceutycznie dopuszczalnych postaci 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 |
-
2016
- 2016-12-12 MX MX2018007129A patent/MX2018007129A/es unknown
- 2016-12-12 BR BR112018011788A patent/BR112018011788A2/pt not_active Application Discontinuation
- 2016-12-12 WO PCT/CZ2016/000130 patent/WO2017097275A1/en active Application Filing
- 2016-12-12 EP EP16818971.0A patent/EP3386945A1/en not_active Withdrawn
-
2018
- 2018-06-06 ZA ZA2018/03749A patent/ZA201803749B/en unknown
- 2018-06-12 CO CONC2018/0005941A patent/CO2018005941A2/es unknown
Also Published As
Publication number | Publication date |
---|---|
MX2018007129A (es) | 2018-11-09 |
WO2017097275A1 (en) | 2017-06-15 |
EP3386945A1 (en) | 2018-10-17 |
CO2018005941A2 (es) | 2018-07-10 |
ZA201803749B (en) | 2019-04-24 |
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