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CN106458857A - 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 - Google Patents

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 Download PDF

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Publication number
CN106458857A
CN106458857A CN201580025325.8A CN201580025325A CN106458857A CN 106458857 A CN106458857 A CN 106458857A CN 201580025325 A CN201580025325 A CN 201580025325A CN 106458857 A CN106458857 A CN 106458857A
Authority
CN
China
Prior art keywords
ahu
salt
calcium
crystal
phenylethylamine
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CN201580025325.8A
Other languages
English (en)
Inventor
李响
龚素娟
吕爱锋
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Lianyungang Hongchuang Pharmaceutical Co ltd
Shanghai Hansoh Biomedical Co Ltd
Original Assignee
Lianyungang Hongchuang Pharmaceutical Co ltd
Shanghai Hansoh Biomedical Co Ltd
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
Priority claimed from CN201410427542.7A external-priority patent/CN105367438A/zh
Priority claimed from CN201410426985.4A external-priority patent/CN105622452A/zh
Priority claimed from CN201410425633.7A external-priority patent/CN105461587A/zh
Application filed by Lianyungang Hongchuang Pharmaceutical Co ltd, Shanghai Hansoh Biomedical Co Ltd filed Critical Lianyungang Hongchuang Pharmaceutical Co ltd
Publication of CN106458857A publication Critical patent/CN106458857A/zh
Pending legal-status Critical Current

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Classifications

    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • 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
    • C07C233/51—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 an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings

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

Abstract

公开了一种NEP抑制剂AHU‑377的结晶形式，其中包括结晶型游离酸、半钙盐、α‑苯乙胺盐及其制备方法和应用。改善了AHU‑377理化性质，工艺成熟，可操作性强，所得产品质量高且均一稳定，提高了化学稳定性，利于储存。

Description

PCT国内申请，说明书已公开。

Claims (35)

  1. PCT国内申请，权利要求书已公开。
CN201580025325.8A 2014-08-27 2015-08-24 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 Pending CN106458857A (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
CN201410427542.7A CN105367438A (zh) 2014-08-27 2014-08-27 AHU-377α-苯乙胺盐多晶型及其制备方法和应用
CN2014104256337 2014-08-27
CN2014104269854 2014-08-27
CN201410426985.4A CN105622452A (zh) 2014-08-27 2014-08-27 Ahu-377结晶型游离酸及其制备方法和应用
CN2014104275427 2014-08-27
CN201410425633.7A CN105461587A (zh) 2014-08-27 2014-08-27 Ahu-377半钙盐晶型及其制备方法和应用
PCT/CN2015/087904 WO2016029828A1 (zh) 2014-08-27 2015-08-24 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

Publications (1)

Publication Number Publication Date
CN106458857A true CN106458857A (zh) 2017-02-22

Family

ID=55398756

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201580025325.8A Pending CN106458857A (zh) 2014-08-27 2015-08-24 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

Country Status (3)

Country Link
CN (1) CN106458857A (zh)
TW (1) TWI718104B (zh)
WO (1) WO2016029828A1 (zh)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110133149A (zh) * 2019-05-31 2019-08-16 重庆三圣实业股份有限公司 一种分离测定lcz696及其杂质的方法
CN115000304A (zh) * 2022-04-29 2022-09-02 中国科学院合肥物质科学研究院 一种基于钙钛矿晶圆的直接型x射线探测器及其制备方法
CN115461052A (zh) * 2020-11-25 2022-12-09 深圳信立泰药业股份有限公司 Arb代谢产物与nep抑制剂的复合物预防和/或治疗肾病的药物用途

Families Citing this family (7)

* Cited by examiner, † Cited by third party
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WO2016135751A1 (en) * 2015-02-25 2016-09-01 Mylan Laboratories Limited Novel process for the preparation of sacubitril and its intermediates
MX2017012110A (es) * 2015-03-20 2018-02-19 Crystal Pharmatech Co Ltd Forma cristalina de ahu377, metodo de preparacion y uso de la misma.
US11786498B2 (en) 2015-07-02 2023-10-17 Novartis Ag Sacubitril calcium salts
WO2017009784A1 (en) 2015-07-14 2017-01-19 Cadila Healthcare Limited Solid state forms of trisodium salt of valsartan/sacubitril complex and sacubitril
EP3386945A1 (en) * 2015-12-11 2018-10-17 Zentiva, K.S. Solid forms of (2r,4s)-5-(biphenyl-4-yl)-4-[(3-carboxypropionyl)amino]-2- -methylpentanoic acid ethyl ester, its salts and a preparation method
CN105753733B (zh) * 2016-04-15 2019-06-18 苏州晶云药物科技股份有限公司 Ahu377的晶型及其制备方法与用途
CN112730721A (zh) * 2020-12-29 2021-04-30 重庆三圣实业股份有限公司 一种分离测定沙库巴曲钙盐及其异构体的方法

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US5217996A (en) * 1992-01-22 1993-06-08 Ciba-Geigy Corporation Biaryl substituted 4-amino-butyric acid amides
CN101516931A (zh) * 2006-06-27 2009-08-26 尤尼威蒂恩技术有限责任公司 用于滚塑和注塑制品的以茂金属催化剂制备的聚合物
CN101516831A (zh) * 2006-09-13 2009-08-26 诺瓦提斯公司 用于制备联芳基取代的4-氨基-丁酸或其衍生物的方法以及其在制备nep抑制剂中的应用
CN105367438A (zh) * 2014-08-27 2016-03-02 上海翰森生物医药科技有限公司 AHU-377α-苯乙胺盐多晶型及其制备方法和应用
CN105431587A (zh) * 2013-07-19 2016-03-23 旭化成纤维株式会社 微细纤维素纤维片
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

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL162661A0 (en) * 2002-01-17 2005-11-20 Novartis Ag Pharmaceutical compositions comprising valsartan and nep inhibitors
TWI560172B (en) * 2011-11-02 2016-12-01 Theravance Biopharma R&D Ip Llc Neprilysin inhibitors

Patent Citations (6)

* 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
CN101516931A (zh) * 2006-06-27 2009-08-26 尤尼威蒂恩技术有限责任公司 用于滚塑和注塑制品的以茂金属催化剂制备的聚合物
CN101516831A (zh) * 2006-09-13 2009-08-26 诺瓦提斯公司 用于制备联芳基取代的4-氨基-丁酸或其衍生物的方法以及其在制备nep抑制剂中的应用
CN105431587A (zh) * 2013-07-19 2016-03-23 旭化成纤维株式会社 微细纤维素纤维片
CN105367438A (zh) * 2014-08-27 2016-03-02 上海翰森生物医药科技有限公司 AHU-377α-苯乙胺盐多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

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110133149A (zh) * 2019-05-31 2019-08-16 重庆三圣实业股份有限公司 一种分离测定lcz696及其杂质的方法
CN110133149B (zh) * 2019-05-31 2022-05-24 重庆三圣实业股份有限公司 一种分离测定lcz696及其杂质的方法
CN115461052A (zh) * 2020-11-25 2022-12-09 深圳信立泰药业股份有限公司 Arb代谢产物与nep抑制剂的复合物预防和/或治疗肾病的药物用途
CN115461052B (zh) * 2020-11-25 2023-12-22 深圳信立泰药业股份有限公司 Arb代谢产物与nep抑制剂的复合物预防和/或治疗肾病的药物用途
CN115000304A (zh) * 2022-04-29 2022-09-02 中国科学院合肥物质科学研究院 一种基于钙钛矿晶圆的直接型x射线探测器及其制备方法

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Publication number Publication date
TWI718104B (zh) 2021-02-11
TW201625520A (zh) 2016-07-16
WO2016029828A1 (zh) 2016-03-03

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Application publication date: 20170222