Amorphous trisodium sacubitril valsartan and process for its preparation

Patent metadata

Field	Value
Publication number	US-2021122708-A1
Application number	US-202017090033-A
Country	US
Kind code	A1
Filing date	Nov 5, 2020
Priority date	Oct 28, 2016
Publication date	Apr 29, 2021
Grant date	—

Abstract

The present invention provides for crystalline Form B1 of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenyl-methyl)-4-amino-2R-methyl butanoic acid ethyl ester sodium salt, crystalline Form B2 of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-2R-methyl butanoic acid ethyl ester sodium salt, a novel process for the preparation of crystalline Form B of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-2R-methyl butanoic acid ethyl ester sodium salt. The present invention also provides for crystalline Form B of (S)—N-(1-Carboxy-2-Methyl-Prop-1-yl)-N-Pentanoyl-N-[2′-(1H-Tetrazol-5-yl)-Biphenyl-4-yl-Methyl]-Amine disodium salt, crystalline Form P of (S)—N-(1-Carboxy-2-Methyl-Prop-1-yl)-N-Pentanoyl-N-[2′-(1H-Tetrazol-5-yl)-Biphenyl-4-yl-Methyl]-Amine disodium salt and processes for their preparation thereof. The present invention further provides an industrial method production of Amorphous Form of Sacubitril valsartan trisodium. The present invention also provides for amorphous solid dispersions of Sacubitril valsartan trisodium with excipients.

First claim

1 - 20 . (canceled)

21 . A process for the preparation of crystalline form B of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-2R-methyl butanoic acid ethyl ester sodium salt, the process comprising:
a) treating N-(3-carb oxyl-1-oxopropyl)-(4 S)-(p-phenylphenylmethyl)-4-amino-2R-methyl butanoic acid ethyl ester (sacubitril) with a sodium source; b) heating the reaction mass and azeotropic removal of water from the reaction mixture; c) isolating the crystalline form B of N-(3-carb oxyl-1-oxopropyl)-(4 S)-(p-phenylphenylmethyl)-4-amino-2R-methyl butanoic acid ethyl ester sodium salt.

22 . The process according to claim 22 , wherein the sodium source is selected from sodium hydroxide, sodium carbonate, sodium bicarbonate, sodium methoxide, and sodium ethoxide.

Assignees

• Biocon Ltd

Inventors

• Charyulu Palle Venkata Raghavendra
• Patel Pratik Rameshchandr
• Venu Thirunelimada Devaiah
• Vidyasagar Reddy Avathu
• Shanmughasamy Rajmahendra

Classifications

• C07B2200/13

  Crystalline forms, e.g. polymorphs · CPC title

• A61K31/216

  of acids having aromatic rings, e.g. benactizyne, clofibrate · CPC title

• C07D257/04 Primary

  Five-membered rings · CPC title

• C07C233/51

  having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings · CPC title

• A61K2300/00

  Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00 · CPC title