EP 3386945 A1 20181017 - SOLID FORMS OF (2R,4S)-5-(BIPHENYL-4-YL)-4-[(3-CARBOXYPROPIONYL)AMINO]-2- -METHYLPENTANOIC ACID ETHYL ESTER, ITS SALTS AND A PREPARATION METHOD
Title (en)
SOLID FORMS OF (2R,4S)-5-(BIPHENYL-4-YL)-4-[(3-CARBOXYPROPIONYL)AMINO]-2- -METHYLPENTANOIC ACID ETHYL ESTER, ITS SALTS AND A PREPARATION METHOD
Title (de)
FESTE FORMEN VON (2R,4S)-5-(BIPHENYL-4-YL)-4-[(3-CARBOXYPROPIONYL)AMINO]-2-METHYLPENTANSÄUREETHYLESTER, DESSEN SALZE UND HERSTELLUNGSVERFAHREN
Title (fr)
FORMES SOLIDES D'ESTER ÉTHYLIQUE D'ACIDE (2R,4S)-5-(BIPHÉNYL-4-YL)-4-[(3-CARBOXYPROPIONYL)AMINO]-2-MÉTHYLPENTANOÏQUE, SES SELS ET SON PROCÉDÉ DE PRÉPARATION
Publication
Application
Priority
- CZ 2015891 A 20151211
- CZ 2015896 A 20151214
- CZ 2016000130 W 20161212
Abstract (en)
[origin: WO2017097275A1] The invention relates to solid forms of the free acid of sacubitril of formula 1, especially a crystalline form, incl. a method of removing chemical impurities from the crude free acid of sacubitril that is characterized in the use of well crystallizing salts of sacubitril with the amines of formula 9, where R1, R2, R3 independently stand for hydrogen or a C1-C7 alkyl, preferably the salt with cyclohexylamine, tert-butylamine or iso-propylamine. The invention further relates to a novel solid, crystalline form of sacubitril (8) - hemisolvate of the potassium salt of sacubitril, incl. a direct and highly efficient and industrially usable preparation methods of a solid form of sacubitril free acid and its pharmaceutically applicable salts, especially the crystalline sodium salt of formula 5, calcium salt of sacubitril of formula 6 and hemisolvate of the potassium salt of sacubitril of formula 8.
IPC 8 full level
C07C 233/47 (2006.01); A61K 31/216 (2006.01)
CPC (source: EP)
A61K 31/216 (2013.01); C07C 233/47 (2013.01); C07B 2200/13 (2013.01)
Citation (search report)
See references of WO 2017097275A1
Designated contracting state (EPC)
AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
Designated extension state (EPC)
BA ME
DOCDB simple family (publication)
WO 2017097275 A1 20170615; BR 112018011788 A2 20181204; CO 2018005941 A2 20180710; EP 3386945 A1 20181017; MX 2018007129 A 20181109; ZA 201803749 B 20190424
DOCDB simple family (application)
CZ 2016000130 W 20161212; BR 112018011788 A 20161212; CO 2018005941 A 20180612; EP 16818971 A 20161212; MX 2018007129 A 20161212; ZA 201803749 A 20180606