PROCESS FOR PREPARING (5S)-{[2-(4-CARBOXYPHENYL)ETHYL] |2-(2-{|3-CHLORO-4'-(TRIFLUOROMETHYL)BIPHENYL-4- YL]METHOXY}PHENYL)ETHYL]AMINOL-5,6,7,8-TETRAHYDROQUINOLINE-2-CARBOXYLIC ACID AND ITS CRYSTALLINE FORMS FOR USE AS PHARMACEUTICALLY ACTIVE COMPOUND

PROCESS FOR PREPARING (5S)-{[2-(4-CARBOXYPHENYL)ETHYL] |2-(2-{|3-CHLORO-4'-(TRIFLUOROMETHYL)BIPHENYL-4- YL]METHOXY}PHENYL)ETHYL]AMINOL-5,6,7,8-TETRAHYDROQUINOLINE-2-CARBOXYLIC ACID AND ITS CRYSTALLINE FORMS FOR USE AS PHARMACEUTICALLY ACTIVE COMPOUND

The present invention relates to a novel and improved process for preparing (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4'-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid of the formula (I) and to novel crystalline forms of it, which...

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Bibliographische Detailangaben
Hauptverfasser: OLENIK, Britta, KEIL, Birgit, FABER, Helene, EGGER, Julian, BECKER, Guido, FEY, Peter, RÖSLER, Bernd, BOTHE, Clemens, SCHIRMER, Heiko
Format: Patent
Sprache:eng ; fre
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Zusammenfassung:The present invention relates to a novel and improved process for preparing (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4'-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid of the formula (I) and to novel crystalline forms of it, which is i.a. the pseudopolymorphic form monohydrate I (I-M-I) or the pseudopolymorphic form monohydrate II (I-M-II), furthermore the present invention relates to a novel and selective crystallization process for preparation of the pseudopolymorphic form monohydrate I (I-M-I) or the pseudopolymorphic form monohydrate II (I-M-II), preferably monohydrate I of formula (I-M-I) and to pharmaceutical compositions comprising monohydrate I of formula (I-M-I) and to its use for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of pulmonary and cardiopulmonary and cardiovascular diseases. La présente invention concerne un nouveau procédé amélioré de préparation d'acide (5S)-{[2-(4-carboxyphényl)éthyl][2-(2-{[3-chloro-4'-(trifluorométhyl)biphényl-4-yl]méthoxy}phényl)éthyl]amino}-5,6,7,8-tétrahydroquinoline-2-carboxylique de formule (I)et de nouvelles formes cristallines de celui-ci, qui est la forme pseudopolymorphe monohydrate I (I-M-I) ou la forme pseudopolymorphe monohydrate II (I-M-II). En outre, la présente invention concerne un nouveau processus de cristallisation sélectif pour la préparation de la forme pseudopolymorphe monohydrate I (I-M-I) ou la forme pseudopolymorphe monohydrate II (I-M-II), de préférence le monohydrate I de formule I (I-M-I) et des compositions pharmaceutiques comprenant du monohydrate I de formule I (I-M-I), ainsi que son utilisation pour le traitement et/ou la prévention de maladies, en particulier pour le traitement et/ou la prévention de maladies pulmonaires et cardiopulmonaires et cardiovasculaires.