Application Type
Patents
Application SubType
PCT
(10) Registration Number and Date
Status
Filed-Formality Examination
(180) Expiration Date
(20) Filing Number and Date
PG P/2025/000004 2023.07.06
(40) Publication Number and Date
(86) PCT Filing Number and Date
(87) PCT Publication Number and Date
(85) National Entry Date
(30) Priority Details
EP 22290046.6
2022.07.07
(72) Inventor
(EN) HORTOBÁGYI, Irén : Külsõ Szilágyi út 114. 6/16 1048 BUDAPEST, Hungary
(EN) KOVÁCS, Szabolcs : Virág utca 24. 8/45 1045 BUDAPEST, Hungary
(EN) PÓTI, Judit : Kóczán út 10/B/1 2230 Gyömrõ, Hungary
(EN) RONSIN, Gael : 15 Square des Haies Vives 67000 Strasbourg, France
(EN) SÁNTÁNÉ CSUTOR, Andrea : Szárnyas utca 22. C 1107 BUDAPEST, Hungary
(74) Representative Name
(EN) A J PARK : C/- ASHURST - PNG, P.O BOX 850, PORT MORESBY, NATIONAL CAIPTAL DISTRICT
(54) Title
(EN) INDUSTRIAL PROCESS FOR THE PREPARATION OF HEXANOIC ACID, 6-(NITROOXY)-, (1S,2E)-3-[(1R,2R,3S,5R)-2-[(2Z)-7-(ETHYLAMINO)-7-OXO-2-HEPTEN-1-YL]-3,5-DIHYDROXYCYCLOPENTYL]-1-(2-PHENYLETHYL)-2-PROPEN-1-YL ESTER AND HIGH PURE PRODUCT
(57) Abstract
(EN)

The present invention relates to a process for preparing hexanoic acid, 6-(nitrooxy)-, (1S,2E)-3-[(1R,2R,3S,5R)-2-[(2Z)-7-(ethylamino)-7-oxo-2-hepten-1-yl]- 3,5-dihydroxycyclopentyl]-1-(2-phenylethyl)-2-propen-1-yl ester Compound (I). In accordance with the present invention, a pharmaceutical grade Compound (I) can be efficiently prepared by a one-pot reactions preparation step that includes the esterification of the 15-OH bimatoprost by coupling bimatoprost phenyl-boronate with 6- (nitrooxy)hexanoic acid and the removal of the boronate ester protecting group, followed by an efficient purification step. The invention refers also to high purity Compound (I) substantially free of the impurity 15-(6-chlorohexanoyl) ester of bimatoprost and to opthalmic pharmaceutical formulations containing the high purity compound. 

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(58) Citations
Document Type Date Action
Event NameDateStatus
Filing2023.07.06Filed
PCT National Phase Entry2023.07.06PCT National Phase
Filing2025.04.11Filed