Abstract: The subject of the invention is process the preparation of travoprost of formula (I) characterized by that the free acid of formula (II) is a.) activated with 2-chloro-1,3-dimethyl-imidazolinium chloride (DMC) and the resulting activated carboxylic acid intermediate is reacted with isopropyl alcohol, or b.) reacted with alkyl haloformate and the resulting mixed anhydride is reacted with isopropyl alcohol, or c.) activated with a straight or branched C1-8 dialkyl dicarbonate and reacted with isopropanol in the presence of water-free magnesium salt.
Type:
Grant
Filed:
November 26, 2013
Date of Patent:
March 22, 2016
Assignee:
CHINOIN GYÓGYSZER ÉS VEGYÉSZETI TERMÉKEK GYÁRA ZRT.
Inventors:
Zoltán Bischof, Ádám Bódis, Mária Kömüves-Mars, Gábor Havasi
Abstract: The invention relates to a process for the preparation of travoprost of formula (I), comprising that, the compound of formula (II), is stereoselectively reduced, the resulting compound of formula (III), is if desired crystallized, the lactone group of the compound of formula (III) is reduced, the p-phenyl-benzoyl protecting group of the thus obtained compound of formula (IV), is removed, the resulting triol of formula (V), is, if desired after crystallization, transformed by Wittig reaction into the acid of formula (VI), which is then esterified.
Type:
Grant
Filed:
December 10, 2012
Date of Patent:
December 15, 2015
Assignee:
CHINOIN GYÓGYSZER ÉS VEGYÉSZETI TERMÉKEK GYÁRA ZRT.
Inventors:
Zsuzsanna Kardos, Tibor Kiss, István Lászlofi, Irén Hortobágyi, Zoltán Bischof, Ádám Bódis, Gábor Havasi
Abstract: The invention relates to a device for the packaging and dispensing of solid shaped bodies, especially oral tablets or/and capsules, which device has a container sealed with a cap suitable for storing shaped bodies, a dispensing opening, and tools forwarding the shaped bodies from the inside of the container to the dispensing opening. The container (5) is constructed in a house (1) in a way that it can be moved like a piston against elastic returning force. The dispensing opening (35) is situated in the bottom (2a) of the house (1); when the device is in a position when it is not used for dispensing, the end-part of the container (5), with an opening (20) for releasing one shaped body at a time situated opposite the end of the container (5) sealed with a cap, fits into the dispensing opening (35) by sealing it, and it is constructed in a way that in the course of the dispensing operations it makes it possible to dispense favourably one shaped body at a time outside of the house (1).
Type:
Grant
Filed:
September 26, 2006
Date of Patent:
October 4, 2011
Assignee:
CHINOIN Gyógyszer és Vegyészeti Termékek Gyára Zrt.
Inventors:
Zoltán Erdélyi, Zoltán Bencz, János Mezei