CHINOIN GYÓGYSZER ÉS VEGYÉSZETI TERMÉKEK GYÁRA ZRT. (Hungary)
Inventor
Juhász, Imre
Hortobágyi, Irén
Altsach, Tamás
Lászlófi, István
Nagyné Borkó, Ágnes
Rozsumberszki, Imre
Havasi, Gábor
Kardos, Zsuzsanna
Buzder-Lantos, Péter
Abstract
Treprostinil is a synthetic prostacyclin derivative with thrombocyte aggregation inhibitory and vasodilatory activity. Treprostinil can be administered in subcutaneous, intravenous, inhalable, or oral forms. Disclosed is a method for the preparation of treprostinil of formula I and its amorphous form, anhydrate form, monohydrate form, and polyhydrate form salts with bases. In the disclosed method, the chiral center in the 3-hydroxyoctyl substituent is formed at the end of the synthesis, so that the method is robust and well scalable. Also disclosed are treprostinil intermediates and the preparation of the intermediates.
C07C 51/347 - Preparation of carboxylic acids or their salts, halides, or anhydrides by reactions not involving formation of carboxyl groups
C07C 41/26 - Preparation of ethers by reactions not forming ether-oxygen bonds by introduction of hydroxy or O-metal groups
C07C 45/30 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by oxidation with halogen containing compounds, e.g. hypohalogenation
C07C 45/65 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by splitting-off hydrogen atoms or functional groupsPreparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by hydrogenolysis of functional groups
C07C 51/09 - Preparation of carboxylic acids or their salts, halides, or anhydrides from carboxylic acid esters or lactones
C07C 51/41 - Preparation of salts of carboxylic acids by conversion of the acids or their salts into salts with the same carboxylic acid part
C07C 67/14 - Preparation of carboxylic acid esters from carboxylic acid halides
C07C 67/29 - Preparation of carboxylic acid esters by modifying the hydroxylic moiety of the ester, such modification not being an introduction of an ester group by introduction of oxygen-containing functional groups
C07C 67/293 - Preparation of carboxylic acid esters by modifying the hydroxylic moiety of the ester, such modification not being an introduction of an ester group by isomerisationPreparation of carboxylic acid esters by modifying the hydroxylic moiety of the ester, such modification not being an introduction of an ester group by change of size of the carbon skeleton
C07C 69/76 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring
C07C 41/30 - Preparation of ethers by reactions not forming ether-oxygen bonds by increasing the number of carbon atoms, e.g. by oligomerisation
C07C 41/48 - Preparation of compounds having groups
C07C 43/315 - Compounds having groups containing oxygen atoms singly bound to carbon atoms not being acetal carbon atoms
C07C 13/547 - Polycyclic hydrocarbons or acyclic hydrocarbon derivatives thereof with condensed rings with three condensed rings at least one ring not being six-membered, the other rings being at the most six-membered
C07C 35/37 - Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a ring other than a six-membered aromatic ring polycyclic, at least one hydroxy group bound to a condensed ring system with a hydroxy group on a condensed ring system having three rings
C07C 59/72 - Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings and other rings
2.
PROCESS FOR THE PREPARATION OF A CHIRAL PROSTAGLANDIN ENOL INTERMEDIATE AND INTERMEDIATE COMPOUNDS USEFUL IN THE PROCESS
CHINOIN GYÓGYSZER ÉS VEGYÉSZETI TERMÉKEK GYÁRA ZRT. (Hungary)
Inventor
Rozsumberszki, Imre
Kardos, Zsuzsanna
Hortobágyi, Irén
Szabó, Tibor
Váradi, Csaba
Bán, Tamás
Abstract
The present invention relates to a process for the preparation of iloprost of formula I through new intermediates, isolation of iloprost of formula I in solid form, as well as preparation of the 16(S)-iloprost and 16(R)-iloprost isomers of formulae (S)-I and (R)-I and isolation of iloprost of formula I and 16(S)-iloprost of formula (S)-I in solid, crystalline form.
C07C 51/09 - Preparation of carboxylic acids or their salts, halides, or anhydrides from carboxylic acid esters or lactones
C07C 67/31 - Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by introduction of functional groups containing oxygen only in singly bound form
C07C 59/46 - Unsaturated compounds containing hydroxy or O-metal groups containing rings other than six-membered aromatic rings
C07C 69/608 - Esters of carboxylic acids having a carboxyl group bound to an acyclic carbon atom and having a ring other than a six-membered aromatic ring in the acid moiety
4.
Process for the preparation of polymorph form B of treprostinil diethanolamine salt
CHINOIN GYÓGYSZER ÉS VEGYÉSZETI TERMÉKEK GYÁRA ZRT. (Hungary)
Inventor
Hortobágyi, Irén
Lászlófi, István
Varga, Zoltán
Juhász, Imre
Ritz, Imola
Kardos, Zsuzsanna
Abstract
The invention relates to a robust and reproducible process for the preparation of polymorph form B of treprostinil diethanolamine salt, comprising the following steps: a. treprostinil is dissolved in methanol, b. to the solution of step a) diethanolamine or its methanol solution is added, c. the reaction mixture of step b) is agitated till dissolution, d. when salt formation is completed in step c), first portion of an aprotic solvent is added to the solution, e. the solution of step d) is filtered to remove insoluble impurities, f. the filtrate of step e) is seeded with polymorph form B of treprostinil diethanolamine salt, g. to the crystal suspension obtained in step f) a second portion of the aprotic solvent is added, h. the suspension of step g) is agitated until crystallisation is completed, i. the crystals are separated, washed and dried.
C07C 51/43 - SeparationPurificationStabilisationUse of additives by change of the physical state, e.g. crystallisation
C07C 59/72 - Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings and other rings
C07C 215/10 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with one amino group and at least two hydroxy groups bound to the carbon skeleton
CHINOIN GYÓGYSZER ÉS VEGYÉSZETI TERMÉKEK GYÁRA ZRT. (Hungary)
Inventor
Rozsumberszki, Imre
Kardos, Zsuzsanna
Hortobágyi, Irén
Szabó, Tibor
Váradi, Csaba
Bán, Tamás
Abstract
The present invention relates to a process for the preparation of iloprost of formula I through new intermediates, isolation of iloprost of formula I in solid form, as well as preparation of the 16(S)-iloprost and 16(R)-iloprost isomers of formulae (S)-I and (R)-I and isolation of iloprost of formula I and 16(S)-iloprost of formula (S)-I in solid, crystalline form.
C07C 59/46 - Unsaturated compounds containing hydroxy or O-metal groups containing rings other than six-membered aromatic rings
C07C 69/608 - Esters of carboxylic acids having a carboxyl group bound to an acyclic carbon atom and having a ring other than a six-membered aromatic ring in the acid moiety
6.
PROCESS FOR THE PREPARATION OF POLYMORPH FORM B OF TREPROSTINIL DIETHANOLAMINE SALT
CHINOIN GYOGYSZER ES VEGYESZETI TERMEKEK GYARA ZRT. (Hungary)
Inventor
Hortobagyi, Iren
Laszlofi, Istvan
Varga, Zoltan
Juhasz, Imre
Ritz, Imola
Kardos, Zsuzsanna
Abstract
The invention relates to a robust and reproducible process for the preparation of polymorph form B of treprostinil diethanolamine salt, comprising the following steps: a. treprostinil is dissolved in methanol, b. to the solution of step a) diethanolamine or its methanol solution is added, c. the reaction mixture of step b) is agitated till dissolution, d. when salt formation is completed in step c), first portion of an aprotic solvent is added to the solution, e. the solution of step d) is filtered to remove insoluble impurities, f. the filtrate of step e) is seeded with polymorph form B of treprostinil diethanolamine salt, g. to the crystal suspension obtained in step f) a second portion of the aprotic solvent is added, h. the suspension of step g) is agitated until crystallisation is completed, i. the crystals are separated, washed and dried.
C07C 51/41 - Preparation of salts of carboxylic acids by conversion of the acids or their salts into salts with the same carboxylic acid part
C07C 59/58 - Unsaturated compounds containing ether groups, groups, groups, or groups
C07C 59/72 - Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings and other rings
C07C 59/90 - Unsaturated compounds containing keto groups containing singly bound oxygen-containing groups
C07C 213/08 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
C12P 15/00 - Preparation of compounds containing at least three condensed carbocyclic rings
7.
PROCESS FOR THE PREPARATION OF POLYMORPH FORM B OF TREPROSTINIL DIETHANOLAMINE SALT
CHINOIN GYÓGYSZER ÉS VEGYÉSZETI TERMÉKEK GYÁRA ZRT. (Hungary)
Inventor
Hortobágyi, Irén
Lászlófi, István
Varga, Zoltán
Juhász, Imre
Ritz, Imola
Kardos, Zsuzsanna
Abstract
The invention relates to a robust and reproducible process for the preparation of polymorph form B of treprostinil diethanolamine salt, comprising the following steps: a. treprostinil is dissolved in methanol, b. to the solution of step a) diethanolamine or its methanol solution is added, c. the reaction mixture of step b) is agitated till dissolution, d. when salt formation is completed in step c), first portion of an aprotic solvent is added to the solution, e. the solution of step d) is filtered to remove insoluble impurities, f. the filtrate of step e) is seeded with polymorph form B of treprostinil diethanolamine salt, g. to the crystal suspension obtained in step f) a second portion of the aprotic solvent is added, h. the suspension of step g) is agitated until crystallisation is completed, i. the crystals are separated, washed and dried.
C07C 59/72 - Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings and other rings
C07C 59/58 - Unsaturated compounds containing ether groups, groups, groups, or groups
C07C 59/90 - Unsaturated compounds containing keto groups containing singly bound oxygen-containing groups
C07C 51/41 - Preparation of salts of carboxylic acids by conversion of the acids or their salts into salts with the same carboxylic acid part
C07C 213/08 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
C12P 15/00 - Preparation of compounds containing at least three condensed carbocyclic rings
8.
PROCESS FOR THE PREPARATION OF OPTICALLY ACTIVE BERAPROST
CHINOIN GYÓGYSZER ÉS VEGYÉSZETI TERMÉKEK GYÁRA ZRT. (Hungary)
Inventor
Hortobágyi, Irén
Lászlófi, István
Kardos, Zsuzsanna
Molnár, József
Takács, László
Bán, Tamás
Abstract
The invention provides a new process for the preparation of optically active Beraprost of formula (I) starting from racemic Beraprost alkyl ester through hydrolysis, enantiomer esterification, preparation of diacyl -Beraprost ester diastereomers and their separation and hydrolysis.
C07D 307/93 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems condensed with a ring other than six-membered
9.
PROCESS FOR THE PREPARATION OF EPOPROSTENOL SODIUM OF ENHANCED STABILITY
C07D 307/77 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
10.
PROCESS FOR THE PREPARATION OF TRIPLE-BOND-CONTAINING OPTICALLY ACTIVE CARBOXYLIC ACIDS, CARBOXYLATE SALTS AND CARBOXYLIC ACID DERIVATIVES
CHINOIN GYÓGYSZER ÉS VEGYÉSZETI TERMÉKEK GYÁRA ZRT. (Hungary)
Inventor
Hortobágyi, Irén
Lászlófi, István
Kardos, Zsuzsanna
Molnár, József
Takács, László
Bán, Tamás
Abstract
The invention provides a new enzimatic process for the preparation of chiral carboxylic acids, their salts and acid derivatives of the general formula (I) by enzymatic hydrolysis of racemic carboxylic acid ester of the general formula (II) and optionally subsequent esterification or acylation.
CHINOIN GYOGYSZER ES VEGYESZETI TERMEKEK GYARA ZRT. (Hungary)
Inventor
Takacs, Laszlo
Fekete, Ibolya
Buzder-Lantos, Peter
Laszlofi, Istvan
Hortobagyi, Iren
Havasi, Gabor
Kardos, Zsuzsanna
Abstract
The subject of the invention is a process for the preparation of Latanoprostene bunod of formula (1) with a purity higher than 95% where chromatography is used applying normal phase gravity silicagel column chromatography where the used silicagel is irregular silicagel or spherical silicagel an as eluent and eluent mixture consisting of an a polar and a polar solvent is used and if desired, contamination of the purified compound of formula I arising from the solvents are removed by silicagel filtration chromatography. The Latanoprostene bunod of formula (I) is as follows:
C07C 405/00 - Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins
12.
PREPARATION OF LATANOPROSTENE BUNOD OF DESIRED, PRE-DEFINED QUALITY BY GRAVITY CHROMATOGRAPHY
CHINOIN GYÓGYSZER ÉS VEGYÉSZETI TERMÉKEK GYÁRA ZRT. (Hungary)
Inventor
Takács, László
Fekete, Ibolya
Buzder-Lantos, Péter
Lászlófi, István
Hortobágyi, Irén
Havasi, Gábor
Kardos, Zsuzsanna
Abstract
The subject of the invention is a process for the preparation of Latanoprostene bunod of formula (I) with a purity higher than 95% where chromatography is used applying normal phase gravity silicagel column chromatography where the used silicagel is irregular silicagel or spherical silicagel an as eluent and eluent mixture consisting of an apolar and a polar solvent is used and if desired, contamination of the purified compound of formula I arising from the solvents are removed by silicagel filtration chromatography.
C07C 405/00 - Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins
13.
PROCESS FOR THE PREPARATION OF CARBOPROST AND ITS TROMETHAMINE SALT
CHINOIN GYÓGYSZER ÉS VEGYÉSZETI TERMÉKEK GYÁRA ZRT. (Hungary)
Inventor
Buzder-Lantos, Péter
Kardos, Zsuzsanna
Hortobágyi, Irén
Lászlófi, István
Juhász, Imre
Fónagy, László
Váradi, Csaba
Nagyné Borkó, Ágnes
Abstract
The subject of the invention is a novel process for the preparation of Carboprost tromethamine salt where alkylation the enone of the general formula (II) is carried out in the presence of a chiral auxiliary in aprotic solvent with a Grignard reagent. The methyl ester epimers of formula (VII) are separated by gravity silicagel chromatography and the salt formation is carried out by using solid tromethamine base.
C07C 405/00 - Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins
CHINOIN GYOGYSZER ES VEGYESZETI TERMEKEK GYARA ZRT. (Hungary)
Inventor
Juhasz, Imre
Hortobagyi, Iren
Altsach, Tamas
Laszlofi, Istvan
Nagyne Borko, Agnes
Rozsumberszki, Imre
Havasi, Gabor
Kardos, Zsuzsanna
Buzder-Lantos, Peter
Abstract
The present disclosure relates to a process for the preparation of Treprostinil of formula I or its amorphous forms, salt anhydrates, and monohydrates and polyhydrates of salts formed with bases. The present disclosure further relates to intermediates of formulae XVII, XVI, XV, XIV, XIII, XII, XI, Xaõ Xb, IX, VIII, VII, VI, V, IVa, IVb, III, and II present in the process of the present disclosure.
CHINOIN GYÓGYSZER ÉS VEGYÉSZETI TERMÉKEK GYÁRA ZRT. (Hungary)
Inventor
Juhász, Imre
Hortobágyi, Irén
Altsach, Tamás
Lászlófi, István
Nagyné Borkó, Ágnes
Rozsumberszki, Imre
Havasi, Gábor
Kardos, Zsuzsanna
Buzder-Lantos, Péter
Abstract
The invention provides a new process for the preparation of treprostinil of formula (I) and its salts using several new intermediates during the building of the ringsystem.
CHINOIN GYÓGYSZER ÉS VEGYÉSZETI TERMÉKEK GYÁRA ZRT. (Hungary)
Inventor
Vajda, Ervin
Hortobágyi, Irén
Lászlofi, István
Buzder-Lantos, Péter
Havasi, Gábor
Tákacs, László
Kardos, Zsuzsanna
Abstract
The subject of the invention is a process for the preparation of high purity prostaglandin acid of the general formula II wherein the bonds marked with dotted lines represent single or double bonds wherein the double bonds may be cis- or trans oriented, Y represents 0 or CH 2, and R3 stands for a phenyl group which is optionally substituted with CF3, wherein the crude prostaglandin acid of the general formula II is purified by normal phase silicagel chromatography.
C07C 405/00 - Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins
CHINOIN GYÓGYSZER ÉS VEGYÉSZETI TERMÉKEK GYÁRA ZRT. (Hungary)
Inventor
Bischof, Zoltán
Bódis, Ádám
Kömüves-Mars, Mária
Havasi, Gábor
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-l,3-dimethylimidazolinium 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.
C07C 405/00 - Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins
CHINOIN GYOGYSZER ES VEGYESZETI TERMEKEK GYARA ZRT (Hungary)
Inventor
Kardos, Zsuzsanna
Kiss, Tibor
Laszlofi, Istvan
Hortobagyi, Iren
Bischof, Zoltan
Bodis, Adam
Havasi, Gabor
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 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.
C07C 405/00 - Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins
C07D 307/935 - Not further condensed cyclopenta [b] furans or hydrogenated cyclopenta [b] furans
CHINOIN GYÓGYSZER ÉS VEGYÉSZETI TERMÉKEK GYÁRA ZRT. (Hungary)
Inventor
Kardos, Zsuzsanna
Kiss, Tibor
Lászlofi, István
Hortobágyi, Irén
Bischof, Zoltán
Bódis, Ádám
Havasi, Gábor
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 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.
C07C 405/00 - Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins
C07D 307/935 - Not further condensed cyclopenta [b] furans or hydrogenated cyclopenta [b] furans
20.
A NEW PALLADIUM CATALYST, METHOD FOR ITS PREPARATION AND ITS USE
The invention relates to palladium(0)-tetrakis{tri-[3,5-bis(trifluoromethyl)- phenylj-phosphine} complex of formula (I), as well as to its preparation and use. This compound is outstandingly stable, and can be used as catalyst with excellent results.
C07C 41/30 - Preparation of ethers by reactions not forming ether-oxygen bonds by increasing the number of carbon atoms, e.g. by oligomerisation
C07C 201/12 - Preparation of nitro compounds by reactions not involving the formation of nitro groups
C07C 43/205 - Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring the aromatic ring being a non-condensed ring
C07C 43/215 - Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring having unsaturation outside the six-membered aromatic rings
C07C 205/06 - Compounds containing nitro groups bound to a carbon skeleton having nitro groups bound to carbon atoms of six-membered aromatic rings
C07C 15/52 - Cyclic hydrocarbons containing only six-membered aromatic rings as cyclic part substituted by unsaturated hydrocarbon radicals polycyclic non-condensed containing a group with formula
C07C 15/54 - Cyclic hydrocarbons containing only six-membered aromatic rings as cyclic part substituted by unsaturated hydrocarbon radicals polycyclic non-condensed containing a group with formula
C07D 217/02 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ringAlkylene-bis-isoquinolines
C07D 217/16 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals substituted by oxygen atoms
21.
PROCESS FOR THE SEPARATION OF OPTICAL ISOMERS OF THE COREY LACTONE
CHINOIN GYÓGYSZER ÉS VEGYÉSZETI TERMÉKEK GYÁRA ZRT. (Hungary)
Inventor
Szánya, Tibor
Hanák, László
Kozma, Gábor
Németh, Attila
Fónagy, László
Kardos, Zsuzsanna
Szabó, Tibor
Vajda, Ervin
Horváth, Géza
Szabóné Ravasz, Bernadett
Strbka, Andrásné
Nagy, Melinda
Molnár, Zoltán
Abstract
The subject of the present invention is the separation of the optical isomers of the racemic hexahydro-5-hydroxy-4-(hydroxymethyl)-2H-cyclopenta⏧b]furan-2-one (旜Corey-lactone”) of formula (I), by liquid chromatography. The laevo-rotatory (-) isomer of the compound of formula (I) is a valuable prostaglandin intermediate.
C07B 57/00 - Separation of optically-active organic compounds
C07D 307/93 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems condensed with a ring other than six-membered
22.
DEVICE FOR THE PACKAGING AND DISPENSING OF SOLID SHAPED BODIES, ESPECIALLY ORAL TABLETS OR/AND CAPSULES
CHINOIN GYOGYSZER ES VEGYESZETI TERMEKEK GYARA ZRT (Hungary)
Inventor
Erdelyi, Zoltán
Bencz, Zoltán
Mezei, János
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) .
B65D 83/04 - Containers or packages with special means for dispensing contents for dispensing annular, disc-shaped, spherical or like small articles, e.g. tablets or pills
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical, veterinary and sanitary substances, infants'
and invalids' foods, plasters, material for bandaging,
material for stopping teeth, dental wax, disinfectants,
preparations for killing weeds and destroying vermin.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Médicaments, préparations chimiques à usage médical et
vétérinaire, drogues pharmaceutiques; préparations pour
détruire les mauvaises herbes et les animaux nuisibles.
01 - Chemical and biological materials for industrial, scientific and agricultural use
03 - Cosmetics and toiletries; cleaning, bleaching, polishing and abrasive preparations
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Produits chimiques pour l'industrie, les sciences et la
photographie, engrais. Produits cosmétiques. Médicaments et préparations pharmaceutiques pour l'usage
humain et vétérinaire, produits chimiques pour la médecine
et l'hygiène, emplâtres, désinfectants, produits pour la
destruction d'animaux et de plantes.
01 - Chemical and biological materials for industrial, scientific and agricultural use
03 - Cosmetics and toiletries; cleaning, bleaching, polishing and abrasive preparations
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Produits chimiques pour l'industrie, les sciences et la
photographie, engrais. Produits cosmétiques. Médicaments et préparations pharmaceutiques pour l'usage
humain et vétérinaire, produits chimiques pour la médecine
et l'hygiène; emplâtres, désinfectants; produits pour la
destruction d'animaux et de plantes.
01 - Chemical and biological materials for industrial, scientific and agricultural use
03 - Cosmetics and toiletries; cleaning, bleaching, polishing and abrasive preparations
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Engrais; produits à conserver les aliments. Produits cosmétiques. Médicaments et produits pharmaceutiques pour l'usage
humain et vétérinaire; drogues pharmaceutiques,
produits chimiques pour la médecine et l'hygiène;
emplâtres; désinfectants; produits pour la destruction
d'animaux et de plantes.
01 - Chemical and biological materials for industrial, scientific and agricultural use
03 - Cosmetics and toiletries; cleaning, bleaching, polishing and abrasive preparations
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Drogues, produits chimiques pour l'industrie, les sciences
et la photographie; engrais; produits phytopathologiques,
produits à conserver. Produits chimiques pour l'hygiène; produits cosmétiques. Médicaments et préparations pharmaceutiques pour l'usage
humain et vétérinaire; drogues, produits chimiques pour la
médecine et l'hygiène; emplâtres; désinfectants; produits
pour la destruction d'animaux et de plantes, produits
phytopathologiques.
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Protective products for plants. Medicines, chemical products for medical and sanitary use,
pharmacy goods, pharmaceutical drugs and preparations,
veterinary products and protective agents for plants;
herbicides and preparations for destroying vermin.