01 - Chemical and biological materials for industrial, scientific and agricultural use
42 - Scientific, technological and industrial services, research and design
Goods & Services
Active chemical ingredients for use in pharmaceutical
substance manufacture. Scientific and technological services, research, development
and innovation services; scientific laboratory services for
analysis of chemicals, pharmaceuticals; technical research
services regarding chemicals, pharmaceuticals.
2.
PROCESS FOR PREPARING OPTICALLY ACTIVE SECONDARY AMINES AND THEIR USE AS INTERMEDIATES
LL1 44 alkyl, preferably R1144 alkyl, preferably R2nn-propyl and the use of the obtained optically amine compounds of formula (IV) for the preparation of rotigotine.
C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07B 57/00 - Separation of optically-active organic compounds
C07C 215/48 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by hydroxy groups
C07C 269/00 - Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups
C07C 269/06 - Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups
C07C 271/18 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by doubly-bound oxygen atoms
C07C 271/12 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
01 - Chemical and biological materials for industrial, scientific and agricultural use
42 - Scientific, technological and industrial services, research and design
Goods & Services
Active chemical ingredients for use in the manufacture of pharmaceuticals. Scientific and technological services, research, development and innovation; Scientific laboratory services for analysing chemicals and pharmaceuticals; technical surveying in relation to the following goods: Chemical products, Pharmaceutical goods.
6.
PROCESS FOR PREPARING DAPRODUSTAT AND COCRYSTALS THEREOF
The present invention provides crystal forms of daprodustat, which are cocrystals comprising daprodustat free acid and a daprodustat pharmaceutically acceptable metal salt, wherein the metal salt is an alkali metal salt. The invention also refers to processes for the preparation of said cocrystals of daprodustat in good yield and high purity suitable for industrial scale, to pharmaceutical compositions containing them and to their use in therapy. The present invention also provides an efficient process for the preparation of daprodustat or a pharmaceutically or veterinary acceptable salt thereof in good yield and high purity suitable for industrial scale applications which involves improved conditions for the preparation of key intermediates.
It is provided a method for the purification of vilanterol trifenatate of formula (I)
It is provided a method for the purification of vilanterol trifenatate of formula (I)
It is provided a method for the purification of vilanterol trifenatate of formula (I)
comprising crystallizing vilanterol trifenatate from a ketone solvent selected from the group consisting of methyl ethyl ketone (MEK), methyl isobutyl ketone (MIK), ethyl isopropyl ketone, methyl isopropyl ketone, 3-methyl-2-pentanone, and a mixture thereof.
C07C 213/10 - SeparationPurificationStabilisationUse of additives
C07C 217/48 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing rings
8.
PROCESS FOR PREPARING PYRIDINOYLPIPERIDINES 5-HT1F AGONISTS AND SALTS THEREOF
The present invention provides an efficient and environmentally friendly process suitable for industrial scale application for the preparation of pyridinoylpiperidines as 5-HT1F agonists and salts thereof, in particular 2,4,6-trifluoro-N-[6-(l-methylpiperidine-4-carbonyl)pyridine-2-yl]benzamide or a pharmaceutically acceptable acid addition salt thereof, preferably the hemisuccinate salt, in good yield and high purity. The present invention also provides crystalline acid addition salts of 2,4,6-trifluoro-N-[6-(l-methylpiperidine-4-carbonyl)pyridine-2-yl]benzamide suitable for purification at industrial scale.
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
The present invention provides an oral solid pharmaceutical composition in the form of a multiparticulate composition comprising an immediate release core comprising levetiracetam or a pharmaceutically acceptable salt thereof coated with a modified release layer, a process for the preparation of the composition of the invention, and its use in therapy.
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61K 31/4015 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
10.
Process for preparing 1-deoxy-1-methylamino-d-glucitol 2-(3,5-dichlorophenyl)-6-benzoxazolecarboxylate
The present invention relates to an improved process for the preparation of 1-deoxy-1-methylamino-D-glucitol 2-(3,5-dichlorophenyl)-6-benzoxazolecarboxylate, also known as tafamidis meglumine. The process of the present invention is particularly suitable for industrial scale manufacture of tafamidis meglumine with excellent purity and high yields.
Method for the purification of vilanterol trifenatate It is provided a method for the purification of vilanterol trifenatate of formula (I) comprising crystallizing vilanterol trifenatate from a ketone solvent selected from the group consisting of methyl ethyl ketone (MEK), methyl isobutyl ketone (MIK), ethyl isopropyl ketone, methyl isopropyl ketone, 3-methyl-2-pentanone, and a mixture thereof.
C07C 213/10 - SeparationPurificationStabilisationUse of additives
C07C 217/08 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to an acyclic carbon atom
C07C 57/38 - Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms containing six-membered aromatic rings polycyclic
12.
METHOD FOR THE PURIFICATION OF VILANTEROL TRIFENATATE
Method for the purification of vilanterol trifenatate It is provided a method for the purification of vilanterol trifenatate of formula (I) comprising crystallizing vilanterol trifenatate from a ketone solvent selected from the group consisting of methyl ethyl ketone (MEK), methyl isobutyl ketone (MIK), ethyl isopropyl ketone, methyl isopropyl ketone, 3-methyl-2-pentanone, and a mixture thereof.
C07C 57/38 - Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms containing six-membered aromatic rings polycyclic
C07C 213/10 - SeparationPurificationStabilisationUse of additives
C07C 217/08 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to an acyclic carbon atom
13.
PROCESS FOR PREPARING 1-DEOXY-1-METHYLAMINO-D-GLUCITOL 2-(3,5-DICHLOROPHENYL)-6-BENZOXAZOLECARBOXYLATE
The present invention relates to an improved process for the preparation of 1-deoxy-1-methylamino-D- glucitol 2-(3,5-dichlorophenyl)-6-benzoxazolecarboxylate, also known as tafamidis meglumine. The process of the present invention is particularly suitable for industrial scale manufacture of tafamidis meglumine with excellent purity and high yields.
The present invention provides an improved process for the manufacture (R)-6-hydroxy-8-[1-hydroxy-2-[2-(4-methoxyphenyl)-1,1-dimethyl-ethylamino-ethyl]-2H-1,4-benzoxazin-3(4H)-one, in high purity and high yield, through the use of 1,1-dimethyl-2-(4-methoxyphenyl)ethyl amine L-tartrate salt, 1,1-dimethyl-2-(4-methoxyphenyl)ethyl amine maletate salt or the camphorsulfonate salt of intermediate (4). The invention also relates to said salts, to processes for preparing them and to their use for the manufacture of (R)-6-hydroxy-8-[1-hydroxy-2-[2-(4-methoxyphenyl)-1,1-dimethyl-ethylamino-ethyl]-2H-1,4-benzoxazin-3(4H)-one or a pharmaceutically acceptable salt thereof.
The present invention provides a new process for stabilizing the particle size of micronized glycopyrronium salt (such as glycopyrronium bromide) which yields a micronized product exhibiting improved chemical and polymorphic stability even after prolonged storage. The invention also relates to compositions comprising said stabilized glycopyrronium salt (such as glycopyrronium bromide) and to dry powder inhaler devices and capsules or blisters comprising the stabilized glycopyrronium salt (such as glycopyrronium bromide). The glycopyrronium salt (such as glycopyrronium bromide) or compositions of the invention may be used as a medicament, for instance in the treatment of asthma, chronic obstructive pulmonary disease or cystic fibrosis or related diseases.
A61J 3/02 - Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms into the form of powders
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
A61K 31/4015 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
16.
PROCESS FOR PREPARING 4-[(1-HYDROXY-1,3-DIHYDRO-2,1-BENZOXABOROL-5-YL)OXY]BENZONITRILE (CRISABOROLE)
The present invention relates to a new one-pot synthesis employing 4-(4-bromo-3-(hydroxymethyl)phenoxy)benzonitrile (compound B) for preparing (4-[(1-hydroxy-1,3-dihydro-2,1-benzoxaborol-5-yl)oxy]benzonitrile (crisaborole) and pharmaceutically acceptable salts thereof in high yield and high purity. The novel process of the present invention is particularly suitable for industrial scale manufacture of crisaborole and its salts with excellent purity and good yields. The present invention also describes an intermediate, 4-(3-formyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenoxy)benzonitrile (compound I), which is inter alia suitable for preparing (4-[(1-hydroxy-1,3-dihydro-2, 1-benzoxaborol-5-yl)oxy]benzonitrile (crisaborole) and pharmaceutically acceptable salts thereof, as well as a another process suitable for industrial scale applications, employing the intermediate compound I in the preparation of crisaborole and pharmaceutically acceptable salts thereof, in high yield and high purity.
IMPROVED PROCESS FOR THE MANUFACTURE OF R-6-HYDROXY-8-[1-HYDROXY-2-[2-(4-METHOXYPHENYL)-1,1-DIMETHYLETHYLAMINOETHYL]-2H-1,4-BENZOXAZIN-3(4H)-ONE HYDROCHLORIDE
The present invention provides an improved process for the manufacture (R)-6- hydroxy-8-[1-hydroxy-2-[2-(4-methoxyphenyl)-1,1-dimethyl-ethylamino-ethyl]-2H-1,4- benzoxazin-3(4H)-one, in high purity and high yield, through the use of 1,1-dimethyl-2- (4-methoxyphenyl)ethyl amine L-tartrate salt, 1,1-dimethyl-2-(4-methoxyphenyl)ethyl amine maletate salt or the camphorsulfonate salt of intermediate (4). The invention also relates to sais salts, to processes for preparing them and to their use for the manufacture of (R)-6-hydroxy-8-[1-hydroxy-2-[2-(4-methoxyphenyl)-1,1-dimethyl- ethylamino-ethyl]-2H-1,4-benzoxazin-3(4H)-one or a pharmaceutically acceptable salt thereof.
C07C 309/07 - Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing oxygen atoms bound to the carbon skeleton
18.
PHARMACEUTICAL FORMULATIONS OF PRASUGREL AND PROCESSES FOR THE PREPARATION THEREOF
The present invention relates to a process for the micronization of prasugrel, to prasugrel formulations for micronization, to micronized prasugrel compositions obtained or obtainable by the process of the invention and compositions comprising thereof (e.g. granulates or tablets). It further relates to the pharmaceutical use of said compositions, in particular in the treatment of coagulation disorders. More specifically, said process for obtaining a micronized prasugrel composition comprises: a) mixing prasugrel with a water-insoluble hydrophilic excipient, optionally in combination with other excipients; and b) micronizing the composition obtained in a).
A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
The present invention provides a new process for stabilizing the particle size of micronized glycopyrronium salt (such as glycopyrronium bromide)which yields a micronized product exhibiting improved chemical and polymorphic stability even after prolonged storage. The invention also relates to compositions comprising said stabilized glycopyrronium salt (such as glycopyrronium bromide) and to dry powder inhaler devices and capsules or blisters comprising the stabilized glycopyrronium salt (such as glycopyrronium bromide). The glycopyrronium salt (such as glycopyrronium bromide) or compositions of the invention may be used as a medicament, for instance in the treatment of asthma, chronic obstructive pulmonary disease or cystic fibrosis or related diseases.
A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
20.
Process for preparing (3RS)-3-[(2SR)-(2-cyclopentyl-2-hydroxy-2-phenylacetyl)oxy]-1,1-dimethylpyrrolidinium bromide
The present invention relates to an efficient and environmentally friendly process for preparing (3RS)-3-[(2SR)-(2-cyclopentyl-2-hydroxy-2-phenylacetyl)oxy]-1,1-dimethylpyrrolidinium bromide with high yield and purity suitable for industrial scale applications.
The present invention provides an efficient and environmentally friendly process for the preparation of (R)-3-[(-1-methylpyrrolidin-2-yl)methyl]-5-(2-phenylsulfonylethyl)-1H-indole (eletriptan) and pharmaceutically acceptable salts thereof, in good yield and high purity, which is also suitable for industrial scale applications. The present invention also provides new acid addition salts of (R)-3-[(-1-methylpyrrolidin-2-yl)methyl]-5-(2-phenylsulfonylethyl)-1H-indole, which are also suitable for preparing (R)-3-[(-1-methylpyrrolidin-2-yl)methyl]-5-(2-phenylsulfonylethyl)-1H-indole and pharmaceutically acceptable salts thereof, in good yield and high purity. The present invention additionally provides tert-butylcarbonyl protected precursors to the compound eletriptan.
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
22.
COMPOUNDS OF R-(-)-(E)-[4-(2,4-DICHLOROPHENYL)-1,3-DITHIOLAN-2-YLIDENE]-1 -IMIDAZOLYLACETONITRILE-HA (LULICONAZOLE-HA) AS ANTIFUNGALS
The present invention refers to compound R-(-)-(E)-[4-(2,4-dichlorophenyl)-1,3-dithiolan-2-ylidene]-1-imidazolylacetonitrile HA, wherein HA is an acid; and to a process for their preparation. The present invention also refers to the use of compound R-(-)-(E)-[4-(2,4-dichlorophenyl)-1,3-dithiolan-2-ylidene]-1-imidazolylacetonitrile HA for the manufacturing of luliconazole and pharmaceutically acceptable salts or co-crystals thereof in high yield and purity. The present invention further is directed to this compound R-(-)-(E)-[4-(2,4-dichlorophenyl)-1,3-dithiolan-2-ylidene]-1-imidazolylacetonitrile HA in the treatment of fungal infections.
C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
The present invention provides a solid pharmaceutical composition in the form of immediate release tablets, comprising pregabalin particles having specific particle size distribution with a D(50) value from 100 to 420 and/or a D(90) value from 300 μm to 850 μm, having a good dissolution profile and a good stability. The invention also encompasses a simplified process for preparing the solid pharmaceutical composition in the form of immediate release tablets by direct compression.
A61K 31/197 - Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
24.
MIXED SOLVATE OF (R)-5-[2-(5,6-DIETHYLINDAN-2-YLAMINO)-1-HYDROXYETHYL] -8-HYDROXY-1H-QUINOLIN-2-ONE L-TARTRATE
The present invention provides an improved process for the manufacture of indacaterol or a pharmaceutically acceptable salt thereof, preferably indacaterol maleate, in high chemical and enantiomeric purity and high yield, via a mixed solvate of (R)-5-[2-(5,6-diethylindan-2-ylamino)-1-hydroxyethyl]-8-hydroxy-1H-quinolin-2-one L-tartrate salt, compound of formula (II).
The present invention relates to a solid form of 4-(2-methyl-1 H-imidazol-1-yl)-2,2- diphenylbutanenitrile phosphate intermediate and its use for preparing imidafenacin, and an improved process for preparing 4-(2-methyl-1-imidazolyl)-2,2- diphenylbutanamide, also known as imidafenacin, in good yield and purity using said solid form.
C07D 233/61 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms not forming part of a nitro radical, attached to ring nitrogen atoms
26.
PROCESS FOR PREPARING (3RS)-3-[(2SR)-(2-CYCLOPENTYL-2-HYDROXY-2-PHENYLACETYL)OXY]-1,1-DIMETHYLPYRROLIDINIUM BROMIDE
The present invention relates to an efficient and environmentally friendly process for preparing (3RS)-3-[(2SR)-(2-cyclopentyl-2-hydroxy-2-phenylacetyl)oxy]-1,1-dimethylpyrrolidinium bromide with high yield and purity suitable for industrial scale applications.
The present invention relates to a novel process for the manufacture of 1-(4- methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1 H- pyrazolo[3,4-c]pyridine-3-carboxamide and pharmaceutically acceptable salts thereof with high yield and purity suitable for industrial scale applications and reducing the steps of the global process.
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A monoclinic crystalline form of asenapine maleate is described, which is characterized in that it is not micronised and has a particle size distribution characterized by a d90 of 40 μm or less. A process for the preparation of a monoclinic crystalline form of asenapine maleate is also described, the process comprising the following steps: a) providing a mixture of monoclinic asenapine maleate and an organic solvent which, under the conditions of the process, acts as an antisolvent; b) stirring the mixture at a temperature between 15 and 60° C.; and c) collecting the crystals, wherein the organic solvent is selected from alcohols, ketones, ethers, esters, hydrocarbons or mixtures thereof.
C07D 491/044 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
29.
Polymorphic form of a long-acting beta-2 adrenoceptor agonist
New polymorphic form of a long-acting beta-2 adrenoceptor agonist A new polymorphic form of arformoterol tartrate, designated as form D, is provided and which is characterized by at least one of the following: (i) a powder X-ray diffraction pattern having peaks at approximately 6.8, 13.3, 13.6, 3.8, 14.1, 18.2, 18.7, 20.0±0.2 degrees two theta; or (ii) a DSC thermogram showing an endothermic peak with an onset at approximately 19-120° C., and a maximum at approximately 129-131° C., followed by an exothermic peak with a maximum at approximately 137-138° C.; wherein the DSC thermogram of form D has a further endothermic peak with an onset at approximately 168-170° C.1 Processes for preparing the new polymorphic form, uses thereof and intermediates for the preparation thereof, are also provided.
C07C 233/43 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of a saturated carbon skeleton
30.
PROCESS FOR THE MANUFACTURE OF (R)-5-[2-(5,6-DIETHYLINDAN-2-YLAMINO)-1-HYDROXYETHYL]-8-HYDROXY-(1H)-QUINOLIN-2-ONE
The present invention provides an efficient process for manufacturing (R)-5-[2-(5,6-diethyl-indan-2-yl-amino)-1-hydroxyethyl]-8-hydroxy-(1H)-quinolin-2-one, commonly known as indacaterol, or a pharmaceutically acceptable salt thereof, comprising intermediates of synthesis of Formula (II) and Formula (III).
The present invention refers to solid forms of agomelatine, a process for their preparation and pharmaceutical compositions containing them. The present invention also relates to a process for the manufacture of N-[2-(7-methoxy- -naphthalenyl) ethyl]acetamide (agomelatine) with improved yields and purity and reducing the steps of the global process.
A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
C07C 233/18 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
A61P 25/00 - Drugs for disorders of the nervous system
32.
Stable micronised monoclin form of asenapine maleate and its synthesis
A stable micronized monoclinic form of asenapine maleate is described, which comprises 5% by weight or less of orthorhombic form or any other crystalline form of asenapine maleate, wherein the asenapine maleate has a particle size distribution characterized by a d90 equal to or below 40 μm. Processes for preparing the stable micronized monoclinic form of asenapine maleate are also described. Formula (I).
Comprising reacting compound (IV) with compound (V) in a solvent to give (S)-mitiglinide (II) and compound (III) as a by- product; removing the solvent and adding ethyl acetate to precipitate compound (III); collecting the solid and applying at least one cycle process comprising: - refluxing the solution of compound (III) with an organic solvent to give (S)-mitiglinide (II) and further compound (III) as a by-product, - removing the organic solvent and adding ethyl acetate to precipitate compound (III); and - separating the mother liquors from the solid, and mixing all the mother liquors; removing the ethyl acetate from the mother liquors to obtain (S)-mitiglinide.
The present invention provides a process for obtaining dronedarone or salts thereof characterized in that in an organic phase comprising one or more non-polar solvents, 5-amino-3-[4-(3-di-n-butylaminopropoxy)benzoyl]-2-n-butyl-benzofuran is reacted with methane sulfonyl chloride without the addition of a base. The invention also provides a process for obtaining intermediates of dronedarone environmentally friendly and industrially viable.
New polymorphic form of a long-acting beta-2 adrenoceptor agonist A new polymorphic form of arformoterol tartrate, designated as form D, is provided and which is characterised by at least one of the following: (i) a powder X-ray diffraction pattern having peaks at approximately 6.8, 13.3, 13.6, 3.8, 14.1, 18.2, 18.7, 20.0 ±0.2 degrees two theta; or (ii) a DSC thermogram showing an endothermic peak with an onset at approximately 19-120 ºC, and a maximum at approximately 129-131 ºC, followed by an exothermic peak with a maximum at approximately 137-138 ºC; wherein the DSC thermogram of form D has a further endothermic peak with an onset at approximately 168-170 ºC.1 Processes for preparing the new polymorphic form, uses thereof and intermediates for the preparation thereof, are also provided.
C07C 233/43 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of a saturated carbon skeleton
The present invention is directed to novel compounds of formula (I) as well as to the process for their preparation. Novel compounds of formula (I) can be converted into asenapine through an efficient process. The invention also relates to novel intermediates used in this process and their use in the preparation of compounds of formula (I).
PHARMACEUTICAL COMPOSITIONS OF 4'-[(1,4'DIMETHYL-2'-PROPYL[2,6'-BI-1H-BENZIMIDAZOL]-1'-YL)METHYL]-[1,1'-BIPHENYL]-2-CARBOXYLIC ACID AND 6-CHLORO-3,4-DIHYDRO-2H-1,2,4-BENZOTHIADIAZINE-7-SULFONAMIDE-1,1-DIOXIDE
This invention relates to stable solid immediate release pharmaceutical compositions of 4'-[(1,4'dimethyl-2'-propyl[2,6'-bi-1H-benzimidazol]-1'-yl)methyl]-[1,1'-5 biphenyl]-2-carboxylic acid, also known as telmisartan and hydrochlorothiazide (HCTZ or HCT), a thiazide diuretic, which also affords dosage uniformity; process thereof and their use in the treatment of hypertension and essential hypertension.
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A61K 31/54 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
The present invention relates to a process for the manufacturing of a rivaroxaban or a pharmaceutically acceptable salt thereof, wherein the process comprises obtaining an acid addition salt of a 4-{4-[(5S))-5-(aminomethyl)-2-oxo-1,3-oxozoladine-3- yl]phenyl}morpholin-3-one, and reacting the acid addition salt with the suitable reagents to obtain rivaroxaban or a salt thereof.
C07D 413/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
The present invention is directed to an improved process for preparing, prasugrel and maleate salt of Prasugrel and, optionally other pharmaceutically acceptable salts from, prasugrel and said maleate salt, in high yields and purity, which can be used at industrial scale. The process of the present invention comprises the steps of bromination, condensation, acetylating and optionally converting into maleate salt and, if desired, conversion into another pharmaceutically acceptable salt from it. The present process is advantageous in terms of productivity, efficacy, purity and also prevents the use of toxic substances.
A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
C07C 45/63 - 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 introduction of halogenPreparation 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 substitution of halogen atoms by other halogen atoms
A monoclinic crystalline form of asenapine maleate is described, which is characterized in that it is not micronised and has a particle size distribution characterized by a d90 of 40 μm or less. A process for the preparation of a monoclinic crystalline form of asenapine maleate is also described, the process comprising the following steps: a) providing a mixture of monoclinic asenapine maleate and an organic solvent which, under the conditions of the process, acts as an antisolvent; b) stirring the mixture at a temperature between 15 and 60°C; and c) collecting the crystals, wherein the organic solvent is selected from alcohols, ketones, ethers, esters, hydrocarbons or mixtures thereof.
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
A stable micronised monoclinic form of asenapine maleate is described, which comprises 5% by weight or less of orthorhombic form or any other crystalline form of asenapine maleate, wherein the asenapine maleate has a particle size distribution characterised by a d90 equal to or below 40 μm. Processes for preparing the stable micronised monoclinic form of asenapine maleate are also described. Formula (I).
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
The present invention is directed to a novel salt of a montelukast intermediate, the process of preparation thereof, the use of such salt in the preparation of sodium montelukast and a process for the preparation of sodium montelukast making use of said salt.
The present invention provides a process for obtaining dronedarone or salts thereof characterized in that in an organic phase comprising one or more non-polar solvents, 5-amino-3-[4-(3-di-n-butylaminopropoxy)benzoyl]-2-n-butyl-benzofuran is reacted with methane sulfonyl chloride without the addition of a base. The invention also provides a process for obtaining intermediates of dronedarone environmentally friendly and industrially viable.
The present invention is directed to novel compounds of formula (I) as well as to the process for their preparation. Novel compounds of formula (I) can be converted into asenapine through an efficient process. The invention also relates to novel intermediates used in this process and their use in the preparation of compounds of formula (I).
The present invention is directed to novel compounds of formula (I) as well as to the process for their preparation. Novel compounds of formula (I) can be converted into asenapine through an efficient process. The invention also relates to novel intermediates used in this process and their use in the preparation of compounds of formula (I).
This invention relates to stable solid oral pharmaceutical compositions of 8-chloro-6,11-dihydro-11-(4-piperidylidene)5H-benzo[5,6]cyclohepta[1,2-b]pyridine, also known as descarboethoxyloratadine (desloratadine or DCL) consisting of a tablet core and a filmogenic coating and their preparation methods. The stable solid oral pharmaceutical compositions of desloratadine contains less than 0.1 % by weight of total degradation impurities (measured by HPLC). Stable solid oral pharmaceutical compositions containing small particle size of desloratadine are also disclosed.
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
The invention relates to a method and compounds for the preparation of clevidipine butyrate, a very short acting hypertensive calcium antagonist, as well as the synthesis of these compounds useful for the preparation of clevidipine (also known as clevidipine butyrate). Moreover the invention also discloses polymorphic forms of clevidipine butyrate, useful for the preparation of pharmaceutical compositions, and processes to prepare them.
The present invention refers to an improved method for the preparation of compound 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylic acid substantially free of its 3H-I isomer. The invention also refers to the use of said intermediate for the preparation of Rufinamide and for obtaining a new polymorphic form of Rufinamide, designed as Form R-5. The invention also refers to said new polymorph of Rufinamide, and to the composition containing it and its use as medicament. The new polymorph of Rufinamide shows good stability and appropriate physico-chemical properties for its manipulation on industrial scale. Polymorph Form R-5 will be suitable to use as pharmaceutical for the treatment of convulsions, especially for the treatment of epilepsy.
The present invention provides a novel process for obtaining Bosentan, with few synthesis steps, by coupling the intermediate pyrimidine compound of formula I with the sulfonamide compound of formula II. The use of said efficient process prevents the use of hazardous chemicals and thus it is of considerable interest for obtaining Bosentan in a large industrial scale. The invention also refers to the novel intermediates of formula II and to a process for its production.
The present invention relates to an improved process for obtaining Paliperidone, I, comprising alkylating compound VI, or a salt thereof, with compound V, or a salt thereof, using a base selected from triethylamine or diisopropylethylamine and, optionally, a solvent. Moreover, the invention relies on the preparation of intermediates used in such process.
The present invention refers to an improved process for the preparation of telmisartan or a pharmaceutical acceptable salt thereof through hydrolysis compounds of formula general (I) wherein R is tert-butyl ester (Ia) or salts thereof. Preferably, the invention discloses the preparation of telmisartan through hydrolysis of novel organic salts of compounds of formula (I), particularly wherein R is tert-butyl ester (Ia). The invention also relates to a process for the preparation of these novel organic salts, in particular wherein R is tert-butyl ester (Ia) and its use in the preparation of telmisartan.
The present invention relates to a new pharmaceutical composition of entacapone, levodopa and carbidopa or pharmaceutically acceptable salts or hydrates thereof characterized in that it comprises a first mixture of entacapone and levodopa and a second mixture of levodopa and carbidopa. The invention also relates to a preparation method of said composition.
Relates to a new polymorphic form of Granisetron base, Form I, to methods for obtaining thereof, to the method for obtaining Granisetron.HCl and its use for preparing pharmaceutical formulations. The Form I is characterized by the X-ray powder diffractogram shown in FIG. 1. Included in summarised form are the methods and solvents for obtaining the Form I: 1) Evaporation of hexane at atmospheric pressure; 2) Evaporation of acetone at atmospheric pressure; 3) Evaporation of toluene at atmospheric pressure; 4) Cooling of a saturated solution of diethyl ether to reflux temperature; 5) Evaporation of 2-propanol atmospheric pressure; 6) Evaporation of tetrahydrofuran at atmospheric pressure; and 7) Cooling of a saturated solution of acetonitrile to reflux temperature.
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
C07D 451/14 - Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamineCyclic acetals thereof containing 9-azabicyclo [3.3.1] nonane ring systems, e.g. granatane, 2-aza-adamantaneCyclic acetals thereof
A61P 1/08 - Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigoAntiemetics
The present invention provides a novel process for obtaining Bosentan, with few synthesis steps, by coupling the intermediate pyrimidine derivative of formula I with the sulfonamide derivative of formula II. The use of said process prevents the protection of the hydroxyl group of the sulfonamide II and thus is of considerable interest for obtaining Bosentan in a large industrial scale. The invention also refers to the intermediates of formula II and to a process for its production.
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
55.
Method for preparing a mixed solvate of olanzapine
An improved method is provided for preparing a mixed solvate of olanzapine/water/tetrahydrofuran in a proportion of 1:1:1/2. Said improvement is characterised in that said mixed solvate is basically prepared by means of methylation of the N-desmethylolanzapine with dimethyl sulphate, using tetrahydrofuran and water as solvents.
The present invention relates to micronisable salmeterol xinafoate polymorph I characterized by a mean particle size between 5 and 15 μm and a bulk density between 0.1 and 0.2 g/mL, to a method for its preparation and to its use in the preparation of micronised salmeterol xinafoate.
The present invention relates to an improved process for obtaining Paliperidone, I, comprising alkylating compound VI, or a salt thereof, with compound V, or a salt thereof, using a base selected from triethylamine or diisopropylethylamine and, optionally, a solvent. Moreover, the invention relies on the preparation of intermediates used in such process.
The present invention refers to the novel cyclopropylamine salt of montelukast in crystalline form and its use in the process for the preparation of highly pure amorphous montelukast sodium.
This invention relates to a an orally disintegrating tablet obtainable by direct compression of a dry powdered mix-ture, said mixture comprising up to 15% by weight of calcium silicate, at least 50% of a diluent, a disintegrant agent and an active ingredient. It also relates to a process for preparing the tablets by homogeneous blending the specific excipients in powder form and subsequent direct compression of the mixture. Said tablets disintegrate quickly in the cavity of the mouth, in particular in less than 15 seconds.
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
This invention relates to a an orally disintegrating tablet obtainable by direct compression of a dry powdered mixture, said mixture comprising up to 15% by weight of calcium silicate, at least 50% of a diluent, a disintegrant agent and an active ingredient. It also relates to a process for preparing the tablets by homogeneous blending the specific excipients in powder form and subsequent direct compression of the mixture. Said tablets disintegrate quickly in the cavity of the mouth, in particular in less than 15 seconds.
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
61.
POLYMORPHIC FORM OF GRANISETRON BASE, METHODS FOR OBTAINING IT AND FORMULATION CONTAINING IT
Relates to a new polymorphic form of Granisetron base, Form I, to methods for obtaining thereof, to the method for obtaining Granisetron • HCl and its use for preparing pharmaceutical formulations. The Form I is characterized by the X-ray powder dif f ractogram shown in Figure 1. Included in summarised form are the methods and solvents for obtaining the Form I: 1) Evaporation of hexane at atmospheric pressure; 2) Evaporation of acetone at atmospheric pressure; 3) Evaporation of toluene at atmospheric pressure; 4) Cooling of a saturated solution of diethyl ether to reflux temperature; 5) Evaporation of 2-propanol at atmospheric pressure; 6) Evaporation of tetrahydrofuran at atmospheric pressure; and 7) Cooling of a saturated solution of acetonitrile to reflux temperature.
C07D 451/14 - Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamineCyclic acetals thereof containing 9-azabicyclo [3.3.1] nonane ring systems, e.g. granatane, 2-aza-adamantaneCyclic acetals thereof
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
A61P 1/08 - Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigoAntiemetics
62.
Synthesis intermediates useful for preparing zolmitriptan
In particular, this invention relates to the synthesis intermediates (IV), (V), (VI) and (VIII) useful for preparing zolmitriptanzohnitriptan or a pharmaceutically acceptable salt thereof, which includes a) Ppreparation of the diazonium salt of the aniline hydrochloride (II); followed by reduction and acidification to give hydrazine (III); b) In situ Reaction of the hydrazine hydrochloride (III) with α-keto-δ-valerolactone, to give the hydrazone (IV); c) Fischer indole synthesis of the hydrazone (IV), to give the pyranoindolone of formula (V); d) Ttransesterification of the pyranoindolone (V) to provide the compound (VI), in which R means a straight or branched C1-C4 alkyl; e) Conversion of the hydroxyl group of the compound (VI) into dimethylamino to give the indolecarboxylate (VII), in which R means a straight or branched C1-C4 alkyl; f) Ssaponification of the 2-carboalkoxy group of the compound (VII), to provide indolecarboxylic acid (VIII); g) Ddecarboxylation of the indolecarboxylic acid (VIII), to provide zolmitriptan and, eventually, to provide a pharmaceutically acceptable salt thereof.
C07D 263/04 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
63.
PROCESS FOR OBTAINING A VALSARTAN SALT USEFUL FOR OBTAINING VALSARTAN
The invention relates to a new salt of Valsartan, in particular to the high-purity dilithium salt of Valsartan, its polymorphs and solvates or hydrates thereof, useful for obtaining Valsartan with a high yield. The process for obtaining the dilithium salt of Valsartan (I) comprises i) Coupling of the intermediate (II) with the 2-(1H-tetrazole-5-il)-phenylboronic acid of formula (III), wherein said coupling takes place in the presence of a lithium base, and a mixture of water and water-miscible organic solvent and a palladium catalyst, to give the dilithium salt of Valsartan of formula (I).
A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
The present invention refers to a granule for the preparation of pharmaceutical compositions comprising a core comprising quetiapine or a pharmaceutically acceptable salt thereof as active ingredient and a binder agent, and a coating layer comprising a lubricant agent. In addition, this invention provides new solid pharmaceutical compositions containing quetiapine as well as process for their preparation.
The present invention refers to a process for the synthesis of (1-{1-(R)-(E)-{3-[2-(7-chloro-quinolin-2-yl)-vinyl]-phenyl}-3-[2-(1-hydroxy-1-methyl-ethyl)-phenyl]-propylsulf anylmethyl}-cyclopropyl)-acetic acid or its salts, comprising the reaction between 7-Chloro-2-vinyl-quinoline and a compound of formula (I) wherein X is a halogen atom or a group of formula -OSO2R, wherein R is selected from the group consisting of CF3, tolyl, methyl and F; in the presence of a palladium based catalyst. The invention is also directed to intermediates compounds of the process.
An improved method is provided for preparing a mixed solvate of olanzapine/water/tetrahydrofuran in a proportion of 1:1:1/2. Said improvement is characterised in that said mixed solvate is basically prepared by means of methylation of the N-desmethylolanzapine with dimethyl sulphate, using tetrahydrofuran and water as solvents.
The invention relates to a solid formulation for the oral administration of olanzapine that comprises a core of anhydrous olanzapine Form I or a pharmaceutically acceptable salt thereof and, optionally, pharmaceutically acceptable excipients, said core being coated with a functional polymer that acts as filmogenic agent. The method for obtaining it comprises: i) providing anhydrous olanzapine Form I or a salt thereof and, optionally, pharmaceutically acceptable excipients in solid form; ii) providing a functional polymer that acts as filmogenic agent; iii) preparing a dispersion of said functional polymer in an aqueous medium,- and applying the dispersion obtained in step iii) onto the solid form of step i) .
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
68.
PROCESS FOR OBTAINING VALINE DERIVATIVES USEFUL FOR OBTAINING A PHARMACEUTICALLY ACTIVE COMPOUND
The invention provides a method for obtaining the intermediate (II), useful for manufacturing Valsartan and a drug directed to a treatment of arterial hypertension or heart failure. The process comprises a) Imination of the aldehyde group of a compound (VII) by L-Valine (IV) salts with organic or inorganic bases and a polar solvent or water, where X means halogen or an-OSO2R group, where R is CF3, tolyl, methyl or F; to give an imine-type compound (VIII), where B+ is the protonated form of an organic base or an alkaline cation; b) Reduction of the imine group of the compound (VIII) followed by acidification, to give the compound (VI); and c) N-Acylation of the compound (VI) with valeryl chloride to give the compound (II). Steps a) and b) can be performed in a 'one pot' reaction.
The present invention relates to a method for obtaining Dolasetron that comprises: a) Esterification of the alcohol of formula (IV) with indole-3-carboxylic acid (compound (III)) or a reactive derivative thereof, to give a compound of formula (V), followed by step b) which includes Dieckmann reaction of the intermediate (V), by reaction with a strong organic or inorganic base, to give the intermediate (VI), and step c) which comprises dealcoxycarbonylation of the intermediate (VI) to give Dolasetron base and, if desired, a pharmaceutically acceptable salt thereof, hydrates or solvates of the base of said salt. The invention also relates to the intermediates (V) and (VI), and methods for obtaining them. With the method of the present invention Dolasetron is obtained at industrial scale with good yields, with decreased use of reactants and solvents, while said method is also of greater atomic efficiency.
