Abstract

The subject of the present invention is a transdermal preparation containing pharmaceutically active ingredient, wherein the particles of the active ingredient are coated with highly volatile silicones or a mixture thereof, and these coated particles are dispersed in a gel or cream base. The volatile silicone component is hexamethyldisiloxane and/or octamethyltrisiloxane and/or decamethylpentacyclo-siloxane. A further subject of the present invention is a method for the preparation of such pharmaceutical compositions.

IPC Classes  ?

• A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
• A61K 31/5415 - 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 ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
• A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
• A61K 31/4174 - Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
• A61K 9/06 - OintmentsBases therefor
• A61K 47/02 - Inorganic compounds
• A61K 31/4164 - 1,3-Diazoles
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 9/16 - AgglomeratesGranulatesMicrobeadlets

Abstract

The invention relates to a process for the preparation of 5-chloro-N-({(5-S)-2-oxo3-[4-(3-oxo-morj)holine-4-yl)-phenyl]-1,3-oxazolidine-5-yl}-methyl) thiophen-2-carboxamide having the INN rivaroxaban. The invention also relates to intermediates formed in the above process.

IPC Classes  ?

• 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
• C07D 303/36 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by nitrogen atoms
• 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 265/32 - 1,4-OxazinesHydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms

Abstract

The invention relates to erlotinib salts selected from the group consisting of the maleic acid salt, salicylic acid salt. L-mandelic acid alt. adipinic acid salt. 1.5-naphthalene-disulfonic acid salt. L-pyroglutamic acid salt. 1 -hydroxy-2-naphthoic acid salt, and mandelic acid salt and amorphous and crystalline forms, hydrates and solvates thereof. The erlotinib salts of the present invention are useful in therapy, particularly for the treatment or prophylaxis of non- small cell lung carcinoma and pancreas rarcinoma.

IPC Classes  ?

• C07D 239/94 - Nitrogen atoms
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61P 35/00 - Antineoplastic agents

Abstract

The invention relates to the new co crystals of 5-chloro-N-///5S/-2-oxo-3-/4-/3- oxo-moφholine-4-yl/-phenyl/-l,3-oxazolidine-5-yl/-methyl/-thiophen-2- carboxamide having the INN rivaroxaban formed with oxalic acid and gamma- cyclodextrine. The invention also relates to a process for the preparation of the co crystal of rivaroxaban and oxalic acid of the Formula 2. According to said process amorphous or crystalline rovaroxaban or a hydrate, solvate or co crystal of rivaroxaban is dissolved in an organic solvent, water or a mixture of an organic solvent and water, to the solution oxalic acid is added and the solvent is removed. According to the invention there is also provided a process for the preparation of the co crystal of rivaroxaban and gamma-cyclodextrin of the Formula 3 /wherein n is 0.9-1.1, preferably n=l/. According to said process amorphous or crystalline rivaroxaban or a hydrate, solvate or co crystal of rivaroxaban is dissolved in an organic solvent, water or a mixture of an organic solvent and water, to the solution gamma-cyclodextrine is added and the solvent is removed.

IPC Classes  ?

• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• 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
• A61P 7/02 - Antithrombotic agentsAnticoagulantsPlatelet aggregation inhibitors

Abstract

The invention relates to a process for the preparation of 5-chloro- N- ({(5-S)-2-oxo3-[4-(3-oxo-morj)holine-4-yl)-phenyl]-l,3-oxazolidine-5-yl}-methyl) thiophen-2-carboxamide having the INN rivaroxaban. The process is characterized by the reactions according to claim 1. The invention also relates to intermediates formed in the above process.

IPC Classes  ?

• C07D 303/36 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by nitrogen atoms
• 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

Abstract

The present invention relates to a process for the preparation of dabigatran etexilate of the formula (1) or the pharmaceutically accepted salts thereof.

IPC Classes  ?

• C07D 401/12 - 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 chain containing hetero atoms as chain links

Abstract

The present invention is related to methods for the preparation of pharmaceutically acceptable salts of (+)-7-[4-(4-fluorophenyl)-6- isopropyl-2-(methanesulfonyl-methyl-amino)-pyrimidin-5-yl]-(3R, 5S, 6E)-dihydroxy-hept-6-enoic acid, intermediates thereof and methods for producing said intermediates.

IPC Classes  ?

• C07D 239/42 - One nitrogen atom

Abstract

The present invention is related to intermediates useful in the preparation of pharmceutically acceptable salts of (+)-7-[4-(4- fluorophenyl)-6-isopropyl-2-(methanesulfonyl-methyl-amino)- pyrimidin-5-yl]-(3R,5S)-dihydroxy-hept-6-enoic acid and polymorphs of said intermediates, methods for preparation thereof and use thereof.

IPC Classes  ?

• C07D 239/42 - One nitrogen atom
• A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim

Abstract

The invention relates to non-sulfonic acid type new rasagiline salts, a process for the preparation thereof, pharmaceutical compositions containing said salts and the use thereof for the treatment or prophylaxis of various diseases, namely Parkinson's disease, amnesia, mental disorders, depression, hyperactive syndrome, affective disease, neurodegenerative disease, neurotoxic injury, cerebral ischemy, traumatic head injury, traumatic vertebral injury, schizophrenia, attention defective disorder, multiple sclerosis, withdrawal symptoms or the damage of the optic nerve.

IPC Classes  ?

• C07C 211/42 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of an unsaturated carbon skeleton containing condensed ring systems with six-membered aromatic rings being part of the condensed ring systems
• C07D 275/06 - Heterocyclic compounds containing 1, 2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems with hetero atoms directly attached to the ring sulfur atom
• C07C 59/245 - Saturated compounds having more than one carboxyl group containing hydroxy or O-metal groups
• C07C 65/10 - Salicylic acid
• C07C 59/06 - Glycolic acid
• C07C 309/23 - Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings other than six-membered aromatic rings
• A61K 31/135 - Amines, e.g. amantadine having aromatic rings, e.g. methadone

Abstract

The present invention is related to crystalline forms of rosuvastatin zinc (2:1) salt. The polymorphs are suitable for use as pharmaceutically active ingredients in the treatment of the diseases of the lipid metabolism including hypercholesterolemia, hyperlipidemia, dyslipidemia or atherosclerosis.

IPC Classes  ?

• C07D 239/42 - One nitrogen atom
• A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
• A61P 3/06 - Antihyperlipidemics

Abstract

The present invention is related to a safe and industrially applicable method for the preparation of 2-acetoxy-5-(2-fluoro-α-cyclopropyl- carbonyl-benzyl)-4,5,6,7-tetrahydro-4H-thieno[3,2-c]pyridine in a quality suitable for use as pharmaceutically active ingredient wherein the concentration of the impurities of the Formula.(XXIV) or (XXIVa) is reduced.

IPC Classes  ?

• C07D 495/04 - Ortho-condensed systems
• 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

Abstract

The present invention is related to a method for purifying diatomaceous earth wherein the natural colloidal structure of the material is retained, which comprises preparing a suspension of diatomaceous earth in a liquid wherein diatomaceous earth is insoluble, separating diatomaceous earth from the suspension, treating diatomaceous earth with an inorganic or organic acid, heat-treating the thus obtained product at a temperature not higher than 300°C, subjecting the product obtained to oxidative treatment and drying the purified product. The invention also relates to a product obtainable by the above-mentioned method.

IPC Classes  ?

• C01B 33/12 - SilicaHydrates thereof, e.g. lepidoic silicic acid
• C04B 33/02 - Preparing or treating the raw materials individually or as batches
• A61K 47/02 - Inorganic compounds

Abstract

The object of the present invention is a process for preparing 1-[2-(3- hydroxyadamant-1-yl-amino)acetyl]pyrrolidine-(2S)-carbonitrile of the Formula I, or vildagliptin complexes of the Formula IV, in particular vildagliptin calcium-chloride trihydrate complex of the Formula II starting from (±)-1-[2-(3-hydroxiadamant-1-yl- amino)acetyl]pyrrolidine-2-carbonitrile of the Formula III (racemic base).

IPC Classes  ?

• C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

Abstract

The present invention relates to new salts of febuxostat formed by inorganic or organic acids or bases, to a new polymorh and solvate of febuxostat and the invention relates to their production and their use primarily for the prevention or treatment of gout or hyperuricemia.

IPC Classes  ?

• C07D 277/56 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
• A61K 31/425 - Thiazoles
• A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents

Abstract

The invention is related to the use of the solution of elemental iodine prepared in an organosiloxane solvent as antiseptic or disinfectant agent and formulations suitable for such use.

IPC Classes  ?

• A01N 59/12 - Iodine, e.g. iodophorsCompounds thereof
• A01N 25/02 - Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of applicationSubstances for reducing the noxious effect of the active ingredients to organisms other than pests containing liquids as carriers, diluents or solvents
• A61K 8/20 - HalogensCompounds thereof
• A61K 8/89 - Polysiloxanes
• A61K 33/18 - IodineCompounds thereof
• A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• A01P 1/00 - DisinfectantsAntimicrobial compounds or mixtures thereof
• A61P 31/02 - Local antiseptics

Abstract

The present invention is related to solid pharmaceutical preparations containing diatomaceous earth (diatomite) or a natural mineral mixture containing diatomaceous earth as filler besides the active ingredient and optional other auxiliary agents. A further object of the invention is a method for manufacturing such pharmaceutical preparations.

IPC Classes  ?

• A61K 9/20 - Pills, lozenges or tablets
• A61K 47/02 - Inorganic compounds

Abstract

The present invention relates to a sustained release pharmaceutical composition. Particularly, a sustained release compressed tablet which contains coated compacted granules containing the active ingredient quetiapine and further excipients. If desired, one or more coatings are on the surface of the tablet.

IPC Classes  ?

• A61K 9/20 - Pills, lozenges or tablets
• A61K 31/554 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem

Abstract

The present invention relates to novel polymorphous salts of dabigatran etexilate of the formula 11 and process for the preparation thereof.

IPC Classes  ?

• C07D 401/12 - 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 chain containing hetero atoms as chain links
• A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• A61P 7/02 - Antithrombotic agentsAnticoagulantsPlatelet aggregation inhibitors

Abstract

The invention relates to stabilized pharmaceutical composition comprising pregabalin and a disaccharide or higher polyol as stabilizer and optionally a conventional pharmaceutically acceptable carrier. The stabilized pharmaceutical composition according to the invention is useful in the treatment of a number of diseases such as epilepsy, Alzheimer's disease or Parkinson's disease.

IPC Classes  ?

• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 31/195 - Carboxylic acids, e.g. valproic acid having an amino group

Abstract

The object of the present invention is a process for preparing the 2-acetoxy-5-(2-fluor-α- cyclopropyl-carbonyl-benzyl)-4,5,6,7-tetrahydro-4H-tieno[3,2-c]pyridine (prasugrel) of the formula (I). The process starts form crystalline 5-trityl-4,5,6,7-tetrahydro-tieno[3,2- c]pyridine of the formula (VI). Further objects of the present invention are two novel crystalline forms of 5-trityl-4,5,6,7- tetrahydro-tieno[3,2-c]pyridine of the formula (VI) and the use thereof for preparing the compound of the formula (V) and process preparing thereof.

IPC Classes  ?

• C07D 495/04 - Ortho-condensed systems

Abstract

The object of the present invention is a one-pot process for preparing the 2-acetoxy-5-(2-fluoro-α-cyclopropyl-carbonyl-benzyl)-4,5,6,7-tetrahydro-4H-tieno[3,2-c]-pyridine (prasugrel) of the formula (I) by reacting the 5,6,7,7a-tetrahydro-4H-tieno[3,2-c]-pyridine-2-on of the formula (II) with 2-bromo-1-cyclopropyl-2-(2-fluorophenyl)-etanone of the formula (III) or with 2-chloro-l-cyclopropyl-2-(2-fluorphenyl)-etanone of the formula (IIIa) and acetylating of the formed compound of the formula (IV), wherein the reaction is carried out in the presence of an organic base with an acetylation agent without isolating the compound of the formula (IV). The coupling and acetylation are carried out in the presence of the same organic base such as triethylamine, N,N-diisopropyl-ethylamine or pyridine. At the end of the process the prasugrel of the formula (I) is purified by recrystallization from an organic solvent or a mixture of solvents.

IPC Classes  ?

• C07D 495/04 - Ortho-condensed systems

Abstract

The present invention relates to the use of novel vildagliptin complexes for the manufacture of high purity vildagliptin of Formula I and/or pharmaceutical acceptable salts thereof. Further objects of the present invention are pharmaceutically acceptable complexes of vildagliptin and/or amorphous and crystalline forms, anhydrous forms, amorphous and crystalline hydrates, amorphous and crystalline solvates of the complexes and a process for the preparation thereof. Another object of the present invention is the high purity vildagliptin and pharmaceutically acceptable salts thereof prepared form the vildagliptin complexes of the present invention, a process for the preparation thereof and pharmaceutical compositions containing vildagliptin base, pharmaceutically acceptable salts and/or complexes and use thereof for the treatment of type 2 diabetes (NIDDM). The present invention provides pharmaceutically advantageous high purity vildagliptin complexes.

IPC Classes  ?

• C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• A61K 31/401 - ProlineDerivatives thereof, e.g. captopril
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Abstract

The present invention relates to compounds 2,3,4-benzothiadiazepine-2,2-dioxide derivatives and enantiomers of the general Formula (I) wherein 'a' represents single or double bond, R1 and R2 represent, independently, hydrogen, halogen, cyano, alkyl, alkoxy, trifluoromethyl, or if 'a' represents single bond, R1 and R2 together form =N-S-N= group, R3 and R4 represent, independently, hydrogen, alkyl, alkenyl, cycloalkyl, aryl or aralkyl, R5 and R6 represent, independently, hydrogen, halogen, cyano, alkyl, alkoxy, trifluoromethyl and/or enantiomers and/or pharmaceutically suitable acid addition salts thereof. The invention further relates to a process for their preparation, medicaments containing said compounds and the use thereof for the treatment of disorders of the central nervous system.

IPC Classes  ?

• C07D 285/06 - 1,2,3-ThiadiazolesHydrogenated 1,2,3-thiadiazoles
• C07D 285/36 - Seven-membered rings
• C07D 309/24 - Methylol radicals
• A61K 31/554 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
• A61P 25/00 - Drugs for disorders of the nervous system

Abstract

The present invention relates to a process for manufacturing microcrystalline ezetimibe containing granulate, wherein a) ezetimibe is dissolved; b) the dissolved ezetimibe is precipitated with water, which if necessary contains pharmaceutical excipients, preferably lauryl-sulfate derivatives, and c) granulates are formed from the obtained suspension by spraying the suspension onto pharmaceutical excipients. A further aspect of the present invention is the granulate obtained by the present process and the pharmaceutical composition containing such granulate.

IPC Classes  ?

• A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/50 - Microcapsules
• A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

The present invention relates to crystalline Form I rosuvastatin zinc (2:1) salt, method of preparation thereof and use thereof as pharmaceutically active ingredient for the treatment of diseases related to lipid metabolism including hyperlipoproteinemia, hypercholesteremia, dyslipidemia and atherosclerosis.

IPC Classes  ?

• C07D 239/42 - One nitrogen atom
• A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
• A61P 3/06 - Antihyperlipidemics

Abstract

The object of the present invention is an osmotic component, stabilizer and wetting agent containing laxative suppository, wherein the osmotic component and the stabilizer is PEG 200 and/or a polyethylene glycols with higher molecular weight.

IPC Classes  ?

• A61K 9/02 - SuppositoriesBougiesBases for suppositories or bougies

Abstract

Rosuvastatin salts and method for preparation thereof FORMULA (II). The present invention relates to (E)-(+)-7- [4-(4-fluorophenyl)-6- isopropyl-2-(methansulfonyl-methylamino)-pyrimidin-5-yl]-(3R,55)- dihydroxy-hept-6-enoic acid salts formed with transition metals. Iron, copper, zinc and manganese salts of rosuvastatin of the general Formula (II) are suitable as pharmaceutically active ingredients for the preparation of medicaments for the treatment of the diseases of the lipid metabolism.

IPC Classes  ?

• C07D 239/42 - One nitrogen atom
• A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
• A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

1-4 alkyl group, having a straight or branched chain. The process can be applied preferably on industrial scale. Compound of formula (II), wherein R represents a fluorine atom in position 2 is an intermediate of the preparation process of prasugrel, which is a platelet inhibitor used in the therapy.

IPC Classes  ?

• C07D 495/04 - Ortho-condensed systems
• C07C 45/45 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by condensation
• 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

Abstract

The subject of the present invention is a transdermal preparation containing pharmaceutically active ingredient, wherein the particles of the active ingredient are coated with highly volatile silicones or a mixture thereof, and these coated particles are dispersed in a gel or cream base. The volatile silicone component is hexamethyldisiloxane and/or octamethyltrisiloxane and/or decamethylpentacyclo-siloxane. A further subject of the present invention is a method for the preparation of such pharmaceutical compositions.

IPC Classes  ?

• A61K 9/14 - Particulate form, e.g. powders
• A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
• A61K 31/5415 - 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 ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
• A61K 31/19 - Carboxylic acids, e.g. valproic acid
• A61K 31/195 - Carboxylic acids, e.g. valproic acid having an amino group
• A61K 31/4164 - 1,3-Diazoles
• A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
• A61K 31/04 - Nitro compounds
• A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
• A61P 37/08 - Antiallergic agents
• A61P 31/04 - Antibacterial agents
• A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
• A61K 9/06 - OintmentsBases therefor
• A61K 47/02 - Inorganic compounds
• A61K 31/4174 - Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 9/16 - AgglomeratesGranulatesMicrobeadlets

Abstract

The present invention relates to semisolid transdermal pharmaceutical preparation having enhanced stability and bioavailability, wherein the particles are coated by a volatile silicon oil component and the thus obtained suspension is dispersed in a gel or cream base.

IPC Classes  ?

• A61K 9/06 - OintmentsBases therefor
• A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• A61K 9/50 - Microcapsules
• A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers

Abstract

The invention relates to an apparatus and method for testing transdermal medicaments, wherein the sample tested in a membrane penetration cell resides in the open sample compartment of said cell and is exposed to environmental factors such as temperature, air flow, light and air humidity during testing the absorption and penetration.

IPC Classes  ?

• G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing

Abstract

The present invention relates to the enantiomers of 5,7-dichloro-3-{4-[4-(4- chlorophenyl)-piperazin-1-yl]butyl} -3-ethyl- 1,3-dihydro-2H-indol-2-one of the Formula (II) pharmaceutically acceptable salts thereof, process for the preparation thereof, medicinal products containing said enantiomers and the use thereof and their pharmaceutically acceptable salts in the treatment of the disorders of the central nervous system.

IPC Classes  ?

• C07D 209/34 - Oxygen atoms in position 2
• A61K 31/4045 - Indole-alkylaminesAmides thereof, e.g. serotonin, melatonin
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia

Abstract

The present invention relates to a new process for the preparation of rosuvastatin [7-[4-(4-Fluorophenyl)-6-isopropyl-2- (methanesulphonyl-methyl-amino)-pyrimidin-5-yl]-(3R,51S)- dihydroxy-hept-6-enoic acid] of the formula (I) salts formed with bivalent cations, preferably with calcium or zinc ions, characterized in that rosuvastatin tert.-butylammonium salt is reacted with the appropriate bivalent cation, preferably with calcium or zinc ions in a mixture of a water immiscible or slightly miscible organic solvent and water and the formed salt is isolated.

IPC Classes  ?

• C07D 239/42 - One nitrogen atom
• A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
• A61P 3/06 - Antihyperlipidemics

Abstract

The subject of the invention is a vaginal suppository with improved efficacy containing an antifungal active ingredient, wherein the said active ingredient is present simultaneously in dissolved and suspended form in the suppository base containing polyethylene-glycol and polysorbate. The ratio of the suspended and dissolved active ingredient in the suppository is reproducible and said ratio does not change during the storage. A further subject of the present invention is a process for manufacturing said pharmaceutical formulations.

IPC Classes  ?

• A61K 9/02 - SuppositoriesBougiesBases for suppositories or bougies
• A61K 31/4164 - 1,3-Diazoles

Abstract

Stable solid pharmaceutical composition containing amlodipine or pharmaceutical acceptable salts thereof and bisoprolol or pharmaceutical acceptable salts thereof as well as pharmaceutically accepted excipients, packaged in a damp- proof package and further comprising less than 0.5 % of the compound of the formula (3) based on the weight of the active ingredients.

IPC Classes  ?

• A61K 9/20 - Pills, lozenges or tablets
• A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
• A61K 31/4422 - 1,4-Dihydropyridines, e.g. nifedipine, nicardipine

Abstract

The present invention is related to a method for the preparation of N-methyl-aryloxy-propanamine derivatives, which comprises reacting a suitable uretane derivative of the Formula (XXIV) with a Grignard reagent.

IPC Classes  ?

• C07C 213/02 - 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 involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
• C07C 333/20 - Esters of dithiocarbamic acids having nitrogen atoms of dithiocarbamate groups bound to hydrogen atoms or to acyclic carbon atoms
• C07C 217/20 - 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 a carbon atom of a six-membered aromatic ring the six-membered aromatic ring or condensed ring system containing that ring being further substituted by halogen atoms, by trihalomethyl, nitro or nitroso groups, or by singly-bound oxygen atoms

Abstract

The present invention relates to the process for the preparation of 1-(3,4-dimethoxy-phenyl)-5-ethyl-7,8-dimethoxy-4-methyl-5H-2,3-benzodiazepine of the Formula (I) by reacting 3,4,3',4'-tetramethoxy-6-(α-aceto-propyl)-benzofenon of the general Formula (II) with hydrazine or hydrazine-hydrate in alcoholic medium, and isolating and purifying the reaction product with a clarifier, which comprises using during the clarifying step a recrystallization solution having an iron content lower than 7 ppm.

IPC Classes  ?

• C07D 243/02 - Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 2

Abstract

The present invention relates to a process for the preparation of cyclohexanol derivatives of the general formula (I), wherein R stands for a hydrogen atom or a methyl group, in a one-step process from a cyano compound of the general formula (II).

IPC Classes  ?

• C07C 213/02 - 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 involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
• C07C 215/64 - 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 rings other than six-membered aromatic rings being part of the carbon skeleton
• C07C 217/74 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified 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 rings other than six-membered aromatic rings being part of the carbon skeleton

Abstract

The present invention relates to new polymorph and amorphous forms of desvenlafaxine fumarate of the chemical formula (II). and I or III, or IV polymorph forms, of desvenlafaxine fumarate monohydrate and processes for the preparation thereof.

IPC Classes  ?

• C07C 215/64 - 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 rings other than six-membered aromatic rings being part of the carbon skeleton
• A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
• A61P 25/24 - Antidepressants

Abstract

The invention relates to a process for the preparation of compounds of general formula (III), wherein R represents fluorine or chlorine atom and X represents chlorine or bromine atom, by halogenation of cyclopropyl benzyl ketone of general formula (II), wherein R represents fluorine or chlorine atom and the halogenation is carried out in the mixture of aqueous hydrogen halide and aqueous hydrogen peroxide in the presence of a water miscible solvent or in the presence of a phase transfer catalyst; or the halogenation is carried out in the mixture of sulfuric acid and an alkali metal salt of aqueous hydrogen halide. The process can be applied preferably on industrial scale.

IPC Classes  ?

• 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
• C07D 495/04 - Ortho-condensed systems
• C07C 49/567 - Unsaturated compounds containing keto groups bound to rings other than six-membered aromatic rings containing halogen

Abstract

The present invention provides an improved process for the preparation of (+)-7-[4-(4-fluorophenyl)-6-isopropyl-2-(methanesulfonyl-methyl-amino)-pyrimidin-5-yl]-(3R,5S)- dihydroxy-hept-6-enoic acid and sodium salt thereof. A further subject of the present invention is high purity (+)-7-[4-(4-fluorophenyl)-6-isopropyl-2-(methanesulfonyl-methyl-amino)-pyrimidin-5-yl]-(3R,5S)-dihydroxy-hept-6-enoic acid sodium salt and process for the preparation thereof. The compound of the general Formula (I) and sodium salt thereof are valuable pharmaceutical intermediates during the production of high purity pharmaceutically active ingredients suitable for the regulation of lipid metabolism.

IPC Classes  ?

• C07D 239/42 - One nitrogen atom

Abstract

The subject of the present invention is an improved process for the preparation of (+)-7-[4-(4-fluorophenyl)-6-isopropyl-2-(methanesulfonyl-methyl-amino)-pyrimidin-5-yl]-(3i-,55)-dihydroxy-hept-6-enoic acid zinc salt (2:1), which allows the reproducible manufacture of said compound on industrial scale in high purity. The compound of the Formula (I) can be used for the treatment of diseases related to lipid metabolism.

IPC Classes  ?

• C07D 239/42 - One nitrogen atom

Abstract

The subject of the present invention is a transdermal preparation containing pharmaceutically active ingredient, wherein the particles of the active ingredient are coated with highly volatile silicones or a mixture thereof, and these coated particles are dispersed in a gel or cream base. The volatile silicone component is hexamethyldisiloxane and/or octamethyltrisiloxane and/or decamethylpentacyclo-siloxane. A further subject of the present invention is a method for the preparation of such pharmaceutical compositions.

IPC Classes  ?

• A61K 31/00 - Medicinal preparations containing organic active ingredients
• A61K 9/06 - OintmentsBases therefor
• A61K 47/02 - Inorganic compounds
• A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates

Abstract

The present invention relates to new selective 5HT6 receptor binding benzofuran derivatives of general formula (I) wherein, Z represents a hydrogen atom, C1-4 acyl group, C1-6 alkyl sulfonyl group, phenyl sulfonyl group substituted with one or more halogen atom; or naphthyl sulfonyl group optionally substituted with a halogen atom, tetrahydro naphthyl sulfonyl group, (lS)(+)-10-camphor-sulfonyl group, (lR)(-)-10-camphor-sulfonyl group or benzofuranyl sulfonyl group, substituted with a halogen atom and C1 -4 alkyl group, Y represents C2-6 alkylene group, R1 and R2 represent, independently, a hydrogen atom, C1-4 alkyl group, benzyl group, or together with one or more halogen atoms, trifluoromethyl group, or C1-4 alkoxy group substituted 4-phenyl-piperazine-l-yl group; and/or their pharmaceutically suitable acid addition salts, to the process for producing said compounds, to pharmaceutical compositions containing said compounds and to their use in treatment and/or prevention of disorders of the central nervous system and cardiovascular system.

IPC Classes  ?

• 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
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• C07D 307/83 - Oxygen atoms
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 25/00 - Drugs for disorders of the nervous system

Abstract

The present invention relates to a controlled release pharmaceutical composition in a layered pellet form containing carvedilol, wherein the pellet contains a core (1) containing a solid organic acid, a primery coating layer (2), an acid dissolution controlling layer (3), a layer (4) containing the active ingredient and a further enteric layer (5).

IPC Classes  ?

• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/50 - Microcapsules

Abstract

The present invention relates to solid dosage forms (tablets film-tablets, capsules) containing clopidogrel hydrogensulphate of the polymorph form 1.

IPC Classes  ?

• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/28 - DrageesCoated pills or tablets

Abstract

Process for the preparation of a desloratadine adduct forme with carbon dioxide of the formula: (I)

IPC Classes  ?

• C07D 401/04 - 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 directly linked by a ring-member-to-ring- member bond

Abstract

(I) The present invention relates to new benzo[1,2,3]thiadiazine-1,1 dioxide derivatives of the general Formula (I), medicament containing such compounds and the use thereof in the medicin Benzo[1,2,3]thiadiazine-1,1-dioxide derivatives of the gener Formula (I) are suitable for the prevention or treatment of the disease of the central nervous system.

IPC Classes  ?

• C07D 285/16 - ThiadiazinesHydrogenated thiadiazines
• A61K 31/549 - 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 having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
• A61P 25/00 - Drugs for disorders of the nervous system

Abstract

(I) The present invention is related to new 3,4-dihydroberizo[1,2,3]thiadiazine-1,1-dioxide derivatives of the Formula (I), medicaments containing said new compounds, process for the preparation thereof and the use of said derivatives in the medicine. The compounds according to the present invention are suitable for the treatment or prevention of disorders of the central nervous system.

IPC Classes  ?

• C07D 285/15 - Six-membered rings
• 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

Abstract

The invention relates the use of 4-chloro-5-{2-[4-(6-fluoro-1,2- benz[d]isoxazole-3-yl)piperidin-1-yl]ethyl-amino}-2-methyl-3- (2H) pyridazinone of the Formula (I) or pharmaceutically acceptable salts thereof for the preparation of medicaments suitable for the improvement of cognitive function or obtaining neuroprotective effect. The medicaments containing 4-chloro-5-{2-[4-(6-fiuoro-1,2- benz[d]isoxazol-3-yl)piperidin-1-yl]ethyl-amino}-2-methyl-3- (2H) pyridazinone of the Formula (I) or therapeutically acceptable salt thereof can be used for the treatment or prevention of neuronal death, mental decline, sclerosis multiplex, Creuzfeld-Jacobs disease, Huntingdon- syndrome, amyotrophic lateral sclerosis, Parkinson-disease, memory disturbance, loss of memory, amnesia, stroke or for the improvement of memory function or learning ability.

IPC Classes  ?

• A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

Abstract

The present invention is related to a process for the preparation of a pellet mass, wherein the premix containing one or more pharmaceutically active ingredient(s) is homogenized to obtain a starting powder mixture; spraying a granulating liquid onto said powder mixture, spheronizing, drying and fractionating the thus obtained particles, wherein the starting or partially pelletized powder mixture is blended with seeding pellets having identical or essentially similar composition but smaller average particle size than the particle size of the desired product fraction of the pellets. The pellets containing potassium chloride active ingredient obtained in the above process or according to a process known from the art can be provided with a controlled-release coating in a rolling-bed apparatus having non-perforated wall.

IPC Classes  ?

• A61K 9/16 - AgglomeratesGranulatesMicrobeadlets

Abstract

The compounds of the general Formula (I), wherein R1 is aryl or alkyl; R2 represents alkyl; R3 represents alkyl or aralkyl, are valuable pharmaceutical intermediates, which can be prepared by reacting a compound of the general Formula (IV) (wherein the definitions of R1 and R2 are as above), with at least 2 molar equivalents of the compound of the general Formula (VI) (wherein X represents halogen or tertiary butyloxycarbonyloxygroup and R3 is as defined above). The known compounds of the general Formula (II) (wherein R1 and R2 are as defined above) are prepared by reacting the compounds of the general Formula (I) with thionyl chloride. The compounds of the general Formula (I) are new intermediates useful in the synthesis of pharmaceutically active ingredients, particularly in the preparation of ACE-inhibitors, e.g. enalapril, perindopril or ramipril.

IPC Classes  ?

• C07C 269/04 - 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 from amines with formation of carbamate groups
• C07C 271/22 - 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 carboxyl groups
• C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07D 209/52 - Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
• C07D 263/44 - Two oxygen atoms
• C07K 5/06 - Dipeptides

Abstract

The present invention is related to rosuvastatin zinc salt of the Formula (I), process for preparation thereof and medicinal products containing said salt. Rosuvastatin zinc salt according to the present invention is prepared by reacting rosuvastatin with a zinc alcoholate, zinc enolate or an inorganic or organic zinc salt and isolating the thus obtained rosuvastatin zinc salt (2:1).

IPC Classes  ?

• C07D 239/42 - One nitrogen atom
• A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
• A61P 3/06 - Antihyperlipidemics

Abstract

The present invention is related to rosuvastatin zinc salt of the Formula (I), process for preparation thereof and medicinal products containing said salt. Rosuvastatin zinc salt according to the present invention is prepared by reacting rosuvastatin with a zinc alcoholate, zinc enolate or an inorganic or organic zinc salt and isolating the thus obtained rosuvastatin zinc salt (2:1).

IPC Classes  ?

• A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
• A61P 3/06 - Antihyperlipidemics
• C07D 239/42 - One nitrogen atom

Abstract

The subject of the present invention is the provision of new salts of duloxetine of the Formula (I) with organic acids, process for their preparation and medicinal products containing thereof. The new salts are essetially free from the impurity of the Formula (II) and possess high purity and high stability. The new duloxetine salts are prepared by reacting duloxetine free base dissolved in an organic solvent with an approximately equimolar amount of an organic acid. Particularly advantageous crystalline salts are those formed with fumaric acid, citric acid or (-)-mandelic acid.

IPC Classes  ?

• A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• C07D 333/20 - Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms

Abstract

The present invention relates to a process for the preparation of 2-⏧4-(&agr;-phenyl-p-chlorobenzyl)-piperazin-1-yl]-ethoxy}-acetic acid-N,N-dimethylamide of the Formula (I) and enantiomers thereof. The compound of the Formula (I) or enantiomers thereof are important pharmaceutical intermediates suitable for direct transformation into non-sedating antihistamine type pharmaceutical active ingredients cetirizine and levocetirizine.

IPC Classes  ?

• C07D 295/088 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain

Abstract

The present invention is related to l-⏧(4-chlorophenyl)-phenylmethyl]-4-(2,2,2-trichloroethoxycarbonyl)-piperazine of the Formula (IV) and optically isomers thereof, process for preparation thereof and the use of the compound of the Formula (IV) in the preparation of l-(4-chlorophenyl)-phenylmethyl-piperazine and optical isomers and salts thereof. l-(4-chlorophenyl)-phenylmethyl-piperazine and optical isomers thereof are important intermediates in the preparation of non-sedating antihistamine-type active pharmaceutical ingredients.

IPC Classes  ?

• C07D 295/06 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals
• C07D 295/18 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof

Abstract

According to the present invention, 2-chloroethoxy-acetic acid-N,N-dimethylamide of the Formula (I) is prepared by reacting 2-hydroxyethoxy-acetic acid-N,N-dimethylamide of the Formula (II) in a solvent optionally in the presence of a catalyst with thionyl chloride and removing the solvent by distillation.

IPC Classes  ?

• C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
• C07C 235/06 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms

Abstract

The invention relates to a process for the preparation of 2 -methyl-4 - (4-methylpiperazin- 1-yl) - 10H- thieno- ⏧2 , 3 -b] ⏧1 , 5] benzodiazepine (olanzapine) of the formula (I) by reacting 4-amino-2-methyl-10H-thieno ⏧2,3- b] ⏧1/5] benzodiazepine hydrochloride of the formula (II) with N-methylpiperazine in an organic solvent, which comprises carrying out the reaction in the mixture of toluene and 1, 3-dimethyl-2- imidazolidinone . The invention also encompasses new 2-methyl-4- (4-methylpiperazin-l-yl) -10H-thieno ⏧2,3- b] ⏧1,5] benzodiazepine dihydrochloride trihydrate of the formula (IB) , the preparation thereof and pharmaceutical compositions comprising said new compound.

IPC Classes  ?

• C07D 495/04 - Ortho-condensed systems
• A61K 31/5513 - 1,4-Benzodiazepines, e.g. diazepam

Abstract

The present invention relates to a controlled release pharmaceutical composition in a layered pellet form containing carvedilol. The composition contains a core containing a solid organic acid, an enteric coating layer on the core, a layer containing carvedilol and a water-soluble adhesive on the surface of the enteric coating, and a dissolution controlling layer containing a mixture of a water-soluble and an enteric polymers.

IPC Classes  ?

• A61K 9/50 - Microcapsules
• A61K 31/403 - 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 carbocyclic rings, e.g. carbazole

Abstract

The present invention relates to a new crystalline polymorph B-52 form of atorvastatin hemicalcium salt ⏧A ⏧(3R, 5R) -7 - ⏧3-phenyl-4 - ⏧ (phenyl carbamoyl] -2- (4 -fluorophenyl) -5- (1-methyletliyl) -IH- pyrrole-1-yl] -3, 5-dihydroxy-heptanoic acid calcium salt (2:1)] , medicinal preparations containing the new polymorph form, process for the preparation thereof and the use of the new polymorph form for the preparation of medicinal products .

IPC Classes  ?

• C07D 207/34 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
• 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
• A61P 3/06 - Antihyperlipidemics