The invention pertains to pharmaceutical compositions containing a GIP (glucose-dependent insulino-tropic polypeptide) and GLP-1 (Glucagon-like peptide-1) receptor agonist. In particular, the invention provides pharmaceutical compositions containing tirzepatide. The pharmaceutical compositions according to the invention are physically and chemically stable, are easy to manufacture and suitable for parenteral administration. The invention further provides methods for making the same as specified in the claims.
The invention relates to a veterinary composition for topical application to the skin comprising a) an isoxazoline compound, b) optionally, a macrocyclic lactone compound, c) one or more penetration enhancers, d) optionally, one or more veterinary acceptable solvents, e) optionally, one or more veterinary acceptable cosolvents, and f) optionally, one or more antioxidants.
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
A01N 25/22 - 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 ingredients stabilising the active ingredients
A01N 25/32 - Ingredients for reducing the noxious effect of the active substances to organisms other than pests, e.g. toxicity reducing compositions, self-destructing compositions
A01N 43/80 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms, as ring hetero atoms five-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,2
A01N 43/90 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
3.
FIXED COMBINATION OF TELMISARTAN, AMLODIPINE AND INDAPAMIDE FOR THE TREATMENT OF HYPERTENSION
The present invention relates to a fixed combination medicinal product that is highly efficient and safe when being used in treating essential hypertension or/and reducing the risk of development of a condition associated with essential hypertension, and that additionally ensures excellent patient compliance. The fixed combination medicinal product comprises (a) telmisartan at a dose of 40 mg, amlodipine at a dose of 5 mg, and indapamide at a dose of 1.5 mg for modified release or at a dose of 2.5 mg for immediate release, (b) telmisartan at a dose of 80 mg, amlodipine at a dose of 5 mg, and indapamide at a dose of 1.5 mg for modified release or at a dose of 2.5 mg for immediate release, or (c) telmisartan at a dose of 80 mg, amlodipine at a dose of 10 mg, and indapamide at a dose of 1.5 mg for modified release or at a dose of 2.5 mg for immediate release. The fixed combination medicinal product is administered once or twice, preferably once a day and is used as (α) a first-line antihypertensive therapy for a hypertensive patient, (β) a second-line antihypertensive therapy for a hypertensive patient who is a non-responder to a previous antihypertensive therapy, or (γ) a substitution antihypertensive therapy for a hypertensive patient whose blood pressure is adequately controlled by a previous antihypertensive therapy.
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
4.
Bilayer tablet formulation comprising dapagliflozin and metformin
The present invention relates to a bilayer tablet comprising metformin extended release formulation as the first layer and dapagliflozin formulation as the second layer, wherein both layers comprising hydroxypropyl cellulose as a binder. The invention also relates to a process for the manufacturing of the said tablet.
The invention relates to a pharmaceutical composition comprising benzydamine hydrochloride and cetylpyridinium chloride. The composition comprises a soft core and an outer layer surrounding the soft core.
The present invention relates to a monolayer tablet for immediate release, a method of manufacturing the monolayer tablet, and the use of the monolayer tablet in treating essential hypertension or/and reducing the risk of development of a condition associated with essential hypertension. The monolayer tablet comprises (a) an intragranular phase comprising (a1) amorphous telmisartan and (a2) alkaline agent; and (b) an extragranular phase comprising (b1) one or more other antihypertensive agents selected from amlodipine, hydrochloro- thiazide and indapamide, and (b2) disintegrant.
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A61K 31/4422 - 1,4-Dihydropyridines, e.g. nifedipine, nicardipine
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
The present invention relates to a tablet composition comprising granules, characterized in that granules comprise a solid dispersion of enzalutamide and a concentration enhancing polymer on a carrier and a process for its preparation.
The invention relates to a solid dispersion comprising Vericiguat and a polymer matrix. The solid dispersion is preferably prepared by hot melt extrusion or melt granulation. The invention further relates to pharmaceutical dosage forms comprising the solid dispersion.
The invention relates to an improved process for the preparation of substituted chalcones using a base that plays double role in the process, as it removes free water and catalyzes aldol condensation. Consequently, the process is cost efficient and is easily scalable to industrial level. The substituted chalcones are useful intermediates in the synthesis of isoxazolines such as Fluralaner, Afoxolaner and Sarolaner, which are known systemic insecticides and acaricides.
C07C 67/343 - Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by isomerisationPreparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by change of size of the carbon skeleton by increase in the number of carbon atoms
C07C 69/76 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring
C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
C07C 237/22 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
The invention relates to veterinary compositions comprising Oclacitinib. Preferably, the compositions are prepared by granulation and comprise an intragranular phase as well as an extragranular phase.
C12P 17/18 - Preparation of heterocyclic carbon compounds with only O, N, S, Se, or Te as ring hetero atoms containing at least two hetero rings condensed among themselves or condensed with a common carbocyclic ring system, e.g. rifamycin
C12P 41/00 - Processes using enzymes or microorganisms to separate optical isomers from a racemic mixture
C07D 249/00 - Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
29 KRK0017-WO Abstract: The invention relates to physiologically acceptable acid addition salts of Ribociclib and pharmaceutical compositions thereof. In particular, the invention relates to tablet formulations containing Ribociclib malate monohydrate, Ribociclib hydrochloride dihydrate or Ribociclib hydrochloride anhydrate.
The invention relates to an oral pharmaceutical dosage form, which is a bilayer tablet comprising a first layer and a second layer, wherein the pharmaceutical dosage form comprises (i) valsartan or a physiologically acceptable salt thereof; preferably wherein the pharmaceutical dosage form provides conventional release of valsartan or the physiologically acceptable salt thereof; and (ii) indapamide or a physiologically acceptable salt thereof; preferably wherein the pharmaceutical dosage form provides modified release of indapamide or the physiologically acceptable salt thereof. The invention further relates to a process for preparing such pharmaceutical dosage form.
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
RRN,NRRN,NN,N,2-trimethylpentan-1-amine or salts thereof in crystal form at high purity level as well as its use in the manufacture of highly pure tapentadol. By consequence, highly pure tapentadol is also provided in yet another aspect of the invention.
C07C 213/10 - SeparationPurificationStabilisationUse of additives
C07C 215/54 - 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 linked by carbon chains having at least three carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
C07C 217/62 - 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 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 singly-bound oxygen atoms linked by carbon chains having at least three carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
The invention relates to a soft chewable veterinary dosage form comprising (a) at least one active agent; (b) a humectant selected from sorbitol, preferably in combination with propylene glycol, liquid polyethylene glycol, glycerol or liquid paraffin; and at least one additional excipient selected from the group of (c) forming agent; (d) filler; (e) a liquid component; and (f) flavor.
The present invention relates to a process for purification of linagliptin. Furthermore, the present application pertains to linagliptin purified by this process, as well as to a novel compound and its use.
C07D 473/06 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
The present invention relates to a pharmaceutical composition comprising apremilast, as well as to a process for the preparation thereof. Furthermore, the present invention pertains to a method for crystallizing apremilast, and to apremilast obtainable by this method. Furthermore, apremilast and pharmaceutical compositions for use as a medicament are disclosed.
C30B 1/02 - Single-crystal growth directly from the solid state by thermal treatment, e.g. strain annealing
C30B 7/14 - Single-crystal growth from solutions using solvents which are liquid at normal temperature, e.g. aqueous solutions the crystallising materials being formed by chemical reactions in the solution
SYNTHESIS OF (1R,2S,5S)-N-((S)-1-CYANO-2-((S)-2-OXOPYRROLIDIN-3-YL)ETHYL)-3-((S)-3,3-DIMETHYL-2- (2,2,2-TRIFLUOROACETAMIDO)BUTANOYL)-6,6-DIMETHYL-3-AZABICYCLO[3.1.0]HEXANE-2-CARBOXAMIDE
The invention relates to a process for the synthesis of (1R,2S,5S)-N-((S)-1-cyano-2-((S)-2-oxopyrroli- din-3-yl)ethyl)-3-((S)-3,3-dimethyl-2-(2,2,2-trifluoroacetamido)butanoyl)-6,6-dimethyl-3-azabicy- clo[3.1.0]hexane-2-carboxamide.
C07D 403/12 - 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 chain containing hetero atoms as chain links
20.
COMBINATION OF CETYLPYRIDINIUM AND BENZYDAMINE WITH VIRUCIDAL EFFECT ON SARS-COV-2
The invention relates to a pharmaceutical dosage form comprising (i) a physiologically acceptable cetylpyridinium salt and (ii) benzydamine or a physiologically acceptable salt thereof for use in the prevention and/or treatment of a coronavirus infection. Preferably, the coronavirus is a severe acute respiratory syndrome-related coronavirus, more preferably a severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2).
The present application relates to a process for purifying a tetrazole-containing-sartan or a tetrazole-containing-sartan intermediate, the process comprising the steps of (a) providing a composition comprising an azide-impurity together with a tetrazole-containing-sartan or with an intermediate of a tetrazole-containing-sartan; (b) treating the composition provided in step (a) with a reducing agent; preferably reacting the azide-impurity with a reducing agent thereby obtaining an amine-impurity; and (c) optionally, isolating the tetrazole-containing-sartan or the intermediate of the tetrazole-containing-sartan from the composition. The application further relates to a process for the synthesis of tetrazole-containing-sartans which ensures azide-impurities free final active pharmaceutical ingredients as well as azide-impurities free intermediates of tetrazole-containing-sartans that are suitable for the subsequent synthesis of tetrazole-containing-sartans.
The invention relates to a bilayer tablet comprising telmisartan in combination with indapamide. Pref- erably, the bilayer tablet provides immediate release of telmisartan and prolonged release of indapamide. The invention also provides a method of producing said bilayer tablet.
The present invention relates to a process for preparing a solid pharmaceutical composition comprising linagliptin and metformin hydrochloride, as well as to the solid pharmaceutical composition obtainable by this process.
The invention relates to a multilayer tablet comprising (i) a naproxen layer containing naproxen or a physiologically acceptable salt thereof and providing immediate release of the naproxen or the physio- logically acceptable salt thereof; and (ii) a paracetamol layer containing paracetamol and providing im- mediate release of the paracetamol. The multilayer tablet is preferably prepared by wet granulation such that the naproxen layer and the paracetamol layer both comprise an extragranular phase and an intragranular phase. Preferably, both extragranular phases contain microcrystalline cellulose. Preferably, the intragranular phase and the extragranular phase of the paracetamol layer both contain a disintegrant, whereas the naproxen layer does not contain disintegrant in any phase. The total content of excipients in both intragranular phases is particularly low.
A61K 9/24 - Layered or laminated unitary dosage forms
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
A61K 9/00 - Medicinal preparations characterised by special physical form
The invention relates to a pharmaceutical formulation comprising a mixture of a first granular compo- sition comprising valsartan disodium salt and a second composition, which is preferably non-granular, comprising or essentially consisting of sacubitril sodium salt. The second composition may be non- granular or granular. The invention further relates to a pharmaceutical dosage form comprising such pharmaceutical formulation and to a process for preparing such pharmaceutical formulation.
A61K 31/216 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
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
26.
PROCESS FOR THE PREPARATION OF RIBOCICLIB AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
The invention relates to the synthesis of Ribociclib, and in particular to the synthesis of a 4-[6-[[7-cyclopentyl-6-(dimethylcarbamoyl)pyrrolo[2,3-d]pyrimidin-2-yl]amino]-3-pyridyl]-piperazine-1-carboxylate, which is an important intermediate in the synthesis of Ribociclib. Further, the invention relates to novel physiologically acceptable salts of Ribociclib.
The invention relates to a tablet comprising Edoxaban and to a process for the manufacture of the tablet. The tablet comprises a core and optionally a coating encapsulating said core, wherein the core comprises Edoxaban, a pharmaceutically acceptable salt and/or solvate thereof; and one or more saccharides selected from glucose, fructose, disaccharides, oligosaccharides, and mixtures thereof; wherein the core does not comprise sugar alcohol.
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
28.
BILAYER TABLET COMPRISING EZETIMIBE AND ATORVASTATIN
The invention relates to solid pharmaceutical dosage forms comprising Ezetimibe and Atorvastatin in separate layers, and to manufacturing methods for making the same. The solid dosage forms are multi- layer tablets, preferably bilayer tablets, suitable for oral administration.
A61K 9/24 - Layered or laminated unitary dosage forms
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 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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
29.
FORMULATION CONTAINING DEXKETOPROFEN AND TRAMADOL AND METHOD FOR MAKING THE SAME
The present invention provides pharmaceutical compositions comprising dexketoprofen and tramadol, which are stable and easy to manufacture. The pharmaceutical compositions of the present invention are characterized by dexketoprofen being provided in an intragranular phase and tramadol being provided in an extragranular phase or vice versa. In addition, the present invention provides a simple method for manufacturing such pharmaceutical compositions. The key aspect of the manufacturing method according to the present invention is the preparation of a granulate containing dexketoprofen or, in another embodiment, tramadol by means of dry granulation, prior to admixing of tramadol, or in the other embodiment dexketoprofen, and optional further excipients. Medical uses of the pharmaceutical compositions of the present invention are also provided.
A metformin starting material for incorporation into a pharmaceutical dosage form comprising metformin or a physiologically acceptable salt thereof, wherein the content of metformin is at least 99.0 wt- %, relative to the total weight of the metformin starting material, wherein the material has a content of dimethylamine of not more than 180 ppm, relative to the weight of metformin, and wherein metformin is present as a powder having a volume median diameter D(50) of not more than 200 um, determined by laser diffraction analysis. A process for the preparation of a metformin starting material, the process comprising the steps of : (i) providing metformin or a physiologically acceptable salt thereof; ( ii) grinding the metformin or physiologically acceptable salt thereof thereby obtaining ground metformin or physiologically acceptable salt thereof; and(iii) subjecting the metformin or physiologically acceptable salt thereof, or the ground metformin or physiologically acceptable salt thereof, to elevated temperature and/or reduced pressure thereby obtaining dried metformin or physiologically acceptable salt thereof. A process for the preparation of a pharmaceutical dosage form comprising metformin or a physiologically acceptable salt thereof and having a content of N-nitroso dimethylamine of not more than 48 ppb, relative to the total weight of metformin in the pharmaceutical dosage form, wherein the process comprises the aforementioned process.
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
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 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
A61K 31/7042 - Compounds having saccharide radicals and heterocyclic rings
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
31.
PREPARATION OF HIGHLY PURE AMORPHOUS DAPAGLIFLOZIN
A novel and improved process for the preparation of amorphous dapagliflozin is disclosed. The present invention further provides pharmaceutical compositions containing amorphous dapagliflozin, optionally in a combination with one or more other active substances and methods for making the same.
Pharmaceutical compositions are provided which contain at least one SGLT2 inhibitor. Specifically, the present invention provides pharmaceutical compositions containing one or more SGLT2 inhibitor such as dapagliflozin, optionally in a combination with one or more other active substances.
COMPOSITION FOR THE PREPARATION OF PERINDOPRIL ARGININE GRANULES, A METHOD FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITION COMPRISING THE GRANULES
The present invention relates to granules comprising perindopril arginine, as well as to a process for the preparation of granules comprising perindopril arginine. Furthermore, the present invention pertains to a pharmaceutical composition comprising granules comprising perindopril arginine.
The invention provides solid pharmaceutical dosage forms and methods for making the same, wherein the pharmaceutical dosage forms comprise Empagliflozin in the form of an amorphous solid solution with at least one polymer. The pharmaceutical dosage forms according to the invention exhibit excellent stability especially in terms of physical stabilization of amorphous form of Empagliflozin.
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
The present invention discloses new pharmaceutical compositions containing a Glucagon-like peptide-1 (GLP-1) analogue optionally in a combination with one or more other active substances. The present invention further provides methods for making the same.
C07D 261/04 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
An analytical method is disclosed for quantitative determination of an Iceland moss herbal preparation in a herbal product, wherein ribitol and/or arabitol is used as an analytical marker.
B01D 15/36 - Selective adsorption, e.g. chromatography characterised by the separation mechanism involving ionic interaction, e.g. ion-exchange, ion-pair, ion-suppression or ion-exclusion
B01D 15/12 - Selective adsorption, e.g. chromatography characterised by constructional or operational features relating to the preparation of the feed
The present invention provides a chewable tablet comprising diosmin, microcrystalline cellulose, mannitol, an acidulant and a flavoring agent and a process for preparing the same.
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 9/14 - VasoprotectivesAntihaemorrhoidalsDrugs for varicose therapyCapillary stabilisers
The present invention relates to pharmaceutical compositions comprising apixaban, and to methods for preparing these pharmaceutical compositions. Furthermore, the present invention pertains to the use of pharmaceutical compositions comprising apixaban as a medicament.
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 present invention discloses new pharmaceutical compositions containing a Glucagon-like peptide-1 (GLP-1) analogue optionally in a combination with one or more other active substances. The present invention further provides methods for making the same.
The present invention relates to process for preparing apixaban, in particular polymorphic form N-1 thereof, as well as to a method for the preparation of crystalline apixaban, especially apixaban polymorphic form N-1.
The present invention relates to processes for the preparation of polymorphic form D2 of robenacoxib and to pharmaceutical formulations thereof. The polymorphic form of robenacoxib obtained by the processes of the present invention is characterized by high polymorphic purity.
C07C 229/42 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to carbon atoms of at least one six-membered aromatic ring and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton with carboxyl groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by saturated carbon chains
A61K 31/196 - Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
A61P 29/02 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
The present invention provides solid pharmaceutical formulations and methods for making the same, wherein the pharmaceutical formulations comprise ticagrelor and is free of water soluble fillers. The pharmaceutical formulations of the present invention exhibit desirable dissolution profiles and are bioequivalent to the marketed composition.
The present invention provides solid pharmaceutical formulations and methods for making the same, wherein the pharmaceutical formulations comprise lenalidomide in the form of a pharmaceutically acceptable salt. The pharmaceutical formulations of the present invention exhibit superior stability especially in terms of disproportionation of the lenalidomide salt: this undesired effect is prevented by incorporating an acid into the formulation and/or by avoiding the use of proton-accepting excipients and/or by selecting a combination of excipients such that the resulting formulation exhibits acidic properties.
The present invention pertains to a process for the preparation of polymorph form X of agomelatine, which comprises providing agomelatine, and crystallizing agomelatine in the presence of at least one of an acid and a salt thereof, and to a polymorph form of agomelatine.
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
46.
PHARMACEUTICAL COMPOSITION CONTAINING AGOMELATINE AND PROCESS FOR THE PREPARATION THEREOF
The present invention relates to a pharmaceutical composition comprising agomelatine, in particular agomelatine in crystalline form, especially agomelatine in in polymorphic form X or I,and a pH modifier and optionally polymeric material, as well as to a process for the preparation thereof.
The present invention is related to a stable topical veterinary composition comprising:• a) selamectin, • b) dimethyl sulfoxide (DMSO) in an amount between 0.5-15% w/v,• c) an organic solvent and • d) optionally an antioxidant.
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
A01N 43/90 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
The present invention relates to novel solid state forms of bilastine, processes for their preparation, and pharmaceutical compositions comprising them.
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
A61K 31/4523 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
The present invention relates to a stable pharmaceutical composition in the form of fast dispersible tablets that comprises tyrosine-kinase inhibitor, which is preferably imatinib or a pharmaceutically acceptable salt thereof. The composition is produced by a simple, reliable, straightforward, cost-effective process and by use of standard pharmaceutical excipients. Fast dispersible tablets obtained according to present invention are dispersible in water and/or other aqueous liquids, characterized with disintegration time of less than 3 minutes using purified water at 15-25 °C, preferably at 25°C.
The object of the present invention is a pharmaceutical tablet composition comprising an NSAID and a PPI and having improved stability and bioavailability. The present invention relates to a pharmaceutical tablet composition comprising: a) a multilayer tablet core comprising: i) a non-steroidal anti- inflammatory drug (NSAID) layer comprising an NSAID and at least one pharmaceutically acceptable excipient; ii) an optional middle layer; iii) a proton pump inhibitor (PPI) layer comprising multiple units of PPI coated with a protective coating; b) a barrier coating surrounding the multilayer tablet core; and c) a gastro-resistant coating surrounding the barrier coating.
PHARMACEUTICAL COMPOSITION COMPRISING CANDESARTAN OR PHARMACEUTICALLY ACCEPTABLE SALTS OR ESTERS THEREOF AND AMLODIPINE OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
The invention relates to a solid pharmaceutical composition comprising candesartan or pharmaceutically acceptable salts or esters thereof and amiodipine or pharmaceutically acceptable salts thereof. More specifically, the invention discloses the pharmaceutical composition comprising at least one portion comprising candesartan cilexetil and at least one another portion comprising amiodipine or pharmaceutically acceptable salts thereof in a fixed dosage form.
The present invention relates to a pharmaceutical composition comprising etoricoxib, at least one pH modifier and optionally at least one additional pharmaceutically acceptable excipient. In particular, the pH modifier is selected from the group of excipients having a pH value of a 1 % (w/v) aqueous dispersion, preferably suspension, above 6.6, preferably above 7.0.
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
53.
PHARMACEUTICAL FORMULATION COMPRISING AN OPIOID AGONIST AND AN OPIOID ANTAGONIST PREPARED BY MELT GRANULATION USING LIPID ESTERS
The present invention provides pharmaceutical formulations containing opioid agonist such as oxycodone and opioid antagonist such as naloxone. These pharmaceutical formulations exhibit satisfactory release properties for both drugs.
The present Invention relates to an improved process for preparation of tadalafil and crystallization and/or purification thereof, wherein the processes are conducted at increased pressure. The invention relates also to a process for preparation of tadalafil co-precipitates and to a solid pharmaceutical composition comprising tadalafil co-precipitates and at least one water soluble diluent and/or water insoluble non-swellable diluent, wherein the composition is substantially free of water insoluble swellable diluents.
The present invention relates to a stable pharmaceutical composition that comprises active substance metformin or a pharmaceutically acceptable salt thereof in combination with DPP- IV inhibitor, which is preferably vildagliptin or a pharmaceutically acceptable salt thereof, which can be produced by a simple, reliable, straightforward, cost-effective process of wet granulation and use of standard pharmaceutical excipients. According to the wet granulation process of the present invention metformin granulate is obtained, to which vildagliptin portion is admixed as in drug particles or granulated form.
The present invention relates to a pharmaceutical composition comprising (a) as the active ingredient, rasagiline in the form of pharmaceutically acceptable salt, (b) diluent, (c) lubricant and/or glidant and optionally (d) disintegrant, (e) binder, wherein the composition is not prepared by wet granulation process. The composition is preferably prepared by direct compression.
The present invention relates to a dermal composition for control of parasitic insects and acarides comprising imidacloprid and permethrin as active ingredients, dimethyl sulfoxide and optionally one or more veterinarily acceptable excipients.
A01N 51/00 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds having the sequences of atoms O—N—S, X—O—S, N—N—S, O—N—N or O-halogen, regardless of the number of bonds each atom has and with no atom of these sequences forming part of a heterocyclic ring
A01N 53/00 - Biocides, pest repellants or attractants, or plant growth regulators containing cyclopropane carboxylic acids or derivatives thereof
58.
HOMOGENOUS PHARMACEUTICAL ORAL DOSAGE FORMS COMPRISING LERCANIDIPINE AND ENALAPRIL OR THEIR PHARMACEUTICALLY ACCEPTABLE SALTS TOGETHER WITH AN ORGANIC ACID
The invention relates to pharmaceutical oral dosage forms of the active substances lercanidipine and enalapril, as well the pharmacologically acceptable salts thereof, characterized in that the pharmaceutical oral dosage forms comprise an organic acid to stabilize both enalapril and lercanidipine, and their pharmaceutically acceptable salts.
The subject of the invention includes a high drug load pharmaceutical composition comprising dronedarone or its pharmaceutically acceptable salts, in particular dronedarone HCI as the active pharmaceutical ingredient, comprising micronized particles of the active ingredient and optionally ionic surfactants.
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
60.
STABLE AQUEOUS FORMULATIONS COMPRISING POORLY WATER SOLUBLE ACTIVE INGREDIENTS
The present invention relates to a formulation comprising one or more active ingredients of poor water solubility for medical or non-medical use in the rearing of animals. The inventive formulation is suitable for administration to the animals via their drinking water. It exhibits superior stability. Said formulation comprises an active ingredient, a thickener combination and water, wherein the thickener combination comprises at least one thickener selected from the following groups A, B, C and D: (A) cellulose derivatives, such as methyl cellulose, sodium carboxy methyl cellulose, (B) non-cellulosic polysaccharide thickeners such as xanthan gums, Arabic gum, (C) cross-linked polyacrylic acid polymers, (D) hydrocolloidal hydrated silicates.
A61K 9/00 - Medicinal preparations characterised by special physical form
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 47/36 - PolysaccharidesDerivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
The invention relates to a process for the manufacture of new polymorph of imatinib base, the preparation of mesylate salt thereof and their inclusion into pharmaceutical compositions which have an improved stability and purity, as well as processes for their preparation.
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
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
The invention describes an improved process for the synthesis of duloxetine and/or pharmaceutically acceptable salts thereof enabling preparation of duloxetine and/or pharmaceutically acceptable salts thereof with high chemical and enatiomeric purity. The process includes addition of an organic acid in the phase of formation of a duloxetine salt with an acid, preferably in the form of hydrochloride, and optionally in the phase of recrystallization of the formed duloxetine salt, wherein an organic acid is preferably selected from the group comprising formic acid, acetic acid, propanoic acid, butanoic acid or any mixtures thereof, more preferably acetic acid.
The invention relates to an improved process for the preparation of valsartan wherein the cycloaddition reaction is performed is an ether as reaction solvent, with a metal salt azide and in the present of zinc halides.
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
64.
EFFICIENT SYNTHESIS FOR THE PREPARATION OF MONTELUKAST AND NOVEL CRYSTALLINE FORM OF INTERMEDIATES THEREIN
The present invention describes the improved process for the preparation of montelukast acid (VII) and its pharmaceutically acceptable salts and esters using a novel synthesis step. The process is cost effective, environment friendly, and easily scale up to commercial level and leads to products having high chemical and optical purity. Moreover, the present invention provides a novel crystalline intermediate (IV) that is useful in this process and a method for its production. In a further aspect, the process of the present invention includes a step of removing ketone by-products be derivatization.
The invention relates to a process with a two-step drying process for the preparation of a granulate comprising valsartan which is used for solid pharmaceutical compositions comprising valsartan and the final oral dosage form.˙
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
66.
NOVEL CRYSTALLINE FORMS OF IVABRADINE HYDROCHLORIDE
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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
The invention relates to rivaroxaban, more particularly to a process for preparation of rivaroxaban or a pharmaceutically acceptable salt or solvate thereof and its crystallization in order to obtain product having desired quality properties.
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
The present invention relates the synthesis of vildagliptin in the presence of phase transfer catalysts; as well as the use of vildagliptin or its pharmaceutically acceptable salts for the preparation of solid oral dosage forms.
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 31/4015 - 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
The invention relates to a preparation and purification processes of solifenacin salts, particularly to a crystallization process of solifenacin succinate, leading to high purity of the obtained product as well as to the desired average particle size and desired modality of the particle size distribution.
C07D 453/02 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
The invention described herein is in the field of separation processes, more particularly, in the field of selective crystallization methods for purification of organic substances.
Pharmaceutical compositions comprising solifenacin or its pharmaceutically acceptable salts as the active pharmaceutical ingredient prepared by dry technological methods, preferably by the direct compression or roller compaction method, i.e. by the process in the absence of a liquid solvent, and the process for their preparation, are disclosed.
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 13/10 - Drugs for disorders of the urinary system of the bladder
73.
PHARMACEUTICAL COMPOSITIONS COMPRISING PRASUGREL BASE OR ITS PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS AND PROCESSES FOR THEIR PREPARATION
The subject of the invention includes a pharmaceutical composition comprising prasugrel or its pharmaceutically acceptable salts as the active pharmaceutical ingredient, prepared in the absence of water and characterized in that they do not contain lactose or mannitol.
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 describes a new process for optical resolution of [N-[[3,4- dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]methyl]-N-methylamine] which is an intermediate in the preparation of ivabradine.
C07C 213/10 - SeparationPurificationStabilisationUse of additives
C07C 217/58 - 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 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 singly-bound oxygen atoms with amino groups and the six-membered aromatic ring, or the condensed ring system containing that ring, bound to the same carbon atom of the carbon chain
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
75.
USE OF AMPHIPHILIC COMPOUNDS FOR CONTROLLED CRYSTALLIZATION OF STATINS AND STATIN INTERMEDIATES
The invention relates to an improved process comprising amphiphilic compounds for the crystallization of an intermediate used in the process for the preparation of statins and statin intermediates.
C07D 405/06 - 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 carbon chain containing only aliphatic carbon atoms
C07D 207/337 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile 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
77.
SOLID PHARMACEUTICAL COMPOSITION COMPRISING AT LEAST ONE STABILIZING AGENT
The present invention is directed to a solid stable pharmaceutical composition comprising desloratadine and at least one stabilizing agent selected from the group consisting of alkali metal hydroxides and alkali earth metal hydroxides and aluminium hydroxide.
The present application pertains to pharmaceutical compositions comprising paliperidone or a pharmaceutically acceptable salt thereof as the active substance, wherein the pharmaceutical composition is in the form of pellets comprising a core particle, optionally one or more intermediate coatings, at least one prolonged release coating and optionally one or more outer coatings, in this order, wherein the active substance is present in the core particle, and wherein the pellets have a maximum diameter of 2 mm or less and exhibit favourable release characteristics.
C07D 453/02 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
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 13/10 - Drugs for disorders of the urinary system of the bladder
The present invention belongs to the field of chemical synthesis and relates to an improved process for the preparation of paliperidone and its pharmaceutically acceptable salts as an active ingredient of a medicament for treatment of schizophrenia. It relates also to a process of crystallization of paliperidone and to the dihydrate form of the compound.
The present invention provides for a solid pharmaceutical composition comprising at least one solid matrix particle comprising paliperidone or a pharmaceutically acceptable salt thereof as an active substance and wherein said solid pharmaceutical composition provides for prolonged release of said active substance.
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
82.
PREPARATION OF DULOXETINE AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS BY THE USE OF ASYMMETRIC TRANSFER HYDROGENATION PROCESS
The invention deals with the preparation of duloxetine or its pharmaceutically acceptable salts with high enantiomeric and chemical purity via beta-keto amines wherein the amino group is optionally protected and the subsequent asymmetric transfer hydrogenation using chiral Ru- or Rh-catalyst to the corresponding alcohol.
This invention relates to improved processes for the production of lipstatin and/or orlistat and means therefore. In particular, the invention relates to microorganisms characterized by abolished or reduced activity of the BKD complex, e.g. mutated branched- chain 2-oxo acid dehydrogenase (BKD) having reduced or abolished activity, nucleotide sequences suitable for achieving reduced or abolished BKD activity, and microorganisms having reduced or abolished BKD activity. The invention in particular relates to lipstatin- producing microorganisms of the genus Streptomyces. Furthermore, this invention relates to the use of these nucleotide sequences, microorganisms or BKD having reduced or abolished activity in the production of lipstatin and/or orlistat.
The present invention relates to a pharmaceutical composition comprising an active core comprising duloxetine or its pharmaceutically acceptable derivatives, a separating layer comprising a pH modifier and a gastro-resistant coating comprising a gastro-resistant polymer selected from methacrylic acid copolymers and optionally an over-coating layer. The present invention also relates to a process for the preparation of duloxetine hydrochloride. It also relates to a packaged medicament.
The present invention provides for a multi particulate matrix system (MPMS) comprising at least one type of particles which contains galantamine or a pharmacologically acceptable salt thereof as an active substance, wherein said at least one type of particles provides for prolonged release of said active substance, and wherein all particles present in the MPMS are uncoated. The present invention further provides for a process for preparing a MPMS.
A61K 9/22 - Sustained or differential release type
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
86.
STABLE SOLID PHARMACEUTICAL COMPOSITION COMPRISING CANDESARTAN OR PHARMACEUTICALLY ACCEPTABLE FORMS THEREOF
The invention relates to a stable solid pharmaceutical composition comprising candesartan or its pharmaceutically acceptable forms and at least one plasticizer selected from the group consisting of phthalate esters, sebacates, alginates, citrate esters, polyacrylate and polymethacrylate polymers, polymers and copolymers of ethylene, vinyl and/or acetate, various sugar alcohols, triacetin, menthol and any mixture thereof.
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
87.
CRYSTALLINE 1-(CYCLOHEXYLOXYCARBONYLOXY) ETHYL 1-((2'-CYANOBIPHENYL-4-YL)METHYL)-2-ETHOXY-1H-BENZO[D]IMIDAZOLE-7-CARBOXYLATE AND A PROCESS FOR ITS PREPARATION
The present invention relates to 1-(cyclohexyloxycarbonyloxy)ethyl 1-((2'-cyanobiphenyl-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate in crystalline form and a process for its preparation, which is useful intermediate in the preparation of candesartan cilexetil. The present invention also relates to the preparation of candesartan cilexetil and pharmaceutical composition comprising candesartan cilexetil.
The present invention relates to a pharmaceutical composition comprising at least one cholesterol absorption inhibitor in amorphous form and at least one hydrophilic polymer, wherein the amorphous cholesterol absorption inhibitor is finely distributed within the hydrophilic polymer or at least one amorphous cholesterol absorption inhibitor and at least one hydrophilic polymer are dispersed onto a carrier.
The present invention relates to the method of preparing of ezetimibe and in particular to novel intermediates for its synthesis and an improved process for preparing such intermediates. Said intermediates may be obtained in high yields and purity in a fast and cost efficient manner. The present invention relates to a novel crystalline form of ezetimibe as well.
C07D 205/08 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
The present invention relates to the synthesis of 1-amino-3,5-dimethyladamantane ('memantine') and its hydrochloric acid salt form. In particular a new intermediate (N-chloro-acetylamino-3,5-dimethyladamantane) for the synthesis of memantine as well as a new process for the preparation of memantine and its hydrochloric acid salt form using said intermediate is disclosed.
C07C 233/06 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
C07C 209/62 - Preparation of compounds containing amino groups bound to a carbon skeleton by cleaving carbon-to-nitrogen, sulfur-to-nitrogen, or phosphorus-to-nitrogen bonds, e.g. hydrolysis of amides, N-dealkylation of amines or quaternary ammonium compounds
C07C 211/38 - 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 a saturated carbon skeleton containing condensed ring systems
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
The present invention relates to novel polymorphic forms of rosiglitazone base, as well as to a process for their preparation and pharmaceutical formulations containing it. The present polymorphic forms of rosiglitazone base are characterized by small average particle sizes and high solubility bestowing the compounds an improved bioavilability.
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/435 - 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
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
The present invention relates to novel polymorphic forms of Ziprasidone sulfates Ziprasidone Hn+ X Z H2O wherein Ziprasidone is a compound of the formula; H is hydrogen; n is 1 or 2; 2- X is HSO4- or SO42-; and Z is O to 30., as well as to a process for their preparation and pharmaceutical formulations containing it. The present polymorphic forms of Ziprasidone sulfates are characterized by small average particle sizes and high solubility bestowing the compounds an improved bioavailability.
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 275/04 - Heterocyclic compounds containing 1, 2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
93.
PROCESS FOR PREPARATION OF 0-DESMETHYLVENLAFAXINE AND ITS ANALOGUES
The present invention belongs to the field of organic chemistry and refers to a process for the preparation of O-desmethylvenlafaxine (l-[2-Dimethylamino)-l-(4-hydroxyphenyl)ethyl]cyclo- hexanol), its analogues and pharmaceutical acceptable salts thereof. The invention also relates to a catalytic hydrogenation of cyano-group of the substituted acetonitrile.
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
C07C 255/37 - Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by etherified hydroxy groups
The present invention pertains to the production of secondary metabolites and particularly to the production of lipstatin. Lipstatin, a potent inhibitor of the pancreas lipase, is reported to be useful in the treatment and/or prevention of obesity and related diseases. The present invention describes a process allowing the production of said enzyme inhibitor in high yields and high purity.
The present invention also pertains to processes for the preparation of form A and form T, which involves dissolving duloxetine hydrochloride in particular solvents and cooling the solution to obtain crystals that are dried.
The present invention concerns preferably surfactant-free solid pharmaceutical formulations comprising, as an active ingredient, at least one of irbesartan and pharmaceutically acceptable salts thereof, and at least one disintegrant. Preferably, the active ingredient comprises irbesartan hydrochloride. Also, the present invention is directed to a process for the manufacture of such formulations, including a wet granulation process (A) and a direct granulation process (B).
The present invention relates to the synthesis of antibacterial compounds such as Chloramphenicol and its analogues Thiamphenicol and Florfenicol and particularly to a new reaction for the preparation of the intermediate compound aminodiolphenylsulfone. This reaction permits the introduction of modified residues to obtain modified antibiotics with an improved stability towards the action of bacterial resistant determinants. In addition, higher purities may be also obtained due to an improved procedure requiring fewer purification steps.
C07C 315/04 - Preparation of sulfonesPreparation of sulfoxides by reactions not involving the formation of sulfone or sulfoxide groups
C07C 317/32 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
98.
PROCESS FOR THE PREPARATION OF CANDESARTAN CILEXETIL
The present invention provides an improved synthesis for the manufacture of candesartan and pharmaceutically acceptable salts and esters thereof as active ingredients of a medicament for the treatment of hypertension and related diseases and conditions which comprises the removal of the tetrazolyl protecting group in an organic solvent, and in the presence of a Lewis acid.
C07D 403/10 - 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 aromatic rings
patents