Patents Assigned to LEK Pharmaceuticals d.d.
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Publication number: 20080188552Abstract: Lovastatin, pravastatin, simvastatin, mevastatin, atorvastatin, and derivatives and analogs thereof are known as HMG-CoA reductase inhibitors and are used as antihypercholesterolemic agents. The majority of them are produced by fermentation using microorganisms of different species identified as species belonging to Aspergillus, Monascus, Nocardia, Amycolatopsis, Mucor or Penicillium genus, some are obtained by treating the fermentation products using the methods of chemical synthesis or they are the products of total chemical synthesis.Type: ApplicationFiled: September 18, 2007Publication date: August 7, 2008Applicant: LEK Pharmaceuticals d.d.Inventor: Zlatko Pflaum
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Publication number: 20080176888Abstract: The present invention relates to a stable pharmaceutical composition comprising sirolimus. The pharmaceutical composition comprises sirolimus in the amorphous form, a fatty acid ester and a pharmaceutically acceptable polymer wherein the fatty acid ester is present at a concentration of less than 10% w/w compared to the total weight of the composition.Type: ApplicationFiled: January 24, 2008Publication date: July 24, 2008Applicant: LEK PHARMACEUTICALS D.D.Inventors: Sebastjan Reven, Igor Legen, Zdenka Jerala-Strukelj
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Publication number: 20080161557Abstract: The invention belongs to the field of organic chemistry and relates to a new process for the purification of olanzapine comprising preparation of acid addition salts of olanzapine and transformation thereof into a pharmaceutically acceptable pure and discoloured final product. The present invention also relates to new processes for the preparation of pure olanzapine.Type: ApplicationFiled: March 17, 2005Publication date: July 3, 2008Applicant: LEK PHARMACEUTICALS D.D.Inventors: Tomaz Mesar, Anton Copar, Hubert Sturm, Johannes Ludescher
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Publication number: 20080118564Abstract: New composition of candesartan cilexetil is prepared using up to 20% of carrageenan which suitably stabilized the active ingredient against degradation during the tableting.Type: ApplicationFiled: January 24, 2006Publication date: May 22, 2008Applicant: LEK PHARMACEUTICALS D.DInventors: Zdenka Jerala-Strukelj, Igor Legen
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Publication number: 20080004256Abstract: The compounds of the formula I and pharmaceutically acceptable salts thereof and a process for preparing the same and pharmaceutical compositions containing the same are described wherein the substituents have the meaning as specified in the description. The compounds are used as thrombin inhibitors.Type: ApplicationFiled: September 12, 2007Publication date: January 3, 2008Applicant: LEK PHARMACEUTICALS D.D.Inventors: Uros Urleb, Anamarija Zega, Mojca Stegnar, Bakija Trampus, Tomaz Solmajer, Gregor Mlinsek
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Patent number: 7285547Abstract: The compounds of the formula (formula 1) and pharmaceutically acceptable salts thereof and a process for preparing the same and pharmaceutical compositions containing the same are described wherein the substituents have the meaning as specified in the description. The compounds are used as thrombon inhibitors.Type: GrantFiled: December 20, 2001Date of Patent: October 23, 2007Assignee: LEK Pharmaceuticals d.d.Inventors: Uros Urleb, Anamarija Zega, Mojca Stegnar, Bakija Alenka Trampus, Tomaz Solmajer, Gregor Mlinsek
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Patent number: 7271269Abstract: Pharmaceutically suitable crystalline and amorphous alkali and earth-alkali salts of 2-n-butyl-4-chloro-5-hidrox-ymethyl-1-[[2?-(1 H-tetrazole-5-yl)[1.1?-biphenyl]-4-yl]-1 Himidazole have been prepared and new manufacturing, purification and isolation procedure for said salts in high purity have been described. Stable pharmaceutical compositions containing new crystalline potassium salts of 2-n-butyl-5-chloro-5hidroxymethyl-1-[[2?-(1H-tetrazole-5-yl)[1.1?-biphenyl]-44-yl]-1H-imidazole have been prepared.Type: GrantFiled: January 29, 2004Date of Patent: September 18, 2007Assignee: Lek Pharmaceuticals D.D.Inventors: Ljubomir Antoncic, Anton Copar, Peter Svete, Breda Husu-Kovacevic, Zoran Ham, Boris Marolt
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Publication number: 20070208071Abstract: The present invention relates to oxidative degradation products of atorvastatin calcium and the process of the preparation thereof. The present invention also relates to atorvastatin calcium substantially free of oxidative degradation products and the pharmaceutical compositions containing such atorvastatin calcium.Type: ApplicationFiled: July 15, 2005Publication date: September 6, 2007Applicant: LEK PHARMACEUTICALS D.D.Inventors: Rok Grahek, Darko Kocjan, Andrej Bastarda, Andrej Kocijan, Matjaz Kracun
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Patent number: 7153970Abstract: 3-ethyl 5-methyl (+/?) 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate benzenesulfonate, containing overall impurities of significantly less than 0.3% is disclosed, as well as process for its preparation, according to which substance of 3-ethyl 5-methyl (+/?) 2-[2-(N-trialkylamino)ethoxymethyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate is converted with benzenesulfonic acid in ethanol solution, at a temperature between 20° C. and reflux temperature, followed by isolation and purification of 3-ethyl 5-methyl (+/?) 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate benzenesulfonate. Amlodipine benzenesulfonate is useful as an antiishemic and antihypertensive agent.Type: GrantFiled: July 5, 2002Date of Patent: December 26, 2006Assignee: Lek Pharmaceuticals d.d.Inventors: Borut Furlan, Marijan Resnik
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Patent number: 7141602Abstract: Lovastatin, pravastatin, simvastatin, mevastatin, atorvastatin, and derivatives and analogs thereof are known as HMG-CoA reductase inhibitors and are used as antihypercholesterolemic agents. The majority of them are produced by fermentation using microorganisms of different species identified as species belonging to Aspergillus, Monascus, Nocardia, Amycolatopsis, Mucor or Penicillium genus, Streptomyces, Actinomadura, Micromonospora, some are obtained by treating the fermentation products using the method of chemical synthesis or they are the products of total chemical synthesis. The purity of the active ingredient is an important factor for manufacturing the safe and effective pharmaceutical, especially if the pharmaceutical product must be taken on a longer term basis in the treatment or prevention of high plasma cholesterol. The accumulation of the impurities from the pharmaceuticals of lower purity may cause many side effects during the medical treatment.Type: GrantFiled: October 30, 2003Date of Patent: November 28, 2006Assignee: LEK Pharmaceuticals d.d.Inventors: Rok Grahek, Dusan Milivojevic, Andrej Bastarda
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Patent number: 7112590Abstract: The invention relates to compounds that are heterocyclic derivatives of dipeptides and dipeptides mimetics and pharmaceutically acceptable salts thereof.Type: GrantFiled: May 4, 2001Date of Patent: September 26, 2006Assignees: LEK Pharmaceuticals d.d., University of Ljubljana, Faculty of PharmacyInventors: Danijel Kikelj, Lucija Peterlin, Petra Marinko, Matej Breznik, Mojca Stregnar, Bakija Alenka Trampuz, Marjana Fortuna
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Patent number: 7030151Abstract: Atorvastatin calcium, the substance known by the chemical name (R—(R*,R*))-2-(4-fluorophenyl)-?, ?-dihydroxy-5-(1-methylethyl)-3-phenyl-((phenylamino)carbonyl)-1H-pyrrole-1-heptanoic acid hemi calcium salt is known as HMG-CoA reductase inhibitor and is used as an antihypercholesterolemic agent. Atorvastatin in the pharmaceutical compositions available in the market, is usually prepared as its calcium salt since it enables atorvastatin to be conveniently formulated in the pharmaceutical formulations, for example, in tablets, capsules, powders and the like for oral administration. Atorvastatin calcium can exist in an amorphous form or in one of the at least four known crystalline forms (Form I, Form II, Form III and Form IV). Atorvastatin calcium is the substance which is sparingly soluble in water, with pKa 4,5, and it has been found that the crystalline forms are less soluble than the amorphous form, which may cause problems in bioavailability of atorvastatin in the body.Type: GrantFiled: March 13, 2002Date of Patent: April 18, 2006Assignee: Lek Pharmaceuticals d.d.Inventors: Janez Ker{hacek over (c)}, Mateja Salobir, Sa{hacek over (s)}a Bavec
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Patent number: 6984399Abstract: The present invention relates to a novel solid pharmaceutical formulation containing lovastatin and simvastatin, respectively, with a particle size D(0.9) between 15 and 100 ?m and a specific particle surface area between 1 and 4 m2/g, and to the process for its preparation. The present invention also relates to the method for production of lovastatin and simvastatin with the size of crystals which are suitable for the preparation of the pharmaceutical formulation of the present invention. The novel solid pharmaceutical formulation is useful for treating hypercholesterolemia and hyperlipidemia.Type: GrantFiled: December 19, 2003Date of Patent: January 10, 2006Assignee: Lek Pharmaceuticals d.d.Inventors: Zlatko Pflaum, Mateja Salobir, Zdenka Jerala, Aleksander Resman
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Patent number: 6891047Abstract: Atorvastatin, the substance known by the chemical name [R-(R*,R*)]-2-(4-fluorophenyl)-?,? dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemi calcium salt, is readily available in one of its crystalline forms as it is known from the prior art. The present invention relates to a novel process for preparing atorvastatin in an amorphous form by precipitating the atorvastatin using a solvent of a second type from a solution of atorvastatin which is provided with a solvent of a first type. This process is useful for the conversion of atorvastatin in a crystalline form into atorvastatin in an amorphous form.Type: GrantFiled: July 7, 2003Date of Patent: May 10, 2005Assignee: LEK Pharmaceuticals d.d.Inventor: Zlatko Pflaum
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Patent number: 6838566Abstract: Lovastatin, pravastatin, simvastatin, mevastatin, atorvastatin, and derivatives and analogs thereof are known as HMG-CoA reductase inhibitors and are used as antihypercholesterolemic agents. The majority of them are produced by fermentation using microorganisms of different species identified as species belonging to Aspergillus, Monascus, Nocardia, Amycolatopsis, Mucor or Penicillium genus, some are obtained by treating the fermentation products using the methods of chemical synthesis or they are the products of total chemical synthesis.Type: GrantFiled: December 16, 2002Date of Patent: January 4, 2005Assignee: LEK Pharmaceuticals d.d.Inventor: Zlatko Pflaum
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Patent number: 6825015Abstract: A process for the isolation and purification of HMG-CoA reductase inhibitors from a mycelium biomass is described, which process comprises: clarifying a mycelium broth and concentrating the clarified broth to a lower volume, acidifying of the concentrate to a pH value in the range of 4.5 to 7.5, followed by extracting the HMG-CoA reductase inhibitor with ethyl acetate, crystallization of the HMG-CoA reductase inhibitor from a water-miscible or water-soluble organic solvent, and crystallization of the HMG-CoA reductase inhibitor from an organic solvent having limited miscibility or solubility with water. The crystallization steps may also be reverse. The concept of a combination of the specified crystallization steps can also be used for the purification of a crude HMG-CoA reductase inhibitor.Type: GrantFiled: October 16, 2000Date of Patent: November 30, 2004Assignee: LEK Pharmaceuticals d.d.Inventors: Zlatko Pflaum, Dusan Milivojevic, David Senica
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Stabilized pharmaceutically effective composition and pharmaceutical formulation comprising the same
Patent number: 6806290Abstract: Lovastatin, pravastatin, simvastatin, mevastatin, atorvastatin, and derivatives and analogs thereof are known as HMG-CoA reductase inhibitors and are used as antihypercholesterolemic agents. The majority of them are produced by fermentation using microorganisms of different species identified as species belonging to Aspergillus, Monascus, Nocardia, Amycolatopsis, Mucor or Penicillium genus, and some are obtained by treating the fermentation products using the methods of chemical synthesis or they are the products of total chemical synthesis. The aforementioned active substances may be destabilized by the environmental factors, their degradation may also be accelerated by interactions with other pharmaceutical ingredients, such as fillers, binders, lubricants, glidants and disintegrating agents, therefore the pharmaceutical ingredients and the process for preparation of the pharmaceutical formulation should be meticulously chosen to avoid the aforementioned undesired interactions and reactions.Type: GrantFiled: November 15, 2002Date of Patent: October 19, 2004Assignee: LEK Pharmaceuticals d.d.Inventors: Zlatko Pflaum, Janez Kerc -
Publication number: 20040138295Abstract: The present invention relates to a novel solid pharmaceutical formulation containing lovastatin and simvastatin, respectively, with a particle size D(0.9) between 15 and 100 &mgr;m and a specific particle surface area between 1 and 4 m2/g, and to the process for its preparation. The present invention also relates to the method for production of lovastatin and simvastatin with the size of crystals which are suitable for the preparation of the pharmaceutical formulation of the present invention. The novel solid pharmaceutical formulation is useful for treating hypercholesterolemia and hyperlipidemia.Type: ApplicationFiled: December 19, 2003Publication date: July 15, 2004Applicant: Lek Pharmaceuticals d.d.Inventors: Zlatko Pflaum, Mateja Salobir, Zdenka Jerala, Aleksander Resman
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Patent number: 6740775Abstract: A crystalline form of the sodium salt of pravastatin, which is known by the chemical name 1-naphthaleneheptanoic acid, 1,2,6,7,8,8a-hexahydro-&bgr;, &dgr;,6-trihydroxy-2-methyl-8-(2-methyl-1-oxobutoxy)-, mono sodium salt, which is useful as a pharmaceutical substance. A method for its preparation and isolation, a pharmaceutical formulation containing the sodium salt of pravastatin in the crystalline form and a pharmaceutically acceptable carrier, and the pharmaceutical method of treatment are also disclosed.Type: GrantFiled: April 4, 2003Date of Patent: May 25, 2004Assignee: LEK Pharmaceuticals d.d.Inventor: Zlatko Pflaum
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Patent number: 6695969Abstract: Lovastatin, pravastatin, simvastatin, mevastatin, atorvastatin, and derivatives and analogs thereof are known as HMG-CoA reductase inhibitors and are used as and antihypercholesterolemic agents. The majority of them are produced by fermentation using microorganisms of different species identified as species belonging to Aspergilus, Monascus, Nocardia, Amycolatopsis, Mucor or Penicilium genus, some are obtained by treating the fermentation products using the method of chemical synthesis or they are the products of total chemical synthesis. The purity of the active ingredient is an important factor for manufacturing the safe and effective pharmaceutical, especially if the pharmaceutical product must be taken on a longer term basis in the treatment or prevention of high plasma cholesterol. The accumulation of the impurities from the pharmaceuticals of lower purity may cause many side effects during the medical treatment.Type: GrantFiled: January 3, 2001Date of Patent: February 24, 2004Assignee: LEK Pharmaceuticals d.d.Inventors: Rok Grahek, Dusan Milivojevic, Andrej Bastarda