Patents by Inventor Anton Copar

Anton Copar has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 9512097
    Abstract: The present invention relates to a process for the preparation of 3-aroyl-5-aminobenzofuran derivatives useful as antiarrhythmic drugs which avoids the use of nitro intermediates.
    Type: Grant
    Filed: November 11, 2011
    Date of Patent: December 6, 2016
    Assignee: Lek Pharmaceuticals D.D.
    Inventors: Frank Richter, Erwin Schreiner, Samo Pirc, Anton Copar
  • Patent number: 8697741
    Abstract: A process for the preparation of amorphous atorvastatin calcium. The process includes providing a reaction mixture having a pH between 6.5 and 8.0 containing a sodium salt of atorvastatin and tetrahydrofuran. A non-cyclic chlorinated organic solvent selected from the group consisting of dichloromethane, trichloroethane, tetrachloroethane and chloroform or addition of cyclic hydrocarbon solvent selected from the group consisting of cyclohexane, cyclopentane and methyl cyclohexane is added to provide a mixture of organic solvents. An equivalent or an excess quantity of a source of calcium ions selected from the group consisting of calcium acetate and calcium chloride is added. Amorphous atorvastatin calcium is isolated from an organic phase comprising the mixture of organic solvents.
    Type: Grant
    Filed: March 4, 2009
    Date of Patent: April 15, 2014
    Assignee: LEK Pharmaceutical D.D.
    Inventors: Ljubomir Antoncic, Gorazd Sorsak, Anton Copar
  • Patent number: 8604194
    Abstract: Novel pharmaceutically acceptable salts of desvenlafaxine with physiologically ubiquitous ions selected from sugar acids and vitamins, processes for their preparation, pharmaceutical compositions containing them and uses therefor are described.
    Type: Grant
    Filed: January 29, 2009
    Date of Patent: December 10, 2013
    Assignee: Lek Pharmaceuticals D.D.
    Inventors: Furlan Borut, Anton Copar
  • Publication number: 20130317100
    Abstract: The present invention relates to a process for the preparation of 3-aroyl-5-aminobenzofuran derivatives useful as antiarrhythmic drugs which avoids the use of nitro intermediates.
    Type: Application
    Filed: November 11, 2011
    Publication date: November 28, 2013
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Frank Richter, Erwin Schreiner, Samo Pirc, Anton Copar
  • Patent number: 8445693
    Abstract: One embodiment disclosed in the invention is the efficient synthesis of halogenated biaryl starting material via Grignard chemistry and the use thereof. Another embodiment of the invention is the reaction of catalyzed carbonylation of the 3?-(2?-halo-biphenyl-4-ylmethyl)-1,7?-dimethyl-2?-propyl-1H,3?H-[2,5?]bibenzoimidazolyl (TLMH) using either gaseous carbon monoxide in a solvent mixture containing water; or formic acid salts optionally together with acetic acid in anhydrous solvent.
    Type: Grant
    Filed: March 19, 2009
    Date of Patent: May 21, 2013
    Assignee: Lek Pharmaceuticals D.D.
    Inventors: Zdenko Casar, Anton Copar, Jerome Cluzeau, Andrej Premrl
  • Patent number: 8410285
    Abstract: A process for obtaining 2?-halo-4-methylbiphenyls is described, which comprises reacting 4 halotoluene with a 1,2-dihalobenzene in the presence of elemental metal such as magnesium, lithium or zinc, wherein 0 to 0.9 molar, particularly 0 to 0.2 molar excess of 4-halotoluene in regard to 1,2-dihalobenzene is used, and arised organometal intermediates are quenched by elemental mental halogen. In addition, the coupling of arised 2?-halo-4-methylbiphenyls with 2-(1-propyl)-4-methyl-6-(1?-methylbenzimidazole-2-il)benzimidazole to afford 3?-(2?-halo-biphenyl-4-ylmethyl)-1,7?-dimethyl-2?-propyl-1H,3?H-[2,5?]bibenzoimidazolyl, which can be further converted to organometallic compound and said organometallic compound is further reacted with formic acid derivative, such as N,N-dimethylformamide, alkylformiate or carbon dioxide to obtain telmisartan, is also described.
    Type: Grant
    Filed: March 19, 2009
    Date of Patent: April 2, 2013
    Assignee: LEK Pharmaceuticals D.D.
    Inventors: Anton Copar, Zdenko Casar, Andrej Premrl
  • Patent number: 8367848
    Abstract: Present invention refers to the process of preparing amorphous atorvastatin calcium without intermediate isolation of crystal or undefined mixture of crystal and amorphous atorvastatin calcium, respectively. Forming of calcium atorvastatin salt is carried out in a mixture of chlorinated organic solvent or cyclic hydrocarbon solvent, respectively, the non-hydroxylic organic solvent, and water, the source of calcium ions is calcium acetate or calcium chloride, respectively.
    Type: Grant
    Filed: April 9, 2004
    Date of Patent: February 5, 2013
    Assignee: LEK Pharmaceuticals D.D.
    Inventors: Ljubomir Antoncic, Gorazd Sorsak, Anton Copar
  • Publication number: 20120149895
    Abstract: The present invention discloses a process for dimethylation of active methylene groups. Specifically, the invention discloses a process for preparing 3-amino-2,2-dimethylpropanamide. Compounds produced by the present dimethylation process such as 3-amino-2,2-dimethylpropanamide can be used as intermediates in the route of synthesis of therapeutic, prophylactic or diagnostic agent, for example aliskiren or cryptophycin. Particularly, the invention relates to embodiments further extending to processes for preparing pharmaceutical dosage form comprising said therapeutic, prophylactic or diagnostic agents. More specifically, the invention relates to the use of compounds produced by the present dimethylation process for the manufacture of therapeutic, prophylactic or diagnostic agents or for the manufacture of pharmaceutical dosage forms comprising said therapeutic, prophylactic or diagnostic agents.
    Type: Application
    Filed: March 30, 2010
    Publication date: June 14, 2012
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Branko Jenko, Anton Copar
  • Patent number: 7968727
    Abstract: 4-bromomethyl-2?-formylbiphenyl and 4-bromomethyl-2?-hydroxymethylbiphenyl are useful starting material for the preparation various angiotenzin II antagonists, which are prepared from 4-bromomethyl-2?-cyanobiphenyl or 4?-bromomethylbiphenylcarboxyilic derivatives using selected hydride reagent.
    Type: Grant
    Filed: March 30, 2006
    Date of Patent: June 28, 2011
    Assignee: Lek Pharmaceuticals, D.D.
    Inventors: Anton Copar, Ljubomir Antoncic, Matej Antoncic
  • Publication number: 20110105539
    Abstract: A process for obtaining 2?-halo-4-methylbiphenyls is described, which comprises reacting 4 halotoluene with a 1,2-dihalobenzene in the presence of elemental metal such as magnesium, lithium or zinc, wherein 0 to 0.9 molar, particularly 0 to 0.2 molar excess of 4-halotoluene in regard to 1,2-dihalobenzene is used, and arised organometal intermediates are quenched by elemental mental halogen. In addition, the coupling of arised 2?-halo-4-methylbiphenyls with 2-(1-propyl)-4-methyl-6-(1?-methylbenzimidazole-2-il)benzimidazole to afford 3?-(2?-halo-biphenyl-4-ylmethyl)-1,7?-dimethyl-2?-propyl-1H,3?H-[2,5?]bibenzoimidazolyl, which can be further converted to organometallic compound and said organometallic compound is further reacted with formic acid derivative, such as N,N-dimethylformamide, alkylformiate or carbon dioxide to obtain telmisartan, is also described.
    Type: Application
    Filed: March 19, 2009
    Publication date: May 5, 2011
    Applicant: LEK Pharmaceuticals D.D.
    Inventors: Anton Copar, Zdenko Casar, Andrej Premrl
  • Publication number: 20110098329
    Abstract: One embodiment disclosed in the invention is the efficient synthesis of halogenated biaryl starting material via Grignard chemistry and the use thereof. Another embodiment of the invention is the reaction of catalyzed carbonylation of the 3?-(2?-halo-biphenyl-4-ylmethyl)-1,7?-dimethyl-2?-propyl-1H,3?H-[2,5?]bibenzoimidazolyl (TLMH) using either gaseous carbon monoxide in a solvent mixture containing water; or formic acid salts optionally together with acetic acid in anhydrous solvent.
    Type: Application
    Filed: March 19, 2009
    Publication date: April 28, 2011
    Applicant: LEK Pharmaceuticals D.D.
    Inventors: Zdenko Casar, Anton Copar, Jerome Cluzeau, Andrej Premrl
  • Patent number: 7923570
    Abstract: The present invention relates to a new process for the preparation of crystalline perindopril. The present invention also relates to new alkyl ammonium salts of perindopril and the processes for the preparation thereof.
    Type: Grant
    Filed: July 24, 2006
    Date of Patent: April 12, 2011
    Assignee: Lek Pharmaceuticals, D.D.
    Inventors: Branko Jenko, Anton Copar
  • Publication number: 20110082213
    Abstract: Novel pharmaceutically acceptable salts of desvenlafaxine with physiologically ubiquitous ions selected from sugar acids and vitamins, processes for their preparation, pharmaceutical compositions containing them and uses therefor are described.
    Type: Application
    Filed: January 29, 2009
    Publication date: April 7, 2011
    Inventors: Furlan Borut, Anton Copar
  • Publication number: 20090318521
    Abstract: 4-bromomethyl-2?-formylbiphenyl and 4-bromomethyl-2?-hydroxymethylbiphenyl are useful starting material for the preparation various angiotenzin II antagonists, which are prepared from 4-bromomethyl-2?-cyanobiphenyl or 4?-bromomethylbiphenylcarboxyilic derivatives using selected hydride reagent.
    Type: Application
    Filed: March 30, 2006
    Publication date: December 24, 2009
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Anton Copar, Ljubomic Antoncic, Matej Antoncic
  • Publication number: 20090182030
    Abstract: A process for the preparation of amorphous atorvastatin calcium. The process includes providing a reaction mixture having a pH between 6.5 and 8.0 containing a sodium salt of atorvastatin and tetrahydrofuran. A non-cyclic chlorinated organic solvent selected from the group consisting of dichloromethane, trichloroethane, tetrachloroethane and chloroform or addition of cyclic hydrocarbon solvent selected from the group consisting of cyclohexane, cyclopentane and methyl cyclohexane is added to provide a mixture of organic solvents. An equivalent or an excess quantity of a source of calcium ions selected from the group consisting of calcium acetate and calcium chloride is added. Amorphous atorvastatin calcium is isolated from an organic phase comprising the mixture of organic solvents.
    Type: Application
    Filed: March 4, 2009
    Publication date: July 16, 2009
    Applicant: Lek Pharmaceuticals d.d.
    Inventors: Ljubomir Antoncic, Gorazd Sorsak, Anton Copar
  • Patent number: 7553856
    Abstract: A novel crystalline form of the substrate known under the chemical name 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfiny]-1H-benzimidazole, and having the generic name omeprazole, hereinafter referred to as omeprozole form C, is disclosed. Further, a process for the preparation of omeprazole form C, a pharmaceutical formulation containing omeprazole form C in admixture with pharmaceutically acceptable excipients and the use of omeprazole form C for treatment of gastrointestinal disorders are disclosed.
    Type: Grant
    Filed: October 12, 2005
    Date of Patent: June 30, 2009
    Assignee: Lek Pharmaceuticals d.d.
    Inventors: Natasa H Milac, Anton Copar, Barbara Podobnik, Andreja C Belcic, Alenka Kosak, Brina Ornik, Uros Urleb
  • Publication number: 20090012140
    Abstract: New alkali and earth-alkali salts of telmisartan in amorphous form and a new crystalline sodium salt of telmisartan have been prepared by preparing a solution despite low solubility of telmisartan and rapidly vacuum evaporating to dryness.
    Type: Application
    Filed: November 9, 2005
    Publication date: January 8, 2009
    Applicant: LEK PHARMACEUTICALS D.D
    Inventors: Ljubomir Antoncic, Anton Copar
  • Publication number: 20080306135
    Abstract: The present invention relates to a new process for the preparation of crystalline perindopril. The present invention also relates to new alkyl ammonium salts of perindopril and the processes for the preparation thereof.
    Type: Application
    Filed: July 24, 2006
    Publication date: December 11, 2008
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Branko Jenko, Anton Copar
  • Publication number: 20080161557
    Abstract: 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: Application
    Filed: March 17, 2005
    Publication date: July 3, 2008
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Tomaz Mesar, Anton Copar, Hubert Sturm, Johannes Ludescher
  • Publication number: 20080033207
    Abstract: In the present invention, the process for the preparation of tamsulosin hydrochloride and subsequent purification with thermal crystallisation to provide essentially pure tamsulosin hydrochloride is disclosed.
    Type: Application
    Filed: December 27, 2004
    Publication date: February 7, 2008
    Inventors: Borut Furlan, Anton Copar