Abstract: The present invention relates to a pharmaceutical formulation comprising aliskiren or a pharmaceutically acceptable salt thereof as the active ingredient, wherein the pharmaceutical formulation is present in a solid dosage form suitable for oral administration based on a granulate obtained by a hot-melt and solvent-free granulation process, and to a process for manufacturing a pharmaceutical formulation.
Type:
Application
Filed:
March 20, 2008
Publication date:
June 10, 2010
Applicant:
KRKA, TOVARNA ZDRAVIL, D.D., NOVO MESTO
Inventors:
Franc Vrecer, Vida Skrabanja, Natalija Zajc, Urska Gojak
Abstract: A process for preparing venlafaxine in a high yield as well as processes for producing venlafaxine hydrochloride of form I having a very hight polymorphic purity are described.
Abstract: The present invention describes a novel process for the preparation of levocetirizine and pharmaceutically acceptable acid addition salts thereof using diglycolic acid or derivatives thereof and new intermediates used in that process.
Type:
Application
Filed:
March 12, 2008
Publication date:
April 29, 2010
Applicant:
KRKA, TOVARNA ZDRAVIL, D.D., NOVO MESTO
Inventors:
Jaroslav Tihi, Rok Zupet, Anica Pecavar, Ivanka Kolenc, Darja Pavlin
Abstract: The invention relates to a process for preparing lansoprazole. It is also directed to lansoprazole having a specific surface area and a pharmaceutical composition comprising lansoprazole.
Type:
Grant
Filed:
November 8, 2005
Date of Patent:
February 16, 2010
Assignee:
KRKA tovarna zdravil, d.d..
Inventors:
Berta Kotar-Jordan, Franc Vre{hacek over (c)}er, Mojca {hacek over (S)}egula {hacek over (Z)}akelj, Gregor Ritlop
Abstract: Processes for the preparation of clopidogrel hydrogen sulfate of polymorphic form I are described which include use of specific solvents and process measures to avoid formation of undesired by-products.
Abstract: 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.
Abstract: The invention relates to a solid pharmaceutical composition comprising donepezil hydrochloride hydrate and a process for its preparation. In particular it relates to a composition and a process wherein the donepezil hydrochloride retains its polymorphic form and is therefore highly stable against conversion into other polymorphic forms.
Type:
Application
Filed:
October 19, 2005
Publication date:
May 21, 2009
Applicant:
KRKA, TOVARNA ZDRAVIL D.D., NOVO MESTO
Inventors:
Miha Vrbinc, Berta Kotar-Jordan, Rok Zupet, Matej Smrkolj
Abstract: The present invention relates to an improved process for the manufacture of olmesartan and pharmaceutically acceptable salts and esters thereof as an active ingredient of a medicament for the treatment of hypertension and related diseases and conditions.
Abstract: The invention provides a process for the preparation of a sartan derivative of formula (I) (formula as filed in paper form) (I) wherein the substituents have the meaning indicated in the description, or a pharmaceutically acceptable salt thereof, comprising reacting 2-cyanophenylboronic acid or a derivative thereof with a p-halobenzyl-1H-imidazole derivative of formula (VI), (formula as filed in paper form) (VI) wherein (part of formula as filed in paper form), X, Y, R1 and R2 are as defined above, and Z is I, Br or Cl, in the presence of a transition metal catalyst and an inorganic or organic base.
Type:
Application
Filed:
September 20, 2006
Publication date:
December 18, 2008
Applicant:
KRKA, d.d. Novo mesto
Inventors:
Miroslav Veverka, Martin Putala, Heinrich Brath, Silvo Zuppancic
Abstract: The present invention relates to the field of pharmaceutical technology and in particular to novel dosage forms of medicaments containing as active ingredients simvastatin and ezetimibe, or pharmaceutically acceptable salts thereof. The present pharmaceutical compositions are characterized in that the contact of the compositions with oxygen is substantially reduced, such as by coating the composition, providing a medicament useful for the treatment and prevention of atherosclerosis and related conditions, in an environment having an essentially reduced oxygen or humidity, respectively, content.
Abstract: The invention relates to a solid pharmaceutical composition comprising donepezil hydrochloride hydrate and a process for its preparation. In particular it relates to a composition and a process wherein the donepezil hydrochloride retains its polymorphic form and is therefore highly stable against conversion into other polymorphic forms.
Type:
Application
Filed:
October 19, 2005
Publication date:
March 13, 2008
Applicant:
KRKA, TOVARNA ZDRAVIL D.D., NOVO MESTO
Inventors:
Miha Vrbinc, Berta Kotar-Jordan, Rok Zupet, Matej Smrkolj
Abstract: The invention relates to a novel and well defined Oolvate form of olanzapine which contains 2 molecules of water and 1 molecule of isopropanol per 2 molecules of olanzapine, and which can be converted into other, forms of olanzapine, in particular form (I) of olanzapine, as well as processes for preparing form (I) olanzapine.
Type:
Application
Filed:
March 7, 2005
Publication date:
August 16, 2007
Applicant:
KRKA, Tovarna Zdravil, D.D.
Inventors:
Berta Kotar-Jordan, Roman Lenarsic, Marija Grcman, Matej Smrkolj, Anton Meden, Igor Simonic, Rok Zupet, Joze Gnidovec, Primoz Benkic
Abstract: A process for preparing venlafaxine in a high yield as well as processes for producing venlafaxine hydrochloride of form I having a very high polymorphic purity are described.
Abstract: The invention relates to a process for preparing a solid pharmaceutical composition of perindopril or a salt thereof which avoids a wet granulation step and results in very stable pharmaceutical compositions, like tablets.
Type:
Application
Filed:
March 29, 2005
Publication date:
July 26, 2007
Applicant:
KRKA, TOVARNA ZDRAVIL, D.D., NOVO MESTO
Abstract: A process for the preparation of inhibitors of HMG-CoA reductase, such as simvastatin, from 4-silyloxytetrahydropyran-2-ones with triethylamine trihydrofluoride being used as the desilylation reagent is described. The reaction is performed in organic solvents, a mixture thereof or without solvents. It is characteristic of this reaction that no additional impurities are obtained and that it takes place without the use of additional catalysts and with low excesses of the reagent.
Type:
Grant
Filed:
March 17, 2003
Date of Patent:
August 22, 2006
Assignee:
KRKA, Tovarna Zdravil, D. D.
Inventors:
Silvo Zupancic, Dusan Krasovec, Pavel Zupet
Abstract: A process for the preparation of compounds of formula (I)
wherein
R is a C1 to C12 alkyl group and
R1 is a protecting group or H
which process comprises
(a) converting the diol lactone of formula (II)
to the protected diol lactone of formula (IIa) wherein R1 is a protecting group
(b) acylating the protected diol lactone (IIa) to give compound (I) wherein R1 is a protecting group,
(c) optionally removing the protecting group R1 to give compound (I) wherein R1 is H; and
wherein steps (a) and/or (b) are carried out in the presence of N-methylimidazole.
Type:
Grant
Filed:
September 22, 2000
Date of Patent:
June 26, 2001
Assignee:
KRKA, Tovarna Zdravil, D.D.
Inventors:
Silvo Zupan{haeck over (c)}i{haeck over (c)}, Anton Stimac, Jo{haeck over (z)}e Gnidovec
Abstract: There is disclosed a process for the isolation of the hypolipaemic active substance lovastatin from a sample, e.g. fermentation broth, mycelium or filtrate of Aspergillus terreus (ATCC 20542) or Aspergillus oryzae (ATCC 74135) by extraction with butyl acetate. Simultaneously with the concentration of the extract, lactonisation takes place. There follows a direct crystallization of lovastatin in the lactone form from butyl acetate.
Type:
Grant
Filed:
December 5, 1995
Date of Patent:
January 27, 1998
Assignee:
KRKA tovarna zdravil, p.o
Inventors:
Pavica Hajko, Tanja Vesel, Ivan Radez, Miroslav Pokorny
Abstract: A process for preparing N-[1(S)-ethoxycarbonyl-3-phenylpropyl]-L-alanine N-carboxy anhydride from N-[1(S)-ethoxycarbonyl-3 -phenylpropyl]-L-alanine and N,N'-carbonyldiimidazole and the condensation thereof with L-proline silyl ester hydrochloride. The condensation product is used as an angiotensin converting enzyme (ACE) inhibitor.