Abstract: The present invention relates to a process for preparing pyrimidine derivatives of the formula V, in particular as intermediates useful for preparing pyrimidine derivatives of a class that is effective at inhibiting the biosynthesis of cholesterol in humans, such as HMG-CoA reductase inhibitors, e.g. rosuvastatin.
Abstract: The present invention relates to an oral dispersible tablet comprising at least one filler selected from sugars and sugar alcohols, and microcrystalline cellulose.
Abstract: The invention relates to a method for producing tablets comprising a polyallylamine polymer, comprising the steps (i) preparation of a polyallylamine polymer or pharmaceutically compatible salts thereof, optionally in a mixture with one or more pharmaceutical excipients; (ii) compaction to give a slug; (iii) granulation of the slug; and (iv) compression of the resulting granules to give tablets; and also to tablets, sachets and slugs comprising a compacted polyallylamine polymer. In addition, the invention relates to tablets comprising a polyallylamine polymer, in particular Sevelamer, with a bimodal pore size distribution.
Abstract: The invention relates to pharmaceutical compositions with modified release properties comprising 5-Chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophencarboxamid and process of preparing such compositions.
Type:
Application
Filed:
August 10, 2009
Publication date:
August 4, 2011
Applicant:
RATIOPHARM GMBH
Inventors:
Katrin Rimkus, Frank Muskulus, Sandra Brueck, Jana Paetz
Abstract: The invention relates to pharmaceutical compositions which contain the active agent Aliskiren and are suitable for the production of tablets by dry pressing, so that prior wet granulation can be obviated. The invention also relates to tablets which can be obtained by dry pressing of these pharmaceutical compositions and to a method for producing these tablets. The invention furthermore relates to the use of the novel pharmaceutical compositions and tablets for treating hypertension and illnesses associated therewith.
Abstract: The present invention relates to a process for preparing pyrrole derivatives of a class that is effective at inhibiting the biosynthesis of cholesterol in humans, and more particularly to improved synthetic methods for preparing 3,5-dihydroxy-7-pyrrol-1-yl heptanoic acids from 1,4-diketo starting materials. The invention further relates to intermediates in this process formula (I).
Type:
Grant
Filed:
December 16, 2005
Date of Patent:
April 26, 2011
Assignee:
ratiopharm GmbH
Inventors:
Pavel Bobal, Jaroslav Frantisek, Jiri Stohandl, Kane Denike, Armin Boerner, Vitali Tararov, Andrei Korostylev, Gerd Koenig, Nicolas Jeker
Abstract: The present invention relates to a process for preparing pentanoic diacid derivatives useful for preparing pyrimidine derivatives, in particular as intermediates useful for preparing pyrimidine derivatives of a class that is effective at inhibiting the biosynthesis of cholesterol in humans, such as HMG-CoA reductase inhibitors, e.g. rosuvastatin.
Abstract: The present invention relates to a solid pharmaceutical composition comprising at least two layers, wherein the first layer contains a non-peptide angiotensin II receptor antagonist or a pharmaceutically acceptable salt thereof in a dissolving matrix and the second layer contains a diuretic or a pharmaceutically acceptable salt thereof. The invention also provides methods for the production of said pharmaceutical compositions.
Type:
Application
Filed:
March 17, 2009
Publication date:
January 13, 2011
Applicant:
ratiopharm GmbH
Inventors:
Sunil R. Mhase, Ganesh V. Gat, Jawed Hussain
Abstract: The present invention relates to Escitalopram having a small median particle size and a solid pharmaceutical composition comprising the same.
Type:
Application
Filed:
October 18, 2007
Publication date:
December 23, 2010
Applicant:
ratiopharm GmbH
Inventors:
Parshwakumar V. Kalyankar, Ganesh V. Gat, Jawed Hussain
Abstract: The present invention relates to a pharmaceutical composition comprising N-[2-(diethylamino)ethyl]-5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide or a pharmaceutically acceptable salt thereof as active pharmaceutical ingredient.
Abstract: The present invention relates to novel formulations comprising ezetimibe as active ingredient. In particular the invention relates to a pharmaceutical composition comprising 5 to 20 wt-% ezetimibe, 50 to 85 wt-% diluent, 3 to 25 wt-% disintegrant, 1 to 10 wt-% binder, and 0.5 to 1 wt-% lubricant, characterized in that the ezetimibe has a particle size distribution of d(0.9) of 5 ?m to 35 ?m and d(0.5) of 3 ?m to 20 ?m, as well as methods for preparing said formulations.
Abstract: The present invention relates to processes for preparing a compound of the general formula (Ia) wherein X is a halogen atom, or a pharmaceutically acceptable salt thereof, wherein a compound of the formula (II) wherein X is as defined above and Y and Z independently represent a leaving group each, is reacted with an optically active amino alcohol to form a first mixture of diastereomers.
Type:
Grant
Filed:
February 10, 2009
Date of Patent:
September 21, 2010
Assignee:
ratiopharm GmbH
Inventors:
Jiri Stohandl, Jaroslav Frantisek, Winfried Ness
Abstract: The invention relates to novel salts of the active substance rasagiline. The salts show excellent processability even after prolonged storage and an excellent storage stability usually superior to known salts after being processed into tablets.
Abstract: The invention relates to a process for the manufacture of an 1,2,4-triazol-1-yl compound of the formula [A], or a salt thereof, wherein each of R3 and R4 is hydrogen or lower alkyl, said process comprising reacting a hydrazine compound of the formula [B] wherein R is hydrogen or acyl, R2 is hydrogen or a protecting group, are hydrogen or lower alkyl, and R6 is hydrogen or COOR7, or a salt thereof, with a 1,2,4-triazolyl forming reagent. In addition, novel intermediates for the synthesis of the anti-migraine agent Rizatriptan and methods for their synthesis are presented.
Type:
Grant
Filed:
January 27, 2005
Date of Patent:
August 31, 2010
Assignee:
ratiopharm GmbH
Inventors:
Pierre Martin, Ulrich Berens, Andreas Boudier, Oliver Dosenbach
Abstract: The present invention relates to a new method for the production of valsartan, a valine derivative having the chemical N name is (S)—N-(1-carboxy-2-methylprop-1-yl)-N-pentanoyl-N-[2?-(1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]amine, and pharmacologically acceptable salts thereof. Furthermore the invention relates to new intermediate compounds which are suitable for the production of valsartan and new methods for the production of intermediate compounds which are suitable for the production of valsartan.
Type:
Application
Filed:
December 11, 2007
Publication date:
August 26, 2010
Applicant:
ratiopharm GmbH
Inventors:
Jiri Stohandl, Pavel Bobal, Jaroslav Frantisek
Abstract: The present invention is directed to the novel polymorphic Form A and Form B of Rizatriptan benzoate, processes for the preparation thereof and pharmaceutical compositions comprising these crystalline forms.
Type:
Grant
Filed:
January 5, 2005
Date of Patent:
August 17, 2010
Assignee:
ratiopharm GmbH
Inventors:
Paul Adriaan Van Der Schaaf, Jörg Berghausen, Fritz Blatter, Martin Szelagiewicz, Ulrich Berens
Abstract: The invention relates to a method for producing a medicament containing tadalafil. In said method, tadalafil is mixed with suitable adjuvants and is heated to a temperature of about 100° C. to about 200° C., preferably about 150° C. to about 200° C., especially about 200° C.
Type:
Application
Filed:
June 23, 2008
Publication date:
July 15, 2010
Applicant:
ratiopharm GmbH
Inventors:
Rainer Alles, Julia Schulze Nahrup, Katrin Rimkus
Abstract: The present invention relates to a process for the preparation of a medicament containing vardenafil hydrochloride trihydrate in solid form, in which vardenafil hydrochloride trihydrate is processed with suitable pharmaceutical auxiliaries at a temperature of from approx. 20° C. to approx. 45° C.
Type:
Application
Filed:
June 12, 2008
Publication date:
June 24, 2010
Applicant:
ratiopharm GmbH
Inventors:
Yogesh S. Deshpande, Sandra Brueck, Julia Schulze Nahrup, Birgit Schnitter, Ganesh Gat, Javed Hussain
Abstract: Solid pharmaceutical composition containing: (a) pregabaline as active principle and (b) one or several pharmaceutical auxiliary agents, the composition being essentially free from saccharides and comprising no further amino acids, apart from pregabaline.
Type:
Application
Filed:
April 23, 2008
Publication date:
June 17, 2010
Applicant:
RATIOPHARM GMBH
Inventors:
Julia Schulze-Nahrup, Alexander Lehmann, Frank Muskulus