Abstract: This invention provides novel dicarboxylic acid salt forms of varenicline, wherein the acid is selected from maleic acid, fumaric acid, adipic acid, galactaric acid and malic acid. This invention provides also a carboxylic acid salt form of varenicline, wherein the acid is S-2-pyrrolidinon-5-carboxylic acid. This invention also provides methods for making these salt forms.
Type:
Application
Filed:
March 6, 2009
Publication date:
May 5, 2011
Applicant:
Medichem, S.A.
Inventors:
Stephen Benedict David Winter, Monica Benito Velez
Abstract: Described is a process of preparing a pure solid or crystalline racemic 3,3-diarylpropylamine compound and the compounds formed thereof. The solid and crystalline forms of racemic 3,3-diarylpropylamine compound are especially suitable for producing highly pure 3,3-diarylpropylamine salts such as tolterodine tartrate. Also described are the highly pure solid or crystalline forms of racemic tolterodine, racemic tolterodine salt and tolterodine tartrate.
Type:
Application
Filed:
December 9, 2010
Publication date:
April 21, 2011
Applicant:
Medichem S.A.
Inventors:
Maria Angeles Conde Martinez, Ignasi Auquer i Pedemonte
Abstract: The invention relates to solid forms of the anti-epileptic agent lacosamide (I). The invention also relates to mixtures of solid forms of lacosamide. The invention further relates to mixtures of lacosamide enantiomers crystallized in a conglomerate Form and the use thereof in providing enantiomerically enriched lacosamide, preferably lacosamide enriched with the (R)-enantiomer of lacosamide.
Abstract: Described is a process of preparing a pure solid or crystalline racemic 3,3-diarylpropylamine compound and the compounds formed thereof. The solid and crystalline forms of racemic 3,3-diarylpropylamine compound are especially suitable for producing highly pure 3,3-diarylpropylamine salts such as tolterodine tartrate. Also described are the highly pure solid or crystalline forms of racemic tolterodine, racemic tolterodine salt and tolterodine tartrate.
Type:
Grant
Filed:
November 27, 2007
Date of Patent:
February 1, 2011
Assignee:
Medichem S.A.
Inventors:
Maria Angeles Conde Martinez, Ignasi Auqueri Pedemonte
Abstract: The present invention is related to processes suitable for industrial synthesis of pregabalin from (R)-(?)-3-(carbamoylmethyl)-5-methylhexanoic using sodium hypochlorite as described herein. In addition, the present invention is related to pregabalin which is substantially free of impurities and pharmaceutical compositions comprising pregabalin.
Abstract: The invention relates to new crystalline polymorphic forms of N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidine)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide (i.e., sunitinib base), including Form I, Form II, and Form IV, processes for preparing crystalline polymorphic forms of sunitinib base, and pharmaceutically acceptable salts of new crystalline polymorphic forms of sunitinib base and pharmaceutical compositions comprising new crystalline polymorphic forms of sunitinib base, salts of new crystalline polymorphic forms of sunitinib base and mixtures thereof.
Type:
Application
Filed:
December 12, 2008
Publication date:
November 11, 2010
Applicant:
Medichem, S.A.
Inventors:
Stephen Benedict David Winter, Bernardino Mangion
Abstract: The invention relates, in general, to an improved process for preparing compounds (e.g., 3-(3-trifluoromethylphenyl)propanal (Compound III, below)), which are key intermediates for the synthesis of cinacalcet, its salts and/or solvates thereof, as well as the use of such compounds prepared by such process for the preparation of cinacalcet and/or its salts or solvates.
Type:
Application
Filed:
June 8, 2007
Publication date:
October 21, 2010
Applicant:
Medichem, S.A.
Inventors:
Tibor Szekeres, Jozsef Repasi, Andras Szabo, Bernardino Mangion
Abstract: The invention relates to 2-amino-3-benzoylbenzeneacetamide, i.e. nepafenac, crystals having reduced chargeability, to processes for the preparation thereof, and to the use thereof for preparing pharmaceutical formulations.
Type:
Application
Filed:
March 12, 2010
Publication date:
September 16, 2010
Applicant:
Medichem, S.A.
Inventors:
Ana Gavaldá Escudé, Ernesto Duran Lopez
Abstract: The invention relates to processes for preparing rasagiline mesylate that avoid the use of alcohol solvents, thereby producing rasagiline mesylate free of any alkyl mesylates, including isopropyl mesylate. The invention further relates to processes for purifying rasagiline mesylate to obtain a product free of alkyl mesylates, and to the thus obtained rasagiline mesylate.
Type:
Grant
Filed:
May 21, 2009
Date of Patent:
August 24, 2010
Assignee:
Medichem, S.A.
Inventors:
Jordi Bosch i Llado, Maria Carmen Burgarolas Montero, Judit Masllorens Llinas
Abstract: The invention relates, in general, to an improved process for converting compounds of Formula II (below) to compounds of Formula III (below), which are key intermediates for the synthesis of ezetimibe, or to ezetimibe itself, wherein in Formulas II and III, R represents hydrogen, alkyl, or a hydroxyl protecting group (e.g., benzyl group, a substituted benzyl group, or a silyl group). The invention further includes the use of the described process and the use of compounds of Formula III made by the described process for the preparation of ezetimibe.
Type:
Application
Filed:
September 29, 2007
Publication date:
July 1, 2010
Applicant:
Medichem S.A.
Inventors:
Ana Gavalda Escude, Jordi Bosch i Llado, Ulrike Nettekoven
Abstract: The present invention provides an improved synthetic strategy for the preparation of solifenacin and pharmaceutically acceptable salts thereof.
Abstract: The invention relates to new polymorphic forms of olopatadine hydrochloride, designated herein as olopatadine hydrochloride Forms A and B, and methods of preparing, purifying and treating them.
Abstract: This invention provides novel crystalline acid salt forms of 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine, i.e. sitagliptin, to processes for their preparation and isolation, and to pharmaceutical compositions comprising the same.
Type:
Application
Filed:
July 29, 2009
Publication date:
March 18, 2010
Applicant:
Medichem S.A.
Inventors:
Stephen Benedict David WINTER, Monica BENITO VELEZ, Ernesto DURAN LOPEZ
Abstract: This invention provides improved methods for making solifenacin and pharmaceutically acceptable salts thereof. The instant methods are unexpectedly advantageous in their simplicity and efficiency.
Abstract: The invention relates to the malic acid salt of N-[2-(diethylamino)ethyl]-5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxamide, to the use thereof as an intermediate for preparing the malic acid salt of sunitinib, and to pharmaceutical compositions comprising said malic acid salt of sunitinib.
Type:
Application
Filed:
June 12, 2009
Publication date:
December 24, 2009
Applicant:
Medichem, S.A.
Inventors:
Bernardino Mangion, Stephen Benedict David Winter
Abstract: Disclosed is a process for preparing purified ranolazine of formula (I), which is indicated for the chronic treatment of angina, comprising reacting 1-[(2,6-dimethylphenyl)aminocarbonyl]piperazine with 1-phenoxy-2,3-epoxypropane in an inert solvent followed by precipitating the ranolazine.
Abstract: Disclosed is a process for preparing anti-inflammatory compound nepafenac comprising preparing a compound of formula (V) wherein a N-halosuccinimide is used as the halogenating agent, followed by desulfurization using Raney Nickel. Also disclosed is a polymorphic form B of 2-amino-3-benzoyl-?-(methylthio)-benzeneacetamide (i.e.
Type:
Application
Filed:
June 12, 2009
Publication date:
December 17, 2009
Applicant:
Medichem, S.A.
Inventors:
Gabriel Tojo Suarez, Ana Gavalda Escude