Abstract: The invention relates to an improved process for preparing cinacalcet hydrochloride. The invention provides an efficient and economic process for preparing cinacalcet hydrochloride which is suitable for industrial implementation i.e., affords cinacalcet hydrochloride with high purity, and uses small volumes of acidifying agent and solvents.
Abstract: The present invention relates to voriconazole, processes of preparing voriconazole, and pharmaceutical compositions and therapeutic uses thereof. In particular, the present invention also relates to voriconazole prepared from voriconazole having a substantially undefined shape and/or crystal habit. The invention further relates to voriconazole having a modified sphericity factor and/or specific surface area and/or Sauter diameter compared to voriconazole known from the prior art.
Type:
Grant
Filed:
July 23, 2010
Date of Patent:
October 16, 2012
Assignee:
Medichem, S.A.
Inventors:
Ernesto Duran Lopez, Juan Contreras Lascorz
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:
Grant
Filed:
June 12, 2009
Date of Patent:
October 2, 2012
Assignee:
Medichem, S.A.
Inventors:
Gabriel Tojo Suárez, Ana Gavaldá Escudé
Abstract: The invention relates to processes for preparing rasagiline mesylate that avoid the use of alcohol solvents, thereby producing rasagiline mesylate five 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:
September 2, 2011
Date of Patent:
August 7, 2012
Assignee:
Medichem, S.A.
Inventors:
Jordi Bosch I Llado, Maria Carmen Burgarolas Montero, Judit Masllorens Llinas
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:
March 29, 2012
Publication date:
July 19, 2012
Applicant:
Medichem S.A.
Inventors:
Stephen Benedict David WINTER, Monica BENITO VELEZ, Ernesto DURAN LOPEZ
Abstract: This invention provides improved processes for the preparation of 5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrole, asenapine. These processes allow the preparation of asenapine at industrial scale in good yields and high stereoselectivity.
Type:
Application
Filed:
December 23, 2011
Publication date:
June 28, 2012
Applicant:
Medichem, S.A.
Inventors:
Jordi BOSCH i LLADÓ, Ernesto DURAN LOPEZ
Abstract: The invention relates, in general, to an improved process for preparing lamotrigine, Formule (I). Processes for preparing and purifying lamotrigine, including lamotrigine hydrate, lamotrigine monohydrate and anhydrous lamotrigine, are described.
Abstract: The invention relates to 2-{2-amino-3-[hydroxy(phenyl)methyl]phenyl}acetamide, a process for its preparation, and its use as a reference marker and reference standard for analyzing the purity of nepafenac.
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:
Grant
Filed:
June 12, 2009
Date of Patent:
April 10, 2012
Assignee:
Medichem, S.A.
Inventors:
Bernardino Mangion, Stephen Benedict David Winter
Abstract: The invention provides an improved process for the preparation of a benzonaphthalene derivative including, in particular, the manufacture of high purity adapalene. The invention further includes a method for assessing the color of adapalene by means of a quantitative colorimetric measurement of the produced adapalene.
Abstract: The present invention provides an improved process for preparing a compound of formula (IIIA), an intermediate of the synthesis of varenicline. Also, the present invention provides an improved process for preparing varenicline, or a pharmaceutically acceptable salt or solvate thereof. Furthermore, the present invention provides a process for decolorizing varenicline, or a salt or solvate thereof. Still further, the present invention provides a process of preparing varenicline L-tartrate with improved yield. Still further, the present invention relates to the use of compound of formula (V), or a salt or solvate thereof, as a reference marker and reference standard for assessing the purity of varenicline, or a salt or solvate thereof.
Abstract: The invention relates to processes for preparing rasagiline mesylate that avoid the use of alcohol solvents, thereby producing rasagiline mesylate five 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:
Application
Filed:
September 2, 2011
Publication date:
December 22, 2011
Applicant:
Medichem, S.A.
Inventors:
Jordi BOSCH I LLADO, Maria Carmen Burgarolas Montero, Judit Masllorens Llinas
Abstract: The invention relates to cinacalcet hydrochloride, new polymorphic crystalline forms of cinacalcet hydrochloride, amorphous cinacalcet hydrochloride and synthetic processes for their preparation.
Abstract: A process for preparing substituted pyrrolidine compounds, including (5)-2-{1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl]-3-pyrrolidinyl}-2,2-diphenylacetamide hydrobromide, commonly known in the art as darifenacin, comprising reacting a pyrrolidine compound with a benzofuran derivative in the presence of a phase-transfer catalyst.
Abstract: The invention comprises a process for preparing quetiapine and/or its salts, including, quetiapine fumarate. The process generally comprises reacting dibenzothiazepinone (dibenzo[bf][1,4]thiazepin-11(10H)-one) with phosphorous oxychloride in the presence of triethylamine in an aromatic organic solvent such as toluene or, preferably, xylene at reflux temperature to obtain an aromatic hydrocarbon solution of 11-chloro-dibenzo[bf][1,4]thiazepine. Thereafter, the 11-chloro-dibenzo[bf][1,4]thiazepine is reacted with 2-(2-piperazin-1-ylethoxy)-ethanol to yield, following several processing steps, quetiapine. Compound I can then be further reacted with fumaric acid at elevated temperature to yield quetiapine fumarate. The resulting quetiapine fumarate obtained is suitable for use in pharmaceutical preparations.
Type:
Grant
Filed:
April 21, 2006
Date of Patent:
November 1, 2011
Assignee:
Medichem S.A.
Inventors:
Jordi Bosch I Lladó, Maria Carmen Burgarolas Montero, Iolanda Chamorro Gutiérrez
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:
July 14, 2010
Date of Patent:
September 27, 2011
Assignee:
Medichem, S.A.
Inventors:
Jordi Boschi I Llado, Maria Carmen Burgarolas Montero, Judit Masllorens Llinas
Abstract: The invention relates to a process for tightly controlling the particle size of cinacalcet hydrochloride, i.e. a process for preparing large or small crystals of cinacalcet hydrochloride, which yields cinacalcet hydrochloride in a narrow, reproducible and consistent distribution of particles, which hence does not require to reprocess, rework or destroy material of undesired size, which is efficient and cost-effective, and which is suitable for industrial implementation.
Abstract: The present invention relates to voriconazole, processes of preparing voriconazole, and pharmaceutical compositions and therapeutic uses thereof. In particular, the present invention also relates to voriconazole prepared from voriconazole having a substantially undefined shape and/or crystal habit. The invention further relates to voriconazole having a modified sphericity factor and/or specific surface area and/or Sauter diameter compared to voriconazole known from the prior art.
Type:
Application
Filed:
July 23, 2010
Publication date:
June 30, 2011
Applicant:
Medichem, S.A.
Inventors:
Ernesto Duran Lopez, Juan Contreras Lascorz