Abstract: The invention relates to a process for the preparation of 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid and of the trihydrated monosodium salt thereof, consisting of reacting 4-aminobutyric acid with a phosphonation mixture formed by phosphorous acid and methanesulfonic anhydride and thereafter hydrolyzing the product of said reaction and isolating the products by adjustment of the pH.
Type:
Grant
Filed:
January 28, 2002
Date of Patent:
June 3, 2003
Assignee:
Medichem, S.A.
Inventors:
Jordi Bosch i Lladó, Eugenia Pagans Lista, Ma del Carmen Onrubia Miguel
Abstract: The invention describes a process for the preparation of pharmaceutical grade gabapentin, consisting of neutralizing an alcoholic solution of gabapentin hydrochloride with basic ion exchange resins and thereafter directly isolating the gabapentin, without requiring either the formation or the isolation of intermediates other than the pharmaceutical grade product.
Type:
Grant
Filed:
October 18, 2001
Date of Patent:
March 4, 2003
Assignee:
Medichem, S.A.
Inventors:
Jordi Bosch Lladó, Mà del Carmen Onrubia Miguel, Eugènia Pagans Lista
Abstract: The invention discloses a process for the preparation of the polymorh A of doxazosin meylate, consisting essentially of reacting doxazosin base with methanesulfonic acid in a mixture of solvents containing an alcohol and a chlorinated solvent, subsequently removing the chlorinated solvent by distillation and precipitating the desired product in an alcohol, after heating the suspension formed to the reflux temperature of the solvent.
Type:
Grant
Filed:
August 14, 2001
Date of Patent:
February 25, 2003
Assignee:
Medichem, S.A.
Inventors:
Carmen Arnalot I Aguilar, Jordi Bosch I Lladó, Ma Carmen Onrubia Miguel
Abstract: The non-hydrated gabapentin polymorph is prepared by drying an aqueous solution of gabapentin by spray drying or turbo-drying and it is used for the preparation of pharmaceutical grade gabapentin by subjecting the polymorph to crystallisation from solvents.
Type:
Grant
Filed:
November 21, 2000
Date of Patent:
February 18, 2003
Assignee:
Medichem, S.A.
Inventors:
Jordi Bosch Lladó, Rafael García Cruz, Elias Molins Grau, Maria del Carmen Onrubia Miguel
Abstract: A process for the preparation of venlafaxin and/or the physiologically acceptable addition salts thereof that consists of reacting a compound of general formula (II) where R is a C1-C10 alkyl, aryl, aralkyl or cycloalkyl group of 3 to 6 atoms of carbon, with a organomagnesium compound of general formula (III) where X is an atom of halogen and, if desired, a salt of the thus obtained venlafaxin is formed by reaction thereof with a physiologically acceptable acid.
Type:
Grant
Filed:
January 25, 2002
Date of Patent:
January 14, 2003
Assignee:
Medichem, S.A.
Inventors:
Carmen Arnalot i Aguilar, Jordi Bosch i Lladó, Pelayo Camps Garcia, Maria del Carmen Onrubia Miguel, Núria Soldevilla Madrid
Abstract: The form B of paroxetine maleate polymorph is characterized by determined data of X ray diffraction: it has a chemical stability which is superior to that of the form A of paroxetine maleate. This superior stability enables to use the new polymorph for the fabrication of medicaments intended to the treatment of troubles related to dysfunctions of the central nervous system. The process for producing the paroxetine maleate comprises the preparation of paroxetine maleate solution and a consequent precipitation.
Type:
Grant
Filed:
January 4, 2001
Date of Patent:
August 27, 2002
Assignee:
Medichem, S.A.
Inventors:
Alberto Stampa Diez del Corral, Jordi Bosch Lladó, Elias Molins Grau, Maria del Carmen Onrubia Miguel
Abstract: The process consists of the reductive coupling between the compounds: 8-chloro-5,6-dihydrobenzo[5,6]cyclohepta[1,2-b]pyridin-11-one (formula VII) ##STR1## and ethyl 4-oxopiperidine-1-carboxylate (formula IV) ##STR2## through the action of low-valent titanium species.
Type:
Grant
Filed:
April 13, 1998
Date of Patent:
July 4, 2000
Assignee:
Medichem, S.A.
Inventors:
Alberto Stampa, Pelayo Camps, Gloria Rodriguez, Jordi Bosch, Maria del Carmen Onrubia
Abstract: New polycyclic aminopyridine compounds which are acetylcholinesterase inhibitors, process for preparing them and their use. The polycyclic aminopyridine compounds correspond to the formula ##STR1## in which the various radicals have the meanings stated in the specification. The process for preparing these compounds is characterized in that ketones of general formula (II) are reacted with aminonitriles of general formula (III) and, if necessary, the compounds of formula (I) are alkylated, aralkylated or acylated, or alternatively the corresponding keto precursor is reduced. The compounds of the general formula (I) are especially suitable for the preparation of medicaments against memory disorders such as senile dementia or Alzheimer's disease.
Type:
Grant
Filed:
August 12, 1997
Date of Patent:
October 12, 1999
Assignee:
Medichem, S.A.
Inventors:
Pelayo Camps Garcia, Diego Munoz-Torrero Lopez-Ibarra, Diana Marina Gorbig Romeu, Joan Contreras Lascorz, Monserrat Simon Fornell, Jordi Morral Cardoner, Rachid El Achab, Albert Badia Sancho, Josep Eladi Banos Diez, Nuria Maria Vivas
Abstract: This invention refers to a new process for the preparation of D-(-)-3-acetylthio-2-methylpropionic acid, an important intermediate in the synthesis of the antihypertensive Captopril, consisting of the resolution of the racemic mixture of said acid through formation of the mixture of the diastereomeric salts thereof, in an appropriate solvent, with the low molecular weight L-(+)-2-aminobutanol as a base, selective crystallization of the diastereomeric salt of D-(-)-3-acetylthio-2-methylpropionic acid with L-(+)-2-aminobutanol and release of the D-(-)-3-acetylthio-2-methylpropionic acid through displacement of the base with a stronger acid.
Type:
Grant
Filed:
October 19, 1993
Date of Patent:
November 22, 1994
Assignee:
Medichem, S.A.
Inventors:
Alberto Stampa Diez Del Corral, Maria del Carmen Onrubia Miguel, Jose Irurre Perez
Abstract: A process for the preparation of 4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxides, of the formula: ##STR1## in which R may be phenyl, aryl substituted with halogen (Cl, Br or I) or with C.sub.1 -C.sub.6 alkyl groups, 2, 3 or 4-pyridyl or pyridyls substituted with halogen (Cl, Br or I) or with C.sub.1 -C.sub.6 alkyl groups, 5-methyl-isoxazolyl or 2-thiazolyl.In the process a C.sub.1 -C.sub.6 alkyl 4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxylate 1,1-dioxide is reacted with a magnesium derivative of formula:R-NH-Mg-Xin which X is halogen, preferably Br and R is the same as defined for formula (I). The compounds produced by the described process have analgesic and antiinflammatory properties.