Abstract: Crystalline aripiprazole Type II can be formed without solid state heat treatment. Instead a liquid is used such as in crystallizing from a solvent, especially 2-propanol, dimethyl sulfoxide, or a combination thereof with ethyl acetate, or in a solvent mediated solid-solid transformation, typically in ethyl acetate.
Type:
Grant
Filed:
December 24, 2009
Date of Patent:
January 10, 2012
Assignee:
Synthon BV
Inventors:
Gerrit J. B. Ettema, Raymond J. H. Westheim, Faysal Kalmoua
Abstract: Crystalline aripiprazole Type II can be formed without solid state heat treatment. Instead a liquid is used such as in crystallizing from a solvent, especially 2-propanol, dimethyl sulfoxide, or a combination thereof with ethyl acetate, or in a solvent mediated solid-solid transformation, typically in ethyl acetate.
Type:
Grant
Filed:
March 17, 2006
Date of Patent:
February 2, 2010
Assignee:
Synthon BV
Inventors:
Gerrit J. B. Ettema, Raymond J. H. Westheim, Faysal Kalmoua
Abstract: Anastrozole can be purified by crystallization from an aqueous-based solvent system. The aqueous-based solvent system can contain dilute acid, or an alcohol or both.
Abstract: Crystalline aripiprazole Form B can be formed by crystallizing from a solvent selected from 1-propanol, 2-propanol, 1-butanol, ethyl acetate, acetonitrile or a combination thereof.
Type:
Grant
Filed:
November 18, 2005
Date of Patent:
January 5, 2010
Assignee:
Synthon BV
Inventors:
Gerrit Jan Ettema, Raymond Westheim, Faysal Kalmoua
Abstract: The reaction of methylmagnesium halide is improved by the presence of a cerium (III) salt such as cerium trichloride. The reactions are typically associated with the production of montelukast, a pharmaceutically useful compound of the following formula and salts thereof. Further enhancements can be derived from certain intermediates, salts thereof and/or purification thereof before and/or after the reaction involving methylmagnesium halide.
Type:
Grant
Filed:
November 20, 2006
Date of Patent:
October 13, 2009
Assignee:
Synthon BV
Inventors:
Petr Benovsky, Lambertus Thijs, Arjanne Overeem, Jakub Castulik, Jie Zhu, Petr Bartos, Radomir Skoumal
Abstract: The (S)-citalopram content of a mixture of (R)- and (S)-citalopram can be enriched by using L-tartaric acid as the resolving agent in the presence of formaldehyde.
Abstract: A solid form of a compound of formula 1: is provided. The compound of formula 1 can be obtained in solid state by precipitation from a solution containing the same. The compound is useful as leukotriene antagonist and can be formulated into a pharmaceutical composition that also includes a pharmaceutically acceptable excipient.
Type:
Grant
Filed:
October 8, 2004
Date of Patent:
June 30, 2009
Assignee:
Synthon BV
Inventors:
Arjanne Overeem, Dennie J. M. van den Heuvel
Abstract: A process for making aminoalkylphenyl carbamates, especially rivastigmine, can use less severe conditions using bis(p-nitrophenyl)carbonate (IX) as a phenol activator compound.
Abstract: A process for making montelukast, a pharmaceutically useful compound of the following formula and salts thereof: using a compound of formula (4) is provided.
Type:
Grant
Filed:
March 17, 2005
Date of Patent:
March 10, 2009
Assignee:
Synthon IP, Inc.
Inventors:
Arjanne Overeem, Reinerus G. Gieling, Jie Zhu, Lambertus Thijs
Abstract: Desvenlafaxine is formed from venlafaxine by the use of a demethylating agent comprising a metal sulfide, such as sodium sulfide, and optionally selenium.
Abstract: A process for making montelukast, a pharmaceutically useful compound of the following formula and salts thereof: using a compound of formula (11) is provided.
Type:
Grant
Filed:
November 20, 2006
Date of Patent:
January 13, 2009
Assignee:
Synthon BV
Inventors:
Petr Benovsky, Lambertus Thijs, Arjanne Overeem, Jakub Castulik, Jie Zhu, Petr Bartos, Radomir Skoumal
Abstract: Several salts of olanzapine, including olanzapine malonate, olanzapine glycolate, olanzapine maleate, and olanzapine benzoate, have been found to have favorable solid state characteristics.
Abstract: The formation of risperidone is enhanced by the use of enriched Z-isomer oxime intermediate(s) of formula (3) or (7). The oxime(s) can be isomerically enriched by a variety of techniques including the use of the novel acetic acid salt thereof, which affords, inter alia, resolution of the isomers and/or by heat conversion.
Abstract: Amlodipine free base can be formulated into a convenient oral dosage form, especially a tablet, without excessive stickiness or tablet punch residue. The amlodipine free base can be crystalline Form I or a novel Form II. Methods of making and using the amlodipine free base are set forth.
Type:
Grant
Filed:
December 21, 2001
Date of Patent:
February 26, 2008
Assignee:
Synthon IP Inc.
Inventors:
Jacobus M. Lemmens, Theodorus H. A. Peters, Franciscus B. G. Benneker, Rolf Keltjens