Patents Assigned to Synthon BV
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Patent number: 6653481Abstract: Amlodipine and related analogues thereof are prepared by the following general reaction scheme: R1 and R2 each independently represent a C1-C4 alkyl group. The process provides for the formation of compounds of formula (1) in good yield and purity. Further, the compounds of formula (1) can be used as calcium channel blockers or as reference standards or reference markers for checking the purity of amlodipine.Type: GrantFiled: August 27, 2001Date of Patent: November 25, 2003Assignee: Synthon BVInventors: Theodorus H. A. Peters, Franciscus B. G. Benneker, Pavel Slanina, Jiri Bartl
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Patent number: 6638535Abstract: Hypnotic pharmaceutical compositions are made from pellets and exhibit a modified release. Zolpidem or a pharmaceutically acceptable salt thereof is a typical hypnotic. The pellets are preferably spherical and exhibit a dissolution profile that includes 60% of the hypnotic agent being release from the pellet not earlier than 5 minutes from the start of a specified in vitro dissolution test. Although the modified release profile can include 50% of the hypnotic agent being released not earlier than 15 minutes after the start of the dissolution test, the pellet preferably does not contain a release rate controlling excipient or coating. Instead, microcrystalline cellulose and the active constitute the majority of the pellet, e.g. 90% or more. Spherical pellets are also made by a convenient method that is applicable to any pharmaceutically active agent.Type: GrantFiled: April 13, 2001Date of Patent: October 28, 2003Assignee: Synthon BVInventors: Jacobus M. Lemmens, Dennie J. M. van den Heuvel, Johannes J. Platteeuw, Frans van Dalen
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Publication number: 20030195249Abstract: Venlafaxine besylate compounds provide certain advantages over venlafaxine hydrochloride and are useful in forming pharmaceutical compositions and n treating venlafaxine-treatable diseases and conditions. Venlafaxine besylate can be easily formulated into an extended release dosage form including a hydrogel tablet as well as other matrix-based tablet compositions. A preferred tablet making process involves hot melt granulation.Type: ApplicationFiled: March 27, 2003Publication date: October 16, 2003Applicant: SYNTHON BVInventors: Rolf Keltjens, Johannes Jan Platteeuw, Juan Cucala Escoi, Inocencia Margallo Lana, Frantisek Picha, Montserrat Gallego Luengo
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Publication number: 20030190353Abstract: Low water soluble salts of venlafaxine, especially venlafaxine maleate, are provided. Such salts can provide a variety of dosage forms including hydrogel-based extended release dosage forms.Type: ApplicationFiled: March 27, 2003Publication date: October 9, 2003Applicant: SYNTHON BVInventors: Marinus J. M. Oosterbaan, Rolf Keltjens
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Publication number: 20030190352Abstract: Solid venlafaxine base can be advantageously employed in making pharmaceutical compositions, especially extended release compositions.Type: ApplicationFiled: March 27, 2003Publication date: October 9, 2003Applicant: SYNTHON BVInventors: Juan Cucala Escoi, Montserrat Gallego Luengo, Marinus J. M. Oosterbaan, Frantisek Picha
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Publication number: 20030190351Abstract: A pharmaceutical composition is provided comprising venlafaxine hydrochloride and sodium carboxymethyl cellulose. The composition can be formulated to provide controlled release of the venlafaxine hydrochloride.Type: ApplicationFiled: March 27, 2003Publication date: October 9, 2003Applicant: Synthon BVInventors: Johannes Jan Platteeuw, Inocencia Margallo Lana, Arturo Siles Ortega
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Patent number: 6602893Abstract: A derivative of amlodipine having the following formula is useful as a pharmaceutical, either alone or in combination with amlodipine, in treating angina and hypertension.Type: GrantFiled: August 27, 2001Date of Patent: August 5, 2003Assignee: Synthon BVInventors: Jacobus M. Lemmens, Theodorus H. A. Peters, Franciscus B. G. Benneker
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Patent number: 6600047Abstract: A process for making amlodipine maleate comprises reacting amlodipine or an acid addition salt thereof with maleic acid under an acidic environment to form an amlodipine maleate product. The process allows for the formation of amlodipine maleate substantially free from amlodipine aspartate.Type: GrantFiled: August 27, 2001Date of Patent: July 29, 2003Assignee: Synthon BVInventors: Franciscus B. G. Benneker, Pavel Slanina, Frantisek Picha
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Patent number: 6562984Abstract: Lactonization of statins can be achieved using a lactonization agent that forms a hydrated complex with the produced water that is insoluble in the reaction solvent. By binding the produced water in an insoluble complex, the reaction is pulled to the lactone side, using mild conditions in short reactions times and with reduced risk of impurities.Type: GrantFiled: March 11, 2002Date of Patent: May 13, 2003Assignee: Synthon BVInventors: Theodorus H. A. Peters, Frantisek Picha, Jacobus M. Lemmens
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Patent number: 6538012Abstract: Amlodipine hemimaleate is useful as a calcium channel blocker and can be used to treat or prevent angina or hypertension.Type: GrantFiled: August 27, 2001Date of Patent: March 25, 2003Assignee: Synthon BVInventor: Gerrit J. B. Ettema
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Patent number: 6521758Abstract: Tosylate salts are useful in purifying 4-(fluorophenyl)-3-carbinol-piperidines from the corresponding des-fluoro impurity. The purified compounds are advantageously used in paroxetine synthesis.Type: GrantFiled: May 14, 2001Date of Patent: February 18, 2003Assignee: Synthon BVInventors: Jacobus M. Lemmens, Theodorus H. A. Peters, Pavel Slanina
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Patent number: 6518288Abstract: Amlodipine fumarate salt compounds are useful as calcium channel blockers and in treating or preventing angina or hypertension. The fumarate salts avoid the formation of certain potential impurities that have been found to be associated with amlodipine maleate.Type: GrantFiled: August 27, 2001Date of Patent: February 11, 2003Assignee: Synthon BVInventors: Jacobus M. Lemmens, Theodorus H. A. Peters, Franciscus B. G. Benneker, Frantisek Picha
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Patent number: 6479525Abstract: An amlodipine derivative having the following formula is useful, either alone or in combination with amlodipine, as a pharmaceutical in treating angina and hypertension.Type: GrantFiled: August 27, 2001Date of Patent: November 12, 2002Assignee: Synthon BVInventors: Jacobus M. Lemmens, Theodorus H. A. Peters, Franciscus B. G. Benneker
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Patent number: 6281360Abstract: Imidazopyridine compounds of the formula 1 are can be made in high purity, e.g. greater than 95% pure, by a process that use a novel intermediate of formula 5: wherein R1 and R2 each independently represent hydrogen or a lower alkyl group and Y and Z each independently represent a lower alkyl group. By this process, zolpidem, a commercial pharmaceutical of the formula 1 can be effectively made.Type: GrantFiled: February 25, 2000Date of Patent: August 28, 2001Assignee: Synthon BVInventors: Gerrit Jan Bouke Ettema, Jacobus Maria Lemmens, Theodorus Hendricus Antonius Peters, Frantisek Picha
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Patent number: 6271398Abstract: A process for the production of simvastatin and its analogues that is efficient, economical and convenient involves the use of hydroxyl protected intermediates of formula (III) or (VII). These intermediates allow for direct alkylation of the butyrate side chain followed by deprotection and reformation of the lactone ring. R1 is hydrogen or methyl; R2 represents a straight or branched chain alkyl group having 1 to 8 carbon atoms, a cycloalkyl group having 3 to 7 carbon atoms, or an aralkyl group having 1 to 6 carbon atoms in the alkyl chain; R3 and R4 each independently represent an alkyl group, an ether group, a thioether group, an aryl group, an aralkyl group, an alkenyl group, a cyclic ether group, or a cyclic thioether group; and R5 and R6 each independently represent hydrogen, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, or an ether group.Type: GrantFiled: June 19, 2000Date of Patent: August 7, 2001Assignee: Synthon BVInventors: Frans Van Dalen, Jacobus Maria Lemmens, Gertruda Antonetta Philomina Van Helvoirt, Theororus Hendricus Antonius Peters, Frantisek Picha
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Patent number: 6242460Abstract: Zolpidem salts having improved physical stability do not exhibit a melting endotherm corresponding to zolpidem free base when heated at 5° C./minute from about 25° C. to 250° C. The salts are generally easy to reproduce, even on an industrial scale and are easier to handle due to the increased stability than the known zolpidem tartrate. The zolpidem salts are typically pharmaceutically acceptable salts and can be used in formulating pharmaceutical compositions and in pharmaceutical uses; e.g. as a hypnotic.Type: GrantFiled: November 26, 1999Date of Patent: June 5, 2001Assignee: Synthon BVInventors: Gerrit Jan Bouke Ettema, Jacobus Maria Lemmens, Theodorus Hendricus Antonius Peters, Frantisek Picha