Synthon B.v.

Synthon IP Inc.

Synthon Bct Technologies, LLC

Noven Therapeutics, LLC

Jacobus Maria Lemmens

Frantisek Picha

Theodorus H A Peters

Frans Van Dalen

Franciscus B G Benneker

Theodorus Hendricus Antonius Peters

Hans Jan Hoorn

Gerrit Jan Bouke Ettema

Theodorus Hendricus Antonium Peters

Franciscus Bernardus Gemma Benneker

Johannes Jan Platteeuw

Rolf Keltjens

Gerrit J B Ettema

Pavel Slanina

Karel Pospisilik

Dennie J M Van Den Heuvel

Franciscus Bernardus Benneker

Theodorus Hendricus Peters

Gertruda Antonetta Philomina Van Helvoirt

Theororus Hendricus Antonius Peters

Johannes J Platteeuw

Peter F A Bakker

Arlette Vanderheijden

The invention relates to a compound, and pharmaceutically acceptable salts, having the formula I: wherein:

Crystalline paroxetine methane sulfonate

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.

Amlodipine free base

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. 

Amide derivative of amlodipine

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 

An amlodipine maleate pharmaceutical composition is provided with good stability when formulated with a pH within the range of 5.5 to 7, when measured as a 20 wt % aqueous slurry. The stability can also be aided by making the pharmaceutical composition from amlodipine maleate particles having an average particle size of greater than 20 microns, preferably greater than 100 microns.

Pharmaceutical compositions comprising amlodipine maleate

The invention relates to a compound, and pharmaceutically acceptable salts, having the formula I:wherein:

4-phenylpiperidine compounds

Amlodipine aspartate and amlodipine maleamide are used as reference standards or markers in determining the purity of amlodipine maleate substances and products.

Reference standards for determining the purity or stability of amlodipine maleate and processes therefor

Amlodipine besylate forms are described, including amlodipine besylate hydrates and novel amlodipine besylate anhydrates. A method of making various amlodipine besylate forms from an aqueous medium as well as the use of the same as a calcium channel blocker are described.

Amlodipine salt forms and processes for preparing them

A new process to obtain pramipexole and related products is described. The process involves the reaction of new compounds of formula (6), wherein R is hydrogen or acyl group, R and R are either the same and each of them represents an alkoxy group of 1-4 carbons or they together form a C -C alkylenedioxy group or an oxo-group, with an alkylamine in the presence of a reducing agent or a hydrogen gas with hydrogenation catalyst. A process to obtain new compounds of formula (6) is also described.

Process for preparation of 2-amino-6 (alkyl) amino-4,5,6,7-tetrahydrobenzothiazoles

The synthesis of paroxetine can be made more convenient by using a solvent system comprising an aliphatic alcohol and a hydrocarbon co-solvent. The solvent system is used particularly in the hydrolysis of paroxetine phenylcarbamate and preferably uses butanol and toluene as the system.

Process for the production of paroxetine

Paroxetine salt compositions having improved stability are formed by controlling the pH to 6.5 or less. The compositions can be made with the aide of water without significant coloration problems. The paroxetine salts include paroxetine hydrochloride salts but preferably use paroxetine sulfonate salts such as paroxetine methane sulfonate.

Paroxetine compositions and processes for making the same

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.

Modified release formulations containing a hypnotic agent

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.

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.

Lactonization process

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.

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Jacobus Maria Lemmens