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Assignee: Synthon BV


Location: Nijmegen, NL
No. of patents: 43

1    
NumberTitleIssue Date
8093387Process of making crystalline type II aripiprazole
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 soli...
01/10/2012
8030355Tablet composition with a prolonged release of tamsulosin
A tamsulosin controlled release tablet is formed using a water-swellable matrix-forming composition as a release controlling mechanism. The matrix forming composition comprises (i) a pH-sensitive swellable hydrophilic polymer, which is a cross-linked polyacrylic aci...
10/04/2011
8026388Process for making 1-hydroxyalkylidene-1,1-biphosphonic acids
Synthesis of biphosphonate compounds can be advantageously carried out in a solvent/diluent comprising a compound of formula (3) wherein R is hydrogen or a C1-C6 alkyl group; each of R1 is a C1-C6 alkyl group or both R1 gro...
09/27/2011
7989623Process for making n-(diphenylmethyl)piperazines
The compound of formula (8), in racemic or single enantiomeric form, is useful in making N-(diphenylmethyl)-piperazines such as cetirizine and levocetrizine. wherein Z is preferably phenyl. ...
08/02/2011
7977480Synthesis of paliperidone
A 9-hydroxy or 9-acyloxy group can be added to a pyridopyrimidinone ring structure by a process comprising acylating a compound of formula (5) under Vilsmeier-Haack or Friedel-Crafts conditions to form a compound (6); and transforming with a peroxo-compound to obtai...
07/12/2011
7959948Pharmaceutical composition of quetiapine fumarate
A pharmaceutical composition comprising (i) quetiapine or a pharmaceutically acceptable salt thereof, especially quetiapine fumarate; (ii) a mixed excipient comprising an intimate admixture of polyvinylacetate and polyvinylpyrrolidone in a weight ratio from 5:2 to 1...
06/14/2011
7932385Paliperidone ketone
A compound of formula (7.2) or an acid addition salt thereof. The compound can be used as a reference standard for monitoring the presence thereof in a paliperidone sample, including monitoring the completion of a paliperid...
04/26/2011
7928250Process for making duloxetine and related compounds
A compound of formula 10 is useful in making duloxetine. ...
04/19/2011
7928114Crystalline erlotinib
Crystalline Forms of erlotinib are made. The crystalline materials are useful as pharmaceutical active agents in treating various cancers as well as in forming erlotinib salts. ...
04/19/2011
7902198Crystalline aripiprazole solvates
Alcoholates of aripiprazole are useful as pharmaceuticals and/or as intermediates in making aripiprazole Form A or Form B. ...
03/08/2011
7875729Process for making asenapine
Asenapine and related trans-isomer bicyclic compounds can be obtained by reducing a compound of formula (C) to preferentially form a trans-isomer compound of formula (D), followed by subsequent ring closure to form a compound of formula (B) such as asenapine.
01/25/2011
7786138Process for making montelukast and intermediates therefor
A compound of the following formula wherein R′ is a straight or branched C1-C4 alkyl group is useful in processes associated with the synthesis of montelukast and its salts. ...
08/31/2010
7655806Process for purification of anastrozole
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. ...
02/02/2010
7655798Process of making crystalline Type II aripiprazole
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 soli...
02/02/2010
7642353Process of making crystalline aripiprazole
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. ...
01/05/2010
7601741Process for making montelukast and intermediates therefor
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
10/13/2009
7566793Process for resolving citalopram
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. ...
07/28/2009
7553853Solid-state montelukast
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 b...
06/30/2009
7531684Process for making aminoalkylphenyl carbamates and intermediates therefor
A process for making aminoalkylphenyl carbamates, especially rivastigmine, can use less severe conditions using bis(p-nitrophenyl)carbonate (IX) as a phenol activator compound. ...
05/12/2009
7476748Process for making montelukast and intermediates therefor
A process for making montelukast, a pharmaceutically useful compound of the following formula and salts thereof: using a compound of formula (11) is provided. ...
01/13/2009
7446116Montelukast amantadine salt
An amantadine salt of montelukast is useful in purification of montelukast or its salts and as a pharmaceutical active ingredient. ...
11/04/2008
7018658Pharmaceutical pellets comprising tamsulosin
Tamsulosin pellets having an advantageous release profile are formed. The pellets have an enteric coating and release less than 10% of the tamsulosin in two hours in SGF. ...
03/28/2006
6919087Pharmaceutical compositions comprising amlodipine maleate
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 amlodipi...
07/19/2005
6858738Process for making amlodipine, derivatives thereof, and precursors therefor
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 provid...
02/22/2005
6835853Process for resolution of tamsulosin and compounds, compositions, and processes associated therewith
Optically impure tamsulosin including racemic tamsulosin can be resolved into optically pure (R)- or (S)-tamsulosin by the use of diastereomeric sulfonate salts of tamsulosin in a fractional crystallization technique. Racemic tamsulosin free base is a useful startin...
12/28/2004
6830933Reference standards for determining the purity or stability of amlodipine maleate and processes therefor
Amlodipine aspartate and amlodipine maleamide are used as reference standards or markers in determining the purity of amlodipine maleate substances and products. ...
12/14/2004
6828339Amlodipine salt forms and processes for preparing them
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 desc...
12/07/2004
6818766Process for making bicalutamide and intermediates thereof
Bicalutamide and/or its intermediates are made by the use of p-fluorobenzenesulfinic acid salt as a reagent. ...
11/16/2004
6770761Process for preparation of 2-amino-6 (alkyl) amino-4,5,6,7-tetrahydrobenzothiazoles
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, R3 and R4 are either the same and each of them represents an alkoxy g...
08/03/2004
6727367Process for resolution of 2-amino-6-propylamino-4,5,6,7-tetrahydrobenzthiazole and compounds therefor
A process for resolving or enriching (R,S) 2-amino-6-propylamino-4,5,6,7-tetrahydrobenzothiazole (pramipexole) into optical isomers uses a monovalent salt thereof, e.g. pramipexole monohydrochloride, as a substrate. The monovalent salt is treated with an optically a...
04/27/2004
6717015Venlafaxine besylate
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 extende...
04/06/2004
6696496Low water-soluble venlafaxine salts
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....
02/24/2004
6653481Process for making amlodipine
Amlodipine and related analogues thereof are prepared by the following general reaction scheme: ##STR1## R1 and R2 each independently represent a C1 -C4 alkyl group. The process provides for the formation of com...
11/25/2003
6638535Modified release formulations containing a hypnotic agent
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 6...
10/28/2003
6602893Amide 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. ##STR1##...
08/05/2003
6600047Process for making amlodipine maleate
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 substanti...
07/29/2003
6562984Lactonization process
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 lact...
05/13/2003
6538012Amlodipine hemimaleate
Amlodipine hemimaleate is useful as a calcium channel blocker and can be used to treat or prevent angina or hypertension....
03/25/2003
6518288Amlodipine fumarate
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 ma...
02/11/2003
6479525Aspartate derivative of amlodipine
An amlodipine derivative having the following formula is useful, either alone or in combination with amlodipine, as a pharmaceutical in treating angina and hypertension. ##STR1##...
11/12/2002
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