Hovione Inter Limited

Plurichemie Anstalt

Hovione Scientia Limited

Hollis-eden Pharmaceuticals, Inc.

Merial Limited

Hovlone Inter Limited

Hovione Inter Ag

William Heggie

Philip R Page

Ivan Villax

Zita Mendes

Michael B Hursthouse

Luis Sobral

Jose Rafael Antunes

Susana Marto

Indira Ghatak

Clarence Nathaniel Ahlem

Jose Manuel Galindro

Dionisio Martin

Filipe Gaspar

João Bandarra

Alexandre J Ganchas De Carvalho

Patrick R Bazinet

Zita Maria De Mouro Vaz Azevedo Mendes

Pedro Santos

Luis Carvalho

Alexandre Carvalho

Joao J De Oliveira Bandarra

Richard Somerville

Luis D Carvalho

Luis Daniel Dos Anjos De Carvalho

John Naber

Filipe Tomas

Emilia Leitäo

Cristina Maria Sanches Simoes De Faria

Ana Cristina Cruz

João José Bandarra

Emilia Leitao

António Carlos Silva Henriques

Joana Baptista

José Galindro

Emilia Leitão

João António Moínho Bandarra

Antonio Carlos Silva Henriques

Jose Refael Antunes

Emilia Perpétua Tavares Leitao

Joao Bandarra

Pedro Paulo Santos

Zita Maria Mendes

Joao Jose De Oliveira Bandarra

Alexandre Jose De Carvalho

Jose Galindro

The invention relates to a process for the preparation of one or more intermediate chemical compounds useful in the preparation of non-ionic contrast agents wherein the process is carried out continuously using one or more flow procedures.

Process for the preparation of intermediates useful in the preparation of non-ionic contrast agents

A process for preparing compounds of formula [II] by esterification of the C-17 hydroxyl group of 6&#x3b1;,9&#x3b1;-difluoro-11&#x3b2;,17&#x3b1;-dihydroxy-16&#x3b1;-methyl-3-oxoandrosta-1,4-diene-17&#x3b2;-carbothioic acid, the compound of formula [I] comprises treating compound [I] with a slight excess of an acyl chloride of general formula R&#x2014;COCl, where R represents &#x2014;CH2CH3, &#x2014;CH2CH2CH3 or &#x2014;CH(CH3)2, in an inert solvent, in the presence of a tertiary amine.  Preferably the process is carried out using pyridine in the presence of acetone at a temperature of from 5&#xb0; C. to &#x2212;20&#xb0; C.

Process for the esterification of a carbothioic acid

The invention provides crystalline minocycline base. In particular, three crystalline polymorphic forms, designated Form I, Form II and Form III, of minocycline base are provided. These are characterized by XRD and IR data. Processes for preparing the new polymorphic forms are also provided. For example, Form I is prepared by dissolving and/or suspending amorphous minocycline base in an organic solvent chosen from ethers followed by crystallization from the mixture.

Crystalline minocycline base and processes for its preparation

Particles containing a tetracycline or one of its pharmaceutically acceptable salts and an antioxidant, formulations containing the same and their use in the treatment of infectious diseases are described. Methods of encapsulation of a tetracycline or one of its pharmaceutically acceptable salts and an antioxidant are also disclosed.

Particles of tetracyclines and protecting agent

A new compound, (S)-5-(2-acetoxypropanamido)-2,4,6-triiodoisophthalic acid, of formula II (S)-5-(2-acetoxypropanamido)-2,4,6-triiodoisophthalic acid. Said new compound is of use for the production of triiodinated contrast agent, especially lopamidol, with low content of acetyl and hydroxyacetyl analogs. The new compound may be formed from 5-amino-2,4,6-triiodoisophtalic acid by acylating with (S)-1-chloro-1-oxopropan-2-yl acetate. The new compound may then be converted to the respective acid dichloride by reacting with a chlorinating reagent, which is a further object of the present invention, followed by the amidation with 2-amino-1,3-propanediol and acetate hydrolysis. 

Manufacture of a triiodinated contrast agent

A process for obtaining 21-disodium phosphate pregnane derivative compounds of formula (I), wherein X&#x2550;R&#x2550;H or X&#x2550;F and R=&#x3b1;-CHor X&#x2550;F and R=&#x3b2;-CH: comprises spray drying a solution comprising compound of formula (I). 

Process for obtaining steroidal phosphate compounds

The present invention relates to methods for synthesizing macrolide compounds which are known to have antibacterial activity, and are useful in the therapy of bacterial infections in mammals. More specifically, the invention relates to methods for synthesizing the macrolide antibiotic, gamithromycin utilizing a novel configuration of catalysts, chemical structures, and/or methods. An embodiment of the present invention may include allowing multiple chemical reactions to proceed without the isolation of chemical intermediates. Thus, multiple reactions may occur in one reaction vessel allowing for a considerable decrease in the cycle-time. The present invention also provides a novel method for inhibiting degradation while isolating a structure of a pharmaceutical composition.

Method of synthesizing macrolide compounds

A process for producing tamsulosin of formula I and pharmaceutically acceptable addition salts, thereof comprises the steps of:      

Process for the preparation of tamsulosin and intermediates thereof

A process for the production of iohexol comprises alkylating 5-Acetamido-N,N'-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophthalamide using 2(2-methoxy-ethoxy)-ethanol as solvent in the presence of a base, and optionally isolating crude iohexol from the reaction mixture. Preferably, the alkylating agent is 1-chloro-2,3 propanediol and the base is an alkali metal hydroxide such as sodium hydroxide or potassium hydroxide.

Process for the manufacture of iohexol

The invention provides compositions comprising formula 1 steroids, e.g., 16&#x3b1;-bromo-3&#x3b2;-hydroxy-5&#x3b1;-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16&#x3b1;-bromo-3&#x3b2;-hydroxy-5&#x3b1;-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen (viral) replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using certain steroids and steroid analogs. The invention also provides methods to make and use these immunomodulatory compositions and formulations.

Pharmaceutical compositions and treatment methods

The invention provides compositions comprising, 16&agr;-bromo-3&bgr;-hydroxy-5&agr;-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16&agr;-bromo-3&bgr;-hydroxy-5&agr;-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen (viral) replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using certain steroids and steroid analogs. The invention also provides methods to make and use these immunomodulatory compositions and formulations.

A process for the purification of roxithromycin, an antibiotic for therapeutic purposes, in which the purification is carried out by the dissolution or suspension of the product in methanol followed by cooling. Purification may also be obtained by addition of a non-solvent and/or by concentration of the mixture, thus obtaining a purified product.

Process for the purification of roxithromycin

The invention provides a new process for the preparation of mometasone 17-furoate, a steroid derivative useful in the treatment of inflammatory disease, by direct esterification of the 17 hydroxyl group without prior protection of the free 11 hydroxy function.

Process for the preparation of mometasone furoate

The present invention refers to a process for the preparation of 4-(des-dimethylamino)-tetracyclines, which compounds have a therapeutical application. The starting tetracyclines are treated with a methylating agent and the resulting trimethylammonium salts are reduced by electrolysis in an aqueous solution at acidic pH, in the presence of an adequate electrolyte. A direct electrical current with a potential of 0.5-1.5 volts is applied between two convenient electrodes until the reaction is complete. The 4-(des-dimethylamino)-tetracyclines are isolated by extraction with an organic solvent.

Process for the preparation of 4-(des-dimethylamino)-tetracyclines

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William Heggie