Apotex Inc.

Other

Khashayar Karimian

Tim Fat Tam

Wanren Li

Regis C Leung-Toung

Sue S Lee

Denis Desilets

Mehrnoush Motamedi

Tullio Cappelletto

Yong Tao

Yiwei Li

Salvatore Zinghini

Bo Lei

Tao Xin

Ian Egle

Jolanta Maria Wodzinska

Rudolf Kubela

Yuri Goldberg

Regis C S H Leung-Toung

Steve Patrick Bryson

Gary Doucette

John F Braganza

A novel form of azithromycin and processes for preparation of pure azithromycin monohydrate isopropanol clathrate (3 molecules of isopropanol for every 10 molecules of azithromycin monohydrate) has been obtained. Preparation of the novel form of azithromycin comprises the steps of dissolving azithromycin in isopropanol, followed by the slow addition of water to the organic solution.

Azithromycin monohydrate isopropanol clathrate and methods for the manufacture thereof

A process is disclosed for the preparation of simvastatin which enables highly regio selective C-methylation of the 2&prime;-position group of lovastatin without requiring protection/deprotection of 13-OH of lovastatin and lactone ring opening/closure.

Process to manufacture simvastatin and intermediates

Thiadiazole compounds useful as inhibitors of cysteine activity dependent enzymes

Novel 1,2,4-thiadiazole compounds are provided, which are effective as inhibitors of cysteine activity-dependent enzymes and in particular of cysteine proteases. The compounds are useful in treating acne by inhibition of transglutaminase, common cold by inhibition of human rhinovirus 3C protease and inflammatory joint disease by inhibition of cathepsins. The compounds of the present invention are 3,5-disubstituted 1,2,4-thiadazole of the general formula (I): ##STR1## where Z is a nitrogen containing group with recognition sequence for the enzyme and Y is a substituent that tunes the reactivity of the inhibitor towards the thiol group of the cysteine activity-dependent enzyme. The Y group may also serve in recognition.

Thiadiazole compounds useful as inhibitors of cysteine activity

Thiols are trapped, and converted to disulfide compounds, by a process of reacting them with compounds containing a 1,2,4-thiadiazole ring structure carrying a substituent at position 3 of the thiadiazole ring, and being unsubstituted at position N-2. The process is useful pharmacologically, in inhibiting certain thiol-containing enzymes such as H.sup.+ /K.sup.+ -ATPase (the proton pump), and industrially, in selective removal of thiol compounds from gas or liquid mixtures.

Process for scavenging thiols

Novel thiadiazole compounds are provided, which are effective as proton pumps inhibitors, useful in treating peptic ulcers by inhibition of the proton pump enzyme H.sup.+ /K.sup.+ -ATPase. The compounds are 3-substituted 1,2,4-thiadiazolo [4,5-.alpha.]benzimidazole and 3-substituted imidazo[1,2-d]-1,2,4-thiadiazoles corresponding to the general formula: ##STR1## where X and Z either represent an optionally substituted benzene ring fused to the diazole nucleus, or represent a variety of independent chemical groupings (hydrogen, lower alkyl, halo, etc.) and Y is selected from a wide range, e.g. heterocyclics and carbonyl groups.

Proton pump inhibitors

Process for the manufacture of bis-triazole compounds and intermediates

Novel 3,5-disubstituted 1,2,4-thiadiazole compounds are provided, which are effective in treating peptic ulcers by the inhibition of H.sup.+ /K.sup.+ -ATPase. The compounds of the present invention are 3,5-disubstituted 1,2,4-thiadiazole corresponding to the general formula (I): ##STR1## where R.sup.1 is a group with cell penetration properties for the inhibition of the enzyme in-vitro and in-vivo, and Y is a substituent that tunes the reactivity of the inhibitor towards the cysteine residue of H.sup.+ /K.sup.+ -ATPase. The Y group may also serve in recognition.

Thiadiazole compounds useful as inhibitors of H.sup.+ /K.sup.+  atpase

Methods for the manufacture of cetirizine

Novel process for the preparation of quinolone carboxylic acid derivatives of general formula I, and intermediates thereof as illustrated in Scheme 1 wherein the key intermediate is a compound of formula IX. ##STR1##

Methods for the manufacture of quinolone carboxylic acids derivatives

Process for the manufacture of triazolone compounds and in particular nefazodone and intermediates useful in the manufacture thereof.

Methods for the manufacture of neofazodone

A process for preparing pure amorphous cefuroxime axetil comprising the steps of dissolving crystalline cefuroxime axetil in a highly polar organic solvent and adding the resulting solution to water, or alternatively, dissolving crystalline cefuroxime axetil in a highly polar solvent and adding small quantities of water to the organic solution and adding the resulting organic-aqueous solution to water.

Methods for the manufacture of amorphous cefuroxime axetil

Process for the manufacture of naphthylmethylamine derivatives and among them terbinafine as potential antimycotic agents.

Methods for the manufacture of terbinafine

The invention relates to a novel process to prepare 1,4-dihydropyridines and in particular amlopidine and in novel intermediates obtained during the synthesis of the 1,4-dihydropyridines which have potential activity as antihypertensive agents.

Growing community of inventors

Mississauga, Canada

Khashayar Karimian