The Boots Company Plc

Knoll Aktiengesellschaft

Abbott Laboratories Corporation

James Edward Jeffery

Antonin Kozlik

Eric C Wilmshurst

Paul Rafferty

David John Calderwood

Adrian John Fisher

John R Housley

Bruce Jeremy Sargent

David N Johnston

Bernard John Armitage

Colin Gerhart Pryce Jones

Colin Gerhart Jones

John Stuart Nicholson

Kenneth J Nichol

James G Tantum

Derek Whybrow

Eric C Wilmhurst

Imidazole derivatives for blocking the release of arachidonic acid from phospholipids

Imidazole derivatives as therapeutic agents

Compounds of formula I ##STR1## where R.sub.1 -R.sub.3, L.sub.1, T, L.sub.2 --N--Q--Y and R.sub.6 are as defined in the specification, and pharmaceutically acceptable salts thereof which are antiinflammatory, antiallergic and immunomodulant agents, compositions containing these compounds and processes to make them.

Phenoxy-, phenylthio-, benzoyl-alkyleneaminoalkylene-imidazole

Compounds of the formula I ##STR1## and pharmaceutically acceptable salts thereof in which R.sub.1 represents hydrogen, halo, cyano, cyanoalkyl, alkyl, alkoxy, phenoxy, phenyl, alkoxycarbonyl, --NR.sub.13 R.sub.14, --N(R.sub.15)SO.sub.2 R16, halogenated alkoxy, halogenated alkyl, arylalkoxy, hydroxy, phenylalkyl, alkoxycarbonylvinyl, --S(O).sub.n R.sub.7, alkoxycarbonylalkyl, carboxyalkyl, --CONR.sub.11 R.sub.12 carbamoylvinyl, --OSO.sub.2 R.sub.21, 4,5-dihydrothiazol-2-yl, 4,4-dimethyl-2-oxazolin-2-yl or --NR.sub.60 R.sub.61 ; or R.sub.1 represents a group of formula --(O).sub.z --L.sub.3 G wherein z equals 0 or 1, L.sub.3 represents a C.sub.1-4 alkylene chain, G represents a group of formula a), b), c), or d): a) --NR.sub.22 R.sub.23 ; b) --S(O).sub.m R.sub.26 ; c) CONR.sub.27 R.sub.28 ; d) --OR.sub.29 ; R.sub.2 and R.sub.3 independently represent hydrogen, halo, alkyl, alkoxy, --NR.sub.13 R.sub.14, halogenated alkoxy, halogenated alkyl, hydroxy, --S(O).sub.n R.sub.7 or --NR.sub.60 R.sub.61 ; L.sub.1 represents e) a bond, or f) alkylene, cycloalkylene or cycloalkylidene; T represents a bond or O, S, SO, SO.sub.2, a carbonyl group, or 1,3-dioxolan-2-ylidene; L.sub.2 represents alkylene, cycloalkylene, or cycloalkylidene; R.sub.6 represents hydrogen or alkyl (optionally substituted by alkoxycarbonyl or hydroxy); Q represents a C.sub.1-9 alkylene chain (optionally substituted by alkyl or hydroxy); and Y represents an optionally substituted imidazole ring; which are antiinflammatory, antiallergic and immunodulant agents. Compositions containing these compounds and processes to make them are also disclosed.

Therapeutic 1,4-thiazepines

A process for the preparation of N,N-dimethyl-1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutylamine hydrochloride monohydrate, a non-hygroscopic material which can be used as a pharmaceutical in the treatment of depression.

Process for the manufacture of

Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof; in which R.sub.1 and R.sub.2, which are the same or different, are H or an optionally substituted hydrocarbon group or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form an optionally substituted heterocyclic ring;

Arylcyclobutylmethylamine therapeutic agents

N,N-Dimethyl-1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutylamine hydrochloride monohydrate is a non-hygroscopic material which can be used as a pharmaceutical in the treatment of depression.

Therapeutic compound

Arylcyclobutylmethylamines

Compounds of formula I ##STR1## in which R.sub.1 is a heterocyclic ring containing one or more heteroatoms selected from N, O and S;

Antidepressant amines

Compounds of formula I ##STR1## in which R.sub.1 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-7 cycloalkyl, cycloalkylalkyl or optionally substituted phenyl; R.sub.2 is H or C.sub.1-3 alkyl; R.sub.3 and/or R.sub.4 are H, formyl, C.sub.1-3 alkyl, C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, C.sub.3-7 cycloalkyl or R.sub.3 and R.sub.4 together with the nitrogen atom form a heterocyclic ring system; R.sub.5 and/or R.sub.6 are H, halo, CF.sub.3, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, C.sub.1-3 alkylthio or R.sub.5 and R.sub.6 together with the carbon atoms to which they are attached form a second benzene ring show therapeutic activity in the treatment of depression. Pharmaceutical compositions and processes for preparing compounds of formula I are disclosed.

Therapeutic agents

Compounds of formula I ##STR1## in which R.sub.1 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-7 cycloalkyl, cycloalkylalkyl or optionally substituted phenyl; R.sub.2 is H or C.sub.1-3 alkyl; R.sub.3 and/or R.sub.4 are H, formyl, C.sub.1-3 alkyl, C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, C.sub.3-7 cycloalkyl or R.sub.3 and R.sub.4 together with the nitrogen atom form a heterocyclic ring system; R.sub.5 and/or R.sub.6 are H, halo, CF.sub.3, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, C.sub.1-3 alkylthio or R.sub.5 and R.sub.6 together with the carbon atoms to which they are attached form a second benzene ring show therapeutic acitivity in the treatment of depression. Pharmaceutical compositions and processes for preparing compounds of formula I are disclosed.

Growing community of inventors

Nottingham, United Kingdom

James Edward Jeffery