Beecham Group Plc

Smithkline Beecham Corporation

Smithkline Beegham P.l.c.

John M Evans

Geoffrey Stemp

Frederick Cassidy

Mervyn Thompson

Robin E Buckingham

Kenneth Willcocks

Neil Upton

Wai Ngor Chan

Charles S Fake

Robert N Willette

Valerie A Ashwood

Graham A Showell

Helen Kate Morgan

Roger Edward Markwell

Gordon Burrell

Charles D Nicholson

Dieter Angersbach

Andrew Parsons

Antonio Kuok Vong

Kuok Keong Vong

Benzopyran derivatives and analogs are disclosed as useful for the treatment and/or prophylaxis of neuralgia, trigeminal neuralgia, neuropathic pain, dental pain and cancer pain.

Use of benzopyranols to treat neurological disorders

This invention relates to substituted benzopyran amides useful in treating certain medical conditions and to processes for preparing these compounds.

Benzopyrans and their use as therapeutic agents

A compound of formula (I) or pharmaceutically acceptable salt thereof: ##STR1## wherein either Y is N and R.sub.2 is hydrogen, or Y is C--R.sub.1 ; where either one of R.sub.1 and R.sub.2 is hydrogen and the other is selected from the class of hydrogen, C.sub.3-8 cycloalkyl, C.sub.1-6 alkyl optionally interrupted by oxygen or substituted by hydroxy, C.sub.1-6 alkoxy or substituted arminocarbonyl, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkoxy, nitro, cyano, halo, trifluoromethyl, CF.sub.3 S, or a group CF.sub.3 --A--, or a group CF.sub.2 H--A'--, trifluoromethoxy, C.sub.1-6 alkylsulphinyl, perfluoro C.sub.2-6 alkylsulphonyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxysulphinyl, C.sub.1-6 alkoxysulphonyl, aryl, heteroaryl, arylcarbonyl, heteroarylcarbonyl, phosphono, arylcarbonyloxy, heteroarylcarbonyloxy, arylsulphinyl, heteroarylsulphinyl, arylsulphonyl, heteroarylsulphonyl, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.1-6 alkyl-thiocarbonyl, C.sub.1-6 alkoxy-thiocarbonyl, C.sub.1-6 alkyl-thiocarbonyloxy, 1-mercapto C.sub.2-7 alkyl, formyl, or aminosulphinyl, aminosulphonyl or aminocarbonyl, or C.sub.1-6 alkylsulphinylamino, C.sub.1-6 alkylsulphonylamino, C.sub.1-6 alkoxysulphinylamino or C.sub.1-6 alkoxysulphonylamino, or ethylenyl terminally substituted by C.sub.1-6 alkylcarbonyl, nitro or cyano, or --C(C.sub.1-6 alkyl)NOH or --C(C.sub.1-6 alkyl)NNH.sub.2, or one of R.sub.1 and R.sub.2 is nitro, cyano or C.sub.1-3 alkylcarbonyl and the other is methoxy or amino optionally substituted by one or two C.sub.1-6 alkyl or by C.sub.2-7 alkanoyl; or R.sub.1 and R.sub.2 together are --(CH.sub.2).sub.4 -- or --CH.dbd.CH--CH.dbd.CH--, or form an optionally substituted triazole or oxadiazole ring; R.sub.3 to R.sub.9 represent various substituent groups; and X is oxygen or NR.sub.10 where R.sub.10 is hydrogen or C.sub.1-6 alkyl.

Pharmaceutical composition containing bicyclic type compounds

Bicyclic compounds with pharmaceutical activity

Benzopyran-3-ols having anxiolytic and anticonvulsant activity are claimed.

Benzo- and pyridopyran derivatives having anxiolytic and anti-convulsant

C.sub.4 -amide substituted compounds and their use as therapeutic agents

The invention relates to certain cis and trans benzopyrans having substituted benzamides at position C-4 and to their use in treating and/or preventing certain CNS disorders.

Treatment

4-(Fluorobenzoylamino)-3,4-dihydro-benzopyran derivatives are disclosed to possess anxiolytic and anti-convulsant activities.

Compounds of the formula (I) or pharmaceutically acceptable salts thereof ##STR1## where R.sub.2 -R.sub.7, Y, a and b are as defined, are useful in the treatment of hypertension and respiratory tract disorders.

Amino pyrimidin-7-yl substituted benzopyrans for treatment of

A compound of the following formula: ##STR1## wherein: R.sub.1 and R.sub.2 is hydrogen or C.sub.1-4 alkyl or R.sub.1 and R.sub.2 together are C.sub.2-5 polymethylene; R.sub.3 is hydroxy, C.sub.1-6 alkoxy or C.sub.1-7 alkylcarbonyloxy; R'.sub.4 is ethyl, isopropyl, t-butyl or cyclopentyl, and R.sup.1.sub.6 is hydrogen or C.sub.1-6 alkyl.

Benzopyran intermediates

A compound of the formula ##STR1## wherein: one of R.sub.1 and R.sub.2 is hydrogen or C.sub.1-4 alkyl and the other is C.sub.1-4 alkyl or R.sub.1 and R.sub.2 together are C.sub.2-5 polymethylene; and R'.sub.4 is ethyl, isopropyl, t-butyl or cyclopentyl.

Epoxybenzopyrans

A pharmaceutical product comprising a potassium channel activator antihypertensive agent and a .beta.-blocker antihypertensive agent as a combined preparation for simultaneous, separate or sequential use in therapy of hypertension.

Pharmaceutical preparations

Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: X, Y and R.sub.1 -R.sub.6 are as defined have blood pressure lowering activity and K+ channel activator activity and are useful in the treatment of hypertension.

Active compounds

A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein all the symbols are defined in the specification; having pharmacological activity, including blood pressure lowering activity, a process and intermediates for their preparation and their use as pharmaceuticals.

Growing community of inventors

Roydon, United Kingdom

John M Evans