Pennwalt Corporation

Fisons Ltd.

Astra Ab

Astra Aktiebolag

Edwin S Wu

John E Macor

Ronald C Griffith

Alexander Kover

Hans F Schmitthenner

William L Albrecht

A compound of formula ##STR1## X is O or S; Y is O or S; G and D are independently nitrogen or carbon with the proviso that no more than one of G, D, or E is nitrogen; E is N or C--R.sub.4 ; R.sub.1 is hydrogen or methyl; R.sub.2 is hydrogen or fluoro; R.sub.3 is hydrogen, halogen, C.sub.1 to C.sub.3 alkyl, --OR.sub.5, --CN, --CONH.sub.2, --CO.sub.2 R.sub.5, --NR .sub.5 R.sub.6 or phenyl optionally substituted with one to three of the following substituents: halogen, C.sub.1 to C.sub.3 alkyl, --NO.sub.2, --CN, or --OCH.sub.3 ; R.sub.4 is hydrogen, halogen, C.sub.1 to C.sub.3 alkyl, --OR.sub.5, --CN, --CONH.sub.2, --CO.sub.2 R.sub.5, --NR.sub.5 R.sub.6 or phenyl optionally substituted with one to three of the following substituents: halogen, C.sub.1 to C.sub.3 alkyl, --NO.sub.2, --CN, or --OCH.sub.3 ; or R.sub.2 and R.sub.3 or R.sub.3 and R.sub.4 may together represent a fused phenyl ring optionally substituted with one or two of the following substituents: halogen, C.sub.1 to C.sub.3 alkyl, --NO.sub.2, --CN, or --OCH.sub.3 ; R.sub.5 and R.sub.6 are independently hydrogen or C.sub.1 to C.sub.3 alkyl; or an enantiomer thereof, and pharmaceutically acceptable salts thereof, processes for preparing the, compositions containing them, and their use in therapy, especially in the treatment or prophylaxis of psychotic disorders and intellectual impairment disorders, as well as intermediates and use of intermediates in synthesis.

Azabicyclic esters of carbamic acids useful in therapy

Compounds of general formula I, ##STR1## wherein R.sup.1 represents hydrogen or alkyl C.sub.1-3, R.sup.2 represents hydrogen, alkyl C.sub.1-6, alkenyl C.sub.3-6 or alkynyl C.sub.3-6, n and m are integers from 1 to 3, provided that n+m=4, and one of X and Y represents CH.sub.2 and the other represents CHR.sup.3, C=CHR.sup.4 or C=NR.sup.5, in which R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13, R.sup.14, R.sup.15, R.sup.16 and R.sup.17 are as defined in the specification, and their salts are useful as pharmaceuticals, in particular as central muscarinic acetylcholine receptors. The compounds are therefore useful in the treatment of diseases such as presenile and senile dementia, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania and Tourette Syndrome, and also as analgesic agents for use in the treatment of severe painful conditions such as rheumatism, arthritis, and terminal illness.

Spirofurane derivatives

Compounds of general formula I, ##STR1## wherein R.sup.1 represents hydrogen or alkyl C.sub.1-3,

Compounds of general formula I, ##STR1## wherein: A represents (CH.sub.2).sub.m optionally substituted by R.sub.3,

Spiro-isoxazolidine derivatives as cholinergic agents

7-[3-[(3,4-dihydroxyphenethyl)amino]-2-hydroxypropoxy]-flavone hydrobromide, and related flavonoids are disclosed to inhibit leukotrienes and 5-lipoxygenase; preferred compounds also inhibit rat anaphylaxis.

Synthetic flavonoids as inhibitors of leukotrienes and 5-lipoxygenase

Compounds such as 6-[3-(cyclopropylamino)-2-hydroxypropoxy]aurone hydrochloride showing inhibitory activity against LTC.sub.4 -induced contraction of guinea pig ileum are useful as inhibitors of allergic reactions.

Aurone oxypropanolamines

Ester derivatives of N-substituted and N,N-disubstituted aminopropanoloxy flavones in which the aminopropanoloxy side chain is inserted at either the 5-, 6-, 7- or 8-position of the flavone nucleus, and N-substituted and N,N-disubstituted aminopropanoloxy flavones in which the aminopropanoloxy side chain is inserted at the 8-position of the flavone nucleus; useful as anti-dysrhythmic agents.

Flavonoxypropanolamines and esters of flavonoxypropanolamines as

In a process for preparing 7-[3-(propylamino)-2-hydroxypropoxy]flavone by the reaction of 7-(2,3-epoxypropoxy)flavone and n-propylamine, the improvement which resides in treating the beta-aminochalcone by-product with a weak organic acid to convert the chalcone to the desired aminated flavone.

Preparation of 7-(3-(propylamino)-2-hydroxypropoxy)flavone

Chromone derivatives such as 7-(3-n-propylamino-2-hydroxypropoxy)-2-phenyl-chromones which are useful as pharmaceuticals having antihypertensive properties.

Chromones

Chromone derivatives such as 7-(3-n-propylamino-2-hydroxypropoxy)-2,3-diphenylchromones which are useful as pharmaceuticals having antihypertensive properties.

Chromone derivatives such as 7-(3-amino-2-hydroxypropoxy)-3-phenylchromones which are useful for preparing other chemical compounds and for pharmaceutical uses such as antihypertensive and anti-inflammatory agents.

Isoflavones useful as anti-inflammatory agents

Chromone derivatives such as 6 or 7-(3-amino-2-hydroxypropoxy)-2-phenylchromones, -3-phenylchromones or -2,3-diphenylchromones which are useful as antihypertensive agents.

Growing community of inventors

Rochester, NY, United States of America

Edwin S Wu