Akzo N.v.

Robert T Logan

Robert G Roy

James Redpath

George McGarry

David B McFadzen

John H Pick

Gilbert F Woods

James Cairns

The invention concerns a 4-aryl-imidazole derivative having the formula I ##STR1## wherein X is 0 or NOH,

4-aryl-imidazole derivatives

The invention relates to the use of the benzo[b]-thiophene-2-carboximidamide derivative having formula I ##STR1## or pharmaceutically acceptable salts thereof, for the preparation of a medicament which is suitable for the treatment of heart failure, having high bioavailability without inducing nausea, vomiting and/or restlessness.

Use of a benzo[b]thiopene-2-carboximidamide derivative

The invention concerns a 4-aryl-thiazole or imidazole derivative having the formula I ##STR1## wherein X is 0 or NOH,

4-aryl-thiazole derivatives

The invention provides novel pregnane derivatives having the formula: ##STR1## wherein X=F, Cl or Br; R.sub.1 =F or Cl; R.sub.2 =H(.beta.OH) or O; R.sub.3 =alkyl(1-4 C); R.sub.4 =alkyl(1-4 C); and the dotted line indicates the optional presence of a double bond. The novel compounds have been found to possess immunomodulating properties.

Pregnane derivatives as immunomodulators

A method is provided for treating patients suffering from or susceptible to bronchoconstriction, particularly for patients suffering from an asthmatic attach which comprises the use of benzothiophene, benzofuran, dihydronaphthalene or indene derivatives represented by formula I ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is independently H, (1-4C) alkyl, (1-4C) halogen substituted alkyl, OH, (1-4C) alkoxy, (1-4C) halogen substituted alkoxy, NO.sub.2, CN, halogen, an unsubstituted or (1-4C) alkyl substituted amino group, or wherein two adjacent groups R.sup.1, R.sup.2, R.sup.3 or R.sup.4 together form methylenedioxy;

Compounds with bronchodilator activity

The invention relates to pyridazinone compounds of the general formula I: ##STR1## wherein R.sup.1 represents one to four substituents, which may be the same or different and are selected from H, OH, halogen, NO.sub.2, unsubstituted or C1-C4 alkyl substituted amino, C1-C4 alkyl, C1-C4 halogen substituted alkyl, O--ALK--NR.sup.4 R.sup.5, C1-C4 alkoxy, whereby two substituents taken together may also represent a methylenedioxy group;

Pyridazinone derivatives

The invention relates to compounds of the general formula I ##STR1## wherein R.sub.1 represents one up to and including four, the same or different substituents selected from alkyl(1-6 C), alkoxy(1-6 C), hydroxy, halogen, NO.sub.2, CF.sub.3 or the group --NR.sub.5 R.sub.6, whereby two substituents taken together may also represent a methylene-dioxy group,

Positive inotrophic benzothiazole and benzothiophene compositions and

The invention relates to compounds of the general formula I ##STR1## wherein R.sub.1 represents one up to and including four, the same or different substituents selected from alkyl(1-6 C), alkoxy(1-6 C), hydroxy, halogen, NO.sub.2, CF.sub.3 or the group --NR.sub.5 R.sub.6,

Indene and naphthalene derivatives

The invention relates to compounds of the general formula I ##STR1## wherein R.sub.1 represents one up to and including four, the same or different substituents selected from alkyl(1-6 C), alkoxy(1-6 C), hydroxy, halogen, NO.sub.2 CF.sub.3 or the group --NR.sub.5 R.sub.6, whereby two substituents taken together may also represent a methylene-dioxy group,

Benzothiophene derivatives

The present invention relates to novel 21-alkylated steroids of the pregnane series having the formula: ##STR1## wherein R.sub.1 =alkyl (1-4 C); R.sub.2 =carboxyacyl (1-18 C); X=H, F or Cl; Y=O, H(OH), H(lower acyloxy), H(F) or H(Cl) with the proviso that Y is not H(F) when X is F; and the dotted line indicates the optional presence of a double bond, to processes for their preparation and to pharmaceutical compositions containing same. The novel compounds possess strong anti-inflammatory properties, when applied locally and cause little or systemic, thymolytic, adrenolytic and salt-retaining effects.

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Lanark, United Kingdom

Robert T Logan