The Boots Company Plc

Knoll Aktiengesellschaft

Knoll Aktiengesellachaft

Roy V Davies

James Fraser

Kenneth J Nichol

Sharon C Cheetham

Frank Kerrigan

Paul Anthony Bradley

Gerald Bernard Tometzki

Malcolm F Sim

Roger Bernard Titman

David B Yates

David George Webber

Michael Henry Hockley

Nicholas J Holman

Raymond Parkinson

Michael D Brown

Richard D Green

Condensed thiazole derivatives, having 5-HT receptor affinity

A compound of the formula (I), ##STR1## as defined in the specification, having immunomodulatory activity, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the compound, and processes to make and to use the compound are described.

Azolyl-cyclic amine derivates with immunomodulatory activity

Quinolone sulphonates having antihypertensive activity

Novel 7(4H)-thieno[3,2-b]pyridinones of the formula I, ##STR1## wherein R is lower alkyl, and R.sub.1 is hydrogen, lower alkyl, lower alkoxy, halo, trifluoromethyl, or phenyl optionally substituted with one or two substituents selected from halo, lower alkyl, lower alkoxy and trifluoromethyl. The compounds are useful in the treatment of cardiovascular diseases. Pharmaceutical compositions containing the novel compounds and processes for preparing the novel compounds are also described.

Thieno[3,2-b]pyridine-6-carboxamide compounds useful in treating

Quinolones of the formula I ##STR1## in which the dotted line between positions 2 and 3 of the quinolone ring represents an optional bond; R is hydrogen or lower alkyl; R.sub.1 is lower alkyl; and R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, are hydrogen, halo, lower alkyl, lower alkoxy, lower alkylthio, lower alkylsulphinyl, lower alkylsulphonyl, trifluoromethyl, cyano, fluorinated lower alkoxy, phenyl optionally substituted by one or two substituents selected from lower alkyl, lower alkoxy, lower alkylthio, halo and trifluoromethyl, the group --OAr or the group --S(O).sub.n Ar in which Ar is phenyl optionally substituted by one or two substituents selected from lower alkyl, lower alkoxy, lower alkylthio, halo and trifluoromethyl and n is 0, 1 or 2, or the group --NR.sub.5 R.sub.6 or the N-oxide thereof in which R.sub.5 and R.sub.6, which may be the same or different, are lower alkyl or, together with the nitrogen atom to which they are attached, form a 5-7 membered ring optionally containing an additional hetero atom selected from oxygen, nitrogen and sulphur have utility as antihypertensive agents. Novel quinolones are those of the above-defined formula I, provided that (a) when the optional 2,3-bond is present R.sub.1 is methyl and R is hydrogen, at least one of R.sub.2, R.sub.3 and R.sub.4 is other than hydrogen and (b) when the optional 2,3-bond is present, R is lower alkyl and R.sub.3 and R.sub.4 are hydrogen, R.sub.2 is other than hydrogen or lower alkoxy. Pharmaceutical compositions comprising a novel quinolone of the above formula I together with a pharmaceutically acceptable carrier are described and claimed. Processes for preparing the novel quinolones are also described.

1,4dihydroquinoline-3-carboxamides

Quinolones with antihypertensive activity have the general formula I, ##STR1## wherein X is the residue of an optionally substituted benzene ring; R is lower alkyl; R.sub.3 is hydrogen or lower alkyl; R.sub.1 and R.sub.2, which may be the same or different, are hydrogen, lower alkyl, or, together with the nitrogen atom to which they are attached, form a 5 to 7 membered saturated heterocyclic ring optionally containing an additional hetero atom selected from nitrogen, oxygen and sulphur and optionally substituted by 1 or more lower alkyl groups; and the dotted line between positions 2 and 3 of the quinolone nucleus represents an optional bond. The compounds are useful as antihypertensive agents. They are also indicated for use in treating heart failure and ischaemic heart disease. With the exception of the three compounds 1-methyl-4-oxo-1,4-dihydroquinoline-3-sulphonamide, 1,N-dimethyl-4-oxo-1,4-dihydroquinoline-3-sulphonamide and 6,7-dimethoxyl-methyl-4-oxo-1,4-dihydroquinoline-3-sulphonamide, the quinolones of formula I are novel. Pharmaceutical compositions containing the compounds of formula I are described. Processes for preparing the novel quinolones are also described.

Quinolone sulphonamides useful as antihypertensive agents

Novel thienopyridones with antihypertensive activity have the formula I, ##STR1## wherein the ring A represents an optionally substituted thiophene ring; m is 0 or 1; n is 0, 1 or 2; R is lower alkyl and R.sub.1 is lower alkyl. The fused thieno-ring may carry one or two substituents. Formula I encompasses thieno[3,2-b]pyridones, thieno[3,4-b]pyridones and thieno[2,3-b]pyridones. Processes for preparing the novel thienopyridones and pharmaceutical compositions containing them are described. Pharmaceutically acceptable acid addition salts of the compounds of formula I are also described. The thienopyridones of formula I are antihypertensive agents and are also indicated for use in treating heart failure and ischaemic heart disease.

Antihypertensive thienopyridines

Novel quinolones of formula I ##STR1## and pharmaceutically acceptable acid addition salts thereof in which the dotted line between positions 2 and 3 of the quinolone ring represents an optional bond, R is hydrogen, 1-methyl or 2-lower alkyl; R.sub.1 is lower alkyl; R.sub.2 is hydrogen, halo, lower alkyl, lower alkoxy, trifluoromethyl, cyano, difluoromethoxy, methylsulphinyl, phenylsulphinyl or the group --NR.sub.4 R.sub.5 or the N-oxide thereof wherein R.sub.4 and R.sub.5, which may be the same or different, are lower alkyl or, together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino or morpholino radical; and R.sub.3 is hydrogen, fluoro, lower alkyl or lower alkoxy provided that, when R.sub.3 is lower alkoxy, R.sub.2 is other than lower alkoxy have utility as antihypertensive agents. Processes for preparing the quinolones and pharmaceutical compositions containing them are disclosed.

Antihypertensive 3-tetrazoyl-4-quinolones

Novel quinolones of the general formula ##STR1## wherein n is 0, 1 or 2; R.sub.1 is C.sub.1-4 alkyl; and R.sub.3 is hydrogen, C.sub.1-4 alkyl, methoxy, methylthio, halo or trifluoromethyl. These compounds have antihypertensive activity and may be used for treating hypertension in mammals. The quinolones are administered in novel therapeutic compositions comprising a quinolone of the above general formula together with a pharmaceutically acceptable carrier. Processes for making the novel quinolones are described.

3-Methylsulfonylmethyl-4-quinolinones useful for treating hypertension

3-Methylthiomethyl-and 3-methylsulfinylmethyl-4-quinolinones useful for

Compositions which contain a quinolone compound of the general formula ##STR1## wherein n is 0, 1 or 2; R.sub.1 is lower alkyl optionally substituted by hydroxy or C.sub.1-4 alkoxycarbonyl; allyl; propynyl or phenyl- lower alkyl in which the phenyl ring is optionally substituted by 1 or 2 C.sub.1-4 alkoxy groups; R.sub.2 is C.sub.1-4 alkyl with the proviso that when n is 0, R.sub.2 is methyl; and R.sub.3, R.sub.4 and R.sub.5, which may be the same or different, are hydrogen, lower alkyl, lower alkoxy, lower alkanoyl, halo, trifluoromethyl or lower alkylthio show antihypertensive activity. Compounds of general formula ##STR2## in which n, R.sub.1 R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as described above are novel subject to the following provisos (a) when R.sub.3, R.sub.4 and R.sub.4 and R.sub.5 are hydrogen R.sub.2 is methyl and R.sub.1 is lower alkyl, R.sub.1 contains more than one carbon atom, and

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Nottinghamshire, United Kingdom

Roy V Davies