Ethene derivatives.

摘要

Ethene derivatives of the general formula:
<Chemistry id="chema01" num="0001"><Image id="ia01" he="6" wi="73" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein R<Sup>5</Sup> represents a heterocyclyl group, containing 1, 2 or 3 rings and one or more heteroatoms selected from nitrogen, oxygen, sulphur and selenium atoms, which is unsubstituted or substituted by one or more substituents R<Sup>8</Sup> [which may be the same or different and each represents a

halogen atom or an amino, carboxy, cyano, nitro, hydroxy, oxo, formyl, trifluoromethyl, aryl, aryloxy, arylthio, benzyloxycarbonylamino, sulphamoyl, tetrazol-5-yl, carbamoyl, thiocarbamoyl, arylcarbamoyl or aroyl group, or a straight-or branched-chain alkyl group containing from 1 to 10 carbon atoms, or a straight- or branched-chain alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylamino, alkylsulphamoyl, arylalkyl or arylalkoxy group containing from 1 to 10 carbon atoms in the alkyl moiety, a straight- or branched-chain alkanoyl, alkoxycarbonyl, alkoxycarbonylamino, alkylcarbamoyl or alkanoylamino group containing from 2 to 6 carbon atoms, an N-benzyloxycarbonyl-N-alkylamino group wherein the alkylamino moiety is straight- or branched-chain and contains from 1 to 6 carbon atoms, or a dialkylsulphamoyl, dialkylamino or dialkylcarbamoyl group wherein the alkyl moieties may be straight or branched and may each contain from 1 to 6 carbon atoms and may be linked together to form a ring, or a group of the formula -CR<Sup>4</Sup>=CR<Sup>2</Sup>R<Sup>3</Sup>, or an aryl group which is unsubstituted or substituted by one or more substituents R<Sup>S</Sup> (as hereinbefore defined), or a heterocyclylalkyl or arylalkyl group wherein the heterocyclyl or aryl moiety is as hereinbefore defined and the alkyl moiety is straight- or branched-chain and contains 1 or 2 carbons atoms, and R<Sup>1</Sup> represents a group of the general formula:
<Chemistry id="chema02" num="0002"><Image id="ia02" he="7" wi="83" file="IMGA0002.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein R<Sup>6</Sup> represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 6 carbon atoms which may be substituted by one or more substituents R<Sup>S</Sup> (as hereinbefore defined) or an aryl group which may be substituted by one or more substituents R<Sup>8</Sup> (as hereinbefore defined), or R<Sup>5</Sup> represents a quinonoidal group R<Sup>7</Sup> derived from a nitrogen-containing heterocyclyl group within the definition of R<Sup>5</Sup> as hereinbefore defined, bearing on said ring-nitrogen atom a substituent selected from straight- and branched-chain alkyl groups containing from 1 to 6 carbon atoms which may be substituted by one or more substituents R<Sup>S</Sup> (as hereinbefore defined), and aryl groups which may be substituted by one or more substituents R<Sup>S</Sup> (as hereinbefore defined), and R<Sup>1</Sup> represents an atom =N-, R<Sup>4</Sup> represents a hydrogen atom or a straight- or branched-chain alkoxy or alkylthio group containing from 1 to 6 carbon atoms, a trifluoromethyl group or a straight- or branched-chain alkyl group containing from 1 to 6 carbon atoms which may be substituted by one or more substituents R<Sup>8</Sup> (as hereinbefore defined), or an aryl group which may be substituted by one or more substituents R<Sup>8</Sup> (as hereinbefore defined), R<Sup>2</Sup> represents a cyano or formyl group, a straight- or branched-chain alkoxycarbonyl or alkylsulphonyl group containing up to 6 carbons, or a dialkylcarbamoyl or dialkylthiocarbamoyl group wherein the alkyl groups may be the same or different and each may be straight or branched and each contains from 1 to 6 carbon atoms, or an aryloxycarbonyl, arylsulphinyl or arylsulphonyl group wherein the aryl moiety may be substituted by one or more substituents R<Sup>8</Sup> (as hereinbefore defined), R<Sup>3</Sup> represents a group within the definition of R<Sup>2</Sup> or a hydrogen atom or a nitro group or an aryl or aroyl group which may be substituted by one or more substituents R<Sup>8</Sup> (as hereinbefore defined) or a straight- or branched-chain alkanoyl group containing up to 6 carbon atoms, and m and n each represents 1 or 2, and pharmaceutically acceptable salts thereof, with the provisos that the following classes of compounds are excluded:-
<UnorderedLists id="ula01" listStyle="none"><ListItem>(i) compounds of formula I wherein R<Sup>5</Sup> represents a pyridyl group which is unsubstituted or substituted by one or more substituents R<Sup>9</Sup> which may be the same or different and each represents a group within the definition of R<Sup>e</Sup> other than oxo, straight- or branched-chain alkyl containing from 7 to 10 carbon atoms, straight- or branched-chain alkoxy, alkylthio, alkylsulphonyl, alkylamino, alkylsulphamoyl or arylalkyl containing from 7 to 10 carbon atoms in the alkyl moiety, straight- or branched-chain alkylsulphinyl or arylalkoxy containing from 1 to 10 carbon atoms in the alkyl moiety, or a group -CR<Sup>4</Sup>=CR<Sup>2</Sup>R<Sup>3</Sup> as hereinbefore defined, R<Sup>2</Sup> and R<Sup>3</Sup> may be the same or different and each represents a phenylsulphonyl group which may be unsubstituted or substituted by one or more substituents R<Sup>9</Sup> (as hereinbefore defined), R' represents a group of formula II, R<Sup>4</Sup> and R<Sup>6</Sup> represent hydrogen atoms and m and n both represent 1;</ListItem><ListItem>(ii) compounds of formula I wherein R<Sup>5</Sup> represents a 5-halogenopyrid-2-yl group, R<Sup>2</Sup> and R<Sup>3</Sup> both represent cyano groups, R<Sup>1</Sup> represents a group of formula II, R<Sup>4</Sup> and R° represent hydrogen atoms and m and n both represent 1; and</ListItem><ListItem>(iii) compounds of formula I wherein R<Sup>5</Sup> represents a 1,2,4-triazolo[4,8-a]-quinoline group which is unsubstituted or substituted by one or more substituents R<Sup>10</Sup> which may be the same or different and each represents a group within the definition of R<Sup>9</Sup> or a straight- or branched-chain alkylsulphinyl group containing from 1 to 6 carbon atoms, R<Sup>2</Sup> and R<Sup>3</Sup> may be the same or different and each represents a cyano group, a straight- or branched-chain alkoxycarbonyl group containing from 2 to 6 carbon atoms, or a phenylsulphonyl group which may be unsubstituted or substituted by one or more substituents R<Sup>10</Sup> (as hereinbefore defined), R' represents a group of formula II, R<Sup>4</Sup> and R<Sup>6</Sup> represent hydrogen atoms and m and n both represent 1, possess useful pharmacological properties.</ListItem></UnorderedLists>