Abstract: The present invention relates to carbapenems and provides a compound of the formula (I) ##STR1## wherein: R.sup.1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxyethyl;R.sup.2 is hydrogen or C.sub.1-4 alkyl;R.sup.3 is hydrogen or C.sub.1-4 alkyl;P is of the formula (IA), (IB) or (IC) ##STR2## and in the formula (IB) the naphthyl group may be bonded to the nitrogen of the linking carbamoyl group at either ring; Z is carboxy, sulfonic acid, sulfinic acid, C.sub.1-4 alkanamidosulfonyl (--SO.sub.2 NHCOC.sub.1-3 alkyl), benzamidosulfonyl, C.sub.1-4 alkylsulfonylcarbamoyl (--CONHSO.sub.2 C.sub.1-4 alkyl), phenylsulfonylcarbamoyl, C.sub.1-4 alkoxy carbamoyl, hydroxycarbamoyl, sulfoamino, N--C.sub.1-4 alkanesulfonamido, cyanocarbamoyl, cyanosulfamoyl, tetrazol-5-yl, 3-hydroxyisoxazol-4-yl and 3-hydroxyisoxazol-5-yl;and P is optionally further substituted provided that when P is of the formula (IA) or (IC), Z is not carboxy;or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof.

Abstract: The present invention provides a compound of the formula: ##STR1## or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof wherein:A is a group of the formula (IA) or (IB): ##STR2## R.sup.1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl; R.sup.2 is hydrogen or C.sub.1-4 alkyl;R.sup.3 and R.sup.4 are the same or different and are a variety of substituents X is alkanediyl containing 1-6 carbon atoms optionally interrupted by O, S(O).sub.x (wherein x is zero, one or two), --CONR.sup.5 -- or --NR.sup.5 -- or wherein R.sup.5 is hydrogen or C.sub.1-4 alkyl;or X is alkenediyl containing 1-6 carbon atoms optionally interrupted by O, S(O).sub.x or --NR.sup.5 --.

Abstract: The present invention relates to carbapenems and provides a compound of the formula (I) ##STR1## wherein: R.sup.1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl;R.sup.2 is hydrogen or C.sub.1-4 alkyl;R.sup.3 is hydrogen or C.sub.1-4 alkyl;A is a 5-membered heteroaryl ring containing one nitrogen atom and up to two additional heteroatoms selected from nitrogen, oxygen and sulphur; and is bonded to the nitrogen of the linking carbamoyl group by a carbon atom in the ring, is substituted with the carboxy group on a carbon atom in the ring and is optionally further substituted on a carbon atom in the ring; andin any ring --NH--, H is optionally replaced by C.sub.1-4 alkyl; or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them are also described.

Abstract: The present invention relates to carbapenems and provides a compound of the formula (I) ##STR1## wherein: R.sup.1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl;R.sup.2 is hydrogen or C.sub.1-4 alkyl;R.sup.3 is hydrogen or C.sub.1-4 alkyl; and the thienyl ring is optionally further substitued by one or two substituents selected from halo, cyano, C.sub.1-4 alkyl, nitro, hydroxy, carboxy, C.sub.1-4 alkoxy, trifluoromethyl, C.sub.1-4 alkoxycarbonyl, amino, C.sub.1-4 alkylamino, di-C.sub.1-4 alkylamino, sulfonic acid, C.sub.1-4 alkylS(O).sub.n -- (wherein n is 0-2), C.sub.1-4 alkanoylamino, C.sub.1-4 alkanoyl(N-C.sub.1-4 alkyl)amino, carbamoyl, C.sub.1-4 alkylcarbamoyl, di-C.sub.1-4 alkylcarbamoyl and N-C.sub.1-4 alkanesulfonamido; or by a tetramethylene group attached to adjacent carbon atoms on the thienyl ring; or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof.

Abstract: The present invention relates to carbapenems and provides a compound of the formula (I) ##STR1## wherein: R.sup.1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl;R.sup.2 is hydrogen or C.sub.1-4 alkyl;R.sup.3 is hydrogen or C.sub.1-4 alkyl;and the pyridyl group is bonded to the nitrogen of the linking carbamoyl group by a carbon atom, is substituted with the carboxy group on a carbon atom and is optionally substituted on one or two pyridyl ring carbon atoms; or a pharmaceutically acceptable salt or in vivo hydrolyzable ester thereof. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.

Abstract: The present invention relates to carbapenems and provides a compound of the formula (I) ##STR1## wherein: R.sup.1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl;R.sup.2 is hydrogen or C.sub.1-4 alkyl;R.sup.3 is hydrogen or C.sub.1-4 alkyl;P.sup.1 is of the formula: ##STR2## and one or two of A,B,C,D,E,F,G and H, are nitrogen and the remainder are CH; and P is bonded to the nitrogen of the linking carbamoyl group by a carbon atom, in either ring, is substituted by the carboxy group on a carbon atom, in either ring, and is optionally further substituted, by up to three substitutents, on a carbon atom, in either ring; or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them are also described.

Abstract: Cephalosporin compounds having a 3-position substituent of the formula (I) are described:--CH.sub.2 --S--Q--(Y).sub.n --Pwherein Q is a 5- or 6-membered heterocyclic ring, P is a benzene ring substituted by groups R.sup.1 and R.sup.2 which are ortho with respect to one another, wherein R.sup.1 is hydroxy or an in vivo hydrolysable ester thereof and R.sup.2 is hydroxy, an in vivo hydrolysable ester thereof, carboxy, sulpho, hydroxymethyl, methanesulphonamido or ureidos; or P is a group of the formula (II) or (III): ##STR1## wherein M is oxygen or a group NR.sup.3 wherein R.sup.3 is hydrogen or C.sub.1-4 alkyl; said ring P being further optionally substituted; and --(Y).sub.n -- is a bond or various linking groups or --(Y)--.sub.n may be such so that rings Q and P are fused.The use of such compounds as antibacterial agents is described as are processes for their preparation and intermediates therefor.

Abstract: Cephalosporin compounds having a 3-position substituent of the formula (I) are described,--CH.sub.2 --Y--Q (I)wherein Y is a bond or a linking group --NR.sup.4 --Y'--, --O--Y'--, --S--Y'-- wherein R.sup.4 is hydrogen, various optionally substituted alkyl groups, alkenyl, alkanoyl or alkanesulphonyl, and Y' is a bond or various optionally substituted alkylene groups; and Q is a benzene ring (optionally fused to a further benzene ring so forming a naphthyl group or optionally fused to a 5 or 6 membered heterocyclic aromatic group containing 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur), said benzene ring being substituted by groups R.sup.1 and R.sup.2 which are ortho with respect to one another, wherein R.sup.1 is hydroxy or an in vivo hydrolysable ester thereof and R.sup.2 is hydroxy, an in vivo hydrolysable ester thereof, carboxy, sulpho, hydroxymethyl, methanesulphonamido or ureido; or Q is a group of the formula (II) or (III): ##STR1## wherein M is oxygen or a group NR.sup.3 wherein R.

Abstract: Cephalosporin compounds having a 3-position substituent of the formula (I) are described:--CH.sub.2 --S--Q--(Y).sub.n --Pwherein Q is a 5- or 6-membered heterocyclic ring, P is a benzene ring substituted by groups R.sup.1 and R.sup.2 which are ortho with respect to one another, wherein R.sup.1 is hydroxy or an in vivo hydrolysable ester thereof and R.sup.2 is hydroxy, an in vivo hydrolysable ester thereof, carboxy, sulpho, hydroxymethyl, methanesulphonamido or ureido; or P is a group of the formula (II) or (III): ##STR1## wherein M is oxygen or a group NR.sup.3 wherein R.sup.3 is hydrogen or C.sub.1-4 alkyl; said ring P being further optionally substituted; and --(Y).sub.n -- is a bond or various linking groups or --(Y)--.sub.n may be such so that rings Q and P are fused.The use of such compounds as antibacterial agents is described as are processes for their preparation and intermediates therefor.

Abstract: A cephalosporin derivative of the formula I: ##STR1## in which X is S, O, CH.sub.2 or SO, ##STR2## represents one of C-7 acyl groups known in the cephalosporin art, R3 is hydrogen or methoxy, R4 is hydrogen, optionally substituted alkyl or allyl, and R5 is an aromatic heterocyclic ring system which is linked via carbon, and which contains a quaternized nitrogen atom.

Abstract: Cephalosporin compounds having a 3-position substituent of the formula (I) are described:--CH.sub.2 --Y--Q (I)wherein Y is a bond or a linking group --NR.sup.4 --Y'--, --O--Y'--, 13 S--Y'-- wherein R.sup.4 is hydrogen, various optionally substituted alkyl groups, alkenyl, alkanoyl or alkanesulphonyl, and Y' is a bond or various optionally substituted alkylene groups; and Q is a benzene ring (optionally fused to a further benzene ring so forming a naphthyl group or optionally fused to a 5 or 6 membered heterocyclic aromatic group containing 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur), said benzene ring being substituted by groups R.sup.1 and R.sup.2 which are ortho with respect to one another, wherein R.sup.1 is hydroxy or an in vivo hydrolyzable ester thereof and R.sup.2 is hydroxy, and in vivo hydrolyzable ester thereof, carboxy, sulpho, hydroxymethyl, methanesulphonamido or ureido; or Q is a group of the formula (II) or (III): ##STR1## wherein M is oxygen or a group NR.sup.3 wherein R.

Abstract: Cephalosporin compounds having a 3-position substituent of the formula (I) are described:--CH.sub.2 --S--Q--(y).sub.n --Pwherein Q is a 5- or 6-membered heterocyclic ring, P is a benzene ring substituted by groups R.sup.1 and R.sup.2 which are ortho with respect to one another, wherein R.sup.1 is hydroxy or an in vivo hydrolysable ester thereof and R.sup.2 is hydroxy, an in vivo hydrolysable ester thereof, carboxy, sulpho, hydroxymethyl, methanesulphonamido or ureido; or P is a group of the formula (II) or (III): ##STR1## wherein M is oxygen or a group NR.sup.3 wherein R.sup.3 is hydrogen or C.sub.1-4 alkyl; said ring P being further optionally substituted; and --(Y).sub.n -- is a bond or various linking groups or --(Y)--.sub.n may be such so that rings Q and P are fused.The use of such compounds as antibacterial agents is described as are processes for their preparation and intermediates therefor.

Abstract: A cephalosporin derivative of the formula I: ##STR1## in which X is ##STR2## represents one of C-7 acyl groups known in the cephalosporin art, R3 is hydrogen or methoxy, R4 is hydrogen, optionally substituted alkyl or allyl, and R5 is an aromatic heterocyclic ring system which is linked via carbon, and which contains a quaternized nitrogen atom.

Abstract: Cephalosporin compounds having a 3-position substituent of the formula (I) are described:--CH.sub.2 --Y--Q (I)wherein Y is a linking group --NR.sup.4 CO--Y'--, --NR.sup.4 SO.sub.2 --Y'--, --OCO--Y;-- or --SCO--Y'-- wherein R.sup.4 is hydrogen, various optionally substituted alkyl groups or alkenyl and Y' is a bond or various optionally substituted alkylene or alkenylene groups; and Q is a benzene ring (optionally fused to a further benzene ring so forming a naphthyl group or optionally fused to a 5 or 6 membered heterocyclic aromatic group containing 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur), said benzene ring (or in the case of naphthyl either benzene ring) being substituted by groups R.sup.1 and R.sup.2 which are ortho with respect to one another, wherein R.sup.1 is hydroxy or an in vivo hydrolyzable ester thereof and R.sup.

Abstract: An antibacterial cephalosporin derivative of the formula I: ##STR1## in which X is S,O,CH.sub.2 or S0; R2 is hydrogen, methoxy or formylamino; R3 is carboxy or a biodegradable ester thereof; R1 represents a variety of groups known in the cephalosporin art and R4 represents a group NR42R43 wherein R42 is hydrogen, lower alkyl or benzyl and R43 is one of a group of neutral heterocyclic species defined in the specification. Pharmaceutical compositions, manufacturing processes and intermediates are also described. In a specific embodiment, 3-substituted aminomethyl cephalosporin derivatives in which X is S or SO are disclosed.

Abstract: According to the invention there is provided a antibacterial cephalosporin derivative of the formula: ##STR1## in which X is sulphur, oxygen, methylene or sulphinyl; R3 is hydrogen or methoxy; R1 and R2 are known in the cephalosporin art and R4 is an aminomethyl group in which the amino group carries one of various positively charged nitrogen-containing species set out in the specification and optionally a further substituent selected from hydrogen, lower alkyl, benzyl or heteroarylloweralkyl groups.

Abstract: A cephalosporin derivative of the formula I: ##STR1## in which X is S, O, CH.sub.2 or SO, R1 is (optionally-substituted) imidazol-2-yl or one of the C-7 acyl groups known in the cephalosporin art, R2 is hydrogen or methoxy, R3 is carboxy or a biodegradable ester thereof and -R4 is of the formula XII, XIII or XIV: ##STR2## in which R32-R40 inclusive are as defined in the specification; and the salts thereof. Pharmaceutical compositions, methods of manufacture and intermediates are also described.

Abstract: A process for the manufacture of a cephalosporin derivative of the formula I ##STR1## in which X is sulphur, oxygen or sulphinyl; R.sup.1 is any one of the C-3 substituents from antibacterially-active cephalosporins known in the art; R.sup.2 is hydrogen or 1-6C alkyl; R.sup.3 is hydrogen or 1-6C alkyl; and the pharmaceutically-acceptable acid-addition and base-addition salts thereof, characterized by cyclization of a compound of the formula II: ##STR2## or a derivative thereof in which the carbonyl group is masked, or an acid-addition salt thereof, in which R.sup.4 and R.sup.5 individually have one of the values for R.sup.2 and R.sup.3, R.sup.6 is a nitrogen-protecting group and R.sup.7 is hydrogen or any one of the cephalosporin 3-carboxylic acid protecting groups known in the art;whereafter when the product from the cyclization retains the protecting group R.sup.7 (when R.sup.7 is other than hydrogen) the protecting group R.sup.

Abstract: An antibacterial cephalosporin derivative of the formula I: ##STR1## in which X.sup.1 is sulphinyl; R.sup.1 is any one of the C-3 substituents from antibacterially-active cephalosporins known in the art; R.sup.2 is any one of the C-4 substituents from antibacterially-active cephalosporins known in the art; R.sup.3 is hydrogen, 1-6C alkoxy or 1-6C alkylthio; X.sup.2 is nitrogen or a radical N.sup..sym. R.sup.5 ; R.sup.4 and R.sup.5 are a variety of radicals described in the specification; --A-- is of the formula II or III: ##STR2## in which R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10 and R.sup.11 are a variety of substituents described in the specification; and the pharmaceutically-acceptable acid- and base-addition salts thereof. Pharmaceutical compositions and manufacturing processes are also described.

Abstract: A cephalosporin derivative of the formula: ##STR1## in which R.sup.0 is a hydrogen atom or a methyl radical, R.sup.1 is any one of the C-3 substituents from antibacterially-active cephalosporins known in the art; R.sup.2 is any one of the C-4 substituents from antibacterially-active cephalosporins known in the art; R.sup.3 is a hydrogen atom or a 1-6C alkoxy or 1-6C alkylthio radical; X.sup.1 is a sulphur or oxygen atom, a CH.sub.2 radical or a radical of the formula NR.sup.7 in which R.sup.7 is a hydrogen atom, a 1-6C alkyl, formyl or benzyl radical; X.sup.2 is a nitrogen atom or a radical of the formula N.sup..sym. -R.sup.7 ; R.sup.4 and R.sup.7, and R.sup.5 and R.sup.6 are a variety of substituents which are described in the specification; and the pharmaceutically-acceptable acid- or base-addition salts thereof. Pharmaceutical compositions, manufacturing processes and intermediates are also described.