Abstract: A method is disclosed for manufacturing a pharmaceutical tablet for oral administration, the tablet combining both immediate-release and prolonged-release modes of drug delivery and using an immediate-release drug that is either insoluble in water or only sparingly soluble and is present in a very small amount compared to the prolonged-release drug. The method involves the use of particles of the immediate-release drug that are equal to or less than 10 microns in diameter, applied as a layer or coating over a core of the prolonged-release drug, the layer or coating being either the drug particles themselves, applied as an aqueous suspension, or a solid mixture containing the drug in admixture with a material that disintegrates rapidly in gastric fluid.

Abstract: A method is disclosed for manufacturing a pharmaceutical tablet for oral administration, the tablet combining both immediate-release and prolonged-release modes of drug delivery and using an immediate-release drug that is either insoluble in water or only sparingly soluble and is present in a very small amount compared to the prolonged-release drug. The method involves the use of particles of the immediate-release drug that are equal to or less than 10 microns in diameter, applied as a layer or coating over a core of the prolonged-release drug, the layer or coating being either the drug particles themselves, applied as an aqueous suspension, or a solid mixture containing the drug in admixture with a material that disintegrates rapidly in gastric fluid.

Abstract: The present invention relates to a cephalosporin compound represented by the following general formula (I), its pharmaceutically acceptable non-toxic salt, physiologically hydrolyzable ester, hydrate or solvate, or isomers thereof, which is useful as an antibiotic agent: ##STR1## in which R.sup.1 represents hydrogen or an amino-protecting group,R.sup.2 and R.sup.3 can be identical or different and each represent hydrogen or a hydroxy-protecting group, orR.sup.2 and R.sup.3 together can form a diol-protecting cyclic group,R.sup.4 represents hydrogen or a carboxyl-protecting group,R.sup.5 represents hydrogen, C.sub.1-4 alkyl, alkoxycarbonyl, carboxyl or sulfomethyl,R.sup.6 represents hydrogen, amino or substituted amino, andR.sup.7 represents C.sub.1-4 alkyl, amino or substituted amino, orR.sup.5 and R.sup.6 together with the carbon atoms to which they are attached can form a 3 to 7-membered cyclic group, orR.sup.6 and R.sup.

Abstract: Cephalosporin compounds of formula (I): ##STR1## wherein: R.sup.1 is a hydrogen or an amino protecting group;R.sup.2 and R.sup.3 are, independently, a hydrogen or a hydroxy protecting group, or form together a cyclic diol protecting group;R.sup.4 and R.sup.5 are, independently, a hydrogen or a carboxyl protecting group;X and Y are a nitrogen and a carbon atom, respectively, or a carbon and a nitrogen atom, respectively;R.sup.6 and R.sup.7 are, independently, a hydrogen or an amino, substituted amino, hydroxy, alkoxy, C.sub.1-4 alkyl, carboxyl or alkoxy carbonyl group, or jointly form a C.sub.3-7 cycloalkyl group together with the carbon to which they are attached, when X and Y are a nitrogen and a carbon, respectively, or R.sup.7 is a hydrogen or an amino group when X and Y are a carbon and a nitrogen, respectively; andQ is .dbd.CH-- or .dbd.

Abstract: The present invention provides a process for preparing cephem derivatives having the following general formula (I): ##STR1## in which R.sup.1 represents a carboxy group or a protected carboxy group which can form the salt of --COO.sup.- M.sup.+ with an alkali metal ion (M.sup.+) such as sodium, or may represent --COO.sup.- when R.sup.2 has a substituent having positive electric charge such as pyridinium, pyrimidinium or thiazolium,R.sup.2 represents hydrogen, acyloxymethyl, heterocyclic methyl or heterocyclic thiomethyl, each of which can be substituted with appropriate substituents,R.sup.3 represents hydrogen or an amino-protecting group,R.sup.4 represents C.sub.1 -C.sub.4 alkyl or phenyl, or together with the oxygen or phosphorus atom to which it is attached may form a 5- or 6-membered heterocyclic ring, andQ represents N or CH, characterized in that a reactive thiophosphate derivative of thia(dia)zole acetic acid having the following general formula (II): ##STR2## wherein R.sup.3, R.sup.

Abstract: The present invention relates to a cephalosporin compound represented by the following general formula (I): ##STR1## its pharmaceutically acceptable non-toxic salt, physiologically hydrolyzable ester, hydrate or solvate, or isomers thereof, in whichR.sup.1 represents hydrogen or an amino-protecting group,R.sup.2 and R.sup.3 can be identical or different and independently of one another represent hydrogen or a hydroxy-protecting group, orR.sup.2 and R.sup.3 together can form a cyclic diol-protecting group,R.sup.4 represents hydrogen or a carboxyl-protecting group,R.sup.5, R.sup.6 and R.sup.7 independently of one another represent hydrogen, amino or substituted amino, hydroxy, alkoxy, C.sub.1-4 alkyl, carboxyl or alkoxycarbonyl, orR.sup.5 and R.sup.6 together with the carbon atoms to which they are attached can form a C.sub.3-7 cycle, andQ represents CH or N,and to a process for preparation thereof and a pharmaceutical composition containing the compound (I) as an active ingredient.

Abstract: The present invention relates to a novel reactive thiophosphate derivative of thia(dia)zole acetic acid which can be very effectively used in the preparation of .beta.-lactam antibiotics, and which is represented by the following general formula (I): ##STR1## in which R.sup.1 represents hydrogen or an amino-protecting group;R.sup.2 represents hydrogen, C.sub.1 -C.sub.4 alkyl, or --C(R.sup.a)(R.sup.b)CO.sub.2 R.sup.c, wherein R.sup.a and R.sup.b are identical or different from each other and represent hydrogen or C.sub.1 -C.sub.4 alkyl, or R.sup.a and R.sup.b together with a carbon atom to which they are bound can form a C.sub.3 -C.sub.7 cycloalkyl group and R.sup.c is hydrogen or a carboxy-protecting group;R.sup.3 represents C.sub.1 -C.sub.4 alkyl or phenyl or R.sup.3 together with an oxygen atom and a phosphorus atom to which it is bound can form a 5- or 6-membered heterocyclic ring; andQ represents N or CH, and to a process for preparing the same.

Abstract: The present invention provides a cephalosporin compound represented by formulas (I-S) and (I-R) ##STR1## wherein: R.sup.1 is a C.sub.1-4 alkyl, C.sub.3-4 alkenyl, C.sub.3-4 cycloalkyl, amino optionally substituted with a C.sub.1-4 alkyl radical, phenyl, or 2-,4- or 6- substituted phenyl group with two or fewer substitutents chosen from C.sub.1-4 alkyl, C.sub.1-3 alkoxy, halogen and hydroxy radicals;R.sup.2 is hydrogen or a C.sub.1-4 alkyl group;R.sup.a and R.sup.b, which should be different from each other, are hydrogen or a C.sub.1-4 alkyl group; andQ is N or CH,and the pharmaceutically acceptable non-toxic salts, physiologically hydrolyzable esters, hydrates and solvates thereof, which possess potent and broad antibacterial activities. The invention also provides processes for preparing these compounds and to pharmaceutical compositions containing them as active ingredients.

Abstract: The present invention relates to novel cephalosporin compounds, pharmaceutically acceptable non-toxic salts, physiologically hydrolyzable esters, hydrates and solvates and isomers thereof which possess potent and broad antibacterial activities. The compounds of the present invention have a (4-amino-1-substituted-alkapyrimidinium-4-yl)thiomethyl group in 3-position of the cephem nucleus and is specifically represented by the following formula(I): ##STR1## wherein: R.sup.1 is a hydrogen atom or a C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl or --C(R.sup.A)(R.sup.B)COOH group wherein R.sup.A and R.sup.B are independently a hydrogen atom or a C.sub.1-4 alkyl group, or form a C.sub.3-7 cycloalkyl group together with the carbon atom to which they are attached;R.sup.2 is an unsubstituted or substituted amino, C.sub.1-4 alkyl or C.sub.3-7 cycloalkyl group; andn is an integer ranging from 2 to 7.

Abstract: The present invention relates to a cephalosporin compound including the pharmaceutically acceptable non-toxic salts, physiologically hydrolyzable esters, hydrates and solvates thereof of the formula(I) and its isomers: ##STR1## wherein: R.sup.1 is a C.sub.1-4 alkyl, C.sub.3-4 alkenyl, C.sub.3-4 alkynyl or --C(R.sup.3)(R.sup.4)COOH wherein R.sup.3 and R.sup.4, which may be the same or different, are hydrogen, C.sub.1-4 alkyl group, or constitute a C.sub.3-7 cycloalkyl group with the carbon atoms to which R.sup.3 and R.sup.4 are attached;R.sup.2, which may be attached to N.sup.a or N.sup.b, is a C.sub.1-4 alkyl, C.sub.3-4 alkenyl, C.sub.3-7 cycloalkyl, aryl or amino group; andQ.sub.1 and Q.sub.2, which may be the same or different, are CH or N.

Abstract: The present invention relates to new cephalosporin compounds of the formula(I), pharmaceutically acceptable non-toxic salts thereof, and physiologically hydrolyzable esters and solvates thereof, which have potent and broad antibacterial activities ##STR1## wherein R.sup.1 is a C.sub.1.about.4 alkyl, C.sub.3.about.4 alkenyl, C.sub.3.about.4 alkynyl group, or --C(R.sup.a)(R.sup.b)CO.sub.2 H.sub.1 wherein R.sup.a and R.sup.b are the same or different, and each is a hydrogen atom or a C.sub.1.about.4 alkyl group, or R.sup.a and R.sup.b form a C.sub.3.about.7 cycloalkyl group with the carbon atom to which they are linked;R.sup.2 is a C.sub.1.about.4 alkyl, C.sub.3.about.4 alkenyl or C.sub.3.about.4 cycloalkyl group, a substituted or unsubstituted amino group, or a substituted or unsubstituted phenyl group;R.sup.3 is hydrogen or a C.sub.1.about.4 alkyl group; andQ is N or CH.The invention further relates to a process for preparing said compounds, and to pharamaceutical compositions containing said compounds.

Abstract: The present invention provides certain novel cephalosporin derivatives represented by following formula(I), which are especially useful as intermediates for the preparation of cephalosporin compounds possessed with potent and broad antibacterial activities. ##STR1## wherein: R.sup.1 is a C.sub.1-4 alkyl, C.sub.3-4 alkenyl, C.sub.3-4 cycloalkyl, amino optionally substituted with a C.sub.1-4 alkyl radical, or phenyl group optionally substituted on its 2-, 4-and/or 6-position with a halogen, C.sub.1-4 alkyl, C.sub.1-3 alkoxy or hydroxy radical;R.sup.2 is hydrogen or a C.sub.1-4 alkyl group; andn is either 0 or 1.The invention also relates to processes for preparing these intermediates and their pharmacologically active cephalosporin antibiotics.

Abstract: The present invention relates to novel cephalosporin compounds having high antimicrobial activity, which are shown by the formula(I), and to a process for preparing them ##STR1## wherein R.sup.1 is a hydrogen atom or an amino protecting group;R.sup.2 is acetoxy; andR.sup.3 is a hydrogen atom or a carboxyl protecting group (wherein when R.sup.2 contains quaternary ammonium, r.sup.2 and R.sup.3 may form a zwitter ion).The present invention also relates to the non-toxic and pharmaceutically acceptable salts of the cephalosporin compounds of the formula (I). Also described are compositions containing the antibiotics according to the present invention.