Abstract: Novel cephem derivatives represented by the general formula ##STR1## wherein Ar is an optionally substituted lipophilic phenyl, naphthyl, benzthiazolyl or pyridyl group; R.sup.1 represents a group of the formula ##STR2## in which R.sup.8 and R.sup.9 are each independently hydrogen, C.sub.1 -C.sub.6 alkyl or (C.sub.1 -C.sub.6)alkoxycarbonyl, said C.sub.1 -C.sub.6 alkyl group being optionally substituted by 1-5 hydroxy or C.sub.1 -C.sub.6 alkoxy groups; m is either 0 or 1; A is a C.sub.2 -C.sub.10 alkyl group optionally substituted by 1-5 hydroxy groups; and R.sup.2 and R.sup.3 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl. The derivatives are gram-positive antibacterial agents especially useful in the treatment of diseases caused by methicillin-resistant Staphylococcus aureus.

Abstract: Tri- and tetra substituted thiepane and compositions having use as immunogens, therapeutics, diagnostics and for other industrial purposes are disclosed. The compositions inhibit proteolytic activity of viral enzymes and are useful for the inhibition of such enzymes as well as in assays for the detection of such enzymes. Embodiments in which antigenic polypeptides are bonded to the compositions are useful in raising antibodies against the thiepane haptens or the polypeptide. Labeled thiepanes of this invention are useful as diagnostic reagents.

Abstract: Novel cephem derivatives represented by the general formula ##STR1## in which the Acyl substituent is a group of the formula ##STR2## wherein Ar is a lipophilic optionally substituted phenyl, naphthyl, pyridyl or benzthiazolyl group; R.sup.1 is selected from certain optionally substituted aliphatic, aromatic, arylaliphatic or sugar moieties and R.sup.2 and R.sup.3 are each independently hydrogen, alkyl or aminoalkylcarbonylamino are gram-positive antibacterial agents, especially useful in the treatment of infectious diseases caused by methicillin-resistant Staphylococcus aureus (MRSA).

Abstract: Novel cephem derivatives represented by the general formula ##STR1## in which the Acyl substituent is a group of the formula ##STR2## wherein Ar is a lipophilic optionally substituted phenyl, naphthyl, pyridyl or benzthiazolyl group; R.sup.1 is selected from certain optionally substituted aliphatic, aromatic, arylaliphatic or sugar moieties and R.sup.2 and R.sup.3 are each independently hydrogen, alkyl or aminoalkylcarbonylamino are gram-positive antibacterial agents, especially useful in the treatment of infectious diseases caused by methicillin-resistant Staphylococcus aureus (MRSA).

Abstract: Novel cephem derivatives represented by the general formula ##STR1## in which the Acyl substituent is a group of the formula ##STR2## where Ar is a substituted phenyl or optionally substituted naphthyl or benzthiazolyl group and A is a substituted-pyridinium group are gram-positive antibiotics, especially useful in the treatment of diseases caused by methicillin-resistant Staphylococcus aureus.

Abstract: A composition comprising a compound of the formula: ##STR1## wherein: X is H or OH;Y is a group capable of hydrogen bonding to amino, guanidino, or imidazole function, or a group comprising an acidic hydrogen atom, a protected acidic group, or an anion;E is N or CR.sub.1, wherein R.sub.1 is H, OH, CN, F, Cl, Br, or I;A.sub.4, A.sub.5, and A.sub.6 are each independently N, CH, CR.sub.40 or CZ wherein R.sub.40 is R.sub.43, OR.sub.43, SR.sub.43, S(O)R.sub.43, S(O).sub.2 R.sub.43, or NR.sub.43 R.sub.44 wherein R.sub.43 comprises an alkyl of 1 to 3 carbon atoms, an acyl of 2 to 3 carbon atoms, or an alkyl of 1 to 3 carbon atoms substituted with an acyl of 2 to 3 carbon atoms, and R.sub.44 is H or an alkyl of 1 to 2 carbon atoms, and Z is a group capable of hydrogen bonding to carboxyl, or a group comprising a basic heteroatom, a protected basic heteroatom, or a cation.

Abstract: The present invention concerns nucleotide analogs and their compositions and use. In particular it relates to novel (phosphonomethoxy) methoxy purine/pyrimidine derivatives.

Abstract: Thymidine kinase inhibitor of formula I ##STR1## in which R is C.sub.1-6 alkyl or AR(CH.sub.2).sub.n --, wherein Ar represents phenyl optionally substituted with one to five same or different halogen, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; and n equals one to six.A further aspect of the present invention provides a method of inhibiting viral thymidine kinase. Yet another aspect of the invention relates to treating herpes simplex viral infections in mammals. Yet another aspect of the invention provides a pharmaceutical formulation.

Abstract: The present invention concerns nucleotide analogs and their compositions and use. In particular it relates to novel (phosphonomethoxy) methoxy purine/pyrimidine derivatives.

Abstract: Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## in which A represents a C.sub.1 -C.sub.6 straight or branched chain alkylene group; R.sup.5 represents an optionally substituted aliphatic cycloaliphatic, cycloaliphatic-aliphatic, aryl, araliphatic, heteroaryl, heteroaraliphatic, heterocyclyl or heterocyclyl-aliphatic radical and ##STR2## represents a nitrogen-containing aromatic heterocycle attached to the alkylene group A at a ring carbon atom and quaternized by substituent R.sup.5. Such derivatives are useful as potent antibacterial agents.

Abstract: Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## in which A represents a C.sub.1 -C.sub.6 straight or branched chain alkylene group; R.sup.5 represents an optionally substituted aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aryl, araliphatic, heteroaryl, heteroaraliphatic, heterocyclyl or heterocyclyl-aliphatic radical and ##STR2## represents a nitrogen-containing aromatic heterocycle attached to the alkylene group A at a ring carbon atom and quaternized by substituent R.sup.5. Such derivatives are useful as potent antibacterial agents.

Abstract: Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## wherein A represents C.sub.2 -C.sub.6 straight or branched chain alkylene group and R.sup.10 and R.sup.11 each independently represents optionally substituted aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aryl, heterocyclyl, heterocyclyl-aliphatic, heteroaryl or heteroaraliphatic, or R.sup.10 and R.sup.11 taken together with the S.sup..sym. to which they are attached represent an optionally substituted sulfur-containing heterocyclic ring. Such derivatives are useful as potent antibacterial agents. Also disclosed are processes for the preparation of such derivatives.

Abstract: Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## in which A represents cyclopentylene, cyclohexylene or C.sub.2 -C.sub.6 alkylene optionally substituted by one or more C.sub.1 -C.sub.4 alkyl groups; R.sup.5 represents either (a) an optionally substituted aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aryl, araliphatic, heteroaryl, heteroaraliphatic, heterocyclyl or heterocyclyl-aliphatic radical or (b) a divalent phenylene or C.sub.1 -C.sub.4 alkylene group joined to the ##STR2## ring so as to form a bridged polycyclic group; and ##STR3## represents a quaternized nitrogen-containing non-aromatic heterocycle. Such derivatives are useful as potent antibacterial agents.

Abstract: Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## in which A represents a C.sub.1 -C.sub.6 straight or branched chain alkylene group; R.sup.5 represents an optionally substituted aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aryl, araliphatic, heteroaryl, heteroaraliphatic, heterocyclyl or heterocyclyl-aliphatic radial and ##STR2## represents a nitrogen-containing aromatic heterocycle attached to the alkylene group A at a ring carbon atom and quaternized by substituent R.sup.5. Such derivatives are useful as potent antibacterial agents.

Abstract: Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## in which A represents cyclopentylene, cyclohexylene or C.sub.2 -C.sub.6 alkylene optionally substituted by one or more C.sub.1 -C.sub.4 alkyl groups and ##STR2## represents a quaternized nitrogen-containing aromatic heterocycle. Such derivatives are useful as potent antibacterial agents. Also disclosed are processes for the preparation of such derivatives and novel intermediates utilized in these processes.

Abstract: Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## in which A represents cyclopentylene, cyclohexylene or C.sub.2 -C.sub.6 alkylene optionally substituted by one or more C.sub.1 -C.sub.4 alkyl groups; R.sup.5 represents either (a) an optionally substituted aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aryl, araliphatic, heteroaryl, heteroaraliphatic, heterocyclyl or heterocyclyl-aliphatic radical or (b) a divalent phenylene or C.sub.1 -C.sub.4 alkylene group joined to the ##STR2## ring so as to form a bridged polycyclic group; and ##STR3## represents a quaternized nitrogen-containing non-aromatic heterocycle. Such derivatives are useful as potent antibacterial agents.

Abstract: Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## in which A represents cyclopentylene, cyclohexylene or C.sub.2 -C.sub.6 alkylene optionally substituted by one or more C.sub.1 -C.sub.4 alkyl groups and ##STR2## represents a quaternized nitrogen-containing aromatic heterocycle. Such derivatives are useful as potent antibacterial agents. Also disclosed are processes for the preparation of such derivatives and novel intermediates utilized in these processes.

Abstract: Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## in which A represents cyclopentylene, cyclohexylene or C.sub.2 -C.sub.6 alkylene optionally substituted by one or more C.sub.1 -C.sub.4 alkyl groups; R.sup.5 represents either (a) an optionally substituted aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aryl, araliphatic, heteroaryl, heteroaraliphatic, heterocyclyl or heterocyclyl-aliphatic radical or (b) a divalent phenylene or C.sub.1 -C.sub.4 alkylene group joined to the ##STR2## ring so as to form a bridged polycyclic group; and ##STR3## represents a quaternized nitrogen-containing non-aromatic heterocycle. Such derivatives are useful as potent antibacterial agents.