Abstract: The present invention provides compounds which inhibit an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.

Abstract: The present invention provides a method of inhibiting influenza and flaviviral replication based on a mechanism of action in which HA-mediated fusion or E protein mediated fusion is inhibited by a fusion inhibiting agent which binds, complexes or otherwise becomes associated with HA or E protein during the translation of the target protein and/or its vesicular transport.

Abstract: The invention provides complexes of the formula: ##STR1## wherein X is chloro, hydrogen, vinyl, or --CH.sub.3,Z is CH.sub.2 or S;n is 0-5;Y is phenyl or 1,4-cyclohexadien-1-yl;R.sub.1 and R.sub.2 are hydrogen or hydroxy, with the proviso that R.sub.1 and R.sub.2 are not both hydrogen andR.sub.3 is --COO.sup.-, --COO(C.sub.1 -C.sub.4 alkyl), --NO.sub.2 or ##STR2## wherein R.sub.4 is C.sub.1 -C.sub.4 alkyl.

Abstract: The present invention provides antiretroviral methods using the compounds of formula (I)X-X1-P1-Val-Z-Leu-P2-Ywherein:Z is Statine or ACHPA;and when Z is Statine,X is H-Pro-paF, H-Pro-His, Ac-Tyr, Ac-NA, Ac-Trp, Ac-YOM, Ac-Phe, Ac-paF, H-His, Ac-His or Ac-Gly-Tyr-YOM,X1 is Pro Ser or Ac,P1 is Phe, paF or YOM,P2 is Phe or Leu, andY is NH.sub.2, paF--NH.sub.2, His--NH.sub.2, Phe--NH.sub.2 or Tyr-Lue--NH.sub.2,provided that when X1 is Ac then there is no X residue;and when Z is ACHPA,X is H-Pro-His, H-Pro-paF, Ac-paF or Ac-His,P1 is Phe,P2 is Phe, andY is paF--NH.sub.2 and His--NH.sub.2.The invention further provides methods for determining the retroviral protease inhibitory activity of compounds using viral polypeptides made using recombinant DNA techniques.

Abstract: Provided are compounds of the formula (1): ##STR1## wherein R' is hydrogen, methyl or NH.sub.2 C(O)CH.sub.2 --;R" and R'" are independently methyl or hydrogen;R and R.sup.y are independently hydroxy or hydrogen;R.sub.1 is hydroxy, hydrogen, or hydroxysulfonyloxy;R.sub.7 is hydroxy, hydrogen, hydroxysulfonyloxy or phosphonooxy;R.sub.2 is a novel acyl side chain. Also provided are novel formulations, methods of inhibiting fungal and parasitic activity, and a process for preparing dideoxy (R=H) forms of the compounds.

Abstract: Provided are compounds of the formula (1): ##STR1## wherein R' is hydrogen, methyl or NH.sub.2 C(O)CH.sub.2 --;R" and R'" are independently methyl or hydrogen;R and R.sup.Y are independently hydroxy or hydrogen;R.sub.1 is hydroxy, hydrogen, or hydroxysulfonyloxy;R.sub.7 is hydroxy, hydrogen, hydroxysulfonyloxy or phosphonooxy;R.sub.2 is a novel acyl side chain. Also provided are novel formulations, methods of inhibiting fungal and parasitic activity, and a process for preparing dideoxy (R=H) forms of the compounds.

Abstract: Two new groups of A-21978C cyclic peptides, anhydro- and isomer-A21978C peptide derivatives, have antibacterial activity and are useful as intermediates. The two groups are prepared via transpeptidation of the parent cyclic peptides. Pharmaceutical formulations containing the new peptides as active ingredients and methods of treating infections caused by susceptible Gram-positive bacteria with the formulations are also provided.The invention also provides an antibacterial composition containing the new drug substance LY 146032 in substantially pure form.

Abstract: A series of benzimidazole compounds having the following general structure are provided which inhibit the growth of picornaviruses (e.g., rhinoviruses, enteroviruses, polioviruses, coxsackieviruses of the A and B groups, echo virus and Mengo virus) and flaviviruses (e.g., hepatitis C and bovine diarrheal virus). ##STR1## A method for inhibiting picornaviruses and flaviviruses is also provided which includes administering to a host an effective amount of the inventive benzimidazole compounds.

Abstract: Pharmaceutical formulations of cefaclor, suitable for the direct-compression manufacture of dispersible tablets, containing the antibiotic cefaclor in an amount between 35% and 50% by weight of the total weight of the formulation, along with suitable excipients and coadjuvants selected from disintegrators, diluents, lubricants, antiadherents, sweeteners, fragrances and, optionally, flavorings, opacifiers and colorants. Said formulations are suitable for the manufacture of dispersible tablets which disintegrate in less than three minutes in water at 19.degree.-21.degree. C., and are suitable for the treatment of infections caused by bacteria strains sensitive to cefaclor.

Abstract: New glycopeptide antibiotic A82846, comprising A82846A, A82846B and A82846C, is produced by Nocardia orientalis strains NRRL 18098, NRRL 18099 and NRRL 18100. The A82846 antibiotics have activity against Gram-positive bacteria comparable to that of vancomycin.

Abstract: The present application provides a series of benzimidazole compounds which inhibit the growth of picornaviruses, such as rhinoviruses, enteroviruses, polioviruses, coxsackieviruses of the A and B groups, echo virus and Mengo virus and flaviviruses such as hepatitis C and bovine diarrheal virus.

Abstract: The present invention provides a group of novel compounds that inhibit the proteolytic activity of 3C proteases which are found in picornaviruses, particularly rhinoviruses. In picornaviruses the RNA genome is translated into a single large viral polyprotein precursor. The precursor demonstrates auto-proteolytic activity, cleaving itself into mature viral gene products. Therefore, compounds of the current invention are particularly useful in treating picornaviral infections by interrupting the processing of the viral gene products into mature and infectious viral particles. The current invention also provides a novel process the preparation of compounds of the current invention. The process entails the selective reduction of an imide intermediate representing a marked improvement over processes known in the art for making peptidyl-aldehydes.

Abstract: The invention relates to an improved process for preparing cephalosporins by reaction compounds such as 7-amino-cephalosporanic acid, 7-amino-3-deacetoxy-cephalosporanic acid or their derivatives with derivatives of .alpha.-amino acids in the presence of a properly immobilized penicillin acylase enzyme under the following conditions, independently, or in combination: (1) at a temperature ranging from 0.degree. C. to +20.degree. C.; or (2) at ambient pH; with a high molar ratio of .alpha.-amino acid to a cephalosporanic nucleus.

Abstract: Provided are pharmaceutical formulations, and methods of inhibiting fungal and parasitic activity using a compound of formula I ##STR1## where: R', R", R'", R.sup.x1, R.sup.x2, R.sup.y1, R.sup.y2, R.sup.y3, R.sup.y4, and R.sup.0 are as defined above; andR.sup.2 is ##STR2## each R.sup.2a is independently hydroxy, halo, nitro, amino, trifluoromethyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkylthio;a is 1, 2, 3 or 4;R.sup.3 is C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12 alkoxy or --O--(CH.sub.2).sub.m --?O--(CH.sub.2).sub.n !.sub.p --O--(C.sub.1 -C.sub.12 alkyl);m is 2, 3 or 4;n is 2, 3 or 4; andp is 0 or 1;or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides HIV protease inhibitors, intermediates for preparing HIV protease inhibitors. The enzyme, HIV protease, represents a viable target for the inhibition of HIV viral replication, thus providing a method for treating and/or preventing HIV infection.

Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of their use.

Abstract: Certain vinyl acetylene benzimidazole compounds which inhibit the growth of picornaviruses, such as rhinoviruses, enteroviruses, cardioviruses, polioviruses, coxsackieviruses of the A and B groups, echo virus and Mengo virus.

Abstract: Provided are pharmaceutical formulations, and methods of inhibiting fungal and parasitic activity using a compound of formula I: ##STR1## wherein R', R", R.sup.x1, R.sup.x2, R.sup.y1 -R.sup.y4, R.sup.z1, R.sup.z2, a, b, c, d, e, R.sup.0, R.sup.1 and R.sup.2 are defined as in the specification.

Abstract: Provided are pharmaceutical formulations, and methods of inhibiting fungal and parasitic activity using a compound of formula I: ##STR1## wherein: R' is hydrogen, methyl or NH.sub.2 C(O)CH.sub.2 --;R" and R'" are independently methyl or hydrogen;R.sup.x1, R.sup.x2, R.sup.y1, R.sup.y2, R.sup.y3, and R.sup.y4 are independently hydroxy or hydrogen;R.sub.0 is a group of the formula ##STR2## R.sub.1 is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, phenyl, p-halo-phenyl, p-nitrophenyl, phenoxy, benzyl, p-halo-benzyl, or p-nitro-benzyl; andR.sub.2 is an acyl side chain as defined herein.

Abstract: Various 3-substituted 3-cephems useful as anti-bacterial agents are provided, Also provided are pharmaceutical compositions comprising same and methods for treating bacterial infections in man and other animals.