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 hereinabove; andR.sup.2 is ##STR2## R.sup.3 is ##STR3## R.sup.3a is C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy; R.sup.3b and R.sup.3c are independently phenyl or naphthyl;R.sup.3d 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;p is 0 or 1;or a pharmaceutically acceptable salt thereof.

Abstract: Provided are pharmaceutical formulations, and methods of inhibiting fungal and parasitic activity using a compound of formula I: ##STR1## wherein: R.sup.z1 is hydrogen, --CH.sub.2 OH, --CHOHCH.sub.3 or --CHOHCH.sub.2 C(O)NH.sub.2 ;R.sup.z2 is hydrogen, --CH.sub.2 OH or --CHOHCH.sub.3 ;R.sup.z3 is hydrogen or methyl;R.sup.x1 is hydrogen, hydroxy or O--R.sup.x1' ;R.sup.x1' is C.sub.1 -C.sub.6 alkyl, benzyl, --(CH.sub.2).sub.2 Si(CH.sub.3).sub.3, --CH.sub.2 CH.dbd.CH.sub.2, --CH.sub.2 CHOHCH.sub.2 OH, --(CH.sub.2).sub.a COOH, --(CH.sub.2).sub.b NR.sup.w1 R.sup.w2, --(CH.sub.2).sub.c POR.sup.w3 R.sup.w4 or --[(CH.sub.2).sub.2 O].sub.d --(C.sub.1 -C.sub.6)alkyl;a, b and c are independently 1, 2, 3, 4, 5 or 6;R.sup.w1 and R.sup.w2 are independently hydrogen, C.sub.1 -C.sub.6 alkyl, or R.sup.w1 and R.sup.w2 combine to form --CH.sub.2 (CH.sub.2).sub.e CH.sub.2 --;R.sup.w3 and R.sup.w4 are independently hydroxy, or C.sub.1 -C.sub.6 alkoxy;d is 1 or 2;e is 1, 2 or 3;R.sup.x2, R.sup.y1, R.sup.y2, R.sup.y3 and R.sup.

Abstract: The invention provides compounds of the formula: ##STR1## wherein the variables are hereinbelow described; and salts thereof. Also, pharmaceutical formulations and methods for treating bacterial infections in man or other animals using the above compounds are disclosed.

Abstract: Provided are pharmaceutical formulations, and methods of inhibiting fungal and parasitic activity using a compound of formula I ##STR1## wherein: 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 hereinabove; andR.sup.2 is ##STR2## R.sup.3 is ##STR3## R.sup.3a, R.sup.3b, R.sup.3c and R.sup.3d are independently hydrogen, C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.12 alkynyl, C.sub.1 -C.sub.12 alkoxy, C.sub.1 -C.sub.12 alkylthio, halo, or --O--(CH.sub.2).sub.m --[O--(CH.sub.2).sub.n ].sub.p --O--(C.sub.1 -C.sub.12 alkyl) or --O--(CH.sub.2).sub.q --X--R.sup.4 ;m is 2, 3 or 4;n is 2, 3 or 4;p is 0 or 1;q is 2, 3 or 4;X is pyrrolidino, piperidino or piperazino; andR.sup.4 is hydrogen, C.sub.1 -C.sub.12 alkyl, C.sub.3 -C.sub.12 cycloalkyl, benzyl or C.sub.3 -C.sub.12 cycloalkylmethyl;or a pharmaceutically acceptable salt thereof.

Abstract: An HIV protease inhibiting compound of formula I ##STR1## wherein: R is C.sub.1 -C.sub.6 alkyl, cycloalkyl, heterocycle, unsaturated heterocycle, aryl, cycloalkyl (C.sub.1 -C.sub.4)alkyl, heterocycle(C.sub.1 -C.sub.4)alkyl, unsaturated heterocycle (C.sub.1 -C.sub.4)alkyl, aryl(C.sub.1 -C.sub.4)alkyl, or --A--(CH.sub.2).sub.q --R.sup.0, where A is --O--, --NH-- or --S--; q is 0, 1, 2 or 3; and R.sup.0 is cycloalkyl, aryl, heterocycle or unsaturated heterocycle; ##STR2## where R.sup.1 is aryl, cycloalkyl, heterocycle or unsaturated heterocycle; R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.3 is an amino acid side chain, --CH.sub.2 CH.sub.3, --CH.sub.2 CH.sub.2 CH.sub.3, --CH.sub.2 (CH.sub.2).sub.2 CH.sub.3, --C(CH.sub.3).sub.3, cyano(C.sub.1 -C.sub.4)alkyl, unsaturated heterocycle (C.sub.1 -C.sub.4)alkyl, aryl(C.sub.1 -C.sub.4)alkyl, --(CH.sub.2).sub.s --A.sup.0 --(CH.sub.2).sub.r --R.sup.4, or --CH.sub.2 --C(O)--NR.sup.2 --(CH.sub.2).sub.r --R.sup.5, where s is 1, 2, 3 or 4; r is 0, 1, 2 or 3; A.sup.

Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.

Abstract: The present application provides a series of 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. Such compounds are also useful as intermediates for preparing additional benzimidazole antiviral compounds.

Abstract: The invention provides compounds of the formula ##STR1## wherein X is CH.sub.2, S or O;R.sub.1 is a 3 position substituent such as hydrogen, hydroxy, halo, trifluoromethyl, C.sub.2 F.sub.5, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 substituted alkyl, C.sub.1 -C.sub.6 alkenyl, C.sub.1 -C.sub.6 alkynyl, CH.sub.2 O(CO)R', CH.sub.2 O(CO)NH.sub.2, CO.sub.2 R', thio(C.sub.1 -C.sub.6)alkyl, thio(C.sub.1 -C.sub.6)alkenyl, oxo(C.sub.1 -C.sub.6)alkyl, phosphine oxide, quaternary ammonium group, substituted or unsubstituted thiazolothio, or oxo (C.sub.1 -C.sub.6)alkenyl;whereinR' is hydrogen, C.sub.1 -C.sub.6 alkyl, or C.sub.1 -C.sub.6 alkenyl;R.sub.2 is hydrogen or a carboxy protecting group;R.sub.3 is ##STR2## or (CH.sub.2).sub.n ; whereinR.sub.6 is hydrogen Me, CH.sub.2 F, CF.sub.3, C.sub.2 H.sub.5, CH.sub.2 CH.sub.2 F, CH.sub.2 CF.sub.3, C.sub.2 F.sub.5, CH.sub.2 CO.sub.2 R', CH.sub.2 CONH.sub.2, C(Me).sub.2 CO.sub.2 R', or C(Me).sub.2 CONH.sub.2 ; and n is 0-5;R.sub.4 is ##STR3## wherein Z is O, S, NH, or CH.sub.

Abstract: The invention provides compounds of the formula ##STR1## wherein X is CH.sub.2, S or O; R.sub.1 is a 3 position substituent such as hydrogen, hydroxy, halo, trifluoromethyl, C.sub.2 F.sub.5, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 substituted alkyl, C.sub.1 -C.sub.6 alkenyl, C.sub.1 -C.sub.6 alkynyl, CH.sub.2 O(CO)R', CH.sub.2 O(CO)NH.sub.2, CO.sub.2 R', thio(C.sub.1 -C.sub.6)alkyl, thio(C.sub.1 C.sub.6)alkenyl, oxo(C.sub.1 -C.sub.6)alkyl, phosphine oxide, quaternary ammonium group, substituted or unsubstituted thiazolothio, or oxo(C.sub.1 -C.sub.6)alkenyl;wherein R' is hydrogen, C.sub.1 -C.sub.6 alkyl, or C.sub.1 -C.sub.6 alkenyl;R.sub.2 is hydrogen or a carboxy protecting group;R.sub.3 is ##STR2## (CH.sub.2).sub.n ; wherein R.sub.6 is hydrogen Me, CH.sub.2 F, CF.sub.3, C.sub.2 H.sub.5, CH.sub.2 CH.sub.2 F, CH.sub.2 CF.sub.3, C.sub.2 F.sub.5, CH.sub.2 CO.sub.2 R', CH.sub.2 CONH.sub.2, C(Me).sub.2 CO.sub.2 R', or C(Me).sub.2 CONH.sub.2 ; and n is 0-5;R.sub.4 is ##STR3## wherein Z is O, S, NH, or CH.sub.

Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.

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

Abstract: The present invention provides HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.

Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.

Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection.

Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.

Abstract: N-Terminal .beta.,.gamma.-didehydrovaline di- and tri-peptides are reacted with isopenicillin N synthetase to form 3-exomethylenecepham-4-carboxylic acids, e.g., .delta.-(L-.alpha.-aminoadipoyl)-L-cysteinyl-D-.beta.,.gamma.-didehydroval ine is incubated with the purified enzyme to provide 7.beta.-(L-.alpha.-aminoadipoylamino)-3-exomethylenecepham-4-carboxylic acid. The 3-exocepham products are useful intermediates to 3-alkoxy-3-cephem and the 3-halo-3-cephem antibiotics.

Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.

Abstract: Provided is a process for isolating cefaclor from an acylation reaction mixture by adding anthraquinone-1,5-disulfonic acid to the mixture. The acid highly selectively precipitates with cefaclor so that isolation and recovery is streamlined.

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

Abstract: The invention provides complexes of the formula: ##STR1## wherein X is chloro, hydrogen, vinyl, or --CH.sub.3,Z is O;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.