Abstract: Triazole derivatives of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.

Abstract: Triazole derivatives of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.

Abstract: Sulfonyl derivatives of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome or Syndrome X, and other symptoms associated with NIDDM.

Abstract: The present invention provides a method for the treatment or prevention of conditions which can be ameliorated by Smo antagonism, which method comprises administration to a patient in need thereof of an effective amount of a compound of formula I or a composition comprising a compound of formula I: or a pharmaceutically acceptable salt or solvate thereof; wherein: 2 of X, Y and Z represent nitrogen atoms, and the other represents an oxygen atom; R1 and R2 are taken together with the atom to which they are attached and represent a cyclobutyl ring, optionally substituted with 1-2 fluorine atoms, and R3 represents hydrogen or a fluorine atom; or R1 represents methyl, R2 represents methyl or a fluorine atom and R3 represents a fluorine atom.

Abstract: Pyrazole carboxamides of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.

Abstract: Compounds having Formula (I), including pharmaceutically acceptable salts and prodrugs thereof: are selective inhibitors of the 11?-HSD1 enzyme. They inhibit the 11?-HSD1-mediated conversion of cortisone and other 11-keto-glucocorticoids to cortisol and other 11?-hydroxy-glucocorticoids. The 11?-HSD1 inhibitors therefore decrease the amount of cortisol in target tissues, thereby modulating the effects of cortisol.

Abstract: Triazole derivatives of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.

Abstract: Triazole derivatives of structural formula I are selective inhibitors of the 11&bgr;-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.

Abstract: The present invention pertains to the combinatorial synthesis of antibacterial agents that inhibit the Mur-pathway enzymes involved in bacterial cell wall assembly. The method uses p-alkoxybenzylidene as the linker for the attachment of a derivatized muramic acid to the polymeric resin support. This intermediate becomes the starting point for the combinatorial synthesis, which in conjunction with split-pooling techniques allows rapid synthesis of diverse analogues for high-throughput screening (HTS). The invention is further directed to the libraries of these finished compounds that vary at the peptide, N-acyl and anomeric UDP positions.

Abstract: Transfer ribonucleic acid (tRNA) synthetase inhibitors, salts, and pharmaceutically acceptable compositions thereof of the general formula: wherein Ar is aryl and heteroaryl; L is —C(O)N(Q)CH2—, or —CR10R11OCR12R13—; Q is hydrido, —(CH2)mCO2H and —(CH2)mCO2CH3, m is 1, 2, 3, and 4; R1, R2, R9, R10, R11, R12 and R13 are hydrido or lower alkyl; wherein Het is a heterocyclic moiety, the inhibitors are suitable for use as antimicrobial agents.

Abstract: Compounds, pharmaceutically acceptable salts, and compositions thereof of the general formula: wherein Ar is aryl and heteroaryl; R1, R2, R3, and R4 are hydrido, alkyl, cyano, heteroaryl, hydroxy, amino, acylamino, halo, alkoxy, aryloxy, carboxyamido, alkenyl, cycloalkyl, heterocyclyl, acyl, acyloxy, carboalkoxy, carboxy, thio, sulfinyl, sulfonyl and sulfoxy, R5, R6, R7, and R8 are hydrido and lower alkyl; and Het is a nitrogen-containing heterocyclic ring.

Abstract: Transfer ribonucleic acid (tRNA) synthetase inhibitors, salts, and pharmaceutically acceptable compositions thereof of the general formula: 1

Abstract: Transfer ribonucleic acid (tRNA) synthetase inhibitors, salts, and pharmaceutically acceptable compositions thereof of the general formula: wherein Ar is aryl and heteroaryl; L is —C(O)N(Q)CH2—, or —CR10R11OCR12R13—; Q is hydrido, —(CH2)mCO2H and —(CH2)mCO2CH3, m is 1, 2, 3, and 4; R1, R2, R9, R10, R11, R12 and R13 are hydrido or lower alkyl; wherein Het is a heterocyclic moiety, the inhibitors are suitable for use as antimicrobial agents.

Abstract: Compounds, pharmaceutically acceptable salts, and compositions thereof of the general formula: 1

Abstract: Compounds, pharmaceutically acceptable salts, and compositions thereof of the general formula: wherein Ar is aryl and heteroaryl; R1, R2, R3, and R4 are hydrido, alkyl, cyano, heteroaryl, hydroxy, amino, acylamino, halo, alkoxy, aryloxy, carboxyamido, alkenyl, cycloalkyl, heterocyclyl, acyl, acyloxy, carboalkoxy, carboxy, thio, sulfinyl, sulfonyl and sulfoxy, R5, R6, R7, and R8 are hydrido and lower alkyl; and Het is a nitrogen-containing heterocyclic ring.

Abstract: Compounds of formula I: as well as pharmaceutically acceptable salts thereof and compositions useful as carbapenem antibacterial agents are disclosed.

Abstract: Transfer ribonucleic acid (tRNA) synthetase inhibitors, salts, and pharmaceutically acceptable compositions thereof of the general formula: wherein Ar is aryl and heteroaryl; L is —C(O)N(Q)CH2—, or —CR10R11OCR12R13—; Q is hydrido, —(CH2)mCO2H and —(CH2)mCO2CH3, m is 1, 2, 3, and 4; R1, R2, R9, R10, R11, R12 and R13 are hydrido or lower alkyl; wherein Het is a heterocyclic moiety, the inhibitors are suitable for use as antimicrobial agents.

Abstract: Carbapenems of the formula: ##STR1## are disclosed as useful antibacterial agents. Pharmaceutical compositions and methods of use are also disclosed.

Abstract: A process of producing 8a- and 9a- azalide compounds is disclosed, comprised of reacting an 8a- aza or 9a- aza azalide eastern fragment or a derivative thereof with a compound of the formula:X--A'--Ywherein X and Y are appropriate reactive groups and A' is a fragment or compound which forms the western portion of the azalide, andcyclizing this intermediate to form the target 8a- or 9a-azalide compound. Compounds of formula I, II and III as well as other azalides can be synthesized according to this process.

Abstract: A method of making compounds of the formulae: ##STR1## wherein X is ##STR2## R.sup.1 is hydrogen, methyl, C.sub.1-10 alkoxycarbonyl or arylsulfonyl when X is CH.sub.3 CH.sub.2 CHNH.sub.2 and is additionally aralkoxycarbonyl when X is NH.sub.2 ; one of R.sup.2 and R.sup.3 is hydrogen and the other is OH, NHR.sup.1 or NMeR.sup.1 where R.sup.1 is as defined above; R.sup.4 is hydrogen or C.sub.1-10 alkyl when X is CH.sub.3 CH.sub.2 CHNH.sub.2 and is additionally aralkyl when X is NH.sub.2 ; R.sup.5 is hydrogen or C.sub.1-3 alkyl when X is CH.sub.3 CH.sub.2 CHNH.sub.2 ; R.sup.5 is hydrogen when X is NH.sub.2 ; one of R6 and R7 is hydrogen and the other is methyl except when X is CH.sub.3 CH.sub.2 CHNH.sub.2 and R.sup.2 is H, in which case R.sup.6 is methyl and R.sup.7 is hydrogen. These compounds are made from erythromycin-derived fragments of the formulae: ##STR3## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are defined as before for when X is NH.sub.2 ; R.sup.5 is hydrogen or C.sub.1-3 alkyl; if R.sup.