摘要:
The present invention comprises compounds of the formula ##STR1## and the biologically acceptable acid addition salts thereof wherein R.sub.1 represents hydrogen, or lower alkyl having 1-4 carbon atoms; R.sub.2 represents p-hydroxybenzyl or benzyl; R.sub.3 represents an alkyl having 1-6 carbon atoms; R.sub.4 represents amino or guanidino; R.sub.5 represents p-nitrophenyl, methylnitrophenyl, dinitrophenyl, naphthyl, or nitronaphthyl; and n is 3 or 4.
摘要:
The present invention encompasses the acid addition salts of a compound of the formula ##STR1## wherein R.sub.1 represents phenylsulfonyl, benzoyl, carbobenzoxy, and the halo, loweralkyl having 1-4 carbon atoms, loweralkoxy having 1-3 carbon atoms, phenyl, or hydroxy substituted derivatives thereof; or alkanoyl having 2-12 carbon atoms; and R.sub.2 represents alkyl having 1-10 carbon atoms, or alkoxyalkyl having 2-6 carbon atoms, cycloalkyl having 5-7 carbon atoms, or benzyl and the halo, loweralkyl having 1-4 carbon atoms, loweralkoxy having 1-3 carbon atoms, hydroxy, carboxy, or phenyl substituted derivatives thereof.Compounds of the present invention are useful as analytical reagents. Enzymatic hydrolysis provides --S--R.sub.2 which can be further reacted with 5,5'-dithiobis (2-nitrobenzoic acid) to provide a colored product by which the enzyme concentration can be determined spectrophotometrically.
摘要:
The present invention encompasses acid addition salts of a compound of the formula ##STR1## wherein: R.sub.1 represents phenylsulfonyl, benzoyl, carbobenzoxy, and the halo, loweralkyl having 1-4 carbon atoms, loweralkoxy having 1-3 carbon atoms, phenyl, or hydroxy substituted derivatives thereof; or alkanoyl having 2-12 carbon atoms; R.sub.2 represents alkyl having 1-10 carbon atoms, alkoxyalkyl having 2-6 carbon atoms, cycloalkyl having 5-7 carbon atoms, benzyl and the halo, loweralkyl having 1-4 carbon atoms, loweralkoxy having 1-3 carbon atoms, carboxy, hydroxy, or substituted derivatives thereof; R.sub.3 represents hydrogen or guanyl, and m is 3 or 4.Compounds of the present invention are useful as analytical reagents. Enzymatic hydrolysis provides --S--R.sub.2 which can be further reacted with 5,5'-dithiobis (2-nitrobenzoic acid) to provide a colored product by which the enzyme concentration can be determined spectrophotometrically.
摘要:
This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent. The exemplary compounds have the following formula: wherein X is selected from the group consisting of substituted phenyl, substituted or unsubstituted heteroaryl and unsubstituted cycloalkyl; R3a is selected from the group consisting of H, unsubstituted C1 or C2 or C3 or C4 or C5 or C6 alkyl and unsubstituted C3 or C4 or C5 or C6 cycloalkyl; R3b is selected from the group consisting of H, unsubstituted C1 or C2 or C3 or C4 or C5 or C6 alkyl and unsubstituted C3 or C4 or C5 or C6 cycloalkyl; with the proviso that R3a and R3b, along with the atom to which they are attached, are optionally joined to form a 3 or 4 or 5 or 6 membered ring, with the proviso that R3a and R3b cannot both be H, or a salt thereof.
摘要:
Novel monosubstituted and disubstutituted oxaboroles and pharmaceutical compositions containing such oxaboroles are provided, which are useful for treating bacterial infections, as well as combinations of these oxaboroles with at least one additional therapeutically effective agent.
摘要:
This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.
摘要:
This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.
摘要:
Compositions and methods of use of borole derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.
摘要:
Antimicrobial compounds having the formula ##STR1## as well as pharmaceutically acceptable salts, esters or prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.