摘要:
Disclosed are 6-, 1- and 2-substituted-1-carbadethiapen-2-em-3-carboxylic acids having the structure: ##STR1## wherein: R.sup.1, R.sup.6, R.sup.7 and R.sup.8 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, alkenyl, aryl and aralkyl. Such compounds as well as their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
摘要:
Disclosed are 6-substituted amino-2-substituted-pen-2-em-3-carboxylic acids of the following structure: ##STR1## wherein R.sup.1 is hydrogen or acyl, R.sup.2 is hydrogen or methoxyl, and R.sup.3 is inter alia, hydrogen, --R, --OR, --SR, --NR.sub.2, R is alkyl, aryl, aralkyl, heterocyclyl or heterocyclylalkyl; n is 0 or 1; when n=1, R.sup.3 is not --SR.Such compounds and their pharmaceutically acceptable salt, and ester derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
摘要:
Disclosed are 1-substituted-pen-2-em-3-carboxylic acids (I) and their pharmaceutically acceptable salts and esters which are useful as antibiotics; such compounds are prepared by total synthesis. ##STR1## wherein R.sup.1 is, inter alia, substituted and unsubstituted alkyl, aryl and aralkyl.
摘要:
The invention concerns 3-amino-4-(2-hydroxyethylthio)-2-oxo-azetidine compounds of the formula ##STR1## wherein R.sub.1.sup.a represents hydrogen or an amino protective group R.sub.1.sup.A, R.sub.1.sup.b represents hydrogen or an acyl group Ac.sub.1, or R.sub.1.sup.a and R.sub.1.sup.b together denote a bivalent amino protective group, R.sub.2 represents hydrogen or an acyl radical Ac.sub.2, and each of the radicals R.sub.3 and R.sub.4 represents hydrogen or an organic radical bonded via a carbon atom, or salts of such compounds having salt-forming groups.
摘要:
There is described the preparation of novel 2-penem-3-carboxylic acid compounds having the formula ##STR1## and easily cleavable esters and carboxylic acid salts thereof. The compounds of formula I, particularly the dextrorotatory isomers thereof, are potent antibacterial agents or are of use as intermediates in the preparation of such agents.
摘要:
Novel non-nucleoside solid supports and phosphoramidite building blocks for preparation of synthetic oligonucleotides containing at least one non-nucleosidic moiety conjugated to a ligand of practical interest and synthetic processes for making the same are disclosed. Furthermore, oligomeric compounds are prepared using said solid supports and phosphoramidite building blocks, preferably followed by removal of protecting groups to provide oligonucleotides conjugated to ligands of interest.
摘要:
The present invention relates to highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using therefor. The invention involves a multi-step synthesis to produce the lactam compounds. In one step of the reaction sequence, asymmetric hydrogenation of a lactam-enamide was performed to produce an intermediate that can ultimately be converted to a series of pharmaceutical compounds. The invention also contemplates the in situ synthesis of an intermediate of the multi-step synthesis, which provides economic advantages to the overall synthesis of the lactam compounds.
摘要:
Herbicidal compositions containing a bisphosphonic acid compound of the formula ##STR1## wherein n is 0, 1, 2, 3, 4, 5 or 6, or an agrochemically acceptable salt or hydrolyzable ester thereof and methods of controlling undesirable plant growth using these bisphosphonic acid containing compositions. The herbicidal compositions exhibit desirable efficacy when applied to plants post-emergence, but exhibit little significant activity when applied to plants pre-emergence. Novel aza-bisphosphonic acid compounds are also disclosed.
摘要:
The present invention provides a compound of the formula: ##STR1## or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof wherein:A is a group of the formula (IA) or (IB): ##STR2## R.sup.1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl; R.sup.2 is hydrogen or C.sub.1-4 alkyl;R.sup.3 and R.sup.4 are the same or different and are a variety of substituents X is alkanediyl containing 1-6 carbon atoms optionally interrupted by O, S(O).sub.x (wherein x is zero, one or two), --CONR.sup.5 -- or --NR.sup.5 -- or wherein R.sup.5 is hydrogen or C.sub.1-4 alkyl;or X is alkenediyl containing 1-6 carbon atoms optionally interrupted by O, S(O).sub.x or --NR.sup.5 --.