摘要:
A .beta.-lactamase inhibitor of the formula ##STR1## and the pharmaceutically acceptable salts thereof are presented. Also presented are intermediates and synthetic processes for the manufacture of the formula I compound.The compound inhibits the activity of enzymes which inactivate certain .beta.lactam antibiotics.
摘要:
The amino acid 2-amino-4-(2-aminoethoxy)-trans-but-3-enoic acid can be conveniently prepared via novel intermediates from a 2,2'-disubstituted diethyl ether and a dialkyl N-protected amidomalonate starting material using a multi-step process. Preferred starting materials are bis-2-chloroethyl ether and diethyl acetamidomalonate. The process, in a preferred embodiment, proceeds through the key intermediate ethyl-2-acetamido-4-[2-(2-phthalimido)ethoxy]-but-2-enoate.
摘要:
There are presented antibacterial cephalosporine having broad antimicrobial activity, having the formula ##STR1## wherein R is hydrogen or a carboxylic acid-protecting group: R.sub.1 represents a substituted piperazinyl group of formula ##STR2## or a substituted pyrrolidinylamino group of formula ##STR3## or a substituted pyrrolidinylmethylamino group of formula ##STR4## where the piperazinyl or pyrrolidinyl group may be optionally substituted with one or more lower alkyl groups, and where Q represents a substituted quinolinyl or naphthyridinyl group: R.sub.2 is selected from the group consisting of hydrogen, lower alkoxy, lower alkylthio and amido; R.sub.3 is hydrogen or an acyl group: and m is 0, 1 or 2, but preferably 0; as well as the corresponding readily hydrolyzable esters. pharmaceutically acceptable salts and hydrates of these compounds.
摘要:
There are presented anti-bacterial cephalosporins having broad antimicrobial activity of the formula ##STR1## wherein R.sub.1 is an antibiotically active quinolonyl; R.sub.2 is selected from the group consisting of hydrogen, lower alkoxy, amino, lower alkylthio and amido; R.sub.3 is selected from the group consisting of hydrogen, and acyl group, and m is 0, 1 or 2 and the readily hydrolysable esters or salts of these compounds and hydrates of the compounds of formula I or of their esters or salts.
摘要:
There are presented antibacterial cephalosporins having broad antimicrobial activity as well as intermediates for their formation, such compounds having the formula ##STR1## wherein R is hydrogen or a carboxylic acid-protecting group; R.sub.1 is a substituted piperazinium group of the formula ##STR2## in which Q represents a substituted quinolinyl or naphthyridinyl group and the piperazine nucleus may be optionally substituted with one or more lower alkyl groups; R.sub.2 is selected from the group consisting of hydrogen, lower alkoxy, lower alkylthio and amido; R.sub.3 is hydrogen or an acyl group; and m is 0, 1 or 2, preferably 0;as well as the corresponding readily hydrolyzable esters, pharmaceutically acceptable salts and hydrates of these compounds.
摘要:
The present invention is directed to compounds of the formula ##STR1## wherein R.sub.1 is lower alkyl and R.sub.2 is lower alkyl or aryl. Also provided are methods for preparation of these compounds. The compounds of formula I above are useful as plant growth regulants.
摘要:
A novel family of .beta.-lactam antibacterials, synthetic methods and intermediates useful in the production of such antibacterials, and the use of such compounds as antibacterials are disclosed. The novel compounds have the formula ##STR1## wherein, Z.sup.1 is a group --OR.sup.1, --NR.sup.3 R.sup.4, or --SR.sup.5 ;Z.sup.2 is a group --OR.sup.2, --NR.sup.3 R.sup.4, or --SR.sup.6 ;R.sup.1 and R.sup.2 may be either the same or different and each is H, lower alkyl, aralkyl, aryl or heteroaryl;R.sup.3 and R.sup.4 may be either the same or different and each is H, lower alkyl, aralkyl, aryl or heteroaryl;R.sup.5 and R.sup.6 may be either the same of different and each is H, lower alkyl, aralkyl, aryl or heteroaryl;R.sup.7 is H, lower alkyl, or lower alkoxycarbonyl; and,R.sup.8 is acyl;as well as pharmaceutically acceptable salts thereof.
摘要翻译:公开了一种新颖的β-内酰胺类抗生素,合成方法和用于生产这种抗菌剂的中间体,以及使用这些化合物作为抗菌剂。 该新化合物具有式“IMAGE”,其中,Z1为基团-OR1,-NR3R4或-SR5; Z2是基团-OR2,-NR3R4或-SR6; R 1和R 2可以相同或不同,各自为H,低级烷基,芳烷基,芳基或杂芳基; R 3和R 4可以相同或不同,各自为H,低级烷基,芳烷基,芳基或杂芳基; R 5和R 6可以是不同的,并且各自是H,低级烷基,芳烷基,芳基或杂芳基; R7是H,低级烷基或低级烷氧基羰基; R8是酰基; 以及其药学上可接受的盐。
摘要:
Antibacterial compounds of the formula ##STR1## in which R.sub.1 is a cyclic or secondary acyclic amino group which independently has antibacterial activity:R.sub.2 is hydrogen, lower alkoxy, lower alkylthio or formamido;R.sub.3 is hydrogen or an organic group bonded through carbon, oxygen, sulfur or nitrogen;R.sub.4 is an electronegative acidic group; or R.sub.3 and R.sub.4 together form a heterocycle; andR.sub.5 is a hydrogen or lower alkyl, except when R.sub.3 and R.sub.4 form a heterocycle, in which case R.sub.5 is hydrogen only; and methods of using same.
摘要:
The present invention provides oral formulations of poorly bioavailable and/or poorly absorbable, and/or poorly water soluble therapeutic agents. The invention features pharmaceutical composition including a biopolymer, a therapeutic agent, for example an antimicrobial agent such as ceftriaxone, and an absorption enhancer, for example a polyoxyethylene alkyl ether absorption enhancer. Methods of making and using the pharmaceutical compositions is also described.