摘要:
There is presented optically uniform .beta.-lactams of the formulae ##STR1## wherein Z is a readily cleavable acyl group, R.sup.1 is amino or a group convertible into amino, R.sup.2 is hydrogen or a readily cleavable protecting group and R.sup.3 and R.sup.4 each are a lower hydrocarbon group which optionally contains oxygen and which is attached via a carbon atom, whereby these groups can also be joined with one another to form a ring, with the proviso that R.sup.1 is a readily cleavable acylamino when R.sup.2 is hydrogen,and the corresponding optical antipodes, their manufacture and use in the manufacture of antimicrobially-active .beta.-lactams as well as novel intermediates usable in their manufacture.
摘要:
Antibiotic cephalosporin compounds, method of making and pharmaceutical composition thereof represented by the general formula ##STR1## wherein R.sup.1 is amino, lower alkylamino, a protected amino, a protected lower alkylamino, hydroxy or lower alkoxy,R.sup.2 is hydrogen, acyloxy, pyridium or a heterocyclicthio group which may have suitable substituent(s),R.sup.3 is carboxy or its derivative,A is carbonyl, hydroxy(lower)alkylene or a protected hydroxy(lower)alkylene andR.sup.4 is hydrogen or halogen, orR.sup.2 and R.sup.3 are linked together to represent a group of the formula --COO--, this divisional application being directed to intermediate compounds of the formula: ##STR2##
摘要:
Phthalimides of the formula I ##STR1## where R is a substituent and the ring A can be further substituted, are cleaved by a process in which a compound of the formula I is treated with an alkanolamine.The compounds prepared according to the invention are useful intermediates for the preparation of dyes, drugs and plastics.
摘要:
Benzhydrylpiperazinyl Thiazole compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, amino, or mono- or di- substituted amino, in which the substituent is selected from lower alkyl, acyl and di(lower)alkylaminomethylene,R.sup.2 is hydrogen, halogen, lower alkyl or aryl,R.sup.3 is ar(lower)alkyl optionally substituted by halogen,A is lower alkylene optionally interrupted by a sulfur atom, andY is C.sub.1 -C.sub.3 alkylene,having antiallergic activity.
摘要:
Histamine H.sub.2 -antagonists of the formula ##STR1## wherein p is 1 or 2; R.sup.1 is hydroxy, amino, substituted amino or a 5- to 9-membered fully saturated nitrogen-containing heterocyclic ring attached via its nitrogen atom; m is an integer of from 0 to 2; n is an integer of from 2 to 4; Z is sulfur, oxygen or methylene; and A is an optionally substituted phenyl, imidazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, triazolyl, thiadiazolyl, oxadiazolyl, furyl, thienyl or pyridyl ring; and nontoxic pharmaceutically acceptable salts, hydrates, solvates or N-oxides thereof are novel anit-ulcer agents. Intermediates and processes for their preparation are disclosed.
摘要:
2-Amino-4-(4-benzyloxyphenyl)thiazole compounds of the formula: ##STR1## wherein X is hydrogen, a halogen, a lower alkyl having 1 to 4 carbon atoms or trifluoromethyl; R is hydrogen, a lower alkyl having 1 to 4 carbon atoms, a lower alkenyl having 2 to 4 carbon atoms or a carboxylic acyl having 1 to 6 carbon atoms; and n is 1 or 2, or pharmaceutically acceptable salts thereof, are novel compounds and are useful as a prophylactic agent or therapeutic agent against hyperlipemia in mammals including human beings.
摘要:
This invention encompasses orally effective antiulcer agents of the formula ##STR1## wherein X is hydroxy, (C.sub.1 -C.sub.5)-alkoxy, phenoxy, benzyloxy, or --NH(CH.sub.2).sub.n Y wherein n is an integer of value 2 to 4 and Y is di-(C.sub.1 -C.sub.3)-alkylamino, 1-pyrrolidinyl, 1-piperidinyl or 4-morpholinyl;R' and R" when taken together are (C.sub.3 -C.sub.8)-alkylene, with the proviso that the ring so formed is 5- to 8-membered;R' and R" when taken separately are each independently hydrogen, (C.sub.1 -C.sub.6)-alkyl or (C.sub.5 -C.sub.6)-cycloalkyl, with the proviso that when X is other than --NH(CH.sub.2).sub.n Y, at least one of R' and R" is other than hydrogen;the pharmaceutically acceptable cationic salts thereof when X is hydroxyl, and the pharmaceutically acceptable anionic salts thereof when X is --NH(CH.sub.2).sub.n Y.
摘要:
Antibiotic cephalosporin compounds, method of making and pharmaceutical composition thereof represented by the general formula ##STR1## wherein R.sup.1 is amino, lower alkylamino, a protected amino, a protected lower alkylamino, hydroxy or lower alkoxy,R.sup.2 is hydrogen, acyloxy, pyridium or a heterocyclicthio group which may have suitable substituent(s),R.sup.3 is carboxy or its derivative,A is carbonyl, hydroxy(lower)alkylene or a protected hydroxy(lower)alkylene andR.sup.4 is hydrogen or halogen, orR.sup.2 and R.sup.3 are linked together to represent a group of the formula --COO--.
摘要:
A class of amides disclosed to be useful as selective pre-emergent and post-emergent herbicides are those having the general structural formula ##STR1## in which R.sup.1 is hydrogen or methyl, R.sup.2 is ethyl, isopropyl, cyclopropyl, tert.butyl, methylamino, dimethylamino, ethylamino or methoxymethylamino, R.sup.3 is phenyl, 4-chlorophenyl, 3,4-dichlorophenyl, 4-methylphenyl or 4-methoxyphenyl, R.sup.4 is hydrogen or C.sub.1 to C.sub.3 lower alkyl, and R.sup.5 is hydrogen or methyl, with the further stipulation that either, but not both R.sup.4 and R.sup.5 may be hydrogen.
摘要:
New compounds which are herbicide antagonists that are useful for protection of plants from various herbicides are members of the group having the general structural formulas: ##STR1## in which R is hydrogen or C.sub.1 to C.sub.4 alkyl, alkenyl or alkynyl, branched or straight chain, R.sup.1 is C.sub.1 to C.sub.3 alkyl, alkenyl or alkynyl, branched or straight chain, with the total number of carbon atoms in R and R.sup.1 being less than six, preferably less than four, on compounds with both R and R.sup.1 substituents. The novel plant protection agents may be applied both to seeds and to the soil.