摘要:
A compound represented by the formula (I) is disclosed. The compound of the formula (I) is useful as a fine particle drug carrier. When used as the fine particle drug carrier, the compound efficiently avoids a reticuloendothelial system and has a long circulation time in blood. ##STR1##
摘要:
Sialic acid- containing glycolipid derivatives represented by the following general formula, their production method, and the particulate carriers that contain as a constituent the sialic acid-containing glycolipid derivative(s). ##STR1## wherein represents the .alpha.- or the .beta.- linkage, R.sup.1, a hydrogen atom or an acetyl group,R.sup.2, a hydrogen atom, a lower alkyl group with 1-4 carbon atoms, an alkaline metal ion, or such,X, an oxygen or sulfur atom or a residue represented by the following formula (II) or (III),--O(CH.sub.2).sub.m NHCO-- (II) where m represents an integer from 1 to 10.--O(CH.sub.2).sub.m CONH-- (III)Y, the formula (IV). ##STR2## where A represents a linear or branched chain acylamino group with 10-40 carbon atoms, or such B, a hydrogen atom, a carboxyl group or such, or the formula (V), and ##STR3## n, an integer of 0 to 3.
摘要:
Cephalosporin compounds of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and are a hydrogen atom or a lower alkyl group of 1-5 carbon atoms and A is a hydrogen atom or a nucleophilic compound residue or pharmacologically acceptable salts thereof have excellent antibacterial activity against Gram positive and Gram negative microorganisms.
摘要:
A therapeutic and/or prophylactic agent for viral infection, particularly human immunodeficiency virus (HIV) infection, which comprises as an active ingredient a lactam compound represented by formula (I) ##STR1## wherein X represents --COOR, wherein R represents a hydrogen atom or a straight-chain or branched-chain alkyl group having from 1 to 8 carbon atoms, or ##STR2## wherein n represents an integer of 2 or 3 and A represents methine when n is 2 or a quarternary carbon atom when n is 3, or a pharmaceutically acceptable salt or ester derivative thereof.
摘要:
A novel ester of a cephem compound having a carboxyl group at the 4-position in the nucleus; a process for preparing the same by reacting a cephem carboxylic acid or its salt with a halogenide; and a method for removing the protective group for the carboxyl group in the nucleus of a cephem compound by contacting it with an alcohol, or with an organic solvent in the presence of a Lewis acid.
摘要:
Sugar lactams such as N-(3-phenylpropyl)-1-deoxynojirimycin, 1-deoxynojirimycin, D-glucaro-.delta.-lactam, 6-O-triphenylmethyl-D-gluco-.delta.-lactam, etc. and new derivatives thereof which markedly inhibit metastasis of cancer cells.
摘要:
A 9,3"-di-acyl derivative of a macrolide antibiotic can be readily produced by reacting a macrolide antibiotic or an acyl derivative thereof with an organic acid halide, particularly an alkanoic acid halide, in a solvent and in the presence of a molecular sieve consisting of a synthetic zeolite and then de-acylating partially the resultant acylation products by a partial hydrolysis in an aqueous alcohol to give the 9,3"-di-acyl derivative of the macrolide antibiotic.
摘要:
A process for preparing a cephalosporanic acid derivative or a 7-acylaminocephalosporanic acid derivative which comprises subjecting an esterifying agent to reaction in liquid sulfur dioxide in the presence of a base with an N-protected-cephalosporin C to obtain a diester, subjecting the diester to reaction in an inert solvent with an iminohalide forming agent to produce an iminohalide, subjecting the iminohalide with a lower alcohol to produce an iminoether, subjecting the product produced, after subjecting the iminoether to reaction with a reactive derivative of an organic acid, to hydrolysis and further eliminating the ester group of the carboxylic acid.
摘要:
Sugar lactams such as N-(3-phenylpropyl)-1-deoxynojirimycin, 1-deoxynojirimycin, D-glucaro-.delta.-lactam, 6-O-triphenylmethyl-D-gluco-.delta.-lactam, etc., and new derivatives thereof which inhibit metastasis of cancer cells.
摘要:
This is a class of antibacterial compounds of the formula: ##STR1## wherein Y is straight or branched alkyl or alkenyl chain, cycloalkanomethyl of 3-6 carbon atoms, each group being optionally substituted by halogen, or a group ##STR2## wherein n is 0 or an integer of 1-3, A is a group --COR.sup.3 wherein R.sup.3 is hydroxy, a group ##STR3## wherein R.sup.4 and R.sup.5, which may be the same or different, are hydrogen or alkyl of 1-5 carbon atoms, a group ##STR4## or a 5- or 6-membered heterocyclic group containing nitrogen and/or sulfur, and R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, alkyl of 1-5 carbon atoms, or R.sup.1 and R.sup.2 may be combined together to form cycloalkylidene of 3-5 carbon atoms, and Z is a group of the formula: ##STR5## wherein m is 0 or an integer of 3-5, R.sup.6 is hydrogen or alkyl of 1-3 carbon atoms, and R.sup.7, when m is an integer of 3-5, is alkyl of 1-5 carbon atoms, alkenyl, cyclopropyl, a group --(CH.sub.2).sub.p B wherein p is 0 or an integer of 1-3 and B is amino, alkyl-substituted amino, hydroxy, carboxy, carbamoyl, trifluoromethyl, sulfonic acid, sulfonic acid amide, alkylthio or cyano or, when m is 0, is alkyl of 1-5 carbon atoms, which may optionally be substituted by halogen, alkenyl, a group ##STR6## wherein R.sup.8 is hydrogen, alkyl of 1-4 carbon atoms or phenyl, or cyclopropyl, and a salt thereof.