Abstract: Compound of formula IVe ##STR1## where Het is 2-pyridyl or 2-benzothiazolyl, are useful as acylating agents in preparing 7-[2-(2-amino-4-thiazol)-2-oxoacetyl]-cephalosporin intermediates.

Abstract: The invention relates to novel derivatives of quinolonecarboxylic acid and naphthyridonecarboxylic acid which are linked to a .beta.-lactam antibiotic, to their salts, to processes for their preparation and to antibacterial agents containing these derivatives.

Abstract: Digitoxigenin and dihydrodigitoxigenin 3.beta.-derivatives, a process for their preparation and pharmaceutical compositions containing same for the treatment of cardiovascular disorders such as heart failure and hypertension are disclosed.

Abstract: R-(-)-1-(5-Hydroxyhexyl)-3-methyl-7-propylxanthine, a process for its preparation, and pharmaceuticals which contain this compound and which are suitable, in particular, for the prophylaxis and treatment of cerebral vascular disorders.

Abstract: This invention provides bicyclic heterocyclic derivatives and their pharmaceutically acceptable salts useful for the treatment of hypertension, urethral and lower urinary tract contractions, and other disorders. The compounds are also useful for binding .alpha..sub.1 -adrenergic and 5HT.sub.1A serotonergic receptors, in vitro or in vivo.

Abstract: The present invention is related to compounds which inhibit pancreatic cholesterol esterase. The compounds have the formula: ##STR1## wherein R.sup.1 is H or C.sub.1-6 alkyl;R.sup.2 is H or C.sub.1-6 alkyl;R.sup.3 is H or C.sub.1-6 alkyl;X is CHR.sup.6, S or O;R.sup.6 is H or C.sub.1-6 alkyl;R.sup.4 is a hydrophobic moiety; and pharmaceutically acceptable salts thereof.

Abstract: The object of the invention is to provide a .beta.-lactam compound and a 2-substituted methyl-3-cephem compound, both of which are of value as intermediates for the synthesis of cephem antibiotics.The .beta.-lactam compound of the invention may be represented by the general formula ##STR1## wherein R.sup.1 represents a protected amino group, for instance; R.sup.2 represents hydrogen for instance; R.sup.3 represents hydrogen or a carboxy-protecting group; R.sup.4 represents an aryl group which may be substituted; R.sup.5 represents an alkenyl group which may be substituted, for instance. The 2-substituted methyl-3-cephem compound of the invention may be represented by the general formula ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above; R.sup.6 represents an aryl group which may be substituted.

Abstract: The compound of the formula: ##STR1## where R.sub.1 and R.sub.5 are independently hydrogen, fluorine, chlorine, bromine, iodine, trifluoromethyl, cyano, nitro, CO.sub.2 H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.8 cycloalkyl, cycloalkylalkyl, C.sub.3 -C.sub.8 cycloalkyloxy, C.sub.2 -C.sub.7 alkylcarbonyl, C.sub.2 -C.sub.7 alkylcarbonyloxy, C.sub.2 -C.sub.7 alkoxycarbonyl, mono- or di-alkylaminocarbonyl, tetrazolyl, --OH, --(CH.sub.2).sub.1-6 OH, --SH, --NH.sub.2 or --(CH.sub.2).sub.1-6 NR.sub.8 R.sub.9 where R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkylcarbonyl, C.sub.2 -C.sub.7 alkoxycarbonyl and R.sub.9 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.2 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.3 and R.sub.4 are hydrogen or taken together with the carbon atoms to which they are attached form a double bond; R.sub.6 and R.sub.7 are independently H, C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.3 -C.sub.

Abstract: Compounds of the formula ##STR1## where Z, A, and R are as disclosed herein and pharmaceutically compatible, readily hydrolyzable esters and salts of these compounds are disclosed.The compounds have .beta.-lactamase inhibiting properties and are useful in the control of .beta.-lactamase-forming pathogens in combination with .beta.-lactam antibiotics. They also exhibit antibacterial activity of their own and can accordingly be used themselves in the control or treatment of infectious diseases.

Abstract: A 6.beta.-substituted penicillanic acid of the formula XII: ##STR1## or a pharmaceutically acceptable salt or ester thereof, whereinA and B are each hydrogen wherein the carbon atoms to which A and B are attached are linked by a single bond, or A and B together form a bond, wherein the carbon atoms to which A and B are attached are linked by a double bond,R1 is selected from the group consisting of a) hydrogen, b) a pharmaceutically acceptable salt and c) a pharmaceutically acceptable group selected from the group consisting of C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl, C.sub.3-10 cycloalkyl, C.sub.

Abstract: A cephalosporin derivative having a quaternary salt type substituent group at the 3-position, represented by formula (I): ##STR1## wherein X is a carbon atom or a nitrogen atom; Y is a sulfur atom, an oxygen atom or a nitrogen atom substituted with a substituted or unsubstituted lower alkyl group; R.sup.1 is a hydrogen atom, a lower alkyl group or a substituted lower alkyl group; R.sup.2 is a lower alkyl group, a substituted lower alkyl group, a lower alkylene group or a substituted lower alkylene group; and A is an unsaturated six-membered heterocyclic ring containing at least one nitrogen atom, or a pharmaceutically acceptable salt thereof is disclosed. The derivatives have excellent antibacterial activities and can be used as a drug for the treatment of various bacterial infections.

Abstract: The present invention is concerned with a method for the preparation of a compound of the general formula 2 ##STR1## by reaction of a compound of the formula 3Ar--Y (3)with a compound of the general formula 4 ##STR2## wherein Ar means a (hetero)aryl group, preferably selected from phenyl, naphtyl, furyl, thienyl, pyridyl, bicylic heteroaryl and tricyclic heteroaryl, which (hetero)aryl group is optionally sustituted with one to five non-strongly-electron-withdrawing substituents;M is a metal from the groups I or II of the periodic table;R.sub.12 is an electronegative group; andis 0 or 1.The invention also relates to compounds prepared according to this method and to new substituted aryl(homo)piperazines.

Abstract: An optically active pyridobenzoxazine derivative represented by formula (I): ##STR1## wherein R.sup.1 and R.sup.2 wherein R.sup.1 and R.sup.2, which may be the same or different, each represent an alkyl group having from 1 to 6 carbon atoms, a halogenated alkyl group having from 1 to 6 carbon atoms, a hydroxyalkyl group having from 1 to 6 carbon atoms, or an alkoxymethyl group having from 2 to 7 carbon atoms; R.sup.3 represents a hydrogen atom, an alkyl group having from 1 to 6 carbon atoms, an acyl group having from 2 to 7 carbon atoms, a halogen-substituted or unsubstituted alkyloxycarbonyl group having from 2 to 7 carbon atoms, a phenylmethyloxycarbonyl group, or a phenylmethyloxycarbonyl group whose phenyl moiety is substituted with a halogen atom, a nitro group, or a methoxy group; R.sup.4 represents a methyl or fluoromethyl group which is in a .beta.-configuration; R.sup.

Abstract: The present invention relates to new 1-.beta.-methyl-2-thiolic carbapenem derivatives represented by the following general formula (I) and producing method thereof. ##STR1## The above-mentioned compound is very stable against DHP-1 enzyme due to effective shielding of carbapenem ring structually and is highly effective in both gram-positive and gram-negative microorganism, especially has a remarkable effect on the Pseudomonas aeruginosa known as a disease germ having strong resistance.

Abstract: The present invention provides a cephalosporin compound represented by formulas (I-S) and (I-R) ##STR1## wherein: R.sup.1 is a C.sub.1-4 alkyl, C.sub.3-4 alkenyl, C.sub.3-4 cycloalkyl, amino optionally substituted with a C.sub.1-4 alkyl radical, phenyl, or 2-,4- or 6- substituted phenyl group with two or fewer substitutents chosen from C.sub.1-4 alkyl, C.sub.1-3 alkoxy, halogen and hydroxy radicals;R.sup.2 is hydrogen or a C.sub.1-4 alkyl group;R.sup.a and R.sup.b, which should be different from each other, are hydrogen or a C.sub.1-4 alkyl group; andQ is N or CH,and the pharmaceutically acceptable non-toxic salts, physiologically hydrolyzable esters, hydrates and solvates thereof, which possess potent and broad antibacterial activities. The invention also provides processes for preparing these compounds and to pharmaceutical compositions containing them as active ingredients.

Abstract: A process for preparing a purified hydroxymetal phthalocyanine with stable charging characteristics and small dark decay and an electrophotographic photoreceptor containing the same are disclosed. The process comprises dissolving or slurrying a precursor of a hydroxymetal phthalocyanine in an acid, precipitating a hydroxymetal phthalocyanine in a solvent or a basic solution, and heat treating the resulting hydroxymetal phthalocyanine in a basic solution. The purified hydroxymetal phthalocyanine wherein the metal is gallium is further subjected to a solvent treatment to provide a new crystal showing further improved electrophotographic characteristics.

Abstract: As new antibacterial agent are provided cephalosporin derivatives having a general formula (I): ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group or a substituted lower alkyl group, R.sup.2 is a hydrogen atom or an ester-forming group easily cleavable by an esterase present in the digestive tracts, R.sup.3 and R.sup.4 may be the same and each is independently a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkenyl group, hydroxyl group, amino group or a lower alkoxy group, and a pharmaceutically acceptable salt thereof.The cephalosporin derivative of formula (I) is useful as an orally or injectably administrable cephalosporin derivative which exhibits in combination a high antibacterial activity and a favorable characteristic capable of giving a high concentration of this compound in blood when administered.

Abstract: Enterally absorbable diastereomers of 1-(isopropoxycarbonyloxy)ethyl (6R,7R)-7-[2-(2-aminothiazol-4-yl)-2-(Z)-(methoxyimino)acetamido]-3-(metho xymethyl)-3-cephem-4-carboxylate of the formula I ##STR1## and their physiologically acceptable salts and also diastereomerically pure salts of the compounds of the formula II ##STR2## where HX is a mono- or polybasic acid and where X is an inorganic or organic physiologically acceptable anion, and a process for the preparation of these compounds of the formula I or II, which comprises first precipitating the more sparingly soluble diastereomer of the formula IV in the mixing together of 1 equivalent of a solution of the diastereomer mixture of the formula III with 0.

Abstract: The present invention relates the removal of t-butyldimethylsilyl protecting groups in the preparation of penems which are useful antibiotics. The invention provides a process for preparing a compound of the formula I: ##STR1## wherein R is a free or protected hydroxy or amino group or an alkoxy, acyloxy or an optionally substituted carbamoyloxy group, and R.sub.1 is selected from:a) hydrogen;b) a C.sub.2 -C.sub.4 alkenyl group;c) a p-NO.sub.2 benzyl group;d) a linear or branched alkanoyloxy C.sub.1 -C.sub.2 alkyl group; ande) (2-oxo-1,3-dioxolen-4-yl)methyl optionally substituted by C.sub.1 -C.sub.

Abstract: 4-Substituted pyrazolo[3,4-d]pyrimidine derivatives and a method of synthesis for the derivatives are described. The 4-substituted pyrazolopyrimidine derivatives are useful as cardiotonic agents and antiarryhythmic agents.