Abstract: Dextrorotatory isomer of 6-(5-chloro-2-pyridyl)-5[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine, its preparation and pharmaceutical compositions containing it which are usable as tranquillizers and hypnotics.

Abstract: This invention is directed to dihydropyrimidine compounds of the following formula: which are selective antagonists for human &agr;1C receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotence, cardiac arrhythmia and for the treatment of any disease where antagonism of the &agr;1C receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Abstract: A compound of formula I wherein R1 is hydrogen, methyl, ethyl, methoxy or methylthio; R2 and R3 each independently is hydrogen or lower alkyl; R4 is hydrogen, lower alkyl, methoxy, ethoxy or benzyloxy; R5 is lower alkyl, lower cycloalkyl, (CH2)mC(O)OR6 wherein m is the integer 1 or 2 and R6 is lower alkyl, phenyl optionally substituted; optionally Het or Het(lower alkyl); or R4 and R5 together with the nitrogen atom to which they are attached form a nitrogen containing ring optionally substituted with C(O)O-benzyl or with phenyl optionally substituted with C(O)OR7 wherein R7 is lower alkyl or (lower alkyl)phenyl; and Z is lower alkyl or optionally substituted phenyl or Het; with the proviso that when Z is (CH2)p-(Het), then R2 and R3 each is hydrogen; or a therapeutically acceptable acid addition salt thereof which compound is useful in the treatment of HCMV infections.

Abstract: An A-ring substituted chemical compound has the formula wherein Y is —CR3, R1, R2, R3 and R6 are, independently, hydrogen, an allyl group, a benzyl group, a propargyl group, an alkoxyl group, a halogen, a haloalkyl group, an amino group, or a cyano group, R4 is an alkyl group, an allyl group, a propargyl group or a benzyl group, and R5 is an alkyl group, or a benzyl group.

Abstract: A cephem compound, wherein the cephem ring has a substituent at the 3-position, which substituent is shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R1 is hydrogen, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; A is an optionally substituted lower alkylene, an optionally substituted lower alkenylene or a single bond; B is an optionally substituted imino or a single bond; or A and B taken together may form a single bond; and D is a single bond or a group of the formula (a): The cephem compounds of the present invention are useful as antibiotic agents.

Abstract: A method of synthesizing compounds having the formula via a 4+1 radical annulation/cyclization wherein the precursor is reacted with an aryl isonitrile having the formula wherein X is selected from the group consisting of Br and I, ≡Y is ≡N or ≡C—R3, R1, R2, and R6 are independently hydrogen, a normal alkyl group, a branched alkyl group, an allyl group, a benzyl group, an alkynyl group, a propargyl group, an alkoxyl group, a halogen group, a trialkylsilyl group, an amino group, an alkyl amino group, a dialkylamino group, an aminoalkyl group, a cyano group, or R16CO—, wherein R16 is an alkyl group, an alkoxyl group, or an amino group, R3 is hydrogen, a normal alkyl group, a branched alkyl group, an allyl group, a benzyl group, an alkynyl group, a propargyl group, an alkoxyl group, a halogen group, a trialkylsilyl group, an amino group, an alkyl amino group, a dialkylamino group, an aminoalkyl group, a cyano group, or R16CO

Abstract: The invention relates to a new process for the depletion of 7-amino-3-[(E)-1-propen-1-yl]-3-cephem-4-carboxylic acid in mixtures of 7-amino-3-[(Z)-1-propen-1-yl]-3-cephem-4-carboxylic acid and 7-amino-3-[(E)-1-propen-1-yl]-3-cephem-4-carboxylic acid, by means of the crystalline hydrochloride or a metal or amine salt of 7-amino-3-[(Z/E)-1-propen-1-yl]-3-cephem-4-carboxylic acid or by adsorption chromatography.

Abstract: A radiolabeled compound of a formula: ##STR1## is described. R1 and R2 are each independently selected from the group consisting of hydrogen, alkyl, hydroxy, alkoxy, halo, haloalkyl, carboxy, carbalkoxy and salts thereof; and A, B, C and D are each independently selected from the group consisting of a hydrogen and an electron withdrawing group, provided that at least one of A, B, C and D is [18]fluorine.

Abstract: A new antibacterially active agent has been isolated from Streptomyces clavuligerus. This new compound which is designated clavulanic acid has the formula (I): ##STR1## In addition to being a broad spectrum antibiotic of medium potency, clavulanic acid and its salts and esters have the ability to enhance the effectiveness of .beta.-lactam antibiotics against many .beta.-lactamase producing bacteria.

Abstract: The subject invention concerns compounds of formula (I): whereinn=1 or 2;R.sup.1 is H, NH.sub.2 or halogen;R.sup.2 is H or NH.sub.2 ;R.sup.3 represents the group CR.sup.6 R.sup.7 R.sup.8 where R.sup.6, R.sup.7 and R.sup.8 are the same or different and are each H, C.sub.1-6 alkyl or C.sub.1-6 haloalkyl;R.sup.4 and R.sup.5 are the same or different and are selected from the group consisting of H, CO.sub.2 H, CO.sub.2 C.sub.1-6, NHSO.sub.2 CF.sub.3, tetrazole and (CR.sup.9 R.sup.10).sub.p (Y).sub.q (CR.sup.9 R.sup.10).sub.t Z where (CR.sup.9 R.sup.10), or (CR.sup.9 R.sup.10).sub.t is straight or branched chain bearing the substituents R.sup.9 and R.sup.10 when p or t>1;R.sup.9 and R.sup.10 are the same or different and are each C.sub.0-6 alkyl-Z;p=1-3;q=0 or 1;t=0-4, provided that t>0 when q=1;Y=O, NH or S(O).sub.m where m=0-2; andZ is selected from a group consisting of H, CN, CO.sub.2 H, CO.sub.2 C.sub.1-6 alkyl, NHSO.sub.2 CF.sub.3 tetrazole, triazole, CONH.sub.2, CON(C.sub.1-6 alkyl).sub.2, CONH(C.sub.

Abstract: The invention relates to novel 2-bromo- and 2-nitroxy derivatives of 3-,bromo- and 3-dibromo-4-oxo-azetidines, to processes for the preparation thereof and to the use thereof.According to the invention 2-bromo- and 2-nitroxy derivatives of 3-bromo- and 3-dibromo-4-oxo-azetidines are prepared by reacting derivatives of protected penicillanic lanic acid 1,1-dioxides with DBN reactant (1,5-diazabicyclo/3.4.

Abstract: Compounds of formula (I): ##STR1## wherein: R.sup.1 is hydrogen or a hydroxy-protecting group; R.sup.2 is alkyl, alkoxy, halogen, optionally substituted phenyl or optionally substituted phenoxy; R.sup.3 is optionally substituted pyridyl, optionally substituted quinolyl or phenyl group which has a substituent of formula --CYNR.sup.5 R.sup.6, where Y is oxygen or sulfur, and R.sup.5 and R.sup.6 are each alkyl, aryl or aralkyl, or R.sup.5 and R.sup.6 and the nitrogen to which they are attached together form a heterocyclic group; is R.sup.4 hydrogen or an amino-protecting group; and Z is sulfur or oxygen; are valuable intermediates in the preparation of carbapenem compounds and retain a desirable configuration during conversion to such carbapenem compounds.

Abstract: There is provided a process for the manufacture of insecticidal 2-aryl-4-halopyrrole compounds via the in situ sequential oxidation, ring halogenation and side chain halogenation of an appropriate 2-aryl-1-methyl-2-pyrroline precursor.

Abstract: Cobalt prophyrins of the following formula (l): ##STR1## or a salt or ligand complex thereof and their synthesis, pharmaceutical compositions and use in controlling obesity.

Abstract: A process for the direct and regioselective functionalization of phenothiazine which allows one to introduce an SH group in position 2 is described. The thus-obtained 2-mercapto-phenothiazine is easily transformed into 2-methylthio-phenothiazine, an important intermediate for the preparation of pharmacological active compounds. One of the reaction routes (described in detail in the specification) involves the production of an N-aryl-phenothiazine-2-sulfinic acid [compound (III)] which can be isolated as a salt (e.g., an alkaline salt) by treatment with an aqueous alkaline solution. Thus compound (III-A) is produced.

Abstract: A modifying agent for a conductive substrate which comprises a flavin derivative represented by the formula: ##STR1## wherein R1 represents a hydrogen atom or an acyl groups, R2 and R3 each represent a hydrogen atom or a lower alkyl group having one to four carbon atoms, and R4 represents a thiocyanato group or a mercapto group.

Abstract: A composition of matter is provided comprising a crystalline saponin-containing complex, wherein said crystalline complex is derived from a steroidal-saponin-containing plant material. Said crystalline complex is derived from a saponin-containing plant material by forming a mixture comprising saponin-containing aqueous plant extract solids and a mixture comprising methanol, acetone and water in a volume ratio of about 0.1-20:0.1-20:1.0, and allowing the solution to stand at ambient temperature and pressure for a period of time sufficient to form the crystalline saponin-containing complex while plant fats and non-saponin carbohydrates remain substantially in solution.

Abstract: The invention relates to a dealkylation chemical process for preparing imidazoquinoxalines bearing hydrogen substitution in the five position, and to valuable pharm-intermediates of the formula I ##STR1## wherein ##STR2## wherein R' is C.sub.1-6 -alkyl, C.sub.3-7 -cycloalkyl, phenyl, thienyl, or C.sub.1-3 -alkoxymethyland wherein R.sup.6 and R.sup.7 independently are hydrogen,halogen or CF.sub.3, used in that process. The intermediates also have anticonvulsant and anxiolytic properties.

Abstract: The present invention is novel derivatives of pyrrolo[3,2-d]pyrimidines and pharmaceutical compositions and methods of use therefor. The derivatives are inhibitors of purine nucleoside phosphorylase selectively cytotoxic to T-cells but not to B-cells in the presence of 2'-deoxyguanosine and, therefore, are for use in the treatment of autoimmune diseases, gout, psoriasis or rejection of transplantation.

Abstract: A process for treating psoriasis by externally applying to the skin of a warm-blooded animal a composition comprising:(A) a pharmaceutically effective amount of an active-type vitamin D.sub.3,(B) a substantially water-free carrier containing the active-type vitamin D.sub.3 dissolved or uniformly dispersed therein, and(C) a solvent selected from fatty acid esters, higher alcohols with 10 or more carbons and propylene carbonate.