Abstract: 4,10-dinitro-2,6,8,12-tetraoxa-4,10-diazatetracyclo[5.5.0.0.sup.5,9 0.sup.3,11 ]dodecane is synthesized by reacting a diacyl-2,3,5,6-tetraoxypiperazine or tetraoxadiazaisowurtzitane derivative, a strong acid, and a nitrate source, such that an exothermic reaction occurs which proceeds at a temperature above ambient temperature. The reaction product is precipitated by cooling. It may be purified by washing with methanol and/or sodium bicarbonate and by simmering in nitric acid.

Abstract: Compounds and pharmaceutically acceptable salts thereof formally derived by bridging the 1- and 2-positions of 1H-imidazo[4,5-c]quinolin-4-amines. Also, methods of using such compounds and pharmaceutical formulations containing such compounds. Said compounds are useful to induce interferon biosynthesis in an animal.

Abstract: Disclosed are compounds of the formula: ##STR1## wherein: A represents arylalkyl, aryl or heteroaryl; X is nitrogen or CH; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent organic or inorganic substituents;and the pharmaceutically acceptable salts thereof; useful for treating disorders of the central nervous system.

Abstract: Synthetic intermediates of 1-arylethyl-3-substituted piperidines.

Abstract: Novel magnetic resonance imaging agents comprise complexes of paramagnetic ions with hydrazide derivatives of polyaminocarboxylic acid chelating agents. The complexes are represented by the formula of: ##STR1## wherein A is --CHR.sup.2 --CHR.sup.3 -- or ##STR2## M.sup.+Z is a paramagnetic ion of an element with an atomic number of 21-29, 42-44 58-70, and a valence, Z, of +2 or +3; R.sup.1 groups may be the same or different and are selected from the group consisting of --O.sup.- and ##STR3## The R.sup.4, R.sup.5 and R.sup.6 groups are as defined in the disclosure. These novel imaging agents are characterized by excellent NMR image-contrasting properties and by high solubilities in physiological solutions. A novel method of performing an NMR diagnostic procedure involves administering to a warm-blooded animal an effective amount of a complex as described above and then exposing the warm-blooded animal to an NMR imaging procedure, thereby imaging at least a portion of the body of the warm-blooded animal.

Abstract: The invention relates to a method of preparing N-oxo-tetrahydro-.beta.-carbolines having formula 1. ##STR1## by an intramolecular ringclosure reaction of compounds of formula 2. ##STR2## wherein Z is an aldehyde function or acetal function, or is a functional group which can be converted into such a function during the ringclosure reaction.The eudistomin derivatives within the group of compounds having formula 1 have strong antiviral and antitumour activity.

Abstract: Disclosed is a process for producing a staurosporine derivative represented by Formula (I): Q is defined as in specification: ##STR1## The staurosporine derivative (I-1) possesses selective protein kinase C-inhibitory and cell growth-inhibiting activities, and platelet-increasing activity.

Abstract: Chromogenic lactam compounds of the formula ##STR1## in which the ring A is an aromatic or heteroaromatic radical which has 6 ring atoms and may contain a fused aromatic ring, it being possible for both the ring A and the fused ring to be substituted;the ring B is an unsubstituted or substituted benzene ring;Z is ##STR2## R is hydrogen; unsubstituted or substituted C.sub.1 -C.sub.12 alkyl, cycloalkyl having 5 to 10 carbon atoms; unsubstituted or substituted aryl or aralkyl; C.sub.1 -C.sub.12 acyl; N-(lower alkyl)carbamoyl; or N-arylcarbamoyl which is unsubstituted or substituted on the ring;Q is C.sub.1 -C.sub.12 alkylene, aryl-C.sub.1 -C.sub.4 alkylene, 1,2-cycloalkylene, 1,2- or 1,8-arylene or aralkylene; andX.sub.1 and X.sub.2, independently of one another, are each hydrogen; unsubstituted or substituted alkyl having a maximum of 12 carbon atoms; acyl having 1 to 8 carbon atoms; cycloalkyl having 5 to 10 carbon atoms; or unsubstituted or ring-substituted aralkyl or aryl; or (X.sub.1 and X.sub.

Abstract: The imidazo[1,2-b]pyridazine compounds of the formula: ##STR1## wherein R.sub.1 is a hydrogen or halogen atom, or a lower alkyl group optionally having substituent(s), R.sub.2 and R.sub.3 are, independently, a hydrogen atom, a lower alkyl group optionally having substituent(s), a cycloalkyl group or a phenyl group optionally having substituent(s) or R.sub.2 and R.sub.3 together with the adjacent nitrogen atom to which they bond may form a heterocyclic ring optionally having substituent(s), X is an oxygen atom or S(O).sub.n (n=0 to 2), Alk is a straight or branched chain alkylene group containing 1-10 carbon atoms and optionally having substituent(s), or their pharmaceutically acceptable salts which possess antiallergic, anti-inflammatory and anti-PAF activities, and their production and use.

Abstract: The invention relates to a method of preparing N-oxo-tetrahydro-.beta.-carbolines having formula 1. ##STR1## wherein R.sub.1 is lower alkyl or alkoxy, halogen, trifluoromethyl, lower alkylthio, hydroxy, amino, lower mono- or dialkyl- or acylamino.n has the value 0, 1 or 2,R.sub.2 is hydrogen, lower alkyl or acyl,R.sub.3 is hydrogen, lower alkyl or alkoxycarbonyl, or a phenyl group optionally substituted with a group R.sub.

Abstract: The present invention provides a sulfur-containing heterocyclic compound of the formula (I) ##STR1## wherein ring A is a benzene ring which may be substituted; R is a hydrogen atom or a hydrocarbon group which may be substituted; B is a carboxyl group which may be esterified or amidated; X is --CH(OH)-- or --CO--; k is 0 or 1; and k' is 0, 1 or 2 or a pharmaceutically acceptable salt thereof.Also, it provides a process for producing the compound (I) or a salt thereof and a pharmaceutical preparation for use in the treatment of osteoporosis comprising the compound (I) or salt thereof.The compounds (I) and salts thereof show excellent bone resorption inhibitory activity.

Abstract: Disclosed are the compounds of formula I ##STR1## wherein R.sub.1 -R.sub.3 represent hy drogen or lower alkyl; m represents the integer 2 or 3; n represents the integer 1 or 2; Het represents a pyrrole or imidazole ring bonded at any two adjacent positions and optionally substituted by one or two of lower alkyl; and pharmaceutically acceptable salts of compounds of formula I wherein Het represents optionally substituted imidazole; their methods of preparation; pharmaceutical compositions thereof, and their use for treating cognitive disorders in mammals.

Abstract: The invention provides lactam derivatives of the general formula (I) ##STR1## wherein n represents 2 or 3; Im represents an imidazolyl group of the formula: ##STR2## wherein one of the groups represented by R.sup.1, R.sup.2 and R.sup.3 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl- group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; Y represents a group --(CH.sub.2).sub.m --, wherein m represents 2, 3 or 4; or Y represents a group --X(CH.sub.2).sub.p --, wherein p represents 2 or 3, X represents an oxygen or a sulphur atom or a group NR.sup.4, where R.sup.4 is a C.sub.1-6 alkyl group, and X is attached to the benzene ring moiety of the molecule; and physiologically acceptable salts and solvates thereof.The compounds of formula (I) are potent and selective antagonists of 5-hydroxytryptamine at 5-HT.sub.

Abstract: The invention relates to new 1,7-annelated esters and amides of indolecarboxylic acids having general formula 2, ##STR1## wherein the symbols have the meanings given in the specification. The compounds and their salts are very strong and selective antagonists of "neuronal" 5-hydroxytryptamine (5-HT) receptors, and can be used for the treatment of symptoms which are caused by over-stimulation of these receptors.

Abstract: Tetracyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, X, Y, Z and n are as hereinafter described, and salts thereof, prepared starting from corresponding tricyclic compounds, are described. The compounds I and some of the said tricyclic compounds have antibacterial activity, and are therefore useful as antibacterial agents.

Abstract: The invention concerns novel phenoxyacetic acid amide derivatives of the formula I (and pharmaceutically acceptable salts thereof) in which R.sup.1 is hydrogen or fluoro, R.sup.2 is phenyl, cycloalkyl, alkyl or alkenyl as defined herein, and R.sup.3 is hydrogen, methyl or ethyl, or R.sup.2 and R.sup.3 together form polymethylene as defined herein. The invention also includes pharmaceutical compositions containing the amide derivatives, means for the manufacture of the said derivatives and for their use in the treatment of obesity and related conditions and/or in the manufacture of novel medicaments.

Abstract: Fungicidal substituted 2-phenyl-2,2-difluoroethylthiolcarbonates of the formula ##STR1## in which R.sup.1 represents hydrogen, alkoxycarbonyl, alkoxyalkoxycarbonyl, alkylthioalkoxycarbonyl, halogenoalkoxycarbonyl, cyanoalkoxycarbonyl, alkenoxycarbonyl, alkynoxycarbonyl and cycloalkyloxycarbonyl, or represents cycloalkylalkoxycarbonyl,R.sup.2 represents hydrogen or alkyl, or represents phenyl, orR.sup.1 and R.sup.2 together represent the butadiene-1,4-diyl radical,R.sup.3 represents alkoxy, alkoxyalkoxy, alkylthioalkoxy, fluoroalkoxy, cyanoalkoxy, alkenoxy, alkynoxy, cycloalkyloxy and cycloalkylalkoxy, or represents the group ##STR2## in which R.sup.4 represents alkyl, alkoxyalkyl, alkylthioalkyl, cyanoalkyl, fluoroalkyl, alkenyl, alkinyl or cycloalkyl,R.sup.5 represents hydrogen, alkyl, alkoxyalkyl, alkylthioalkyl, fluoroalkyl, cyanoalkyl, alkenyl, alkinyl or cycloalkyl, orR.sup.4 and R.sup.

Abstract: Tetracyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, X, Y, Z and n are as herein described, and salts thereof, are described. The compounds of formula III have antibacterial activity, and are therefore useful as antibacterial agents.

Abstract: A process for the preparation of a 1,8-bridged 4-quinolone-3-carboxylic acid of the formula ##STR1## wherein the substituents are defined hereinbelow. Some of the compound are new. The old and new compounds are antibacterials and promote animal growth.

Abstract: The novel 2-amino-alkenylsulfonylureas of the formula (I) ##STR1## in which R.sub.1 and R.sub.2 denote hydrogen, alkyl, cycloalkyl or (substituted) phenyl, or R.sub.1 and R.sub.2, together with the common nitrogen atom, form a 5-membered to 7-membered (hetero)aliphatic ring, R.sub.3 denotes hydrogen, cycloalkyl, alkyl, alk(en)(yn)yloxy, alkylsulfen(in)(on)yl, --SO.sub.2 (N)(mono- or di-alkyl), (substituted) phenyl, benzyl, substituted hydroxycarbonyl or (substituted) aminocarbonyl, R.sub.4 has the meaning of R.sub.3 and additionally denote formyl, alkanoyl, (substituted) benzoyl, cycloalkylcarbonyl or C.sub.6 H.sub.5 --CH.sub.2 --O--CO--, or R.sub.3 and R.sub.4, together with the olefinic carbon atoms connecting them, form a 5-membered to 8-membered aliphatic ring system, R.sub.5 denotes H, alkyl, alkenyl, alkynyl, alkoxy or alkoxycarbonyl and R.sub.

Abstract: Antibacterially active new 1,8-bridged 4-quinolone-3-carboxylic acid derivatives of the formula ##STR1## in which Y is carboxyl or a derivative thereofR.sup.1, R.sup.2, R.sup.3, R.sup.4, X.sup.1, X.sup.2 and X.sup.5 are H or various radicals,Z is O, NH, substituted NH, --CON< or --SO.sub.2 N<,m and n are 0 or 1, andA, B, D and E are CH or substituted C or up to three of them are N,and physiologically acceptable salts thereof. Novel intermediates are described as well as processes for making the intermediates and end products.

Abstract: This invention relates to compounds of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 independently represent hydrogen or a substituent selected from lower alkyl, lower alkoxy, halogen, alkanoyl of 2 to 7 carbon atoms, lower alkoxycarbonyl, halolower alkyl, hydroxy, cyano, amino, mono- or diloweralkyl amino, C.sub.2 -C.sub.7 alkanoylamino, carboxy, carboxylower alkyl, hydroxyloweralkyl, carbamoyl, carbamoyloxy, lower alkyl- or aryl-carbonyl, (lower alkoxy)-lower alkoxy, phenyl or a phenyl group itself optionally substituted by a substituent as hereinbefore defined excepting phenyl, or an adjacent pair of R.sup.1-4 together with the carbon atoms to which they are attached complete a six membered unsaturated carbocyclic or nitrogen containing heterocyclic ring, optionally substituted by one or more of the substituents listed above for R.sup.1 ; m represents 0 or 1; and R.sup.5, R.sup.6, R.sup.7 and R.sup.

Abstract: A compound of the formula ##STR1## R.sub.1 is hydrogen, alkali metal, alkaline earth metal, lower alkyl, pivaloyloxymethyl or phthalidyl;R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are the same or different and are hydrogen, halogen, lower alkoxy or ##STR2## wherein R.sub.6 and R.sub.7 are lower alkyl or R.sub.6 and R.sub.7 together with the nitrogen atom to which they are attached form a five- to seven-membered unsubstituted or substituted heterocyclic ring containing said nitrogen atom as the sole hetero atom or containing nitrogen, sulfur or oxygen as additional hetereo atoms;A is a saturated or unsaturated hydrocarbon chain of one to five carbon atoms, unsubstituted or substituted by lower alkyl; lower alkoxy; lower alkylthio; hydroxy; halogen; lower alkyl substituted by halogen, amino, loweralkoxycarbonyl, carboxy, lower-alkoxy, loweralkylthio, loweracyloxy or hydroxy; loweralkylamino; carboxy; nitro; cyano; carbonyl; imino; or by substituted or unsubstituted phenyl, phenylthio, phenylamino or phenoxy; andR.

Abstract: Novel compounds of the formula IIIa ##STR1## wherein R.sup.1a, R.sup.2a, R.sup.3a and R.sup.4a are the same or different and are hydrogen, an alkyl, alkoxy optionally completely or predominantly substituted by fluorine or chlorine, halogen, --CN, --CF.sub.3, --NO.sub.2, --COR, --COOR, aryl, aryloxy or arylalkoxy group, or adjacent groups R.sup.1a, R.sup.2a, R.sup.3a and R.sup.4a together with the adjacent carbon atoms in the benzimidazole ring form a 5-, 6- or 7-membered monocyclic ring or a 9-, 10- or 11-membered bicyclic ring, which rings may be saturated or unsaturated and may contain 0-3 heteroatoms selected from N and O and which rings may be optionally substituted with 1-4 substitutents selected from alkyl groups with 1-3 carbon atoms, halogen perferably F or Cl, alkylene radicals containing 4-5 carbon atoms giving spiro compounds, or two or four of these substituents together form one or two oxy groups ##STR2## whereby if R.sup.1a, R.sup.2a, R.sup.3a and R.sup.

Abstract: The subject invention concerns novel and useful antiviral compounds referred to as eudistomins. These compounds are obtainable from well-known and available marine organisms. Their utility is as antiviral agents as well as antibacterial and antitumor agents in some cases.