Abstract: Novel magnetic resonance imaging agents comprise complexes of paramagnetic ions with aminoalkylamide derivatives of diethylenetriaminepentaacetic acid ("DTPA") or ethylenediaminetetraacetic acid ("EDTA") or other polyaminocarboxylic or cyclic polyaminocarboxylic chelating agents. 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: An improved process is described for obtaining triazacyclononanes, esepcially 1,4,7-trimethyl-1,4,7-triazacyclononame. The first step involves reacting diethylenetriamine (DET) with a sulfonylation agent to form a sulfonamidated DET, in an aqueous medium with an inorganic base. In a second step, but preferably within the same reactor vessel without isolating intermediates, the sulfonamidated DET aqueous mixture is contacted with an aprotic organic solvent in the presence of a cyclizing unit such as ethylene glycol ditosylate or ethylene dibromide, thereby resulting in a cyclized sulfonamidated triamine compound. Thereafter the protecting groups are removed and the amine is alkylated, preferably within a single reaction vessel without isolation of intermediates.

Abstract: There are disclosed polychelant compounds, that is multi-site metal chelating agents, and chelates formed therewith. The polychelants and especially their paramagnetic metal, heavy metal or radioactive metal polychelates are particularly suitable for use in diagnostic imaging, heavy metal detoxification or radiotherapy. The polychelants have a linear or branched oligomeric structure comprising alternating chelant and linker moieties bound together by amide or ester moieties the carbonyl groups whereof being adjacent the chelant moieties, each polychelant comprising at least two said chelant moieties capable of complexing a metal ion.

Abstract: A drug is described which includes a physico-chemical complex between molecules of a phospholipid and an aminoketone derivative of fluoroglucinol which is useful, particularly when administered topically in the form of a liposomal aqueous microdispersion, for increasing the microcirculatory flow-rate and volume in the capillaries to the skin, both in normal conditions and in peripheral vasculopathy (primary or secondary Raynaud's disease), acrocyanosis and blocked arteries caused by arteriosclerosis, diabetes or endoangioitis obliterans.

Abstract: A fluorescent compound, which is readily capable of forming a stable complex with a rare-earth metal ion having fluorescence with satisfactory intensity even in an aqueous system and long fluorescence lifetime when formed a complex with the rare-earth metal ion, a complex of the fluorescent compound and the rare-earth metal ion, and a labelled reagent made therefrom, together with a specific binding assay using said labelling agent.A fluorescent compound expressed by the following formula A, typically exemplified by 2,15-diaza[3,3](2,9)-1,10-phenanthrolinophane-N.sup.2,N.sup.15 -diacetic acid.

Abstract: Quinoline derivatives of the formula: ##STR1## , wherein R is hydrogen, alkyl or aralkyl; m and n are 0 or 1, and each of rings A, B and C can have substituents, which are useful as inhibitors for acyl-CoA:Cholesterolacyltransferase.

Abstract: The present invention is directed toward a process for extracting compounds from plant material, comprisinga) contacting hydrolyzed plant material with a supercritical fluid and optionally with a co-solvent and p1 b) recovering the compound from the supercritical fluid.In another embodiment, the present invention is directed toward a process for removing a compound from plant material, comprising contacting the plant material with an acid, a supercritical fluid and a co-solvent, and recovering the compound from the supercritical fluid. The sterols, diosgenin and sarsapogenin, are efficiently extracted from barbasco root and Yucca seed, respectively.

Abstract: Compounds which are amino acid derivatives and have the formula ##STR1## in which R.sup.1 is hydrogen or methyl, R.sup.2 is ethyl, propyl or imidazol-4-yl, R.sup.3 is isobutyl, cyclohexylmethyl or benzyl, and A is defined as herein are useful as renin inhibitors.

Abstract: Amine salts of alkane-1,n-dicarboxylic acid mono-(2-sulfatoethyl)amides of the Formula IHOC(O)--(CH.sub.2).sub.n --C(O)--N(R.sub.1)--CH.sub.2 CH.sub.2 SO.sub.3.sup.--+ HN(R.sub.2).sub.3 Iwherein R.sub.1 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.8 alkyl and phenyl, R.sub.2 is C.sub.1 -C.sub.8 alkyl or (R.sub.2).sub.3 when taken together with the nitrogen atom is pyridinyl; and n is an integer from 4 to 20, their preparation and use to prepare water-soluble esters of corticosteroids.

Abstract: The invention relates to new benzazole derivatives of the formula I ##STR1## wherein X is oxygen or sulphur, R.sub.1 is lower alkyl, lower alkenyl or cycloalkyl, R.sub.2 and R.sub.3 independently of one another are each hydrogen, lower alkyl or cycloalkyl radicals or taken together are a substituted or unsubstituted bivalent hydrocarbon residue of aliphatic character in which the carbon atoms of the chain may be interrupted by a heteroatom, R.sub.4 is either a group ##STR2## wherein R.sub.5 and R.sub.6 independently of one another are lower alkyl or cycloalkyl radicals, optionally substituted, or taken together R.sub.5 and R.sub.6 are a substituted or unsubstituted bivalent hydrocarbon residue of aliphatic character in which the carbon atoms of the chain may be interrupted by a heteroatom, or, R.sub.4 is a group ##STR3## where R.sub.7 is a lower alkyl group, and their salts and N-oxides. The products are useful as anthelmintic effective agents. The products can be prepared to methods known per se.

Abstract: Processes for the preparation of biotinylated polynucleotides and analogues thereof and protected intermediate products for use in such processes are described and claimed. The processes may be conveniently used in the automated synthesis of biotinylated polynucleotide on a DNA synthesizer. The polynucleotides so prepared may be used as labelled probes e.g. as diagnostic tools for clinical and research uses.

Abstract: Novel benzoheterocyclic compounds of the formula: ##STR1## wherein R.sup.1 is H, halogen, OH, etc,; R.sup.2 is H, alkyl, halogen or alkoxy; R.sup.3 is phenyl-alkanoylamino, or ##STR2## R.sup.4 is H, --NR.sup.6 R.sup.7, alkenyloxy, HO-alkyl, --O--CO--A--NR.sup.8 R.sup.9, etc.; R.sup.5 is H, OH, etc., or a salt thereof, which have excellent vasopressin antagonistic activities and useful as vasodilator, hypotensive agent, water diuretics, platelet agglutination inhibitor, and a vasopressin antagonistic composition containing the compound as the active ingredient.

Abstract: A storage stable porfimer sodium (polyhematoporphyrin ether/ester) composition useful in the photodynamic therapy of cancer and other conditions is provided. The composition is characterized in that the percentage of ester linked porphyrin oligomers is less than 10% of the composition. Improved processes for preparing such compositions are also provided wherein acetylated hematoporphyrin is treated with alkali for sufficient time and temperature to reduce the amount of porphyrin oligomers joined by ester linkages to less than 10% of the composition.

Abstract: New 11.beta.-phenyl-14.beta.H-steroids of general formula (I), where Z is an oxygen atom or the hydroxyimino-grouping N.about.OH, and M and N are either jointly a second compound or L is a hydrogen atom and M is an .alpha.-permanent hydroxy group and either A and B together are a second compound and D is a hydrogen atom, where R.sup.1 is a five or six-part heteroalkyl residue or a cycloalkyl, cycloalkenyl or aryl residue or A is a hydrogen atom and B and D together are a methylene bridge, where R.sup.1 besides the aforementioned residues may be a possibly substituted hydrocarbon residue with up to 10 C atoms, a possibly substituted amino group, a hydroxy or C.sub.1-8 alkoxy, mercapto or thioalkyl group, R.sup.2 is a methyl or ethyl residue, and R.sup.3 /R.sup.4 represents the usual combination of substituents on the C17 atom in steroid chemistry, having antigestagenic and other properties.

Abstract: A chelated compound of the formula: ##STR1## where R.sub.1 is independently at each occurrence, ##STR2## R.sub.2 is independently at each occurrence hydrogen, lower alkyl, lower alkyl ester, lower alkyl ether, hydroxy or halogen; A is H, Li, Na, Ca+, Mg+or Zn+; and Mn is trivalent manganese; provided that, at least two and no more than three R.sub.1 radicals are ##STR3## The compound of the invention is particularly suitable for use in a physiologically compatible composition comprising a physiologically compatible liquid carrier for magnetic resonance imaging. The compound is also suitable as a chelate for removal of manganese from a system.The invention also comprises a method for enhanced magnetic imaging of a mammal organism which comprises introducing the composition at a level of from 20 to 200 mg/Kg of body weight into the circulatory system of the organism; and making a magnetic resonance image of at least a portion of said organism at from 30 minutes to 36 hours after said introduction.

Abstract: A process for preparing compounds of the formula ##STR1## which comprises reacting an imidazolide of the formula ##STR2## with an amine of the formula NHR.sub.4 R.sub.5 in the presence of a Grignard reagent to form a compound of formula I or reacting an imidazolide of formula II with a compound of the formula R.sub.6 Mgx to form a compound of formula I.

Abstract: Invented are 4-aza-5-alpha-8(14)-17 substituted-androsten-3-ones having an 8(14), 7(8), or 16(17) double bond, optionally also having a 1(2) double bond, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-alpha-reductase.

Abstract: This invention provides a method for treating the symptoms of obesity which comprises administering to a human or other mammal suffering from the symptoms of obesity an effective amount of a compound selected from the group consisting of the optically active compounds especially the (-) negative stereoisomers represented by the formula: ##STR1## wherein R.sub.1 R.sub.2,R.sub.3,R.sub.4,R.sub.5 and R.sub.6 are defined by the specification substituted or unsubstituted phenyls, pyridyl, hydroxyphenyl, ##STR2## X is oxygen or sulfur, Y is selected from the group consisting of hydroxy, nitro, cyano, azido, amino, acylamino, carboxyamido, trifluoromethyl, sulfate, sulfonamido, halogen, hydrocarbyl and hetero atom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus and said hydrocarbyl radicals comprise from 1 to 12 carbon atoms, and a is an integer of from zero to 3,R.sub.2, R.sub.3 and R.sub.

Abstract: The present invention relates to a number of innovative electrophilic substitution reactions involving 2,5-dithienylpyrrole (2,5-DTP). More specifically, these reactions are used in the synthesis of monomers for preparing functionalized conducting organic polymers.The electrophilic substitution reactions in this invention are accomplished under conditions not requiring the use of N-1 pyrrole blocking groups to direction reaction at the pyrrole C-3 position. This is because the steric bulk of the 2,5-dithienyl groups prevent N-acylation and therefore direct reactions with electrophiles at the pyrrole C-3 position.The reaction conditions chosen have also demonstrated a greater regioselectively towards functionalization at the pyrrole 3-position than the basic reaction conditions suggested in the prior art. This result may be explained by an activation of the pyrrole 3-position towards electrophilic substitution. This is attributed to an electron donating resonance contribution of the 2,5 thienyl groups.