Abstract: A complex of branched beta cyclodextrin and steroid is formed by mixing a steroid and a branched beta cyclodextrin together in water for a period of about 4 to 24 hours under ambient conditions. The solubility of the steroid is increased about 95 times by employing the complex.

Abstract: Alkyl glycosides and alkyl oligoglycosides of low iodine color number can be preparedby acid-catalyzed condensation of saccharides in an aqueous solution with short-chain alcohols at elevated temperature in a counter-current reaction column.

Abstract: Administration of adenine nucleotides to a host is followed by their rapid degradation to adenosine and inorganic phosphate which promote increases in liver ATP pools. The turnover of expanded liver ATP pools supply the adenosine precursor for the subsequent expansions of red blood cell (total blood) and blood plasma (extracellular) ATP pools. Thus, the administration of AMP, ATP or their degradation products adenosine and inorganic phosphate to a host, achieve the beneficial increases in liver, total blood and blood plasma ATP levels.

Abstract: The A21 receptor extracelluar site and the A2 receptor extracellular site of adenosine analogues are structurally different and that binding orientations of adenosine or adenosine analogues are different at these sites and this may be used to determine their structure. Novel pyrimidine compounds are described.

Abstract: The present invention relates to an efficient new route for the preparation of (+)-nojirimycin and (+)-1-deoxynojirimycin which involves the stereoselective reductive amination of 1,2-O-isopropylidene-5-oxo-.alpha.-D-glucuronolactone. The reductive amination uses particular oximes of the 5-oxo compound.

Abstract: The present invention provides pradimicin analogs which exhibit improved water solubility relative to parent compounds. These novel agents are useful in treatment of fungal infections.

Abstract: Phosphoric acid derivatives represented by formula (I): ##STR1## wherein X is a halogen and R is --(CH.sub.2).sub.n CH.sub.3 (n=0 to 3), or salts thereof are stable to non-enzymatic hydrolysis and are capable of specifically reacting with acid phosphatase. Therefore, the activity of acid phosphatase in the sample can be determined extremely accurately by reacting said compound with a sample containing acid phosphatase and quantitatively determining the reaction product by colorimetry.

Abstract: Chemically and sterically pure synthetic amphiphilic glycoconjugates for neurological use of the formula (I): ##STR1## in which: the saccharide ring represents a monosaccharide such as glucose, galactose or mannose;X represents O or NH and, when X represents O, R is a choline radical whereas, when X represents NH, R is an amino acid or peptide radical; R' represents a saturated or unsaturated linear or branched C.sub.8 -C.sub.18 aliphatic chain, or a ##STR2## group where m is between 7 and 17 and; n is a whole number from 1 to 5.

Abstract: A composition for testing periodontal diseases which diagnoses or prognosticates contraction or progress of the diseases or diagnoses the therapeutic value by promptly determining peptidase-like enzymatic activity in a specimen. The composition is a combination of a compound of the formula [1] or [2] or a mixture thereof, a chromogen and an oxidase:X-T-Pro-Y [1]orX'-Z'-Arg-Y' [2]wherein Pro is proline residue; Arg is arginine residue; X and X' are hydrogen or an amino protecting group, respectively; Y and Y' are a residue of a compound which can increase oxidation reaction rate of a chromogen with a oxidase in the presence of oxygen and is attached to the C-terminal of Pro or Arg, respectively; and T and Z' are an amino acid or peptide residue composed of 0 to 4 amino acids or their protected derivatives the C-terminal of which is attached to the N-terminal of Pro or Arg, respectively.

Abstract: Novel oligonucleotide analogs are provided having improved cellular uptake, improved resistance to nucleases, and good hybridization to target RNA. Such analogs are provided having substantially non-chiral, non-ionic linking functionalities between the sugars and sugar analogs thereof. In accordance with preferred embodiments, the 4' position of a sugar or sugar analog at one nucleoside is linked to the 3' position of a second sugar or sugar analog of a second nucleoside by a linking function that comprises a two- or three- carbon backbone chain. In accordance with preferred embodiments, the linking functions comprise the formula)--R.sub.1 --O where R.sub.1 comprises a two or three carbon backbone. Such linking functions also, preferably comprise ether functionalities to effect such linkage. Processes for the automated synthesis of oligonucleotide analogs are also provided.

Abstract: Depolymerization of stabilized solutions of highly polymerized and nicked polydeoxyribonucleotides, as obtained through stabilizing aggregation of raw nucleic acids, the depolymerization being carried out by heating at controlled temperature and being controlled as a function of the variation of the reversible hyperchromicity, followed by the removal of the hydrogen bonds in the double stranded filaments and by thermal stabilization of the single stranded filaments, polydeoxyribonucleotide is obtained. The polydeoxyribonucleotide has the following formula of random sequence:P.sub.1-5, (dAp).sub.12-24, (dGp).sub.10-20, (dTp).sub.13-26, (dCp).sub.10-20,whereinP=phosphoric radicaldAp=deoxyadenylic monomerdGp=deoxyguanylic monomerdTp=deoxythymidylic monomerdCp=deoxycytidylic monomerand has well defined chemico-physical properties, reproducible in industrial production.

Abstract: Compounds are disclosed for treating AIDS, herpes, and other viral infections by means of lipid derivatives of antiviral agents. The compounds consist of nucleoside analogues having antiviral activity which are linked, commonly through a phosphate group at the 5' position of the pentose residue, to one of a selected group of lipids. The lipophilic nature of these compounds provide advantages over the use of the nucleoside analogue alone. It also makes it possible to incorporate them into the lamellar structure of liposomes, either alone or combined with similar molecules. In the form of liposomes, these antiviral agents are preferentially taken up by macrophages and monocytes, cells which have been found to harbor the target HIV virus. Additional site specificity may be incorporated into the liposomes with the addition of ligands, such as monoclonal antibodies or other peptides or proteins which bind to viral proteins.

Abstract: The present invention provides a process for preparing lactone intermediates to 2',2'-difluoronucleosides whereby reversion back to the lactone's open chain precursor is minimized and the desired erythro enantiomer can be selectively isolated from an enantiomeric mixture of erythro and threo lactones in crystalline form. Also provided is a process for producing 2'-deoxy-2',2'-difluoronucleosides in about a 1:1 .alpha./.beta. anomeric ratio, and processes for selectively isolating .beta.-2'-deoxy-2',2'-difluorocytidine, or an organic or inorganic acid addition salt thereof, from the 1:1 .alpha./.beta. mixture.

Abstract: The present invention relates to a novel process for the elimination of steroid compounds contained in a substance of biological origin by complexing the steroidal compounds by means of a cyclodextrin, in an aqueous medium, under agitation at a temperature between 20.degree. and 80.degree. C. and then separating the complexes so formed.

Abstract: cDNA encoding a human .alpha..sub.2 -plasmin inhibitor precursor protein represented by an amino acid sequence from the -39th Met to the 452nd Lys in FIG. 1 of the accompanying drawings; an amino acid sequence of a human .alpha..sub.2 -plasmin inhibitor precursor represented by an amino acid sequence from the -39th Met to the 452nd Lys in FIG. 1 of the accompanying drawings; and genomic DNA encoding a human .alpha..sub.2 -plasmin inhibitor protein which is composed of exons II, III, IV, V, VI, VII, VIII, IX and X in FIG. 4 of the accompanying drawings, said exons being bonded to one another via introns.

Abstract: The present invention relates to a pharmaceutical composition for treating a heart disease which comprises a therapeutically effective amount of diadenosine 5',5'"-P.sup.1, P.sup.4 -tetraphosphate as an active ingredient in admixture with a pharmaceutically acceptable carrier or diluent. The pharmaceutical composition is particularly characterized by having antiarrhythmic and coronary vasodilative activities. The present invention also relates to a method for treating a subject having a heart disease or particularly arrhythmia, which comprises administering to the subject an effective amount of the pharmaceutical composition.

Abstract: A compound of the following formula (I) exhibits an excellent antitumor activity ##STR1## wherein R.sub.1 and R.sub.2 represent hydrogen atom, respectively, or include both straight or branch chain alkylidene group of 1-10 carbon atoms; R.sub.3 represents hydrogen atoms, straight and branch chain alkyl group of 1-10 carbon atoms, straight or branch chain alkyloxycarbonyl group of 1-10 carbon atoms or 3-membered to 6-membered heterocycle containing one nitrogen atom with adjacent alkylene group such as pyrrolidine and N-butoxycarbonyl-pyrrolidine; R.sub.4 and R.sub.5 represent hydrogen atom or alkyl group of 1-5 carbon atoms, respectively; and n represents 0 or an integer of 1-10, or pharmaceutically acceptable salt thereof.

Abstract: The saccharides of formula I, ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 independently are optionally substituted acyl, are novel. They possess interesting pharmacological, especially immunostimulant, antiinflammatory and antitumor properties. They may be obtained by deprotection of a corresponding compound in protected form.

Abstract: The present invention relates to the derivatives of the formula ##STR1## and the corresponding enantiomers and diastereoisomers and, if appropriate, their addition salts, and to their use in therapeutics, especially in the central nervous system as analgesics, anticonvulsants, antiepileptics, anxiolytics, antidepressants and neuroprotectors, and in the cardiovascular system as antiarrhythmics, antihypertensives and platelet aggregation inhibitors.