Abstract: The invention relates to nitrosourea derivatives, a process for their preparation and pharmaceutical compositions containing them.The nitrosourea derivatives of the invention correspond to the following formula (I): ##STR1## in which: R can represent a hydrogen atom or an alkyl group from 1 to 30 carbon atoms, X represents a hydroxy group or an --NR.sub.1 R.sub.2 group, Y represents a hydrogen atom, a hydroxy group or an --NR'.sub.1 R'.sub.2 group, where R.sub.1 and/or R'.sub.1 each represent a hydrogen atom or a ##STR2## group, Hal being a halogen, and R.sub.2 and/or R'.sub.2 can each represent a hydrogen atom or an alkyl group comprising from 1 to 6 carbon atoms, R' and R" can represent hydrogen or OH, provided that at least X represents ##STR3## with R.sub.1 representing ##STR4## or Y represents ##STR5## with R'.sub.1 representing ##STR6## and provided that either R' represents hydrogen or R" represents hydrogen, and R' and R" cannot be simultaneously hydrogen atoms.

Abstract: A second-step virus binding receptor is found in nature on the surface of animal and plant cells. This receptor is thought to be needed for virus penetration into target cells. The second-step receptor has been found to bind a wide variety of viruses belonging to a number of different families. The second-step receptor and natural or synthetic substances which correspond to or are analogous to the binding epitope of the second-step receptor in that they are able to bind to a site on the virus which recognizes the binding epitope of the natural second-step receptor, are therefore indicated for the diagnosis, prophylaxis or treatment of viral infections.

Abstract: A natural polymer material PF-102 and salts thereof are widely available as a convenient flocculant for fine suspended matters. PF-102 can be produced by, for example, an imperfect fungus Paecilomyces I-1 (FERM BP-1180).

Abstract: Short chained ligosaccharides of high structural homogeneity constituted essentially by hexasaccharides of the formula: ##STR1## in which R represents a hydrogen atom or the --SO.sub.3.sup.31 group. These hexasaccharides have a highly selective activity on certain steps in blood coagulation and are useful as anti-thrombotic medicaments.

Abstract: 3,3'-Neotrehalosadiamine antibiotic is prepared by fermentation of B. pumilus K169-B91 (ATCC No. 53206) in a nutrient medium preferably comprising soybean meal, corn starch, calcium carbonate and magnesium sulfate. The antibiotic and pharmaceutically acceptable salts and hydrates thereof and compositions containing these are useful to treat bacterial infections in mammals.

Abstract: A double sulfate salt of 1-desoxy-(5-hydroxytryptamino)-D-fructose (DSF) and 1-methylhydantoin-2-imide (creatinine) represents a new solid crystalline phase of unit composition, pharmaceutical quality and remarkable stability.It is prepared by glycosylation of serotonin with D-glucose, formation of the double salt by addition of sulfuric acid and creatinine and crystallization of the double salt in the presence of ethanol.The DFS is preferably isolated from the reaction medium by way of the addition complex DFS.Ca(OH).sub.2 which is precipitated by the addition of calcium hydroxide. The calcium hydroxide is then eliminated by addition of sulfuric acid and the double salt is crystallized as described above.DFS is the active principle of a medicament effective, in particular, in the treatment of leprosy.

Abstract: [1,2,4]triazolo[1,5-c]quinazoline compounds of the formula ##STR1## wherein R.sub.1 is optionally substituted phenyl, pyridyl, furyl thienyl, dihydro or tetrahydro furanyl or thienyl, pyranyl, or 0-ribofuranosyl; R.sub.2 is hydrogen or lower alkyl; X is oxygen or NR.sub.3, R.sub.3 is as defined in the claims, and ring A is unsubstituted or substituted as set forth in the claims. The compounds wherein X is N--R.sub.3 are especially useful as adenosine antagonists and for the treatment of asthma. The compounds wherein X is oxygen are useful as benzodiazepine antagonists and as intermediates in the synthesis of the compounds wherein X is N--R.sub.3.

Abstract: Platinum complexes and Di- or Tricarboxylic acids which is then reacted with the appropriate di- or tricarboxylic acid in aqueous medium.

Abstract: An ellipticine derivative having the structure: ##STR1## as well as process for the preparation of such ellipticine derivatives. The ellipticine derivatives have antineoplastic or antitumor activity.

Abstract: Compounds of the formula: ##STR1## wherein R.sub.1, R.sub.3 and R.sub.4 each independently represents a hydrogen atom or a protecting group;R.sub.2 represents a halogen atom or a group of formula --NR.sub.a R.sub.b (where R.sub.a and R.sub.b, which may be the same or different, each represents a hydrogen atom or an alkyl group; or R.sub.a and R.sub.b may be linked to form, together with the nitrogen atom to which they are attached, a heterocyclic ring which optionally contains a further heteroatom);and their physiological equivalents as well as salts thereof with acids, exhibit antiviral activity against RNA viruses such as Influenza and/or are intermeidates for the preparation of antivirally active compounds.

Abstract: New compounds of the general formula I ##STR1## in which R.sup.1 and R.sup.2 each denote a hydrogen atom or an acyl or benzyl protective group,R.sup.1 and R.sup.2 together denote an alkylidene or benzylidene protective group,R.sup.4 denotes a hydrogen atom, an acyl or benzyl protective group or a 2,3,4-tri-O-benzyl-.alpha.-L-fucopyranosyl or .alpha.-L-fucopyranosyl radical,R.sup.5 denotes H, OH, NH.sub.2, NHNH.sub.2, N.sub.3, O-alkyl, O-aryl, NH--(CH.sub.2).sub.m NH.sub.2, where m=2-5, lysine, polylysine or a carrier,n denotes a number from 1 to 10 andR.sup.3 denotes a hydrogen atom, an acyl or benzyl protective group or an .alpha.-D-glycopyranosyl radical of the general formula II ##STR2## in which R.sup.6 denotes a hydrogen atom or an acyl or benzyl protective group,R.sup.7 denotes a hydrogen atom or halogen andR.sup.

Abstract: A biologically active compound can be solubilized by reaction in different sequences to form a derivative carrying the active moiety, a linking group such as an optionally substituted diisocyanate radical, a polyether moiety such as a polyoxyethylene radical, and a terminal group such as a butyl radical, e.g. ##STR1## n=1 to 400. The active materials can be agricultural chemicals, pharmaceuticals, and the like.

Abstract: The compound 2-.beta.-D-ribofuranosylthiazole-4-carboxamide is used to treat malignant tumors in warm blooded animals. Esters of this compound such as 2-(2,3,5-tri-O-acetyl-.beta.-D-ribofuranosyl)thiazole-4-carboxamide and 2-(5-O-phosphoryl-.beta.-D-ribofuranosyl)thiazole-4-carboxamide are also useful for treating tumors in warm blooded animals.

Abstract: Disclosed herein are tolrestat and oxotolrestat amides and methods of preparation. The amides are new aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.

Abstract: Disclosed herein are tolrestat amides and methods of preparation. The amides are new aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.

Abstract: New compounds, 2',3'-dideoxy-2'-fluorokanamycin A and 1-N-(.alpha.-hydroxy-.omega.-aminoalkanoyl) derivatives thereof, particularly 1-N-(DL- or L-3-amino-2-hydroxypropionyl)- and 1-N-(L-4-amino-2-hydroxybutyryl)-2',3'-dideoxy-2'-fluorokanamycins A are now provided, which are each useful as antibacterial agent. 2',3'-Dideoxy-2'-fluorokanamycin A is prepared by a process comprising condensing a 6-azido-4-O-protected-2,3,6-trideoxy-2-fluoro-.alpha.-D-ribo-hexopyranosyl bromide with the 4-hydroxyl group of a 6-O-(2',4',6'-tri-O-protected-3'-N-protected-3'-amino-3'-deoxy-.alpha.-D-g lucopyranosyl)-1,3-bis-N-protected-2-deoxystreptamine, reducing the resulting condensation product to convert its azido group into an amino group, and removing the remaining amino-protecting and hydroxyl-protecting groups from the reduction product.

Abstract: 1-Azidoaldoses are obtained by reacting 1-fluoroaldoses with metal azides in polar, water-miscible, preferably water-containing, solvents. The hydroxyl groups do not react at the same time, so that they need not be protected or can be present in a derivatized form.

Abstract: A novel compound, 3-(.beta.-D-ribofranosyl)pyrazolo-[3,4-e] [1,3]oxazine-5,7-dione, exhibiting a function of inhibiting propagation or growth of various virus, and a process for preparing the same.

Abstract: It is disclosed that L-fructose can be produced in high yield from L-sorbose. The process involves the inversion of the hydroxyl groups on carbon atoms C3 and C4 of L-sorbose to produce L-fructose. This inversion can be accomplished in simple, commercial equipment with the aid of common reagents. L-sorbose or an appropriately blocked derivative thereof is reacted so as to introduce or create a good leaving group, preferably mesyl or tosyl, at chiral carbon C3 thereby displacing the hydroxyl previously at that position. The leaving group is then displaced, preferably under alkaline conditions, in such a way that the hydroxyl oxygen atom at chiral carbon C4 attaches to chiral carbon C3, thereby displacing the leaving group while forming a 3,4-oxirane (epoxide) ring. The 3,4-oxirane ring forms in a downward position relative to the Haworth presentation thereby inverting chiral carbon C3 during formation of the 3,4-oxirane ring.

Abstract: A chemical process for preparing 2-.beta.-D-ribofuranosylselenazole-4-carboxamide, comprises reacting 2,3,5-tri-O-benzoyl-.beta.-D-ribofuranosyl-1-carbonitrile with gaseous hydrogen selenide in a polar organic solvent.

Abstract: Aminodeoxy derivatives of 3-deoxy-D-manno-2-octulosonic acid (KDO) are potent inhibitors of bacterial enzymes and a novel class of antibacterial agents.

Abstract: Derivatives of 3-deoxy-D-manno-2-octulosonic acid (KDO) are potent inhibitors of bacterial enzymes and a novel class of antibacterial agents.

Abstract: A class of novel 2-.beta.-D-ribofuranosylselenazole-4-carboxamide nucleoside and nucleotide compounds and methods for their production are provided. Compounds of the class typically have pharmacological properties, especially antitumor and antiviral properties, and are well tolerated, being useful, for example, in treating tumors and viral infections in warm blooded animals.

Abstract: A class of novel 2-.beta.-D-ribofuranosylselenazole-4-carboxamide nucleoside and nucleotide compounds and methods for their production are provided. Compounds of the class typically have pharmacological properties, especially antitumor and antiviral properties, and are well tolerated, being useful, for example, in treating tumors and viral infections in warm blooded animals.

Abstract: Platinum complexes of polyhydroxylated alkylamines and 2-polyhydroxylated alkyl-1,2-diaminoethanes useful for inducing regression and/or palliation of cancer diseases in mammals.

Abstract: Beta-glycosyl C-nucleoside compounds showing growth inhibitory activity against leukemic cells, of the following formula, are provided: ##STR1## wherein X is NR.sub.10, S or OR.sub.10 is H or alkyl with 1 to 6 carbon atoms. ##STR2## wherein R.sub.6, R.sub.7 and R.sub.8 are independently selected from H or alkyl of 1 to 6 carbon atoms; or ##STR3## wherein R.sub.16, R.sub.11 and R.sub.12 are independently selected from H or alkyl of 1-6 carbon atoms;R.sub.3 is OH, SR.sub.13, or OR.sub.9 ;R.sub.4 is OH, SR.sub.14, or OR.sub.15 ;R.sub.9, R.sub.13, R.sub.14 and R.sub.15 are individually selected from C.sub.1 -C.sub.6 alkyl and C.sub.1 to C.sub.6 acyl;R.sub.5 is OH or H,R'.sub.5 is OH or H with the provison that at least one of R.sub.5 or R'.sub.5 is H; excluding 2-deazoxoformycin; andHCl salts thereof.

Abstract: The invention disclosed herein relates to novel 1-deoxyglycosides, preferably 1-deoxy-D-mannopyranosides and 1-deoxy-L-rhamnopyranosides, having in the 1-position of the pyranose ring an aralkylthio/aralkenylthio, aralkyloxy/aralkenyloxy or aralkanoylamino/aralkenoylamino substituent; and to novel processes for preparing these 1-substituted-1-deoxyglycosides starting with the corresponding tetra-O-acetylglycopyranosyl bromide or amine. The 6-hydroxy group of 1-substituted-1 deoxyglycopyranosides can also be replaced by other functional groups. These aralkylthio/aralkenylthio, aralkyloxy/aralkenyloxy and aralkanoylamino/aralkenoylamino 1-deoxyglycosides are potent inhibitors of antigen-specific T-cell proliferation and are also useful as inhibitors of delayed-type hypersensitivity reactions.

Abstract: A class of novel 2-.beta.-D-ribofuranosylselenazole-4-carboxamide nucleoside and nucleotide compounds and methods for their production are provided. Compounds of the class typically have pharmacological properties, especially antitumor and antiviral properties, and are well tolerated, being useful, for example, in treating tumors and viral infections in warm blooded animals.

Abstract: An improved method is disclosed for producing amino polyols useful in preparing polyurethane foams. The improvement concerns charging ammonia, a primary amine or a secondary amine to the reaction vessel at the end of the oxide digestion step. The amine or ammonia scavenges the residual oxide and the resulting alkanol amine becomes one of the components of the polyol mixture. Alkanol amines are beneficial components of urethane polyols.In prior art industrial practice, residual oxide is vented to a scrubber system and then stripped to a low concentration.

Abstract: Disclosed is a chiral, total synthesis of thienamycin from D-glucose which proceeds via intermediates I, II, III and IV to known lactone V which is known to be useful via acid VI in the total synthesis of thienamycin (VII): ##STR1## wherein R.sup.1 is hydrogen or a removable protecting group; R is a removable protecting group.

Abstract: The invention relates to novel aminoacridine-.alpha.,.beta.-(D)- and -(L)-N-glycoside derivatives, the salts thereof and to a novel process for the preparation of such compounds and salts. The novel compounds have the formula I ##STR1## wherein R is hydrogen or a group of the formula II ##STR2## wherein n=0 or 1, p=1 or 2, A.sup.-p is an anion, preferably halogenide, R.sup.1 is hydrogen or a methyl group andR.sup.2 is hydrogen or a sugar residue, or R is dimethylamine,and the two substituentsX and X.sup.1 are identical or different and stand for hydrogen, a group of the formula II, dimethylamine, halogen, a C.sub.1-4 alkyl group, a C.sub.1-4 alkoxy group, for a nitro-, cyano-, carbomethoxy-, carbamoyl-, phenyl- or a C.sub.1-4 alkylphenyl group,with the restriction that at least one of the substituents R, X and X.sup.1 represents a group of formula II with R.sup.2 =sugar residue, andR.sup.3 is hydrogen or a C.sub.1-5 alkyl group.

Abstract: 2-.beta.-D-Ribofuranosylthiazole-4-carboxamidine (I) and salts are provided as well as a means for their production and use. The compounds typically show unique pharmacological activity, especially antienzyme and cytotoxic activity.

Abstract: The text describes compounds having the formula I ##STR1## wherein R.sup.1 denotes a hydrogen atom or an acyl or benzyl protective group, R.sup.1 and R.sup.2 together denote an alkylidene or benzylidene protective group, R.sup.2 and R.sup.3 denote hydrogen atoms or acyl or benzyl protective groups or a .beta.-galactopyranosyl radical or a 2,3,4,6-tetra-0-acetylated derivative thereof, R.sup.4 denotes an azido, amino or acetamido group, R.sup.5 denotes --0--alkyl, --0--aryl, --0--benzyl, --NHNH.sub.2, --N.sub.3 or --OH and n denotes 1 to 10, and also a process for their preparation and their use as antigens or immunoadsorbents.

Abstract: The invention relates, inter alia, to a process for the provision of 6-amino-6-desoxy-2,3-O-isopropylidene-.alpha.-L-sorbofuranose derivatives which comprises treating a 2,3-O-isopropylidene-6-sulphonated-.alpha.-L-sorbofuranase with an amine in an aqueous medium in an autoclave, followed by reaction of the reactions product in a basic medium to provide the free amine of Formula I as described hereinafter. The invention also includes the products obtained by the reaction and the invention further includes the process for providing the compounds of Formula VII as described hereinafter by treatment of a compound of Formula I as described hereinafter with an acid, followed by hydrogenation. The products of the invention are useful as medicaments or intermediates for medicaments.

Abstract: Chiral Schiff bases according to the general formula: ##STR1## and chiral transition metal complexes thereof, wherein at least the carbon atom of the monosaccharide to which the iminyl nitrogen atom is attached is asymmetric, and at least one of the carbon atoms adjacent the aforesaid carbon atom bears a hydroxyl group, R.sup.1 and R.sup.6 which may be the same or different, are hydrogen or lower alkyl, R.sup.2 is hydrogen, or lower alkyl or together with R.sup.10 forms a divalent hydrocarbon group, R.sup.3 is hydrogen, a sugar residue, or --CH.sub.2 OR.sup.10 in which R.sup.10 is hydrogen, lower alkyl or together with R.sup.2 forms a divalent hydrocarbon group, R.sup.4 is hydrogen or --CH.sub.2 OR.sup.10 in which R.sup.10 is hydrogen, or a lower alkyl, R.sup.5 is hydrogen, OR.sup.1 or a sugar residue, provided that both R.sup.4 and R.sup.5 are not hydrogen, R.sup.7 and R.sup.8 which may be the same or different, are hydrogen, or lower alkyl, or where p is 1, may with the cyclic ring to which CR.sup.7 R.sup.

Abstract: Dextransucrase synthesis of dextran from sucrose is inhibited by substituted sucrose compounds which have an inhibiting group bonded to the 5-position ring carbon. Oral compositions containing such substituted sucrose compounds can be used to control dextran formation in the mouth, and dextran comprises the principal component of dental plaque.

Abstract: The invention relates to new compositions to be used as cosmetics. The new cosmetics according to the invention contain as active agent 0.06 to 10% by weight of a reaction product of nicotinic acid, a nicotinic acid salt or a nicotinic acid halide and a polyhydroxy compound of the general formula (I), ##STR1## wherein n is an integer of 1 to 15 and R.sub.1 and R.sub.2 each stand for hydrogen, or R.sub.2 represents hydrogen and R.sub.1 is an alkyl group, or R.sub.1 is hydroxyalkyl and R.sub.2 is an alkyl group, orwhen n is equal to 1, R.sub.1 and R.sub.2 may also form together a group of the general formula --(CHOH).sub.m --, wherein m is an integer of 1 to 4, or a group of the general formula --(CHOH).sub.q --CHNH.sub.2 --(CHOH).sub.p --, wherein Q is an integer of 0 to 2 and p is an integer of 1 to 3, or R.sub.1 may represent a group of the general formula --(CHOH).sub.m --H, wherein m is an integer of 1 to 4, and at the same time R.sub.2 stands for hydrogen.

Abstract: The present invention provides a novel compound cyanoethylpullulan which is a cyanoethylation product of pullulan. Pullulan is readily cyanoethylated by the reaction with acrylonitrile in the presence of an alkali catalyst such as sodium hydroxide.The cyanoethylpullulan having a degree of cyanoethylation of at least 50% has various unique properties in the heat resistance, solubility in organic solvents, film-forming property, adhesive bonding to metals and the like in comparison with related cyanoethylated products such as cyanoethylcellulose and cyanoethylated polyvinyl alcohol.

Abstract: Novel arabinofuranosyl nucleosides and nucleotides having 2'-azido,2'-amino, or 2'-hydrocarbylamino substituents, which have antitumor, antiviral, and antimicrobial properties, are prepared by condensation of a pyrimidine, purine, or 1,3-oxazine base with an acylated 2-azido-2-deoxyarabinofuranosyl halide, followed by deblocking and catalytic hydrogenation, where appropriate, to convert the 2'-azido group to a 2'-amino group and, if desired, alkylation or the like to convert the 2'-amino group to a 2'-hydrocarbylamino group.

Abstract: This invention relates to a poly-ion complex comprising chitin or N-acylchitosan derivative having carboxymethyl and polyelectrolyte.

Abstract: Methyl-D-ribofuranoside is p-nitrobenzoylated to yield crystalline methyl 2,3,5-tri-O-(p-nitrobenzoyl)-.beta.-D-ribofuranoside which can be used to prepare a stable, crystalline 2,3,5-tri-O-(p-nitrobenzoyl)-.beta.-D-ribofuranosyl bromide which in turn is useful as a precursor of natural or synthetic purine and pyrimidine nucleosides, as well as of glycosides. This bromide can also be cyanated to yield crystalline 2,5-anhydro-3,4,6-tri-O-(p-nitrobenzoyl)-D-allononitrile which in turn can be hydrolyzed and subsequently reacted with polyamino pyrimidines to yield nucleoside analogs such as 8-.beta.-D-ribofuranosyl adenine. This bromide also can by hydrolyzed to yield crystalline 2,3,5-tri-O-(p-nitrobenzoyl)-D-ribofuranose which in turn can be p-nitrobenzolated to yield crystalline 1,2,3,5-tetra-O-(p-nitrobenzoyl)-.beta.-D-ribofuranose. This latter compound can be brominated to produce an alphabromide derivative which is useful as a precursor of nucleosides.

Abstract: The present invention relates to new nitroso-urea derivatives, particularly to N.sub.1 -glucofuranosid-6-yl-N.sub.3 -nitroso-ureas, of the general formula I ##STR1## wherein anyone of R.sub.1, R.sub.2, R.sub.3 and R.sub.5 represent hydrogen, optionally substituted alkyl, aralkyl or acyl, or R.sub.1 and R.sub.2 together or R.sub.3 and R.sub.5 together also represent alkylidene or cycloalkylidene, and R.sub.6 represents optionally substituted alkyl; and to processes for producing them.

Abstract: Controlled release pesticides are prepared by reacting an isocyanate derivative of a pesticide with a polymer having pendant groups containing a reactive hydrogen to obtain a novel pesticide-polymer system in which the pesticide is chemically bonded to the polymer. Active pesticidal material is released from the pesticide-polymer system by hydrolysis or chemical depolymerization under conditions of use.

Abstract: Pesticide polymers comprising a polymer with a macromolecular backbone and pendant groups having pesticidal groups chemically linked thereto are prepared by reacting a pesticide having a replaceable hydrogen with a multifunctional isocyanate to form a pesticide-isocyanate adduct and then reacting the adduct with the polymer substrate in a mutual solvent to form the pesticide polymers. The chemical linkages connecting the pesticide-adduct to the pendant groups are cleaved under environmental conditions of use to controllably release an effective amount of the active pesticide.

Abstract: Compounds of the formula ##STR1## are useful antihypertensive agents.

Abstract: Novel 2,2', 2"-[s-phenenyltris(sulfonylimino)]tris-[2-deoxy-.alpha.-D-glucopyranose], dodecakis (H-sulfate) compounds and their salts which are useful as inhibitors of the complement system of warm-blooded animals, and the compound 2,2',2"-[s-phenenyltris(sulfonylimino)]tris[2-deoxy-D-glucopyranose] which is a new intermediate for the preparation of the active dodecakis (H-sulfate) compounds.

Abstract: 2,2',2"-[s-Phenenyltris(carbonylimino)]tris-2-deoxy-D-glucopyranose and salts thereof, useful as complement inhibitors.

Abstract: The present invention relates to a novel substance, viz. the N-methyl-d-glucosamine complex of 4-methyluracil of the formula: ##SPC1##A process for producing same, and use thereof.The method for producing said substance consists in reacting 4-methyluracil with an equimolar amount of N-methyl-d-glucosamine in an aqueous medium at a temperature of from 20.degree. to 50.degree. C, followed by isolation of the desired product from the solution.The N-methyl-d-glucosamine complex of 4-methyluracil possesses a pharmacological activity and is useful in medicine as a medicated compound which is a cell-growth biostimulator increasing unspecific immunity and accelerating reparative regeneration of macroorganism tissues. The medicated compound has a high activity, sufficiently wide range of therapeutical applications, and a low toxicity.Said complex may be also useful as a growth stimulator for baking, nutrient, and other yeast.

Abstract: A red colorant having the general formula ##SPC1##In whichR represents an aliphatic radical, andR' represents the radical of a compound of the formula H.sub.2 N--R', which compound is an amino sugar, a polymer of an amino sugar, a polyamino acid or an amino alcohol.