Abstract: The invention relates to sulphated K5 antigen and sulphated K5 antigen fragments containing at least 3 monosaccharide units and salts thereof, having interesting antiangiogenic and antitumor activities and a favorable ratio of the activities with respect to anticoagulant properties. In addition, the compounds can be used for the treatment of diseases caused by envelope viruses.

Abstract: A method and article useful for preparing stable polysaccharide gels from aqueous solutions of water-soluble polysaccharides bearing pendant carboxylate groups. The gels produced may be of the foamed or nonfoamed variety.

Abstract: The invention relates to bisaldonamides, in which the underlying aldonic acids can be linked glycosidically in the 3-, 4- or 6-position with a galactopyranosyl, mannopyransyl, glucopyranosyl or oligopyranosyl radical. They are starting products for the preparation of the corresponding polysulfuric acid esters.

Abstract: Complexes of iron or other metals with sulphonated derivatives of chitosan, having the following general formula (I): ##STR1## in which: R is H or a C.sub.1 -C.sub.5 alkyl group, or an arylalkyl group;A is H or an alkaline metal or an alkaline earth metal;X is a pharmacologically acceptable anion;m is a whole number from 50 to 1000;n is zero or a whole number from 1 to 10;M is Fe.sup.II, Fe.sup.III, Mg, Ca or Bi.

Abstract: According to the process of the invention, a glycosaminoglycan is used in the form of a salt soluble in an organic medium and is subjected to the action of a given sulfation agent.

Abstract: Derivatives of 1,2-O-isopropylidene-.alpha.,D-glucofuranose and intermediates for preparing these derivatives are described. These derivatives are useful for treating animals and mammals with inflammatory and/or autoimmune disorders such as autoimmune deficiency syndrome, psoriasis, atopic dermatitus, rheumatoid arthritis, osteoarthritis, scleroderma and systemic lupus erythematosus.

Abstract: The invention relates to polysulfuric acid esters of bis-aldonamides in which the underlying aldonic acids can be linked glycosidically with a galactopyranosyl, mannopyranosyl, glucopyranosyl or oligopyranosyl radical in the 3-, 4- or 6-position. They are therapeutically active compounds, whose preparation and pharmaceutical compositions are likewise described.

Abstract: Novel derivatives are disclosed as obtained from chondroitin sulfate, dermatan sulfate and hyaluronic acid, having a molar ratio between sulfate groups and carboxylic groups like that of heparin and furthermore characterized by possessing, as the heparin, the sulfoamino group at the carbon atom at the 6 position of hexosamine.The novel compounds show a very remarkable clearing activity in comparison with the starting mucopolysaccharides, this activity being similar and for some derivatives comparable with that of heparin.Moreover, differently from what normally happens upon sulfating the sulfomucopolysaccharides, the anticoagulating activity of the novel compounds is negligible or anyhow very reduced.The compounds of the present invention find use in the therapy of arteriosclerosis.

Abstract: Derivatives of -.alpha.,D-glucofuranose .alpha.,D-allanfuranose and intermediates for preparing these derivatives are described. These derivatives are useful for treating animals and mammals with inflammatory and/or autoimmune disorders such as psoriasis, atopic dermatitus, rheumatoid arthritis, osterarthritis, scleroderma and systemic lupus erythematosus.

Abstract: The present invention relates to sulfated oligosaccharides or their derivatives such as the following compound and being useful for diagnosing or treating diseases such as immunity-related diseases and mucopolysaccharide diseases. ##STR1## (M is an alkali metal).

Abstract: Quaternary ammonium salts of polysaccharides possessing hypochlolesterolemic activity and having the following general formula: ##STR1## in which A represents the monomer unit of a natural polysaccharide, m is a whole number between 100 and 1000, n is a whole number between 0 and 4, B is O or S or NH or NR, R is a linear alkyl radical of 1-4 carbon atoms, and X.sup.(-) is an anion such as Cl.sup.-, Br.sup.-, I.sup.-, HSO.sub.4.sup.-, CH.sub.3 O--SO.sub.3.sup.-.Said salts are prepared by reacting a pretreated natural polysaccharide with a a quaternary ammonium salt functionalized at one of its ends with an epoxy group.

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: Process for the preparation of oligosaccharides by a controlled chemical depolymerization of natural polysaccharides, such as heparins, heparan sulfates, dermatan sulfates, chondroitinsulfates, hyaluronic acid, by a radicalic reaction in an aqueous solution, at a temperature ranging between 20.degree. and 70.degree. C., in the presence of a catalyst selected in the group consisting of Cu++, Fe++, Cr+++, Cr.sub.2 O.sub.7 - as well as the resulting oligosaccharides and their related pharmaceutical compositions. The products exhibit high antithrombotic activity, little or no anticoagulant activity, high fibinolytic activity an antiinflammatory activity.

Abstract: New amines and amides of carboxylated polysaccharides having the nitrogen of the amido and amino groups directly attached to the polysaccharides and method of making same, based on reacting in solution a material having carboxyl-containing polysaccharides, such as carboxymethyl cellulose, with ammonium donors having the general formula >NH such as primary and secondary amine reagents and with or without a reducing agent to obtain amides or amines. These products may be used for instance in biological separations, for the immobilization of proteins, for the removal of metal ions, as thickeners, and as suspension agents.

Abstract: Degradation products, termed pseudaglycones, of LL-E33288, BBM-1675, FR-900405, FR-900406, PD 114759, PD 115028, CL-1577A, CL-1577B, CL-1577D, CL-1577E and CL-1724 antibiotics/antitumor agents are disclosed anad described.

Abstract: Sialic acid derivatives and process for preparing these compounds. In these compounds, a phenylthio group is stereo-selectively incorporated at the 3-position of the sialic acid. These compounds are useful as intermediates for synthesizing various glycosides such as ganglioside, a blood type determining factor, GQ.sub.1b etc. The present invention also relates to sialic acid-containing oligosaccharide derivatives and process for preparing them.

Abstract: This invention relates to glucopyranose compounds of formula (I) and (IA) ##STR1## and the non-toxic salts thereof wherein the substituents are as defined herein. Such materials possess enhancing activity of cellular immunity (e.g. mitogenic activity) to living tissue and therefore are useful as anti-tumor agents.

Abstract: There is disclosed oligosaccharide compounds having heparin-like anticomplement activity and reduced anticoagulant activity as compared with heparin on a weight or molar basis. The oligosaccharide compounds have at least 5 and no greater than 25 saccharide units. The oligosaccharides can have an even nuber of saccharide units with a terminus nonreducing sugar, or an odd number of saccharide units without a terminus nonreducing sugar. There is also disclosed anticomplement pharmaceutical compositions with reduced anticoagulant side effect activity and a process for preparing the oligosaccharide compounds.

Abstract: The present invention provides a process for selective production of a 2-.alpha.-O-glycoside compound of sialic acid which is useful as a starting material or intermediate for medicines and biochemical reagents. The process comprises reacting an alkylthiosialic acid derivative represented by the formula [I]: ##STR1## wherein R represents an acyl group and R.sup.1 and R.sup.2 each represents a lower alkyl group with a compound having alcoholic hydroxyl group at a low temperature in a polar solvent having no hydroxyl group in the presence of a Lewis acid selected from the group consisting of methyl triflate, trimethylsilyl triflate and dimethyl(methylthio)sulfonium triflate. The present invention further provides novel compounds.

Abstract: A sulfated polysaccharide DS4152 useful as an angiogenesis inhibitor or antitumor agent is provided selectively. As the sodium salt, it has the following physicochemical characteristics. Molecular weight by the gel filtration method: 29,000.+-.3,000. Elemental analysis: C: 24.42-25.76%, H: 3.34-3.98%, N: 0.51-0.89%, S: 10.6-11.7% and P: 0.77-1.06%. Sugar and protein contents: Sugar content (%): 57.+-.3 (by phenol sulfuric acid method; standard: galactose). Protein content (%): 1.+-.0.5 (by the Lowry-Folin's method; standard: bovine serum albumin). Specific rotatory power [.alpha.].sub.D.sup.25 : -37.degree..+-.1.degree. (0.5% aq. solution). Characteristic absorption bands in infrared absorption spectrum: 1240, 840 (shoulder), 810 (cm.sup.-1 ; KBr).

Abstract: The salt formed between the polyanions forming the Trichosaccharide and the NH.sub.2 groups of 2,4-diamino-6-piperidino-pyrimidine-3-oxide represents a novel trichogenic factor by which the activity of the single components is enhanced and the seriously toxic side effects of Minoxidil are done away with.

Abstract: This invention relates to novel 3'-demethoxy epipodophyllotoxin glucosides, their use as anti-tumor agents, and pharmaceutical compositions thereof.

Abstract: Thiol gels are prepared from hydroxyl containing polymers by forming a 2-fluoro-1-methylpyridoxy derivative of the polymer followed by reacting the derivative with sodium dimethyldithiocarbamate and reducing to produce a sulfhydryl substituted polymer. Alternatively, the derivative is reacted with dithiothreitol to produce a sulfhydryl substituted polymer having free sulfhydryl groups spaced from the polymer. The thiol gel can be activated by means of 2,2'-dipyridyl disulfide and reacted with a free sulfhydryl containing biologically active ligand in order to provide an insolubilized ligand which can be used for various purposes including use as an immobilized biologically active material or use as a matrix in covalent chromatography.

Abstract: Novel compounds with anti-proliferative and mucosaprotective activity are obtained by sulfating trestatins.

Abstract: A process for preparing dermatan sulphate (DS) of pharmaceutical purity from animal organs rich in mucopolysaccharides (MPS), by: (a) stabilizing the fresh organs by freezing them either as such or in the form of powder, (b) micronizing the material containing the MPS with an aqueous CaCl.sub.2 solution, (c) digesting the homogenate comprising the raw material and the CaCl.sub.2 with proteolytic enzymes at alkaline pH and at low temperature, (d) acidifying, heating and filtering the lysate, (e) treating the filtrate with quaternary ammonium salts able to undergo complexing with and thus precipitate either the DS along or all the MPS selectively, (f) recovering and purifying the DA either directly from the ammonium salt complex containing it or from the complex obtained from the mixture of ammonium salt complexes of all the MPS by fractional solubilization with acetone.

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: There is disclosed a tetrasaccharide, a hexasaccharide, on octasaccharide and a decasaccharide all capable of inhibiting complement activation and having less tha 33% of undigested native heparin's anticoagulation activity.

Abstract: Method of treatment of diseases caused by retroviruses which comprises administering therapeutically effective amount of a natural or synthetic oligo- or polysaccharide having at least one S-oxoacid group attached to the saccharic carbon atom through a linking group of lower molecular weight or a pharmaceutically acceptable salt thereof to a subject in need of such treatment.

Abstract: Compositions and methods useful for identification or diagnostic use, or inhibition of adherence of uropathogenic bacteria to cells, all in connection with uropathogenic bacterial infections, containing as an active constituent the structural element, preferably in terminal position:.alpha.--D--Galp--(1-4)--D--Gal.Process for identification or quantification of such structural element in native biological material from mammals including man, comprising using antibodies, the generation of which has been initiated by such composition. A process for the identification of bacterial acceptor structures (pili, syn. fimbriae) recognizing the described structural element, comprising using this recognition. A process for purifying acceptor structures of bacteria, comprising using for the purification the affinity between such structural element and the corresponding acceptor structures on the bacteria.

Abstract: Pharmaceutical preparations for topical administration containing a pharmacologically active substance together with hyaluronic acid or a molecular weight fraction thereof. The hyaluronic acid may be in the form of the free acid or may be a salt with an alkali or alkaline earth metal, magnesium, aluminum or ammonium, or in the form of a salt with one or more pharmacologically active substances.

Abstract: The adsorbent consists of a solid phase, completely or partially penetrated by or surface-coated with a hydrophilic molecular polymer netting to which has been bound substituents or cross bridges having chain sequences of the structureX--CH.sub.2 --CH.sub.2 --SO.sub.2 --CH.sub.2 --CH.sub.2 --S--Ywhere X is ether oxygen, a thioether sulfur atom or a nitrogen atom and Y is a substituted or unsubstituted alkyl, aryl or heteroaromatic group. The solid phase consists of particles with a diameter of less than 1 mm and the molecular polymer netting consisting of a cross-linked polyhydroxy polymer such as a polysaccharide, preferably a polygalactane such as agar or agarose or a cross-linked polyamide, e.g. polyacryl amide. Y can be hydroxy alkyl or mercapto alkyl, or phenyl alkyl or phenyl substituted with halogen or nitro groups. The adsorbent is prepared by first converting in a known manner a hydrophilic polymer containing OH and/or CONH.sub.

Abstract: Covalently modified bacterial polysaccharides and proteins; covalent conjugates of such polysaccharides linked by a bigeneric spacer, which permits proof of covalency and facilitates purification of conjugated materials, with immunogenic bacterial membrane or other proteins, which conjugates are useful components of bacterial vaccines; and methods of preparing such polysaccharides, proteins and conjugates and of confirming the covalency of the linkage between polysaccharides and proteins.

Abstract: The administration of "active" chondroitin sulfate A (CSA), "active" chondroitin sulfate C (CSC), or mixtures thereof to mammals including humans suffering from cancer, bacterial infections, trauma, irritation, placement of foreign objects, tubes or instruments, or damage of the upper or lower urinary tract, and related transitional cell surfaces to prevent cancer cell implantation or adherence, bacterial infestation or adherence, trauma, irritation, or damage from placement of foreign objects, tubes or instruments in the kidney, renal pelvis, ureter, bladder, urethra and related transitional cell surfaces by the irrigation of said surfaces and/or tubes and instruments with a solution of said drugs or mixtures thereof.

Abstract: Damage to endothelial and epithelial cells subject to trauma can be substantially reduced by using a wafer of a viscoelastic material. This method is particularly useful when applied prior to ophthalic surgery, particularly intraocular lens implantation surgery. Lens implantation is facilitated by the compression of lens haptics by this delivery system.

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: Sulfamates of the following formula (I): ##STR1## wherein X is O or CH.sub.2 and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as herein defined have been found to exhibit anticonvulsant activity and are thus useful in the treatment of conditions such as epilepsy. Further, pharmaceutical compositions containing a compound of formula (I) as well as methods for their use and intermediates form part of the present invention.

Abstract: Metal-containing or metal-free phthalocyanine-polysaccharide complex defined below is used for removal of mutagens and carcinogens present in aqueous solutions, the said complex having formula of ##STR1## wherein Pc is a metal-containing or metal-free phthalocyanine residue, A is an alkylene group having 2 to 6 carbon atoms or an arylene group having 1 to 3 rings, the integers m and n satisfy both 2<m+n.ltoreq.4 and 1.ltoreq.n.ltoreq.2, and Z is an activated polysaccharide residue.

Abstract: A chondroitin or a chondroitin sulfate covalently or ionically bonded to a drug substance of the group consisting of chloramphenicol, methotrexate, adriamycin, vinblastine, vincristine, vindesine, 6-mercaptopurine, 5-fluorouracil, the penicillin antibiotics, the cephalosporin antibiotics, and the 1-oxacephalosporin antibiotics to form a prodrug which, when injected into animal tissue, undergoes natural conversion in the physiological environment to provide controlled release of the drug or an active drug complex.

Abstract: An improved multi-step process for the production of 2-.beta.-D-ribofuranosylthiazole-4-carboxamide.

Abstract: Cell-specific ligands comprising conjugates of saccharides and amino acids or peptides are synthesized from amino acids such as ornithine, lysine, peptides such as dilysine, diornithine or oligolysine and selected saccharides having reactive functional groups protected by appropriate blocking groups. Such glycopeptides are useful as tissue specific substances, which when coupled with bioactive materials through metabolizable or hydrolyzable linkages, deliver such bioactive materials to the selected site. In this manner, antiinflammatory drugs such as dexamethasone are linked through a metabolizable or hydrolyzable linkage and on administration to an animal suffering from inflammatory disease carries the drug to the site of inflammation for intracellular release. Other examples include the macrophage ligand N.sup.2 -N.sup.2, N.sup.6 -Bis-[3-(.alpha.-D-mannopyranosylthio)propionyl]-6-lysyl-N.sup.6 -[3-(.alpha.-D-mannopyranosylthio)propionyl]-L-lysine, 5, which when coupled to .beta.

Abstract: O-.alpha.-D-glucopyranosyl(1.fwdarw.4)-[O-.alpha.-D-glucopyranosyl-(1.fwdar w.4)].sub.n -O-.beta.-D-glucopyranosyl(1.fwdarw.6)-.beta.-D-fructofuranosyl-O-.alpha.- D-galactopyranosyl(1.fwdarw.6)-.alpha.-D-glucopyranoside sulfate salts, useful as inhibitors of the complement system and the process of making such compounds.

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

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: The present invention relates to a chloral derivative having the general formula ##STR1## in which Y' is a polysaccharide consisting of a chain of anhydroglucose, modified anhydroglucose or uronic acid units as substituent group and in which R is selected from --H, --COCH.sub.2 OH, --[(CH.sub.2).sub.n 0].sub..chi. --H in which n is 2 to 5 and .chi. is 1 to 7; --CH.sub.2 OSO.sub.2 X' or --CH.sub.2 COOX' in which X' is NH.sub.4 or a single equivalent of a non-toxic metallic cation, --(CH.sub.2).sub.n H where n is 1 to 7, --(CH.sub.2).sub.n (OH).sub..chi. Y where Y is --H or --CH.sub.3 n is 1 to 7, .chi. is 1 to 12 and the --OH groups are attached to any or all of the carbon atoms by substitution and wherein when Y.sup.1 is a chain of unmodified anhydroglucose units, these units have the following configurations:.alpha.-D-glucopyranosyl units having a predominantly 1-4 linkage.beta.-D-glucopyranosyl units having a predominantly 1-4 linkage and/or.beta.

Abstract: The novel derivatives correspond to the general formula II: ##STR1## in which: R.sub.1 R.sub.2 R.sub.3 and R.sub.4 represent identical or different groups which can each be a hydrogen or halogen atom or an alkyl group, alkoxy, or benzyloxy group and R is the residue of an R--CHO aldehyde selected from among linear or branched saturated aliphatic aldehydes including 1 to 4 carbon atoms or again represents the Z--CH.dbd.CH radical in which Z represents a hydrogen atom, a linear or branched saturated alkyl group, an aromatic nucleus or an aromatic heterocyclic nucleus or again R represents the radical HO CH.sub.2 (CH OH)n--in which n has the value of 3 or 4. The novel compounds have high solubility in water and antibacterial activity and potentiating power.

Abstract: A novel plasminogen activating enzyme-specific competitive inhibitor is disclosed consisting of an amino-terminated .alpha.-N-substituted aminocarboxylic acid, such as .alpha.-N-benzylsulfonyl-p-aminophenylalanine, or the acid derivatives thereof. The competitive inhibitor ligand, when covalently coupled to the surface of a water-insoluble solid support material through a spacer chain of at least 4 carbon atoms, is useful as a biospecific extracting agent for use in affinity chromatography of plasminogen activating enzymes, such as urokinase, cytokinase, and the like, from crude aqueous preparations thereof, such as mammalian urine, mammalian body tissue preparations, mammalian plasma and spent tissue culture growth medium.

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

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: Water-soluble local anaesthetic compounds having sustained effect are prepared by reacting a chondroitin derivative with a basic local anaesthetic compound.