Abstract: The present invention provides novel lipophilic drug derivatives which are capable of being formulated in liposomes or micelles. These drug derivatives are known therapeutic agents which are covalently attached to a fatty acid chain of a phospholipid, glyceride, ceramide or 1,2-diacyloxypropane-3-amine. The linkage between the therapeutic agent and the lipid is one which can be cleaved in vivo, allowing the therapeutic agent to be separated from the micellar or liposomal formulation.

Abstract: The present invention relates to a water-soluble conjugate having antithrombin-binding activity comprising a substantially straight-chained organic polymer backbone having at least 30 molecules of sulfated glycosaminoglycans distributed along the polymer backbone, wherein the sulfated glycosaminoglycans are attached to the polymer backbone at a single point of attachment which is not responsible for the antithrombin-binding activity. The present invention also relates to a surface having antithrombin-binding properties prepared with the conjugate and methods of preparing said conjugate and said surface.

Abstract: Selectin receptor binding is modulated by a method which utilizes heparin-like oligosaccharides.

Abstract: N-acyl-N,N'-di-lysogangliosides, N'-acyl-N,N'-di-lysogangliosides and N,N'-diacyl-N,N'-di-lysogangliosides, wherein the acyl groups are derived from an aliphatic acid having from 1 to 24 carbon atoms, substituted by one or more polar groups are disclosed. The acyl-di-lysogangliosides of the invention exhibit an inhibiting action on protein kinase C activation and, thus, can be utilized in therapies for various pathologies of the nervous system. Pharmaceutical compositions and therapeutic utilities for the lysoganglioside derivatives are also disclosed.

Abstract: The process of the invention relates to a process for the preparation of a ganglioside mixture, free from contaminants associated with non-conventional, life-threatening viruses, without altering the biological and pharmacological characteristics of the mixture on the central and peripheral nervous systems.

Abstract: The present invention is concerned with novel sulfuric acid esters of sugar alcohols and sugar alcohol-like compounds of the formula ##STR1## Also described are methods for the treatment and/or prophylaxis of arteriosclerotic changes in the vascular wall as well as a process for the manufacture of the compounds of formula I and their salts.

Abstract: A method for the topical treatment of herpes virus infections of the skin and mucous membranes is disclosed- This method uses a topical preparation comprising an anti-vital drug in combination with a potentiating drug which is an anti-inflammatory or an anti-oxidant drug. A preferred preparation includes zinc pentosan polysulphate in combination with bufexamac.

Abstract: A method for treating and/or inhibiting gastric and duodenal ulcers, comprising administering a pharmaceutical composition comprising an oligosaccharide of Formula I(NeuAc-.alpha.(2-3)-Gal-.beta.(1)-(--X--).sub.m -(--Y--).sub.n -).sub.p -ZwhereinX=a chemical bond or a group capable of linking the galactose to either the linking group Y or the multivalent support Z;wherein the C.sub.1 glycosidic oxygen of galactose may be replaced by N, S or C;Y=a linking group;Z=a multivalent support;m=0 or 1;n=0 or 1; andp=an integer of 2-1,000 is described. Also described is a method for treating and/or inhibiting gastric and duodenal ulcers, comprising administering a pharmaceutical composition comprising an oligosaccharide of Formula IINeuAc-.alpha.(2-3)-Gal-.beta.(1)-AwhereinA=a group capable of bonding to the galactose;wherein the C.sub.1 glycosidic oxygen of galactose may be replaced by N, S or C.

Abstract: The invention relates to 3-deoxy oligosaccharides of formula I: ##STR1## in which X represents an --OSO.sub.3.sup.- radical, a radical of formula R--O, a radical of formula: ##STR2## or a radical of formula: ##STR3## Y represents a radical of formula: ##STR4## R represents an alkyl radical, R.sub.1, R.sub.3, R.sub.5, R.sub.7, R.sub.8, R.sub.10, R.sub.12 and R.sub.13 represent a hydroxyl radical, an alkoxy radical or an --OSO.sub.3.sup.- radical,R.sub.2, R.sub.4, R.sub.6, R.sub.9 and R.sub.11 represent a hydrogen atom, a hydroxyl radical, an alkoxy radical or an --OSO.sub.3.sup.- radical, with the proviso that at least R.sub.2 or R.sub.4 or R.sub.6 or R.sub.9 or R.sub.11 represents a hydrogen atom,and their pharmaceutically acceptable salts with a base.

Abstract: A composition for removing or inactivating harmful components including virus from blood or other extracellular liquids comprises a crown ether compound substituted on a polysaccharide, preferably dextran. The composition may be soluble in water, preferably for intraveneous application, or insoluble for extracorporeal application.

Abstract: A method for obtaining oligosaccharides starts with allylation of position (3') of .beta.-lactosides followed by controlled benzylation, which leads to perbenzylated and partially benzylated compounds. The latter are glycosylated at position 3, not benzylated, with a donor of .varies.-fucopyranosyl to yield protected trisaccharides. These and perbenzylated .beta.-Lactosides are deallylated and, later, are glycosylated with 2-azido-2-deoxy-.varies.-D-galactopyranosyl to yield protected tetrasaccharides and trisaccharides, respectively. The debenzylation of said products accompanied by the reduction of the azido group and simultaneous acetylation of the amino group produces intermediary products which, by O-deacetylation, leads respectively to the final tetrasaccharides and trisaccharides.

Abstract: Novel NeuAc-Gal dissacharide sialidase substrates and inhibitors which are locked into rigid conformation by the attachment of an alkyl group at the C-6 arm of the galactose core are provided. Also provided is a method for the inhibition of sialidase activity.

Abstract: Novel compounds which are chemically linked inhibitors of the proteases Elastase and Cathepsin G prevent connective tissue degradation associated with neutrophil induced inflammatory disease.

Abstract: Stable parenteral antitumor formulations contain elsamitrucin salt, a stabilizer and a buffer. The formations are optionally stored in sealed containers under air or nitrogen headspace.

Abstract: A method is disclosed of preparing amidated water soluble cellulose acetates by amidating water soluble cellulose acetate. Methods are also provided for preparing aminated water soluble cellulose acetates of varying plasticities, film- and fiber-forming characteristics, and other properties by methanolysis of naturally-occurring chitin or by amination of water soluble cellulose acetate.

Abstract: A dermatological pharmaceutical composition for stimulating hair growth and for the treatment of conditions of the skin selected from the group consisting of(a) benign moles, papillomas and seborrheic keratoses;(b) unsightly freckles, pimples and blemishes;(c) stasis dermatitis;(d) dermal ulcers; and(e) fungal nail infections; and(f) gingival and mucous membrane inflammations;the composition comprising an effective amount of tannic acid, a debriding agent and a pharmaceutically acceptable carrier therefore.

Abstract: Disclosed is a method for producing a surface-crosslinked, modified polysaccharide having improved absorption properties. The method involves forming a mixture of water and a crosslinking agent, adding a generally water-soluble, modified polysaccharide to said mixture wherein the surface of the polysaccharide becomes crosslinked, and drying the modified polysaccharide. Also described is a surface-crosslinked, modified polysaccharide having improved absorption properties.

Abstract: The object of the present invention is to provide a new SLe-type sugar chain derivative represented by the following formula (I), which is useful as a pharmaceutical and which contains moranoline: ##STR1## wherein R.sub.1 represents hydrogen, a lower alkyl, a lower alkenyl or a lower alkynyl; R.sup.2 and R.sup.3 differ from each other and represent a galactosyl, sialylgalactosyl or fucosyl group; R.sub.4 represents a hydroxyl group or an acetamido group. The present invention comprises a sugar chain derivative containing a moranoline, and having a new structure. Possessing cell adhesion inhibitory activity, the compounds of the present invention antagonizes selectin, serving well in the treatment of inflammation, inflammation-associated thrombosis, asthma and rheumatism, and in the prevention and treatment of immunological diseases and cancer.

Abstract: Fermentation product A83543, comprising major components A83543A and A83543D and minor components A83543B, A83543C, A83543E, A983543F, A83543G, A83543H and A83543J, is produced by a newly described species, Saccharopolyspora spinosa. The A83543 components and their acid-addition salts (A83543 compounds) are useful as insecticides, particularly against Lepidoptera and Diptera species. Insecticidal, miticidal or ecto-parasiticidal combinations, compositions and methods are provided.

Abstract: A process and product formulated by complexing d,1- or 1-p-boronophenylalanine (BPA) with a saccharide in an aqueous solution formation of the complex being facilitated by raising the pH of this solution to a higher pH of about 10 or lowering the pH of the solution to a lower pH of about 2 and then readjusting the pH to a body physiological pH of about 7.4. This BPA saccharide complex can then be delivered by i.v. or other injection or administered orally as a key component of the BNCT cancer treatment process. The pH manipulation causes a much higher solubility of BPA and thus a higher boron concentration in the tumor, thereby improving the therapy.