Plural Nitrogens Containing Patents (Class 536/55)
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Patent number: 5550116Abstract: The invention relates to N,O-sulphated heparosans consisting of chains or of a mixture of chains of molecular mass between 1500 and 15,000 Da, characterized by a repeated disaccharide structure of formula I: ##STR1## in which: E represents an acetyl group in 0 to 80% of the disaccharide units of the said N,O-sulphated heparosan, and a sulphate group and possibly a hydrogen atom in the remaining disaccharide units,G represents a hydrogen atom and a sulphate group, and the pharmaceutically acceptable salts of thesaid N,O-sulphated heparosans. The heparosans are useful as anticoagulants.Type: GrantFiled: February 15, 1995Date of Patent: August 27, 1996Assignee: SanofiInventors: Jean Claude Lormeau, Bruno Chevallier, Marc L. V. Salom e, Guy E. M. Tenaille d'Estais
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Patent number: 5541166Abstract: A method of anti-metastatic and/or anti-inflammatory treatment of an animal or human patient comprises administration to the patient of an effective amount of at least one sulphated polysaccharide which blocks or inhibits endoglycosidase, particularly heparanase, activity. Suitable sulphated polysaccharides include heparin and modified heparin, fucoidan, pentosan sulphate, dextran sulphate and carrageenan lambda.Type: GrantFiled: March 16, 1992Date of Patent: July 30, 1996Assignee: The Australian National UniversityInventors: Christopher R. Parish, John M. Snowden
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Patent number: 5525711Abstract: The invention provides novel pteridine nucleotides which are highly fluorescent under physiological conditions and which may be used in the chemical synthesis of fluorescent oligonucleotidcs. The invention further provides for fluorescent oligonucleotides comprising one or more pteridine nucleotides. In addition the invention provides for pteridine nucleotide triphosphates which may be used as the constituent monomers in DNA amplification procedures.Type: GrantFiled: May 18, 1994Date of Patent: June 11, 1996Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: Mary E. Hawkins, Wolfgang Pfleiderer, Michael D. Davis, Frank Balis
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Patent number: 5523294Abstract: 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.Type: GrantFiled: July 12, 1993Date of Patent: June 4, 1996Assignee: FIDIA S.p.A.Inventors: Francesco Della Valle, Aurelio Romeo
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Patent number: 5519008Abstract: Triterpenoid acid derivatives have been found to have structures similar to natural ligands to the extent that these derivatives bind to natural selectin receptors including endothelial leukocyte adhesion molecule-1 (ELAM-1) and leukocyte/endothelial cell adhesion molecule-1 (LECAM-1). The molecules can be administered to the patients by themselves or in pharmaceutical formulations; in order to alleviate inflammation and/or treat other abnormalities associated with the excessive binding of leukocytes to endothelial receptors.Type: GrantFiled: September 10, 1992Date of Patent: May 21, 1996Assignee: Glycomed IncorporatedInventors: Narasinga Rao, Mark B. Anderson, John J. Naleway, John H. Musser
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Patent number: 5516864Abstract: This invention describes novel sensors for ions that are based on the combination of xanthylium-based dyes with metal-binding N,N'-diaryldiaza crown ethers. These sensors are primarily useful for detection and quantitation of alkali-metal ions in aqueous solution. Binding of the ion results in a change in the fluorescence properties of the indicating dye that can be correlated with the ion concentration. Methods are provided for attaching reactive groups on these sensors for conjugation to dyes, lipids and polymers and for enhancing entry of the indicators into living cells.Type: GrantFiled: January 19, 1995Date of Patent: May 14, 1996Assignee: Molecular Probes, Inc.Inventors: Michael A. Kuhn, Richard P. Haugland
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Patent number: 5498604Abstract: 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.Type: GrantFiled: November 17, 1994Date of Patent: March 12, 1996Assignees: Nippon Shinyaku Company, Limited, Akira HasegawaInventors: Akira Hasegawa, Makoto Kiso, Yoshiaki Yoshikuni
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Patent number: 5489675Abstract: 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.Type: GrantFiled: November 3, 1993Date of Patent: February 6, 1996Assignee: E. I. Du Pont de Nemours and CompanyInventor: Subramaniam Sabesan
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Patent number: 5489578Abstract: Sulfated oligosaccharides which bind to L-selectin receptors and act as agonists are formulated into pharmaceutical formulations and administered by injection to treat inflammation. Compounds which act as metabolic inhibitors of carbohydrate sulfation and inhibit the sulfation of naturally occurring ligands for L-selectin receptors are administered locally by injection to alleviate and/or prevent inflammation. The sulfated oligosaccharides can be administered in combination with the chlorates and sulfatases in order to obtain a combined effect which is useful in preventing and/or alleviating inflammation. A preferred group of ligands are obtained by the hydrolysis of GlyCAM-1 by separation procedures including high pH anion exchange chromatography. The invention describes compounds that have the recognition determinants for L-selectin on GlyCAM-1 as Galactose-6-sulfate and/or N-acetylglucosamine-6-sulfate, in concert with sialic acid and fucose.Type: GrantFiled: May 2, 1996Date of Patent: February 6, 1996Assignee: The Regents of the University of CaliforniaInventors: Steven D. Rosen, Stefan Hemmerich
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Patent number: 5474987Abstract: The present invention relates to methods for the prevention and/or treatment of pathological processes involving the induction of TNF-.alpha. secretion comprising a pharmaceutically acceptable carrier and a low molecular weight heparin (LMWH). In the pharmaceutical compositions of the present invention, the LMWH is present in a low effective dose and is administered at intervals of about 5-8 days. Furthermore, the LMWH is capable of inhibiting in vitro TNF-.alpha. secretion by resting T cells and/or macrophages in response to T cell-specific antigens, mitogens, macrophage activators, disrupted extracellular matrix (dECM), laminin, fibronectin, and the like.Type: GrantFiled: February 3, 1995Date of Patent: December 12, 1995Assignee: Yeda Research and Development Co. Ltd.Inventors: Irun R. Cohen, Ofer Lider, Rami Hershkoviz
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Patent number: 5472582Abstract: The present invention provides for the use of the fluorescent label 2-aminoacridone for use in separating carbohydrate mixtures and analyzing the structure of carbohydrates. Carbohydrates for analysis may be labeled by 2-aminoacridone and subsequently separated from one another by electrophoresis. The electrophoresis may be in one or two dimensions. Band produced by the electrophoresis may be visualized and quantitated directly by UV illumination or by means of a charge coupled device for photoelectric detection. 2-aminoacridone labelling of carbohydrate may also be used to analyze the structure of carbohydrates by cleaving (or adding to) various 2-aminoacridone labeled carbohydrates by carbohydrate modifying enzymes of known specificity, and subsequently separating the carbohydrates by electrophoresis in either one or two dimensions. The subject invention also provides for kits for performing 2-aminoacridone labelling and electrophoresis.Type: GrantFiled: July 9, 1993Date of Patent: December 5, 1995Assignee: Astromed LimitedInventor: Peter Jackson
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Patent number: 5470842Abstract: Ligands in the form of N-acetyllactosamines which bind to endothelial leukocyte adhesion molecule-1 (ELAM-1) are disclosed. The ligand compounds can be formulated into pharmaceutical compositions and/or assay compositions used to alleviate inflammation and assay for the presence of (qualitative) and amount of (quantitative) ELAM-1 and thereby determine the presence, location and degree of inflammation.Type: GrantFiled: March 2, 1992Date of Patent: November 28, 1995Assignee: Glycomed, IncorporatedInventors: Brian K. Brandley, Michael Tiemeyer, Stuart J. Swiedler, Margaret Moreland, Hans Schweingruber
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Patent number: 5464942Abstract: This invention relates to compounds prepared by linking glycosaminoglycan to phospholipid or lipid, which are expected to exert a pharmacological effect for inhibiting metastasis because of their excellent function to inhibit adhesion of cancer cells to blood vessel endothelial cells and extracellular matrix. This phospholipid- or lipid-linked glycosaminoglycan can be produced for example by: cleaving and oxidizing reducing terminal group of glycosaminoglycan, and allowing an aldehyde group or a lactone compound of the thus-formed derivative or a carboxyl group in the glycosaminoglycan chain to react with a primary amino group of a phospholipid; or linking a glycosaminoglycan derivative to a phospholipid or a lipid by allowing a primary amino group of the derivative to react with a carboxyl group of the phospholipid or lipid. This phospholipid- or lipid-linked glycosaminoglycan is useful as a metastasis inhibitor because it has no toxicity.Type: GrantFiled: March 24, 1991Date of Patent: November 7, 1995Assignee: Seikagaku Kogyo Kabushiki KaishaInventors: Katsukiyo Sakurai, Nobuo Sugiura, Koji Kimata, Sakaru Suzuki
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Patent number: 5449773Abstract: Bis(platinum) and tris(platinum) complexes derived from 6,6'-diamino-6,6'-dideoxy-1',2-anhydrosucrose and 1',6,6'-triamino-1',6,6'-trideoxy-2,3,3',4,4'-penta-O-methylsucrose are disclosed as possessing anti-tumor activity.Type: GrantFiled: January 24, 1995Date of Patent: September 12, 1995Assignee: Hawaiian Sugar Planters' AssociationInventors: Navzer D. Sachinvala, Hong Chen, Eichii Furusawa
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Patent number: 5446140Abstract: A blend of cellulose acetate and starch acetate used to make fibers, filaments, yarns, fabrics, plastic materials and other uses is disclosed. Additionally, the invention relates to the process of making said blend; cigarette filters made from tow composed of said blend; cigarettes made with filters made from tow of said blend as well as acetate flake and other compositions containing said blend.Type: GrantFiled: January 5, 1995Date of Patent: August 29, 1995Assignee: Hoechst Celanese CorporationInventors: Joanne C. Maheras, John B. Hopkins, Jr., Heribert Tatzlaff
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Patent number: 5403827Abstract: There is provided a process for preparing epoxy-heparide polysaccharides of formula (I): ##STR1## wherein A is a pyran ring with substituents 1 and 4 in the axial position and 5 in the equatorial position, and R and R' are hexosamines which constitute a polysaccharide chain bonded to said ring A by a glucoside, and one of R and R' is H when the ring A is in the terminal position of said polysaccharide chains, and said heparide has a COCH.sub.3 to COOH ratio of 0.5, said process comprisinga) N-desulfation of heparin to obtain the corresponding heparamine;b) acetylation of the heparamine of step (a) to obtain the corresponding heparide;c) epoxidation of the heparide of step (b) by treating the heparide with hydrogen peroxide in an alkaline reaction medium at pH 12-14; andd) cooling the solution obtained in step (c) to a temperature of between 15.degree. and 25.degree. C. and adjusting the pH to between 5.8 and 6.0.Type: GrantFiled: November 2, 1993Date of Patent: April 4, 1995Assignee: Laboratori Derivati Organici S.p.A.Inventor: Luigi De-Ambrosi
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Patent number: 5380832Abstract: Disclosed are ganglioside GM.sub.3 analogs represented by the formula ##STR1## in which X represents a radical of the following formula ##STR2## wherein at least one of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is hydrogen and the remainder is hydroxyl; ##STR3## wherein at least one of R.sub.5 and R.sub.6 is hydrogen and the remainder is methyl; ##STR4## wherein m is an integer of 15 to 25, l is an integer of 0 to 3, n is an integer of 11 to 15 and Ac represents acetyl. The ganglioside GM.sub.3 analogs are expected to possess an inhibitory activity for influenza virus.Type: GrantFiled: May 16, 1994Date of Patent: January 10, 1995Assignees: The Nisshin Oil Mills, Ltd., Akira HasegawaInventors: Akira Hasegawa, Makoto Kiso
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Patent number: 5367062Abstract: Derivatives of disubstituted and deoxydisubstituted .alpha.-D-lyxofuranosides and intermediates for preparing these derivatives are described. These compounds exhibit significant antiinflammatory and anti-proliferative activity and are useful for treating inflammatory and/or autoimmune disorders such as psoriasis, asthma, atopic dermatitis, rheumatoid arthritis, osteoarthritis, scleroderma, systemic lupus erythematosus, and cancer (particularly melanoma and colon cancer).Type: GrantFiled: August 21, 1992Date of Patent: November 22, 1994Assignee: Medicarb Inc.Inventors: Sudershan K. Arora, Peter J. Schied
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Patent number: 5366963Abstract: A method for suppressing immune responses in animals by administering a mixture of gangliosides to the animal where the gangliosides have heterogeneous ceramide structures containing fatty acid portions with carbon chain lengths of 21-30 or less than 18 carbon atoms. Ganglioside mixtures which are homogeneous with respect to the fatty acid portion are also effective immunosuppressive agents when the carbon chain length of the fatty acid portion is less than 18. Compositions containing the above specified ganglioside mixtures are also disclosed.Type: GrantFiled: February 23, 1993Date of Patent: November 22, 1994Assignee: The Regents of the University of CaliforniaInventor: Stephan Ladisch
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Patent number: 5350841Abstract: Novel ganglioside derivatives comprised of a basic natural or semisynthetic ganglioside, in which the carboxyl group in the sialic part of the natural or semisynthetic ganglioside is converted into a carboxylamide with an aliphatic amino acid with a carboxylic or sulfonic acid function, and salts thereof are prepared. The semisynthetic ganglioside components can be chosen from the group consisting of N-acyl-N-lyso-gangliosides, N'-acyl-N'-lyso-gangliosides and N,N'-diacyl-N,N'-di-lyso-gangliosides, wherein "acyl" designates a moiety of an optionally substituted aliphatic acid. The ganglioside derivatives can be used in pharmaceutical preparations to be used in nervous system pathologies.Type: GrantFiled: July 31, 1992Date of Patent: September 27, 1994Assignee: Fidia S.p.A.Inventors: Aurelio Romeo, Gino Toffano, Alberta Leon
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Patent number: 5349089Abstract: Cationic polysaccharide derivatives are prepared by reacting a polysaccharide with a polycationic reagent having one polysaccharide reactive group and at least two cationic groups. Suitable reagents include polycationic alkyl, aryl, alkaryl, cycloaliphatic, or heterocyclic amines, some of which are novel compositions. The polycationic polysaccharide derivatives prepared from these reagents are useful in the manufacture of paper.Type: GrantFiled: January 11, 1993Date of Patent: September 20, 1994Assignee: National Starch and Chemical Investment Holding CorporationInventors: Peter T. Trzasko, Michael T. Philbin
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Patent number: 5326752Abstract: The compounds are of the formula ##STR1## wherein each R.sup.1 is independently H or lower alkyl (1-4C); R.sup.2 is H, lower alkyl (1-4C), alkylaryl or one or more additional saccharide residues; R.sup.3 and R.sup.4 are independently H, alkyl (1-6C), aryl or R.sup.3 and R.sup.4, taken together, form a five or six-membered ring optionally containing a hetroatom selected from the group consisting of O, S, and NR.sup.1 ; wherein said five- or six-membered ring may further be substituted by one or more substituents selected from the group consisting of (CHOR.sup.1).sup.m H wherein m is 1-4, OR.sup.1, OOCR.sub.1, NR.sup.1, NCOR.sup.1 and SR.sup.1 ; Y is H, OR.sup.1, OOCR.sup.1, NR.sup.1.sub.2, NCOR.sub.1 or SR.sub.1 ; and X is --CHR.sup.5 (CHOR.sup.1).sub.2 CHR.sup.6 OR.sup.1 wherein R.sup.5 and R.sup.6 are independently H, lower alkyl (1-4C) optionally substituted with one or more R, or result in a five- or six-membered ring optionally containing a heteroatom selected from the group consisting of O, S and NR.sup.Type: GrantFiled: November 27, 1991Date of Patent: July 5, 1994Assignee: Glycomed IncorporatedInventors: Mina Nashed, Falguni Asgupta, Saeed Abbas, John Musser, Darwin Asa
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Patent number: 5296360Abstract: The present invention provides a process for preparing ganglioside G.sub.Ml characterized in that neuraminidase isozyme S is allowed to act on gangliosides to produce ganglioside G.sub.Ml.Type: GrantFiled: June 28, 1991Date of Patent: March 22, 1994Assignee: Marukin Shoyu Co., Ltd.Inventors: Tsunetake Sugimori, Yoji Tsukada, Yasuhiro Ohta
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Patent number: 5281702Abstract: The invention relates to N-deacetyl-lysogangliosides and physiologically acceptable salts thereof, especially those of formula (I): ##STR1## wherein R represents --CH.dbd.CH(CH.sub.2)nCH.sub.3 or --CH.sub.2 CH.sub.2 (CH.sub.2)nCH.sub.3 ;n is 12 or 14;R.sup.1 represents ##STR2## or hydrogen; and R.sup.2 represents hydrogen or acetyl; for use in therapy.The compounds are useful as inhibitors of phospholipases A.sub.2, and of superoxide production, as antiproliferative and immunosuppressant agents in the treatment of autoimmune diseases. The invention also relates to the use of N-deacetyl-lysogangliosides for the manufacture of medicaments for the treatment of the aforementioned conditions.Type: GrantFiled: June 18, 1991Date of Patent: January 25, 1994Assignee: Wellcome Foundation LimitedInventors: Ezio Tubaro, Giovanni Cavallo
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Patent number: 5280016Abstract: A non-anticoagulant (NAC) form of heparin which shows antiproliferative activity with respect to smooth muscle cells is useful in the prevention of restenosis and other conditions benefited by antiproliferative activity with respect to smooth muscle cells. This NAC form of heparin is prepared by oxidizing heparin/heparan sulfate to a desired level with periodate followed by reduction of the resulting aldehyde groups; all under conditions which prevent depolymerization of the heparin.Type: GrantFiled: September 3, 1991Date of Patent: January 18, 1994Assignee: Glycomed IncorporatedInventors: H. Edward Conrad, Yuchuan Guo
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Patent number: 5272146Abstract: Certain new 1,2-dihydroellipticine compounds having activity against CNS specific cancer cell lines because of their ease of passage across the blood-brain barrier are disclosed along with formulations and methods for treating CNS cancers employing these compounds.Type: GrantFiled: October 2, 1992Date of Patent: December 21, 1993Assignees: The United States of America as represented by the United States Department of Health and Human Services, Purdue Research FoundationInventors: Rudiger D. Haugwitz, Venkatachala L. Narayanan, Mark Cushman, Jurjus Jurayj
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Patent number: 5264425Abstract: Salts of glycosaminoglycans (heparin, its fractions or fragments which are supersulfated, dermatan sulfate, heparan sulfate, and modified heparins) with bases of formula (I), ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 represent H, alkyl, or cycloalkyl; R.sub.5 and R.sub.6 represent H, or alkyl; R.sub.7 and R.sub.8 represent H or alkyl; n and m are integers from 1-4 and X is --O--CO--O--, which salts have the pharmacological properties of the glycosaminoglycans themselves, and are orally and rectally administrable.Type: GrantFiled: November 15, 1990Date of Patent: November 23, 1993Assignee: Italfarmaco S.p.A.Inventors: Alma Dal Pozzo, Maurizio Acquasaliente, Giancarlo Sportoletti, Monique Sarret, Paolo Ferruti, Francesco De Santis
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Patent number: 5252728Abstract: The present invention consists in a process for obtaining polymers with antiviral activity which is characterized in that beginning with oligo or polysaccharides with a specific structure, polymers with a specific number of carbonyl groups are obtained by oxidation; in that the carbonyl groups of the oxidized oligo/polysaccharides are made to react with amino groups of molecules carrying amino and sulfonated groups, such as aliphatic aminosulfonates, in water or in mixtures of water with water-miscible solvents, under specific temperature, time, and pH conditions, giving rise to polymers carrying sulfonated groups, which are purified by conventional processes; in that the sulfonated polymers thus obtained have antiviral activity and either lack or present very low toxicity and anticoagulant activity, and are thus suitable for the production of pharmaceutical preparations suitable for use in topical or systemic antiviral therapy in humans or in animals. It is applicable in the pharmaceutical industry.Type: GrantFiled: December 13, 1991Date of Patent: October 12, 1993Assignee: Laboratorios Andromaco S.A.Inventors: Juan P. P. Ranieri, Antonio F. G. Gomez-Pamo, Luis C. Llamas, Jesus A. Armendariz, Juan A. Leal Ojeda, Carmen G. Benito
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Patent number: 5227481Abstract: Cationic polysaccharide derivatives are prepared by reacting a polysaccharide with a polycationic reagent having one polysaccharide reactive group and at least two cationic groups. Suitable reagents include polycationic alkyl, aryl, alkaryl, cycloaliphatic, or heterocyclic amines, some of which are novel compositions. The polycationic polysaccharide derivatives prepared from these reagents are useful in the manufacture of paper.Type: GrantFiled: April 9, 1991Date of Patent: July 13, 1993Assignee: National Starch and Chemical Investment Holding CorporationInventors: John J. Tsai, Peter T. Trzasko, Michael T. Philbin, Robert L. Billmers, Martin M. Tessler, Joseph A. Van Gompel, Morton W. Rutenberg
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Patent number: 5220009Abstract: Novel 3,7-disubstituted phenothiazinium salts are active in the photochemical disinfection of aqueous effluents. The novel salts are of the general formula ##STR1## wherein: either R.sub.1 is a saccharide residue;R.sub.2 is alkyl, cycloalkyl, aryl, aralkyl or heterocyclyl, any alkyl or alkylene chain being optionally interrupted by one or more heteroatoms, and Y is alkylene optionally substituted by alkyl, cycloalkyl, aryl or aralkyl; orR.sub.1 and R.sub.2 are each methyl and Y is a bond; and when R.sub.1 is a saccharide residue X is an anion selected from halogen, R.sub.3 CO.sub.2.sup.-, R.sub.3 SO.sub.3.sup.- and R.sub.3 OSO.sub.3.sup.-, wherein R.sub.3 is alkyl, cycloalkyl, aryl, aralkyl or heterocyclyl, andwhen R.sub.1 and R.sub.2 are each methyl, X is an anion selected from R.sub.3 SO.sub.3.sup.-, R.sub.3 OSO.sub.3.sup.- wherein R.sub.3 is as defined above and R.sub.4 CO.sub.2.sup.-, wherein R.sub.4 is an aldose or ketose residue, an N-protected .alpha.-amino acid residue or a .omega.-carboxy-.alpha.Type: GrantFiled: April 25, 1991Date of Patent: June 15, 1993Assignee: Yeda Research and Development Company LimitedInventors: Yehuda Mazur, Aureliu Acher, Lea Shragina, Moshe Avramoff
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Patent number: 5164377Abstract: The present invention relates to sulphated glycosamino glycuronan with antithrombotic activity consisting essentially of salts of dermatan sulphate, chondroitin sulphate and heparan sulphate, characterized bya) an average molecular weight between 4000 and 8000 daltons;b) a nitrogen content between 2.4 and 3.0%;c) a sulphur content between 7.5 and 9.5%;d) a sodium content between 9 and 11%;e) a dermatan sulphate content between 5 and 25%;f) a chondroitin sulphate content less than 9%;g) an anti-Xa activity between 11 and 20 .mu./mg; andh) an antithrombin III dependent antithrombin activity of less than 1 .mu./mg.Type: GrantFiled: October 3, 1990Date of Patent: November 17, 1992Assignee: Akzo N.V.Inventors: Gijsbert W. K. Van Dedem, Francois E. A. Van Hou Denhoven, Dirk G. Meuleman, Huibert C. T. Moelker, Adrianus L. M. Sanders
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Patent number: 5137876Abstract: The compound having the formula: ##STR1## has antiviral activity, specifically in the prevention or treatment of infection by retroviruses, including HIV, and immunosuppressive activity, either as a compound, pharmaceutically acceptable salt, or a pharmaceutical composition ingredient, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing or treating viral infections and modulating immune responses in vivo are also described.Type: GrantFiled: October 12, 1990Date of Patent: August 11, 1992Assignee: Merck & Co., Inc.Inventors: Malcolm MacCoss, Laura C. Meurer, Richard L. Tolman
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Patent number: 5126439Abstract: The present invention is directed to new artificial base pairs comprising complementary artificial purines and pyrimidines and methods of using artificial complementary base pairs.Type: GrantFiled: September 22, 1988Date of Patent: June 30, 1992Assignee: Temple UniversityInventor: Harry P. Rappaport
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Patent number: 5102883Abstract: The pyrimidine biosynthesis inhibitors dichloroallyl lawsone, N-(phosphonoacetyl)-L-aspartic acid (PALA), pyrazofurin, and derivatives thereof, are useful as immunomodulatory and anti-inflammatory agents. Pharmaceutical formulations containing these compounds are useful for the treatment of autoimmune diseases, chronic inflammatory diseases, and of organ transplantation rejections.Type: GrantFiled: October 31, 1989Date of Patent: April 7, 1992Assignee: Du Pont Merck Pharmaceutical CompanyInventors: Neil R. Ackerman, Bruce D. Jaffee
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Patent number: 5101026Abstract: The present invention relates to ganglioside related compounds having, for example, the following formula: ##STR1## where R.sub.1 represents H or COCH.sub.3 (hereinafter abbreviated to "AC"); R.sub.2 represents H or CH.sub.3 ; and R.sub.3 represents --OH, ##STR2## These ganglioside related compounds are useful as membrane receptors, tumor markers, cell growth controlling substances, etc., and useful for immunotherapy for cancer, etc.Type: GrantFiled: August 6, 1987Date of Patent: March 31, 1992Assignee: MECT CorporationInventors: Tomoya Ogawa, Mamoru Sugimoto, Masaaki Numata, Masayoshi Ito, Yoshiyasu Shitori, Shigeki Nunomura
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Patent number: 5089392Abstract: Fluorogenic substrates and compositions containing the same are useful for detecting enzymatic activity within intact cells. The fluorogenic substrates are lysosomotropic derivatives of 2,3-dicyano-hydroquinone (DCH). These derivatives may be employed for detecting lysosomal enzymatic activity within intact cells using fluorescent microscopy and cytometry.Type: GrantFiled: March 30, 1990Date of Patent: February 18, 1992Assignee: The United States of America as represented by of the Department of Health and Human ServicesInventors: Stephen P. F. Miller, Roscoe O. Brady
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Patent number: 5077277Abstract: Derivatives of antibiotics derived from the microorganism Streptomyces lydicus subspecies tanzanius, referred to as antibiotics LL-E19020 alpha and beta, are produced by chemical reaction. The derivatives are also active antibiotics useful in the treatment of bacterial infections.Type: GrantFiled: September 5, 1989Date of Patent: December 31, 1991Assignee: American Cyanamid CompanyInventors: Douglas W. Phillipson, Guy T. Carter, Donald B. Borders
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Patent number: 5070191Abstract: An antifungal compound, demethylallosamidin, represented by the formula: ##STR1## is disclosed. Methods of production and antifungal compositions comprising demethylallosamidin are also provided.Type: GrantFiled: April 27, 1990Date of Patent: December 3, 1991Assignee: Ajinomoto Co., Inc.Inventors: Yasuhiro Yamada, Shohei Sakuda, Seiji Takayama
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Patent number: 5059685Abstract: Cationized derivatives of natural polysaccharides having a polyglucoside structure with 50-5000 monomer units and one or more side chains bonded to the glucoside nucleus by a nitrogen or oxygen atom or an amide group, said side chains having one or more quaternary nitrogen atoms so that each monomer unit has a cation charge density exceeding two. The new compounds are particularly active as hypocholesterolemic agents.Type: GrantFiled: February 5, 1991Date of Patent: October 22, 1991Assignee: Etablissement TexcontorInventor: Franco Conti
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Patent number: 5041427Abstract: Compounds are disclosed which are useful in a method of treating animals to protect them from the toxic effects of Gram negative endotoxin. They include the diphosphoryl lipid A (DPLA) which can be obtained from R. sphaeroides ATCC 17023 grown at about 26.degree. C.Type: GrantFiled: January 19, 1990Date of Patent: August 20, 1991Assignee: Wisconsin Alumni Research FoundationInventors: Kuni K. Takayama, Nilofer Qureshi
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Patent number: 5010184Abstract: Novel ionically modified polysaccharides which contain .alpha.-glycosidic linkages, the ionic groups of which are attached to the polysaccharide component through the grouping of the formula--CO--NH--CH.sub.2 --O--,the carbonyl group being attached to the ionic group and the oxygen atom being attached to the polysaccharide component, are prepared by reacting the polysaccharides with compounds that contain N-methylolamide groups, and are used for treating effluents and, in particular, for separating mixtures of substances containing ionic components by chromatography.Type: GrantFiled: June 21, 1989Date of Patent: April 23, 1991Assignee: Ciba-Geigy CorporationInventor: Jurg Merz
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Patent number: 4990500Abstract: Oxirane-pseudooligosaccharides of the formula I ##STR1## in which z is zero or 1, their physiologically acceptable salts with acids, a process for their preparation, pharmaceutical preparations, and their use are described. The compounds have an .alpha.-glucosidase-inhibiting action.Type: GrantFiled: August 11, 1987Date of Patent: February 5, 1991Assignee: Hoechst AktiengesellschaftInventors: Laszlo Vertesy, Joachim Betz, Hans-Wolfram Fehlhaber, Karl Geisen
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Patent number: 4983726Abstract: 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.Type: GrantFiled: November 24, 1989Date of Patent: January 8, 1991Assignee: Sanofi S.A.Inventors: Pierre Roger, Patrick Choay, Claude Monneret, Jean-Paul Fournier
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Patent number: 4980462Abstract: 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.Type: GrantFiled: June 19, 1989Date of Patent: December 25, 1990Assignee: Symbicom AktiebolagInventors: Karl-Anders Karlsson, Erling Norrby, Goran Wadell
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Patent number: 4963666Abstract: Method of crosslinking carboxyl-containing polysaccharides in that the polysaccharide is at first activated with a bi- or polyfunctional reagent, and then after removal of any potential excess of activating reagent the crosslinking is performed during drying. The invention also comprises a material produced according to this method.Type: GrantFiled: January 27, 1988Date of Patent: October 16, 1990Assignee: Pharmacia ABInventor: Tomas Malson
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Patent number: 4956459Abstract: Compounds of the formula: ##STR1## wherein each of R.sub.1 and R.sub.2 is independently selected from the group consisting of halogen, hydroxy, or mono carboxylic acid or R.sub.1 and R.sub.2 together is a multifunctional carboxylic acid residue which forms a ring with the platinum atom through two oxygens of said multifunctional carboxylic acid; R.sub.3 is a deoxy mono or disaccharide or a derivative thereof; and R.sub.4 is selected from the group consisting of hydrogen, C.sub.1-4 -alkyl, phenyl, benzyl, substituted phenyl or substituted benzyl, wherein substituents are selected from the group consisting of halogen, nitro, C.sub.1-2 -alkoxy, carboxy, carbony ester or phenyl or a pharmaceutically acceptable salt thereof are disclosed. Compositions containing these compounds and methods using these compounds are also discussed.Type: GrantFiled: January 14, 1988Date of Patent: September 11, 1990Assignee: Georgetown UniversityInventors: Abdolhossen Talebian, Dianna C. Green, Charles F. Hammer, Philip S. Schein
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Patent number: 4925932Abstract: A double sulfate salt of 1-desoxy-(5-hydroxytryptamino)-D-fructose (DFS) and 1-methylhydantoin-2-imide (creatinine) is prepared by adding creatinine to an aqueous solution of DFS containing sulfuric acid having a pH of approximately 3. The double salt may be isolated by crystallizing it in the presence of a water-miscible solvent such as ethanol. DFS may be prepared by glycosylation of 5-hydroxytryptamine with D-glucose and then adding an excess of calcium hydroxide to the glycosylation reaction medium for precipitating DFS.CA(OH).sub.2 from which the DFS may be isolated for preparing the double salt as described above. Recycling and treatment of mother liquors enables yields to be increased.Type: GrantFiled: November 13, 1987Date of Patent: May 15, 1990Assignee: Nestec S.A.Inventors: Raymond Bertholet, Pierre Hirsbrunner
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Patent number: 4904771Abstract: 5'-Pseudouridyl-N-oleoyl carbamate represented by the formula: ##STR1## This compound is physiologically active in that it markedly enhances the actions of glucocorticoids and hence is useful as an alternative to conventional steroid drugs.Type: GrantFiled: December 3, 1987Date of Patent: February 27, 1990Inventors: Nobuhiko Katsunuma, Hiroshi Kido, Ikutoshi Matsuura, Yoshihiko Ishitani
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Patent number: 4902791Abstract: 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.Type: GrantFiled: April 14, 1988Date of Patent: February 20, 1990Assignee: Sanofi S.A.Inventors: Pierre Roger, Patrick Choay, Claude Monneret, Jean-Paul Fournier, Alain Martin
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Patent number: 4859769Abstract: 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.Type: GrantFiled: November 5, 1986Date of Patent: August 22, 1989Assignee: Symbicom ABInventors: Karl-Anders Karlsson, Erling Norrby, Goran Wadell