Viscosity Or Degree Of Polymerization Changed (e.g., Degrading, Cross Linking, Etc.) Patents (Class 536/41)
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Patent number: 5932709Abstract: The present invention relates to chemotherapeutic agents, and more particularly, to novel analogs of camptothecin. The camptothecin analogs display increased solubility through the hydrophilicity of added non-ionic sugar substituents. In accordance with the present invention, a member from the class of novel camptothecin analogs is to be delivered in vivo as a chemotherapeutic agent to fight cancer growth in the body.Type: GrantFiled: June 16, 1997Date of Patent: August 3, 1999Assignee: University of MichiganInventors: Brian Keith Shull, Clarke Slemon, Masato Koreeda
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Patent number: 5932555Abstract: The present invention relates to compound 0406TP-1 represented by the general formula (I): ##STR1## wherein Ac represents an acetyl group and Me represents a methyl group, or a pharmaceutically acceptable salt thereof, having excellent antitumor activity and immunosuppressive activity.Type: GrantFiled: January 22, 1998Date of Patent: August 3, 1999Assignee: Higeta Shoyu Co., Ltd.Inventors: Hisayuki Komaki, Akira Nemoto, Yasushi Tanaka, Yuzuru Mikami, Katsukiyo Yazawa, Jun'ichi Kobayashi
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Patent number: 5929037Abstract: Disclosed is the trisaccharide .alpha.-D-Glcp-(1-2)-.alpha.-D-Glcp-(1-3)-.alpha.-D-Glcp and compounds related thereto as well as pharmaceutical compositions thereof.Type: GrantFiled: June 7, 1995Date of Patent: July 27, 1999Assignee: Alberta Research CouncilInventors: Om Srivastava, Roman Szweda
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Patent number: 5925622Abstract: An aryl glucuronide of 2-hydroxy-N-(5-nitro-2-thiazolyl)benzamide, preferably an O-aryl glucuronide, as well as methods for the convenient synthesis of these aryl glucuronides, highly stable and low toxicity pharmaceutical composition containing these aryl glucuronides, and methods for use of these pharmaceutical compositions, for example, for treatment of inflammation, infections, etc.Type: GrantFiled: July 13, 1998Date of Patent: July 20, 1999Assignee: Romark Laboratories, L.C.Inventors: Jean-Fran.cedilla.ois Rossignol, Marc S. Ayers
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Patent number: 5925747Abstract: Pumpable water-containing surfactant concentrates with a solids content of 30 to 60% by weight containing(a) alkyl and/or alkenyl oligoglycosides and(b) amphoteric or zwitterionic surfactantsin a ratio by weight of 10:90 to 90:10, based on the solids content; processes for their preparation and their use in the production of surface-active formulations.Type: GrantFiled: April 4, 1997Date of Patent: July 20, 1999Assignee: Henkel Kommanditgesellschaft auf AktienInventors: Guenter Uphues, Joerg Kahre, Ansgar Behler, Peter Neumann, Hermann Hensen, Werner Seipel, Holger Tesmann
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Patent number: 5919768Abstract: The present invention provides compounds having structure (II), and the pharmaceutically acceptable salts, esters, amides and prodrugs thereof.Type: GrantFiled: February 11, 1998Date of Patent: July 6, 1999Assignee: Texas Biotechnology CorporationInventors: Timothy P. Kogan, Brian Dupre, Ian L. Scott, Huong Bui, Kathy L. Wheeler, Karin M. Keller, Jamal M. Kassir
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Patent number: 5912330Abstract: Novel crystalline maltosyl glucoside is obtained by crystallizing maltosyl glucoside from a maltosyl glucoside solution, prepared by exposing either an aqueous solution containing trehalose and an .alpha.-glucosyl saccharide or an aqueous solution containing a reducing partial starch hydrolysate to the action of a saccharide-transferring enzyme. The crystalline maltosyl glucoside has non-hygroscopicity, non-reducibility, superior solubility, less fermentability, and other properties of stabilizing oligopeptides and biologically-substances as well as preventing retrogradation of amylaceous substances. These features render it very useful in various compositions including foods, beverages, cosmetics, pharmaceuticals and shaped bodies.Type: GrantFiled: September 19, 1997Date of Patent: June 15, 1999Assignee: Kabushiki Kaisha Hayashibara Seibutsu Kagaku KenkyujoInventors: Akihiko Tabuchi, Takashi Shibuya, Toshiyuki Sugimoto, Toshio Miyake
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Patent number: 5910519Abstract: Shaped hydrogel articles such as soft contact lenses are prepared by the steps of:(1) molding or casting a polymerization mixture comprising:(a) a monomer mixture comprising a major proportion of one or more hydrophilic monomers such as 2-hydroxyethyl methacrylate, and one or more cross-linking monomers; and(b) an inert, displaceable diluent selected from the group consisting of:(i) ethoxylated alkyl glucoside;(ii) ethoxylated bisphenol A;(iii) polyethylene glycol;(iv) mixture of propoxylated and ethoxylated alkyl glucoside;(v) single phase mixture of ethoxylated or propoxylated alkyl glucoside and C.sub.2-12 dihydric alcohol;(vi) adduct of .epsilon.-caprolactone and C.sub.2-6 alkanediols and triols;(vii) ethoxylated C.sub.3-6 alkanetriol; and(viii) mixtures of one or more of (i) through (vii),under conditions to polymerize said monomer mixture to produce a shaped gel of a copolymer of said monomers and said diluent; and(2) thereafter replacing said diluent with water.Type: GrantFiled: August 1, 1997Date of Patent: June 8, 1999Assignee: Johnson & Johnson Vision Products, Inc.Inventors: Ivan M. Nunez, Frank F. Molock, Laura D. Elliott, James D. Ford
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Patent number: 5910579Abstract: Disclosed are novel synthetic processes for the preparation of the trisaccharide .alpha.Gal(1.fwdarw.4).beta.Gal(1.fwdarw.4)Glc-OR compounds.Type: GrantFiled: September 30, 1997Date of Patent: June 8, 1999Assignee: Synsorb Biotech Inc.Inventors: Robert E. Yeske, Robert A. Verhagen, Joaquin Roberto Mendez
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Patent number: 5908928Abstract: A novel surfactant of formula I:R.sub.1 O(R.sub.2 O).sub.b (Z).sub.a OCH.sub.2 COO.sup.- X.sup.+Iwherein R.sub.1 is a monovalent organic radical having from about 6 to about 30 carbon atoms; R.sub.2 is divalent alkylene radical having from 2 to 4 carbon atoms; Z is a saccharide residue having 5 or 6 carbon atoms; b is a number having a value from 0 to about 12; a is a number having a value from 1 to about 6; and X is an alkali metal ion.Type: GrantFiled: November 10, 1997Date of Patent: June 1, 1999Assignee: Henkel CorporationInventors: Norman Milstein, Barry A. Salka
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Patent number: 5905071Abstract: The present invention relates to (2-aminoacylamino-2-deoxy-glycosyl)-amides, which are substituted on the nitrogen atom of the amino acid, of the general formula (I) ##STR1## in which the substituents have the meaning given in the description, to processes for their preparation and to their use in medicaments.Type: GrantFiled: June 25, 1996Date of Patent: May 18, 1999Assignee: Bayer AktiengesellschaftInventors: Oswald Lockhoff, Burkhard Mielke, Helmut Brunner, Klaus Schaller
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Patent number: 5891655Abstract: Disclosed are fibroblast growth factor (FGF) binding and FGF receptor activation, and a method of identifying small molecular weight compounds that interact with FGF to modulate its activity such as, e.g., activators and inhibitors. Illustrative small oligosaccharides, namely di- and tri-saccharides, are shown to be effective modulators of FGF binding and FGF receptor activation.Type: GrantFiled: April 23, 1997Date of Patent: April 6, 1999Assignee: Washington UniversityInventor: David M. Ornitz
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Patent number: 5891854Abstract: Cosmetic ceutical formulations characterized by an effective, content of pharmaceutically and/or cosmetically unobjectionable hexosyl glycerides and/or (hexosyl)hexosyl glycerides.Type: GrantFiled: October 24, 1996Date of Patent: April 6, 1999Assignee: Beiersdorf AGInventors: Joachim Thiem, Oliver Scheel, Gunther Schneider
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Patent number: 5891862Abstract: The present invention includes polymerizable monomers comprising a fucoside moiety. In one embodiment, the monomer has a polymerizable functional group, such as an olefinic bond, to which the fucoside moiety is attached by a spacer group, for example, an alkylene group, or an alkylene group wherein one or more carbon atoms are substituted by heteroatoms, such as oxygen, nitrogen or sulfur atoms. The present invention also includes polymers comprising one or more fucoside moieties, such as pendant fucoside moieties, which can inhibit or prevent rotavirus infection in a mammal. Such a polymer can comprise, for example, a monomer of the present invention. The polymer can be a homopolymer or a copolymer, and can have, for example, a polyacrylamide, polyacrylate or polystyrene backbone.Type: GrantFiled: September 20, 1996Date of Patent: April 6, 1999Assignee: GelTex Pharmaceuticals, Inc.Inventors: W. Harry Mandeville, III, John S. Petersen, Venkata R. Garigapati, Thomas X. Neenan
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Patent number: 5892064Abstract: A chemiluminescent assay method and compositions are described which use a dialkyl-substituted dioxetane which is deprotected to trigger a chemiluminescent reaction. Chemiluminescent 1,2-dioxetane compounds substituted on the dioxetane ring with two nonspirofused alkyl groups which can be triggered by a reagent to generate light are disclosed. Dialkyl-substituted dioxetanes are useful for the detection of triggering agents including enzymes. The enzyme may be present alone or linked to a member of a specific binding pair in an immunoassay, DNA probe assay or other assay where the enzyme is bound to a reporter molecule.Type: GrantFiled: November 26, 1997Date of Patent: April 6, 1999Assignee: Lumigen, Inc.Inventors: Arthur Paul Schaap, Hashem Akhavan-Tafti
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Patent number: 5889164Abstract: This invention provides a novel chromanol glycoside which is a water soluble antioxidant excellent in heat and pH stability and production method thereof. It is a chromanol glycoside represented by the general formula (1): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 independently are a hydrogen atom or a lower alkyl group, R.sup.5 is a hydrogen atom, a lower alkyl group, or a lower acyl group, X is a monosaccharide residue or an oligosacoharide residue, providing the hydrogen atom of the hydroxyl group of saccharide residue may be substituted by a lower alkyl group or a lower acyl group, n is an integer in the range of 0 to 4, and m is an integer in the range of 1 to 6.Type: GrantFiled: September 27, 1995Date of Patent: March 30, 1999Assignee: CCI CorporationInventors: Hironobu Murase, Tsutomu Kunieda, Tetsuya Tsujii
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Patent number: 5885968Abstract: Triantennary cluster glycoside, wherein each glycoside residue is attached to the branching point of the cluster by a spacer of a long, flexible, hydrophilic chain comprising at least 4 atoms in the chain. The glyciside spacer preferably comprises at least two hydrophilic groups. Use of the triantennary cluster glycoside in pharmaceutical preparations, for instance hypolipidemic medicines.Type: GrantFiled: May 4, 1995Date of Patent: March 23, 1999Assignees: Rijksuniversiteit te Leiden, Nederlandse HartstichtingInventors: Ericus Anna Leonardus Biessen, Theodorus Josephus Cornelis van Berkel, Jacobus Hubertus van Boom
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Patent number: 5886238Abstract: Alkene precursors for preparing dialkyl-substituted dioxetanes. The dioxetanes are useful for the detection of triggering agents including enzymes.Type: GrantFiled: August 28, 1996Date of Patent: March 23, 1999Assignees: Lumigen, Inc., The Board of Governors of Wayne State UniversityInventors: Arthur Paul Schaap, Hashem Akhavan-Tafti
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Patent number: 5885972Abstract: This invention relates to .alpha. and .beta.-L-pyranosyl nucleosides of Formula (I), wherein the nucleoside substitution on the pyranosyl carbohydrate molecule comprises a substituted or unsubstituted purine (adenine or guanine) or pyrimidine (cytosine, uracil, thymine and hypoxanthine) base. Also provided are methods to make the .alpha. and .beta.-L-pyranosyl nucleosides and methods of using such to treat cancer in a mammal.Type: GrantFiled: October 2, 1996Date of Patent: March 23, 1999Assignee: Genencor International, Inc.Inventors: Alexander L. Weis, Charles T. Goodhue
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Patent number: 5883079Abstract: 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)-pGal-.beta.(1)-(--X--).sub.m --(--Y--).sub.n -).sub.p -ZwhereinX=a chemical bond or a group capable of linking the p 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)-pGal-.beta.(1)-AwhereinA=a group capable of bonding to the p galactose;wherein the C.sub.1 glycosidic oxygen of galactose may be replaced by N, S or C.Type: GrantFiled: May 12, 1998Date of Patent: March 16, 1999Assignee: Neose Technologies, Inc.Inventors: David A Zopf, Paul M. Simon, Stephen Roth, Edward J. McGuire, Dennis H. Langer
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Patent number: 5882902Abstract: Method for synthesis of GalNAc.alpha.-serine or GalNAc.alpha.-threonine containing compounds, including at least one reaction where an .alpha.-saccharide or .alpha.-glycoside of GalNAca is used as gylcosyl donor and a derivative of serine of threonine is used as acceptor in a transglycosylation reaction with N-acetyl-.alpha.-D-galactosaminidase as the catalyst, wherein said acceptor has been modified in its N-terminal .alpha.-amino group and optionally in its c-terminal carboxyl group.Type: GrantFiled: May 12, 1997Date of Patent: March 16, 1999Assignee: Bioflexin ABInventor: Kurt Nilsson
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Patent number: 5880160Abstract: The present invention relates to novel colchicine derivatives having antiproliferative, antineoplastic, antiinflammatory and muscle relaxant activities; said derivatives include novel colchine nitrogen amides for use either as such or after derivatization of the hydroxyl at C.sub.3 of the aromatic ring and at C.sub.10 of the tropolone ring. These novel compounds have a cytotoxicity on human tumoral cell lines comparable with colchicine but, in comparison with the latter, they are much more active on cells resistant to the usual antiblastics. The compounds can be included in pharmaceutical formulations useful for the intravenous, oral and topical administrations.Type: GrantFiled: June 27, 1996Date of Patent: March 9, 1999Assignee: Indena S.p.A.Inventors: Ezio Bombardelli, Bruno Gabetta
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Patent number: 5874411Abstract: Disclosed are novel oligosaccharide glycosides having mammalian immunosuppressive and tolerogenic properties, pharmaceutical compositions containing such oligosaccharide glycosides and to methods of using such oligosaccharide glycosides to modulate cell-mediated immune responses in a mammal.Type: GrantFiled: November 13, 1996Date of Patent: February 23, 1999Assignee: Glycomed IncorporatedInventors: Om P. Srivastava, Geeta Srivastava, Roman Szweda, David R. Bundle, Ole Hindsgaul, H. Rizk Hanna, Kevin Holme, Frank W. Barresi, Minghui Du
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Patent number: 5869460Abstract: There are described sulfated and phosphated saccharide erivatives of the Formula ##STR1## wherein R.sub.1 is hydrogen atom or a residue of sulfate, phosphate or L-fucose; R.sub.2, R.sub.3 and R.sub.4 are hydrogen atom or a residue of sulfate or phosphate, respectively; 1 is an integer of 0 or 1;m is an integer of 0-15; and n is an integer of 0-21, or pharmaceutically acceptable salts thereof, a process for the preparation of the derivatives and salts as well as use thereof, as an anti-inflammatory agent.Type: GrantFiled: October 29, 1996Date of Patent: February 9, 1999Assignee: Sanwa Kaguku Kenkyusho Co., Ltd.Inventors: Toshinao Usui, Takao Igami, Takuji Kakigami, Hitoshi Hamashima, Takahito Jomori, Akira Tashita, Yoshiro Ishiwatari, Shoji Yokochi, Takahiko Mitani, Yasuo Suzuki, Akira Hasegawa
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Patent number: 5869699Abstract: A new class of stable dioxetanes bears a polycyclic stabilizing group and aryloxy moiety, the oxygen atom of which is provided with a protective group which can be removed by an enzymatic or chemical trigger admixed with the dioxetane. The polycyclic stabilizing group is preferably spiroadamantane. The group further bears an alkoxy, aryloxy, aralkyloxy or cycloalkyloxy moiety which is partially or completely substituted with halogens, particularly fluorine and chlorine. Proper selection of electron active groups on the stabilizing moiety, the aryl group and the OR group yields enhanced enzyme kinetics, superior light intensity and excellent detection sensitivity in various assays.Type: GrantFiled: June 10, 1997Date of Patent: February 9, 1999
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Patent number: 5866376Abstract: The present invention is directed to biosurfactant stabilized emulsions of high viscosity hydrocarbons such as high viscosity crude oil wherein the biosurfactant is a metabolite of Pseudomonas aeruginosa (USB-CS1) and two methods for making the same. Preferably, the viscosity of the biosurfactant stabilized emulsions is below about 500 centipoise and, more preferably, below about 100 centipoise at ambient temperatures.Type: GrantFiled: February 25, 1997Date of Patent: February 2, 1999Assignee: Universidad Simon BolivarInventors: Carlos Ali Rocha, Dosinda Gonzalez, Maria Lourdes Iturralde, Ulises Leonardo Lacoa, Fernando Antonio Morales
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Patent number: 5863771Abstract: A saccharide composition comprising maltooligosyl derivatives of turanose and palatinose which can be readily produced, separated, and purified in a relatively-high yield from maltooligosylsucrose by allowing non-reducing saccharide-forming enzymes to act on aqueous solutions containing maltooligosylsucrose. These saccharides are reducing oligosaccharides with a mild and high-quality sweetness and can be used orally and parenterally, as well as being readily metabolized and used by living bodies.Type: GrantFiled: March 3, 1997Date of Patent: January 26, 1999Assignee: Kabushiki Kaisha Hayashibara Seibutsu Kagaku KenkyujoInventors: Hajime Aga, Takashi Shibuya, Shigeharu Fukuda, Toshio Miyake
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Patent number: 5861492Abstract: The invention relates to methods that permit the rapid construction of oligosaccharides and other glycoconjugates. Methods for forming multiple glycosidic linkages in solution in a single step are disclosed. The invention takes advantage of the discovery that the relative reactivity of glycoside residues containing anomeric sulfoxides and nucleophilic functional groups can be controlled. In another aspect of the invention, the reactivity of activated anomeric sugar sulfoxides is utilized in a solid phase method for the formation of glycosidic linkages. The methods disclosed may be applied to the preparation of specific oligosaccharides and other glycoconjugates, as well as to the preparation of glycosidic libraries comprising mixtures of various oligosaccharides, including glycoconjugates, which can be screened for biological activity.Type: GrantFiled: January 9, 1997Date of Patent: January 19, 1999Assignee: The Trustees of Princeton UniversityInventor: Daniel Evan Kahne
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Patent number: 5854219Abstract: The invention relates to 9-N-ethenyl derivatives of 9 (S)-erythromycylamine, new semisynthetic antibiotics of the macrolide class of the general formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and represent nitryl, a carboxyl group of the formula COOR.sup.3, wherein R.sup.3 represents a C.sub.1 -C.sub.4 alkyl group, or a keto group of the formula COR.sup.4, wherein R.sup.4 represents a C.sub.1 -C.sub.4 alkyl group, to their pharmaceutically acceptable addition salts with inorganic or organic acids, to a process for their preparation, to a process for the preparation of the pharmaceutical compositions as well as to the use of the obtained pharmaceutical compositions in the treatment of bacterial infections.Type: GrantFiled: October 23, 1997Date of Patent: December 29, 1998Assignee: PLIVA, farmaceutska, kemijska, prehrambena i kozmeticka industrija, dionicko drustvoInventors: Nedjeljko Kujundzic, Dina Pavlovic, Gabrijela Kobrehel, Gorjana Lazarevski, Zeljko Kelneric
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Patent number: 5852204Abstract: The present invention relates to heterocyclic compounds which have been found to have anti-tumor activity. More specifically, the invention concerns pyrrolo?3,2-b!carbazoles and 1H-?1! benzothieno ?2,3-f! indoles, methods for their preparation, pharmaceutical formulations containing them and their use as anti-tumor agents. The compounds have low toxicity against normal cell lines while exhibiting anti-tumor cell activity.Type: GrantFiled: August 16, 1996Date of Patent: December 22, 1998Assignee: University College Cardiff Consultants LimitedInventors: David Drysdale Miller, Sadie Vile, Patrick Vivian Richard Shannon, Laddawan Chunchatprasert, Alan Thomas Hudson
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Patent number: 5849679Abstract: A non-ionic surfactant represented by the general formula (1) or (2) shown below, an emulsified composition and a dispersion containing same are disclosed. Also disclosed is a method of preparing glycoside compound having nonionic surface active properties. The nonionic surfactant has good safety to human bodies and is excellent in producing foam with good feeling in touch.General formula ?1!:?Z(OH).sub.q-1 !--O?C.sub.3 H.sub.5 (OH)O!--R.sup.1 ?1!wherein ?Z(OH).sub.q-1 ! stands for a saccharide residue excluding the hydroxyl group connected to the carbon atom in anomeric position among q hydroxyl groups connected to the saccharide compound of the formula ?Z(OH).sub.q !, --O?C.sub.3 H.sub.5 (OH)O!-- for a glycerol residue excluding 2 hydrogen atoms from glycerol HO?C.sub.3 H.sub.5 (OH)O!--H, and R.sup.1 for an aliphatic group having 1-12 carbon atoms,General formula ?2!:?Z(OH).sub.q-1 !--O?C.sub.3 H.sub.5 (OH)O!.sub.x --R.sup.2 ?2!wherein ?Z(OH)!.sub.Type: GrantFiled: June 13, 1996Date of Patent: December 15, 1998Assignee: Lion CorporationInventors: Haruhiko Toda, Hiroshi Miyake, Kazuhiko Matsuda, Masahiro Sato
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Patent number: 5849716Abstract: The present invention relates to a sphingoglycolipid represented by the following formula (I) which is effective at a small dose and has an anti-tumor activity and an immunostimulating effect with few side-effects: ##STR1## wherein X denotes an integer from 10 to 24, Y denotes an integer from 9 to 13,R.sub.1 represents a hexosyl, pentosyl, deoxyhexosyl, aminohexosyl, N-acetylaminohexosyl or a halide thereof or a sialic acid,R.sub.2 represents H or a group OR.sub.2 ', wherein R.sub.2 ' represents H or a galactosyl or glucosyl group,R.sub.3 represents H or a group OR.sub.3 ', wherein R.sub.3 ' represents H or a galactosyl or glucosyl group,R.sub.4 represents a galactosyl group or H,R.sub.5 represents a methyl or isopropyl group,R.sub.6 and R.sub.7 respectively represents H or form a double bond between the two carbon atoms to which R.sub.6 and R.sub.7 are attached,except for the case where R.sub.1 represents .alpha.-galactosyl and R.sub.4 represents H.Type: GrantFiled: April 21, 1995Date of Patent: December 15, 1998Assignee: Kirin Beer Kabushiki KaishaInventors: Koji Akimoto, Yasuhiko Koezuka
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Patent number: 5846943Abstract: Disclosed are novel solid support matrices having a toxin-binding oligosaccharide covalently attached to a solid support through a linking arm which has at least 8 atoms separating the oligosaccharide from the solid support. The disclosed solid support matrices are useful for neutralizing toxins from disease-causing microrganisms.Type: GrantFiled: November 8, 1996Date of Patent: December 8, 1998Assignee: Synsorb Biotech, Inc.Inventors: Ole Hindsgaul, Ulf J. Nilsson
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Patent number: 5847206Abstract: New fluorinated derivatives useful as surfactants or in the transport of drug or markers, or in drug targeting, and preparations containing the derivatives, for medical, cosmetic and veterinary uses, having the formula: ##STR1## wherein R.sub.F is a fluorinated radical, X is a linear or branched alkylene, R.sup.1 is H or CH.sub.3, R.sup.2 is a radical having at least one OH group, R.sup.3 is a radical derived from an amino acid or a peptide, 1.ltoreq.n.ltoreq.50 and 0.ltoreq.m.ltoreq.200 with 0.2.ltoreq.n/n+m.ltoreq.1.These derivatives can be used as prodrugs or in formulating pharmaceutical, cosmetic and veterinary preparations, in biology and medicine, notably in compositions acting as carriers of oxygen and other gases, of contrast agents, or as carriers of substances used in therapy, or as carriers of markers.Type: GrantFiled: June 7, 1995Date of Patent: December 8, 1998Assignee: Alliance Pharmaceutical Corp.Inventors: Andre Pavia, Bernard Pucci, Jean G. Riess, Leila Zarif
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Patent number: 5847161Abstract: A new class of stable dioxetanes bears a polycyclic stabilizing group and aryloxy moiety, the oxygen atom of which is provided with a protective group which can be removed by an enzymatic or chemical trigger admixed with the dioxetane. The polycyclic stabilizing group is preferably spiroadamantane. The group further bears an alkoxy, aryloxy, aralkyloxy or cycloalkyloxy moiety which is partially or completely substituted with halogens, particularly fluorine and chlorine. Proper selection of electron active groups on the stabilizing moiety, the aryl group and the OR group yields enhanced enzyme kinetics, superior light intensity and excellent detection sensitivity in various assays.Type: GrantFiled: June 13, 1997Date of Patent: December 8, 1998
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Patent number: 5844103Abstract: The present invention relates to a new class of carbohydrate based nonionic surfactant, i.e., alkyl and alkenyl glycasuccinamide, and a process for their manufacture.Type: GrantFiled: March 24, 1995Date of Patent: December 1, 1998Assignee: Lever Brothers Company, Division of Conopco, Inc.Inventors: Van Au, Robert Vermeer, Bijan Harichian
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Patent number: 5843922Abstract: The invention provides a method for preparation of a bifidobacteria-nourishing medium by subjecting a saccharide-based feedstock containing fructosyl units to flash flow conditions. The resulting shearform matrix is then treated to provide a medium having fructosyl-containing oligosaccharide. Preferably, the shearform matrix is treated by subjecting it to acid thermolysis conditions. Also provided is a method of nourishing mammalian alimentary tract for preferential growth of bifidobacteria. In addition, there is provided a medium for nourishing bifidobacteria and comestible products made therefrom.Type: GrantFiled: June 11, 1996Date of Patent: December 1, 1998Assignee: Fuisz Technologies Ltd.Inventors: Roy L. Whistler, James N. BeMiller
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Patent number: 5843910Abstract: The present invention relates to novel colchicine derivatives of formula (1), where Y is a --CH.sub.2 --CH--NH--R.sub.3 group or a --CH--CH.sub.2 OR.sub.3 group and the other variables are as defined in claim 1, having antiproliferative, antitumoral and anti-inflammatory activities. The novel compounds have a cytotoxicity on human tumoral cell lines comparable with colchicine, but, in comparison with the latter, they are less toxic and more selective, particularly on cells resistant to the usual medicaments. Some compounds have a marked activity on TNF and interleukine 2, and therefore are very potent anti-inflammatory agents. They can be included in pharmaceutical formulations useful for the parenteral, oral and topical administrations.Type: GrantFiled: March 21, 1997Date of Patent: December 1, 1998Assignee: Indena S.p.A.Inventors: Ezio Bombardelli, Bruno Gabetta
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Patent number: 5843909Abstract: The present invention relates to (3.beta., 4.alpha.,16.beta.)-16,23,28-trihydroxyolean-12-ene-3-yl-.beta.-D-glucopyra nuronic acid derivatives and a method for preparing the same from Gymnema inodorum leaves, which comprises treating Gymnema inodorum leaves with an aqueous acid solution, extracting the leaves with an alcohol and/or water, concentrating the extract and subjecting to liquid-liquid partition extraction with water and 1-butanol, concentrating and drying/caking the 1-butanol phase under reduced pressure, defatting the cake, extracting soluble components from the cake with a high polar solvent, concentrating and drying/caking the extract to obtain a purified Gymnema inodorum leaf extract, and then applying the purified extract to HPLC to obtain fractions containing glucose absorption inhibiting substances.Type: GrantFiled: June 13, 1997Date of Patent: December 1, 1998Assignee: Kowa Chemical Industries Co., Ltd.Inventors: Mikito Atsuchi, Yuri Hirao, Yoshio Iwasaki
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Patent number: 5843907Abstract: 2-O-.alpha.-D-Glucopyranosyl-L-ascrobic acid is crystallizable in its supersaturated solution. Crystalline 2-O-.alpha.-D-glucopyranosyl-L-ascorbic acid is substantially nonhygroscopic, free flowing, free of deliquescence, consolidation and direct reducing activity, but is readily soluble in water. Because of these, crystalline 2-O-.alpha.-D-glucopyranosyl-L-ascorbic acid is handleable with an ease, and superiorly high in stability and physiological activities. Thus, crystalline 2-O-.alpha.-D-gluco-pyranosyl-L-acorbic acid is favorably useful in vitamin C-enriching agents, foodstuffs, pharmaceuticals and cosmetics.Type: GrantFiled: February 27, 1995Date of Patent: December 1, 1998Assignee: Kabushiki Kaisha Hayashibara Seibutsu Kagaku KenkyujoInventors: Shuzo Sakai, Masaru Yoneyama, Toshio Miyake
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Patent number: 5840919Abstract: Novel 1,2-dioxetanes with improved chemiluminescent properties, such as signal intensity, S/N ratio, T1/2, etc. are provided by spiroadamantyl 1,2-dioxetanes, wherein the remaining carbon atom of the ring bears an alkoxy, aryloxy, or arylalkoxy substituent, and either a phenyl or naphthyl ring, this aromatic ring bearing, at the meta position on the phenyl group, or a non-conjugated position on the naphthyl ring, a OX moiety wherein X is an enzyme-cleavable group, which when removed from the dioxetane, leaves the oxyanion which decomposies with chemiluminescence, the aryl ring further bearing an electron active substituent Z. The nature and placement of the Z substituent, at a position not adjacent the point of attachment to the dioxetane ring, strongly influences the properties of the dioxetane. Assays, as well as kits for the performance of those assays, include the dioxetane, an enzyme capable of cleaving the X group, and in certain cases, membranes and chemiluminscent enhancement agents.Type: GrantFiled: October 17, 1995Date of Patent: November 24, 1998
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Patent number: 5840881Abstract: A composition is disclosed comprising a water-insoluble or slightly water-soluble compound and a branched cyclodextrin-carboxylic acid. The branched cyclodextrin-carboxylic acid significantly increases the water-solubility of the compound. Also disclosed is a method of enhancing water-solubility of the compound.Type: GrantFiled: May 8, 1995Date of Patent: November 24, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Yoshiaki Uda, Takako Yamauchi, Yasushi Nakagawa, Toshihiro Ishiguro, Masahide Oka, Takamasa Yamaguchi, Ikuo Nogami
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Patent number: 5840861Abstract: New A83543 components, including fermentation products A83543K, A835430, A83543P, A83543U, A83543V, A83543W and A83543Y and N-demethyl derivatives, and salts thereof, are useful for the control of insects and mites. The pseudoaglycones of the new A83543 components are useful for the preparation of A83543 components. Methods are provided for making the new A83543 components by culturing of Saccharopolyspora spinosa NRRL 18395, NRRL 18537, NRRL 18538, or NRRL 18539, or NRRL 18743 or NRRL 18719 or NRRL 18823 in suitable culture medium. Insecticidal and ectoparasiticidal compositions containing new A83543 components are also provided.Type: GrantFiled: February 8, 1995Date of Patent: November 24, 1998Assignee: DowElancoInventors: Jon S. Mynderse, Mary C. Broughton, Walter M. Nakatsukasa, James A. Mabe, Jan R. Turner, Lawrence Creemer, Mary L. B. Huber, Herbert A. Kirst, James W. Martin
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Patent number: 5837689Abstract: Compounds that possess selectin binding activity are described that have a three-dimensionally stable configuration for sialic acid and fucose, or analogs, derivatives, or mimics of these groups, such that sialic acid and fucose or their mimics are separated by a linker that permits binding between those groups and the selecting, such compounds being represented by the following general structural formula I: ##STR1##Type: GrantFiled: February 21, 1996Date of Patent: November 17, 1998Assignee: Glycomed IncorporatedInventors: Mark B. Anderson, Daniel E. Levy, Peng Cho Tang, John H. Musser, Narasinga Rao
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Patent number: 5834437Abstract: The object of the present invention is to provide asiatic acid derivatives, its pharmaceutically acceptable salts or esters.Asiatic acid, its trisaccharide asiaticoside and mddecassic acid, extracted from Centella asiatica have been used for a long time in the management of skin scars and chronic ulcers. In this invention, asiatic acid derivatives synthesized from asiatic acid show excellent wound-healing properties.Type: GrantFiled: December 1, 1995Date of Patent: November 10, 1998Assignee: Dong Kook Pharmaceutical Co., Ltd.Inventors: Sang-Sup Jew, Hee-Doo Kim, Young-Hoon Jung, Eun-Hee Park, Sung-Ki Seo, Tae-Gyu Nam, Duc-Ky Hahn, Jae-Ho Park, Pil-Jong Sim, Min-Jung Lim, Kyung-Haw Lim
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Patent number: 5830872Abstract: Esters associating phenylacetic, 3-phenylpropionic, 4-phenylbutyric and n-butyric acids with Su(OH).sub.n monosaccharides or sugar alcohols, of general formula (I), in which the Su(OH).sub.n precursor is a monosaccharide or sugar alcohol, selected so that its structure or that of its derivatives ensures that internal interesterification does not take place either because the ester based on the general formula does not have a free hydroxyl grouping, or because with regard to the ester grouping, the free hydroxyl groupings are remotely located and/or badly aligned and/or bonded to a secondary carbon atom, and in which the Su(OH).sub.n monosaccharide or sugar alcohol is preferably D-mannose carrying the ester grouping on the anomeric carbon atom or else is a pentitol, for example, xylitol carrying the ester grouping on the C-1 primary carbon atom. These novel esters are useful as drugs, in particular in the treatment of haemoglobin diseases and premalignant or malignant tumours.Type: GrantFiled: March 11, 1997Date of Patent: November 3, 1998Assignee: L'Associazione di volontariato "Pro La Fondazione Futuro Senza Thalassemia"Inventors: Pierre Jean Baldwin, Olivier Claude Eric Douillet, Philippe Rene Michel Pouillart, Gino Lino Ronco, Pierre Joseph Villa
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Patent number: 5831080Abstract: The present invention relates to organosilicon compounds containing glycoside radicals, having units of the formula ##STR1## in which R is identical or different and represents a hydrogen atom or an organic radical,a is 0, 1, 2 or 3,b is 0, 1, 2 or 3 andR.sup.1 can be identical or different and represents a radical of the formulaZ--(R.sup.2 O).sub.c --R.sup.3 -- (II)in whichZ represents a glycoside radical which is built up from 1 to 10 monosaccharide units,R.sup.2 can be identical or different and represents an alkylene radical,c is 0 or a number from 1 to 20, andR.sup.3 represents an alkylene radical, with the proviso that the sum of a and b is less than or equal to 3 and the organosilicon compound comprising units of the formula (I) contains at least one radical R.sup.1 per molecule.Type: GrantFiled: April 22, 1996Date of Patent: November 3, 1998Assignee: Wacker-Chemie GmbHInventors: Johann Sejpka, Franz Wimmer
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Patent number: 5830873Abstract: A propiophenone derivative of the formula ?I!: ##STR1## wherein X is O, S or methylene, OY is a protected or unprotected OH, Z is .beta.-D-glucopyranosyl or 4-O-(.alpha.-D-glucopyranosyl)-.beta.-D-glucopyranosyl or wherein one or more hydroxy groups of these groups may optionally be acylated, and the dotted line means the presence or absence of a double bond, or a pharmaceutically acceptable salt thereof. Said compounds have excellent hypoglycemic activity so that they are useful in the prophylaxis or treatment of diabetes.Type: GrantFiled: April 27, 1995Date of Patent: November 3, 1998Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Kenji Tsujihara, Mitsuya Hongu, Nobuyuki Funami, Masanori Inamasu, Kenji Arakawa
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Patent number: 5830920Abstract: Compounds of the formula ##STR1## wherein n.sup.1 -n.sup.9 are each independently 0 or 1;m.sup.1 -m.sup.9 are each independently 0 or 1, but with the proviso that at least one of m.sup.1, m.sup.2 and m.sup.3, at least one of m.sup.4, m.sup.5 and m.sup.6 and, when present, at least one of m.sup.7, m.sup.8 and m.sup.9 is 1; and whereinX.sup.1 -X.sup.18 each independently is --O--, --CONR.sup.1,--NR.sup.1 CO-- or --NR.sup.1 --;R.sup.1 is hydrogen or lower alkyl;W is a benzene or s-triazine;Y.sup.1 -Y.sup.9 each independently is an aromatic ring systems;A.sup.1 -A.sup.3 each independently is a residue of a sugar alcohol devoid of the 1-hydroxy group or a derivative thereof, a residue of a sugar acid devoid of the 1-carboxy group or a derivative thereof or tris-(hydroxymethyl)-methyl;D is the di-residue of a sugar alcohol devoid of 2 hydroxy groups or a derivative thereof or the di-residue of a sugar dicarboxylic acid devoid of 2 carboxy group or a derivative thereof;Q.sup.1 -Q.sup.3 and Z.sup.Type: GrantFiled: April 26, 1996Date of Patent: November 3, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Chucholowski, Jurgen Fingerle, Niggi Iberg, Hans Peter Marki, Rita Muller, Michael Pech, Marianne Rouge, Gerard Schmid, Thomas Tschopp, Hans Peter Wessel
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Patent number: 5831044Abstract: A process for making glycosides having enhance color properties comprising the steps of: (a) reacting a reducing saccharide with excess fatty alcohol to obtain a glycoside reaction mixture; (b) adding an effective amount of an unsaturated aliphatic carboxylic acid, including hydroxy-substituted derivatives thereof and their salt, to the glycoside reaction mixture; and (c) evaporating excess fatty alcohol from the glycoside reaction mixture to form a glycoside mixture.Type: GrantFiled: February 5, 1996Date of Patent: November 3, 1998Assignee: Henkel CorporationInventors: Patrick M. McCurry, Jr., John Frederick Hessel