Cyclopentanohydrophenanthrene Ring System Patents (Class 536/5)
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Publication number: 20030129150Abstract: The invention relates to extracts of the plant Mourera fluviatilis and to cosmetic and/or pharmaceutical preparations that contain an extract of the plant Mourera fluviatilis.Type: ApplicationFiled: August 26, 2002Publication date: July 10, 2003Inventors: Gilles Pauly, Philippe Moser, Olga Freis
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Publication number: 20030125263Abstract: This invention discloses a method for preparing a therapeutic or diagnostic complex comprised of a nucleic acid ligand and a lipophilic compound or non-immunogenic, high molecular weight compound by identifying a nucleic acid ligand by SELEX methodology and associating the nucleic acid ligand with a lipophilic compound or a non-immunogenic, high molecular weight compound. The invention further discloses complexes comprising one or more nucleic acid ligands in association with a lipophilic compound or non-immunogenic, high molecular weight compound.Type: ApplicationFiled: September 30, 2002Publication date: July 3, 2003Applicant: GILEAD SCIENCES, INC.Inventors: Larry Gold, Paul G. Schmidt, Nebojsa Janjic
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Publication number: 20030118635Abstract: The present invention pertains to complexes comprising sterols and saponins. The complexes are capable of binding a genetic determinant including a polynucleotide. The complexes may further comprise a lipophilic moiety, optionally a lipophilic moiety comprising a contacting group and/or a targeting ligand, and/or a saccharide moiety. The complexes may further comprise an immunogenic determinant and/or an antigenic determinant and/or a medicament and/or a diagnostic compound. The complexes may in even further embodiments be encapsulated by an encapsulation agent including a biodegradable microsphere. The present invention also pertains to pharmaceutical compositions and methods of treatment of an individual by therapy and/or surgery, methods of cosmetic treatment, and diagnostic methods practised on the human or animal body.Type: ApplicationFiled: April 4, 2002Publication date: June 26, 2003Inventors: Kristian Dalsgaard, Nikolai Soren Kirkby
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Publication number: 20030087835Abstract: This invention relates to a group of novel sapogenins, their use in anti-cancer applications, and to a process for their production. More particularly, this invention pertains to a novel group of dammarane sapogenins, PAM-120, PBM-110 and PBM-100 (the dammarance sapogenine structure is specifically clean of any sugar moieties (glycons) at any position and hydroxyl at C-20) and PAN-20 and PAN-30 (the dammarance sapogenin structure has sugar moieties but is free of hydroxyl at C-20), obtained by chemical cleavage of dammarane saponins. The invention also includes a novel application of the said sapogenins for anti-cancer treatment by using them separately or together, and/or jointly with other drugs, as well as to the process of producing these novel sapogenins. Said novel dammarane sapogenins show surprising anti-cancer effect when applied, particularly against multi-drug resistant cancers.Type: ApplicationFiled: July 24, 2001Publication date: May 8, 2003Inventors: Dong Huang, Dong Feng Qi
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Publication number: 20030087836Abstract: This invention relates to a group of novel sapogenins, their use in anti-cancer applications, and to a process for their production. More particularly, this invention pertains to a novel group of dammarane sapogenins, PAM-120, PBM-110 and PBM-100 (the dammarance sapogenine structure is specifically clean of any sugar moieties (glycons) at any position and hydroxyl at C-20) and PAN-20 and PAN-30 (the dammarance sapogenin structure has sugar moieties but is free of hydroxyl at C-20), obtained by chemical cleavage of dammarane saponins. The invention also includes a novel application of the said sapogenins for anti-cancer treatment by using them separately or together, and/or jointly with other drugs, as well as to the process of producing these novel sapogenins. Said novel dammarane sapogenins show surprising anti-cancer effect when applied, particularly against multi-drug resistant cancers.Type: ApplicationFiled: October 19, 2001Publication date: May 8, 2003Inventors: Dong Huang, Dong Feng Qi
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Publication number: 20030064492Abstract: Linked nucleosides having at least one functionalized nucleoside that bears a substituent such as a steroid molecule, a reporter molecule, a non-aromatic lipophilic molecule, a reporter enzyme, a peptide, a protein, a water soluble vitamin, a lipid soluble vitamin, an RNA cleaving complex, a metal chelator, a porphyrin, an alkylator, a pyrene, a hybrid photonuclease/intercalator, or an aryl azide photo-crosslinking agent exhibit increased cellular uptake and other properties. The substituent can be attached at the 2′-position of the functionalized nucleoside via a linking group.Type: ApplicationFiled: May 23, 2002Publication date: April 3, 2003Applicant: Isis Pharmaceuticals, Inc.Inventors: Muthiah Manoharan, Phillip Dan Cook, Clarence Frank Bennett
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Publication number: 20030050229Abstract: A method and composition for treating a host infected with hepatitis C comprising administering an effective hepatitis C treatment amount of a described 1′, 2′ or 3′-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.Type: ApplicationFiled: May 23, 2001Publication date: March 13, 2003Inventors: Jean-Pierre Sommadossi, Paulo LaColla
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Publication number: 20030039977Abstract: Nucleosides and oligonucleosides functionalized to include carbamate functionality, and derivatives thereof. In certain embodiments, the compounds of the invention further include steroids, reporter molecules, reporter enzymes, lipophilic molecules, peptides or proteins attached to the nucleosides through the carbamate group.Type: ApplicationFiled: August 21, 2001Publication date: February 27, 2003Applicant: ISIS Pharmaceuticals, Inc.Inventors: Phillip Dan Cook, Muthiah Manoharan
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Publication number: 20030008834Abstract: The present invention relates to mononucleoside phosphate compounds that have the benefits of a dinucleotide pharmaceutical. These mononucleoside phosphates can be made from a mononucleotide that has been modified by attaching a degradation resistant substituent on the terminal phosphate of a polyphosphate mononucleotide. By attaching this degradation resistant substituent, the stability from degradation matches or exceeds those of certain dinucleotides.Type: ApplicationFiled: February 27, 2002Publication date: January 9, 2003Inventors: Benjamin R. Yerxa, James G. Douglass, Sammy Ray Shaver, Ward M. Peterson, Edward G. Brown, Christopher S. Crean
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Publication number: 20030004321Abstract: Novel analogs of fusidic acid are described with one or more carbohydrate units attached. Certain glycosylated analogs of fusidic acid have enhanced solubility properties in diluents or excipient of choice as compared to unmodified fusidic acid. Certain glycosylated analogs may be employed as chemotherapeutic agents and particular analogs may be useful for fighting anti-microbial infections.Type: ApplicationFiled: July 2, 2002Publication date: January 2, 2003Inventors: Roeland Tuinman, Masato Koreeda, Brian Keith Shull
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Publication number: 20020198174Abstract: Methods and ophthalmic compositions comprising a lipophilic drug in aqueous formulation with cyclodextrin or a cyclodextrin derivative.Type: ApplicationFiled: April 12, 2002Publication date: December 26, 2002Applicant: Allergan Sales, Inc.Inventor: Robert T. Lyons
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Publication number: 20020177150Abstract: Linked nucleosides having at least one functionalized nucleoside that bears a substituent such as a steroid molecule, a reporter molecule, a non-aromatic lipophilic molecule, a reporter enzyme, a peptide, a protein, a water soluble vitamin, a lipid soluble vitamin, an RNA cleaving complex, a metal chelator, a porphyrin, an alkylator, a pyrene, a hybrid photonuclease/intercalator, or an aryl azide photo-crosslinking agent exhibit increased cellular uptake and other properties. The substituent can be attached at the 2′-position of the functionalized nucleoside via a linking group.Type: ApplicationFiled: February 11, 2002Publication date: November 28, 2002Applicant: ISIS Pharmaceutical, Inc.Inventors: Muthiah Manoharan, Phillip Dan Cook, Clarence Frank Bennett
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Publication number: 20020160396Abstract: The present invention provides a labeled nucleotide having formula: 1Type: ApplicationFiled: January 14, 2002Publication date: October 31, 2002Inventors: Hendrick Jan Houthoff, Jan Reedijk, Tinka Jelsma, Robert Jochem Heetebrij, Herman Hendricus Volkers
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Patent number: 6462182Abstract: Novel analogs of fusidic acid are described with one or more carbohydrate units attached. Certain glycosylated analogs of fusidic acid have enhanced solubility properties in diluents or excipient of choice as compared to unmodified fusidic acid. Certain glycosylated analogs may be employed as chemotherapeutic agents and particular analogs may be useful for fighting anti-microbial infections.Type: GrantFiled: July 14, 2000Date of Patent: October 8, 2002Assignee: The University of MichiganInventors: Roeland Tuinman, Masato Koreeda, Brian Keith Shull
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Publication number: 20020128210Abstract: Methods of treating a fungal or yeast infection and of killing or inhibiting fungi or yeast are disclosed. The methods use derivatives of triterpenes that are abundant in birch bark and other plants. The triterpenes include betulin, allobetulin, and lupeol.Type: ApplicationFiled: October 1, 2001Publication date: September 12, 2002Inventors: Pavel A. Krasutsky, Robert M. Carlson, Raj Karim
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Publication number: 20020107209Abstract: A method of treating polycystic kidney disease is described. The method involves administering soyasaponin Bb to an animal in need thereof.Type: ApplicationFiled: September 28, 2001Publication date: August 8, 2002Inventors: Bruce J. Holub, F. William Collins, Dominique P. Bureau, Diana J. Philbrick
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Publication number: 20020082433Abstract: Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering derivatives of 2-methoxyestradiol of the general formula: 1Type: ApplicationFiled: August 24, 2001Publication date: June 27, 2002Inventors: Gregory E. Agoston, Jamshed H. Shah, Kimberly A. Hunsucker, Victor S. Pribluda, Theresa M. LaVallee, Shawn J. Green, Christopher J. Herbstritt, Xiaoguo H. Zhan, Anthony M. Treston
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Patent number: 6392069Abstract: This invention provides methods and compositions for enhancing transfer of an agent into a cell. The agents can include polypeptides, polynucleotides such as genes and antisense nucleic acids, and other molecules. In some embodiments, the agents are modulating agents that can modulate a cellular activity or function when introduced into the cell. The methods and compositions are useful for introducing agents into individual cells, as well as cells that are present as a tissue or organ.Type: GrantFiled: July 8, 1998Date of Patent: May 21, 2002Assignee: Canji, Inc.Inventors: Heidrun Engler, Tattanahalli L. Nagabhushan, Stephen Kenneth Youngster
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Patent number: 6376657Abstract: A pharmaceutical composition which contains an extract obtainable from a plant of the genus Trichocaulon or Hoodia containing an appetite suppressant agent having the formula (1). A process for obtaining the extract and a process for synthesizing compound (1) and its analogues and derivatives is also provided. The invention also extends to the use of such extracts and compound (1) and its analogues for the manufacture of medicaments having appetite suppressant activity. The invention further provides novel intermediates for the synthesis of compound (1).Type: GrantFiled: October 13, 1999Date of Patent: April 23, 2002Assignee: CSIRInventors: Fanie Retief Van Heerden, Robert Vleggaar, Roelof Marthinus Horak, Robin Alec Learmonth, Vinesh Maharaj, Rory Desmond Whittal
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Patent number: 6368831Abstract: A method of treating a hyperproliferative disorder in a subject in need of such treatment, comprising administering to said subject, in combination, a treatment effective amount of: (a) a ceramide-generating retinoid such as fenretinide or a pharmaceutically acceptable salt thereof; and (b) at least one (and in certain embodiments at least two) ceramide degredation inhibitor, such as compounds selected from the group consisting of (i) glucosylceramide synthesis inhibitors and/or 1-acylceramide synthesis inhibitors, (ii) sphingosine-1-phosphate synthesis inhibitors, and (iii) protein kinase C inhibitors. A preferred glucosyl ceramide synthesis inhibitor is 1-phenyl-2-palmitoylamino-3-morpholino-1-propanol. A preferred sphingosine-1-phosphate synthesis inhibitor is D-erythro-N,N-dimethylsphingosine. A preferred protein kinase C inhibitor is L-threo-dihydrosphingosine.Type: GrantFiled: December 23, 1999Date of Patent: April 9, 2002Assignee: Childrens Hospital Los AngelesInventors: Barry J. Maurer, C. Patrick Reynolds
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Publication number: 20020028919Abstract: Novel xylo nucleoside or xylo nucleotide analogs, polynucleotides comprising xylo nucleotide substitution, processes for their synthesis and incorporation into polynucleotides.Type: ApplicationFiled: September 21, 2001Publication date: March 7, 2002Applicant: Ribozyme Pharmaceuticals, Inc.Inventors: Jasenka Matulic-Adamic, Leonid Beigelman
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Publication number: 20010041676Abstract: Serum levels of therapeutically useful glucocorticosteroids are substantially increased by oral administration of the corresponding glycoside or orthoester glycoside.Type: ApplicationFiled: January 16, 2001Publication date: November 15, 2001Inventors: Michael F. Holick, Halasya Ramanathan
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Patent number: 6306376Abstract: Arbutin monoesters are employed in a composition for topical application, as a depigmenting and/or bleaching agent for human skin, hair and/or head hair. The invention relates to a method of manufacturing a composition of at least one arbutin monoester in a physiologically acceptable medium for depigmenting and/or bleaching human skin, hair and/or head hair.Type: GrantFiled: July 8, 1998Date of Patent: October 23, 2001Assignee: L'OrealInventor: Michel Philippe
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Patent number: 6280777Abstract: A soya extract having a content of glucoside isoflavones of at least 13% by weight and a content of 0.6 to 1.5 parts by weight of group 3 soya saponins per 1 part by weight of glucoside isoflavones. Also, pharmaceutical compositions containing this extract and methods of administering the extract to treat conditions such as pre- or post-menopausal symptoms, cancer, such as breast or prostate cancer, or alcoholism. The extracts are made by a process which includes the steps of treating ripe whole soya beans or oil-free soya flour with an aliphatic alcohol to obtain a first extract; concentrating the first extract to form a concentrated first extract; purifying the concentrated first extract by treatment with at least one aliphatic hydrocarbon; and extracting active components from the purified concentrated first extract with a water-immiscible aliphatic alcohol to obtain a second extract. Preferably, the final extract is concentrated dried to form the desired soya extract.Type: GrantFiled: January 28, 2000Date of Patent: August 28, 2001Assignee: Indena S.p.A.Inventors: Ezio Bombardelli, Bruno Gabetta
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Patent number: 6274558Abstract: A method of treating cardiac malfunction by administering a positive inotropic effect-producing amount of Hypothalamic Inhibitory factor (HIF).Type: GrantFiled: September 19, 1997Date of Patent: August 14, 2001Assignee: The General Hospital CorporationInventor: Garner Haupert, Jr.
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Patent number: 6274559Abstract: Compositions and methods of treating or preventing hepatotoxicity utilizing asiatic acid derivatives of Formula 1 are disclosed.Type: GrantFiled: August 27, 1999Date of Patent: August 14, 2001Assignee: Dong Kook Pharmaceutical Co., Ltd.Inventors: Sang Sup Jew, Hyeung Geun Park, Hee Doo Kim, Young Hoon Jung, Young Choong Kim, Hong Pyo Kim, Mi Kyeong Lee, Hee Sung Choi, Eung Seok Lee, Chi Hyoung Yoo, Doo Yeon Lim, Jeong Hoon Kim, Hee Man Kim
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Patent number: 6262029Abstract: The present invention is directed to novel bidesmosidic saponin derivatives comprising a triterpene aglycone core substituted at positions 3 and 28 with a monosaccharide or an oligosaccharide which can be the same or different, and having an aldehyde group attached to the core, preferably at the 4-position. The novel derivatives include a lipophilic group that is covalently attached to the 4-position of a fucosyl group that is required in the 28-oligosaccharide substituent. These derivatives preferably have Formula I: wherein Z and R1 to R3 are defined herein. The present invention is also directed to pharmaceutical and veterinary compositions comprising one or more compounds of the present invention. These compositions may be employed as immunopotentiators in animals and humans. The present invention is also directed to methods of making these compounds and to methods of using these compounds as immunostimulating agents and as adjuvants.Type: GrantFiled: August 13, 1999Date of Patent: July 17, 2001Assignee: Galenica Pharmaceuticals, Inc.Inventors: Jeffery B. Press, Dante J. Marciani
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Publication number: 20010007859Abstract: This invention provides 5&agr;-pregnane-3,&bgr;,(20S), 21-triol, 20-O-&bgr;-glucuronide and 5&agr;-pregnane-3&bgr;,20R-diol, 20-O-&bgr;-glucuronide and pharmaceutically acceptable salts thereof which are useful as progestational agents.Type: ApplicationFiled: October 8, 1999Publication date: July 12, 2001Inventors: CHRISTOPHER P. MILLER, BACH D. TRAN, MICHAEL D. COLLINI
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Patent number: 6150336Abstract: The invention relates to certain steroidal glycoside derivatives useful as hypocholesterolemic agents and anti-atherosclerosis agents. The present invention is also directed to pharmaceutical compositions comprising such derivatives and use of such derivatives in treating hypercholesterolemia or atherosclerosis.Type: GrantFiled: November 21, 1997Date of Patent: November 21, 2000Assignee: Pfizer Inc.Inventors: Michael P. Deninno, Peter A. McCarthy
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Patent number: 6103884Abstract: Novel analogs of fusidic acid are described with one or more carbohydrate units attached. Certain glycosylated analogs of fusidic acid have enhanced solubility properties in diluents or excipient of choice as compared to unmodified fusidic acid. Certain glycosylated analogs may be employed as chemotherapeutic agents and particular analogs may be useful for fighting anti-microbial infections.Type: GrantFiled: March 27, 1996Date of Patent: August 15, 2000Assignee: The University of MichiganInventors: Masato Koreeda, Roeland Tuinman, Brian Keith Shull
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Patent number: 6093805Abstract: Novel glycosides, especially steroidal and non-steroidal glycosides are provided. The steroidal and non-steroidal glycosides preferably are prepared from aglycons which possess valuable properties such as pharmacological properties. The glycosides are prepared from useful aglycons and possess useful properties which are the same as those of their respective unglycosylated aglycons. The glycosides are provided in acylated and deacylated form. The acylated glycosides after hydrolysis of the acyl groups possess enhanced water solubility properties, as illustrated in the case where the aglycon is acetominophen.Type: GrantFiled: August 21, 1997Date of Patent: July 25, 2000Assignee: The Regents of the University of MichiganInventors: Brian K. Shull, Roeland J. Tuinman, Todd A. Houston, R. Erich Klemke, Masato Koreeda
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Patent number: 6080725Abstract: The present invention is directed to vaccines comprising (1) one or more bacterial, viral or tumor-associated antigens; and (2) one or more saponin-lipophile conjugate in which a lipophilic moiety such as a lipid, fatty acid, polyethylene glycol or terpene is covalently attached to a non-acylated or desacylated triterpene saponin via a carboxyl group present on the 3-O-glucuronic acid of the triterpene saponin. The attachment of a lipophile moiety to the 3-O-glucuronic acid of a saponin such as Quillaja desacylsaponin, lucyoside P, or saponin from Gypsophila, Saponaria and Acanthophyllum enhances their adjuvant effects on humoral and cell mediated immunity. Additionally, the attachment of a lipophile moiety to the 3-O-glucuronic acid residue of non- or des-acylsaponin yields a saponin analog that is easier to purify, less toxic, chemically more stable, and possesses equal or better adjuvant properties than the original saponin.Type: GrantFiled: April 13, 1999Date of Patent: June 27, 2000Assignee: Galenica Pharmaceuticals, Inc.Inventor: Dante J. Marciani
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Patent number: 6075132Abstract: Disclosed are ursodeoxycholic acid derivatives having an increased solubility in water, and methods for producing the derivatives. To produce the derivatives, ursodeoxycholic acid is protected at its carboxyl group with a benzyl group, then reacted with tetrabenzyl-acetic acid-oxyglucoside of the following formula (1), and de-benzylated; or ursodeoxycholic acid is protected at its hydroxyl group with a t-butyldimethylsilyl group, then reacted with tetrabenzyl-2-hydroxyethyloxyglucoside of the following formula (2), and de-t-butyldimethylsilylated and de-benzylated.Type: GrantFiled: April 30, 1998Date of Patent: June 13, 2000Assignees: Bio Research Corporation of Yokohama, Ensuiko Sugar Refining Co., Ltd., Kaken Pharmaceutical Co., Ltd.Inventors: Tadakatsu Mandai, Hiroshi Okumoto, Katsuyoshi Nakanishi, Koji Hara, Katsuhiko Mikuni, Kozo Hara, Teruhiko Umetsu
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Patent number: 6075139Abstract: Sucrose ester and ether products, useful as food or beverage bulking agents, reduced calorie sweeteners, fat replacement agents, stabilizing agents, thickening agents and emulsifying agents; adhesives; biodegradable plastics and films; sizing agents for paper and textiles; ethical pharmaceuticals and new fibers are prepared by using a two-phase reaction system in which sucrose is dissolved in an alkaline, aqueous solution and an acidic reagent such as a bifunctional acid dichloride or epoxide is added to the sucrose in a water-immiscible organic solvent. Several types of products are produced: water-insoluble sucrose ester (ether) copolymers; water-soluble sucrose ester (ether) copolymers; sucrose ester (ether) dimers; and intramolecular, cyclic sucrose esters (ethers). These products can be further varied by using different kinds of acid dichlorides or epoxides that contain different kinds of functional groups.Type: GrantFiled: July 24, 1996Date of Patent: June 13, 2000Assignee: Iowa State University Research Foundation, Inc.Inventors: John F. Robyt, Rupendra Mukerjea
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Patent number: 6027732Abstract: Lipid-containing particles such as iscoms, iscom-matrix or vesicles such as micelles or liposomes that comprise one or more hydrophobic receptor molecules for targeting and antigenic substances, which receptor molecules have been integrated in the particle and are chosen from lipid-containing receptors or receptors that are hydrophobic, which receptor molecules bind to the antigenic substances.Type: GrantFiled: September 17, 1998Date of Patent: February 22, 2000Inventors: Bror Morein, Karin Lovgren Bengtsson, Jill Ekstrom
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Patent number: 6017906Abstract: The present invention relates to methods of preventing or treating an infection or disease caused by an infectious agent. The present invention also relates to the augmentation of the efficacy of existing anti-infective agents by the co-administration of the compounds described herein.Type: GrantFiled: May 5, 1998Date of Patent: January 25, 2000Assignee: Intercardia, Inc.Inventors: Clifford S. Mintz, Natan A. Kogan, Ramesh Kakarla, Helena R. Axelrod, Michael J. Sofia
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Patent number: 5977081Abstract: The present invention is directed to novel chemical compounds in which a lipophilic moiety such as a lipid, fatty acid, polyethylene glycol or terpene is covalently attached to a non-acylated or desacylated triterpene saponin via a carboxyl group present on the 3-O-glucuronic acid of the triterpene saponin. The attachment of a lipophile moiety to the 3-O-glucuronic acid of a saponin such as Quillaja desacylsaponin, lucyoside P, or saponin from Gypsophila, Saponaria and Acanthophyllum enhances their adjuvant effects on humoral and cell mediated immunity. Additionally, the attachment of a lipophile moiety to the 3-O-glucuronic acid residue of non- or des-acylsaponin yields a saponin analog that is easier to purify, less toxic, chemically more stable, and possesses equal or better adjuvant properties than the original saponin.Type: GrantFiled: May 20, 1998Date of Patent: November 2, 1999Assignee: Galenica Pharmaceuticals, Inc.Inventor: Dante J. Marciani
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Patent number: 5948405Abstract: Fucans with low molecular weight having anticoagulant, antithrombinic and antithrombotic activity.Fucan sulfates having molecular weight between 14000 and 29000 Dalton show a remarkable anticoagulant activity both in the global coagulation mechanism (APTT) and in the last phase of coagulation (antithrombinic activity). These compounds are useful also as antithrombotic drugs.Type: GrantFiled: December 18, 1997Date of Patent: September 7, 1999Assignee: Crinos Industria Farmacobiologica S.p.A.Inventors: Armando Cedro, Roberto Porta, Franco Cattaneo, Fabio Trento, Laura Ferro, Ennio Lanzarotti
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Patent number: 5945404Abstract: A glycoside represented by formula (I), wherein dexamethasone or betamethasone is the aglycon and the 21-position is substituted by a simple sugar or an acylated sugar selected from the group consisting of glucose, galactose, mannose, rhamnose, fucose, N-acetylglucosamine, N-acetylgalactosamine, galacturonic acid, glucuronic acid and sialic acid.Type: GrantFiled: September 10, 1997Date of Patent: August 31, 1999Assignee: Nissin Shokuhin Kabushiki KaishaInventors: Kei Sugai, Motoaki Goto, Satoshi Yoshida, Yumiko Noda, Takayuki Ishii, Nobuyuki Kibushi, Hutoshi Nishikawa
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Patent number: 5925537Abstract: According to this invention, Prevotella sp. S-1 strain (Bacteroidaceae family, KFCC-10923) is cultured in a medium supplemented with Panax ginseng saponin so as to collect the metabolites of saponin generated and accumulated in the medium, thus ensuring their selective production with high efficiency.This invention related to a process for the preparation of the metabolites of protopanaxadiol saponin, wherein Prevotella sp. S-1 strain (Bacteroidaceae family, KFCC-10923), is cultured at a medium supplemented with Panax ginseng saponin and then, the metabolites of protopanaxadiol saponin contained in the medium--20-O-.beta.-D-glucopyranosyl-20(s)-protopanaxadiol, 20-O-?.alpha.-L-arabinopyranosyl-20(s)-protopanaxadiol, and 20-0-?.alpha.-L-arabinopuranosyl(1.fwdarw.6)-.beta.-D-glucopyranosyl!-20(s )-protopanaxadiol --are generated and accumulated for collecting them thereof.Type: GrantFiled: December 1, 1997Date of Patent: July 20, 1999Assignees: Il Hwa Co., Ltd., Happy World Inc.Inventors: Jong Hwan Sung, Jae Doo Huh, Hideo Hasegawa, Satoshi Matsumiya, Masamori Uchiyama
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Patent number: 5908833Abstract: Novel compounds which are a glucocorticosteroid (GCS) chemically bound to a sugar, having the general formulaGCS.sup.1 --O--Sugar.sup.1for colon- or ileum-specific delivery of the GCS to inflamed bowel mucosa, as well as processes for their preparation, pharmaceutical preparations containing the compounds and the use of said compounds in therapy.Type: GrantFiled: December 13, 1996Date of Patent: June 1, 1999Assignee: Aktiebolaget AstraInventors: Ralph Lennart Brattsand, Peter Edman, Thomas Hogberg, Stinabritt Nilsson, Bror Arne Thalen, Jan Erik Ulmius
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Patent number: 5874423Abstract: A human cataractous lens nuclei methanolic extract characterized in that it comprises substances having a molecular weight lower than 3000 daltons, inhibiting ATP hydrolysis by Na.sup.+,K.sup.+ -ATPase having affinity to the ouabain binding site on the enzyme and cross-reacting with an antibody directed against digoxin. Compounds of the general formula are disclosed: ##STR1## or of the general formula: ##STR2## in which R is hydrogen, an amino acid, a di- or tripeptide or a mono-, di- or trisaccharide. Pharmaceutical preparations and methods of using the compounds are also disclosed.Type: GrantFiled: September 12, 1996Date of Patent: February 23, 1999Assignee: Yissum Research Development Co. of the Hebrew University of JerusalemInventors: David Lichtstein, Joseph Deutsch, Irit Gati
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Patent number: 5872103Abstract: Methods for the prevention of neoplasms by treatment with cardiac glycosides are described. Individuals at a high risk of developing neoplasia or cancer may be treated with a therapeutically effective dose of a cardiac glycoside prophylactically. Individuals who convert cardiac glycosides to inactive metabolites may be treated with a modified regimen which prevents inactivation of the drug.Type: GrantFiled: March 19, 1991Date of Patent: February 16, 1999Inventor: Dino A. Belletti
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Patent number: 5864022Abstract: The present invention relates to a process for the preparation and manufacture of 3-amino-substituted glycosylated bile acid derivatives. Intermediates and related compounds are also disclosed. In particular, the present invention permits the conversion of cholic acid esters to the 3-amino-7,12-bis(glucosyl)cholic acid esters via an azide intermediate. Conditions for the purification and isolation of the desired product is also disclosed to provide an overall manufacturing process suitable for large-scale production.Type: GrantFiled: March 24, 1997Date of Patent: January 26, 1999Assignee: Intercardia, Inc.Inventors: Anna K. Chen, Ramesh Kakarla, Dashan Liu, Michael J. Sofia, Thomas C. Zebovitz
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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: 5852182Abstract: Nucleosides and linked nucleosides functionalized to include alkylthiol chemical functionality at ribofuranosyl positions, nucleosidic base positions, or on internucleoside linkages. In certain embodiments, the compounds of the invention further include steroids, reporter molecules, reporter enzymes, lipophilic molecules, peptides or proteins attached to the nucleosides through the alkylthio group.Type: GrantFiled: June 2, 1995Date of Patent: December 22, 1998Assignee: ISIS Pharmaceuticals Inc.Inventors: Phillip Dan Cook, Muthiah Manoharan
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Patent number: 5849889Abstract: The present invention relates to new 14-aminosteroids, pharmaceutical compositions containing the new compounds and methods of treatment for humans or other mammals afflicted with congestive heart failure.Type: GrantFiled: February 20, 1997Date of Patent: December 15, 1998Assignee: The Procter & Gamble CompanyInventors: Paul Michael Dybas, Roland Norman Johnson, Randy Stuart Muth, Song Liu, David Edward Portlock
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Patent number: 5843670Abstract: As a novel digoxigenin derivative which makes the labeling procedure simple, can be used to label a naturally-occurring nucleic acid, and enables highly sensitive assay, carbodiimide group-containing digoxigenin derivative represented by the following formula is used as the label in a nucleic acid detection method or immunoassay.Type: GrantFiled: April 22, 1997Date of Patent: December 1, 1998Assignee: Nisshinbo Industries, Inc.Inventors: Osamu Suzuki, Gen Masuda, Namiko Shiohata, Kazuko Matsumoto
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Patent number: 5804562Abstract: Crystalline spirostanyl glycosides and processes for making them are disclosed. The crystalline spirostanyl glycosides are useful for treatment of hypercholesterolemia or atherosclerosis.Type: GrantFiled: May 1, 1997Date of Patent: September 8, 1998Assignee: Pfizer Inc.Inventors: Douglas John Allen, Richard A. Buzon, Michael P. Deninno, Harry Austin Watson, Jr., Jonathan B. Zung
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Patent number: 5804563Abstract: The invention is directed to synthetic receptor(s) which comprises a polyfunctional organic template covalently linked to two or more oligomers which may independently be the same or different and may independently be straight chain or branched. The template may be linked to an identifier which uniquely defines the synthetic receptor. The identifier is a stable chemical molecule or a plurality of stable chemical molecules distinguishable and detectable to picomolar levels or may be an oligonucleotide. In an preferred embodiment, the template is covalently linked to a solid support which is linked to an identifier.Type: GrantFiled: April 8, 1996Date of Patent: September 8, 1998Assignee: The Trustees of Columbia University in The City of New YorkInventors: W. Clark Still, Ge Li