Oxygen Of The Saccharide Radical Bonded To A Nonsaccharide Hetero Ring By Acyclic Carbon Bonding Patents (Class 514/32)
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Patent number: 6887854Abstract: Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.Type: GrantFiled: May 13, 2003Date of Patent: May 3, 2005Assignee: Mallinckrodt Inc.Inventors: Samuel Achilefu, Hermo N. Jimenez, Raghavan Rajagopalan, Richard B. Dorshow, Joseph E. Bugai
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Patent number: 6852484Abstract: The present inventors have discovered that Asparagine Synthase is essential for fungal pathogenicity. Specifically, the inhibition of Asparagine Synthase gene expression in fungi results in no signs of successful infection or lesions. Thus, Asparagine Synthase can be used as a target for the identification of antibiotics, preferably antifungals. Accordingly, the present invention provides methods for the identification of compounds that inhibit Asparagine Synthase expression or activity. The methods of the invention are useful for the identification of antibiotics, preferably antifungals.Type: GrantFiled: December 10, 2001Date of Patent: February 8, 2005Assignee: Icoria, Inc.Inventors: Sze-Chung Lo, Maria Victoria Montenegro-Chamorro, Sheryl Frank, Blaise Darveaux, Sanjoy Mahanty, Ryan Heiniger, Amy Skalchunes, Huaqin Pan, Rex Tarper, Jeffrey Shuster, Matthew M. Tanzer, Lisbeth Hamer, Kiichi Adachi, Todd M. DeZwaan
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Patent number: 6849607Abstract: Purpurin-carbohydrate conjugates and their method of preparation and use for treatment of cancer cells. The conjugates have the general formula: wherein R6 and R7 taken together are ?NR11 or are independently —OR11, where at least one R11 is preferably a mono or polysaccharide moiety and R1-R8 are various groups formed from carbon and hydrogen and optionally oxygen and nitrogen where R3 and R4 may together from a covalent bond.Type: GrantFiled: May 7, 2002Date of Patent: February 1, 2005Assignee: Health Research, Inc.Inventors: Ravindra K. Pandey, Thomas J. Dougherty
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Patent number: 6833445Abstract: Provided are reagents and methods useful for the synthesis of guanidinylated compounds. Also provided are methods for assaying molecules, including guanidinylated molecules that modulate viral infection and replication.Type: GrantFiled: January 21, 2003Date of Patent: December 21, 2004Assignee: The Regents of the University of CaliforniaInventors: Murray Goodman, Yitzhak Tor, Tracy Baker, Nathan Luedtke
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Patent number: 6833362Abstract: A composition for accelerating the disposal of ethanol from bodily fluid. Certain additives can accelerate the metabolic oxidation of ethanol, and others in addition act as catalysts or “pseudo” enzymes for the oxidation. Additives include the oxidant Nicotinamide Adenine Dinucleotide and a variety of other additives such as transition metal ions and complexes thereof which favor the oxidation reaction. The compositions described can act as a sobriety inducer and/or as an effective palliative for the unpleasant effects of overuse of ethanol.Type: GrantFiled: June 7, 2001Date of Patent: December 21, 2004Inventors: Ward Beryl Bowen, Jr., Daniel Salman Daniel
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Publication number: 20040109902Abstract: Aqueous preparations of substantially equimolor amounts of a zinc salt and clindamycin phosphate form a polymer useful in the topical treatment of acne and rosacea, with very low systemic levels of clindamycin.Type: ApplicationFiled: January 28, 2004Publication date: June 10, 2004Inventors: Emma Louise McDonagh, Rebecca Louise Kanis
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Patent number: 6716421Abstract: This invention relates to devices, kits, and methods for eliminating termite colonies. The kits, devices, and methods employ a termiticidal bait matrix containing a) a termiticide selected such that the termiticide causes death to about 50 to about 100% of termites within about 24 to about 84 days after the termites begin to ingest the termiticide or the bait matrix comprising the termiticide, b) a cellulose containing material, and c) water. The termiticidal bait matrix can be used in a bait station installed in the ground. The kits are suitable to be used by consumers in their homes.Type: GrantFiled: March 5, 2001Date of Patent: April 6, 2004Assignee: University of Florida Research Foundation, Inc.Inventors: Philip Frederick Brode, III, Garry Steven Garrett, Leo Timothy Laughlin, Randall Stryker Matthews, Dale Edwin Barker, Daniel James Kinne, Gary Eugene McKibben, Christopher Miles Miller, Timothy Robert Probst
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Patent number: 6608103Abstract: This invention relates to an inhibitor having inhibitory activity against neovasculation, cell multiplication, lumen formation and fibroblast growth factor which comprises &bgr;-, &ggr;- or &dgr;-tocotrienol.Type: GrantFiled: February 1, 2002Date of Patent: August 19, 2003Assignees: Fuji Chemical Industry Co., Ltd.Inventors: Teruo Miyazawa, Heiji Ikushima
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Patent number: 6538027Abstract: This invention provides compositions for repelling insects, particularly biting insects, such as mosquitoes, ticks, and biting flies comprising ratite oil, active fractions of ratite oil obtained by flash chromatography or compositions comprising mixtures of fatty acids found in ratite oil. Also provided are compositions for repelling insects comprising ratite oil, active fractions of ratite oil or compositions comprising mixtures of fatty acids found in ratite oil further comprising at least one additional insect repellent. Methods of repelling insects, particularly biting insects, are provided comprising topically applying ratite oil, active fractions of ratite oil, or compositions comprising mixtures of fatty acids found in ratite oil; or ratite oil, active fractions thereof, or compositions comprising fatty acids found in ratite oil and further comprising at least one additional insect repellent.Type: GrantFiled: February 15, 2001Date of Patent: March 25, 2003Assignee: AgraQuest, Inc.Inventors: Denise C. Manker, Pamela Gail Marrone, Stephen Judd
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Patent number: 6525182Abstract: Provided are reagents and methods useful for the synthesis of guanidinylated compounds. Also provided are methods for assaying molecules, including guanidinylated molecules that modulate viral infection and replication.Type: GrantFiled: January 22, 2001Date of Patent: February 25, 2003Assignee: Regents of the University of CaliforniaInventors: Murray Goodman, Yitzhak Tor, Tracy Baker, Nathan Luedtke
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Patent number: 6518250Abstract: An agent for preventing and curing the hindrance of ischemic reperfusiton is disclosed which has as an active component thereof a chromanol glycoside represented by the following general formula: [wherein R1, R2, R3, and R4 independently denote a hydrogen atom or a lower alkyl group, R5 denotes a hydrogen atom, a lower alkyl group, or a lower acyl group, X denotes a monosaccharide residue or an oligosaccharide residue which may have a lower alkyl group or a lower acyl group substituted for the hydrogen atom of the hydroxyl group of the saccharide residue, n denotes an integer of 0-6, and m denotes an integer of 1-6]. The agent, even in a small dosage, acts safely and effectively on the affected part and allows the hindrances of ischemic reperfusion induced in heart, stomach, small intestine, liver, spleen, kidney, brain, and skin, and the hindrance induced during the transplantation of an internal organ to be prevented and cured.Type: GrantFiled: November 14, 2001Date of Patent: February 11, 2003Assignee: CCI CorporationInventors: Toshikazu Yoshikawa, Hironobu Murase, Norimasa Yoshida
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Patent number: 6506734Abstract: The present invention relates to glycoconjugates of 20(S)-camptothecin, in which a 3-O-methylated &bgr;-L-fucose unit is linked to the 20-hydroxyl group of a camptothecin derivative via a thiourea-modified peptide spacer. The invention furthermore relates to processes for the preparation of the compounds according to the invention and to their use as medicaments, in particular in connection with oncoses.Type: GrantFiled: October 27, 1999Date of Patent: January 14, 2003Assignee: Bayer AktiengesellschaftInventors: Hans-Georg Lerchen, Karsten von dem Bruch, Jörg Baumgarten, Michael Sperzel
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Patent number: 6492335Abstract: The present invention relates to glycoconjugates of camptothecin derivatives in which at least one carbohydrate component is linked via suitable spacers with the 20-hydroxyl group of a camptothecin derivative. The invention furthermore relates to processes for preparing the compounds according to the invention and to their use as medicaments, in particular in connection with cancer.Type: GrantFiled: March 24, 1999Date of Patent: December 10, 2002Assignee: Bayer AktiengesellschaftInventors: Hans-Georg Lerchen, Karsten von dem Bruch, Jörg Buamgarten, Michael Sperzel
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Patent number: 6486129Abstract: The present invention relates to compounds of formula (1), wherein R1 is phenyl, naphthyl, 1,2,3,4-tetrahydronaphthyl, (iso)quinolinyl, tetrahydro(iso)quinolinyl, 3,4-dihydro-1H-isoquinolinyl, chromanyl or the camphor group, which groups may optionally be substituted with one or more substitutents selected from (1-8C)alkyl or (1-8C)alkoxy; R2 and R3 are independently H or (1-8C)alkyl; R4 is (1-8C)alkyl or (3-8C)cycloalkyl; or R3 and R4 together with the nitrogen atom to which they are bonded are a nonaromatic (4-8)membered ring optionally containing another heteroatom, the ring optionally being substituted with (1-8C)alkyl or SO2-(1-8C)alkyl; Q is a spacer having a chain length of 10 to 70 atoms; and Z is a negatively charged oligosaccharide residue comprising two to six monosaccharide units, the charge being compensated by positively charged counterions; or a pharmaceutically acceptable salt thereof or a prodrug thereof.Type: GrantFiled: December 18, 2000Date of Patent: November 26, 2002Assignees: Akzo Nobel N.V., University LeidenInventors: Cornelia Maria Tromp, Johannes Egbertus Maria Basten, Constant Adriaan Anton van Boeckel, Rogier Christian Buijsman
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Publication number: 20020155141Abstract: An antifungal composition suitable for parenteral administration to a mammal includes an amount of pimaricin or an antifungal derivative thereof that is effective to inhibit the growth of a fungal infection in a mammal; a pharmaceutically acceptable dipolar aprotic solvent; and a pharmaceutically acceptable aqueous secondary solvent. The composition can be used in methods of preventing or treating a systemic fungal infection in a mammal. The composition can be prepared by dissolving pimaricin or an antifungal derivative thereof in the pharmaceutically acceptable dipolar aprotic solvent; adding to the solution a pharmaceutically acceptable aqueous secondary solvent; and in a preferred method, by subsequently lypohilizing the composition, whereby a dry, shelf-stable composition is produced. This dry composition can be reconstituted into an aqueous solution suitable for parenteral administration.Type: ApplicationFiled: October 8, 1999Publication date: October 24, 2002Inventor: BORJE S. ANDERSSON
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Patent number: 6290929Abstract: This invention is a method of treating cancer, including carcinomas and sarcomas, through the administration of a pharmaceutical composition containing an arylaldehyde 5-oxo-1,2,4-triazine hydrazide derivative. The arylaldehyde 5-oxo-1,2,4-triazine hydrazide derivative is selected from the group consisting of those with the formula: wherein R and R1 are independently selected from the group consisting of hydrogen and alkyl wherein the alkyl group has up to 7 carbon atoms; or a pharmaceutical salt thereof; a prodrug thereof; a metabolite thereof; and mixtures thereof. Pharmaceutical compositions comprising these compounds and their use in various treatment methods are claimed. The compounds can be used in conjunction with other chemotherapeutic agents and potentiators.Type: GrantFiled: July 28, 2000Date of Patent: September 18, 2001Assignee: The Procter & Gamble CompanyInventor: James Berger Camden
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Patent number: 6239114Abstract: Compositions and methods for the prevention and treatment of neoplastic diseases are described. Individuals at a high risk of developing or having neoplasia undergoing conventional therapies may be treated with an effective dose of triterpene derivatives in limonoids, polyphenolic flavonoid compounds, tocotrienols or a combination of these agents.Type: GrantFiled: January 12, 2000Date of Patent: May 29, 2001Assignee: KGK SynergizeInventors: Najla Guthrie, Elzbieta Maria Kurowska
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Patent number: 6221357Abstract: A method for inhibiting a collagen-induced platelet aggregation in a mammal comprises administering an effective amount of a flavonoid derived from citrus peels thereto.Type: GrantFiled: September 2, 1999Date of Patent: April 24, 2001Assignee: Korea Research Institute of Bioscience and BiotechnologyInventors: Song-Hae Bok, Tae-Sook Jeong, Han-Ik Cho, Dong-Soon Lee
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Patent number: 6172205Abstract: This invention provides a process for the preparation of a Eleutherobin derivative of the formula: wherein R1 is a hydrogen, ester, nitrile or C2H4—R wherein R4 is a carbohydrate, an alcohol an amine, an amide, an alkyne, or, R2 is a linear or branched alkyl moiety, R3 is an ester, an amide, a carbamate, an acetal compound,an ether or a urethane, R4 is a hydrogen or CH2,position C2 and C3 is cis or trans,position C8 is &agr; or &bgr; and a compound is produced having the structures: Additionally, this experiment provides a method for inhibiting growth of cancerous cells comprising contracting an amount of Eleutherobin derivative effective to inhibit the growth of said cells. Further provided is a method for treating cancer in a subject which comprises administering to the subject a therapeutically effective amount of the Eleutherobin derivative.Type: GrantFiled: December 11, 1998Date of Patent: January 9, 2001Assignee: The Trustees of Columbia in the City of New YorkInventors: Samuel J. Danishefsky, Xiao-Tao Chen, Clare E. Gutteridge, Samit K. Bhattacharya, Bishan Zhou
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Patent number: 6107276Abstract: The pharmaceutical compositions including a slightly soluble drug incorporated in a water-swellable, but water-insoluble cross-linked polymer, a surface active agent, and an oil show much improved dissolution and, consequently, bioavailability in respect of the drug as is or used with a polymeric carrier of said type.Type: GrantFiled: December 23, 1997Date of Patent: August 22, 2000Assignee: Vectorpharma International S.p.A.Inventors: Fabio Carli, Daniela Lombardi, Pierandrea Esposito, Luca Dobetti, Luigi Boltri
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Patent number: 6022866Abstract: A method is provided of inhibiting the narrowing of the vascular tubular walls of an animal by the proliferation of endothelial cells in the area of trauma after the vascular tubular walls have been traumatized, the method comprising the administration of a therapeutically effective non-toxic amount of a form of hyaluronic acid selected from the group consisting of hyaluronic acid and pharmaceutically acceptable salts thereof to the animal to inhibit the narrowing of the vascular tubular walls by the proliferation of endothelial cells into the area of trauma.Type: GrantFiled: March 24, 1995Date of Patent: February 8, 2000Assignee: Hyal Pharmaceutical CorporationInventors: Rudolf Edgar Falk, Samuel Simon Asculai, Eva Anne Turley
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Patent number: 5977077Abstract: Therapeutic compositions for the treatment of infectious diseases are disclosed. These compositions comprise xanthones and xanthone derivatives, such as 2,3,4,5,6-pentahydroxyxanthone. Also disclosed are methods for the treatment of infectious diseases using such compounds.Type: GrantFiled: March 20, 1996Date of Patent: November 2, 1999Assignee: Interlab CorporationInventors: Rolf Walter Winter, Michael Kevin Riscoe, David J. Hinrichs
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Patent number: 5972993Abstract: A method for treating skin conditions, such as rosacea and sensitive skin, that manifest as a tendency towards flushing and blushing is provided. Also provided herein, are compositions for the treatment of rosacea and sensitive skin that are comprised of at least one antioxidant selected from the following groups of antioxidants: (a) phenolic compounds that contain at least one hydroxyl group connected directly to a benzene ring and to another unsaturated chemical grouping, (b) sulfur-containing compounds that contain at least one sulfhydryl groups or sulfur-containing compounds that contain at least one disulfide group, or (c) polyene compounds that have conjugated systems of double bonds.Type: GrantFiled: March 20, 1998Date of Patent: October 26, 1999Assignee: Avon Products, Inc.Inventor: Dmitri Ptchelintsev
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Patent number: 5965571Abstract: Parkinson's disease can be treated with an at least one cholinesterase inhibitor. The cholinesterase inhibitor has been found to alleviate both any symptoms of dementia as well as to reduce rigidity and improve motor function.Type: GrantFiled: August 21, 1997Date of Patent: October 12, 1999Assignee: New York UniversityInventor: Michael Hutchinson
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Patent number: 5945406Abstract: Compounds of formula (I): ##STR1## wherein: R is halogen;Y is hydrogen, NH.sub.2, SH or OH;X is: ##STR2## wherein: either R.sub.1 or R.sub.2 is a bond, with the other being hydrogen;either R.sub.3 or R.sub.4 is hydrogen, with the other being hydrogen, OH, OAc or NHAc;R.sub.5 is OH or OAc;either R.sub.7 or R.sub.8 is hydrogen, with the other being OH or OAc;R.sub.9 is hydrogen, CH.sub.2 OH or CH.sub.2 OAc;with the proviso that when R.sub.4 is OH, OAc or NHAc then R.sub.8 is hydrogen;and enantiomers of such compounds, are disclosed. Pharmaceutical formulations comprising such compounds, their use in the treatment of various disease states, and methods of treatment employing the compounds are also provided.Type: GrantFiled: December 23, 1997Date of Patent: August 31, 1999Assignee: Oxford Glycosciences (UK) Ltd.Inventor: Stephen Martin Courtney
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Patent number: 5929113Abstract: This invention provides a method for repelling biting insects such as mosquitoes, ticks, and biting flies by topically applying to the skin of a subject emu oil, fractions of emu oil obtained by flash chromatography or a composition comprising emu oil or active fractions thereof and at least one other insect repellent such as citronella, DEET or saponin. Also provided are compositions for repelling biting insects comprising diluted fractions of emu oil, and compositions comprising emu oil or active fractions thereof and at least one other insect repellent such as citronella, DEET or saponin.Type: GrantFiled: June 16, 1997Date of Patent: July 27, 1999Assignee: AgraQuest, Inc.Inventors: Denise C. Manker, Pamela Gail Marrone, Stephen Judd
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Patent number: 5925621Abstract: A method for the reduction in the risk of transmitting a sexually transmitted disease--especially HIV and/or HSV--during sexual activity is provided. This method generally comprises the application of an effective amount of an inhibitory agent, preferably as a topical formulation, to the area or areas of sexual contact prior to engaging in sexual activity. Inhibitory agents which are useful in the present invention include, for example, phosphorylated hesperidins, sulfonated hesperidins, polystyrene sulfonates, substituted benzenesulfonic acid formaldehyde co-polymers, H.sub.2 SO.sub.4 -modified mandelic acids, and the like. This method can be used by heterosexuals, homosexuals, and/or bisexuals engaged in a wide variety of sexual activities. In addition to anti-STD activity, these agents may also act as vaginal contraceptives; moreover, they generally have fewer side effects than conventional vaginal contraceptives (e.g., nonoxynol-9).Type: GrantFiled: October 14, 1997Date of Patent: July 20, 1999Assignee: Rush-Presbyterian, St. Luke's Medical CenterInventors: Lourens Jan Dirk Zaneveld, Robert Anthony Anderson, Jr., Xiao Hui Diao, Paul Robert Young, Jr., Donald Paul Waller, Sanjay Garg, Calvin J. Chany, II
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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: 5843937Abstract: The present invention relates to novel DNA alkylating agents and the prodrugs of these agents which are useful as antitumor agents and DNA labelling agents. The compounds are hydroxy dihydrobenzindole oligopeptides and prodrugs thereof wherein the monomeric constituents are derived from monocyclic or bicyclic heterocyclic aromatic residues.Type: GrantFiled: May 23, 1996Date of Patent: December 1, 1998Assignee: Panorama Research, Inc.Inventors: Yuqiang Wang, Susan C. Wright, James W. Larrick
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Patent number: 5776925Abstract: Methods for cancer chemosensitization are provided. Texaphyrins are new chemosensitizers for enhancing the cytotoxicity of chemotherapeutic agents. The enhancement appears to be P-glycoprotein-independent since texaphyrins are effective in both a P-glycoprotein-expressing and a P-glycoprotein -nonexpressing cell line. Methods are provided for the treatment of cancers such as leukemia, lymphoma, carcinoma, and sarcoma using a texaphyrin as a chemosensitizer.Type: GrantFiled: January 25, 1996Date of Patent: July 7, 1998Assignee: Pharmacyclics, Inc.Inventors: Stuart W. Young, Richard A. Miller
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Patent number: 5750563Abstract: A preparation for epidermis containing kojic acid and/or its derivative, which has improved preparation stability, is provided. The preparation stability is imparted by adding to the preparation at least one member selected from the group consisting of alcohols and polyphenols.Type: GrantFiled: October 3, 1995Date of Patent: May 12, 1998Assignee: Sansho Seiyaku Co., Ltd.Inventor: Shinsuke Honda
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Patent number: 5677285Abstract: Provided are new derivatives of neuraminic acid of formula (I), where Ac represents an acyl residue of an aliphatic, araliphatic, aromatic, alicyclic, or heterocyclic carboxylic acid, including carboxylic amides, their 2-hydrocarbyl-glycosides, and their peracylated derivatives at the hydroxy groups of both these series of amides. These compositions are therapeutically useful in providing a protective effect against the neurotoxicity induced by excitatory amino acids, and can therefore be used in therapies of the central nervous system.Type: GrantFiled: April 26, 1995Date of Patent: October 14, 1997Assignee: Fidia S.P.A.Inventors: Aurelio Romeo, Gunter Kirschner, Hari Manev, Martino Trimarco, Gino Toffano
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Patent number: 5672618Abstract: The present invention discloses compounds that are highly isozyme selective protein kinase C beta-1 and beta-2 isozyme inhibitors. Accordingly, the present invention provides a method of selectively inhibiting protein kinase C isozymes beta-1, and beta-2. As isozyme selective inhibitors of beta-1 and beta-2, the compounds are therapeutically useful in treating conditions associated with diabetes mellitus and its complications, as well as other disease states associated with an elevation of the beta-1 and beta-2 isozyme.Type: GrantFiled: May 25, 1995Date of Patent: September 30, 1997Assignee: Eli Lilly and CompanyInventors: William F. Heath, Jr., John H. McDonald, III, Michael Paal, Theo Schotten, Wolfgang Stenzel
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Patent number: 5646124Abstract: The present invention relates to a method of treating a patient suffering from a neoplastic disease state comprising administering to said patient an effective antineoplastic amount of N,N'-bis[3-(ethylamino)propyl]-1,7-heptanediamine in conjunctive therapy with an effective antineoplastic amount of a cytotoxic agent selected from the group consisting of an antineoplastic vinca alkaloid, an antineoplastic antibiotic, an antineoplastic antimetabolite and an antineoplastic platinum coordination complex, wherein a synergistic antineoplastic effect results.Type: GrantFiled: June 2, 1995Date of Patent: July 8, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Nellikunja J. Prakash, Terry L. Bowlin
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Patent number: 5635486Abstract: The present invention provides an ophthalmic composition comprising a sleep inducing substance or a sleep inhibiting substance, and the sleep inducing substance or the sleep inhibiting substance is derived from an organism. Thus, the invention provides an ophthalmic composition comprising a sleep adjusting substance which normalizes irregularity of the rhythm of sleep and a liquid ophthalmic medicament comprising the composition, the composition and the medicament being safe and obtainable by anyone, and a method for regulating the rhythm of sleep comprising instilling the ophthalmic medicament including the sleep adjusting substance to an individual.Type: GrantFiled: September 7, 1994Date of Patent: June 3, 1997Assignee: Kanegafuchi Kagaku Kogyo Kabushiki KaishaInventors: Kozo Yamamoto, Takayoshi Hidaka
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Patent number: 5583115Abstract: Antimicrobial compounds having the formula ##STR1## as well as pharmaceutical compositions comprising such compounds and methods of treating bacterial infection and colitis by the administration thereof.Type: GrantFiled: May 9, 1995Date of Patent: December 10, 1996Assignee: Abbott LaboratoriesInventors: James B. McAlpine, Jill E. Hochlowski
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Patent number: 5525480Abstract: The present invention provides N- and O-substituted aminophenol derivatives of the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, G and L are as hereinbefore defined. The present invention also provides intermediates for the preparation of these aminophenol derivatives of general formula (I), as well as the use of the aminophenol derivatives of general formula (I) for the determination of hydrolases, as well as for the preparation of agents for carrying out determinations of hydrolysis.Type: GrantFiled: June 9, 1994Date of Patent: June 11, 1996Assignee: Boehringer Mannheim GmbHInventors: Gerd Zimmermann, Dieter Mangold
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Patent number: 5478812Abstract: 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 oligosaccharide 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: February 10, 1994Date of Patent: December 26, 1995Assignee: CCI CorporationInventors: Hironobu Murase, Tsutomu Kunieda, Tetsuya Tsujii
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Patent number: 5466450Abstract: A novel antibiotic complex designated BU-4224V produced by fermentation of Kibdelosporangium albatum sp. nov. Strain R761-7. The complex may be separated chromatographically into bioactive components designated BU-4224V A, B.sub.1, B.sub.2, and C. The components BU-4224V B.sub.1 and B.sub.2 display both antiviral and antimicrobial activity, while component BU-4224V A has antimicrobial activity and component BU-4224V C has antiviral activity.Type: GrantFiled: July 20, 1993Date of Patent: November 14, 1995Assignee: Bristol-Myers Squibb Co.Inventors: Mitsuaki Tsunakawa, Tetsuro Yamasaki, Koji Tomita, Osamu Tenmyo
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Patent number: 5371074Abstract: Novel 2-substituted saccharins which inhibit the enzymatic activity of proteolytic enzymes, are useful in the treatment of degenerative diseases and have the formula 0010wherein:L is --O--, --S--, --SO-- or --SO.sub.2 --; m and n are each independently 0 or 1; R.sub.1 is halo, lower-alkanoyl, 1-oxophenalenyl, phenyl or substituted phenyl, heterocyclyl or substitued heterocyclyl or, when L is --O-- and n is 1, cycloheptatrienon-2-yl or, when L is --S-- and n is 1, cyano or lower-alkoxythiocarbonyl or, when L is --SO.sub.2 -- and n is 1, lower-alkyl or trifluoromethyl; R.sub.2 is hydrogen, lower-alkoxycarbonyl, phenyl or phenylthio; and R.sub.3 and R.sub.4 are each hydrogen or various substituents and processes for preparation and pharmaceutical compositions and method of use thereof are disclosed.Type: GrantFiled: May 24, 1993Date of Patent: December 6, 1994Assignee: Sterling Winthrop Inc.Inventors: Richard P. Dunlap, Neil W. Boaz, Albert J. Mura, Dennis J. Hlasta, Ranjit C. Desai, Chakrapani Subramanyam, Lee H. Latimer, Eric P. Lodge
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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: 5360794Abstract: The compounds of the present invention are deoxy disubstituted or dideoxy disubstituted derivatives of .alpha.-D-mannofuranoside and .beta.-L-gulofuranoside hexoses which exhibit anti-inflammatory and anti-proliferative activity. Pharmaceutical compositions containing the compounds and methods of treating inflammatory and/or autoimmune disorders employing the compounds are disclosed.Type: GrantFiled: August 3, 1992Date of Patent: November 1, 1994Assignee: Medicarb Inc.Inventor: Sudershan K. Arora
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Patent number: 5262401Abstract: A porphycene having the structure ##STR1## wherein each R.sup.1 is, independently, (a) --(CH.sub.2).sub.n --X, where n= 1-4, X is OR.sup.2 and R.sup.2 is C.sub.1-6 alkyl, aralkyl or aryl; CN; OH; OSO.sub.2 R.sup.2 ; NH.sub.2 ; NHR.sup.2 ; NR.sup.2.sub.2 ; SH; SR.sup.2 ; S(O).sub.1-2 R.sup.2 ; COOH; CO.sub.2 R.sup.2 ; C(O)NH.sub.2 ; C(O)NHR.sup.2 ; C(O)NR.sup.2.sub.2 ; halogen; or CHO;(b) --(CH.sub.2).sub.m CH.dbd.CH.sub.2 where m is 0-2; or(c) --(CH.sub.2).sub.n --O--G where G is a mono- or oligosaccharide;(d) --(CH.sub.2).sub.2n --X, where X is an amino acid, oligopeptide covalently bonded by an ether-, ester- or amine-bond or --Y--(CH.sub.2).sub.n -porphycene.sup.2 (porphycene.sup.2 being a compound of the same structure and Y is a direct bond; --O--; or --CH.dbd.CH.sub.2); or(e) where one, two or three of the substituents R.sup.1 are C.sub.1-6 alkyl or aryl and the remaining substituents are as above under (a)-(d), and salts and metal complexes thereof.Type: GrantFiled: April 29, 1992Date of Patent: November 16, 1993Assignee: Cytopharm, Inc.Inventors: Emanuel Vogel, Clemens Richert, Thomas Benninghaus, Martin Muller, Alexander D. Cross
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Patent number: 5256646Abstract: A novel antibiotic complex designated BU-4224V produced by fermentation of Kibdelosporangium albatum sp. nov. Strain R761-7. The complex may be separated chromatographically into bioactive components designated BU-4224V A, B.sub.1, B.sub.2, and C. The components BU-4224V B.sub.1 and B.sub.2 display both antiviral and antimicrobial activity, while component BU-4224V A has antimicrobial activity and component BU-4224V C has antiviral activity.Type: GrantFiled: July 27, 1990Date of Patent: October 26, 1993Assignee: Bristol-Myers Squibb CompanyInventors: Mitsuaki Tsunakawa, Tetsuro Yamasaki, Koji Tomita, Osamu Tenmyo
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Patent number: 5210077Abstract: Antibodies (polyclonal and monoclonal) having specificity for cytokinins having a glycosylated isoprenoid side chain are described. The antibodies simultaneously recognize a purine ring, an isoprenoid side chain, and a 4'-O-glycoside. The antibodies were elicited using a novel hapten, 9-(2-carboxyethyl) cytokinin-O-glycoside. Immunoassay methods for the determination of cytokinins having a glycosylated isoprenoid side chain which utilize the antibodies are also described.Type: GrantFiled: April 6, 1989Date of Patent: May 11, 1993Assignee: The United States of America as represented by the Secretary of AgricultureInventors: David L. Brandon, Joseph W. Corse
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Patent number: 5120718Abstract: Compounds which inhibit Candida acid protease are disclosed which have the formula: ##STR1## wherein R.sub.1 is loweralkyl, loweralkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkenylalkyl, arylalkyl or (heterocyclic)alkyl;R.sub.2 is loweralkyl, cycloalkylalkyl or arylalkyl;R.sub.3 is --OH or --NH.sub.2 ;R.sub.4 is(a) --CH(OH)--R.sub.5 wherein R.sub.5 is loweralkyl, cycloalkyl or cycloalkylalkyl or(b) --CH.sub.2 CH(R.sub.6)C(O)NHR.sub.7 wherein R.sub.6 is loweralkyl and R.sub.7 is loweralkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, hydroxyalkyl, alkoxyalkyl, thioalkoxyalkyl, carboxyalkyl, alkoxycarbonylalkyl, cyanoalkyl or (heterocyclic)alkyl; andA is ##STR2## wherein R.sub.8 is arylalkyl, B is --C(O) or --S(O).sub.2 -- and R.sub.9 is aryl, arylalkyl, heterocyclic or (heterocyclic)alkyl; or ##STR3## wherein R.sub.10 is arylalkyl and R.sub.11 is (a) --C(O)R.sub.12 wherein R.sub.12 is alkoxy, arylalkoxy, aryl, arylalkyl, heterocyclic or (heterocyclic)alkyl or (b) --S(O).sub.2 --R.sub.Type: GrantFiled: June 13, 1991Date of Patent: June 9, 1992Assignee: Abbott LaboratoriesInventors: Robert C. Goldman, William R. Baker, Hwan-Soo Jae, Biswanath De, Thomas M. Zydowsky, Edwin de Lara
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Patent number: 5057302Abstract: The present invention provides bifunctional chelating agents comprising a unique substrate reactive moiety incorporated into a carboxymethyl arm of a polyaminopolycarboxylate chelating framework capable of forming stable complexes with metal ions.Type: GrantFiled: January 4, 1988Date of Patent: October 15, 1991Assignee: Abbott LaboratoriesInventors: David K. Johnson, Steven J. Kline
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Patent number: 5041425Abstract: A specified citrus limonoid such as limonin and nomilin is isolated from the citrus and is found to be useful to treat a tumor. It is useful as an additive to food.Type: GrantFiled: June 23, 1989Date of Patent: August 20, 1991Assignee: Toyotama Perfumery Co., Ltd.Inventors: Shin Hasegawa, Luke K. T. Lam
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Patent number: 5023090Abstract: A topical composition comprising LYCD together with known topically active useful medicinal agents such as anti-wrinkling, antibiotic, anticancer, antifungal, antiinflammatory such as anti-acne, antiviral, wound healing, and hair-growing agents. The LYCD works together with the other active agents to achieve a synergistic result more effective than can be obtained from the topical agents individually, and more effective than could be predicted from the mere addition of the known efficacies of the individual ingredients.Type: GrantFiled: April 2, 1990Date of Patent: June 11, 1991Inventor: Robert H. Levin
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Patent number: 5011827Abstract: The invention relates to elaiophyline derivatives of the formula I ##STR1## in which R.sup.1 and R.sup.1' are identical or different and represent a radical of the formula II/or III ##STR2## in which R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.7 have the meanings given. The invention furthermore relates to a process for the preparation of these elaiophyline derivatives and also the use of the lattere as medicaments, in particular as anthelmintically acting medicaments.Type: GrantFiled: October 28, 1988Date of Patent: April 30, 1991Assignee: Hoechst AktiengesellschaftInventors: Gerhard Kretzschmar, Dieter Duwel, Susanne Grabley, Peter Hammann, Gerhard Seibert, Hartmut Voelskow, Carlo Giani