Oxygen Containing Hetero Ring Patents (Class 514/99)
  • Patent number: 7625885
    Abstract: A compound or groups of compounds, present in an active principle, derived from tunicates of the species Synoicum adareanum, as well as to pharmaceutical compositions comprising these compounds. Extracts from tunicates show selective toxicity against several different cancer cell lines in the NCI 60 cell line panel. These compounds are useful in the effective treatment of cancers, particularly malignant melanomas, colon cancer, and renal cancer cell lines.
    Type: Grant
    Filed: February 17, 2005
    Date of Patent: December 1, 2009
    Assignees: University of South Florida, The UAB Research Foundation
    Inventors: Bill J Baker, Thusahara Diyabalanage, James B McClintock, Charles D Amsler
  • Publication number: 20090252773
    Abstract: An emulsion composition of the present invention includes (A) a salt of a higher fatty acid ester of ascorbic acid-2-phosphoric acid ester, (B) a polyglycerin fatty acid monoester including polyglycerin having a mean polymerization degree of 8 to 12 and an unsaturated fatty acid residual group of 14 to 22 carbon atoms, (C) a polyglycerin fatty acid monoester comprising polyglycerin having a mean polymerization degree of 2 to 6 and an unsaturated fatty acid residual group of 14 to 22 carbon atoms, and (D) a hydrocarbon oil, wherein the blending ratio by mass between the component (B) and the component (C) is in the range of 1:1 to 3:1, and the blending ratio by mass between the total of the components (B) and (C) and the component (D) is in the range of 10:1 to 1:4.
    Type: Application
    Filed: July 3, 2007
    Publication date: October 8, 2009
    Applicant: Showa Denko K.K.
    Inventors: Tadashi Yoneda, Naoko Ito, Kazuo Furuya
  • Publication number: 20090221530
    Abstract: Methods of treating a microbial infection in a subject by administering to the subject an effective amount of a compound that modulates an enzymatic activity of a relaxase polypeptide is provided. Methods of inhibiting bacterial conjugation by modulating activity of a relaxase polypeptide in a bacterium are also provided. Novel compounds that modulate relaxase enzymes and assays for measuring kinetics of relaxase enzymes and selecting for modulators of relaxase enzyme activity are further provided.
    Type: Application
    Filed: November 8, 2006
    Publication date: September 3, 2009
    Inventors: Matthew R. Redinbo, Scott Lujan, Steven W. Matson
  • Publication number: 20090186856
    Abstract: There is provided a dietary or health supplement comprising an effective amount of a micronutrient selected from the group consisting of phosphate derivatives of tocopherol, ubiquinol, ascorbic acid, tocotrienol, retinol and mixtures thereof delivered with an acceptable carrier.
    Type: Application
    Filed: September 18, 2008
    Publication date: July 23, 2009
    Applicant: VITAL HEALTH SCIENCES PTY. LTD.
    Inventors: Simon Michael West, David Kannar
  • Publication number: 20090131363
    Abstract: This invention relates to novel compounds that are hydroxyethylamino sulfonamide derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel hydroxyethylamino sulfonamide derivatives that are derivatives of darunavir. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering a human immunodeficiency virus (HIV) protease inhibitor, such as darunavir.
    Type: Application
    Filed: October 24, 2008
    Publication date: May 21, 2009
    Inventor: Scott L. Harbeson
  • Publication number: 20090098221
    Abstract: The present invention provides methods of treating creatine responsive states, such as a neurological disorder (i.e., Huntington's disease, Parkinson's disease, amyotrophic lateral sclerosis, muscular dystrophy, Charcot Marie Tooth syndrome, Alzheimer's disease, or creatine transporter defect) or a skin disorder, by administering a creatine-ascorbyl derivative.
    Type: Application
    Filed: May 5, 2008
    Publication date: April 16, 2009
    Inventor: Belinda Tsao Nivaggioli
  • Publication number: 20090075942
    Abstract: The present application describes deuterium-enriched fosamprenavir, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: September 5, 2008
    Publication date: March 19, 2009
    Applicant: Protia, LLC
    Inventor: Anthony W. Czarnik
  • Patent number: 7488786
    Abstract: This invention discloses a process for producing a polymer by controlled polymerization which comprises polymerizing at least one monomer in the presence of a free radical control agent of the structural formula: (Z)-(R1)n, wherein n represents an integer from 1 to about 6; wherein Z represents an aromatic or aliphatic moiety containing from 1 to about 20 carbon atoms; wherein R1 represents a moiety of the structural formula: wherein R2 represents a moiety selected from the group consisting of alkyl groups, alkenyl groups, alkynyl groups, aryl groups, heteroaryl groups, and alkaryl groups; wherein the alky groups, alkenyl groups, alkynyl groups, aryl groups, heteroaryl groups, and alkaryl groups can be substituted, unsubstituted, linear, branched or cyclic; and wherein Ar represents a p-alkoxyphenyl group having an alkoxy moiety that contains from 1 to 8 carbon atoms.
    Type: Grant
    Filed: August 24, 2007
    Date of Patent: February 10, 2009
    Assignee: The Goodyear Tire & Rubber Company
    Inventor: Dane Kenton Parker
  • Publication number: 20090035275
    Abstract: Pharmaceutical and cosmetic formulations and methods for optimizing the intracellular concentrations of NAD are provided. The present methods and compounds relate to the use of PBEF, PRPP and various forms of nicotinamide, individually or in combination, for therapeutic, cyto-protective, cosmetic and anti-aging purposes. PBEF, PRPP and nicotinamide, individually or in combination, as administered according to the invention, increase the metabolic fitness, health and performance of the cell, and thereby increase the cell's level of health during its lifecycle. By way of the present formulations and methods, optimizing the intracellular concentration of NAD+ facilitates a balance among the numerous intracellular interactions of NAD+, and its related pathways, such that the health of the cell and its resistance to stress and trauma are increased. This increased robustness attendant to the invention also facilitates the delay of apoptosis.
    Type: Application
    Filed: October 29, 2004
    Publication date: February 5, 2009
    Inventors: John Geoffrey Pickering, Eric Peter Van Der Veer
  • Publication number: 20090004279
    Abstract: A method for improvement of tolerance for therapeutically effective agents delivered by inhalation comprising a pretreatment of a patient with a nebulized lidocaine or a lidocaine-like compound administered immediately or up to about thirty minutes before administration of the primary therapeutically effective agent. The pretreatment of the patient with the nebulized lidocaine or a lidocaine-like compound improves airway tolerance and deposition of the agent in the lungs and makes such deposition more safe, efficacious, controllable and predictable. The method of the invention is especially useful for enhancement of deposition of immunosuppressive agents in the lung(s) of transplant patients, improved tolerance of the drugs by reducing cough, and improving pulmonary drug deposition.
    Type: Application
    Filed: September 10, 2008
    Publication date: January 1, 2009
    Inventors: Thomas Hofmann, Alan Bruce Montgomery, Kevin Stapleton, William R. Baker
  • Publication number: 20080318901
    Abstract: The present invention is directed to compositions comprising lysophosphatidic acid analogs and methods of using such analogs as agonist or antagonists of LPA receptor activity. In addition the invention is directed to LPA receptor agonists that vary in the degree of selectivity at individual LPA receptors (i.e. LPA1, LPA2 and LPA3). More particularly the present invention is directed to LPA analogs wherein the glycerol is replaced with ethanolamine and a variety of substitutions have been linked at the second carbon atom.
    Type: Application
    Filed: May 6, 2005
    Publication date: December 25, 2008
    Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATION
    Inventors: Kevin R. Lynch, Timothy L. Macdonald, Brian H. Heasley
  • Publication number: 20080305039
    Abstract: Compounds of the formula: are described wherein: A1 is ascorbic acid, dehydroascorbic acid, ascorbyl-2-phosphate, an analog thereof, or a salt thereof; L is a linking group coupled to A1 at the C5 or C6 position thereof; and B1 is an active agent such as an imaging agent or therapeutic agent (e.g. a bisphosphonate), along with pharmaceutically acceptable salts and prodrugs thereof. The compounds are useful for, among other things, improving cartilage uptake of active agents administered for joint diseases such as osteoarthritis and rheumatoid arthritis, and for improving gastrointestinal absorption of bisphosphonates.
    Type: Application
    Filed: April 21, 2006
    Publication date: December 11, 2008
    Inventors: Virginia Byers Kraus, Amy Lynn McNulty, Eric John Toone
  • Patent number: 7462674
    Abstract: This invention discloses a process for producing a polymer by controlled polymerization which comprises polymerizing at least one monomer in the presence of a free radical control agent of the structural formula: (Z)-(R1)n, wherein n represents an integer from 1 to about 6; wherein Z represents an aromatic or aliphatic moiety containing from 1 to about 20 carbon atoms; wherein R1 represents a moiety of the structural formula: wherein R2 represents a moiety selected from the group consisting of alkyl groups, alkenyl groups, alkynyl groups, aryl groups, heteroaryl groups, and alkaryl groups; wherein the alky groups, alkenyl groups, alkynyl groups, aryl groups, heteroaryl groups, and alkaryl groups can be substituted, unsubstituted, linear, branched or cyclic; and wherein Ar represents a p-alkoxyphenyl group having an alkoxy moiety that contains from 1 to 8 carbon atoms.
    Type: Grant
    Filed: October 18, 2007
    Date of Patent: December 9, 2008
    Assignee: The Goodyear Tire & Rubber Company
    Inventor: Dane Kenton Parker
  • Publication number: 20080274077
    Abstract: The present invention is based on the discovery that suppressing the activity of the Nogo receptor (NgR) alone does not result in extensive axon regeneration unless the intrinsic growth program of neurons is also activated Accordingly, the present invention is directed to methods of stimulating axon regeneration using a combination therapy wherein agents that inhibit NgR activity or downstream pathways activated by inhibitory signals are combined with agents that activate the growth pathway of neurons (e.g. polypeptide growth factors, activators of macrophages, purine nucleosides, or hexoses).
    Type: Application
    Filed: December 16, 2004
    Publication date: November 6, 2008
    Applicant: Children's Medical Center Corporation
    Inventors: Larry I. Benowitz, Dietmar Fischer
  • Publication number: 20080269173
    Abstract: Disclosed is a composition for stimulating growth of dermal papilla cells and promoting hair follicle growth comprising vitamin C derivatives.
    Type: Application
    Filed: January 6, 2006
    Publication date: October 30, 2008
    Inventors: Young-Kwan Sung, Moon-Kyu Kim, Jung-Chul Kim
  • Publication number: 20080253982
    Abstract: It is an object to provide an L-ascorbic acid derivative which can keep the L-ascorbic acid stable to heat and light and thus has a long shelf life, which is high in permeability into the skin, which can be quickly hydrolyzed by phosphatase, an enzyme that is ubiquitous in vivo, and which exhibits physiological activities that are inherent to L-ascorbic acid and beneficial to health, a method for producing such an L-ascorbic acid derivative, and a skin-whitening cosmetic material. There is provided an ascorbic acid derivative comprising an L-ascorbic acid-2-phosphate ester or a salt thereof wherein the phosphate ester has a branched alkyl group, the L-ascorbic acid-2-phosphate ester being of formula [13].
    Type: Application
    Filed: August 9, 2007
    Publication date: October 16, 2008
    Inventors: Hiroharu Shibayama, Koichi Ueda, Hachiro Indo, Satoshi Tachibana, Hiroshi Nishikawa, Masaru Yamabe
  • Publication number: 20080167270
    Abstract: The invention is related to phosphorus substituted anti-infective compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: September 20, 2007
    Publication date: July 10, 2008
    Inventors: Constantine G. Boojamra, Aesop Cho, William J. Watkins
  • Publication number: 20080145450
    Abstract: A process for delivering and/or removing metal from a biological system by loading a titanate sorbent with a biometal either before introduction into the system for delivery to a site within the system or after introduction into the system for delivery to a site where there is an excess accumulation of metal and thereafter the sorbent is loaded at the site with the excess metal and is removed from the system.
    Type: Application
    Filed: December 14, 2006
    Publication date: June 19, 2008
    Inventors: David T. Hobbs, John C. Wataha, Jill Lewis, Regina L. W. Messer
  • Publication number: 20070281909
    Abstract: Membrane permeable prodrugs of creatine phosphate, pharmaceutical compositions comprising membrane permeable prodrugs of creatine phosphate, and methods of treating diseases such as ischemia, heart failure, and neurodegenerative disorders comprising administering prodrugs of creatine phosphate or pharmaceutical compositions thereof are disclosed.
    Type: Application
    Filed: June 6, 2007
    Publication date: December 6, 2007
    Inventors: Noa Zerangue, Qingzhi Gao, William J. Dower
  • Patent number: 7208481
    Abstract: The present invention relates to methods of use of aminodiphosphonate to modulate apolipoprotein E levels and the use of such compounds in therapy, including cardiovascular and neurological disease states.
    Type: Grant
    Filed: February 14, 2003
    Date of Patent: April 24, 2007
    Assignee: ILEX Products, Inc.
    Inventors: Hieu Trung Phan, Lân Mong Nguyen, Raymond Azoulay, Vinh Van Diep, Eric Joseph Niesor, Craig Leigh Bentzen, Yves Gyon Gellin, Anne Perez, Jean-Luc Thulliard
  • Patent number: 7144867
    Abstract: The present invention relates to new classes of anti-cancer compounds. In particular, the present invention provides glycoside compounds as anti-cancer agent, alone, or in combination with other anti-cancer agents or therapies.
    Type: Grant
    Filed: January 27, 2005
    Date of Patent: December 5, 2006
    Assignees: Northwestern University, Coastside Bio Resources
    Inventors: Thomas E. Adrian, Peter D. Collin
  • Patent number: 7038039
    Abstract: A desired isomer is selectively prepared by phosphorolyzing and isomerizing an anomer mixture of a 1-phosphorylated saccharide derivative while crystallizing one of the isomers to displace the equilibrium. Furthermore, using the action of a nucleoside phosphorylase, a nucleoside is prepared from the 1-phosphorylated saccharide derivative obtained and a base with improved stereoselectivity and a higher yield. This process is an anomer-selective process for preparing a 1-phosphorylated saccharide derivative and a nucleoside.
    Type: Grant
    Filed: February 13, 2001
    Date of Patent: May 2, 2006
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Hironori Komatsu, Hirokazu Awano, Nobuyuki Fukazawa, Kiyoshi Ito, Ichirou Ikeda, Tadashi Araki, Takeshi Nakamura, Tamotsu Asano, Junya Fujiwara, Tomoyuki Ando, Katsutoshi Tsuchiya, Kyoko Maruyama, Hideki Umetani, Takahiro Yamauchi, Hitoki Miyake
  • Patent number: 7030103
    Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.
    Type: Grant
    Filed: October 8, 2002
    Date of Patent: April 18, 2006
    Assignee: Methylgene, Inc.
    Inventors: Jeffrey M. Besterman, Daniel Delorme, Jubrail Rahil
  • Patent number: 7019024
    Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 9, 2001
    Date of Patent: March 28, 2006
    Assignee: Allelix Neuroscience Inc.
    Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
  • Patent number: 6919322
    Abstract: Novel FBPase inhibitors of the formula I are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.
    Type: Grant
    Filed: March 7, 2001
    Date of Patent: July 19, 2005
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Brett C. Bookser, Qun Dang, K. Raja Reddy
  • Patent number: 6900315
    Abstract: The present invention relates to novel compounds, compositions and methods for inhibiting the growth, elaboration and/or replication of HIV in human patients and to the prevention and treatment of human acquired immunodeficiency syndrome (AIDS) and other diseases caused by retroviral infection. More particularly, in preferred aspects, the present invention provides a method for the use of novel prodrug forms of 9-(2,3-Dideoxy-?-D-glycero-pent-2-enofuranosyl) guanine (d4G) for the prevention and treatment of both wild type and drug-resistant Human Immunodeficiency Virus (HIV), the causative pathogen of AIDS. Compounds according to the present invention are based upon the chemical formula: where X is OCH3, N3, NHCH3, N(CH3)2 or an aminocyclopropyl group; R1 is H or a C1 to C20 acyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group; and R2 is H or a C1 to C20 acyl or alkyl group.
    Type: Grant
    Filed: February 5, 2002
    Date of Patent: May 31, 2005
    Assignees: Yale University, University of Georgia Research Foundation, Inc.
    Inventors: Karen S. Anderson, Adrian Staffin Ray, Chung K. Chu, Yang Zhenjun
  • Patent number: 6831105
    Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
    Type: Grant
    Filed: November 26, 2002
    Date of Patent: December 14, 2004
    Assignee: Esperion Therapeutics, Inc.
    Inventor: Jean-Louis Henri Dasseux
  • Publication number: 20040127430
    Abstract: The present invention relates to chiral monophosphorus compounds and their transition metal complexes, to a process for preparing chiral monophosphorus compounds and their transition metal complexes and also to their use in asymmetric syntheses.
    Type: Application
    Filed: September 11, 2003
    Publication date: July 1, 2004
    Inventors: Benjamin Meseguer, Hans-Christian Militzer, Sergio Castillon, Carmen Claver, Ester Guiu
  • Publication number: 20040127467
    Abstract: A new and efficient synthesis of the (+)-pancratistatin phosphate prodrug 2a has been accomplished. Selective protection (tetraacetate 4) of (+)-pancratistatin (1a) was followed by phosphorylation (to 5) with dibenzyl chlorophosphite (prepared in situ from dibenzyl phosphite). Cleavage of the acetate (with sodium methoxide) and benzyl (by hydrogenolysis) protecting groups followed by concomitant reaction with two equivalents of sodium methoxide afforded good yield of disodium (+)-pancratistatin phosphate (2a). Further increases in yields of the prodrug (2a) were realized by avoiding heat in the final purification steps. Fourteen (2b-o) additional metal and ammonium derived phosphate prodrugs were also synthesized.
    Type: Application
    Filed: October 16, 2003
    Publication date: July 1, 2004
    Inventors: George R Pettit, Brian Orr, Sylvie Ducki
  • Patent number: 6737416
    Abstract: A compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof: wherein R1 represents hydrogen atom, an alkyl group, a substituted alkyl group and the like; R2 and R3 represent hydrogen atom, an alkyl group, a substituted alkyl group, an alkoxyl group and the like; X represents —CH2—, —O—, or —NH—; A represents the following group (II): [in which R7 and R8 represent hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group and the like; R9 and R10 represents hydrogen atom, a halogen atom, hydroxyl group, phenyl group, an alkyl group and the like] and the like; and E represents hydrogen atom and the like, which has inhibitory activity against carboxypeptidase B and is useful for therapeutic and/or preventive treatment of a thrombotic disease.
    Type: Grant
    Filed: October 7, 2002
    Date of Patent: May 18, 2004
    Assignee: Meiji Seika Kaisha Ltd.
    Inventors: Kenichi Fushihara, Chika Kikuchi, Tetsuya Matsushima, Kenichi Kanemoto, Eriko Satoh, Takehiro Yamamoto, Kokichi Suzuki
  • Publication number: 20040091509
    Abstract: There are disclosed skin treatment compositions containing cell signaling compounds, which induce and promote the biosynthesis and/or bioactivity of endogenous chemicals that mediate cell to cell communication in the skin between keratinocytes, fibroblasts and other cell types present in the skin. The cell signaling compound is selected from the group consisting of: andrographolide and its derivatives; adenosine cyclic phosphate and its derivatives; hydrolyzed milk proteins; sunflower seed extract; plankton extract; phytol and its derivatives; and mixtures thereof.
    Type: Application
    Filed: October 17, 2003
    Publication date: May 13, 2004
    Applicant: Avon Products, Inc.
    Inventors: Glen T. Anderson, Dmitri S. Ptchelintsev, Gopinathan K. Menon, John A. Duffy
  • Publication number: 20040092485
    Abstract: One of the object of the present invention is to provide an L-ascorbic acid 2-phosphate metal salt, which causes no clouding and scarcely precipitates or deposits even when added to a cosmetic material or the like having blended therein an organic acid.
    Type: Application
    Filed: September 2, 2003
    Publication date: May 13, 2004
    Inventors: Yoshio Fujiwara, Yuji Kobayashi, Makoto Saito
  • Publication number: 20040033988
    Abstract: Compounds of the formula: 1
    Type: Application
    Filed: February 27, 2003
    Publication date: February 19, 2004
    Applicant: Wyeth
    Inventors: Jeremy I. Levin, James M. Chen, Derek C. Cole, Mila T. Du, Leif M. Laakso
  • Publication number: 20040029812
    Abstract: The invention relates to a method of treating with furanone derivatives and the phmaceutically acceptable salts therof, one or more conditions of the skin, in particular regulating skin condition, regulating signs of skin aging, treating a number of conditions suchas contact dermatitis, skin irritation, rosacea, acne, psoriasis, and preventing and protecting skin tissue against age-related damage or damage resulting from insults such as harmful (UV) radiation or environmental pollution, stress and fatigue.
    Type: Application
    Filed: July 30, 2003
    Publication date: February 12, 2004
    Inventors: Sekhar Boddupalli, Gail Walkinshaw, Bing Wang
  • Publication number: 20040022866
    Abstract: The use of certain salts and aminoacids as stabilizer of the antibiotic Fosfomycin Tromethamol and pharmaceutical compositions containing them, is described.
    Type: Application
    Filed: July 10, 2003
    Publication date: February 5, 2004
    Applicant: ZAMBON GROUP S.P.A.
    Inventors: Luca Rampoldi, Luca Pirrone, Sarah Faccin, Alessandro Grassano, Giovanni Gurrieri
  • Publication number: 20040023930
    Abstract: The novel active compound combinations of certain cyclic ketoenols and the active compounds (1) to (95) listed in the description have very good insecticidal and acaricidal properties.
    Type: Application
    Filed: April 11, 2003
    Publication date: February 5, 2004
    Inventors: Ernst Bruck, Christoph Erdelen, Reiner Fischer
  • Publication number: 20030236231
    Abstract: The invention relates to polycyclic aryl and heteroaryl substituted benzene compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
    Type: Application
    Filed: November 13, 2002
    Publication date: December 25, 2003
    Inventors: Michael S South, John J Parlow
  • Publication number: 20030190338
    Abstract: Synergistic immixtures of ascorbic acid with at least one monosaccharide ester of ascorbic acid and/or at least one metal salt of phosphorylated ascorbic acid more effectively increase the synthesis of epidermal ceramides in human skin, especially types IV to VII ceramides, as well as improve the barrier function, moisture content and/or suppleness/surface appearance of the skin and which otherwise combat/prevent intrinsic aging thereof and are useful for the treatment of dermatitis.
    Type: Application
    Filed: April 30, 2003
    Publication date: October 9, 2003
    Applicant: SOCIETE L'OREAL S.A.
    Inventors: Isabelle Castiel, Corinne Ferraris, Armelle La Valle-Bouchard
  • Publication number: 20030176361
    Abstract: Furanone derivatives and the pharmaceutically acceptable salts thereof have cytoprotective activity and protective activity for neuroinflammation, and neurodegenerative disorders; they are useful in the treatment of stroke, cerebral ischemia, myocardial infarction, myocardial ischemia, chronic heart failure, inflammation and other oxidative stress-related conditions, as well as Alzheimer's disease and senile dementia; they are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.
    Type: Application
    Filed: January 28, 2003
    Publication date: September 18, 2003
    Inventors: Bing Wang, Wei Zhang, Jiangao Song, Ughetta del Balzo, Lesley Brown, Gail Walkinshaw
  • Publication number: 20030176358
    Abstract: There is provided a method of treating environmental stress due to the adverse effects of tobacco smoke and automobile exhaust gases. The method of treatment comprises applying to the skin a liniment composition containing one or more ingredients selected from among a group consisting of sulfur containing amino acids, metabolic intermediates of sulfur containing amino acids, tannin and vitamin C and its derivatives. A preferred sulfur containing amino acid is glutathione and preferred metabolic intermediates of sulfur containing amino acids are thiotaurine or hypotaurine. Also, hydroxycarboxylic acid or its derivatives can advantageously be added to this liniment composition to treat environmental stress.
    Type: Application
    Filed: January 7, 2000
    Publication date: September 18, 2003
    Inventors: MARIKO EGAWA, TETSUO SAKAMOTO, YOSHIYUKI KOHNO
  • Publication number: 20030162752
    Abstract: The instant invention relates to sulphamate compounds of formula I, wherein A represents a ring structure, B represents a ring structure, D a ring structure, C is a bond, E is a link joining ring structure B to the ring structure D, X represents a suitable first group, and Y represents a suitable second group; wherein one ring of the compound is a phenolic ring; and wherein any one of ring structures A, B and D has bound thereto a sulphamate group.
    Type: Application
    Filed: December 20, 2002
    Publication date: August 28, 2003
    Inventors: Michael John Reed, Barry Victor Lloyd Potter
  • Patent number: 6608045
    Abstract: The present invention relates to Streptomyces sp. producing tautomycetin which possesses an immunosuppressive or antibacterial activities, a process for preparing tautomycetin from the said microorganism, and an immunosuppressant or immunosuppressive pharmaceutical composition comprising tautomycetin as an active ingredient which suppresses interleukin-2 production, CD69 and interleukin-2 receptor(IL-2R) expression on the cell surface, and graft rejection in the organ transplantation. The present inventors isolated a soil microorganism which produces a substance possessing antibiotic and immunosuppressive activities, and identified the said microorganism and substance as a novel Streptomyces sp. and tautomycetin, respectively.
    Type: Grant
    Filed: May 17, 1999
    Date of Patent: August 19, 2003
    Assignee: Chong Kun Dang Corporation
    Inventors: Hyoung Sik Chun, Jong Gwan Kim, Hung Bae Chang, Seung Kee Moon, Hyeog Jin Son, Chung Il Hong, Jung Woo Kim, Nam Hyun Lyu
  • Publication number: 20030100537
    Abstract: The invention relates to calcium (3S) tetrahydro-3-furanyl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-(phosphonooxy) propylcarb-amate, to processes for its preparation, and to its use in the treatment of diseases caused by retroviruses.
    Type: Application
    Filed: November 25, 2002
    Publication date: May 29, 2003
    Inventors: Ian Gordon Armitage, Andrew David Searle, Hardev Singh
  • Publication number: 20030096795
    Abstract: The invention relates to calcium (3S) tetrahydro-3-furanyl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-(phosphonooxy)propylcarb-amate, to processes for its preparation, and to its use in the treatment of diseases caused by retroviruses.
    Type: Application
    Filed: November 25, 2002
    Publication date: May 22, 2003
    Inventors: Ian Gordon Armitage, Andrew David Searle, Hardev Singh
  • Patent number: 6566304
    Abstract: The invention relates to use of (a) compounds of phosphorus containing at least partly lipophilic organic radicals together with (b) urea and/or urea derivatives in selected quantity ratios of (a) to (b) as a soil additive for biologically controlling plant-parasitic soil nematodes by strengthening the correspondingly antagonistic soil potential, more particularly by strengthening the growth of antagonistic and/or nematicidal rhizosphere bacteria and/or corresponding mycorrhiza strains—and at the same time strengthening the growth of cultivated plants in soil. The multicomponent mixtures which strengthen bacterial growth are preferably introduced into the region of the plant roots in the form of an aqueous preparation using plant-compatible emulsifiers before and/or during plant growth. Components (a) and (b) are used in such quantity ratios that the ratio by weight of C to N is no higher than 6:1 and preferably no higher than 5:1.
    Type: Grant
    Filed: February 6, 2001
    Date of Patent: May 20, 2003
    Assignee: Cognis Deutschland GmbH
    Inventors: Doris Bell, Bettina Kopp-Holtwiesche, Stephan Von Tapavicza
  • Publication number: 20030092738
    Abstract: Compounds of formula (I) wherein the substituent groups defined by R1, R2, R3 and R4 are each independently selected of H, C(═O)R, P(═O)R′R″, S(═O)R′R″, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl; wherein each of the R′, R″ groups is independently selected from the group consisting of H, OH, NO2, NH2, SH, CN, halogen, ═O, C(═O)H, C(═O)CH3, CO2H, CO2CH3, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstitued aryl; wherein R1, R2, R3 could form part of a heterocyclic ring; R2 can be independently an internal salt; wherein X1, X2 and X3 on formula (I) are independently placed in any particular position of the chain and independently selected of H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′
    Type: Application
    Filed: October 10, 2002
    Publication date: May 15, 2003
    Inventors: Tatsuo Higa, Junichi Tanaka, Dolores Garcia Gravalos
  • Patent number: 6559137
    Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.
    Type: Grant
    Filed: June 23, 2000
    Date of Patent: May 6, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Roger Dennis Tung, Michael Robin Hale, Christopher Todd Baker, Eric Steven Furfine, Istvan Kaldor, Wieslaw Mieczylaw Kazmierski, Andrew Spaltenstein
  • Publication number: 20030078239
    Abstract: The present invention relates to novel ketone compounds, compositions comprising ketone compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising a ketone compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
    Type: Application
    Filed: October 11, 2001
    Publication date: April 24, 2003
    Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
  • Publication number: 20030073639
    Abstract: There is provided a method of treating environmental stress due to the adverse effects of tobacco smoke and automobile exhaust gases. The method of treatment comprises applying to the skin a liniment composition containing one or more ingredients selected from among a group consisting of sulfur containing amino acids, metabolic intermediates of sulfur containing amino acids, tannin and vitamin C and its derivatives. A preferred sulfur containing amino acid is glutathione and preferred metabolic intermediates of sulfur containing amino acids are thiotaurine or hypotaurine. Also, hydroxycarboxylic acid or its derivatives can advantageously be added to this liniment composition to treat environmental stress.
    Type: Application
    Filed: November 7, 2002
    Publication date: April 17, 2003
    Applicant: Shiseido Co., Ltd.
    Inventors: Mariko Egawa, Tetsuo Sakamoto, Yoshiyuki Kohno
  • Publication number: 20030060425
    Abstract: The invention provides compositions comprising formula 1 steroids, e.g., 16&agr;-bromo-3 &bgr;-hydroxy-5&agr;-androstan-17-one hemihydrate and one or more excipients, including compositions that comprise a liquid formulation comprising less than about 3% v/v water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16&agr;-bromo-3&bgr;-hydroxy-5&agr;-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using the compounds. The invention also provides methods to make and use these immunomodulatory compositions and formulations.
    Type: Application
    Filed: March 29, 2001
    Publication date: March 27, 2003
    Inventors: Clarence N. Ahlem, James M. Frincke, Luis Daniel dos Anjos de Carvalho, William Heggie, Patrick T. Prendergast, Christopher L. Reading, Krupakar Paul Thadikonda, Russell N. Vernon