Oxygen Containing Hetero Ring Patents (Class 514/99)
  • Patent number: 8361444
    Abstract: A fosfomycin plus tobramycin combination formulation for delivery by aerosolization is described. The concentrated fosfomycin tobramycin combination formulation containing an efficacious amount of fosfomycin plus tobramycin is able to inhibit susceptible bacteria. Fosfomycin and tobramycin are formulated separately in a dual ampoule such that when reconstituted, the pH is between 4.5 and 8.0 or as a dry powder. The method for treatment of respiratory tract infections by a formulation delivered as an aerosol having mass median aerodynamic diameter predominantly between 1 to 5?, produced by a jet or ultrasonic nebulizer (or equivalent) or dry powder inhaler.
    Type: Grant
    Filed: December 14, 2010
    Date of Patent: January 29, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: William Baker, David MacLeod
  • Patent number: 8324378
    Abstract: Described herein are neutral prodrugs of phosphorus-containing inhibitors of farnesyl transferase that include one or more phosphate fragments or analogs of phosphate fragments. Analogs of phosphate fragments include various linkers other than oxygen connecting the phosphate fragment to the remaining portion of the drug, such as but not limited to linkers forming phosphoramidates, phosphonates, difluorophosphonates, phosphordiamidates, and the like.
    Type: Grant
    Filed: August 29, 2008
    Date of Patent: December 4, 2012
    Assignee: Purdue Research Foundation
    Inventors: Richard Frederic Borch, Richard Anthony Gibbs, Michelle Martin Clark, Farid Fouad
  • Patent number: 8318700
    Abstract: Methods and compositions are provided for treating lung diseases, including but not limited to infections and small cell and non-small cell lung cancer, by conjugating a drug of interest to glycerol ethers or glycerol phosphate ethers.
    Type: Grant
    Filed: January 18, 2012
    Date of Patent: November 27, 2012
    Assignee: The Regents of the University of California
    Inventors: Karl Y. Hostetler, James R. Beadle
  • Publication number: 20120283177
    Abstract: The invention relates to a pharmaceutical composition for treating the human immunodeficiency virus (HIV) in humans, including three or four active principles selected as: a nucleoside reverse transcriptase inhibitor (NARTI) selected from lamivudine and emtricitabine; a nucleoside or nucleotide reverse transcriptase inhibitor (NARTI) selected from didanosine, abacavir and tenofovir; and the combination of ritonavir with a protease inhibitor (PI) selected from lopinavir, fosamprenavir, atazanavir and darunavir; or an non-nucleoside reverse transcriptase inhibitor (NNRTI) selected from efavirenz and etravirine; for daily administration to said human being one to four days per week.
    Type: Application
    Filed: November 19, 2010
    Publication date: November 8, 2012
    Inventor: Jacques Leibowitch
  • Publication number: 20120283222
    Abstract: Compounds represented by formula (I): wherein each symbol is as defined in the description, and pharmaceutically acceptable salts thereof are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.
    Type: Application
    Filed: May 31, 2012
    Publication date: November 8, 2012
    Applicant: Ajinomoto Co., Inc.
    Inventors: Atsushi KONISHI, Munetaka Tokumasu, Tamotsu Suzuki, Takahiro Koshiba, Koji Ohsumi, Osamu Ikehara, Yuko Kodama
  • Publication number: 20120208787
    Abstract: The present invention relates to a crystalline form of fosamprenavir calcium. The crystalline form of the present invention is designated as Form II of fosamprenavir calcium. The present invention also relates to a process for the preparation of crystalline Form II of fosamprenavir calcium. The present invention further relates to a pharmaceutical composition comprising crystalline Form II of fosamprenavir calcium. The present invention relates further to a method of treating a HIV infection using crystalline Form II of fosamprenariv calium.
    Type: Application
    Filed: June 29, 2010
    Publication date: August 16, 2012
    Applicant: RANBAXY LABORATORIES LIMITED
    Inventors: Satish Manohar Bhoge, Prakash Kshirsagar, Santosh Richhariya, Kaptan Singh
  • Publication number: 20120196835
    Abstract: The invention provides compounds, compositions, and methods for studying the Rohmer pathway and for treating bacterial infections or parasitic infections. The parasitic infection can be a protozoan infection, such as malaria. The compounds and compositions can also be used as antibiotics, for example, to kill bacteria or parasites, or to inhibit bacterial or parasite growth. The invention further provides inhibitors of isoprenoid biosynthesis enzymes, and methods of inhibiting the activity of isoprenoid biosynthesis enzymes. The compounds can be, for example, alkynes or allenes that bind to a unique Fe of an Fe4S4 cluster of an isoprenoid biosynthesis enzyme.
    Type: Application
    Filed: October 8, 2010
    Publication date: August 2, 2012
    Inventors: Eric Olafield, Ke Wang, Weixue Wang, Yonghui Zhang
  • Patent number: 8197838
    Abstract: A novel method of preparing a controlled release composition is disclosed. Specifically, the present invention relates to a method of preparing controlled release compositions of ascorbic acid phosphate and absorbable polymers. Also disclosed is a novel controlled release composition of ascorbic acid phosphate made by the method of the present invention.
    Type: Grant
    Filed: January 14, 2011
    Date of Patent: June 12, 2012
    Assignee: Advanced Technologies and Regenerative Medicine, LLC.
    Inventors: Yufu Li, Stephen Wohlert, Chunlin Yang
  • Publication number: 20120142640
    Abstract: The present invention relates to novel alkyne and alkene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: November 28, 2011
    Publication date: June 7, 2012
    Applicant: ALLERGAN, INC.
    Inventors: Santosh C. Sinha, Smita S. Bhat, Evelyn G. Corpuz, Ken Chow, Wenkui K. Fang, Wha-Bin Im
  • Publication number: 20120135965
    Abstract: The present invention relates to amorphous Fosamprenavir calcium and processes for its preparation, a pharmaceutical composition comprising it and a method for treating a HIV infection therewith.
    Type: Application
    Filed: May 20, 2010
    Publication date: May 31, 2012
    Applicant: RANBAXY LABORATORIES LIMITED
    Inventors: Satish Manohar Bhoge, Prakash Kshirsagar, Santosh Richhariya, Anshul Agrawal, Kaptan Singh
  • Publication number: 20120135062
    Abstract: A wound dressing material comprising: a wound dressing carrier, N-acetyl cysteine or a salt or derivative thereof, and a stabilized ascorbate. Suitably, the stabilized ascorbate comprises an ascorbate-2-polyphosphate. Also provided are wound dressing comprising the materials, methods of treatment with the materials, and methods of making the materials.
    Type: Application
    Filed: May 5, 2010
    Publication date: May 31, 2012
    Applicant: SYSTAGENIX WOUND MANAGEMENT (US),INC.
    Inventor: Lorraine Nisbet
  • Publication number: 20120129813
    Abstract: The present invention relates to novel derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: November 18, 2011
    Publication date: May 24, 2012
    Inventors: Todd M. Heidelbaugh, Phong X. Nguyen
  • Publication number: 20120121698
    Abstract: The present invention relates to, inter alia, pharmaceutical compositions comprising EPA and one or more cardiovascular agents, and to therapeutic methods for treating various diseases and disorders using the same.
    Type: Application
    Filed: April 29, 2010
    Publication date: May 17, 2012
    Applicant: AMARIN PHARMA, INC.
    Inventors: Mehar Manku, Jonathan Rowe
  • Publication number: 20120122818
    Abstract: Methods and compositions are provided for treating lung diseases, including but not limited to infections and small cell and non-small cell lung cancer, by conjugating a drug of interest to glycerol ethers or glycerol phosphate ethers.
    Type: Application
    Filed: January 18, 2012
    Publication date: May 17, 2012
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Karl Y. Hostetler, James R. Beadle
  • Publication number: 20120093922
    Abstract: The present invention relates to, inter alia, pharmaceutical compositions comprising EPA and one or more cardiovascular agents, and to therapeutic methods for treating various diseases and disorders using the same.
    Type: Application
    Filed: April 29, 2010
    Publication date: April 19, 2012
    Applicant: AMARIN CORPORATION PLC
    Inventors: Mehar Manku, Jonathan Rowe
  • Publication number: 20120065171
    Abstract: Novel Fostriecin (or FST) derivatives represented by formula (I), the pharmaceutical compositions and preparation methods thereof. The pharmaceutical uses of these compounds, especially the use for the preparation of pharmaceutical compositions for treating tumor, inhibiting cell over growth, or lowering myocardial infarction and the injury to cells.
    Type: Application
    Filed: October 1, 2010
    Publication date: March 15, 2012
    Applicants: Dalian University of Technology, BayGen Pharm Technology Co., Ltd.
    Inventors: Li Tang, Rongguo Qiu
  • Publication number: 20120045455
    Abstract: Methods of using phosphotetrahydropyran compounds for treatment of fibrotic and scarring disorders, e.g. pulmonary fibrosis, fibrosis associated with surgical procedures, wound healing disorders, scar formation, sclerotic disorders, ocular fibrotic disorders, ocular healing disorders, ocular fibrosis after surgery, glaucoma, tendon scarring disorders, joint scarring disorders, kidney interstitial fibrosis and glomerular fibrosis and tubular fibrosis of the kidney.
    Type: Application
    Filed: April 28, 2010
    Publication date: February 23, 2012
    Applicant: Pharmaxis Pty Limited
    Inventors: Alan D. Robertson, Diego Silva, Ian Alexander McDonald
  • Publication number: 20120015011
    Abstract: Disclosed is a cosmetic composition having a double-shell type nano-structure. More particularly, the nano-structure of the cosmetic composition includes: a water-soluble bioactive ingredient core; a core shell containing poly(ethyleneglycol)-poly(caprolactone)-poly(ethyleneglycol) (PE-PCL-PEG) triblock copolymer in order to include the bioactive ingredient core therein; and an outer shell containing phospholipids or derivatives thereof in order to enclose the core shell therein. Such a cosmetic composition improves stability of active components which are prone to oxidation, light degradation, heat degradation, etc., is formed in a nanoparticle size which in turn shows high transdermal absorption and is very useful to prepare a cosmetic composition stably encapsulating various bioactive ingredients with anti-wrinkle effects, whitening effects, and so forth.
    Type: Application
    Filed: February 9, 2011
    Publication date: January 19, 2012
    Applicant: WOONGJIN COWAY CO., LTD.
    Inventors: Sung-Bo SHIM, Byoung-Young JEON, Joo-Hyuck LIM, Jong-Keun CHOI, Yong-Joon JOO, Jin-Hun CHO
  • Patent number: 8093230
    Abstract: The invention concerns the use of mercaptoethane sulfonate-sodium (Mesna) to increase the solubility of Ifosfamide in storage-stable, concentrated and/or highly-concentrated (supersaturated) aqueous pharmaceutical preparations, storage-stable, concentrated and/or highly-concentrated (supersaturated) aqueous pharmaceutical Ifosfamide preparations for parenteral administration as well as a process for their production.
    Type: Grant
    Filed: September 28, 2004
    Date of Patent: January 10, 2012
    Assignee: Baxter International Inc.
    Inventor: Berthold Roessler
  • Publication number: 20110288053
    Abstract: The invention is related to phosphorus substituted compounds with antiviral activity, 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: July 20, 2011
    Publication date: November 24, 2011
    Applicant: Gilead Sciences, Inc.
    Inventors: Constantine G. Boojamra, Carina Cannizzaro, James M. Chen, Xiaowu Chen, Aesop Cho, Lee S. Chong, Maria Fardis, Heolun Jin, Ralph F. Hirschmann, Alan X. Huang, Choung U. Kim, Thorsten Kirschberg, Christopher P. Lee, William A. Lee, Richard L. Mackman, David Y. Markevitch, David A. Oare, Vidya K. Prasad, Hyung-Jung Pyun, Adrian S. Ray, Rosemarie Sherlock, Sundaramoothi Swaninathan, William J. Watkins, Jenneifer Zhang
  • Publication number: 20110287083
    Abstract: Bioabsorbable compositions of A) blends of bioabsorbable homopolymers and/or copolymers containing glycolide and lactide and B) salts of fatty acids and/or fatty acid esters are described. Processes for making the compositions and surgical articles made totally or in part therefrom, including suture coatings, are also described.
    Type: Application
    Filed: July 21, 2011
    Publication date: November 24, 2011
    Applicant: Tyco Healthcare Group LP
    Inventor: Ahmad R. Hadba
  • Publication number: 20110280855
    Abstract: The field of invention relates to Vitamin C compositions, and in particular to Vitamin C compositions containing ascorbate-glucose transport enhancers. In at least one aspect, a composition is provided herein that includes ascorbate in an amount from about 0.1% by weight of actives to about 99.9% by weight of actives, and at least one ascorbate-glucose transport enhancer in an amount from about 0.01% by weight of actives to about 99.0% by weight of actives. In other aspects, methods of improving the transport of ascorbate into cells and tissues, and improving the ascorbate or antioxidant status of a person, are provided that include providing a composition comprising ascorbate and at least one ascorbate-glucose transport enhancer.
    Type: Application
    Filed: June 3, 2011
    Publication date: November 17, 2011
    Inventor: Neil Levin
  • Publication number: 20110269675
    Abstract: A method for the treatment and/or prophylaxis of an osteonecrotic bone disease in a mammal in need thereof, such as, e.g., idiopathic or secondary osteonecrosis, avascular bone necrosis, glucocorticoid induced bone ischemia/osteonecrosis, Legg-Calve-Perthes disease and femoral head necrosis, the method comprising administering an effective dose of a strontium-containing compound (a) to the mammal. A method for the treatment and/or prophylaxis of an osteonecrotic bone disease, such as, e.g., idiopathic or secondary osteonecrosis, avascular hone necrosis, glucocorticoid induced bone ischemia/osteonecrosis and femoral head necrosis, in a mammal who is to be or is treated with a therapeutic agent (b) known to or suspected of inducing apoptosis and/or necrosis of bone cells, the method comprising administering a strontium-containing compound (a) in combination with (b).
    Type: Application
    Filed: July 14, 2011
    Publication date: November 3, 2011
    Inventors: Christian HANSEN, Henrik NILSSON, Stephan CHRISTGAU, Henry G. BONE, III
  • Publication number: 20110269677
    Abstract: The invention provides protease inhibitors that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the protease inhibitors not attached to the water-soluble oligomer.
    Type: Application
    Filed: March 12, 2008
    Publication date: November 3, 2011
    Applicant: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, Lin Cheng, Tacey X. Viegas, Xuyuan Gu, Franco J. Duarte, Wen Zhang
  • Publication number: 20110257078
    Abstract: There is described a composition comprising a therapeutically active imidazole, and derivatives thereof, and an agent active on a bacterial cell surface selected from the group consisting of one or more of colistin, nisin, D-cycloserine, fosfomycin, fosfomycin trometamol, fosfomycin disodium and polymixin B, and derivatives thereof.
    Type: Application
    Filed: July 17, 2009
    Publication date: October 20, 2011
    Applicant: E-THERAPEUTICS PLC
    Inventors: Malcolm Philip Young, Catherine Mary Thomas
  • Publication number: 20110251159
    Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.
    Type: Application
    Filed: June 17, 2011
    Publication date: October 13, 2011
    Applicant: Threshold Pharmaceuticals, Inc.
    Inventors: Mark Matteucci, Jian-Xin Duan, Hailong Jiao, Jacob Kaizerman
  • Patent number: 8017596
    Abstract: The invention concerns novel phosphonate derivatives, preparation method, use thereof as ligands modulating T ?9?2 lymphocyte activity and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: January 14, 2010
    Date of Patent: September 13, 2011
    Assignee: Innate Pharma, S.A.
    Inventors: Jean-Louis Montero, Ibrahim Zgani, Chantal Menut, Valérie Gallois
  • Patent number: 8017597
    Abstract: An object of the present invention is to elucidate an analgesic effect as one of new cPA bioactivities and thus to provide a novel analgesic agent. The present invention provides an analgesic agent which comprises a cyclic phosphatidic acid derivative that is one type of phospholipid.
    Type: Grant
    Filed: October 19, 2010
    Date of Patent: September 13, 2011
    Assignee: Ochanomizu University
    Inventors: Kimiko Murofushi, Harumi Kanashiki
  • Patent number: 8003625
    Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.
    Type: Grant
    Filed: June 29, 2006
    Date of Patent: August 23, 2011
    Assignee: Threshold Pharmaceuticals, Inc.
    Inventors: Mark Matteucci, Jian-Xin Duan, Hailong Jiao, Jacob Kaizerman
  • Publication number: 20110165202
    Abstract: The present invention relates to solid state forms of fosamprenavir calcium salt, process for preparing said solid state forms, and pharmaceutical compositions thereof.
    Type: Application
    Filed: January 6, 2011
    Publication date: July 7, 2011
    Applicant: PLIVA HRVATSKA D.O.O.
    Inventors: Edislav LEKSIC, Dragan SEPAC, Dubravka PAVLICIC
  • Publication number: 20110123468
    Abstract: Described is the use of benzotropolone and their derivatives, especially the compounds of formula (1); wherein R2, R3, R4, R5 and R6 independently of one another are hydrogen; OH; C1-C30alkyl, C2-C30al-kenyl, C1-C30alkoxy, C3-C12cycloalkyl or C1C30hydroxyalkyl, which may be substituted by one or more E and/or interrupted by one or more D; C6-C20aryl, which may be substituted by one or more G; C4-C20heteroaryl, which may be substituted by one or more G, C2-C18alkenyl, C2-C18alkynyl, C7-C25aralkyl, CN, or —CO—R17; C1-C30mono- or dialkylamino; COR9; COOR9; CONR9R10; CN; SO2R9; OCOOR9; OCOR9; NHCOOR9; NR9COR10; NH2; *—(CO)—NH—(CH2)n1—(PO)—(OR11)2; —(CO)—O—(CH2)n1—(PO)—(OR11)2; sulphate; sulphonate; phosphate; phosphonate; —(CH2)n2—[O—(SO2)]n3—OR11; —O—(CH2)n4(CO)n5—R11; —(O)n6—(CH2)n7—(PO)—(OR9)2; —(O)n6—(CH2)n7—SO2—OR9; halogen; organosilanyl; organo-siloxanyl; or a sugar residue linked directly in an ?- or ?-mode via the anomeric oxygen to the benzotropolone system or via a linear or branched alkylene, alkenyle
    Type: Application
    Filed: June 18, 2009
    Publication date: May 26, 2011
    Applicant: BASF SE
    Inventors: Barbara Wagner, Reinhold Ohrlein, Bernd Herzog, Kai Eichin, Gabriele Baisch, Stephanie Portmann
  • Publication number: 20110117030
    Abstract: A fosfomycin plus tobramycin combination formulation for delivery by aerosolization is described. The concentrated fosfomycin tobramycin combination formulation containing an efficacious amount of fosfomycin plus tobramycin is able to inhibit susceptible bacteria. Fosfomycin and tobramycin are formulated separately in a dual ampoule such that when reconstituted, the pH is between 4.5 and 8.0 or as a dry powder. The method for treatment of respiratory tract infections by a formulation delivered as an aerosol having mass median aerodynamic diameter predominantly between 1 to 5?, produced by a jet or ultrasonic nebulizer (or equivalent) or dry powder inhaler.
    Type: Application
    Filed: December 14, 2010
    Publication date: May 19, 2011
    Inventors: William Baker, David MacLeod
  • Patent number: 7943118
    Abstract: A fosfomycin plus tobramycin combination formulation for delivery by aerosolization is described. The concentrated fosfomycin tobramycin combination formulation containing an efficacious amount of fosfomycin plus tobramycin is able to inhibit susceptible bacteria. Fosfomycin and tobramycin are formulated separately in a dual ampoule such that when reconstituted, the pH is between 4.5 and 8.0 or as a dry powder. The method for treatment of respiratory tract infections by a formulation delivered as an aerosol having a mass median aerodynamic diameter predominantly between 1 to 5?, produced by a jet or ultrasonic nebulizer (or equivalent) or dry powder inhaler.
    Type: Grant
    Filed: May 2, 2005
    Date of Patent: May 17, 2011
    Assignee: Gilead Sciences, Inc.
    Inventors: William Baker, David MacLeod
  • Patent number: 7943588
    Abstract: The present invention is a method for preventing or treating neuropathic pain. Using an agent to decrease the expression or activity of Toll-like receptor 4 (TLR4), behavioral hypersensitivity is attenuated thereby preventing or treating neuropathic pain in a subject in need of such treatment.
    Type: Grant
    Filed: March 27, 2007
    Date of Patent: May 17, 2011
    Assignee: Trustees of Dartmouth College
    Inventors: Joyce A. DeLeo, Flobert Y. Tanga
  • Publication number: 20110104232
    Abstract: A novel method of preparing a controlled release composition is disclosed. Specifically, the present invention relates to a method of preparing controlled release compositions of ascorbic acid phosphate and absorbable polymers. Also disclosed is a novel controlled release composition of ascorbic acid phosphate made by the method of the present invention.
    Type: Application
    Filed: January 14, 2011
    Publication date: May 5, 2011
    Inventors: Yufu Li, Stephen Wohlert, Chunlin Yang
  • Publication number: 20110008461
    Abstract: A PEPCK inhibitor can include identifying a molecule that has a size capable of fitting into and interacting with the PEPCK binding site and at least one of the following: (a) a first terminal substituent having co-planar atoms acting as metal ligands to the active site metal ion PEPCK; (b) at least one of an atom or substituent at positions 2 or 3 from the first terminal substituent includes a neutral carbon center or include an oxygen, sulfur, selenium, or other atom with similar physiochemical properties; (c) at least one of an atom or substituent at positions 2 or 3 from the first terminal substituent is devoid of an electropositive atom or substituents; or (d) a second terminal substituent opposite of the first terminal substituent, said second terminal substituent having an atom that is a hydrogen boding acceptor and/or is negatively charged.
    Type: Application
    Filed: July 12, 2010
    Publication date: January 13, 2011
    Inventors: Gerald Carlson, Todd Holyoak, Sarah Sullivan, Rose Mary Stiffin
  • Publication number: 20110002879
    Abstract: The invention provides a combination comprising a cytotoxic compound, a signalling inhibitor, an ancillary agent, or two or more further anti-cancer agents, and a compound having the formula (Ib): or salts or tautomers or N-oxides or solvates thereof; wherein X is a group R1-A-NR4—; A is a bond, C?O, NRg(C?O) or O(C?O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from fluorine, hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from O, S, NH, SO, SO2; R2 is hydrogen; halogen; C1-4 alkoxy (e.g.
    Type: Application
    Filed: April 1, 2010
    Publication date: January 6, 2011
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Jayne Elizabeth CURRY, John Francis LYONS, Matthew Simon SQUIRES, Neil Thomas THOMPSON, Kyla Merriom THOMPSON, Paul Graham WYATT, Neil James GALLAGHER
  • Publication number: 20110003764
    Abstract: The present invention relates to a drug combination capable of conferring therapeutic benefits in the treatment of both AIDS and malaria. In particular, it relates to a drug combination including at least one quinolinic antimalarial compound such as chloroquine or hydroxychloroquine, and at least one inhibitor of the Human Immunodeficiency Virus (HIV) protease enzyme. This drug combination is capable of inhibiting the replication of both HIV and Plasmodium sp. It also relates to the direct antimalarial effects of the HIV PIs.
    Type: Application
    Filed: May 26, 2009
    Publication date: January 6, 2011
    Inventor: Andrea Savarino
  • Publication number: 20100305065
    Abstract: There is provided the use of compounds of formula wherein R1, R2, R3 and E have meanings given in the description, for the preparation of a medicament for killing clinically latent microorganisms. There is also provided the use of compounds of formula I for treating microbial infections, as well as certain compounds of formula (I) per se.
    Type: Application
    Filed: May 16, 2008
    Publication date: December 2, 2010
    Applicant: HELPERBY THERAPEUTICS LIMITED
    Inventors: Mandy Christine Beswick, Susan Mary Cramp, Yanmin Hu, Thomas David Pallin, Hazel Joan Dyke, Anthony Coates
  • Publication number: 20100298272
    Abstract: A new anticancer compounds of formula (1) Drugs and pharmaceutical compositions to be used in human or veterinary medicine, which include at least one compound of formula (1).
    Type: Application
    Filed: July 7, 2008
    Publication date: November 25, 2010
    Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Jean-Luc Pirat, David Virieux, Ludovic Clarion, Jean-Noel Volle, Norbert Bakalara, Marcel Mersel, Jerome Montbrun, Henri-Jean Cristau
  • Publication number: 20100249072
    Abstract: Described herein are neutral prodrugs of phosphorus-containing inhibitors of farnesyl transferase that include one or more phosphate fragments or analogs of phosphate fragments. Analogs of phosphate fragments include various linkers other than oxygen connecting the phosphate fragment to the remaining portion of the drug, such as but not limited to linkers forming phosphoramidates, phosphonates, difluorophosphonates, phosphordiamidates, and the like.
    Type: Application
    Filed: August 29, 2008
    Publication date: September 30, 2010
    Applicant: PURDUE RESEARCH FOUNDATION
    Inventors: Richard Frederic Borch, Richard Anthony Gibbs, Michelle Martin Clark, Farid Fouad
  • Publication number: 20100216697
    Abstract: The invention relates to the use of a pharmaceutical composition for the local treatment or prevention of a tissue infection at an infection site, the pharmaceutical composition comprising at least two different antibiotics of group A or pharmaceutically acceptable derivatives thereof, or an antibiotic of group A and at least one antibiotic of group B or pharmaceutically acceptable derivatives thereof. Group A comprises primarily intracellular active antibiotics working as inhibitor of bacterial RNA polymerase; as inhibitor of gyrase; or as inhibitor of bacterial protein synthesis. Group B comprises primarily extracellular active antibiotics working as inhibitor of bacterial cell wall synthesis; or inhibitor of bacterial protein synthesis; or by direct destabilisation or rupture of the bacterial cell wall.
    Type: Application
    Filed: July 23, 2008
    Publication date: August 26, 2010
    Applicant: BIOMET DEUTSCHLAND GmbH
    Inventor: Nicole Duewelhenke
  • Publication number: 20100204184
    Abstract: The invention concerns novel phosphonate derivatives, preparation method, use thereof as ligands modulating T ?9?2 lymphocyte activity and pharmaceutical compositions comprising them.
    Type: Application
    Filed: January 14, 2010
    Publication date: August 12, 2010
    Applicants: LABORATOIRES MAYOLY SPINDLER, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE MONTPELLIER II
    Inventors: Jean-Louis Montero, Ibrahim Zgani, Chantal Menut, Valérie Gallois
  • Publication number: 20100167936
    Abstract: The invention relates to the use of at least one ascorbic acid derivative for the functionalisation of matrices, and to specific ascorbic acid derivatives and processes for the preparation thereof.
    Type: Application
    Filed: June 27, 2007
    Publication date: July 1, 2010
    Inventors: Thomas Rudolph, Philipp Buehle, Herwig Buchholz
  • Publication number: 20100152139
    Abstract: An emulsified skin external preparation containing a salt of a higher fatty acid ester of ascorbic acid-2-phosphate is provided, and the decomposition and consequent decrease of the salt are prevented and thereby the stability of the preparation is enhanced. A method for stabilizing the skin external preparation containing a salt of a higher fatty acid ester of ascorbic acid-2-phosphate is provided. The emulsified skin external preparation includes 0.03 to 25% by mass of a salt of a higher fatty acid ester of ascorbic acid-2-phosphate (A), and 0.05 to 25% by mass of a glycerin mono fatty acid ester (B), the higher fatty acid ester of ascorbic acid-2-phosphate being represented by Formula (1): . . . (1) wherein R is a higher fatty acid residue.
    Type: Application
    Filed: July 24, 2006
    Publication date: June 17, 2010
    Applicant: SHOWA DENKO K.K.
    Inventors: Tadashi Yoneda, Naoko Ito, Kazuo Furuya
  • Publication number: 20100137254
    Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered along or in combination with one or more anti-neoplastic agents.
    Type: Application
    Filed: June 29, 2006
    Publication date: June 3, 2010
    Inventors: Mark Matteucci, Jian-Xin Duan, Hailong Jiao
  • Publication number: 20100105638
    Abstract: The present invention relates to the use of ascorbyl phosphate and niacinamide to suppress the crystallization of biotin in cosmetic or dermatological compositions. Furthermore, the invention relates to cosmetic or dermatological compositions comprising ascorbyl phosphate, niacinamide, biotin and a cosmetically acceptable carrier.
    Type: Application
    Filed: February 28, 2008
    Publication date: April 29, 2010
    Inventors: Kerstin Den-Braven, Christine Saecker, Horst Westenfelder
  • Publication number: 20100099636
    Abstract: A hydrous gel substantially comprising at least two polymers selected from the group consisting of polyacrylic acid, sodium polyacrylate and partially neutralized polyacrylate, and water, the polymers being crosslinked by containing an aluminum compound, wherein the pH when the hydrous gel is 100-fold diluted with purified water is from 6.5 to 8.5. A hydrous gel which can stably hold an ascorbic acid or a derivative thereof, has high gel strength, exhibits good adhesion to an adherend and causes no liquid syneresis can be provided.
    Type: Application
    Filed: December 18, 2009
    Publication date: April 22, 2010
    Applicant: SHOWA DENKO K.K.
    Inventor: Tetsuya ISHII
  • Publication number: 20100063005
    Abstract: The present invention provides methods for treating a bacterial infection and/or bacterial airway colonization in a subject by administering via pulmonary administration an effective amount of fosfomycin as the only active pharmaceutical ingredient. Methods of the present invention are useful in treating bacterial pneumonia infection of any type and/or airway colonization, cystic fibrosis with bacterial infection and/or bacterial lung and/or airway colonization.
    Type: Application
    Filed: December 11, 2007
    Publication date: March 11, 2010
    Inventor: Kaare Fiala
  • Publication number: 20100063003
    Abstract: Pet food comprising trisodium L-ascorbic acid-2-monophosphate (STAY-050) or sodium-calcium L-ascorbic acid-2-monophosphate (STAY-C35), or mixtures thereof and, optionally, a polymer (for fixation of the ascorbate on the dental surface) and use 5 thereof as additive to pet food for preventing or treating calculus, plaque, gingivitis and periodontal disease and for enhancing the antioxidative capacity in the whole organism.
    Type: Application
    Filed: November 12, 2009
    Publication date: March 11, 2010
    Applicant: DSM IP ASSETS B.V.
    Inventors: Stephanie Krammer, Joachim Pheiffer