2,4-diketone Pyrimidine Or Derivative (e.g., Uracil, Etc.) Patents (Class 514/50)
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Publication number: 20120093738Abstract: The present invention relates to taste-masked oral formulations of influenza antivirals. The taste-masked pharmaceutical formulations for oral administration comprise one or more influenza antivirals, at least one taste-masking agent and at least one pharmaceutically acceptable excipient. Further, the taste-masked influenza antiviral formulations of the present invention are provided in the form of dispersible tablets, effervescent tablets, orally disintegrating tablets, chewable tablets, bite-dispersion tablets or the like, wherein the bitter taste of influenza antivirals is masked thereby providing palatable formulations.Type: ApplicationFiled: June 10, 2010Publication date: April 19, 2012Applicant: Rubicon Research Private LimitedInventors: Pratibha Sudhir Pilgaonkar, Maharukh Tehmasp Rustomjee, Anilkumar Surendrakumar Gandhi
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Patent number: 8158607Abstract: The disclosure herein relates to a new Lamivudine polymorphic form, methods of making the same, and pharmaceutical formulations thereof. A (?) cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one in the form of monoclinic crystals has characteristic powder X-ray diffractogram, as disclosed herein, is disclosed along with a process for preparation of the same. A pharmaceutical composition in solid dosage unit form comprising a therapeutically effective amount of a new Lamivudine polymorphic form in combination with a pharmaceutically acceptable carrier is also disclosed along with a pharmaceutical composition useful for treating HIV infections in humans.Type: GrantFiled: February 9, 2007Date of Patent: April 17, 2012Assignee: Lupin LimitedInventors: Girij Pal Singh, Dhananjai Srivastava, Manmeet Brijkishore Saini, Pritesh Rameshbhai Upadhyay
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Patent number: 8158606Abstract: It has been discovered that ?-L-2?-deoxynucleosides are active against drug-resistant hepatitis B virus with mutations. A method for treating lamivudine resistant HBV (M552V) in a host is provided that includes administering a ?-L-2?-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug. In addition, a method for preventing lamivudine resistant HBV (M552V) mutation from occurring in a naïve host is provided that includes administering a ?-L-2?-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug. A method for preventing and/or suppressing the emergence of the HBV double mutant (L528M/M552V) in a host is also provided that includes administering a ?-L-2?-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug.Type: GrantFiled: March 21, 2011Date of Patent: April 17, 2012Assignee: Novartis, AGInventors: David Standring, Jean-Pierre Sommadossi, April Patty, Maria Seifer
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Patent number: 8158605Abstract: The present invention is directed toward compounds of Formula (I) as follows: wherein, R is H, R5C(O); R1 is where the crossing dashed line illustrates the bond formed joining R1 to the molecule of Formula (I); R2 and R3 are independently OH or H, provided that R2 and R3 are not simultaneously OH; R4 is H or R5C(O), provided that R and R4 are not simultaneously H; and R5 is a C3-C26 alkenyl, or a pharmaceutical salt thereof. Methods of making and using these compounds are also disclosed.Type: GrantFiled: September 25, 2008Date of Patent: April 17, 2012Assignee: Mount Sinai School of MedicineInventors: Lewis Silverman, James Holland
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Publication number: 20120077772Abstract: The present invention relates to the oral solid pharmaceutical composition comprising lamivudine or a pharmaceutically acceptable salt thereof with isomalt as a filler. The present invention also relate to the combination of lamivudine and other Anti-HIV agents. Thus, for example, the present invention provides a stable tablet formulation comprising lamivudine, isomalt, crospovidone, calcium stearate and opadry white.Type: ApplicationFiled: May 27, 2009Publication date: March 29, 2012Applicant: HETERO RESEARCH FOUNDATIONInventors: Bandi Parthasaradhi Reddy, Male Srinivas Reddy, Pothireddy Venkateswar Reddy, Muppidi Vanaja Kumari
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Patent number: 8143234Abstract: The present invention provides methods of improving a cognitive function or a neurological function, treating or ameliorating a decline in a cognitive function or a neurological function, increasing cytidine levels, or treating a neurological disorder in a subject, comprising administering a uridine, a uridine precursor, or a derivative or metabolite thereof to the subject. The invention also provides methods of improving neural function, comprising contacting the neuron with a uridine, a uridine precursor, or a derivative or metabolite thereof.Type: GrantFiled: September 20, 2004Date of Patent: March 27, 2012Assignee: Massachusetts Institute of TechnologyInventors: Richard J. Wurtman, Carol Watkins
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Publication number: 20120070415Abstract: Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a nucleoside, a nucleotide and an analog thereof. Examples of viral infections include a respiratory syncytial viral (RSV) and influenza infection.Type: ApplicationFiled: September 19, 2011Publication date: March 22, 2012Applicant: ALIOS BIOPHARMA, INC.Inventors: Leonid Beigelman, Jerome Deval, David Bernard Smith, Guangyi Wang, Vivek Kumar Rajwanshi
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Publication number: 20120065156Abstract: Compounds of the formula I: including any possible stereoisomers thereof, wherein: R4 is a monophosphate, diphosphate or triphosphate ester; or R4 is R7 is optionally substituted phenyl, optionally substituted naphthyl, or optionally substituted indolyl; R8 and R8? are hydrogen, C1-C6alkyl, benzyl, or phenyl; or R8 and R8? form C3-C7cycloalkyl; R9 is C1-C10alkyl, C3-C7cycloalkyl, phenyl or phenyl-C1-C6alkyl, wherein the phenyl moiety in phenyl or phenyl-C1-C6alkyl is optionally substituted; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical formulations and the use of compounds I as HCV inhibitors.Type: ApplicationFiled: May 11, 2010Publication date: March 15, 2012Inventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Raboisson, Koen Vandyck, Steven Maurice Van Hoof, Lili Hu, Abdellah Tahri
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Publication number: 20120065145Abstract: This application provides compositions and methods useful in the treatment of certain cancers. In part, this application is based on the recognition that certain molecules that target abasic lesions or AP sites in DNA improve, augment, or potentiate the chemotherapeutic efficacy of certain anticancer agents.Type: ApplicationFiled: July 22, 2011Publication date: March 15, 2012Inventors: Stanton L. Gerson, Lili Liu
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Publication number: 20120064127Abstract: It has now been found that after administration to a diseased person or person that is at risk for developing such disease of a neutraceutical or pharmaceutical composition that comprises a) a lipid fraction comprising at least one of docosahexaenoic acid (DHA), docosapentaenoic acid (DPA) and eicosapentaenoic acid (EPA); b) a protein fraction comprising proteinaceous material from non-human origin which provide at least cysteine and/or taurine; and c) a mineral fraction comprising at least one of manganese and molybdenum, the health of these persons improves. Membrane function of several types of mammalian cells improves, which allows efficient treatment of immune related disorders, such as allergy, autoimmune diseases, cancer, cognitive dysfunction and other diseases of the nervous system, neuropathies, such as diabetic neuropathies and neuropathic pains, neuronal damage during insulin resistance, and gut diseases and support of the development of gut and lung function during growth or recovery.Type: ApplicationFiled: November 11, 2011Publication date: March 15, 2012Applicant: N.V.NUTRICIAInventor: Robert J.J. Hageman
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Publication number: 20120040020Abstract: The present disclosure relates to pyrazine compounds of formula I: wherein L, n, R1, and R2 are as described in the specification. These compounds are useful as inhibitors of ATR protein kinase. The disclosure also relates to pharmaceutically acceptable compositions comprising the compounds of the disclosure; methods of treating of various diseases, disorders, and conditions using the compounds of the disclosure; processes for preparing the compounds of the disclosure; intermediates for the preparation of the compounds of the disclosure; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.Type: ApplicationFiled: October 27, 2011Publication date: February 16, 2012Applicant: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Steven John Durrant, David Kay, Michael O'Donnell, Ronald Marcellus Alphonsus Knegtel, Somhairle MacCormick, Joanne Pinder, Stephen Clinton Young, Haley Marie Binch, Thomas Cleveland, Lev Tyler Dewey Fanning, Dennis James Hurley, Pramod Joshi, Urvi Jagdishbhai Sheth, Alina Silina, Philip Michael Reaper, Anisa Nizarali Virani
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Publication number: 20120034184Abstract: The present invention relates to the use of nucleoside derivatives of formula I wherein B signifies a 9-purinyl residue B1 of formula or a 1-pyrimidyl residue B2 of formula wherein the symbols are as defined in the specification, and of pharmaceutically acceptable salts thereof; for the treatment of diseases mediated by the Hepatitis C Virus (HCV), for the preparation of a medicament for such treatment and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: October 17, 2011Publication date: February 9, 2012Inventors: Rene Robert Devos, Christopher John Hobbs, Wen Rong Jiang, Joseph Armstrong Martin, John Herbert Merrett, Isabel Najera, Nobuo Shimma, Takuo Tsukuda
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Publication number: 20120027879Abstract: Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II: aqueous polar solvent, active compound, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant.Type: ApplicationFiled: August 3, 2011Publication date: February 2, 2012Inventor: Harry A. DUGGER, III
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Publication number: 20120027846Abstract: Methods of using azide-modified biomolecules, such as fatty acids, carbohydrates and lipids, to treat a plant, an insect or an animal infected with a virus or to inhibit infectivity of a virus, such as the human immunodeficiency virus, are provided. Also provided are methods of labeling a virus, such as human immunodeficiency virus, with an azide-modified biomolecule, such as a fatty acid, a carbohydrate, or an isoprenoid lipid. Also, provided are methods of tracking a virus in vivo, with an azide-modified biomolecule, such as a fatty acid, a carbohydrate, or an isoprenoid lipid. The azide-modified biomolecules may be combined with a pharmaceutically acceptable excipient to produce a pharmaceutical composition, optionally containing another anti-viral agent and/or a delivery agent, such as a liposome.Type: ApplicationFiled: July 28, 2011Publication date: February 2, 2012Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Brian AGNEW, David GRAHAM, Upinder SINGH, Scott GRECIAN
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Patent number: 8101652Abstract: Antitumor combinations comprising a taxane and at least one antimetabolite for treating neoplastic diseases are described.Type: GrantFiled: December 30, 2003Date of Patent: January 24, 2012Assignee: Aventis Pharma S.A.Inventor: Marie-Christine Bissery
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Patent number: 8097595Abstract: Induction of telomere shortening, G2 arrest and apoptosis in telomerase positive cancer cells using acyclic nucleoside analogs has been disclosed. In addition, methods for impairment or prevention of tumorigenic telomerase positive cells from having a chance to grow into a tumor and methods for promoting tumor regression (decrease in size of an established tumor) using acyclic nucleoside analogs has been disclosed.Type: GrantFiled: May 12, 2010Date of Patent: January 17, 2012Assignee: ALT Solutions, Inc.Inventor: Igor E. Bondarev
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Patent number: 8097600Abstract: A method and preparation for the stimulation of tear secretion in a subject in need of such treatment is disclosed. The method comprises administering to the ocular surfaces of the subject a purinergic receptor agonist such as uridine 5?-triphosphate (UTP), dinucleotides, cytidine 5?-triphosphate (CTP), adenosine 5?-triphosphate (ATP), or their therapeutically useful analogs and derivatives, in an amount effective to stimulate tear fluid secretion and enhance drainage of the lacrimal system. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include: topical administration via a liquid, gel, cream, or as part of a contact lens or selective release membrane; or systemic administration via nasal drops or spray, inhalation by nebulizer or other device, oral form (liquid or pill), injectable, intra-operative instillation or suppository form.Type: GrantFiled: June 28, 2010Date of Patent: January 17, 2012Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, Karla M. Jacobus, William Pendergast, Janet L. Rideout
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Publication number: 20120010165Abstract: To provide a radiation therapy potentiator, which, when employed in combination with cancer radiation therapy, can reduce radiation dose and can mitigate adverse effects. The invention provides a radiation therapy potentiator containing, as an effective ingredient, a uracil derivative represented by formula (1) (wherein R1 represents a halogen atom or a cyano group; and R2 represents a 4- to 8-membered heterocyclic group having 1 to 3 nitrogen atoms and optionally having as a substituent a lower alkyl group, an imino group, a hydroxyl group, a hydroxymethyl group, a methanesulfonyloxy group, or an amino group; an amidinothio group in which a hydrogen atom attached to a nitrogen atom may be substituted by a lower alkyl group; a guanidino group in which a hydrogen atom attached to a nitrogen atom may be substituted by a lower alkyl group or a cyano group; a lower alkylamidino group; or a 1-pyrrolidinylmethyl group) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 23, 2011Publication date: January 12, 2012Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventor: Masakazu FUKUSHIMA
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Publication number: 20120010161Abstract: The present invention relates to compounds of azapeptide or azapeptidomimetic type of formula (I): in which R1, R2, R3, X1, X2, X3, X4 and Y are as defined in claim 1, to pharmaceutical compositions containing them and to such compounds as adjuvant for an anticancer or anti-infectious medicament.Type: ApplicationFiled: January 25, 2010Publication date: January 12, 2012Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE CLAUDE BERNARD LYON IInventor: Joelle Paris
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Publication number: 20120003316Abstract: This invention relates to a multi-configured, transmucosal pharmaceutical dosage form and, more particularly, to a pharmaceutical dosage form which has a single monolithic/heterogeneous layer or a plurality of such layers. The dosage form is suitable for the delivery of one or more pharmaceutical compositions via the buccal, sublingual, rectal, vaginal or transmucosal delivery route in a human or animal body. It provides for selected delivery profiles resulting from, but not limited to, a porosity-enabled composite matrix of one or more layers/components of the pharmaceutical composition/s. The invention also provides for a method of manufacturing said transmucosal pharmaceutical dosage form in a plurality of configurations.Type: ApplicationFiled: June 3, 2009Publication date: January 5, 2012Inventors: Deshika Reddy, Oluwatoyin Ayotomilola Adeleke, Viness Pillay, Yahya Choonara
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Publication number: 20120004191Abstract: The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or a pyrroloquinolinyl-pyrrolidine-2,5-dione compound in combination with a therapeutically effective amount of a second anti-proliferative agent.Type: ApplicationFiled: July 1, 2011Publication date: January 5, 2012Applicant: ArQule, Inc.Inventors: Giovanni Abbadessa, Dennis S. France, Chang-Rung Chen, Thomas C.K. Chan
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Publication number: 20110312880Abstract: The present invention relates to compounds, in particular, dual antagonists comprising a nucleoside reverse transcriptase inhibitor (NRTI) or a nucleoside competititive reverse transcriptase inhibitor and a non-nucleoside reverse transcriptase inhibitor (NNRTI), linked together using a chemical linker, which may be used to inhibit HIV (HIV-1) reverse transcriptase and in the treatment of HIV infections, more severe cases of HIV infections, including ARC and AIDS, including reducing the likelihood of these infections and disease states.Type: ApplicationFiled: April 9, 2009Publication date: December 22, 2011Inventors: Karen S. Anderson, Roger Hunter
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Patent number: 8076310Abstract: Disclosed herein are novel phosphonate nucleosides and thiophosphonate nucleosides comprising a phosphonalkoxy-substituted or phosphonothioalkyl-substituted five-membered, saturated or unsaturated, oxygen-containing or sulfur-containing ring coupled to a heterocyclic nucleobase such as a pyrimidine or purine base. The invention further relates to compounds having HIV (Human Immunodeficiency Virus) replication inhibiting properties and to compounds having antiviral activities with respect to other viruses. The invention also relates to methods for preparation of all such compounds and pharmaceutical compositions comprising them. The invention further relates to the use of said compounds as a medicine and in the manufacture of a medicament useful for the treatment of subjects suffering from HIV infection, as well as for treatment of other viral, retroviral or lentiviral infections and to the treatment of animals suffering from FIV, viral, retroviral or lentiviral infections.Type: GrantFiled: March 4, 2005Date of Patent: December 13, 2011Assignee: K.U.Leuven Research & DevelopmentInventors: Piet Herdewijn, Christophe Pannecouque, Tongfei Wu, Erik De Clerq
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Publication number: 20110301115Abstract: Provided are methods of treating subclinical sun damage and of inducing a chemocytotoxic response in skin. Methods of treating subclinical sun damage include the steps of: topically administering to skin of a patient a composition comprising a chemocytotoxic agent in an amount effective to induce erythema, scaling, crusting, or combinations thereof and resolve at least a portion of the subclinical sun damage, where the skin has a condition of no clinical sign of sun damage and the patient was not previously treated for actinic keratosis or nonmelanoma skin cancer. The chemocytotoxic agent can comprise a fluorinated pyrimidine antimetabolite such as 5-fluorouracil (FU), 5-fluorouridine (FUR), 5-fluorouridine-5?-monophosphate (FUMP), 5-fluorodeoxyuridine (FUdR), 5-fluorodeoxyuridine-5?-monophosphate (FdUMP), or combinations thereof.Type: ApplicationFiled: January 18, 2011Publication date: December 8, 2011Inventor: Robert K. Ilowite
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Patent number: 8071567Abstract: The present invention relates to the use of nucleoside derivatives of formula Ia wherein the symbols are as defined in the specification, and of pharmaceutically acceptable salts thereof and to pharmaceutical compositions containing such compounds.Type: GrantFiled: September 16, 2009Date of Patent: December 6, 2011Assignee: Roche Palo Alto LLCInventors: Rene Robert Devos, Christopher John Hobbs, Wen Rong Jiang, Joseph Armstrong Martin, John Herbert Merrett, Isabel Najera, Nobuo Shimma, Takuo Tsukuda
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Publication number: 20110293521Abstract: Certain embodiments disclosed relate to compositions, including therapeutic compositions, methods, articles of manufacture, systems, and devices. Certain embodiments relate to anti-viral compositions, methods, articles of manufacture, systems and devices.Type: ApplicationFiled: May 28, 2010Publication date: December 1, 2011Inventors: Roderick A. Hyde, Muriel Y. Ishikawa, Jordin T. Kare, Eric C. Leuthardt, Lowell L. Wood, JR., Victoria Y.H. Wood
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Publication number: 20110293719Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: ApplicationFiled: June 30, 2011Publication date: December 1, 2011Applicant: Ardea Biosciences, Inc.Inventors: Barry D. Quart, Jean-Luc Girardet, Esmir Gunic, Li-Tain Yeh
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Publication number: 20110294737Abstract: Platelets are induced to proliferate, form extensions and produce daughter cells by various methods, including culturing platelets under thrombocytopenic conditions. Expansion of platelet cell numbers increases the storage life of platelets. Modulation of RT activity can be used to produce new daughter platelets. Therefore, the invention provides a new therapeutic use for RT inhibitors that can now be used for treatment of thrombocytopenia and related disorders. Likewise, application of soluble protein factor that may be secreted and/or released by platelets cultured under thrombocytopenic conditions may also be used as a therapeutic agent to increase platelet numbers.Type: ApplicationFiled: October 7, 2009Publication date: December 1, 2011Inventors: Hansjorg Schwertz, Robert C. Blaylock, Larry W. Kraiss, Guy A. Zimmerman, Andrew S. Weyrich
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Patent number: 8067391Abstract: The present invention includes methods of treating or preventing malaria by administering an anti-malarial effective amount of 6-substituted uridine derivatives to a subject need thereof. The invention also includes new 6-substituted uridine derivatives for use as therapeutics, in particular to treat malaria.Type: GrantFiled: October 3, 2006Date of Patent: November 29, 2011Assignee: University Health NetworkInventors: Lakshmi P. Korta, Emil F. Pai, Angelica M. Bello, Masahiro Fujihashi
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Patent number: 8067392Abstract: Compounds, compositions, and methods are provided for treatment of disorders related to mitochondrial dysfunction. The methods comprise administering to a mammal a composition containing pyrimidien nucleotide precursors in amounts sufficient to treat symptoms resulting from mitochondrial respiratory chain deficiencies.Type: GrantFiled: February 16, 2011Date of Patent: November 29, 2011Assignee: Wellstat Therapeutics CorporationInventor: Reid W. Von Borstel
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Publication number: 20110287092Abstract: Compositions comprising decitabine and tetrahydrouridine for the treatment of blood disorders and hematological and solid malignancies are described.Type: ApplicationFiled: December 21, 2009Publication date: November 24, 2011Applicant: The Board of Trustees of the University of IllinoisInventors: Joseph Desimone, Yogen Saunthararajah
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Patent number: 8063025Abstract: Compounds having the formula I or II wherein R1, R2, B, and V are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: GrantFiled: November 26, 2008Date of Patent: November 22, 2011Assignee: Metabasis Therapeutics, Inc.Inventors: Scott J. Hecker, K. Raja Reddy, Zhili Sun, Brett C. Bookser, David Bernard Smith
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Publication number: 20110280959Abstract: A fungicidal composition containing, as active ingredients, (a) a benzoylpyridine derivative represented by the following formula or its salt: wherein X is a halogen atom, a nitro group, a substitutable hydrocarbon group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group, a hydroxyl group, a substitutable alkylthio group, a cyano group, a carboxyl group which may be esterified or amidated, or a substitutable amino group, n is 1, 2, 3 or 4; R1 is a substitutable alkyl group, R2? is a substitutable alkyl group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group or a hydroxyl group, p is 1, 2 or 3, and R2? is a substitutable alkoxy group or a hydroxyl group, provided that at least two of R2? and R2? optionally form a condensed ring containing an oxygen atom and (b) at least one other fungicide.Type: ApplicationFiled: May 26, 2011Publication date: November 17, 2011Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Hisaya NISHIDE, Shigeyuki Nishimura, Shigeru Mitani, Koji Minamida, Fumio Kanamori, Munekazu Ogawa, Shigehisa Kanbayashi, Toyoshi Tanimura, Koji Higuchi, Hidemasa Kominami, Tomohiro Okamoto, Akihiro Nishimura
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Publication number: 20110268801Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: ApplicationFiled: June 30, 2011Publication date: November 3, 2011Applicant: Ardea Biosciences, Inc.Inventors: Barry D. Quart, Jean-Luc Girardet, Esmir Gunic, Li-Tain Yeh
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Publication number: 20110269709Abstract: The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.Type: ApplicationFiled: December 23, 2010Publication date: November 3, 2011Inventor: Apparao Satyam
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Publication number: 20110263526Abstract: The present invention relates to nitric oxide releasing prodrugs of known drugs or therapeutic agents which are represented herein as compounds of formula (I) wherein the drugs or therapeutic agents contain one or more functional groups independently selected from a carboxylic acid, an amino, a hydroxyl and a sulfhydryl group. The invention also relates to processes for the preparation of the nitric oxide releasing prodrugs (the compounds of formula (I)), to pharmaceutical compositions containing them and to methods of using the prodrugs.Type: ApplicationFiled: April 22, 2011Publication date: October 27, 2011Applicant: PIRAMAL LIFE SCIENCES LIMITEDInventor: Apparao SATYAM
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Publication number: 20110262533Abstract: The invention discloses a formulation prepared by granulating at least one anti-retro viral drug and at least one pharmaceutically acceptable additive, using an organic solvent; milling the product; finally processing the milled product to form tablets or capsules.Type: ApplicationFiled: June 10, 2011Publication date: October 27, 2011Inventors: Kiran Kumar Narsaiah VELAVENI, Sanjay Deshraj Verma, Akhilesh Ashok Dixit, Abhijit Mukund Deshmukh, Sanjeev Meharchand Sethi
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Publication number: 20110262525Abstract: This invention relates to compositions and methods useful for treating various cancers. Therapeutic combinations and methods of use thereof are also covered in the present application.Type: ApplicationFiled: December 11, 2007Publication date: October 27, 2011Applicant: SCHERING CORPORATIONInventors: Yan Wang, Chen Zong, Cynthia Seidel-Dugan, Yaolin Wang, Siu-Long Yao, Brian Der-Hua Lu, Mohamad H. Ladha
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Publication number: 20110257120Abstract: This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2?-deoxy-?-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2?-deoxy-?-L-erythro-pentofuranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2?-deoxy-?-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2?-deoxy-?-L-erythro-pentofuranonucleoside or in combination with another anti-hepatitis B agent.Type: ApplicationFiled: June 27, 2011Publication date: October 20, 2011Applicants: Idenix Pharmaceuticals, Inc., L'Universite Montpellier II, Centre National de la Recherche ScientifiqueInventors: Gilles Gosselin, Jean-Louis Imbach, Martin L. Bryant
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Publication number: 20110257109Abstract: The present invention encompasses compositions and methods that activate P2Y receptors for the increased production of new synapses in the central nervous system. The formulations of the invention may be administered to a healthy subject or to a subject in need thereof to restore synapses.Type: ApplicationFiled: April 19, 2011Publication date: October 20, 2011Inventor: Richard WURTMAN
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Patent number: 8034375Abstract: The present invention provides combination therapy methods of treating proliferative diseases (such as cancer) comprising a first therapy comprising administering to an individual an effective amount of a taxane in a nanoparticle composition, and a second therapy which may include, for example, radiation, surgery, administration of chemotherapeutic agents, or combinations thereof. Also provided are methods of administering to an individual a drug taxane in a nanoparticle composition based on a metronomic dosing regime.Type: GrantFiled: February 21, 2006Date of Patent: October 11, 2011Assignee: Abraxis Bioscience, LLCInventors: Neil P. Desai, Patrick Soon-Shiong
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Publication number: 20110244027Abstract: The present invention relates to 2?-Fluoro-6?-methylene carbocyclic nucleosides, pharmaceutical compositions containing these nucleosides and their use in the treatment or prophylaxis of a number of viral infections and secondary disease states and conditions thereof, especially including Hepatitis B virus (HBV) and secondary disease states and conditions thereof (cirrhosis and liver cancer), Heptatitis C virus (HCV), Herpes Simplex virus I and II (HSV-1 and HSV-2), cytomegalovirus (CMV), Varicella-Zoster Virus (VZV) and Epstein Barr virus (EBV) and secondary cancers which occur thereof (lymphoma, nasopharyngeal cancer, including drug resistant (especially including lamivudine and/or adefovir resistant) and other mutant forms of these viruses.Type: ApplicationFiled: May 13, 2011Publication date: October 6, 2011Applicant: University of Georgia Research CenterInventors: Chung K. Chu, Jianing Wang
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Publication number: 20110245156Abstract: Compounds are disclosed. Compositions that include the compounds are disclosed. Methods of making and using the compounds are also disclosed.Type: ApplicationFiled: December 9, 2009Publication date: October 6, 2011Applicant: CYTOKINE PHARMASCIENCES, INC.Inventor: Thais M. Sielecki-Dzurdz
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Publication number: 20110236437Abstract: Provided herein are nanoparticles and methods for using nanoparticles. The nanoparticles include at least three antiretroviral agents. When introduced to cells the nanoparticles cause an increase in the intracellular concentration of the antiretroviral agents to a level that is at least the IC50 against HIV-I or HIV-2. This concentration may be maintained for at least 21 days after the cells are contacted with the nanoparticle. When administered to a subject the nanoparticles cause the concentration of the antiretroviral agents to increase to at least 100 ng/ml in the serum of the subject, at least 0.5 ?g/gram tissue in an organ of the subject, or a combination thereof. Such a concentration may be maintained for at least 21 days after the administration.Type: ApplicationFiled: December 11, 2009Publication date: September 29, 2011Applicant: Creighton UniversityInventor: Christopher J. Destache
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Publication number: 20110230433Abstract: Described herein are novel methods and compositions for treatment of cancer by increasing the mutation rate of cancer cells beyond an error threshold, over which the cancer cells are no longer viable. In particular, mutagenic compounds such as nucleoside analogs for treatment of cancer are also described herein.Type: ApplicationFiled: March 16, 2011Publication date: September 22, 2011Applicant: UNIVERSITY OF WASHINGTONInventors: Lawrence A. Loeb, Edward J. Fox, Marc J. Prindle
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Publication number: 20110223241Abstract: Compositions which comprise a liposomal water-soluble camptothecin and optionally a liposomal fluoropyrimidine in combination with a vascular epithelial growth factor (VEGF) inhibitor such as cetuximab or an epidermal growth factor receptor (EGFR) inhibitor such as bevacizumab are useful in achieving enhanced therapeutic effects for the treatment of cancer.Type: ApplicationFiled: October 16, 2009Publication date: September 15, 2011Applicant: Celator Pharmaceuticals, Inc.Inventors: Paul Tardi, Lawrence Mayer, David Bermudes
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Patent number: 8017594Abstract: To provide a novel anti-psychosocial stress agent which is highly safety and can be continuously taken, more particularly, a novel anti-psychosocial stress agent which prevents or alleviates psychosocial stress. The invention provides an anti-psychosocial stress agent containing, as an active ingredient, uridylic acid, uridine, or uracil. Since uridylic acid, uridine, or uracil, which is an active ingredient of the anti-psychosocial stress agent of the present invention, is inexpensively available and is a biological component, the agent exhibits high safety and can be continuously taken. Therefore, the anti-psychosocial stress agent of the present invention is effective for mitigating, alleviating, or relieving psychosocial stress, which is an issue in modern society. When the anti-psychosocial stress agent is taken before development of symptoms associated with psychosocial stress, the symptoms can be prevented.Type: GrantFiled: June 26, 2007Date of Patent: September 13, 2011Assignee: Yamasa CorporationInventors: Kazuki Endo, Noriyuki Ashida
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Publication number: 20110212913Abstract: The invention provides compositions comprising a therapeutically effective amount of a compound of general formula (I): wherein R1, R2 and R3 may be independently selected from H, OH and OMe; wherein X is C1 or C2 and wherein for C2 each carbon is linked by a single or multiple bond (preferably a double bond) and is substituted with one or more H or OH; for use as a medicament for treating or preventing the development of medical conditions characterised by inappropriate platelet aggregation.Type: ApplicationFiled: November 2, 2009Publication date: September 1, 2011Applicant: PROVEXIS NATURAL PRODUCTS LIMITEDInventor: Niamh O'Kennedy
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Patent number: 8008274Abstract: The present invention provides a method of treating edematous retinal disorders. The method comprises administration of a pharmaceutical formulation comprising a hydrolysis-resistant P2Y receptor agonist to stimulate the removal of pathological extraneous fluid from the subretinal and retinal spaces and thereby reduce the accumulation of said fluid associated with retinal detachment and retinal edema. The P2Y receptor agonist can be administered with therapeutic and adjuvant agents commonly used to treat edematous retinal disorders. The present invention also provides a method of treating cystic fibrosis. The present invention also provides a method of treating sinusitis. The present invention further provides P1-(2?-deoxycytidine 5?-)P4-(uridine 5?-)tetraphosphate, tetra-(alkali metal) salts such as tetrasodium, tetralithium, tetrapotassium, and mixed (tetra-alkali metal) salts.Type: GrantFiled: May 6, 2009Date of Patent: August 30, 2011Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, Ward M. Peterson, Janet L. Rideout, William Pendergast
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Publication number: 20110207688Abstract: The present invention relates to a method of treating an HIV-I infection with a compound according to formula I where R1, R2, R3, R4, R5, are as defined herein.Type: ApplicationFiled: February 20, 2010Publication date: August 25, 2011Inventors: James Patrick Dunn, Todd Richard Elworthy, Dimitrios Stefanidis, Zachary Kevin Sweeney