Diazoles (including Hydrogenated) Patents (Class 514/94)
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Publication number: 20100215743Abstract: The present invention provides methods of treating or preventing a medical condition that is responsive to a bisphosphonate compound in a subject. The methods comprise administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of the bisphosphonate no less frequently than a bi-weekly dosage schedule. In some embodiment, the bisphosphonate compound is zoledronic acid.Type: ApplicationFiled: February 25, 2010Publication date: August 26, 2010Inventor: Thomas W. Leonard
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Publication number: 20100216747Abstract: An object of the present invention is to provide a preventive drug and a therapeutic drug for diseases caused by abnormal bone metabolism, especially osteoporosis, which is more effective than conventional drugs. Combined use of N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}-benzamidine, or a salt thereof; and at least one compound selected from the group consisting of etidronic acid, clodronic acid, pamidronic acid, tiludronic acid, risedronic acid, minodronic acid, ibandronic acid, zoledronic acid, and salts thereof can exert higher bone resorption inhibitory effect and provide a preventive effect and a therapeutic effect for diseases caused by abnormal bone metabolism, especially osteoporosis as compared with administration of the respective agents respectively.Type: ApplicationFiled: August 1, 2008Publication date: August 26, 2010Applicant: TEIJIN PHARMA LIMITEDInventors: Eiji Ochiai, Miyuki Nishiga, Kenichiro Takagi, Yoshiaki Azuma
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Publication number: 20100190751Abstract: The present invention relates to combinations comprising neramexane and a Glutamate Release Inhibitor (GRI) and the use of such combinations in the treatment of neurodegenerative disorders.Type: ApplicationFiled: July 25, 2008Publication date: July 29, 2010Applicant: MERZ PHARMA GmbH & CO. KGaAInventors: Angelika Hanschmann, Michael Althaus, Alexander Gebauer, Christopher Parsons, Wojciech Danysz
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Publication number: 20100190752Abstract: A composition of matter comprising in combination as component (a) at least one 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol compound, and as component (b) at least one antiepileptic, a pharmaceutical formulation and a dosage form comprising said composition of matter, and a method of treating pain, e.g. neuropathic pain, in which components (a) and (b) are administered simultaneously or sequentially to a mammal, whereby component (a) may be administered before or after component (b) and whereby components (a) or (b) are administered to the mammal either via the same or a different pathway of administration.Type: ApplicationFiled: January 26, 2010Publication date: July 29, 2010Applicant: Gruenenthal GmbHInventors: Klaus Schiene, Petra Bloms-Funke, Thomas Christoph
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Patent number: 7763596Abstract: This invention is directed to a method for treating an inflammatory condition, treating haematological and other malignancies, causing immunosuppression, or preventing or treating transplant rejection in man or other animals which comprises administering to a patient a compound that has the structure of Formula (I) or Formula (II) as defined below, or a pharmaceutically acceptable derivative thereof or pro-drug therefor, wherein R?NH2, NHR1, NHOR2, NHNHR2, NHCOR2, and R1?C(1-4)alkyl, C(3-6)cycloalkyl, Cn, where n=1-3, R2=methyl, ethyl, R3=alkyl, cycloalkyl, substituted alkyl, substituted cycloalkyl, aryl, heteroaryl, substituted aryl, or substituted hetrecoaryl; wherein R4, R5?C(1-4)alkyl. Novel compounds according to Formula (III), wherein R6 and R7 are any of H, CH3CO, CH3CH2CO, CH3CH2CH2CO provided that R6 and R7 are not both H, or Formula (IV), wherein R8 and R9 are any of H, CH3CO, CH3CH2CO or CH3CH2CH2CO, having use in such methods, are also described.Type: GrantFiled: April 19, 2007Date of Patent: July 27, 2010Assignee: The University of ManchesterInventors: Stephen Alexander Barr, Michael Anthony McKervey, Hughes Jean-Pierre Miel, David William Ray, Andrew Michael Brass
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Publication number: 20100183742Abstract: Compositions containing, and, methods administering, TH302, are useful in treatment of cancer and other hyper-proliferative diseases.Type: ApplicationFiled: December 21, 2007Publication date: July 22, 2010Applicant: Threshold Pharmaceuticals, IncInventors: Steve Ammons, Jian-Xin Duan, Donald Jung, Mark Matteucci
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Publication number: 20100166865Abstract: A method of Nanoparticle-based therapy for a mammalian subject is disclosed. The method uses Nanoparticles and/or Nanoparticles with outer surfaces that contain an affinity moiety effective to bind specifically to a biological surface at which the therapy is aimed, and a hydrophilic polymer coating. The hydrophilic polymer coating is made up of polymer chains either covalently linked or surface adsorbed to the polymer components.Type: ApplicationFiled: August 15, 2007Publication date: July 1, 2010Applicant: NOVARTIS AGInventors: Saran Kumar, Wen-Chung Shieh, Seema Tomer, Joseph Lawrence Zielinski
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Publication number: 20100168067Abstract: This invention relates to the finding that the presence of polymorphisms in and around the farnesyl diphosphate synthase (FDPS) gene is predictive of the densitometric response of patients with bone disorders, such as osteoporosis, subsequent to commencing treatment with amino-bisphosphonates. Methods relating to the identification of individuals having bone disorders which are responsive to bisphosphonates and predicting the responsiveness of individuals with bone disorders to treatment with a bisphosphonate are provided.Type: ApplicationFiled: March 19, 2007Publication date: July 1, 2010Applicant: UCL BUSINESS PLCInventors: John Chamberlain, Halina Fitz-Clarence, Mark Thomas
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Publication number: 20100144679Abstract: The present invention provides a multi-component kit comprising a therapeutically effective amount of a bisphosphonate or analogue thereof in combination with an effective amount of Vitamin D, a metabolite thereof, a precursor thereof or an analogue thereof, wherein the kit provides instructions for daily dosing and correct chronological order of administration of components to provide a dosing regime for reducing secondary osteoporotic skeletal fractures in subjects at risk for vitamin D deficiency.Type: ApplicationFiled: March 21, 2008Publication date: June 10, 2010Applicant: DUKE UNIVERSITYInventor: Kenneth W. Lyles
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Publication number: 20100137255Abstract: Membrane permeable prodrugs of creatine phosphate analogs, pharmaceutical compositions comprising membrane permeable prodrugs of creatine phosphate analogs, and methods of treating diseases such as ischemia, heart failure, and neurodegenerative disorders comprising administering prodrugs of creatine phosphate analogs, or pharmaceutical compositions thereof are disclosed.Type: ApplicationFiled: February 3, 2010Publication date: June 3, 2010Applicant: XenoPort, Inc.Inventors: Noa Zerangue, Qingzhi Gao, William J. Dower
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Publication number: 20100137254Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered along or in combination with one or more anti-neoplastic agents.Type: ApplicationFiled: June 29, 2006Publication date: June 3, 2010Inventors: Mark Matteucci, Jian-Xin Duan, Hailong Jiao
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Publication number: 20100120720Abstract: The invention relates to the use of a hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor and of a farnesyl-pyrophosphate synthase inhibitor, or of one of their associated physiologically acceptable salts, in the preparation of a composition, particularly a pharmaceutical composition, for use in the treatment of human or animal, pathological or nonpathological situations related to the accumulation and/or the persistence of prenylated proteins in cells, such as during progeria (Hutchinson-Gilford syndrome), restrictive dermopathy or physiological aging.Type: ApplicationFiled: July 5, 2007Publication date: May 13, 2010Applicant: UNIVERSITE DE LA MEDITERRANEE AIX-MAR SEILLE IIInventors: Nicolas Levy, Pierre Cau, Carlos Lopez-Otin
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Publication number: 20100112061Abstract: A mutual prodrug of a MRA and a (?-agonist for formulation for delivery by aerosolization to inhibit pulmonary bronchoconstriction is described. The mutual prodrug is preferably formulated in a small volume solution (10-500 ?L) dissolved in a quarter normal saline having pH between 5.0 and 7.0 for the treatment of respiratory tract bronchoconstriction by an aerosol having mass median average diameter predominantly between 1 to 5?, produced by nebulization or by dry powder inhaler.Type: ApplicationFiled: December 12, 2007Publication date: May 6, 2010Inventors: William Baker, Marcin Stasiak, Sundaramoorthi Swaminathan, Musong Kim
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Patent number: 7687481Abstract: The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and/or cardiometabolic disorders.Type: GrantFiled: March 9, 2007Date of Patent: March 30, 2010Assignee: Jenrin Discovery, Inc.Inventors: John Francis McElroy, Robert J. Chorvat
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Patent number: 7687636Abstract: The invention relates to polymorphs of zoledronic acid and zoledronate sodium salts, amorphous zoledronate sodium salt, processes for making the polymorphs and amorphous zoledronate sodium salt, and pharmaceutical compositions containing the polymorphs and amorphous zoledronate sodium salt.Type: GrantFiled: September 25, 2006Date of Patent: March 30, 2010Assignee: Teva Pharmaceutical Industries LtdInventors: Judith Aronhime, Revital Lifshitz-Liron
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Publication number: 20100068211Abstract: A method of preventing or treating ionizing radiation-associated loss of bone mass, bone density or bone strength in a subject is provided, comprising administering to the subject an amount of an antiresorptive or osteoclast inhibiting compound sufficient to prevent or mitigate loss of bone mass, density or strength. A method of preventing or treating radiation-associated increase in the number or activity of osteoclasts in a subject is also provided, comprising administering to the subject an amount of an antiresorptive compound sufficient to reduce osteoclast numbers or reduce osteoclast activity and prevent resulting loss of bone mass, density or strength.Type: ApplicationFiled: February 9, 2009Publication date: March 18, 2010Inventors: Ted A. Bateman, Jeffrey S. Willey
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Patent number: 7678778Abstract: The present disclosure relates to salts and compositions of isophosphoramide mustard and isophosphoramide mustard analogs. In one embodiment the salts can be represented by the formula wherein A+ represents an ammonium species selected from the protonated (conjugate acid) or quaternary forms of aliphatic amines and aromatic amines, including basic amino acids, heterocyclic amines, substituted and unsubstituted pyridines, guanidines and amidines; and X and Y independently represent leaving groups. Also disclosed herein are methods for making such compounds and formulating pharmaceutical compositions thereof. Methods for administering the disclosed compounds to subjects, particularly to treat hyperproliferative disorders, also are disclosed.Type: GrantFiled: October 25, 2005Date of Patent: March 16, 2010Assignee: DEKK-TEC, Inc.Inventor: Lee Roy Morgan
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Publication number: 20100056481Abstract: The invention relates to new crystalline forms of low water soluble salts of zoledronic acid, the process for preparation of these crystalline forms, compositions containing these crystalline forms, and the use of these crystalline forms in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans. The invention relates to the crystalline form of the free acid monohydrate of zoledronic acid, the process for preparation of the crystalline form of the free acid monohydrate of zoledronic acid, compositions containing the crystalline form of the free acid monohydrate of zoledronic acid, and the use of crystalline form of the free acid monohydrate of zoledronic acid in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans.Type: ApplicationFiled: November 26, 2007Publication date: March 4, 2010Inventors: Alexandra Glausch, Olivier Lohse, Michael Mutz, Holger Petersen, Juergen Sigg, Caspar Vogel, Hans-Joachim Weber
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Publication number: 20100048511Abstract: Provided is a solid dispersion comprising vitamin D or a derivative thereof and a cyclodextrin; a complex formulation for the prevention or treatment of osteophorosis, which includes the solid dispersion and a bisphosphonate; and a method for preparing said complex formulation. The complex formulation can maintain a constant therapeutic level of vitamin D or a derivative thereof through its improved drug stability, while enhancing the patient compliance by minimizing inconvenience and adverse effects when administered to patients.Type: ApplicationFiled: November 6, 2007Publication date: February 25, 2010Applicant: HANMI PHARM CO., LTD.Inventors: Jong Soo Woo, Hong Gi Yi, Ju Nam Jin
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Publication number: 20100015203Abstract: The present invention provides a non-clottable matrix on a solid support comprising immobilized and crosslinked fibrinogen. The matrix may further comprise, in and/or on the matrix, one or several biologically active compound(s) and/or pharmacological substance(s). The matrix may be composed of one or several fibrinogen layer(s). The solid support according to the present invention may be selected from the group consisting of orthopaedic devices, implants, stitches, stents, pins, screws, plates, and sutures.Type: ApplicationFiled: February 26, 2008Publication date: January 21, 2010Applicant: ADDBIO ABInventors: Pentti Tengvall, Ella Cathrine Vikinge
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Publication number: 20100016260Abstract: The invention provides compounds of formula I and formula II, their preparation, and their use as pharmaceutically active immunosuppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as other disorders modulated by lymphopenia or SIP receptors.Type: ApplicationFiled: August 1, 2007Publication date: January 21, 2010Applicant: PRAECIS PHARMACEUTICALS INCORPORATEDInventors: Hongfeng Deng, Ghotas Evindar, Sylvie Bernier, Gang Yao, Aaron Coffin, Hongfang Yang, Raksha A. Acharya
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Publication number: 20090318390Abstract: The invention relates to a combination which comprises (a) a bisphosphonate, a platinum compound or a vasculostatic compound and (b) an epothilone derivative of formula I wherein A represents O or NRN, wherein RN is hydrogen or lower alkyl, R is hydrogen or lower alkyl and Z is O or a bond, in which the active ingredients (a) and (b) are present in each case in free form or in the form of a pharmaceutically acceptable salt and optionally at least one pharmaceutically acceptable carrier for simultaneous, separate or sequential use, in particular for the delay of progression or treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition, a commercial package or product comprising such a combination; the use of such a combination for the preparation of a medicament for the delay of progression or treatment of a proliferative disease and to a method of treatment of a warm-blooded animal.Type: ApplicationFiled: August 28, 2009Publication date: December 24, 2009Applicant: NOVARTIS AGInventors: TianLing Chen, Diane Greeley, John David Rothermel, Markus Wartmann, Jeanette Marjorie Wood
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Publication number: 20090286758Abstract: The present invention provides novel pyrazolines that are useful as cannabinoid receptor antagonists/inverse agonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, dyslipidemias, cardiovascular disorders, hepatic disorders, and a combination thereof.Type: ApplicationFiled: May 19, 2009Publication date: November 19, 2009Applicant: JENRIN DISCOVERYInventors: John F. McElroy, Robert J. Chorvat
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Patent number: 7608612Abstract: The present invention provides radiosensitizer compositions, in controlled-release formulations or other acceptable formulations, particularly nitrohistidine radiosensitizer compositions, which may be administered by any suitable means including oral, intravenous, arterial infusion, intraperitoneal, intramuscular, subcutaneous, surgical, and topical. Optionally, radiosensitizer compositions may be formulated with other agents, including chemotherapy agents and agents that provide a synergistic radiosensitizing effect. Methods of potentiating radiotherapy cancer treatment of cancers in humans, particularly of astrocytomas, are also presented, wherein a radiosensitizer composition is administered and radiotherapy is directed to the site of the tumor. Chemotherapy regimens may also be used as adjuvant therapy.Type: GrantFiled: January 20, 2006Date of Patent: October 27, 2009Inventors: Richard H. Matthews, Nuran Ercal, Robert Zand
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Patent number: 7582768Abstract: The invention relates to polymorphs of zoledronic acid and zoledronate sodium salts, amorphous zoledronate sodium salt, processes for making the polymorphs and amorphous zoledronate sodium salt, and pharmaceutical compositions containing the polymorphs and amorphous zoledronate sodium salt.Type: GrantFiled: September 25, 2006Date of Patent: September 1, 2009Assignee: Teva Pharmaceutical Industries LtdInventors: Judith Aronhime, Revital Lifshitz-Liron
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Publication number: 20090215728Abstract: This invention relates to arylaminoaryl-alkyl-substituted imidazolidone-2,4-diones of formula (I) and also to their physiologically tolerated salts: Wherein R, R?, R1 to R10, A, D, E, G, L and p are as defined herein. The invention also relates to processes for preparing them, pharmaceutical compositions comprising them and their therapeutic use. The compounds are suitable, for example, as anti-obesity drugs and for treating cardiometabolic syndrome.Type: ApplicationFiled: February 5, 2009Publication date: August 27, 2009Applicant: SANOFI-AVENTISInventors: Gerhard JAEHNE, Siegfried STENGELIN, Matthias GOSSEL, Thomas KLABUNDE, Irvin WINKLER
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Publication number: 20090215712Abstract: This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereofs, wherein R1 to R4 are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodeficiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).Type: ApplicationFiled: August 25, 2008Publication date: August 27, 2009Inventors: Lyn Howard JONES, Charles Eric Mowbray, David Anthony Price, Matthew Duncan Selby, Paul Anthony Stupple
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Publication number: 20090209493Abstract: A pharmaceutical composition for treatment of malignancies, in particular multiple myeloma (MM), comprises in combination a bisphosphonate, e.g. zoledronic acid or a salt or ester, and an HMG-CoA reductase inhibitor for simultaneous, sequential or separate use. Also provided is a method of treating a patient suffering from a malignant disease comprising administering to the patient an effective amount of a bisphosphonate and an effective amount of an HMG-CoA reductase inhibitor.Type: ApplicationFiled: April 28, 2009Publication date: August 20, 2009Inventors: Cindy Maree Baulch-Brown, Andrew Spencer
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Publication number: 20090209422Abstract: Certain substituted aminoalkyl heteroaryl and heterocyclyl derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula I: wherein R, R1, R2, R3 and R4 are folly described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of an additional compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: ApplicationFiled: May 2, 2006Publication date: August 20, 2009Applicant: Bayer CropScience AGInventors: John A. Dixson, George Theodoridis, Zeinab M. Elshenawy, Benjamin J. Dugan, Manorama M. Patel, John W. Lyga, Stephen F. Donovan, Ping Ding
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Publication number: 20090203648Abstract: A phosphocalcic compound modified by a gem-bisphosphonic acid or one of its salts, a method for preparing same, as well as its use for preparing an injectable composition. The modified phosphocalcic compound is obtained by adding a gem-bisphosphonic acid or one of its alkali metal or alkaline earth salts to a suspension of a precursor phosphocalcic compound in ultras-pure water, while stirring the reaction medium at room temperature, then in recovering by centrifuging the formed compound. The compound is useful for making an injectable composition, for use in the treatment of bone remodeling equilibrium.Type: ApplicationFiled: April 14, 2009Publication date: August 13, 2009Applicants: Centre National de la Recherche Scientifique, Universite de Nantes, Institut National de la Sante et de la Recherche MedicaleInventors: Bruno Bujoli, Solen Josse, Jerome Guicheux, Pascal Janvier, Jean-Michel Bouler, Guy Daculsi
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Publication number: 20090186834Abstract: Various azetidinone, pyrrolidine, imidazolidine, and oxazolidine derivatives are described, as are pharmaceutical compositions containing these compounds and methods of treatment of diseases using these compounds. Other embodiments are also described.Type: ApplicationFiled: March 24, 2006Publication date: July 23, 2009Applicant: MICROBIA, INC.Inventors: John Talley, Eduardo Martinez, Daniel Zimmer, Regina Lundrigan
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Publication number: 20090181108Abstract: A method of treating otosclerosis in a human in need thereof by administering a bisphosphonate in a defined dosing schedule. The invention demonstrates an effective response and sustained benefit in the treatment of otosclerosis. Particularly, the method involves administration of a bisphosphonate in a stepped-up dosage amount, e.g., in a dose that is at least one and a half times the recommended dose for osteoporosis. It also includes administration of a time-dependent dose of more than one bisphosphonate, specifically, alternating administration of a first bisphosphonate with a second bisphosphonate. The inventive method further includes intravenous administration of a bisphosphonate, and optionally oral administration of a bisphosphonate.Type: ApplicationFiled: February 13, 2009Publication date: July 16, 2009Inventor: Kenneth H. Brookler
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Publication number: 20090143337Abstract: C2-C5-Alkyl-substituted [(imidazol-1-yl)-1-hydroxy-1-phosphono-ethyl]-phosphonic acids, as well as methods or processes for their manufacture, their use in the manufacture of pharmaceutical formulations, their use in the treatment of diseases, methods of using them in the treatment of diseases, pharmaceutical formulations encompassing them and/or the compounds for use in the treatment of diseases, are described. The compounds are able to inhibit excessive or inappropriate bone resorption and for the treatment of other diseases which are caused by excessive prenylation of target proteins, such as Hutchinson-Gilford progeria syndrome. The compounds are of the formula I, wherein one of R1 and R2 is hydrogen and the other is C2-C5-alkyl that is branched or unbranched, and can be in free form, in the form of an ester, and/or of a salt.Type: ApplicationFiled: November 26, 2008Publication date: June 4, 2009Applicant: NOVARTIS AGInventors: Sven Weiler, Leo Widler, Jean-Michel Rondeau, Simona Cotesta, Wolfgang Jahnke
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Publication number: 20090130113Abstract: The present invention relates to antibodies against sclerostin and compositions and methods of use for said antibodies to treat disease related to bone abnormalities such as osteoporosis. An embodiment of the invention herein provides an antibody or a functional protein comprising an antigen-binding portion of said antibody for a target in sclerostin polypeptide, characterized in that the antibody or functional protein specifically binds to sclerostin polypeptide and can increase at least one of bone formation, bone mineral density, bone mineral content, bone mass, bone quality and bone strength in a mammal.Type: ApplicationFiled: October 10, 2008Publication date: May 21, 2009Inventors: Michaela Kneissel, Christine Halleux, Shou-Ih Hu, Beate Diefenbach-Streiber, Josef Prassler
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Publication number: 20090118237Abstract: A method of using carisoprodol, phenytoin or fosphenytoin comprises informing a user that co-administration of carisoprodol with phenytoin or fosphenytoin results in an increase in free phenytoin blood levels, a decrease in total phenytoin levels, or both. In another embodiment, a method of using carisoprodol, phenytoin or fosphenytoin comprises informing a user that when co-administering carisoprodol with phenytoin or fosphenytoin, the level of free phenytoin in a patient serum should be monitored, the level of total phenytoin should be monitored, or both. Also included are methods and articles of manufacture.Type: ApplicationFiled: October 1, 2007Publication date: May 7, 2009Applicant: MUTUAL PHARMACEUTICAL COMPANY, INC.Inventors: Richard H. Roberts, Jie Du, Matthew W. Davis
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Publication number: 20090104206Abstract: Novel etiology and pathogenesis of premenstrual headache and premenstrual migraine are presented and novel treatment methods are provided. Present invention identifies how declining estrogen results in a transient elevation in extracellular calcium concentrations via osteoclast upregulation. The elevated extracellular calcium pathogenesis is then traced, from bone to brain, and includes depolarization of nerves, hyperactive neurotransmitter release, and hyperactive muscle contractility. Treatment methods are provided that target the earliest steps of the underlying etiology, in order to provide the most efficacious treatment possible. The treatment methods presented include use of compounds such as calcitonin and SERMs such as raloxifene.Type: ApplicationFiled: October 19, 2007Publication date: April 23, 2009Inventors: Mark Zamoyski, Justin John Zamoyski
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Publication number: 20090082312Abstract: The present application describes deuterium-enriched zoledronic acid, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 18, 2008Publication date: March 26, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090081158Abstract: Provided herein are phosphadiazine polymerase inhibitor, for example, of any of Formulas IV, IV?, I?, II?, or IVa, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.Type: ApplicationFiled: August 27, 2008Publication date: March 26, 2009Applicant: Idenix Pharmaceuticals, Inc.Inventors: Cyril Dousson, Dominique Surleraux, Jean-Laurent Paparin, Claire Pierra, Arlene Roland
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Publication number: 20090074886Abstract: This invention relates to methods of treating or preventing bone loss by administering to a human or animal subject pyrimidine and pyridine derivatives that inhibit the activity of glycogen synthase kinase 3 (GSK3), to pharmaceutical compositions containing the compounds, and to the use of the compounds and compositions alone or in combination with other pharmaceutically active agents.Type: ApplicationFiled: December 1, 2008Publication date: March 19, 2009Inventors: Christina N. Bennett, Kurt D. Hankenson, Stephen D. Harrison, Kenneth A. Longo, Ormond A. MacDougald, Allan S. Wagman
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Publication number: 20090075941Abstract: Methods of treating a subject with neoplasm (e.g., mesothelioma) or at risk of developing neoplasm by administering a mevalonate pathway inhibitor such as a nitrogen-containing bisphosphonate are disclosed. Examples of nitrogen-containing bisphosphonates include alendronate, ibandronate, minodronate, neridronate, olpadronate, pamidronate, risedronate, and zoledronate. The methods can further include the administration of a p38 inhibitor. Further disclosed are compositions and kits including a nitrogen-containing bisphosphonate and optionally a p38 inhibitor.Type: ApplicationFiled: April 11, 2007Publication date: March 19, 2009Applicant: THE UAB RESEARCH FOUNDATIONInventors: Katri Selander, Pierre Triozzi
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Publication number: 20090035281Abstract: The combination of an interleukin-6 (IL-6) antagonist and an antiproliferative drug is described. In its preferred embodiment, the present invention describes the combination of an IL-6 superantagonist, particularly a superantagonist totally incapable of binding gp130 and an antiproliferative drug belonging to the glucocorticoid class (SANT-7 and dexamethasone). The combination according to the present invention has shown surprising synergism in an animal model of multiple myeloma and the ability to overcome the resistance to the antiproliferative drug developed by myeloid cells. The combination according to the present invention is useful for the preparation of a medicament for the treatment of tumours, particularly IL-6-dependent tumours.Type: ApplicationFiled: March 7, 2006Publication date: February 5, 2009Inventors: Rocco Savino, Pierfrancesco Tassone, Salvatore Venuta
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Publication number: 20080318901Abstract: 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: ApplicationFiled: May 6, 2005Publication date: December 25, 2008Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Kevin R. Lynch, Timothy L. Macdonald, Brian H. Heasley
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Publication number: 20080254089Abstract: A pharmaceutical product comprises a container containing a bisphosphonate solution, in which at least the internal surface of the container comprises a plastic material and in which the container is heat sterilisable, and which is in the form of an infusion solution preconcentrate for administration of the bisphosphonate to a patient in need of bisphosphonate treatment.Type: ApplicationFiled: June 18, 2008Publication date: October 16, 2008Inventors: Alexandra Glausch, Rolf Loeffler, Juergen Sigg
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Publication number: 20080242639Abstract: Cyclocreatine phosphate can be prepared in large quantities from inexpensive starting materials to afford a stable product.Type: ApplicationFiled: December 29, 2005Publication date: October 2, 2008Inventors: Farghaly Ahmed, Salwa A. Elgebaly
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Publication number: 20080227755Abstract: Bisphosphonates, in particular more potent N-bisphosphonates such as zoledronic acid and derivatives, can be used with satisfactory results for treatment of RA by intermittent administration, wherein the periods between bisphosphonate administrations are from about 2 months up to about 4 months, e.g. once every 3 months.Type: ApplicationFiled: April 22, 2008Publication date: September 18, 2008Inventor: Victor Sloan
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Publication number: 20080207563Abstract: Disclosed are methods for synergistically inhibiting the proliferation of tumor cells by contacting the tumor cells with a MEK inhibitor compound and erlotinib, either sequentially or simultaneously. Also disclosed are methods for inhibiting the proliferation of tumor cells in a human, by administering to the human, sequentially or simultaneously, an amount of erlotinib and a MEK inhibitor compound, wherein the amounts are effective, in combination, to synergistically inhibit the proliferation of the tumor cells in the human.Type: ApplicationFiled: February 21, 2008Publication date: August 28, 2008Inventor: Huifeng Niu
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Publication number: 20080199454Abstract: The present invention relates to compounds of formula I which are prodrugs of caspase inhibitors and pharmaceutically acceptable salts thereof. This invention further relates to the release of caspase inhibitors from these compounds through selective bond cleavage. This invention further relates to pharmaceutical compositions comprising these compounds, which are particularly well-suited for treatment of caspase-mediated diseases, including inflammatory and degenerative diseases. This invention further relates to methods for preparing compounds of this invention.Type: ApplicationFiled: December 21, 2007Publication date: August 21, 2008Inventors: Michael Mortimore, Julian M.C. Golec
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Publication number: 20080193564Abstract: Use of a bisphosphonate in the preparation of a medicament for the treatment of osteoporosis post hip fracture to prevent or reduce subsequent osteoporotic skeletal fractures in a patient in need of such treatment, and particularly to a patient who has undergone recent repair of the hip fracture and corresponding methods of treatment.Type: ApplicationFiled: April 16, 2008Publication date: August 14, 2008Inventors: Zebulun David Horowitz, Kenneth W. Lyles
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Publication number: 20080132471Abstract: The present invention provides for methods of administering by a pulmonary route an effective amount of a bisphosphonate active agent to a subject. Aspects of the invention including administering the active agent to the subject in conjunction with one or more mucosal membrane protecting agents, where the protecting agent may include one or more of a protecting enzyme and/or a protecting amino acid and/or a protecting peptide. Also provided are inhalant compositions for use in practicing methods according to embodiments of the invention. Methods and compositions according to embodiments of the invention find use in a variety of different applications, including but not limited to, the treatment of bone adsorption disease conditions.Type: ApplicationFiled: November 6, 2007Publication date: June 5, 2008Inventors: Toru Hibi, Akira Yamamoto, Maria Nakatani, Hidemasa Katsumi
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Patent number: 7354911Abstract: Containing the 1,3-benzodioxol compound represented by the formula (I): together with a pesticidal active ingredient in a pesticidal composition enhances a pest control effect of the pesticidal composition.Type: GrantFiled: March 15, 2007Date of Patent: April 8, 2008Assignee: Sumitomo Chemical Company, LimitedInventors: Noritada Matsuo, Hiroshi Okamoto