Nitrogen Containing Patents (Class 514/459)
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Publication number: 20090137601Abstract: The present invention relates to compounds that inhibit of a5b1 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to compounds that inhibit a5b1, and also that exhibit appropriate selectivity profile(s) against other integrins.Type: ApplicationFiled: November 22, 2006Publication date: May 28, 2009Applicant: ASTRAZENECA ABInventors: Simon Thomas Barry, Jason Grant Kettle, David Alan Rudge
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Publication number: 20090137530Abstract: A novel amine compound represented by the following formula (I), which is superior in immunosuppressive action, rejection suppressive action and the like, and shows reduced side effects such as bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or hydrates thereof, or solvate, as well as a pharmaceutical composition containing this compound and a pharmaceutically acceptable carrier. wherein R is a hydrogen atom or P(?O)(OH)2, X is an oxygen atom or a sulfur atom, Y is CH2CH2 or CH?CH, R1 is cyano or alkyl having a carbon number of 1 to 4 and substituted by a halogen atom(s), R2 is alkyl having a carbon number of 1 to 4 and optionally substituted by a hydroxyl group(s) or a halogen atom(s), R3 and R4 may be the same or different and each is a hydrogen atom or alkyl having a carbon number of 1 to 4, and n is 5-8.Type: ApplicationFiled: December 15, 2006Publication date: May 28, 2009Applicant: Mitsubishi Tanabe Pharma CorporationInventors: Masatoshi Kiuchi, Kaoru Marukawa, Nobutaka Kobayashi, Kunio Sugahara
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Publication number: 20090118306Abstract: The present invention generally relates to a novel therapeutical use of liver X receptor (LXR) agonsits. More specifically, the present invention relates to the use of LXR agonist for the preparation of a medicament useful for the treatment and/or the prevention of a disease associated with beta cells degeneration, such as diabetes, and a method for increasing ex vivo viability of pancreatic islet cells, comprising contacting said islet cells with a LXR agonist.Type: ApplicationFiled: May 10, 2006Publication date: May 7, 2009Applicant: LABORATOIRE FOURNIER S.A. French Limited CompayInventors: Bernadette Husson, Pierre Broqua, Jean-Louis Junien
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Publication number: 20090110739Abstract: Compositions and methods for delivery of a pharmaceutical to an individual. Delivery vehicles are provided in a formulation of a pharmaceutical that is encapsulated in a synthetic self assembled nanoparticle that includes a lipid binding protein and a lipid monolayer. The interior of the particle represents a hydrophobic core region where lipophilic highly-water insoluble drug molecules may be incorporated. In contrast to liposomes, that include an aqueous interior core surrounded by phospholipid bilayer, the drug carrier nanoparticle described here is composed of a monolayer and a hydrophobic interior.Type: ApplicationFiled: May 15, 2008Publication date: April 30, 2009Applicant: University of North Texas Health Science Center at Forth WorthInventors: Andras G. Lacko, Walter J. McConathy
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Publication number: 20090093449Abstract: The present invention relates to formulations of concentrated azalide antibiotics and methods for making and using them. Specifically, the invention relates to a method of treating an infection comprising administering to a patient in need thereof, an effective amount of a concentrated aqueous azalide antibiotic formulation made according to the method comprising dissolving an azalide antibiotic in an aqueous solution comprising a strong acid. The invention also relates to methods for making concentrated aqueous azalide antibiotic formulations for use in pulmonary infection, a nasopharyngeal infection, an otic infection, an ocular infection, a dermal or a vaginal infection. The invention also relates to concentrated aqueous azalide antibiotic formulations made by dissolving an azalide antibiotic in an aqueous solution comprising a strong acid.Type: ApplicationFiled: October 4, 2007Publication date: April 9, 2009Inventors: Lyle Bowman, S. Kumar Chandrasekaran, Roy Duane Archibald, Stephen Pham, David Mufson
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Publication number: 20090082423Abstract: Disclosed are amide, thioamide, urea and thiourea compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, and diabetic-related diseases.Type: ApplicationFiled: September 10, 2008Publication date: March 26, 2009Inventors: Sampath-Kumar Anandan, Richard D. Gless, JR.
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Publication number: 20090076062Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.Type: ApplicationFiled: September 13, 2007Publication date: March 19, 2009Inventors: Juergen Klaus Maibaum, Daniel Kaspar Baeschlin, Holger Sellner
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Publication number: 20090074871Abstract: The invention is directed toward an improved formable bone composition for application to a bone defect site to promote new bone growth at the site which comprises a new bone growth inducing compound of demineralized lyophilized allograft bone particles ranging from about 100 to 850 microns. The bone particles are mixed in an excipient carrier combination containing carboxymethylcellulose, sodium hyaluronate, and a sodium phosphate saline buffer, the carboxymethylcellulose component of the carrier ranging from about 5.0 to about 11.0% of the composition and the sodium hyaluronate component of the carrier ranging from about 0.3 to about 0.7% of the composition, the composition having a pH between 6.5-7.5.Type: ApplicationFiled: September 14, 2007Publication date: March 19, 2009Inventors: Moon Hae Sunwoo, Victor A. Lizano, Arthur A. Gertzman
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Publication number: 20090076133Abstract: The present application describes deuterium-enriched zanamivir, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 8, 2008Publication date: March 19, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Patent number: 7504434Abstract: The invention relates to compounds of general formula (I), in which: R is an amino or guanidino group; R2 is acetyl or trifluoroacetyl; n and q are either the same or different and selected from 0, 1 or 2; and X is an optionally substituted phenyl, optionally substituted naphthyl or optionally substituted phenyl-Y-optionally substituted phenyl in which Y is selected from a covalent bond, CH2, CH2CH2, O or SO2, or a pharmaceutically acceptable derivative thereof, with the proviso that when X is phenyl or naphthyl, n and q are both 2 and when X is phenyl-Y-phenyl in which Y is a covalent bond, then n and q are not both 0, methods for their preparation, pharmaceutical formulations containing them or their use in the prevention or treatment of a viral infection.Type: GrantFiled: April 2, 2007Date of Patent: March 17, 2009Assignee: Biota Scientific Management Pty Ltd.Inventors: Derek A. Demaine, Haydn T. Jones, Simon J. F. MacDonald, Andrew McM Mason, Stephen E. Shanahan
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Publication number: 20090068255Abstract: The application of matrix metalloproteinase (MMP) inhibitors to the skin inhibits the degradation of proteins found in the skin including collagen, elastin, and other basement membrane and extracellular matrix protein. MMP inhibitors may be used in both cosmetic compositions and pharmaceutical compositions for application to skin. MMP inhibitors are formulated with a cosmetically suitable vehicle or pharmaceutically acceptable excipient for application to the skin as creams, lotions, ointments, solutions, face masks, etc. As cosmetics, the inventive MMP inhibitor compositions are applied to the skin to prevent or reduce the appearance of wrinkles, pigmentation changes, loss of elasticity, or other effects associated with aging or sun damage. As pharmaceuticals, the inventive MMP inhibitor compositions may also be applied to the skin to treat or prevent a skin disease (e.g., proliferative disease, inflammatory disease).Type: ApplicationFiled: April 30, 2008Publication date: March 12, 2009Inventors: Betty Yu, Amir Nashat, Daniel Griffith Anderson, David Thomas Puerta, Benjamin Adams, Scott Clark, Yushan Kim, Eric George Spengler, Ronald P. McLaughlin, Susan Eilidh Bedford, Zhi Li
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Patent number: 7498311Abstract: A method for treating migraine in non-epileptic subjects which involves administering to subjects an effective amount of a pharmaceutical composition comprising a sulfamate of the following formula:Type: GrantFiled: January 6, 2006Date of Patent: March 3, 2009Assignee: New England Medical Center Hospitals, Inc.Inventors: Bruce L. Ehrenberg, Anita K. Wagner
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Publication number: 20090053149Abstract: A surfactant can be added, safely and effectively, to a drug solution containing any antimicrobial agent, such as an antibiotic like tobramycin, that is suitable for administration to the lungs via inhalation. Thus, when an aerosolized drug solution includes surfactant, Marangoni flows cause the drug particles, once deposited in the lungs, to spread over a wider surface area, thereby ensuring greater antimicrobial efficacy. A solution that contains, for example, an antibiotic and tyloxapol or another surfactant providing a similar surface tension to the composition is optimally delivered by the functional combination of a breath-actuated nebulizer and a high-flow compressor.Type: ApplicationFiled: August 21, 2008Publication date: February 26, 2009Inventors: Tim Corcoran, Amy Lise Marcinkowski, Joseph Pilewski, Kristina Thomas
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Publication number: 20090053290Abstract: Transdermal delivery compositions and topical compositions for application to the skin are provided. The transdermal delivery composition includes at least two penetrants working synergistically but by disparate biochemical pathways. In one embodiment, the transdermal delivery system includes benzyl alcohol and lecithin organogel. The transdermal delivery compositions are used in a variety of topical compositions as a means of transdermally delivering and topically administering different drugs and agents, including compositions promoting collagen biosynthesis, retinoids and skin lighteners, chemical denervation agents such as BOTOX®, anti-fungal agents, anesthetics and non-steroidal anti-inflammatory drugs (NSAIDs). In addition, these topical compositions may be used in combination with non-ablative treatment modalities, such as microdermabrasion, laser-based skin remodeling and radio-frequency-based skin remodeling.Type: ApplicationFiled: March 8, 2007Publication date: February 26, 2009Inventors: Bruce J. Sand, Michael Babich, Ali Zendedel Haghighi
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Publication number: 20090047358Abstract: Phospholipid based powders for drug delivery applications are disclosed. The powders comprise a polyvalent cation in an amount effective to increase the gel-to-liquid crystal transition temperature of the particle compared to particles without the polyvalent cation. The powders are hollow and porous and are preferably administered via inhalation.Type: ApplicationFiled: October 24, 2008Publication date: February 19, 2009Inventors: Jeffry G. WEERS, Thomas E. Tarara, Luis A. Dellamary, Jean G. Riess, Ernest G. Schutt
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Publication number: 20090042823Abstract: Methods and uses of RNAi-inducing agents for medicaments and treating or preventing a viral infection.Type: ApplicationFiled: August 11, 2008Publication date: February 12, 2009Applicant: MDRNA, INC.Inventors: Michael V. Templin, Shaguna Seth, Gregory Mark Severson
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Publication number: 20090035315Abstract: Improved treatments of joint diseases, such as, e.g.Type: ApplicationFiled: June 17, 2005Publication date: February 5, 2009Inventors: Stephan Christgau, Christian Hansen, Henrik Nilsson
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Publication number: 20090012153Abstract: The invention relates to novel compounds of formula (I): H2N—CH(R1)—CH2—S—S—CH2—CH(R2)—CONH—R5, wherein R1 is a hydrocarbon chain, phenyl or benzyl radical, methylene radical substituted by a 5 or 6 atom heterocycle; R2 is a phenyl or benzyl radical, a 5 or 6 atom aromatic heterocycle, methylene group substituted by a 5 or 6 atom heterocycle; R5 is a CH(R3)—COOR4 radical, wherein R3 is hydrogen, an OH or OR group, a saturated hydrocarbon group, a phenyl or benzyl radical and OR4 is hydrophile ester, or 5 or 6 membered heterocycle comprising several heteroatoms selected from a group consisting of nitrogen, sulphur and oxygen, with at least two nitrogene atoms, wherein said heterocycle is substitutable by an alkyl C1-C6, phenyl or benzyl radical.Type: ApplicationFiled: June 26, 2008Publication date: January 8, 2009Applicant: PharmaleadsInventors: Bernard Roques, Marie-Claude Fournie-Zaluski
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Publication number: 20090010880Abstract: The present invention is directed to compounds, compositions and methods comprising the aminoglycoside moiety represented by Formula II for treating and preventing the spread of positive sense single-stranded RNA envelope viral infections. One embodiment of the present invention uses geneticin or its analogs, including 2-amino-2,7-dideoxy-alpha-D-glycero-D-gluco-heptopyranose, as the antiviral agent. The compounds, compositions and methods of the present invention are applicable to infections resulting from Hepatitis C virus, West Nile virus, Yellow Fever virus, Dengue virus, Bovine Viral Diarrhea virus, Equine Arteritis virus, and/or Sindbis virus.Type: ApplicationFiled: June 6, 2008Publication date: January 8, 2009Applicant: Institute for Hepatitis and Virus ResearchInventors: Alexander V. Birk, Edward J. Dubovi, Hazel H. Szeto
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Publication number: 20090010860Abstract: Disclosed is the use of the compounds of formula wherein Q is —OH; —OR7; —NH2; —NHR7; —NR7R8; or —N?R9; T is —COR5; —CN; or —SO2—(C6-C12)aryl; R1 is hydrogen; —OR7, —SR7; —NHR7; —NR7R8; C1-C22alkyl; C2-C12Alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; C7-C12aralkyl; C1-C12heteroalkyl, C2-C11heteroaralkyl; C6-C10aryl; or C1-C9heteroaryl; R2 and R3 independently from each other are C1-C22alkyl; C2-C12alkenyl; C2-C12alkinyl; C3-C12cycloalkyl, C3-C12cycloalkenyl; C7-C12aralkyl; C1-C12heteroalkyl; C3-C12cycloheteroalkyl; C2-C11heteroaralkyl, C6-C10aryl; or C1-C9heteroaryl; R4 is cyano; COR7, COOR7; CONH2; CONHR7; CONR7R8; SO2(C6-C12)aryl, C2-C12alk-1-enyl; C3-C12cycloalk-1-enyl; C2-C12alk-1-inyl; C2-C12heteroalkyl, C3-C5heterocycloalkyl, C6-C10aryl; or C1-C9heteroaryl; R5 is —COR7; —COOR7; —OR7; —SR7, —NHR7, —NR7R8; C2-C12alkyl; C2-C12alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; C7-C12aralkyl; C1-C12alkylphenyl; C1-C12alkoxy-C8-C10aryl; C1-C12heteroalkyl; C2-C11heteroaralkyl; CType: ApplicationFiled: June 20, 2005Publication date: January 8, 2009Inventors: Barbara Wagner, Frank Bienewald, Heinz Wolleb, Olof Wallquist, Bernd Herzog, Thomas Ehlis, Jurg Haase
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Publication number: 20090004173Abstract: The present invention encompasses methods and compositions useful in the diagnosis and treatment of drug resistant leukemia. The invention provides a number of genes that are differentially expressed between drug resistant and drug sensitive acute lymphoblastic leukemia (ALL). These genes act as biomarkers for drug resistant leukemia, and further serve as molecular targets for drugs useful in treating drug resistant leukemia. Accordingly, the invention provides methods of diagnosing drug resistant leukemia and methods of selecting a therapy for subjects affected by drug-resistant leukemia. The invention also provides methods for screening for compounds for treating drug-resistant leukemia, and improved methods for treating drug-resistant leukemia. Compositions of the invention include arrays, computer readable media, and kits for use in the methods of the invention.Type: ApplicationFiled: May 18, 2005Publication date: January 1, 2009Applicant: St. Jude Children's Research HospitalInventors: William E. Evans, Robert Pieters, Meyling H. Cheok, Monique L. den Boer, Wenjian Yang
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Publication number: 20090004279Abstract: A method for improvement of tolerance for therapeutically effective agents delivered by inhalation comprising a pretreatment of a patient with a nebulized lidocaine or a lidocaine-like compound administered immediately or up to about thirty minutes before administration of the primary therapeutically effective agent. The pretreatment of the patient with the nebulized lidocaine or a lidocaine-like compound improves airway tolerance and deposition of the agent in the lungs and makes such deposition more safe, efficacious, controllable and predictable. The method of the invention is especially useful for enhancement of deposition of immunosuppressive agents in the lung(s) of transplant patients, improved tolerance of the drugs by reducing cough, and improving pulmonary drug deposition.Type: ApplicationFiled: September 10, 2008Publication date: January 1, 2009Inventors: Thomas Hofmann, Alan Bruce Montgomery, Kevin Stapleton, William R. Baker
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Patent number: 7470672Abstract: This invention is in the field of chemical restructuring of pharmaceutical agents known to cause tissue toxicity as a side effect, by producing their orotate derivatives. More particularly, it concerns orotate derivatives of the anthracyclines, doxorubicin and daunorubicin, that are found to reduce levels of the pharmaceutical agent in noncancerous tissues. There orotate derivatives are equally efficacious in inhibiting the SCCAKI-1 kidney tumor in animals and the reduction in the heart tissue of doxorubicin compared with doxorubicin HCl suggests a reduction in toxicity induced by free radical generation by the anthrracyclines.Type: GrantFiled: July 31, 2006Date of Patent: December 30, 2008Assignee: Savvipharm Inc.Inventor: Rashida A. Karmali
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Patent number: 7468388Abstract: The invention relates to compounds of general formula (I); in which R is an amino or guanidino group; R2 is acetyl or trifluoroacetyl; X is CONH, NHCO or O; n is an integer from 2 to 6; and Y is C2-C9 alkyl C3-8 cycloalkyl, C1-C4 alkoxyalkyl, an amino acid or dipeptide, or a pharmaceutically acceptable derivative thereof, methods for their preparation, pharmaceutical formulations containing them or their use in the prevention or treatment of a viral infection.Type: GrantFiled: April 12, 2007Date of Patent: December 23, 2008Assignee: Biota Scientific Management Pty Ltd.Inventors: Betty Jin, Simon J. F. MacDonald, Darryl McConnell, Van T. T. Nguyen, Stephen E. Shanahan, Wen-Yang Wu
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Publication number: 20080306136Abstract: The invention provides compounds of formula I: useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: ApplicationFiled: April 1, 2008Publication date: December 11, 2008Inventors: Shon R. Pulley, John A. Tucker
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Patent number: 7459165Abstract: The present invention relates to polypeptides of Pseudomonas aeruginosa which may be used to prevent, diagnose and/or treat Pseudomonas aeruginosa infection.Type: GrantFiled: November 13, 2002Date of Patent: December 2, 2008Assignee: ID Biomedical CorporationInventors: Nathalie Charland, Josee Hamel, Bernard Brodeur, Denis Martin, Isabelle Charlebois, Diane Bussiere
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Publication number: 20080279961Abstract: It is demonstrated in the present invention that G-quadruplex ligands can be used to both shorten telomeres and inhibit telomerase by causing telomere uncapping. The invention relates to compositions and methods of treating cancer stem cells comprising the administration of G-quadruplex ligands, such as 3,11-difluoro-6,8,13-trimethyl-8H-quino[4,3,2-kl]acridinium methosulfate (RHPS4), which can effectively inhibit or reduce the growth of cancer stem cells. The invention also relates to a synergistic effect in inhibiting or reducing the growth cancer stem cells when a G-quadruplex ligand is combined with a mitotic spindle poison, such as paclitaxel, or other agents used in the treatment of cancer and disease. The invention also relates to RHPS4 inducing non-cancerous cell and non-cancerous stem cell proliferation.Type: ApplicationFiled: May 9, 2008Publication date: November 13, 2008Inventor: Angelika M. BURGER
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Publication number: 20080261982Abstract: Stilbene derivatives exhibit killing and suppression of growth activity against a variety of cancer cells, and are effective at suppressing tumor growth in vivo. The stilbene derivatives may be used in the treatment of diseases characterized by cell hyperproliferation including human malignancies and non-malignant diseases such as liver cirrhosis. Stilbenes may also disrupt abnormal vessels in tumor to achieve vascular disrupting effect to suppress tumor growth. Water soluble pro-drug forms of stilbene derivatives are particularly useful in suppressing tumor growth in vivo.Type: ApplicationFiled: April 23, 2007Publication date: October 23, 2008Inventors: Ruey-min Lee, Daniele Simoni
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Patent number: 7432298Abstract: Fluorescent polymeric materials are disclosed comprising a polymer and one or more lipid soluble rhodamine dyes. The materials are especially useful in the preparation of multicolored microparticles, especially multicolored polystyrene microparticle, for use in the multiplexed analysis of a plurality of analytes in a single sample. When excited by a light source, the materials give off a unique emission based on the nature, concentration and ratio of the dyes therein. Methods of preparing and using said materials are also disclosed.Type: GrantFiled: May 4, 2004Date of Patent: October 7, 2008Assignee: Applied Biosystems Inc.Inventors: Joe Y. L. Lam, Steven M. Menchen, Ruiming Zou, Scott C. Benson
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Publication number: 20080220079Abstract: Sustained release spherical or non-spherical pellets comprising (a) an active ingredient (b) a wax-like agent, and (c) a spheronizing agent are provided. Oral dosage forms comprising said pellets and methods for preparing and using such pellets and dosage forms are also provided.Type: ApplicationFiled: February 29, 2008Publication date: September 11, 2008Applicant: FARNAM COMPANIES, INC.Inventors: Andrew Xian Chen, Patricia D. Kigin
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Publication number: 20080214617Abstract: Carbamate compounds having a structure represented by formula I (where R1, R2, R3, R4, R5 and R6 are as defined herein) are useful as anti-tumor agents.Type: ApplicationFiled: February 20, 2008Publication date: September 4, 2008Inventors: Hong Fu, Yaoquan Liu
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Patent number: 7420002Abstract: Compounds that provide for sustained systemic concentrations of GABA analogs following oral administration to animals are disclosed. Pharmaceutical compositions including, and methods using, such compounds are also disclosed.Type: GrantFiled: June 11, 2002Date of Patent: September 2, 2008Assignee: XenoportInventors: Mark Gallop, Kenneth C. Cundy, Randall A. Scheuerman, Ronald W. Barrett, Noa Zerangue
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Patent number: 7419967Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods For inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: GrantFiled: August 25, 2005Date of Patent: September 2, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael R Hale, Clarence W Andrews, III, Eric S Furfine, Ronald G Sherrill, Andrew Spaltenstein, Gregory T Lowen
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Publication number: 20080207569Abstract: Provided herein are methods for treatment of a liver disease by administering a matrix metalloproteinase inhibitor. Also provided are methods for reducing liver damage associated with a liver disease by administering the matrix metalloproteinase inhibitor described herein. Further provided are methods for lowering an elevated level of liver enzymes by administering the matrix metalloproteinase inhibitor.Type: ApplicationFiled: February 28, 2008Publication date: August 28, 2008Inventor: Alfred P. Spada
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Patent number: 7417059Abstract: The present invention is directed to a class of cyclohexene derivatives bearing sulfamoyl and ester groups which have an inhibitory activity on nitric oxide (NO) production and cytokine production, and are useful as an agent for the prophylaxis and/or treatment of diseases such as, cardiac disease, autoimmune disease, inflammatory disease, central nervous system disease, infectious disease, sepsis, and septic shock.Type: GrantFiled: March 31, 2005Date of Patent: August 26, 2008Assignee: Takeda Pharmacetical Company LimitedInventors: Norikazu Tamura, Takashi Ichikawa, Masayuki Ii
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Publication number: 20080199458Abstract: A composition for influenza treatment includes an immune enhancer and an anti-viral agentType: ApplicationFiled: January 16, 2008Publication date: August 21, 2008Inventors: Jian-Er LIN, Wei Dong Xie, Kee Hung Chu
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Patent number: 7414074Abstract: Lactones of Formula (I) which are pharmaceutically active in diseases associated with inflammationType: GrantFiled: March 31, 2005Date of Patent: August 19, 2008Assignee: Novartis AGInventors: Josef Gottfried Meingassner, Klaus Thirring
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Publication number: 20080193428Abstract: The present invention relates to the use of benzoic acid and/or its sodium salt in combination with saccharide(s) as active components in the manufacture of a vaginal composition for modulating vaginal flora and vaginal acidity, thereby maintaining the pH value of vaginal secretion within a range from 3.5 to 4.5; and the present invention further relates to a vaginal composition and a method for modulating and maintaining normal vaginal flora and vaginal acidity.Type: ApplicationFiled: April 27, 2006Publication date: August 14, 2008Applicants: Shenzhen Phlora Biotechnology Limited, HK Phlora Health Science & Technology Ltd.Inventors: Ruyun Zhou, Zhongming Zeng
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Publication number: 20080171687Abstract: Sterile, stable pharmaceutical formulations of poorly water-soluble drugs dissolved in dimethyl isosorbide, a water-miscible solvent, as well as methods for their preparation and administration.Type: ApplicationFiled: September 16, 2005Publication date: July 17, 2008Applicant: Abraxis Bioscience, Inc.Inventors: Neil P. Desai, Chunlin Tao, Andrew Yang, Bridget Beal-Grim, Tapas De, Patrick Soon-Shiong
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Publication number: 20080171787Abstract: Colchicine neoglycosides, method for their synthesis and methods for their use are disclosed. The invention provides analogs of colchicine glycosylated to include a sugar moiety on a colchicine scaffold that is generally unglycosylated in nature. The colchicine neoglycosides disclosed herein are shown to have cytotoxic effects equivalent to at least the known cytotoxins paclitaxel and doxorubicin. Further, the neoglycosides disclosed according to the invention have physiologic effects not previously recognized in the alkaloid family that includes colchicine but recognized in other cytotoxic drug families such as the taxanes which act by stabilizing tubulin formation.Type: ApplicationFiled: October 8, 2007Publication date: July 17, 2008Applicant: Wisconsin Alumni Research FoundationInventors: Jon S. Thorson, Ahmed Aqeel
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Publication number: 20080167371Abstract: Compounds of Formula (I) that act as antagonists at the mu, kappa and/or delta opioid receptors and therefore useful in the treatment of diseases, conditions and/or disorders that benefit from such antagonism in animals are described herein. where R, R1, R2a, R2b, R3, R4, V, R6, R7, R8, R9, W and X are described herein.Type: ApplicationFiled: November 13, 2007Publication date: July 10, 2008Inventors: Roger B. Ruggeri, George T. Magnus-Aryitey, Benjamin Aaron Thuma
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Publication number: 20080166293Abstract: Peptides have been discovered which are capable of binding to and internalizing with the human transferrin receptor (hTfR). The sequences HAIYPRH (Seq. ID No. 1) and THRPPMWSPVWP (Seq. ID No. 2) are capable of binding to and internalizing with the human transferrin receptor. When these molecules were fused with other molecules, the fusion product was internalized in cells expressing hTfR. The sequences have use for targeting other peptides and proteins into cells expressing hTfR.Type: ApplicationFiled: February 18, 2008Publication date: July 10, 2008Inventors: Jeffrey A. Engler, Jae Hwy Lee, James F. Collawn, Bryan A. Moore
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Patent number: 7396828Abstract: The invention provides prodrugs of inhibitors of PI-3 kinase. The compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.Type: GrantFiled: April 20, 2005Date of Patent: July 8, 2008Assignee: Semafore Pharmaceuticals, Inc.Inventors: Joseph R. Garlich, Donald L. Durden, Mary Patterson, Jingdong Su, Robert G. Suhr
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Publication number: 20080161362Abstract: The present invention relates to metalloprotein inhibitors comprising: a. an organic substituent and at least one zinc binding group (ZBG) covalently attached thereto; or b. a ZBG substituted by a side chain wherein the ZBG is of formula (I): wherein X is O or S and each R1, R2, R3, and R4 is individually hydrogen or an organic radical. The metalloprotein inhibitors are useful for preventing or treating a pathological disease, condition, or symptom that is associated with pathological metalloprotein activity and/or that is alleviated by inhibition of said activity.Type: ApplicationFiled: April 28, 2005Publication date: July 3, 2008Applicant: Regents of the University of California, San Diego UCSD Technology transfer officeInventors: David T. Puerta, Seth M. Cohen, Jana A. Lewis
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Patent number: 7390803Abstract: The present invention is directed to compounds of the formula (I) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R27, R28, R29, R30, R31, X, m, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity.Type: GrantFiled: October 24, 2003Date of Patent: June 24, 2008Assignee: Merck & Co., Inc.Inventors: Gabor Butora, Sander G. Mills, Alexander Pasternak, Kothandaraman Shankaran, Lihu Yang, Changyou Zhou, Stephen D. Goble
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Publication number: 20080145371Abstract: A composition for treating a subject is provided. The composition includes dimeric or polymeric secretory IgA therapeutic. Formulating agents are mixed with the dimeric or polymeric secretory IgA to yield a dosing form of a capsule, tablet, and a suppository. A process for manufacturing a medicament for the treatment of C. difficile associated disease in a human is also provided that the modification of dimeric or polymeric IgA with secretory component to form a dimeric or polymeric secretory IgA therapeutic. The dimeric or polymeric secretory IgA therapeutic is then mixed with formulating agents to create a capsule, tablet, or suppository dosing form. The therapeutic is amenable to enrobement directly through microencapsulation or the dosing form is coated with an enteric coating. A method of C. difficile treatment with the therapeutic is also provided that is amenable to supplementation with concurrent or prior antibiotic administration.Type: ApplicationFiled: August 16, 2007Publication date: June 19, 2008Inventor: Michael R. Simon
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Publication number: 20080138406Abstract: The present invention is a composition delivering effective amounts of Glucosamine, Devils Claw, and SAM in a single dosage unit.Type: ApplicationFiled: December 4, 2007Publication date: June 12, 2008Inventor: Jarret Morrow
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Publication number: 20080139505Abstract: The present invention provides compounds of formula (I): pharmaceutical compositions thereof, and methods of using the same, processes or preparing the same, and intermediates thereof.Type: ApplicationFiled: November 15, 2005Publication date: June 12, 2008Inventors: Thomas Daniel Aicher, Guillermo S. Cortez, Todd Michael Groendyke, Albert Khilevich, James Allen Knobelsdorf, Fredrik Pehr Marmsater, Jeffrey Michael Schkeryantz, Tony Pisal Tang, Nicholas Andrew Magnus
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Publication number: 20080132442Abstract: The biodegradable drug delivery systems described here are formulated for implantation into the nail unit and its surrounding tissues for the treatment of various nail unit conditions. The systems include greater than 30% by weight of the active agent, and may be formulated as solutions, solids, semisolids, microparticles, or crystals. Methods related to the implantation and use of the biodegradable drug delivery systems for treating nail unit conditions are also described.Type: ApplicationFiled: February 11, 2008Publication date: June 5, 2008Inventors: Frank M. Kochinke, Corinne Bright
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Patent number: 7378399Abstract: What is described are a compound of the formula (I) Wherein A-B is —CH?CH— or —CH2—CH2—; n is 0 or 1; R1, is C1-C12alkyl, C3-C8cycloalkyl or C2-C12alkenyl; R2 and R3 for instance are either, (i) independently from each other for instance -Q, —C(?Y)-Q, or —C(?Y)—O-Q; or (ii) together form with the nitrogen atom to which they are bound a three- to seven-membered ring, (iii) together are ?C(R4)R5; R4 and R5 are, independently from each other, for instance -Q, —C(?Y)-Q, or —C(?Y)—O-Q; Y is O or S; Q is for instance H or unsubstituted or mono- to pentasubstituted C1-C12alkyl; or, if appropriate, an E/Z isomer, E/Z isomer mixture and/or tautomer thereof; a process for preparing these compounds, their isomers and tautomers and the use of these compounds, their isomers and tautomers; pesticidal compositions whose active compound is selected from these compounds and their tautomers; intermediates for the preparation of the said compounds of the formula (I), methods for the preparation of the compounds of the formula (Type: GrantFiled: February 3, 2004Date of Patent: May 27, 2008Assignee: Merial LimitedInventors: Jerome Cassayre, Hans Tobler, Thomas Pitterna, Peter Maienfisch, Fiona Murphy Kessabi, Laura Quaranta, Ottmar Franz Hueter