Patents Issued in August 12, 2008
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Patent number: 7410950Abstract: The present invention relates to peptides of CaV2.2 and their use in the treatment of pain. The sequence of the peptides is derived from the C-terminus of CaV2.2. and is believed to inhibit the interaction of CaV2.2 with Mint1-PDZ1. The invention is related to use of this peptide to treat pain and to use of this peptide in binding reaction with int-PDZ to screen for small molecules that can inhibit pain.Type: GrantFiled: March 31, 2005Date of Patent: August 12, 2008Assignee: Board of Regents, The University of Texas SystemInventors: Mary Garry, Ilya Bezprozvanny
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Patent number: 7410951Abstract: Derivatives of hemiasterlin or Geodiamolide G having anti-mitotic activities and useful in treating cancer. These derivatives are represented by formula I wherein Y, n, R1, R2, R3, R7, R70, R71, R72, R74, and R75 are as defined in the specification.Type: GrantFiled: January 14, 2005Date of Patent: August 12, 2008Assignee: The University of British ColumbiaInventors: Raymond Andersen, John Coleman, Dilip De Silva, Fangming Kong, Edward Piers, Debra Wallace, Michel Roberge, Theresa Allen
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Patent number: 7410952Abstract: The invention relates to derivatives of azithromycin, processes for the manufacture thereof and pharmaceutical compositions thereof preferably together with azithromycin.Type: GrantFiled: April 16, 2004Date of Patent: August 12, 2008Assignee: Sandoz AGInventors: Albert Codony, José Diago, Rafael Garcia, Jordi Rifa
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Patent number: 7410953Abstract: The present invention is to offer a pharmaceutical agent which is capable of suppressing the growth of cancer in cancer cells and the surrounding tissues thereof or in tissue of non-diseased part. An anticancer agent having a mannan-binding protein or gene thereof as an effective component. Examples of a mannan-binding protein are a protein which has an amino acid sequence described in SEQ ID NO:1 of the Sequence Listing and a protein which has an amino acid sequence where one or more amino acid residue(s) is/are subjected to at least one of substitution, deletion, addition and insertion in the amino acid sequence and also has an activity as mannan-binding protein. Examples of a gene are a gene which codes an amino acid sequence described in SEQ ID NO:1 or NO:2 of the Sequence Listing or modified amino acid sequence, or a gene which contains said gene.Type: GrantFiled: October 4, 2001Date of Patent: August 12, 2008Assignee: Takara Bio, Inc.Inventor: Toshisuke Kawasaki
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Patent number: 7410954Abstract: The present invention provides an adenovirus serotype 30 (Ad30) fiber amino acid sequence. The present invention also provides polynucleotides and expression vectors encoding an Ad30 fiber and viral particles and cells containing such expression vectors. The present invention further provides methods of treating genetic diseases or cancers in a mammal using the polynucleotides, polypeptides, expression vectors, viral particles and cells of the present invention.Type: GrantFiled: July 15, 2003Date of Patent: August 12, 2008Assignee: University of Iowa Research FoundationInventors: Beverly L. Davidson, Lane K. Law
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Patent number: 7410955Abstract: The present invention relates to novel therapeutical use of agonist ligands specific to G2A receptor. More particularly, the present invention relates to methods for treating a disease or disorder associated with neutrophil accumulation and hyperactivity and/or excessive release of IL-8, or with microbial infection, in a subject, comprising administering LPC (lysophosphatidylcholine), SPC(sphingophosphorylcholine) or derivatives thereof to the subject. The agonist ligands for G2A receptor according to the present invention and pharmaceutical- or therapeutical composition comprising said ligands can be used effectively in treatment of a disease or disorder associated with neutrophil accumulation and hyperactivity and/or excessive release of IL-8, specifically inflammatory diseases and diseases associated with ischemia-reperfusion injury as well as microbial infection.Type: GrantFiled: March 25, 2003Date of Patent: August 12, 2008Assignee: Biosynergen, Inc.Inventors: Yung-Hi Kim, Dong-Keun Song, Hong-Won Suh, Sung-Oh Huh
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Patent number: 7410956Abstract: 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: GrantFiled: February 11, 2003Date of Patent: August 12, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Mortimore, Julian M. C. Golec
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Patent number: 7410957Abstract: The present invention refers to a pharmaceutical composition of a bisphosphonic acid or salt thereof, and an excipient thereof, and a method of treating disorder characterized by pathologically increased bone resorption comprising orally administering at least 150% of the expected efficious daily dose of a bisphosphonic acid or a pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable excipients thereof and administering the dose at a period of one two or three consecutive days per month.Type: GrantFiled: May 6, 2003Date of Patent: August 12, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Frieder Bauss, Bernhard Pichler, Stephen Turley
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Patent number: 7410958Abstract: The invention provides novel compounds that are quaternary amine derivatives of betulin and other triterpenes. The compounds have antibacterial, antifungal, and surfactant properties.Type: GrantFiled: December 18, 2006Date of Patent: August 12, 2008Assignee: Regents of the University of MinnesotaInventors: Pavel A. Krasutsky, Dmytro Avilov, Tatiana Sergeeva, Dmytro A. Krasutskyy, Oksana Kolomitsyna
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Patent number: 7410959Abstract: A pharmaceutical composition includes, as an active ingredient, a compound according to formula 1436 as shown in FIG. 1, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or excipient. Various pharmaceutical products may be produced including this pharmaceutical composition. Such pharmaceutical products may be used for the treatment of obesity or diabetes. Methods for using the pharmaceutical compositions also are described. In these methods, various diseases are treated or other body functions are activated or inhibited by administering an effective amount of the pharmaceutical composition. For example, diabetes and obesity may be treated by administering an effective amount of the pharmaceutical compositions. Weight gain, and growth factor production can be inhibited by administering an effective amount of these pharmaceutical compositions.Type: GrantFiled: July 13, 2000Date of Patent: August 12, 2008Assignee: Genaera CorporationInventors: Michael Zasloff, Jon Williams, William Kinney, Mark Anderson, Michael McLane
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Patent number: 7410960Abstract: A compound of formula I or a salt thereof [ML1L2]2+??(I) where M is selected from the group consisting of platinum(II), palladium (II) and copper(II); L1 is an intercalator moiety; and L2 is a bidentate ligand, provided that when L2 is other than a bidentate ligand containing an aryl or phenyl group, L2 is a chiral bidentate ligand.Type: GrantFiled: February 22, 2002Date of Patent: August 12, 2008Assignees: The University of Western Sydney, The University of SydneyInventors: Ronald Ralph Fenton, Janice Aldrich-Wright
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Patent number: 7410961Abstract: The present invention is further directed to compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R16, R17, R18, R19, R20, R21 and R22 are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.Type: GrantFiled: January 14, 2005Date of Patent: August 12, 2008Assignee: Merck & Co., Inc.Inventors: Lihu Yang, Sander G. Mills, Changyou Zhou, Stephen D. Goble, Alexander Pasternak
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Patent number: 7410962Abstract: Compounds having neutral endopeptidase (NEP) and/or human soluble endopeptidase (hSEP) inhibitory activity corresponding to the formula I, wherein the substituents R1, R2, R3 and R4 have the meanings given in the description and also pharmaceutical compositions containing these compounds, in particular pharmaceutical compositions suitable for treating or inhibiting cardiovascular diseases, sexual dysfunction and/or adverse conditions associated with apoptosis.Type: GrantFiled: July 3, 2007Date of Patent: August 12, 2008Assignee: Solvay Pharmaceuticals GmbHInventors: Dagmar Hoeltje, Yvan Fischer, Dieter Ziegler, Michael Weske, Katrin Michaelis, Yasmin Karimi-Nejad, Josef Messinger, Axel Pahl, Constanze Hoefer, Hrissanthi Ikonomidou, Lechoslaw Turski
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Patent number: 7410963Abstract: The invention relates to compounds having PDE2 inhibitory activities, as well as therapeutic methods by administering said compounds, in particular for treating various diseases of the central or peripheral nervous system. It further deals with pharmaceutical compositions comprising said compounds and methods for preparing said compounds.Type: GrantFiled: December 23, 2004Date of Patent: August 12, 2008Assignee: VIA Pharmaceuticals, Inc.Inventors: Mustapha Abarghaz, Stefano Biondi, Jérôme Duranton, Emmanuelle Limanton, Cesare Mondadori, Patrick Wagner
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Patent number: 7410964Abstract: Compounds of formula I: inhibit gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease.Type: GrantFiled: May 7, 2004Date of Patent: August 12, 2008Assignee: Merck Sharp & Dohme Ltd.Inventors: Kevin Dinnell, Karl Richard Gibson, Timothy Harrison, Richard Alexander Jelley, Alan John Nadin, Paul Joseph Oakley, Andrew Pate Owens, Duncan Edward Shaw, Brian John Williams
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Patent number: 7410965Abstract: A delayed release pharmaceutical formulation containing 1-dimethylamino-3-(3-methoxyphenyl)-2-methylpentan-3-ol or a pharmaceutically acceptable salt thereof in a matrix; said matrix containing from 1 to 80 wt. % of at least one pharmaceutically acceptable, matrix-forming, hydrophilic or hydrophobic polymer and having the following in vitro dissolution rate relative to 100 wt. % of the 1-dimethylamino-3-(3-methoxyphenyl)-2-methylpentan-3-ol contained in the formulation: 3-35 wt. % released after 0.5 hour, 5-50 wt. % released after 1 hour, 10-75 wt. % released after 2 hours, 15-82 wt. % released after 3 hours, 30-97 wt. % released after 6 hours, more than 50 wt. % released after 12 hours, more than 70 wt. % released after 18 hours, and more than 80 wt. % released after 24 hours.Type: GrantFiled: November 29, 2004Date of Patent: August 12, 2008Assignee: Gruenenthal GmbHInventors: Johannes Bartholomaeus, Iris Ziegler
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Patent number: 7410966Abstract: The use of compounds of formula (I) wherein R1, R3, R10, m and Ar are as defined in the Specification and pharmaceutically acceptable salts thereof in the manufacture of a medicament for the treatment or prophylaxis of diseases or conditions in which inhibition of kinase Itk activity is beneficial is disclosed.Type: GrantFiled: August 13, 2003Date of Patent: August 12, 2008Assignee: AstraZeneca ABInventors: Henrik Johansson, Karolina Lawitz, Grigorios Nikitidis, Peter Sjö, Peter Storm
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Patent number: 7410967Abstract: Fungicidal compounds of general formula (1) wherein R, R1, R2, W, X, Y and Z are as defined in the specificationType: GrantFiled: December 3, 2003Date of Patent: August 12, 2008Assignee: Syngenta Crop Protection, Inc.Inventors: Patrick Jelf Crowley, Markus Dobler, Urs Mueller, John Williams
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Patent number: 7410968Abstract: The present invention relates to compounds represented by formula (I): where the structural variables are as defined herein. The compounds are useful for promoting hydration of mucosal surfaces.Type: GrantFiled: August 26, 2005Date of Patent: August 12, 2008Assignee: PARION SCIENCES, Inc.Inventors: Michael R. Johnson, Bruce F. Molino, Jianzhong Zhang, Bruce Sargent
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Patent number: 7410969Abstract: Antitumor compounds have the five membered fused ring ecteinascidin structure of the formula (XIV). The present compounds lack a 1,4-bridging group as found in the ecteinascidins.Type: GrantFiled: January 26, 2005Date of Patent: August 12, 2008Assignee: Pharma Mar, S.A.Inventors: Ignacio Manzanares, María Jesús Martin, Alberto Rodriguez, Simon Munt, Carmen Cuevas, Marta Perez
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Patent number: 7410970Abstract: The invention concerns substituted 1,4-di-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of emesis, anxiety, depression, pain, pancreatitis and IBS.Type: GrantFiled: October 7, 2003Date of Patent: August 12, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, François Maria Sommen, Benoît Christian Albert Ghislain De Boeck, Joseph Elisabeth Leenaerts, Yves Emiel Maria Van Roosbroeck, Gaston Stanislas Marcella Diels
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Patent number: 7410971Abstract: A compound represented by the following general formula (1) or (100), a salt thereof or a hydrate of the foregoing has excellent cell adhesion inhibitory action or cell infiltration inhibitory action, and is useful as a therapeutic or prophylactic agent for various inflammatory diseases and autoimmune diseases associated with adhesion and infiltration of leukocytes, such as inflammatory bowel disease (particularly ulcerative colitis or Crohn's disease), irritable bowel syndrome, rheumatoid arthritis, psoriasis, multiple sclerosis, asthma and atopic dermatitis. wherein R10 represents optionally substituted cycloalkyl, etc., R20-23 represent hydrogen, alkyl, alkoxy, etc., R30-32 represent hydrogen, alkyl, oxo, etc., and R40 represents optionally substituted alkyl, etc.Type: GrantFiled: December 24, 2004Date of Patent: August 12, 2008Assignee: Eisai R&D Management Co., Ltd.Inventors: Tetsuya Kawahara, Makoto Kotake, Naoki Yoneda, Shinsuke Hirota, Masayoshi Ohkuro
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Patent number: 7410972Abstract: The invention provides N-pyrazinyl-thienylsulphonamides of formula (I) for use in the treatment of chemokine mediated diseases.Type: GrantFiled: December 17, 2002Date of Patent: August 12, 2008Assignee: AstraZeneca ABInventors: Andrew Baxter, Timothy Johnson, Nicholas Kindon, Bryan Roberts, John Steele, Michael Stocks, Nicholas Tomkinson
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Patent number: 7410973Abstract: The present invention relates to novel 4-amino-substituted pyrimidine derivatives which stimulate soluble guanylate cyclase, to processes for the preparation thereof, and to the use thereof for producing medicaments, in particular medicaments for the treatment of central nervous system diseases.Type: GrantFiled: July 7, 2003Date of Patent: August 12, 2008Assignee: Bayer Healthcare AGInventors: Achim Feurer, Joachim Luithle, Stephan-Nicholas Wirtz, Gerhard König, Johannes-Peter Stasch, Elke Stahl, Rudy Schreiber, Frank Wunder, Dieter Lang
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Patent number: 7410974Abstract: The present invention includes novel compounds of the formula (I) wherein X is absent or trans or cis CHCH, R1 is (C1-C10) alkyl unsubstituted or substituted by one to three hydroxy, (C1-C10) alkenyl unsubstituted or substituted by one to three hydroxy, (C1-C10) alkynyl unsubstituted or substituted by one to three hydroxy, or aryl unsubstituted or substituted by one to three hydroxy; R2 is hydrogen, alkyl or aryl; R3 and R4 are, independently of each other, H, halogen, or a solubilizing group, with the provisio that at least one of R3 and R4 is halogen; and pharmaceutically acceptable salts thereof. The invention also includes pharmaceutically acceptable formulations of said compounds which exhibit antibiotic activity against a wide spectrum of microorganisms including organisms which are resistant to multiple antibiotic families and are useful as antibacterial agents for treatment or prophylaxis of bacterial infections, or their use as antiseptics, agents for sterilization or disinfection.Type: GrantFiled: August 6, 2004Date of Patent: August 12, 2008Assignee: Ulysses Pharmaceutical Products, Inc.Inventors: Suzanne Chamberland, Francois Malouin
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Patent number: 7410975Abstract: The invention provides methods and compositions useful for modulating signaling through Toll-like receptors. The methods involve contacting a TLR-expressing cell with a small molecule having a core structure including at least two rings. Certain of the compounds are 4-primary amino quinolines. Many of the compounds and methods are useful specifically for inhibiting immune stimulation involving at least one of TLR9, TLR8, TLR7, and TLR3. The methods may have use in the treatment of autoimmunity, inflammation, allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer, and immunodeficiency.Type: GrantFiled: June 18, 2004Date of Patent: August 12, 2008Assignees: Coley Pharmaceutical Group, Inc., Coley Pharmaceutical GmbHInventors: Grayson B. Lipford, Alexandra Forsbach, Charles Zepp
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Patent number: 7410976Abstract: The invention relates to a compound of a formula (I): or a pharmaceutically acceptable salt or ester thereof, useful as a therapeutic agent for various ACC-related disorders.Type: GrantFiled: July 14, 2006Date of Patent: August 12, 2008Assignee: Merck & Co., Inc.Inventors: Takeru Yamakawa, Hideki Jona, Kenji Niiyama, Koji Yamada, Tomoharu Iino, Mitsuru Ohkubo, Hideaki Imamura, Jun Shibata, Jun Kusunoki, Lihu Yang
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Patent number: 7410977Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.Type: GrantFiled: April 22, 2005Date of Patent: August 12, 2008Assignee: Merck & Co., Inc.Inventors: Robert S. Meissner, James J. Perkins
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Patent number: 7410978Abstract: A pharmaceutical composition of a pharmaceutically acceptable trospium salt, with upon administration to a human patient generates an average steady state blood levels of trospium with a minimum (Cmin) and maximum (Cmax) blood levels of about 0.5-2.5 ng/ml and about 2.0-6.0 ng/ml, respectively.Type: GrantFiled: November 4, 2004Date of Patent: August 12, 2008Assignee: Supernus Pharmaceuticals, Inc.Inventors: Argaw Kidane, Henry H. Flanner, Padmanabh Bhatt, Arash Raoufinia
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Patent number: 7410979Abstract: The present invention relates to anti-HCV dihaloacetamide compounds in synergistic combination with an interferon and/or ribavirin and pharmaceutical compositions thereof for inhibition of the replication of HCV virus. The present invention also relates to the use of the compositions to inhibit HCV replication and/or proliferation and to treat or prevent HCV infections.Type: GrantFiled: November 19, 2004Date of Patent: August 12, 2008Assignee: Rigel Pharmaceuticals, Inc.Inventor: Henry Lu
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Patent number: 7410980Abstract: A crystal of (1S,2S,3R,4S,5R,8R,9S,10R,13S)-4-acetoxy-2-benzoyloxy-9,10-[(1S)-2-(dimethylamino)ethylidenedioxy]-5,20-epoxy-1-hydroxytax-11-en-13-yl (2R,3S)-3-(tert-butoxycarbonylamino)-3-(3-fluoro-2-pyridyl)-2-hydroxypropionate, which has characteristic peaks at diffraction angles (2?) of 6.2°, 10.3°, 10.7°, 11.4°, and 12.0° in a powder X-ray diffraction pattern, and a method for preparing the aforementioned crystal, which comprises the step of performing crystallization by using an organic solvent selected from the group consisting of a ketone type solvent, a nitrile type solvent, and a mixture thereof, or a mixture of said organic solvent and water.Type: GrantFiled: November 29, 2002Date of Patent: August 12, 2008Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Seishiro Uchida, Yoshihiro Takayanagi, Makoto Ono
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Patent number: 7410981Abstract: An imidazole compound represented by the formula (I), a salt thereof and a compound of the formula (V), which is one of the intermediates thereof. wherein each symbol is as defined in the present specification. The compound of the present invention shows a superior anti-ulcer activity, a gastric acid secretion inhibitory action, a mucosa-protecting action, an anti-Helicobacter pylori action and the like. Since it shows low toxicity, the compound is useful as a pharmaceutical product.Type: GrantFiled: June 13, 2003Date of Patent: August 12, 2008Assignee: Takeda Pharmaceutical Company LimitedInventors: Keiji Kamiyama, Hiroshi Banno, Fumihiko Sato
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Patent number: 7410982Abstract: There is provided a heretoaryloxy/thio 3-substituted propanamine compound of formula (I) wherein A is selected from —O— and —S—; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C1-C4 alkyl and C1-C4 alkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C1-C4 alkyl, and C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl —S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, and thienopyridyl, each of which may be optionally substituted with up to 4 or, where possible, up to 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro acetyl, —CF3, —SCF3 aType: GrantFiled: October 24, 2003Date of Patent: August 12, 2008Assignee: Eli Lilly and CompanyInventors: Serge Louis Boulet, Sandra Ann Filla, Peter Thaddeus Gallagher, Kevin John Hudziak, Anette Margareta Johansson, Rushad E. Karanjawala, John Joseph Masters, Brian Michael Mathes, Richard Edmund Rathmell, Maria Ann (nee Fagan) Whatton, Victor Matassa, Chad Nolan Wolfe
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Patent number: 7410983Abstract: The present invention relates to a combination of a peroxisome proliferator activated receptor (PPAR) activator and a benzoquinone and their use in treating and/or preventing disorders characterized by endothelial dysfunction, such as cardiovascular disease, strokes and myocardial infarction. According to a preferred embodiment of the invention the benzoquinone or precursor thereof is a ubiquinone or precursor thereof, more preferably, coenzyme Q10 or a precursor thereof, and the PPAR activator is a fibrate or a thiazolidinedione, more preferably fenofibrate.Type: GrantFiled: October 23, 2001Date of Patent: August 12, 2008Assignee: Fournier Laboratories Ireland LimitedInventors: Gerald Francis Watts, David Alan Playford
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Patent number: 7410984Abstract: The present invention relates to novel pyridone derivatives capable of inhibiting ?4 integrin mediated cell adhesion, processes for their preparation, compositions comprising them and their use in the treatment of diseases capable of being modulated by the inhibition of cell adhesion.Type: GrantFiled: August 8, 2003Date of Patent: August 12, 2008Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Jason Witherington, Richard Leonard Elliott
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Patent number: 7410985Abstract: The present invention provides an cycloalkyl derivative of 3-hydroxy-4-pyridinone which is useful for the chelation of metal ions such as iron. Its preparation and use is described. In particular, the invention concerns the removal of iron in chemical and biological systems including chelating agents having the formula (I); wherein R1 is X with the proviso that R2 is Y; or R1 is T with the proviso that R2 is W; or R1 is X with the proviso that R2 R5 N when taken together form a heterocyclic ring selected from piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl, wherein the group piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl is either unsubstituted or substituted with one to three C1 to C6 alkyl groups.Type: GrantFiled: November 18, 2004Date of Patent: August 12, 2008Assignee: Apotex Inc.Inventors: Tim Fat Tam, Michael Spino, Wanren Li, Yingsheng Wang, Yanqing Zhao, Birenkumar Hasmukhbhai Shah
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Patent number: 7410986Abstract: 4-aryl pyrimidine compounds of general formula and salts thereof: wherein X is CH or N; R1 is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, etc.; R2 is hydrogen or hydroxy; R3 is hydrogen, C1-6 alkyl, etc.; R4 is hydrogen, hydroxy, halogen, amino, etc.; R5 is hydroxy, amino, carboxy, etc.; R6 is hydrogen, carbamoyl, cyano, carboxy, C1-6 alkoxycarbonyl, etc. and R7 is amino or C1-6 alkanoylamino. The compounds (I) or the salts thereof have an excellent anti-inflammatory activity and the like.Type: GrantFiled: November 19, 2001Date of Patent: August 12, 2008Assignee: Bayer AktiengesellschaftInventors: Toshiki Murata, Sachiko Sasaki, Takashi Yoshino, Yuka Ikegami, Tsutomu Masuda, Mitsuyuki Shimada, Takuya Shintani, Makoto Shimazaki, Timothy B. Lowinger, Karl B. Ziegelbauer, Kinji Fuchikami, Masaomi Umeda, Hiroshi Komura, Nagahiro Yoshida
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Patent number: 7410987Abstract: A method of treating pain or pruritis comprising administering to a patient in need thereof a pharmaceutically effective amount of a ? opioid receptor agonist of the formula wherein R is an alkyl having an amino group as a substituent; and R1 is acyl.Type: GrantFiled: May 15, 2006Date of Patent: August 12, 2008Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Maki Tokai, Takahiro Honda, Masashi Niwa, Yaeko Osumi, Ken-ichi Fujimura, Shin-ichi Kohno
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Patent number: 7410988Abstract: 2-Amido-4-substituted-aryl-thiazole-based compounds exhibiting ATP-utilizing enzyme inhibitory activity, methods of using compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions comprising compounds exhibiting ATP-utilizing enzyme inhibitory activity, are disclosed.Type: GrantFiled: August 11, 2005Date of Patent: August 12, 2008Assignee: Genentech, Inc.Inventors: John K. Dickson, Jr., Carl Nicholas Hodge, Jose Serafin Mendoza, Ke Chen
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Patent number: 7410989Abstract: The present invention relates to novel compounds and methods that are useful in treating members of the Flaviviridae family of viruses. Compounds of the present invention will have a structure according to Formulas (I)-(VI) as recited throughout the application.Type: GrantFiled: November 20, 2006Date of Patent: August 12, 2008Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc., Auburn UniversityInventors: Christine C. Dykstra, Maurice Daniel Givens, David A. Stringfellow, Kenny Brock, David Boykin, Arvid Kumar, W. David Wilson, Richard R. Tidwell, Chad F. Stephens
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Patent number: 7410990Abstract: This invention features a compound of formula (I): R1 is aryl or heteroaryl; each of R2 and R4, independently, is H, halogen, CN, alkyl, ORa, or NRaRb; R3 is H, halogen, CN, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cyclyl, heterocyclyl, ORa, OC(O)Ra, OC(O)NRaRb, NRaRb, NRaC(O)Rb, NRaS(O)RbNRaS(O)2Rb, NRaC(O)NRbRc, NRaC(S)NRbRc, NRaC(NRb)NRcRd, NRaC(O)ORb, S(O)NRaRb, S(O)2NRaRb, S(O)Ra, S(O)2Ra, C(O)Ra, C(O)ORa, or C(O)NRaRb; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; A is O, S, S(O), S(O)2, or NRe; B is N or CRf; X is O, S, S(O), S(O)2, NRe, or C(O); Y is a covalent bond, C(O), C?NRa, O, S, S(O), S(O)2, or NRe; Z is N or CH; each of U and V, independently, is N or CR; and W is O, S, or NRe; in which each of Ra, Rb, Rc, and Rd, independently, is H, alkyl, aryl, heteroaryl, cyclyl, or heterocyclyl; Re is H, alkyl, aryl, acyl, or sufonyl; and Rf is H, alkyl, aryl, acyl, sulfonyl, alkoxyl, amino, ester, amide, CN, or halogen.Type: GrantFiled: October 3, 2006Date of Patent: August 12, 2008Assignee: Synta Pharmaceuticals Corp.Inventors: Lijun Sun, Mitsunori Ono, Yumiko Wada, Weiwen Ying, Teresa Przewloka, Elena Kostik
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Patent number: 7410991Abstract: The invention provides substituted pyrazolidinone compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing preterm labor, dysmenorrhea, asthma, hypertension, infertility or fertility disorder, undesired blood clotting, preeclampsia or eclampsia, an eosinophil disorder, sexual dysfunction, osteporosis and other destructive bone disease or disorder, and other diseases and disorders associated with the prostaglandin EP2 and/or EP4 receptors.Type: GrantFiled: October 23, 2002Date of Patent: August 12, 2008Assignee: Laboratoires Serono S.A.Inventors: Gian Luca Araldi, Yihua Liao, Adulla P. Reddy, Zhong Zhao
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Patent number: 7410992Abstract: This invention relates to potent potassium channel blocker compounds of Formula (I) or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans, or a pharmaceutically acceptable salt, in vivo hydrolysable ester, enantiomer, diastereomer or mixture thereof: formula (II) represents C6-10 aryl or C3-10 heterocyclyl, said aryl or heterocyclyl optionally substituted with 1-3 groups selected from Ra; Z represents (CH2)nPO(OR)(OR*).Type: GrantFiled: August 31, 2004Date of Patent: August 12, 2008Assignee: Merck & Co. Inc.Inventors: Meng Hsin Chen, James B. Doherty, Luping Liu, Swaminathan Natarajan, Robert M. Tynebor
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Patent number: 7410993Abstract: This invention generally relates to the derivatives of 3,6 disubstituted azabicyclo[3.1.0] hexanes. The compounds of this invention are muscarinic receptor antagonists which are useful, inter-alia, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to a process for the preparation of the compounds of the present invention, pharmaceutical compositions containing the compounds of the present invention and the methods for treating the diseases mediated through muscarinic receptors.Type: GrantFiled: August 9, 2002Date of Patent: August 12, 2008Assignee: Ranbaxy Laboratories LimitedInventors: Anita Mehta, Arundutt V. Silamkoti, Miriyala Bruhaspathy, Jang Bahadur Gupta
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Patent number: 7410994Abstract: This invention relates to compounds, which are generally anti-inflammatory and analgesic compounds, and which are represented by Formula I: wherein A is a —CH2—, —O—, —S—, or —S(O)—; and the other substituents are as defined in the specification; or individual isomers, mixtures of isomers, and pharmaceutically acceptable salts thereof.Type: GrantFiled: March 2, 2006Date of Patent: August 12, 2008Assignee: Roche Palo Alto LLCInventors: Chris Allen Broka, Jeffrey Allen Campbell
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Patent number: 7410995Abstract: This invention relates to pharmaceutical compositions and methods for treating a vision disorder, improving vision, treating memory impairment, or enhancing memory performance using N-linked sulfonamides of heterocyclic thioesters.Type: GrantFiled: August 14, 1998Date of Patent: August 12, 2008Assignee: GPI Nil Holdings Inc.Inventors: Douglas T. Ross, Hansjörg Sauer, Gregory S. Hamilton, Joseph P. Steiner
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Patent number: 7410996Abstract: There is provided a compound of formula (I) wherein A is selected from —O— and —S—; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C1-C4 alkyl and C1-C4 alkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C1-C4 alkyl, and C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, up to 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0,Type: GrantFiled: October 24, 2003Date of Patent: August 12, 2008Assignee: Eli Lilly and CompanyInventors: Serge Louis Boulet, Sandra Ann Filla, Peter Thaddeus Gallagher, Kevin John Hudziak, Anette Margareta Johansson, Rushad E. Karanjawala, John Joseph Masters, Victor Giulio Matassa, Brian Michael Mathes, Richard Edmund Rathmell, Maria Ann Whatton, Chad Nolan Wolfe
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Patent number: 7410997Abstract: Compounds represented by formula (1), wherein X is, for example, CH, CH2, CHR (wherein R is a lower alkyl group or a substituted lower alkyl group) or CRR? (wherein R and R? are the same as the above defined R); Y is, for example, CH, CH2 or C?O; Z is, for example, O, S, S?O or SO2; U is C or N; R1 to R4 are each independently, for example, a hydrogen atom, OR, SR (wherein R is the same as defined above), or an aromatic ring, a substituted aromatic ring or a heterocycle; at least one of R5 and R8 is, for example, OH and the remaining of R5 and R8 are each independently, for example, a hydrogen atom or OH, optical isomers thereof, conjugates thereof or pharmaceutically acceptable salts thereof are provided. These compounds are characterized in having a wide range of pharmacological actions such as an excellent relaxing action of tracheal smooth muscles, an inhibition of airway hypersensitivity and an inhibition of infiltration of inflammatory cells into the airway and, in addition, high safety.Type: GrantFiled: December 5, 2003Date of Patent: August 12, 2008Assignee: Nippon Sulsan Kaisha, Ltd.Inventors: Shuji Jinno, Takaaki Okita, Naomi Ohtsuka, Shinya Yamashita, Junichiro Hata, Jiro Takeo
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Patent number: 7410998Abstract: Benzopyran-based inhibitors of NADH:ubiquinone oxidoreductase for inhibiting the growth of cancer cells.Type: GrantFiled: September 6, 2001Date of Patent: August 12, 2008Assignee: The Scripps Research InstituteInventors: Kyriacos C. Nicolaou, Jeffrey Pfefferkorn, Guo-Qiang Cao, Anthony Roecker
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Patent number: 7410999Abstract: The present invention relates to novel compounds and methods that are useful in treating members of the Flaviviridae family of viruses. Compounds of the present invention will have a structure according to Formulas (I)-(VI) as recited throughout the application.Type: GrantFiled: November 20, 2006Date of Patent: August 12, 2008Assignees: University of North Carolinia at Chapel Hill, Georgia State University Research Foundation, Inc., Auburn UniversityInventors: Christine C. Dykstra, Maurice Daniel Givens, David A. Stringfellow, Kenny Brock, David Boykin, Arvid Kumar, W. David Wilson, Richard R. Tidwell, Chad F. Stephens