Patents Issued in October 12, 2010
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Patent number: 7811985Abstract: The invention relates to peptides having the general formula (I), or a salt or amide thereof, wherein R1 and R2 are either the same or different, wherein R1 and R2 are each selected from the group consisting of hydrogen and a saturated or unsaturated hydrocarbon residue, said residue having from 1 to 10 carbon atoms, wherein Z1 is selected from the group consisting of histidine and proline, wherein Z2 is selected from the group consisting of an arginine and a peptide comprising an initial arginine and having from 2 to 30 amino acids. The invention also relates to methods using the peptides of the present invention in the treatment of inflammation.Type: GrantFiled: September 6, 2007Date of Patent: October 12, 2010Assignee: Ikaria Development Subsidiary Two LLCInventor: Peter Petzelbauer
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Patent number: 7811986Abstract: The present invention relates to cDNA sequences from a region of amplification on chromosome 20 associated with disease. The sequences can be used in hybridization methods for the identification of chromosomal abnormalities associated with various diseases. The sequences can also be used for treatment of diseases.Type: GrantFiled: July 22, 2008Date of Patent: October 12, 2010Assignees: The Regents of The University of California, The Hospital for Sick ChildrenInventors: Joe W. Gray, Colin Conrad Collins, Soo-in Hwang, Tony Godfrey, David Kowbel, Johanna Rommens
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Patent number: 7811987Abstract: The invention provides a method for reducing CD36 expression in a cell. The method comprises contacting the cell with an effective amount of an aromatic-cationic peptide having at least one net positive charge; a minimum of four amino acids; a maximum of about twenty amino acids; a relationship between the minimum number of net positive charges (pm) and the total number of amino acid residues (r) wherein 3 pm is the largest number that is less than or equal to r+1; and a relationship between the minimum number of aromatic groups (a) and the total number of net positive charges (pt) wherein 2a is the largest number that is less than or equal to pt+1, except that when a is 1, pt may also be 1.Type: GrantFiled: May 1, 2009Date of Patent: October 12, 2010Assignee: Cornell Research Foundation, Inc.Inventors: Hazel H. Szeto, Shaoyl Liu, Sunghee Cho
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Patent number: 7811988Abstract: The present invention provides novel lipid mixtures for synthetic surfactants. In particular, the invention provides a specific lipid mixture containing a specific amount of polyunsaturated phospholipids to be used for the preparation of synthetic surfactants. Said surfactants and pharmaceutical compositions thereof are useful for the treatment of surfactant deficiencies like respiratory distress syndrome (RDS).Type: GrantFiled: May 26, 2004Date of Patent: October 12, 2010Assignee: Chiesi Farmaceutici S.p.A.Inventors: Jan Johansson, Tore Curstedt, Bengt Robertson
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Patent number: 7811989Abstract: The invention provides analogs of PYY. The invention also provides compositions and methods useful for controlling biological activities such as cell proliferation, nutrient transport, lipolysis, and intestinal water and electrolyte secretion.Type: GrantFiled: January 13, 2004Date of Patent: October 12, 2010Assignee: Ipsen Pharma S.A.S.Inventor: Zheng Xin Dong
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Patent number: 7811990Abstract: Described herein are methods and compositions for the treatment of spinal disorders mediated by nucleus pulposus. The compositions can include a soluble cytokine receptor and/or a TNF-? blocking antibody.Type: GrantFiled: April 20, 2007Date of Patent: October 12, 2010Assignee: Sciaticon ABInventors: Kjell Olmarker, Bjorn Rydevik
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Patent number: 7811991Abstract: Methods are described for preventing or reducing ischemia and/or systemic inflammatory response in a patient such as perioperative blood loss and/or systemic inflammatory response in a patient subjected to cardiothoracic surgery, e.g. coronary artery bypass grafting and other surgical procedures, especially when such procedures involve extra-corporeal circulation, such as cardiopulmonary bypass.Type: GrantFiled: October 30, 2007Date of Patent: October 12, 2010Assignee: Dyax Corp.Inventors: Robert C. Ladner, Arthur C. Ley
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Patent number: 7811992Abstract: Disclosed are compositions and methods for treating ischemia and molecules related to hibernation states. FPA molecules having the sequence set forth in SEQ ID NO: 2 can be used for as anti-infarction agents.Type: GrantFiled: February 5, 2003Date of Patent: October 12, 2010Assignee: Stasys Technologies, Inc.Inventors: James E. Skinner, Jerry M. Anchin
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Patent number: 7811993Abstract: Novel BRAFV600E mutant peptides or a pharmaceutically acceptable salt thereof, that induce MHC Class I-dependent cytotoxic T cell responses in mammals are useful in prophylactic, diagnostic and therapeutic treatments for melanoma. Such compounds are also useful in drug development for non-peptide mimics of the compounds described herein and in the development of therapeutic or diagnostic antibodies.Type: GrantFiled: June 28, 2006Date of Patent: October 12, 2010Assignee: The Wistar Institute of Anatomy and BiologyInventors: Dorothee Herlyn, Rajasekaran Somasundaram, Laszlo Otvos, Jr.
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Patent number: 7811994Abstract: A method for the identification of peptides having an affinity for the surface of fungi is provided as is a method for the identification of peptides capable of affecting the development of a fungus. Also provided are compositions containing peptides identified using the method of the present invention. In addition, isolated polynucleotides, vectors, expression cassettes and transformed cells capable of expressing peptides identified by the method of the present invention are provided.Type: GrantFiled: April 13, 2009Date of Patent: October 12, 2010Assignee: The Curators of the University of MissouriInventors: James T. English, Francis J. Schmidt, George P. Smith, Roy O. Morris, Sharon Bishop-Hurley
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Patent number: 7811995Abstract: This invention generally relates to peptides useful for medical diagnosis and treatment of pathogenic disorders. More specifically, the invention relates to immunostimulatory peptides which can stimulate the production of therapeutically beneficial cytokines and, in combination with antibodies against human pathogens such as the immunodeficiency virus (HIV), inhibit replication of such pathogens. The peptides interact synergistically with pathogen-directed antibodies without producing or sustaining serious side-effects such as inflammation, and provide the potential for treatment modalities that are non-specific with respect to pathogen and cell type. Therefore, the peptides of the present invention have wide applicability with respect to medical treatment of pathogen-mediated infections, and the potential to enhance well-being.Type: GrantFiled: December 12, 2007Date of Patent: October 12, 2010Assignee: Susavion Biosciences, Inc.Inventors: Laura L. Eggink, Kenneth J. Hoober
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Patent number: 7811996Abstract: The invention provides compositions and methods for reducing one or more symptoms of an autoimmune disease, inflammatory disease, and/or transplant rejection, by the administration to a subject in need thereof a pharmaceutically effective amount of a purified compound of any one of Formulae A-E. The invention's methods are useful for the prevention, amelioration, and treatment of autoimmune disease, inflammatory disease, and/or transplant rejection.Type: GrantFiled: November 1, 2002Date of Patent: October 12, 2010Assignee: The Regents of the University of CaliforniaInventor: Michael David
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Patent number: 7811997Abstract: The invention relates to a composition containing total triterpenoid sapogenins extracted from bamboo, the preparation method and use thereof. These total triterpenoid sapogenins are extracted from many parts of bamboo such as bamboo shavings in Gramineae by CO2 Supercritical Fluid Extraction technique. In the extract, the content of total triterpenoid sapogenins is 10-90%, while the contents of friedelin and lupenone are 5-35% and 1-10%, respectively. The extract in the invention has good physiological and pharmacological activities such as anti-free radical, anti-oxidation, anti-tumor and anti-hypertension. It can be used in medicines or functional foods for the treatment or prevention of cardiovascular and cerebrovascular diseases and tumor. It is also useful in cosmetics field.Type: GrantFiled: April 28, 2003Date of Patent: October 12, 2010Inventors: Ying Zhang, Xiaoqin Wu, Zhuoyu Yu, Yunlong Zhu, Lingen Chen, Shenggen Lou
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Patent number: 7811998Abstract: Novel analogues and derivatives of novobiocin are provided, including compounds having modifications to the amide side chain, coumarin ring, and sugar moieties. The compounds of the present invention are useful as heat shock protein 90 inhibitors, and may be used as anticancer and neuroprotective agents.Type: GrantFiled: October 1, 2009Date of Patent: October 12, 2010Assignees: University of Kansas, The United States of America as represented by the Department of Health and Human ServicesInventors: Brian S. Blagg, Len Neckers, Xiao Ming Yu
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Patent number: 7811999Abstract: This invention provides a method of treating a subject suffering from an obstructive respiratory disease, including the step of administering to a subject a compound comprising a lipid or phospholipid moiety bound to a physiologically acceptable monomer, dimer, oligomer, or polymer, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof, in an amount effective to treat the subject suffering from an obstructive respiratory disease.Type: GrantFiled: November 17, 2004Date of Patent: October 12, 2010Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem, Ltd.Inventors: Saul Yedgar, David Shoseyov
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Patent number: 7812000Abstract: The invention relates to the therapeutic use of oligonucleotides as immunostimulatory agents in immunotherapy applications. More particularly, the invention provides immunomers for use in methods for generating an immune response or for treating a patient in need of immunostimulation. The immunomers of the invention comprise at least two oligonucleotides linked at their 3? ends, internucleoside linkages or functionalized nucleobase or sugar to a non-nucleotidic linker, at least one of the oligonucleotides being an immunostimulatory oligonucleotide and having an accessible 5? end.Type: GrantFiled: October 3, 2007Date of Patent: October 12, 2010Assignee: Idera Pharmaceuticals, Inc.Inventors: Sudhir Agrawal, Ekambar R. Kandimalla, Dong Yu, Lakshmi Bhagat
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Patent number: 7812001Abstract: RNA aptamers and methods for identifying the same are disclosed. The RNA aptamers selectively bind coagulation factors, E2F family members, Ang1 or Ang2, and therapeutic and other uses for the RNA aptamers are also disclosed.Type: GrantFiled: October 26, 2007Date of Patent: October 12, 2010Assignee: Duke UniversityInventors: Bruce A. Sullenger, Christopher P. Rusconi
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Patent number: 7812002Abstract: The invention provides novel double stranded oligoribonucleotides that inhibit the Nrf2 gene. The invention also provides a pharmaceutical composition comprising one or more such oligoribonucleotides, and a vector capable of expressing the oligoribonucleotide. The present invention also relates to methods and compositions for treating or preventing the incidence or severity of a cancerous disease, particularly various lung cancers.Type: GrantFiled: March 19, 2008Date of Patent: October 12, 2010Assignee: Quark Pharmaceuticals, Inc.Inventor: Elena Feinstein
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Patent number: 7812003Abstract: Provided herein are methods to suppress specificity protein (Sp) activity in a cell associated with a cell proliferative disease. The methods are effective to inhibit a microRNA in the cell using an antisense microRNA oligonucleotide which results in an increase in expression of a specificity protein (Sp) suppressor gene thereby inducing Sp degradation, apoptosis or growth arrest by releasing inhibitors of G2/M (Myt-1) or inhibition. Also provided are methods of treating a cancer using the antisense microRNA oligonucleotide. In addition the present invention provides antisense microRNA-27a oligonucleotides useful in the methods described herein.Type: GrantFiled: August 1, 2008Date of Patent: October 12, 2010Inventors: Stephen H. Safe, Sudhakar Chintharlapalli, Susanne U. Talcott
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Patent number: 7812004Abstract: The invention relates to novel inulin products and compositions thereof, to their manufacture, to their use for modifying and modulating the bacterial flora and the fermentation pattern of inulin in the large intestine of humans, mammals or other vertebrates, to their use for providing improved inulin-associated nutritional effects/benefits, as well as to their use for the manufacture of consumer products and compositions for providing said effects/benefits in healthy, disfunctioned and diseased humans, mammals and other vertebrates. The novel inulin products consist of a particular mixture of an easily fermentable inulin (EFI) component and a hardly fermentable inulin (HFI) component. The nutritional effects/benefits include dietary fiber effects, improved mineral absorption, particularly calcium and magnesium, bone mineral density increase, reduction of bone mineral density loss, modulation of lipid metabolism, stimulation of the immune system, and anti-cancer effects.Type: GrantFiled: February 14, 2001Date of Patent: October 12, 2010Assignee: Tiense Suikerraffinaderij N.V.Inventors: Anne Frippiat, Jan Van Loo, Georges Smits
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Patent number: 7812005Abstract: The present invention relates to the use of glycosaminoglycan fractions having an average molecular weight of 2400 (±200) D for the preparation of pharmaceutical compositions suitable for the treatment of emotional dysfunctions, especially depressive disorders, anxiety disorders, anxiety neurosis, agitation, confusion.Type: GrantFiled: May 19, 2004Date of Patent: October 12, 2010Inventors: Umberto Cornelli, Luigi De Ambrosi, Stanley Lorens, Jawed Fareed, John Lee, Israel Hanin, Ronald Mervis
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Patent number: 7812006Abstract: The invention relates to conjugates derived from the reductive amination of the pneumococcus serotype 5capsular polysaccharide. The conditions for reductive amination differ from conventional conditions in that they make it possible to avoid the appearance of an undesirable compound which harms the immunogenicity of the conjugates. In carbon NMR spectrum, this undesirable compound is characterized by a resonance signal between 13 and 14 ppm. The aminated polysaccharides used to produce the conjugates therefore have a carbon NMR spectrum lacking a resonance signal between 13 and 14 ppm. The invention offers two conditions for reductive amination. According to a first method, the reductive amination is carried out at a slightly acidic pH (4-6.5) for at the very most 4 hours. According to a second method, the polysaccharide is first of all reduced, then fragmented and, finally, subjected to a reductive amination per se, under conditions which may or may not be conventional.Type: GrantFiled: January 15, 2004Date of Patent: October 12, 2010Assignee: Aventis Pasteur S.A.Inventors: Noëlle Mistretta, Emilie Danve, Monique Moreau
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Patent number: 7812007Abstract: Alkali and alkali-earth metal salts of polysaccharides derived from heparin, their method of preparation and the pharmaceutical compositions containing them.Type: GrantFiled: April 1, 2005Date of Patent: October 12, 2010Assignee: Aventis Pharma S.A.Inventors: Christelle Pecquet, Elisabeth Perrin, Christian Viskov
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Patent number: 7812008Abstract: This invention provides compounds of Formula (I); or a tautomer or pharmaceutically acceptable salts thereof useful as antibacterial agents.Type: GrantFiled: February 14, 2006Date of Patent: October 12, 2010Assignee: Wyeth LLCInventors: Phaik-Eng Sum, Tarek Mansour
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Patent number: 7812009Abstract: A pharmaceutical composition for intramammary administration to a nonhuman mammal comprising an antibacterial agent and prednisolone, wherein the composition comprises at least 20 mg of prednisolone, and its use for the treatment of clinical mastitis.Type: GrantFiled: December 10, 2003Date of Patent: October 12, 2010Assignee: Intervet International B.V.Inventors: Peter Gerardus Franciscus Cox, Joseph Antonius Clemens Maria Lohuis, Selma Marianne Hensen
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Patent number: 7812010Abstract: Formulations for topical or local administration of drugs directly to the breast or chest to produce a regional or local effect with lower systemic drug levels than when an effective amount is administered systemically are disclosed herein. In a preferred embodiment, the drug is administered to the surface of the breast, areola, or directly to the nipple. The formulations provide increased patient comfort, increased bioavailability and relatively high blood levels in the region to be treated with a reduction of side effects compared to those administered systemically. The preferred formulations contain drugs in the form of micro or nanoparticles, which may be formed of drug alone or in combination with an excipient or carrier. The excipient or carrier may modify the release rates or enhance absorption into the affected area. The drug formulation may be in the form of a cream, lotion or foam.Type: GrantFiled: January 2, 2004Date of Patent: October 12, 2010Assignee: Femmepharma, Inc.Inventors: Gerianne T. DiPiano, Peter Kevin Mays, John Ziemniak
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Patent number: 7812011Abstract: The invention relates to a FXR agonist of formula (I) and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof.Type: GrantFiled: February 28, 2005Date of Patent: October 12, 2010Assignee: Intercept Pharmaceuticals, Inc.Inventor: Roberto Pellicciari
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Patent number: 7812012Abstract: To reduce amounts of fat accumulated in abdominal cavity and to prevent or ameliorate visceral fat type obesity, considered to be a main factor of metabolic syndrome, the present invention provides an agent or a food or drink which contains a compound having a lophenol skeleton, or an organic solvent extract or a hot water extract of a Liliaceae plant, or a fraction thereof containing the compound is used as an active ingredient.Type: GrantFiled: September 21, 2006Date of Patent: October 12, 2010Assignee: Morinaga Milk Industry Co., Ltd.Inventors: Miyuki Tanaka, Eriko Misawa
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Patent number: 7812013Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt, solvate or ester thereof, wherein U, W, X, L, Y, M, Z, c, d, e, f, g, h, s, t, R1, R2, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and R18 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: GrantFiled: June 12, 2006Date of Patent: October 12, 2010Assignee: Schering CorporationInventors: Ulrich Iserloh, Zhaoning Zhu, Andrew Stamford, Johannes H. Voigt
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Patent number: 7812014Abstract: The present invention provides a compound of formula I wherein one of A and B is hydrogen and the other an optionally substituted fused bicyclic heteroaryl group as defined herein; X is O; R5 is H, C1-C6 alkyl, C5-C6 cycloalkyl, or CHR3OCOC1-C6 alkyl; and R3 is hydrogen, C1-C6 alkyl, C5-C6 cycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl; or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.Type: GrantFiled: August 21, 2008Date of Patent: October 12, 2010Assignee: Wyeth LLCInventors: Aranapakam Mudumbai Venkatesan, Tarek Suhayl Mansour, Takao Abe, Itsuki Yamamura, Tsuyoshi Takasaki, Atul Agarwal, Osvaldo Dos Santos, Fuk-Wah Sum, Yang-I Lin
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Patent number: 7812015Abstract: The invention relates to the use of inhibitors of acid sphingomyelinase and/or of inhibitors of products of the reaction catalyzed by this enzyme, for the prophylaxis and/or treatment of infectious diseases and/or diseases which are influenced by infections during the course thereof. The cited products especially include ceramide. Preferrably neutralizing antibodies and/or antidepressants, especially tricyclic and/or tetracyclic antidepressants, are used as inhibitors.Type: GrantFiled: August 21, 2003Date of Patent: October 12, 2010Inventor: Erich Gulbins
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Patent number: 7812016Abstract: The present invention features compounds that are HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.Type: GrantFiled: May 12, 2004Date of Patent: October 12, 2010Assignee: SmithKline Beecham CorporationInventor: Brian A. Johns
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Patent number: 7812017Abstract: The present invention relates to novel compounds of formula (I): wherein m, n, R0, R1, R2, R3 and R4 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds for the preparation of a medicament against 5-HT6 receptor-related disorders.Type: GrantFiled: July 3, 2007Date of Patent: October 12, 2010Assignee: Biovitrum AB (publ.)Inventors: Johan Angbrant, Rune Ringom, Kristin Hammer, Erik Ringberg, Bengt Lindqvist, Gary Johansson, Peter Brandt, Katarina Beierlein, Björn M Nilsson
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Patent number: 7812018Abstract: This invention provides alpha-carboline compounds of formula I: wherein R1, R2, R3, R4, R5, and x are as described in the specification. The compounds are useful for treating inflammatory diseases and cancer.Type: GrantFiled: February 15, 2007Date of Patent: October 12, 2010Assignee: Millennium Pharmaceuticals, Inc.Inventors: Michael E. Hepperle, Julie Fields Liu, R. Scott Rowland, Dilrukshi Vitharana
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Patent number: 7812019Abstract: Compounds that are antagonists of the VR1 receptor, having formula (I) or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein A1, A2, A3, A4, R7, R8, R9, X, Y, Z, L, n, and m, are as defined herein, and are useful in disorders prevented or ameliorated by inhibiting the VR1 receptor.Type: GrantFiled: November 22, 2005Date of Patent: October 12, 2010Assignee: Abbott LaboratoriesInventors: Arthur Gomtsyan, Erol K. Bayburt, Robert G. Schmidt, Jr., Chih-Hung Lee, Brian S. Brown, Tammie K. Jinkerson, John R. Koenig, Jerome F. Daanen, Steven P. Latshaw
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Patent number: 7812020Abstract: The present invention relates to pyridine derivatives of the general formula (I) and their use as openers of the KCNQ family potassium ion channels for the treatment of CNS disorders.Type: GrantFiled: March 2, 2006Date of Patent: October 12, 2010Assignee: H. Lundbeck A/SInventors: Christian Wenzel Tornøe, Nikolay Khanzhin, Mario Rottländer, William Patrick Watson, Daniel Rodriguez Greve
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Patent number: 7812021Abstract: The invention relates to a compound of general formula wherein Ar, R1, R2, R3, R4, n, o, p, s, X and are as defined herein or to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. The compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: GrantFiled: August 21, 2008Date of Patent: October 12, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Philippe Jablonski, Kenichi Kawasaki, Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Xihan Wu
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Patent number: 7812022Abstract: The present invention provides 2-pyrimidinyl pyrazolopyridine compounds, compositions containing the same, as well as processes for the preparation and their use as pharmaceutical agents.Type: GrantFiled: December 6, 2005Date of Patent: October 12, 2010Assignee: GlaxoSmithKline LLCInventors: David Edward Uehling, Kirk Lawrence Stevens, Scott Howard Dickerson, Alex Gregory Waterson, Philip Anthony Harris, Douglas McCord Sammond, Robert Dale Hubbard, Holly Kathleen Emerson, Joseph W. Wilson
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Patent number: 7812023Abstract: The present invention relates to morpholine and thiomorpholine derivatives of the general formula I or pharmaceutically acceptable salts thereof and their use.Type: GrantFiled: November 5, 2009Date of Patent: October 12, 2010Assignee: H. Lundbeck A/SInventors: Christian Wenzel Tornøe, Mario Rottländer, Nikolay Khanzhin, Andreas Ritzèn, William Patrick Watson
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Patent number: 7812024Abstract: The present invention provides modulators of serotonin receptors, pharmaceutical compositions containing such modulators and methods for treating various diseases, conditions and disorders associated with modulation of serotonin receptors such as, for example: metabolic diseases, which includes but is not limited to obesity, diabetes, diabetic complications, atherosclerosis, impaired glucose tolerance and dyslipidemia; central nervous system diseases which includes but is not limited to, anxiety, depression, obsessive compulsive disorder, panic disorder, psychosis, schizophrenia, sleep disorder, sexual disorder and social phobias; cephalic pain; migraine; and gastrointestinal disorders using such compounds and compositions.Type: GrantFiled: May 14, 2007Date of Patent: October 12, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Guohua Zhao, Chet Kwon, Philip D. Stein
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Patent number: 7812025Abstract: A compound represented by the formula (I) or a salt thereof; and an agent for protecting a brain/neuronal cell or a therapeutic agent for sleep disorder comprising the compound or salt: wherein Z represents an oxygen or sulfur; R1 represents an aryl or heterocyclic group which may be substituted, provided that R1 is not a 3-ethyl-6-methoxy-2-methyl-5-naphthalen-1-yl group; R1a represents a hydrogen atom, a hydrocarbon group which may be substituted, a hydroxyl group or the like; R2 represents a piperidin-1,4-diyl or piperazin-1,4-diyl which may be substituted; R3 represents a bivalent group which is formed by removing two hydrogen atoms from a benzene ring or 6-membered aromatic heterocyclic ring which may have a substituent, provided that R3 is not a pyridazin-3,6-diyl; and R4 represents a group which is formed by removing one hydrogen atom from a benzene ring or 5- to 6-membered heterocyclic ring which may be substituted, provided that the substituent on the heterocyclic ring is not a phenylethyl group whicType: GrantFiled: August 11, 2006Date of Patent: October 12, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Takahiro Matsumoto, Masakuni Kori, Mitsunori Kouno
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Patent number: 7812026Abstract: The present invention relates to novel imidazole derivatives having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). The compounds are represented by the general formula (I) wherein R1, R2, R3 and R4 are as defined in the description. For example, R1 may be phenyl, R2 may be dimethylamino pyrrolidin-1-yl, R3 may be alkoxy and R4 may be alkyl, ai arylalkyl, aryloxyalkyl, aryloxy or heterocyclylalkyl.Type: GrantFiled: December 21, 2006Date of Patent: October 12, 2010Assignee: AstraZeneca ABInventors: Udo Bauer, Wayne Brailsford, Linda Gustafsson, Tor Svensson
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Patent number: 7812027Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: May 11, 2007Date of Patent: October 12, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Tesfaye Biftu, Ping Chen, Danqing Feng, Ann E. Weber
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Patent number: 7812028Abstract: The present invention relates to a method of raising HDL cholesterol comprising administering to a patient in need thereof a compound of the formula wherein A, G, R1 to R8 and R17 are as defined in the description.Type: GrantFiled: February 6, 2009Date of Patent: October 12, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Mirjana Andjelkovic, Agnes Benardeau, Evelyne Chaput, Paul Hebeisen, Matthias Nettekoven, Ulrike Obst Sander, Constantinos G. Panousis, Stephan Roever
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Patent number: 7812029Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.Type: GrantFiled: February 8, 2008Date of Patent: October 12, 2010Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li
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Patent number: 7812030Abstract: Methods, compositions, and kits are presented for local tissue protection during systemic administration of anticancer therapeutic agents.Type: GrantFiled: February 25, 2008Date of Patent: October 12, 2010Assignee: Asymmetric Therapeutics, LLCInventor: John P. Ford
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Patent number: 7812031Abstract: The present invention relates to substituted pyrimidine compounds of formula I useful as orexin receptor antagonists. The invention also relates to pharmaceutical compositions containing said compounds.Type: GrantFiled: August 10, 2006Date of Patent: October 12, 2010Assignee: Sanofi-AventisInventors: Peter Aranyi, Maria Balogh, Sandor Batori, Judit Bence, Michel Finet, Zoltan Kapui, Christophe Philippo, Tibor Szabo, Zoltan Szlavik, Zsuzsanna Tomoskozi, Katalin Urban-Szabo, Olivier Venier
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Patent number: 7812032Abstract: A rapamycin analog composition includes a crystalline form of a rapamycin analog. The crystal can be a hydrate, dehydrate, solvate, or desolvate.Type: GrantFiled: July 23, 2007Date of Patent: October 12, 2010Assignee: Abbott LaboratoriesInventors: Shekhar Viswanath, Larry Bartelt, Robert Leanna, Michael Rasmussen, Madhup Dhaon, Rodger Henry, Thomas Borchardt, Shuang Chen, Geoff Zhang
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Patent number: 7812033Abstract: Method for enhancing in a mammalian cell the activity of an enzyme associated with Gaucher Disease by administering a competitive inhibitor of glucocerebrosidase in an amount effective to enhance the activity of the enzyme. Preferred compounds for use in the method are imino sugars and related compounds. In particular, C8-12-alkyl derivatives of N-alkyl-deoxynojirimycin, isofagomine compounds, and calystegine compoiunds are effective to enhance glucocerebrosidase activity.Type: GrantFiled: September 27, 2006Date of Patent: October 12, 2010Assignee: Mount Sinai School of Medicine of New York UniversityInventors: Jian-Qiang Fan, Satoshi Ishii, Naoki Asano
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Patent number: 7812034Abstract: Liposarcomas are treated using HIV protease inhibitors, particularly nelfinavir. The protease inhibitors may be used alone or in combination with traditional cancer treatments, such as chemotherapy, radiotherapy, or surgery.Type: GrantFiled: November 2, 2004Date of Patent: October 12, 2010Assignee: City of HopeInventors: Warren Chow, Chu-Chih Shih