Nitrogen, Other Than As Nitro Or Nitroso, Attached Directly To The Six Membered Hetero Ring By Nonionic Bonding Patents (Class 514/313)
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Publication number: 20120321696Abstract: A novel function for the p53 gene related to resolution of deep venous thrombosis is disclosed herein. Lack of the p53 gene results in impaired thrombus resolution in a clinically relevant in vivo model of deep venous thrombus resolution. It is further shown that augmentation of p53 activity with quinacrine accelerates thrombus resolution in vivo, and that this beneficial effect is completely dependent on p53. p53-based therapy is therefore provided to accelerate thrombus resolution in patients, and to prevent or ameliorate the debilitating long-tem complications of deep venous thrombosis such as post-thrombotic syndrome.Type: ApplicationFiled: October 1, 2010Publication date: December 20, 2012Inventor: Rajabrata Sarkar
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Publication number: 20120322770Abstract: This invention provides methods of inhibiting replication of a poxvirus by contacting a poxvirus with a compound having formula I, formula XXI, formula XXXII, or formula XLI which in turn reduce, inhibit, or abrogate poxvirus DNA polymerase activity and/or its interaction with its processivity factor. Formula I, formula XXI, formula XXXII, or formula XLI can be utilized to treat humans and animals suffering from a poxvirus infection. Pharmaceutical compositions for treating poxvirus infected subjects are also provided.Type: ApplicationFiled: August 21, 2012Publication date: December 20, 2012Inventor: Robert P. RICCIARDI
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Publication number: 20120316124Abstract: The present invention relates to compounds formula (I), wherein P is P1, P2, heterocyclyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5, R6, R17, R18, R19 and R20 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: February 17, 2011Publication date: December 13, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Thomas Pitterna, Myriem El Qacemi, Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik
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Publication number: 20120308608Abstract: Provided herein are Compounds that induce interferon production and methods for identifying such Compounds. Also provided herein are compositions comprising such Compounds and methods of using such Compounds to treat interferon-sensitive diseases such as viral infections, cancer, and multiple sclerosis.Type: ApplicationFiled: January 31, 2011Publication date: December 6, 2012Inventors: Megan Shaw, Mila Ortigoza, Adolfo Garcia-Sastre, Peter Palese
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Publication number: 20120302601Abstract: The present invention is directed to topical ophthalmic compositions of a lipophilic compound and an oligomeric or polymeric carrier wherein the compositions are useful in the treatment and prevention of macular degeneration. The invention also includes methods of treating macular degeneration by using a topical ophthalmic composition of a lipophilic compound and an oligomeric or polymeric carrier.Type: ApplicationFiled: December 9, 2010Publication date: November 29, 2012Applicant: Neuron Systems, Inc.Inventors: Thomas A. Jordan, John Clifford Chabala, Gerald D. Cagle
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Publication number: 20120301439Abstract: Methods of treatment of diseases that include or are characterized by inappropriate or pathological neovascularization are disclosed. These diseases include diseases of the eye, such as diabetic retinopathy, retinopathy of prematurity, and choroidal neovascularization which can occur in age-related macular degeneration (AMD). Disclosed methods include administering agents that cause directly or indirectly upregulation of the ABCA1 transporter protein in macrophages. These agents include, without limitation, LXR agonists. In some embodiments, inhibitors of CETP expression or activity can also be effective. Administration routes can include, without limitation, intraocular, periocular, or systemic administration.Type: ApplicationFiled: May 24, 2012Publication date: November 29, 2012Applicant: WASHINGTON UNIVERSITYInventor: Rajendra S. Apte
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Publication number: 20120301422Abstract: The invention provides a method of enhancing the action of a pharmaceutical agent selected from the group consisting of the anti-infective agents, the group comprising of the antimicrobial agents, the anthelmintic agents and the anti-ectoparasitic agents, but excluding coal tar solution and H1-antagonist antihistamines, and from the group consisting of the CPNS agents selected from the group of compounds acting on the central or peripheral nervous system, but excluding coal tar solution and H1-antagonist antihistamines and also excluding anti-inflammatory, analgesic and antipyretic agents and also provides an enhanced method for the administration of a nucleic acid substance to the cells of an animal, a plant or a micro-organism.Type: ApplicationFiled: January 16, 2003Publication date: November 29, 2012Inventor: Petrus Johannes Meyer
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Patent number: 8318770Abstract: Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4 and R5 are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.Type: GrantFiled: December 1, 2010Date of Patent: November 27, 2012Assignee: Roche Palo Alto LLCInventor: Ryan Craig Schoenfeld
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Publication number: 20120295889Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: May 16, 2012Publication date: November 22, 2012Applicant: Merck Serono S.A.Inventors: Ulrich Abel, Holger Deppe, Achim Feurer, Ulrich Grädler, Kerstin Otte, Renate Sekul, Meinolf Thiemann, Andreas Goutopoulos, Matthias Schwarz, Xuliang Jiang
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Publication number: 20120289545Abstract: The present invention relates to maleate salt forms of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, methods of preparing crystalline maleate salt forms, the associated compounds, and pharmaceutical compositions containing the same. The maleate salts are useful in treating cancers, particularly those affected by kinases of the epidermal growth factor receptor family.Type: ApplicationFiled: April 6, 2012Publication date: November 15, 2012Inventors: Qinghong Lu, Mannching Sherry Ku, Warren Chew, Gloria Cheal, Anthony F. Hadfield, Mahmoud Mirmehrabi
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Patent number: 8309129Abstract: A pharmaceutical composition comprises nanoparticles comprising a poorly water-soluble drug, ethylcellulose, and a bile salt.Type: GrantFiled: April 21, 2008Date of Patent: November 13, 2012Assignee: Bend Research, Inc.Inventors: Warren Kenyon Miller, Michael Mark Morgen, Daniel Tod Smithey
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Publication number: 20120283256Abstract: The present invention relates to compounds having the following Formula (I) for use in the prevention and/or the treatment of diseases involving formation of amyloid plaques and/or where a dysfunction of the APP metabolism occurs.Type: ApplicationFiled: December 16, 2010Publication date: November 8, 2012Inventors: Andre Delacourte, Patricia Melnyk, Stephane Burlet, Nicolas Lefur
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Publication number: 20120283260Abstract: The invention provides compositions and methods for treating and/or preventing ocular disorders associated with increased intraocular pressure. In particular, the compounds are bradykinin agonists.Type: ApplicationFiled: July 24, 2012Publication date: November 8, 2012Applicants: ASTELLAS PHARMA INC., ALCON RESEARCH, LTD.Inventors: Keith D. Combrink, Suchismita Mohapatra, Mark R. Hellberg, Najam A. Sharif, Ganesh Prasanna, Iok-Hou Pang, Bryon Severns, Hwang-Hsing Chen, Abdelmoula Namil
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Publication number: 20120283265Abstract: The present invention relates to compound Formula (I) wherein: Formula (II) means a pyridazine, a pyrimidine or a pyrazine group, R independently represent a hydrogen atom, a halogen atom or a group chosen among a CN group, a hydroxyl group, a COOR1 group, a (C1-C3)fluoroalkyl group, a (C1-C3)fluoroalkoxy group, a NO2 group, a NR1R2 group, a (C1-C4)alkoxy group, a phenoxy group and a (C1-C3)alkyl group, said alkyl being optionally mono-substituted by a hydroxyl group, n is 1, 2 or 3, n is 1 or 2, R is a hydrogen atom, a halogen atom or a group chosen among a (C1-C3)alkyl group, a hydroxyl group, a COOR1 group, a NO2 group, a NR1R2 group, a morpholinyl or a morpholino group, a N-methylpiperazinyl group, a (C1-C3)fluoroalkyl group, a (C1-C4)alkoxy group and a CN group, Z is N or C, Y is N or C, X is N or C, W is N or C, T is N or C, U is N or C, for use as an agent for preventing, inhibiting or treating AIDS. Some of said compounds are new and also form part of the invention.Type: ApplicationFiled: June 14, 2010Publication date: November 8, 2012Applicants: SOCIETE SPLICOS, UNIVERSITE DE MONTPELLIER 2, INSTITUT CURIE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Jamal Tazi, Florence Mahuteau, Romain Najman, Didier Scherrer, Noelie Campos, Aude Garcel
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Publication number: 20120283620Abstract: Hydrophobic weak base compounds such as hydrophobic weak base chemotherapeutic agents (which are not an anthracycline) for use in the treatment of medical conditions such as proliferative disease or disorder in a subject, in combination with illumination of a region in a body of the subject which is characterized by the presence of proliferating cells, are disclosed. The hydrophobic weak base compound and a wavelength of illumination are selected such that the hydrophobic weak base compound acts as a therapeutically effective photosensitizer when exposed to the illumination.Type: ApplicationFiled: March 8, 2012Publication date: November 8, 2012Inventors: Yehuda G. ASSARAF, Yamit Adar Turgeman, Andrzej M. Skladanowski, Arjan W. Griffioen, Henk Verheul, Kristy Gotink, Hubert Van Den Bergh, Patrycja Nowak-Sliwinska
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Publication number: 20120277230Abstract: The present invention relates to compound (I) wherein: means a pyridazine, a pyrimidine or a pyrazine group, R independently represent a hydrogen atom, a halogen atom or a group chosen among a CN group, a hydroxyl group, a COOR1 group, a (C1-C3)fluoroalkyl group, a (C1-C3)fluoroalkoxy group, a NO2 group, a NR1R2 group, a (C1-C4)alkoxy group, a phenoxy group and a (C1-C3)alkyl group, said alkyl being optionally mono-substituted by a hydroxyl group, n is 1, 2 or 3, n is 1 or 2, R is a hydrogen atom, a halogen atom or a group chosen among a (C1-C3)alkyl group, a hydroxyl group, a COOR1 group, a NO2 group, a NR1R2 group, a morpholinyl or a morpholino group, a N-methylpiperazinyl group, a (C1-C3)fluoroalkyl group, a (C1-C4)alkoxy group and a CN group, Z is N or C, Y is N or C, X is N or C, W is N or C, T is N or C, U is N or C, for use as an agent for preventing, inhibiting or treating cancer. Some of said compounds are new and also form part of the invention.Type: ApplicationFiled: June 14, 2010Publication date: November 1, 2012Applicants: SOCIETE SPLICOS, UNIVERSITE MONTPELLIER 2, INSTITUT CURIE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Pierre Roux, Florence Mahuteau, Romain Najman, Jamal Tazi, Gilles Gadea, Didier Scherrer, Carsten Brock, Nathalie Cahuzac
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Patent number: 8299094Abstract: Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R?, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.Type: GrantFiled: December 13, 2010Date of Patent: October 30, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Xiangdong Alan Wang, Li-Qiang Sun, Sing-Yuen Sit, Ny Sin, Paul Michael Scola, Yan Chen
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Publication number: 20120269810Abstract: Methods and compositions that down regulate the activity of orexins to treat panic disorder and panic-like responses associated with hypercapnic conditions are disclosed.Type: ApplicationFiled: October 21, 2010Publication date: October 25, 2012Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATIONInventors: Anantha Shekhar, Philip L. Johnson
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Patent number: 8293764Abstract: Contemplated compounds disrupt interaction between BRCA2 and RAD51, likely by binding to RAD51. Based on the crucial role of the BRCA2-RAD51 complex formation in DNA repair and the role of RAD51 in the control of entry into S-phase from G1, numerous compositions and methods are presented. Among other advantageous uses, contemplated compounds may be employed as protective agents for non-neoplastic cells in chemotherapy before exposure of the cells to a chemotherapeutic drug, and/or as DNA-damage sensitizer for neoplastic cells.Type: GrantFiled: October 19, 2005Date of Patent: October 23, 2012Assignee: The Regents of the University of CaliforniaInventors: Wen-Hwa Lee, Phang-Lang Chen, Jiewen Zhu
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Publication number: 20120264708Abstract: Provided is a method of treating or preventing age-related macular degeneration (AMD) in a patient subject to, or symptomatic of the disease, wherein the method comprises restoring normal lysosomal pH (pHL), or acidifying an abnormally elevated pHL, thus decreasing or preventing a damaging accumulation of lipofuscin or waste products in the retinal pigment epithelium (RPE) cells of the eye of the patient. Further, this method is achieved by modulating the action of the P2X7 and/or P2Y12 receptors of the RPE cells, specifically decreasing the acidity (pHL) of the RPE lysosomes by administering selected receptor antagonists affecting the action of the P2X7 and/or P2Y12 receptors of the RPE. Methods for selecting and quantifying the effectiveness of drugs to restore pHL and determine outer segment clearance rates is also provided using a high through-put screening protocol.Type: ApplicationFiled: April 27, 2012Publication date: October 18, 2012Inventors: Claire Mitchell, Alan Laties
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Publication number: 20120264704Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.Type: ApplicationFiled: October 26, 2007Publication date: October 18, 2012Inventors: Kai Thede, Ingo Flamme, Felix Oehme, Jens-Kerim Ergüden, Friederike Stoll, Joachim Schuhmacher, Hanno Wild, Peter Kolkhof, Hartmut Beck, Metin Akbaba, Mario Jeske
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Publication number: 20120263736Abstract: The invention provides methods for predicting the likelihood that a subject will develop a sterile inflammation or will have an increased propensity to later develop a sterile inflammation, for determining whether a subject with tissue damage should be administered an antimicrobial agent (at full or a reduced dosage) or an anti-inflammatory agent, and for treating a subject with tissue damage. In the methods, an increased ratio of the amount of mitochondrial nucleic acid or peptide to the amount of microbial nucleic acid or peptide indicates a subject that has an increased likelihood of developing a sterile inflammation or an increased propensity to later develop a sterile inflammation, or a subject that should not be administered, or that should be administered at a reduced dosage, an antimicrobial agent or one or more anti-inflammatory agents and not an antimicrobial agent. Kits for detecting mitochondrial and/or microbial nucleic acids or peptides are provided.Type: ApplicationFiled: December 3, 2010Publication date: October 18, 2012Applicant: Beth Israel Deaconess Medical Center, Inc.Inventor: Carl J. Hauser
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Patent number: 8288410Abstract: The present invention relates to quinolinium antiinfective agents in which the qunolinium nucleus is fused to an indole ring or the qunolinium nucleus is linked to a cyclic structure through an opened indole or a benzothiophene or benzofuran ring. The compound is further substituted with various substituent groups. The compounds are represented by formula (I), (II) and (III): Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: July 8, 2008Date of Patent: October 16, 2012Assignee: Florida Agricultural and Mechanical UniversityInventor: Seth Y. Ablordeppey
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Publication number: 20120252839Abstract: Compounds are described that are useful for treating an apoptosis-associated disease, which are specifically cytotoxic to tumor cells that are overexpressing Bcl-xL, and are much less cytotoxic in isogenic cells that are not overexpressing Bcl-xL. Also described is a method for treating an apoptosis-associated disease in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of an active compound that is specifically cytotoxic to tumor cells that are overexpressing Bcl-xL, and are much less cytotoxic in isogenic cells that are not overexpressing Bcl-xL. Several scaffolds of active compounds are described.Type: ApplicationFiled: April 2, 2012Publication date: October 4, 2012Applicant: FRED HUTCHINSON CANCER RESEARCH CENTERInventors: David HOCKENBERY, Julian SIMON
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Publication number: 20120245147Abstract: Methods for screening for inhibitors of endoplasmic reticulum (ER) stress are provided. These methods involve the addition of thapsigargin, which induces ER stress, and a test agent to mammalian cells in multi-well plates. Cell survival can be readily monitored by measuring intracellular ATP content using a bioluminescent reagent. Screening a commercially available library of 50,000 compounds led to the identification of 93 hit compounds that were subjected to secondary assays to confirm their ability to rescue cells from thapsigargin-induced cell death.Type: ApplicationFiled: April 19, 2012Publication date: September 27, 2012Inventors: John C. REED, In-Ki Kim
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Patent number: 8268865Abstract: Disclosed are compounds having at least one quaternary alkyl ammonium functionality. The compounds inhibit bacterial efflux pump inhibitors and are used in combination with an anti-bacterial agent to treat or prevent bacterial infections. These combinations can be effective against bacterial infections that have developed resistance to anti-bacterial agents through an efflux pump mechanism.Type: GrantFiled: May 6, 2008Date of Patent: September 18, 2012Assignee: Rempex Pharmaceuticals, Inc.Inventors: Tomasz Glinka, Olga Lomovskaya, Keith Bostian, David M. Wallace
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Publication number: 20120232110Abstract: This disclosure relates to compositions including certain compounds identified by a quantitative, high throughput assay to be effective in inhibiting the ability of a bacterium to kill a host organism, as well as methods for using these compounds for treating bacterial infections.Type: ApplicationFiled: June 25, 2010Publication date: September 13, 2012Applicants: NORTHEASTERN UNIVERSITY, THE GENERAL HOSPITAL CORPORATIONInventors: Terence Moy, Annie Conery, Kim Lewis, Frederick M. Ausubel, Read Pukkila-Worley
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Publication number: 20120225872Abstract: A method of preparing a compound of formula (I), A method for treating cancer or inhibiting growth of cancer cells including administering to a patient mammal in need thereof a pharmaceutical preparation including the compound. A method of treating or preventing a physiological disorder caused by abnormal protein tyrosine kinase activity in a mammal including administering to a mammal a pharmaceutical preparation including the compound.Type: ApplicationFiled: May 11, 2012Publication date: September 6, 2012Inventor: Hesheng ZHANG
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Publication number: 20120225862Abstract: Provided are certain heteroaryl benzamides, compositions, and methods of their manufacture and use.Type: ApplicationFiled: July 21, 2010Publication date: September 6, 2012Applicants: AUCKLAND UNIVSERVICES LIMITED, THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITYInventors: Patrick D. Sutphin, Denise A. Chan, Sandra Turcotte, William Alexander Denny, Michael Patrick Hay, Anna Claire Giddens, Muriel Marie Bonnet, Amato J. Giaccia
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Publication number: 20120225875Abstract: Novel hetarylaminoquinoline derivatives of formula (I) wherein X, Z, Het, R1, R2, R3 and R4 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.Type: ApplicationFiled: October 12, 2010Publication date: September 6, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Alfred Jonczyk, Christiane Amendt, Frank Zenke
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Publication number: 20120225874Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutical composition thereof, with all the variables being defined in the text. The present invention further relates to the use of the compounds herein for treatment of or delay progression to overt to diseases in which CETP is involved.Type: ApplicationFiled: May 17, 2012Publication date: September 6, 2012Applicant: NOVARTIS AGInventors: Masashi KISHIDA, Naoko MATSUURA, Hidetomo IMASE, Yuki IWAKI, Ichiro UMEMURA, Osamu OHMORI, Eiji KAWAHARA
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Publication number: 20120225931Abstract: The present invention relates, inter alia, to methods and compositions for regulating the host response to biomaterials, including inhibiting inflammation from and rejection of biomaterials using salicylate compounds and/or TLR7/TLR9 antagonists as described herein.Type: ApplicationFiled: September 28, 2010Publication date: September 6, 2012Applicant: Yale UniversityInventors: Wajahat Z. Mehal, Themis Kyriakides
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Patent number: 8258145Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs, and in particular to the use of these compounds in treating brain cancer.Type: GrantFiled: July 3, 2007Date of Patent: September 4, 2012Assignee: Myrexis, Inc.Inventors: Sui Xiong Cai, Mark B. Anderson, Adam Willardsen, Nilantha Sudath Sirisoma
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Publication number: 20120220627Abstract: The invention relates to substituted 2-amino-quinoline-3-carboxamides, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: ApplicationFiled: August 26, 2011Publication date: August 30, 2012Applicant: Grunenthal GmbHInventors: Sven KÜHNERT, Gregor BAHRENBERG, Dagmar KAULARTZ, Achim KLESS, Wolfgang SCHRÖDER
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Publication number: 20120214803Abstract: The present invention relates to novel hepcidin antagonists, pharmaceutical compositions comprising them and the use thereof as medicaments for the use in the treatment of iron metabolism disorders, such as, in particular, iron deficiency diseases and anemias, in particular anemias in connection with chronic inflammatory diseases.Type: ApplicationFiled: February 2, 2012Publication date: August 23, 2012Applicant: VIFOR (INTERNATIONAL) AGInventors: Wilm Buhr, Susanna Burckhardt, Franz Dürrenberger, Felix Funk, Peter O. Geisser, Vincent A. Corden, Stephen M. Courtney, Graham Dawson, Tara Davenport, Mark Slack, Mark P. Ridgill, Chrostopher J. Yarnold, Susan Boyce, Albertus A. Ellenbroek
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Publication number: 20120208814Abstract: Tetrahydroquinoline compounds of formula (I) or a salt thereof, pharmaceutical compositions containing such compounds and their use in therapy, in particular in the treatment of diseases or conditions for which a bromodomain inhibitor is indicted.Type: ApplicationFiled: November 3, 2010Publication date: August 16, 2012Inventors: Emmanuel Hubert Demont, Romain Luc Marie Gosmini
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Publication number: 20120208800Abstract: The use of compounds in the treatment of autoimmune and inflammatory diseases or conditions, pharmaceutical compositions containing such compounds and to methods for identifying compounds for use in the treatment of such diseases or conditions.Type: ApplicationFiled: November 3, 2010Publication date: August 16, 2012Inventors: Chun-Wa Chung, Edwige Nicodeme
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Publication number: 20120208840Abstract: The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity, wherein these compounds selected from the group consisting of wherein A, B, C, D, X, Y, Z and R3 are defined in the specification. Said compounds are useful for treating a disease or condition of a mammal selected from the group consisting of ocular diseases; systemic vascular barrier related diseases; allergies and other inflammatory diseases; cardiac diseases or conditions; fibrosis; pain and wounds.Type: ApplicationFiled: September 28, 2010Publication date: August 16, 2012Applicant: ALLERGAN, INC.Inventors: Wenkiu K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha-Bin Im
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Publication number: 20120208798Abstract: Tetrahydroquinoline compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.Type: ApplicationFiled: November 3, 2010Publication date: August 16, 2012Inventors: Emmanuel Hubert Demont, Neil Stuart Garton, Romain Luc Marie Gosmini, Thomas George Christopher Hayhow, Jonathan Seal, David Matthew Wilson, Michael David Woodrow
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Publication number: 20120202849Abstract: Disclosed herein is a novel synergistic pharmaceutical composition comprising hydroxychloroquine with insulin sensitizing agents and lipid lowering agents such as statins along with pharmaceutical excipients/carriers useful in treating Non-Alcoholic Fatty Liver Disease.Type: ApplicationFiled: October 12, 2010Publication date: August 9, 2012Inventor: Anil Pareek
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Publication number: 20120202817Abstract: A compound having the following formula [I] or a pharmaceutically acceptable salt thereof: wherein A is an aromatic five-membered heterocycle which optionally is fused with a cycloalkane ring; B is an alkylene; R1 and R2 are hydrogen, hydroxyl, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, heterocycle, amino, alkylamino, arylamino or acyl, or R1 and R2 join together to form a heterocycle; X and Y are hydrogen, halogen, hydroxyl, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, mercapto, alkylthio, arylthio, carboxyl, an ester of carboxyl, an amide of carboxyl, cyano or nitro; p is 0, 1 or 2; and q is 0 or 1. The compound is useful for treating diseases in which angiogenesis or augmentation of vascular permeability is involved.Type: ApplicationFiled: April 18, 2012Publication date: August 9, 2012Applicant: SANTEN PHARMACEUTICAL CO., LTD.Inventors: Takahiro Honda, Hisashi Tajima, Yoshimasa Sasabuchi, Kenji Kawashima, Kazuyoshi Okamoto, Minoru Yamamoto, Masakazu Ban
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Patent number: 8236328Abstract: A pharmaceutical composition comprises a dispersion comprising a low-solubility drug and a matrix combined with a concentration-enhancing polymer. At least a major portion of the drug is amorphous in the dispersion. The compositions improve the stability of the drug in the dispersion, and/or the concentration of drug in a use environment.Type: GrantFiled: July 8, 2008Date of Patent: August 7, 2012Assignee: Bend Research, Inc.Inventors: Walter C. Babcock, William J. Curatolo, Dwayne T. Friesen, Rodney J. Ketner, Julian B. Lo, James A. S. Nightingale, Ravi M. Shanker, James B. West
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Publication number: 20120196882Abstract: The invention provides methods and compounds for the treatment and prevention of malaria infection and transmission in a mammal by administering compounds of the invention to a mammal having or suspected of having a malaria infection. The invention also provides pharmaceutical compositions that can kill or arrest the growth of Plasmodium organisms, and especially Plasmodium falciparum, thereby preventing or blocking transmission of malaria as well as treating malaria infection.Type: ApplicationFiled: August 27, 2010Publication date: August 2, 2012Inventors: Dipak Raj, Sittiporn Pattaradilokrat, Ron Johnson, Ruili Huang
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Publication number: 20120196894Abstract: The present invention relates to compositions and methods that modulate at least one TRP family member. Specifically, the present invention relates to novel TRPA1 antagonists and their use in the treatment of pain such as chronic inflammatory and neuropathic pain. Compounds that can modulate one or more TRPA1 functions are useful in many aspects including, but not limited to, maintaining calcium homeostasis; maintaining sodium homeostasis; modulating intracellular calcium levels; modulating membrane polarization (membrane potential); modulating cation levels; and/or treating or preventing diseases, disorders, or conditions associated with calcium homeostasis, sodium homeostasis, calcium or sodium dyshomeostasis, or membrane polarization/hyperpolarization (including hypo and hyperexcitability), and/or treating or preventing diseases, disorders, or conditions associated with regulation or misregulation of TRPA1 expression or function.Type: ApplicationFiled: September 28, 2010Publication date: August 2, 2012Inventors: Mark T. Bilodeau, Melissa Egbertson, Ahren Green, John C. Hartnett, Yiwei Li
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Patent number: 8232403Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutical composition thereof, with all the variables being defined in the text. The present invention further relates to the use of the compounds herein for treatment of or delay progression to overt to diseases in which CETP is involved.Type: GrantFiled: May 8, 2007Date of Patent: July 31, 2012Assignee: Novartis AGInventors: Masashi Kishida, Naoko Matsuura, Hidetomo Imase, Yuki Iwaki, Ichiro Umemura, Osamu Ohmori, Eiji Kawahara
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Publication number: 20120184523Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.Type: ApplicationFiled: March 22, 2012Publication date: July 19, 2012Applicant: Exelixis, Inc.Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takbuchi, Yong Wang, Wei Xu
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Publication number: 20120178733Abstract: The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.Type: ApplicationFiled: August 19, 2011Publication date: July 12, 2012Inventors: Bing-Yan Zhu, Shawn M. Bauer, Zhaozhong J. Jia, Gary D. Probst, Yanchen Zhang, Robert M. Scarborough
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Publication number: 20120172376Abstract: The present invention relates to novel heterocyclic compounds of formula I wherein the variables are as defined in the claims or the description, which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), compositions containing the compounds, their use for preparing a medicament for the treatment of a medical disorder susceptible to the treatment with a compound that modulates, preferably inhibits, the activity of glycogen synthase kinase 3?, and methods of treatment of medical disorders susceptible to treatment with a compound that modulates glycogen synthase kinase 3? activity using the compounds.Type: ApplicationFiled: December 29, 2011Publication date: July 5, 2012Applicant: Abbott GmbH & Co. KGInventors: Sean Colm Turner, Helmut Mack, Margaretha Henrica Maria Bakker, Marcel van Gaalen, Carolin Hoft, Wilfried Hornberger
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Publication number: 20120165365Abstract: The present invention embraces bis-acridine and bis-quinoline intercalators having a bis(4-aminophenyl)ether tether, and diglycolate salts thereof, for selectively decreasing colon cancer and glial cell proliferation and preventing or treating colon cancers and gliomas.Type: ApplicationFiled: July 13, 2010Publication date: June 28, 2012Applicant: Trustees of Dartmouth CollegeInventors: Gordon W. Gribble, Dmitry A. Androsov
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Publication number: 20120165369Abstract: The present invention relates to quinolinium antiinfective agents in which the qunolinium nucleus is fused to an indole ring or the qunolinium nucleus is linked to a cyclic structure through an opened indole or a benzothiophene or benzofuran ring. The compound is further substituted with various substituent groups. The compounds are represented by formula (I), (II) and (III): Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: July 8, 2008Publication date: June 28, 2012Inventor: Seth Y. Ablordeppey