Chalcogen Bonded Directly To Ring Carbon Of The Thiazole Ring Patents (Class 514/369)
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Patent number: 8372807Abstract: Described herein are compounds useful in the reduction of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, a compound disclosed herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: GrantFiled: May 20, 2010Date of Patent: February 12, 2013Assignee: Ardea Biosciences, Inc.Inventors: Martha De La Rosa, Jean-Luc Girardet, Karen Watson
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Patent number: 8367665Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification.Type: GrantFiled: April 16, 2009Date of Patent: February 5, 2013Assignee: Karo Bio ABInventors: Patrik Rhönnstad, Elisabet Kallin, Theresa Apelqvist, Mattias Wennerstål, Aiping Cheng
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Publication number: 20130028966Abstract: The invention provides compounds represented by the formulae: (I) and (II) where the compounds are useful in treating, for example, viral and/or parasitic infections. Also provided are pharmaceutical compositions comprising the compounds and methods of treatment using the compounds.Type: ApplicationFiled: April 13, 2011Publication date: January 31, 2013Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Benhur Lee, Michael E. Jung, Jihye Lee, Frederic Vigant, Peter J. Bradley, Michael C. Wolf, Bettina E. Hajagos
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Patent number: 8362049Abstract: This application relates to novel urea glucokinase activators and use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes. Further encompassed is a pharmaceutical composition comprising a compound according to the invention and a process for preparing such.Type: GrantFiled: March 8, 2012Date of Patent: January 29, 2013Assignee: Novo Nordisk A/SInventors: Anthony Murray, Jesper Lau, Per Vedsoe, Lise Brown Christiansen
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Publication number: 20130023529Abstract: Embodiments of the invention include methods and compositions involving aldose reductase inhibitors for the treatment of inflammation, including uveitis and asthma.Type: ApplicationFiled: July 11, 2012Publication date: January 24, 2013Applicant: The Board of Regents of the University of Texas SystemInventors: Satish K. Srivastava, Kota V. Ramana
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Publication number: 20130022610Abstract: Methods for treating abnormal glycosylated hemoglobin (HbA1c) levels in a patient in need thereof, wherein the provided methods comprise administering to a patient in need a therapeutically effective amount of an Interleukin-1? modulator. Also, the invention provides compositions comprising at least one lipid modifying agent and an IL-1? modulator.Type: ApplicationFiled: July 19, 2012Publication date: January 24, 2013Inventors: Mannching Sherry Ku, Chih-Kuang Chen, Wei-Shu Lu, Chih-Ming Chen, I-Yin Lin
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Patent number: 8357709Abstract: The present invention is directed to 2,4-disubstituted pyrrolidine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. 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 orexin receptors are involved.Type: GrantFiled: October 15, 2009Date of Patent: January 22, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Paul J. Coleman, Christopher D. Cox, John D. Schreier
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Publication number: 20130019348Abstract: This document discloses molecules having the following formula (“Formula One”) The molecules disclosed in this document are related to the field of processes to produce molecules that are useful as pesticides (e.g., acaricides, insecticides, molluscicides, and nematicides), such molecules, and processes of using such molecules to control pests.Type: ApplicationFiled: July 11, 2012Publication date: January 17, 2013Applicant: DOW AGROSCIENCES LLCInventors: Gary D. Crouse, David A. Demeter, Thomas C. Sparks, Nick X. Wang, William H. Dent, III, Carl Deamicis, Noormohamed M. Niyaz, Erich W. Baum, Lindsey G. Fischer, Natalie C. Giampietro
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Patent number: 8354440Abstract: Compositions and methods for inhibiting translation using 3-(5-tert-Butyl-2-Hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using 3-(5-tert-butyl-2-hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are described.Type: GrantFiled: September 15, 2011Date of Patent: January 15, 2013Assignee: President and Fellows of Harvard CollegeInventors: José A. Halperin, Amarnath Natarajan, Bertal Huseyin Aktas, Yun-Hua Fan, Han Chen
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Publication number: 20130005767Abstract: Disclosed herein are compounds of the formula or salts or bioisosteres thereof. Therapeutic methods, medicaments, and compositions related thereto are also disclosed.Type: ApplicationFiled: September 14, 2012Publication date: January 3, 2013Applicant: Allergan, Inc.Inventors: David W. Old, Vinh X. Ngo
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Publication number: 20130005715Abstract: The present invention provides an animal repellent comprising, as an active ingredient, a compound having an odor innately inducing fear in animals, which is free from acclimation of animals to the aforementioned odor. The present invention relates to animal repellent comprising, as an active ingredient, at least one kind selected from a heterocyclic compound represented by the formula (I): wherein ring A is a 3- to 7-membered heterocycle containing at least one hetero atom selected from a nitrogen atom, a sulfur atom and an oxygen atom, and R1 and R2 are each independently hydrogen, a halogen atom, an optionally substituted alkyl group, an optionally substituted alkoxy group, an acyl group, an optionally esterified carboxyl group, an optionally substituted thiol group, an optionally substituted amino group or an oxo group, or a salt thereof, a chain sulfide compound and alkyl isothiocyanate.Type: ApplicationFiled: February 8, 2011Publication date: January 3, 2013Applicants: Scent Science International Inc,., OSAKA BIOSCIENCE INSTITUTEInventors: Ko Kobayakawa, Reiko Kobayakawa
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Publication number: 20130005718Abstract: Compositions and methods for managing or treating chronic pain are provided. More particularly, methods are provided for managing or treating chronic pain by administering to a patient in need thereof an effective amount of propofol or a propofol derivative having limited anesthetic properties. Methods of modulating HCN channel gating are also provided. Pharmaceutically acceptable compositions for, e.g., modulating HCN channel gating are further provided.Type: ApplicationFiled: August 10, 2010Publication date: January 3, 2013Inventors: Gareth R. Tibbs, Pamela Flood, Peter Goldstein
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Patent number: 8344009Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: GrantFiled: October 7, 2010Date of Patent: January 1, 2013Assignee: Janssen Pharmaceutica, NVInventors: Michael Gaul, Alexander Kim, Lily Lee Searle, Raymond Patch, Dionisois Rentzeperis, Guozhang Xu, Xizhen Zhu
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Patent number: 8338466Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: GrantFiled: January 18, 2010Date of Patent: December 25, 2012Assignee: Abbott LaboratoriesInventors: Aaron R. Kunzer, Steven W. Elmore, Laura A. Hexamer, Cheol-Min Park, Andrew J. Souers, Gerard M. Sullivan, Gary T. Wang, Xilu Wang, Michael D. Wendt
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Patent number: 8338465Abstract: Disclosed are methods for the prevention or treatment of tuberculosis in a subject infected with Mycobacterium tuberculosis by administering rhodanine derivatives of formula (I), as well as some novel such compounds. Other embodiments are also disclosed.Type: GrantFiled: June 8, 2007Date of Patent: December 25, 2012Assignee: Cornell Research Foundation, Inc.Inventors: Jasbir Singh, Carl F. Nathan, Ruslana Bryk, Raghu Samy, Krzysztof Pupek, Mark Gurney
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Publication number: 20120322728Abstract: The present invention relates to thiazolidinedione analogues and pharmaceutical compositions that are useful for treating and/or preventing diabetes mellitis, optionally in combination with a second treatment. Furthermore, the present invention also provides methods of inducing remission of the symptoms of diabetes mellitis in a patient comprising administering a thiazolidinedione analogue and a GLP-1 agonist.Type: ApplicationFiled: December 15, 2010Publication date: December 20, 2012Applicant: Metabolic Solutions Development Company, LLCInventors: Gerard R. Colca, Rolf F. Kletzien, Steven P. Tanis, Scott D. Larsen
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Publication number: 20120316138Abstract: The present invention relates to thiazolidinedione analogues and pharmaceutical compositions that are useful for treating and/or preventing obesity or diabetes, optionally in combination with a second treatment therapy such a diet restriction or an increase in duration or exertion in physical activity.Type: ApplicationFiled: December 15, 2010Publication date: December 13, 2012Applicant: METABOLIC SOLUTIONS DEVELOPMENT COMPANY, LLCInventors: Gerard R. Colca, Rolf F. Kletzien, Steven P. Tanis, Scott D. Larsen
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Publication number: 20120315303Abstract: Methods and intravascular treatment devices for treating atherosclerosis are provided.Type: ApplicationFiled: May 4, 2012Publication date: December 13, 2012Applicant: Medtronic Vascular, Inc.Inventors: AYALA HEZI-YAMIT, SUSAN EDWARDS, CAROL SULLIVAN, OLUWASHOLA SHAKIRAT SULAIMON, LORI GARCIA, STEFAN TUNEV
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Patent number: 8329647Abstract: The invention provides compositions and methods for determining insulin resistance and/or pancreatic ?-cell dysfunction in a subject. The invention also provides compositions and methods for treating a subject according to the insulin resistance and/or pancreatic ?-cell dysfunction in the subject.Type: GrantFiled: July 17, 2009Date of Patent: December 11, 2012Assignee: IKFE Institut fur Klinische Forschung und Entwicklung GmbHInventors: Andreas Pfuetzner, Thomas Forst
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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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Patent number: 8324237Abstract: The invention includes processes mainly for the treatment of a inflammatory diseases, such as inflammatory bowel disease, arthritis, atherosclerosis, asthma, allergy, inflammatory kidney disease, circulatory shock, multiple sclerosis, chronic obstructive pulmonary disease, skin inflammation, periodontal disease, psoriasis and T cell-mediated diseases of immunity, including allergic encephalomyelitis, allergic neuritis, transplant allograft rejection, graft versus host disease, myocarditis, thyroiditis, nephritis, systemic lupus erthematosus, and insulin-dependent diabetes mellitus. The processes involve treating a patient with a pharmaceutical composition containing an active ingredient that inhibits the activity of sphingosine kinase.Type: GrantFiled: May 19, 2006Date of Patent: December 4, 2012Inventors: Charles D. Smith, Kevin J. French, Lynn W. Maines
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Publication number: 20120302612Abstract: The invention relates to pharmaceutical compositions containing at least one thiazolidin-4-one derivative to prevent or treat disorders associated with an activated immune system. Furthermore, the invention relates to novel thiazolidin-4-one derivatives notably for use as pharmaceutically active compounds. Said compounds particularly act also as immunosuppressive agents.Type: ApplicationFiled: August 9, 2012Publication date: November 29, 2012Inventors: Christoph BINKERT, Martin BOLLI, Boris MATHYS, Claus MUELLER, Michael SCHERZ, Oliver NAYLER
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Publication number: 20120302581Abstract: The instant disclosure relates to compositions that may be useful as therapeutic agents for the treatment of disorders associated or caused by Ras deregulation or dysregulation, for example, disorders associated with alterations in the NF1 gene such as neurofibromatosis type I, fungal infections such as those caused by Candida albicans, and proliferative disorders such as glioblastoma.Type: ApplicationFiled: August 12, 2011Publication date: November 29, 2012Inventors: Nancy Ratner, Yolanda Sanchez, Gunnar Johansson, William Seibel
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Patent number: 8318778Abstract: This application relates to novel urea glucokinase activators and use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes. Further encompassed is a pharmaceutical composition comprising a compound according to the invention and a process for preparing such.Type: GrantFiled: January 8, 2008Date of Patent: November 27, 2012Assignee: Novo Nordisk A/SInventors: Anthony Murray, Jesper Lau, Per Vedsø, Lise Brown Christiansen
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Publication number: 20120294936Abstract: The present invention relates to metformin extended release (XR) formulations with improved compactability to provide reduced mass tablets, granulations, and capsules.Type: ApplicationFiled: November 12, 2010Publication date: November 22, 2012Applicants: ASTRAZENECA UK LIMITED, BRISTOL-MYERS SQUIBB COMPANYInventors: Admassu Abebe, Kyle Martin, Jatin M. Patel, Peter Timmins
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Publication number: 20120295950Abstract: Methods for screening molecules that modulate the activity of Retinol Binding Protein 4 (RBP4) and their use in treatment of insulin resistance are described. Also described are methods of diagnosing insulin resistance and related conditions by detecting modulation of RBP4 activity.Type: ApplicationFiled: May 22, 2012Publication date: November 22, 2012Applicant: Beth Israel Deaconess Medical Center, Inc.Inventors: Barbara B. Kahn, Qin Yang, Tim Graham, Odile Peroni
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Publication number: 20120295920Abstract: HIV inhibitors of formula wherein R1 is halo, C1-4alkoxy, trifluoromethoxy; n is 0 or 1; A is CH or N; R5 and R6 are hydrogen, C1-4alkyl, halo; R7 and R8 are C1-4alkyl or C1-4alkoxyC1-4alkyl; R9 is C1-4alkyl, cyclopropyl, trifluoromethyl, C1-4alkoxy, or dimethylamino; R10 is hydrogen, C1-4alkyl, cyclopropyl, trifluoromethyl, C1-4alkoxy, or dimethylamino; pharmaceutically acceptable addition salts and solvates thereof; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds.Type: ApplicationFiled: December 10, 2010Publication date: November 22, 2012Inventors: Genadiy Kalayanov, Bart Rudolf Romanie Kesteleyn, Kevin Parkes, Bengt Bertil Samuelsson, Wim Bert Griet Schepens, Johannes Wilhelmus J. Thuring, Hans Kristian Wallberg, Jörg Kurt Wegner
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Publication number: 20120289557Abstract: The present invention provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to stimulate the synthesis of proteins sufficient to consolidate long-term memory. The present invention also provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to downregulate PKC.Type: ApplicationFiled: July 30, 2012Publication date: November 15, 2012Inventor: Daniel L. Alkon
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Patent number: 8309543Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: May 23, 2012Date of Patent: November 13, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jesus E. Gonzalez, III, Andreas P. Termin, Esther Martinborough, Nicole Hilgraf
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Patent number: 8309610Abstract: This invention relates to solid crystalline forms of (1RS,3RS,6RS)-6-Dimethylaminomethyl-1-(3-methoxy-phenyl)cyclohexane-1,3-diol hydrochloride (1), methods of producing 1, methods of use of 1, use of 1 as analgesics and pharmaceutical compositions comprising 1.Type: GrantFiled: February 21, 2006Date of Patent: November 13, 2012Assignee: Gruenenthal GmbHInventors: Michael Gruss, Helmut Buschmann, Andreas Fischer, Wolfgang Hell, Dagmar Lischke
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Patent number: 8304441Abstract: The present invention relates to thiazolidinedione analogues that are useful for treating hypertension, diabetes, and inflammatory diseases.Type: GrantFiled: November 16, 2011Date of Patent: November 6, 2012Assignee: Metabolic Solutions Development Company, LLCInventors: Gerard R. Colca, Robert C. Gadwood, Tim Parker
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Publication number: 20120270899Abstract: The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a cardiovascular disease in an individual using such pharmaceutical compositions.Type: ApplicationFiled: February 3, 2012Publication date: October 25, 2012Inventors: Robin Mark Bannister, John Brew, Suzanne Jane Dilly, Gregory Alan Stoloff, Wilson Caparros-Wanderley
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Publication number: 20120264771Abstract: Provided is a method of inhibiting growth of androgen receptor positive cancer cells. The method entails administering to an individual diagnosed with or suspected of having an androgen receptor positive cancer and administering to the individual a composition containing a compound that can inhibit the growth of the androgen receptor positive cancer.Type: ApplicationFiled: October 25, 2010Publication date: October 18, 2012Applicants: PANACELA LABS, INC., HEALTH RESEARCH INC.Inventors: Katerina Gurova, Natalya Narizhneva
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Publication number: 20120264744Abstract: A series of oxazole and thiazole compounds are shown herein to be small molecule inhibitors of the Wnt pathway that specifically target the activity of the stabilized pool of ?-catenin. Oxazole and thiazole compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, cancer, and others.Type: ApplicationFiled: April 17, 2012Publication date: October 18, 2012Inventors: Ramanuj DASGUPTA, Foster GONSALVES, Susan Katherine LOGAN, Eugine LEE
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Publication number: 20120263792Abstract: Drug tablets that include a prolonged-release core and an immediate-release layer or shell are prepared with a thin barrier layer of drug-free polymer between the prolonged-release and immediate-release portions of the tablet. The barrier layer is penetrable by gastrointestinal fluid, thereby providing lull access of the gastrointestinal fluid to the prolonged-release core, but remains intact during the application of the immediate-release layer, substantially reducing or eliminating any penetration of the immediate-release drug into the prolonged-release portion.Type: ApplicationFiled: June 22, 2012Publication date: October 18, 2012Applicant: DEPOMED, INC.Inventors: JONG LIM, John N. Shell, Jenny Louie-Helm
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Publication number: 20120263716Abstract: The method of treating a person having a cancer selected from carcinoma, sarcoma or hematopoietic cancer by administering (a) an effective amount of at least one anti-cancer drug selected from the group consisting of an epidermal growth factor receptor (EGFR) inhibitor, a vascular endothelial growth factor receptor (VEGFR) inhibitor and a Raf kinase inhibitor and (b) an effective amount of 5-(4-(6-(4-amino-3,5-dimethyl-phenoxy)-1-methyl-1H-benzimidazol-2-ylmethoxy)-benzyl)-thiazolidine-2,4-dione.dihydrochloride provided that said carcinoma is not lung cancer when an EGFR inhibitor is erlotinib. The invention also provides a pharmaceutical composition that may be used in practicing said method.Type: ApplicationFiled: June 19, 2012Publication date: October 18, 2012Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Kosaku FUJIWARA, Naomi Shimazaki
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Publication number: 20120258929Abstract: The present invention provides an agent that modulates physiological condition of pests, wherein the agent has an ability to modulate the activity of an insect peptidyl-dipeptidase A; a method for assaying pesticidal activity of a test substance, which comprises a step of measuring the activity of a peptidyl-dipeptidase A in a reaction system in which the peptidyl-dipeptidase A contacts with a test substance, and the like.Type: ApplicationFiled: June 23, 2006Publication date: October 11, 2012Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Yasutaka Shimokawatoko, Marc Van De Craen, Irene Nooren, Sandra Turconi, Yann Naudet, Guy Nys, Jurgen Debaveye
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Publication number: 20120258991Abstract: A method of treating a cancer selected from the group consisting of breast cancer, pancreatic cancer, kidney cancer, prostate cancer, medulloblastoma, rhabdomyosarcoma, Ewing sarcoma, liposarcoma, multiple myeloma or leukemia. An effective amount of 5-(4-(6-(4-amino-3,5-dimethyl-phenoxy)-1-methyl-1H-benzimidazol-2-ylmethoxy)-benzyl)-thiazolidine-2,4-dione.dihydrochloride is administered to a patient having said cancer.Type: ApplicationFiled: June 18, 2012Publication date: October 11, 2012Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Kosaku FUJIWARA, Naomi SHIMAZAKI
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Publication number: 20120252740Abstract: Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, traumatic brain injury, stroke, malaria, an autoimmune disease, autism, and inflammation, also are disclosed.Type: ApplicationFiled: July 2, 2010Publication date: October 4, 2012Inventors: Alan Kozikowski, Kyle V. Butler, Jay H. Kalin
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Publication number: 20120252854Abstract: A crystalline form of a hydrate of a dihydrochloride 5-(4-{[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1-H-benzimidazol-2-yl]methoxy}benzyl)-1,3-thiazolidine-2,4-dione represented by the following formula: wherein the crystalline form shows main peaks at interplanar spacings of 10.42, 5.85, 5.52, 3.84, 3.46 and 2.95 angstroms in X-ray powder diffraction obtained with Cu K? line radiation (wavelength ?=1.54 angstroms).Type: ApplicationFiled: May 7, 2012Publication date: October 4, 2012Applicant: DAIICHI-SANKYO COMPANY, LIMITEDInventors: Hisaki Kajino, Yutaka Ikeuchi, Hiroshi Miyamoto, Eiji Numagami, Satoru Nihei
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Patent number: 8278268Abstract: Combination therapy comprising PPAR modulators and glucose reabsorption inhibitors useful for the treatment of diabetes and Syndrome X are disclosed.Type: GrantFiled: October 24, 2007Date of Patent: October 2, 2012Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Jacqueline C. Bussolari, Xiaoli Chen, Bruce R. Conway, Keith T. Demarest, Hamish N. M. Ross, Rafael Severino
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Publication number: 20120245166Abstract: Methods for enhancing memory and/or learning and prevent neurodegeneration by administration of certain heterocyclic and aromatic compounds are described. The methods are particularly useful for treating patients suffering from a neurodegenerative disease such as (without limitation) Alzheimer's, Parkinsons's, Lou Gehrig's (ALS) disease or memory or learning impairment. A neuronal human cell-based assay that assess NF-kB gene up-regulation using a luciferase reporter is also provided that screens for compounds useful in methods for enhancing memory or learning.Type: ApplicationFiled: October 14, 2010Publication date: September 27, 2012Applicant: Southern Research InstituteInventors: Maurizio Grimaldi, Judith Varady Hobrath, Subramaniam Ananthan, Joseph A. Maddry
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Patent number: 8273746Abstract: Embodiments of the invention include methods and compositions involving aldose reductase inhibitors for the treatment of inflammation, including uveitis and asthma.Type: GrantFiled: March 24, 2008Date of Patent: September 25, 2012Assignee: The Board of Regents of the University of Texas SystemInventors: Satish K. Srivastava, Kota V. Ramana
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Publication number: 20120238569Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, asthma and COPD.Type: ApplicationFiled: February 17, 2012Publication date: September 20, 2012Inventors: Paul Gillespie, Christophe Michoud, Kenneth Carey Rupert, Kshitij Chhabilbhai Thakkar
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Patent number: 8268816Abstract: The application describes an assay for the identification of small molecule modulators of integrin CD11b/CD18 and small molecules capable of modulating activity of this receptor. For example, one such compound useful as an agonist of integrin CD11b/CD18 is the compound of Formula (I): Such compounds may be used in certain embodiments for treating a disease or condition selected from inflammation, immune-related disorders, cancer, ischemia-reperfusion injury, stroke, neointimal thickening associated with vascular injury, bullous pemphigoid, neonatal obstructive nephropathy, and cardiovascular disease, or in other embodiments for the treatment of a disease or condition selected from immune deficiency, acquired immune deficiency syndrome (AIDS), myeloperoxidase deficiency, Wiskott-Aldrich syndrome, chronic granulomatous disease, hyper-IgM syndromes, leukocyte adhesion deficiency, Chediak-Higashi syndrome, and severe combined immunodeficiency.Type: GrantFiled: June 19, 2009Date of Patent: September 18, 2012Inventors: Vineet Gupta, M. Amin Arnaout
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Publication number: 20120232031Abstract: Described herein are injectable formulations for intra-articular or peri-articular administration, wherein the formulation is administered to treat joint pain. An injectable formulation for intra-articular or peri-articular administration disclosed herein comprises a therapeutically-effective amount of a leukotriene synthesis inhibitor compound formulated for intra-articular or peri-articular administration.Type: ApplicationFiled: October 19, 2010Publication date: September 13, 2012Applicant: Panmira Pharmaceuticals, LLCInventors: John Howard Hutchinson, Petpiboon Peppi Prasit, Isabelle Marguerite Dearmond
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Patent number: 8263631Abstract: Method of treating persons having carcinoma, sarcoma or hematopoietic cancer by administering (i) a compound of the formula (I) and (ii) an epidermal growth factor receptor (EGFR) inhibitor, a vascular endothelial growth factor receptor (VEGFR) inhibitor and pharmaceutical compositions for use in said method. A method for treating gastric cancer, colon cancer, lung cancer, breast cancer, pancreas cancer, kidney cancer, prostate cancer, medulloblastoma, rhabdomyosarcoma, Ewing sarcoma, liposarcoma, multiple myeloma and leukemia by administering a compound of the formula (I).Type: GrantFiled: July 30, 2008Date of Patent: September 11, 2012Assignee: Daiichi Sankyo Company, LimitedInventors: Kosaku Fujiwara, Naomi Shimazaki
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Publication number: 20120225895Abstract: The present invention provides a pest control agent having a novel skeleton, which can be synthesized industrially, and also has excellent biological activity and residual effects. Specifically, the present invention provides a 1-heterodiene derivative represented by Formula (1) or a salt thereof, and a pest control agent including, as an active ingredient, a 1-heterodiene derivative or a salt thereof.Type: ApplicationFiled: November 9, 2010Publication date: September 6, 2012Inventors: Jyun Takahashi, Takehiko Nakamura, Masahiro Miyazawa, Isami Hamamoto, Jyun Kanazawa
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Patent number: RE43728Abstract: The invention relates to pharmaceutical compositions containing at least one thiazolidin-4-one derivative to prevent or treat disorders associated with an activated immune system. Furthermore, the invention relates to novel thiazolidin-4-one derivatives notably for use as pharmaceutically active compounds. Said compounds particularly act also as immunosuppressive agents.Type: GrantFiled: November 16, 2004Date of Patent: October 9, 2012Assignee: Actelion Pharmaceuticals Ltd.Inventors: Christoph Binkert, Martin Bolli, Boris Mathys, Claus Mueller, Michael Scherz, Oliver Nayler
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Patent number: RE43833Abstract: The invention relates to pharmaceutical compositions containing at least one thiazolidin-4-one derivative to prevent or treat disorders associated with an activated immune system. Furthermore, the invention relates to novel thiazolidin-4-one derivatives notably for use as pharmaceutically active compounds. Said compounds particularly act also as immunosuppressive agents.Type: GrantFiled: August 9, 2011Date of Patent: November 27, 2012Assignee: Actelion Pharmaceuticals Ltd.Inventors: Christoph Binkert, Martin Bolli, Boris Mathys, Claus Mueller, Michael Scherz, Oliver Nayler