Nitrogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/352)
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Patent number: 8211913Abstract: Compounds of formula (I): as well as pharmaceutically acceptable salts and esters thereof used in the form of pharmaceutical compositions.Type: GrantFiled: February 17, 2009Date of Patent: July 3, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Kurt Amrein, Daniel Hunziker, Bernd Kuhn, Alexander Mayweg, Werner Neidhart
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Patent number: 8211912Abstract: The present invention relates to methods for decreasing cellular DNA repair in a target patient; decreasing cellular NAD+ biosynthesis in a target patient; increasing efficiency of radiation therapy in a target patient; modulating nicotinamide phosphoribosyl transferase activity in a patient; or sensitizing a patient to a DNA damaging therapy. The invention relates to methods for treating a patient who received a toxic dose of an nicotinamide phosphoribosyl transferase inhibitor. The invention also relates to pharmaceutical compositions comprising a physiologically acceptable carrier; an effective amount of a NMPRT inhibitor; and nicotinic acid. The invention also relates to methods for treating a patient diagnosed with or suspected to have a cancer deficient in nicotinic acid pathway.Type: GrantFiled: September 25, 2008Date of Patent: July 3, 2012Assignee: Gemin X Pharmaceuticals CanadaInventors: Anne Roulston, Pierre Beauparlant
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Publication number: 20120165343Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.Type: ApplicationFiled: December 22, 2011Publication date: June 28, 2012Applicant: Pfizer Inc.Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
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Publication number: 20120164078Abstract: A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at about 12 hours and the use of the composition to treat various neurological diseases, including multiple sclerosis. A method of selecting individuals based on responsiveness to a treatment, including, for example, identifying individuals who responded to treatment with a sustained release fampridine composition.Type: ApplicationFiled: March 2, 2012Publication date: June 28, 2012Inventors: Andrew R. Blight, Lawrence Maranucci, Ron Cohen
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Publication number: 20120165339Abstract: A cyclopropane derivative represented by the following formula (I) or a pharmaceutically acceptable salt thereof has orexin receptor inhibitory action, and thus, is extremely useful as an agent for preventing or treating sleep disorder or dyssomnia caused by orexin, including insomnia as a typical example: wherein A1, A2 and A3 each independently represent an aryl group, a heterocyclyl group or the like, R1, R2 and R3 each independently represent a hydrogen atom, a C1-6 alkyl group or the like, X represents an oxygen atom or the like, and L represents a bond or the like.Type: ApplicationFiled: December 20, 2011Publication date: June 28, 2012Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Taro Terauchi, Ayumi Takemura, Yuji Kazuta, Fumihiro Ozaki, Takashi Doko, Yu Yoshida, Toshiaki Tanaka, Keiichi Sorimachi, Yoshimitsu Naoe, Carsten Beuckmann
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Publication number: 20120157502Abstract: The present invention is directed to compounds of Formula I: or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity.Type: ApplicationFiled: February 27, 2012Publication date: June 21, 2012Applicant: Pfizer Inc.Inventor: Paul V. RUCKER
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Patent number: 8202893Abstract: One aspect of this disclosure relates generally to lipid compounds that exert diverse effects in the endocannabinoid system, such as regulating CB1 and CB2 receptor or moderating other bio-macromolecules within the endocannabinoid system. Some of the compounds showed improved receptor binding affinity, and/or improved receptor subtype selectivity, and improved bio-stability. Some of the compounds exhibit activities to regulate the enzymes that moderate the bio-disposal of endogenous cannabinoids, such as the fatty acid amide hydrolase (FAAH). Some of the compounds exhibit activities to inhibit the anandamide transporter. Other aspects of the invention are pharmaceutical preparations employing these ligands and methods of administering therapeutically effective amounts of the preparations to provide a physiological effect.Type: GrantFiled: October 12, 2005Date of Patent: June 19, 2012Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Chen Li, Dai Lu
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Patent number: 8202889Abstract: The present invention relates to methods of inhibiting bacterial IMPDH comprising administering compounds of formula I: or pharmaceutically acceptable salts thereof. The present invention also relates to pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infections.Type: GrantFiled: September 8, 2006Date of Patent: June 19, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Paul Charifson, Trudy Grossman, Emanuele Perola
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Publication number: 20120148560Abstract: A pharmaceutical composition for treating or preventing one or both of neural anoxia and reperfusion injury, which includes a pharmacological activator of the PKG pathway, and methods of treating or preventing medical conditions using a pharmacological activator of the PKG pathway.Type: ApplicationFiled: December 15, 2011Publication date: June 14, 2012Applicant: Florida Atlantic UniversityInventors: Kenneth DAWSON-SCULLY, Sara Louise Milton
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Publication number: 20120142668Abstract: Disclosed are 4-amino-2-butenamides of Formula (I) having pharmacological activity, pharmaceutical compositions containing them, and methods for the treatment of diseases mediated by the cathepsin C enzyme such as chronic obstructive pulmonary disease.Type: ApplicationFiled: August 11, 2010Publication date: June 7, 2012Inventors: Niall Anderson, Ann M. Bullion, Neysa Nevins, Michael R. Palovich, Steven L. Sollis, Michael D. Wall, Jakob Busch-Petersen, Brian Evans, Huijie Li
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Patent number: 8183267Abstract: The preparation of flupirtine carboxylate acid addition salts having the following formula (2), wherein R represents hydrogen or a C1-C6 alkyl group, with the proviso that RCOOH is neither maleic acid nor gluconic acid, is described.Type: GrantFiled: June 9, 2009Date of Patent: May 22, 2012Assignee: AWD. Pharma GmbH & Co. KGInventors: Christoph Martin Hoock, Asal Qadan
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Publication number: 20120121724Abstract: The present invention is related to the composition and methods of manufacture of orally-dissolvable, edible films as a vehicle for the non-invasive administration of nitroglycerin, as well as other therapeutic agents either with or without nitroglycerin, through the mucosal tissues of the oral cavity. The films include a water soluble film-forming polymer such as pullulan. Methods for producing the films are also disclosed.Type: ApplicationFiled: January 20, 2012Publication date: May 17, 2012Inventor: Todd Maibach
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Publication number: 20120122870Abstract: Ischemia-reperfusion injury remains a primary cause of morbidity and mortality in individuals who experience disruption of normal blood flow to one or more major organs. For example, there are no clinically proven strategies that prevent acute renal failure following cardiac surgery. The present invention provides a variety of methods for the treatment or prevention of ischemia-reperfusion injury. In one aspect of the invention, a method for treating or preventing ischemia-reperfusion injury includes administering to a subject an effective amount of a sphingosine kinase inhibitor. Sphingosine kinase inhibitors are very effective in the protection against IR-induced acute renal failure and liver failure. Moreover, the effects occur very early after administration, requiring only a very short time of treatment. Toxicology studies with sphingosine kinase inhibitors demonstrate that they have low toxicity, even in long-term treatment.Type: ApplicationFiled: May 10, 2010Publication date: May 17, 2012Applicants: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT, APOGEE BIOTECHNOLOGY CORPORATIONInventors: Charles D. Smith, Zhi Zhong, Lynn W. Maines
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Publication number: 20120122934Abstract: Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.Type: ApplicationFiled: May 18, 2011Publication date: May 17, 2012Inventors: Orion D. Jankowski, Kieron E. Wesson, Paul Mollard, William D. Shrader
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Patent number: 8178563Abstract: The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.Type: GrantFiled: May 4, 2007Date of Patent: May 15, 2012Assignee: IRM LLCInventors: Wenqi Gao, Jiqing Jiang, Yongqin Wan, Dai Cheng, Dong Han, Xu Wu, Shifeng Pan
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Publication number: 20120115827Abstract: The present invention relates to a novel 3-aminobenzamide, compound represented by the following formula which effectively inhibits vanilloid receptor subtype 1 (VR1) activity (wherein, for example, R1 is a C1-6 alkyl group which may be substituted, R2 is a hydrogen atom, a C1-6 alkyl group or a C1-6 alkoxy group which may be substituted, R3 is a hydrogen atom or a C1-6 alkyl group, R4 is a C1-6 alkyl group, a C1-6 alkoxy group, or a halo C1-6 alkyl group, m is an integer of 1 to 5 and P is a carbon or hetero ring) or a pharmaceutically acceptable salt thereof. The pharmaceutical composition comprising as active ingredients the 3-aminobenzamide, compound or a pharmaceutically acceptable salt thereof is useful for treating diseases involved in VR1 activity such as pain, acute pain, chronic pain, neuropathicpain, rheumatoid arthritis pain, and neuralgia.Type: ApplicationFiled: June 7, 2011Publication date: May 10, 2012Applicant: Japan Tobacco Inc.Inventors: Yoshihisa Koga, Shinji Yata, Takashi Watanabe, Takuya Matsuo, Masahiro Sakata, Wataru Kondo
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Patent number: 8173677Abstract: The present invention relates to methods for decreasing cellular DNA repair in a patient diagnosed with or suspected to have chronic lymphocytic leukemia (CLL); decreasing cellular NAD+ biosynthesis in a patient diagnosed with or suspected to have CLL; or sensitizing a patient diagnosed with or suspected to have CLL to a DNA damaging therapy. The invention relates to methods for treating a patient diagnosed with or suspected to have CLL.Type: GrantFiled: March 25, 2009Date of Patent: May 8, 2012Assignee: Gemin X Pharmaceuticals Canada Inc.Inventors: Anne Roulston, Pierre Beauparlant
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Publication number: 20120108573Abstract: The present invention relates to compounds of the formula I wherein A1, A2, R1, R3, X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula fare capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of the formula I.Type: ApplicationFiled: January 6, 2012Publication date: May 3, 2012Inventors: Ursula SCHINDLER, Karl SCHÖNAFINGER, Hartmut STROBEL
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Publication number: 20120108642Abstract: The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4, R5, m, and n are defined in the specification are TRPV1 antagonists. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: ApplicationFiled: December 27, 2011Publication date: May 3, 2012Inventors: Arthur R. Gomtsyan, Robert G. Schmidt, Erol K. Bayburt, Jerome F. Daanen, Michael E. Kort
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Patent number: 8163750Abstract: The present invention relates to compounds of formula (I): wherein R1, R2, R2?, L, Het, p and p? are as defined herein, compositions containing them, and their use as medicinal products.Type: GrantFiled: November 24, 2009Date of Patent: April 24, 2012Assignee: Sanofi-AventisInventors: Fabienne Thompson, Patrick Mailliet, Jean-Marie Ruxer, Helene Goulaouic, Francois Vallee, Herve Minoux, Fabienne Pilorge, Luc Bertin, Stephane Hourcade, Maria Mendez-Perez, Peter Hamley
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Patent number: 8163778Abstract: Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof wherein the residues have the significance given in claim 1 and which can be used in the form of pharmaceutical compositions.Type: GrantFiled: November 24, 2008Date of Patent: April 24, 2012Assignee: Hoffmann-LA Roche Inc.Inventors: Wolfgang Haap, Paul Hebeisen, Eric Argirios Kitas, Bernd Kuhn, Peter Mohr, Hans Peter Wessel
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Publication number: 20120095062Abstract: The present invention is directed to compounds of Formula I: or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity.Type: ApplicationFiled: December 21, 2011Publication date: April 19, 2012Applicant: Pfizer Inc.Inventors: Hengmiao (Henry) CHENG, Xiao HU, Kenvin D. JEROME, Mark OBUKOWICZ, Lisa OLSON, Paul V. RUCKER, Ronald Keith WEBBER
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Publication number: 20120094964Abstract: The present invention relates to sulfamoyl benzoic acid derivatives of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPM8 receptor.Type: ApplicationFiled: May 6, 2010Publication date: April 19, 2012Inventors: Tadashi Inoue, Masashi Ohmi, Kiyoshi Kawamura, Kazuo Ando, Yuji Shishido
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Publication number: 20120095044Abstract: Disclosed herein are compounds that are tissue-nonspecific alkaline phosphatase inhibitors. The disclosed compounds are used to treat, prevent, or abate vascular calcification, arterial calcification and other cardiovascular diseases.Type: ApplicationFiled: December 7, 2011Publication date: April 19, 2012Inventors: Jose Luis Millan, Eduard Sergienko
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Patent number: 8158642Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: October 15, 2009Date of Patent: April 17, 2012Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Christopher Michael Semko, Ying-zi Xu, Frank Stappenbeck, Jenifer Lea Smith, Kassandra Inez Rossiter, Juri Y. Fukuda, Andrei W. Konradi
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Patent number: 8158660Abstract: The present invention is directed to compounds of Formula I: or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity.Type: GrantFiled: May 8, 2009Date of Patent: April 17, 2012Assignee: Pfizer Inc.Inventors: Hengmiao Cheng, Xiao Hu, Kevin D. Jerome, Mark G. Obukowicz, Lisa Maria Olson, Paul V. Rucker, Ronald Keith Webber
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Publication number: 20120087913Abstract: Methods and compositions for enhancing the ability of hypoxia-activated bioreductive agents to kill tumor cells within solid tumors are provided. Local regions of hypoxia are created within a tumor, or within a region containing a tumor, resulting in enhanced activation of hypoxia-activated bioreductive agents (e.g. tirapazamine) within the local region. The activated hypoxia-activated bioreductive agents kill tumor cells in the hypoxic region by catalyzing DNA stand breakage within the tumor cells. Because the activity is localized, side effects that typically occur as a result of systemic administration of bioreductive agents are reduced.Type: ApplicationFiled: April 8, 2009Publication date: April 12, 2012Inventors: Ruey-min Lee, Peck-sun Lee
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Publication number: 20120088800Abstract: 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: A, m, n, p, a, X, Y and Z are defined in the specification. These compounds are useful for treating a disease or condition selected from the group consisting of glaucoma, dry eye, angiogenesis and pulmonary edema.Type: ApplicationFiled: June 25, 2010Publication date: April 12, 2012Applicant: ALLERGAN, INC.Inventors: Wenkui K. Fang, Ken Chow
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Publication number: 20120088802Abstract: The present invention is directed to compounds of Formula I: or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity.Type: ApplicationFiled: May 8, 2009Publication date: April 12, 2012Applicant: Pfizer, Inc.Inventors: Hengmiao (Henry) Cheng, Xiao Hu, Kevin D. Jerome, Mark Obukowicz, Lisa Olson, Paul V. Rucker, Ronald Keith Webber
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Publication number: 20120088746Abstract: Compounds are disclosed that have a formula represented by the following: Formula (I). 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, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: May 10, 2007Publication date: April 12, 2012Applicants: PFIZER INC., RENOVIS, INC.Inventors: Yuji Shishido, Kazunari Nakao, Satoshi Nagayama, Hirotaka Tanaka, Matthew Alexander James Duncton, Matthew Cox, John Kincaid, Kiran Sahasrabudhe, Maria de Los Angeles Estiarte-Martinez
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Publication number: 20120088803Abstract: Provided is a novel control agent for soft rot and a novel control method for the same. The control agent for soft rot of a plant contains 3-chloro-N-(3-chloro-5-trifluoromethyl-2-pyridyl)-alpha,alpha,alpha-trifluoro-2,6-dinitro-p-toluidine as an active ingredient, which is applied to plant cultivation soil.Type: ApplicationFiled: June 4, 2010Publication date: April 12, 2012Applicant: Ishihara Sangyo Kaisha, LtdInventors: Yoshikazu Kurata, Hiroyuki Hayashi
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Publication number: 20120088661Abstract: The present invention relates to fungicidal mixtures comprising, as active components, 1) azolylmethyloxiranes of the general formula I wherein the variables have the meanings described in the application, 2) a fungicidal compound II, and 3) optionally a further fungicidal compound II, where the compounds II of components 2 and 3 independently of one another are selected from the group consisting of the compounds described in the application, with the proviso that components 2 and 3 are not identical, and to the use of the fungicidal mixtures for controlling phytopathogenic fungi and to the compositions comprising them.Type: ApplicationFiled: June 15, 2010Publication date: April 12, 2012Applicant: BASF SEInventors: Jochen Dietz, Egon Haden, Jens Renner, Sarah Ulmschneider, Alice Glättli, Marianna Vrettou-Schultes, Silke Stolz
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Patent number: 8148409Abstract: The present invention is directed to compounds of Formula I: or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity.Type: GrantFiled: July 20, 2009Date of Patent: April 3, 2012Assignee: Pfizer Inc.Inventor: Paul V. Rucker
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Publication number: 20120077764Abstract: Novel formulations containing a fluorinated chloramphenicol or thiamphenicol derivative antibiotic such as florfenicol, and methods for using such formulations in the treatment and prevention of infectious diseases of bovines and swine, including bovine respiratory disease.Type: ApplicationFiled: September 2, 2011Publication date: March 29, 2012Inventors: Keith A. FREEHAUF, Allan Weingarten, Robert D. Simmons, Kanwal Jit Varma
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Publication number: 20120071519Abstract: Provided herein are crystalline forms of a maleate salt of betrixaban, compositions and methods of preparation or use thereof.Type: ApplicationFiled: August 31, 2011Publication date: March 22, 2012Inventors: Vincent R. Capodanno, Liam Corcoran, Michael McNevin, Itzia Zoraida Arroyo, Robert M. Wenslow, Richard G. Ball, Eric L. Margelefsky, Timothy K. Maher, Anjali Pandey
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Patent number: 8138349Abstract: The present invention is concerned with new polymorphic forms of flupirtine maleate, processes for preparing the new polymorphic forms, pharmaceutical compositions containing them, therapeutic uses thereof and methods of treatment employing them.Type: GrantFiled: July 13, 2007Date of Patent: March 20, 2012Assignee: Pliva Hrvatska D.O.O.Inventors: Aleksandar Danilovski, Maja Dev{hacek over (c)}ić, Marina Marinković, Ernest Me{hacek over (s)}trović, Tina Mundorfer, Iva Tunjić
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Publication number: 20120064007Abstract: A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at about 12 hours and the use of the composition to treat various neurological diseases, including multiple sclerosis. A method of selecting individuals based on responsiveness to a treatment, including, for example, identifying individuals who responded to treatment with a sustained release fampridine composition.Type: ApplicationFiled: November 18, 2011Publication date: March 15, 2012Inventors: Andrew R. Blight, Lawrence Maranucci, Ron Cohen
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Publication number: 20120065247Abstract: Provided herein are compounds and methods for use in preventing or treating a viral infection mediated by a virus comprising an IRES-containing RNA molecule or cancer related to an increase or decrease in IRES-mediated translation of an RNA molecule. Also provided are methods of inhibiting or promoting IRES-mediated translation. Also provided are methods of screening for an agent that inhibits IRES-mediated translation.Type: ApplicationFiled: March 26, 2010Publication date: March 15, 2012Applicants: DiscoveryBiomed, Inc., The UAB Research FoundationInventors: Sunnie R. Thompson, Erik Mills Schwiebert, John H. Streiff
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Patent number: 8133907Abstract: The present invention is directed to compounds of formula (I) or a pharmaceutically acceptable salt thereof; wherein A is (1); X is selected from CH, CF and N; R5 is selected from H, C1-C6 alkyl, C1-C6 fluoroalkyl, and —OR12; R9 is selected from H —NR13C(O)R14 and —C(O)NR10R11; R12 is selected from H, C1-C6 alkyl and C3-C6 cycloalkyl, for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes.Type: GrantFiled: July 14, 2006Date of Patent: March 13, 2012Assignee: Eli Lilly and CompanyInventors: Larry Chris Blaszczak, Brian Michael Mathes, Shon Roland Pulley, Michael Alan Robertson, Scott Martin Sheehan, Qing Shi, Brian Morgan Watson, Michael Robert Wiley
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Publication number: 20120059039Abstract: Septic shock is known to lead to, at the end stage, systematic inflammatory reaction syndrome and multiple organ failure (MOF) and cause the patients' death. In both diseases, the patient dies finally of MOF, and the infiltration by inflammatory cells plays a key role for MOF. Thus, development of therapeutic agents for septic shock by suppressing the infiltration by inflammatory cells has been desired. To provide a therapeutic or preventive agent for shock, comprising as an active ingredient a diaminotrifluoromethylpyridine derivative represented by the formula (I) or its salt: wherein X is a cycloalkylcarbonyl group, an alkenylcarbonyl group, a thiophenecarbonyl group or a benzoyl group which may be substituted by a halogen atom; and Y is an alkylsulfonyl group.Type: ApplicationFiled: May 17, 2010Publication date: March 8, 2012Applicant: Ishihara Sangyo Kaisha LtdInventors: Shuichi Yotsuya, Hiroshi Shikama
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Publication number: 20120059024Abstract: The present invention relates generally to the field of pain management. More particularly, the present invention relates to analgesic combinations of an opioid and flupirtine or retigabine which reduce the risk of substance abuse in pain management. Such combinations are referred to as abuse-deterrent fixed dose combinations (FDC).Type: ApplicationFiled: January 28, 2010Publication date: March 8, 2012Applicant: RELEVARE AUST. PTY LTDInventors: Ian Robert Chambers Cooke, Colin Stanley Goodchild, Claudia C. Gregorio-King
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Publication number: 20120052055Abstract: Invented is a method of treating thrombocytopenia in a human, in need thereof which comprises the in vivo administration of a therapeutically effective amount of a peptide or a non-peptide TPO receptor agonist and an anti-clotting agent or agents, and optional further active ingredients, to such human.Type: ApplicationFiled: May 6, 2010Publication date: March 1, 2012Applicant: Glaxosmithkline LLCInventors: Connie L. Erickson-Miller, Michael Arning
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Publication number: 20120052122Abstract: Disclosed is a method of treatment of chronic obstructive pulmonary disease associated with chronic bronchitis in a patient at risk of exacerbations. The method includes administering to a patient with a history of chronic obstructive pulmonary disease associated with chronic bronchitis and at risk of exacerbations, a maintenance dose of 500 micrograms per day of roflumilast. Also disclosed is a method of increasing pre-bronchodilator FEV1 or post-bronchodilator FEV1 in such a patient, and increasing pre-bronchodilator FVC or post-bronchodilator FVC in such a patient. Further disclosed is a method of reducing the rate of exacerbations in such a patient.Type: ApplicationFiled: August 24, 2011Publication date: March 1, 2012Applicant: Nycomed GmbHInventor: Dirk Bredenbroeker
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Publication number: 20120052118Abstract: The present invention provides an apparatus and process for making softgel capsules having incorporated therein other solid dosage forms selected from the group consisting of pellets, smaller capsules, smaller tablets, sustained release solid dosage forms, immediate release solid dosage forms, extended release solid dosage forms and zero order release solid dosage forms, said apparatus comprising: (a) two spreader boxes; (b) two casting drums; (c) a pair of rotary dies having means for suction; (d) a liquid fill system; (e) a wedge for heating gelatine ribbons and feeding said fill; and (f) two lateral dispensing devices said lateral dispensing devices including hoppers having said solid dosage forms, channelguides for transporting said solid dosage forms and a grasping claw for dispensing said solid dosage form into the softgel pocket formed in the rotary dies.Type: ApplicationFiled: July 18, 2011Publication date: March 1, 2012Inventors: Carlos Salazar Altamar, Gustavo Anaya, Braulio Teran, Newman Aguas Navarro, Willmer Herrera
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Publication number: 20120046230Abstract: The present invention is directed to methods of using combination therapies containing [2-({4-[(dimethylamino)iminomethyl]phenyl}carbonylamino)-5-methoxyphenyl]-N-(5-chloro(2-pyridyl))carboxamide for the treatment of thrombotic disease(s) and pharmaceutical compositions thereof.Type: ApplicationFiled: August 19, 2011Publication date: February 23, 2012Inventors: Uma Sinha, Stanley J. Hollenbach, Patrick Andre
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Publication number: 20120046243Abstract: There is disclosed aminopyridine-and aminopyrimidinecarboxamide compounds useful as pharmaceutical agents, synthesis processes, and pharmaceutical compositions which include aminopyridine- and aminopyrimidinecarboxamides compounds. More specifically, there is disclosed a genus of CXCR2 inhibitor compounds that are useful for treating a variety of inflammatory and neoplastic disorders.Type: ApplicationFiled: August 22, 2011Publication date: February 23, 2012Applicant: Syntrix Biosystems Inc.Inventors: Dean Y. Maeda, John A. Zebala, Aaron D. Schuler
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Publication number: 20120041034Abstract: A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at least 12 hours, preferably 24 hours or more and the use of the composition to treat various neurological diseases.Type: ApplicationFiled: July 20, 2011Publication date: February 16, 2012Inventors: Andrew R. Blight, Ron Cohen
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Publication number: 20120035217Abstract: There is provided compounds of formula I, wherein Y, ring A, D1, D2a, D2b, D3, L1, Y1, L2 and Y2 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.Type: ApplicationFiled: March 12, 2010Publication date: February 9, 2012Applicant: BIOLIPOX ABInventors: Peter Nilsson, Benjamin Pelcman, Martins Katkevics, Edgars Suna, Ilya Popovs
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Patent number: 8110689Abstract: Benzanilides of the formula: in which X represents hydrogen, halogen, nitro, C1-6 alkylthio, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl or C1-6 alkylsulfonyloxy; Y represents halogen or C1-6 alkyl; R1 represents C1-6 alkyl, C1-6 alkylthio-C1-6 alkyl, C1-6 alkylsulfinyl-C1-6 alkyl or C1-6 alkylsulfonyl-C1-6 alkyl; R2 represents hydrogen, C1-6 alkyl or C1-6 haloalkyl; R3 represents hydrogen or hydroxy; W represents CH or N; and Q represents optionally substituted phenyl or optionally substituted pyridyl wherein the substituent is at least one group selected from the group consisting of halogen, C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 haloalkylthio, C1-6 haloalkylsulfinyl and C1-6 haloalkylsulfoxy; provided that when R3 is hydroxy, R2 is not C1-6 alkyl, or when R2 is C1-6 haloalkyl, R3 is hydroxy, W is CH, and the substituents of Q are two or more C1-6 haloalkyl. Insecticides comprising the benzanilides are herein provided.Type: GrantFiled: June 2, 2006Date of Patent: February 7, 2012Assignee: Bayer Cropsciene AGInventors: Katsuaki Wada, Tetsuya Murata, Katsuhiko Shibuya, Eiichi Shimojo
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Publication number: 20120028930Abstract: The present invention includes salts and polymorphs of flupirtine including, but not limited to carboxylic acid salts and sulfonic acid salts and their polymorphs. The present invention also includes pharmaceutical compositions comprising the salts and polymorphs of flupirtine. The invention also relates to the therapeutic use of the flupirtine salts and polymorphs to treat nervous system disorders, pain disorders, musculoskeletal disorders, and other diseases and conditions.Type: ApplicationFiled: February 25, 2011Publication date: February 2, 2012Applicant: Bionevia Pharmaceuticals Inc.Inventors: Isabel KALOFONOS, William Martin Doyle