Nitrogen In R Patents (Class 514/619)
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Publication number: 20130184343Abstract: A compound of formula (I): wherein A1, A2, A3, A4, R1, R2, G1, G2, Q1 and Q2 are as defined in claim 1; or salts or N-oxides thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.Type: ApplicationFiled: March 4, 2013Publication date: July 18, 2013Applicants: Syngenta Crop Protection LLC, Syngenta Participations AGInventor: Syngenta Participations AG
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Patent number: 8486858Abstract: The present invention relates to compositions, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.Type: GrantFiled: September 14, 2010Date of Patent: July 16, 2013Assignee: Bayer CropScience AGInventors: Thomas Seitz, Ulrike Wachendorff-Neumann, Peter Dahmen
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Patent number: 8487130Abstract: Described is a new cooling agent represented by Structure I and compositions with known coolers having cooling properties and the application of Structure I in foodstuffs and chewing gum:Type: GrantFiled: February 25, 2011Date of Patent: July 16, 2013Assignee: International Flavors & Fragrances Inc.Inventors: Arkadiusz Kazimierski, Mark L. Dewis
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Publication number: 20130178457Abstract: Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors of Formula (I).Type: ApplicationFiled: July 5, 2012Publication date: July 11, 2013Applicant: LUPIN LIMITEDInventors: Sanjeev Anant KULKARNI, Sachin MADAN, Nirmal Kumar JANA, Prashant Vitthalrao TALE, Narasimha Murthy CHEEMALA, Sachin Jaysing MAHANGARE, Prashant Popatrao VIDHATE, Chaitanya Prabhakar KULKARNI, Sapana Suresh PATEL, Amolsing Dattu PATIL, Seema Prabhakar ZADE, Rohan Mahadev SHINDE, Venkata P. PALLE, Rajender Kumar KAMBOJ
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Publication number: 20130158035Abstract: Screening methods for identifying compounds and compounds and pharmaceutical compositions for treating and preventing cancer are disclosed. The compounds affect signal transduction downstream of the MET receptor.Type: ApplicationFiled: August 23, 2011Publication date: June 20, 2013Applicant: Brigham Young UniversityInventor: Marc Hansen
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Publication number: 20130158112Abstract: A pharmaceutical composition for inhibiting amyloid beta peptide in a subject includes a compound having the formula (I): where M is selected from a substituted or unsubstituted alkyl, halo, alkoxy, aryl, cyclic, or heterocyclic group; p is an integer from 0-3; X1 is a 3-9 atoms in length linker connecting A and B; B is selected from a substituted or unsubstituted aryl, alkoxy or amine group; and a pharmaceutically acceptable salt thereof; and a pharmaceutical carrier.Type: ApplicationFiled: June 20, 2012Publication date: June 20, 2013Inventors: Jonathan D. Smith, Enakshi Chakrabarti, Subrata Ghosh, Marti Sayre, Gregory Tochtrop
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Publication number: 20130123203Abstract: Disclosed herein are methods and compositions for treating autism. Disclosed herein are methods and compositions for treating an autism spectrum disorder.Type: ApplicationFiled: October 31, 2012Publication date: May 16, 2013Inventors: Paul Talalay, Andrew W. Zimmerman, Kirby D. Smith
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PHARMACEUTICAL COMPOSITION IN WHICH SOLUBILITY OF PARTIALLY SOLUBLE TRICYCLIC DERIVATIVE IS IMPROVED
Publication number: 20130101647Abstract: A pharmaceutical composition includes lipid nanoparticles which include two or more of a phospholipid, cholesterol, and an ionic lipid, and a tricyclic derivative, wherein the solubility of the tricyclic derivative is improved. It is possible to solubilize a partially soluble tricyclic derivative in a high concentration even without using a solubilization aid harmful to the human body, to maintain improved solubility even if water is added for the use as an injection, and to show stability even if stored for a long time, by preparing lipid nanoparticles. Therefore, the lipid nanoparticles of the present invention can be used for preparing a pharmaceutical preparation containing a partially soluble tricyclic derivative as an active ingredient.Type: ApplicationFiled: June 23, 2011Publication date: April 25, 2013Applicant: JEIL PHARMACEUTICAL CO., LTD.Inventors: Myung-Hwa Kim, Kwang-Woo Chun, In-Hae Ye, Jong-Hee Choi -
Patent number: 8426431Abstract: The invention is directed to substituted 2-aminoacetamides represented by formula (II): and to pharmaceutically acceptable salts and prodrugs thereof, wherein the substituents are defined herein. The invention is also directed to the use of substituted 2-aminoacetamides in methods for the treatment of neuronal damage following global and focal ischemia, and for the treatment, prevention or amelioration of pain, anxiety, or manic depression, as anticonvulsants, as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.Type: GrantFiled: January 7, 2011Date of Patent: April 23, 2013Assignee: Purdue Neuroscience CompanyInventors: Nancy C. Lan, Yan Wang, Sui Xiong Cai
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Publication number: 20130095035Abstract: The present invention relates generally to methods and compositions for targeting of intracellular molecules involved in proliferation and protein synthesis of activated cells using polyanionic multivalent macromolecules. In particular aspect, multiple sulfate groups linked to polyol are specifically targeted to the cytoplasm and nucleus of proliferating and activated cells. The invention further comprises novel polyanionic macromolecular compounds and formulations.Type: ApplicationFiled: January 31, 2011Publication date: April 18, 2013Applicant: MIVENION GMBHInventors: Kai Licha, Michael Schirner, Pia Welker, Rainer Haag, Marie Weinhart, Florian Paulus
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Publication number: 20130095067Abstract: The present invention provides for the treatment or prevention of Hepadnaviridae infection and disease caused by Hepadnaviridae infection. In particular, the invention provides compositions and methods that affect the ability of Hepadnaviridae to utilize the host's cellular machinery as part of the virus' lifecycle. The invention relates to the discovery that interfering with the normal ability of viruses to utilize the host cell machinery with LSD1 inhibitors reduces HBV replication. Thus, the treatment and prevention of Hepadnaviridae infection and disease caused by Hepadnaviridae according to the invention comprises administering to an individual in need of treatment, a therapeutically effective amount of a LSD1 inhibitor. The individual in need of treatment can be a human or, e.g., another mammal.Type: ApplicationFiled: February 24, 2011Publication date: April 18, 2013Inventors: Jonathan Alleman Baker, Matthew Colin Thor Fyfe
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Publication number: 20130090386Abstract: The present invention relates to a compound of Formula 1, wherein: (A) is heteroaryl or aryl; each (A?), if present, is independently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A?) is substituted with 0, 1, 2, or 3 substituents independently chosen from halo, haloalkyl, haloalkoxy, aryl, arylalkoxy, alkyl, alkoxy, amido, —CH2C(=0)NH2, heteroaryl, cyano, sulfonyl, and sulfinyl; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is —NH—; (L) is chosen from a single bond, —CH2—, —CH2CH2—, —CH2CH2CH2—, and —CH2CH2CH2CH2—; and (D) is an aliphatic carbocyclic group or benzocycloalkyl, wherein said aliphatic carbocyclic group or said benzocycloalkyl has 0, 1, 2, or 3 substituents independently chosen from —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), alkyl, halo, amido, cyano, alkoxy, haloalkyl, and haloalkoxy.Type: ApplicationFiled: April 19, 2011Publication date: April 11, 2013Inventors: Alberto Ortega Munoz, Juio Castro-Palomino Laria, Matthew Colin Thor Fyfe
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Patent number: 8410173Abstract: The present invention relates to a method of treating pulmonary arterial hypertension by administering a therapeutically effective amount of a selective JAK2 inhibitor to a patient in need thereof.Type: GrantFiled: February 28, 2007Date of Patent: April 2, 2013Assignee: YM Biosciences Australia Pty LtdInventor: Lawrence S. Zisman
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Publication number: 20130065885Abstract: The present invention relates generally to therapeutic formulations. More particularly, this present invention provides an oral delivery system for a therapeutic compound that is a base, a salt of a base or an amphoteric compound or a salt of a amphoteric compound with pharmacological, physiological or biochemical activity or a proactive form thereof. The present invention even more particularly provides a swallow formulation comprising a therapeutic compound that is a base, a salt of a base, an amphoteric compound or a salt of an amphoteric compound which facilitates the rapid delivery of the therapeutic compound to the circulatory system.Type: ApplicationFiled: September 14, 2012Publication date: March 14, 2013Applicant: IMAGINOT PTY LTD.Inventors: Michael Stephen Roberts, Ruoying Jiang, Keivan Bezanehtak, Greg Andrew Davey, George Alexander Davidson, Geraldine Ann Elliott, Stephen Douglas Chandler, Mantu Sarkar
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Publication number: 20130059851Abstract: A method of identifying a subject having cancer who is likely to benefit from treatment with a combination therapy with a RAF inhibitor and a second inhibitor is provided. A method of treating cancer in a subject in need thereof is also provided and includes administering to the subject an effective amount of a RAF inhibitor and an effective amount of a second inhibitor, wherein the second inhibitor is a MEK inhibitor, a CRAF inhibitor, a CrkL inhibitor or a TPL2/COT inhibitor. A method of identifying a kinase target that confers resistance to a first inhibitor is also provided.Type: ApplicationFiled: March 9, 2011Publication date: March 7, 2013Applicant: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Levi A. Garraway, Cory M. Johannessen
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Patent number: 8389766Abstract: A compound of formula (I): wherein A1, A2, A3, A4, R1, R2, G1, G2, Q1 and Q2 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, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.Type: GrantFiled: December 12, 2007Date of Patent: March 5, 2013Assignee: Syngenta Crop Protection LLCInventors: Pierre Jung, Christopher Richard Syles Godfrey, William Lutz, Peter Maienfisch, Andre Stoller, Werner Zambach
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Patent number: 8377985Abstract: Methods of treating bone cancer are disclosed. The methods comprise administering to a patient a therapeutically effective amount of a compound of formula (Ia) wherein R1, R2, R3, R4, and R5 are described herein, wherein at least two of the five R1, R2, R3, R4, and R5 substituents are always hydrogen, at least one of the five substituents is always nitro, and at least one substituent positioned adjacent to a nitro is always iodo, and pharmaceutically acceptable salts thereof.Type: GrantFiled: June 30, 2008Date of Patent: February 19, 2013Assignee: BiPar Sciences, Inc.Inventors: Jerome Mendeleyev, Hassan Lemjabbar-Alaoui, Valeria S. Ossovskaya
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Publication number: 20130040965Abstract: The invention provides aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, n, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: October 17, 2012Publication date: February 14, 2013Applicant: THERAVANCE, INC.Inventors: Michael R. Leadbetter, Sean G. Trapp, Daniel D. Long, John R. Jacobsen, Sabine Axt
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Publication number: 20130035284Abstract: The present invention concerns methods and compositions involving small molecule inhibitors for the treatment or prophylaxis of flavivirus infection, such as dengue virus and West Nile virus.Type: ApplicationFiled: March 5, 2012Publication date: February 7, 2013Applicant: The Board of Regents of the University of Texas SystemInventors: Stanley J. Watowich, Suzanne M. Tomlinson, Scott Gilbertson
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Publication number: 20130034562Abstract: This invention provides use of a SARM compound or a composition comprising the same in treating and preventing muscle wasting in patients with non-small cell lung cancer (NSCLC); treating pre-cachexia or early cachexia (preventing muscle wasting in a cancer patient); treating and preventing loss of physical function due to cancer or cancer therapy; increase of physical function; and increasing survival in a patient with NSCLC, wherein the patients are subjected to cancer therapy.Type: ApplicationFiled: July 25, 2012Publication date: February 7, 2013Inventors: James T. Dalton, Duane D. Miller
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Publication number: 20130035328Abstract: The invention relates to compounds having antiviral activity and methods utilizing the compounds to treat viral infections.Type: ApplicationFiled: July 19, 2012Publication date: February 7, 2013Inventors: Peter William Gage, Gary Dinneen Ewart, Lauren Elizabeth Wilson, Wayne Best, Anita Premkumar
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Publication number: 20130034536Abstract: Provided herein are methods and compositions comprising bile acid transport inhibitors and/or enteroendocrine peptide enhancing agents and/or FXR agonists for the treatment of pancreatitis or prevention of pancreatitis.Type: ApplicationFiled: August 3, 2012Publication date: February 7, 2013Applicant: Lumena Pharmaceuticals, Inc.Inventor: Bronislava GEDULIN
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Patent number: 8361927Abstract: Combination comprising Prothioconazol and Metominostrobin preferably as a mixture, agrochemical formulation or composition for curatively and/or preventively controlling phytopathogenic fungi and/or microorganisms of plants and crops.Type: GrantFiled: December 21, 2010Date of Patent: January 29, 2013Assignee: Bayer CropScience AGInventors: Ulrike Wachendorff-Neumann, Anton Kraus, Ingo Wetcholowsky, Peter Dahmen, Hiroyuki Hadano
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Patent number: 8357722Abstract: The present invention is related to a compound according to formula (I), wherein R1 and R2 are each and independently selected from the group comprising alkyl; n is any integer between 1 and 4; R3 is an acyl selected from the group comprising lysyl, ornithyl, 2,4-diaminobutyryl, histidyl and an acyl moiety according to formula (II), wherein m is any integer from 1 to 3 and Y? is a pharmaceutically acceptable anion.Type: GrantFiled: September 12, 2011Date of Patent: January 22, 2013Assignee: Silence Therpeutics AGInventors: Oliver Keil, Jorg Kaufmann, Ansgar Santel
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Publication number: 20130011482Abstract: A medicament delivery system is disclosed. The system comprises a descending formulation for delivering the medicament and an ascending formulation to protect a patient being treated with the medicament from the side effects thereof.Type: ApplicationFiled: September 14, 2012Publication date: January 10, 2013Inventors: Jose G. Rocca, Khalid Shah
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Publication number: 20130005802Abstract: Methods of treating Wnt/Frizzled-related diseases, comprising administering niclosamide compounds are provided. Methods of predicting whether a disease will respond to treatment with a niclosamide compound are also provided.Type: ApplicationFiled: September 21, 2010Publication date: January 3, 2013Inventors: Wei Chen, Minyong Chen, H. Kim Lyerly, Lawrence S. Barak, Robert Mook, Takuya Osada, Michael A. Morse
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Publication number: 20130005759Abstract: MicroRNAs are a class of endogenous regulators of gene function. Aberrant regulation of microRNAs has been linked to various human diseases, most importantly cancer. Small molecule intervention of microRNA misregulation has the potential to provide new therapeutic approaches to such diseases. microRNA miR-122 is the most abundant microRNA in the liver and is involved in hepatocellular carcinoma development and hepatitis C virus (HCV) infection. Small molecule inhibitors and activators of the microRNA miR-122 are described, and methods for their identification are reported. These small molecule inhibitors reduce viral replication in liver cells and thus represent a new approach to the treatment of HCV infections. Moreover, small molecule activation of miR-122 in liver cancer cells selectively induced apoptosis through caspase activation, and thus has implications in cancer chemotherapy.Type: ApplicationFiled: January 21, 2011Publication date: January 3, 2013Inventors: Alexander Deiters, Douglas D. Young
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Publication number: 20130005712Abstract: The present invention relates to a composition for noxious organisms-controlling agent having a synergistic effect and a method for using said composition, which comprises, as active ingredients thereof, one or more compounds selected from the phthalamide derivatives represented by general formula (I) being useful as an insecticide or acaricide and one or more compounds selected from the compounds having insecticidal, acaricidal or nematocidal activity: wherein R1, R2 and R3 may be the same or different and each represent hydrogen atom, C3-C6 cycloalkyl, -A1--Qp, etc., each of X and Y may be the same or different and represents hydrogen atom, halogen atom, etc., n is an integer of 1 to 4, m is an integer of 1 to 5, and each of Z1 and Z2 represents O or S.Type: ApplicationFiled: September 11, 2012Publication date: January 3, 2013Inventors: Kazuyuki Sakata, Masayuki Morimoto, Hiroshi Kodama, Tetsuyosi Nishimatsu
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Patent number: 8344181Abstract: the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents O, S, NR6, SO or SO2; R1 represents hydrogen, cyano, hydroxy, or C1-4alkyl optionally substituted with halo, R2 represents hydrogen, C1-4alkyl, or C1-4alkyloxy-; R3 represents hydrogen, C1-4alkyl, C1-4alkyloxy- or R3 combined with R2 form together a divalent radical selected from the group consisting of —O—CH2— (a), —NR7—CH2— (b), —(CR8R9)m- (c) and —CR10? (d) wherein m represents 1 or 2 and R7, R8, R9 and R10 are each independently selected from hydrogen or C1-4alkyl; R4 represents hydrogen, halo, hydroxy, cyano, amino, NR11R12, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy and halo or R4 represents C1-4alkyl optionally substituted with one or where possible two or three substituents selected from hydroxy and halo; R5 represents hydrogen, halo, cyano, amino, phenyl, hydroxy, C1-4alkyloxycarbonyl, hydroxType: GrantFiled: August 26, 2005Date of Patent: January 1, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Libuse Jaroskova, Joannes Theodorus Maria Linders, Louis Jozef Elisabeth Van Der Veken, Gustaaf Henri Maria Willemsens, François Paul Bischoff
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Publication number: 20120329790Abstract: The present invention is a dentinal drug delivery composition composed of cationic and/or neutral porous particles containing an effective amount of a therapeutic agent and a method for using the same to provide a dental treatment.Type: ApplicationFiled: November 23, 2010Publication date: December 27, 2012Applicant: University of Medicine and Dentistry of New JerseyInventor: Kenneth Markowitz
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Publication number: 20120322753Abstract: The production method prepares a solid preparation by dissolving water-insoluble and/or water indissolvable alkaline active pharmaceutical ingredient in an acidifier-containing acid solution to obtain medicated acid liquid; homogeneously mixing alkalizer, adjuvants and the medicated acid liquid, and carrying out wet granulation. The alkalizer is a reagent to reduce the acidity of the mixture of the alkalizer and the medicated acid liquid relative to the acidity of the medicated acid liquid. The preparation method avoids the problems in mechanical pulverization, such as environmental pollution, great loss and serious security risks. This method is simply operated, has high safety coefficient and is convenient for industrialized production. Also disclosed is the solid preparation produced by the method. The solid preparation produced by the method has better dissolution performance than that produced by prior art, and has better or at least equivalent stability and content uniformity with prior art.Type: ApplicationFiled: December 28, 2010Publication date: December 20, 2012Applicants: SHANGHAI ZHONGXI SUNVE PHARMACEUTICAL CO., LTD., SHANGHAI ZHONGXI PHARMACEUTICAL COMPANYInventors: Siji Zheng, Bo Tan
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Publication number: 20120322879Abstract: The invention relates to methods and compositions for promoting cognitive function and/or treating cognitive function disorders and impairments. In particular the methods are accomplished by administering to a subject CI-994 or dinaline or a pharmaceutically acceptable salt, ester, prodrug or metabolite thereof.Type: ApplicationFiled: August 27, 2012Publication date: December 20, 2012Inventors: Li-Huei Tsai, Ji-Song Guan, Stephen J. Haggarty, Edward Holson, Florence Wagner, Johannes Graeff
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Publication number: 20120316230Abstract: The present invention relates to compounds of formula (I), where R1 and R2, which may be identical or different, are selected from the group comprising H, CnH2n-1, a linear or branched alkyl group having 1 to 6 carbons, or together form an aromatic or aliphatic ring with 5 or 6 atoms; R3 is —CO—CH3, —NHOH, —OH, or —OR6 where R6 is a linear or branched alkyl group having 1 to 6 carbon atoms; R4 is H, linear or branched alkyl group having from 1 to 6 atoms, phenyl, benzyl, —CF3 or CF2CF3, vinyl or allyl; R5, R7, R8 are hydrogen atoms; or R3 and R4, R4 and R5, or R7 and R8 together form a ring, fused to the benzene, aromatic or aliphatic ring with 5 or 6 atoms comprising from 1 to 2 heteroatoms selected independently from the group comprising N, O, and use thereof in the medical field.Type: ApplicationFiled: February 15, 2012Publication date: December 13, 2012Inventors: Giancarlo Naccari, Sergio Baroni
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Publication number: 20120301402Abstract: A method for assessing if a subject has or is at risk of developing cardiac arrhythmia is described. The method includes determining the activity of Rap1A protein in a bodily sample of the subject and comparing the activity of Rap1A protein from the bodily sample of the subject to at least one Rap1A control. A decreased level of Rap1A activity in the bodily sample of the subject as compared to the at least one Rap1A control indicates that the subject is at risk of developing or has cardiac arrhythmia. Methods for evaluating the efficacy of treatment of a subject having decreased Rap1A activity with an antiarrhythmic agent are also described.Type: ApplicationFiled: April 27, 2012Publication date: November 29, 2012Applicant: NATIONWIDE CHILDREN'S HOSPITAL, INC.Inventors: Maqsood Ahmed Chotani, John Anthony Bauer, Mandar Shankar Joshi, Selvi Chrysolyte Jeyaraj
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Patent number: 8318779Abstract: The present invention concerns lysine related derivatives, their use as protease inhibitors, in particular as HIV aspartyl protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. The present invention also concerns combinations of the present lysine related derivatives with another anti retroviral agent. It further relates to their use in assays as reference compounds or as reagents.Type: GrantFiled: May 30, 2007Date of Patent: November 27, 2012Assignee: Janssen R&D IrelandInventors: Tim Hugo Maria Jonckers, Inge Dierynck, Stefaan Julien Last, Herman De Kock
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Patent number: 8309608Abstract: The present invention relates to the use of compounds which enhance the transcription of endothelial nitric oxide synthase (eNOS) for treating stem and progenitor cells in the cell therapy of patients with ischemic heart diseases such as coronary heart disease or ischemic cardiomyopathy. Treatment of such cells which are isolated from bone marrow, for example, with an eNOS transcription enhancer prior to their administration improves their functional activity and ameliorates neovascularization of the heart and cardiac regeneration.Type: GrantFiled: November 2, 2004Date of Patent: November 13, 2012Assignee: Sanofi-Aventis Deutschland GmbHInventors: Andreas Zeiher, Stefanie Dimmeler, Christopher Heeschen, Hartmut Ruetten
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Patent number: 8309603Abstract: This invention is directed to a feed composition and method of affecting the carcass composition by increasing the lean mass, reducing the fat mass, and/or reducing the percent fat mass comprising SARM compounds.Type: GrantFiled: March 23, 2010Date of Patent: November 13, 2012Assignee: University of Tennessee Research FoundationInventors: James T. Dalton, Duane D. Miller, Jeff Kearbey
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Publication number: 20120264823Abstract: The invention relates to compounds of Formula (I): (A?)x-(A)-(B)—(Z)-(L)-C(?O)NH2 or pharmaceutically acceptable salts or solvates thereof, wherein: (A) is heteroaryl or aryl; each (A?), if present, is indepedently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A?) is substituted with 0, 1, 2 or 3 substituents independently chosen from halo, haloalkyl, aryl, arylalkoxy, alkyl, alkoxy, cyano, sulfonyl, sulfinyl, and carboxamide; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is —NH—; and (L) is —(CH2)mCR1,R2—, wherein m is 0, 1, 2, 3, 4, 5, or 6, and wherein R1 and R2 are each independently hydrogen or C1-C6 alkyl; provided that, if (L) is —CH2— or —CH(CH3)—, then X is not 0. The compounds of the invention are useful in the treatment of diseases such as cancer and neurodegenerative diseases.Type: ApplicationFiled: April 19, 2010Publication date: October 18, 2012Inventors: Alberto Ortega Muñoz, Julio Castro-Palomino Laria, Matthew Colin Thor Fyfe
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Publication number: 20120251632Abstract: The invention provides a method of improving one or more clinical outcomes of an individual experiencing an acute respiratory attack. The acute respiratory attack may include acute reversible bronchospasm, severe acute bronchospasm, or acute exacerbation of asthma. The method includes administering to an individual suffering from an acute respiratory attack an effective amount of bedoradrine or a pharmaceutically acceptable salt thereof in combination with a standard of care (SOC) treatment regimen.Type: ApplicationFiled: June 15, 2012Publication date: October 4, 2012Inventors: Kazuko MATSUDA, Yuichi Iwaki, Kirk W. Johnson
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Publication number: 20120231070Abstract: The invention provides a method for obtaining local anesthetics encapsulated in liposomes, such as multi vesicular liposomes, with high encapsulation efficiency and slow release in vivo. When the encapsulated anesthetic is administered as a single intracutaneous dose, the duration of anesthesia and half-life of the drug at the local injection site is increased as compared to injection of unencapsulated anesthetic. The maximum tolerated dose of the encapsulated anesthetic is also markedly increased in the liposomal formulation over injection of unencapsulated anesthetic. These results show that the liposomal formulation of local anesthetic is useful for sustained local infiltration and nerve block anesthesia.Type: ApplicationFiled: May 21, 2012Publication date: September 13, 2012Applicant: PACIRA PHARMACEUTICAL, INC.Inventors: Sinil Kim, Taehee Kim, Sharad Murdande
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Patent number: 8236334Abstract: Disclosed is a method for protecting a tree from insects by injecting the tree with a fungicide and/or an antibiotic, and applying a composition to the surface of the tree, said composition comprising water, an insect repellent, an antihistamine, and an insect poison.Type: GrantFiled: September 6, 2005Date of Patent: August 7, 2012Inventor: James S. Bass
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Patent number: 8236826Abstract: An object of the present invention is to provide a medicinal drug much improved in anti tumor activity and excellent in safety. According to the present invention, there is provided a medicinal drug containing a compound represented by the following general formula (1) or a salt thereof as an active ingredient: [Formula 1] wherein X1 represents a nitrogen atom or a group —CH?, R1 represents a group —Z—R6, in which Z represents a group —CO—, a group —CH(OH)— or the like, R6 represents a 5- to 15-membered monocyclic, dicyclic or tricyclic saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms, R2 represents a hydrogen atom or a halogen atom, Y represents a group —O—, a group —CO—, a group —CH(OH)— or a lower alkylene group, and A represents [Formula 2] wherein R3 represents a hydrogen atom, a lower alkoxy group or the like, p represents 1 or 2, R4 represents an imidazolyl lower alkyl group or the like.Type: GrantFiled: December 4, 2006Date of Patent: August 7, 2012Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hironori Matsuyama, Kenji Ohnishi, Takashi Nakagawa, Hideki Takasu, Makoto Sakamoto, Kumi Higuchi, Keisuke Miyajima, Satoshi Yamada, Masaaki Motoyama, Yutaka Kojima, Koichi Yasumura, Takeshi Kodama, Shun Otsuji, Keizo Kan, Takumi Sumida
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Patent number: 8222453Abstract: The present invention provides novel benzamide derivatives of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables A, W, Y, Z, R8, and R9 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.Type: GrantFiled: June 7, 2007Date of Patent: July 17, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Eldon Scott Priestley, Xiaojun Zhang
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Publication number: 20120178697Abstract: The Wnt signaling pathways are involved in embryo development as well as in tumorigenesis. Dishevelled (Dvl) tranduces Wnt signals from the receptor Frizzled (Fz) to downstream components in canonical and non-canonical Wnt signaling pathways, and the Dvl PDZ domain plays an essential role in both pathways, and the Dvl PDZ domain binds directly to Fz receptors. In the present invention using NMR-assisted virtual ligand screening, several compounds were identified and were found to bind to the Dvl PDZ domain. Molecular dynamics simulation was used to analyze the binding between the PDZ domain and these compounds in detail. These compounds provide a basis for rational design of high-affinity inhibitors of the PDZ domain, which can block Wnt signaling by interrupting the Fz-Dvl interaction.Type: ApplicationFiled: April 1, 2005Publication date: July 12, 2012Inventors: Jie Zheng, Jufang Shan, Dianqing Wu
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Publication number: 20120178785Abstract: Compounds, compositions and methods are provided which are useful in the treatment of conditions such as central or peripheral nervous system disorders through the modulation of potassium ion flux through voltage-dependent potassium channels and/or depressing cortical and/or peripheral neuron activity are disclosed. Novel derivatives of N-phenylanthranilic acid are also disclosed.Type: ApplicationFiled: March 20, 2012Publication date: July 12, 2012Applicant: Ramot at Tel-Aviv University Ltd.Inventors: Bernard ATTALI, Asher Peretz
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Publication number: 20120157539Abstract: The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.Type: ApplicationFiled: January 31, 2012Publication date: June 21, 2012Inventors: James T. DALTON, Christina BARRETT, Duane D. MILLER, Seoung-Soo HONG, Yali HE, Michael L. MOHLER, Ramesh NARAYANAN, Zhongzhi WU
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Publication number: 20120142671Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.Type: ApplicationFiled: November 1, 2011Publication date: June 7, 2012Applicant: Portola Pharmaceuticals, Inc.Inventors: Zhaozhong J. Jia, Yonghong Song, Qing Xu, Brian Kane, Shawn M. Bauer, Anjali Pandey
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Publication number: 20120122787Abstract: The present invention is directed to, inter alia, methods of treating or ameliorating an effect of a polycystic disease. This method include administering to a patient in need thereof an amount of a modulator of a histone deacetylase (HDAC) path-way, which is sufficient to treat or ameliorate an effect of a polycystic disease, particularly a polycystic kidney disease.Type: ApplicationFiled: July 9, 2010Publication date: May 17, 2012Inventor: Rong Li
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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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Publication number: 20120114633Abstract: Organic compounds showing the ability to inhibit effector toxin secretion or translocation mediated by bacterial type III secretion systems are disclosed. The disclosed type III secretion system inhibitor compounds are useful for combating infections by Gram-negative bacteria such as Salmonella spp., Shigella flexneri, Pseudomonas spp., Yersinia spp., enteropathogenic and enteroinvasive Escherichia coli, and Chlamydia spp. having such type III secretion systems.Type: ApplicationFiled: April 6, 2010Publication date: May 10, 2012Inventors: Donald T. Moir, Daniel Aiello, Norton P. Peet, John D. Williams