Nitrogen Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/351)
  • Publication number: 20140256774
    Abstract: A method of treating at least one of inflammation, psoriasis, and/or hypertension comprising administering to a patient in need there of an effective gamma-ketoaldehyde scavenging amount of a gamma-ketoaldehyde scavenging compound.
    Type: Application
    Filed: July 12, 2012
    Publication date: September 11, 2014
    Applicant: VANDERBILT UNIVERSITY
    Inventors: L. Jackson Roberts, Venkataraman Amarnath, David G. Harrison
  • Publication number: 20140256748
    Abstract: 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid is useful in the modulation of blood or serum uric acid levels. In some embodiments, 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid is used in the treatment or prevention of disorders related to aberrant levels of uric acid. In some embodiments, 2-((3-(4-cyanonaph-thalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid is used for reducing serum uric acid levels in a human. Also described herein are compositions comprising 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid, and their use in the modulation of blood or serum uric acid levels.
    Type: Application
    Filed: October 2, 2012
    Publication date: September 11, 2014
    Inventors: Li-Tain Yeh, Barry D. Quart
  • Publication number: 20140243362
    Abstract: The present invention is directed to novel retinoid-related orphan receptor gamma (ROR?) modulators of formula (I), processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR? wherein R1 to R7 are as defined in claim 35.
    Type: Application
    Filed: September 25, 2012
    Publication date: August 28, 2014
    Inventors: Veronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le
  • Publication number: 20140243335
    Abstract: This invention provides compounds of formula (I): wherein R1, R1b, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: May 5, 2014
    Publication date: August 28, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Emily F. Calderwood, Kenneth M. Gigstad, Alexandra E. Gould, Sean J. Harrison, He Xu
  • Patent number: 8815917
    Abstract: Described herein is the DP2 antagonist [2?-(3-benzyl-1-ethyl-ureidomethyl)-6-methoxy-4?-trifluoromethyl-biphenyl-3-yl]-acetic acid, or a pharmaceutically acceptable salt thereof. Also described are methods of preparing the DP2 antagonist, or a pharmaceutically acceptable salt thereof. Also described herein are pharmaceutical compositions suitable for administration to a mammal that include the DP2 antagonist, or a pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating respiratory diseases or conditions, allergic diseases or conditions, inflammatory diseases or conditions, as well as other prostaglandin D2-dependent or prostaglandin D2-mediated diseases or conditions.
    Type: Grant
    Filed: July 29, 2010
    Date of Patent: August 26, 2014
    Assignee: Panmira Pharmaceuticals, LLC
    Inventors: Jason Edward Brittain, Brian Andrew Stearns, Christopher David King, Kevin Ross Holme
  • Publication number: 20140235637
    Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 21, 2014
    Applicant: InterMune, Inc.
    Inventors: Karl Kossen, Scott D. Seiwert, Vladimir Serebryany, Donald Ruhrmund, Leonid D. Beigelman, Luca Francesco Mario Raveglia, Stefania Vallese, Ivana Bianchi, Tao Hu
  • Patent number: 8809329
    Abstract: The present invention provides a method for diagnosing schizophrenia, and a schizophrenia diagnostic reagent or device for use in the method. The present invention further provides a therapeutic or ameliorating agent for schizophrenia, which is effective for the treatment or amelioration of schizophrenia. The therapeutic or ameliorating agent for schizophrenia contains a carbonyl scavenger or a carbonyl-modified protein formation inhibitor as an active ingredient. The method for diagnosing schizophrenia according to the present invention includes measuring at least one parameter in a subject, the parameter being selected from the group consisting of: (1) a genetic abnormality of glyoxalase I gene; (2) the expression level or activity of glyoxalase I in a biological sample; (3) the amount of a carbonyl compound or a carbonyl-modified protein that is a protein modified with the carbonyl compound; and (4) the amount of pyridoxal in a biological sample.
    Type: Grant
    Filed: July 31, 2008
    Date of Patent: August 19, 2014
    Assignees: Tokyo Metropolitan Institute of Medical Science, Renascience Co., Ltd.
    Inventors: Masanari Itokawa, Toshio Miyata, Makoto Arai
  • Patent number: 8795630
    Abstract: Compounds useful for the early diagnosis of malignant tumors, multiple sclerosis, and especially Alzheimer's Disease and related dementias; especially compounds of Formula (I) wherein R1 is selected from the group consisting of hydrogen, cyano, fluoro, iodo, alkyl, and aryl; R2 is selected from the group consisting of hydrogen, alkyl, and aryl; X is selected from the group consisting of CH2, CH2O, oxygen, OCH2, CH2S, SCH2, NH, N-alkyl, and N-aryl; Y is an optional spacer group, absent or selected from the group consisting of oxygen, sulfur, NH, N-alkyl, and N-aryl; and Z is selected from the group consisting of alkyl substituted with cyano, fluoro, or iodo and aryl substituted with cyano, fluoro, or iodo. In a preferred embodiment, R1 and R2 are hydrogen, X is CH2O, Y is absent, and Z is phenyl substituted with fluoro, cyano, or iodo. In some embodiments, Z is more specifically 18F-phenyl or 123I-phenyl or 131I-phenyl. Other compounds are also provided.
    Type: Grant
    Filed: August 28, 2009
    Date of Patent: August 5, 2014
    Assignee: Treventis Corporation
    Inventors: Sultan Darvesh, Eric Joy, Earl Martin, Ian Macdonald, Ian Pottie
  • Patent number: 8791147
    Abstract: The present invention relates generally to novel calcimimetic compounds and pharmaceutical compositions comprising them. The invention also relates to methods of treating of diseases or disorders related to the function of the calcium sensing receptor using the compounds represented in Formula (I). Where Cy1 is pyridinonyl, pyridinyl, quinolinyl or 9-ethyl-9H-beta-carbolinyl, each of which optionally substituted and where Cy2 is phenyl naphthyl.
    Type: Grant
    Filed: October 7, 2009
    Date of Patent: July 29, 2014
    Assignee: Amgen Inc.
    Inventors: Christopher Fotsch, Paul Harrington
  • Patent number: 8778978
    Abstract: Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof compositions that are hydroxybenzoate salts of E-metanicotine-type compounds. The formation of hydroxybenzoate salts of the E-metanicotine compounds is also useful in purifying the E-metanicotine compounds, as the hydroxybenzoate salts tend to crystallize out, leaving impurities such as Z-metanicotine compounds, and compounds where the double bond has migrated, in solution. If desired, the hydroxybenzoate salts can be converted to either the free base (the E-metanicotine) or to another pharmaceutically acceptable salt form.
    Type: Grant
    Filed: October 3, 2013
    Date of Patent: July 15, 2014
    Assignee: Targacept, Inc.
    Inventors: Julio A. Munoz, John Genus, James R. Moore
  • Patent number: 8779197
    Abstract: 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: Grant
    Filed: October 10, 2008
    Date of Patent: July 15, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Weichuan Caroline Chen, Paul Krenitsky, Pramod Joshi, Andreas Termin, Dean Wilson
  • Publication number: 20140187539
    Abstract: Heteroaryloxy-substituted benzoic acid amides of general formula I wherein the groups R1 to R7 as well as X and Y are defined according to claim 1, including the tautomers, the stereoisomers, the mixtures and the salts thereof. The compounds according to the invention are suitable for the treatment of respiratory complaints, particularly COPD and asthma.
    Type: Application
    Filed: March 4, 2014
    Publication date: July 3, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Holger WAGNER, Elke LANGKOPF, Frank HIMMELSBACH, Rolf GOEGGEL, Birgit JUNG
  • Patent number: 8765732
    Abstract: The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: July 1, 2014
    Assignee: Epizyme, Inc.
    Inventors: Kevin Wayne Kuntz, Richard Chesworth, Kenneth William Duncan, Heike Keilhack, Natalie Warholic, Christine Klaus, Sarah Kathleen Knutson, Timothy James Nelson Wigle, Masashi Seki, Syuji Shirotori, Satoshi Kawano
  • Patent number: 8765790
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Grant
    Filed: July 3, 2013
    Date of Patent: July 1, 2014
    Assignee: H. Lundbeck A/S
    Inventors: Jørgen Eskildsen, Anette Graven Sams, Ask Püschl
  • Publication number: 20140178374
    Abstract: The disclosure relates to BAX activators and therapeutic uses relates thereto. In certain embodiments, the disclosure relates to methods of treating or preventing cancer, such as lung cancer, comprising administering a therapeutically effective amount of a pharmaceutical composition comprising a compound disclosed herein or pharmaceutically acceptable salt to a subject in need thereof.
    Type: Application
    Filed: August 17, 2012
    Publication date: June 26, 2014
    Applicants: BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM, EMORY UNIVERSITY
    Inventors: Xingming Deng, Jia Zhou, Chunyong Ding
  • Publication number: 20140171472
    Abstract: The present invention provides pharmaceutical compositions comprising dosage units of pyridoxamine, or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier, and methods for their use in limiting the progression of renal disease and/or diabetic complications in human diabetic patient.
    Type: Application
    Filed: February 20, 2014
    Publication date: June 19, 2014
    Applicant: NephroGenex, Inc.
    Inventors: Thorsten Degenhardt, Robert Schotzinger, J. Wesley Fox
  • Publication number: 20140155420
    Abstract: The invention provides small molecule inhibitors of EYA2 phosphatase activity and EYA2 binding to Six1. These inhibitors are proposed for use in methods of treating cancer in a subject, such as those involving Six1 and/or EYA2 disregulation. In some embodiments, the invention further provides for the administration of a second cancer therapy to the subject.
    Type: Application
    Filed: January 10, 2012
    Publication date: June 5, 2014
    Applicants: The Regents of the University of Colorado, a body corporate, Department of Health and Human Services
    Inventors: Rui Zhao, Heide L. Ford, Noel Southall, Erika Englund, Samarjit Patnaik, Marc Ferrer, Wei Zheng, Seameen Dehdashti, Juan Marugan
  • Publication number: 20140148438
    Abstract: There is provided compositions and methods for the treatment of respiratory conditions such as pulmonary hypertension and sickle-cell disease in a patient in need thereof. The composition and method are for treating a patient in need thereof by inhalation of a composition containing amino acid ester compounds comprising at least one nitric oxide releasing group and pharmaceutical salts thereof.
    Type: Application
    Filed: September 22, 2011
    Publication date: May 29, 2014
    Inventor: Michael Farber
  • Publication number: 20140140932
    Abstract: The present disclosure provides functionalized magnetic nanoparticles (MNPs) comprising a functional group that binds to ?-amyloid deposits and/or neurofibrillary tangles. The present disclosure provides compositions comprising the functionalized MNPs, and methods of using the functionalized MNPs in imaging ?-amyloid deposits and neurofibrillary tangles.
    Type: Application
    Filed: April 4, 2012
    Publication date: May 22, 2014
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventor: Masoud Akhtari
  • Publication number: 20140142083
    Abstract: The present invention relates to substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Application
    Filed: April 13, 2012
    Publication date: May 22, 2014
    Applicant: EPIZYME, INC.
    Inventors: Kevin Wayne Kuntz, Richard Chesworth, Kenneth William Duncan, Heike Keilhack, Natalie Warholic, Christine Klaus, Sarah K. Knutson, Timothy James Nelson Wigle, Masashi Seki
  • Publication number: 20140135320
    Abstract: The present invention relates to antimalarial compounds and their use against protozoa of the genus Plasmodium, including drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds.
    Type: Application
    Filed: November 8, 2013
    Publication date: May 15, 2014
    Applicant: Jacobus Pharmaceutical Company, Inc.
    Inventors: Gavin David Heffernan, David Penman Jacobus, Kurt William Saionz, Guy Alan Schiehser, Hong-Ming Shieh, Wenyi Zhao
  • Publication number: 20140135360
    Abstract: The present invention relates to antimalarial compounds and their use against protozoa of the genus Plasmodium, including drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds.
    Type: Application
    Filed: November 8, 2013
    Publication date: May 15, 2014
    Applicant: Jacobus Pharmaceutical Company, Inc
    Inventors: Gavin David Heffernan, David Penman Jacobus, Guy Alan Schiehser, Hong-Ming Shieh, Wenyi Zhao
  • Patent number: 8722895
    Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.
    Type: Grant
    Filed: April 9, 2013
    Date of Patent: May 13, 2014
    Assignee: Akebia Therapeutics, Inc.
    Inventors: Richard M. Kawamoto, Shengde Wu, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer, Namal C. Warshakoon
  • Publication number: 20140128363
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.
    Type: Application
    Filed: January 14, 2014
    Publication date: May 8, 2014
    Inventors: Matthew Frank Brown, Ye Che, Anthony Marfat, Michael Joseph Melnick, Justin Ian Montgomery, Usa Reilly
  • Publication number: 20140128393
    Abstract: The present invention relates to methods of treating cancer by administering the EZH2 inhibitor compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Application
    Filed: October 15, 2013
    Publication date: May 8, 2014
    Applicant: EPIZYME, INC.
    Inventors: Sarah K. Knutson, Natalie Warholic, Heike Keilhack
  • Publication number: 20140121217
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein A, Y, L, R1, W1 and W2 are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: January 2, 2014
    Publication date: May 1, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Lijun Sun, Jun Jiang, Yu Xie
  • Publication number: 20140107122
    Abstract: The present invention relates to substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 17, 2014
    Inventors: Kevin Wayne Kuntz, John Emmerson Campbell, Masashi Seki
  • Patent number: 8697669
    Abstract: The invention relates to agents containing a folic acid, vitamin B6 and vitamin B12 and to the use thereof in hyperhomocystenemia for controlling homocysteine levels. The inventive agents are particularly suitable for preventive and acute treatment of vascular diseases of pregnant women and neurodegenerative diseases and are particularly advantageous in cases of hyperhomocysteinemia whose treatment with homocysteine level reducing agents causes secondary effects. Pharmaceutical agents and food supplements comprising the corresponding active substance combination, agents in the form of commercial packages containing corresponding combination preparations or monopreparations for a combined application are, in particular, also disclosed.
    Type: Grant
    Filed: March 1, 2006
    Date of Patent: April 15, 2014
    Assignee: Phrontier S.A.R.L.
    Inventor: Martin Goerne
  • Publication number: 20140088046
    Abstract: The present invention provides novel phenicol derivatives, their use for the treatment of infections in mammals, pharmaceutical composition containing these novel compounds, and methods for the preparation of these compounds.
    Type: Application
    Filed: September 5, 2013
    Publication date: March 27, 2014
    Applicant: ZOETIS LLC
    Inventors: Denis Billen, Michael Curtis, Richard Andrew Ewin, Richard M. Goodwin, Paul D. Johnson, Timothy Allan Johnson, Graham M. Kyne, Todd M. Maddux, Susan Mary Kult Sheehan, Rajendran Vairagoundar
  • Publication number: 20140088158
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: November 27, 2013
    Publication date: March 27, 2014
    Applicant: SANOFI
    Inventors: Josef PERNERSTORFER, Heinz-Werner KLEEMANN, Matthias SCHAEFER, Alena SAFAROVA, Marcel PATEK
  • Publication number: 20140088156
    Abstract: The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.
    Type: Application
    Filed: February 14, 2012
    Publication date: March 27, 2014
    Applicant: The Regents of the University of California
    Inventors: Bruce D. Hammock, Sung Hee Hwang, Aaron T. Wecksler, Christophe Morisseau
  • Publication number: 20140080874
    Abstract: The present invention provides methods for treating or limiting development of inflammatory disorders.
    Type: Application
    Filed: November 20, 2013
    Publication date: March 20, 2014
    Applicant: Vanderbilt University - Center for Technology Transfer and Commercialization
    Inventor: Billy G. Hudson
  • Patent number: 8664248
    Abstract: The present invention relates to methods of treating hepatitis C infection, HIV infection, AIDS, or AIDS-related complex, or inhibiting HIV replication by administering a compound of Formula I wherein: X is H or OH; Y is H or OH; R1 is H or halogen (F, Cl, Br, I); R2 is H or halogen (F, Cl, Br, I); R3 is H, C1-6 alkyl, C1-6 fluoroalkyl, or benzyl; R4 is H, C1-6 alkyl, or benzyl; and R5 is H or C1-6 alkyl; or pharmaceutically acceptable salts thereof, to a mammal.
    Type: Grant
    Filed: September 6, 2012
    Date of Patent: March 4, 2014
    Assignee: TaiMed Biologics, Inc.
    Inventors: Brent Richard Stranix, Guy Milot, Jean-Emmanuel Bouchard
  • Publication number: 20140051655
    Abstract: Alpha 4 inhibitors are used in treatment of inflammatory and autoimmune diseases, such as multiple sclerosis, Crohn's Disease, rheumatoid arthritis and asthma. Rare occurrences of progressive multifocal leucoencephalopathy during treatment with an alpha-4 agent suggest the possibility that it may be related to such treatment. Monitoring for the JC virus and educating caregivers and patients about the manifestations of progressive multifocal leucoencephalopathy can improve the safety of alpha 4 inhibitor therapy.
    Type: Application
    Filed: March 5, 2013
    Publication date: February 20, 2014
    Applicant: Elan Pharmaceuticals, Inc.
    Inventor: Elan Pharmaceuticals, Inc.
  • Publication number: 20140051668
    Abstract: Disclosed are novel compounds having the structure of Formula (I): which are useful for treating mammals for dependence upon substances of addiction, for example addiction to a dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and/or alcohol. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of a compound of Formula (I) and methods of using the compounds of Formula (I) in the treatment of addiction to a dopamine-producing agent.
    Type: Application
    Filed: August 13, 2013
    Publication date: February 20, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Carina E. Cannizzaro, Michael Graupe, Juan A. Guerrero, Yafan Lu, Robert G. Strickley, Chandrasekar Venkataramani, Jeff Zablocki
  • Publication number: 20140044806
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Application
    Filed: October 16, 2013
    Publication date: February 13, 2014
    Applicant: H. Lundbeck A/S
    Inventors: Jørgen Eskildsen, Anette Graven Sams, Ask Püschl
  • Publication number: 20140039014
    Abstract: Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof compositions that are hydroxybenzoate salts of E-metanicotine-type compounds. The formation of hydroxybenzoate salts of the E-metanicotine compounds is also useful in purifying the E-metanicotine compounds, as the hydroxybenzoate salts tend to crystallize out, leaving impurities such as Z-metanicotine compounds, and compounds where the double bond has migrated, in solution. If desired, the hydroxybenzoate salts can be converted to either the free base (the E-metanicotine) or to another pharmaceutically acceptable salt form.
    Type: Application
    Filed: October 3, 2013
    Publication date: February 6, 2014
    Applicant: Targacept, Inc.
    Inventors: Julio A. Munoz, John Genus, James R. Moore
  • Publication number: 20140031331
    Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: September 19, 2013
    Publication date: January 30, 2014
    Inventors: Wilhelm Amberg, Michael Ochse, Udo Lange, Andreas Kling, Berthold Behl, Wilfried Hornberger, Mario Mezler, Charles W. Hutchins
  • Publication number: 20140010898
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Application
    Filed: July 3, 2013
    Publication date: January 9, 2014
    Inventors: Jorgen Eskildsen, Anette Graven Sams, Ask Püschl
  • Publication number: 20130331382
    Abstract: The present invention provides for compounds of formula (I) wherein A1, A2, A3, A4, J, and X3 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, diabetes, obesity, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula I.
    Type: Application
    Filed: March 12, 2013
    Publication date: December 12, 2013
    Inventors: Robert D. HUBBARD, Le WANG, Chang H. PARK, Chaohong SUN, Keith F. McDANIEL, John K. PRATT, Todd N. SOLTWEDEL, Michael D. WENDT, John H. HOLMS, Dachun LIU, George S. SHEPPARD
  • Patent number: 8598213
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Grant
    Filed: July 6, 2012
    Date of Patent: December 3, 2013
    Assignee: H. Lundbeck A/S
    Inventors: Jørgen Eskildsen, Anette Graven Sams, Ask Püschl
  • Publication number: 20130317000
    Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Application
    Filed: May 21, 2013
    Publication date: November 28, 2013
    Applicants: XENON PHARMACEUTICALS INC., GENENTECH, INC
    Inventors: Sultan Chowdhury, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Qi Jia, Daniel Ortwine, Brian Safina, Shaoyi Sun, Daniel P. Sutherlin, Alla Yurevna Zenova
  • Publication number: 20130317001
    Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Application
    Filed: May 21, 2013
    Publication date: November 28, 2013
    Applicants: XENON PHARMACEUTICALS INC., GENENTECH, INC.
    Inventors: Jean-Christophe Andrez, Sultan Chowdhury, Shannon Marie Decker, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Qi Jia, Jun Li, Daniel F. Ortwine, Brian Safina, Tao Sheng, Shaoyi Sun, Daniel P. Sutherlin, Michael Scott Wilson, Alla Yurevna Zenova
  • Patent number: 8591928
    Abstract: A pesticide granule is provided that includes a base carrier particle. A liquid pesticide coating is applied to the particle surface. The coating may contain adjuvants. The coating has sufficient tack to adhere a second powdered pesticide to the carrier particle. The usage of tackifying agents to render the particle surface tacky enough to adhere powdered pesticide is reduced or eliminated. The powdered pesticide is sized to a mean diameter of less than 10% of the carrier diameter to promote adhesion. The synergistic rapid acting pesticide delivery associated with the granule results in the usage of less pesticide to control a given pest with reduced environmental impact. Bifenthrin is a representative of the liquid pesticide.
    Type: Grant
    Filed: January 3, 2011
    Date of Patent: November 26, 2013
    Assignee: The Andersons, Inc.
    Inventors: Timothy D. Birthisel, James R. Lynch, Matthew G. Johnston
  • Publication number: 20130310386
    Abstract: Methods for treating eye diseases associated with inflammation and/or vascular proliferation in subjects are disclosed. The methods include administering therapeutically effective amounts of a tranilast compound, in particular (E)-2-[[3-(3-Methoxy-4-propargyloxy)phenyl)-1-oxo-2-propenyl]amino]benzoic acid or (E)-2-[[3,4-Bis(difluoromethoxy)phenyl)-1-oxo-2-propenyl]amino]benzoic acid or pharmaceutically acceptable salts or solvates thereof.
    Type: Application
    Filed: November 10, 2011
    Publication date: November 21, 2013
    Applicant: Fibrotech Therapeutics Pty Ltd
    Inventors: Darren James Kelly, David Stapleton
  • Publication number: 20130310425
    Abstract: Polymorph forms of (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4-penten-2-amine p-hydroxybenzoate, and methods for their preparation, pharmaceutical composition containing said polymorph(s) and use, are disclosed. The polymorphs can be administered to patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, to treat and/or prevent such disorders.
    Type: Application
    Filed: May 14, 2013
    Publication date: November 21, 2013
    Applicant: Targacept, Inc.
    Inventors: Gary Maurice Dull, Julio A. Munoz
  • Patent number: 8586570
    Abstract: Peptidyl sensors comprise a metal-binding peptide and one or two kinase recognition sequences with a hydroxyamino acid that can be phosphorylated in the presence of a kinase.
    Type: Grant
    Filed: April 27, 2011
    Date of Patent: November 19, 2013
    Assignee: Massachusetts Institute of Technology
    Inventors: Barbara Imperiali, Elvedin Lukovic, Dora Carrico-Moniz
  • Publication number: 20130303568
    Abstract: 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: Application
    Filed: April 22, 2013
    Publication date: November 14, 2013
    Inventors: Nancy C. LAN, Yan Wang, Sui Xiong Cai
  • Patent number: 8580826
    Abstract: Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof compositions that are hydroxybenzoate salts of E-metanicotine-type compounds. The formation of hydroxybenzoate salts of the E-metanicotine compounds is also useful in purifying the E-metanicotine compounds, as the hydroxybenzoate salts tend to crystallize out, leaving impurities such as Z-metanicotine compounds, and compounds where the double bond has migrated, in solution. If desired, the hydroxybenzoate salts can be converted to either the free base (the E-metanicotine) or to another pharmaceutically acceptable salt form.
    Type: Grant
    Filed: October 26, 2011
    Date of Patent: November 12, 2013
    Assignee: Targacept, Inc.
    Inventors: Julio A. Munoz, John Genus, James R. Moore
  • Publication number: 20130295074
    Abstract: The present invention provides pharmaceutical compositions comprising dosage units of pyridoxamine, or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier, and methods for their use in limiting the progression of renal disease and/or diabetic complications in human diabetic patient.
    Type: Application
    Filed: July 5, 2013
    Publication date: November 7, 2013
    Inventors: Thorsten Degenhardt, Robert Schotzinger, J. Wesley Fox