Morpholines (i.e., Fully Hydrogenated 1,4- Oxazines) Patents (Class 514/231.2)
  • Patent number: 10233146
    Abstract: The present invention provides a compound having the structure: wherein X is C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, cyano, aryl, heteroaryl, alkylaryl, alkylheteroaryl, alkenylaryl, alkenylheteroaryl, alkynylaryl, alkynylheteroaryl, alkoxy, alkenyloxy, alkynyloxy, aryloxy, heteroaryloxy, acyl, alkylhydroxy, alkylamino, alkenylamino, alkynylamino, amido, carboxyl, or carboxyl ester, or forms an unsubstituted or substituted cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, indane or tetralin with Y, Y is H or forms an unsubstituted or substituted cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, indane or tetralin with X, or forms an unsubstituted or substituted monocycle with Z; and Z is H or forms an unsubstituted or substituted monocycle with Y; wherein when X and Y are both H, then X is C2 alkenyl or C2 alkynyl, and when Y is H forms a substituted cyclohexyl, cycloheptyl with X, the cyclohexyl is other than a trisubstituted cyclohexyl bearing CH3, i-Pr and (CH2)2CO2CH3 groups or CH3, i-Pr and (
    Type: Grant
    Filed: April 14, 2016
    Date of Patent: March 19, 2019
    Assignees: THE RESEARCH FOUNDATION FOR THE STATE UNIVERSITY OF NEW YORK, UNIVERSITY OF DUNDEE
    Inventors: Tadashi Honda, Wei Li, Suqing Zheng, Albena Dinkova-Kostova
  • Patent number: 10195198
    Abstract: Provided herein include methods and compositions for treating diseases or conditions. In some embodiments provided are methods for treating one or more diseases or conditions selected from the group consisting of hypertension, heart failure, dyspnea, and sleep apnea. In certain embodiments provided are methods that include administering a compound of formula (I) as disclosed herein. In some embodiments provided are methods that include administering a P2X3 and/or a P2X2/3 receptor antagonist.
    Type: Grant
    Filed: July 2, 2015
    Date of Patent: February 5, 2019
    Assignee: Afferent Pharmaceuticals, Inc.
    Inventors: Anthony P. Ford, Julian Paton
  • Patent number: 10196364
    Abstract: The present disclosure provides substituted pyrimidine carboxamides of Formula (I) and the pharmaceutically acceptable salts and solvates thereof wherein A1, X, A2, W1, W2, W3, E, Z, and R4 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.
    Type: Grant
    Filed: April 6, 2017
    Date of Patent: February 5, 2019
    Assignee: Purdue Pharma L.P.
    Inventors: Jeffrey Lockman, Chiyou Ni, Jae Hyun Park, Minnie Park, Bin Shao, Laykea Tafesse, Jiangchao Yao, Mark A. Youngman
  • Patent number: 10188106
    Abstract: The present invention relates to a pesticide composition intended for protecting plants, crops or seeds against fungal diseases or insect damages, and the corresponding methods of protection by application of the said composition. More precisely, the subject of the present invention is a pesticide composition based on a tetrazolyloxime derivative and a fungicide or an insecticide active substance or compound.
    Type: Grant
    Filed: May 19, 2015
    Date of Patent: January 29, 2019
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Pierre-Yves Coqueron, Marie-Claire Grosjean-Cournoyer, Pierre Hutin, Gilbert Spica, Arnd Voerste, Ulrike Wachendorff-Neumann
  • Patent number: 10139729
    Abstract: A resin composition for pattern reversal can be embedded between traces of the pattern of a stepped substrate formed on the substrate to be processed and can form a smooth film. A polysiloxane composition for coating used in the steps of forming an organic underlayer film on a semiconductor substrate, applying a silicon hard mask-forming composition onto the underlayer film and baking the applied silicon hard mask-forming composition to form a silicon hard mask, applying a resist composition onto the silicon mask to form a resist film, exposing the resist film to light and developing the resist film after exposure to give a resist pattern, etching the silicon mask, etching the underlayer film, applying the polysiloxane composition for coating onto the patterned organic underlayer film to expose an upper surface of the underlayer film by etch back, and etching the underlayer film to reverse the pattern.
    Type: Grant
    Filed: August 11, 2015
    Date of Patent: November 27, 2018
    Assignee: NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Hiroaki Yaguchi, Makoto Nakajima, Wataru Shibayama, Satoshi Takeda, Hiroyuki Wakayama, Rikimaru Sakamoto
  • Patent number: 9902720
    Abstract: A series of substituted pyrazolo[1,5-a]pyridine derivatives, being potent modulators of human TNF? activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: December 8, 2014
    Date of Patent: February 27, 2018
    Assignee: UCB BIOPHARMA SPRL
    Inventors: Daniel Christopher Brookings, Victoria Elizabeth Jackson, Boris Kroeplien
  • Patent number: 9756863
    Abstract: The present invention relates to a novel bacterial strain belonging to Lysobacter capsici species, Lysobacter capsici AZ78, bacteria of said bacterial strain, and bacterial preparations related thereto, as well as to uses of the above for preparing a plant protection product—as well as to plant protection products comprising any of the above as well as to further related uses and methods.
    Type: Grant
    Filed: April 22, 2014
    Date of Patent: September 12, 2017
    Assignee: Fondazione Edmund Mach
    Inventors: Gerardo Puopolo, Ilaria Pertot
  • Patent number: 9650664
    Abstract: Use of photochemically cleavable compounds in course of one or multi-photon irradiation experiments.
    Type: Grant
    Filed: October 3, 2012
    Date of Patent: May 16, 2017
    Assignee: Femtonics KFT
    Inventors: Imre Gyula Csizmadia, Zoltan Mucsi, Gergely Szalay, Attila Kaszas, Csilla Lukacsne Haveland, Orsolya Majercsik, Attila Potor, Gergely Katona, Jozsef Balazs Rozsa, Dorina Gundisch, Balazs Chiovini, Denes Palfi
  • Patent number: 9550788
    Abstract: The invention relates to substituted aminoindanes and analogs thereof of formula I and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.
    Type: Grant
    Filed: July 24, 2014
    Date of Patent: January 24, 2017
    Assignee: SANOFI
    Inventors: Nils Rackelmann, Laurent Bialy, Heinrich Englert, Klaus Wirth, Petra Arndt, John Weston, Uwe Heinelt, Markus Follmann
  • Patent number: 9527823
    Abstract: The invention provides hydroxybupropion analogs capable of inhibiting the reuptake of one or more monoamines and/or acting as antagonists at nicotinic acetylcholine receptors. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin and/or may selectively bind to one or more nicotinic acetylcholine receptor subtypes. Such compounds may be used to treat conditions that are responsive to modification of monoamine levels and/or antagonism of nicotinic acetylcholine receptors, including drug dependency, depression, and obesity.
    Type: Grant
    Filed: November 10, 2014
    Date of Patent: December 27, 2016
    Assignees: Research Triangle Institute, Dignity Health, Virginia Commonwealth University
    Inventors: Frank Ivy Carroll, Bruce E. Blough, Hernan A. Navarro, S. Wayne Mascarella, Ana Zamfira Muresan, M. Imad Damaj, Ronald J. Lukas
  • Patent number: 9493396
    Abstract: The invention relates to naphthalene compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine for the treatment of diseases, disorders associated with the modulation of calcium sensing receptor modulators (Ca SR). The invention also relates to pharmaceutical compositions containing such compounds in treating diseases disorders associated with calcium sensing receptor modulators (Ca SR) channel modulators.
    Type: Grant
    Filed: August 26, 2014
    Date of Patent: November 15, 2016
    Assignee: LUPIN ATLANTIS HOLDINGS SA
    Inventors: Prathap Sreedharan Nair, Ganesh Bhausaheb Gudade, Mahadeo Bhaskar Tryambake, Chetan Sanjay Pawar, Sanjeev Anant Kulkarni, Venkata P. Palle, Rajender Kumar Kamboj
  • Patent number: 9452117
    Abstract: Alkyl nitrate ester compounds are provided for the delivery of nitric oxide to targeted muscle tissues, and in particular, to normal and dystrophic muscles. In one aspect, nitrate ester compounds are provided having the following formula: wherein, R1 is ONO2, CH2ONO2, CnH2n+1OH, CnH2n+1OH, CH3, CH2CH3, CH2CH2CH3, or H; R2 is ONO2, CH2ONO2, Cn?H2n?+1OH, Cn?H2n?+1OH, CH3, CH2CH3, CH2CH2CH3, or H; R3 is ONO2, CH2ONO2, Cn??H2n?+1OH, Cn?H2n?+1OH, CH3, CH2CH3, CH2CH2CH3, or H; and R4 is ONO2, CH2ONO2, Cn??H2n?+1OH, Cn?H2n?+1OH, CH3, CH2CH3, CH2CH2CH3, or H; wherein n is an integer from 0 to 9, n? is an integer from 0 to 9, and n? is an integer from 0 to 9, and n+n?+n??9, and wherein at least one of R1, R2, and R3 is an ester nitrate selected from the group consisting of ONO2, CH2ONO2, and combinations thereof.
    Type: Grant
    Filed: May 31, 2012
    Date of Patent: September 27, 2016
    Assignee: The Charlotte-Mecklenburg Hospital Authority
    Inventors: Guqi Wang, Qi Long Lu
  • Patent number: 9375431
    Abstract: The present invention provides 2,4-disubstituted pyrimidine compounds useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: March 3, 2015
    Date of Patent: June 28, 2016
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Kwangho Lee, Deqiang Niu, Russell C. Petter, Matthew F. Baevsky, Juswinder Singh
  • Patent number: 9340534
    Abstract: Described herein are compounds of formula I compositions and methods for the treatment of diseases affecting the eye, including glaucoma or ocular hypertension.
    Type: Grant
    Filed: July 27, 2015
    Date of Patent: May 17, 2016
    Assignee: ALLERGAN, INC.
    Inventors: Robert M. Burk, Todd S. Gac
  • Patent number: 9309219
    Abstract: Provided are 4?-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.
    Type: Grant
    Filed: July 26, 2013
    Date of Patent: April 12, 2016
    Assignee: Celgene Corporation
    Inventors: Hon-Wah Man, Roger Shen-Chu Chen, George W. Muller, Alexander L. Ruchelman, Ehab M. Khalil, Weihong Zhang
  • Patent number: 9040528
    Abstract: The present invention relates to compounds of Formula (I): to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to methods for their preparation.
    Type: Grant
    Filed: January 13, 2014
    Date of Patent: May 26, 2015
    Assignee: AstraZeneca AB
    Inventors: Kevin Barvian, Gregory Steven Basarab, Madhusudhan Reddy Gowravaram, Sheila Irene Hauck, Fei Zhou
  • Publication number: 20150133297
    Abstract: The present invention relates to new antifungal compositions and their use in the treatment of agricultural products.
    Type: Application
    Filed: April 25, 2013
    Publication date: May 14, 2015
    Inventors: Jacobus Stark, Eva Louise Wilhelmine Sack
  • Publication number: 20150126436
    Abstract: The present invention provides a method of treatment of Scedosporium spp.
    Type: Application
    Filed: May 13, 2013
    Publication date: May 7, 2015
    Applicant: BIODIEM LIMITED
    Inventors: Julie Phillips, Tania Sorrell, Sharon Chen
  • Patent number: 9006454
    Abstract: The invention relates to compounds of formula (I) wherein R1, R2, X1, X2, Y, Ra, Rb, Q have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis and also in the treatment of cancer disorders.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: April 14, 2015
    Assignee: Merck Serono S.A.
    Inventors: Siva Sanjeeva Rao Thunuguntla, Hosahalli Subramanya, Satish Reddy Kunnam, Sekhar Reddy Sanivaru Vijay, Chakrapani Bingi, Raviraj Kusanur, Matthias Schwarz, Michael Arlt
  • Patent number: 8999365
    Abstract: A compound of formula I: wherein R1 is a straight or branched alkyl group containing 8 to 16 carbon atoms at the 2- or 3-position of the morpholino ring, and R2 is a straight or branched alkyl group containing 2 to 10 carbon atoms, substituted with a hydroxy group except in the alpha-position, the sum of the carbon atoms in the groups R1 and R2 being at least 10 and preferably 10 to 20, is used to prevent biofilm formation on a surface. The compounds are particularly useful as coatings or treatments for medical devices, including stents, catheters and wire guides.
    Type: Grant
    Filed: February 1, 2006
    Date of Patent: April 7, 2015
    Assignee: Sinclair Pharmaceuticals Limited
    Inventors: Jonathan Lane, Olof Torgny Sjodin
  • Publication number: 20150087642
    Abstract: Provided herein are methods of utilizing bile acid transport inhibitors and/or enteroendocrine peptide enhancing agents for the treatment of obesity, diabetes, and inflammatory gastrointestinal conditions.
    Type: Application
    Filed: November 26, 2014
    Publication date: March 26, 2015
    Inventors: Bronislava GEDULIN, Andrew A. YOUNG, Howard E. GREENE
  • Publication number: 20150080369
    Abstract: The present invention is directed to novel retinoid-related orphan receptor gamma (ROR?) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR?.
    Type: Application
    Filed: April 25, 2013
    Publication date: March 19, 2015
    Inventors: Veronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le, Lena Shukla
  • Patent number: 8975249
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: October 31, 2011
    Date of Patent: March 10, 2015
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Kwangho Lee, Deqiang Niu, Russell C. Petter, Matthew F. Baevsky, Juswinder Singh
  • Patent number: 8906908
    Abstract: The invention provides hydroxybupropion analogues capable of inhibiting the reuptake of one or more monoamines and/or acting as antagonists at nicotinic acetylcholine receptors. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin and/or may selectively bind to one or more nicotinic acetylcholine receptor subtypes. Such compounds may be used to treat conditions that are responsive to modification of monoamine levels and/or antagonism of nicotinic acetylcholine receptors, including drug dependency, depression, and obesity.
    Type: Grant
    Filed: November 19, 2012
    Date of Patent: December 9, 2014
    Assignees: Research Triangle Institute, Dignity Health, Virginia Commonwealth University
    Inventors: F. Ivy Carroll, Bruce E. Blough, Hernan A. Navarro, S. Wayne Mascarella, Ana Zamfira Muresan, M. Imad Damaj, Ronald J. Lukas
  • Patent number: 8895077
    Abstract: The present invention relates to methods for preventing or treating infectious diseases caused by extracellular microorganisms, such as bacteria and fungi, by systemically administering to a patient a compound containing gallium. The extracellular microorganisms targeted by the present methods include methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus faecalis (VRE), E. coli O157:H7, fluoroquinolone-resistant Salmonella typhi, and the like. Furthermore, in the present methods, gallium compounds can be co-administered with one or more conventional antimicrobial agents to treat infectious diseases with reduced risks of creating multi-drug resistant pathogens. The methods of the present invention is also applicable to those microorganisms, such as ulcer-causing Helicobacter pylori, complete eradication of which so far has been difficult to achieve.
    Type: Grant
    Filed: March 28, 2008
    Date of Patent: November 25, 2014
    Assignee: Mount Sinai School of Medicine
    Inventors: Daniel P. Perl, Sharon Moalem
  • Publication number: 20140329811
    Abstract: The present invention provides a method for preferentially reducing the proliferation of cystic epithelial cells in the kidney or bile duct in a mammal in need thereof by administering a 20-HETE synthesizing enzyme inhibitor or a 20-HETE antagonist to the mammal in an amount sufficient to preferentially reduce the proliferation of cystic epithelial cells over normal epithelial cells such as tubule epithelial cells in the kidney or bile duct. The present invention also provides a method for preventing or treating autosomal dominant polycystic kidney disease (ADPKD), autosomal recessive polycystic kidney disease (ARPKD), ARPKD associated congenital hepatic fibrosis, ARPKD associated Caroli's disease, or cholangiocarcinoma in a mammal in need thereof by administering a 20-HETE synthesizing enzyme inhibitor or a 20-HETE antagonist to the mammal in an amount sufficient to prevent or treat the disease.
    Type: Application
    Filed: June 12, 2014
    Publication date: November 6, 2014
    Inventors: William E. Sweeney, Ellis D. Avner, Richard J. Roman
  • Publication number: 20140296068
    Abstract: This document discloses molecules having the following formula (Formula One) and processes related thereto.
    Type: Application
    Filed: October 24, 2012
    Publication date: October 2, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Negar Garizi, Tony K. Trullinger, Ricky Hunter, Yu Zhang, Noormohamed M. Niyaz, Daniel Knueppel, Christian T. Lowe, Ann M. Buysse
  • Patent number: 8846947
    Abstract: Provided herein are sirtuin-modulating compounds of formula (II). The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders relating to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Grant
    Filed: July 2, 2009
    Date of Patent: September 30, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Chi B. Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
  • Publication number: 20140286931
    Abstract: The present invention relates to new biphenyl-3-carboxylic acid modulators of beta-3-adrenoceptor activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: June 5, 2014
    Publication date: September 25, 2014
    Inventor: Chengzhi Zhang
  • Publication number: 20140235593
    Abstract: In one aspect, the invention relates to novel substituted 2-alkyl-1-oxo-N-phenyl-3-heteroaryl-1,2,3,4-tetrahydroisoquinoline-4-carboxamides; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating and/or preventing malaria. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: August 24, 2012
    Publication date: August 21, 2014
    Applicants: ST. JUDE CHILDREN'S RESEARCH HOSPITAL, RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY, MMV MEDICINES FOR MALARIA VENTURE
    Inventors: Rodney Kiplin Guy, Fangyi Zhu, Wendyam Armand Guiguemde, David Floyd, Spencer Knapp, Philip Stein, Steve Castro
  • Patent number: 8796267
    Abstract: This invention relates to novel N-[[3-[3-Fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]-acetamide derivatives, their acceptable acid addition salts, solvates and hydrates. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by antimicrobial agents.
    Type: Grant
    Filed: June 17, 2008
    Date of Patent: August 5, 2014
    Assignee: Concert Pharmaceuticals, Inc.
    Inventors: Roger Tung, Scott Harbeson
  • Patent number: 8791110
    Abstract: Described herein are 4-methyl-piperazine-1-carbothioic acid amide derivatives and analogs, as well as compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by hemorrhagic fever viruses, such as Arenaviruses.
    Type: Grant
    Filed: December 29, 2011
    Date of Patent: July 29, 2014
    Assignee: Siga Technologies, Inc.
    Inventors: Sean M. Amberg, Dongcheng Dai, Tove C. Bolken, Dennis E. Hruby
  • Publication number: 20140194415
    Abstract: This invention relates to spirocyclic piperidines according to Formula (I) and the use of spirocyclic piperidines for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of spirocyclic piperidines in the treatment of cancer.
    Type: Application
    Filed: August 16, 2012
    Publication date: July 10, 2014
    Applicant: GlaxoSmithKline Intellectual Property (No2) Limite
    Inventors: Jonathan Michael Ghergurovich, Michael Lee Moore, Cynthia Ann Parrish, Lance Howard Ridgers, Hongyi Lu
  • Publication number: 20140179518
    Abstract: The present invention relates to pesticidal mixtures comprising as active components 1) at least one cyanosulfoximine compound I of the formula I wherein R1, R2 and G are defined as in the description; and 2) at least one fungicidal compounds II selected from azoles, strobilurins, carboxamides, carbamates, heterocyclic and various other compounds as defined in the description, in synergistically effective amounts. The invention relates further to methods and use of these mixtures for combating insects, arachnids or nematodes and harmful fungis in and on plants, and for protecting such plants being infested with pests, especially also for protecting seeds.
    Type: Application
    Filed: December 20, 2013
    Publication date: June 26, 2014
    Applicant: BASF SE
    Inventors: Delphine BREUNINGER, Henricus Maria Martinus BASTIAANS, Wolfgang VON DEYN, Matthias POHLMAN, Juergen LANGEWALD, Egon HADEN
  • Patent number: 8759536
    Abstract: Disclosed are novel rhodanine derivatives which are inhibitory of HIV activity. Also provided are a method for preparing the novel rhodanine derivatives, and a pharmaceutical composition for the prevention or treatment of AIDS containing the rhodanine derivatives as active ingredients. Having high inhibitory activity against HIV, the rhodanine derivatives can be effectively used in the prophylaxis or therapy of AIDS.
    Type: Grant
    Filed: June 17, 2011
    Date of Patent: June 24, 2014
    Assignee: Avixgen Inc.
    Inventors: Ji Chang You, Gyoon Hee Han, Chul Ho Lee, Doo Na Song, Koo Hwan Chung
  • Publication number: 20140163024
    Abstract: Compounds of the formula Ia or Ib: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: December 10, 2013
    Publication date: June 12, 2014
    Applicant: GENENTECH, INC.
    Inventors: Benjamin Fauber, Olivier Rene, Monique Bodil van Niel, Simon Gaines, Jonathan Killen, Stuart Ward
  • Publication number: 20140155369
    Abstract: An agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that activates a serotonin 5-HT2C receptor, an agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that stimulates an androgen binding site, and a method of screening for a drug for the prophylaxis or treatment of abdominal pressure incontinence, which includes electrostimulating the abdominal muscles or a nerve controlling them of an animal to increase the abdominal pressure, and measuring the leak point pressure at that time.
    Type: Application
    Filed: January 16, 2014
    Publication date: June 5, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Izumi KAMO, Tadatoshi HASHIMOTO
  • Patent number: 8735384
    Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein ring A, B1, B2, B3, L, R1, R2, ring Z, m and n of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula (I), intermediates and processes useful for the preparation of compounds of Formula (I).
    Type: Grant
    Filed: January 14, 2011
    Date of Patent: May 27, 2014
    Assignee: Amgen Inc.
    Inventors: Nick A. Paras, James Brown, Yuan Cheng, Stephen A. Hitchcock, Ted Judd, Patricia Lopez, Ana Elena Minatti, Thomas Nixey, Timothy Powers, Christopher M. Tegley, Qiufen Xue, Bryant Yang, Wenge Zhong
  • Patent number: 8722742
    Abstract: Use of chemical compounds obtained in silico for the preparation of pharmaceutical compositions to attenuate or inhibit Dengue virus infection. Particularly, through the interference or the modulation of several stages of viral replication cycle related with the entry of virus into host cells and the assembly of mature progeny virions. The invention also comprises the use of such pharmaceutical compositions for prophylactic and/or therapeutic treatment of infection caused by all four serotypes of Dengue virus and other flaviviruses.
    Type: Grant
    Filed: February 27, 2009
    Date of Patent: May 13, 2014
    Assignee: Centro de Ingenieria Genetica y Biotecnologia
    Inventors: Yuliet Mazola Reyes, Glay Chinea Santiago, Osmany Guirola Cruz, Roberto Vera Alvarez, Vivian Huerta Galindo, Noralvis Fleitas Salazar, Alexis Musacchio Lasa
  • Publication number: 20140113895
    Abstract: A compound or its pharmaceutically acceptable salt, optionally including both individual enantiomeric forms, a racemate, diastereomers and mixtures thereof, composition and method are disclosed that can provide analgesia and reduce inflammation. A contemplated compound has a structure that corresponds to Formula A, wherein the R group substituents, d, e, f, k, n, m, D, E, F, K, G, P, Q, W, and Z are defined within.
    Type: Application
    Filed: December 20, 2013
    Publication date: April 24, 2014
    Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
  • Publication number: 20140100224
    Abstract: The present application is related to compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders associated with p75 expression, such as degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such compounds.
    Type: Application
    Filed: June 26, 2013
    Publication date: April 10, 2014
    Applicants: The University of North Carolina at Chapel Hill, U.S. Government represented by the Department of Veterans Affairs, The Regents of the University of California
    Inventors: Frank M. Longo, Stephen M. Massa
  • Patent number: 8686184
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, a, R4, R5, and R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: April 1, 2014
    Assignee: Theravance, Inc.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
  • Patent number: 8658641
    Abstract: The present invention relates to compounds of Formula (I); to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to methods for their preparation.
    Type: Grant
    Filed: October 13, 2009
    Date of Patent: February 25, 2014
    Assignee: AstraZeneca AB
    Inventors: Kevin Barvian, Gregory Steven Basarab, Madhusudhan Reddy Gowravaram, Sheila Irene Hauck, Fei Zhou
  • Publication number: 20140051693
    Abstract: Cerebral palsy impaired speech in children and adolescents are effectively treated by administration of a psychostimulant. Low doses of the psychostimulant significantly increases the percentage of correctly pronounced intelligible syllables or words and the ability to more intelligibly communicate. The improvement in speech persists after cessation of or prior to continued psychostimulant treatment.
    Type: Application
    Filed: October 22, 2013
    Publication date: February 20, 2014
    Inventors: Bruce Roseman, Gilla Kaplan
  • Publication number: 20140038823
    Abstract: The present invention relates to active compound combinations, in particular within a fungicide composition, which comprises (A) a N-cyclopropyl-N-[substituted-benzyl]-3-(difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxamide or thiocarboxamide derivative and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively or eradicatively 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 not at least to the treated seed.
    Type: Application
    Filed: April 18, 2012
    Publication date: February 6, 2014
    Inventors: Peter Dahmen, Philippe Desbordes, Christophe Dubost, Stephanie Gary, Frank Goehlich, Hendrik Helmke, Thomas Seitz, Ulrike Wachendorff-Neumann, Ingo Wetcholowsky
  • Patent number: 8642596
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel semicarbazides, sulfonyl carbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to Arenaviridae (Junin, Machupo, Guanavito, Sabia and Lassa), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).
    Type: Grant
    Filed: December 6, 2005
    Date of Patent: February 4, 2014
    Assignee: Siga Technologies, Inc.
    Inventors: Yijun Deng, Theodore J. Nitz, Thomas R. Bailey, Yuanming Zhang, Sylvie Laquerre
  • Patent number: 8637576
    Abstract: Benzamide derivatives of formulae I and II, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof, and pharmaceutical compositions comprising the same, are described and have therapeutic utility, particularly in the treatment of diabetes, obesity, and related conditions and disorders: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are defined as provided herein.
    Type: Grant
    Filed: October 20, 2009
    Date of Patent: January 28, 2014
    Assignee: Amgen Inc.
    Inventors: Jay P. Powers, Michael R. Degraffenreid, Xiao He, Lisa D. Julian, Dustin L. McMinn, Daqing Sun, Yosup Rew, Xuelei Yan
  • Patent number: 8598165
    Abstract: A method of inhibiting formation of cancerous metabolites, of inhibiting cytochrome P450 2A13 from forming carcinogen metabolites, and/or inhibiting formation of cancerous lung cells in a subject can include: providing a morpholine compound that selectively interacts with cytochrome P450 2A13 over cytochrome P450 2A6; administering a therapeutically effective amount of the morpholine compound or derivative to the subject. The morpholine compound or derivative can be substantially more selective for interacting with the cytochrome P450 2A13 over the cytochrome P450 2A6. The morpholine compound or derivative can also be substantially non-interactive with other physiological components. The morpholine compound or derivative can include a structure that selectively interacts with cytochrome P450 2A13 over cytochrome P450 2A6, such as Compounds 1-34 of Formulas A-D.
    Type: Grant
    Filed: November 24, 2008
    Date of Patent: December 3, 2013
    Assignee: University of Kansas
    Inventors: Emily Scott, Anuradha Roy
  • Patent number: 8580297
    Abstract: The invention suggests amphoteric lipids wherein one or more amphoteric groups having an isoelectric point between 4 and 9 are substituted on a membranous or membrane-forming amphiphilic substance, as well as liposomes containing such compounds.
    Type: Grant
    Filed: November 8, 2011
    Date of Patent: November 12, 2013
    Assignee: Marina Biotech, Inc.
    Inventors: Frank Essler, Steffen Panzner, Gerold Endert
  • Publication number: 20130281452
    Abstract: Substituted 4-aminobenzamides, pharmaceutical compositions containing these compounds and also methods of using these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
    Type: Application
    Filed: April 18, 2013
    Publication date: October 24, 2013
    Inventors: Gregor BAHRENBERG, Sven KUEHNERT, Simon LUCAS, Wolfgang SCHROEDER