Divalent Chalcogen Or Acyclic Nitrogen Double Bonded Directly To Ring Carbon Of The Diazole Ring, Or Tautomeric Equivalent Patents (Class 514/386)
  • Patent number: 8367712
    Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of ?-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
    Type: Grant
    Filed: August 23, 2010
    Date of Patent: February 5, 2013
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Ying Huang, Guoqing Li, Andrew W. Stamford
  • Patent number: 8357710
    Abstract: There is provided a compound of formula I, wherein R1a, R1b, X, Y1, Y2, Y3, Y4, Z1, Z2, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.
    Type: Grant
    Filed: April 12, 2006
    Date of Patent: January 22, 2013
    Assignee: Vicore Pharma AB
    Inventors: Mathias Alterman, Anders Hallberg, Murugaiah Andappan Murugaiah Subbaiah
  • Publication number: 20130018044
    Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.
    Type: Application
    Filed: December 21, 2010
    Publication date: January 17, 2013
    Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michel Pawlotsky
  • Patent number: 8354442
    Abstract: Imidazol-4-one or imidazole-4-thione compounds of formula (I): wherein X, R1, R2, R3, R4, R5, and R6 are defined herein. Also disclosed is a method for treating a cannabinoid receptor-mediated disorder with these compounds.
    Type: Grant
    Filed: October 30, 2009
    Date of Patent: January 15, 2013
    Assignee: National Health Research Institutes
    Inventors: Kak-Shan Shia, Chien-Huang Wu, Teng-Kuang Yeh, Yu-Sheng Chao
  • Publication number: 20130012434
    Abstract: The present invention relates to compounds of the general formula: wherein ring A, ring B, R1, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
    Type: Application
    Filed: March 22, 2011
    Publication date: January 10, 2013
    Inventors: Michael K. Wong, Brian J. Lavey, Wensheng Yu, Joseph A. Kozlowski, Duanc E. DeMong, Xing Dai, Andrew W. Stamford, Michael W. Miller, Guowei Zhou, De-Yi Yang, William J. Greenlee
  • Publication number: 20130005704
    Abstract: The present application relates to novel, substituted 4-arylimidazol-2-ones and 5-aryl-1,2,4-triazolones, processes for the production thereof, the use thereof alone or in combinations for the treatment and/or prevention of diseases and the use thereof for the production of medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular diseases.
    Type: Application
    Filed: December 26, 2011
    Publication date: January 3, 2013
    Applicant: BAYER PHARMA AKTIENGESELLSHAFT
    Inventors: Heinrich Meier, Eckhard Bender, Ulf Brüggemeier, Ingo Flamme, Dagmar Karthaus, Peter Kolkhof, Daniel Meibom, Dirk Schneider, Verena Voehringer, Chantal Fürstner, Jörg Keldenich, Dieter Lang, Elisabeth Pook, Carsten Schmeck
  • Publication number: 20130005785
    Abstract: The present disclosure provides mucoadhesive aqueous-based gel formulations of metronidazole useful for a variety of purposes, including intravaginal application as a therapeutic approach towards the treatment of individuals suffering from and/or diagnosed with bacterial vaginosis.
    Type: Application
    Filed: August 23, 2012
    Publication date: January 3, 2013
    Applicant: Medicis Pharmaceutical Corporation
    Inventors: Michael T. NORDSIEK, Kodumudi S. Balaji
  • Patent number: 8334313
    Abstract: The invention encompasses ureido substituted benzoic acid compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions.
    Type: Grant
    Filed: December 29, 2010
    Date of Patent: December 18, 2012
    Assignee: PTC Therapeutics, Inc.
    Inventors: Richard G. Wilde, James J. Takasugi, Seongwoo Hwang, Ellen M. Welch, Guangming Chen
  • Publication number: 20120316209
    Abstract: A sensitive, multicomponent diagnostic test for infection with T. cruzi, the causative agent of Chagas disease, including methods of making and methods of use. Also provided is a method for screening T. cruzi polypeptides to identify antigenic polypeptides for inclusion as components of the diagnostic test, as well as compositions containing antigenic T. cruzi polypeptides.
    Type: Application
    Filed: August 9, 2012
    Publication date: December 13, 2012
    Applicant: University of Georgia Research Foundation, Inc.
    Inventors: Rick L. Tarleton, Ronald D. Etheridge, JR.
  • Publication number: 20120270838
    Abstract: The present invention relates to a compound represented by the following formula (1): wherein W, X, Y, R1, R2, R33, R34, m and n are as defined in the claims, or a pharmacologically acceptable salt thereof.
    Type: Application
    Filed: April 27, 2010
    Publication date: October 25, 2012
    Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHA
    Inventors: Toru Esaki, Yoshikazu Nishimura, Yoshiaki Isshiki, Naoki Okamoto, Yoshiyuki Furuta, Akemi Mizutani, Masateru Ohta, Wayne Wen Lai, Tomoya Kotake
  • Patent number: 8288426
    Abstract: A composition comprising fenamidone (a) and an insecticide compound (b) in a (a)/(b) weight ratio of from 1/1000 to 1000/1. A composition further comprising an additional fungicidal compound. A method for preventively or curatively combating the pests and diseases of crops by using this composition.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: October 16, 2012
    Assignee: Bayer CropScience AG
    Inventors: Heike Hungenberg, Wolfgang Thielert, Koen Van Den Eynde
  • Patent number: 8273793
    Abstract: Disclosed is a method for producing precursors for 2-[18F]fluorophenylalanine and 6-[18F]fluoro-L-meta-tyrosine and the ?-methylated derivatives thereof, to the precursor, and to a method for producing 2-[18F]fluorophenylalanine and 6-[18F]fluoro-L-meta-tyrosine and the ?-methylated derivatives thereof from particular precursor. A compound of formula (3) is provided which enables an automated synthesis of L-3,4-dihydroxy-6-[18F]fluorophenylalanine and 6-[18F]fluoro-L-meta-tyrosine. The enantiomeric purity of the product is ?98%.
    Type: Grant
    Filed: November 21, 2008
    Date of Patent: September 25, 2012
    Assignee: Forschungszentrum Juelich GmbH
    Inventors: Franziska Wagner, Johannes Ermert, Heinrich Hubert Coenen
  • Patent number: 8242117
    Abstract: Provided are 5-membered heterocycle-based p38 kinase inhibitors. Further provided are pyrazole and imidazole-based p38 kinase, including p38? and p38? kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: August 14, 2012
    Assignee: Novartis AG
    Inventors: Olga M. Fryszman, Hengyuan Lang, Jiong Lan, Edcon Chang, Yunfeng Fang
  • Publication number: 20120178666
    Abstract: Prodrugs of guanfacine with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and a method for providing therapeutic benefit in the treatment of ADHD/ODD (attention deficient hyperactivity disorder and oppositional defiance disorder) with guanfacine prodrugs are provided herein. Additionally, methods for minimizing or avoiding the adverse gastrointestinal side effects associated with guanfacine administration, as well as improving the pharmacokinetics of guanfacine are provided herein.
    Type: Application
    Filed: September 15, 2010
    Publication date: July 12, 2012
    Applicant: SHIRE LLC
    Inventors: Richard Franklin, Robert G. Tyson, Bernard T. Golding, Rhys Whomsley
  • Patent number: 8207182
    Abstract: The present invention relates to substituted cyclic urea derivatives corresponding to formula I, to processes for the preparation thereof, to medicinal drugs containing such compounds, to the use of such compounds in the preparation of medicinal drugs and in related treatment methods.
    Type: Grant
    Filed: October 19, 2007
    Date of Patent: June 26, 2012
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Bernd Sundermann, Hans Schick, Helmut Sonnenschein
  • Patent number: 8193227
    Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
    Type: Grant
    Filed: December 10, 2004
    Date of Patent: June 5, 2012
    Assignee: Abbott Laboratories
    Inventors: Charles A. Flentge, Hui-Ju Chen, David A. DeGoey, William J. Flosi, David J. Grampovnik, Peggy P. Huang, Dale J. Kempf, Larry L. Klein, Allan C. Krueger, Darold L. Madigan, John T. Randolph, Minghua Sun, Ming C. Yeung, Chen Zhao
  • Patent number: 8188291
    Abstract: The present invention relates to heteroaryl-substituted carboxamides of the formula I, in which Het, A, X, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired.
    Type: Grant
    Filed: June 17, 2009
    Date of Patent: May 29, 2012
    Assignee: Sanofi-Aventis
    Inventors: Hartmut Strobel, Paulus Wohlfart, Heinz-Werner Kleemann, Gerhard Zoller, David William Will
  • Publication number: 20120129793
    Abstract: The present application describes compounds of Formula I and Formula IA and as disclosed herein, that are useful as anti-microbial agents, including as antibacterial, disinfectant, antifungal, germicidal or antiviral agents.
    Type: Application
    Filed: October 18, 2011
    Publication date: May 24, 2012
    Inventors: Rakesh K. Jain, Timothy Shiau, Charles Francavilla, Eddy Low, Eric Douglas Turtle, Donogh John Roger O'Mahony
  • Patent number: 8168666
    Abstract: There is provided a novel LXR? agonist useful as a preventative and/or therapeutic agent for arteriosclerosis; arteriosclerosis such as those resulting from diabetes; hyperlipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases caused by inflammatory cytokines, skin diseases such as allergic skin diseases, diabetes or Alzheimer's disease. The agonist is a carbinol derivative represented by the following general formula (1) or salt thereof, or their solvate.
    Type: Grant
    Filed: November 29, 2007
    Date of Patent: May 1, 2012
    Assignee: Kowa Company, Ltd.
    Inventors: Takayuki Matsuda, Ayumu Okuda, Minoru Koura, Yuki Yamaguchi, Sayaka Kurobuchi, Yuuichirou Watanabe, Kimiyuki Shibuya
  • Patent number: 8158666
    Abstract: A process for making (R)-5-(2-aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione and pharmaceutically acceptable salts thereof, and for making intermediates useful in the formation of said compound.
    Type: Grant
    Filed: January 31, 2008
    Date of Patent: April 17, 2012
    Assignee: Bial-Portela & C.A., S.A.
    Inventors: Patrício Manuel Vieira Araújo Soares Da Silva, Alexander Beliaev, David Alexander Learmonth
  • Publication number: 20120082646
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Application
    Filed: March 25, 2010
    Publication date: April 5, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: David A. Betebenner, John K. Pratt, David A. DeGoey, Pamela L. Donner, Charles A. Flentge, Douglas K. Hutchinson, Warren M. Kati, Allan C. Krueger, Kenton L. Longenecker, Clarence J. Maring, John T. Randolph, Todd W. Rockway, Michael D. Tufano, Rolf Wagner, Dachun Liu
  • Publication number: 20120071531
    Abstract: Process for the protection of fish and invertebrates and all their stages of development against or for the treatment of mycoses caused by fungi of the genera Saprolegnia, Aphanomyces, Achlyaflagellata and other species important in aquacultures by use of 2-[[[[1-[3-(1-fluoro-2-phenylethyl)oxy]phenyl]ethylidene]amino]oxy]methyl]alpha-(methoxyimino)-N-methyl-alphaE-benzeneacetamide, amisulbrom, cyazofamid, enestrobin, famoxadone, fenamidone, fluoxastrobin, orysastrobin, picoxystrobin and pyribencarb. This use leads to an inhibition or destruction of pathogenic fungi. The composition, comprising at least one fungicide selected from the abovementioned group for use in fish farming and keeping is suitable for the prophylaxis and therapy of diseases of fish in aquaculture, in breeding ponds, breeding tanks, aquariums, natural stretches of game fish waters, ponds, and marine fish farms. Addition to the water and feed and direct application are the associated use forms.
    Type: Application
    Filed: November 22, 2011
    Publication date: March 22, 2012
    Applicant: Bayer CropScience AG
    Inventors: Isolde Häuser-Hahn, Klaus Stenzel, Ulrike Wachendorff-Neumann
  • Patent number: 8129423
    Abstract: Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R6 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.
    Type: Grant
    Filed: October 12, 2007
    Date of Patent: March 6, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Jean Ackermann, Kurt Amrein, Daniel Hunziker, Bernd Kuhn, Alexander V. Mayweg, Werner Neidhart, Tadakatsu Takahashi
  • Patent number: 8119674
    Abstract: Novel 4-phenylimidazole-2-thione tyrosinase inhibiting compounds corresponding to the following general formula (I): formulated into pharmaceutical or cosmetic compositions are useful for the treatment or prevention of pigmentary disorders, or for preventing and/or treating signs of skin aging, and/or for body or hair hygiene.
    Type: Grant
    Filed: December 4, 2009
    Date of Patent: February 21, 2012
    Assignee: Galderma Research & Development
    Inventors: Jean-Guy Boiteau, Corinne Millois Barbuis, Sandrine Talano
  • Publication number: 20120022059
    Abstract: The present invention relates to novel substituted furancarboxamides, methods for their production, their use for the treatment and/or prevention of diseases, as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially retroviral diseases, in humans and/or animals.
    Type: Application
    Filed: June 16, 2011
    Publication date: January 26, 2012
    Applicant: AiCuris GmbH & Co. KG
    Inventors: Kai THEDE, Susanne Greschat, Steffen Wildum, Daniela Paulsen
  • Publication number: 20120022123
    Abstract: The present invention relates to novel substituted (thiophenyl-carbonyl)imidazolidinones, methods for their production, their use for the treatment and/or prevention of diseases, as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially retroviral diseases, in humans and/or animals.
    Type: Application
    Filed: June 16, 2011
    Publication date: January 26, 2012
    Applicant: AiCuris GmbH & Co. KG
    Inventors: Kai THEDE, Susanne GRESCHAT, Steffen WILDUM, Daniela PAULSEN
  • Publication number: 20120015910
    Abstract: Novel active compound combinations comprising a carboxamide of the general formula (I) (group 1) in which A, R1, R2 and R3 are as defined in the description, and the active compound groups (2) to (23) listed in the description have very good fungicidal properties.
    Type: Application
    Filed: September 23, 2011
    Publication date: January 19, 2012
    Applicant: Bayer CropScience AG
    Inventors: Ulrike Wachendorff-Neumann, Peter Dahmen, Ralf Dunkel, Hans-Ludwig Elbe, Anne Suty-Heinze, Heiko Rieck
  • Patent number: 8071635
    Abstract: Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardiovascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardiovascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardiovascular and/or sedatory activity.
    Type: Grant
    Filed: February 16, 2008
    Date of Patent: December 6, 2011
    Assignee: Allergan, Inc.
    Inventors: Ken Chow, Todd Heidelbaugh, Daniel Gil, Michael Garst, Larry A. Wheeler, Phong X. Nguyen, Dario G. Gomez
  • Patent number: 8063086
    Abstract: Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardiovascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardiovascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardiovascular and/or sedatory activity.
    Type: Grant
    Filed: October 17, 2007
    Date of Patent: November 22, 2011
    Assignee: Allergan, Inc.
    Inventors: Ken Chow, Todd M. Heidelbaugh, Daniel W. Gil, Michael E. Garst, Larry A. Wheeler
  • Patent number: 8063087
    Abstract: Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardiovascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardiovascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardiovascular and/or sedatory activity.
    Type: Grant
    Filed: July 25, 2008
    Date of Patent: November 22, 2011
    Assignee: Allergan, Inc.
    Inventors: Ken Chow, Todd Heidelbaugh, Daniel Gill, Michael Garst, Larry A. Wheeler, Phong X. Nguyen, Dario G. Gomez
  • Patent number: 8039013
    Abstract: The present invention relates to novel active substance combinations which contain spiroxamine, which is known, a known azole and a known carboxamide and which are very suitable for controlling undesired phytopathogenic fungi.
    Type: Grant
    Filed: September 3, 2005
    Date of Patent: October 18, 2011
    Assignee: Bayer CropScience AG
    Inventors: Peter Dahmen, Ulrike Wachendorff-Neumann, Ralf Dunkel
  • Publication number: 20110218192
    Abstract: The present invention is directed to a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof. Pharmaceutical composition comprising a compound represented by Structural Formula (I) and method of use of these compound for inhibiting BACE activity in a subject in need of such treatment are also described.
    Type: Application
    Filed: August 14, 2009
    Publication date: September 8, 2011
    Applicant: VITAE PHARMACEUTICALS, INC.
    Inventors: Lawrence W. Dillard, Jing Yuan, Lanqi Jia, Yajun Zheng
  • Publication number: 20110212962
    Abstract: There are provided inter alia compounds of formula (I) wherein R1, Ar, L, X, R3 and Q are as defined in the specification for use in therapy, especially in the treatment of inflammatory diseases.
    Type: Application
    Filed: October 2, 2009
    Publication date: September 1, 2011
    Inventors: Kazuhiro Ito, Peter Strong, William Garth Rapeport, Peter John Murray, John King-Underwood, Jonathan Gareth Williams, Stuart Thomas Onions, Simon Christopher Hirst, David Michel Adrien Taddei, Catherine Elisabeth Charron
  • Patent number: 8003653
    Abstract: The present invention is directed to imidazolidinone compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: November 10, 2006
    Date of Patent: August 23, 2011
    Assignee: Merck. Sharp & Dohme Corp.
    Inventors: James C. Barrow, Kenneth E. Rittle, Phung Le Bondiskey
  • Publication number: 20110200484
    Abstract: A disinfecting, nonbleaching N-halamine for use in contact lens soaking solutions. The N-halamine compound is soluble in water and contact lens formulation solutions to the extent necessary to provide disinfection, but not to cause significant bleaching of dye materials incorporated into the contact lenses.
    Type: Application
    Filed: February 17, 2011
    Publication date: August 18, 2011
    Applicant: Auburn University
    Inventors: Shelby D. Worley, Xuehong Ren, Hasan B. Kocer
  • Patent number: 7989483
    Abstract: Novel 4-heteroarylimidazole-2-thione tyrosinase inhibiting compounds corresponding to the following general formula (I): formulated into pharmaceutical or cosmetic compositions are useful for the treatment or prevention of pigmentary disorders, or for preventing and/or treating signs of skin aging, and/or for body or hair hygiene.
    Type: Grant
    Filed: December 4, 2009
    Date of Patent: August 2, 2011
    Assignee: Galderma Research & Development
    Inventors: Jean Guy Boiteau, Corinne Millois Barbuis, Karine Bouquet
  • Patent number: 7973066
    Abstract: The use of a compound of formula (I), is disclosed in treating and/or preventing 5 chemotherapy-induced peripheral neurotoxicity (CIPN). The invention includes pharmaceutical compositions wherein the compound of formula (I) is present in a mixture with anticancer agents. An improved anticancer treatment with reduced CIPN-related side effects is also provided.
    Type: Grant
    Filed: November 14, 2007
    Date of Patent: July 5, 2011
    Assignee: Neurotune AG
    Inventors: Carlo Farina, Carla Ghelardini, Paola Petrillo
  • Patent number: 7968580
    Abstract: The present invention is directed to novel imidazolidin-2-one derivatives having a structure according to Formula I wherein a, b, R1, R2, R3, and R4 are as defined above, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
    Type: Grant
    Filed: March 30, 2009
    Date of Patent: June 28, 2011
    Assignee: Janssen Pharmaceutica NV
    Inventors: James C. Lanter, Zhihua Sui
  • Patent number: 7960423
    Abstract: Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardivascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardivascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardivascular and/or sedatory activity.
    Type: Grant
    Filed: October 17, 2007
    Date of Patent: June 14, 2011
    Assignee: Allergan, Inc
    Inventors: Ken Chow, Todd M. Heidelbaugh, Daniel W. Gil, Michael E. Garst, Larry A. Wheeler
  • Publication number: 20110136735
    Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: November 30, 2010
    Publication date: June 9, 2011
    Inventors: David BARNES, Gregory Raymond BEBERNITZ, Scott Louis COHEN, Robert Edson DAMON, Robert Francis DAY, Monish JAIN, Rajeshri Ganesh KARKI, Louise Clare KIRMAN, Tajesh Jayprakash PATEL, Brian Kenneth RAYMER, Herbert Franz SCHUSTER, Wei ZHANG
  • Publication number: 20110124618
    Abstract: The present invention relates to novel substituted (pyrazolylcarbonyl)imidazolidinones, methods for their preparation, their use for the treatment and/or prophylaxis of diseases, as well as their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of retroviral diseases, in humans and/or animals.
    Type: Application
    Filed: September 17, 2010
    Publication date: May 26, 2011
    Applicant: AiCuris GmbH & Co. KG
    Inventors: Kai THEDE, Susanne GRESCHAT, Steffen WILDUM, Daniela PAULSEN
  • Patent number: 7947722
    Abstract: The objective of the present invention is to provide an optically active imidazolidinone derivative widely usable for synthesizing an optically active amino acid, a method of easily producing the derivative, and a method of easily producing an optically active amino acid by using the derivative. The objective can be achieved by producing an optically active amino acid using a novel optically active imidazolidinone derivative represented by a general formula (3) and the like. According to the method of the present invention, an optically active imidazolidinone derivative can be obtained by preferential crystallization from a mixture of isomers of the imidazolidinone derivative. Therefore, an optically active amino acid can be easily and stereoselectively produced without cumbersome procedures required for the conventional methods, such as resolution of diastereomers, synthesis from an optically active amino acid and resolution of isomers by silica gel column chromatography.
    Type: Grant
    Filed: May 14, 2007
    Date of Patent: May 24, 2011
    Assignee: Kaneka Corporation
    Inventors: Yasuhiro Saka, Akio Fujii, Kazumi Okuro, Masaru Mitsuda
  • Publication number: 20110098319
    Abstract: The invention relates to novel derivatives of short-chain fatty acids, in particular derivatives of butyric acid, useful for all the known clinical applications of the latter, which show physicochemical characteristics suitable for an easy oral administration, being devoid of the unpleasant organoleptic properties that characterize butyrate. The new compounds are amide derivatives which can be synthesized by reaction of the corresponding fatty acid halide with a naturally occurring amino acid, phenylalanine or a suitable derivative thereof, and which are in a poorly hygroscopic, easily weighable form, stable to acids and alkalis and able to release the acid at the small and large bowel level in a constant manner over time. They do not have disagreeable odors and are practically tasteless, thus allowing the manufacture of preparations for oral administration also suitable for the therapy of chronic diseases and in the pediatric field.
    Type: Application
    Filed: April 21, 2009
    Publication date: April 28, 2011
    Inventors: Roberto Berni Canani, Antonio Calignano, Orietta Mazzoni, Anna Coruzzo
  • Patent number: 7928132
    Abstract: Methods of ameliorating episodes of accute or chronic colitis are provided by using methimazole derivatives and tautomeric cyclic thiones in combination with another pharmaceutical compound.
    Type: Grant
    Filed: August 6, 2004
    Date of Patent: April 19, 2011
    Assignee: Ohio University
    Inventors: Leonard D. Kohn, Douglas J. Goetz, Uruguaysito Benavides-Peralta, Mariana Gonzalez-Murguiondo, Norikazu Harii, Christopher J. Lewis, Giorgio Napolitano, Nilesh D. Dagia
  • Publication number: 20110071152
    Abstract: Provided are 5-membered heterocycle-based p38 kinase inhibitors. Further provided are pyrazole and imidazole-based p38 kinase, including p38? and p38? kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders.
    Type: Application
    Filed: November 19, 2010
    Publication date: March 24, 2011
    Inventors: Olga M. FRYSZMAN, Hengyuan LANG, Jiong LAN, Edcon CHANG, Yunfeng FANG
  • Publication number: 20110071126
    Abstract: The present invention is directed to a compound represented by the following structural formula or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions and method of use of the compounds are also described.
    Type: Application
    Filed: March 12, 2010
    Publication date: March 24, 2011
    Inventors: Salvacion CACATIAN, David A. CLAREMON, Lawrence W. DILLARD, Klaus FUCHS, Niklas HEINE, Lanqi JIA, Katerina LEFTHERIS, Brian McKEEVER, Angel MORALES-RAMOS, Suresh B. SINGH, Shankar VENKATRAMAN, Guosheng WU, Zhongren WU, Zhenrong XU, Jing YUAN, Yajun ZHENG
  • Publication number: 20110065763
    Abstract: A composition comprising at least one physiologically tolerated film-forming agent, at least one physiologically tolerated solvent, at least one plasticizer and a compound of the formula I or a stereoisomeric form or a physiologically tolerated salt of any of the foregoing. The composition is suitable for treatment of androgenic alopecia or hirsutism, that is, for avoiding undesirable hair growth, and for treatment of seborrhea and acne, and can furthermore be employed in cosmetics.
    Type: Application
    Filed: November 17, 2010
    Publication date: March 17, 2011
    Inventors: Karl Theodor Kraemer, Manfred Bohn
  • Patent number: 7902241
    Abstract: The invention encompasses ureido substituted benzoic acid compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions.
    Type: Grant
    Filed: June 17, 2008
    Date of Patent: March 8, 2011
    Assignee: PTC Therapeutics, Inc.
    Inventors: Richard G. Wilde, James J. Takasugi, Seongwoo Hwang, Ellen M. Welch, Guangming Chen
  • Publication number: 20110003825
    Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of ?-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
    Type: Application
    Filed: August 23, 2010
    Publication date: January 6, 2011
    Applicant: Schering Corporation
    Inventors: Ying Huang, Guoqing Li, Andrew W. Stamford
  • Patent number: 7838545
    Abstract: Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardiovascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.
    Type: Grant
    Filed: July 2, 2008
    Date of Patent: November 23, 2010
    Assignee: Allergan, Inc.
    Inventors: Todd M. Heidelbaugh, Ken Chow, Phong X. Nguyen, Daniel W. Gill, John E. Donello, Michael E. Garst, Larry A. Wheeler