Nitrogen Attached Directed Or Indirectly To Morpholine Ring By Nonionic Bonding Patents (Class 544/162)
  • Publication number: 20100317582
    Abstract: The invention relates to novel cyclic hydrocarbon compounds and derivatives thereof, processes for the preparation thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.
    Type: Application
    Filed: November 20, 2008
    Publication date: December 16, 2010
    Applicant: LEO Pharma A/S
    Inventors: Jef Fensholdt, Sophie Elisabeth Havez, Bjarne Nørremark
  • Publication number: 20100304966
    Abstract: Compounds of the formula I in which the substituents have the meaning given in the description, processes for preparing these compounds, compositions comprising them and their use for controlling harmful fungi.
    Type: Application
    Filed: October 9, 2008
    Publication date: December 2, 2010
    Applicant: BASF SE
    Inventors: Joachim Rheinheimer, Barbara Nave, Doris Kremzow, Stefan Redlich, Christian Pilger, Claudia Rosenbaum, Wassilios Grammenos
  • Patent number: 7834013
    Abstract: The present invention relates generally to novel therapeutic compounds and more particularly to novel compounds, their use as GPR40 agonists, processes for their manufacture, and intermediates useful in their preparation.
    Type: Grant
    Filed: November 15, 2004
    Date of Patent: November 16, 2010
    Assignee: GlaxoSmithKline LLC
    Inventors: David Francis Corbett, Kate Anna Dwornik, Dulce Maria Garrido, Stephen Carl McKeown, Wendy Yoon Mills, Andrew James Peat, Terrence Lee Smalley, Jr.
  • Publication number: 20100279997
    Abstract: A compound, composition and method are disclosed that can provide analgesia. A contemplated compound has a structure that corresponds to Formula A, wherein A, B, X, R1, R2, R7 and R8, and the dashed lines are defined within.
    Type: Application
    Filed: October 28, 2009
    Publication date: November 4, 2010
    Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
  • Publication number: 20100280024
    Abstract: The present invention relates to renin inhibitors of formula (I), their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to a process of preparing compounds of general formula (I), their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.
    Type: Application
    Filed: October 13, 2008
    Publication date: November 4, 2010
    Inventors: Jigar Desai, Pravin S. Thombare, Mukul R. Jain, Pankaj Ramanbhai Patel
  • Patent number: 7767666
    Abstract: Certain substituted butyl and butynyl benzyl amine compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases.
    Type: Grant
    Filed: June 21, 2007
    Date of Patent: August 3, 2010
    Assignee: Janssen Pharmaceutica NV
    Inventors: John M. Keith, Michael A. Letavic, Emily M. Stocking
  • Publication number: 20100179109
    Abstract: Disclosed are compounds of Formula (I) wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.
    Type: Application
    Filed: April 4, 2008
    Publication date: July 15, 2010
    Inventors: Jonh J. Baldwin, Salvacion Cacatian, David Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Bahman Ghavimi-Alagha, Damiano Ghirlanda, Alexey V. Ishchenko, Lara S. Kallander, Brian Lawhorn, Colin A. Leach, Qing Lu, Gerard McGeehan, Jaclyn R. Patterson, Robert D. Simpson, Suresh B. Singh, Patrick Stoy, Lamont R. Terrell, Colin Tice, Zhenrong Xu, Jing Yuan, Catherine C. K. Yuan, Jing Zhang, Wei Zhao
  • Patent number: 7745451
    Abstract: Fused heterocyclic compounds are disclosed that have formula 1: where A, B, L, N, R1, R3, R4?, Y and Z are as defined herein. The compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.
    Type: Grant
    Filed: May 4, 2006
    Date of Patent: June 29, 2010
    Assignee: Renovis, Inc.
    Inventors: Michael G. Kelly, John Kincaid, Carl J. Kaub
  • Publication number: 20100144588
    Abstract: Novel iminium-type coupling agents containing proton acceptors in their iminium moiety, which can be used beneficially as coupling agents in various chemical polypeptide and/or polynucleotide syntheses, and are particularly useful as yield enhancing and racemization suppressing coupling agents for use in peptide syntheses, are disclosed. Further disclosed are a process of preparing such iminium-type coupling agents and their use in the preparation of polypeptides and/or polynucleotides.
    Type: Application
    Filed: May 15, 2008
    Publication date: June 10, 2010
    Applicant: LUXEMBOURG BIO TECHNOLOGIES LTD.
    Inventors: Fernando Albericio, Ayman El-Faham, Yoav Luxembourg, Ariel Ewenson
  • Publication number: 20100113778
    Abstract: An improved process for preparing o-chloromethylphenylglyoxylic esters of the formula which comprises converting a compound of the formula by reaction with magnesium into the corresponding Grignard reagent which is then reacted with a compound of the formula to give the compound of the formula which is then cleaved by reaction with a chloroformic ester of the formula CICOOR4 or by reaction with phosgene to give the compound of the formula (I), followed by the isolation of the compound of the formula (I), and also an improved process for preparing (E)-2-(2-chloromethylphenyl)-2-alkoximinoacetic esters of the formula and intermediates for their preparation.
    Type: Application
    Filed: April 10, 2008
    Publication date: May 6, 2010
    Inventors: John-Matthias Wiegand, Karsten Luettgen, Wolfgang Skranc
  • Publication number: 20100105686
    Abstract: The present invention relates to new sulfonamide derivatives of formula (I) wherein R1-R8 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these same compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.
    Type: Application
    Filed: October 27, 2007
    Publication date: April 29, 2010
    Inventors: Gyula Beke, Eva Bozo, Sandor Farkas, Katalin Hornok, Gyorgy Keseru, Eva Schmidt, Eva Szentirmay, Istvan Vago, Monika Vastag
  • Publication number: 20100069630
    Abstract: The present invention discloses novel naphthalenyloxypropenyl derivatives useful for inhibiting the enzyme activity of histone deacetylase, leading effective suppression of cancer cell proliferation.
    Type: Application
    Filed: November 1, 2007
    Publication date: March 18, 2010
    Applicants: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY, CRYSTALGENOMICS, INC
    Inventors: Cheol Hae Lee, Hee Jung Jung, Jae Hak Kim, Won Jang Jeong, Joong Myung Cho, Seong Gu Ro, Young Lan Hyun, Cheol Soon Lee
  • Publication number: 20100036119
    Abstract: The present invention relates to ?,?-difluoroamines, fluorinating reagents comprising ?,?-difluoroamines and also processes for preparing ?,?-difluoroamines and fluorinating reagents comprising ?,?-difluoroamines.
    Type: Application
    Filed: October 16, 2009
    Publication date: February 11, 2010
    Applicant: LANXESS DEUTSCHLAND GMBH
    Inventors: WOLFGANG EBENBECK, PETRA HILGERS, ALBRECHT MARHOLD, JAN ALEXANDER BARTEN, ALEXANDER KOLOMEITSEV, GERD-VOLKER ROSCHENTHALER
  • Patent number: 7622464
    Abstract: Compounds of formula (I): wherein: R1 represents substituted or unsubstituted heteroaryl; Y represents —(CRnaRnb)n—; Rna and Rnb are each independently hydrogen or C1-6alkyl; n is an integer from 0 to 5; R2 represents unsubstituted or substituted aryl or unsubstituted or substituted heteroaryl; R3 and R4 each independently represent hydrogen or C1-6-alkyl; R7 represents hydrogen or C1-6alkyl; R8 represents hydrogen or C1-6alkyl; and salts and solvates thereof; are CCR3 antagonists and are thus indicated to be useful in therapy.
    Type: Grant
    Filed: March 27, 2003
    Date of Patent: November 24, 2009
    Assignee: Glaxo Group Limited
    Inventors: Rachael Ann Ancliff, Caroline Mary Cook, Colin David Eldred, Paul Martin Gore, Lee Andrew Harrison, Martin Alistair Hayes, Simon Teanby Hodgson, Duncan Bruce Judd, Suzanne Elaine Keeling, Xiao Qing Lewell, Gail Mills, Graeme Michael Robertson, Stephen Swanson, Andrew John Walker, Mark Wilkinson
  • Publication number: 20090286775
    Abstract: New bicyclic derivatives of formula (I), wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as p38 kinase inhibitors.
    Type: Application
    Filed: June 28, 2006
    Publication date: November 19, 2009
    Applicant: PALAU PHARMA, S.A.
    Inventors: Carmen Almansa Rosales, Marina Virgili Bernadó
  • Patent number: 7619115
    Abstract: Novel ortho-substituted N?-benzylidene-(3-hydroxyphenyl)acetohydrazides of the formula (I), in which R1-R9 have the meanings indicated in claim 1, are SGK inhibitors and can be used for the treatment of SGK-induced diseases and conditions, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in fibroses and inflammatory processes of any type.
    Type: Grant
    Filed: June 6, 2005
    Date of Patent: November 17, 2009
    Assignee: Merck Patent GmbH
    Inventors: Rolf Gericke, Dieter Dorsch, Werner Mederski, Norbert Beier, Florian Lang
  • Publication number: 20090275583
    Abstract: The invention relates to compounds, pharmaceutical compositions and methods useful for treating viral infection.
    Type: Application
    Filed: April 13, 2009
    Publication date: November 5, 2009
    Applicant: Myriad Genetics, Incorporated
    Inventors: Kraig Yager, In Chul Kim, Michael Saunders, David Gerrish, Dange Vijay Kumar, Mark B. Anderson
  • Patent number: 7595399
    Abstract: The compounds of the invention are inhibitors of alpha4 containing integrin-mediated binding to ligands such as VCAM-1 and MAdCAM.
    Type: Grant
    Filed: February 4, 2004
    Date of Patent: September 29, 2009
    Assignee: Genentech, Inc.
    Inventors: David Y. Jackson, Frederick C. Sailes, Daniel P. Sutherlin
  • Publication number: 20090216015
    Abstract: The present invention relates to novel base stable ionic liquids and uses thereof as solvents in chemical reactions, especially base catalysed chemical reactions and reactions comprising the use of strong basis.
    Type: Application
    Filed: January 4, 2006
    Publication date: August 27, 2009
    Applicant: The Queen's University of Belfast
    Inventors: Martyn J. Earle, Ute Frohlich, Susanne Huq, Suhas Katdare, Rafal Marcin Lukasik, Ewa Bogel, Natalia Vladimirovna Plechkova, Kenneth Richard Seddon
  • Patent number: 7572790
    Abstract: Compound of formula (I): or pharmaceutically acceptable derivatives thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.
    Type: Grant
    Filed: April 7, 2004
    Date of Patent: August 11, 2009
    Assignee: SmithKline Beecham Corporation
    Inventors: Nicola Mary Aston, Paul Bamborough, Katherine Louise Jones, Vipulkumar Kantibhai Patel, Stephen Swanson, Ann Louise Walker
  • Publication number: 20090181943
    Abstract: This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula compounds of the Formula (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein groups L, M, X and Y are as defined herein.
    Type: Application
    Filed: April 9, 2008
    Publication date: July 16, 2009
    Applicant: METHYLGENE INC.
    Inventors: Pierre Tessier, Silvana Leit, David Smil, Robert Deziel, Alain Ajamian, Yves Andre Chantigny, Celia Dominguez
  • Publication number: 20090163496
    Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.
    Type: Application
    Filed: October 30, 2007
    Publication date: June 25, 2009
    Applicant: UNIVERSITY OF WASHINGTON
    Inventors: Niels H. ANDERSEN, Jason BOWMAN
  • Patent number: 7531651
    Abstract: Compounds of formula (I): wherein A? represents the benzenesulphonate (besylate) anion;. R represents H or C1-6 alkyl; and n is a number from 0.8 to 2.2 are CCR3 antagonists and are therefore indicated to be useful in therapy are described.
    Type: Grant
    Filed: March 27, 2003
    Date of Patent: May 12, 2009
    Assignee: Glaxo Group Limited
    Inventors: John Spencer Cook, Robert Philip Landon, Andrew John Walker, Mark Wilkinson
  • Patent number: 7528131
    Abstract: This disclosure relates to novel substituted morpholinyl compounds and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a 5HT4 serotonin receptor agonist.
    Type: Grant
    Filed: April 18, 2008
    Date of Patent: May 5, 2009
    Assignee: Concert Pharmaceuticals Inc.
    Inventors: Rose A. Persichetti, Scott L. Harbeson
  • Publication number: 20090062530
    Abstract: A compound represented by the formula (I): [In the formula, Link represents a saturated or unsaturated straight hydrocarbon chain having 1 to 3 carbon atoms, C2 to C6 in the aromatic ring (E) independently represent a ring-constituting carbon atom, one of the ring-constituting carbon atoms may be replaced with V, V represents nitrogen atom, or carbon atom substituted with Zx, Zx represents a saturated alkyl group having 1 to 4 carbon atoms and the like, Rs represents -D-Rx etc., D represents a single bond, oxygen atom and the like, Rx represents a saturated alkyl group having 3 to 8 carbon atoms and the like, AR represents a partially unsaturated or completely unsaturated condensed bicyclic carbon ring or a heterocyclic ring, and Y represents hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms and the like] or a salt thereof. A compound having prostaglandin production-suppressing action and leukotriene production-suppressing action is provided.
    Type: Application
    Filed: October 8, 2008
    Publication date: March 5, 2009
    Applicant: Asahi Kasei Pharma Corporation
    Inventors: Motoshi Shoda, Hiroshi Kuriyama
  • Publication number: 20090042730
    Abstract: The invention relates to novel aryl ketones of the formula (I) in which A1, A2, Q, R1, R2, X, Y and Z are as defined in the description, their use as herbicides and processes and intermediates for their preparation.
    Type: Application
    Filed: September 4, 2008
    Publication date: February 12, 2009
    Inventors: Stefan Herrmann, Dorothee Hoischen, Kristian Kather, Klaus-Helmut Muller, Otto Schallner, Hans-Georg Schwarz, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
  • Publication number: 20090029999
    Abstract: This invention provides compounds having the structural formula: wherein: R1 is an acyl or sulfonyl group, R2 is an acyl group selected from the group consisting of acyl groups derived from cycloaliphatic, aromatic or heterocyclic monocarboxylic acids, imidazolylcarbonyl and triazolylcarbonyl, and R3 is hydrogen or an amino-protecting group, a stereoisomer thereof, a solvate thereof, or a salt thereof, being useful as anti-inflammatory agents and anti-cancer agents.
    Type: Application
    Filed: June 23, 2008
    Publication date: January 29, 2009
    Applicant: UNIVERSITEIT GENT
    Inventors: Wim VANDEN BERGHE, Karolien DE Bosscher, Serge Van Calenbergh, Guy Haegeman, Carl Jeffrey Lacey, Valerie Gossye, Ruben Hoya Arias, Sarah Gerlo
  • Publication number: 20090023734
    Abstract: The invention provides compounds and methods for treating cell proliferative diseases. The invention provides new inhibitors of histone deacetylase enzymatic activity, compositions of the compounds comprising the inhibitors and a pharmaceutically acceptable carrier, excipient, or diluent, and methods of using the compounds to inhibit cellular proliferation in vitro and therapeutically.
    Type: Application
    Filed: January 8, 2007
    Publication date: January 22, 2009
    Applicant: METHYLGENE INC.
    Inventors: Stephane Raeppel, Frederic Gaudette, Isabelle Paquin, Arkadii Vaisburg, Daniel Delorme
  • Publication number: 20090023736
    Abstract: Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: April 28, 2008
    Publication date: January 22, 2009
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Keizo Koya, Weiwen Ying, Teresa Przewloka, Lijun Sun
  • Patent number: 7476686
    Abstract: The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections.
    Type: Grant
    Filed: December 17, 2004
    Date of Patent: January 13, 2009
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Dawei Chen, Milind Deshpande, Andrew Thurkauf, Avinash Phadke, Xiangzhu Wang, Yiping Shen, Cuixian Liu, Jesse Quinn, Junko Ohkanda, Shouming Li
  • Patent number: 7476672
    Abstract: This invention is directed to acetylenic compounds as inhibitors of a nicotinamide adenine dinucleotide oxidase hydride donor useful in treating or ameliorating a reactive oxygen species mediated inflammatory disorder.
    Type: Grant
    Filed: January 10, 2006
    Date of Patent: January 13, 2009
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Scott Beers, Elizabeth A. Malloy, Michael P. Wachter
  • Publication number: 20080261981
    Abstract: Novel amino acid derivatives are provided that are useful for management of disorders such as obesity and immunological diseases. The derivatives are also useful in lowering blood glucose levels in hyperglycemic disorders and for treating related disorders such as body weight gain, elevated free fatty acid, cholesterol and triglyceride levels and other disorder exacerbated by obesity.
    Type: Application
    Filed: June 3, 2008
    Publication date: October 23, 2008
    Inventors: DEBENDRANATH DEY, Abjiheet Nag, Bindu Pandey, Preeti Balse, Partha Neogi, Bishwajit Nag
  • Publication number: 20080234274
    Abstract: The present invention relates to compounds and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases S, K, F, L and B. Of particular interest are diseases associated with Cathepsin S. In addition this invention also discloses processes for the preparation of such inhibitors.
    Type: Application
    Filed: June 3, 2008
    Publication date: September 25, 2008
    Applicant: ASTRAZENECA AB
    Inventors: Andrew Bailey, Garry Pairaudeau, Anil Patel, Stephen Thom
  • Publication number: 20080200461
    Abstract: The present invention provides compounds of formula I: along with methods of use thereof for the control of agricultural pests, particularly fungal pests, weedy pests and insect pests, as well as use as pharmaceuticals, particularly the treatment of obesity, metabolic syndrome, atherosclerosis, cardiovascular disease and insulin resistance, e.g.
    Type: Application
    Filed: February 20, 2008
    Publication date: August 21, 2008
    Inventors: Richard Anderson, Takeo Hokama, Shy-Fuh Lee, Rafael Oey, Tedd Elich, Steven Breazeale
  • Publication number: 20080200467
    Abstract: Disclosed are alpha keto amide and alpha hydroxy amide compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, pulmonary, and diabetic-related diseases.
    Type: Application
    Filed: November 2, 2007
    Publication date: August 21, 2008
    Inventors: Dinesh Patel, Richard D. Gless, Heather K. Webb Hsu, Sampath Kumar Anandan, Bhaskar R. Aavula
  • Publication number: 20080194536
    Abstract: The present invention relates to a compound represented by the following formula: (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, or a combination thereof, wherein Ro, R1, R1?, R2, R2?, R3 and n are defined herein. The present invention further relates to a method of treating a patient from endometreosis or uterine fibroids.
    Type: Application
    Filed: April 14, 2006
    Publication date: August 14, 2008
    Inventors: Marlys Hammond, David G. Jones, Istvan Kaldor, Lara S. Kallander, Xi Lang, Scott Kevin Thompson, Philip Stewart Turnbull, David G. Washburn
  • Publication number: 20080139564
    Abstract: Certain substituted phenyl propyl amine compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases.
    Type: Application
    Filed: November 14, 2007
    Publication date: June 12, 2008
    Inventors: John M. Keith, Jennifer M.B. Miller, Emily M. Stocking
  • Patent number: 7361655
    Abstract: The subject invention relates to carboxamidine derivatives, to pharmaceutical compositions containing the carboxamidine derivatives of the invention, and the use thereof for the treatment of vascular diseases and in the preparation of pharmaceutical compositions for the treatment of vascular diseases.
    Type: Grant
    Filed: July 12, 2004
    Date of Patent: April 22, 2008
    Assignee: CytRx Corporation
    Inventors: Zita Jegesné Csákai, Ede Márványos, László Ürögdi, Magdolna Bathóné Török, László Dénes
  • Patent number: 7338952
    Abstract: This invention is directed to acetylenic compounds as inhibitors of a nicotinamide adenine dinucleotide oxidase hydride donor useful in treating or ameliorating a reactive oxygen species mediated inflammatory disorder.
    Type: Grant
    Filed: January 10, 2006
    Date of Patent: March 4, 2008
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Scott Beers, Elizabeth A. Malloy, Michael P. Wachter
  • Patent number: 7335681
    Abstract: Novel prodrugs of amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.
    Type: Grant
    Filed: September 15, 2006
    Date of Patent: February 26, 2008
    Assignee: The Regents of the University of Michigan
    Inventor: James A. Shayman
  • Publication number: 20080021023
    Abstract: The present invention relates to morpholinyl, and pyrrolidinyl analogs, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.
    Type: Application
    Filed: July 20, 2007
    Publication date: January 24, 2008
    Inventors: Krista B. Goodman, Michael J. Neeb, Clark A. Sehon, Andrew Q. Viet, Gren Z. Wang
  • Publication number: 20080004258
    Abstract: Certain substituted butyl and butynyl benzyl amine compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases.
    Type: Application
    Filed: June 21, 2007
    Publication date: January 3, 2008
    Inventors: John M. Keith, Michael A. Letavic, Emily M. Stocking
  • Publication number: 20080004443
    Abstract: Sulfonated block copolymer suitable for use as proton exchange membranes for fuel cells comprise sulfonated polyaryletherketone blocks and polyethersulfone blocks. The sulfonated polyaryletherketone blocks comprise structural units of formula I wherein R1 is C1-C10 alkyl, C3-C12 cycloalkyl, C6-C14 aryl, allyl, alkenyl, alkoxy, halo, or cyano; Ar1 and Ar2 are each independently C6-C20 aromatic radicals, or Ar1 and Ar2, taken together with an intervening carbon atom, form a bicyclic C6-C20 aromatic radical or a tricyclic C6-C20 aromatic radical; M is H, a metal cation, a non-metallic inorganic cation, an organic cation or a mixture thereof; and a is 0 or an integer from 1 to 4.
    Type: Application
    Filed: July 3, 2006
    Publication date: January 3, 2008
    Inventors: Daniel Joseph Brunelle, Hongyi Zhou, Hongwei Liu, Joyce Hung, Marianne Elisabeth Harmon, David Roger Moore
  • Patent number: 7314872
    Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S. More particularly, the present invention provides compounds having Formula I: wherein Q is morpholinyl; and A, R5, R6, R7, R8, R9 and Ar are substituents.
    Type: Grant
    Filed: August 18, 2004
    Date of Patent: January 1, 2008
    Assignee: IRM LLC
    Inventors: Hong Liu, Arnab Chatterjee, David C. Tully, Phillip Alper, Badry Bursulaya, Jianhua Guo, David H. Woodmansee, Daniel Mutnick, Donald S. Karanewsky, Yun He
  • Publication number: 20070255057
    Abstract: A method of nitrating a compound selected from the group consisting of is provided.
    Type: Application
    Filed: February 27, 2007
    Publication date: November 1, 2007
    Inventors: Miall Cedilote, Thomas Patrick Cleary, Pingsheng Zhang
  • Patent number: 7288540
    Abstract: Substituted phenylalkynes of formula (I) compositions containing them and their methods of use to treat histamine related disorders are described, wherein R1, R2, R3, R4, R5 and n are as defined.
    Type: Grant
    Filed: July 20, 2006
    Date of Patent: October 30, 2007
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Richard Apodaca, Xiaohu Deng, Jill A. Jablonowski, Neelakandha Mani, Chennagiri R. Pandit, Wei Xiao
  • Publication number: 20070238710
    Abstract: This invention concerns N-(ortho phenylaminoaryl), N?-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.
    Type: Application
    Filed: April 11, 2007
    Publication date: October 11, 2007
    Applicant: ARDEA BIOSCIENCES
    Inventors: Shunqi Yan, Jean-Michel Vernier, Zhi Hong
  • Patent number: 7247748
    Abstract: Disclosed is a compound having the formula (I) pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables are as defined herein.
    Type: Grant
    Filed: March 26, 2003
    Date of Patent: July 24, 2007
    Assignee: SmithKline Corporation
    Inventors: Scott K. Thompson, James S. Frazee, Lara S. Kallander, Chun Ma, Joseph P. Marino, Michael J. Neeb, Ning Wang
  • Patent number: 7217706
    Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.
    Type: Grant
    Filed: February 14, 2002
    Date of Patent: May 15, 2007
    Assignee: Astellas Pharma Inc.
    Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
  • Patent number: 7176330
    Abstract: A novel fluorescent group-containing carbodiimide compound having at least one group selected from a carboxyl group, a sulfo group, a phosphono group and a phospho group which have substitution of an alkali metal, an alkaline earth metal or a basic group containing a nitrogen or phosphorus atom, which is prepared by using a novel fluorescent group-containing carbodiimide compound precursor having a halogen atom or a sulfonic acid group; and a method for detecting a nucleic acid by hybridization utilizing a nucleic acid labeled with a labeling substance, which utilizes the fluorescent group-containing carbodiimide compound as the labeling substance.
    Type: Grant
    Filed: September 2, 2003
    Date of Patent: February 13, 2007
    Assignee: Nisshingo Industries, Inc.
    Inventors: Naoki Kimura, Namiko Shiohata, Yoko Yoshikawa