Hydroxy, Bonded Directly To Carbon, Or Ether In Substituent Q (h Of -oh May Be Replaced By A Substituted Or Unsubstituted Ammonium Ion Or A Group Ia Or Iia Light Metal) Patents (Class 564/165)
  • Publication number: 20110301179
    Abstract: A compound (particularly useful for inhibiting cancer) according to formula I: or a pharmaceutically acceptable salt thereof, wherein: x is 0 or 1; R1-R6 are each independently H, —CN, —NO2, —NO, —OH, halogen, hydroxyalkyl, carboxyl, substituted carboxyl, aminocarbonyl, alkoxy, carbonyl or substituted carbonyl; R7 is H, alkyl, alkyl amino, aminoacyl, hydroxyacyl, heteroaryl, heterocycloalkyl, alkyl heteroaryl or alkyl heterocycloalkyl; R8 is H or alkyl; A is O or N; and Ar is an aryl, substituted aryl, heteroaryl, or substituted heteroaryl, provided that if R7 is H then Ar is aryl substituted with alkyl amino.
    Type: Application
    Filed: October 21, 2009
    Publication date: December 8, 2011
    Inventors: Xiangshu Xiao, Bingbing Li
  • Patent number: 8063105
    Abstract: The present invention relates to novel renin inhibitors of the general Formula (I), and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds. These novel renin inhibitors are used in treating cardiovascular events and renal insufficiency.
    Type: Grant
    Filed: July 20, 2006
    Date of Patent: November 22, 2011
    Assignee: Merck Canada Inc.
    Inventors: Christopher I. Bayly, Austin C. Chen, Daniel Dube, Laurence Dube, Michel Gallant, Patrick Lacombe, Dwight MacDonald, Daniel McKay, David A. Powell, Erich L. Grimm
  • Publication number: 20110263604
    Abstract: The invention relates to phenylcyclopropylamine acetamide derivatives and their use in treating diseases.
    Type: Application
    Filed: April 18, 2011
    Publication date: October 27, 2011
    Applicant: Oryzon Genomics, S.A.
    Inventors: Nathalie Guibourt, Alberto Ortega Munoz, Julio Castro-Palomino Laria
  • Publication number: 20110244531
    Abstract: The invention relates to a process for the preparation of compounds that are important building blocks in convergent synthesis routes to 2(S),4(S),5(S),7(S)-2,7-dialkyl-4-hydroxy-5-amino-8-aryl-octanoyl amides or pharmaceutically acceptable salts thereof, such as the compound Aliskiren, and to a process for the preparation of these octanoyl amides, comprising reacting said building block.
    Type: Application
    Filed: July 23, 2009
    Publication date: October 6, 2011
    Inventors: Andreas Hendrikus Maria De Vries, Gerardus Karel Maria Verzijl, Petrus Johannes Hermsen, Anna Maria Cornelia Francisca Castelijns
  • Publication number: 20110230465
    Abstract: Compounds of formula I: wherein X, R2, R3, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
    Type: Application
    Filed: September 16, 2010
    Publication date: September 22, 2011
    Applicant: BOEHRINGER INGLEHEIM INTERNATIONAL GMBH
    Inventors: Timothy STAMMERS, Xavier BARBEAU, Pierre BEAULIEU, Megan BERTRAND-LAPERLE, Christian BROCHU, Paul J. EDWARDS, Pasquale FORGIONE, Cédrickx GODBOUT, Oliver HUCKE, Marc-André JOLY, Serge LANDRY, Olivier LEPAGE, Julie NAUD, Marc PESANT, Martin POIRIER, Maude POIRIER, Bounkham THAVONEKHAM
  • Publication number: 20110212943
    Abstract: Provided herein are novel bridged cyclic derivatives of the general formula (I), their analogs, tautomeric forms, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds can inhibit HDACs and are useful as therapeutic or ameliorating agent for diseases that are involved in cellular growth such as malignant tumors, autoimmune diseases, skin diseases, infections, inflammation, neurode-generative disorders etc.
    Type: Application
    Filed: October 14, 2009
    Publication date: September 1, 2011
    Applicant: ORCHID RESEARCH LABORATORIES LIMITED
    Inventors: Gopalan Balasubramanian, Ponpandian Thanasekaran, Sridharan Rajagopal, Bharathimohan Kuppusamy, Virendra Kachhadia, Vignesh Radhakrishnan, Sivasudar Velaiah, Shridhar Narayanan, Mandar Bhonde, Praveen Rajendran, Sriram Rajagopal
  • Publication number: 20110207654
    Abstract: The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as opioid agonists.
    Type: Application
    Filed: February 24, 2011
    Publication date: August 25, 2011
    Inventors: Christopher Gordon Barber, Dafydd Rhys Owen, Lisa Rosemary Thompson
  • Publication number: 20110195979
    Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R4 and Ar are as defined in description and in claims, can be used as a medicament.
    Type: Application
    Filed: February 7, 2011
    Publication date: August 11, 2011
    Inventors: Li Chen, Xianfeng Lin, Zongxing Qiu, Guozhi Tang, Lisha Wang, Jim Zhen Wu, Wengang Yang
  • Publication number: 20110104765
    Abstract: Provided herein are compositions including diastereomers in substantially diastereomerically pure form and enantiomers in substantially enantiomerically pure form, and processes for preparing them and converting them to metyrosine.
    Type: Application
    Filed: October 29, 2010
    Publication date: May 5, 2011
    Inventors: Kevin John HALLORAN, Alex COMELY, Zhengming CHEN, Shyam KRISHNAN
  • Patent number: 7910774
    Abstract: The present invention relates to synthetic routes to prepare a compound of the formula wherein R1 is halogen, C1-6halogenalkyl, C1-6alkoxy-C1-6alkyloxy or C1-6alkoxy-C1-6alkyl; R2 is halogen, C1-4alkyl or C1-4alkoxy; R3 and R4 are independently branched C3-6alkyl; and R5 is cycloalkyl, C1-6alkyl, C1-6hydroxyalkyl, C1-6alkoxy-C1-6alkyl, C1-6alkanoyloxy-C1-6alkyl, C1-6aminoalkyl, C1-6alkylamino-C1-6alkyl, C1-6dialkylamino-C1-6alkyl, C1-6alkanoylamino-C1-6alkyl, HO(O)C—C1-6alkyl, C1-6alkyl-O—(O)C—C1-6alkyl, H2N—C(O)—C1-6alkyl, C1-6alkyl-HN—C(O)—C1-6alkyl or (C1-6alkyl)2N—C(O)—C1-6alkyl; or a pharmaceutically acceptable salt thereof as well as key intermediates obtained when following these routes as well as their preparation.
    Type: Grant
    Filed: August 30, 2005
    Date of Patent: March 22, 2011
    Assignee: Novartis AG
    Inventors: Gottfried Sedelmeier, Stuart John Mickel, Heinrich Rueeger
  • Publication number: 20110046129
    Abstract: 2-Phenylethylamino substituted carboxamide derivatives and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies are presented.
    Type: Application
    Filed: September 9, 2010
    Publication date: February 24, 2011
    Applicant: Newron Pharmaceuticals S.p.A.
    Inventors: Florian Thaler, Mauro Napoletano, Cibele Sabido-David, Ermanno Moriggi, Carla Caccia, Laura Faravelli, Alessandra Restivo, Patricia Salvati
  • Publication number: 20110021506
    Abstract: This invention is directed to compounds and salts that are generally useful as anthelmintic agents or as intermediates in processes for making anthelmintic agents. This invention also is directed to processes for making the compounds and salts, pharmaceutical compositions and kits comprising the compounds and salts, uses of the compounds and salts to make medicaments, and treatments comprising the administration of the compounds and salts to animals in need of the treatments.
    Type: Application
    Filed: December 16, 2008
    Publication date: January 27, 2011
    Applicant: INTERVET INTERNATIONAL B.V.
    Inventors: Christophe Pierre Alain Chassaing, Jörg Schröder, Thomas Simon Ilg, Manfred Uphoff, Thorsten Meyer
  • Publication number: 20100331567
    Abstract: The present invention relates to a process for the preparation of iodinated phenols, —in particular, it relates to a process including the electrochemical iodination of 3,5-disubstituted phenols of formula (1) to the corresponding 3,5-disubstituted-2,4,6-triiodophenols of formula (2), which are useful intermediates for the synthesis of x-ray contrast media, and to the preparation of the contrast media themselves. Furthermore, the present invention includes the electrochemical iodination of 3,5-disubstituted anilines of formula (6) to the corresponding 3,5-disubstituted-2,4,6-triiodoanilins of formula (7).
    Type: Application
    Filed: February 16, 2009
    Publication date: December 30, 2010
    Applicant: BRACCO IMAGING S.P.A.
    Inventors: Giovanni Battista Giovenzana, Camilla Cavallotti, Luciano Lattuada, Fulvio Uggeri
  • Publication number: 20100324046
    Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Application
    Filed: June 24, 2008
    Publication date: December 23, 2010
    Inventors: Paul Harrington, Richard W. Heidebrecht, JR., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, Paul Tempest, Kevin J. Wilson, David J. Witter
  • Publication number: 20100324141
    Abstract: A process for obtaining therapeutically active 2-[4-(3- and 2-(fluorobenzyloxy)benzylamino]-propanamides and their salts with pharmaceutically acceptable acids with a high degree of purity, i.e. with a content of dibenzyl derivatives impurities lower than 0.03% by weight. The process is carried out by submitting a Schiff base intermediate to a reduction reaction with a reducing agent in an amount of organic solvent to allow the formation (and presence during a substantial portion of the reduction reaction) of a suspension of the Schiff base.
    Type: Application
    Filed: December 1, 2008
    Publication date: December 23, 2010
    Applicant: NEWRON PHARMACEUTICALS S.P.A.
    Inventors: Elena Barbanti, Laura Faravelli, Patricia Salvati, Renato Canevotti, Francesco Ponzini
  • Publication number: 20100298330
    Abstract: The present invention is related to the preparation and pharmaceutical In use of novel haloallylamine derivatives as SSAO/VAP-1 inhibitors having the structure of Formula I, as defined in the specification:(I). The invention also relates to methods of using invention compounds, or pharmaceutically acceptable salt or derivatives thereof, for the treatment of a variety of indications, e.g., inflammatory diseases.
    Type: Application
    Filed: November 19, 2008
    Publication date: November 25, 2010
    Applicant: PHARMAXIS LTD.
    Inventors: Ian A. McDonald, Craig Ivan Turner, Mandar Deodhar, Jonathan Stuart Foot
  • Publication number: 20100298402
    Abstract: Described are novel compounds of the formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites, and prodrugs thereof. These novel compounds can inhibit pSTAT3/IL-6 and are useful as a therapeutic or ameliorating agent for diseases that are involved in cellular growth such as malignant tumors, autoimmune diseases, skin diseases, infections, inflammation, etc.
    Type: Application
    Filed: November 4, 2008
    Publication date: November 25, 2010
    Applicant: ORCHID RESEARCH LABORATORIES LIMITED
    Inventors: Sridharan Rajagopal, Thangapazham Selvakumar, Kuppusamy Bharathimohan, Virendra Kachhadia, Sriram Rajagopal, Rajendran Praveen, Ramachandran Balaji
  • Publication number: 20100215710
    Abstract: Methods for increasing rate of healing of wounds in epithelial tissues by administration of beta-2 adrenergic receptor antagonists to target patients are provided. Methods for decreasing cell growth around implanted devices and methods for decreasing wound contraction by administration of beta-2 adrenergic receptor agonists are also provided. Pharmaceutical compositions and kits including beta-2 adrenergic receptor agonists and antagonists are described, as are devices coated with beta-2 adrenergic receptor agonists.
    Type: Application
    Filed: April 10, 2006
    Publication date: August 26, 2010
    Inventors: Roslyn Rivkah Isseroff, Christine E. Pullar
  • Publication number: 20100210631
    Abstract: Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives, pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing them are useful as sodium and/or calcium channel modulators for preventing, alleviating and curing pathologies wherein the above mechanisms play a pathological role. The compounds may be particularly used for the prevention, alleviation, and curing of, for example, neurological, cognitive, psychiatric, inflammatory, urogenital, and gastrointestinal diseases.
    Type: Application
    Filed: May 14, 2008
    Publication date: August 19, 2010
    Applicant: NEWRON PHARMACEUTICALS S.P.A.
    Inventors: Piero Melloni, Alessandra Restivo, Emanuela Izzo, Simona Francisconi, Elena Colombo, Cibele Sabido-David
  • Patent number: 7759520
    Abstract: The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor.
    Type: Grant
    Filed: February 23, 2005
    Date of Patent: July 20, 2010
    Assignee: University of Tennessee Research Foundation
    Inventors: James T. Dalton, Duane D. Miller, Donghua Yin, Yali He
  • Publication number: 20100124550
    Abstract: The present invention relates to new amide inhibitors of renin, pharmaceutical compositions thereof, and methods of use thereof
    Type: Application
    Filed: November 20, 2009
    Publication date: May 20, 2010
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Thomas G. Gant, Manouchehr M. Shahbaz
  • 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
  • Patent number: 7700655
    Abstract: A medicament for the preventive and/or therapeutic treatment of allergic diseases and/or endometriosis and/or hysteromyoma which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in the main chain is 2 to 5 (said connecting group may be substituted), A represents hydrogen atom or acetyl group, E represents an aryl group which may be substituted or a hetero aryl group which may be substituted, ring Z represents an arene which may have one or more substitutents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —X-E wherein each of X and E has the same meaning as that defined above, or a heteroarene which may have one or more substitutents in addition to the group represe
    Type: Grant
    Filed: April 9, 2007
    Date of Patent: April 20, 2010
    Assignee: Institute of Medicinal Molecular Design, Inc.
    Inventors: Susumu Muto, Akiko Itai
  • Publication number: 20100016403
    Abstract: Compounds of Formula I are useful for the treatment of anxiety disorders such as generalized anxiety disorder (GAD), panic attack, post traumatic stress disorder (PTSD), obsessive compulsive disorder (OCD) and social phobias. wherein: A is chosen from: aryl or heteroaryl, A being optionally substituted with up to 5 independently-selected groups R8; R1 is chosen from: alkyl or haloalkyl; R2 is chosen from: H, C(O)R6, C(O)OR6, SO2R6 or C(O)NR6R7; R3, R4 and R5 are independently chosen from: H or alkyl; R6 and R7 are independently chosen from: H or alkyl; and R8 is chosen from: OH, CN, halo, alkyl, alkoxy, haloalkyl, haloalkoxy, C(O)R6, C(O)OR6, SO2R6 or C(O)NR6R7.
    Type: Application
    Filed: December 14, 2007
    Publication date: January 21, 2010
    Inventors: Guy Higgins, Abdelmalik Slassi, Methvin Isaac
  • Patent number: 7629358
    Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
    Type: Grant
    Filed: March 16, 2005
    Date of Patent: December 8, 2009
    Assignee: Pfizer Inc
    Inventors: Alan Daniel Brown, Charlotte Alice Louise Lane, Paul Alan Glossop, David Anthony Price, Russell Andrew Lewthwaite, Mark Edward Bunnage, Kim James, Graham Lunn
  • Publication number: 20090281085
    Abstract: Compounds according to the formula below are disclosed herein: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Application
    Filed: February 3, 2009
    Publication date: November 12, 2009
    Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello, Rong Yang, Cédric Chauvignac
  • Publication number: 20090281103
    Abstract: The present invention relates to novel renin inhibitors of the general Formula (I), and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds. These novel renin inhibitors are used in treating cardiovascular events and renal insufficiency.
    Type: Application
    Filed: July 20, 2006
    Publication date: November 12, 2009
    Inventors: Christopher I. Bayly, Austin C. Chen, Daniel Dube, Laurence Dube, Michel Gallant, Patrick Lacombe, Dwight MacDonald, Daniel McKay, David A. Powell, Erich L. Grimm
  • Patent number: 7615664
    Abstract: Compounds of the general formula (I) in which the substituents R, R1, R2, R3, R4, R5 and R6 are each as defined in claim 1 have renin-inhibiting properties and can be used as medicaments.
    Type: Grant
    Filed: December 9, 2005
    Date of Patent: November 10, 2009
    Assignee: Speedel Experimenta AG
    Inventors: Peter Herold, Stefan Stutz, Robert Mah, Vincenzo Tschinke, Christiane Marti
  • Publication number: 20090253701
    Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.
    Type: Application
    Filed: June 12, 2009
    Publication date: October 8, 2009
    Inventors: Daniel Kaspar Baeschlin, Juergen Klaus Maibaum, holger Sellner
  • Publication number: 20090253166
    Abstract: Methods for the selective conjugation of peptides which comprises an enzymatic incorporation of a functional group at the C-terminal end of a peptide followed by reaction with a second compound comprising the moiety to be conjugated to the peptide, wherein said second compound comprises a functional group which selectively reacts with the incorporated functional group.
    Type: Application
    Filed: March 18, 2009
    Publication date: October 8, 2009
    Applicant: Novo Nordisk A/S
    Inventors: Magali A. Zundel, Bernd Peschke, Florencio Zaragoza Dorwald, Niels Peter Fiil, Nils Langeland Johansen, Henning Ralf Stennicke
  • Publication number: 20090238756
    Abstract: Compositions and methods for imaging and for chemotherapy and radiotherapy are disclosed. More particularly, the invention concerns agents comprising a targeting moeity comprising a beta-adrenergic receptor targeting compound conjugated or embedded with ethylenediamine. The present invention also concerns methods of application of such agents for imaging and treatment of cardiovascular diseases, and kits for preparing a radiolabeled therapeutic or diagnostic agent.
    Type: Application
    Filed: December 19, 2008
    Publication date: September 24, 2009
    Inventors: David J. Yang, Chang-Sok Oh, Saady Kohanim, Dong-Fang Yu, Richard Mendez, E. Edmund Kim
  • Patent number: 7582782
    Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.
    Type: Grant
    Filed: November 25, 2004
    Date of Patent: September 1, 2009
    Assignee: Novartis AG
    Inventors: Daniel K Baeschlin, Juergen K Maibaum, Holger Sellner
  • Patent number: 7563888
    Abstract: The present invention is a process for the preparation of diphenylazetidinone derivatives of the formula (I) or forms thereof comprising the substituents X, R1 and/or R2 as defined herein. More specifically, the invention comprises methods for the preparation of these compounds by cyclization of certain ?-amino carboxamides or ?-amino carboxylic esters. These diphenylazetidinone compounds are useful in the treatment of high blood serum cholesterol levels and the maintenance of the reduced cholesterol levels achieved thereby.
    Type: Grant
    Filed: November 7, 2006
    Date of Patent: July 21, 2009
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Joachim-Heiner Jendralla, Guenter Billen, Wendelin Frick, Bernd Junker, Theodor Andreas Wollman
  • Publication number: 20090176853
    Abstract: The invention provides adamantane derivatives of formula (I), a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy. In formula (I) D represents CH2 or CH2CH2, E represents C(O)NH or NHC(O) and R3 represents a group of formula (I).
    Type: Application
    Filed: December 4, 2008
    Publication date: July 9, 2009
    Inventors: Lilian Alcaraz, Moya Caffrey, Mark Furber, Timothy Luker, Michael Mortimore, Austen Pimm, Philip Thorne, Paul Willis
  • 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
  • Publication number: 20090156678
    Abstract: A process for obtaining therapeutically active 2-[4-(3- and 2-(fluorobenzyloxy)benzylamino]propanamides and their salts with pharmaceutically acceptable acids with high purity degree, in particular, with a content of dibenzyl derivatives impurities lower than 0.03%, preferably lower than 0.01% by weight. The process is carried out by submitting the Schiff bases intermediates 2-[4-(3- and 2-fluorobenzyloxy)benzylideneamino]propanamides to catalytic hydrogenation in the presence of a heterogeneous catalyst in a protic organic solvent.
    Type: Application
    Filed: December 18, 2008
    Publication date: June 18, 2009
    Applicant: NEWRON PHARMACEUTICALS S.P.A.
    Inventors: Elena Barbanti, Carla Caccia, Patricia Salvati, Francesco Velardi, Tiziano Ruffilli, Luigi Bogogna
  • Patent number: 7547731
    Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
    Type: Grant
    Filed: July 3, 2007
    Date of Patent: June 16, 2009
    Assignee: Pfizer Inc
    Inventors: Alan Daniel Brown, Mark Edward Bunnage, Charlotte Alice Louise Lane, Russell Andrew Lewthwaite, Paul Alan Glossop, Kim James, David Anthony Price
  • Publication number: 20090149544
    Abstract: This invention relates to novel alpha-aminoamide derivatives, their pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an inhibitor of monoamine oxidase type B (MAO-B) and/or a sodium (Na+) channel blocker, and/or a calcium (Ca2+) channel modulator.
    Type: Application
    Filed: October 22, 2008
    Publication date: June 11, 2009
    Applicant: CoNCERT Pharmaceuticals, Inc.
    Inventor: Julie F. Liu
  • Publication number: 20090131473
    Abstract: The present invention relates generally to novel 2-(aryloxy)acetamides of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables W, Y, Z, R7, R8, and R9 are as defined herein. These compounds are selective inhibitors of the serine protease coagulation factor VIIa which can be used as medicaments.
    Type: Application
    Filed: March 8, 2007
    Publication date: May 21, 2009
    Inventors: Alexandra A. Nirschl, Xiaojun Zhang
  • Publication number: 20090082378
    Abstract: This present disclosure relates to compounds of formula (I): The present disclosure also relates to pharmaceutical compositions comprising the compounds of formula (I) and to their methods of use in therapy.
    Type: Application
    Filed: April 24, 2007
    Publication date: March 26, 2009
    Inventors: Carlos Puig Duran, Maria Prat Quinones, Daniel Perez Crespo
  • Publication number: 20090074673
    Abstract: The disclosure provides, in part, compositions and methods for producing cellular labels for tracking cells by MRI. The disclosure provides, in part, methods for labeling, detecting and quantifying cell numbers in vivo.
    Type: Application
    Filed: July 10, 2008
    Publication date: March 19, 2009
    Applicant: Carnegie Mellon University
    Inventors: Jelena Janjic, Eric T. Ahrens
  • Publication number: 20090060917
    Abstract: The compound of formula (I) is a water-stable, long acting ?2-selective adrenoceptor agonist useful as a bronchodilator in the treatment of bronchoconstriction associated with reversible obstructive airways diseases and the like.
    Type: Application
    Filed: August 21, 2008
    Publication date: March 5, 2009
    Applicant: Sepracor Inc.
    Inventors: Craig R. Abolin, H. Scott Wilkinson, Paul McGlynn, William K. McVicar
  • Patent number: 7482487
    Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
    Type: Grant
    Filed: March 10, 2005
    Date of Patent: January 27, 2009
    Assignee: Pfizer Inc
    Inventors: Alan Daniel Brown, Justin Stephen Bryans, Paul Alan Glossop, Charlotte Alice Louise Lane, Simmon John Mantell
  • Publication number: 20080319057
    Abstract: 2-Phenylethylamino substituted carboxamide derivatives of formula (I); wherein J, W, R0, R1, R2, R3, and R4 have the meanings as defined in the specification and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them as active ingredient and their use as sodium and/or calcium channel modulators useful in preventing alleviating and curing a wide range of pathologies, including neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urology, and gastrointestinal diseases where the above mechanisms have been described as playing a pathological role, are described.
    Type: Application
    Filed: November 29, 2006
    Publication date: December 25, 2008
    Inventors: Florian Thaler, Mauro Napoletano, Cibele Sabido-David, Ermanno Moriggi, Carla Caccia, Laura Faravelli, Alessandra Restivo, Patricia Salvati
  • Publication number: 20080269221
    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: August 10, 2007
    Publication date: October 30, 2008
    Inventors: Niels H. Andersen, Jason Bowman, Alice Erwin, Eric Harwood, Toni Kline, Khisimuzi Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar
  • Publication number: 20080221217
    Abstract: The present invention is directed to compounds of formula (I) or a pharmaceutically acceptable salt thereof; wherein A is (xx); X is selected from CH, CF and N, R5 is selected from H, C1-C6 alkyl, C1-C6 fluoroalkyl, and —OR12, R9 is selected from H and —C(O)NR1OR11, R12 is selected from H, C1-C6 alkyl and C3-C6 cycloalkyl for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes.
    Type: Application
    Filed: July 14, 2006
    Publication date: September 11, 2008
    Inventors: Larry Chris Blaszczak, Shon Roland Pulley, Michael Alan Robertson, Scott Martin Sheehan, Qing Shi, Brian Morgan Watson, Michael Robert Wiley
  • Publication number: 20080176947
    Abstract: Compounds of the general formula (I) in which the meanings of the substituents R1 and R2 are as stated in claim 1, have renin-inhibiting properties and can be used as medicines.
    Type: Application
    Filed: March 10, 2006
    Publication date: July 24, 2008
    Inventors: Peter Herold, Robert Mah, Vincenzo Tschinke, Stefan Stutz, Dirk Behnke, Aleksandar Stojanovic, Stjepan Jelakovic, Christiane Marti
  • Publication number: 20080167381
    Abstract: Compounds of the general formula (I) in which R is heterocyclyl which is bonded via a carbon atom and is mono- or polysubstituted by C1-6-alkyl, trifluoromethyl, nitro, amino, C1-6-alkylamino, di-C1-6-alkylamino, C2-6-alkenyl, C2-6-alkynyl, C1-6-alkoxy, C1-6-alkylcarbonyloxy, C0-6-alkylcarbonylamino, C1-6-alkoxycarbonylamino, hydroxyl, halogen, oxide, cyano, optionally N-mono- or N,N-di-C1-8-alkylated carbamoyl, optionally esterified carboxyl or C1-6-alkylenedioxy, or is substituted by oxo and mono- or polysubstituted by C1-6-alkyl, trifluoromethyl, nitro, amino, C1-6-alkylamino, di-C1-6-alkylamino, C2-6-alkenyl, C2-6-alkynyl, C1-6-alkoxy, C1-6-alkylcarbonyloxy, C0-6-alkylcarbonylamino, C1-6-alkoxycarbonylamino, hydroxyl, halogen, oxide, cyano, optionally N-mono- or N,N-di-C1-8-alkylated carbamoyl, optionally esterified carboxyl or C1-6-alkylenedioxy, and salts, especially pharmaceutically usable salts have renin-inhibiting properties and can be used as medicaments.
    Type: Application
    Filed: December 9, 2005
    Publication date: July 10, 2008
    Inventors: Peter Herold, Stefan Stutz, Robert Mah, Vincenzo Tschinke
  • Publication number: 20080153902
    Abstract: Compounds of the general formula (I) in which the substituents R, R1, R2, R3, R4, R5 and R6 are each as defined in claim 1 have renin-inhibiting properties and can be used as medicaments.
    Type: Application
    Filed: December 9, 2005
    Publication date: June 26, 2008
    Inventors: Peter Herold, Stefan Stutz, Robert Mah, Vincenzo Tschinke, Christiane Marti
  • Patent number: 7390925
    Abstract: There is provided a series of substituted oxime-containing acyl guanidines of Formula (I) or a stereoisomer; or a nontoxic pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
    Type: Grant
    Filed: March 29, 2007
    Date of Patent: June 24, 2008
    Assignee: Bristol-Myers Squibb Company
    Inventors: Yong-Jin Wu, Samuel Gerritz, Shuhao Shi, Shirong Zhu