Nitrogen Containing Patents (Class 514/459)
  • Publication number: 20120070417
    Abstract: The invention relates to pharmaceutical compositions that contain a calcium salt as an active ingredient and also comprise another anti-influenza agent, and to methods for treating or preventing influenza virus infection.
    Type: Application
    Filed: March 26, 2010
    Publication date: March 22, 2012
    Applicant: PULMATRIX, INC.
    Inventors: Richard Batycky, David L. Hava, Robert W. Clarke, Michal M. Lipp
  • Publication number: 20120065171
    Abstract: Novel Fostriecin (or FST) derivatives represented by formula (I), the pharmaceutical compositions and preparation methods thereof. The pharmaceutical uses of these compounds, especially the use for the preparation of pharmaceutical compositions for treating tumor, inhibiting cell over growth, or lowering myocardial infarction and the injury to cells.
    Type: Application
    Filed: October 1, 2010
    Publication date: March 15, 2012
    Applicants: Dalian University of Technology, BayGen Pharm Technology Co., Ltd.
    Inventors: Li Tang, Rongguo Qiu
  • Publication number: 20120058937
    Abstract: A new class of neuramidase inhibitor prodrugs is provided characterized by a prodrug moiety of a carboxyl group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide or a carbonyl ethoxy tripeptide, a guanidine group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide, a carbonyl ethoxy tripeptide; a primary alcohol modified to form an esterified single amino acid, dipeptide or tripeptide of zanavimir of the unaltered therapeutic agent. Exemplary therapeutic agents so modified to form prodrugs include zanavimir, oseltamivir and peramivir. The prodrug has increased oral bioavailability relative to the unaltered neuraminidase inhibitor and is effective in the inhibition of viral infections involving neuraminidase in the viral reproductive cycle.
    Type: Application
    Filed: April 15, 2009
    Publication date: March 8, 2012
    Applicant: TSRL, Inc.
    Inventors: John Hilfinger, Gordon Amidon
  • Publication number: 20120046355
    Abstract: The present invention describes compounds of Formula I or a pharmaceutically acceptable salts or derivatives thereof. Compositions comprising compounds of Formula I are also described. The present invention further relates to a method of producing non-2-enonate compounds.
    Type: Application
    Filed: May 4, 2010
    Publication date: February 23, 2012
    Inventors: Ian C. Schoenhofen, Dennis M. Whitfield, Susan M. Logan
  • Publication number: 20120046331
    Abstract: This invention relates to new antifungal agents, compositions thereof, and methods for inhibiting the growth of fungi involved in infection and disease of keratinized tissue, such as onychomycosis. The invention also relates to new antifungal agents, compositions thereof, and methods for treating and/or preventing fungal infection and/or disease of keratinized tissue, such as onychomycosis. The invention further relates to a kit comprising said antifungal agent and use of said kit in treatment of fungal infection and/or disease of keratinized tissue, such as onychomycosis.
    Type: Application
    Filed: August 19, 2011
    Publication date: February 23, 2012
    Inventor: Jeffrey M. Besterman
  • Publication number: 20120041038
    Abstract: Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Application
    Filed: October 21, 2011
    Publication date: February 16, 2012
    Applicant: Acucela Inc.
    Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Thomas L. Little, JR., Ryo Kubota
  • Publication number: 20120041039
    Abstract: Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Application
    Filed: October 21, 2011
    Publication date: February 16, 2012
    Applicant: Acucela Inc.
    Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Thomas L. Little, JR., Ryo Kubota
  • Publication number: 20120041011
    Abstract: The present invention relates to substituted benzofused derivatives, which can he used as vanilloid receptor ligands, method of treating diseases, conditions and/or disorders modulated by vanilloid receptors with them, and processes for preparing them.
    Type: Application
    Filed: July 1, 2011
    Publication date: February 16, 2012
    Applicant: Glenmark Pharmaceuticals S.A.
    Inventors: Laxmikant Atmaram GHARAT, Uday Mukund JOSHI, Neelima KHAIRATKAR-JOSHI, Suresh Mahadev KADAM
  • Publication number: 20120041036
    Abstract: An object of the present invention is to provide an excellent agent for treating or preventing dementia, schizophrenia based on serotonin 5-HT5A receptor modulating action. It was discovered that acylguanidine derivatives, in which the guanidine is bonded to one ring of a naphthalene via a carbonyl group and a cyclic group is bonded to the other ring thereof, exhibit potent the 5-HT5A receptor modulating action and excellent pharmacological actions based on the action. The present invention is useful as an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder or attention deficit hyperactivity disorder.
    Type: Application
    Filed: February 8, 2010
    Publication date: February 16, 2012
    Inventors: Isao Kinoyama, Yohei Koganemaru, Takehiro Miyazaki, Takuya Washio
  • Publication number: 20120035255
    Abstract: The present invention relates to compounds having general formula (I), i.e. poly-alkyl-bis-maltolic molecules and in particular to derivates of [(3-hydroxy-4-pyron-2-yl)methyl]-amine and pharmaceutically acceptable salts thereof, and to the use thereof as anti-neoplastic drugs, in particular, for the preparation of a medicament for the treatment of neoplastic diseases.
    Type: Application
    Filed: November 27, 2009
    Publication date: February 9, 2012
    Applicant: Universita' Degli Studi Di Urbino
    Inventors: Mirco Fanelli, Vieri Fusi
  • Publication number: 20120035179
    Abstract: The present invention provides compounds of Formula I useful as modulators of ABC transporter activity, or a pharmaceutically acceptable salt thereof, wherein RB, n, B, RC, RD, RE, A, and Z are described generally and in classes and subclasses below. The present invention also provides pharmaceutical compositions, methods and kits associated with Formula I, useful for as modulators, and for the treatments of disease and disease conditions associated with ABC transporter proteins.
    Type: Application
    Filed: March 9, 2011
    Publication date: February 9, 2012
    Inventors: Sara S. Hadida-Ruah, Mark Miller, Ashvani Singh, Matthew Hamilton, Peter D.J. Grootenhuis
  • Publication number: 20120022039
    Abstract: The invention relates to substituted indanes and derivatives thereof, to physiologically acceptable salts and physiologically functional derivatives thereof, to the production thereof, to drugs containing at least one substituted indane according to the invention or derivative thereof, and to the use of the substituted indanes according to the invention and to derivatives thereof as MCH antagonists.
    Type: Application
    Filed: February 12, 2010
    Publication date: January 26, 2012
    Applicant: SANOFI
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Klaus Wirth
  • Publication number: 20120022100
    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: September 28, 2011
    Publication date: January 26, 2012
    Inventors: Juergen Klaus Maibaum, Daniel K. Baeschlin, Holger Sellner
  • Publication number: 20120014898
    Abstract: The present invention relates to the use of a composition comprising a compound of the formula I: wherein R is C2H5 or C2H3, or a pharmaceutically acceptable salt thereof, for preventing hair loss or stimulating hair growth.
    Type: Application
    Filed: July 29, 2010
    Publication date: January 19, 2012
    Inventor: Gee-Hwoon LEE
  • Publication number: 20120016017
    Abstract: The present invention relates to a compound of the formula I: wherein R is C2H5 or C2H3, or a pharmaceutically acceptable salt thereof, and a process for preparing said compound of the formula I. The invention also relates to the use of a composition comprising said compound of the formula I or a pharmaceutically acceptable salt thereof as an active ingredient, for treating or preventing cancers.
    Type: Application
    Filed: July 29, 2010
    Publication date: January 19, 2012
    Inventor: Gee-Hwoon LEE
  • Publication number: 20120015942
    Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: July 18, 2011
    Publication date: January 19, 2012
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Emily F. Calderwood, Dylan B. England, Alexandra E. Gould, Sean J. Harrison, Liting Ma
  • Publication number: 20120016019
    Abstract: The present invention relates to a compound of the formula I: wherein R is C2H5 or C2H3, or a pharmaceutically acceptable salt or hydrate thereof, and a process for preparing said compound of the formula I. The invention also relates to the use of a composition comprising said compound of the formula I or a pharmaceutically acceptable salt or hydrate thereof as an active ingredient, for treating or preventing cancers.
    Type: Application
    Filed: March 9, 2011
    Publication date: January 19, 2012
    Inventor: Gee-Hwoon LEE
  • Publication number: 20120016018
    Abstract: The present invention relates to the novel use of a composition comprising a compound of the formula I: wherein R is C2H5 or C2H3, or a pharmaceutically acceptable salt thereof, for inducing multiple nuclear divisions of cells; inducing tissues, blood vessels or organs to regenerate after the multiple nuclear divisions; or inducing stem cells to differentiate into immunocytes after the multiple nuclear divisions.
    Type: Application
    Filed: July 29, 2010
    Publication date: January 19, 2012
    Inventor: Gee-Hwoon LEE
  • Publication number: 20120015936
    Abstract: The invention relates to substituted tetrahydronaphthalenes, to derivatives thereof, to physiologically acceptable salts thereof, to physiologically functional derivatives, to the production thereof, to drugs containing at least one substituted tetrahydronaphthalene according to the invention or derivative thereof, and to the use of the substituted tetrahydronaphthalenes according to the invention and to derivatives thereof as MCH antagonists.
    Type: Application
    Filed: February 12, 2010
    Publication date: January 19, 2012
    Applicant: SANOFI
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Klaus Wirth
  • Publication number: 20120010161
    Abstract: The present invention relates to compounds of azapeptide or azapeptidomimetic type of formula (I): in which R1, R2, R3, X1, X2, X3, X4 and Y are as defined in claim 1, to pharmaceutical compositions containing them and to such compounds as adjuvant for an anticancer or anti-infectious medicament.
    Type: Application
    Filed: January 25, 2010
    Publication date: January 12, 2012
    Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE CLAUDE BERNARD LYON I
    Inventor: Joelle Paris
  • Publication number: 20120010227
    Abstract: The invention relates to a pharmaceutical composition with a content in active ingredient that can be an antimycotic, so that the composition is suitable for the treatment of onychomycoses, in particular severe onychomycoses. The inventive formulation is an ointment-like thermogel at body temperature and an inviscid thermogel at lower temperatures and facilitates the permeation of sufficient active ingredient quantities through human fingernails and toenails, in order to also treat severe onychomycoses.
    Type: Application
    Filed: July 29, 2010
    Publication date: January 12, 2012
    Applicant: Technische Universitat Braunschweig
    Inventors: Lusiana, Christel Müller-Goymann
  • Patent number: 8093289
    Abstract: An oral composition contains 3-{5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6-yl)methoxy]phenyl}propionic acid or a salt thereof and polyvinylpyrrolidone is advantageous as an oral medication composition (1) which can be produced without requiring new manufacturing equipment; (2) which can be produced with simple steps; (3) which maintains stable solubility even with changes in the pH of the gastrointestinal tract and of which gastrointestinal tract absorption is improved.
    Type: Grant
    Filed: May 25, 2007
    Date of Patent: January 10, 2012
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Sahoe Kakuda, Tatsuhito Yahata, Masashi Kaneko
  • Publication number: 20120004269
    Abstract: Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Application
    Filed: August 3, 2011
    Publication date: January 5, 2012
    Applicant: Acucela Inc.
    Inventors: Ian Leslie Scott, Vladimir Aleksandrovich Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Jennifer Gage, Feng Hong
  • Publication number: 20120004298
    Abstract: Ionic ophthalmic devices, methods of treating chemoattractant cytokine receptor 2 (CCR2) mediated inflammatory conditions, and methods of making such devices are disclosed herein.
    Type: Application
    Filed: June 29, 2011
    Publication date: January 5, 2012
    Inventors: Hassan Chaouk, Dijana Draganovic, Vandeeta Khanolkar
  • Publication number: 20120003306
    Abstract: The invention discloses a pharmaceutical composition of bioactive nanoparticles composed of chitosan, poly-glutamic acid, and a bioactive agent for oral delivery. The chitosan-based nanoparticles are characterized with a positive surface charge and enhanced permeability for oral drug delivery.
    Type: Application
    Filed: September 8, 2011
    Publication date: January 5, 2012
    Inventors: Hsing-Wen Sung, Kiran Sonaje, Hosheng Tu
  • Patent number: 8080541
    Abstract: The present invention relates to the use of a compound of formula I wherein R1, R2, R3, R4, X and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomers and/or optical isomers for the treatment of psychoses, pain, dysfunction in memory and learning, attention deficit, schizophrenia, dementia disorders or Alzheimer's disease.
    Type: Grant
    Filed: August 19, 2010
    Date of Patent: December 20, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Publication number: 20110306621
    Abstract: An object of the present invention is to provide an excellent agent for treating or preventing dementia, schizophrenia based on a serotonin 5-HT5A receptor modulating action. It was confirmed that acylguanidine derivatives, which has the characteristic structure in which the guanidine is bonded to one ring of a naphthalene via a carbonyl group and a cyclic group is bonded to the other ring thereof, exhibit potent 5-HT5A receptor modulating action and excellent pharmacological action based on the action. The present invention is useful as an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder or attention deficit hyperactivity disorder.
    Type: Application
    Filed: February 8, 2010
    Publication date: December 15, 2011
    Inventors: Isao Kinoyama, Takehiro Miyazaki, Yohei Koganemaru, Nobuyuki Shiraishi, Yuichiro Kawamoto, Takuya Washio
  • Publication number: 20110306542
    Abstract: Compounds that bind the glucagon-like peptide 1 receptor (GLP-1) receptor are provided including compounds which are modulators of the GLP-1 receptors and compounds which are capable of inducing a stabilizing effect on the receptor for use in structural analyses of the GLP-1 receptor. Methods of synthesis, methods of therapeutic and/or prophylactic use, and methods of use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor of such compounds are provided.
    Type: Application
    Filed: June 9, 2011
    Publication date: December 15, 2011
    Applicant: Receptos, Inc.
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Liming Huang, Junko Tamiya, Mark T. Griffith, Thomas Fowler, Andrew Novak, Michael Knaggs, Premji Meghani
  • Patent number: 8071575
    Abstract: Bone targeted compounds and methods are provided. Compounds can include a Bone Targeting Portion (RT), having an affinity for bone; a Bone Active Portion (RA) for interacting with and affecting bone; and a Linking Portion (RL) connecting the Bone Targeting Portion and the Bone Active Portion.
    Type: Grant
    Filed: February 22, 2008
    Date of Patent: December 6, 2011
    Assignee: University of Louisville Research Foundation
    Inventors: William M. Pierce, Jr., K. Grant Taylor, Leonard C. Waite
  • Publication number: 20110294830
    Abstract: The present invention provides a nitrogen-containing compound represented by formula (I1) (in formula (I1), R0 represents a nitro group or the like, Z represents an optionally substituted aryl group or the like, R3 represents a hydrogen atom or the like, Y represents a nitro group or the like, n represents an integer of 0 to 3, D represents an optionally substituted 5-membered to 8-membered hydrocarbon ring group or heterocyclic group having or not having a substituent other than substituent X, X represents a group represented by formula (II-1) (in formula (II-1), R1 and R2 respectively and independently represent a hydrogen atom or the like), A represents a carbon atom or the like, n1 represents an integer of 0 to 2) or a salt thereof, and an insecticide, miticide, sanitary insect pest control agent, or harmful organism control agent including as an active ingredient thereof the nitrogen-containing compound or the salt thereof.
    Type: Application
    Filed: February 5, 2010
    Publication date: December 1, 2011
    Applicant: Nippon Soda Co., Ltd.
    Inventors: Jyun Iwata, Masahiro Kawaguchi, Akiko Mizui
  • Publication number: 20110281879
    Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
    Type: Application
    Filed: January 12, 2011
    Publication date: November 17, 2011
    Applicant: ViroBay, Inc.
    Inventor: Craig Mossman
  • Publication number: 20110280813
    Abstract: The invention is related to various methods for inhibiting or reducing biofilm formation, treating a biofilm production-related disorder, preventing biofilm formation, and screening for neuraminidase inhibitors.
    Type: Application
    Filed: November 13, 2009
    Publication date: November 17, 2011
    Inventors: Alice Prince, Liang Tong
  • Patent number: 8058307
    Abstract: Compounds of the general formula (formula I) in which the meanings of the substituents R1 to R6 are as indicated in claim 1, have renin-inhibiting properties and can be used as medicines.
    Type: Grant
    Filed: September 14, 2006
    Date of Patent: November 15, 2011
    Assignee: Novartis AG
    Inventors: Peter Herold, Robert Mah, Vincenzo Tschinke, Stefan Stutz, Aleksandar Stojanovic, Stjepan Jelakovic, Christiane Marti
  • Patent number: 8053413
    Abstract: The present invention relates to a method for preventing or ameliorating a sleep-related breathing disorder. The method involves the use of one or a combination of cholecystokinin (CCK) receptor antagonists.
    Type: Grant
    Filed: June 6, 2006
    Date of Patent: November 8, 2011
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: David W. Carley, Miodrag Radulovacki
  • Publication number: 20110262356
    Abstract: Luminescent and/or electroactive nanoparticles suitable for MRI (Magnetic Resonance Imaging) and/or PET (Positron Emission Tomography) are prepared by mixing luminescent or electroactive compounds and ethyl oxide/propyl oxide block-copolymers in an organic solvent, which is thereafter evaporated in order to obtain a residue; and by hydrolyzing-condensating tetraalkoxysilanes in an aqueous solution in the presence of the residue; the obtained nanoparticles show no or a negligible release of the luminescent or electroactive compounds and are useful for bio-analytic and bio-medic applications.
    Type: Application
    Filed: July 31, 2009
    Publication date: October 27, 2011
    Applicants: CYANAGEN S.R.L., ALMA MASTER STUDIORUM-UNIVERSITA' DI BOLOGNA
    Inventors: Sara Bonacchi, Ricarrdo Juris, Marco Montalti, Luca Prodi, Enrico Rampazzo, Nelsi Zaccheroni, Leopoldo Della Ciana, Serena Fabbroni, Stafano Grilli, Ettore Marzocchi
  • Publication number: 20110263556
    Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.
    Type: Application
    Filed: October 20, 2010
    Publication date: October 27, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Henning PRIEPKE, Henri DOODS, Raimund KUELZER, Roland PFAU, Dirk STENKAMP, Robert ROENN, Benjamin PELCMAN
  • Publication number: 20110263580
    Abstract: This invention relates to a method for treating or preventing diseases associated with the deposition of ?-amyloid peptide in the brain, such as Alzheimer's disease, said method involving administration of a gamma-secretase inhibitor in an intermittent dosing regime to a patient in need thereof.
    Type: Application
    Filed: December 4, 2009
    Publication date: October 27, 2011
    Inventor: Thomas Miller
  • Publication number: 20110263699
    Abstract: Metabolites of [2-(3-methoxyphenyl)-cyclohexylmethyl]dimethylamine as free bases and/or in the form of physiologically acceptable salts, corresponding medicaments, the use of [2-(3-methoxyphenyl)-cyclohexylmethyl]-dimethylamine and the metabolites thereof for producing a medicament used for treating depression, and related methods of treating depression, pain and urinary incontinence.
    Type: Application
    Filed: July 1, 2011
    Publication date: October 27, 2011
    Applicant: GRUENENTHAL GmbH
    Inventors: Elmar Friderichs, Wolfgang Strassburger, Ulrich Jahnel, Derek Saunders, Hagen-Heinrich Hennies, Werner Englberger, Helmut Buschmann, Joerg Holenz, Oswald Zimmer
  • Publication number: 20110257226
    Abstract: There is provided a halogen-containing organosulfur compound having a controlling effect on arthropod pests represented by the formula (I): wherein m represents 0, 1 or 2; n represents 0, 1 or 2; A represents an optionally substituted 3- to 8-membered saturated heterocyclic group; Q represents a fluorine atom or a C1-C5 haloalkyl group having at least one fluorine atom; R1, R1a and R3 independently represent an optionally halogenated C1-C4 chain hydrocarbon group, etc.; R2, R2a and R4 independently represent an optionally halogenated C1-C4 chain hydrocarbon group, etc.
    Type: Application
    Filed: December 24, 2009
    Publication date: October 20, 2011
    Inventor: Hiromasa Mitsudera
  • Publication number: 20110256188
    Abstract: There is provided a dry powder pharmaceutical composition for inhalation useful for preventing and/or treating influenza virus infections contains as a medicinal component a compound represented by formula (I): and optionally a compound represented by formula (II): , a pharmacologically acceptable salt thereof, or a hydrate thereof.
    Type: Application
    Filed: December 24, 2009
    Publication date: October 20, 2011
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Makoto Miyajima, Shigeru Noda, Kazuhiro Inoue, Michiko Kumon, Katsuyasu Ishida, Hitoshi Ishizuka
  • Publication number: 20110245335
    Abstract: The present invention relates in general to a compound which is characterized by a formula selected from the following formulas A, B, C, D, E or F; or a pharmaceutically acceptable salt thereof. The present invention further relates to pharmaceutical composition comprising the inhibitor(s) of the invention and to their use in the treatment of (for treating) a disease which is associated with an excess transport of hyaluronan across a lipid bilayer. The present invention furthermore relates to the use of at least one inhibitor of the invention for the preparation of a pharmaceutical composition for the treatment of (for treating) a disease which is associated with an excess transport of hyaluronan across a lipid bilayer. The present invention also relates to a method for manufacturing a pharmaceutical composition comprising the steps of formulating the inhibitor defined herein in a pharmaceutically acceptable form.
    Type: Application
    Filed: December 14, 2009
    Publication date: October 6, 2011
    Inventor: Peter Prehm
  • Publication number: 20110243914
    Abstract: The invention relates to new compounds for cancer therapy or diagnosis and more specifically to the use of a non-toxic B subunit of Shiga toxin mutant as a vector for diagnostic products or drugs in over-expressing Gb3 receptor cells, such compounds having the following formula: STxB-Z(n)-Cys-Y(m)-T wherein STxB is the Shiga Toxin B subunit or a functional equivalent thereof, Z(n) whrein n is 0 or 1 and when n is 1, Z is an amino-acid residue devoidof sulfydryl group, or is a polypeptide, Cys is the amino-acid residue for Cysteine, T is a molecule linked by a covalent bound to the S part of Cys, selected in a group comprising: agents for in vivo diagnosis, cytotoxic agents, prodrugs, or enzymes for the conversion of a prodrug to a drug, Y(m) wherein m is 0 or 1 and when m is 1, Y is a linker between T and Cys, said linker being either cleavable or not cleavable for the release of T after the internalization of the hybrid compound into said cells.
    Type: Application
    Filed: June 13, 2011
    Publication date: October 6, 2011
    Inventors: Ludger JOHANNES, David Grierson, Sylvie Robine, Jean-Claude Florent, Philipe Maillard, Jacky Roger
  • Publication number: 20110230346
    Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, and CKE have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides and/or fungicides. Moreover, the invention relates to selectively herbicidal compositions comprising, firstly, the biphenyl-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising in particular biphenyl-substituted cyclic ketoenols through the addition of ammonium or phosphium salts and optionally penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as insecticides and/or nematicides and/or acaricides and/or fungicides and/or for preventing unwanted plant growth.
    Type: Application
    Filed: February 10, 2011
    Publication date: September 22, 2011
    Applicant: Bayer CropScience AG
    Inventors: Reiner FISCHER, Stefan Lehr, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Chieko Ueno, Arnd Voerste, Elmar Gatzweiler, Ines Heinemann, Ulrich Görgens
  • Publication number: 20110229437
    Abstract: The present invention provides a method of treating asthma by administering a therapeutically effective amount of an antiviral agent to a patient. The antiviral agent may be a neuraminidase inhibitor, a viral fusion inhibitor, a protease inhibitor, a DNA polymerase inhibitor, a signal transduction inhibitor, a nucleoside reverse transcriptase inhibitor (NRTI), a non-nucleoside reverse transcriptase inhibitor (NNRTI) or an interferon. The antiviral agent may be administered to the patient by inhalation, nasally, intravenously, orally, subcutaneously, intramuscularly or transdermally. For example, the antiviral agent may be formulated for delivery as aerosols to the patient.
    Type: Application
    Filed: September 17, 2010
    Publication date: September 22, 2011
    Applicant: MUTUAL PHARMACEUTICAL COMPANY, INC.
    Inventor: Richard H. Roberts
  • Publication number: 20110230452
    Abstract: The present invention relates generally to pharmaceutical agents, and in particular, to metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of dual acting MMP-2 and MMP-9 inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP-2 and MMP-9 inhibitors for the treatment of pain and other diseases. Additionally, the present invention relates to methods for treating pain, addiction and/or withdrawal symptoms in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.
    Type: Application
    Filed: September 23, 2010
    Publication date: September 22, 2011
    Inventor: Irving Sucholeiki
  • Publication number: 20110212056
    Abstract: Provided herein are methods for treatment of a liver disease by administering a combination of a matrix metalloproteinase inhibitor and a caspase inhibitor. Also provided are methods for reducing liver damage associated with a liver disease by administering the MMP and caspase inhibitors described herein. Further provided are methods for lowering an elevated level of liver enzymes.
    Type: Application
    Filed: May 9, 2011
    Publication date: September 1, 2011
    Inventor: Alfred P. Spada
  • Publication number: 20110207604
    Abstract: A species of Burkholderia sp with no known pathogenicity to vertebrates but with pesticidal activity (e.g., plants, insects, fungi, weeds and nematodes) is provided. Also provided are natural products derived from a culture of said species and methods of controlling pests using said natural products.
    Type: Application
    Filed: February 24, 2011
    Publication date: August 25, 2011
    Applicant: MARRONE BIO INNOVATIONS
    Inventors: Ratnakar Asolkar, Marja Koivunen, Pamela Marrone, Ana-Lucia Cordova-Kreylos, Huazhang Huang
  • Patent number: 8003689
    Abstract: This invention provides metabolites of SARM compounds including inter alia glucuronidated metabolites and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, muscle wasting disease and/or disorder, a bone related disease and/or disorder, metabolic syndrome, diabetes and associated diseases, and others.
    Type: Grant
    Filed: June 19, 2009
    Date of Patent: August 23, 2011
    Assignee: GTx, Inc.
    Inventor: Karen A. Veverka
  • Publication number: 20110196014
    Abstract: Provided are methionine analogs which may be useful for inhibiting protein synthesis, inhibiting microbial growth and/or treating infectious diseases. In some instances, the analogs exhibit bactericidal, antibacterial, anti-infective, antimicrobial, sporicidal, disinfectant, antifungal and/or antiviral properties. Also provided are methods of treatment and methods of preparation, as well as kits and unit dosages.
    Type: Application
    Filed: July 31, 2009
    Publication date: August 11, 2011
    Inventors: Mansour Bassiri, Afsaneh Rahimi-Larijani
  • Publication number: 20110190349
    Abstract: The present invention relates to a compound of formula I wherein R1/R2 are independently from each other hydrogen, (CR2)o-cycloalkyl, optionally substituted by lower alkyl or hydroxy, or are lower alkyl or heterocycloalkyl, and o is 0 or 1; and R may be the same or different and is hydrogen or lower alkyl; or R1 and R2 may form together with the N atom to which they are attached a heterocycloalkyl group, selected from the group consisting of pyrrolidinyl, piperidinyl, 3-aza-bicyclo[3.1.0]hex-3-yl or 2-aza-bicyclo[3.1.
    Type: Application
    Filed: January 21, 2011
    Publication date: August 4, 2011
    Inventors: Sabine Kolczewski, Emmanuel Pinard