Nitrogen Patents (Class 562/430)
  • Publication number: 20150148544
    Abstract: A compound of the general formula X—[NR—CO—Ar—CO—(CH?CH)n—(CH2)2-L]m (I) in which X represents a polymer; R represents a hydrogen atom or an alkyl, aryl or alkyl-aryl group; Ar represents an unsubstituted or substituted heteroaryl or aryl group; n represents 0 or an integer of from 1 to 4; L represents a leaving group; and m represents an integer of from 1 to 8. The compounds find use in the conjugation of biological molecules.
    Type: Application
    Filed: February 4, 2015
    Publication date: May 28, 2015
    Inventor: Antony Godwin
  • Publication number: 20150141513
    Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of neurological degenerative disorders and neurological diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of narcolepsy, shift work sleep disorder, and as an adjunct treatment for obstructive sleep apnea/hypopnea, hypersomnias, like idiopathic hypersomnia, Psychiatric/neurodegenerative disorders, ADHD, Psychiatric/neurodegenerative disorders, Depersonalization disorder, Cognitive enhancement, Fatigue, Post-chemotherapy cognitive impairment and weight loss.
    Type: Application
    Filed: April 19, 2013
    Publication date: May 21, 2015
    Inventor: Mahesh Kandula
  • Publication number: 20150094276
    Abstract: This invention relates to novel substituted styryl benzylsulfones that are multikinase inhibitors and pharmaceutically acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by an agent that inhibits kinases, such as phosphatidylinositol 3-kinase (PI3-K) and polo-like kinase (PLK-1).
    Type: Application
    Filed: April 19, 2013
    Publication date: April 2, 2015
    Inventor: Roger D. Tung
  • Patent number: 8993780
    Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Grant
    Filed: December 10, 2013
    Date of Patent: March 31, 2015
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20150038708
    Abstract: In one aspect, the invention relates to substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: August 5, 2014
    Publication date: February 5, 2015
    Inventors: James Turkson, Patrick Gunning
  • Patent number: 8933267
    Abstract: The present invention relates to a compound according to formula I in particular as anti-ulcer agent and/or anti-Helicobacter pylori agent, wherein R1 is selected from linear or branched C1-C6 alkyl, H, thioether and benzyl, and R2 is selected from linear or branched C1-C10 alkanediyl and pharmaceutical compositions thereof.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: January 13, 2015
    Assignee: King Saud University
    Inventors: Amani S. Awaad, Reham Moustafa El-Meligy, Ahmed M. Alafeefy
  • Patent number: 8895746
    Abstract: The present invention provides compounds S3I-201.1066 (Formula 1) and S3I-201.2096 (Formula 2) as selective Stat3 binding agents that block Stat3 association with cognate receptor pTyr motifs, Stat3 phosphorylation and nuclear translocation, Stat3 transcriptional function, and consequently induced Stat3-specific antitumor cell effects in vitro and antitumor response in vivo.
    Type: Grant
    Filed: November 10, 2013
    Date of Patent: November 25, 2014
    Assignees: University of Central Florida Research Foundation, Inc., The Governing Council of the University of Toronto
    Inventors: James Turkson, Patrick Gunning
  • Publication number: 20140329778
    Abstract: The present invention relates to a compound according to formula I in particular as anti-ulcer agent and/or anti-Helicobacter pylori agent, wherein R1 is selected from linear or branched C1-C6 alkyl, H, thioether and benzyl, and R2 is selected from linear or branched C1-C10 alkanediyl and pharmaceutical compositions thereof
    Type: Application
    Filed: March 13, 2014
    Publication date: November 6, 2014
    Applicant: King Saud University
    Inventors: Amani S. AWAAD, Reham Moustafa EL-MELIGY, Ahmed M. ALAFEEFY
  • Patent number: 8822467
    Abstract: The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: September 2, 2014
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Brian F. McGuinness, Koc-Kan Ho, Suresh Babu, Guizhen Dong, Jingqi Duo, Thuy X. H. Le, Kurt W. Saionz
  • Publication number: 20140228325
    Abstract: The present invention relates to alkene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: February 6, 2014
    Publication date: August 14, 2014
    Applicant: Allergan, Inc.
    Inventors: Wenkui K. Fang, Ken Chow, Evelyn G. Corpuz
  • Publication number: 20140194416
    Abstract: The invention relates to N-hydroxylsulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxylsulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxylsulfonamide derivatives.
    Type: Application
    Filed: March 11, 2014
    Publication date: July 10, 2014
    Applicants: Cardioxyl Pharmaceuticals, Inc., The Johns Hopkins University
    Inventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
  • Publication number: 20140128469
    Abstract: The present invention provides a compound of Formula I: as defined herein, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: May 8, 2012
    Publication date: May 8, 2014
    Applicant: CONCERT PHARMACEUTICALS INC.
    Inventor: Roger Tung
  • Publication number: 20140094614
    Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Application
    Filed: December 10, 2013
    Publication date: April 3, 2014
    Applicant: Allergan, Inc.
    Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20140094455
    Abstract: Compounds, including 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels and methods of using them to treat disorders or diseases mediated by aquaporins.
    Type: Application
    Filed: August 19, 2013
    Publication date: April 3, 2014
    Applicant: ARIZONA BOARD OF REAGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA
    Inventors: Gary A. Flynn, Andrea J. Yool, Elton Rodrigues Migliati, Leslie S. Ritter
  • Publication number: 20140094466
    Abstract: In alternative embodiments, the invention provides compositions that inhibit the polypeptide SSH-2, or SlingSHot-2, a phosphatase enzyme that regulates actin filaments, and methods for making and using them, including methods comprising administering compositions of the invention to regulate or modify actin filament polymerization by inhibiting SSH-2, where in one embodiment compositions of the invention slow or inhibit F-actin depolymerization and severing. In alternative embodiments, compositions and methods of the invention are used to slow or inhibit cell motility and/or internal remodeling. In alternative embodiments, compositions and methods of the invention are used to slow or inhibit, or reverse, or ameliorate the progression of a cancer or a metastasis or other uncontrolled or unregulated cell growth, and/or Alzheimer's disease.
    Type: Application
    Filed: March 15, 2012
    Publication date: April 3, 2014
    Inventors: Jason H. Haga, Shu Chien, Matt Mui, Marshall J. Levesque, Phillip D. Pham
  • Patent number: 8686154
    Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.
    Type: Grant
    Filed: June 10, 2009
    Date of Patent: April 1, 2014
    Assignee: Emisphere Technologies, Inc.
    Inventors: Donald J. Sarubbi, Eugene N. Barantsevitch
  • Patent number: 8658803
    Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Grant
    Filed: October 23, 2012
    Date of Patent: February 25, 2014
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20140024717
    Abstract: The present invention relates to a process for the preparation of the mono sodium salt of the derivative 3,5-diiodo-O-[3-iodo-4-(sulphooxy)phenyl]-L-tyrosine (T3S) by starting from the corresponding phenolic compound, in the presence of chloro-sulfonic acid and dimethylacetamide as a solvent. The so obtained T3S compound may conveniently be isolated in a pure form as a solid in good yields. The present invention further relates to the process for T3S preparation, wherein the starting reagent is T2 and further comprising the formulation of such compound in tablets. Furthermore, the invention discloses non-radioactive immunoassays based on T3S derivatives.
    Type: Application
    Filed: April 5, 2012
    Publication date: January 23, 2014
    Applicant: BRACCO IMAGING S.p.A.
    Inventors: Pier Lucio Anelli, Maria Argese, Luciano Lattuada, Federico Maisano, Sonia Gazzetto, Laura Galimberti, Valeria Boi, Giovanni Rivolta, Livio Cavalieri, Fulvia Vella
  • Publication number: 20140011129
    Abstract: A polymerizable monomer is provided which is represented by the following formula (1): wherein R1 represents a hydrogen atom or an alkyl group; A represents —CO— or —SO2—; and the moiety represented by the formula (1) is, at the part shown by an asterisk *, linked to a moiety represented by the following formula (2), at any position of a, b, c or d thereof; wherein the sites among a, b, c and d at which the moiety represented by the formula (2) is not linked to the moiety represented by the formula (1) each has a hydrogen atom or a substituent selected from the group consisting of an alkyl group, an alkoxy group and a sulfonic acid group, or any of which may connect at mutually adjoining positions to form a ring.
    Type: Application
    Filed: March 27, 2012
    Publication date: January 9, 2014
    Applicant: CANON KABUSHIKI KAISHA
    Inventors: Yasuaki Murai, Kei Inoue, Ryuji Murayama, Kazuyuki Sato, Masashi Hirose
  • Publication number: 20140011130
    Abstract: To provide a polymeric compound having superior charge-providing properties, the polymeric compound contains at least one unit represented by the following general formula (5). In the general formula (5), R1 represents a hydrogen atom or an alkyl group; R2 to R4 each represent a hydrogen atom, an alkyl group, an alkoxy group, a hydroxyl group or a halogen atom, or R3 and R4 may combine each other to form a ring; and A represents a divalent linking group.
    Type: Application
    Filed: March 27, 2012
    Publication date: January 9, 2014
    Applicant: CANON KABUSHIKI KAISHA
    Inventors: Kei Inoue, Yasuaki Murai, Ryuji Murayama, Kazuyuki Sato, Soichiro Kawakami, Masashi Hirose
  • Publication number: 20130331450
    Abstract: Disclosed are compositions and methods for treating bacterial infections.
    Type: Application
    Filed: March 15, 2013
    Publication date: December 12, 2013
    Applicant: Purdue Research Foundation
    Inventors: Cynthia Stauffacher, Mark Alfred Lipton, Mohamed Naguieb Saleem, Tim Jonathan Schmidt, Calvin Nicklaus Steussy, JR., Victor W. Rodwell
  • Patent number: 8586749
    Abstract: The present invention provides compounds S3I-201.1066 (Formula 1) and S3I-201.2096 (Formula 2) as selective Stat3 binding agents that block Stat3 association with cognate receptor pTyr motifs, Stat3 phosphorylation and nuclear translocation, Stat3 transcriptional function, and consequently induced Stat3-specific antitumor cell effects in vitro and antitumor response in vivo.
    Type: Grant
    Filed: April 5, 2010
    Date of Patent: November 19, 2013
    Assignees: University of Central Florida Research Foundation, Inc., Governing Council of the University of Toronto
    Inventors: James Turkson, Patrick Gunning
  • Patent number: 8524194
    Abstract: The invention is directed to radiolabelled MMP selective compounds, a processes for the preparation thereof, and uses thereof. The derivatives of the invention have formula (I) wherein Y represents O, CH2, (CH2)2, S, NH, or C(?O)NH; X represents 1-5 substituents, wherein said substituents can be the same or different and wherein at least one of said substituents comprises a radioisotope suitable for PET and/or SPECT and/or a ?-emitter; Z is S; Q is chosen from the group consisting of 3-pyridyl and carboxyl; and R is chosen from the group consisting of C(?O)—NH—OH, (II), (III, (IV). The MMP selective compounds of the invention are selective for MMPs and can be used for the identification and treatment of unstable atherosclerotic plaques.
    Type: Grant
    Filed: May 14, 2009
    Date of Patent: September 3, 2013
    Assignee: Academisch Medisch Centrum Bij de Universiteit van Amsterdam
    Inventors: Bertha Louise Frederike Van Eck-Smit, Victorine Augustine Pinas, Albert Dirk Windhorst
  • Publication number: 20130225621
    Abstract: In one aspect, the invention relates to substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: August 2, 2011
    Publication date: August 29, 2013
    Applicants: University of Toronto Mississauga, University of Central Florida Research Foundation, Inc.
    Inventors: James Turkson, Patrick Gunning
  • Publication number: 20130217652
    Abstract: The present invention relates to novel thiobenzyl and sulfinylbenzyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: February 20, 2013
    Publication date: August 22, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Publication number: 20130203727
    Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I).
    Type: Application
    Filed: July 1, 2011
    Publication date: August 8, 2013
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Kerim Babaoglu, Elizabeth Bacon, Kyla Bjornson, Hongyan Guo, Randall L. Halcomb, Paul Hrvatin, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Paul Roethle, James Taylor, James D. Trenkle, Randall W. Vivian, Lianhong Xu
  • Patent number: 8501242
    Abstract: The present invention relates to compounds as novel thymidylate synthase inhibitors, novel strategies to treat or prevent neoplasia in a subject, methods and compositions thereof.
    Type: Grant
    Filed: May 29, 2010
    Date of Patent: August 6, 2013
    Assignee: University of Florida Research Foundation
    Inventors: David A. Ostrov, Carmen J. Allegra
  • Publication number: 20130190338
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: March 11, 2013
    Publication date: July 25, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Publication number: 20130190370
    Abstract: The present invention relates to TP receptor antagonists, which have the ability to bind to TP receptor and optionally cross the blood brain barrier. The invention also provides compositions and methods for treating a disorder wherein activation of TP receptor is detrimental.
    Type: Application
    Filed: July 27, 2011
    Publication date: July 25, 2013
    Applicant: The Trustees of the University of Pennsylvania
    Inventors: John Q. Trojanowski, Virginia M.Y. Lee, Kurt R. Brunden, Amos B. Smith, Donna M. Huryn, Carlo Ballatore, Anne-Marie Hogan, Francesco Piscitelli
  • Publication number: 20130183252
    Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.
    Type: Application
    Filed: February 10, 2012
    Publication date: July 18, 2013
    Applicant: Senomyx, Inc.
    Inventors: Xiaodong LI, Andrew Patron, Catherine Tachdjian, Hong Xu, Qing Li, Alexey Pronin, Guy Servant, Lan Zhang, Thomas Brady, Vincent Darmohusodo, Melissa Arellano, Victor Selchau, Brett Weylan Ching, Donald S. Karanewsky, Paul Brust, Jing Ling, Wen Zhao, Chad Priest
  • Patent number: 8445706
    Abstract: An unnatural amino acid including a phosphate mimicking group for mimicking a phosphate group in phosphoamino acids and a protein phosphatase modifying group for covalently binding protein phosphatases. A probe for detecting disease including a phosphate mimicking group for mimicking a phosphate group in phosphoamino acids and a protein phosphatase modifying group for covalently binding protein phosphatases. A method for detecting the presence of disease by administering the unnatural amino acid, binding the unnatural amino acid with a phosphatase, detecting a signal, and detecting the presence of disease. A method of identifying a known protein phosphatase, and a method of identifying an unknown protein phosphatase. A method of making the unnatural amino acid.
    Type: Grant
    Filed: September 1, 2009
    Date of Patent: May 21, 2013
    Assignee: Board of Trustees of Northern Illinois University
    Inventor: Kui Shen
  • Publication number: 20130109866
    Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Application
    Filed: October 23, 2012
    Publication date: May 2, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Publication number: 20130102609
    Abstract: The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin.
    Type: Application
    Filed: December 14, 2012
    Publication date: April 25, 2013
    Applicant: LIGAND PHARMACEUTICALS INC.
    Inventor: Ligand Pharmaceuticals Inc.
  • Publication number: 20130096127
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: November 29, 2012
    Publication date: April 18, 2013
    Applicant: NOVARTIS AG
    Inventor: NOVARTIS AG
  • Publication number: 20130096319
    Abstract: The present invention is related to a novel process for the preparation of amisulpride (I) which involves: methylation of 4-amino-salicylic-acid (VI) with dimethyl sulphate and base, optionally in presence of TBAB to obtain 4-amino-2-methoxy methyl benzoate (VII) and (ii) oxidation of 4-amino-2-methoxy-5-ethyl thio benzoic acid (IX) or 4-amino-2-methoxy-5-ethyl thio methyl benzoate (X) with oxidizing agent in the presence of sodium tungstate or ammonium molybdate to give 2-methoxy-4-amino-5-ethyl-sulfonyl benzoic acid (IV) or 2-methoxy-4-amino-5-ethyl-sulfonyl methyl benzoate (XI) respectively.
    Type: Application
    Filed: June 9, 2011
    Publication date: April 18, 2013
    Applicant: Lupin Limited
    Inventors: Dinesh Jayntibhai Paghdar, Mahesh Ramkumar Kolekar, Tushar Nandkumar Deshpande, Suryaprakash Pandurang Patil, Yuvraj Atmaram Chavan, Purna Chandra Ray, Girij Pal Singh
  • Publication number: 20130046103
    Abstract: The present invention provides several synthetic methods for preparing N-(2-butylbenzofuran-5-yl)-N-(methylsulfonyl)methanesulfonamide, a compound of formula (3), an intermediate in the preparation of Dronedarone. The present invention further provides a process for preparing Dronedarone, comprising the steps of converting 2-butyl-5-bis(methanesulfon)-amidobenzofuran of formula (3) to Dronedarone, wherein the 2-butyl-5-bis(methanesulfon)-amidobenzofuran of formula (3) is prepared by the processes of the present invention.
    Type: Application
    Filed: February 10, 2011
    Publication date: February 21, 2013
    Applicant: MAPI PHARMA LIMITED
    Inventors: Ehud Marom, Michael Mizhiritskii, Shai Rubnov
  • Publication number: 20120289554
    Abstract: This invention relates to novel 4-dimethylaminobutyric acid derivatives of the formula wherein A1, A2, R1, m and n are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit carnitine palmitoyl transferase (CPT) activity, in particular CPT2 activity, and can be used as medicaments in methods for the treatment of diseases modulated by CPT2 inhibitors.
    Type: Application
    Filed: July 24, 2012
    Publication date: November 15, 2012
    Inventors: Mirjana Andjelkovic, Simona M. Ceccarelli, Odile Chomienne, Gerald Lewis Kaplan, Patrizio Mattei, Jefferson Wright Tilley
  • Publication number: 20120282180
    Abstract: The present invention relates to the field of therapeutic and diagnostic agents and more specifically to compounds of formula (I) that are inhibitors of matrix-metalloproteinases (MMPs) and are useful in the treatment of diseases related thereto such as cardiovascular diseases, inflammatory diseases and malignant diseases. One embodiment of the invention is a compound of formula (I) labeled with a 18-fluorine atom having matrix metalloproteinase inhibitory activity suitable for diagnostic imaging. Also disclosed in the present invention is a pharmaceutical composition comprising the inhibitors of matrix-metalloproteinases (MMPs) of the invention or the corresponding labeled compounds useful as diagnostic imaging agents of the invention in a form suitable for mammalian administration.
    Type: Application
    Filed: June 8, 2011
    Publication date: November 8, 2012
    Inventors: Hartmuth C. Kolb, Guenter Haufe, Malte Behrends, Klaus Kopka, Stefan Wagner, Verena Hugenberg, Hans-Joerg Breyholz, Sven Hermann, Michael Schaefers
  • Publication number: 20120263714
    Abstract: The present invention relates to substituted halophenoxybenzamide derivative compounds of general formula (I) in which R1, R2, R3, R3a, R4, R5, R6, Ra, Rb, Rc, and X are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: October 12, 2010
    Publication date: October 18, 2012
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Marion Hitchcock, Ingo Hartung, Florian Pühler, Gerhard Siemeister, Roland Neuhaus
  • Publication number: 20120252997
    Abstract: Fluorinated arylene-containing compounds and fluorinated polymers formed from fluorinated arylene-containing compounds, and methods are described. Fluorinated polymers formed from fluorinated arylene-containing compound can be used to provide a low energy surface.
    Type: Application
    Filed: December 17, 2010
    Publication date: October 4, 2012
    Inventors: Yu Yang, George G.I. Moore, John C. Clark
  • Publication number: 20120252894
    Abstract: The invention relates to a compound which inhibits the importation of chloride into neurons or a compound which improve the outflow of chloride from neurons thereby promoting the inhibitory actions of GABA and alleviating pain and stress of the fetus during delivery and the newborn. The invention also relates to a pharmaceutical composition for use in a method for alleviating pain and stress of the fetus during delivery and the newborn comprising a compound according to the invention and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: March 30, 2012
    Publication date: October 4, 2012
    Inventors: Giniatullin Rashid, Khazipov Roustem, Ben-Ari Yehezkel, Mazzuca Michel, Tyzio Roman
  • Patent number: 8268885
    Abstract: The present invention relates to small molecules as entry inhibitors of the HIV virus, processes for their preparation as well as pharmaceutical compositions, their use as medicines, and diagnostic kits comprising them. The present invention also concerns combinations of the present entry inhibitors with other anti-retroviral agents. It further relates to their use in assays as reference compounds or as reagents. The compounds of the present invention are useful for preventing or treating infection by HIV and for treating AIDS.
    Type: Grant
    Filed: September 10, 2004
    Date of Patent: September 18, 2012
    Assignee: Janssen R&D Ireland
    Inventors: Koenraad Lodewijk August Van Acker, Piet Tom Bert Paul Wigerinck, Lieve Emma Jan Michiels, Abdellah Tahri
  • Publication number: 20120232104
    Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R2, R3, R4, A, X, Y1, Y2, Y3, Y4 and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
    Type: Application
    Filed: May 22, 2012
    Publication date: September 13, 2012
    Inventors: Konrad Bleicher, Simona Maria Ceccarelli, Odile Chomienne, Patrizio Mattei, Tanja Schulz-Gasch, Christoph Martin Stahl
  • Patent number: 8247602
    Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions that include the compounds described herein, and methods of using such antagonists of PGD2 receptors, alone or in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Grant
    Filed: September 27, 2011
    Date of Patent: August 21, 2012
    Assignee: Panmira Pharmaceuticals, LLC
    Inventors: John Howard Hutchinson, Thomas Jon Seiders, Jeannie M. Arruda
  • Publication number: 20120208988
    Abstract: Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR?R?, Q is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Y is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Z is H or C1-C4 alkyl, R? is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C6-C12 heteroaryl, —NR?R? or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.
    Type: Application
    Filed: November 11, 2011
    Publication date: August 16, 2012
    Applicant: MOLECULAR INSIGHTS PHARMACEUTICALS, INC.
    Inventors: John W. Babich, Craig N. Zimmerman, Kevin P. Maresca
  • Patent number: 8242118
    Abstract: The present invention relates to a sulfonamide derivative which is useful as an active ingredient of pharmaceutical preparations. The sulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of asthma, atopic dermatitis, allergic rhinitis and other inflammatory/immunological disorders.
    Type: Grant
    Filed: April 19, 2010
    Date of Patent: August 14, 2012
    Assignee: Axikin Pharmaceuticals Inc.
    Inventors: Yingfu Li, Akihiko Watanabe, Timothy B. Lowinger, Kevin Bacon, Norihiro Kawamura, Takuya Shintani, Tetsuo Kikuchi, Toshiya Moriwaki, Klaus Urbahns, Keiko Fukushima, Noriko Nunami, Takashi Yoshino, Toshiki Murata, Megumi Yamauchi, Hiroko Yoshino
  • Publication number: 20120202854
    Abstract: Compounds of formula (I): in which R1, R2, R7, R8, R9, R10 and A have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.
    Type: Application
    Filed: April 17, 2012
    Publication date: August 9, 2012
    Applicant: ARRAY BIOPHARMA INC.
    Inventors: George Doherty, Adam Cook
  • Publication number: 20120196933
    Abstract: The present invention concerns prodrugs of mexiletine (and mexiletine's active metabolite) pharmaceutical compositions containing such prodrugs. Methods for treating myotonic conditions, while reducing the inherent adverse GI side effects associated with mexiletine, increasing the bioavailability of mexiletine, and improving the pharmacokinetic reproducibility of mexiletine with the aforementioned prodrugs are also provided.
    Type: Application
    Filed: December 22, 2011
    Publication date: August 2, 2012
    Inventors: Richard Franklin, Bernard T. Golding, Robert G. Tyson
  • Publication number: 20120164097
    Abstract: Bad odors on textile materials are often caused by body odor. The invention relates to a textile material treatment method for inhibiting body odor on textile materials, by which means the treated textiles, after having been worn, even after sweat-inducing sports activities, have a significantly reduced bad odor or even no odor. The invention also relates to a perfume composition and to a textile material treatment agent, respectively comprising urea derivatives and/or phenacylthiazolium salts, that counteract the formation of body odor.
    Type: Application
    Filed: March 8, 2012
    Publication date: June 28, 2012
    Applicant: Henkel AG & Co. KGaA
    Inventors: Ursula Huchel, Markus Egert, Andreas Bauer, Andreas Gerigk, Frank Pessel
  • Publication number: 20120156212
    Abstract: The present invention relates to compounds as novel thymidylate synthase inhibitors, novel strategies to treat or prevent neoplasia in a subject, methods and compositions thereof.
    Type: Application
    Filed: May 29, 2010
    Publication date: June 21, 2012
    Inventors: David A. Ostrov, Carmen J. Allegra