Patents Examined by Kahsay T. Habte
  • PPAR active compounds
    Patent number: 8053463
    Abstract: Compounds are described that are active on at least one of PPAR?, PPAR?, and PPAR?, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPAR?, PPAR?, and PPAR?, wherein the compounds have the formula: wherein: X2 and X3 are independently CH or N; and one of X1 and X4 is N or CR4 and the other of X1 and X4 is N or CH.
    Type: Grant
    Filed: March 5, 2008
    Date of Patent: November 8, 2011
    Assignee: Plexxikon Inc.
    Inventors: Jack Lin, Byunghun Lee, Shenghua Shi, Chao Zhang, Dean R. Artis, Prabha N. Ibrahim, Weiru Wang, Rebecca Zuckerman
  • Medicaments for the treatment of chronic obstructive pulmonary disease
    Patent number: 8044046
    Abstract: A pharmaceutical composition comprising a compound of formula 1 wherein: n is 1 or 2; R1 is hydrogen, C1-C4-alkyl, halogen, OH, or —O—C1-C4-alkyl; R2 is hydrogen, C1-C4-alkyl, halogen, OH, or —O—C1-C4-alkyl; R3 is hydrogen, C1-C4-alkyl, OH, halogen, —O—C1-C4-alkyl, —O—C1-C4-alkylene-COOH, or —O—C1-C4-alkylene-CO—O—C1-C4-alkyl, or an acid addition salt thereof with a pharmacologically acceptable acid, or a solvate or hydrate thereof; and a pharmaceutically acceptable excipient or carrier, and methods for using the pharmaceutical formulation in the treatment of chronic obstructive pulmonary disease (COPD).
    Type: Grant
    Filed: May 18, 2005
    Date of Patent: October 25, 2011
    Assignee: Boehringer Ingelheim Pharma GmbH & Co KG
    Inventors: Ingo Konetzki, Kurt Schromm, Hermann Schollenberger, Sabine Pestel, Andreas Schnapp, Thierry Bouyssou, Frank Buettner, Claudia Heine, Philipp Lustenberger, Christoph Hoenke, Klaus Rudolf
  • 5-substituted benzoxazines
    Patent number: 8044047
    Abstract: The present invention is concerned with 5-substituted benzoxazine derivatives of formula (I) wherein X, R1 and R2 are as described herein, as well as their manufacture, pharmaceutical compositions containing them. Compounds of the present invention are 5-HT5A receptor antagonists, and are useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders.
    Type: Grant
    Filed: August 28, 2009
    Date of Patent: October 25, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Sabine Kolczewski, Olivier Roche, Lucinda Steward, Juergen Wichmann, Thomas Woltering
  • 5-hydroxymethyl-oxazolidin-2-one antibacterials
    Patent number: 8039466
    Abstract: The invention relates to novel chimeric antibiotics of formula I wherein R1 represents OH, OPO3H2 or OCOR5; R2 represents H, OH or OPO3H2; R3 represents H or halogen; R4 is H, (C1-C3)alkyl, or cycloalkyl; R5 represents piperidin-4-yl or R5 is the residue of a naturally occurring amino acid, of the enantiomer of a naturally occurring amino acid or of dimethylaminoglycine; n is 0 or 1; and to salts (in particular pharmaceutically acceptable salts) of compounds of formula I. These chimeric compounds are useful in the manufacture of medicaments for the treatment of infections (e.g. bacterial infections).
    Type: Grant
    Filed: November 23, 2007
    Date of Patent: October 18, 2011
    Assignee: Actelion Pharmaceutical Ltd.
    Inventors: Christian Hubschwerlen, Philippe Panchaud, Jean-Luc Specklin
  • Anti-infective agents against intracellular pathogens
    Patent number: 8039502
    Abstract: A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of Formula I: wherein X wherein X is —CF3, Ar is selected from and R is selected from where R? is L-Lys, D-Lys, ?-Ala, L-Lue, L-Ile, Phe, SO2CH2CH2NH2, SO2NH2, Asn, Glu or Gyl, and R? is methyl, ethyl, allyl, CH2CH2OH, CH2CN, CH2CH2CN, CH2CONH2,
    Type: Grant
    Filed: July 24, 2008
    Date of Patent: October 18, 2011
    Assignee: The Ohio State University Research Foundation
    Inventors: Ching-Shih Chen, Hao-Chieh Chiu, Dasheng Wang, John S. Gunn, Larry S. Schlesinger
  • Enantiomerically pure beta agonists, process for the manufacture thereof and use thereof as medicaments
    Patent number: 8034809
    Abstract: Enantiomerically pure compounds of general formula 1 wherein the groups R1, R2, R3, R4, and X? may have the meanings given in the claims and in the specification, processes for preparing them and the use thereof as pharmaceutical compositions, particularly as pharmaceutical compositions for the treatment of respiratory complaints.
    Type: Grant
    Filed: December 15, 2008
    Date of Patent: October 11, 2011
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Philipp Lustenberger, Ingo Konetzki, Peter Sieger
  • Phthalazine derivatives with angiogenesis inhibiting activity
    Patent number: 8034814
    Abstract: The invention relates to new phthalazine derivatives of formula I, and to processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof alone or in combination with one or more other pharmaceutically active compounds for the treatment especially of a disease that responds to the inhibition of especially the vascular endothelial growth factor receptor kinase, preferably the treatment of a proliferative disease, or the treatment of inflammatory rheumatic or rheumatoid arthritis and/or pain; and the use of such a compound alone or in combination with one or more other pharmaceutically active compounds for the manufacture of a pharmaceutical preparation for the treatment of said diseases in an animal.
    Type: Grant
    Filed: November 24, 2010
    Date of Patent: October 11, 2011
    Assignee: Novartis AG
    Inventors: Guido Bold, Paul William Manley
  • Bicyclic sulfonamide derivatives which are L-CPT 1 inhibitors
    Patent number: 8030308
    Abstract: The invention is concerned with novel heterobicyclic derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, V, W, X and Y 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: Grant
    Filed: November 8, 2010
    Date of Patent: October 4, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, Konrad Bleicher, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei, Ulrike Obst Sander
  • Potassium channel inhibitors
    Patent number: 8030332
    Abstract: The present invention relates to dipyridin-3-ylmethoxy compounds and derivatives thereof having the structure I useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
    Type: Grant
    Filed: January 29, 2007
    Date of Patent: October 4, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: B. Wesley Trotter, Richard C. A. Isaacs, Zhicai Wu, Jacob M. Hoffman, Mark T. Bilodeau, Ahren Iver Green
  • Cyclopropyl amines as modulators of the histamine Hreceptor
    Patent number: 8026242
    Abstract: Certain cyclopropyl amines are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases.
    Type: Grant
    Filed: February 16, 2011
    Date of Patent: September 27, 2011
    Inventors: Nicholas I. Carruthers, Michael A. Letavic
  • Pyridyl benzoxazine derivatives, pharmaceutical composition comprising the same, and use thereof
    Patent number: 8026235
    Abstract: Discloses is a benzoxazine benzimidazole derivative, represented by Chemical Formula 1, functioning as an antagonist to the vanilloid receptor-1, a pharmaceutical composition comprising the same, and the use thereof. The benzoxazine benzimidazole derivative can be useful for preventing or treating a disease associated with antagonistic activity of vanilloid receptor-1, without hyperthermia: wherein, R1, R2, R3, R4 and R5 are as defined in the specification.
    Type: Grant
    Filed: October 21, 2010
    Date of Patent: September 27, 2011
    Assignee: Daewoong Pharmaceutical Co., Ltd.
    Inventors: Ji Duck Kim, Hong-Chul Yoon, In Woo Kim, Min Jae Cho, In Young Lee, Sang Ho Lee, Eun Kyung Park, Kwon Jo Lim, Sang Hyun Nam
  • Bicyclic amides as kinase inhibitors
    Patent number: 8026247
    Abstract: The invention relates to compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases.
    Type: Grant
    Filed: September 14, 2005
    Date of Patent: September 27, 2011
    Assignee: Novartis AG
    Inventors: Guido Bold, Hans-Georg Capraro, Giorgio Caravatti, Andreas Floersheimer, Pascal Furet, Paul W. Manley, Andrea Vaupel
  • Substituted piperidines as renin inhibitors
    Patent number: 8022069
    Abstract: The present invention relates to compounds of the general formula (I) and the salts thereof, preferably the pharmaceutically acceptable salts thereof; in which R has the meaning explained in the description, a process for their preparation and the use of these compounds as medicines, especially as renin inhibitors.
    Type: Grant
    Filed: February 6, 2009
    Date of Patent: September 20, 2011
    Assignee: Novartis AG
    Inventors: Dirk Behnke, Peter Herold, Stjepan Jelakovic, Robert Mah, Vincenzo Tschinke
  • Process of making 3-phenylimino-3H-phenothiazine
    Patent number: 8022204
    Abstract: A method of forming a 3-phenylimino-3H-phenothiazine or a 3-phenylimino-3H-phenoxazine mediator includes providing a first reactant including phenothiazine or phenoxazine, providing a first solvent, providing a second reactant and providing a second solvent. The first reactant, first solvent, second reactant and second solvent are combined to form a reactants solution. Sodium persulfate is added to the reactants solution to couple the first and second reactants resulting in a reaction solution including the 3-phenylimino-3H-phenothiazine or the 3-phenylimino-3H-phenoxazine mediator.
    Type: Grant
    Filed: December 9, 2008
    Date of Patent: September 20, 2011
    Assignee: Bayer Healthcare LLC
    Inventors: Karen L. Marfurt, Henry C. Arndt
  • Substituted piperidines as renin inhibitors
    Patent number: 8022068
    Abstract: The present invention relates to compounds of the general formula (I) and the salts thereof, preferably the pharmaceutically acceptable salts thereof; in which R has the meaning explained in the description, a process for their preparation and the use of these compounds as medicines, especially as renin inhibitors.
    Type: Grant
    Filed: February 6, 2009
    Date of Patent: September 20, 2011
    Assignee: Novartis AG
    Inventors: Dirk Behnke, Peter Herold, Stjepan Jelakovic, Robert Mah, Vincenzo Tschinke
  • 2-(2-hydroxyphenyl) benzothiadiazines useful for treating obesity and diabetes
    Patent number: 8022066
    Abstract: The present invention relates to novel compounds that act as chemical uncouplers. Compounds of the invention are useful, inter alia, in the treatment, including prevention, of obesity, diabetes and a number of diseases or conditions associated therewith.
    Type: Grant
    Filed: November 15, 2007
    Date of Patent: September 20, 2011
    Assignee: High Point Pharmaceuticals, LLC
    Inventors: Anders Klarskov Petersen, Preben Houlberg Olesen, Lise Brown Christiansen, Holger Claus Hansen, Flemming Elmelund Nielsen
  • N-(2-(2-(5-hydroxy-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-8-yl)ethylamino)ethyl)-3-(phenethoxy)propanamide derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy
    Patent number: 8017602
    Abstract: The present invention provides a compound of formula (I) wherein W, R1, R2 and R3 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: June 18, 2009
    Date of Patent: September 13, 2011
    Assignee: AstraZeneca AB
    Inventors: Roger Victor Bonnert, Stephen Connolly, Anthony Ronald Cook, Richard Evans, Piotr Raubo
  • Pyrimido [4,5-B]-oxazines for use as DGAT inhibitors
    Patent number: 8017603
    Abstract: Compounds of formula (I) or salts thereof, wherein A, and R1 to R5 are as defined in the specification, are DGAT-1 inhibitors and are thereby useful in the treatment of, for example, obesity. Processes to make compounds of formula (I) are also described.
    Type: Grant
    Filed: June 8, 2010
    Date of Patent: September 13, 2011
    Assignee: AstraZeneca AB
    Inventors: Alan Martin Birch, Paul David Kemmitt
  • Tricyclic antibiotics
    Patent number: 8012961
    Abstract: The invention relates to antibacterial compounds of formula (I) wherein U represents CH or N; W represents CH or N; R1 represents alkoxy, halogen or CN; ring A represents a pyrrolidin-1,3-diyl-, a piperidin-1,3-diyl or a morpholin-2,4-diyl group and B represents CH2; or ring A is selected from the groups drawn below: wherein R2 represents H, F or hydroxymethyl, and B is absent; G represents a group selected from the group consisting of ?—CH?CH-E, wherein Y1, Y2, Y3 and Z independently represent CH or N; Q represents O or S; and E represents phenyl which is mono- or di-substituted wherein the substituents are each independently halogen; and to pharmaceutically acceptable salts of such compounds.
    Type: Grant
    Filed: April 14, 2009
    Date of Patent: September 6, 2011
    Assignee: Actelion Pharmaceutical Ltd.
    Inventors: Christian Hubschwerlen, Georg Rueedi, John-Philippe Surivet, Cornelia Zumbrunn-Acklin
  • 3,4-dihydro-2H-benzo[1,4]oxazine and thiazine derivatives as CETP inhibitors
    Patent number: 8012963
    Abstract: The invention is directed to compounds of Formula (I) described herein useful as CETP inhibitors, compositions containing them, and methods of using them.
    Type: Grant
    Filed: May 18, 2010
    Date of Patent: September 6, 2011
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Gee-Hong Kuo, Thomas Rano, Aihua Wang, Catherine Prouty, Keith T. Demarest, Patricia Pelton