Patents Examined by Kristin Bianchi
  • Processes for the preparation of rivaroxaban and intermediates thereof
    Patent number: 8101609
    Abstract: This invention provides a process for the preparation of S-Rivaroxaban and/or R-Rivaroxaban comprising reacting, in the presence of a first base, a compound of Formula 9: with a compound of Formula 8:
    Type: Grant
    Filed: April 26, 2010
    Date of Patent: January 24, 2012
    Assignee: Apotex Pharmachem Inc.
    Inventors: Prabhudas Bodhuri, Gamini Weeratunga
  • Nitrogenated trans-stilbene analogs, method for the obtention and medical applications thereof
    Patent number: 8097656
    Abstract: This invention is related to new nitrogenated trans-stilbene compounds, more specifically, imine, pyrrole and indole derivatives, with procedures for the preparation and use thereof as pharmaceutical compositions for the treatment and/or chemoprevention of those mammalian diseases such as cancer, fibrosclerosis and acute/chronic inflammation, graft-versus-host reaction, ischemic-reperfusion tissue injury in stroke and heart attack, neurodegeneration, and during organ transplantation, whose pathogenic and pathophysiological mechanisms depend on or are significantly contributed by undesirable oxidative stress, angiogenic and proliferative responses.
    Type: Grant
    Filed: August 23, 2010
    Date of Patent: January 17, 2012
    Assignees: Dominion Pharmakine S.L, Universidad del Pais Vasco
    Inventors: Fernando Pedro Cossio, Eneko Aldaba Arevalo, Yosu Ion Vara Salazar, Aizpea Zubia Olascoaga, Silvia Vivanco Amato, Miren Lorea Mendoza Arteche, Clarisa Salado Pogonza, Natalia Gallot Escobal, Fernando Vidal Vanaclocha
  • Heterocyclyl substituted tetrahydronaphthalene derivatives as 5-HT7 receptor ligands
    Patent number: 8097641
    Abstract: The present invention relates to heterocyclyl-substituted-tetrahydro-naphthalen compounds of general formula (I), methods for their preparation, and compositions comprising these compounds as well as their use for the treatment or prophylaxis of various disorders in humans or animals.
    Type: Grant
    Filed: February 6, 2008
    Date of Patent: January 17, 2012
    Assignee: Laboratorios del Dr. Esteve, S.A.
    Inventors: Monica Garcia-Lopez, Antonio Torrens-Jover, Helmut H. Buschmann
  • Derivative having PPAR agonistic activity
    Patent number: 8097610
    Abstract: A compound of the formula (I): or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 24, 2006
    Date of Patent: January 17, 2012
    Assignees: Shionogi & Co., Ltd., Institute of Medicinal Molecular Design, Inc.
    Inventors: Akiko Itai, Susumu Muto, Ryuko Tokuyama, Hiroshi Fukasawa, Takafumi Ohara, Terukazu Kato
  • Cannabinoid receptor antagonists/inverse agonists useful for treating metabolic disorders, including obesity and diabetes
    Patent number: 8088809
    Abstract: The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and/or cardiometabolic disorders.
    Type: Grant
    Filed: January 12, 2010
    Date of Patent: January 3, 2012
    Assignee: Jenrin Discovery, Inc.
    Inventors: John F. McElroy, Robert J. Chorvat
  • JAK-2 modulators and methods of use
    Patent number: 8088767
    Abstract: This invention relates to the field of protein tyrosine kinases and inhibitors thereof. In particular, the invention relates to inhibitors of JAK-2, pharmaceutical compositions of the compounds for inhibiting JAK-2, methods of inhibiting JAK-2 in a cell, comprising contacting a cell in which inhibition of JAK-2 is desired with a compound or pharmaceutical composition comprising a compound according to the invention. The also comprises methods of treating a disease or condition that involves JAK-2 comprising administering to a patient a pharmaceutical composition comprising a compound according to the invention.
    Type: Grant
    Filed: September 28, 2007
    Date of Patent: January 3, 2012
    Assignee: Exelixis, Inc.
    Inventors: Adam Antoni Galan, Jeff Chen, Hongwang Du, Timothy Forsyth, Tai Phat Huynh, Henry William Beecroft Johnson, Patrick Kearney, James W. Leahy, Matthew Sangyup Lee, Grace Mann, Brian Hugh Ridgway, Craig Stacy Takeuchi, Peiwen Zhou
  • Substituted N-phenyl-bipyrrolidine carboxamides and therapeutic use thereof
    Patent number: 8088808
    Abstract: The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I). Wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefor.
    Type: Grant
    Filed: March 15, 2010
    Date of Patent: January 3, 2012
    Assignee: Sanofi
    Inventors: Werngard Czechtizky, Zhongli Gao, William Joseph Hurst, Lothar Schwink, Siegfried Stengelin
  • 3-3-di-substituted-oxindoles as inhibitors of translation initiation
    Patent number: 8088816
    Abstract: Compositions and methods for inhibiting translation using 3-(5-tert-Butyl-2-Hydroxy-phenyl) -3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using 3-(5-tert-butyl-2-hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are described.
    Type: Grant
    Filed: June 9, 2010
    Date of Patent: January 3, 2012
    Assignee: President and Fellows of Harvard College
    Inventors: José A. Halperin, Amarnath Natarajan, Huseyin Aktas, Yun-Hua Fan, Han Chen
  • Biphenyl amide lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
    Patent number: 8088776
    Abstract: The present invention discloses novel compounds of Formula I: possessing 11 ?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11 ?-HSD type 1 activity.
    Type: Grant
    Filed: April 19, 2007
    Date of Patent: January 3, 2012
    Assignee: Eli Lilly and Company
    Inventors: Thomas Daniel Aicher, Zhaogen Chen, Ronald Jay Hinklin, Gary Alan Hite, Alexei Pavlovych Krasutsky, Renhua Li, Jefferson Ray McCowan, Ashraf Saeed, Nancy June Snyder, James Lee Toth, Owen Brendan Wallace, Leonard Larry Winneroski, Jr., Yanping Xu, Jeremy Schulenburg York
  • Organic compounds
    Patent number: 8084450
    Abstract: 3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4-substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed.
    Type: Grant
    Filed: December 28, 2005
    Date of Patent: December 27, 2011
    Assignee: Novartis AG
    Inventors: Werner Breitenstein, Takeru Ehara, Claus Ehrhardt, Philipp Grosche, Yuko Hitomi, Yuki Iwaki, Takanori Kanazawa, Kazuhide Konishi, Juergen Klaus Maibaum, Keiichi Masuya, Atsuko Nihonyanagi, Nils Ostermann, Masaki Suzuki, Atsushi Toyao, Fumiaki Yokokawa
  • Compounds for enzyme inhibition
    Patent number: 8080576
    Abstract: One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.
    Type: Grant
    Filed: February 19, 2010
    Date of Patent: December 20, 2011
    Assignee: Onyx Therapeutics, Inc.
    Inventors: Kevin D. Shenk, Francesco Parlati, Han-Jie Zhou, Catherine Sylvain, Mark S. Smyth, Mark K. Bennett, Guy J. Laidig
  • Compounds for enzyme inhibition
    Patent number: 8080545
    Abstract: One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.
    Type: Grant
    Filed: February 19, 2010
    Date of Patent: December 20, 2011
    Assignee: Onyx Therapeutics, Inc.
    Inventors: Kevin D. Shenk, Francesco Parlati, Han-Jie Zhou, Catherine Sylvain, Mark S. Smyth, Mark K. Bennett, Guy J. Laidig
  • Renin inhibitors
    Patent number: 8076359
    Abstract: The present invention relates to disubstituted piperidinyl renin inhibitor compounds having the structure (Formula I) and their use in treating cardiovascular events and renal insufficiency.
    Type: Grant
    Filed: November 14, 2007
    Date of Patent: December 13, 2011
    Assignee: Merck Canada Inc.
    Inventors: Daniel Dube, Michel Gallant, Erich L. Grimm, Helene Juteau, Sebastien Laliberte, Tom Yao-Hsiang Wu
  • Indole carboxamides as IKK2 inhibitors
    Patent number: 8071584
    Abstract: The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula (I): wherein R1, R2, R3, R4, and m are as defined herein. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, rhinitis, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Grant
    Filed: March 20, 2008
    Date of Patent: December 6, 2011
    Assignee: GlaxoSmithKline LLC
    Inventors: Jeffrey Charles Boehm, Jakob Busch-Petersen, Wei Fu, Qi Jin, Jeffrey K. Kerns, Huijie Li, Guoliang Lin, Xichen Lin, Christopher E. Neipp
  • Method and intermediates for the preparation of derivatives of N-(1-benzhydrylazetidin-3-yl)-N-phenylmethylsulfonamide
    Patent number: 8071788
    Abstract: The invention relates to a novel method for the synthesis of N-{1-[bis(4-chlorophenyl)methyl]azetidin-3-yl}-N-(3,5 -difluorophenyl)methylsulfonamide.
    Type: Grant
    Filed: December 11, 2009
    Date of Patent: December 6, 2011
    Assignee: Sanofi-Aventis
    Inventors: Philippe Boffelli, Michel Delthil, Luc Grondard, Maxime Lampilas, Joel Malpart, Stephane Mutti, Lahlou Nait-Bouda, Joerg Reike-Zapp
  • 1,2-disubstituted heterocyclic compounds
    Patent number: 8071595
    Abstract: 1,2-disubstituted heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described. Also described are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Among the disorders which may be treated are neurological, neurodegenerative and psychiatric disorders including, but not limited to, those associated with cognitive deficits or schizophrenic symptoms.
    Type: Grant
    Filed: June 24, 2009
    Date of Patent: December 6, 2011
    Assignee: EnVivo Pharmaceuticals, Inc.
    Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
  • N,N-disubstituted aminoalkylbiphenyl antagonists of prostaglandin Dreceptors
    Patent number: 8067445
    Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Grant
    Filed: January 29, 2009
    Date of Patent: November 29, 2011
    Assignee: Panmira Pharmaceuticals, LLC
    Inventors: John Howard Hutchinson, Brian Andrew Stearns, Jill Melissa Scott, Yen Pham Truong, Jeffrey Roger Roppe, Nicholas Simon Stock, Jeannie M. Arruda, Thomas Jon Seiders, Bowei Wang, Deborah Volkots
  • Tetrahydronaphthalen-2-ol derivatives
    Patent number: 8063102
    Abstract: The present invention relates to novel tetrahydronaphthalen-2-ol derivatives, to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular to their use for the manufacture of a medicament for the prevention or treatment of lower urinary tract symptoms, benign prostate hyperplasia, prostate cancer, hot flushes, anxiety, depression, breast cancer, medullary thyroid carcinoma, ovarian cancer, inflammatory bowel disease, arthritis, endometriosis, and colon cancer.
    Type: Grant
    Filed: March 11, 2010
    Date of Patent: November 22, 2011
    Assignee: N.V. Organon
    Inventors: Herman Thijs Stock, Neeltje Miranda Teerhuis, Gerrit Herman Veeneman
  • Inhibitors of MEK
    Patent number: 8063049
    Abstract: This invention concerns to N-(2-aylamino)aryl sulfonamides, which are inhibitors of MEK, methods of using such compounds in the treatment of hyperproliferative diseases, and to pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: November 22, 2011
    Assignee: Ardea Biosciences, Inc.
    Inventors: Yung-hyo Koh, Zhi Hong, Jean-Michel Vernier, Andreas Maderna
  • Substituted 1,3-diphenylprop-2-en-1-one derivatives, preparation and uses thereof
    Patent number: 8058308
    Abstract: The invention concerns novel substituted 1,3-diphenylprop-2-en-1-one derivatives, pharmaceutical compositions comprising same, their therapeutic uses, in particular for treating cerebral ischemia. The invention also concerns a method for preparing said derivatives.
    Type: Grant
    Filed: April 11, 2011
    Date of Patent: November 15, 2011
    Assignee: Genfit
    Inventors: Jamila Najib, Karine Caumont-Bertrand