Plural Nitrogens In The Hetero Ring Patents (Class 540/492)
  • Patent number: 10457831
    Abstract: The present invention relates to an oxidatively curable coating formulation comprising an oxidatively curable alkyd-based resin and a diazacycloalkane-based chelant, which chelant may optionally be complexed with a suitable transition metal ion. The formulations may be paints or other oxidatively curable coating compositions. The invention also provides methods for making such formulations and compositions resultant from the curing of such formulations.
    Type: Grant
    Filed: August 6, 2015
    Date of Patent: October 29, 2019
    Assignee: CATEXEL LIMITED
    Inventors: Ronald Hage, Johannes Wietse De Boer, Karin Maaijen
  • Patent number: 10036048
    Abstract: The process for obtaining a naphthoquinone derivative from Streptomyces sp. includes providing a seed inoculum of a strain of Streptomyces sp.; culturing the Streptomyces sp. in a culture nutrient medium; centrifuging the culture nutrient medium to provide a supernatant and a biomass precipitate; admixing a water immiscible solvent to the supernatant to produce a water immiscible solvent extract layer and a water layer; and isolating the antimicrobial and cytotoxic compound from the water immiscible solvent extract layer by performing silica gel chromatography.
    Type: Grant
    Filed: December 12, 2017
    Date of Patent: July 31, 2018
    Assignee: KING SAUD UNIVERSITY
    Inventors: Naif Abdullah Al-Dhabi, Savarimuthu Ignacimuthu, Chandrasekar Balachandran, Veeramuthu Duraipandiyan
  • Patent number: 10030010
    Abstract: The present invention relates to a process for the preparation of a compound of formula (A), Further, the present invention relates to the respective compound (A) as such and to its use in the preparation of antifungal agent.
    Type: Grant
    Filed: August 4, 2015
    Date of Patent: July 24, 2018
    Assignee: Sandoz AG
    Inventors: Roland Barth, Kathrin Höferl-Prantz, Frank Richter, Gerhard Widschwenter
  • Patent number: 9745307
    Abstract: Disclosed are the ERK inhibitors of formula (I) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I). This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier. This invention also provides a method of inhibiting ERK (i.e., inhibiting the activity of ERK2) in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of formula (I).
    Type: Grant
    Filed: April 25, 2014
    Date of Patent: August 29, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jongwon Lim, Xianhai Huang, Ronald D. Ferguson, Wei Zhou, Christopher W. Boyce, Phieng Siliphaivanh, David J. Witter, Milana M. Maletic, Joseph A. Kozlowski, Kevin J. Wilson
  • Publication number: 20150132258
    Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
    Type: Application
    Filed: November 14, 2014
    Publication date: May 14, 2015
    Inventor: George D. Hartman
  • Patent number: 8975219
    Abstract: A fabric cleaning composition comprising from 1% to 20% by weight of the fabric cleaning composition of an oxygen-based bleaching source and a hueing agent, and wherein the neat composition has a pH between 2.5 and 5.5, and a method of using said fabric cleaning composition.
    Type: Grant
    Filed: May 16, 2012
    Date of Patent: March 10, 2015
    Assignee: The Procter & Gamble Company
    Inventors: Margherita Scartozzi, Luca Sarcinelli, Sophie Anne Marguerite Goellner, Enza Ceccobelli, Leo Gagliardi
  • Publication number: 20150031676
    Abstract: This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.
    Type: Application
    Filed: February 20, 2013
    Publication date: January 29, 2015
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Mario Lobell, Walter Hübsch, Hartmut Schirok, Mélanie Héroult, Dirk Brohm, Marie-Pierre Collin, Sylvia Grünewald, Klemens Lustig, Ulf Bömer, Verena Vöhringer, Niels Lindner
  • Publication number: 20150025058
    Abstract: Compounds of the formula I in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of cancer, rheumatoid arthritis and/or systemic lupus
    Type: Application
    Filed: January 22, 2013
    Publication date: January 22, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Carl Deutsch, Daniel Kuhn, Tatjana Ross, Lars Burgdorf
  • Publication number: 20150005284
    Abstract: Compounds of the formula I in which R1, R2 and X have the meanings indicated in Claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseases.
    Type: Application
    Filed: January 3, 2013
    Publication date: January 1, 2015
    Applicant: Merck Patent GmbH
    Inventors: Hans Michael Eggenweiler, Guenter Hoelzemann, Dieter Dorsch
  • Patent number: 8906913
    Abstract: The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof.
    Type: Grant
    Filed: June 22, 2010
    Date of Patent: December 9, 2014
    Assignee: Panacea Biotec Limited
    Inventors: Rajesh Jain, Sanjay Trehan, Jagattaran Das, Gurmeet Kaur, Sandeep Kanwar, Nishan Singh, Gurmeet Kaur Nanda, Sitaram Kumar Magadi, Sudhir Kumar Sharma
  • Publication number: 20140350243
    Abstract: The present invention relates to compounds of the formula (1) which are suitable for use in electronic devices, in particular organic electroluminescent devices.
    Type: Application
    Filed: August 7, 2014
    Publication date: November 27, 2014
    Applicant: Merch Patent GmbH
    Inventors: Amir Hossain Parham, Christof Pflumm, Teresa Mujica-Fernaud
  • Publication number: 20140296214
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.
    Type: Application
    Filed: October 12, 2012
    Publication date: October 2, 2014
    Inventors: Michael J. Orwat, Donald J.P. Pinto, Leon M. Smith, II, Shefali Srivastava
  • Patent number: 8846660
    Abstract: A compound having a 7-membered nitrogen-containing ring skeleton represented by the formula (I), which is useful for the prevention or treatment of diseases, in which chymase is involved and a pharmaceutical containing the same for the prevention or treatment of a disease, in which chymase is involved.
    Type: Grant
    Filed: December 24, 2010
    Date of Patent: September 30, 2014
    Assignee: Daiichi Sankyo Company, Ltd.
    Inventors: Tsuyoshi Muto, Taisaku Tanaka, Junko Futamura, Seiichi Imajo, Hajime Sugawara
  • Patent number: 8835626
    Abstract: The present invention relates to compounds of the formula (1) which are suitable for use in electronic devices, in particular organic electroluminescent devices.
    Type: Grant
    Filed: February 25, 2011
    Date of Patent: September 16, 2014
    Assignee: Merck Patent GmbH
    Inventors: Amir Hossain Parham, Christof Pflumm, Teresa Mujica-Fernaud
  • Patent number: 8791103
    Abstract: The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: July 29, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Henning Priepke, Kai Gerlach, Roland Pfau, Norbert Hauel, Iris Kauffmann-Hefner, Georg Dahmann, Herbert Nar, Sandra Handschuh, Wolfgang Wienen, Annette Schuler-Metz
  • Publication number: 20140148443
    Abstract: Disclosed are compounds of Formula I or pharmaceutically acceptable salts thereof, wherein X1, X2, X3, R1, R2 and R3 are as described in this application, and methods of using the compounds in the treatment of cancer.
    Type: Application
    Filed: November 20, 2013
    Publication date: May 29, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Xin-Jie Chu, Allen John Lovey, Binh Thanh Vu, Chunlin Zhao
  • Publication number: 20140128361
    Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.
    Type: Application
    Filed: January 6, 2014
    Publication date: May 8, 2014
    Applicants: Pharmacopeia Drug Discovery, Inc., Merck Sharp & Dohme Corp.
    Inventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voight, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X.H. Le, Jeffrey H. Lowrie, Kurt W. Salonz, Suresh D. Babu
  • Patent number: 8716312
    Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
    Type: Grant
    Filed: November 17, 2009
    Date of Patent: May 6, 2014
    Assignee: Merck Sharp & Dohme Corporation
    Inventors: Pauline C. Ting, Robert Aslanian, Mary Ann Caplen, Jianhua Cao, Tin-Yau Chan, David Kim, Hyunjin Kim, Jae-Hun Kim, Rongze Kuang, Joe F. Lee, John Schwerdt, Heping Wu, Nicolas Zorn
  • Patent number: 8697688
    Abstract: Pyrrolobenzodiazepine dimers I having a C2-C3 double bond and an aryl group at the C2 position on one monomer unit, and a C2-C3 double bond and either a conjugated double or triple bond at the C2 position or an alkyl group at the C2 position on the other monomer unit, and conjugates of these compounds.
    Type: Grant
    Filed: April 15, 2011
    Date of Patent: April 15, 2014
    Assignees: Seattle Genetics Inc., Spirogen Sarl
    Inventors: Philip Wilson Howard, Luke Masterson, Arnaud Tiberghien, Scott Jeffrey, Patrick Burke, Peter Senter
  • Publication number: 20140080816
    Abstract: The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT2C receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT2C receptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT2C receptor.
    Type: Application
    Filed: September 13, 2013
    Publication date: March 20, 2014
    Inventors: Hannes Koolman, Wilfried Braje, Helmut Mack, Andreas Haupt, Ana Lucia Relo, Karla Drescher, Margot Bakker, Viktor Lakics, Carolin Hoft, Ruxu Xu, Xiaona Zhao
  • Patent number: 8623324
    Abstract: Chemically reactive dyes that are intramolecularly crosslinked with a water-soluble bridge, their bioconjugates and their uses are described. Reactive fluorescent dyes that have a water-soluble bridge are superior to those of conjugates of spectrally non-crosslinked dyes or the dyes that are crosslinked with a hydrophobic bridge. The invention includes reactive fluorescent dyes, their biological conjugates and uses.
    Type: Grant
    Filed: July 12, 2011
    Date of Patent: January 7, 2014
    Assignees: AAT Bioquest Inc., Becton, Dickinson and Company
    Inventors: Timothy Dubrovsky, Barnaby Abrams, Zhenjun Diwu, Qinglin Meng, Jinfang Liao, Haitao Guo
  • Patent number: 8598160
    Abstract: This invention relates to novel compounds of the Formula (I), any of the formulas I1-I26 1a1-3-1j1-3 or pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Grant
    Filed: February 13, 2009
    Date of Patent: December 3, 2013
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: David A. Claremon, Linghang Zhuang, Yuanjie Ye, Suresh B. Singh, Colin M. Tice, Robert D. Simpson
  • Publication number: 20130303516
    Abstract: The present invention relates to novel triazine compounds of formula (1), methods of their preparation, pharmaceutical compositions containing these compounds and the use of these compounds to treat proliferative disorders such as tumors and cancers and also other conditions and disorders related to or associated with dysregulation of PI3 Kinases, PI3 Kinase pathway, mTOR and/or the mTOR pathway.
    Type: Application
    Filed: January 25, 2012
    Publication date: November 14, 2013
    Inventors: Sundeep Dugar, Dinesh Mahajan, Chandraban Rhushikesh Deokar, Peter Frank Hollinger, Kamal Kishore Kapoor
  • Publication number: 20130296551
    Abstract: A 7-membered heterocyclic compound having the formula (I), or its salt, or a solvate thereof with a chymase inhibitory action and useful for the prevention or treatment of various diseases, in which chymase is involved: a method for producing the same, and a pharmaceutical composition useful for the prevention or treatment of diseases, in which chymase is involved, including the compound of having the formula (I), or its pharmaceutically acceptable salt, or a solvate thereof are provided.
    Type: Application
    Filed: July 3, 2013
    Publication date: November 7, 2013
    Inventors: Tsuyoshi MUTO, Taisaku Tanaka, Hiroshi Maruoka, Seiichi Imajo, Yoshiaki Tomimori
  • Patent number: 8563539
    Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway.
    Type: Grant
    Filed: December 23, 2010
    Date of Patent: October 22, 2013
    Assignee: Jasco Pharmaceuticals, LLC
    Inventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Robert B. Nicewonger, Yvonne L. Flanders, Stephane A. Dumas
  • Publication number: 20130245006
    Abstract: The invention relates to indolizine derivatives of general formula (I), where A, B, m, W, n and R2 are as defined in claim 1, as well as to the method for preparing same and to the therapeutic use thereof.
    Type: Application
    Filed: November 16, 2011
    Publication date: September 19, 2013
    Applicant: SANOFI
    Inventors: Jean-Michel Altenburger, Franck Caussanel, Sergio Mallart, Marie-Claire Philippo-Orts
  • Publication number: 20130231275
    Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases particularly bacterial infections.
    Type: Application
    Filed: April 17, 2013
    Publication date: September 5, 2013
    Applicant: Novartis AG
    Inventors: Simon Bushell, Matthew J. Lamarche, Jennifer Leeds, Lewis Whitehead
  • Patent number: 8513239
    Abstract: There are provided compounds of the formula or the pharmaceutically acceptable salts thereof, wherein X, Y, Z, V1, V2, R1, R2, R3, R4 and R5 are herein described. These compounds are useful as anticancer agents.
    Type: Grant
    Filed: October 9, 2008
    Date of Patent: August 20, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David Joseph Bartkovitz, Jianping Cai, Xin-Jie Chu, Hongju Li, Allen John Lovey, Binh Thanh Vu, Chunlin Zhao
  • Publication number: 20130210768
    Abstract: The present invention is directed to 5-substituted 1,3-dihydro-2H-imidazo[4,5-b]pyridine-2-one derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia.
    Type: Application
    Filed: June 6, 2011
    Publication date: August 15, 2013
    Inventors: Kenneth L. Arrington, Vadim Dudkin, Mark E. Layton, Joseph E. Pero, Alexander J. Reif
  • Publication number: 20130196973
    Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
    Type: Application
    Filed: March 13, 2012
    Publication date: August 1, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Asitha Abeywardane, Michael J. Burke, Thomas Martin Kirrane, Matthew Russell Netherton, Anil Kumar Padyana, Lana Louise Smith Keenan, Hidenori Takahashi, Michael Robert Turner, Qiang Zhang, Qing Zhang
  • Publication number: 20130172549
    Abstract: Heteroaryl amide derivatives are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Application
    Filed: January 29, 2013
    Publication date: July 4, 2013
    Applicant: H. Lundbeck A/S
    Inventor: H. Lundbeck A/S
  • Patent number: 8460704
    Abstract: The invention relates to an extended release pharmaceutical composition comprising nevirapine.
    Type: Grant
    Filed: June 4, 2008
    Date of Patent: June 11, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Michael L. Cappola, Svetlana Sienkiewicz, Glenn Charles Snow, Feng-Jing Chen
  • Patent number: 8445674
    Abstract: The invention is concerned with novel bicyclic compounds of formula (I), wherein n, m, p, A, L, R1, R2, R3, R4, R5, R6, R7, R7, R8, R9, and R10 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor may be used, for example, in the prevention and/or treatment of inflammatory diseases, particularly peripheral arterial occlusive diseases or atherothrombosis.
    Type: Grant
    Filed: October 11, 2010
    Date of Patent: May 21, 2013
    Assignee: Hoffmann-La Roche Inc
    Inventors: Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei
  • Patent number: 8440653
    Abstract: The present invention provides compounds of Formula (I) that are useful for modulating the biological activity of the melanocortin-5 receptor (MC5R). Compounds of this invention can be used to treat diseases and/or conditions in which downregulation of MC5R is beneficial. Such diseases and/or conditions include, but are not limited to, acne, seborrhea, seborrheic dermatitis, cancer, and inflammatory diseases.
    Type: Grant
    Filed: February 27, 2009
    Date of Patent: May 14, 2013
    Assignee: Mimetica Pty Ltd
    Inventors: Mark Arnold Thomas Blaskovich, Peter Joseph Cassidy
  • Publication number: 20130096084
    Abstract: The present invention provides a compound of the Formula I: (Formular I should be inserted here) or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2 and R3 are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.
    Type: Application
    Filed: June 22, 2011
    Publication date: April 18, 2013
    Inventors: Yongqi Deng, Liang Zhu, Gerald W. Shipps, JR., Sie-Mun Lo, Binyuan Sun, Xiaohua Huang, Corey Bienstock, Alan B. Cooper, Xiaolei Gao, Xin Yao, Hugh Y. Zhu, Joseph M. Kelly, Sobhana Babu Boga, Abdul-Basit Alhassan, Jayaram R. Tagat, Umar Faruk Mansoor, Kevin J. Wilson, Brendan M. O'Boyle, Matthew Hersh Daniels, Adam Schell, Phieng Siliphaivanh, Christian Fischer
  • Publication number: 20130079321
    Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: September 26, 2012
    Publication date: March 28, 2013
    Applicant: GENENTECH, INC.
    Inventor: GENENTECH, INC.
  • Patent number: 8399681
    Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalac
    Type: Grant
    Filed: August 3, 2012
    Date of Patent: March 19, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gilles Bignan, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
  • Patent number: 8394789
    Abstract: The invention relates to 5,6-dihydropyrrolo[2,1-?]isoquinoline and pyrrolo[2,1-?]isoquinoline derivatives according to general formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.
    Type: Grant
    Filed: February 6, 2009
    Date of Patent: March 12, 2013
    Assignee: MSD Oss B.V.
    Inventors: Rachel Deborah van Rijn, Hubert Jan Josef Loozen, Cornelis Marius Timmers, Lars Anders van der Veen, Willem Frederik Johan Karstens
  • Publication number: 20130053363
    Abstract: [Problem] To provide a compound useful as medicine having PDE4B inhibitory activity, in particular, as an active ingredient of a composition for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like. [Measures for Solution] The present inventors examined compounds having PDE4B inhibitory activity and found that a tricyclic or tetracyclic imidazo[1,2-a]pyridine derivative or salts thereof had a superior PDE4B inhibitory activity, thereby completing the present invention. The imidazo[1,2-a]pyridine derivative can be used as an agent for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like.
    Type: Application
    Filed: October 26, 2012
    Publication date: February 28, 2013
    Applicant: Astellas Pharma Inc.
    Inventor: Astellas Pharma Inc.
  • Publication number: 20130023502
    Abstract: The invention relates to new substituted pyridinyl-pyrimidines of formula 1 wherein ring A is a five-membered saturated or unsaturated carbocyclic ring which optionally comprises one, two or three heteroatoms each independently from each other selected from the group N, S and O, wherein R1, R2, R4, R3, R5 and R6 are defined as in claim 1 and wherein ring A is further optionally substituted by one or two further substituents and the pharmaceutically acceptable salts, diastereomers, enantiomers, racemates, hydrates and solvates of the aforementioned compounds.
    Type: Application
    Filed: January 25, 2012
    Publication date: January 24, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GmbH
    Inventors: Georg Dahmann, Dennis Fiegen, Martin Fleck, Matthias Hoffmann, Jasna Klicic, Stephen Peter East, Spencer Charles R. Napier, John Scott
  • Patent number: 8357679
    Abstract: The present invention relates to hexafluoroisopropanol derivatives having the general formula I to pharmaceutical compositions comprising the same and to the use of these hexafluoroisopropanol derivatives in the treatment of atherosclerosis.
    Type: Grant
    Filed: May 13, 2009
    Date of Patent: January 22, 2013
    Assignee: MSD Oss B.V.
    Inventors: Andrew John Cooke, Andrew Stanley Edwards, Fiona Elizabeth Andrews, David Jonathan Bennett, Olaf Nimz, Emma Louise Carswell
  • Publication number: 20130012700
    Abstract: The present invention relates to compounds of the formula (1) which are suitable for use in electronic devices, in particular organic electroluminescent devices.
    Type: Application
    Filed: February 25, 2011
    Publication date: January 10, 2013
    Applicant: Merck Patent GmbH
    Inventors: Amir Hossain Parham, Christof Pflumm, Teresa Mujica-Fernaud
  • Publication number: 20130012485
    Abstract: Compounds of the formula (I) are provided: wherein V, W, X, Y, Z, R3, R4, R5, R6, R7 and m are as defined in the specification; and pharmaceutically acceptable salts and prodrugs thereof. The compounds may be useful in the treatment or prevention of various diseases and conditions in which dipeptidylpeptidase-IV (DPP-IV) is implicated.
    Type: Application
    Filed: December 20, 2007
    Publication date: January 10, 2013
    Inventors: Daniel Kaspar Bäschlin, Richard Sedrani, Stefanie Flohr, Kenji Namoto, Nils Ostermann, Finton Sirockin, François Gessier, Garry Fenton, Mandy Christine Beswick, David Edward Clark, Bohdan Waszkowycz
  • Publication number: 20130004518
    Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.
    Type: Application
    Filed: September 11, 2012
    Publication date: January 3, 2013
    Applicant: Merck, Sharp & Dohme Corp.
    Inventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voight, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X.H. Le, Jeffrey F. Lowrie, Kurt W. Saionz, Suresh D. Babu
  • Publication number: 20130005710
    Abstract: The present invention provides a novel aminopyridine derivative that is excellent in pharmaceutical effects such as a neuroprotective effect, a neurogenesis or nerve regeneration promoting effect, and a cognitive function improving effect and, preferably, is low toxic and delivered at a high rate to the central nervous system.
    Type: Application
    Filed: November 17, 2010
    Publication date: January 3, 2013
    Inventors: Tetsuya Tsukamoto, Takeshi Wakabayashi, Norihito Tokunaga, Yuhei Miyanohana
  • Patent number: 8343958
    Abstract: The present invention provides compounds of Formula (I) that are useful for modulating the biological activity of the melanocortin-5 receptor (MC5R). Compounds of this invention can be used to treat diseases and/or conditions in which downregulation of MC5R is beneficial. Such diseases and/or conditions include, but are not limited to, acne, seborrhea, seborrheic dermatitis, cancer, and inflammatory diseases.
    Type: Grant
    Filed: June 6, 2011
    Date of Patent: January 1, 2013
    Assignee: Mimetica Pty Ltd
    Inventors: Mark Arnold Thomas Blaskovich, Peter Joseph Cassidy
  • Patent number: 8334283
    Abstract: Compositions for treating, reducing, ameliorating, or preventing infections comprise a fluoroquinolone having Formulae I-VIII and an additional anti-infective agent. Methods for treating, reducing, ameliorating, or preventing such infection use such compositions. Such compositions and methods can be effective against mixed types of pathogens including certain antibiotic-resistant microbial pathogens found in such infections.
    Type: Grant
    Filed: April 3, 2012
    Date of Patent: December 18, 2012
    Assignee: Bausch & Lomb Incorporated
    Inventors: Praveen Tyle, Erning Xia, Hongna Wang, Susan E. Norton, Pramod Kumar Gupta, Keith W. Ward, Lynne Brunner
  • Publication number: 20120309735
    Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
    Type: Application
    Filed: December 16, 2010
    Publication date: December 6, 2012
    Inventors: Michael D. Altman, Kenneth L. Arrington, Jason Burch, Bernard Cote, Jean-Francois Fournier, Jacques Yves Gauthier, Solomon Kattar, Sandra Lee Knowles, Jongwon Lim, Michelle R. Machacek, Alan B. Northrup, Michael H. Reutershan, Joel S. Robichaud, Adam J. Schell, Kerrie B. Spencer
  • Publication number: 20120283239
    Abstract: The invention relates to 1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derived Cathepsin S inhibitors of Formula (I), wherein R1 is H or (C1-3)alkyl; R2 is halogen or (C1-4)alkyl, optionally substituted with one or more halogens; n is 1-3; X is O or CH2; U, V and W are CH; or one of U, V and W is N; Y is a group capable of interacting with the Sn . . . S2 substites of the active site of Cathepsin S; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.
    Type: Application
    Filed: January 13, 2011
    Publication date: November 8, 2012
    Applicant: MSD OSS B.V.
    Inventors: Jiaqiang Cai, David Jonathan Bennett, Philip Stephen Jones
  • Publication number: 20120277192
    Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
    Type: Application
    Filed: December 15, 2010
    Publication date: November 1, 2012
    Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Sathesh Bhat, Jason Burch, Kaleen Konrad Childers, Bernard Cote, Maria Emilia Di Francesco, Anthony Donofrio, Kristina Dupont-Gaudet, John Michael Ellis, Christian Fischer, Jean-Francois Fournier, Jacques Yves Gauthier, Jonathan Grimm, Daniel Guay, David Joseph Guerin, Andrew M. Haidle, Solomon Kattar, Sandra Lee Knowles, Chaomin Li, Jongwon Lim, Michelle R. Machacek, Matthew L. Maddess, Alan B. Northrup, Brendan M. O'Boyle, Ryan D. Otte, Alessia Petrocchi, Michael H. Reutershan, Joel S. Robichaud, Eric Romeo, Adam J. Schell, Tony Siu, Kerrie B. Spencer, Brandon M. Taoka, B. Wesley Trotter, Hyun Chong Woo, Hua Zhou