Chalcogen Attached Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/332)
  • Inhibitors of protein kinases
    Patent number: 8436007
    Abstract: The present invention relates to inhibitors of cyclin-dependent kinases and therapeutic applications thereof. Furthermore, the invention relates to methods of preventing and/or treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases comprising the administration of an effective amount of at least one inhibitor of cyclin-dependent kinases.
    Type: Grant
    Filed: April 24, 2008
    Date of Patent: May 7, 2013
    Assignee: Ingenium Pharmaceuticals GmbH
    Inventors: Philipp Wabnitz, Heike Schauerte, Hans Allgeier, Martin Augustin, Lutz Zeitlmann, Michael A. Pleiss, Gabriele Stumm, Anke Mueller
  • Chemical compounds
    Patent number: 8436167
    Abstract: Two polymorphic forms of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid] calcium salt, processes for making them and their use as HMG Co-A reductase inhibitors are described.
    Type: Grant
    Filed: March 1, 2011
    Date of Patent: May 7, 2013
    Assignee: AstraZeneca UK Limited
    Inventors: Rebecca Jane Booth, Peter Anthony Cittern, Jeffrey Norman Crabb, John Horbury, David Wyn Calvert Jones
  • Prodrug of triazolone compound
    Patent number: 8436009
    Abstract: By oral administration of a compound represented by the following Formula (I): the blood level of Compound (IV): which has an excellent inhibitory action against blood coagulation factor VIIa and the anticoagulant action, reaches a level sufficient for expression of its pharmacological actions. Therefore, the compound of the present invention is useful as a therapeutic and/or prophylactic agent for diseases caused by thrombus formation.
    Type: Grant
    Filed: May 18, 2011
    Date of Patent: May 7, 2013
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Richard Clark, Fumiyoshi Matsuura, Masanobu Shinoda, Shinsuke Hirota, Kazunobu Kira, Hiroshi Azuma, Atsushi Takemura, So Yasui, Kazutomi Kusano, Masaki Mikamoto, Takao Omae
  • SUBSTITUTED AMINOPROPIONIC DERIVATIVES AS NEPRILYSIN INHIBITORS
    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
  • AZAADAMANTANE DERIVATIVES AND METHODS OF USE
    Publication number: 20130096132
    Abstract: The invention relates to compounds that are azaadamantane derivatives, particularly ether- or amine-substituted azaadamantane derivatives and salts and prodrugs thereof, compositions comprising such compounds, methods of using such compounds and compositions, processes for preparing such compounds, and intermediates obtained during such processes.
    Type: Application
    Filed: October 16, 2012
    Publication date: April 18, 2013
    Applicant: ABBVIE INC.
    Inventor: AbbVie Inc.
  • ETHYNYL DERIVATIVES
    Publication number: 20130090347
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein U, V, W, Y, R, R1, R2, R3 and R3? are as described herein. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Application
    Filed: September 27, 2012
    Publication date: April 11, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • REGIOSELECTIVE PREPARATION OF SUBSTITUTED PYRIMIDINES
    Publication number: 20130079519
    Abstract: The present invention relates to a method of making pyrimidines of formula (III) wherein X1, X2, R1 and R2 have the meanings as defined herein.
    Type: Application
    Filed: November 16, 2012
    Publication date: March 28, 2013
    Inventors: Adil DURAN, Stefan GOEPPER, Joerg HALMER, Michael KONRAD
  • Selective NR2B Antagonists
    Publication number: 20130079338
    Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.
    Type: Application
    Filed: September 24, 2012
    Publication date: March 28, 2013
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventor: Bristol-Myers Squibb Company
  • Process for the preparation of statins and their pharmaceutically acceptable salts thereof
    Patent number: 8404841
    Abstract: Novel process for the preparation of statins and their pharmaceutically acceptable salts thereof represented by the general formula-(1) through novel intermediate compounds of general formula-(4).
    Type: Grant
    Filed: October 5, 2007
    Date of Patent: March 26, 2013
    Assignee: MSN Laboratories Limited
    Inventors: Manne Satyanarayana Reddy, Srinivasan Thirumalai Rajan, Maramreddy Sahadeva Reddy
  • PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF AMYLOID-RELATED DISEASES
    Publication number: 20130059871
    Abstract: The present invention provides (I) these compounds are useful in prevention and treatment of neurodegenerative disorders, such as Alzheimer's, Parkinson's and Huntington's as well as type II diabetes.
    Type: Application
    Filed: April 30, 2012
    Publication date: March 7, 2013
    Inventors: David Christopher HORWELL, David Ian Carter SCOPES
  • PHARMACEUTICAL COMPOSITIONS AS INHIBITORS OF DIPEPTIDYL PEPTIDASE-IV (DPP-IV)
    Publication number: 20130059873
    Abstract: The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.
    Type: Application
    Filed: April 3, 2012
    Publication date: March 7, 2013
    Inventors: David J. Madar, Stevan W. Djuric, Melissa J. Michmerhuizen, Hana A. Kopecka, Xiaofeng Li, Kenton L. Longenecker, Zhonghua Pei, Daisy Pireh, Hing L. Sham, Kent D. Stewart, Bruce G. Szczepankiewicz, Paul E. Wiedeman, Hong Yong
  • BIARYL COMPOUNDS AND METHODS OF USE THEREOF
    Publication number: 20130035326
    Abstract: Provided herein are compounds for treatment of KIT, CSF-1R and/or FLT3 kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
    Type: Application
    Filed: August 18, 2010
    Publication date: February 7, 2013
    Applicant: AMBIT BIOSCIENCES CORPORATION
    Inventors: Sunny Abraham, Mark W. Holladay, Gang Liu, Shimin Xu
  • QUINUCLIDINE DERIVATIVES AS MUSCARINIC M3 RECEPTOR ANTAGONISTS
    Publication number: 20130030001
    Abstract: The invention provides named compounds of formula (I), pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions and their use in therapy.
    Type: Application
    Filed: August 1, 2012
    Publication date: January 31, 2013
    Applicants: PULMAGEN THERAPEUTICS (SYNERGY) LIMITED, ASTRAZENECA AB
    Inventors: Richard James BULL, Elizabeth Anne SKIDMORE, Rhonan Lee FORD, Andrew Nigel MATHER, Antonio METE
  • MODULATORS OF THE GPR119 RECEPTOR AND THE TREATMENT OF DISORDERS RELATED THERETO
    Publication number: 20130023494
    Abstract: The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single agent or in combination with one or more additional pharmaceutical agents, such as, an inhibitor of DPP-IV, a biguanide, an SGLT2 inhibitor, or an alpha-glucosidase inhibitor, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.
    Type: Application
    Filed: April 5, 2011
    Publication date: January 24, 2013
    Applicant: ARENA PHARMACEUTICALS, INC.
    Inventors: Robert M. Jones, Sangdon Han, Daniel J. Buzard, Juerg Lehmann, Sanju Narayanan, Dawei Yue
  • SELECTIVE FAK INHIBITORS
    Publication number: 20130022594
    Abstract: A compound of the formula (I): where R1 or R2 is a cyclc amine group and R5 is an aromatic group with a carbonyl containing substituent for use as a FAK inhibitor.
    Type: Application
    Filed: July 6, 2012
    Publication date: January 24, 2013
    Applicant: Cancer Therapeutics CRC Pty Limited
    Inventors: Ian Peter Holmes, Ylva Bergman, Gillian Elizabeth Lunniss, Marica Nikac, Neil Chol, Catherine Fae Hemley, Scott Raymond Walker, Richard Charles Foitzik, Danny Ganame, Romina Lessene
  • Hexafluoroisopropanol derivatives
    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
  • NEW COMPOUNDS
    Publication number: 20130018054
    Abstract: The present invention provides organic compounds of the following structure; A-L1-B—C-D-L2-E that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 17, 2013
    Applicant: NOVARTIS AG
    Inventors: Michael H. SERRANO-WU, Young-shin KWAK, Wenming Liu
  • New compounds, pharmaceutical compositions and uses thereof
    Publication number: 20130018030
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, LP, LQ, X1, X2, X3, A, n and m are as defined in the application. The compounds of formula I have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Application
    Filed: January 20, 2012
    Publication date: January 17, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Frank HIMMELSBACH, Elke LANGKOPF, Bernd NOSSE
  • FAK INHIBITORS
    Publication number: 20130017194
    Abstract: A compound of the formula (I): where R1 or R2 is a cyclc amine group and R5 is an aromatic group with a carbonyl containing substituent for use as a FAK inhibitor.
    Type: Application
    Filed: July 6, 2012
    Publication date: January 17, 2013
    Applicant: Cancer Therapeutics CRC Pty Limited
    Inventors: Ian Peter Holmes, Ylva Bergman, Gillian Elizabeth Lunniss, Marica Nikac, Neil Choi, Catherine Fae Hemley, Scott Raymond Walker, Richard Charles Foitzik, Danny Ganame, Romina Lessene
  • Process for the synthesis of rosuvastatin calcium
    Patent number: 8354530
    Abstract: Present invention represents process for the preparation of HMG-CoA reductase inhibitors, in particular rosuvastatin calcium introducing L-malic acid as the source of chirality for the side chain.
    Type: Grant
    Filed: July 26, 2006
    Date of Patent: January 15, 2013
    Assignee: Lek Pharmaceuticals d. d
    Inventor: Marko Zlicar
  • SULFONYL AMIDE DERIVATIVES FOR THE TREATMENT OF ABNORMAL CELL GROWTH
    Publication number: 20130005964
    Abstract: The present invention relates to a compound of the formula I wherein R1 to R6, A, B, n and m are as defined herein. Such novel sulfonyl amide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: July 24, 2012
    Publication date: January 3, 2013
    Inventors: Michael Joseph Luzzio, Kevin Daniel Freeman-cook, Samit Kumar Bhattacharya, Matthew Merrill Hayward, Catherine Angela Hulford, Christopher Lowell Autry, Xumiao Zhao, Jun Xiao, Kendra Louise Nelson
  • BIARYLAMIDE INHIBITORS OF LEUKOTRIENE PRODUCTION
    Publication number: 20120322795
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, C, R1a, R1b, R2, R3, R4a and R4b are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: December 14, 2011
    Publication date: December 20, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Angela BERRY, Zhidong CHEN, Stephane DE LOMBAERT, Michel Jose EMMANUEL, Pui Leng LOKE, Chuk Chui MAN, Tina Marie MORWICK, Hidenori TAKAHASHI
  • N-LINKED HETEROCYCLIC RECEPTOR AGONISTS FOR THE TREATMENT OF DIABETES AND METABOLIC DISORDERS
    Publication number: 20120322804
    Abstract: Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control.
    Type: Application
    Filed: May 3, 2012
    Publication date: December 20, 2012
    Inventors: Jingyuan Ma, Christopher J. Rabbat, Jiangao Song, Xin Chen, Imad Nashashibi, Zuchun Zhao, Aaron Novack, Dong Fang Shi, Peng Cheng, Yan Zhu, Alison Murphy
  • Regioselective preparation of substituted pyrimidines
    Patent number: 8334383
    Abstract: The present invention relates to a method of making pyrimidines of formula (III), wherein X1, X2, R1 and R2 have the meanings as defined herein.
    Type: Grant
    Filed: March 19, 2009
    Date of Patent: December 18, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Adil Duran, Stefan Goepper, Joerg Halmer, Michael Konrad
  • CETP inhibitors
    Patent number: 8334290
    Abstract: Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Grant
    Filed: October 30, 2006
    Date of Patent: December 18, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Julianne A. Hunt, Florida Kallashi, Jennifer Kowalchick, Dooseop Kim, Cameron J. Smith, Peter J. Sinclair, Ramzi F. Sweis, Gayle E. Taylor, Christopher F. Thompson, Liya Chen, Nazia Quraishi
  • COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM
    Publication number: 20120316182
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: June 8, 2012
    Publication date: December 13, 2012
    Applicant: CalciMedica, Inc.
    Inventors: Jeffrey P. WHITTEN, Jonathan Grey, Jianguo Cao, Zhijun Wang, Evan Rogers
  • Imidazole-2,4-Dione Inhibitors of Casein Kinase 1
    Publication number: 20120316155
    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?), the TGF? pathway and/or the Wnt 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?), the TGF? pathway and/or the Wnt pathway.
    Type: Application
    Filed: February 17, 2011
    Publication date: December 13, 2012
    Applicant: Jasco Pharmaceuticals, LLC
    Inventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Robert B. Nicewonger
  • COFERONS AND METHODS OF MAKING AND USING THEM
    Publication number: 20120295874
    Abstract: The present invention is directed to a monomer useful in preparing therapeutic compounds. The monomer includes one or more pharmacophores which potentially binds to a target molecule with a dissociation constant of less than 300 ?M and a linker element connected to the pharmacophore. The linker element has a molecular weight less than 500 daltons, is connected, directly or indirectly through a connector, to the pharmacophore.
    Type: Application
    Filed: October 7, 2010
    Publication date: November 22, 2012
    Applicants: CORNELL UNIVERSITY, COFERON, INC., PURDUE RESEARCH FOUNDATION
    Inventors: Francis Barany, Maneesh Pingle, Sarah Filippa Giardina, Donald Bergstrom, Lee Daniel Arnold
  • Oxazolidinones as Modulators of MGLUR5
    Publication number: 20120283264
    Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, agonists and partial agonists for the mGluR5 receptor and may be useful for the treatment of various disorders of the central nervous system.
    Type: Application
    Filed: November 2, 2011
    Publication date: November 8, 2012
    Inventors: Andrew P. Degnan, Hong Huang, Lawrence B. Snyder, Fukang Yang, Kevin W. Gillman, Michael F. Parker
  • PYRAZOLIDIN-3-ONE DERIVATIVES
    Publication number: 20120277243
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein G, X, R1, R2, R3, R3?, R4, and R4? are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Application
    Filed: April 24, 2012
    Publication date: November 1, 2012
    Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Preparation of Aminopyrimidine Compounds
    Publication number: 20120277432
    Abstract: A 2-(N-methyl-N-methanesulfonylamino)pyrimidine compound of the formula (3): [R is a hydrocarbyl group], is prepared by the steps of: (I) reacting an isobutyrylacetate ester with 4-fluorobenzaldehyde and urea in the presence of a protonic compound and a metal salt; (II) oxidizing the reaction product of the step (I); (III) reacting the oxidation product of the step (II) with an organic sulfonyl halide or an organic sulfonyl anhydride; and (IV) reacting the reaction product of the step (III) with N-methyl-N-methanesulfonamide.
    Type: Application
    Filed: June 14, 2012
    Publication date: November 1, 2012
    Applicant: ASTRAZENECA UK LTD.
    Inventors: Akio Matsushita, Mizuho Oda, Yasuhiro Kawachi, Jun-ichi Chika
  • PYRIMIDINE AMIDE COMPOUNDS
    Publication number: 20120270875
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, asthma and COPD.
    Type: Application
    Filed: February 17, 2012
    Publication date: October 25, 2012
    Inventors: Paul Gillespie, Christophe Michoud, Kenneth Carey Rupert, Kshitij Chhabilbhai Thakkar, Lin Yi
  • METHOD FOR PRODUCING 2-(2-AMINOPYRIMIDIN-4-YL)-1H-INDOLE-5-CARBOXYLIC ACID DERIVATIVES
    Publication number: 20120271051
    Abstract: This disclosure relates to a novel process for obtaining a compound of formula I: wherein the values of R1, R2, and R3 and P are as described in the specification, and intermediates thereof.
    Type: Application
    Filed: July 3, 2012
    Publication date: October 25, 2012
    Applicant: SANOFI
    Inventors: Joachim GRAESER, Guenter BILLEN, Adolf LINKIES, Tobias METZENTHIN
  • 5-(4-(haloalkoxy)phenyl) pyrimidine-2-amine compounds and compositions as kinase inhibitors
    Patent number: 8293757
    Abstract: The invention provides compounds of formula (1) and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit, PDGFR?, PDGFR?, CSF1R, AbI, BCR-AbI, CSK, JNK1, JNK2, p38, p70S6K, TGF?, SRC, EGFR, trkB, FGFR3. Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2?, BRK, Fms, KDR, c-rapor b-raf kinases.
    Type: Grant
    Filed: August 19, 2008
    Date of Patent: October 23, 2012
    Assignee: IRM LLC
    Inventors: Valentina Molteni, Xiaolin Li, Xiaodong Liu, Donatella Chianelli, Juliet Nabakka, Jon Loren, Shuli You
  • AMINO-HETEROARYL DERIVATIVES AS HCN BLOCKERS
    Publication number: 20120264728
    Abstract: The invention relates to amino-heteroaryl derivatives having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.
    Type: Application
    Filed: December 20, 2010
    Publication date: October 18, 2012
    Inventors: Simon James Anthony Grove, Angus John Morrison, Craig Jamieson, Ronald Palin, John Kinnaird Ferguson Maclean
  • 2-heteroarylamino-pyrimidine derivatives as kinase inhibitors
    Patent number: 8288540
    Abstract: The invention provides compounds of Formula (I) and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit, PDGFR?, PDGFR?, CSF1R, Abl, BCR-Abl, CSK, JNK1, JNK2, p38, p70S6K, TGF?, SRC, EGFR, trkB, FGFR3, Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2?, BRK, Fms, KDR, c-raf or b-raf kinases.
    Type: Grant
    Filed: August 18, 2008
    Date of Patent: October 16, 2012
    Assignee: IRM LLC
    Inventors: Donatella Chianelli, Valentina Molteni, Xiaolin Li, Xiaodong Liu, Juliet Nabakka, Jon Loren
  • Amino-Derivatives As Novel Inhibitors Of Histone Deacetylase
    Publication number: 20120252790
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Application
    Filed: May 15, 2012
    Publication date: October 4, 2012
    Inventors: Patrick René Angibaud, Kristof Van Emelen, Virginie Sophie Poncelet, Bruno Roux
  • INHIBITORS OF SPHINGOSINE KINASE
    Publication number: 20120252789
    Abstract: The present invention relates to compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, M1, M2, M3, M4, Y1, Y2, V, W, n, m and o have the meanings given in Claim 1, and physiologically acceptable salts, derivatives, prodrugs, solvates, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, for use in the treatment of diseases which are influenced by inhibition of Sph kinase 1.
    Type: Application
    Filed: November 22, 2010
    Publication date: October 4, 2012
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Frank Stieber, Dirk Wienke
  • SUBSTITUTED 3-HETEROAROYLAMINO-PROPIONIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS
    Publication number: 20120252809
    Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, L, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: January 24, 2012
    Publication date: October 4, 2012
    Applicant: SANOFI
    Inventors: Sven RUF, Thorsten SADOWSKI, Klaus WIRTH, Herman SCHREUDER, Christian BUNING
  • (1, 1, 1,3,3,3 -HEXAFLUORO-2 HYDROXYPROPAN- 2 -YL) PHENYL DERIVATIVE, PHARMACEUTICAL COMPOSITIONS THEREOF AND THEIR USE FOR THE TREATMENT OF ATHEROSCLEROSIS
    Publication number: 20120238574
    Abstract: The present invention relates to (1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl derivatives having the general formula (I) to pharmaceutical compositions comprising the same and to the use of these (1,1,1,3,3,3-hexafluoro-2-hydroxy-propan-2-yl)phenyl derivatives in the treatment of atherosclerosis.
    Type: Application
    Filed: October 26, 2010
    Publication date: September 20, 2012
    Applicant: N.V. ORGANON
    Inventors: Andrew John Cooke, Emma Louise Carswell, David Jonathan Bennett
  • AMINO-PYRIMIDINE COMPOUNDS AS INHIBITORS OF IKK EPSILON AND/OR TBK1
    Publication number: 20120238540
    Abstract: The invention relates to certain amino-pyrimidine compounds that inhibit IKK epsilon and/or TBK1, methods of making such compounds, pharmaceutical compositions comprising such compounds, and the use of these compounds in treating a variety of diseases and disorders.
    Type: Application
    Filed: April 12, 2012
    Publication date: September 20, 2012
    Applicant: Myrexis, Inc.
    Inventors: Ryan C. HOLCOMB, Kazuyuki Suzuki, Robert J. Halter, Paul R. Sebahar, Donald A. McLeod, Mark D. Shenderovich, Kraig M. Yager, Matthew Gregory Bursavich, Ashantai J. Yungai, Burt Richards, Paul L. Bartel, Daniel A. Wettstein
  • 2-(amino-substituted)-4-aryl pyrimidines and related compounds useful for treating inflammatory diseases
    Patent number: 8268822
    Abstract: A heterocyclic inhibitor having the formula I, with the variables defined herein, which is useful for treating inflammatory and other physiological disorders in which PKC-theta isoform plays a role:
    Type: Grant
    Filed: April 26, 2010
    Date of Patent: September 18, 2012
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Paul E. Fleming, Zhan Shi, Brendan Shaowu Chen, Jane F. Schmidt, John C. Reader, Neal D. Hone, Jeffrey P. Ciavarri
  • HETEROARYL BENZAMIDES, COMPOSITIONS AND METHODS OF USE
    Publication number: 20120225862
    Abstract: Provided are certain heteroaryl benzamides, compositions, and methods of their manufacture and use.
    Type: Application
    Filed: July 21, 2010
    Publication date: September 6, 2012
    Applicants: AUCKLAND UNIVSERVICES LIMITED, THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY
    Inventors: Patrick D. Sutphin, Denise A. Chan, Sandra Turcotte, William Alexander Denny, Michael Patrick Hay, Anna Claire Giddens, Muriel Marie Bonnet, Amato J. Giaccia
  • New compounds, pharmaceutical compositions and uses thereof
    Publication number: 20120214782
    Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Application
    Filed: August 17, 2011
    Publication date: August 23, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Gerald Juergen ROTH, Martin FLECK, Heike NEUBAUER, Bernd NOSSE
  • DIAZABICYCLIC CENTRAL NERVOUS SYSTEM ACTIVE AGENTS
    Publication number: 20120208820
    Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.
    Type: Application
    Filed: January 31, 2012
    Publication date: August 16, 2012
    Inventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
  • Ion channel modulators and methods of uses
    Patent number: 8236815
    Abstract: The invention relates to ion channel modulators of formula Ia, pharmaceutical compositions thereof, and to methods of treating diseases using such compounds where activation or hyperactivity of calcium and/or sodium ion channels is implicated in the disease state.
    Type: Grant
    Filed: March 15, 2010
    Date of Patent: August 7, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Esther Martinborough, Nicole Zimmermann, Robert B. Perni, Michael Arnost, Upul Bandarage, Francois Maltais, Guy Bemis
  • Reverse Amide Compounds As Protein Deacetylase Inhibitors And Methods Of Use Thereof
    Publication number: 20120190693
    Abstract: The present invention relates to novel “reverse amide” compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.
    Type: Application
    Filed: April 2, 2012
    Publication date: July 26, 2012
    Inventors: John H. van Duzer, Ralph Mazitschek, Walter Ogier, James E. Bradner, Guoxiang Huang, Dejian Xie, Nan Yu
  • Pyrrolidine-1,2-dicarboxamide derivatives
    Patent number: 8227462
    Abstract: The present invention relates to a compound of formula (I) or a salt thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.
    Type: Grant
    Filed: September 10, 2009
    Date of Patent: July 24, 2012
    Assignee: Novartis AG
    Inventors: Robin Alec Fairhurst, Vito Guagnano, Patricia Imbach, Giorgio Caravatti, Pascal Furet
  • Sulfonylamino-Derivatives As Novel Inhibitors Of Histone Deacetylase
    Publication number: 20120178741
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, R5, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Application
    Filed: March 21, 2012
    Publication date: July 12, 2012
    Applicant: JANSSEN PHARMACEUTICA N.V.
    Inventors: Kristof Van Emelen, Leo Jacobus Jozel Backx, Sven Franciscus Anna Van Brandt, Patrick René Angibaud, Isabelle Noélle Constance Pilatte, Marc Gustaaf Celine Verdonck, Hans Louis Jos De Winter, Jimmy Arnold Viviane Van heusden
  • BIPIPERIDINYL COMPOUNDS, COMPOSITIONS, CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
    Publication number: 20120178681
    Abstract: Bipiperidinyl compounds of the formula I, are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
    Type: Application
    Filed: March 21, 2012
    Publication date: July 12, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: HAROLD B. WOOD, Alan D. Adams, Stanley Freeman, Jason W. Szewczyk, Conrad Santini, Yong Huang