The Additional Hetero Ring Is Six-membered And Contains Nitrogen Patents (Class 540/597)
  • Patent number: 10370375
    Abstract: The invention relates to a compound of formula (I) wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful as therapeutic agent for organ transplants, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis. Type I diabetes and complications from diabetes, cancer, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, inflammatory bowel diseases, Crohn's disease, Alzheimer's disease, leukemia, osteoarthritis, control of pruritus, chronic respiratory disease or keratoconjunctivitis in mammals.
    Type: Grant
    Filed: August 6, 2018
    Date of Patent: August 6, 2019
    Assignee: Elanco Tiergesundheit AG
    Inventors: Noelle Gauvry, Chouaib Tahtaoui, Pascal Furet, Pierre Ducray
  • Patent number: 10059709
    Abstract: The invention relates to a compound of formula (I) wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful as therapeutic agent for organ transplants, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, Type I diabetes and complications from diabetes, cancer, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, inflammatory bowel diseases, Crohn's disease, Alzheimer's disease, leukemia, osteoarthritis, control of pruritus, chronic respiratory disease or keratoconjunctivitis in mammals.
    Type: Grant
    Filed: March 25, 2015
    Date of Patent: August 28, 2018
    Assignee: Elanco Tiergesundheit AG
    Inventors: Noelle Gauvry, Chouaib Tahtaoui, Pascal Furet, Pierre Ducray
  • Patent number: 9522903
    Abstract: Multifunctional nitroxide derivatives comprising a potassium channel opener and a reactive oxygen species (ROS) degradation catalyst that can act as an anti-oxidant, as well as pharmaceutical compositions comprising them are provided. The multifunctional compounds and pharmaceutical compositions are useful for treatment of diseases, disorders or conditions associated with oxidative stress or endothelial dysfunction.
    Type: Grant
    Filed: July 31, 2015
    Date of Patent: December 20, 2016
    Assignee: Radikal Therapeutics Inc.
    Inventors: Prakash Jagtap, Andrew Lurie Salzman
  • Publication number: 20150141409
    Abstract: Disclosed are a novel rebamipide prodrug, a method for preparing the same, and use thereof. Also, a pharmaceutical composition comprising the novel rebamipide prodrug as an active ingredient is provided. The rebamipide prodrug is increased 25-fold in absorption rate compared to rebamipide itself, and can be applied to the prophylaxis or therapy of gastric ulcer, acute gastritis, chronic gastritis, xerophthalmia, cancer, osteoarthritis, rheumatoid arthritis, or obesity.
    Type: Application
    Filed: June 26, 2013
    Publication date: May 21, 2015
    Inventors: Eui Hwan Cho, Sung Ju Choi, Sung Woo Lee, Hee Jong Shin, Ho Seok Kwon, Jae Woong Lee, Jeong Ho Joo, Hyun Tae Kim, Woo Heon Song, Jong Bae Yoon, Ki Seok Park, Ho Joon Park, Ho Tae Nam
  • 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
  • Publication number: 20150111734
    Abstract: A pesticidal composition comprises at least one compounds selected from a compound of formula, or any agriculturally acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, Q, Z, L, La, and x are as described herein. A method of controlling pests comprises applying the pesticidal composition near a population of pests.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Inventors: Yu Zhang, Asako Kubota, Noormohamed M. Niyaz, Thomas Barton, Tony K. Trullinger, Christian T. Lowe, Paul R. LePlae, Ann M. Buysse, Martin J. Walsh, Negar Garizi, Ricky Hunter, Daniel Knueppel
  • Publication number: 20150105370
    Abstract: Embodiments of the disclosure relate to selectively substituted quinoline compounds that act as antagonists or inhibitors for Toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritis.
    Type: Application
    Filed: October 14, 2014
    Publication date: April 16, 2015
    Inventors: ERIC CARLSON, HANS HANSEN, LYNN HAWKINS, SALLY ISHIZAKA, MATTHEW MACKEY, SHAWN SCHILLER, CHIKAKO OGAWA, HEATHER DAVIS
  • Patent number: 8999975
    Abstract: The present invention is directed to compounds of Formula I: wherein R1, R2 and n are described herein. These compounds and their pharmaceutically acceptable salts thereof are inhibitors of Cathepsin C.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: April 7, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Marc Grundl, Thorsten Oost, Alexander Pautsch, Stefan Peters, Doris Riether, Wolfgang Wienen
  • Patent number: 8987249
    Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: March 24, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Ralf Anderskewitz, Florian Binder, Matthias Grauert, Marc Grundl, Peter Wilhelm Haebel, Thorsten Oost, Alexander Pautsch, Stefan Peters, Viktor Vintonyak
  • Patent number: 8981085
    Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, 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: Grant
    Filed: May 6, 2014
    Date of Patent: March 17, 2015
    Assignee: Array BioPharma Inc.
    Inventors: Yvan Le Huerou, James F. Blake, Indrani W. Gunawardana, Peter J. Mohr, Eli M. Wallace, Bin Wang, Mark Joseph Chicarelli, Michael Lyon
  • Publication number: 20150065478
    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: November 11, 2014
    Publication date: March 5, 2015
    Inventors: Patrick Rene Angibaud, Kristof Van Emelen, Virginie Sophie Poncelet, Bruno Roux
  • Publication number: 20150065490
    Abstract: Compounds of formula I in free or salt or solvate form, wherein X has the meaning indicated in the specification, are useful for treating conditions that are prevented or alleviated by activation of the ?2-adrenoreceptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Application
    Filed: November 6, 2014
    Publication date: March 5, 2015
    Applicant: NOVARTIS AG
    Inventors: Bernard CUENOUD, Robin Alec FAIRHURST, Roger John TAYLOR, David BEATTIE
  • Publication number: 20150057268
    Abstract: Neuropeptide S receptor antagonists are provided that bind in functional assays to neuropeptide S receptors; methods are provided for use of these antagonists in treatment of conditions or disease states that are ameliorated by blocking of the neuropeptide S receptor, including substance abuse and substance abuse relapse; and for use of neuropeptide S receptor antagonists in the manufacture of therapeutics and pro-drugs for therapeutics useful in disease states and conditions sensitive to binding of the neuropeptide S receptor.
    Type: Application
    Filed: December 6, 2012
    Publication date: February 26, 2015
    Applicant: RESEARCH TRIANGLE INSTITUTE
    Inventors: Scott Runyon, Yanan Zhang, Carla Hassler, Brian Gilmour
  • Publication number: 20150057265
    Abstract: The present disclosure describes furo- and thieno-pyridine carboxamide compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
    Type: Application
    Filed: August 22, 2014
    Publication date: February 26, 2015
    Applicant: INCYTE CORPORATION
    Inventors: Yun-Long Li, David M. Burns, Hao Feng, Taisheng Huang, Song Mei, Jun Pan, Oleg Vechorkin, Hai-Fen Ye, Wenyu Zhu, Maria Rafalski, Anlai Wang, Chu-Biao Xue
  • Publication number: 20150051194
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 19, 2015
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. WENTLAND
  • Patent number: 8952004
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R3, A, B, X, and n 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: Grant
    Filed: January 5, 2011
    Date of Patent: February 10, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: John David Ginn, Ronald John Sorcek, Michael Robert Turner, Di Wu, Frank Wu
  • Publication number: 20150031675
    Abstract: The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).
    Type: Application
    Filed: January 31, 2013
    Publication date: January 29, 2015
    Inventors: Jon-Paul Strachan, Daniel Yohannes
  • Publication number: 20150031678
    Abstract: The present invention relates to new substituted pyrazolo[1,5-a]pyridine having a great affinity for sigma receptors, especially sigma-1 receptor, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.
    Type: Application
    Filed: February 21, 2013
    Publication date: January 29, 2015
    Applicant: LABORATORIES DEL DR. ESTEVE S.A.
    Inventors: José Luis Diaz Fernández, Ma Rosa Cuberes Altisent
  • Publication number: 20150023990
    Abstract: Imidazoquinoline compounds with an alkoxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral, and neoplastic, are disclosed.
    Type: Application
    Filed: September 30, 2014
    Publication date: January 22, 2015
    Inventors: Kyle J. Lindstrom, Bryon A. Merrill, Chad A. Haraldson, Michael J. Rice, Tushar A. Kshirsagar, Philip D. Heppner, Joshua R. Wurst, Shri Niwas, Sarah J. Slania
  • Publication number: 20150025056
    Abstract: The present invention provides compounds of the formula I: its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof, solvates thereof, metabolites thereof, and pharmaceutically acceptable salts, wherein the ring A substituent groups are fully defined in the following disclosure. The compounds of formula I are inhibitors of metalloproteases such as matrix metalloproteases and sheddases, and are useful in treating diseases such as rheumatoid arthritis, psoriasis, neoplastic diseases, allergies and all those diseases wherein inhibition of MMPs is desirable.
    Type: Application
    Filed: October 3, 2014
    Publication date: January 22, 2015
    Applicant: Incyte Corporation
    Inventors: Yun-Long Li, Jincong Zhuo, David M. Burns, Wenqing Yao, Ravi Kumar Jalluri
  • Publication number: 20150025235
    Abstract: Benzamide compounds and derivatives thereof, as can be used for selective inhibition of the SIRT2 enzyme and/or therapeutic use in the treatment of Huntington's disease.
    Type: Application
    Filed: May 30, 2014
    Publication date: January 22, 2015
    Inventors: Richard B. Silverman, Hua Wang, Mohammad Khanfar, Aleksey G. Kazantsev
  • Patent number: 8937062
    Abstract: Compositions comprise a fluoroquinolone having Formulae I-VIII for treating, reducing, ameliorating, or preventing infections caused by some bacteria that are resistant to an antibacterial drug. Methods for treating, reducing, ameliorating, or preventing such infections use such compositions.
    Type: Grant
    Filed: March 19, 2008
    Date of Patent: January 20, 2015
    Assignee: Bausch & Lomb Incorporated
    Inventors: Praveen Tyle, Pramod Kumar Gupta, Susan E. Norton, Lynne Brunner, Joseph Blondeau
  • Publication number: 20150018342
    Abstract: The present invention relates to fused pyrroledicarboxamides of the formula (I), in which R1 to R9, X, m and n are as defined in the claims. The compounds of the formula (I) are inhibitors of the acid-sensitive potassium channel TASK-1 and suitable for the treatment of TASK-1 channel-mediated diseases such as arrhythmias, in particular atrial arrhythmias like atrial fibrillation or atrial flutter, and respiratory disorders, in particular sleep-related respiratory disorders like sleep apnea, for example.
    Type: Application
    Filed: February 1, 2013
    Publication date: January 15, 2015
    Applicant: SANOFI
    Inventors: Laurent Bialy, Katrin Lorenz, Klaus Wirth, Klaus Steinmeyer, Gerhard Hessler
  • Publication number: 20150005280
    Abstract: The present application relates to a series of substituted pyrazolo[1,5-a]pyridine compounds, their use as tropomyosin receptor kinase (Trk) family protein kinase inhibitors, method of making and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: December 12, 2012
    Publication date: January 1, 2015
    Applicant: DR. REDDY'S LABORATORIES LTD.
    Inventors: Pradip Kumar Sasmal, Shahadat Ahmed, Ganesh Prabhu, Ashok Tehim, Vidyadhar Paradkar, Marahanakuli Prasanna Dattatreya, Nanjegowda Jagadeesh Mavinahalli
  • Publication number: 20140357599
    Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.
    Type: Application
    Filed: August 18, 2014
    Publication date: December 4, 2014
    Inventors: Mette Knak CHRISTENSEN, Fredrik BJORKLING
  • Publication number: 20140343015
    Abstract: A morphinan derivative represented by the following general formula (I) (in the formula, R1 represents hydrogen, C1-6 alkyl, cycloalkylalkyl (the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms), aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like, R2 represents hydrogen, C1-6 alkyl, C3-6 cycloalkyl, C6-10 aryl, aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like, R3, R4 and R5 represent hydrogen, hydroxy, carbamoyl, C1-6 alkoxy, C6-10 aryloxy and the like, R6a, R6b, R7, R8, R9, and R10 represent hydrogen and the like, X represents O or CH2, and Y represents C?O, SO2, an atomic bond and the like), or an acid addition salt thereof is used as an analgesic.
    Type: Application
    Filed: September 7, 2012
    Publication date: November 20, 2014
    Applicants: NIPPON CHEMIPHAR CO., LTD., THE KITASATO INSTITUTE
    Inventors: Hiroshi Nagase, Hideaki Fujii, Eriko Nakata, Yoshikazu Watanabe, Toshihiro Takahashi
  • Publication number: 20140329803
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula I, where n is 1 or 2; p is 0, 1 or 2; q is 0, 1 or 2; and R1-R6 are as defined herein.
    Type: Application
    Filed: November 16, 2012
    Publication date: November 6, 2014
    Inventors: Miles Congreve, Giles Brown, Julie Cansfield, Benjamin Tehan
  • Patent number: 8877743
    Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; and R1 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.
    Type: Grant
    Filed: June 14, 2013
    Date of Patent: November 4, 2014
    Assignee: Naeja Pharmaceutical Inc.
    Inventors: Samarendra N. Maiti, Dai Nguyen, Jehangir Khan, Rong Ling
  • Publication number: 20140323470
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: wherein R2, W, A, Y and R1 are as defined in the specification, are p38 MAPK inhibitors, and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
    Type: Application
    Filed: July 14, 2014
    Publication date: October 30, 2014
    Applicant: CHIESI FARMACEUTICI S.p.A.
    Inventors: Monique Bodil VAN NIEL, Nicholas Charles Ray, Lilian Alcaraz, Terry Aaron Panchal, Andrew Stephen Robert Jennings, Elisabetta Armani, Andrew Peter Cridland, Christopher Hurley
  • Publication number: 20140296515
    Abstract: The present application relates to novel 6-alkylamino-substituted dicyanopyridines, to their amino acid ester prodrugs, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.
    Type: Application
    Filed: June 17, 2014
    Publication date: October 2, 2014
    Inventors: Alexandros VAKALOPOULOS, Daniel MEIBOM, Barbara ALBRECHT-KÜPPER, Katja ZIMMERMANN, Jörg KELDENICH, Hans-Georg LERCHEN, Peter NELL, Frank SÜßMEIER, Ursula KRENZ
  • Patent number: 8841290
    Abstract: Disclosed is a tetrahydronapthalene compound having Formula I the variables of which are as described herein, methods of preparing same and their use.
    Type: Grant
    Filed: February 12, 2010
    Date of Patent: September 23, 2014
    Assignee: Sanofi
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Klaus Wirth
  • Patent number: 8835648
    Abstract: Heterocyclic compounds that modulate the hedgehog signaling pathway, pharmaceutical composition thereof and their therapeutic applications.
    Type: Grant
    Filed: June 9, 2010
    Date of Patent: September 16, 2014
    Assignee: Siena Biotech S.p.A.
    Inventors: J. Russell Thomas, Gal.la Pericot Mohr, Chiara Caramelli, Giacomo Minetto, Marta Bellini
  • Publication number: 20140256713
    Abstract: The present invention features compounds that are HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
    Type: Application
    Filed: February 21, 2014
    Publication date: September 11, 2014
    Applicants: Shionogi & Co., Ltd., ViiV Healthcare Company
    Inventors: Brian Alvin JOHNS, Eric Eugene BOROS, Takashi KAWASUJI, Cecilia S. KOBLE, Noriyuki KUROSE, Hitoshi MURAI, Ronald George SHERRILL, Jason Gordon WEATHERHEAD
  • Publication number: 20140249135
    Abstract: New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
    Type: Application
    Filed: May 9, 2014
    Publication date: September 4, 2014
    Applicant: NOVARTIS AG
    Inventors: Matthew Burger, Mika Lindvall, Wooseok Han, Jiong Lan, Gisele Nishiguchi, Cynthia Shafer, Cornelia Bellamacina, Kay Huh, Gordana Atallah, Christopher McBride, William Antonios-McCrea, JR., Tatiana Zavorotinskaya, Annette Walter, Pablo Dominguez Garcia
  • Patent number: 8822448
    Abstract: The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, bladder/urethral diseases, and the like, and thus, have found that a pyrazoloquinoline compound has a PDE9-inhibiting action, thereby completing the present invention.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: September 2, 2014
    Assignee: Astellas Pharma Inc.
    Inventors: Hiroyuki Kaizawa, Hirofumi Yamamoto, Kazunori Kamijo, Mari Sugita, Ryushi Seo, Satoshi Yamamoto, Atsushi Ukai
  • Publication number: 20140243520
    Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, 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: May 6, 2014
    Publication date: August 28, 2014
    Applicant: Array BioPharma Inc.
    Inventors: Yvan Le Huerou, James F. Blake, Indrani W. Gunawardana, Peter J. Mohr, Eli M. Wallace, Bin Wang, Mark Joseph Chicarelli, Michael Lyon
  • Publication number: 20140235609
    Abstract: The invention relates to compound of the formula I (I) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation and to medicaments comprising it for treating diseases connected to tehinhibition of H3 receptor.
    Type: Application
    Filed: October 8, 2012
    Publication date: August 21, 2014
    Inventors: Tie-Lin Wang, Xuechun Zhang
  • Publication number: 20140234939
    Abstract: Benzamide compounds and derivatives thereof, as can be used for selective inhibition of the SIRT2 enzyme and/or therapeutic use in the treatment of Huntington's disease.
    Type: Application
    Filed: December 23, 2013
    Publication date: August 21, 2014
    Applicant: Northwestern University
    Inventors: Richard B. Silverman, Hua Wang, Mohammad Khanfar
  • Patent number: 8796257
    Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; Y is OR1 or NR2R3, and R1, R2, R3 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: August 5, 2014
    Assignee: Naeja Pharmaceutical Inc.
    Inventors: Samarendra N. Maiti, Dai Nguyen, Jehangir Khan, Rong Ling
  • Patent number: 8772478
    Abstract: Benzenesulfonamide compounds having a structure of the following general formula (I) are described. Also described, are methods for synthesizing the compounds, and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.
    Type: Grant
    Filed: June 28, 2010
    Date of Patent: July 8, 2014
    Assignee: Galderma Research & Development
    Inventors: Laurence Clary, Sandrine Chambon, Laurent Chantalat, Pascale Mauvais, Olivier Roye, Marlène Schuppli
  • Publication number: 20140187539
    Abstract: Heteroaryloxy-substituted benzoic acid amides of general formula I wherein the groups R1 to R7 as well as X and Y are defined according to claim 1, including the tautomers, the stereoisomers, the mixtures and the salts thereof. The compounds according to the invention are suitable for the treatment of respiratory complaints, particularly COPD and asthma.
    Type: Application
    Filed: March 4, 2014
    Publication date: July 3, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Holger WAGNER, Elke LANGKOPF, Frank HIMMELSBACH, Rolf GOEGGEL, Birgit JUNG
  • Publication number: 20140179686
    Abstract: The present invention relates to novel vanilloid receptor ligands, to a process for the production thereof, to pharmaceutical preparations containing these compounds and to the use of these compounds for the production of pharmaceutical preparations.
    Type: Application
    Filed: February 25, 2014
    Publication date: June 26, 2014
    Applicant: Gruenenthal GmbH
    Inventors: Jeewoo LEE, Hyung Chul Ryu, Robert FRANK, Gregor BAHRENBERG, Jean DE VRY, Thomas CHRISTOPH, Derek John SAUNDERS, Klaus SCHIENE, Bernd SUNDERMANN
  • Publication number: 20140179672
    Abstract: The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: November 1, 2013
    Publication date: June 26, 2014
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Alexandros VAKALOPOULOS, Markus FOLLMANN, Ingo HARTUNG, Philipp BUCHGRABER, Rolf JAUTELAT, Jorma HAßFELD, Niels LINDNER, Alexey GROMOV, Frank WUNDER, Johannes-Peter STASCH, Gorden REDLICH, Volkhart Min-Jian LI, Eva Maria BECKER-PELSTER, Andreas KNORR
  • Publication number: 20140171418
    Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
    Type: Application
    Filed: August 10, 2012
    Publication date: June 19, 2014
    Inventors: Jerôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans
  • Publication number: 20140171407
    Abstract: The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
    Type: Application
    Filed: February 17, 2014
    Publication date: June 19, 2014
    Applicant: Genentech, Inc.
    Inventors: Hazel Joan Dyke, Lewis Gazzard, Karen Williams, Huifen Chen, Samuel Kintz, Joy Drobnick, Joseph P. Lyssikatos, Simon Goodacre, Calum Macleod, Charles Ellwood
  • Publication number: 20140155387
    Abstract: The present invention refers to: a compound having the general formula (I), wherein n is 0, 1, 2 or; m is 0, 1, 2 or 3; o is 0, 1, 2 or 3; W, X, Y and Z are independently selected from CH, N or N-oxide; A is NR4, C?O, C?S, OP(O)(O), P?O, CH2, or a heteroarly selected from the group consisting of (a), (b), (c), (d), (e), (f), (g); V is C?O, O, S, CH2, or NR5; as well as its use in treating inflammatory diseases such as asthma, COPD, inflammation post infection, arthritis, atherosclerosis, pain and dermatitis.
    Type: Application
    Filed: April 20, 2012
    Publication date: June 5, 2014
    Applicants: QURIENT, CO. LTD., INSTITUT PASTEUR KOREA
    Inventors: Zaesung No, Jaeseung Kim, Sung-Jun Han, Jung Hwan Kim, Young Sam Park, Sangchul Lee, Kiyean Nam, Jeongjun Kim, Jinhwa Lee, Sunhee Kang, Min Jung Seo, Saeyeon Lee, Gahee Choi
  • Patent number: 8729081
    Abstract: The present invention provides compounds which antagonize epsilon protein kinase C (PKC?). These compounds have a structural formula (Ia), (Ic) or (II). The present invention also provides pharmaceutical compositions containing these compounds and methods of treating various diseases, conditions, and/or symptoms by using these compounds.
    Type: Grant
    Filed: October 12, 2009
    Date of Patent: May 20, 2014
    Assignee: VM Discovery Inc.
    Inventor: Jay Jie-Qiang Wu
  • Publication number: 20140128376
    Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is a thiazolyl, picolinyl, 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: January 13, 2014
    Publication date: May 8, 2014
    Applicant: Genentech, Inc.
    Inventor: Xiaojing Wang
  • Publication number: 20140113890
    Abstract: The invention provides 4-amino-4-oxobutanoyl peptides of Formula I and the pharmaceutically salts and hydrates thereof. The variables R, R1, R6-R8, R16, R18, R19, M, n, T, Y, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. The 4-amino-4-oxobutanoyl peptides disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptides and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptides as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptides and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections.
    Type: Application
    Filed: December 23, 2013
    Publication date: April 24, 2014
    Applicant: ACHILLION PHARMACEUTICALS, INC.
    Inventors: Avinash Phadke, Dawei Chen, Venkat Gadhachanda, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Atul Agarwal, Ha Young Kim, Shuoming Li, Cuixian Liu, Suoming Zhang, Milind Deshpande
  • Patent number: 8703934
    Abstract: The present application relates to novel substituted 4-amino-3,5-dicyano-2-thiopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of hypertension and other cardiovascular disorders.
    Type: Grant
    Filed: November 17, 2007
    Date of Patent: April 22, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Peter Nell, Nicole Diedrichs, Barbara Albrecht-Küpper, Alexandros Vakalopoulos, Frank Süβmeier, Joerg Keldenich