Chalcogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/141)
  • Patent number: 10308610
    Abstract: The present invention relates to compounds which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
    Type: Grant
    Filed: December 13, 2017
    Date of Patent: June 4, 2019
    Assignees: ABBVIE DEUTSCHLAND GMBH & CO. KG, ABBVIE INC.
    Inventors: Hervé Geneste, Michael Ochse, Karla Drescher, Jürgen Dinges, Clarissa Jakob
  • Patent number: 9969705
    Abstract: A fused heterocyclic compound having an enteropeptidase inhibitory action and use of the compound as a medicament for treatment or prophylaxis of obesity, diabetes mellitus, etc., are provided. Specifically, a compound represented by the following formula (I): wherein each symbol is as defined herein, or a salt thereof and use of the compound as a medicament for treatment or prophylaxis of obesity, diabetes mellitus, etc., are provided.
    Type: Grant
    Filed: February 12, 2015
    Date of Patent: May 15, 2018
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Minoru Sasaki, Keiko Kakegawa, Fumiaki Kikuchi, Zenichi Ikeda, Yoichi Nishikawa
  • Patent number: 9687483
    Abstract: Provided are methods of treating a cerebral cavernous malformation (CCM) and methods of treating cerebral aneurysm in a mammal with certain Rho kinase inhibitors.
    Type: Grant
    Filed: January 26, 2016
    Date of Patent: June 27, 2017
    Assignee: BIOAXONE BIOSCIENCES, INC.
    Inventors: Lisa McKerracher, Lisa M. Bond
  • Patent number: 9040515
    Abstract: This invention relates to compounds of general formula (I) in which R1, R2, U, V, L, M, R5, m, X, Y and Z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.
    Type: Grant
    Filed: December 18, 2013
    Date of Patent: May 26, 2015
    Assignee: Pfizer Inc.
    Inventors: Martin Paul Edwards, Robert Arnold Kumpf, Pei-Pei Kung, Indrawan James McAlpine, Sacha Ninkovic, Eugene Yuanjin Rui, Scott Channing Sutton, John Howard Tatlock, Martin James Wythes, Luke Raymond Zehnder
  • Publication number: 20150141410
    Abstract: Chemical compounds are provided which act on GPR17 receptors and are useful in the treatment or amelioration of chronic and/or acute neurodegenerative diseases, such as multiple sclerosis, inflammatory diseases, pathologies involving the immune system, cardiovascular diseases, and renal diseases.
    Type: Application
    Filed: May 9, 2012
    Publication date: May 21, 2015
    Applicants: UNIVERSITA' DEGLI STUDI DI MILANO, FONDAZIONE ITALIANA SCLEROSI MULTIPLA - FISH ONLUS
    Inventors: Maria Pia Abbracchio, Mario Alberto Battaglia, Ivano Eberini, Marta Fumagalli, Chiara Parravicini, Cristina Sensi, Paola Zaratin
  • Publication number: 20150141424
    Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.
    Type: Application
    Filed: January 12, 2015
    Publication date: May 21, 2015
    Inventors: Qingping ZENG, Andras TORO, John Bruce PATTERSON, Warren Stanfield WADE, Zoltan ZUBOVICS, Yun YANG, Zhipeng WU
  • Patent number: 9034900
    Abstract: The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease.
    Type: Grant
    Filed: October 17, 2014
    Date of Patent: May 19, 2015
    Assignee: Quanticel Pharmaceuticals, Inc.
    Inventors: Michael John Bennett, Juan Manuel Betancort, Amogh Boloor, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal
  • Publication number: 20150126493
    Abstract: The invention provides bicyclic sulfone compounds, pharmaceutical compositions, methods of inhibiting RORy activity, reducing the amount of iL-17 in a subject, and treating immune disorders and inflammatory disorders using such bicyclic sulfone compounds. Another aspect of the invention provides a method of treating a subject suffering from a medical disorder. The method comprises administering to the subject a therapeutically effective amount of one or more bicyclic sulfone compounds described herein. In certain other embodiments, the disorder is rheumatoid arthritis.
    Type: Application
    Filed: May 3, 2013
    Publication date: May 7, 2015
    Inventors: Thomas D. Aicher, Kenneth J. Barr, Vladimir Simov, Willam D. Thomas, Peter L. Toogood, Chad A. Van Huis
  • Publication number: 20150111885
    Abstract: The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Inventors: Michael John Bennett, Juan Manuel Betancort, Amogh Boloor, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal
  • Publication number: 20150111747
    Abstract: 6-Pyridone-2-carbamoylazoles of the general formula (I) are described as herbicides. In this formula (I), W, X and Z represent radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q represents a 5-membered radical such as oxadiazyl.
    Type: Application
    Filed: April 30, 2013
    Publication date: April 23, 2015
    Inventors: Ralf Braun, Stefan Lehr, Arnim Koehn, Hansjoerg Dietrich, Elmar Gatzweiler, Christopher Hugh Rosinger, Dirk Schmutzler
  • Publication number: 20150105385
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Inventors: Alfredo C. CASTRO, Katrina CHAN, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Liansheng LI, Tao LIU, Yi LIU, Pingda REN, Daniel A. SNYDER, Martin R. TREMBLAY
  • Publication number: 20150099732
    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted-2H-isoquinolin-1-one compounds that, inter alia, inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.) and/or Wnt signalling. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to inhibit Wnt signalling; to treat disorders that are ameliorated by the inhibition of PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to treat disorders that are ameliorated by the inhibition of Wnt signalling; to treat proliferative conditions such as cancer, etc.
    Type: Application
    Filed: March 7, 2013
    Publication date: April 9, 2015
    Inventors: Alan Ashworth, Christopher James Lord, Richard James Rowland Elliot, Dan Niculescu-Duvaz, Roderick Porter, Raymond John Boffey, Melanie Jayne Bayford, Stuart Firth-Clark, Ashley Nicholas Jarvis, Trevor Robert Perrior, Rebekah Elisabeth Key
  • Patent number: 8993593
    Abstract: This invention provides a compound of formula A The compound provided herein can affect the opening of, or otherwise modulate, voltage-gated potassium channels. The compound provided herein is useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.
    Type: Grant
    Filed: February 1, 2010
    Date of Patent: March 31, 2015
    Assignee: Valeant Pharmaceuticals International
    Inventors: Jean-Michel Vernier, Martha Alicia De La Rosa, Huanming Chen, Jim Zhen Wu, Gary Lee Larson, Ian Wayne Cheney
  • Patent number: 8957087
    Abstract: This present invention discloses a heterocyclic substituted acardite derivate and application thereof, namely compounds in the general formula (1) or the general formula (2) or pharmaceutically acceptable salts thereof, wherein A is monosubstituted or polysubstituted quinoline, isoquinoline, quinazoline, pyrrole or pyrimidine, and the substituent is halogen, C1-5alkyl, C1-5haloalkyl, C1-5alkoxy, C1-5haloalkoxy, C1-5alkylamino, C1-5haloalkylamino, amino or nitryl; R1 is C1-5alkyl; R2 is one or more selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy; and R3 is one or more selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy. The compound of the present invention and the pharmaceutically acceptable salt thereof can be used for treating tumor or leukemia.
    Type: Grant
    Filed: May 4, 2010
    Date of Patent: February 17, 2015
    Assignees: Jiangsu Provincial Institute of Materia Medica Co., Ltd., Nanjing Luyesike Pharmaceutical Co., Ltd.
    Inventors: Aihua Zhang, Shengtao Yuan, Guang Cheng, Yipeng Shen, Ancheng Ji
  • Patent number: 8957075
    Abstract: The present invention provides inhibitors of O-GIcNAc transferase. Typically, the inhibitors are quinolinone-6-sulfonamides. The invention also provides pharmaceutical compositions thereof and methods for using the same in diabetes and complications thereof, neurodegenerative diseases, cancers, autoimmune diseases, and inflammatory diseases.
    Type: Grant
    Filed: June 1, 2010
    Date of Patent: February 17, 2015
    Assignee: President and Fellows of Harvard College
    Inventors: Suzanne Walker Kahne, Michael Block Lazarus, Benjamin J. Gross
  • Publication number: 20150038528
    Abstract: The present invention relates to novel compounds of formula (I), and compositions capable of inhibiting PHD1 enzyme activity selectively over other isoforms, for example, PHD2 and/or PHD3 enzymes. The invention also relates to compounds of formula (I) for use in disorders such as muscle degeneration, colitis, IBD, and certain ischemias.
    Type: Application
    Filed: March 8, 2013
    Publication date: February 5, 2015
    Inventors: Wen-Bin Ho, Hongda Zhao, Shaojiang Deng, Danny Ng, Lee R. Wright, Min Wu, Xiaoti Zhou, Michael P. Arend, Lee A. Flippin
  • Patent number: 8946260
    Abstract: The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.
    Type: Grant
    Filed: September 14, 2011
    Date of Patent: February 3, 2015
    Assignee: Novartis AG
    Inventors: Mark Gary Bock, Christoph Gaul, Venkateshwar Rao Gummadi, Henrik Moebitz, Saumitra Sengupta
  • Publication number: 20150031721
    Abstract: The present invention relates to the polymorphic forms of the compound of Formula (I), preparation thereof including the preparation of intermediates and pharmaceutical compositions, and use of a polymorph above in the treatment of a disease, a disorder or a condition, or in the manufacturing of a medicament for the treatment of a disease, a disorder or a condition.
    Type: Application
    Filed: July 23, 2012
    Publication date: January 29, 2015
    Inventors: Xinshan Kang, Wei Long, Jianxi Zhang, Yunyan Hu, Yinxiang Wang
  • Publication number: 20150023913
    Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.
    Type: Application
    Filed: July 2, 2013
    Publication date: January 22, 2015
    Inventors: Piyasena Hewawasam, Omar D. Lopez, Yong Tu, Alan Xiangdong Wang, Ningning Xu, John F. Kadow, Nicholas A. Meanwell, Samayamuthula Venkata Satya Arun Kumar Gupta, Indasi J. Gopi Kumar, Suresh Kumar Ponugupati, Makonen Belema
  • Publication number: 20150018352
    Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.
    Type: Application
    Filed: March 7, 2013
    Publication date: January 15, 2015
    Inventors: Thomas Dineen, Charles Kreiman, Matthew Weiss, Stephanie Geuns-Meyer
  • Patent number: 8933096
    Abstract: The invention provides a compound of formula (I): or a salt or prodrug thereof, wherein R1, R4-R8, R10, R2?-R6?, W, and A have any of the values described in the specification, as well as compositions comprising a compound of formula (I). The compounds are useful as antibacterial agents.
    Type: Grant
    Filed: June 9, 2011
    Date of Patent: January 13, 2015
    Assignees: Rugers, The State University of New Jersey, University of Medicine and Dentistry of New Jersey
    Inventors: Edmond J. Lavoie, Ajit Parhi, Daniel S. Pilch
  • Patent number: 8927534
    Abstract: The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; ? is a radical of formula (II), R2 is a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents.
    Type: Grant
    Filed: January 31, 2007
    Date of Patent: January 6, 2015
    Assignee: Shire Orphan Therapies GmbH
    Inventors: Gunther Zischinsky, Roland Stragies, Frank Osterkamp, Dirk Scharn, Gerd Hummel, Holger Kalkhof, Grit Zahn, Doerte Vossmeyer, Claudia Christner-Albrecht, Ulrich Reineke
  • Publication number: 20150005327
    Abstract: The present invention relates to the use of an agent that inhibits the activity of an enzyme that mediates repair of a DNA strand break in the manufacture of a medicament for the treatment of diseases caused by a defect in a gene that mediates homologous recombination.
    Type: Application
    Filed: July 2, 2014
    Publication date: January 1, 2015
    Inventor: Thomas Helleday
  • Patent number: 8912332
    Abstract: The present invention describes tripodal catechol derivatives with a flexible basic framework for the functionalization of surfaces, and methods for their production and use. The central atom of the flexible framework is hereby a tertiary aliphatic carbon atom. The remaining fourth bridgehead position is easily suitable to be further functionalized via so-called click reactions, e.g. with biomolecules, dyes, radiomarkers, polyethylene glycol or active agents.
    Type: Grant
    Filed: September 7, 2011
    Date of Patent: December 16, 2014
    Assignee: Justus-Liebig-Universitaet Giessen
    Inventors: Wolfgang Maison, Faiza Khalil, Elisa Franzmann
  • Patent number: 8895726
    Abstract: The present invention relates to a compound derived from indole corresponding to the following formula II: wherein X represents N, CR8 or N+R8, wherein R8 represents a hydrogen atom, a hydroxyl or alkyl or methoxy group optionally substituted with a phenyl group; R2, R3 and R4 independently represent a hydrogen atom or a halogen atom or an optionally substituted alkyl, amine, alkene, ester, sulfonamide, ether or benzyl group; R5 represents a hydrogen atom or an optionally substituted, saturated or unsaturated alkyl group, amine, benzyl group; R6 represents an optionally substituted C1-C3 alkyl group; R7 represents a hydrogen atom or an optionally substituted C1-C3 alkyl group and R7 is absent when the ring A is in the b position, and A represents a ring; R9 and R10 represent together a carbon bond or independently represent an R11 OR11, SR11 group; wherein R11 represents a hydrogen atom, an optionally substituted, saturated or unsaturated, C1-C3 alkyl group, which may contain one or more sulfur, oxygen or
    Type: Grant
    Filed: February 19, 2008
    Date of Patent: November 25, 2014
    Assignees: The Institut Curie, The University of Montpellier 2 Science and Techniques
    Inventors: Fabrice Lejeune, Jamal Tazi, David Grierson, Christian Rivalle, Florence Mahuteau-Betzer
  • Patent number: 8889871
    Abstract: Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R?, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
    Type: Grant
    Filed: February 18, 2014
    Date of Patent: November 18, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alan Xiangdong Wang, Li-Qiang Sun, Sing-Yuen Sit, Ny Sin, Paul Michael Scola, Yan Chen
  • Publication number: 20140336190
    Abstract: This application relates to chemical compounds which may act as inhibitors of; or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) wherein R1a, R1b, R2, R2b, R3, R4a, R4b, and R5 are described herein.
    Type: Application
    Filed: May 8, 2014
    Publication date: November 13, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Evangelos Aktoudianakis, Gregory Chin, Britton Kenneth Corkey, Jinfa Du, Kristyna Elbel, Robert H. Jiang, Tetsuya Kobayashi, Rick Lee, Ruben Martinez, Samuel E. Metobo, Michael Mish, Manuel Munoz, Sophie Shevick, David Sperandio, Hai Yang, Jeff Zablocki
  • Patent number: 8883763
    Abstract: The use of isoquinolones for preparing drugs, including novel isoquinolones as well as their synthesis method. In particular, isoquinolone derivatives used in the treatment of pathological angiogenesis, and more particularly of cancer.
    Type: Grant
    Filed: March 1, 2011
    Date of Patent: November 11, 2014
    Assignees: Universite Joseph Fourier, Centre National de la Recherche Scientifique, Institut Curie
    Inventors: Andrei Popov, Aurélie Juhem, Jean-Claude Florent, Chi-Hung N'Guyen
  • Patent number: 8883823
    Abstract: The present disclosure relates to crystalline solid forms of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid, the process of preparing the forms, and pharmaceutical compositions and methods of use thereof.
    Type: Grant
    Filed: July 15, 2013
    Date of Patent: November 11, 2014
    Assignee: FibroGen, Inc.
    Inventors: Claudia Witschi, Jung Min Park, Michael D. Thompson, Michael John Martinelli, David A. Yeowell, Michael P. Arend
  • Patent number: 8877929
    Abstract: The present disclosure generally relates to a process for synthesizing optionally substituted 1-chloro-4-methoxyisoquinolines. The present disclosure also relates to intermediates useful in this process.
    Type: Grant
    Filed: December 13, 2012
    Date of Patent: November 4, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Shawn A. Springfield, Wendel W. Doubleday, Percy Sarwood Manchand
  • Publication number: 20140323519
    Abstract: This invention relates to novel heterocyclic compounds that are useful for treating cancer and other cellular proliferative diseases and/or disorders associated with B-Raf activity. The compounds of the invention may be illustrated by the Formula (I).
    Type: Application
    Filed: April 20, 2012
    Publication date: October 30, 2014
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: M. Arshad Siddiqui, Lianyun Zhao, Amit K. Mandal
  • Patent number: 8871788
    Abstract: The present disclosure relates to a series of substituted N-alkyl and N-acyl tetrahydro-isoquinoline derivatives of formula (I). wherein R, R1, R2, X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-alkyl and N-acyl tetrahydro-isoquinoline derivatives of formula (I) and intermediates therefor.
    Type: Grant
    Filed: November 6, 2012
    Date of Patent: October 28, 2014
    Assignee: Sanofi
    Inventors: Zhongli Gao, Ryan Hartung
  • Publication number: 20140315881
    Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.
    Type: Application
    Filed: July 27, 2012
    Publication date: October 23, 2014
    Inventors: Erkan Baloglu, Gary J. Bohnert, Shomir GHOSH, Mercedes Lobera, Darby R. Schmidt, Leonard Sung
  • Patent number: 8865898
    Abstract: A nucleoside analog and a salt thereof represented by any of the general formulae (1) to (10) below: wherein R1, R2, and R3 are the same or different groups, and each of the R1, R2 and R3 is selected from a hydrogen atom, a protecting group for a functional group in nucleic acid synthesis, a phosphate group, a phosphate group protected by a protecting group in nucleic acid synthesis, and an activated phosphate group for solid phase synthesis; and Ar is one of an aromatic hydrocarbon group and a polyaromatic hydrocarbon group.
    Type: Grant
    Filed: November 30, 2011
    Date of Patent: October 21, 2014
    Assignee: Japan Science and Technology Agency
    Inventor: Yoshihito Ueno
  • Patent number: 8865709
    Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.
    Type: Grant
    Filed: September 24, 2013
    Date of Patent: October 21, 2014
    Assignee: Neosome Life Sciences, LLC
    Inventors: Laxman S. Desai, Srinivas Chittaboina
  • Publication number: 20140309253
    Abstract: The invention relates to compounds of the formula wherein R?, R1 through R7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.
    Type: Application
    Filed: June 25, 2014
    Publication date: October 16, 2014
    Inventors: Bertrand Leblond, Cedric Chauvignac, Thierry Taverne, Eric Beausoleil, Anne-Sophie Casagrande, Laurent Desire, Matthew P. Pando, John E. Donello, Rong Yang
  • Patent number: 8859586
    Abstract: The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.
    Type: Grant
    Filed: June 19, 2012
    Date of Patent: October 14, 2014
    Assignee: Novartis AG
    Inventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Joerg Kallen, Keiichi Masuya, Stefan Stutz
  • Patent number: 8859535
    Abstract: The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.
    Type: Grant
    Filed: June 19, 2012
    Date of Patent: October 14, 2014
    Assignee: Novartis AG
    Inventors: Nicole Buschmann, Pascal Furet, Philipp Holzer, Joerg Kallen, Keiichi Masuya, Stefan Stutz
  • Publication number: 20140302987
    Abstract: Use of substituted isoquinolinones, isoquinolinediones, isoquinolinetriones and dihydroisoquinolinones of the general formula (I) or their respective salts where the radicals in the general formula (I) correspond to the definitions given in the description, for enhancing stress tolerance in plants to abiotic stress, for strengthening plant growth and/or for increasing plant yield, and selected processes for preparing the compounds mentioned above.
    Type: Application
    Filed: July 2, 2012
    Publication date: October 9, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GmbH
    Inventors: Jens Frackenpohl, Hans-Joachim Zeiss, Ines Heinemann, Lothar Willms, Thomas Müller, Marco Busch, Pascal Von Koskull-Döering, Christopher Hugh Rosinger, Jan Dittgen, Martin Jeffrey Hills
  • Publication number: 20140303171
    Abstract: Compounds of Formula I are disclosed: wherein A, R1, R2, R3, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 9, 2014
    Inventors: Michael John Boyd, Jean-Francois Chiasson, Sheldon Crane, André Giroux
  • Publication number: 20140303164
    Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
    Type: Application
    Filed: February 28, 2014
    Publication date: October 9, 2014
    Inventors: Gediminas BRIZGYS, Eda CANALES, Chien-Hung CHOU, Michael GRAUPE, Yunfeng Eric HU, John O. LINK, Qi LIU, Yafan LU, Roland D. SAITO, Scott D. SCHROEDER, John R. SOMOZA, Winston C. TSE, Jennifer R. ZHANG
  • Publication number: 20140296219
    Abstract: The present invention is directed to methods, kits, and uses of inhibitors of LCMV mediated NF-?B activation to treat viral infections and inflammatory conditions.
    Type: Application
    Filed: November 14, 2013
    Publication date: October 2, 2014
    Applicant: UNIVERSITY OF MASSACHUSETTS
    Inventors: Robert W. Finberg, Evelyn A. Kurt-Jones, Shenghua Zhou
  • Publication number: 20140275161
    Abstract: Described herein are compounds and compositions for treating glaucoma and/or reducing intraocular pressure. Compositions may comprise an isoquinoline compound and a prostaglandin or a prostaglandin analog. Compounds described herein include those in which an isoquinoline compound is covalently linked to a prostaglandin or a prostaglandin analog, and those in which an isoquinoline compound and a prostaglandin free acid together form a salt.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Inventors: Casey Kopczynski, Cheng-Wen Lin, Jill Marie Sturdivant, Mitchell A. deLong
  • Publication number: 20140275155
    Abstract: This invention relates to bicyclic 1-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: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Matthias GRAUERT, Ralf ANDERSKEWITZ, Marc GRUNDL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS
  • Publication number: 20140275158
    Abstract: The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.
    Type: Application
    Filed: June 19, 2012
    Publication date: September 18, 2014
    Applicant: Novartis AG
    Inventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Joerg Kallen, Keiichi Masuya, Stefan Stutz
  • Publication number: 20140275118
    Abstract: The present invention is directed to compounds of Formula I: wherein X is N or CR1; Y is N or CR2; R1 is H, alkoxy, halo, triazolyl, pyrimidinyl, oxazolyl, isoxazole, oxadiazolyl, or pyrazolyl; R2 is H, alkyl, alkoxy, or halo; Z is NH or O; R3 is H, alkyl, alkoxy, halo, or triazolyl; R4 is H or alkyl; or R3 and R4, together with the atoms to which they are attached, form a 6-membered aryl ring or a 5- or 6-membered heteroaryl ring; R5 is pyridyl, pyrazinyl, or pyrimidinyl, wherein the pyridyl, pyrazinyl, or pyrimidinyl is optionally substituted with halo or alkyl; and n is 1 or 2. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods of using the compounds of the invention are also within the scope of the invention.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Christine F. GELIN, Terry P. LEBOLD, Brock T. SHIREMAN
  • Publication number: 20140275160
    Abstract: Described herein are compounds and compositions for treating glaucoma and/or reducing intraocular pressure. Compositions may comprise an isoquinoline compound and a prostaglandin or a prostaglandin analog. Compounds described herein include those in which an isoquinoline compound is covalently linked to a prostaglandin or a prostaglandin analog, and those in which an isoquinoline compound and a prostaglandin free acid together form a salt.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Inventors: Casey Kopczynski, Cheng-Wen Lin, Jill Marie Sturdivant, Mitchell A. deLong
  • Publication number: 20140275159
    Abstract: This invention relates to 2-Aza-bicyclo[2.2.2]octane-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: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Ralf ANDERSKEWITZ, Matthias GRAUERT, Marc GRUNDL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS
  • Publication number: 20140256734
    Abstract: Disclosed are compounds of Formula 1, or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating Type I hypersensitivity reactions, autoimmune diseases, inflammatory disorders, cancer, non-malignant proliferative disorders, and other conditions associated with BTK.
    Type: Application
    Filed: March 10, 2014
    Publication date: September 11, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: John David Lawson, Mark Sabat, Nicholas Scorah, Christopher Smith, Phong H. Vu, Haixia Wang
  • Patent number: 8822495
    Abstract: The invention relates to azacyclyl-substituted aryldihydroisoquinolinones and their derivatives, and their physiologically tolerated salts and physiologically functional derivatives, their preparation, medicaments comprising at least one azacyclyl-substituted aryldihydroisoquinolinone of the invention or its derivative, and the use of the azacyclyl-substituted aryldihydroisoquinolinones of the invention and their derivatives as MCH antagonists.
    Type: Grant
    Filed: August 14, 2008
    Date of Patent: September 2, 2014
    Assignee: Sanofi
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Gerhard Hessler, Torsten Haack, Petra Lennig