Nitrogen Attached Directly At 2-position By Nonionic Bonding And Sulfur Bonded Directly To The Nitrogen Patents (Class 544/297)
  • Patent number: 10772874
    Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.
    Type: Grant
    Filed: August 12, 2019
    Date of Patent: September 15, 2020
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Bingsong Han, Jian Lin, Dominic J. Reynolds, Bruce Roth, Chase C. Smith, Zhongguo Wang, Po-Wai Yuen, Xiaozhang Zheng
  • Patent number: 10487079
    Abstract: The invention relates to novel heteroaryl carboxamides, processes for their preparation, and their use for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory.
    Type: Grant
    Filed: February 27, 2018
    Date of Patent: November 26, 2019
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Martin Hendrix, Frank-Gerhard Böß, Christina Erb, Joachim Krüger, Christoph Methfessel, Rudy Schreiber, Welf-Burkhard Wiese, Joachim Luithle
  • Patent number: 10227342
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including mutant EGFR and mutant HER2 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including mutant EGFR and mutant HER2 activity, are described herein.
    Type: Grant
    Filed: May 13, 2015
    Date of Patent: March 12, 2019
    Assignee: ARIAD PHARMACEUTICALS, INC.
    Inventors: Wei-Sheng Huang, Yongjin Gong, Feng Li, Nicholas E. Bencivenga, David C. Dalgarno, Anna Kohlmann, William C. Shakespeare, Ranny M. Thomas, Xiaotian Zhu, Angela West, Willmen Youngsaye, Yun Zhang, Tianjun Zhou
  • Patent number: 10000470
    Abstract: A method for preparing nilotinib includes the following steps: performing an aminocarbonylation reaction on a compound A and 3-(4-methyl-1H-imidazole-1-yl)-5-(trifluoromethyl) aniline to obtain an amination product; and performing deprotection treatment of an R group on the amination product to obtain the nilotinib, wherein the compound A has a structure shown in formula I, and in formula I, an R group is selected from benzyl, —COCF3, —CHO or —CO2R?, where an R? group is C1˜C10 alkyl, C1˜C3 alkoxy ethyl or C7˜C19 aralkyl.
    Type: Grant
    Filed: May 26, 2015
    Date of Patent: June 19, 2018
    Assignees: ASYMCHEM LABORATORIES (TIANJIN) CO., LTD, TIANJIN ASYMCHEM PHARMACEUTICAL CO., LTD, JILIN ASYMCHEM LABORATORIES CO., LTD, ASYMCHEM LIFE SCIENCE (TIANJIN) CO., LTD, ASYMCHEM LABORATORIES (FUXIN) CO., LTD
    Inventors: Hao Hong, Gage James, Jiuyuan Li, Changfeng Li, Gaochao Huang
  • Patent number: 9926311
    Abstract: The invention relates to novel heteroaryl carboxamides, a process for their preparation, and pharmaceutical compositions containing them. These materials are useful for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory.
    Type: Grant
    Filed: August 24, 2015
    Date of Patent: March 27, 2018
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Martin Hendrix, Frank-Gerhard Böβ, Christina Erb, Joachim Krüger, Christoph Methfessel, Rudy Schreiber, Welf-Burkhard Wiese, Joachim Luithle
  • Patent number: 9701642
    Abstract: The object of the present invention is to provide a method for producing in high yield with high stereoselectivity an optically active 5-hydroxy-3-ketoester compound which is useful as an intermediate for a pharmaceutical. A novel method for producing an optically active 5-hydroxy-3-ketoester compound in which an asymmetric aldol reaction by use of 1,3-diene compound is carried out in the presence of an optically active binaphthol-titanium complex together with a substituted nitrogen-containing 5 or 6-membered aromatic heterocyclic compound to obtain an optically active 5-hydroxy-3-ketoester compound in high yield with high stereoselectivity; and a novel production intermediate having a crystalline form.
    Type: Grant
    Filed: August 26, 2014
    Date of Patent: July 11, 2017
    Assignee: NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Shouichi Tateyama, Shinya Naitou, Yasutaka Takada, Mariko Ishida, Hirohide Kitsuyama
  • Patent number: 9126938
    Abstract: This invention relates to compounds of Formulas I, II, and III, and their use as inhibitors of phosphatidylcholine transfer protein (PC-TP). The invention further relates to pharmaceutical compositions and methods of treatment of disorders related to the inhibition of PC-TP using the compounds of Formulas I, II, and III. Such disorders include obesity and disorders associated with obesity.
    Type: Grant
    Filed: August 17, 2010
    Date of Patent: September 8, 2015
    Assignee: The Brigham and Women's Hospital, Inc.
    Inventors: David Cohen, Neil Wagle, Gregory D. Cuny, Jun Xian, Marcie Glicksman, Ross L. Stein, Ekaterina Y. Shishova
  • Patent number: 9084826
    Abstract: The invention relates to fatty acid statin conjugates and fatty acid FXR agonist conjugates; compositions comprising an effective amount of a fatty acid statin conjugate or a fatty acid FXR agonist conjugate; and methods for treating or preventing a metabolic disease comprising the administration of an effective amount of a fatty acid statin conjugate or a fatty acid FXR agonist conjugate.
    Type: Grant
    Filed: May 1, 2013
    Date of Patent: July 21, 2015
    Assignee: Catabasis Pharmaceuticals, Inc.
    Inventors: Jill C. Milne, Michael R. Jirousek, Amal Ting, Chi B. Vu, Allison Wensley
  • Patent number: 9067895
    Abstract: The present invention relates in general to the field of organic chemistry and in particular to a process for the preparation of 5-((E)-2-((2S,4R)-4-hydroxy-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethanesulfonylamino)pyrimidine (RSVL) as well as a process for preparing crystalline 5-((E)-2-((2S,4R)-4-(tert-butyldimethylsilyloxy)-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethanesulfonylamino)pyrimidine (RSVLTBS) useful as key intermediates for the preparation of rosuvastatin or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: December 15, 2010
    Date of Patent: June 30, 2015
    Assignee: LEK PHARMACEUTICALS D.D.
    Inventors: Samo Andrensek, Jolanda Anzel, Marjeta Hocevar, Zdenko Casar
  • Publication number: 20150148360
    Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically compositions thereof. Compounds of Formula (I) are inhibitors of histone deacetylases (HDACs) and 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase (HMGR). Also provided are methods of using the compounds and pharmaceutical compositions for inhibiting the activity of HDACs and HMGR, treating diseases associated with HDACs or HMGR (e.g., cancer, hypercholesterolemia, an acute or chronic inflammatory disease, autoimmune disease, allergic disease, pathogen infection, neurodegenerative disease, and a disease associated with oxidative stress), or inhibiting drug resistance of cancer cells.
    Type: Application
    Filed: July 19, 2013
    Publication date: May 28, 2015
    Inventors: Jung-Hsin Lin, Jim-Min Fang, Ting-Rong Chen, Jhih-Bin Chen, Ching-Chow Chen, Tzu-Tang Wei
  • Patent number: 9040696
    Abstract: The present invention is related to methods for the preparation of pharmaceutically acceptable salts of (+)-7-[4-(4-fluorophenyl)-6-isopropyl-2-(methanesulfonyl-methyl-amino)-pyrimidin-5-yl]-(3R,5S,6E)-dihydroxy-hept-6-enoic acid, intermediates thereof and methods for producing said intermediates.
    Type: Grant
    Filed: November 29, 2011
    Date of Patent: May 26, 2015
    Assignee: EGIS Gyogyszergyar Nyilvanosan Mukodo Reszvenytarsasag
    Inventors: Marta Porcs-Makkay, Ferenc Lorant Bartha, Gyorgy Krasznai, Balazs Volk, Gyorgy Ruzsics, Laszlo Pongo, Gyula Lukacs, Tibor Szabo, Jozsef Barkoczy, Jozsef Debreczeni, Adrienn Keszthelyi, Angela Pandur, Eniko Molnar, Matyas Milen, Maria Tothne Lauritz
  • Patent number: 9040692
    Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, R4, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.
    Type: Grant
    Filed: March 11, 2014
    Date of Patent: May 26, 2015
    Assignee: Dart NeuroScience (Cayman) Ltd.
    Inventors: Venkataiah Bollu, James Breitenbucher, Alan Kaplan, Robert Lemus, Andrew Lindstrom, Troy Vickers, Mark E. Wilson, James Zapf
  • Publication number: 20150141449
    Abstract: The present invention relates in general to the field of organic chemistry and in particular to the preparation of N-(4-(4-fluorophenyl)-6-isopropyl-5-methylpyrimidin-2-yl)-N-methylmethanesulfonamide (I), N-(4-(4-fluorophenyl)-5-(bromomethyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide (II) and N-(4-(4-fluorophenyl)-5-(hydroxymethyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide (III), key intermediates in preparation of Rosuvastatin.
    Type: Application
    Filed: January 29, 2015
    Publication date: May 21, 2015
    Inventors: Zdenko CASAR, Janez Kosmrlj
  • Patent number: 9006432
    Abstract: The present invention is directed to processes for the preparation of substituted pyrimidine derivatives, useful as intermediates in the synthesis of histamine H4 receptor modulators, and to intermediates in H4 modulator synthesis.
    Type: Grant
    Filed: November 12, 2013
    Date of Patent: April 14, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Sergio Cesco-Cancian, Hongfeng Chen, Jeffrey S. Grimm, Neelakandha S. Mani, Daniel J. Pippel
  • Patent number: 8993585
    Abstract: The invention encompasses compounds having formula I or II and the compositions and methods using these compounds in the treatment of conditions in which inhibition of PKC and PKD is therapeutically useful.
    Type: Grant
    Filed: July 17, 2008
    Date of Patent: March 31, 2015
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Hui Li, Haoran Zhao, Donald Payan, Rao Kolluri, Kin Tso, John Ramphal, Shihai Gu
  • Patent number: 8987444
    Abstract: The present invention relates to an improved process for the preparation of amide intermediates useful in the preparation of cholesterol reducing agents.
    Type: Grant
    Filed: January 17, 2011
    Date of Patent: March 24, 2015
    Assignee: MSN Laboratories Private Limited
    Inventors: Manne Satyanarayana Reddy, Srinivasan Thirumalai Rajan, Maramreddy Sahadeva Reddy
  • Publication number: 20150051195
    Abstract: The present invention relates to a series of novel compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity.
    Type: Application
    Filed: October 30, 2014
    Publication date: February 19, 2015
    Inventors: Patrick Chaltin, Zeger Debyser, Marc De Maeyer, Arnaud Marchand, Damien Marchand, Wim Smets, Arnout Voet, Frauke Christ
  • Patent number: 8952028
    Abstract: Methods of treating or preventing chemoresistance or relapse growth of cancer cells are provided. Methods of treating or preventing resistance to tyrosine kinase based chemotherapeutic treatment in hematologic and solid tumors are provided. BCR-ABL drug resistance in chronic myelogenous leukemia (CML) and models for conducting further study on the same are presented. The methods comprise administering a therapeutically effective amount of one or more SIRT1 modulators to the cells or subject in need thereof. The methods may be administered in combination with, prior to or subsequent to chemotherapy or may be administered to counteract the effect of a spontaneous genetic mutation. Methods of using SIRT1 inhibitors to treat or prevent insulin and transferrin-induced resistance are also presented. A novel cell model to study mechanisms of acquired chemoresistance is also provided.
    Type: Grant
    Filed: February 5, 2008
    Date of Patent: February 10, 2015
    Assignee: City of Hope
    Inventor: Wenyong Chen
  • Patent number: 8952027
    Abstract: The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.
    Type: Grant
    Filed: October 23, 2012
    Date of Patent: February 10, 2015
    Assignee: Portola Pharmaceuticals, Inc.
    Inventors: Zhaozhong J. Jia, Chandrasekar Venkataramani, Wolin Huang, Mukund Mehrotra, Yonghong Song, Qing Xu, Shawn M. Bauer, Jack W. Rose, Brian Kane, Anjali Pandey
  • Publication number: 20150011546
    Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
    Type: Application
    Filed: February 11, 2013
    Publication date: January 8, 2015
    Inventors: Brian K. Albrecht, James Edmund Audia, Andrew S. Cook, Les A. Dakin, Martin Duplessis, Victor S. Gehling, Jean-Christophe Harmange, Christopher G. Nasveschuk, Rishi G. Vaswani
  • Publication number: 20140371201
    Abstract: The present invention provides compounds of Formula I, and pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav1.7. The compounds are useful for the treatment of diseases associated with the activity of sodium channels such as pain disorders and itch. Also provided are pharmaceutical compositions containing compounds of the present invention.
    Type: Application
    Filed: June 11, 2014
    Publication date: December 18, 2014
    Inventors: Matthew WEISS, Alessandro BOEZIO, Christiane BOEZIO, John R. BUTLER, Margaret Yuhua CHU-MOYER, Erin F. DIMAURO, Thomas DINEEN, Russell GRACEFFA, Angel GUZMAN-PEREZ, Hongbing HUANG, Charles KREIMAN, Daniel LA, Isaac E. MARX, Benjamin Charles MILGRIM, Hanh Nho NGUYEN, Emily PETERSON, Karina ROMERO, Brian SPARLING
  • Publication number: 20140361254
    Abstract: A heterocyclic compound represented by Formula 1 below and an organic light-emitting device including the heterocyclic compound are provided: Ar1, Ar2, Ar3 and X in Formula 1 are defined as in the specification.
    Type: Application
    Filed: September 26, 2013
    Publication date: December 11, 2014
    Applicant: SAMSUNG DISPLAY CO., LTD.
    Inventors: Seok-Hwan Hwang, Young-Kook Kim, Hye-Jin Jung, Jun-Ha Park, Eun-Young Lee, Jin-O Lim, Sang-Hyun Han, Eun-Jae Jeong, Soo-Yon Kim, Jong-Hyuk Lee
  • Patent number: 8906911
    Abstract: Disclosed herein are chemokine receptor antagonists of formula (I) wherein R1, R2, and R3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
    Type: Grant
    Filed: March 29, 2013
    Date of Patent: December 9, 2014
    Assignee: AbbVie Inc.
    Inventors: Michael D. Meyer, Xueqing Wang, Tao Guo, Robert Guo Ping Wei, Lijuan Jane Wang
  • Publication number: 20140357864
    Abstract: The present invention relates to a process for the preparation of a precursor for the synthesis of hexanoic acid derived statins and to the use of said precursor in the manufacture of a medicament.
    Type: Application
    Filed: December 6, 2012
    Publication date: December 4, 2014
    Inventors: Ben De Lange, Dennis Heemskerk, Karin Henderika Maria Bessembinder
  • Publication number: 20140350016
    Abstract: The present invention is directed to compounds, compositions and methods for treating or preventing hepatitis C virus (HCV) infection in human subjects or other animal hosts. The compounds are as also pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof as pharmaceutical compositions and methods for treatment or prevention of HCV infection.
    Type: Application
    Filed: August 8, 2014
    Publication date: November 27, 2014
    Inventors: Steven J. Coats, Franck Amblard, Hongwang Zhang, Longhu Zhou, Richard Anthony Whitaker, Tamara Rosario McBrayer, Raymond F. Schinazi, Junxing Shi
  • Publication number: 20140343056
    Abstract: Herein are disclosed azaindazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
    Type: Application
    Filed: September 12, 2012
    Publication date: November 20, 2014
    Applicant: GlaxoSmithKline LLC
    Inventors: Joelle Lorraine Burgess, Neil W. Johnson, Steven David Knight, Louis Vincent LaFrance, III, William Henry Miller, Kenneth Allen Newlander, Stuart Paul Romeril, Meagan B. Rouse, Dominic Suarez, Xinrong Tian, Sharad Kumar Verma
  • 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
  • Patent number: 8871754
    Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a Plasmodium parasite, such as malaria.
    Type: Grant
    Filed: November 18, 2013
    Date of Patent: October 28, 2014
    Assignees: IRM LLC, Novartis AG
    Inventors: Arnab Kumar Chatterjee, Advait Suresh Nagle, Prasuna Paraselli, Ravinder Reddy Kondreddi, Seh Yong Leong, Pranab Kumar Mishra, Robert Joseph Moreau, Jason Thomas Roland, Wei Lin Sandra Sim, Oliver Simon, Liying Jocelyn Tan, Bryan K S Yeung, Bin Zou, Venkatataiah Bollu
  • Publication number: 20140316135
    Abstract: Provided are a compound of formula (5) and a process for its preparation wherein: R1 represents an alkyl group; R2 represents an aryl group; R3 represents a protecting group or an alkyl group; R4 represents a protecting group or a SO2R5 group where R5 is an alkyl group; R6 represents (PR7R8)+X? or P(?O)R7R8 in which X is an anion and R7 and R8 each independently is an alkyl, aryl, alkoxy, or aryloxy group; P1 represents hydrogen or a protecting group; and W represents ?O or OP2, in which P2 represents hydrogen or a protecting group.
    Type: Application
    Filed: March 25, 2014
    Publication date: October 23, 2014
    Applicant: Redx Pharma Limited
    Inventors: David J. Moody, Jonathan W. Wiffen
  • Publication number: 20140303163
    Abstract: The present invention discloses use of compounds of formula (I) in preventing and treating inflammatory disorder.
    Type: Application
    Filed: March 24, 2011
    Publication date: October 9, 2014
    Inventor: Ying Luo
  • Publication number: 20140296245
    Abstract: This invention is directed to benzensulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of sodium channel-mediated diseases or conditions, such as pain.
    Type: Application
    Filed: October 30, 2012
    Publication date: October 2, 2014
    Inventors: Shaoyi Sun, Alla Yurevna Zenova, Mikhail Chafeev, Qi Jia, Zaihui Zhang, Renata Marcella Oballa
  • Patent number: 8846704
    Abstract: The present invention relates to thiopyrimidine-based compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2 or JAK3 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases and vascular diseases.
    Type: Grant
    Filed: January 31, 2008
    Date of Patent: September 30, 2014
    Assignee: YM Biosciences Austraila Pty Ltd
    Inventors: David Gerard Bourke, Xianyong Bu, Christopher John Burns, Anthony Nicholas Cuzzupe, John Thomas Feutrill, Tracy Leah Nero, Beata Maria Blannin, Jun Zeng, Shaun Patrick Gaynor
  • Patent number: 8846708
    Abstract: The present invention relates to a salt of a pyrimidin derivative of the acid (3R,5S,6E)-7-[4-(4-fluorophenyl)-2-(N-methylmethanesulfonamide)-6-(propan-2-yl)pyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic, to a method for preparing same and to the use thereof in formulating pharmaceutical formulations.
    Type: Grant
    Filed: October 4, 2011
    Date of Patent: September 30, 2014
    Assignee: Laboratorios Senosiain S.A. de C.V.
    Inventors: Juan Pablo Senosiain Peláez, Héctor Senosiain Arroyo, Manuel Francisco Lara Ochoa
  • Patent number: 8846947
    Abstract: Provided herein are sirtuin-modulating compounds of formula (II). The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders relating to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Grant
    Filed: July 2, 2009
    Date of Patent: September 30, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Chi B. Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
  • Patent number: 8841316
    Abstract: A novel solid form of Rosuvastatin comprises as the active ingredient a salt of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)-amino]pyrimidin-5-yl]-(3R,5S)-3,5-dihydroxyhept-6-enoic acid] and vanillin or vanillin derivatives. The crystal comprising the two components, and minor amounts of water, shows improved properties such as crystallization behavior stability and decreased hydroscopic behavior.
    Type: Grant
    Filed: January 31, 2014
    Date of Patent: September 23, 2014
    Assignee: BASF SE
    Inventors: Andreas Hafner, Fritz Blatter, Martin Szelagiewicz, Bernd Siebenhaar
  • Publication number: 20140275531
    Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, R4, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 18, 2014
    Inventors: Venkataiah Bollu, James Breitenbucher, Alan Kaplan, Robert Lemus, Andrew Lindstrom, Troy Vickers, Mark E. Wilson, James Zapf
  • Publication number: 20140275087
    Abstract: The present invention relates to pyrrolidine derivatives of the formula (I), or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such pyrrolidine derivatives, and the use of such pyrrolidine derivatives for therapeutic purposes. The pyrrolidine derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: March 17, 2014
    Publication date: September 18, 2014
    Inventors: Wilhelm Amberg, Frauke Pohlki, Udo Lange, Ying X. Wang, Hongyu H. Zhao, Huan-Qiu Li, Jason T. Brewer, Irini Zanze, Justin Dietrich, Anil Vasudevan, Stevan W. Djuric, Yanbin Lao, Charles W. Hutchins
  • Patent number: 8829200
    Abstract: The present invention relates to compounds of formula (IA) and (IB): and pharmaceutically acceptable salts thereof, wherein R1-R7 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: October 26, 2011
    Date of Patent: September 9, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Zhidong Chen, Stephane De Lombaert, Jonathon Alan Dines, Weimin Liu, Ho Yin Lo, Pui Leng Loke
  • Patent number: 8815862
    Abstract: Methods for the preparation of Rosuvastatin by co-crystals of Rosuvastatin or intermediates are provided. Also provided are co-crystals, pharmaceutical compositions which include such co-crystals and methods for treating conditions associated with hypercholesterolemia by administering such compositions.
    Type: Grant
    Filed: December 3, 2012
    Date of Patent: August 26, 2014
    Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.
    Inventors: Clark Ferrari, Andrea Castellin, Marco Galvagni, Nicolas Tesson, Jordi De Mier, Llorenç Rafecas
  • 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: 8809339
    Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y and A are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Grant
    Filed: January 4, 2013
    Date of Patent: August 19, 2014
    Assignee: Ardelyx, Inc.
    Inventors: Jason G. Lewis, Jeffrey W. Jacobs, Nicholas Reich, Michael R. Leadbetter, Noah Bell, Han-Ting Chang, Tao Chen, Marc Navre, Dominique Charmot, Christopher Carreras, Eric Labonte
  • Publication number: 20140221347
    Abstract: Compounds of formula I: or pharmaceutically acceptable 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: January 9, 2014
    Publication date: August 7, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Gediminas BRIZGYS, Chien-Hung CHOU, Randall L. HALCOMB, Yunfeng Eric HU, Qi LIU, John R. SOMOZA, Winston C. TSE, Jennifer R. ZHANG
  • Patent number: 8796271
    Abstract: This invention provides compounds of formula IA-a or IB-a and subsets thereof: wherein Z, HY, R1, R2, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Grant
    Filed: August 11, 2011
    Date of Patent: August 5, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Masaaki Hirose, Zhigen Hu, Yongbo Hu, Hong Myung Lee, Zhan Shi, Stepan Vyskocil, Tianlin Xu
  • Patent number: 8791049
    Abstract: Provided are improved agricultural processes for the improved cultivation of rice wherein the crops are treated to control undesired vegetative growth using a plant treatment composition comprising both halosulfuron and thifensulfuron to provide improved herbicidal efficacy against Heteranthera limosa, commonly referred to as “duck salad”. Also provided are compositions useful in the improved agricultural processes, as well as herbicidal treatment regimens. Unexpectedly high rates of efficacy against Heteranthera limosa, amongst rice plant in rice crops are disclosed.
    Type: Grant
    Filed: December 13, 2010
    Date of Patent: July 29, 2014
    Assignee: Gowan Co.
    Inventors: Eric Paige Webster, Dominic Frank Alonso, Sergio Comparini, Wallace Keith Majure, Sandra Alcaraz, Charles Paul Grasso, Eric James McEwen, Tak Wai Cheung
  • Publication number: 20140205641
    Abstract: The present invention relates to co-crystals of cyprodinil and dithianon as defined in the description, processes for preparing these co-crystals and also to compositions comprising at least such co-crystals. The invention also relates to the use of such co-crystals or compositions for combating harmful fungi.
    Type: Application
    Filed: August 30, 2012
    Publication date: July 24, 2014
    Applicant: BASF SE
    Inventors: Christian Sowa, Randall Evan Gold, Tiziana Chiodo, Ralf Vogel
  • Publication number: 20140206661
    Abstract: The present invention provides a compound of Formula (X) or a pharmaceutically acceptable salt thereof; 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: January 21, 2014
    Publication date: July 24, 2014
    Applicant: NOVARTIS AG
    Inventors: Jake AXFORD, Natalie DALES, Moo Je SUNG
  • Publication number: 20140194452
    Abstract: The invention relates to pyrazolyl-based carboxamide compounds useful as ICRAC inhibitors, to pharmaceutical compositions containing these compounds and to these compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders, in particular inflammatory diseases and/or inflammatory disorders.
    Type: Application
    Filed: January 10, 2014
    Publication date: July 10, 2014
    Applicant: Grünenthal GmbH
    Inventors: Sonja Nordhoff, Sebastian Wachten, Achim Kless, Felix Voss, Stefanie Ritter
  • Publication number: 20140194451
    Abstract: Compounds which inhibit the small G protein Rho GTPase cell division cycle protein Cdc42 are provided. Morphological analyses of filopodia, western blots of Ccd42 phosphorylation, and effects on cellular wound healing and on growth cone formation all demonstrate that the described compounds are able to inhibit all tested Cdc42-mediated processes. The compounds effectively inhibit, the effects of Cdc42 and effectively inhibit Cdc42-related cellular functions involving actin, such as Golgi organization and cell movement. Furthermore, the described Cdc42 inhibitor compounds may be provided as a medicament for the treatment of various conditions.
    Type: Application
    Filed: November 22, 2013
    Publication date: July 10, 2014
    Inventors: Qun Lu, Huchen Zhou, Yanhua Chen, Amy Friesland
  • Patent number: 8765947
    Abstract: A preparation method of rosuvastatin calcium (Formula 1), which can be used for the production of medicament lowering the levels of LDL-cholesterol and triglycerides in vivo, is provided. Such preparation method is suitable for industrial production. Furthermore, the intermediate crystallines used in the preparation method are provided.
    Type: Grant
    Filed: March 5, 2013
    Date of Patent: July 1, 2014
    Assignee: Changzhou Pharmaceutical Factory
    Inventors: Benshun Chen, Bing Wang, Xiaofeng Jin, Lin Zou
  • Publication number: 20140179681
    Abstract: Provided herein are compounds having anti-proliferative effect. Also provided are compounds that can modulate the activity of multi-domain proteins comprising a dimerization arm and interdomain tether, such as EGFR, where an untethered, extended conformation is the active state and a tethered conformation is the inactive state, resulting in an autoinhibited configuration. Also provided are methods and pharmacophores for identifying such compounds. Other aspects provide methods or therapeutic treatment for proliferative diseases, disorders, or conditions, such as those associated with EGFR.
    Type: Application
    Filed: January 8, 2014
    Publication date: June 26, 2014
    Inventor: Joseph P. Errico