Nitrogen Attached Directly To Diazine Ring By Nonionic Bonding Patents (Class 544/322)
  • Patent number: 10975352
    Abstract: The present invention relates compounds for stabilizing cells and methods of their use.
    Type: Grant
    Filed: June 4, 2019
    Date of Patent: April 13, 2021
    Assignee: The Scripps Research Institute
    Inventors: Yue Xu, Sheng Ding
  • Patent number: 10364229
    Abstract: The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I) which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.
    Type: Grant
    Filed: November 14, 2017
    Date of Patent: July 30, 2019
    Assignee: ADVERIO PHARMA GMBH
    Inventors: Peter Fey, Alfons Grunenberg, Donald Bierer
  • Patent number: 9518028
    Abstract: The present invention relates to process for the preparation of 7-[4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyrimidin-5-yl]-(3R,5S)-dihydroxy-(E)-6-heptenoic acid calcium having formula (I). The compound of formula (I) has adopted name “Rosuvastatin Calcium”. The present invention is also related to novel intermediates of formula (4) and formula (5) used in preparation of formula (I), and process of their preparation.
    Type: Grant
    Filed: November 18, 2013
    Date of Patent: December 13, 2016
    Assignee: SUVEN LIFE SCIENCES LIMITED
    Inventors: Udaya Bhaskara Rao Siripalli, Veera Reddy Arava, Rajendiran Chinnapillai, Anji Reddy Middekadi, Naresh Raju Makaraju, Venkateswarlu Jasti
  • Patent number: 9376397
    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: Grant
    Filed: January 29, 2015
    Date of Patent: June 28, 2016
    Assignee: LEK PHARMACEUTICALS D.D.
    Inventors: Zdenko Casar, Janez Kosmrlj
  • Publication number: 20150126484
    Abstract: The invention provides novel heterocyclic amine compounds according to Formula (I) and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Application
    Filed: September 12, 2012
    Publication date: May 7, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Ruoxi Lan, Bayard R. Huck, Xiaoling Chen, Lizbeth Celeste Deselm, Yufang Xiao, Hui Qiu, Constantin Neagu, Igor Mochalkin, Theresa L. Johnson
  • Publication number: 20150126364
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Q is and Z1, Z2, J1, J2, M, R1a, R1b, R2a, R2b, R2c, R2d, R14 and R14a are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: May 13, 2013
    Publication date: May 7, 2015
    Applicant: E I Du Pont de Nemours and Company
    Inventors: Thomas Francis Pahutski, JR., Matthew James Campbell, Dominic Ming-Tak Chan, Jeffrey Keith Long, Thomas Martin Stevenson
  • Patent number: 9018224
    Abstract: Substituted cyclopropyl compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: April 28, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott Edmondson, Zhiyong Hu, Ping Liu, Gregori J. Morriello, Jason W. Szewczyk, Bowei Wang, Liping Wang, Harold B. Wood, Cheng Zhu, Yuping Zhu, Zhiqiang Guo
  • Patent number: 9006269
    Abstract: Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Wherein Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: April 14, 2015
    Assignee: Vernalis (R&D) Ltd.
    Inventors: Stephen Roughley, Steven Walls, Terance Hart, Rachel Parsons, Paul Brough, Christopher Graham, Alba Macias
  • Publication number: 20150094205
    Abstract: What is described are compounds of the general formula (I) and agrochemically acceptable salts thereof and their use in the field of crop protection.
    Type: Application
    Filed: March 27, 2013
    Publication date: April 2, 2015
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Klemens Minn, Michael Gerhard Hoffmann, Elmar Gatzweiler, Ines Heinemann, Isolde Haeuser-Hahn, Christopher Hugh Rosinger
  • Publication number: 20150080414
    Abstract: The present application relates to novel substituted 5-fluoro-1H-pyrazolopyridines, 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 producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: November 24, 2014
    Publication date: March 19, 2015
    Applicant: BAYER INTELLECTUAL PROPERTY GmbH
    Inventors: Markus FOLLMANN, Johannes-Peter STASCH, Gorden REDLICH, Jens ACKERSTAFF, Nils GRIEBENOW, Walter KROH, Andreas KNORR, Eva-Maria BECKER, Frank WUNDER, Volkhart Min-Jian LI, Elke HARTMANN, Joachim MITTENDORF, Karl-Heinz SCHLEMMER, Rolf JAUTELAT, Donald BIERER
  • Publication number: 20150072986
    Abstract: The present invention provides novel compounds of any one of Formulae (I)-(III), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.
    Type: Application
    Filed: June 11, 2014
    Publication date: March 12, 2015
    Inventors: Winston Zapanta Ong, Pawel Wojciech Nowak, John Thomas Feutrill, Jinsoo Kim, Minh Ngoc Nguyen, Elizabeth Enlow
  • Publication number: 20150065507
    Abstract: The present invention is directed to novel retinoid-related orphan receptor gamma (ROR?) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR?.
    Type: Application
    Filed: April 25, 2013
    Publication date: March 5, 2015
    Applicant: Glaxo Group Limited
    Inventors: Veronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le, Lena Shukla
  • Patent number: 8969338
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein U, V, Y, R1, R2, R2?, R3, R3? and R8 are described herein. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Grant
    Filed: September 27, 2012
    Date of Patent: March 3, 2015
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Publication number: 20150051225
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, and G are defined herein.
    Type: Application
    Filed: August 16, 2013
    Publication date: February 19, 2015
    Applicant: Janssen Pharmaceutica NV
    Inventors: Ishtiyaque Ahmad, Rajagopal Bakthavatchalam, Sivaramakrishna Battula, Henricus Jacobus, Maria Gijsen, Mark Wall
  • Publication number: 20150025062
    Abstract: The present invention is directed to a method of enhancing visual function in a subject, comprising administering to the subject in need of such enhancement, a therapeutically effective amount of an inhibitor of a hyperpolarization-activated cyclic nucleotide-gated (HCN) channel. The present invention is also directed to an ocular implant comprising a therapeutically effective amount of the HCN channel inhibitor.
    Type: Application
    Filed: July 10, 2014
    Publication date: January 22, 2015
    Inventor: Movses H. Karakossian
  • Publication number: 20150025065
    Abstract: The present invention relates to compounds of general formula I, wherein the group R1, R2, X and Y are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the AMP-activated protein kinase (AMPK) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Application
    Filed: July 15, 2014
    Publication date: January 22, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Frank HIMMELSBACH, Elke LANGKOPF, Holger WAGNER
  • Publication number: 20150018349
    Abstract: In one aspect, the invention relates to substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: March 27, 2014
    Publication date: January 15, 2015
    Applicant: University of Utah Research Foundation
    Inventors: David J. Bearss, Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Sunil Sharma
  • Publication number: 20140374706
    Abstract: Disclosed are a compound for an organic optoelectric device, an organic optoelectric device including the same and a display device including the organic optoelectric device, wherein the compound for an organic optoelectric device is represented by the following Chemical Formula 1, In the above Chemical Formula 1, R1 to R7, X, L1 and L2 are the same as described in the detailed description.
    Type: Application
    Filed: November 20, 2013
    Publication date: December 25, 2014
    Inventors: Jin-Seok HONG, Dong-Min KANG, Eun-Sun YU, Soo-Young JEONG, Ji-Hun SHIN, Dong-Kyu RYU, Han-ill LEE, Yu-Na JANG
  • Publication number: 20140332793
    Abstract: A compound represented by Formula 1. An organic electric element includes a first electrode, a second electrode, and an organic material layer between the first electrode and the second electrode. The organic material layer includes the compound. When the organic electric element includes the compound in an organic material layer, luminous efficiency, stability, and life span can be improved.
    Type: Application
    Filed: December 21, 2012
    Publication date: November 13, 2014
    Inventors: Junghwan Park, Sunhee Lee, Soungyun Mun, Daesung Kim, Hwasoon Jung, Wonsam Kim, Jihun Byun, Bumsung Lee
  • Publication number: 20140326970
    Abstract: New carbazole-based compounds are provided that are useful as host materials for singlelayer and multilayer organic light-emitting diode (OLED) devices. Highly efficient single-layer OLEDs have been demonstrated using new N-heterocyclic carbazole-based host materials. Phosphorescent OLEDs with a structure of ITO/MoO3/host/host:dopant/host/Cs2CO3/Al have been fabricated in which the new host materials act simultaneously as electron-transport, holetransport and host layer. Using this design, devices with maximum current and external quantum efficiencies of 92.2 cd and 26.8% were achieved, the highest reported to date for a single-layer OLED.
    Type: Application
    Filed: May 2, 2014
    Publication date: November 6, 2014
    Inventors: Zachary M. Hudson, Suning Wang, Michael G. Helander, Zhibin Wang, Zheng-Hong Lu
  • Publication number: 20140315878
    Abstract: The present invention relates to new sulfonamide URAT-1 inhibitor compounds of formula (I) or a pharmaceutically acceptable salt thereof: to compositions containing them, to processes for their preparation and to intermediates used in such processes, and to methods of treatment, wherein R1, R2, R3, R4, R5 and R6 are as defined in the description.
    Type: Application
    Filed: April 17, 2014
    Publication date: October 23, 2014
    Applicant: PFIZER LIMITED
    Inventors: Robert Ian Storer, Nigel Alan Swain, Robert McKenzie Owen
  • Publication number: 20140309208
    Abstract: Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds are disclosed that are represented by general formula (I). Also disclosed, are pharmaceutical compositions including these compounds and methods of using these compounds and compositions for the treatment of chemokine-mediated pathologies.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 16, 2014
    Inventors: Branislav Musicki, Jerôme Aubert, Jean-Guy Boiteaux, Laurence Clary, Patricia Rossio, Marlène Schuppli-Nollet
  • Publication number: 20140309212
    Abstract: The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.
    Type: Application
    Filed: June 26, 2014
    Publication date: October 16, 2014
    Inventors: Minna Bui, Patrick Conlon, Julio H. Cuervo, Daniel A. Erlanson, Junfa Fan, Bing Guan, Brian T. Hopkins, Tracy J. Jenkins, Gnanasambandam Kumaravel, Alexey A. Lugovskoy, Doug Marcotte, Noel Powell, Daniel Scott, Laura Silvian, Art Taveras, Deping Wang, Min Zhong
  • Publication number: 20140242099
    Abstract: The invention relates to certain compounds or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: October 26, 2012
    Publication date: August 28, 2014
    Inventors: Shoujun Chen, Junyi Zhang, Jun Jiang, Teresa Kowalczyk-Przewloka, Zhiqiang Xia, Shijie Zhang
  • Patent number: 8815871
    Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: August 26, 2014
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Muneaki Kurimura, Shinichi Taira, Takahiro Tomoyasu, Nobuaki Ito, Kuninori Tai, Noriaki Takemura, Takayuki Matsuzaki, Yasuhiro Menjo, Shin Miyamura, Yohji Sakurai, Akihito Watanabe, Yasuyo Sakata, Takumi Masumoto, Kohei Akazawa, Haruhiko Sugino, Naoki Amada, Satoshi Ohashi, Tomoichi Shinohara, Hirofumi Sasaki, Chisako Morita, Junko Yamashita, Satoko Nakajima
  • Publication number: 20140235637
    Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 21, 2014
    Applicant: InterMune, Inc.
    Inventors: Karl Kossen, Scott D. Seiwert, Vladimir Serebryany, Donald Ruhrmund, Leonid D. Beigelman, Luca Francesco Mario Raveglia, Stefania Vallese, Ivana Bianchi, Tao Hu
  • 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: 20140228363
    Abstract: The present invention provides a compound of formula (I): as further described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: April 22, 2014
    Publication date: August 14, 2014
    Applicant: NOVARTIS AG
    Inventors: Matthew Burger, Yu Ding, Wooseok Han, Gisele Nishiguchi, Alice Rico, Robert Lowell Simons, Aaron R. Smith, Victoriano Tamez, JR., Huw Tanner, Lifeng Wan
  • Publication number: 20140219989
    Abstract: The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
    Type: Application
    Filed: July 3, 2012
    Publication date: August 7, 2014
    Inventors: Craig Boyle, William Greenlee, Samuel Chackalamannil, Claire Lankin
  • Publication number: 20140206702
    Abstract: The invention provides compounds of Formulas Ia-Ib, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, Ra, R1, R2, R4, R5 and R16 are defined herein, a pharmaceutical composition that includes a compound of Formulas Ia-Ib and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy.
    Type: Application
    Filed: March 20, 2014
    Publication date: July 24, 2014
    Applicant: GENENTECH, INC.
    Inventors: Yingjie Lai, Jun Liang, Steven R. Magnuson, Kirk D. Robarge, Vickie H. Tsui, Birong Zhang
  • Publication number: 20140206585
    Abstract: A compound of Formula I, Formula IA, Formula IB, or Formula II, or an acid or base addition salt thereof, and use of these compounds as antioxidants. In one embodiment, a compound of Formula II, wherein each of X, Y, and Z are independently a carbon or nitrogen atom; R1 and R2 are each independently a hydrogen or an electron donating group, but are not both hydrogen, and wherein R1, and R2 are each bonded to a carbon atom in their own respective aryl ring.
    Type: Application
    Filed: June 4, 2012
    Publication date: July 24, 2014
    Applicants: UNIVERSITA DI BOLOGNA, Queen's University at Kingston
    Inventors: Derek A. Pratt, Jason J. Hanthorn, Luca Valgimigli
  • Patent number: 8778939
    Abstract: The present invention relates to novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterized by LRRK2 kinase activity, particularly Parkinson's disease and Alzheimer's disease.
    Type: Grant
    Filed: September 27, 2010
    Date of Patent: July 15, 2014
    Assignee: Glaxo Group Limited
    Inventors: Paula Louise Nichols, Andrew John Eatherton, Paul Bamborough, Karamjit Singh Jandu, Oliver James Philps, Daniele Andreotti
  • Publication number: 20140187779
    Abstract: The present invention relates to a process for preparing a compound of formula (I).
    Type: Application
    Filed: May 7, 2012
    Publication date: July 3, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Juan M Rodriguez Delhi, Michael Schul, Christian Stange, Robert HAagenkoetter, Xiao-Jun Wang, Li Zhang, Oriol Massot
  • Publication number: 20140179699
    Abstract: The present invention relates to compounds useful as inhibitors of indoleamine 2,3-dioxygenase (IDO). The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications. The compounds of this invention have formula I-A: wherein the variables are as defined herein.
    Type: Application
    Filed: November 19, 2013
    Publication date: June 26, 2014
    Inventors: Dean Boyall, Christopher Davis, James Dodd, Simon Everitt, Andrew Miller, Peter Weber, James Westcott, Stephen Young
  • Patent number: 8759347
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Grant
    Filed: June 13, 2013
    Date of Patent: June 24, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Carl R. Illig, Shelly K. Ballentine, Jinsheng Chen, Renee Louise DesJarlais, Sanath K. Meegalla, Mark Wall, Kenneth J. Wilson
  • Publication number: 20140162983
    Abstract: The present invention provides novel pyrimidine and pyridine compounds according to Formula (I), Formula (II), Formula (III), Formula (IV) and Formula (V) their manufacture and use for the treatment of hyperproliferative diseases including, but not limited to, cancer, lupus, allergic disorders, Sjogren's disease and rheumatoid arthritis. In preferred embodiments, the present invention describes irreversible kinase inhibitors including, but not limited to, inhibitors of Bruton's tyrosine kinase.
    Type: Application
    Filed: June 10, 2012
    Publication date: June 12, 2014
    Applicant: Merck Patent GmbH
    Inventors: Brian L. Hodous, Lesley Liu-Bujalski, Reinaldo Jones, Donald Bankston, Theresa L. Johnson, Igor Mochalkin, Ngan Nguyen, Hui Qiu, Andreas Goutopoulos, Nadia Brugger
  • Publication number: 20140148471
    Abstract: The present application relates to novel heterocyclic compounds, to the use thereof for controlling animal pests, which include arthropods and especially insects, and to processes for preparing the novel compounds.
    Type: Application
    Filed: January 31, 2014
    Publication date: May 29, 2014
    Applicant: Bayer CropScience AG
    Inventors: Thomas BRETSCHNEIDER, Reiner FISCHER, Martin FÜßLEIN, Peter JESCHKE, Adeline KÖHLER, Joachim KLUTH, Friedrich August MÜHLTHAU, Yoshitaka SATO, Arnd VOERSTE, Eiichi SHIMOJO
  • Patent number: 8735417
    Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: May 27, 2014
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Michael D. Altman, Kenneth L. Arrington, Jason Burch, Bernard Cote, Jean-Francois Fournier, Jacques Yves Gauthier, Solomon Kattar, Sandra Lee Knowles, Jongwon Lim, Michelle R. Machacek, Alan B. Northrup, Michael H. Reutershan, Joel S. Robichaud, Adam J. Schell, Kerrie B. Spencer
  • Patent number: 8729092
    Abstract: The invention discloses a method for the treatment of diseases, particularly those diseases characterized by diminished or aberrant cellular function, including AIDS, cancer, and Alzheimer's Disease. The method comprises administering a therapeutically effective amount of rosuvastatin enantiomer compounds in their (3R,5R), (3S,5R), or (3S,5S) configurations, or pharmaceutically acceptable salts thereof. Biologically-active rosuvastatin enantiomer compounds with (3R,5R), (3S,5R), and (3S,5S) stereochemistry are also disclosed.
    Type: Grant
    Filed: September 24, 2012
    Date of Patent: May 20, 2014
    Inventor: Terence J. Scallen
  • Patent number: 8722882
    Abstract: The present invention relates to Pyriraidine Derivatives of formula (I), compositions comprising a Pyrimidine Derivative, and methods of using the Pyrimidine Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient.
    Type: Grant
    Filed: December 21, 2009
    Date of Patent: May 13, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Bernard R. Neustadt, Andrew Stamford, Jinsong Hao, Charles Lee Jayne, Yan Xia
  • Patent number: 8703944
    Abstract: A method for preparing a rosuvastatin calcium intermediate represented by formula I. The method includes: hydrolyzing an ester compound represented by formula II (in which, R represents C1-C5) in the presence of a metal compound to obtain a carboxylic acid compound represented by formula III; and reducing the carboxylic acid compound in the presence of a reductant.
    Type: Grant
    Filed: February 3, 2013
    Date of Patent: April 22, 2014
    Assignee: Porton Fine Chemicals Ltd.
    Inventors: Wenqing Lin, Hongjie Zheng, Peng Yang
  • Patent number: 8703767
    Abstract: In one aspect, the invention relates to substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: April 1, 2012
    Date of Patent: April 22, 2014
    Assignee: University of Utah Research Foundation
    Inventors: David J. Bearss, Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Sunil Sharma
  • Patent number: 8703768
    Abstract: The invention is concerned with novel nitrogen-containing heteroaryl compounds of formula (I) wherein A1, A2, R1, R2, R3, R4, R5 and R6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as therapeutics.
    Type: Grant
    Filed: June 2, 2011
    Date of Patent: April 22, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Konrad Bleicher, Alexander Flohr, Katrin Groebke Zbinden, Felix Gruber, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rosa Maria Rodriguez-Sarmiento
  • Publication number: 20140088117
    Abstract: Cyclic ether pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R2 is a cyclic ether and X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: September 25, 2013
    Publication date: March 27, 2014
    Applicant: Genentech, Inc.
    Inventors: Jason Burch, Minghua Sun, Xiaojing Wang, Wesley Blackaby, Alastair James Hodges, Andrew Sharpe
  • Publication number: 20140057926
    Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.
    Type: Application
    Filed: August 20, 2013
    Publication date: February 27, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Thorsten OOST, Dennis FIEGEN, Christian GNAMM
  • Publication number: 20140018533
    Abstract: To provide a novel furanone derivative, and a medicine including the same.
    Type: Application
    Filed: March 30, 2012
    Publication date: January 16, 2014
    Applicants: CARNA BIOSCIENCES, INC., SBI BIOTECH CO., LTD.
    Inventors: Takayuki Irie, Ayako Sawa, Masaaki Sawa, Tokiko Asami, Yoko Funakoshi, Chika Tanaka
  • Patent number: 8623866
    Abstract: The invention is concerned with novel nitrogen-containing heteroaryl compounds of formula (I) wherein A1, A2, R1, R2, R3, R4, R5 and R6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as therapeutics.
    Type: Grant
    Filed: June 2, 2011
    Date of Patent: January 7, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Konrad Bleicher, Alexander Flohr, Katrin Groebke Zbinden, Felix Gruber, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rosa Maria Rodriguez-Sarmiento
  • Patent number: 8623877
    Abstract: The present disclosure relates to a series of substituted N-heteroaryl 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-heteroaryl tetrahydro-isoquinoline derivatives of formula (I) and intermediates therefor.
    Type: Grant
    Filed: November 6, 2012
    Date of Patent: January 7, 2014
    Assignee: Sanofi
    Inventors: Zhongli Gao, Ryan Hartung
  • Publication number: 20140001460
    Abstract: A material for electroluminescent devices which comprises a compound in which a heterocyclic group having nitrogen is bonded to carbazolyl group and an organic electroluminescent device having at least one organic thin film layer which is sandwiched between the cathode and the anode and contains the above material in at least one layer, are provided. The material can provide organic electroluminescent devices emitting bluish light with a high purity of color. The organic electroluminescence device uses the material.
    Type: Application
    Filed: August 30, 2013
    Publication date: January 2, 2014
    Applicant: IDEMITSU KOSAN CO., LTD.
    Inventors: Toshihiro IWAKUMA, Chishio HOSOKAWA, Hidetsugu IKEDA, Seiji TOMITA, Takashi ARAKANE
  • Publication number: 20140005178
    Abstract: The present disclosure relates to new azabiphenylaminobenzoic acid derivatives of formula (I); as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy as inhibitors of the dehydroorotate dihydrogenase (DHODH).
    Type: Application
    Filed: August 12, 2013
    Publication date: January 2, 2014
    Applicant: Almirall, S.A.
    Inventors: Julio Cesar CASTRO PALOMINO LARIA, Emma Terricabras Belart, Montserrat Erra Sola, Eloisa Navarro Romero, Siliva Fonquerna Pou, Aranzazu Cardus Figueras, Maria Estrella Lozoya Toribio