Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Diazine Ring Patents (Class 544/406)
  • Patent number: 9750246
    Abstract: The present invention relates to novel bisamide derivatives of formula (I) having insecticidal activity, to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests wherein X0, X1, X2, Y1, Y2, R1, R2, G1 and G2, and Q are as described in formula 1 or salts and n-Oxides thereof.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: September 5, 2017
    Assignee: Syngenta Participations AG
    Inventors: Andrew Edmunds, Andre Stoller, Thomas Pitterna
  • Publication number: 20150126516
    Abstract: A piperidine compound represented by the following Formula (1): wherein ring A, ring B, and ring C are the same or different and each represent a benzene ring or a nitrogen-containing heteroaromatic ring; W represents a C1-C4 alkylene or alkenylene group; X, Y, and Z are the same or different and each represent a halogen atom, a C1-C6 alkyl group, a halo C1-C6 alkyl group, a C1-C6 alkoxy group, or a halo C1-C6 alkoxy group; m, n, and p are the same or different and each represent an integer of 0 to 5; when m is greater than or equal to 2, the Xs are the same or different; when n is greater than or equal to 2, the Ys are the same or different; and when p is greater than or equal to 2, the Zs are the same or different has an excellent controlling efficacy against pests.
    Type: Application
    Filed: April 12, 2013
    Publication date: May 7, 2015
    Inventor: Sadayuki Arimori
  • Patent number: 9000163
    Abstract: Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions.
    Type: Grant
    Filed: October 29, 2013
    Date of Patent: April 7, 2015
    Assignee: Zeria Pharmaceutical Co., Ltd.
    Inventors: Masaaki Nagasawa, Kazuyasu Asami, Ryu Nakao, Nobuyuki Tanaka, Yoshiyuki Aida
  • Publication number: 20150093339
    Abstract: The present invention relates to the discovery that certain non-naturally occurring, non-peptide amide compounds and amide derivatives, such as oxalamides, ureas, and acrylamides, are useful flavor or taste modifiers, such as a flavoring or flavoring agents and flavor or taste enhancer, more particularly, savory (the “umami” taste of monosodium glutamate) or sweet taste modifiers,—savory or sweet flavoring agents and savory or sweet flavor enhancers, for food, beverages, and other comestible or orally administered medicinal products or compositions.
    Type: Application
    Filed: October 8, 2014
    Publication date: April 2, 2015
    Inventors: Catherine TACHDJIAN, Andrew P. PATRON, Sara L. ADAMSKI-WERNER, Farid BAKIR, Qing CHEN, Vincent DARMOHUSODO, Stephen Terrence HOBSON, Xiaodong LI, Ming QI, Daniel H. ROGERS, Marketa RINNOVA, Guy SERVANT, Xiao-Qing TANG, Mark ZOLLER, David WALLACE, Amy XING, Klaus GUBERNATOR
  • Publication number: 20150087836
    Abstract: 5-(Difluoromethyl)pyrazine-2-carboxilic acid, which is a raw material for the construction of 5-(difluoromethyl)pyrazine-2-carboxamide, which is a common partial structural motif of the compound having an A production inhibitory action or a BACE1 inhibitory action, can be industrially advantageously produced by decarboxylating 5-[carboxy(difluoro)methyl]pyrazine-2-carboxylic acid, which is obtainable from 5-chloropyrazine-2-carboxylate.
    Type: Application
    Filed: April 25, 2013
    Publication date: March 26, 2015
    Inventors: Kazuhiro Yoshizawa, Masayuki Omori, Yuzo Watanabe, Mitsuo Nagai, Masabumi Takahashi, Francis G. Fang
  • Patent number: 8969358
    Abstract: The present invention is directed to Buprenorphine Analog compounds of Formula I, II, III, IV or V and including various stereoisomers (such as Formula IA shown below), wherein R1, R3a, R3b, R16, R15, G, Q, X, A and Z are as defined herein. Compounds of the Invention may be useful for preparing medicaments useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors. Compounds of the Invention may be useful for treating Conditions such as pain, constipation, and others modulated by activity of opioid and ORL-1 receptors.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: March 3, 2015
    Assignee: Purdue Pharma L.P.
    Inventors: Richard Goehring, Laykea Tafesse, Jiangchao Yao
  • Publication number: 20150056305
    Abstract: Provided are dithiol mucolytic agents. These agents increase the liquefaction of mucus in a patient with excessive mucus or mucus with increased viscoelastic, cohesive, or adhesive properties. Also provided are a variety of methods of treatment using these inventive mucolytic agents.
    Type: Application
    Filed: August 13, 2014
    Publication date: February 26, 2015
    Applicant: PARION SCIENCES, INC.
    Inventors: Michael R. Johnson, William R. Thelin, Ronald A. Aungst, JR.
  • Publication number: 20150051396
    Abstract: The object of the present invention is to provide a compound which is useful as a production intermediate of pyrazine carboxamide derivative such as 6-fluoro-3-hydroxy-2-pyrazine carboxamide. The present invention provides a pyrazino[2,3-d]isoxazole derivative represented by the formula (I): wherein X represents a halogen atom, a hydroxyl group or a sulfamoyloxy group, and Y represents —C(?O)R or —CN; wherein R represents a hydrogen atom, an alkoxy group an aryloxy group, an alkyl group, an aryl group or an amino group.
    Type: Application
    Filed: October 29, 2014
    Publication date: February 19, 2015
    Applicants: TOYAMA CHEMICAL CO., LTD., FUJIFILM Corporation
    Inventors: Kouki NAKAMURA, Takeshi MURAKAMI, Hiroyuki NAITOU, Naoyuki HANAKI, Katsuyuki WATANABE
  • Publication number: 20150045312
    Abstract: Methods of treating autism, autistic spectrum disorders or Fragile X syndrome comprised of administering molecules that engage the cystine-glutamate exchange (System xc?) and/or elevate the extracellular levels of glutathione in the CNS. Preferred compounds are cysteine/cystine prodrugs or N-acetyl cysteine (NAC) prodrugs.
    Type: Application
    Filed: August 11, 2014
    Publication date: February 12, 2015
    Inventors: Michael Neary, Chad Beyer
  • Publication number: 20150038713
    Abstract: A preparation replete with crystals of a sodium salt of 6-fluoro-3-hydroxy-2-pyrazine carboxamide has superior solubility, and is useful as a preparation for injection.
    Type: Application
    Filed: October 16, 2014
    Publication date: February 5, 2015
    Applicant: Toyama Chemical Co., Ltd.
    Inventors: Keiko TAKAKURA, Namika Nakamatsu, Sakiko Takeshima, Sayuri Uehara
  • Publication number: 20150031885
    Abstract: A preparation replete with a meglumine salt of 6-fluoro-3-hydroxy-2-pyrazine carboxamide has superior solubility, and is useful as a preparation for injection.
    Type: Application
    Filed: October 7, 2014
    Publication date: January 29, 2015
    Applicant: TOYAMA CHEMICAL CO., LTD.
    Inventors: Keiko TAKAKURA, Namika NAKAMATSU, Sakiko TAKESHIMA, Takayoshi NAKASHIMA
  • Patent number: 8933102
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor. Formula (I).
    Type: Grant
    Filed: October 24, 2011
    Date of Patent: January 13, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gregori J. Morriello, Lehua Chang, Scott D. Edmondson
  • Patent number: 8921370
    Abstract: The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): wherein L, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: December 30, 2014
    Assignee: H. Lundbeck A/S
    Inventors: Guiying Li, Hao Zhou, Jesse Weiss, Dario Doller, James Ford Burns
  • Publication number: 20140350030
    Abstract: The present invention provides compounds of formula (I): where R1, R2, X, Y and n are as described herein, and pharmaceutical compositions, uses and methods comprising same.
    Type: Application
    Filed: September 17, 2012
    Publication date: November 27, 2014
    Inventors: Dario Doller, Guiying Li
  • Patent number: 8884009
    Abstract: The invention relates to processes of making bortezomib of formula (1) enantiomers thereof and/or intermediates thereof, comprising at least one step of coupling a carboxylic acid with an amine, wherein the coupling step is performed in a presence of the compound of formula (8), wherein A is C1-C6 alkyl group, preferably wherein A is n-propyl group.
    Type: Grant
    Filed: October 14, 2010
    Date of Patent: November 11, 2014
    Assignee: Synthon BV
    Inventors: Jakub Castulik, Miroslav Zabadal
  • Publication number: 20140323463
    Abstract: [Problem] A compound which is useful as an inhibitor on EGFR T790M mutation kinase activity is provided. [Means for Solution] The present inventors have investigated a compound having an inhibitory action on an EGFR T790M mutation kinase, and have found that a pyrazinecarboxamide compound has an inhibitory action on an EGFR T790M mutation kinase, thereby completing the present invention.
    Type: Application
    Filed: January 15, 2013
    Publication date: October 30, 2014
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Takahiro Matsuya, Yutaka Kondoh, Itsuro Shimada, Shigetoshi Kikuchi, Maiko Iida, Kenichi Onda, Hiroki Fukudome, Yukihiro Takemoto, Nobuaki Shindou, Hideki Sakagami, Hisao Hamaguchi
  • Patent number: 8871976
    Abstract: The invention includes a compound represented by the following structural formula: wherein is described herein. The compounds of the invention are useful in staining embryonic stem cells.
    Type: Grant
    Filed: August 26, 2011
    Date of Patent: October 28, 2014
    Assignees: National University of Singapore, Agency for Science, Technology and Research
    Inventors: Young-Tae Chang, Sung Chan Lee, Nam Young Kang
  • Patent number: 8859558
    Abstract: This present disclosure is related to the field of pyrazine carboxamides and their derivatives and the use of these compounds as fungicides.
    Type: Grant
    Filed: May 31, 2011
    Date of Patent: October 14, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Kristy Bryan, George E. Davis, Paul R. Graupner, Beth Lorsbach, W. John Owen, Francis E. Tisdell
  • Patent number: 8859768
    Abstract: This invention provides compounds of formula IA or IB: wherein HY, R1, R2, and G1, are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Grant
    Filed: August 10, 2011
    Date of Patent: October 14, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Courtney A. Cullis, Krista E. Granger, Jianping Guo, Masaaki Hirose, Gang Li, Miho Mizutani, Tricia J. Vos
  • Patent number: 8853205
    Abstract: Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or CB2 cannabinoid receptors. Aspects disclose hetero pyrrole analogs acting as CB1 and/or CB 1 receptor antagonists, having selectivity for the CB 1 or CB2 receptor, acting as neutral antagonists, acting preferentially on CB 1 receptors located in the peripheral nervous system, and/or acting as nitric oxide donors. Pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect are also disclosed.
    Type: Grant
    Filed: February 19, 2009
    Date of Patent: October 7, 2014
    Assignee: University of Connecticut
    Inventors: Alexandros Makriyannis, Venkata Kiran Vemuri
  • Publication number: 20140275117
    Abstract: The present invention is directed to Buprenorphine Analog compounds of Formula I, II, III, IV or V and including various stereoisomers (such as Formula IA shown below), wherein R1, R3a, R3b, R16, R15, G, Q, X, A and Z are as defined herein. Compounds of the Invention may be useful for preparing medicaments useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors. Compounds of the Invention may be useful for treating Conditions such as pain, constipation, and others modulated by activity of opioid and ORL-1 receptors.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: PURDUE PHARMA L.P.
    Inventors: Richard Goehring, Laykea Tafesse, Jiangchao Yao
  • Publication number: 20140275543
    Abstract: A method for stabilization of potent alkanone-heterocyclic flavorants in dry powder form is provided. Coordination of alkanone-heterocyclic flavorants to transition metal salts results in the formation of stable crystalline complexes, which upon hydration release the free flavorant. Food and topping products containing the stabilized alkanone-heterocyclic flavorant are provided as are methods for stabilizing the alkanone-heterocyclic flavorant.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Keith R. Cadwallader, Ming-Chih Fang
  • Patent number: 8815859
    Abstract: Arylpyrazinone derivatives of formula (I), as insulin secretion stimulators, the preparation and use of these pyrazinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.
    Type: Grant
    Filed: March 31, 2009
    Date of Patent: August 26, 2014
    Assignee: Merck Patent GmbH
    Inventors: Gérard Botton, Eric Valeur, Christine Charon, Micheline Kergoat, Samer Elbawab
  • Patent number: 8759353
    Abstract: The invention relates to compositions and co-crystals each comprising VX-950 and a co-crystal former selected from the group consisting of 4-hydroxybenzoic acid, 4-amino salicylic acid, phenylalanine, threonline, tartaric acid, adipic acid, succinic acetate, proline, methyl 4-hydroxybenzoate, anthranilic acid, and d-Biotin. Also within the scope of this invention are methods of making and using the same.
    Type: Grant
    Filed: February 27, 2008
    Date of Patent: June 24, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Patrick R. Connelly, Irina Kadiyala, Kathy Stavropoulos, Yuegang Zhang, Steven C. Johnston, Govinda Rao Bhisetti, Valdas Jurkauskas, Peter Rose
  • Patent number: 8759539
    Abstract: Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.
    Type: Grant
    Filed: November 11, 2009
    Date of Patent: June 24, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jiafang He, John Bawiec, Weiguo Liu, Gui-Bai Liang, Lihu Yang
  • Patent number: 8748471
    Abstract: Novel 2-alkylcycloalk(en)ylcarboxamides of the formula (I) in which X, s, R1, L, R2 and A are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.
    Type: Grant
    Filed: November 27, 2012
    Date of Patent: June 10, 2014
    Assignee: Bayer CropScience AG
    Inventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Benoit Hartmann, Herbert Gayer, Thomas Seitz, Ulrike Wachendorff-Neumann, Peter Dahmen, Karl-Heinz Kuck
  • Publication number: 20140148468
    Abstract: The invention relates to specific carboxamides, to processes for their preparation, to medicaments comprising these compounds and to the use of these compounds in the preparation of medicaments.
    Type: Application
    Filed: November 27, 2013
    Publication date: May 29, 2014
    Applicant: GRÜNENTHAL GMBH
    Inventors: Simon LUCAS, Sven Kühnert, Gregor Bahrenberg, Wolfgang Schröder
  • Patent number: 8686145
    Abstract: The present invention relates to a process for the preparation of a compound of the general Formula (I), comprising: a) reacting a compound of the general Formula (II) with a compound of the Formula III R2COOH and a compound of the general Formula IV R3NC under such conditions that compound I is formed, wherein R1 represents a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R2 represents a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R3 represents a substituted or unsubstituted alkyl, alkenyl, or alkynyl structure. In further aspect the subject invention relates to the use of the obtained products as intermediates for various peptidomimetics, and preferably as a building block in a convergent synthesis of prolyl dipeptide structures.
    Type: Grant
    Filed: September 16, 2010
    Date of Patent: April 1, 2014
    Assignee: Vereniging Voor Christelijk Hoger Onderwijs, Wetenschappelijk Onderzoek en Patientenzorg C/O Technology Transfer Officer VU & Vumc
    Inventors: Eelco Ruijter, Romano Orru, Anass Znabet, Marloes Polak, Nicholas Turner
  • Patent number: 8686154
    Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.
    Type: Grant
    Filed: June 10, 2009
    Date of Patent: April 1, 2014
    Assignee: Emisphere Technologies, Inc.
    Inventors: Donald J. Sarubbi, Eugene N. Barantsevitch
  • Patent number: 8680100
    Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.
    Type: Grant
    Filed: December 1, 2009
    Date of Patent: March 25, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
  • Publication number: 20140066420
    Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.
    Type: Application
    Filed: October 16, 2013
    Publication date: March 6, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Shizuo KASAI, Tomohiro KAKU, Masahiro KAMAURA
  • Patent number: 8664392
    Abstract: Provided are compounds and compositions of general Formula IX: E1-L-Ar—X-PA, that may be utilized in bioconjugation procedures, where Ar is a chromophore and PA is a functional group capable of being attached to any bioactive molecule of interest. The present invention provides Formulas I-III that are capable of being attached to a bioactive vector for the selective delivery of said photoactive pyrazine derivatives to a desired biological target.
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: March 4, 2014
    Assignee: MediBeacon, LLC
    Inventors: Raghavan Rajagopalan, Richard B. Dorshow
  • Publication number: 20140058104
    Abstract: Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions.
    Type: Application
    Filed: October 29, 2013
    Publication date: February 27, 2014
    Applicant: ZERIA PHARMACEUTICAL CO., LTD.
    Inventors: Masaaki NAGASAWA, Kazuyasu Asami, Ryu Nakao, Nobuyuki Tanaka, Yoshiyuki Aida
  • Publication number: 20140031370
    Abstract: A compound represented by Formula (1): The compound can be used as insecticides.
    Type: Application
    Filed: September 20, 2013
    Publication date: January 30, 2014
    Applicant: MITSUI CHEMICALS, INC.
    Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba
  • Patent number: 8629273
    Abstract: The present invention relates to diazinylpyrazolyl compounds of the formula (I) where R1 to R3, X and Q are as defined in the description, and to their use in crop protection, in particular as insecticides, and also to processes for their preparation and compositions comprising such diazinylpyrazolylimines and -imidoates.
    Type: Grant
    Filed: November 11, 2010
    Date of Patent: January 14, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Hans-Georg Schwarz, Robert Velten, Achim Hense, Simon Maechling, Stefan Werner, Bernd Alig, Eva-Maria Franken, Arnd Voerste, Ulrich Görgens
  • Patent number: 8618292
    Abstract: Compounds represented by the following structure (II) are disclosed: as are methods for making such compounds. Compositions and methods for treating various disease conditions including cancer and non-cancer diseases associated with vascular proliferation are also disclosed.
    Type: Grant
    Filed: July 12, 2012
    Date of Patent: December 31, 2013
    Assignee: Beyondspring Pharmaceuticals, Inc.
    Inventors: Michael Palladino, George Kenneth Lloyd, Yoshio Hayashi
  • Patent number: 8580142
    Abstract: The invention provides a liquid crystal compound having stability to heat, light and so forth, a wide temperature range of a nematic phase, a small viscosity, a suitable optical anisotropy, a suitable elastic constant K33, a suitable and negative dielectric anisotropy, and an excellent compatibility with other liquid crystal compounds. The invention provides a liquid crystal composition containing the compound described above and having stability to heat, light and so forth, a small viscosity, a suitable optical anisotropy, a suitable and negative dielectric anisotropy, a suitable elastic constant K33, a low threshold voltage, a high maximum temperature of a nematic phase, and a low minimum temperature of the nematic phase. The invention also provides a liquid crystal display device having a short response time, a small power consumption, a low driving voltage, and a large contrast, and containing the composition described above which can be used in a large temperature range.
    Type: Grant
    Filed: September 1, 2008
    Date of Patent: November 12, 2013
    Assignees: JNC Corporation, JNC Petrochemical Corporation
    Inventors: Teru Shimada, Masahide Kobayashi
  • Patent number: 8569301
    Abstract: The present invention relates to 6,6-dioxo-6-thia-1,4-diaza-naphthalene derivatives of formula (I) where R1, R2, R3a, R3b, R4 and R5 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for making compounds of formula (I), to herbicidal compositions comprising compounds of formula (I) and to methods of using compounds of formula (I) to control plant growth.
    Type: Grant
    Filed: May 6, 2010
    Date of Patent: October 29, 2013
    Assignee: Syngenta Limited
    Inventors: Nigel James Willetts, Nicholas Phillip Mulholland, Paul Anthony Worthington, Alaric James Avery
  • Publication number: 20130274472
    Abstract: A preparation replete with crystals of a sodium salt of 6-fluoro-3-hydroxy-2-pyrazine carboxamide has superior solubility, and is useful as a preparation for injection.
    Type: Application
    Filed: September 29, 2011
    Publication date: October 17, 2013
    Applicant: TOYAMA CHEMICAL CO., LTD.
    Inventors: Keiko Takakura, Namika Nakamatsu, Sakiko Takeshima, Sayuri Uehara
  • Publication number: 20130261133
    Abstract: The compounds of the invention exhibit antiprotozoal, antimicrobial, and anticancer properties that are useful for the treatment or prevention of infections or cancer in a patient (e.g., a human). For example, the compounds and methods described herein can be used for the treatment or prevention of protozoal infections such as leishmaniasis, malaria, and trypanosoma infections, bacterial infections such as S. aureus and C. albicans, and cancers such as breast, colon, lung, or prostate cancer. The invention further provides methods of synthesizing such compounds as well as kits useful for administering the compounds.
    Type: Application
    Filed: March 14, 2013
    Publication date: October 3, 2013
    Applicant: The University of Montana
    Inventors: John Howard Hoody, David Brian Bolstad
  • Publication number: 20130261122
    Abstract: The present invention is directed to novel substituted bicyclic aromatic compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
    Type: Application
    Filed: December 16, 2011
    Publication date: October 3, 2013
    Applicant: N30 Pharmaceuticls, Inc.
    Inventors: Xicheng Sun, Jian Qiu, Adam Stout
  • Publication number: 20130252974
    Abstract: The present invention relates to 5,6-bisaryl-2-pyridinecarboxamides, to their preparation and to their therapeutic use as urotensin II receptor antagonists.
    Type: Application
    Filed: May 15, 2013
    Publication date: September 26, 2013
    Applicant: SANOFI
    Inventors: Jean-Michel Altenburger, Valerie Fossey, Daniel Galtier, Frederic Petit
  • Patent number: 8536198
    Abstract: The present application describes modulators of MIP-1 of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as set forth above. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators are disclosed.
    Type: Grant
    Filed: July 23, 2008
    Date of Patent: September 17, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Joseph B. Santella, John Hynes, Daniel S. Gardner
  • Publication number: 20130224790
    Abstract: The invention includes a compound represented by the following structural formula: wherein is described herein. The compounds of the invention are useful in staining embryonic stem cells.
    Type: Application
    Filed: August 26, 2011
    Publication date: August 29, 2013
    Applicants: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH, NATIONAL UNIVERSITY OF SINGAPORE
    Inventors: Young-Tae Chang, Sung Chan Lee, Nam Young Kang
  • Publication number: 20130217708
    Abstract: A preparation replete with a meglumine salt of 6-fluoro-3-hydroxy-2-pyrazine carboxamide has superior solubility, and is useful as a preparation for injection.
    Type: Application
    Filed: September 29, 2011
    Publication date: August 22, 2013
    Applicant: Toyama Chemical Co., Ltd.
    Inventors: Keiko Takakura, Namika Nakamatsu, Sakiko Takeshima, Takayoshi Nakashima
  • Patent number: 8513261
    Abstract: Disclosed is a useful tablet which contains a high quantity of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or a salt thereof; has a size that is easy to ingest; has superior release characteristics; and has a hardness that can withstand film coating, packaging, and transportation.
    Type: Grant
    Filed: March 12, 2010
    Date of Patent: August 20, 2013
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Sahoe Kakuda, Setsuko Nishimura, Takafumi Hirota
  • Publication number: 20130203988
    Abstract: The invention relates to processes of making bortezomib of formula (1) enantiomers thereof and/or intermediates thereof, comprising at least one step of coupling a carboxylic acid with an amine, wherein the coupling step is performed in a presence of the compound of formula (8), wherein A is C1-C6 alkyl group, preferably wherein A is n-propyl group.
    Type: Application
    Filed: October 14, 2010
    Publication date: August 8, 2013
    Applicant: Synthon BV
    Inventors: Jakub Castulik, Miroslav Zabadal
  • Publication number: 20130197226
    Abstract: The present invention features pharmaceutical compositions and methods of using the pharmaceutical compositions for treating left ventricular diastolic dysfunction. In particular, the pharmaceutical compositions include an apolipoprotein complex comprising a lipid fraction and a protein fraction.
    Type: Application
    Filed: July 19, 2011
    Publication date: August 1, 2013
    Inventors: Jean-Claude Tardif, David Busseuil, Éric Rhéaume
  • Patent number: 8497374
    Abstract: A synthetic process for producing bortezomib comprising converting racemic boronic esters, such as the pinacol ?-aminoboronic ester, into mixtures of diastereomers [6] by reaction with a suitably protected L-phenylalanine derivative (see Scheme 3), such as N—BOC-L-phenylalanine. The protecting group of the L-phenylalanine moiety is then removed, such as by reacting the diastereomers [6] with an acid, such as hydrochloric acid, to form a mixture of amine salt diastereomers [7] which is then subjected to conditions under which the desired diastereomer (R,S)-[7] is selectively isolated, such as by crystallization, chromatography or stereoselective hydrolysis. The separated desired diastereomer (R,S)-[7] is then converted into bortezomib or bortezomib anhydride.
    Type: Grant
    Filed: May 12, 2011
    Date of Patent: July 30, 2013
    Assignee: Scinopharm Taiwan, Ltd.
    Inventors: Julian Paul Henschke, Aiping Xie, Xin Yan Huang, Yung Fa Chen
  • Publication number: 20130172367
    Abstract: Novel 2-alkylcycloalk(en)ylcarboxamides of the formula (I) in which X, s, R1, L, R2 and A are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.
    Type: Application
    Filed: November 27, 2012
    Publication date: July 4, 2013
    Applicant: BAYER CROPSCIENCE AG
    Inventor: Bayer CropScience AG