Nitrogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/304)
  • Patent number: 11186565
    Abstract: Provided is a novel aromatic ring compound which may have a GPR40 agonist activity and a GLP-1 secretagogue action. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof may have a GPR40 agonist activity and a GLP-1 secretagogue action, may be useful for the prophylaxis or treatment of cancer, obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia and the like, and may afford superior efficacy.
    Type: Grant
    Filed: March 29, 2018
    Date of Patent: November 30, 2021
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Seiji Miwatashi, Yasufumi Miyamoto, Koji Watanabe, Yayoi Nakayama, Yuko Hitomi, Jumpei Aida, Nobuyuki Takakura, Hideki Furukawa, Naoyoshi Noguchi, Yasuhiro Hirata, Kazuaki Takami, Norihito Tokunaga, Tomohiro Okawa, Akito Shibuya, Shizuo Kasai, Toshitake Kobayashi, Tsuyoshi Maekawa
  • Patent number: 10975065
    Abstract: The present invention relates to N-substituted-dioxocyclobutenylamino-3-hydroxy-picolinamide compounds of Formulae (IA and 1B) or a pharmaceutically acceptable salt or hydrate thereof, that inhibit CC chemokine receptor 6 (CCR6), pharmaceutical compositions containing these compounds, and the use of these compounds for treating or preventing diseases, conditions, or disorders ameliorated by inhibition of CCR6.
    Type: Grant
    Filed: September 20, 2019
    Date of Patent: April 13, 2021
    Assignee: Pfizer Inc.
    Inventors: Brian Stephen Gerstenberger, Andrew Christopher Flick, Vincent Michael Lombardo, James John Mousseau, Philippe Marcel Nuhant, Ralph Pelton Robinson, Jr., Mark Edward Schnute, Daniel Wei-Shung Kung, Daniel Copley Schmitt, Atli Thorarensen, John Isidro Trujillo, Rayomand Jal Unwalla, Huixian Wu
  • Patent number: 10660333
    Abstract: The present invention relates to compounds of the general formula (I) in which Q, V, T, W, Y, X and A have the meanings given in the description—and to a process for preparation thereof and to the use thereof for controlling animal pests.
    Type: Grant
    Filed: August 4, 2017
    Date of Patent: May 26, 2020
    Assignee: Bayer CropScience Aktiengesellschaft
    Inventors: Matthieu Willot, Reiner Fischer, Markus Heil, Johannes-Rudolf Jansen, Kerstin Ilg, Daniela Portz
  • Patent number: 10428041
    Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
    Type: Grant
    Filed: November 14, 2018
    Date of Patent: October 1, 2019
    Assignee: NOVIRA THERAPEUTICS, INC.
    Inventors: Ryan C. Clark, Yen Truong, Nicholas Stock, Jason Jacintho
  • Patent number: 10214522
    Abstract: Provided herein, inter alia, are methods and compositions for inhibiting ?v?1 integrin and for treating fibrosis.
    Type: Grant
    Filed: March 10, 2016
    Date of Patent: February 26, 2019
    Assignee: The Regents of the University of California
    Inventors: William F. DeGrado, Dean Sheppard, Hyunil Jo, Nilgun Isik Reed, Youzhi Tang, Joel McIntosh
  • Patent number: 9920071
    Abstract: An object of the present invention is to provide a novel method for producing a compound, a salt thereof, or a hydrate of the compound or the salt, which is an FXa inhibitor. The object can be attained by a production method in which a production method via a compound represented by formula (1-1), etc., from a compound represented by the following formula (1-x), etc., is used for a method for producing a compound represented by the following formula (X), etc. [wherein X represents a halogen atom or the like, and R1 represents an optionally substituted phenyl group].
    Type: Grant
    Filed: February 13, 2015
    Date of Patent: March 20, 2018
    Assignee: Daiichi Sankyo Company, Limited
    Inventor: Tsuyoshi Ueda
  • Patent number: 9833445
    Abstract: The invention provides 5-deuterium-enriched 2,4-thiazolidinediones (e.g., 5-[4-[2-(5-ethyl-2-pyridyl)-2-oxoethoxy]benzyl]-5-deutero-thiazolidine-2,4-dione), deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treatment using the same.
    Type: Grant
    Filed: August 2, 2016
    Date of Patent: December 5, 2017
    Assignee: DEUTERX, LLC
    Inventor: Sheila DeWitt
  • Patent number: 9556129
    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: July 29, 2015
    Date of Patent: January 31, 2017
    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: 9051270
    Abstract: The invention relates to pyridone amide compounds of formula I and I? or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain.
    Type: Grant
    Filed: January 29, 2014
    Date of Patent: June 9, 2015
    Assignee: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Sabina Hadida-Ruah, Corey Anderson, Vijayalaksmi Arumugam, Iuliana Luci Asgian, Brian Richard Bear, Andreas P. Termin, James Philip Johnson
  • Patent number: 9029386
    Abstract: Derivatives of pyridine of the formula wherein one of Y and A is CR and the other is N are kinase inhibitors useful in treating conditions associated with excess kinase activity.
    Type: Grant
    Filed: January 22, 2013
    Date of Patent: May 12, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Christopher John Burns, Michael Francis Harte, James T. Palmer
  • Patent number: 9006451
    Abstract: The present invention provides a compound of general formulae A useful as potential antitumor agents against human cancer cell lines and a process for the preparation thereof.
    Type: Grant
    Filed: February 25, 2014
    Date of Patent: April 14, 2015
    Assignee: Council of Scientific and Industrial Research
    Inventors: Ahmed Kamal, Mohammed Ashraf, Shaikh Faazil Bagwan, Yellamelli Valli Venkata Srikanth, Syed Mohammed Ali Hussaini, Adla Malla Reddy
  • Patent number: 8993258
    Abstract: A fluorinated voltage sensitive dye has the structure wherein p is 0, 1, or 2; Xq? is an anionic counterion having a charge, q, that is 1 or 2; n is 1 or 2; R1 is an optionally substituted C1-C12, alkyl; R2 is hydrogen, and R3 is hydrogen or fluorine; or R2 and R3 collectively form a divalent —CH?CH—CH?CH— group; R4 and each occurrence of R5 are each independently hydrogen or fluorine; R6 is hydrogen or fluorine or trifluoromethyl; and each occurrence of R7 is independently C1-C6 alkyl; provided that the dye comprises at least one fluorine atom. The dye is particularly useful for monitoring the dynamics of action potentials in axons and/or dendrites.
    Type: Grant
    Filed: June 3, 2013
    Date of Patent: March 31, 2015
    Assignee: The University of Connecticut
    Inventors: Ping Yan, Corey D. Acker, Leslie M. Loew
  • Publication number: 20150051245
    Abstract: The invention relates to protein binding inhibitor compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating cell proliferative disorders, especially cancer.
    Type: Application
    Filed: November 13, 2012
    Publication date: February 19, 2015
    Inventors: William G. Cance, Ravindra K. Pandey, Elena V. Kurenova, Manivannan Ethirajan
  • Patent number: 8946437
    Abstract: The present invention provides a novel compound having an excellent antitumor effect, stability and metabolic stability. The compound of the present invention is represented by the following general formula (1) wherein R1 represents a halogen atom, an aryl group, an aryloxy group or a lower alkyl group optionally substituted with one or more halogen atoms; R2 represents hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group; and; m represents an integer of 1 to 3; provided that when m represents 2 or 3, R1s are the same or different.
    Type: Grant
    Filed: October 3, 2011
    Date of Patent: February 3, 2015
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Takashi Nakagawa, Makoto Sakamoto, Kazuya Yamaguchi, Yuki Terauchi, Masamichi Shirakura, Yasuo Harada, Yutaka Kojima, Takumi Sumida
  • Patent number: 8933106
    Abstract: The invention relates to 2-(4-Substituted phenylamino) polysubstituted pyridine compounds as inhibitors of non-nucleoside HIV reverse transcriptase, preparation methods and uses thereof. Specifically, the invention relates to compounds of formula I or the pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined in the description. The compounds of formula I of the invention are a type of anti-HIV active compounds having new backbone structure.
    Type: Grant
    Filed: September 28, 2009
    Date of Patent: January 13, 2015
    Assignee: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
    Inventors: Lan Xie, Xingtao Tian, Kuo-Hsiung Lee, Shibo Jiang, Hong Lu
  • Patent number: 8895738
    Abstract: Disclosed are compounds of Formula 1, wherein R1 is phenyl or pyridinyl, each optionally substituted with Q and up to 3 substituents independently selected from R2; each R2 is independently halogen, cyano, SF5, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkylthio or C1-C4 haloalkylthio; and Q is phenyl or pyridinyl, each optionally substituted with up to 5 substituents independently selected from the group consisting of halogen, cyano, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy and C1-C4 haloalkoxy. 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: Grant
    Filed: December 22, 2011
    Date of Patent: November 25, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventor: Thomas Francis Pahutski, Jr.
  • Publication number: 20140326961
    Abstract: Provided are benzofluorene-based compounds according to the following Formula 1 and an organic light-emitting diode including the same:
    Type: Application
    Filed: October 1, 2013
    Publication date: November 6, 2014
    Applicant: Samsung Display Co., LTD.
    Inventors: Sang-Hyun Han, Seok-Hwan Hwang, Young-Kook Kim, Hye-Jin Jung, Jin-O Lim, Soo-Yon Kim, Eun-Jae Jeong, Jun-Ha Park, Eun-Young Lee, Jong-Hyuk Lee
  • Patent number: 8865908
    Abstract: Process for the preparation of a N-[2-(2-pyridinyl)ethyl]carboxamide derivative of general formula (I) or a salt thereof Intermediate of general formula (II) Intermediate of general formula (III)
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: October 21, 2014
    Assignee: Bayer Cropscience AG
    Inventors: Frederic Lhermitte, Pierre-Yves Coqueron, Philippe Desbordes, Thomas Himmler
  • Patent number: 8859559
    Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
    Type: Grant
    Filed: December 18, 2012
    Date of Patent: October 14, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Armin Heckel, Andreas Blum, Dieter Hamprecht, Joerg Kley
  • Patent number: 8859594
    Abstract: Disclosed are a polymorphs I-VI of N-(6-(4-chlorophenoxy)hexyl)-N?-cyano-N?-(4-pyridyl)guanidine or of a solvate thereof, a preparation method thereof, and a use thereof as a biological active ingredient. The polymorphs are useful in treatment of cancers, and diseases or disorders caused by abnormal cell proliferation.
    Type: Grant
    Filed: October 25, 2011
    Date of Patent: October 14, 2014
    Assignees: Tianjin Hemay Bio-Tech Co., Ltd., Tianjin Michele Sci-Tech Development Co., Ltd.
    Inventors: Hesheng Zhang, Xin Chen
  • Publication number: 20140291646
    Abstract: A pyrene-based compound and an organic light-emitting diode including the same, the pyrene-based compound being represented by Formula 1, below:
    Type: Application
    Filed: March 25, 2014
    Publication date: October 2, 2014
    Applicant: Samsung Display Co., Ltd.
    Inventors: Dong-Woo SHIN, O-Hyun KWON, Mie-Hwa PARK, Seul-Ong KIM, Byoung-Ki CHOI
  • Patent number: 8846948
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3, R3a have meanings given in the description.
    Type: Grant
    Filed: December 7, 2012
    Date of Patent: September 30, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Klaus Rudolf, Daniel Bischoff, Georg Dahmann, Matthias Grauert, Raimund Kuelzer
  • Patent number: 8846922
    Abstract: The present invention relates to functionalized fluoroalkylfluorophosphate salts, in particular as ionic liquids, to the preparation thereof and to the use thereof.
    Type: Grant
    Filed: August 30, 2011
    Date of Patent: September 30, 2014
    Assignee: Merck Patent GmbH
    Inventors: Berthold Theo Hoge, Anne Julia Bader, Nikolai Mykola Ignatyev, Michael Schulte, Wolfgang Hierse, Waldemar Wiebe, Helge Willner
  • Patent number: 8840866
    Abstract: This invention relates to a method of imaging amyloid deposits and to styrylpyridine compounds, and methods of making radiolabeled styrylpyridine compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.
    Type: Grant
    Filed: January 7, 2013
    Date of Patent: September 23, 2014
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Hank F. Kung, Mei-Ping Kung
  • Publication number: 20140273250
    Abstract: Provided herein are methods for selectively detecting an alkyne-presenting molecule in a sample and related detection reagents, compositions, methods and systems.
    Type: Application
    Filed: March 7, 2014
    Publication date: September 18, 2014
    Applicant: LAWRENCE LIVERMORE NATIONAL SECURITY, LLC
    Inventors: Carlos A. VALDEZ, Audrey M. WILLIAMS
  • Patent number: 8796467
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
    Type: Grant
    Filed: December 7, 2012
    Date of Patent: August 5, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Klaus Rudolf, Daniel Bischoff, Georg Dahmann, Matthias Grauert, Raimund Kuelzer, Bernd Wellenzohn
  • Publication number: 20140213598
    Abstract: Disclosed is a substituted cyanoaniline compound or a salt thereof, wherein the compound has a structure represented by General Formula I. The compound of General Formula I has broad-spectrum fungicidal activity in the field of agriculture and effectively prevents against a variety of pathogens such as cucumber downy mildew, wheat powdery mildew, maize rust disease, rice blast and cucumber gray mold. In particular, even at a low dose, the compound effectively prevents and treats rice blast, cucumber gray mold, maize rust disease and cucumber downy mildew. Moreover, the raw materials for preparing the compounds are widely available and the synthesis method therefor is simple and convenient.
    Type: Application
    Filed: June 15, 2012
    Publication date: July 31, 2014
    Applicants: SHENYANG RESEARCH INSTITUTE OF CHEMICAL INDUSTRY CO., LTD., SINOCHEM CORPORATION
    Inventors: Changling Liu, Guang Huang, Jie Lan, Shulin Hao, Zhinian Li, Huichao Li, Aiying Guan, Airu Jiang, Ying Xu
  • 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: 8785648
    Abstract: The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula I or II or a stereoisomer, tautomer, racemic, metabolite, pro- or pre-drug, salt, hydrate, or solvate thereof, wherein Ar, Cy, R1, R3, p and n have the meaning defined in the claims. In particular, the present invention relates to more specifically AGC kinases inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease.
    Type: Grant
    Filed: December 29, 2011
    Date of Patent: July 22, 2014
    Assignee: The Regents of the University of California
    Inventors: Robert Owen Messing, Michael A. Pleiss
  • Patent number: 8754226
    Abstract: Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which X1, X2, L, R3, R4, R5, R6, R6a, R7, R9, R9a, and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.
    Type: Grant
    Filed: May 13, 2011
    Date of Patent: June 17, 2014
    Assignee: Array BioPharma Inc.
    Inventors: Thomas Daniel Aicher, Josef Roland Bencsik, Kevin Ronald Condroski, Jay Bradford Fell, John P. Fischer, Ronald Jay Hinklin, Scott Alan Pratt, Ajay Singh, Timothy M. Turner, David A. Mareska, Steven Armen Boyd
  • Patent number: 8754110
    Abstract: Methods of producing methyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate. One method comprises adding methyl isobutyl ketone to an aqueous solution comprising 4-chloro-2-fluoro-3-methoxyphenyl-boronic acid to form an organic phase comprising the 4-chloro-2-fluoro-3-methoxyphenylboronic acid and an aqueous phase. The organic phase and the aqueous phase are separated. The 4-chloro-2-fluoro-3-methoxyphenylboronic acid is reacted with methyl 4-(acetylamino)-3,6-dichloropyridine-2-carboxylate in methyl isobutyl ketone to produce methyl 4-(acetylamino)-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate, which is deacetylated to produce methyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: June 17, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Jossian Oppenheimer, Mark V. M. Emonds, Christopher W. Derstine, Robert C. Clouse
  • Patent number: 8748445
    Abstract: The present disclosure provides for method of treatment and/or prevention of disease states that require cystine for maintenance or progression of the disease state. In addition, methods for screening and identifying novel therapeutic agents useful in the treatment of such disease states are described. In one embodiment, the disease state is a cancer, such as, but not limited to, glioma. In this embodiment, methods for the treatment and prevention of glioma by inhibiting cystine uptake or decreasing intracellular cystine concentrations are provided. The present disclosure teaches that glioma cells are dependent on system Xc for cystine uptake. Pharmacological inhibition of system Xc causes a rapid depletion of intracellular glutathione, resulting in decreased cell growth. In contrast, non-malignant astrocytes and cortical neurons remain viable in the presence of Xc inhibitors and continue to take up cystine via alternate amino acid transporters.
    Type: Grant
    Filed: October 27, 2005
    Date of Patent: June 10, 2014
    Assignee: The UAB Research Foundation
    Inventors: W. Joon Chung, Harald Sontheimer
  • Patent number: 8735593
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
    Type: Grant
    Filed: March 5, 2013
    Date of Patent: May 27, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Juan-Miguel Jimenez, Philip Collier, Jeremy Green, Gregory Henkel, Michael Liu, Timothy Neuberger
  • Publication number: 20140138632
    Abstract: An amine-based compound and an organic light-emitting diode including the amine-based compound are provided. The amine-based compound may be used between a pair of electrodes of an organic light-emitting diode. For example, the amine-based compound may be used in an emission layer and/or between the emission layer and an anode (for example, in a hole injection layer, a hole transport layer, a functional layer having a hole injection ability and a hole transport ability). Accordingly, an organic light-emitting diode including a first electrode, a second electrode facing the first electrode, and an organic layer that is interposed between the first electrode and the second electrode, and includes the amine-based compound is provided.
    Type: Application
    Filed: March 13, 2013
    Publication date: May 22, 2014
    Inventors: Young-Kook Kim, Seok-Hwan Hwang, 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: 8716421
    Abstract: This invention discloses and claims a series of polycyclic monomers and polymers useful in the production of optical waveguides. The polymers of the invention comprise one or more repeating units represented by the formula (IV): Wherein m, X, R1 and R2 are as defined herein. The films formed from the polymers of this invention exhibit significant changes in refractive index (greater than or equal to 0.5%) after exposure to suitable actinic or thermal energy thereby having superior optical transmission performance, which is of importance for modern optical applications such as wave guiding and optical data storage.
    Type: Grant
    Filed: May 23, 2013
    Date of Patent: May 6, 2014
    Assignees: Promerus, LLC, Sumitomo Bakelite Co., Ltd
    Inventors: Kazuyoshi Fujita, Nanae Kawate, Mari Ueda, Larry F Rhodes
  • Patent number: 8697721
    Abstract: The present applications discloses novel 8-aza-bicyclo[3.2.1]oct-3-yloxy)-chromen-2-one derivatives and their use as monoamine neurotransmitter re-uptake inhibitors. In other aspects the applications discloses the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Grant
    Filed: May 6, 2010
    Date of Patent: April 15, 2014
    Assignee: Aniona APS
    Inventors: Dan Peters, Elsebet Østergaard Nielsen, Karin Sandager Nielsen, Gordon Munro
  • Patent number: 8697744
    Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, Y, Z1, Z2, Z3, M and (A)m are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
    Type: Grant
    Filed: January 12, 2010
    Date of Patent: April 15, 2014
    Assignee: Addex Pharma S.A.
    Inventors: Christelle Boléa, Sylvain Celanire
  • Patent number: 8697733
    Abstract: The present invention relates to novel pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: June 20, 2013
    Date of Patent: April 15, 2014
    Assignee: Allergan, Inc.
    Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha-Bin Im
  • Publication number: 20140099249
    Abstract: Monosubstituted oxalic acid derivatives of the general formula (I) [A]+[O—C(O)—C(O)—O—X???(I) Wherein the meaning is for [A]+ a cation made from an organic moiety A having a formally positively charged heteroatom selected from the group consisting of nitrogen, phosphorus and sulfur X is a C1 to C30 organic residue and wherein the following compounds (I) are disclaimed: Tetramethylammonium monomethyloxalate Methyltri(alkyl)ammonium monomethyloxalate Trimethyl(1-hydroxyethyl)ammonium monomethyloxalate Methyltriethylammonium monomethyloxalate Tetraethylammonium monomethyloxalate n-Propyltriethylammonium mono-n-propyloxalate n-Butyltriethylammonium mono-n-butyloxalate Benzyltriethylammonium monobenzyloxalate cyclohexyldimethylammonium monomethyloxalate Dimethyl-phenylammonium monomethyloxalate.
    Type: Application
    Filed: October 9, 2013
    Publication date: April 10, 2014
    Applicant: BASF SE
    Inventors: Klemens Massonne, Joerg Sundermeyer, Axel Braam
  • Patent number: 8680136
    Abstract: Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to 1 cyclic boronic acid ester derivatives and their use as therapeutic agents.
    Type: Grant
    Filed: August 8, 2011
    Date of Patent: March 25, 2014
    Assignee: Rempex Pharmaceuticals, Inc.
    Inventors: Gavin Hirst, Raja Reddy, Scott Hecker, Maxim Totrov, David C. Griffith, Olga Rodny, Michael N. Dudley, Serge Boyer
  • Patent number: 8674099
    Abstract: The invention relates to compounds of formula (I) wherein the substituents are as defined in the specification, in free form or in the form of a pharmaceutically acceptable salt, solvate, ester, N-oxide thereof; processes for the preparation thereof; to pharmaceuticals containing such compounds, in particular for the use in one or more Protein tyrosine kinase mediated diseases.
    Type: Grant
    Filed: August 16, 2012
    Date of Patent: March 18, 2014
    Assignee: Novartis AG
    Inventors: Pascal Furet, Diana Graus Porta, Vito Guagnano
  • Patent number: 8669257
    Abstract: The present invention provides compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein each of W, Q, R1, R2, R3, R4, R5, m, and n is as defined herein, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: March 22, 2010
    Date of Patent: March 11, 2014
    Assignee: The Johns Hopkins University
    Inventors: Jun O. Liu, Yunzhao Ren, Fan Pan, Curtis R. Chong, Reinhold Penner, Jonathan R. Behr
  • Patent number: 8669209
    Abstract: Soluble granule formulations of amine salts of pyridine containing carboxylic acids with improved handling properties are provided by an improved process in which the pyridine containing carboxylic acid is partially neutralized with an amine.
    Type: Grant
    Filed: November 22, 2010
    Date of Patent: March 11, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Franklin N. Keeney, Neil A. Foster, Martin C. Logan, Maria G. Perry
  • Patent number: 8648203
    Abstract: The present invention relates to an improved process for the synthesis and purification of 3-chloro-N-(3-chloro-5-tri-fluoromethyl-2-pyridyl)-?,?,?-trifluoro-2,6-di-nitro-p-toluidine (fluazinam) and other pyridinamines, which implements methyl isobutyl ketone (MIBK) as the reaction solvent. The process of the invention overcomes the drawbacks of prior art methods, by reducing the side reactions such as hydrolysis, eliminating the need for difficult and labor-intensive purification methods, and providing pure products in higher yields. The present invention relates to novel crystalline polymorphic forms fluazinam, and to mixtures of the polymorphs. The present invention also provides methods for preparing the novel polymorphs, as well as pharmaceutical compositions comprising same, and methods of using the polymorphs as pesticidal agents for combating noxious living organisms on agricultural and horticultural crops.
    Type: Grant
    Filed: April 11, 2012
    Date of Patent: February 11, 2014
    Assignee: Makhteshim Chemical Works Ltd.
    Inventors: Shlomi Cohen, Sharona Zamir
  • Patent number: 8648202
    Abstract: The invention relates to bis(perfluoroalkyl)phosphinous acids, bis(perfluoroalkyl)thiophosphinous acids and derivatives, the synthesis thereof and the use thereof, in particular for the synthesis of air-stable metal complexes for catalytic processes.
    Type: Grant
    Filed: July 10, 2009
    Date of Patent: February 11, 2014
    Assignee: Merck Patent GmbH
    Inventors: Berthold Hoge, Anne Julia Bader, Boris Kurscheid, Nikolai (Mykola) Ignatyev, Emil Ferdinand Aust
  • Publication number: 20140039181
    Abstract: The invention relates to a method for producing a N-substituted amine compound by catalyzed alkylation. The method uses amine and alcohol or two kinds of amines as the reaction materials, employs composite metal oxides catalyst at a reaction temperature of 80-180° C. to catalyze the reaction for 6-36 hours, so as to produce the N-substituted amine compound. The reaction condition of the method of the invention is relatively moderate, using a catalyst made of cheap non-noble metals, which is non-caustic and easy to be separated and reused. The reaction does not need any medium and has relatively high conversion rate and selectivity.
    Type: Application
    Filed: December 28, 2012
    Publication date: February 6, 2014
    Applicant: Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences
    Inventor: Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences
  • Patent number: 8623942
    Abstract: The present invention provides a liquid curable epoxy resin composition that has excellent storage stability and curing properties and provides a cured product having excellent properties, particularly, excellent organic solvent resistance. For that purpose, a clathrate containing a carboxylic acid compound and at least one selected from the group consisting of an imidazole compound represented by formula (I), wherein R1 to R4 each represent a hydrogen atom or the like, and 1,8-diazabicyclo[5.4.0]undecene-7 (DBU) is mixed in an epoxy resin. The liquid curable epoxy resin composition uses a liquid epoxy resin or an organic solvent.
    Type: Grant
    Filed: March 9, 2010
    Date of Patent: January 7, 2014
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Masami Kaneko, Kazuo Ono, Natsuki Amanokura, Naoyuki Kamegaya
  • Patent number: 8618131
    Abstract: This invention provides biphenyl derivatives of formula I: wherein R1, R2, R3, R4, R5, R6, R7, W, a, b and c are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The biphenyl derivatives of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl derivatives are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthmas.
    Type: Grant
    Filed: July 10, 2012
    Date of Patent: December 31, 2013
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Sarah Dunham, Adam D. Hughes, Craig Husfeld, Eric L. Stangeland
  • Publication number: 20130327251
    Abstract: Novel tridentate-, bidentate-, and monodentate-based aromatic adsorbates including self-assembled monolayers (SAMs), especially, mixed multi-component SAMs, where the adsorbates comprise an aromatic ring including one head group or a plurality of dentate head groups and one tunable tail group or a plurality of tail groups and methods for making the same, and methods for using same, their use in the preparation of homogeneously mixed multi-component self-assembled monolayers (SAMs). The adsorbants and SAMs derived therefrom are ideally suited for biosensing, biosensing diagnostics, biological interfacial mimics, surface protections for nanoparticles, inert coatings for artificial implants, and corrosion-resistant coatings for microelectronics components.
    Type: Application
    Filed: March 7, 2013
    Publication date: December 12, 2013
    Applicant: THE UNIVERSITY OF HOUSTON SYSTEM
    Inventors: T. Randall Lee, Supachai Rittikulsittichai, Thomas Frank, Burapol Singhana
  • Patent number: RE45364
    Abstract: A chemical compound represented by the formula [I]: (wherein R1 represents a hydroxyl group or the like, m represents 0 or an integer of 1 to 5, R2 represents a halogen atom or the like, k represents 0 or an integer of 1 to 4, R3, R31, R4, R41, R5, R51, R6, R61, and R7 each independently represents a hydrogen atom or the like, X represents an oxygen atom or the like, and n represents 1), a salt, an N-oxide of the chemical compound represented by formula [I], and a pest control agent containing the formula [I] as its active constituent.
    Type: Grant
    Filed: January 21, 2014
    Date of Patent: February 3, 2015
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Isami Hamamoto, Jun Takahashi, Makio Yano, Daisuke Hanai, Takao Iwasa