Plural Rings In Acid Moiety Patents (Class 560/27)
  • Patent number: 9573103
    Abstract: The present invention relates to a method for producing an additive composition which in particular contains specific urea urethanes. The additive composition is extremely suitable as a wetting agent and dispersant.
    Type: Grant
    Filed: May 5, 2012
    Date of Patent: February 21, 2017
    Assignee: BYK-Chemie GmbH
    Inventors: Bernd Göbelt, René Nagelsdiek, Jürgen Omeis, Frederik Piestert, Wolfgang Pritschins, Natasa Meznaric, Daniela Schröder, Werner Tiegs
  • Patent number: 9550719
    Abstract: The present disclosure provides a process for synthesis of 3-aryl-2-hydroxy propanoic acid derivatives of formula (S)-1. wherein R1 represents H or (C1-C5) alkyl groups and R2 represents (C1-C5) alkyl groups.
    Type: Grant
    Filed: May 9, 2014
    Date of Patent: January 24, 2017
    Assignee: Council of Scientific and Industrial Research
    Inventors: Muthukrishnan Murugan, Mujahid Mohammad
  • Patent number: 9499476
    Abstract: The compound of formula (I) is a water-stable, long acting ?2-selective adrenoceptor agonist useful as a bronchodilator in the treatment of bronchoconstriction associated with reversible obstructive airways diseases and the like. Processes for making the compound of formula (I), as well as related intermediates, are disclosed.
    Type: Grant
    Filed: April 22, 2015
    Date of Patent: November 22, 2016
    Assignee: SUNOVION PHARMACEUTICALS INC.
    Inventors: Craig R. Abolin, H. Scott Wilkinson, Paul McGlynn, William K. McVicar
  • Patent number: 9260378
    Abstract: The present invention relates to a process for the preparation of substituted N-(benzyl)cyclopropanamines of the general formula (II) starting from N-[(aryl)methylene]cyclopropanamine derivatives. The present invention further provides the N-[(aryl)methylene]cyclopropanamine derivatives used as starting compounds in this process according to the invention, and their use for the preparation of substituted N (benzyl)cyclopropanamines.
    Type: Grant
    Filed: November 4, 2011
    Date of Patent: February 16, 2016
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Norbert Lui, Wahed Ahmed Moradi, Thomas Norbert Muller
  • Patent number: 9249128
    Abstract: Serine hydrolases are implicated in malconditions such as cancer, central nervous system disorders, cardiovascular disorders, obesity, and metabolic disorders. Many serine hydrolases expressed in proteomic libraries are of unknown function in vivo. Compounds identified through library versus library screening can be used for treatment of malconditions associated with the specific serine hydrolase KIAA1363 (also known as AADACL1). A library of inhibitors of KIAA1363 was prepared and candidate compounds were identified as a potent inhibitors having submicromolar IC50 values. An exemplary compound of the invention was shown to be an effective inhibitor of prostate cancer pathogenesis. Other inhibitory compounds of the invention comprising fluorophore groups are shown to be effective in spatial and temporal localization of the serine hydrolase in cells and tissues.
    Type: Grant
    Filed: October 21, 2011
    Date of Patent: February 2, 2016
    Assignee: The Scripps Research Institute
    Inventors: Benjamin Cravatt, Daniel Nomura, Jae W. Chang
  • Patent number: 9139515
    Abstract: This invention relates to a novel process for the synthesis of R-biphenylalaninol and to intermediate compounds that are formed in the process according to the invention, i.e. novel intermediates useful in the synthesis of R-biphenylalaninol. The invention also relates to R-biphenylalaninol, The process according to the invention, the intermediates to of R-biphenylalaninol and of R-biphenylalaninol are all useful in the synthesis of pharmaceutically active compounds.
    Type: Grant
    Filed: August 16, 2012
    Date of Patent: September 22, 2015
    Assignee: DPx Holdings B.V.
    Inventors: Petrus Johannes Hermsen, Peter Hans Ermann, Peter Hans Riebel, Michael Wolberg, Andreas Hendrikus Maria De Vries
  • Publication number: 20150119396
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Application
    Filed: October 22, 2012
    Publication date: April 30, 2015
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Angeles Estiarte Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Laria
  • Publication number: 20150098902
    Abstract: The invention relates to fluorinated compounds and their use as anti-epileptic, muscle-relaxing, fever-reducing and peripherally analgesically acting medications and as imaging agents. Novel fluorinated 2-amino-4-(benzylamino)phenyl carbamate derivatives of ezogabine and pharmaceutically acceptable salts or solvates thereof and their use are described.
    Type: Application
    Filed: December 10, 2014
    Publication date: April 9, 2015
    Inventors: Mark E. Duggan, Takeru Furuya, D. Scott Edwards, Ajay Purohit
  • Publication number: 20150087600
    Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
    Type: Application
    Filed: January 21, 2013
    Publication date: March 26, 2015
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Zhenwei Cai, Shunqi Yan, Ding Zhou
  • Publication number: 20150080466
    Abstract: The present invention relates to diphenyl urea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor 2.
    Type: Application
    Filed: September 16, 2014
    Publication date: March 19, 2015
    Inventors: Richard L. Beard, Tien T. Duong, Michael E. Garst
  • Publication number: 20150065711
    Abstract: Disclosed are linear discrete PEG constructs, which can be created and produced in a precise and reproducible way. Key to being able to do these things, where x in the discrete PEGx can vary from about 2 to about 64, is that the processes used to make each linear portion is controlled to give essentially one oligomer/one compound. Having a variable length linear discrete PEG construct that is (a) primarily an linear discrete PEG construct with diagnostic or therapeutic groups attached along a chain of attachment cores, which is attached to a preferential locator; (b) is an m-discrete PEG as the terminal construct on the linear portion, and “hidden”; (c or linear discrete PEG with a terminus group that can be either negatively or positively charged, or neutral; and any of the discrete PEG portions can be designed to be cleaved after entering the cell.
    Type: Application
    Filed: August 15, 2014
    Publication date: March 5, 2015
    Applicant: EquIP, LLC
    Inventor: Paul D. Davis
  • Publication number: 20150044264
    Abstract: Alkyl and/or alkenyl glycerol carbamate prepared by reacting a carbonate selected from the group consisting of glycerol carbonate, diglycerol carbonate, polyglycerol carbonate and mixtures thereof, with an amine of the general formula (I): HNR1R2??(I) wherein R1 represents a hydrogen atom or a hydrocarbon group selected from the group consisting of alkyl groups and alkenyl groups having from 1 to 22 carbon atoms and R2 represents a hydrocarbon group selected from the group consisting of alkyl groups and alkenyl groups having from 4 to 22 carbon atoms, and cyclic alkyl groups having 5 or 6 carbon atoms, are described along with methods for their use as pearlizing agents in surface-active preparations.
    Type: Application
    Filed: August 4, 2014
    Publication date: February 12, 2015
    Inventors: Bin Gu, Brajesh Jha, Sithamalli Chandramouli, Jie Yang
  • Publication number: 20150031688
    Abstract: A dual thyrointegrin antagonist and a method for treating an angiogenesis-mediated disorder and/or a hyperthyroidism disorders by introducing the dual thyrointegrin antagonist into animals (e.g., mammals, human beings). The dual thyrointegrin antagonist includes a chemical structure having a thyroid hormone antagonist and ?v?3 integrin antagonist in the same molecule.
    Type: Application
    Filed: October 9, 2014
    Publication date: January 29, 2015
    Inventor: Shaker A. Mousa
  • Patent number: 8937083
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.
    Type: Grant
    Filed: October 24, 2012
    Date of Patent: January 20, 2015
    Assignee: DowAgroSciences, LLC
    Inventors: Noormohamed M. Niyaz, Negar Garizi, Yu Zhang, Tony K. Trullinger, Ricky Hunter, Ann M. Buysse, Asako Kubota, Paul Renee LePlae, Jr., Daniel Knueppel, Christian T. Lowe, Dan Pernich, David A. Demeter, Timothy C. Johnson
  • Patent number: 8916133
    Abstract: The invention relates to fluorinated compounds and their use as anti-epileptic, muscle-relaxing, fever-reducing and peripherally analgesically acting medications and as imaging agents. Novel fluorinated 2-amino-4-(benzylamino)phenyl carbamate derivatives of ezogabine and pharmaceutically acceptable salts or solvates thereof and their use are described.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: December 23, 2014
    Assignee: SciFluor Life Sciences, LLC
    Inventors: Mark E. Duggan, Takeru Furuya, D. Scott Edwards, Ajay Purohit
  • Publication number: 20140371449
    Abstract: The present invention relates to the field of organic synthesis and describes the synthesis of specific intermediates suitable for the preparation of triazolopyrimidine compounds such as ticagrelor.
    Type: Application
    Filed: December 20, 2012
    Publication date: December 18, 2014
    Applicant: Lek Pharmaceuticals d.d.
    Inventors: Nenad Maras, Ivana Gazic Smilovic, Damjan Sterk
  • Publication number: 20140364602
    Abstract: Methods and intermediates useful for preparing a compound of formula I: and salts thereof.
    Type: Application
    Filed: February 1, 2013
    Publication date: December 11, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Aaron J. Cullen, Richard Hung Chiu Yu
  • Publication number: 20140350285
    Abstract: The present invention relates to novel polymorphs of N-[2-amino-4-(4-fluorobenzylamino)-phenyl]carbamic acid ethyl ester, processes for preparing them, and pharmaceutical composition comprising them. In one aspect, the present invention relates to a novel crystalline polymorph of retigabine designated as crystalline Form I, characterized by XRPD having characteristic peaks at about 4.87, 5.04, 7.03, 9.74, 10.02, 11.6, 18.03, 19.9 and 28.5±0.2 degrees two-theta, which is substantially same as depicted in FIG. 1.
    Type: Application
    Filed: January 30, 2012
    Publication date: November 27, 2014
    Applicant: SYMED LABS LIMITED
    Inventors: Dodda Mohan Rao, Kirla Haritha
  • Publication number: 20140343138
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and Z are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: February 14, 2014
    Publication date: November 20, 2014
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Adam D. Hughes, Erik Fenster, Melissa Fleury, Roland Gendron, Edmund J. Moran
  • Publication number: 20140336252
    Abstract: The present invention provides compounds having the structure represented by general formula I, pharmaceutically acceptable salts thereofagonist, preparation methods therefor and a use thereof in the preparation of a medicine for the treatment of nervous system diseases. The compounds or pharmaceutical compositions thereof can be used as the KCNQ potassium channel agonist for treating nervous system diseases. Compared to retigabine, a compound in the prior art, the compound of the present invention have the same or better therapeutic effect, are easier for synthesis and storage, and less prone to oxidate deterioration.
    Type: Application
    Filed: October 23, 2012
    Publication date: November 13, 2014
    Inventors: Fajun Nan, Min Li, Zhaobing Gao, Fei Chen, Yangming Zhang, Pingzheng Zhou, Haining Hu, Haiyan Xu, Sheng Liu
  • Publication number: 20140323436
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein W is O or S; V is a direct bond or NR3; Q is or CR6aR6b, O, NR7, C?N—O—R7 or C(?O); Y is —C(R5)?N—O—(CR8aR8b)p—X—(CR9aR9b)q—SiR10aR10bR10c; or a phenyl ring substituted as defined in the disclosure; or Z; and R1, R2, R3, R4, R5, R6a, R6b, R7, R8a, R8b, R9a, R9b, R10a, R10b, R10c, Z, p and q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: July 8, 2014
    Publication date: October 30, 2014
    Inventors: Bruce Lawrence FINKELSTEIN, Andrew Edmund TAGGI, Jeffrey Keith LONG, Paula Louise SHARPE, Chi-Ping TSENG, Stephen Frederick MCCANN, Amy X DING, Steven Lewis SWANN, JR.
  • Publication number: 20140315946
    Abstract: Novel compounds and compositions for treating patients in need of relief from HIV, AIDS and AIDS-related diseases are described. Methods for treating HIV, AIDS, and AIDS-related diseases using the compounds described herein are also described.
    Type: Application
    Filed: July 2, 2014
    Publication date: October 23, 2014
    Inventor: Arun K. Ghosh
  • Patent number: 8859539
    Abstract: A dual thyrointegrin antagonist and a method for treating an angiogenesis-mediated disorder and/or a hyperthyroidism disorders by introducing the dual thyrointegrin antagonist into animals (e.g., mammals, human beings). The dual thyrointegrin antagonist includes a chemical structure having a thyroid hormone antagonist and ?v?3 integrin antagonist in the same molecule.
    Type: Grant
    Filed: November 1, 2010
    Date of Patent: October 14, 2014
    Assignee: Vascular Vision Pharmaceutical Company
    Inventor: Shaker A. Mousa
  • Publication number: 20140303377
    Abstract: An object of the present invention is to provide insecticides having high effectiveness.
    Type: Application
    Filed: June 24, 2014
    Publication date: October 9, 2014
    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, Atsuko Kawahara
  • Patent number: 8853427
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Grant
    Filed: June 3, 2013
    Date of Patent: October 7, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes
  • Publication number: 20140296559
    Abstract: This invention relates to a novel process for the synthesis of R-biphenylalaninol and to intermediate compounds that are formed in the process according to the invention, i.e. novel intermediates useful in the synthesis of R-biphenylalaninol. The in vention also relates to R-biphenylalaninol, The process according to the invention, the intermediates to of R-biphenylalaninol and of R-biphenylalaninol are all useful in the synthesis of pharmaceutically active compounds.
    Type: Application
    Filed: August 16, 2012
    Publication date: October 2, 2014
    Applicants: DSM FINE CHEMICALS AUSTRIA NFG. GMBH & CO KG, DSM IP ASSETS B.V.
    Inventors: Petrus Johannes Hermsen, Peter Hans Ermann, Peter Hans Riebel, Michael Wolberg, Andreas Hendrikus Maria De Vries
  • Patent number: 8835668
    Abstract: The invention relates to a new process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a ?-amino-?-biphenyl-?-methylalkanoic acid, or acid ester, backbone, such as N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: September 16, 2014
    Assignee: Novartis AG
    Inventors: David Hook, Jianguang Zhou, Yunzhong Li
  • Publication number: 20140256729
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Application
    Filed: October 22, 2012
    Publication date: September 11, 2014
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Ángeles Estiarte Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Laria
  • Publication number: 20140249320
    Abstract: The present invention relates to pyrrolidin-2-ones according to the formula (1), or salts thereof, wherein R1 is hydrogen or a nitrogen protecting group, methods for their preparation and their use in the preparation of NEP-inhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.
    Type: Application
    Filed: March 25, 2014
    Publication date: September 4, 2014
    Inventors: David Hook, Thomas Ruch, Bernard Riss, Bernhard Wietfeld, Gottfried Sedelmeier, Matthias Napp, Markus Bänziger, Steven Hawker, Lech Ciszewski, Liladhar Murlidhar Waykole
  • Publication number: 20140249306
    Abstract: The present invention provides a novel compound having an antiviral action, in particular, an HIV replication inhibiting action, as well as a pharmaceutical composition, in particular, an anti-HIV agent. wherein, a broken line means the presence or absence of a bond; R1 is substituted or unsubstituted alkyl etc., R2 is substituted or unsubstituted alkyloxy etc.; n is 1 or 2; R3 is a substituted or unsubstituted aromatic carbocyclic group; R4 is a hydrogen atom etc.; R5 is a substituted or unsubstituted aromatic carbocyclic group etc.; Y is a single bond etc.; R6 is substituted or unsubstituted alkyl; R7 is —Z—R71 etc.; Z is —NR72—CO— etc.; R71 is substituted or unsubstituted alkyl etc.; R72 is a hydrogen atom etc.
    Type: Application
    Filed: October 25, 2012
    Publication date: September 4, 2014
    Applicant: Shionogi & Co., Ltd.
    Inventors: Tsutomu Iwaki, Kenji Tomita
  • Publication number: 20140243546
    Abstract: The invention relates to a new process for producing NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a ?-amino-?-biphenyl-?-methylalkanoic acid, or acid ester, backbone. In detail, the new processes, according to the present invention, are ultimately related to the synthesis of intermediates to prepare the above NEP inhibitors, namely compounds according to formula (1), or salt thereof, wherein R1 and R2 are, independently of each other, hydrogen or a nitrogen protecting group, and R3 is a carboxyl group or an ester group, preferably carboxyl group or alkyl ester.
    Type: Application
    Filed: November 11, 2013
    Publication date: August 28, 2014
    Applicant: NOVARTIS AG
    Inventors: David Hook, Bernard Riss, Daniel Kaufmann, Matthias Napp, Erhard Bappert, Philippe Polleux, Jonathan Medlock, Antonio Zanotti-Gerosa
  • Publication number: 20140235580
    Abstract: Provided herein are compounds which mediate the activity of monoacyglycerol lipase (MAGL). Also provided are pharmaceutical compositions comprising a compound provided herein, and methods for treating, preventing and/or managing a MAGL mediated condition using a compound or pharmaceutical composition as provided herein.
    Type: Application
    Filed: September 27, 2012
    Publication date: August 21, 2014
    Inventors: Alfredo C. Castro, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
  • Publication number: 20140163077
    Abstract: The present disclosure relates to novel compounds, compositions containing same and methods for treating or preventing a condition associated with a deficient insulin secretion such as diabetes and metabolic syndrome in a subject in need thereof.
    Type: Application
    Filed: July 31, 2012
    Publication date: June 12, 2014
    Applicant: VAL-CHUM, LIMITED PARTNERSHIP
    Inventors: Murthy S.R. Madiraju, Marc Prentki, Erik Joly
  • Publication number: 20140163252
    Abstract: The invention provides a novel method for the preparation of intermediates useful in a process designed to obtain known 1,2,4-triaminobenzene compounds, and in particular a specific compound thereof having known anticonvulsant activity. Unlike known methods, the novel method does not require advance protection of the amino groups present on the substrate.
    Type: Application
    Filed: October 29, 2013
    Publication date: June 12, 2014
    Applicant: DIPHARMA FRANCIS S.r.I
    Inventors: Emanuele ATTOLINO, Roberto ROSSI, Marco ARTICO
  • Publication number: 20140161839
    Abstract: The present invention relates to a compound of the following general formula (I): R1—NH—CH(R2)—P(?O)(OR3)—CH2—C(R4)(R5)—CONH—CH(R6)—COOR7 (I) or a pharmaceutically acceptable salt of the latter, an isomer or a mixture of isomers in any proportions, especially a mixture of enantiomers, and in particular a racemic mixture, for which R1 represents a —C(?O)—O—C(R8)(R9)—OC(?O)—R10 group; R2 represents an optionally substituted hydrocarbon-based chain, an aryl or heteroaryl group or a methylene group substituted by a heterocycle; R3 represents a hydrogen atom or a —C(R12)(R13)—OC(?O)—R14 group; R4 and R5 form, together with the carbon that bears them, a saturated hydrocarbon-based ring or an optionally substituted piperidine ring or R4 represents a hydrogen atom and R5 represents a phenyl or a benzyl that is optionally substituted, a heteroaromatic ring or a methylene group substituted by a heterocycle; R6 represents an optionally substituted hydrocarbon-based chain or a phenyl or a benzyl that is optionally substi
    Type: Application
    Filed: February 18, 2014
    Publication date: June 12, 2014
    Applicant: PHARMALEADS
    Inventors: Bernard Roques, Herve Poras, Marie-Claude Fournie-Zaluski
  • Patent number: 8735622
    Abstract: The present invention provides compounds, or derivatives or prodrugs thereof, that comprise a methyllysine mimic, and an ?-ketoglutarate mimic that are attached through a linker and methods for using and producing the same. In some embodiments, compounds of the invention are of the formula: M-L-K, or a derivative or a prodrug thereof, wherein M is a methyllysine mimic, L is a linker, and K is an ?-ketoglutarate mimic.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: May 27, 2014
    Assignee: The Regents of the University of Colorado, a body corporate
    Inventors: Xiang Wang, Wenqing Xu
  • Publication number: 20140135493
    Abstract: Disclosed is a process for making diastereomeric compound of the formula (I): wherein m, n and R1 to R4 are as defined herein. The process of the invention provides the compound of formula (I) in high yield and substantially free of the corresponding diastereomers. The compounds of formula (I) prepared by the process of the invention are useful for making pharmaceutically active compounds such as 11-?-hydroxysteroid hydrogenase type 1 (11-?-HSD1) inhibitors.
    Type: Application
    Filed: December 15, 2011
    Publication date: May 15, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Daniel Robert Fandrick, Zhi-Hui Lu, Diana Crimhilda Reeves, Jonathan Timothy Reeves, Chris Hugh Senanayake, Jinhua J. Song, Yongda Zhang
  • Patent number: 8686032
    Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers:
    Type: Grant
    Filed: December 1, 2010
    Date of Patent: April 1, 2014
    Assignee: Chroma Therapeutics Ltd.
    Inventors: Alan Hornsby Davidson, Sanjay Ratilal Patel, Francesca Ann Mazzei, Stephen John Davies, Alan Hastings Drummond, David Festus Moffat, Kenneth William John Baker, Alistair David Graham Donald
  • Publication number: 20140081017
    Abstract: The present invention relates to compositions and methods to selectively treat fungal infection. More particularly, the invention relates to compounds, compositions thereof, and methods for selectively enhancing fungal sensitivity to antifungal compounds.
    Type: Application
    Filed: March 14, 2013
    Publication date: March 20, 2014
    Applicant: METHYLGENE INC.
    Inventor: METHYLGENE INC.
  • Publication number: 20140066500
    Abstract: The present invention provides novel cycloalkylmethylamine derivatives, and methods of preparing cycloalkylmethylamine derivatives. The present invention also provides methods of using cycloalkylmethylamine derivatives and compositions of cycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.
    Type: Application
    Filed: November 6, 2013
    Publication date: March 6, 2014
    Applicant: Reviva Pharmaceuticals, Inc.
    Inventors: Laxminarayan BHAT, Seema BHAT
  • Patent number: 8633228
    Abstract: A pest control agent containing a compound represented by the following Formula (1), wherein A represents a carbon atom, a nitrogen atom, or the like, K represents a non-metal atom group necessary for forming a cyclic linking group derived from a 5- or 6-membered aromatic ring, in combination with A and two carbon atoms to which A bonds, X represents a hydrogen atom, a halogen atom, or the like, n represents an integer of from 0 to 4, T represents —C(?G1)-Q1 (wherein G1 and G2 represent an oxygen atom or the like, Q1 represents a phenyl group which may have a substituent, a heterocyclic group which may have a substituent, or the like), or the like, Q2 represents a phenyl group or the like, G3 represents an oxygen atom or the like, and R1 and R2 each independently represent a hydrogen atom, a C1-C6 alkyl group, or a group represented by -L-D, or the like (provided that at least either R1 or R2 represents a group represented by -L-D); as an active ingredient exhibits an excellent effect.
    Type: Grant
    Filed: June 29, 2009
    Date of Patent: January 21, 2014
    Assignee: Mitsui Chemicals Agro, Inc.
    Inventors: Yumi Kobayashi, Hiroyuki Katsuta, Michikazu Nomura, Hidetaka Tsukada, Atsushi Hirabayashi, Hidenori Daido, Yusuke Takahashi, Shinichi Banba
  • Publication number: 20130345465
    Abstract: This invention relates to a novel chemical process for the synthesis of 2-ethyoxycarbonylamino-5-(4-fluorobenzylamino)-nitrobenzene and its use in the preparation of 2-amino-4-(4-fluorobenzylamino)-1-ethoxycarbonylaminobenzene (retigabine/ezogabine) and its polymorphic forms thereof.
    Type: Application
    Filed: January 16, 2012
    Publication date: December 26, 2013
    Applicant: GLAXO GROUP LIMITED
    Inventors: Russ N. Fitzgerald, Alan Millar, Jennifer Fell Toczko
  • Publication number: 20130317220
    Abstract: Provided herein is a novel process for the preparation of triazolo[4,5-d]pyrimidine derivatives. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of highly pure ticagrelor or a pharmaceutically acceptable salt thereof. Provided further herein is a novel process for the preparation of substituted cyclopentanamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of a ticagrelor intermediate, 2-[[(3aR,4S,6R,6aS)-6-amino-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]-dioxol-4-yl]oxy]-1-ethanol.
    Type: Application
    Filed: December 16, 2011
    Publication date: November 28, 2013
    Applicant: Actavis Group Ptc Ehf
    Inventors: Vignesh Nair, Nikhil Trivedi, Anil Shahaji Khile, Nitin Sharadchandra Pradhan
  • Patent number: 8586536
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Grant
    Filed: December 14, 2011
    Date of Patent: November 19, 2013
    Assignee: Theravance, Inc.
    Inventors: Roland Gendron, Melissa Fleury, Adam D. Hughes
  • Publication number: 20130287686
    Abstract: The invention relates to fluorinated compounds and their use as anti-epileptic, muscle-relaxing, fever-reducing and peripherally analgesically acting medications and as imaging agents. Novel fluorinated 2-amino-4-(benzylamino)phenyl carbamate derivatives of ezogabine and pharmaceutically acceptable salts or solvates thereof and their use are described.
    Type: Application
    Filed: March 13, 2013
    Publication date: October 31, 2013
    Applicant: SCIFLUOR LIFE SCIENCES, LLC
    Inventors: Mark E. Duggan, Takeru Furuya, D. Scott Edwards, Ajay Purohit
  • Publication number: 20130261316
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: June 3, 2013
    Publication date: October 3, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes
  • Publication number: 20130253004
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Application
    Filed: December 6, 2011
    Publication date: September 26, 2013
    Applicant: Amira Pharmaceuticals, Inc.
    Inventors: Thomas Jon Seiders, Bowei Wang, John Howard Hutchinson, Nicholas Simon Stock, Deborah Volkots
  • Publication number: 20130245307
    Abstract: The invention relates to a process for preparation of radiopharmaceutical precursors, and in particular protected amino acid derivatives which are used as precursors for production of radiolabeled amino acids for use in in vivo imaging procedures such as positron emission tomography (PET). Particularly, the invention relates to a process for preparation of a precursor of the [18F]-1-amino-3- fluorocyclobutanecarboxylic acid ([18F] FACBC) PET agent and particularly to the work-up process of this precursor removing generated salts from the intermediate composition.
    Type: Application
    Filed: November 28, 2011
    Publication date: September 19, 2013
    Applicant: GE HEALTHCARE LIMITED
    Inventors: Tom Christian Berg, Anne Nilsen
  • Publication number: 20130237573
    Abstract: A mGlu2/3 receptor antagonist of the formula: its uses, and methods for its preparation are described.
    Type: Application
    Filed: November 15, 2011
    Publication date: September 12, 2013
    Applicant: ELI LILLY AND COMPANY
    Inventors: Bruce Anthony Dressman, Mark Donald Chappell, Adam Michael Fivush, Charles Howard Mitch, Paul Leslie Ornstein, Eric George Tromiczak, Tatiana Natali Vetman
  • Publication number: 20130217660
    Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
    Type: Application
    Filed: May 12, 2011
    Publication date: August 22, 2013
    Inventors: Dong-Ming Shen, John S. Debenham, Thomas H. Graham, Matthew J. Clements, Yong Zhang