1,3-thiazoles (including Hydrogenated) Patents (Class 548/146)
  • Patent number: 9884024
    Abstract: The present invention proposes a design to incorporate drug(s) in the hard capsule shells (body and cap) composition. Drug(s) in the cap and body of the capsule shell may be the same or may be different. Other drug(s) in the form of granules, beads etc. can be filled into the capsules as a core material. The drug(s) in the capsule core material may be the same as in the shell-composition or may be different. Thus, the same capsule may contain different drug(s) as the core material and in the shell. The key advantages of incorporation of drug in the capsule shell compositions are to minimize drug-drug interaction and to obtain a desired rate of release of the drug(s), mainly for potent ones. The concept can be applied to the hard gelatin, and hard non-gelatin capsules.
    Type: Grant
    Filed: May 19, 2014
    Date of Patent: February 6, 2018
    Inventor: Hemant N Joshi
  • Patent number: 9783532
    Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses molecules having the following formula (“Formula One”).
    Type: Grant
    Filed: March 8, 2017
    Date of Patent: October 10, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: Natalie C. Giampietro, Lindsey G. Fischer, Erich W. Baum, Gary D. Crouse, Andrew L. Ward, Thomas C. Sparks, Jeff Petkus
  • Patent number: 9670172
    Abstract: This disclosure provides compounds and methods of using those compounds to treat metabolic disorders and hyperproliferative disorders, including administration of the compounds in conjunction with hormone receptor antagonists.
    Type: Grant
    Filed: August 28, 2014
    Date of Patent: June 6, 2017
    Assignee: MEDIVATION TECHNOLOGIES, INC.
    Inventors: Sarvajit Chakravarty, Roopa Rai, Son Minh Pham, Brahmam Pujala, Ramniwas Jangir, Rambabu Guguloth, Vijay Kumar Sharma
  • Patent number: 9475788
    Abstract: The invention is directed to a compound of formula I, a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing a compound of formula I, and a method of treatment of a disorder or condition selected from the group consisting of Human African Trypanosomiasis (HAT), Chagas disease, Leishmaniasis and malaria.
    Type: Grant
    Filed: October 21, 2015
    Date of Patent: October 25, 2016
    Assignee: MediSynergics, LLC
    Inventors: Dennis Michael Godek, Harry Ralph Howard
  • Patent number: 9346777
    Abstract: The invention is directed to a compound of formula I, as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by administration of the compound, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of Human African Trypanosomiasis (HAT), Chagas disease, Leishmaniasis and malaria, the method comprising administering to a mammal, including a human, in need of such treatment a compound of formula I as described above.
    Type: Grant
    Filed: August 4, 2013
    Date of Patent: May 24, 2016
    Assignee: MediSynergics, LLC
    Inventors: Dennis Michael Godek, Harry Ralph Howard
  • Patent number: 9284291
    Abstract: The invention is directed to a compound of formula I, as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by administration of the compound, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of depression, mood disorders, schizophrenia, Alzheimer's disease, anxiety and addiction, the method comprising administering to a mammal, including a human, in need of such treatment a compound of formula I as described above.
    Type: Grant
    Filed: July 29, 2014
    Date of Patent: March 15, 2016
    Assignee: MediSynergies, LLC
    Inventors: Dennis Michael Godek, Harry Ralph Howard
  • Patent number: 9278964
    Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses molecules having the following formula (“Formula One”).
    Type: Grant
    Filed: March 18, 2015
    Date of Patent: March 8, 2016
    Assignee: Dow AgroSciences LLC
    Inventors: Lindsey G. Fischer, Erich W. Baum, Gary D. Crouse, Jeff Petkus, Andrew Ward, Thomas C. Sparks
  • Patent number: 9273091
    Abstract: Tubulysins are a series of naturally occurring cytotoxic agents that are of interest as anticancer therapeutic agents. Processes and intermediates useful for preparing naturally occurring and non-naturally occurring tubulysins and analogs and derivatives thereof are described.
    Type: Grant
    Filed: October 20, 2014
    Date of Patent: March 1, 2016
    Assignee: Endocyte, Inc.
    Inventors: Iontcho Radoslavov Vlahov, Michael Groaning, Paul Joseph Kleindl, Hari Krishna R. Santhapuram, Fei You, Kevin Yu Wang, Le-Cun Xu, Katheryn Marie Stanford, Allen Ritter, Christopher Paul Leamon
  • Patent number: 9181187
    Abstract: Disclosed is an EP1 antagonist, particularly a compound represented by the formula (I): wherein all symbols are as defined in the description, a salt thereof, a solvate thereof or a prodrug thereof. The compound, a salt thereof, a solvate thereof or a prodrug thereof is effective for prevention, treatment and/or symptom improvement of a dysuria (e.g., slow stream, splitting or spraying of the urine stream, intermittent stream, hesitancy, straining to void or terminal dribble).
    Type: Grant
    Filed: February 15, 2008
    Date of Patent: November 10, 2015
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Takayuki Maruyama, Hiroki Okada, Takashi Konemura
  • Patent number: 9051300
    Abstract: The invention relates to a compound of formula (I), which is suitable for use as a herbicide wherein G is hydrogen or an agriculturally acceptable metal, sulfonium, ammonium or latentiating group; Q is a unsubstituted or substituted C3-C8 saturated or mono-unsaturated heterocyclyl containing at least one heteroatom selected from O, N and S, or Q is heteroaryl or substituted heteroaryl; m is 1, 2 or 3; and Het is an optionally substituted monocyclic or bicyclic heteroaromatic ring; and wherein the compound is optionally an agronomically acceptable salt thereof.
    Type: Grant
    Filed: July 29, 2010
    Date of Patent: June 9, 2015
    Assignee: Syngenta Limited
    Inventors: Stephane André Marie Jeanmart, Adrian Longstaff, Christopher John Mathews, Claire Janet Russell, Russell Colin Viner, Frances Kathryn Wood
  • Patent number: 9029560
    Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses molecules having the following formula (“Formula One”).
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: May 12, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: Lindsey G. Fischer, Erich W. Baum, Gary D. Crouse, Jeff Petkus, Andrew L. Ward, Thomas C. Sparks
  • Patent number: 8987308
    Abstract: Disclosed are compounds of formula (I): or a pharmaceutically acceptable N-oxide, salt, hydrate, solvate, complex, bioisostere, metabolite or prodrug thereof, which are of use in the treatment of infection with, and diseases caused by, Clostridium difficile.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: March 24, 2015
    Assignee: Summit Corporation Plc
    Inventors: Peter David Johnson, Richard John Vickers, Francis Xavier Wilson, Colin Richard Dorgan, Lauren Jayne Sudlow, Stephen Paul Wren, Renate van Well
  • Patent number: 8969578
    Abstract: Disclosed herein are compounds derived from a chemical structure according to the formula (I) wherein X comprises oxygen or sulfur, R1 comprises a phenyl or naphthyl group, R2 comprises an amide group and R3 comprises a phosphate group. The disclosed compounds demonstrate inhibitory activity against STAT3, a protein found in certain tumor tissues and which promotes cellular overproliferation and resistance to apoptosis. The invention includes compositions containing the disclosed compounds, as well as methods of treatment therewith.
    Type: Grant
    Filed: September 17, 2009
    Date of Patent: March 3, 2015
    Assignee: University of Central Florida Research Foundation, Inc.
    Inventors: James Turkson, Andrew D. Hamilton
  • Publication number: 20150057269
    Abstract: The present invention regards compositions and methods for the modulation of amidases capable of hydrolysing N-acylethanolamines useable in the therapy of inflammatory diseases. In particular, the present invention regards a compound of general formula (I): enantiomers, diastereoisomers, racemes and mixtures, polymorphs, salts, solvates thereof, wherein: (a) R is a linear alkyl radical having 13 to 19 carbon atoms or alkenyl radical having 13 to 19 carbon atoms carrying a double bond; (b) X is 0 or S; (c) Y is a 2 or 3 carbon atom alkylene residue, optionally substituted with one or two groups equal or different from each other and selected from among the group consisting of: —CH3, —CH2OH, —COOCH3, —COOH. Y may preferably be: —CH2—CH2—, —CH2—CH2—CH2—, CH(CH3)—CH2—, —CH2—CH(CH3)—, —CH2—C(CH3)2—, —CH2—CH(CH2OH)—, —CH2—C((CH2OH)2)—, —CH?CH—, —CH2—CH(COOCH3)—, —CH2—CH(COOH)—, for use as a medicine.
    Type: Application
    Filed: February 17, 2012
    Publication date: February 26, 2015
    Applicant: Epitech Group S.r.l.
    Inventors: Francesco Della Valle, Maria Federica Della Valle, Gabriele Marcolongo, Vincenzo Di Marzo, Salvatore Cuzzocrea
  • Patent number: 8946442
    Abstract: Foams of ionic compounds are described. Methods of making the foams are also provided. The foams are ionic and can be used for catalysis, separations, gas storage, biosensors, electronics, and electrochemical applications.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: February 3, 2015
    Assignee: E I du Pont de Nemours and Company
    Inventors: Mark Brandon Shiflett, Akimichi Yokozeki
  • Patent number: 8940271
    Abstract: The invention includes compositions for transmucosal administration to an animal comprising at least one active agent and a pharmaceutically acceptable carrier. A preferred active agent is selected from the group consisting of meloxicam, carprofen, enrofloxacin, clemastine, diphenhydramine, digoxin, levothyroxine, cyclosporine, ondansetron, lysine, zolpidem, propofol, nitenpyram, ivermectin, milbemycin, and pharmaceutically acceptable salts, solvates and esters thereof. In another embodiment, the invention includes methods of treating or preventing a condition in an animal comprising transmucosally administering a composition comprising a therapeutically or prophylactically effective amount of an active agent and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: December 15, 2011
    Date of Patent: January 27, 2015
    Assignee: Abbott Laboratories
    Inventors: Mark C. Heit, Antonio M. Benitz, Dennis F. Steadman, David M. Petrick
  • Patent number: 8916592
    Abstract: Compounds of formula I wherein X is O or S(?O)n; n is 0, 1 or 2; R1 is optionally substituted alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, cycloalkyl, halocycloalkyl, cycloalkenyl, halocycloalkenyl, phenyl, hetaryl, phenylalkyl, hetaryl alkyl, optionally fused to phenyl, hetaryl or heterocyclyl; A is —NRb2, —C(=G)GRb, —C(=G)NRb2, —C(?NORb)Rb, C(=G)[N?SRb2], —C(=G)NRb—NRb2, C2-C6-alkandiyl, C2-C6-alkenediyl, C1-C3-alkyl-G-C1-C3-alkyl, wherein Rb is as defined in the description, or optionally substituted phenyl, hetaryl, heterocyclyl, optionally fused to phenyl or heterocyclyl; B is an optionally substituted saturated or partially unsaturated hydrocarbon chain with 1 to 3 carbon chain atoms; D is an optionally substituted saturated or partially unsaturated hydrocarbon chain with 1 to 5 carbon chain atoms or C3-C6-cycloalkyl; G is oxygen or sulfur; or the enantiomers or diastereomers or salts or N-oxides thereof, processes for preparing the compounds I, pesticidal compositions and synergistic m
    Type: Grant
    Filed: December 13, 2006
    Date of Patent: December 23, 2014
    Assignee: Merial Limited
    Inventors: Matthias Pohlman, Michael Hofmann, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Hassan Oloumi-Sadeghi, Takeo Hokama, Christopher Palmer, Jürgen Langewald
  • Patent number: 8901313
    Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.
    Type: Grant
    Filed: March 15, 2012
    Date of Patent: December 2, 2014
    Assignee: Genentech, Inc.
    Inventors: Steven Staben, Jianwen Feng, Pui Leng Loke, Christian A. G. N. Montalbetti
  • Patent number: 8901306
    Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.
    Type: Grant
    Filed: March 2, 2010
    Date of Patent: December 2, 2014
    Assignee: StemSynergy Therapeutics, Inc.
    Inventor: Darren Orton
  • Patent number: 8895592
    Abstract: Disclosed herein are cannabinoid receptor ligands of formula (I) wherein L1, A1, R1g, z, R2, R3, and R4 are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.
    Type: Grant
    Filed: December 16, 2009
    Date of Patent: November 25, 2014
    Assignee: AbbVie Inc.
    Inventors: Jennifer M. Frost, Steven P. Latshaw, Michael J. Dart, William A. Carroll, Arturo Perez-Medrano, Teodozyj Kolasa, Meena V. Patel, Derek W. Nelson, Tongmei Li, Sridhar Peddi, Xueqing Wang, Bo Liu
  • Patent number: 8889880
    Abstract: Tubulysins are a series of naturally occurring cytotoxic agents that are of interest as anticancer therapeutic agents. Processes and intermediates useful for preparing naturally occurring and non-naturally occurring tubulysins and analogs and derivatives thereof are described.
    Type: Grant
    Filed: August 5, 2011
    Date of Patent: November 18, 2014
    Assignee: Endocyte, Inc.
    Inventors: Iontcho Radoslavov Vlahov, Michael Groaning, Paul Joseph Kleindl, Hari Krishna R. Santhapuram, Fei You, Kevin Yu Wang, Le-Cun Xu, Katheryn Marie Stanford, Allen Ritter, Christopher Paul Leamon
  • Patent number: 8883180
    Abstract: The invention relates to active compound combinations, in particular a fungicidal and/or insecticidal composition, comprising Isotianil (3,4-dichloro-N-(2-cyanophenyl)-5-isothiazolecarboxamide) and at least one further insecticide of the anthranilamide group and optionally one further insecticide of the neonicotinoids. Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi and/or microorganisms and/or pests of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.
    Type: Grant
    Filed: August 29, 2013
    Date of Patent: November 11, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Lutz Assmann, Ulrike Wachendorff-Neumann, Peter Dahmen, Heike Hungenberg, Wolfgang Thielert
  • Patent number: 8865753
    Abstract: The present application relates to thiazolylidene containing compounds of formula (I) wherein R1, R2, R3, R4, L2 and A are as defined in the specification. Compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: October 21, 2014
    Assignee: AbbVie Inc.
    Inventors: Teodozyj Kolasa, Jennifer M. Frost, Meena V. Patel, Steven P. Latshaw, Arturo Perez-Medrano, Xueqing Wang, Sridhar Peddi, William A. Carroll, Michael J. Dart
  • Patent number: 8864849
    Abstract: The present specification provides for an agent for coloring keratinic fibers. The agent includes, a cosmetic carrier, a compound of formula (I), R1 and R2 independently of one another denote hydrogen, a C1-C6 alkyl group, a C2-C6 alkenyl group, a hydroxyl group, a halogen, a C1-C6 alkoxy group, an amino group, a nitro group, an acetyl amino group, or a sulfonamide group; or when in ortho-position to one another, form a 5- or 6-membered, saturated or unsaturated ring, which optionally include further heteroatoms.
    Type: Grant
    Filed: May 6, 2014
    Date of Patent: October 21, 2014
    Assignee: Henkel AG & Co. KGaA
    Inventors: Wibke Gross, Ralph Nemitz, Melanie Moch, Astrid Kroos, Antje Gebert
  • Patent number: 8864848
    Abstract: The invention relates to agents for coloring keratinic fibers, in particular human hair, including in a cosmetic carrier at least one compound of the formula (I). The structures the of the general formula (I) have a heterocycle A which bears a quaternary nitrogen atom and thus a positive charge. The invention furthermore relates to the use of these novel azo dyes in agents for coloring hair and to the dyes themselves.
    Type: Grant
    Filed: May 5, 2014
    Date of Patent: October 21, 2014
    Assignee: Henkel AG & Co. KGAA
    Inventors: Wibke Gross, Ralph Nemitz, Melanie Moch
  • Patent number: 8859599
    Abstract: The present invention concerns compounds of general formula (I): Method of preparation and uses thereof.
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: October 14, 2014
    Assignees: CNR—Consiglio Nazionale delle Ricerche, Istituto Scientifico Romagnolo per lo Studio e la Cura dei Tumori (I.R.S.T.) S.r.l.
    Inventors: Greta Varchi, Andrea Guerrini, Anna Tesei, Giovanni Brigliadori
  • Patent number: 8852846
    Abstract: The present invention provides a salt represented by the formula (I): wherein Q1 and Q2 independently each represent a fluorine atom or a C1-C6 perfluoroalkyl group, L1 represents a C1-C20 divalent saturated hydrocarbon group in which one or more —CH2— can be replaced by —O— or —CO—, W represents a group represented by the formula (W1), (W2), (W3), (W4) or (W5): and Z+ represents an organic counter ion.
    Type: Grant
    Filed: April 4, 2012
    Date of Patent: October 7, 2014
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Yukako Anryu, Koji Ichikawa
  • Patent number: 8846730
    Abstract: The present application relates to cannabinoid receptor ligands of formula (I) wherein X1, A1, Rx, R2, R3, R4, and z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions.
    Type: Grant
    Filed: September 4, 2009
    Date of Patent: September 30, 2014
    Assignee: AbbVie Inc.
    Inventors: William A. Carroll, Michael J. Dart, Jennifer M. Frost, Teodozyj Kolasa, Tongmei Li, Bo Liu, Arturo Perez-Medrano, Meena Patel, Xueqing Wang, Sridhar Peddi
  • Patent number: 8841334
    Abstract: The present invention relates to compounds of formula (I), or pharmaceutical salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and L1 are defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions. The present invention also relates to compounds of formula (II), or pharmaceutical salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1a, R2a, Rx, and n are as defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Grant
    Filed: November 19, 2008
    Date of Patent: September 23, 2014
    Assignee: AbbVie Inc.
    Inventors: Alan S. Florjancic, Michael J. Dart, Keith B. Ryther, Arturo Perez-Medrano, William A. Carroll, Meena V. Patel, Karin Rosemarie Tietje, Tongmei Li, Teodozyj Kolasa, Megan E. Gallagher, Sridhar Peddi, Jennifer M. Frost, Derek W. Nelson, Xueqing Wang
  • Patent number: 8834841
    Abstract: The present invention provides novel amino acid compounds useful in detecting and evaluating brain and body tumors. These compounds have the advantageous properties of rapid uptake and prolonged retention in tumors and can be labeled with halogen isotopes such as fluorine-18, iodine-123, iodine-124, iodine-125, iodine-131, bromine-75, bromine-76, bromine-77, bromine-82, astatine-210, astatine-211, and other astatine isotopes. These compounds can also be labeled with technetium and rhenium isotopes using known chelation complexes. The compounds disclosed herein bind tumor tissues in vivo with high specificity and selectivity when administered to a subject. Preferred compounds show a target to non-target ratio of at least 2:1, are stable in vivo and substantially localized to target within 1 hour after administration. Preferred compounds include 1-amino-2-[18F]fluorocyclobutyl-1-carboxylic acid (2-[18F]FACBC) and 1-amino-2-[18]fluoromethylcyclobutyl-1-carboxylic acid (2-[18F]FMACBC).
    Type: Grant
    Filed: April 5, 2013
    Date of Patent: September 16, 2014
    Assignee: Emory University
    Inventor: Mark M. Goodman
  • Patent number: 8828908
    Abstract: Bicyclic dione compounds of formula (I), and derivatives thereof, which are suitable for use as herbicides.
    Type: Grant
    Filed: May 27, 2008
    Date of Patent: September 9, 2014
    Assignee: Syngenta Limited
    Inventors: Christopher John Mathews, Matthew Brian Hotson, Alan John Dowling, James Nicholas Scutt, Mangala Govenkar, Lee Challinor
  • Patent number: 8779153
    Abstract: A compound of Formula (I) or a pharmaceutically acceptable salt thereof: Wherein: Het is a 5 to 10-membered heteroaromatic ring; Either X is N and Y is CR5; or X is C and Y is S; Z is selected from N and CH; R1 is selected from H and C1-2alkyl; R2 is selected from H, C1-2alkyl, OH, —CH2OH and C1-2alkoxy; Each R3 is independently selected from OH, C1-3alkyl, F, Cl, Br, NH2, and C1-3alkoxy; R4 is selected from C1-3alkyl and haloC1-3alkyl; R5 is selected from H, C1-3alkyl and haloC1-3alkyl; R6 and R7 are either i) each independently selected from H, C1-3alkyl and C1-3alkoxy; or ii) R6 and R7 together with the ring to which they are attached form a 9-membered bicylic ring; p is 0-3; and RA is selected from H and C1-3alkyl, compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.
    Type: Grant
    Filed: October 11, 2011
    Date of Patent: July 15, 2014
    Assignee: Glaxo Group Limited
    Inventors: Julia Castro Pichel, Raquel Fernandez Menendez, Esther Pilar Fernandez Velando, Silvia Gonzalez Del Valle, Araceli Mallo-Rubio
  • Patent number: 8772510
    Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R5, W, X, X1, Y, Y1, Z and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used in the treatment of CNS disorders such as schizophrenia, Alzheimer's disease, and Parkinson's disease.
    Type: Grant
    Filed: August 30, 2012
    Date of Patent: July 8, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Stephan Bachmann, Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Markus Rudolph
  • Publication number: 20140162985
    Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Application
    Filed: September 6, 2013
    Publication date: June 12, 2014
    Applicant: ABBVIE INC.
    Inventors: Andrew Burchat, Thomas D. Gordon, Kelly D. Mullen, David C. Ihle, Michael J. Morytko, Kevin P. Cusack, Gloria Y. Lo Schiavo, Lei Wang, Michael Friedman
  • Patent number: 8748463
    Abstract: The invention provides novel classes of HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided as well as methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention.
    Type: Grant
    Filed: July 17, 2012
    Date of Patent: June 10, 2014
    Assignee: Georgetown University
    Inventors: Alan P. Kozikowski, Anatoly Dritschilo, Mira Jung, Pavel A. Petukhov, Bin Chen
  • Patent number: 8685369
    Abstract: One aspect of the invention relates to complexes of a radionuclide with various heteroaryl ligands, e.g., imidazolyl and pyridyl ligands, and their use in radiopharmaceuticals for a variety of clinical diagnostic and therapeutic applications. Another aspect of the invention relates to imidazolyl and pyridyl ligands that form a portion of the aforementioned complexes. Methods for the preparation of the radionuclide complexes are also described. Another aspect of the invention relates to imidazolyl and pyridyl ligands based on derivatized lysine, alanine and bis-amino acids for conjugation to small peptides by solid phase synthetic methods. Additionally, the invention relates to methods for imaging regions of a mammal using the complexes of the invention.
    Type: Grant
    Filed: February 14, 2005
    Date of Patent: April 1, 2014
    Assignee: Molecular Insight Pharmaceuticals, Inc.
    Inventors: John Babich, Kevin Maresca, James Kronauge
  • 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: 8664403
    Abstract: The present invention relates to a process for the preparation of S-[2-[1-(2-ethylbutyl)cyclohexylcarbonylamino]-phenyl]2-methylthiopropionate which is useful as a pharmaceutically active compound.
    Type: Grant
    Filed: December 13, 2011
    Date of Patent: March 4, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans-Juergen Mair, Reinhard Reents, Michelangelo Scalone, Shaoning Wang, Andreas Zogg
  • Patent number: 8653114
    Abstract: The present invention relates to O-CYCLOPROPYLCYCLOHEXYL-CARBOXANILIDES derivatives of formula (I); their process of preparation, their use as fungicide, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Grant
    Filed: June 1, 2011
    Date of Patent: February 18, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Jörg Nico Greul, Jürgen Benting, Peter Dahmen, Ulrike Wachendorff-Neumann
  • Patent number: 8653278
    Abstract: One aspect of the invention relates to isoform-selective HDAC inhibitors. Also provided are methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy. The invention also provides methods for treating cancer, methods for treating neurological diseases and methods for treating malaria. Additionally, the invention provides pharmaceutical compositions comprising an HDAC inhibitor of the invention; and kits comprising an HDAC inhibitor of the invention.
    Type: Grant
    Filed: August 2, 2007
    Date of Patent: February 18, 2014
    Assignees: Georgetown University, The Board of Trustees of the University of Illinois
    Inventors: Alan P. Kozikowski, Mira Jung, Anatoly Dritschilo, Arsen Gaysin, Pavel A. Petukhov, Werner Tueckmantel, Hongbin Yuan, Yufeng Chen
  • Patent number: 8642634
    Abstract: Disclosed are compounds of Formulae 1, 1A, 1B and 1C including all geometric and stereoisomers, N-oxides, and salts thereof, wherein R1, R2, R4a1, R4a2, A, Aa, G, M, W, Z1, Z3, X, J, J1 and n 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: Grant
    Filed: July 27, 2007
    Date of Patent: February 4, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: Robert James Pasteris, Mary Ann Hanagan
  • Patent number: 8637673
    Abstract: Process for preparing 2,2-difluoroethylamine derivatives, wherein compounds of the general formula (IV) are hydrogenated to the corresponding 2,2-difluoroethylamine derivatives of the general formula (III), where the A, R1 and R2 radicals are each as defined in the description:
    Type: Grant
    Filed: March 8, 2010
    Date of Patent: January 28, 2014
    Assignee: Bayer Cropscience AG
    Inventors: Norbert Lui, Stefan Antons
  • Patent number: 8609839
    Abstract: Camphor-derived compounds are disclosed, which are represented as the following formula (I): wherein R1, R2, R3, and R4 each are defined as described in the specification. In addition, a method for manufacturing the camphor-derived compounds and application thereof are disclosed.
    Type: Grant
    Filed: January 19, 2011
    Date of Patent: December 17, 2013
    Assignee: National Tsing Hua University
    Inventors: Biing-Jiun Uang, Bo-Yao Yang
  • Publication number: 20130319530
    Abstract: The present invention provides a compound useful as a photoelectric conversion dye having excellent photoelectric conversion performance. The compound according to the present invention is a thiazole-based compound represented by the following general formula (1), a tautomer or stereoisomer thereof, or a salt thereof. In the general formula (1), R1 represents a hydrogen atom, a substituted or unsubstituted, linear or branched alkyl group, or a substituted or unsubstituted aryl group, R2 represents a hydrogen atom, a substituted or unsubstituted, linear or branched alkyl group, or a cyano group, D represents an organic group comprising an electron-donating substituent, Z represents a linking group having a heteroaromatic ring or at least one hydrocarbon group selected from the group consisting of an aromatic ring, a vinylene group (—CH?CH—), or an ethynylene group (—C?C—), and M represents a hydrogen atom or a salt-forming cation.
    Type: Application
    Filed: February 13, 2012
    Publication date: December 5, 2013
    Applicant: NEC CORPORATION
    Inventors: Katsumi Maeda, Shin Nakamura, Kentaro Nakahara, Terumasa Shimoyama
  • Patent number: 8592467
    Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
    Type: Grant
    Filed: June 22, 2009
    Date of Patent: November 26, 2013
    Assignee: Abbvie Inc.
    Inventors: Marlon D. Cowart, Minghua Sun, Chen Zhao, Guo Zhu Zheng
  • Patent number: 8592465
    Abstract: Compounds according to formula (I) are disclosed where Q is S, N, or O; X is optional, and can be O?, S?, ?N—NH2, ?N—OH, or —OH; Y is optional and can be —N(H)—, O, or C1 to C20 hydrocarbon; and R1 and R2 are each independently substituted or unsubstituted single-, fused- or multiple-ring aryl or (hetero)cyclic ring systems. Methods of making these compounds, pharmaceutical compositions containing the compounds, and their use, particularly for treating or preventing cancer, are also disclosed.
    Type: Grant
    Filed: June 16, 2009
    Date of Patent: November 26, 2013
    Assignees: University of Tennessee Research Foundation, The Ohio State University Research Foundation
    Inventors: Duane D. Miller, Wei Li, Zhao Wang, Yan Lu, Jianjun Chen, James T. Dalton, Chien-Ming Li
  • Patent number: 8586325
    Abstract: Enzyme substrates and associated technology of the present invention are provided. An enzyme substrate of the invention may comprise a biologically functional fluorescent dye and an enzyme-specific substrate moiety attached in such a way that the functionality of the functional dye is diminished. An enzymatic reaction may cleave at least a portion of the substrate moiety from the enzyme substrate to provide a more functional product dye. This product dye may be nonfluorescent or weakly fluorescent, in general, and relatively fluorescent, in a particular condition, such as when bound to a partner biological molecule or an assembly of partner biological molecules. An enzyme substrate of the present invention may thus be useful in fluorescence detection, and/or in any of a variety of useful applications, such as the detection of enzymatic activity in a cell-free system or in a living cell, the screening of drugs, or the diagnosis of disease.
    Type: Grant
    Filed: May 10, 2013
    Date of Patent: November 19, 2013
    Assignee: Biotium, Inc.
    Inventors: Fei Mao, Hui Cen
  • Patent number: 8580710
    Abstract: The present invention relates to pesticidal mixtures comprising as active compounds 1) at least one aminothiazoline compound I of formula I: wherein variables R1, R2, R3, R4, R5, and R6 are as defined in the description of the application and 2) at least one active compound II selected from group A as defined in the description, use of these mixtures for combating insects, acarids, or nematodes, and a method for treating, controlling, preventing or protecting animals against infestation or infection by parasites using these mixtures.
    Type: Grant
    Filed: March 24, 2009
    Date of Patent: November 12, 2013
    Assignee: BASF SE
    Inventors: Markus Kordes, Ronan Le Vezouet, Jürgen Langewald, Ralph Paulini, Deborah L. Culbertson, Douglas D. Anspaugh, Luiz Antonio Jose, Faraneh Oloumi
  • Patent number: 8575356
    Abstract: The present invention relates to novel heterocyclic alkanol derivatives, to processes for preparing these compounds, to compositions comprising these compounds and to their use as biologically active compounds, in particular for controlling harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.
    Type: Grant
    Filed: May 27, 2011
    Date of Patent: November 5, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Carl Friedrich Nising, Pierre Cristau, Hendrik Helmke, Gorka Peris, Tomoki Tsuchiya, Pierre Wasnaire, Jürgen Benting
  • Patent number: 8557805
    Abstract: The present invention provides an agent for the prophylaxis or treatment of diabetes, obesity and the like, a glucokinase activator, containing a compound represented by the formula (I): wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof.
    Type: Grant
    Filed: December 28, 2009
    Date of Patent: October 15, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tsuneo Yasuma, Nobuyuki Takakura, Yasufumi Miyamoto