Chalcogen Attached Directly To The 1,2-diazole Ring By Nonionic Bonding Patents (Class 546/276.1)
  • Patent number: 10414733
    Abstract: The present invention relates to a process for preparing a pyrazole compound of formula V, the process including cyclizing a hydrazone substituted ?,?-unsaturated carbonyl compound of formula IV by reacting it with a suitable reagent, e.g. a reducing agent, an organometallic reagent or a nucleophilic reagent. The compounds of formula V are versatile reaction tools for the preparation of pyrazole derived fine chemicals. The present invention also relates to pyrazole compounds of formulae Va, Vb, Vc, and VI.
    Type: Grant
    Filed: July 30, 2015
    Date of Patent: September 17, 2019
    Assignee: BASF SE
    Inventors: Birgit Gockel, Daniel Saelinger, Sebastian Soergel, Michael Rack
  • Patent number: 10173996
    Abstract: Provided herein are substituted pyrazolylpyridine, pyrazolylpyridazine, and pyrazolylpyrimidine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Grant
    Filed: February 16, 2017
    Date of Patent: January 8, 2019
    Assignee: Celgene Quanticel Research, Inc.
    Inventors: Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
  • Patent number: 10005758
    Abstract: 3-(3-chloro-1H-pyrazol-1-yl)pyridine is prepared by cyclizing 3-hydrazinopyridine-.dihydrochloride with a dialkyl maleate to provide an alkyl 5-oxo-2-(pyridin-3-yl)pyrazolidine-3-carboxylate, by chlorinating to provide an alkyl 3-chloro-1-(pyridin-3-yl)-4,5-dihydro-1H-pyrazole-5-carboxylate, by oxidizing to provide an alkyl 3-chloro-1-(pyridin-3-yl)-1H-pyrazole-5-carboxylate, by converting the ester to the carboxylic acid by hydrolysis to provide 3-chloro-1-(pyridin-3-yl)-1H-pyrazole-5-carboxylic acid hydrochloride, and by removing the carboxylic acid by a decarboxylation reaction.
    Type: Grant
    Filed: October 13, 2017
    Date of Patent: June 26, 2018
    Assignee: Dow AgroSciences LLC
    Inventors: Qiang Yang, Beth Lorsbach, David E. Podhorez
  • Patent number: 9809570
    Abstract: 3-(3-chloro-1H-pyrazol-1-yl)pyridine is prepared by cyclizing 3-hydrazinopyridine-•dihydrochloride with a dialkyl maleate to provide an alkyl 5-oxo-2-(pyridin-3-yl)pyrazolidine-3-carboxylate, by chlorinating to provide an alkyl 3-chloro-1-(pyridin-3-yl)-4,5-dihydro-1H-pyrazole-5-carboxylate, by oxidizing to provide an alkyl 3-chloro-1-(pyridin-3-yl)-1H-pyrazole-5-carboxylate, by converting the ester to the carboxylic acid by hydrolysis to provide 3-chloro-1-(pyridin-3-yl)-1H-pyrazole-5-carboxylic acid hydrochloride, and by removing the carboxylic acid by a decarboxylation reaction.
    Type: Grant
    Filed: October 27, 2016
    Date of Patent: November 7, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: Qiang Yang, Beth Lorsbach, David E. Podhorez
  • Patent number: 9663489
    Abstract: This disclosure relates to the field of preparation of 3-(3-chloro-1H-pyrazol-1-yl)pyridine and intermediates therefrom. These intermediates are useful in the preparation of certain pesticides.
    Type: Grant
    Filed: July 28, 2016
    Date of Patent: May 30, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: Xiaoyong Li, Qiang Yang, Beth Lorsbach
  • Patent number: 9604961
    Abstract: Provided herein are substituted pyrazolylpyridine, pyrazolylpyridazine, and pyrazolylpyrimidine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Grant
    Filed: December 5, 2013
    Date of Patent: March 28, 2017
    Assignee: Celgene Quanticel Research, Inc.
    Inventors: Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
  • Patent number: 9522900
    Abstract: 3-(3-chloro-1H-pyrazol-1-yl)pyridine is prepared by cyclizing 3-hydrazinopyridine-.dihydrochloride with a dialkyl maleate to provide an alkyl 5-oxo-2-(pyridin-3-yl)pyrazolidine-3-carboxylate, by chlorinating to provide an alkyl 3-chloro-1-(pyridin-3-yl)-4,5-dihydro-1H-pyrazole-5-carboxylate, by oxidizing to provide an alkyl 3-chloro-1-(pyridin-3-yl)-1H-pyrazole-5-carboxylate, by converting the ester to the carboxylic acid by hydrolysis to provide 3-chloro-1 -(pyridin-3-yl)-1H-pyrazole-5-carboxylic acid hydrochloride, and by removing the carboxylic acid by a decarboxylation reaction.
    Type: Grant
    Filed: July 28, 2015
    Date of Patent: December 20, 2016
    Assignee: Dow AgroSciences LLC
    Inventors: Qiang Yang, Beth Lorsbach, David E. Podhorez
  • Patent number: 9174962
    Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
    Type: Grant
    Filed: October 17, 2014
    Date of Patent: November 3, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: Qiang Yang, Beth Lorsbach, Greg Whiteker, Gary Roth, Carl DeAmicis, Thomas Clark, Kaitlyn Gray, Yu Zhang, Joseck M. Muhuhi
  • Publication number: 20150112077
    Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Inventors: Qiang YANG, Beth LORSBACH, Gary ROTH, Noormohamed M. NIYAZ, Jeffrey NISSEN, Ronald ROSS, JR., Gregory T. WHITEKER, Carl DeAMICIS, Kaitlyn GRAY, Yu ZHANG
  • Publication number: 20150111925
    Abstract: The present invention relates to compounds described herein Formula (I) and pharmaceutical acceptable salts thereof, which modulate the activity of calcium release-activated calcium (CRAC) channel. The invention also describes the compounds of Formula (I) and pharmaceutical compositions containing such compounds thereof for treating, managing, and/or lessening the severity of diseases, disorders, syndromes or conditions associated with the modulation of calcium release-activated calcium (CRAC) channel.
    Type: Application
    Filed: May 1, 2013
    Publication date: April 23, 2015
    Inventors: Nageswara Rao Irlapati, Gokul Keruji Deshmukh, Nilesh Raghunath Khedkar, Kiran Chandrashekhar Kulkarni, Zubair Abdul Wajid Shaikh, Neelima Sinha, Venkata P. Palle, Rajender Kumar Kamboj
  • Publication number: 20150112078
    Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Inventors: Qiang YANG, Beth LORSBACH, Gregory T. WHITEKER, Gary ROTH, Carl DeAMICIS, Daniel I. KNUEPPEL, Ann M. BUYSSE, Kaitlyn GRAY, Xiaoyong LI, Joseck M. MUHUHI, Ronald ROSS, JR., David E. PODHOREZ, Yu ZHANG
  • Patent number: 8987461
    Abstract: Provided herein are substituted pyrazolylpyridine, pyrazolylpyridazine, and pyrazolylpyrimidine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Grant
    Filed: December 5, 2013
    Date of Patent: March 24, 2015
    Assignee: Quanticel Pharmaceuticals, Inc.
    Inventors: Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennen Wallace
  • Patent number: 8975282
    Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Grant
    Filed: July 19, 2013
    Date of Patent: March 10, 2015
    Assignees: Sunshine Lake Pharma Co., Ltd., Calitor Sciences, LLC
    Inventors: Ning Xi, Yanjun Wu, Min Liao, Yanming Feng
  • Patent number: 8969388
    Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Grant
    Filed: July 19, 2013
    Date of Patent: March 3, 2015
    Assignees: Sunshine Lake Pharma Co., Ltd., Calitor Sciences, LLC
    Inventors: Ning Xi, Yanjun Wu, Min Liao, Yanming Feng
  • Patent number: 8969338
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein U, V, Y, R1, R2, R2?, R3, R3? and R8 are described herein. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Grant
    Filed: September 27, 2012
    Date of Patent: March 3, 2015
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Publication number: 20150057448
    Abstract: Provided are intermediates having the formulas wherein R2, R3, and L are as defined in the specification, which are useful in the preparation of pyridin-2-yl-amino-1,2,4-thiadiazole derivatives.
    Type: Application
    Filed: September 23, 2014
    Publication date: February 26, 2015
    Inventors: Thomas Daniel Aicher, Steven Armen Boyd, Mark Joseph Chicarelli, Kevin Ronald Condroski, Jay Bradford Fell, John P. Fischer, Indrani W. Gunawardana, Ronald Jay Hinklin, Ajay Singh, Timothy M. Turner, Eli M. Wallace
  • Patent number: 8962623
    Abstract: A compound of formula (I): wherein all symbols have the same meanings as defined in the specification; a salt thereof, a solvate thereof, an N-oxide thereof, or a prodrug thereof, has an Itk inhibitory activity, and is useful as a method for preventing and/or treating atopic dermatitis, and the like.
    Type: Grant
    Filed: February 29, 2012
    Date of Patent: February 24, 2015
    Assignee: Locus Pharmaceuticals, Inc.
    Inventors: Rupa S. Shetty, Martha J. Kelly, Bin Liu, Jinming Zou, Kristofer K. Moffett, Younghee Lee, Dora Do-York Wong
  • Publication number: 20150050239
    Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Application
    Filed: July 19, 2013
    Publication date: February 19, 2015
    Applicants: Calitor Sciences, LLC, Sunshine Lake Pharma Co., Ltd.
    Inventors: Ning Xi, Yanjun Wu, Min Liao, Yanming Feng
  • Patent number: 8957254
    Abstract: Process for synthesizing a chemical, in particular an agriculturally or pharmaceutically active compound, including: a first step comprising reacting a carboxylic acid halide with a vinyl ether to prepare a halogenated precursor of an alkenone; a second step comprising eliminating hydrogen halide from such precursor to form an alkenone, preferably by thermolysis under specific conditions; and a third step which uses the formed alkenone as a building block to synthesize the chemical. First step may be done in a liquid reaction medium comprising an alkenone or a halogenated alkenone precursor, or in a liquid reaction medium in turbulent state, specifically by creation of gas bubbles of the carboxylic acid halide herein. Second step may include a flash thermolysis, vacuum thermolysis, thermolysis under stripping with inert gas, and/or a thermolysis at a temperature from >90° C. to 120° C. Third step preferably comprises reacting the alkenone with a nitrogen-containing compound.
    Type: Grant
    Filed: October 4, 2013
    Date of Patent: February 17, 2015
    Assignee: Solvay SA
    Inventors: Max Braun, Stefan Palsherm, Uta Claassen, Alain Lambert
  • Publication number: 20150037280
    Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Application
    Filed: July 19, 2013
    Publication date: February 5, 2015
    Applicants: Sunshine Lake Pharma Co., Ltd., Calitor Sciences, LLC
    Inventors: Ning Xi, Yanjun Wu, Min Liao, Yanming Feng
  • Patent number: 8946250
    Abstract: 3,4-diarylpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
    Type: Grant
    Filed: August 20, 2013
    Date of Patent: February 3, 2015
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Maurizio Pulici, Fabio Zuccotto, Gabriella Traquandi, Sonia Biondaro, Paolo Trifiro′, Alessandra Badari, Stefano Nuvoloni, Giovanni Cervi, Chiara Marchionni, Michele Modugno
  • Publication number: 20150011552
    Abstract: The present invention provides a compound which enhances the production of erythropoietin. The present invention provides, for example, a compound represented by the formula (1) wherein R1: -Q1, -Q1-X-Q2, or -Q1-X-Q2-Y-Q3: a monocyclic or bicyclic aromatic heterocyclic group; Q2, Q3: an aromatic hydrocarbon ring group or a monocyclic aromatic heterocyclic group; X: —CONH—, —CONHCH2—, —CH2OCH2—, —NHCH2CH2—, or the like; Y: a single bond, —O—, —(CH2)n—, or —O—(CH2)n—; m, n: an integer from 1 to 3; R2: H or an alkyl group; and R3: H, an alkoxycarbonyl group, a carboxy group, an aromatic hydrocarbon ring group, or a monocyclic aromatic heterocyclic group.
    Type: Application
    Filed: September 24, 2014
    Publication date: January 8, 2015
    Inventors: Atsunobu SAKAMOTO, Naoki TANAKA, Takeshi FUKUDA
  • Patent number: 8927581
    Abstract: The present invention relates to fungicide N-(2-pyridylpropyl)carboxamide derivative and its oxa, aza and thia analogs of formula (I), their process of preparation and intermediate compound for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions. wherein A, T, W, X, n and Z3 to Z7 represent various substituents.
    Type: Grant
    Filed: August 6, 2009
    Date of Patent: January 6, 2015
    Assignee: Bayer Cropscience AG
    Inventors: Samir Bennabi, Pierre-Yves Coqueron, Philippe Desbordes, Stéphanie Gary, Rachel Rama, Philippe Rinolfi, Jürgen Benting, Peter Dahmen
  • Patent number: 8916591
    Abstract: Compounds of formula (I) have checkpoint kinase 1 (CHK1) inhibitory activity: wherein R1, R2, R5 and R6 are independently selected from hydrogen, hydroxy, methyl, trifluoromethyl, hydroxymethyl, methoxy, trifluoromethoxy, methylamino and dimethylamino; R3, and R4 are independently selected from hydrogen, hydroxy, C1-C3 alkyl, fluoro-(C1-C3)-alkyl, hydroxy-(C1C3)-alkyl, C1-C3 alkoxy, fluoro-(C1-C3)-alkoxy, hydroxy-(C1-C3)-alkoxy, -AIk-N(R11)—R12, -0-AIk-N(R11)—R12, —C(?O)OH, carboxy-(C1-C3)-alkyl, or —C(?O)—NH—R13; AIk is a straight or branched chain divalent C1-C6 alkylene radical; R7 and R8 are independently selected from hydrogen, hydroxy, or C1-C3 alkoxy; X is a straight chain divalent C1-C3 alkylene radical, optionally substituted on one or more carbons by R9 and/or R10; W is selected from —C(?O)—N(—R16)— or —N(—R17)—C(?O)—; Y is hydrogen, C1-C3 alkyl, C1-C3 alkoxy, or halo; and Q is selected from optionally substituted phenyl, optionally substituted cyclohexyl, or an optionally substituted 6-membered mon
    Type: Grant
    Filed: January 20, 2009
    Date of Patent: December 23, 2014
    Assignee: Vernalis (R&D) Ltd
    Inventors: Stephen Stokes, Nicolas Foloppe, Andrea Fiumana, Martin Drysdale, Simon Bedford, Paul Webb
  • Patent number: 8895600
    Abstract: The present invention refers to compounds with inhibitory activity against 14-3-3 proteins and their use in the treatment of tumors, in particular chronic myeloid leukemia. The invention also provides methods for the identification of 14-3-3 protein inhibitors.
    Type: Grant
    Filed: August 9, 2012
    Date of Patent: November 25, 2014
    Assignee: Università degli Studi di Siena
    Inventors: Maurizio Botta, Valentina Corradi, Federico Falchi, Manuela Mancini, Maria Alessandra Santucci
  • Patent number: 8895588
    Abstract: Provided is a compound having a superior acid secretion suppressive action, antiulcer activity and the like. A compound represented by the formula wherein R1 is a substituent, R2 is (i) a hydrogen atom, (ii) a C1-6 alkyl group optionally having a halogen atom or (iii) a cyano group, R3 is (i) a hydrogen atom, (ii) a halogen atom, (iii) a cyano group, (iv) a C1-6 alkyl group optionally having a halogen atom or a C1-6 alkoxy group optionally having a halogen atom, one of R2 and R3 is a hydrogen atom, and the other is a substituent other than a hydrogen atom, or a salt thereof.
    Type: Grant
    Filed: March 25, 2010
    Date of Patent: November 25, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Haruyuki Nishida, Ikuo Fujimori
  • Publication number: 20140323729
    Abstract: Compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.
    Type: Application
    Filed: May 15, 2014
    Publication date: October 30, 2014
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Francesco G. Salituro, Jeffrey O. Saunders
  • Publication number: 20140296200
    Abstract: The present invention provides compounds of the formula: which are useful as inhibitors of PHD, pharmaceutical compositions thereof, methods for treatment of conditions associated with HIF, processes for making the compounds and intermediates thereof.
    Type: Application
    Filed: March 26, 2014
    Publication date: October 2, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Jason W. Brown, Melinda Davis, Anthony Ivetac, Benjamin Jones, Andre A. Kiryanov, Jon Kuehler, Marion Lanier, Joanne Miura, Sean Murphy, Xiaolun Wang
  • Publication number: 20140243366
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: May 1, 2014
    Publication date: August 28, 2014
    Applicant: CalciMedica, Inc.
    Inventors: Jeffrey P. WHITTEN, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Patent number: 8785646
    Abstract: There is provided a process for producing an amide compound having an excellent harmful arthropod-controlling activity and represented by the formula (3): wherein R1, R2 and R3 independently represent a C1-C6 alkyl group optionally substituted with at least one halogen atom etc., R4, R5, R6 and R7 independently represent a halogen atom etc.
    Type: Grant
    Filed: January 18, 2013
    Date of Patent: July 22, 2014
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Yoshihiko Nokura, Hiroshi Ikegami, Markus Jachmann
  • Patent number: 8785372
    Abstract: Provided are 1-aryl-5-alkyl pyrazole compounds, of formula (I): wherein: R1 is hydrogen, cyano, halogen, R8, formyl, —C(O)R8, —C(O)OR8, —C(O)NR9R10, or —C(S)NH2; R2 is R8 or —S(O)mR11; R3 is methyl, ethyl or C1-C4 haloalkyl; R4, R5 and R7 are independently hydrogen, halogen, alkyl, haloalkyl, cyano or nitro; R6 is halogen, alkyl, haloalkyl, alkoxy, haloalkyloxy, cyano, nitro, —C(O)R12, —S(O)nR12 or SF5; Z is a nitrogen atom or C—R13; R8 is alkyl, haloalkyl, cycloalkyl or halocycloalkyl; R9 is hydrogen, alkyl, haloalkyl or alkoxy; R10 is hydrogen, alkyl, haloalkyl or alkoxy; R11 is alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl or cycloalkyl; R12 is alkyl or haloalkyl; R13 is hydrogen, halogen, cyano, nitro, alkyl, haloalkyl, alkoxy or haloalkoxy; m is 0, 1 or 2; and n is 0, 1 or 2; or a salt thereof, the method of making compounds of formula (I) and the use of these compounds against ectoparasites, endoparasites and pests.
    Type: Grant
    Filed: May 15, 2013
    Date of Patent: July 22, 2014
    Assignee: Aventis Agriculture
    Inventors: Hyoung Ik Lee, Loic Patrick Le Hir de Fallois, Philip Reid Timmons, William Glenn Cawthorne, Adalberto Perez de Leon
  • Publication number: 20140194469
    Abstract: Provided herein are substituted pyrazolylpyridine, pyrazolylpyridazine, and pyrazolylpyrimidine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Application
    Filed: December 5, 2013
    Publication date: July 10, 2014
    Applicant: Quanticel Pharmaceuticals, Inc.
    Inventors: Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennen Wallace
  • Patent number: 8772289
    Abstract: N-Thio-anthranilamid compounds of formula (I) wherein A is A1 wherein the variables and the indices are as defined per the description, processes for preparing the compounds I, pesticidal compositions comprising compounds I, use of compounds I for the control of insects, acarids or nematodes, and methods for treating, controlling, preventing or protecting animals against infestation or infection by parasites by use of compounds of formula I.
    Type: Grant
    Filed: November 20, 2012
    Date of Patent: July 8, 2014
    Assignee: BASF SE
    Inventors: Thomas Schmidt, Michael Puhl, Joachim Dickhaut, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Franz-Josef Braun, Toni Bucci, Henry Van Tuyl Cotter, David G. Kuhn, Hassan Oloumi-Sadeghi
  • Publication number: 20140187529
    Abstract: A compound of formula (I): wherein all symbols have the same meanings as defined in the specification; a salt thereof, a solvate thereof, an N-oxide thereof, or a prodrug thereof, has an Itk inhibitory activity, and is useful as a method for preventing and/or treating atopic dermatitis, and the like.
    Type: Application
    Filed: February 29, 2012
    Publication date: July 3, 2014
    Applicant: LOCUS PHARMACEUTICALS, INC.
    Inventors: Rupa S. Shetty, Martha J. Kelly, Bin Liu, Jinming Zou, Kristopher K. Moffett, Younghee Lee
  • Patent number: 8748461
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: June 19, 2012
    Date of Patent: June 10, 2014
    Assignee: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Zachary A. Buchan, Michael T. Sullenberger, Gary D. Gustafson
  • Patent number: 8742119
    Abstract: Compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.
    Type: Grant
    Filed: October 6, 2011
    Date of Patent: June 3, 2014
    Assignee: Agios Pharmaceuticals, Inc.
    Inventors: Francesco G. Salituro, Jeffrey O. Saunders
  • Patent number: 8722208
    Abstract: Disclosed is an organic electroluminescent device (organic EL device) which is improved in luminous efficiency, fully secured of high driving stability, and of a simple structure. The organic EL device is constituted of an anode, organic layers containing a phosphorescent light-emitting layer, and a cathode piled one upon another on a substrate and a phosphine oxide derivative represented by general formula (1) is contained in a phosphorescent light-emitting layer, an electron-transporting layer, a hole-blocking layer, or an exciton-blocking layer. In general formula (1), L1 is a direct bond or an aromatic group with a valence of 1-3 and Ar1 is an aromatic group. The two Ar1 groups linked to the same nitrogen atom may form a nitrogen heterocycle and may further form a fused ring together with the said nitrogen heterocycle.
    Type: Grant
    Filed: February 25, 2010
    Date of Patent: May 13, 2014
    Assignee: Nippon Steel & Sumikin Chemical Co., Ltd.
    Inventors: Takahiro Kai, Hideki Tanaka, Mitsuru Suda, Toshihiro Yamamoto, Megumi Matsumoto
  • Patent number: 8722709
    Abstract: Mineralocorticoid receptor antagonists, of which the following is exemplary.
    Type: Grant
    Filed: November 7, 2011
    Date of Patent: May 13, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Xin Guo, Stephen J. Boyer, Di Wu, Frank Wu
  • Publication number: 20140128406
    Abstract: The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R10R11)—C(?O)—, x-C(R12R13)—C(?S)—, x-O—C(?O)—, x-O—C(?S)—, x-N(R14)—C(?O)—, x-N(R15)—C(?S)—, x-C(R16R17)—SO2— or x-N?C(R30)—, in each case x indicates the bond that is connected to R1; T is CR18 or N; Y1, Y2, Y3, and Y4 are independently CR19 or N; Q is O or S; n is 1 or 2; p is 1 or 2, providing that when n is 2, p is 1.
    Type: Application
    Filed: June 27, 2012
    Publication date: May 8, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Sarah Sulzer-Mosse, Clemens Lamberth, Fredrik Emil Malcolm Cederbaum
  • Publication number: 20140128418
    Abstract: The present invention provides a pyrazole derivative compound and a pharmaceutically acceptable salt thereof. The compound of the invention is remarkably effective for preventing and treating osteoporosis.
    Type: Application
    Filed: February 27, 2012
    Publication date: May 8, 2014
    Applicant: EWHA UNIVERSITY-INDUSTRY COLLABORATION FOUNDATION
    Inventors: Yun Soo Bae, Kee In Lee, Jee Hyun Lee, Soo Young Lee, Sun Choi
  • Patent number: 8685974
    Abstract: Thienylpyri(mi)dinylazole of the formula (I) in which R1 to R8 and X1 have the meanings given in the description, and agrochemically active salts, to their use and to methods and compositions for controlling phytopathogenic harmful fungi in and/or on plants or in and/or on seed of plants and for reducing mycotoxins in plants and parts of the plants, to processes for preparing such compounds and compositions and treated seed and also to their use for controlling phytopathogenic harmful fungi in agriculture, horticulture, forestry, in animal husbandry, in the protection of materials, in the domestic and hygiene field and for the reduction of mycotoxins in plants and parts of the plants.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: April 1, 2014
    Assignee: Bayer CropScience AG
    Inventors: Alexander Sudau, Mazen Es-Sayed, Julia Neumann, Catherine Sirven, Jürgen Benting, Christoph Andreas Braun, Ruth Meissner, Anne-Sophie Rebstock, Samir Bennabi, Philippe Desbordes, Arounarith Tuch, Philippe Rinolfi, Stephane Brunet, Hiroyuki Hadano, Marie-Claire Grosjean-Cournoyer
  • Publication number: 20140073629
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: September 3, 2013
    Publication date: March 13, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Jehrod Burnett BRENNEMAN, John GINN, Michael D. LOWE, Christopher Ronald SARKO, Edward S. TASBER, Zhonghua ZHANG
  • Publication number: 20140066404
    Abstract: The present invention provides pyrazole derivative compounds and pharmaceutically acceptable salts thereof. The compounds of the present invention have an excellent effect of preventing and treating osteoporosis.
    Type: Application
    Filed: November 6, 2013
    Publication date: March 6, 2014
    Applicant: EWHA UNIVERSITY-INDUSTRY COLLABORATION FOUNDATION
    Inventors: Yun Soo Bae, Jee Hyun Lee, Mi Sun Seo, Soo Young Lee, Sun Choi, Kee In Lee, Hye Rin Bin, Do Min Lee
  • Publication number: 20140045859
    Abstract: Compounds are provided for use with glucokinase that comprise the formula: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
    Type: Application
    Filed: October 2, 2013
    Publication date: February 13, 2014
    Applicant: Takeda California, Inc.
    Inventors: Zacharia Cheruvallath, Stephen L. Gwaltney, Andrew John Jennings, Mark Sabat, Mingnam Tang, Haixia Wang, Jeffrey A. Stafford
  • Patent number: 8648088
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein G, X, R1, R2, R3, R3?, R4, and R4? are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Grant
    Filed: April 24, 2012
    Date of Patent: February 11, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Publication number: 20130330366
    Abstract: In one aspect, the invention relates to compounds having the formula XII: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
    Type: Application
    Filed: June 6, 2013
    Publication date: December 12, 2013
    Inventors: Adam D. Hughes, Melissa Fleury
  • Publication number: 20130324457
    Abstract: Provided are 1-aryl-5-alkyl pyrazole compounds, of formula (I): wherein: R1 is hydrogen, cyano, halogen, R8, formyl, —C(O)R8, —C(O)OR8, —C(O)NR9R10, or —C(S)NH2; R2 is R8 or —S(O)mR11; R3 is methyl, ethyl or C1-C4 haloalkyl; R4, R5 and R7 are independently hydrogen, halogen, alkyl, haloalkyl, cyano or nitro; R6 is halogen, alkyl, haloalkyl, alkoxy, haloalkyloxy, cyano, nitro, —C(O)R12, —S(O)nR12 or SF5; Z is a nitrogen atom or C—R13; R8 is alkyl, haloalkyl, cycloalkyl or halocycloalkyl; R9 is hydrogen, alkyl, haloalkyl or alkoxy; R10 is hydrogen, alkyl, haloalkyl or alkoxy; R11 is alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl or cycloalkyl; R12 is alkyl or haloalkyl; R13 is hydrogen, halogen, cyano, nitro, alkyl, haloalkyl, alkoxy or haloalkoxy; m is 0, 1 or 2; and n is 0, 1 or 2; or a salt thereof, the method of making compounds of formula (I) and the use of these compounds against ectoparasites, endoparasites and pests.
    Type: Application
    Filed: May 15, 2013
    Publication date: December 5, 2013
    Applicants: AVENTIS AGRICULTURE, MERIAL LIMITED
    Inventors: Loic Patrick Le Hir de Fallois, Hyoung Ik Lee, Philip Reid Timmons, William Glenn Cawthorne, Jr., Alberto Perez de Leon
  • Patent number: 8598211
    Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3 R4, R5, m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof.
    Type: Grant
    Filed: December 20, 2010
    Date of Patent: December 3, 2013
    Assignees: AbbVie Inc., AbbVie Deutschland GmbH & Co. KG
    Inventors: Andreas Kling, Katja Jantos, Helmut Mack, Achim Möller, Wilfried Hornberger, Gisela Backfisch, Yanbin Lao, Marjoleen Nijsen
  • Publication number: 20130296355
    Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
    Type: Application
    Filed: July 3, 2013
    Publication date: November 7, 2013
    Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Esther Cheng Yin Lee, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
  • Patent number: 8541455
    Abstract: The present invention relates to novel substituted dihydropyrazolone derivatives, to their preparation and to their therapeutic use as activators of the transcription factor HIF.
    Type: Grant
    Filed: June 29, 2011
    Date of Patent: September 24, 2013
    Assignee: Sanofi
    Inventors: Jean-Michel Altenburger, Valérie Fossey, Stéphane Illiano, Géraldine Manette