Nitrogen Attached Directly To The Diazole Ring By Nonionic Bonding Patents (Class 548/371.4)
  • Patent number: 11028265
    Abstract: This disclosure concerns electrically conducting poly(pyrazoles). The concept of oligomerizing and polymerizing substituted aminopyrazole derivatives combined with a monomer activation procedure involving base-mediated conversion of the protonated pyrazole ring nitrogen to amine salt was developed. This disclosure concerns the specific chemistries needed for the synthesis of a pyrazole monomer used in the polymer synthesis. The procedure used for blending the novel polypyrazoles with other compounds needed for construction of solar cells for testing was developed. This disclosure concerns the concept of using these types of heteroatom-rich, electron-deficient oligomers or polymers as n-dopable or p-dopable electron acceptors in photovoltaic cells. This disclosure concerns synthesizing the starting monomer compounds and polypyrazoles.
    Type: Grant
    Filed: December 12, 2018
    Date of Patent: June 8, 2021
    Assignee: The Government of the United States of America, as represented by the Secretary of the Navy
    Inventors: Brett D. Martin, Ian D. Giles, Jawad Naciri, Paul T. Charles, Scott A. Trammell, Jeffrey R. Deschamps, Jeffrey C. Depriest
  • Patent number: 10035774
    Abstract: Pyrazolyl carboxylic acid and pyrazolyl urea derivatives have been synthesized, which are useful in the manufacture of cephalosporin antibiotic compounds.
    Type: Grant
    Filed: December 18, 2015
    Date of Patent: July 31, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kristos Adrian Moshos, Valdas Jurkauskas, Yisheng Yang, Youchu Wang
  • Patent number: 9790210
    Abstract: Compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.
    Type: Grant
    Filed: November 12, 2013
    Date of Patent: October 17, 2017
    Assignee: Array BioPharma Inc.
    Inventors: Steven Wade Andrews, James F. Blake, Barbara J. Brandhuber, Timothy Kercher, Shannon L. Winski
  • Patent number: 9029554
    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: May 12, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: Qiang Yang, Beth Lorsbach, Ronald Ross, Jr., Kaitlyn Gray, Yu Zhang, Gary Roth
  • Publication number: 20150112073
    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, Ronald ROSS, JR., Kaitlyn GRAY, Yu ZHANG, Gary ROTH
  • Patent number: 8916601
    Abstract: Compounds are provided that act as potent antagonists of the CCR(9) receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR(9). The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR(9)-mediated diseases, and as controls in assays for the identification of CCR(9) antagonists.
    Type: Grant
    Filed: February 28, 2013
    Date of Patent: December 23, 2014
    Assignee: ChemoCentryx, Inc.
    Inventors: Xi Chen, Junfa Fan, Pingchen Fan, Antoni Krasinski, Lianfa Li, Rebecca M. Lui, Jeffrey P. McMahon, Jay P. Powers, Yibin Zeng, Penglie Zhang
  • Patent number: 8901153
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: December 2, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Ann M. Buysse, Noormohamed M. Niyaz, David A. Demeter, Yu Zhang, Martin J. Walsh, Asako Kubota, Ricky Hunter, Tony K. Trullinger, Christian T. Lowe, Daniel Knueppel, Akshay Patny, Negar Garizi, Paul Renee LePlae, Jr., Frank Wessels, Ronald Ross, Jr., Carl DeAmicis, Peter Borromeo
  • Patent number: 8889727
    Abstract: An anti-fungal agent for tinea comprising as active ingredient a compound having the skeleton of 2-(1H-pyrazol-1-yl)phenol represented by the following formula (I) or (II) or a salt thereof is provided
    Type: Grant
    Filed: January 30, 2012
    Date of Patent: November 18, 2014
    Assignee: Meiji Seika Pharma Co., Ltd.
    Inventors: Makoto Ohyama, Yuji Tabata, Maiko Iida, Kaori Kaneda, Sho Takahata
  • Publication number: 20140289973
    Abstract: 1-hexyl-1H-pyrazole-4,5-diamine hemisulfate, as represented in formula (IX-a), and its use in oxidative dyeing composition. This pyrazole salt was found to combine good stability as raw material and good shade intensity with a range of common couplers when formulated in hair dyeing composition.
    Type: Application
    Filed: June 17, 2014
    Publication date: October 2, 2014
    Inventors: Wolfram GEIBEL, Ingo WEBER, Armin OSAN, Markus SPECKBACHER
  • Patent number: 8846727
    Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: September 30, 2014
    Assignee: Romark Laboratories, L.C.
    Inventors: Jean-Francois Rossignol, J. Edward Semple
  • Publication number: 20140288074
    Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, fungicides: wherein Q1, R1, R1a, R2, R3 and X 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: March 21, 2014
    Publication date: September 25, 2014
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: ANDREW EDMUND TAGGI, Jeffrey Keith Long, Moumita Kar
  • Patent number: 8785656
    Abstract: A telescoping synthesis of 5-amino-4-nitroso-1-alkyl-1H-pyrazole salt derivatives of formula (I), the compound (I) itself, and its use as an intermediate in the fabrication of 1-alkyl-4,5-diaminopyrazole salts of general formula (IX). The compounds of formula (IX) can be used as precursor dyes in oxidative hair dye compositions. R is a mono- or poly-substituted or unsubstituted, straight or branched, saturated or mono- or poly-unsaturated, alkyl group. HZ and HZ? are organic or mineral acids.
    Type: Grant
    Filed: February 15, 2013
    Date of Patent: July 22, 2014
    Assignee: The Procter & Gamble Company
    Inventors: Wolfram Geibel, Ingo Weber, Armin Osan, Markus Speckbacher
  • Patent number: 8754115
    Abstract: Disclosed are compounds of Formula 1 and Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein Q1, Q2, R1, R2, R4, R5 and X are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 or Formula 1A 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: August 31, 2011
    Date of Patent: June 17, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: Jeffrey Keith Long, Paula Louise Sharpe, Amy X Ding
  • Patent number: 8722905
    Abstract: Disclosed is a dye, having a chemical formula: wherein each R1 is independently selected from hydrogen, —(CxH2x+1), —(CyH2y)—S—(CxH2x+1), or —(CyH2y)—N(CxH2x+1)2; Ar1 is wherein each R2 is independently selected from —(CxH2x+1), —(CxH2x)—S—(CxH2x+1), or (CxH2x)—N(CxH2x+1)2; Ar2 is wherein each R3 is independently selected from hydrogen, —(CxH2x+1), —(CyH2y)—S—(CxH2x+1), or —(CyH2y)—N(CxH2x+1)2; X is sulfur, oxygen, selenium, or N—R4, and R4 is —(CxH2x+1); m is in integer of 1 to 4; x is an integer of 1 to 20; and y is an integer of 0 to 20. The dye can be applied to a photoelectric conversion device.
    Type: Grant
    Filed: August 3, 2012
    Date of Patent: May 13, 2014
    Assignee: Industrial Technology Research Institute
    Inventors: Yao-Shan Wu, Yung-Liang Tung, Jen-An Chen, Chun-Guey Wu, Jheng-Ying Li
  • Patent number: 8691862
    Abstract: The present invention relates to novel crystalline polymorphs, solvate pseudomorphs and amorphous form of 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-4-[(trifluoromethyl)sulfinyl]-1H-pyrazole-3-carbonitrile (fipronil). The present invention also provides methods for preparing the novel polymorphs, pseudomorphs and amorphous form, as well as insecticidal or pesticidal compositions comprising same, and methods of use thereof as pesticidal agents.
    Type: Grant
    Filed: April 27, 2011
    Date of Patent: April 8, 2014
    Assignee: Makhteshim Chemical Works Ltd.
    Inventor: Sharona Zamir
  • Publication number: 20140088105
    Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF1) receptor antagonists.
    Type: Application
    Filed: November 22, 2013
    Publication date: March 27, 2014
    Applicant: NOVARTIS AG
    Inventors: David Beattie, Andrew James Culshaw, Lisa Rooney, Emily Stanley
  • Patent number: 8642626
    Abstract: Provided is a novel compound represented by formula [I] or a pharmaceutically acceptable salt thereof having antagonistic activity against group II metabolism-type glutamic acid (m-Glu) receptors. The compound or pharmaceutically acceptable salt thereof is useful as a prophylactic or therapeutic agent for diseases such as new mood disorders (depressive and bipolar disorders), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, and acute stress disorder), schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, drug dependence, convulsions, tremors, pain, sleep disorders, and the like.
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: February 4, 2014
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Toshio Nakamura, Kazunari Sakagami, Kazuhide Konishi, Kanako Yamamoto, Seiji Masuda, Yohei Matsuda, Kumiko Okada, Tsuyoshi Shibata, Hiroshi Ohta, Akito Yasuhara, Hiroshi Kawamoto
  • Publication number: 20140010773
    Abstract: This invention provides methods for treating diseases or conditions wherein the inhibition of Kit protein kinase may be beneficial, using pharmaceutical or cosmetic compositions comprising N-(4-methoxyphenyl)-1-phenyl-1H-pyrazol-3-amine (FPL-62064) and related compounds. This invention also relates to the treatment of skin disorders, such as hyperpigmentation and cutaneous mastocytosis, and to cosmetic uses such as skin lightening.
    Type: Application
    Filed: March 1, 2012
    Publication date: January 9, 2014
    Applicant: NPHARMAKON, LLC
    Inventors: Dmitri Rebatchouk, Felix Sheinerman
  • Patent number: 8614213
    Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing (CRF1) receptor antagonists.
    Type: Grant
    Filed: August 5, 2009
    Date of Patent: December 24, 2013
    Assignee: Novartis AG
    Inventors: David Beattie, Andrew James Culshaw, Lisa Rooney, Emily Stanley
  • Publication number: 20130317074
    Abstract: An anti-fungal agent for tinea comprising as active ingredient a compound having the skeleton of 2-(1H-pyrazol-1-yl)phenol represented by the following formula (I) or (II) or a salt thereof is provided
    Type: Application
    Filed: January 30, 2012
    Publication date: November 28, 2013
    Inventors: Makoto Ohyama, Yuji Tabata, Maiko Iida, Kaori Kaneda, Sho Takahata
  • Patent number: 8524718
    Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4, M1, M2, M3, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
    Type: Grant
    Filed: September 6, 2012
    Date of Patent: September 3, 2013
    Assignee: Addex Pharma S.A.
    Inventors: Christelle Boléa, Sylvain Celanire
  • Publication number: 20130212810
    Abstract: 1-hexyl-1H-pyrazole-4,5-diamine hemisulfate, as represented in formula (IX-a), and its use in oxidative dyeing composition. This pyrazole salt was found to combine good stability as raw material and good shade intensity with a range of common couplers when formulated in hair dyeing composition.
    Type: Application
    Filed: February 15, 2013
    Publication date: August 22, 2013
    Applicant: THE PROCTER & GAMBLE COMPANY
    Inventor: The Procter & Gamble Company
  • Publication number: 20130217891
    Abstract: A telescoping synthesis of 5-amino-4-nitroso-1-alkyl-1H-pyrazole salt derivatives of formula (I), the compound (I) itself, and its use as an intermediate in the fabrication of 1-alkyl-4,5-diaminopyrazole salts of general formula (IX). The compounds of formula (IX) can be used as precursor dyes in oxidative hair dye compositions. R is a mono- or poly-substituted or unsubstituted, straight or branched, saturated or mono- or poly-unsaturated, alkyl group. HZ and HZ? are organic or mineral acids.
    Type: Application
    Filed: February 15, 2013
    Publication date: August 22, 2013
    Applicant: THE PROCTER & GAMBLE COMPANY
    Inventor: The Procter & Gamble Company
  • Patent number: 8460397
    Abstract: A composition for the oxidative dyeing of keratin fibers, in particular human keratin fibers, comprising (A) a 1-hexyl/heptyl-4,5-diaminopyrazole compound of the general formula (I), its physiologically compatible water-soluble salt, or mixtures thereof; (B) a pyridine compound of the general formula (II), its physiologically compatible water-soluble salt, or mixtures thereof; and (C) an oxidizing agent. wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein and a=1 or 2.
    Type: Grant
    Filed: February 16, 2012
    Date of Patent: June 11, 2013
    Assignee: The Procter & Gamble Company
    Inventors: Muill Lim, Bryan Patrick Murphy, Margaret Ann Popp, Richard Matthew Charles Sutton, Guiru Zhang
  • Publication number: 20130143940
    Abstract: Disclosed are compounds of Formula 1 and Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein Q1, Q2, R1, R2, R4, R5 and X are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 or Formula 1A 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: August 31, 2011
    Publication date: June 6, 2013
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: Jeffrey Keith Long, Mary Ann Hanagan, Eric Allen Marshall, Paula Louise Sharpe, Amy X. Ding
  • Publication number: 20130129839
    Abstract: Disclosed is a fungicidal composition comprising (a) at least one compound selected from the compounds of Formula 1, N-oxides, and salts thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined in the disclosure; and (b) at least one additional fungicidal compound. Also disclosed is a method for controlling plant diseases caused by fungal plant pathogens comprising applying to the plant or portion thereof, or to the plant seed, a fungicidally effective amount of a compound of Formula 1, an N-oxide, or salt thereof (e.g., as a component in the aforesaid composition). Also disclosed is a composition comprising: (a) at least one compound selected from the compounds of Formula 1 described above, N-oxides, and salts thereof; and at least one invertebrate pest control compound or agent.
    Type: Application
    Filed: September 1, 2011
    Publication date: May 23, 2013
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: Jeffrey Keith Long, Vann Gregory, Steven Gutteridge, Andrew Edmund Taggi, James Francis Bereznak
  • Patent number: 8444713
    Abstract: An oxidative dyeing composition comprising a combination of a 1-hexyl/heptyl-4,5-diaminopyrazole compound of formula (I) or a physiologically compatible, water-soluble salt thereof in combination with a naphthalen-1-ol compound of formula (II) or a physiologically compatible, water-soluble salt thereof wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein and a=1 or 2.
    Type: Grant
    Filed: February 16, 2012
    Date of Patent: May 21, 2013
    Assignee: The Procter & Gamble Company
    Inventors: Muill Lim, Bryan Patrick Murphy, Margaret Ann Popp, Richard Matthew Charles Sutton, Guiru Zhang
  • Patent number: 8444714
    Abstract: An oxidative dyeing composition comprising (A) a 1-hexyl/heptyl-4,5-diaminopyrazole compound of the general formula (I), its physiologically compatible water-soluble salt, or mixtures thereof; (B) a benzene-1,3-diol compound of the general formula (II), its physiologically compatible water-soluble salt, or mixtures thereof, and (C) an oxidizing agent. wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein and a=1 or 2.
    Type: Grant
    Filed: February 16, 2012
    Date of Patent: May 21, 2013
    Assignee: The Procter & Gamble Company
    Inventors: Muill Lim, Bryan Patrick Murphy, Margaret Ann Popp, Richard Matthew Charles Sutton, Guiru Zhang
  • Patent number: 8444711
    Abstract: A composition for the oxidative dyeing of keratin fibers, in particular human keratin fibers comprising (A) a 1-hexyl/heptyl-4,5-diaminopyrazole compound of the general formula (I), a physiologically compatible water-soluble salt thereof, or mixtures thereof, and; (B) a benzene-1,3-diamine compound of the general formula (II), a physiologically compatible water-soluble salt thereof or mixtures thereof, and (C) an oxidizing agent. wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein and a=1 or 2.
    Type: Grant
    Filed: February 16, 2012
    Date of Patent: May 21, 2013
    Assignee: The Procter & Gamble Company
    Inventors: Muill Lim, Bryan Patrick Murphy, Margaret Ann Popp, Richard Matthew Charles Sutton, Guiru Zhang
  • Patent number: 8444712
    Abstract: A composition for the oxidative dyeing of keratin fibers, in particular human keratin fibers, comprising (A) a 1-hexyl/heptyl-4,5-diaminopyrazole compound of the general formula (I), its physiologically compatible water-soluble salt, or mixtures thereof; and (B) a benzo[1,3]dioxol-5-ylamine compound of the general formula (II), its physiologically compatible water-soluble salt, or mixtures thereof; and (C) an oxidizing agent wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein and a=1 or 2.
    Type: Grant
    Filed: February 16, 2012
    Date of Patent: May 21, 2013
    Assignee: The Procter & Gamble Company
    Inventors: Muill Lim, Bryan Patrick Murphy, Margaret Ann Popp, Richard Matthew Charles Sutton, Guiru Zhang
  • Patent number: 8444710
    Abstract: Compositions for the oxidative dyeing of keratin fibers, in particular human keratin fibers, comprising (A) a 1-hexyl/heptyl-4,5-diaminopyrazole compound of the general formula (I), its physiologically compatible water-soluble salt, or mixtures thereof and; (B) a m-aminophenol compound of the general formula (II), its physiologically compatible water-soluble salt, or mixtures thereof; and (C) an oxidizing agent. wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein and a=1 or 2.
    Type: Grant
    Filed: February 16, 2012
    Date of Patent: May 21, 2013
    Assignee: The Procter & Gamble Company
    Inventors: Muill Lim, Bryan Patrick Murphy, Margaret Ann Popp, Richard Matthew Charles Sutton, Guiru Zhang
  • Patent number: 8444709
    Abstract: An oxidative dyeing composition comprising a 1-hexyl-4,5-diaminopyrazole compound or a 1-heptyl-4,5-diaminopyrazole compound of formula (I) in combination with a 2-aminophenol compound of formula (II): wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein and a=1 or 2. The composition provides good hair color intensity together with good wash and bleeding fastness.
    Type: Grant
    Filed: February 16, 2012
    Date of Patent: May 21, 2013
    Assignee: The Procter & Gamble Company
    Inventors: Muill Lim, Bryan Patrick Murphy, Margaret Ann Popp, Richard Matthew Charles Sutton, Guiru Zhang
  • Publication number: 20130123500
    Abstract: Provided is a novel compound represented by formula [I] or a pharmaceutically acceptable salt thereof having antagonistic activity against group II metabolism-type glutamic acid (m-Glu) receptors. The compound or pharmaceutically acceptable salt thereof is useful as a prophylactic or therapeutic agent for diseases such as new mood disorders (depressive and bipolar disorders), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, and acute stress disorder), schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, drug dependence, convulsions, tremors, pain, sleep disorders, and the like.
    Type: Application
    Filed: July 29, 2011
    Publication date: May 16, 2013
    Applicant: TAISHO PHARMACEUTICAL CO., LTD
    Inventors: Toshio Nakamura, Kazunari Sakagami, Kazuhide Konishi, Kanako Yamamoto, Seiji Masuda, Yohei Matsuda, Kumiko Okada, Tsuyoshi Shibata, Hiroshi Ohta, Akito Yasuhara, Hiroshi Kawamoto
  • Patent number: 8440709
    Abstract: The present invention relates to novel crystalline polymorphs, solvate pseudomorphs and amorphous form of 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-4-[(trifluoromethyl)sulfinyl]-1H-pyrazole-3-carbonitrile (fipronil). The present invention also provides methods for preparing the novel polymorphs, pseudomorphs and amorphous form, as well as insecticidal or pesticidal compositions comprising same, and methods of use thereof as pesticidal agents.
    Type: Grant
    Filed: December 14, 2006
    Date of Patent: May 14, 2013
    Assignee: Makhteshim Chemical Works Ltd.
    Inventor: Sharona Zamir
  • Publication number: 20120295874
    Abstract: The present invention is directed to a monomer useful in preparing therapeutic compounds. The monomer includes one or more pharmacophores which potentially binds to a target molecule with a dissociation constant of less than 300 ?M and a linker element connected to the pharmacophore. The linker element has a molecular weight less than 500 daltons, is connected, directly or indirectly through a connector, to the pharmacophore.
    Type: Application
    Filed: October 7, 2010
    Publication date: November 22, 2012
    Applicants: CORNELL UNIVERSITY, COFERON, INC., PURDUE RESEARCH FOUNDATION
    Inventors: Francis Barany, Maneesh Pingle, Sarah Filippa Giardina, Donald Bergstrom, Lee Daniel Arnold
  • Patent number: 8188135
    Abstract: Disclosed herein are cannabinoid receptor ligands of formula (I) wherein A1, A5, Rx, X4, and z 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: September 16, 2009
    Date of Patent: May 29, 2012
    Assignee: Abbott Laboratories
    Inventors: William A. Carroll, Michael J. Dart, Jennifer M. Frost, Steven P. Latshaw, Teodozyj Kolasa, Tongmei Li, Sridhar Peddi, Bo Liu, Arturo Perez-Medrano, Meena Patel, Xueqing Wang, Derek W. Nelson
  • Publication number: 20110319430
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein Q1 is a phenyl ring, naphthalenyl ring system, a 5- to 6-membered fully unsaturated heterocyclic ring or an 8- to 10-membered heteroaromatic bicyclic ring system, each as described with optional substituents as defined in the disclosure; Q2 is a phenyl ring, a naphthalenyl ring system, a 5- to 6-membered saturated, partially unsaturated or fully unsaturated heterocyclic ring, or an 8- to 10-membered heteroaromatic bicyclic ring system, each as described with optional substituents as defined in the disclosure; X is O, S(O)m, NR4, CR15R16, C(?O) or C(?S); and R1, R1a, R2, R4, R15, R16 and m 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: March 3, 2010
    Publication date: December 29, 2011
    Applicant: E.I. Du pont Nemours and Company
    Inventors: Jeffrey Keith Long, Wonpyo Hong, Andrew Edmund Taggi
  • Publication number: 20110319398
    Abstract: The disclosure relates to compounds and methods of inhibiting type three secretion system effector molecules, to methods of detecting compounds that inhibit Yops translocation, and to methods of treating or preventing infections by administering compounds described herein to a subject in need thereof.
    Type: Application
    Filed: June 1, 2011
    Publication date: December 29, 2011
    Applicant: TUFTS UNIVERSITY
    Inventor: Joan Mecsas
  • Patent number: 8039640
    Abstract: The invention relates to new morphine compounds of the formula: where R1 represents a C1-6 alkyl radical and the radicals R2 and R3 are independently selected from the group consisting of hydrogen atoms, methyl groups and acetyl groups.
    Type: Grant
    Filed: February 15, 2007
    Date of Patent: October 18, 2011
    Assignee: Universitätsklinikum Freiburg
    Inventor: Rainer Trittler
  • Publication number: 20110237783
    Abstract: Pharmaceutical compositions and compounds are provided. The compounds of the invention demonstrate anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, pharmaceutical compositions of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical compositions are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.
    Type: Application
    Filed: December 23, 2010
    Publication date: September 29, 2011
    Applicant: Valocor Therapeutics, Inc.
    Inventors: Zaihui Zhang, Timothy S. Daynard, Mikhail A. Chafeev, Shisen Wang, Gregory B. Chopiuk, Serguei V. Sviridov
  • Patent number: 7989456
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Grant
    Filed: May 5, 2010
    Date of Patent: August 2, 2011
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael Mortimore, Julian M. C. Golec
  • Patent number: 7981874
    Abstract: The present invention relates to a novel class of phosphorus derivatives. The phosphorus compounds can be used to treat cancer. The phosphorus compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Grant
    Filed: July 16, 2007
    Date of Patent: July 19, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joshua Close, Jonathan Grimm, Richard W. Heidebrecht, Jr., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Scott Peterson, Phieng Siliphaivanh, Paul J. Tempest, Kevin J. Wilson, David J. Witter
  • Publication number: 20110152261
    Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing (CRF1) receptor antagonists.
    Type: Application
    Filed: August 5, 2009
    Publication date: June 23, 2011
    Inventors: David Beattie, Anny-Odile Colson, Andrew James Culshaw, Lisa Rooney, Emily Stanley, Lilya Sviridenko
  • Patent number: 7939550
    Abstract: Provided are aminopyrazole derivatives, a process for the preparation thereof, and a composition for preventing or treating an ischemic disease containing the same. Since the aminopyrazole derivatives of the present invention can reduce an ischemic cell death significantly, they can be effectively used for the prevention and treatment of ischemic diseases mediated by ischemic cell death, or protection of organs.
    Type: Grant
    Filed: October 26, 2007
    Date of Patent: May 10, 2011
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Yong-Sam Jung, Eunhee Kim, Nakjeong Kim, Yun-Suk Lee, Jeehee Suh, Haeyoung Suh, Kyu Yang Yi, Sung-eun Yoo
  • Publication number: 20110065766
    Abstract: The present invention relates, in part, to methods of treatment, prevention, and inhibition of viral disorders. In one aspect, the present invention relates to inhibition of the M2 proton channel of influenza viruses (e.g. influenza A virus) and other similar viroporins (e.g., VP24 of Ebola and Marburg viruses; and NS3 protein of Bluetongue). The present invention further relates, inter alia, to compounds which have been shown to possess antiviral activity, in particular, inhibiting the M2 proton channel of influenza viruses.
    Type: Application
    Filed: September 13, 2010
    Publication date: March 17, 2011
    Inventors: Jizhou Wang, Xiaodong Fan, Lidia Cristian
  • Patent number: 7902248
    Abstract: Disclosed herein are pyrazole glucokinase activators of the formula (I): that are useful for the treatment of metabolic diseases and disorders.
    Type: Grant
    Filed: December 6, 2007
    Date of Patent: March 8, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Steven Joseph Berthel, Robert Francis Kester, Douglas Eric Murphy, Thomas Jay Prins, Frank Ruebsam, Chinh Viet Tran, Dionisios Vourloumis
  • Patent number: 7875728
    Abstract: Pharmaceutical compositions and compounds are provided. The compounds of the invention demonstrate anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, pharmaceutical compositions of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical compositions are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.
    Type: Grant
    Filed: October 18, 2002
    Date of Patent: January 25, 2011
    Assignee: Valocor Therapeutics, Inc.
    Inventors: Zaihui Zhang, Timothy S Daynard, Mikhail A Chafeev, Shisen Wang, Gregory B Chopiuk, Serguei V Sviridov
  • Publication number: 20110003862
    Abstract: Compounds of the formula (I), inhibit D-amino acid oxidase and hence find use in treating degenerative and psychiatric diseases.
    Type: Application
    Filed: February 15, 2007
    Publication date: January 6, 2011
    Applicants: MERCK SHARP & DOHME LIMITED, MERCK & CO., INC.
    Inventors: Philip E. Brandish, Nicholas Brandon, Alister Campbell, Timothy Sparey
  • Patent number: 7863314
    Abstract: Provided are 5-membered heterocycle-based p38 kinase inhibitors. Further provided are pyrazole and imidazole-based p38 kinase, including p38? and p38? kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders.
    Type: Grant
    Filed: June 25, 2004
    Date of Patent: January 4, 2011
    Assignee: Novartis AG
    Inventors: Olga M. Fryszman, Hengyuan Lang, Jiong Lan, Edcon Chang, Yunfeng Fang
  • Publication number: 20100273842
    Abstract: This invention provides an anorectic or anti-obesity composition comprising a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted lower alkyl, Y is —S(O)n— wherein n is 1 or 2, or —CO—, R2 is hydrogen or lower alkyl, R7 is hydrogen or lower alkyl, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, and Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like.
    Type: Application
    Filed: April 26, 2010
    Publication date: October 28, 2010
    Applicant: Shionogi & Co., Ltd.
    Inventors: Takayuki OKUNO, Masahiro Sakagami