Nitrogen Attached Directly To The Diazole Ring By Nonionic Bonding Patents (Class 548/371.4)
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Patent number: 11028265Abstract: 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: GrantFiled: December 12, 2018Date of Patent: June 8, 2021Assignee: The Government of the United States of America, as represented by the Secretary of the NavyInventors: Brett D. Martin, Ian D. Giles, Jawad Naciri, Paul T. Charles, Scott A. Trammell, Jeffrey R. Deschamps, Jeffrey C. Depriest
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Patent number: 10035774Abstract: Pyrazolyl carboxylic acid and pyrazolyl urea derivatives have been synthesized, which are useful in the manufacture of cephalosporin antibiotic compounds.Type: GrantFiled: December 18, 2015Date of Patent: July 31, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Kristos Adrian Moshos, Valdas Jurkauskas, Yisheng Yang, Youchu Wang
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Patent number: 9790210Abstract: 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: GrantFiled: November 12, 2013Date of Patent: October 17, 2017Assignee: Array BioPharma Inc.Inventors: Steven Wade Andrews, James F. Blake, Barbara J. Brandhuber, Timothy Kercher, Shannon L. Winski
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Patent number: 9029554Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.Type: GrantFiled: October 17, 2014Date of Patent: May 12, 2015Assignee: Dow AgroSciences LLCInventors: Qiang Yang, Beth Lorsbach, Ronald Ross, Jr., Kaitlyn Gray, Yu Zhang, Gary Roth
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Publication number: 20150112073Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.Type: ApplicationFiled: October 17, 2014Publication date: April 23, 2015Inventors: Qiang YANG, Beth LORSBACH, Ronald ROSS, JR., Kaitlyn GRAY, Yu ZHANG, Gary ROTH
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Patent number: 8916601Abstract: 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: GrantFiled: February 28, 2013Date of Patent: December 23, 2014Assignee: 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
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Patent number: 8901153Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.Type: GrantFiled: March 7, 2013Date of Patent: December 2, 2014Assignee: 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
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Patent number: 8889727Abstract: 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 providedType: GrantFiled: January 30, 2012Date of Patent: November 18, 2014Assignee: Meiji Seika Pharma Co., Ltd.Inventors: Makoto Ohyama, Yuji Tabata, Maiko Iida, Kaori Kaneda, Sho Takahata
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Publication number: 20140289973Abstract: 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: ApplicationFiled: June 17, 2014Publication date: October 2, 2014Inventors: Wolfram GEIBEL, Ingo WEBER, Armin OSAN, Markus SPECKBACHER
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Patent number: 8846727Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.Type: GrantFiled: May 11, 2010Date of Patent: September 30, 2014Assignee: Romark Laboratories, L.C.Inventors: Jean-Francois Rossignol, J. Edward Semple
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Publication number: 20140288074Abstract: 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: ApplicationFiled: March 21, 2014Publication date: September 25, 2014Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: ANDREW EDMUND TAGGI, Jeffrey Keith Long, Moumita Kar
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Patent number: 8785656Abstract: 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: GrantFiled: February 15, 2013Date of Patent: July 22, 2014Assignee: The Procter & Gamble CompanyInventors: Wolfram Geibel, Ingo Weber, Armin Osan, Markus Speckbacher
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Patent number: 8754115Abstract: 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: GrantFiled: August 31, 2011Date of Patent: June 17, 2014Assignee: E I du Pont de Nemours and CompanyInventors: Jeffrey Keith Long, Paula Louise Sharpe, Amy X Ding
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Patent number: 8722905Abstract: 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: GrantFiled: August 3, 2012Date of Patent: May 13, 2014Assignee: Industrial Technology Research InstituteInventors: Yao-Shan Wu, Yung-Liang Tung, Jen-An Chen, Chun-Guey Wu, Jheng-Ying Li
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Patent number: 8691862Abstract: 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: GrantFiled: April 27, 2011Date of Patent: April 8, 2014Assignee: Makhteshim Chemical Works Ltd.Inventor: Sharona Zamir
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Publication number: 20140088105Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF1) receptor antagonists.Type: ApplicationFiled: November 22, 2013Publication date: March 27, 2014Applicant: NOVARTIS AGInventors: David Beattie, Andrew James Culshaw, Lisa Rooney, Emily Stanley
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Patent number: 8642626Abstract: 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: GrantFiled: July 29, 2011Date of Patent: February 4, 2014Assignee: 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
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Publication number: 20140010773Abstract: 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: ApplicationFiled: March 1, 2012Publication date: January 9, 2014Applicant: NPHARMAKON, LLCInventors: Dmitri Rebatchouk, Felix Sheinerman
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Patent number: 8614213Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing (CRF1) receptor antagonists.Type: GrantFiled: August 5, 2009Date of Patent: December 24, 2013Assignee: Novartis AGInventors: David Beattie, Andrew James Culshaw, Lisa Rooney, Emily Stanley
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Publication number: 20130317074Abstract: 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 providedType: ApplicationFiled: January 30, 2012Publication date: November 28, 2013Inventors: Makoto Ohyama, Yuji Tabata, Maiko Iida, Kaori Kaneda, Sho Takahata
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Patent number: 8524718Abstract: 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: GrantFiled: September 6, 2012Date of Patent: September 3, 2013Assignee: Addex Pharma S.A.Inventors: Christelle Boléa, Sylvain Celanire
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Publication number: 20130212810Abstract: 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: ApplicationFiled: February 15, 2013Publication date: August 22, 2013Applicant: THE PROCTER & GAMBLE COMPANYInventor: The Procter & Gamble Company
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Publication number: 20130217891Abstract: 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: ApplicationFiled: February 15, 2013Publication date: August 22, 2013Applicant: THE PROCTER & GAMBLE COMPANYInventor: The Procter & Gamble Company
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Patent number: 8460397Abstract: 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: GrantFiled: February 16, 2012Date of Patent: June 11, 2013Assignee: The Procter & Gamble CompanyInventors: Muill Lim, Bryan Patrick Murphy, Margaret Ann Popp, Richard Matthew Charles Sutton, Guiru Zhang
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Publication number: 20130143940Abstract: 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: ApplicationFiled: August 31, 2011Publication date: June 6, 2013Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: Jeffrey Keith Long, Mary Ann Hanagan, Eric Allen Marshall, Paula Louise Sharpe, Amy X. Ding
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Publication number: 20130129839Abstract: 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: ApplicationFiled: September 1, 2011Publication date: May 23, 2013Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: Jeffrey Keith Long, Vann Gregory, Steven Gutteridge, Andrew Edmund Taggi, James Francis Bereznak
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Patent number: 8444709Abstract: 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: GrantFiled: February 16, 2012Date of Patent: May 21, 2013Assignee: The Procter & Gamble CompanyInventors: Muill Lim, Bryan Patrick Murphy, Margaret Ann Popp, Richard Matthew Charles Sutton, Guiru Zhang
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Patent number: 8444710Abstract: 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: GrantFiled: February 16, 2012Date of Patent: May 21, 2013Assignee: The Procter & Gamble CompanyInventors: Muill Lim, Bryan Patrick Murphy, Margaret Ann Popp, Richard Matthew Charles Sutton, Guiru Zhang
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Patent number: 8444711Abstract: 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: GrantFiled: February 16, 2012Date of Patent: May 21, 2013Assignee: The Procter & Gamble CompanyInventors: Muill Lim, Bryan Patrick Murphy, Margaret Ann Popp, Richard Matthew Charles Sutton, Guiru Zhang
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Patent number: 8444712Abstract: 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: GrantFiled: February 16, 2012Date of Patent: May 21, 2013Assignee: The Procter & Gamble CompanyInventors: Muill Lim, Bryan Patrick Murphy, Margaret Ann Popp, Richard Matthew Charles Sutton, Guiru Zhang
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Patent number: 8444714Abstract: 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: GrantFiled: February 16, 2012Date of Patent: May 21, 2013Assignee: The Procter & Gamble CompanyInventors: Muill Lim, Bryan Patrick Murphy, Margaret Ann Popp, Richard Matthew Charles Sutton, Guiru Zhang
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Patent number: 8444713Abstract: 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: GrantFiled: February 16, 2012Date of Patent: May 21, 2013Assignee: The Procter & Gamble CompanyInventors: Muill Lim, Bryan Patrick Murphy, Margaret Ann Popp, Richard Matthew Charles Sutton, Guiru Zhang
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Publication number: 20130123500Abstract: 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: ApplicationFiled: July 29, 2011Publication date: May 16, 2013Applicant: TAISHO PHARMACEUTICAL CO., LTDInventors: Toshio Nakamura, Kazunari Sakagami, Kazuhide Konishi, Kanako Yamamoto, Seiji Masuda, Yohei Matsuda, Kumiko Okada, Tsuyoshi Shibata, Hiroshi Ohta, Akito Yasuhara, Hiroshi Kawamoto
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Patent number: 8440709Abstract: 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: GrantFiled: December 14, 2006Date of Patent: May 14, 2013Assignee: Makhteshim Chemical Works Ltd.Inventor: Sharona Zamir
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Publication number: 20120295874Abstract: 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: ApplicationFiled: October 7, 2010Publication date: November 22, 2012Applicants: CORNELL UNIVERSITY, COFERON, INC., PURDUE RESEARCH FOUNDATIONInventors: Francis Barany, Maneesh Pingle, Sarah Filippa Giardina, Donald Bergstrom, Lee Daniel Arnold
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Patent number: 8188135Abstract: 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: GrantFiled: September 16, 2009Date of Patent: May 29, 2012Assignee: Abbott LaboratoriesInventors: 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
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Publication number: 20110319430Abstract: 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: ApplicationFiled: March 3, 2010Publication date: December 29, 2011Applicant: E.I. Du pont Nemours and CompanyInventors: Jeffrey Keith Long, Wonpyo Hong, Andrew Edmund Taggi
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Publication number: 20110319398Abstract: 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: ApplicationFiled: June 1, 2011Publication date: December 29, 2011Applicant: TUFTS UNIVERSITYInventor: Joan Mecsas
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Patent number: 8039640Abstract: 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: GrantFiled: February 15, 2007Date of Patent: October 18, 2011Assignee: Universitätsklinikum FreiburgInventor: Rainer Trittler
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Publication number: 20110237783Abstract: 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: ApplicationFiled: December 23, 2010Publication date: September 29, 2011Applicant: Valocor Therapeutics, Inc.Inventors: Zaihui Zhang, Timothy S. Daynard, Mikhail A. Chafeev, Shisen Wang, Gregory B. Chopiuk, Serguei V. Sviridov
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Patent number: 7989456Abstract: 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: GrantFiled: May 5, 2010Date of Patent: August 2, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Mortimore, Julian M. C. Golec
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Patent number: 7981874Abstract: 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: GrantFiled: July 16, 2007Date of Patent: July 19, 2011Assignee: 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
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Publication number: 20110152261Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing (CRF1) receptor antagonists.Type: ApplicationFiled: August 5, 2009Publication date: June 23, 2011Inventors: David Beattie, Anny-Odile Colson, Andrew James Culshaw, Lisa Rooney, Emily Stanley, Lilya Sviridenko
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Patent number: 7939550Abstract: 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: GrantFiled: October 26, 2007Date of Patent: May 10, 2011Assignee: Korea Research Institute of Chemical TechnologyInventors: Yong-Sam Jung, Eunhee Kim, Nakjeong Kim, Yun-Suk Lee, Jeehee Suh, Haeyoung Suh, Kyu Yang Yi, Sung-eun Yoo
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Publication number: 20110065766Abstract: 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: ApplicationFiled: September 13, 2010Publication date: March 17, 2011Inventors: Jizhou Wang, Xiaodong Fan, Lidia Cristian
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Patent number: 7902248Abstract: Disclosed herein are pyrazole glucokinase activators of the formula (I): that are useful for the treatment of metabolic diseases and disorders.Type: GrantFiled: December 6, 2007Date of Patent: March 8, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Steven Joseph Berthel, Robert Francis Kester, Douglas Eric Murphy, Thomas Jay Prins, Frank Ruebsam, Chinh Viet Tran, Dionisios Vourloumis
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Patent number: 7875728Abstract: 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: GrantFiled: October 18, 2002Date of Patent: January 25, 2011Assignee: Valocor Therapeutics, Inc.Inventors: Zaihui Zhang, Timothy S Daynard, Mikhail A Chafeev, Shisen Wang, Gregory B Chopiuk, Serguei V Sviridov
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Publication number: 20110003862Abstract: Compounds of the formula (I), inhibit D-amino acid oxidase and hence find use in treating degenerative and psychiatric diseases.Type: ApplicationFiled: February 15, 2007Publication date: January 6, 2011Applicants: MERCK SHARP & DOHME LIMITED, MERCK & CO., INC.Inventors: Philip E. Brandish, Nicholas Brandon, Alister Campbell, Timothy Sparey
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Patent number: 7863314Abstract: 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: GrantFiled: June 25, 2004Date of Patent: January 4, 2011Assignee: Novartis AGInventors: Olga M. Fryszman, Hengyuan Lang, Jiong Lan, Edcon Chang, Yunfeng Fang
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Publication number: 20100273842Abstract: 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: ApplicationFiled: April 26, 2010Publication date: October 28, 2010Applicant: Shionogi & Co., Ltd.Inventors: Takayuki OKUNO, Masahiro Sakagami