Hydroxy, Bonded Directly To Carbon, Or Ether In Substituent Q (h Of -oh May Be Replaced By A Substituted Or Unsubstituted Ammonium Ion Or A Group Ia Or Iia Light Metal) Patents (Class 564/150)
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Patent number: 12247143Abstract: A two-stage epoxy bonding oil includes a main agent A and a curing agent B in a weight ratio of 1:1 to 3:1. The curing agent B includes 70 to 90 parts of a linear bifunctional secondary amine curing agent, 10 to 30 parts of a high-melting-point latent curing agent and 1 to 5 parts of an anti-settling agent. A two-stage curing of epoxy bonding oil includes a first-stage curing at room temperature whereby the cured product is in a thermoplastic state and a second-stage curing at 100° C. to 180° C. whereby the cured product is in a thermosetting state. It solves the contradiction between sticking wheels and bonding performance of the bonding layer in field of road and bridge pavement, exploring a new direction for the waterproof bonding layer materials in road and bridge pavement such as steel bridge deck pavement, concrete bridge deck pavement and tunnel pavement.Type: GrantFiled: February 5, 2021Date of Patent: March 11, 2025Assignee: SINOROAD TRANSPORTATION SCIENCE AND TECHNOLOGY CO., LTD.Inventors: Zhixiang Zhang, Kuan Li, Youqiang Pan, Lifeng Chen, Hui Zhang
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Patent number: 11731934Abstract: The instant invention describes hydrazide-containing compounds having therapeutic activity, and methods of treating disorders such as cancer, tumors and cell proliferation related disorders, or affect cell differentiation, dedifferentiation or transdifferentiation.Type: GrantFiled: August 21, 2020Date of Patent: August 22, 2023Assignee: University of Florida Research Foundation, Inc.Inventors: Daiqing Liao, William R. Roush, Ryan L. Stowe
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Patent number: 11708480Abstract: Provided is a rubber composition comprising: a rubber component containing diene-based rubber; a filler, and a compound represented by formula (I) below: (wherein: A is an aryl group and has at least two polar groups, which may be the same or different from each other; R1 and R2 are each independently at least one substituent selected from a group consisting of a hydrogen atom, an acyl group, an amide group, an alkyl group, a cycloalkyl group, and an aryl group; and further, the substituent may include one or more of O, S, and N atoms), so as to provide a rubber composition excellent in low heat generating property and wear resistance.Type: GrantFiled: August 3, 2017Date of Patent: July 25, 2023Assignee: OTSUKA CHEMICAL CO., LTD.Inventors: Satoshi Hamatani, Aya Saiki, Shinya Shinozaki, Mifuyu Ueno, Masaki Abe
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Publication number: 20150099636Abstract: The present invention provides diacylhydrazine ligands and chiral diacylhydrazine ligands for use with ecdysone receptor-based inducible gene expression systems. Thus, the present invention is useful for applications such as gene therapy, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable. An advantage of the present invention is that it provides a means to regulate gene expression and to tailor expression levels to suit the user's requirements.Type: ApplicationFiled: October 9, 2014Publication date: April 9, 2015Inventors: Robert Eugene HORMANN, Bing Li
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Publication number: 20150099865Abstract: A method is disclosed for preparing hydrazides from hydrazine and an acyl chloride which comprises the steps of (a) preparing a stirred substantially uniform slurry comprising hydrazine and an inert solvent at low temperature; and (b) adding an acyl chloride continuously to said slurry. The method avoids or limits production of undesired bis-hydrazide by-products. The method is used to prepare 3-methyl-3-mercaptobutanoic acid hydrazide, a molecule used to link calicheamicin to a monoclonal antibody.Type: ApplicationFiled: October 2, 2014Publication date: April 9, 2015Applicant: WYETH LLCInventors: George Anello CHIARELLO, Ayman SAHLI
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Publication number: 20150094314Abstract: A method of modulating ribonucleotide reductase activity in a neoplastic cell includes administering to the cell an amount of a ribonucleotide reductase allosteric modulator (RRAmod), the amount being effective to inhibit neoplastic cell growth.Type: ApplicationFiled: March 21, 2013Publication date: April 2, 2015Inventor: Chris Dealwis
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Publication number: 20150045441Abstract: The present disclosure provides crystalline polymorphic and amorphous forms of (R)-3,5-dimethyl-benzoic acid N-(1-tert-butyl-butyl)-N?-(2-ethyl-3-methoxy-benzoyl)-hydrazide (Compound 1) or (S)-3,5-dimethyl-benzoic acid N-(1-tert-butyl-butyl)-N?-(2-ethyl-3-methoxy-benzoyl)-hydrazide (Compound 2). The present disclosure further provides compositions comprising crystalline polymorphic and amorphous forms of Compound 1 or Compound 2 and an excipient, methods of making crystalline polymorphic or amorphous forms of Compound 1 or Compound 2, and methods of using crystalline polymorphic or amorphous forms of Compound 1 or Compound 2 to regulate gene expression in a cell or in a subject.Type: ApplicationFiled: October 21, 2014Publication date: February 12, 2015Inventors: Robert E. HORMANN, Inna Shulman, Eva Rödel, Rolf Hilfiker, Susan M. De Paul
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Publication number: 20150010469Abstract: Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer, stereoisomer or deuterated analogue thereof, wherein X, R, R1, R2, R3, R4, M1, M2, L1, L2, J1, J2, a1, a2, b1 and b2 are as defined herein, are provided. Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provided.Type: ApplicationFiled: July 3, 2014Publication date: January 8, 2015Applicants: British Columbia Cancer Agency Branch, University of British ColumbiaInventors: Raymond John Andersen, Javier Garcia Fernandez, Marianne Dorothy Sadar
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Publication number: 20140357894Abstract: Dendrimer-hydrazides are coupled to polycyclic aromatic hydrocarbons for use in the visual detection of the presence of low levels of fluoride in a sample. The dendrimers can have a phenyl core, a first generation of aralkyl ethers, and an optional second generation of aralkyl ethers. The compounds form gels with solvents. In the presence of fluoride ion, the gels undergo color changes and/or gel to liquid phase change.Type: ApplicationFiled: August 14, 2014Publication date: December 4, 2014Inventors: Prasad EDAMANA, Rajamalli PACHAIYAPPAN
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Patent number: 8853451Abstract: A method is disclosed for preparing hydrazides from hydrazine and an acyl chloride which comprises the steps of (a) preparing a stirred substantially uniform slurry comprising hydrazine and an inert solvent at low temperature; and (b) adding an acyl chloride continuously to said slurry. The method avoids or limits production of undesired bis-hydrazide by-products. The method is used to prepare 3-methyl-3-mercaptobutanoic acid hydrazide, a molecule used to link calicheamicin to a monoclonal antibody.Type: GrantFiled: January 31, 2013Date of Patent: October 7, 2014Assignee: Wyeth LLCInventors: George Anello Chiarello, Ayman Sahli
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Patent number: 8791299Abstract: 3D protein modeling and virtual screening of commercially-available compounds were performed to identify new inhibitors of the herpesvirus DNA polymerase, a key enzyme in the viral replication cycle. Two compounds (Nos 2 and 9) were particularly active against HSV-1 and HSV-2 strains and one compound (No 3) inhibited specifically cytomegalovirus (CMV) strains (overall hit rate of 25%). Some of the tested compounds inhibited wild-type viruses and strains resistant to current antiviral agents. New chemical entity derivatives of compound 2 with binding potential to the DNA polymerase retained an excellent activity against HSV-1, HSV-2 and VZV like the parental compound, as well against strains resistant to current antiviral agents. These non-nucleosidic herpesvirus DNA polymerase inhibitors with in vitro activity against drug-resistant clinical isolates warrant further pre-clinical studies.Type: GrantFiled: May 19, 2010Date of Patent: July 29, 2014Assignee: Universite LavalInventors: Guy Boivin, Sheng-Xiang Lin, Melanie Martin, Arezki Azzi
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Patent number: 8715745Abstract: The present invention relates to the use of hydrazone compounds and copper for controlling the growth of fungi.Type: GrantFiled: January 14, 2010Date of Patent: May 6, 2014Assignee: Dow AgroSciences, LLC.Inventors: David H Young, Cruz Avila-Adame, Nneka T Breaux, James M Ruiz, Thomas L Siddall, Jeffery D. Webster, Gerald Shaber
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Publication number: 20140116292Abstract: The present invention relates to a cellulose acetate film used for optical compensation and a retardation enhancer used therein, and relates to a cellulose acetate film which has a high retardation value in the thickness direction (Rth).Type: ApplicationFiled: June 20, 2012Publication date: May 1, 2014Applicant: SK INNOVATION CO., LTD.Inventors: Won Yeob Kim, Min Joung Im, Seung Eon Lee, Myoung Lae Kim, Yong Gyun Cho, Sang Yeup Lee, Ki Yup Kim
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Publication number: 20140112892Abstract: The purpose is to select low-molecular-weight compounds which are effective in inducing differentiation of mesenchymal stem cell into hepatocyte and to develop a safe differentiation-inducing method having excellent efficiency of differentiating mesenchymal stem cell into hepatocyte. Provided are at least one compound selected from the group consisting of compounds represented by formulae (1) and (2), a salt thereof, or a solvate of them; a differentiation inducer comprising at least one compound selected from the group consisting of compounds represented by formulae (1) and (2), a salt thereof, or a solvate of them; and a differentiation inducer comprising a compound represented by formula (8), a salt thereof, or a solvate of them.Type: ApplicationFiled: April 2, 2012Publication date: April 24, 2014Applicants: NATIONAL UNIVERSITY CORPORATION TOTTORI UNIVERSITY, TOKYO WOMEN'S MEDICAL UNIVERSITY, NATIONAL UNIVERSITY CORPORATION TOTTORI UNIVERSITY, TOKYO WOMEN'S MEDICAL UNIVERSITYInventors: Goshi Shiota, Yoshiko Hoshikawa, Noriko Matsumoto, Yoshiaki Matsumi, Minoru Morimoto, Takayuki Tonoi, Hiroyuki Saimoto, Kazuo Ohashi, Teruo Okano
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Publication number: 20140045903Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.Type: ApplicationFiled: July 30, 2013Publication date: February 13, 2014Applicant: Intrexon CorporationInventors: Robert Eugene HORMANN, David W. Potter, Orestes Chortyk, Colin M. Tice, Glenn Richard Carlson, Andrew Meyer, Thomas R. Opie
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Publication number: 20130344608Abstract: Dendrimer-hydrazides are coupled to polycyclic aromatic hydrocarbons for use in the visual detection of the presence of low levels of fluoride in a sample The dendrimers can have a phenyl core, a first generation of aralkyl ethers, and an optional second generation of aralkyl ethers. The compounds form gels with solvents. In the presence of fluoride ion, the gels undergo color changes and/or gel to liquid phase change.Type: ApplicationFiled: June 21, 2012Publication date: December 26, 2013Applicant: INDIAN INSTITUTE OF TECHNOLOGY MADRASInventors: Prasad EDAMANA, Rajamalli PACHAIYAPPAN
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Patent number: 8546613Abstract: The present invention relates to a compound of formulas I, Ia, Ib and II, wherein R1 to R11 are herein defined.Type: GrantFiled: February 17, 2009Date of Patent: October 1, 2013Assignee: Merck Patent GmbHInventors: Thomas Fuchss, Rolf Gericke, Norbert Beier, Florian Lang, Phillipp Lang, Karl Lang
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Publication number: 20130252936Abstract: Compounds, compositions and methods for the treatment of retinal degenerative diseases, such as retinitis pigmentosa, Leber's congenital Amaurosis, Syndromic retinal degenerations, age-related macular degeneration and Usher Syndrome, and hearing loss associated with Usher Syndrome are described herein.Type: ApplicationFiled: March 8, 2013Publication date: September 26, 2013Applicant: Usher III InitiativeInventors: Roland Werner BÜRLI, William Rameshchandra Krishna Esmieu, Christopher James Lock, Karine Fabienne Malagu, Andrew Pate Owens, William E. Harte
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Publication number: 20130211053Abstract: A method is disclosed for preparing hydrazides from hydrazine and an acyl chloride which comprises the steps of (a) preparing a stirred substantially uniform slurry comprising hydrazine and an inert solvent at low temperature; and (b) adding an acyl chloride continuously to said slurry. The method avoids or limits production of undesired bis-hydrazide by-products. The method is used to prepare 3-methyl-3-mercaptobutanoic acid hydrazide, a molecule used to link calicheamicin to a monoclonal antibody.Type: ApplicationFiled: January 31, 2013Publication date: August 15, 2013Applicant: WYETH LLCInventors: George Anello CHIARELLO, Ayman SAHLI
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Patent number: 8492440Abstract: Novel difluorophenyldiacylhydrazide derivatives of the formula I, in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in claim 1, are kinase inhibitors and can be used for the treatment of diseases and complaints such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in any type of fibroses, inflammatory processes, tumours and tumour diseases.Type: GrantFiled: November 2, 2009Date of Patent: July 23, 2013Assignee: Merck Patent GmbHInventors: Thomas Fuchss, Ulrich Graedler, Norbert Beier, Rolf Gericke, Florian Lang
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Publication number: 20130143933Abstract: The present document describes a cancer mutation-selective chemosensitizer that comprise compounds for restoring association between mutated keap1 protein and Nrf2 protein, and inhibition of Nrf2 functions. The present document also describes composition of matter containing the compounds, as well as methods of medical treatment for treating diseases such as cancer with the compounds.Type: ApplicationFiled: November 9, 2012Publication date: June 6, 2013Applicant: TRT Pharma Inc.Inventor: TRT Pharma Inc.
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Publication number: 20130079413Abstract: The present disclosure provides crystalline polymorphic and amorphous forms of (R)-3,5-dimethyl-benzoic acid N-(1-tert-butyl-butyl)-N?-(2-ethyl-3-methoxy-benzoyl)-hydrazide (Compound 1) or (S)-3,5-dimethyl-benzoic acid N-(1-tert-butyl-butyl)-N?-(2-ethyl-3-methoxy-benzoyl)-hydrazide (Compound 2). The present disclosure further provides compositions comprising crystalline polymorphic and amorphous forms of Compound 1 or Compound 2 and an excipient, methods of making crystalline polymorphic or amorphous forms of Compound 1 or Compound 2, and methods of using crystalline polymorphic or amorphous forms of Compound 1 or Compound 2 to regulate gene expression in a cell or in a subject.Type: ApplicationFiled: September 7, 2012Publication date: March 28, 2013Applicant: Intrexon CorporationInventors: Robert E. Hormann, Inna Shulman, Eva Rödel, Rolf Hilfiker, Susan M. De Paul
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Publication number: 20130065962Abstract: The present invention relates to a compound of the general formula (III):Type: ApplicationFiled: January 28, 2011Publication date: March 14, 2013Applicant: INOXIA LIFESCIENCES GMBHInventors: Andreas Kubin, Paul Furtmuller, Gerhard Wolber, Daniela Schuster
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Publication number: 20130040389Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.Type: ApplicationFiled: September 5, 2012Publication date: February 14, 2013Applicant: Intrexon CoporationInventors: Robert Eugene HORMANN, David W. Potter, Orestes Chortyk, Colin M. Tice, Glenn Richard Carlson, Andrew Meyer, Thomas R. Opie
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Patent number: 8324401Abstract: Novel non-steroidal compounds are provided that are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases having the structure of formula (I): or enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, where X is A1QA2-; Q is a bond, —C(?O)—, —OC(O)—, —C(?O)NR5—, —SOp—, —SOpNR5—, —C(O)O—, —NR5C(O)—, —OC(O)NR5—, —NR5C(O)O—, —S(O)pNR5C(O)—, —C(O)NR5S(O)p— —NR5S(O)p—, or —NR5C(?O)NR6—. Y is selected from hydrogen, C1-6alkyl, OR16, substituted C1-6alkyl, cycloalkyl, aryl, heterocyclo and heteroaryl. A1 and A2 are independently selected from a bond, C1-3alkylene, or C1-3alkenylene, and R1-R11 are defined herein. Also provided are pharmaceutical compositions, combinations, and methods of treating obesity, diabetes and inflammatory- or immune-associated diseases comprising said compounds.Type: GrantFiled: August 18, 2009Date of Patent: December 4, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Jingwu Duan, Bin Jiang
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Publication number: 20120283216Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Q is O or S; Z1 and Z2 are each independently CR9 or N; and R1, R2, R3, R4, R5, R6, R7, R8 and R9 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: December 22, 2010Publication date: November 8, 2012Inventors: Alvin Donald Crews, JR., Amy X. Ding, Chi-Ping Tseng
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Publication number: 20120141597Abstract: The present invention relates to the use of hydrazone compounds and copper for controlling the growth of fungi.Type: ApplicationFiled: January 14, 2010Publication date: June 7, 2012Applicant: Dow Agrosciences LLCInventors: David H. Young, Steven Howard Shaber, Gerald Shaber, Cruz Avila-Adame, Nneka T. Breaux, James M. Ruiz, Thomas L. Siddall, Jeffery D. Webster
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Publication number: 20120116090Abstract: The present invention provides diacylhydrazine ligands and chiral diacylhydrazine ligands for use with ecdysone receptor-based inducible gene expression systems. Thus, the present invention is useful for applications such as gene therapy, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable. An advantage of the present invention is that it provides a means to regulate gene expression and to tailor expression levels to suit the user's requirements.Type: ApplicationFiled: December 6, 2011Publication date: May 10, 2012Applicant: Intrexon CorporationInventors: Robert Eugene HORMANN, Bing Li
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Publication number: 20120115851Abstract: An objective of the present invention is to provide compounds that can effectively suppress the concentration of phosphorus in serum to effectively prevent or treat diseases induced by an increase in concentration of phosphate in serum. The compounds according to the present invention are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein A represents an optionally substituted five- to nine-membered unsaturated carbocyclic moiety or a five- to nine-membered unsaturated heterocyclic moiety, and represents a single bond or a double bond, R5 represents optionally substituted aryl or the like, Z represents —N?CHR6R7 or the like, R6 and R7 represent H, optionally substituted alkyl, optionally substituted aryl or the like, R101 and R102 together form ?O, and R103 and R104 represent H, or R101 and R104 together from a bond, and R102 and R103 together form a bond.Type: ApplicationFiled: January 18, 2012Publication date: May 10, 2012Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Nobuaki Eto, Rika Nagao, Tetsuko Kazama
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Publication number: 20120107416Abstract: The present invention relates to the use of hydrazone compounds and copper for controlling the growth of fungi.Type: ApplicationFiled: January 14, 2010Publication date: May 3, 2012Applicant: DOW AGROSCIENCES LLCInventors: David H. Young, Steven Howard Shaber, Gerald Shaber, Cruz Avila-Adame, Nneka T. Breaux, James M. Ruiz, Thomas L. Siddall, Jeffery D. Webster
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Publication number: 20120046322Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.Type: ApplicationFiled: September 23, 2011Publication date: February 23, 2012Applicant: Intrexon CorporationInventors: Robert Eugene HORMANN, David W. Potter, Orestes Chortyk, Colin M. Tice, Glenn Richard Carlson, Andrew Meyer, Thomas R. Opie
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Publication number: 20120021066Abstract: The present invention relates to the use of hydrazone compounds and copper for controlling the growth of fungi.Type: ApplicationFiled: January 14, 2010Publication date: January 26, 2012Applicant: Dow Agrosciences LLCInventors: David H. Young, Steven Howard Shaber, Cruz Avila-Adame, Nneka T. Breaux, James M. Ruiz, Thomas L. Siddall, Jeffery D. Webster
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Publication number: 20120009274Abstract: The present invention relates to the use of hydrazone compounds and copper for controlling the growth of fungi.Type: ApplicationFiled: January 14, 2010Publication date: January 12, 2012Applicant: Dow Agrosciences LLCInventors: David H. Young, Steven Howard Shaber, Cruz Avila-Adame, Nneka T. Breaux, James M. Ruiz, Thomas L. Siddall, Jeffery D. Webster
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Patent number: 8044241Abstract: Estrogen-Related Receptor (ERR) modulating compounds and methods for synthesis of said compounds are described.Type: GrantFiled: May 29, 2009Date of Patent: October 25, 2011Assignee: City of HopeInventors: Barry Forman, Donna Yu
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Publication number: 20110224302Abstract: Novel difluorophenyldiacylhydrazide derivatives of the formula I, in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in claim 1, are kinase inhibitors and can be used for the treatment of diseases and complaints such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in any type of fibroses, inflammatory processes, tumours and tumour diseasesType: ApplicationFiled: November 2, 2009Publication date: September 15, 2011Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Thomas Fuchss, Ulrich Graedler, Norbert Beier, Rolf Gericke, Florian Lang
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Publication number: 20110218353Abstract: Disclosed are fluorovinyl ether functionalized aromatic diesters and derivatives thereof. The compounds disclosed have utility as functionalized monomers and comonomers in polyesters, polyamides, and the like. It has been found that incorporation of the monomers into polymers provides improved soil resistance to shaped articles produced from the polymers.Type: ApplicationFiled: September 1, 2010Publication date: September 8, 2011Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventors: Neville Everton Drysdale, Surbhi Mahajan, Kenneth Gene Moloy, Fredrik Nederberg, Joel M. Pollino, Joachim C. Ritter
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Publication number: 20110189306Abstract: The present invention relates to therapeutic and/or prophylactic uses of hydrazide compounds and to pharmaceutical compositions containing one or more of these compounds as an active component for treating a disease or disorder requiring modulation of vacuolar (H+)-ATPases.Type: ApplicationFiled: January 13, 2011Publication date: August 4, 2011Inventors: Norbert Kartner, Morris Frank Manolson
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Publication number: 20110124664Abstract: Aspects of the present invention relate to compounds and methods useful in modulating angiogenesis and methods of treating or preventing diseases associated with angiogenesis by administering a polycationic compound. The present invention relates to methods of use and compositions for inhibiting angiogenesis-mediated disorders in mammals including animals and humans. Additionally, this invention relates to the combined use of polycations with other anti-angiogenesis agents for the treatment of different angiogenesis-mediated disorders. Additionally, those polycationic compounds can be used with various anti-inflammatory and cytotoxic agents as well as with radio-therapeutic agents in cancer patients to prevent and treat tumor growth and metastasis.Type: ApplicationFiled: December 17, 2010Publication date: May 26, 2011Applicant: POLYMEDIX, INC.Inventors: Shaker Mousa, Dahui Liu
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Publication number: 20110119775Abstract: The invention provides compositions, pharmaceutical preparations and methods for inhibition of cystic fibrosis transmembrane conductance regulator protein (CFTR) that are useful for the study and treatment of CFTR-mediated diseases and conditions. The compositions and pharmaceutical preparations of the invention may comprise one or more hydrazide-containing compounds, and may additionally comprise one or more pharmaceutically acceptable carriers, excipients and/or adjuvants. The methods of the invention comprise, in certain embodiments, administering to a patient suffering from a CFTR-mediated disease or condition, an efficacious amount of a hydrazide-containing compound. In other embodiments the invention provides methods of inhibiting CFTR that comprise contacting cells in a subject with an effective amount of a hydrazide-containing compound.Type: ApplicationFiled: January 21, 2011Publication date: May 19, 2011Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Alan Verkman, Nitin Dattatraya Sonawane, Chatchai Muanprasat
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Publication number: 20110060050Abstract: The present invention relates to a compound of the formula I, Ia and Ib, and its pharmaceutically usable tautomers, salts, stereoisomers and the enantiomers, including mixtures thereof in all ratios.Type: ApplicationFiled: February 17, 2009Publication date: March 10, 2011Applicant: Merck Patent GmbHInventors: Thomas Fuchss, Rolf Gericke, Norbert Beier, Florian Lang, Phillipp Lang, Karl Lang
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Publication number: 20110059957Abstract: The present invention provides a novel benzene derivative or thiophene derivative useful as a VAP-1 inhibitor, or a medicament for the prophylaxis or treatment of a VAP-1 associated disease and the like, namely, a compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 29, 2009Publication date: March 10, 2011Applicant: R-TECH UENO, LTD.Inventors: Tatsuya Matsukawa, Kazuhiro Masuzaki, Akiko Kawasaki, Akiko Akasaka, Yosuke Kawai
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Publication number: 20100298344Abstract: Aspects of the present invention relate to compounds and methods useful in modulating angiogenesis and methods of treating or preventing diseases associated with angiogenesis by administering a polycationic compound. The present invention relates to methods of use and compositions for inhibiting angiogenesis-mediated disorders in mammals including animals and humans. Additionally, this invention relates to the combined use of polycations with other anti-angiogenesis agents for the treatment of different angiogenesis-mediated disorders. Additionally, those polycationic compounds can be used with various anti-inflammatory and cytotoxic agents as well as with radio-therapeutic agents in cancer patients to prevent and treat tumor growth and metastasis.Type: ApplicationFiled: March 10, 2010Publication date: November 25, 2010Inventors: Shaker Mousa, Dahui Liu
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Publication number: 20100292334Abstract: This invention relates to N-acylhydrazone derivatives, which are found to be useful as modulators of the nicotinic acetylcholine receptors. Due to their to pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: November 19, 2008Publication date: November 18, 2010Applicant: NeuroSearch A/SInventors: Antonio Nardi, Jeppe Kejser Christensen, Dan Peters, Tino Dyhring
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Publication number: 20100240654Abstract: A compound represented by the following general formula (1) or a salt thereof or a hydrate of the foregoing is safe while exhibiting suitable physicochemical stability, and is useful as therapeutic or prophylactic agents for diseases associated with thrombus formation. wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc., R2 represents optionally substituted phenyl, etc., R3 represents optionally substituted C6-10 aryl, etc., Z1, Z2 and Z3 each independently represent hydrogen, etc., Z4 represents hydrogen, etc. and X represents a single bond or —CO—, etc.Type: ApplicationFiled: June 1, 2010Publication date: September 23, 2010Inventors: Richard CLARK, Shinsuke HIROTA, Hiroshi AZUMA, Kazunobu KIRA, Nobuhisa WATANABE, Tadashi NAGAKURA, Tatsuo HORIZOE
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Patent number: 7776920Abstract: Novel mandelic hydrazides of the formula (I), in which R1-R11 have the meanings indicated in claim 1, are SGK inhibitors and can be used for the treatment of SGK-induced diseases and complaints, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in fibroses and inflammatory processes of any type.Type: GrantFiled: January 18, 2007Date of Patent: August 17, 2010Assignee: Merck Patent GmbHInventors: Rolf Gericke, Markus Klein, Werner Mederski, Norbert Beier, Florian Lang
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Patent number: 7767716Abstract: Novel acyl hydrazides of the formula (I), in which R1-R9 have the meanings indicated in claim 1, are SGK inhibitors and can be used for the treatment of SGK-induced diseases and complaints, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and renal diseases, generally in fibroses and inflammatory processes of any type.Type: GrantFiled: March 10, 2006Date of Patent: August 3, 2010Assignee: Merck Patent GmbHInventors: Rolf Gericke, Dieter Dorsch, Werner Mederski, Markus Klein, Norbert Beier, Florian Lang
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Publication number: 20090221712Abstract: Novel mandelic hydrazides of the formula (I), in which R1-R11 have the meanings indicated in claim 1, are SGK inhibitors and can be used for the treatment of SGK-induced diseases and complaints, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in fibroses and inflammatory processes of any type.Type: ApplicationFiled: January 18, 2007Publication date: September 3, 2009Inventors: Rolf Gericke, Markus Klein, Werner Mederski, Norbert Beier, Florian Lang
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Patent number: 7544838Abstract: Estrogen-Related Receptor (ERR) modulating compounds and methods for synthesis of said compounds are described.Type: GrantFiled: January 20, 2006Date of Patent: June 9, 2009Assignee: City of HopeInventors: Barry Forman, Donna Yu
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Patent number: 7485752Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.Type: GrantFiled: May 5, 2006Date of Patent: February 3, 2009Assignee: Hoffman-La Roche Inc.Inventor: Christophe Michoud
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Publication number: 20080269206Abstract: The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-6 or encompassed by formulas I-VI) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.Type: ApplicationFiled: March 28, 2008Publication date: October 30, 2008Inventors: Michael Geoffrey Neil Russell, Huw David Vater, Jacqueline Anne Macritchie, Kevin James Doyle, David Brown, Joanne Peach