Hydrazine Containing Patents (Class 564/148)
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Patent number: 11339272Abstract: An additive for rubber that enables a rubber composition to have excellent low heat generating property and processability, a rubber composition containing the additive for rubber, and a tire using the same are provided.Type: GrantFiled: November 29, 2017Date of Patent: May 24, 2022Assignees: BRIDGESTONE CORPORATION, OTSUKA CHEMICAL CO., LTD.Inventors: Satoshi Hamatani, Shinya Shinozaki, Mifuyu Ueno, Masaki Abe
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Patent number: 10870618Abstract: 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 cancer.Type: GrantFiled: October 13, 2017Date of Patent: December 22, 2020Assignee: MUSC FOUNDATION FOR RESEARCH DEVELOPMENTInventors: Chung-Jen James Chou, Jesse McClure, Cheng Zhang, Elizabeth Inks
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Patent number: 10822456Abstract: An azide group-containing fluoropolymer of formula (1) having a perfluoropolyether group of specific molecular structure as the backbone and terminated with an azide group via methylene group is provided.Type: GrantFiled: November 21, 2018Date of Patent: November 3, 2020Assignee: SHIN-ETSU CHEMICAL CO., LTD.Inventors: Ryuto Hayashi, Kenichi Fukuda
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Patent number: 9169210Abstract: 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: GrantFiled: September 5, 2012Date of Patent: October 27, 2015Assignee: 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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Patent number: 9085550Abstract: Estrogen-Related Receptor (ERR) modulating compounds and methods for synthesis of said compounds are described.Type: GrantFiled: September 20, 2011Date of Patent: July 21, 2015Assignee: CITY OF HOPEInventors: Barry Forman, Donna Yu
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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: 20150025042Abstract: Disclosed are compounds of formulae (I), (III), (IV), (VII), (X), (XI), (XII), (XIII) and (XIV), wherein the variables are as defined in the claims, and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.Type: ApplicationFiled: December 16, 2013Publication date: January 22, 2015Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Shoujun Chen, Keizo Koya, Zachary Demko, Lijun Sun
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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: 8809578Abstract: The present invention relates to a novel compound having excellent antioxidant activity, isolated from Ramalina terebrata, and more particularly to a novel compound, RAMALIN™, having excellent antioxidant activity, isolated from the Antarctic lichen Ramalina terebrata, a method for preparing the RAMALIN™, and a pharmaceutical composition, a functional food and a functional cosmetic composition, which contain the RAMALIN™ as an active ingredient. The RAMALIN™ according to the invention has significantly excellent antioxidant effects compared to commercially available antioxidants, and thus can be widely used in agents for treating oxidation-related diseases, anti-aging functional foods, functional cosmetic products for skin whitening and wrinkle reduction, etc.Type: GrantFiled: November 10, 2009Date of Patent: August 19, 2014Assignee: Korea Ocean Research and Development InstituteInventors: Joung Han Yim, Hong Kum Lee, Hari Datta Bhattarai, Paudel Babita, Il Chan Kim, Soon Gyu Hong, Doc Kyu Kim, Yoo Kyung Lee, Sung Gu Lee, Hyun Cheol Oh
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Patent number: 8809395Abstract: The present invention is directed to compounds, intermediates and methods for making valerenic acid and its derivatives as well as the use of such compounds as GABAA receptor ligands.Type: GrantFiled: January 22, 2010Date of Patent: August 19, 2014Assignee: Valericon GmbHInventors: Johann Mulzer, Jürgen Ramharter, Steffen Hering, Sophia Khom
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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: 8741324Abstract: The present invention relates to liquid pesticide concentrate compositions which comprise at least one organic pesticide compound that is sparingly or even insoluble in water and which upon dilution with water form stable aqueous nanoparticulate formulations. The liquid pesticide concentrate compositions of the invention comprise: a) at least one organic pesticide compound C having a water solubility of not more than 1 g/l at 25° C./1013 mbar, b) at least one organic solvent S having a water solubility at least 10 g/l at 25° C.Type: GrantFiled: July 5, 2005Date of Patent: June 3, 2014Assignee: BASF SEInventors: Charles W. Finch, Thomas Byrne, Hassan Oloumi-Sadeghi
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Patent number: 8637608Abstract: Fluoropolymers containing one or more azide group wherein the azide group is not a sulfonyl-azide group and processes of preparing them.Type: GrantFiled: August 17, 2009Date of Patent: January 28, 2014Assignee: 3M Innovative Properties CompanyInventors: Klaus Hintzer, Michael Juergens, Harald Kaspar, Kai H. Lochhaas, Oleg Shyshkov, Andre Streiter, Tilman C. Zipplies, Sabine H. G. Beuermann, Muhammad Imran ul-haq
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Patent number: 8581004Abstract: Disclosed are compounds of Formula (I) and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.Type: GrantFiled: February 20, 2009Date of Patent: November 12, 2013Assignee: Synta Pharmaceuticals Corp.Inventors: Teresa Kowalczyk-Przewloka, Lijun Sun
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Patent number: 8524948Abstract: 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: GrantFiled: September 23, 2011Date of Patent: September 3, 2013Assignee: 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: 20130190296Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Tip-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.Type: ApplicationFiled: November 20, 2012Publication date: July 25, 2013Applicant: Dendreon CorporationInventor: Dendreon Corporation
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Patent number: 8440820Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.Type: GrantFiled: January 11, 2012Date of Patent: May 14, 2013Assignee: Reata Pharmaceuticals, Inc.Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick
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Patent number: 8410152Abstract: Described are compounds having a thiazolhydrazide scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said thiazolhydrazide compounds can be used for prophylaxis and/or treatment of neurodegenerative diseases and conditions.Type: GrantFiled: November 5, 2007Date of Patent: April 2, 2013Assignees: Max-Planck-Gesellschaft zur Forderung der Wissenschaften e. V., Technische Universitat Darmstadt, The Provost Fellows and Scholars of the College of the Holy and Undivided Trinity of Queen Elizabeth near DublinInventors: Eckhard Mandelkow, Eva-Maria Mandelkow, Markus Pickhardt, Jacek Biernat, David George Lloyd, Boris Schmidt, Gregor Larbig
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Patent number: 8383857Abstract: 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 27, 2012Date of Patent: February 26, 2013Assignee: Wyeth LLCInventors: George Anello Chiarello, Ayman Sahli
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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: 20120065235Abstract: Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.Type: ApplicationFiled: August 7, 2008Publication date: March 15, 2012Inventors: Lijun Sun, Jun Jiang
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Patent number: 8110705Abstract: 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: May 20, 2008Date of Patent: February 7, 2012Assignee: Wyeth LLCInventors: George Anello Chiarello, Ayman Sahli
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Patent number: 8071809Abstract: Disclosed herein are accelerants for the formation of oxime-containing compounds from the reaction of a carbonyl-containing compound and a hydroxylamine-containing compound. The oxime-containing compound, the carbonyl-containing compound and the hydroxylamine-containing compound can each be a non-natural amino acid or a non-natural amino acid polypeptide. Also disclosed is the use of such accelerants to form oxime-containing compounds, the resulting oxime-containing compounds, and reaction mixtures containing such accelerants.Type: GrantFiled: November 12, 2010Date of Patent: December 6, 2011Assignee: Ambrx, Inc.Inventors: Feng Tian, Zhenwei Miao
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Publication number: 20110294814Abstract: Disclosed are compounds of Formula (I) and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.Type: ApplicationFiled: February 20, 2009Publication date: December 1, 2011Inventors: Teresa Kowalczyk-Prezewloka, Lijun Sun
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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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Patent number: 7915402Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.Type: GrantFiled: April 20, 2009Date of Patent: March 29, 2011Assignee: Reata Pharmaceuticals, Inc.Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick
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Patent number: 7888533Abstract: Disclosed herein are accelerants for the formation of oxime-containing compounds from the reaction of a carbonyl-containing compound and a hydroxylamine-containing compound. The oxime-containing compound, the carbonyl-containing compound and the hydroxylamine-containing compound can each be a non-natural amino acid or a non-natural amino acid polypeptide. Also disclosed is the use of such accelerants to form oxime-containing compounds, the resulting oxime-containing compounds, and reaction mixtures containing such accelerants.Type: GrantFiled: October 26, 2007Date of Patent: February 15, 2011Assignee: Ambrx, Inc.Inventors: Feng Tian, Zhenwei Miao
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Patent number: 7750042Abstract: One embodiment of the present invention is a compound represented by the Structural Formula (I): Y is a covalent bond of a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C?Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 is an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, or a substituted non-aromatic heterocyclic group, R2-R4 are independently —H, an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, a substituted non-aromatic heterocyclic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring.Type: GrantFiled: March 20, 2008Date of Patent: July 6, 2010Assignee: Synta Pharmaceuticals Corp.Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Noriaki Tatsuta, Yaming Wu, Mitsunori Ono, Zhi-Qiang Xia
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Publication number: 20100136652Abstract: A method is disclosed for making a conjugate of two molecules using a hydrazide thiol linker. In a particular working embodiment, an Fc-specific antibody-enzyme conjugate is made using the method and demonstrated to provide exceptional staining sensitivity and specificity in immunohistochemical and in situ hybridization assays.Type: ApplicationFiled: January 14, 2010Publication date: June 3, 2010Inventors: Christopher Bieniarz, Julia Ashworth-Sharpe, Casey A. Kernag, Jerome W. Kosmeder, Mark Lefever
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Patent number: 7709683Abstract: A method of preparing a bis(thio-hydrazide amide) disalt includes the steps of combining a neutral bis(thio-hydrazide amide), an organic solvent and a base to form a bis(thio-hydrazide amide) solution; and combining the solution and methyl tert-butyl ether, thereby precipitating a disalt of the bis(thio-hydrazide amide). In some embodiments, a method of preparing a bis(thio-hydrazide amide) disalt includes the steps of combining a neutral bis(thio-hydrazide amide) and an organic solvent selected from methanol, ethanol, acetone, and methyl ethyl ketone to make a mixture; adding at least two equivalents of a base selected from sodium hydroxide, potassium hydroxide, sodium methoxide, potassium methoxide, sodium ethoxide and potassium ethoxide to the mixture, thereby forming a solution; and combining the solution and methyl tert-butyl ether to precipitate the disalt of the bis(thio-hydrazide amide).Type: GrantFiled: May 11, 2006Date of Patent: May 4, 2010Assignee: Synta Pharmaceuticals Corp.Inventors: Shoujun Chen, Zhi-Qiang Xia
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Publication number: 20100056777Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.Type: ApplicationFiled: April 20, 2009Publication date: March 4, 2010Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick
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Publication number: 20090311182Abstract: This invention relates to biotechnology, more particularly, to water-soluble polymeric delivery systems for the imaging, evaluation and/or treatment of rheumatoid arthritis and other inflammatory diseases. Using modern MR imaging techniques, the specific accumulation of macromolecules in arthritic joints in adjuvant-induced arthritis in rats is demonstrated. The strong correlation between the uptake and retention of the MR contrast agent labeled polymer with histopathological features of inflammation and local tissue damage demonstrates the practical applications of the macromolecular delivery system of the invention.Type: ApplicationFiled: January 9, 2009Publication date: December 17, 2009Inventors: Dong Wang, Xinming Liu, Ling-Dong Quan
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Patent number: 7619115Abstract: Novel ortho-substituted N?-benzylidene-(3-hydroxyphenyl)acetohydrazides 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 conditions, 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: June 6, 2005Date of Patent: November 17, 2009Assignee: Merck Patent GmbHInventors: Rolf Gericke, Dieter Dorsch, Werner Mederski, Norbert Beier, Florian Lang
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Publication number: 20090253161Abstract: Fluorescent probe compound of Formula Ia or Formula Ib: are described, along with methods of using the same to detect iron, copper, and hydrogen peroxide.Type: ApplicationFiled: April 2, 2009Publication date: October 8, 2009Applicant: Duke UniversityInventors: Katherine J. Franz, Lynne M. Hyman
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Patent number: 7563928Abstract: 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: GrantFiled: August 20, 2007Date of Patent: July 21, 2009Assignee: 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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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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Patent number: 7468458Abstract: Disclosed herein are accelerants for the formation of oxime-containing compounds from the reaction of a carbonyl-containing compound and a hydroxylamine-containing compound. The oxime-containing compound, the carbonyl-containing compound and the hydroxylamine-containing compound can each be a non-natural amino acid or a non-natural amino acid polypeptide. Also disclosed is the use of such accelerants to form oxime-containing compounds, the resulting oxime-containing compounds, and reaction mixtures containing such accelerants.Type: GrantFiled: October 19, 2007Date of Patent: December 23, 2008Assignee: Amerx, Inc.Inventors: Feng Tian, Zhenwei Miao
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Publication number: 20080308007Abstract: The invention concerns a method for preparing a bitumen base, including the following essential steps: a) introducing a bitumen in a container equipped with mixing means, and bringing the bitumen to a temperature of 120° C. to 300° C.; b) introducing at least one chemical blowing additive into the container, and mixing, said chemical blowing additive being of general formula Ar1-R—Ar2 (1) wherein Ar1 and Ar2 independently of each other represent a benzene ring or a system of condensed aromatic rings of 6 to 20 carbon atoms, substituted by at least one hydroxyl group, and R represents an optionally substituted divalent radical, whereof the main chain comprises 6 to 20 carbon atoms and at least one amide and/or ester group. The invention also concerns a bitumen base obtained by implementing said method, as well as the use of such bitumen bases in road surfacing and industrial applications.Type: ApplicationFiled: July 28, 2006Publication date: December 18, 2008Inventors: Laurence Lapalu, Regis Vincent
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Patent number: 7456315Abstract: 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: GrantFiled: February 26, 2004Date of Patent: November 25, 2008Assignee: 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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Patent number: 7405239Abstract: The invention relates to acylhydrazone derivatives of formula (I), which are SGK inhibitors and can be used for the treatment of diseases and afflictions associated with SGK, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systematic and pulmonary hypertension, cardiovascular diseases and kidney diseases and in general for all types of fibroses and inflammatory processes. In said formula: R1 and R5 independently of one another represent H, OH, OA, OAc or methyl; R2, R3, R4, R6, R7, R8, R9 and R10 independently of one another represent H, OH, OA, OAc, OCF3, Hal, NO2, CF3, A, CN, OSO2CH3, SO2CH3, NH2, or COOH; R11 represents H or CH3; A represents an alkyl comprising 1, 2, 3, or 4 C atoms; X represents CH2, CH2CH2, OCH2 or —CH(OH)— and Hal represents F, Cl, Br or I.Type: GrantFiled: September 16, 2004Date of Patent: July 29, 2008Assignee: Merck Patent GmbHInventors: Rolf Gericke, Norbert Beier, Oliver Poeschke, Lars Burgdorf, Helga Drosdat, Florian Lang
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Patent number: 7368473Abstract: One embodiment of the present invention is a compound represented by the Structural Formula (I): Y is a covalent bond of a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C?Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 is an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, or a substituted non-aromatic heterocyclic group, R2-R4 are independently —H, an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, a substituted non-aromatic heterocyclic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring.Type: GrantFiled: October 5, 2005Date of Patent: May 6, 2008Assignee: Synta Pharmaceuticals Corp.Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Noriaki Tatsuta, Yaming Wu, Mitsunori Ono, Zhi-Qiang Xia
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Patent number: 7317125Abstract: 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: January 31, 2006Date of Patent: January 8, 2008Assignee: Hoffman-La Roche Inc.Inventors: David Robert Bolin, Christophe Michoud
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Patent number: 7173063Abstract: Methods for the treatment of a proliferative disorder are provided in which a subject in need of such treatment is administered an effective amount of a compound selected from: compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X1 and X2 are independently H, Cl, F, Br, I, CN, CF3 or NO2, and Ar1 is a substituted or unsubstituted aryl or a substituted or unsubstituted heteroaryl; and compounds of formula (II) wherein X3 and X4 are each independently H, Cl, F, Br, I, CN, CF3 or NO2; Y is (C2–C6)alkylene or (C2–C6)heteroalkylene; and Z is Cl, F, Br, I, CN, CF3 or NO2.Type: GrantFiled: November 10, 2000Date of Patent: February 6, 2007Assignee: Fred Hutchinson Cancer Research CenterInventors: John R. Lamb, Julian Simon, Heather Dunstan, Stephen H. Friend
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Patent number: 7153815Abstract: A insecticide characterized by containing as active ingredient a hydrazone derivative of formula (I) wherein A and Q are an aryl or a heterocyclic group, W is oxygen atom, an aminylene, an alkylene group, an oxyalkylene group or an alkyleneoxy, X1 and X2 are hydrogen atom, an alkyl, an alkenyl, an alkynyl, an aryl, a heterocyclic group, formyl, an acyl, an alkoxycarbonyl, an aryloxycarbonyl, a heterocyclic oxycarbonyl, an alkylsulfinyl, an arylsulfinyl, a heterocyclic sulfinyl, an alkylsulfonyl, an arylsulfonyl or a heterocyclic sulfonyl, Y is oxygen atom or sulfur atom, Z is hydrogen atom, a halogen atom, cyano, an alkyl, an alkenyl, an alkynyl, an amino, an alkoxy or an alkylthio, the substituents may be substituted; and novel hydrazon derivatives.Type: GrantFiled: January 10, 2003Date of Patent: December 26, 2006Assignee: Nihon Nohyaku Co., Ltd.Inventors: Shinji Kawata, Shuko Okui, Shigeru Suzuki, Toshiki Fukuchi, Akiyuki Suwa
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Patent number: 7049343Abstract: A method for the inhibition of high affinity glycine transporters, compounds that inhibit these transporters; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of disease states in which glycine is involved are disclosed.Type: GrantFiled: September 7, 2001Date of Patent: May 23, 2006Assignee: Merck & Co., Inc.Inventors: Syed M. Ali, Kurt R. Brunden, Dario Doller, Brian Herbert, Jack B. Jiang, Amy Jordan
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Patent number: 7038074Abstract: The invention relates generally to a novel type of arginine mimetics which are inhibitors of factor Xa; to pharmaceutical compositions which comprise these mimetics; and to the use of these arginine mimetics for producing compositions for antithrombotic therapy.Type: GrantFiled: February 9, 2001Date of Patent: May 2, 2006Assignee: Wilex AGInventors: Luis Moroder, Stefan Sperl, Jörg Stürzebecher
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Patent number: 6924312Abstract: Disclosed is a compound represented by the Structural Formula (I): Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C?Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 and R2 are independently an aryl group or a substituted aryl group, R3 and R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is ?O or ?S.Type: GrantFiled: January 15, 2003Date of Patent: August 2, 2005Assignee: Synta Pharmaceuticals Corp.Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Noriaki Tatsuta, Yaming Wu, Mitsunori Ono
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Patent number: 6825235Abstract: Disclosed is a method of preparing a thiohydrazide product compound from a hydrazide starting compound. The hydrazide starting compound is represented by Structural Formula (I): The thiohydrazide product compound is represented by Structural Formula (II): In Structural Formulas (I)-(II), R1 and R2 are independently an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R2 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. When R2 is an aryl group or a substituted aryl group, then R5 is a hydrazine protecting group; and when R2 is an aliphatic or substituted aliphatic group, then R5 is —H or a hydrazine protecting group. R10 is —H or a substituted or unsubstituted alkyl group. The method comprising the step of reacting the starting compound with a thionylating reagent.Type: GrantFiled: July 10, 2002Date of Patent: November 30, 2004Assignee: Synta Pharmaceuticals Corp.Inventors: Shoujun Chen, Lijun Sun, Zhi-Qiang Xia, Keizo Koya, Mitsunori Ono
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Patent number: 6800660Abstract: Disclosed is a compound represented by the Structural Formula (I): Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C═Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 and R2 are independently an aryl group or a substituted aryl group, R3 and R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is ═O or ═S.Type: GrantFiled: July 10, 2002Date of Patent: October 5, 2004Assignee: Synta Pharmaceuticals Corp.Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Noriaki Tatsuta, Yaming Wu, Mitsunori Ono