Chalcogen Attached Indirectly To The Hetero Ring By Acyclic Nonionic Bonding Patents (Class 549/495)
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Patent number: 9320722Abstract: Described herein are compositions and methods for the treatment of cancer, and in particular cancers characterized by a high level of ALD3H1 activity, which is associated with chemoresistance to cancer chemotherapeutic agents that are degraded by ALD3H1. The compositions described herein act as competitive inhibitors of ALD3H1 and thereby reduce breakdown of chemotherapeutics by this enzyme, and increase their efficacy for cancer treatment.Type: GrantFiled: September 26, 2014Date of Patent: April 26, 2016Assignee: Indiana University Research and Technology CorporationInventor: Thomas D. Hurley
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Patent number: 8906946Abstract: Compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (hereinafter referred to as TRPM8), having formula: Wherein R is selected from: H, Br, CN, NO2, SO2NH2, SO2NHR? and SO2NR?2, where R? is selected from linear or branched C1-C4 alkyl; X is selected from: F, Cl, C1-C3 alkyl, NH2 and OH Y is selected from: O, CH2, NH and SO2 R1 and R2, independently one from the other, are selected from H, F and linear or branched C1-C4 alkyl; R3 and R4, independently one from the other, are selected from H and linear or branched C1-C4 alkyl; Z is selected from: NR6 and R6R7N+, where R6 and R7 independently one from the other, are selected from: H and linear or branched C1-C4 alkyl R5 is a residue selected from: H and linear or branched C1-C4 alkyl Het is a heteroaryl group selected from a substituted or not substituted pyrrolyl, a substituted or not substituted N-methylpyrrolyl, a substituted or not substituted thiophenyl, a substituted orType: GrantFiled: January 27, 2012Date of Patent: December 9, 2014Assignee: Dompe' S.p.A.Inventors: Alessio Moriconi, Gianluca Bianchini, Andrea Aramini, Laura Brandolini, Chiara Liberati, Silvia Bovolenta, Andrea Beccari, Simone Lorenzi
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Patent number: 8883180Abstract: The invention relates to active compound combinations, in particular a fungicidal and/or insecticidal composition, comprising Isotianil (3,4-dichloro-N-(2-cyanophenyl)-5-isothiazolecarboxamide) and at least one further insecticide of the anthranilamide group and optionally one further insecticide of the neonicotinoids. Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi and/or microorganisms and/or pests of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.Type: GrantFiled: August 29, 2013Date of Patent: November 11, 2014Assignee: Bayer Intellectual Property GmbHInventors: Lutz Assmann, Ulrike Wachendorff-Neumann, Peter Dahmen, Heike Hungenberg, Wolfgang Thielert
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Publication number: 20140094492Abstract: Derivatives of sulindac that lack cyclooxygenase inhibitory activity are provided along with pharmaceutical compositions containing them and use for treatment or prevention of cancer. The derivatives of sulindac are also suitable for treating chronic inflammatory conditions. A method for preparing the derivatives is also provided.Type: ApplicationFiled: March 30, 2012Publication date: April 3, 2014Applicant: Southern Research InstituteInventors: Robert Reynolds, Bini Mathew, Gary A. Piazza
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Publication number: 20140031398Abstract: Compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (hereinafter referred to as TRPM8), having formula: Wherein R is selected from: H, Br, CN, NO2, SO2NH2, SO2NHR? and SO2NR?2, where R? is selected from linear or branched C1-C4 alkyl; X is selected from: F, Cl, C1-C3 alkyl, NH2 and OH Y is selected from: O, CH2, NH and SO2 R1 and R2, independently one from the other, are selected from H, F and linear or branched C1-C4 alkyl; R3 and R4, independently one from the other, are selected from H and linear or branched C1-C4 alkyl; Z is selected from: NR6 and R6R7N+, where R6 and R7 independently one from the other, are selected from: H and linear or branched C1-C4 alkyl R5 is a residue selected from: H and linear or branched C1-C4 alkyl Het is a heteroaryl group selected from a substituted or not substituted pyrrolyl, a substituted or not substituted N-methylpyrrolyl, a substituted or not substituted thiophenyl, a substituted orType: ApplicationFiled: January 27, 2012Publication date: January 30, 2014Inventors: Alessio Moriconi, Gianluca Bianchini, Andrea Aramini, Laura Brandolini, Chiara Liberati, Silvia Bovolenta, Andrea Beccari, Simone Lorenzi
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Publication number: 20130303791Abstract: Described herein are single step methods of making various classes of alkylamine derivatives of furan and tetrahydrofuran by simultaneous contact of a sugar with H2, an acid catalyst and hydrogenation catalyst in the presence of an alkylamide solvent. The hydrogenation catalyst is a heterogeneous catalyst comprising a metal selected from the group consisting of Pt, Pd, and nickel. The acid catalysts may be homogeneous mineral acid or a heterogeneous acid catalyst on substrate. In a preferred practice the two catalysts are provided on a common heterogeneous bifunctional support. Using similar combinations of acid and hydrogenation catalysts, there is also described single step methods for making furandimethanol by simultaneously contacting a hexose with the two separate catalysts in the presence of H2 in an aprotic solvent, such as dimethylformamide. With the same catalyst system and similar reaction conditions, 2,5 furan dialkylethers can also be made in a single step when the solvent includes an ROH alcohol.Type: ApplicationFiled: December 13, 2011Publication date: November 14, 2013Applicant: ARCHER DANIELS MIDLAND COMPANYInventors: Stephen Howard, Alexandra Sanborn
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Publication number: 20130225619Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted heterocyclic amine derivative compound and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.Type: ApplicationFiled: January 18, 2013Publication date: August 29, 2013Applicant: Acucela Inc.Inventors: Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Ryo Kubota
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Publication number: 20130123253Abstract: Disclosed are agents having pharmacological activity against cellular receptors and intracellular signaling, particularly receptors and signaling pathways of central nervous system (CNS) neurotransmitters. Also disclosed are related methods and compositions for the treatment or prevention of diseases or disorders using the agents.Type: ApplicationFiled: May 1, 2012Publication date: May 16, 2013Applicant: HUMAN BIOMOLECULAR RESEARCH INSTITUTEInventor: John CASHMAN
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Publication number: 20130090459Abstract: The present invention relates to methods for rapid crystallization of amino acids, drug molecules, proteins and DNA/peptides. One method for rapid crystallization of functional group-containing molecules selected from the group consisting of amino acids, drug molecules, proteins and DNA/peptides includes (A) providing at least one metal or metal oxide in particulate or thin film form to provide (a) selective nucleation sites for crystallization of the functional group-containing molecules due to interactions of their functional groups and metal surfaces or engineered metal surfaces and (b) a microwave-transparent medium to create a thermal gradient between the metal surfaces or engineered metal surfaces and a warmer solution containing functional group-containing molecules to be crystallized, and (B) conducting microwave heating to cause the functional group-containing molecules to be crystallized.Type: ApplicationFiled: October 11, 2012Publication date: April 11, 2013Applicant: MORGAN STATE UNIVERSITYInventor: Morgan State University
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Publication number: 20130023463Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: ApplicationFiled: April 19, 2012Publication date: January 24, 2013Applicant: ABBOTT LABORATORIESInventors: Charles A. Flentge, Hui-Ju Chen, David A. DeGoey, William J. Flosi, David J. Grampovnik, Peggy P. Huang, Dale J. Kempf, Larry L. Klein, Allan C. Krueger, Darold L. Madigan, John T. Randolph, Minghua Sun, Ming C. Yeung, Chen Zhao
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Publication number: 20120232294Abstract: Process for preparing alkanolamines which have a primary amino group (—NH2) and a hydroxyl group (—OH) by alcohol amination of diols having two hydroxyl groups (—OH) by means of ammonia with elimination of water, wherein the reaction is carried out homogeneously catalyzed in the presence of at least one complex catalyst comprising at least one element selected from groups 8, 9 and 10 of the Periodic Table and also at least one donor ligand.Type: ApplicationFiled: March 8, 2012Publication date: September 13, 2012Applicant: BASF SEInventors: Thomas SCHAUB, Boris Buschhaus, Marion Kristina Brinks, Mathias Schelwies, Rocco Paciello, Johann-Peter Melder, Martin Merger
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Publication number: 20120015911Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.Type: ApplicationFiled: September 20, 2011Publication date: January 19, 2012Applicant: Bellus Health Inc.Inventors: Xianqi Kong, Xinfu Wu, Abderrahim Bouzide, Isabelle Valade, David Migneault, Francine Gervais, Daniel Delorme, Benoit Bachand, Mohamed Atfani, Sophie Levesque, Bita Samim
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Publication number: 20110306493Abstract: The invention relates to sulfoximinamid compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to the use of the sulfoximinamid compounds, of their salts or of compositions comprising them for combating animal pests. Furthermore the invention relates also to methods of applying such sulfoximine compounds. The sulfoximinamid compounds of the present invention are defined by the following formula I: wherein Q, Het, R1, R2, R3, R4 and n are defined as in the description.Type: ApplicationFiled: June 19, 2009Publication date: December 15, 2011Applicant: BASF SEInventors: Ralph Paulini, Delphine Breuninger, Wolfgang Von Deyn, Henricus Maria Martinus Bastiaans, Carsten Beyer, Douglas D. Anspaugh, Hassan Oloumi-Sadeghi, Faraneh Oloumi
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Publication number: 20110137049Abstract: The invention provides a chiral iridium aqua complex which has good preservation stability, can be easily produced, and enables asymmetric transfer hydrogenation in a higher yield and with higher stereoselectivity.Type: ApplicationFiled: July 6, 2009Publication date: June 9, 2011Applicants: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: Erick M. Carreira
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Patent number: 7943803Abstract: A clathrate compound containing a polymolecular host compound as a host compound and an agricultural chemical active ingredient having a saturated solubility in water at 25° C. of not less than 500 ppm as a guest compound.Type: GrantFiled: May 4, 2010Date of Patent: May 17, 2011Assignee: Nippon Soda Co., Ltd.Inventors: Natsuki Amanokura, Tetsuya Sahara, Hiroshi Suzuki, Yuichi Maekawa, Kiyoshi Katsuura, Yoshihiro Enomoto
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Publication number: 20110098353Abstract: A metal complex of formula (III) wherein: M is a transition metal and A1, A2, X, X?, Y, L1?, R1? and R2? are as defined herein, is useful in medical imaging and therapy.Type: ApplicationFiled: July 5, 2006Publication date: April 28, 2011Inventors: Jonathan Robin Dilworth, Josephine Mary Peach, Julia May Heslop, Paul Stephen Donnelly
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Publication number: 20110003827Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: ApplicationFiled: December 10, 2004Publication date: January 6, 2011Inventors: Charles A. Flentge, Hui-Ju Chen, David A. DeGoey, William J. Flosi, David J. Grampovnik, Peggy P. Huang, Dale J. Kempf, Larry L. Klein, Allan C. Krueger, Darold L. Madigan, John T. Randolph, Minghua Sun, Ming C. Yeung, Chen Zhao
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Publication number: 20100274006Abstract: A clathrate compound containing a polymolecular host compound as a host compound and an agricultural chemical active ingredient having a saturated solubility in water at 25° C. of not less than 500 ppm as a guest compound.Type: ApplicationFiled: May 4, 2010Publication date: October 28, 2010Applicant: NIPPON SODA CO., LTDInventors: Natsuki Amanokura, Tetsuya Sahara, Hiroshi Suzuki, Yuichi Maekawa, Kiyoshi Katsuura, Yoshihiro Enomoto
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Publication number: 20100056528Abstract: The invention provides sulfonamide compounds of formula (I) as defined herein, pharmaceutical compositions containing the same and methods of treatment using such compounds and pharmaceutical compositions. These compounds have a common wide range of beneficial therapeutic indications, in particular as analgesic and anti-inflammatory agents.Type: ApplicationFiled: December 19, 2007Publication date: March 4, 2010Inventors: Avihai Yacovan, Iris Alroy, Alexander Aizikovich, Sima Mirilashvili, Flavio Gryszpan
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Patent number: 7598423Abstract: This application relates to a substituted hydroxyphenyl ketone compound of formula I, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and its use in treating migraine. This application also relates to processes for preparing a compound of formula I, and intermediate compounds useful therein.Type: GrantFiled: November 15, 2005Date of Patent: October 6, 2009Assignee: Eli Lilly and CompanyInventors: Thomas Daniel Aicher, Guillermo S. Cortez, Todd Michael Groendyke, Albert Khilevich, James Allen Knobelsdorf, Fredrik Pehr Marmsater, Jeffrey Michael Schkeryantz, Tony Pisal Tang, Nicholas Andrew Magnus
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Publication number: 20090176990Abstract: Disclosed is an improved process for producing nitroguanidine derivatives represented by the following general formula (3), which has an insecticidal activity, or a salt thereof.Type: ApplicationFiled: February 7, 2007Publication date: July 9, 2009Applicant: Mitsui Chemicals, Inc.Inventors: Hisato Kamekawa, Tomotaka Miyashita, Hiroyuki Katsuta, Toshio Kitashima
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Patent number: 7547716Abstract: A medicament for enhancing an effect of a cancer therapy based on a mode of action of DNA injury, which comprises as an active ingredient a compound represented by the general formula (I) or a physiologically acceptable salt thereof: wherein R represents an aryl-substituted alkyl group, an heteroaryl-substituted alkyl group, a cycloalkyl-substituted alkyl group, or a cyclic hydrocarbon group wherein said cyclic hydrocarbon group may be saturated, partly saturated, or aromatic; or Z may bind to R to form a cyclic structure, Z represents a hydrogen atom or a C1 to C6 alkyl group. The medicament enhanced the effect of the cancer therapy and decreases a dose of an anticancer agent and/or radiation, and therefore, can reduce side effects resulting from the cancer therapy.Type: GrantFiled: June 7, 2002Date of Patent: June 16, 2009Assignee: Institute of Medicinal Molecular Design, Inc.Inventors: Susumu Muto, Masayuki Komukai, Akiko Itai
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Patent number: 7528157Abstract: Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(?O), S(?O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(?O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.Type: GrantFiled: December 22, 2006Date of Patent: May 5, 2009Assignee: Asterand UK LimitedInventors: Alexander W. Oxford, Richard J. Davis, Robert A. Coleman, Kenneth L. Clark, David E. Clark, Neil V. Harris, Garry Fenton, George Hynd, Keith A. J. Stuttle, Jonathan M. Sutton, Christopher G. Newton
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Patent number: 7259166Abstract: 2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a polar ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.Type: GrantFiled: April 10, 2006Date of Patent: August 21, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Wendy Lea Corbett, Joseph Samuel Grimsby, Nancy-Ellen Haynes, Robert Francis Kester, Paige Erin Mahaney, Jagdish Kumar Racha, Ramakanth Sarabu, Ka Wang
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Patent number: 7166622Abstract: Compounds of Formula I, wherein R1–R8 are defined herein are provided, together with pharmaceutically acceptable salts, hydrates, metabolites, and/or prodrugs thereof. Uses of these compounds for inhibiting beta amyloid production and for the prevention and treatment of Alzheimer's Disease and Down's syndrome are described.Type: GrantFiled: June 9, 2003Date of Patent: January 23, 2007Assignees: Wyeth, ArQule, Inc.Inventors: Anthony Frank Kreft, Derek Cecil Cole, Kevin Roger Woller, Joseph Raymond Stock, Kristina Martha Kutterer, Dennis Martin Kubrak, Charles William Mann, William Jay Moore, David Scott Casebier
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Patent number: 7098201Abstract: A compound of the formula (I): wherein X is hydroxy, protected hydroxy or optionally substituted amino; Y is —COORA wherein RA is hydrogen or ester residue, —CONRBRC wherein RB and RC each is independently hydrogen or amide residue, optionally substituted aryl or optionally substituted heteroaryl; and A1 is optionally substituted heteroaryl; provided that a compound wherein Y and/or A1 is optionally substituted indol-3-yl is excluded, a tautomer, a prodrug, a pharmaceutically acceptable salt or a hydrate thereof has an inhibitory activity against an integrase.Type: GrantFiled: June 18, 2003Date of Patent: August 29, 2006Assignee: Shionogi & Co., Ltd.Inventors: Toshio Fujishita, Tomokazu Yoshinaga, Akihiko Sato
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Patent number: 6855835Abstract: Allomorph of Z isomer of N-[2-[[[5-(dimethylamino)methyl-2-furanyl]methyl]thio]ethyl]-N?-methyl-2-nitro-1,1-ethenediamine hydrochloride, with two carbon atoms linked by a rigid ethylenic bond, marked by an asterisk (*), characterized by the following structural formula: wherein -Fur- represents a furane ring.Type: GrantFiled: August 29, 2002Date of Patent: February 15, 2005Assignee: Pharmexcel SRLInventor: Paolo Alberto Veronesi
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Patent number: 6747146Abstract: Method of producing compounds of formula wherein R1 is hydrogen or C1-C4-alkyl; R2 is hydrogen, C1-C8-alkyl, C3-C6-cycloalkyl, or a radical —N(R3)R4; or R2 and R6 together are —CH2—CH2—S—; R3 and R4 are hydrogen, C1-C4-alkyl, C3-C6-cycloalkyl or a radical —CH2B; R6 is hydrogen, C1-C8-alkyl, aryl or benzyl; or R3 and R6 together are —CH2—CH2—, —CH2—CH2—CH2—, —CH2—O—CH2—, —CH2—S—CH2— or —CH2—N(R5)—CH2—; X is CH—CN; CH—NO2 or N—NO2; A is an optionally substituted, aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical; and B is optionally substituted phenyl, 3-pyridyl or thiazolyl; characterised in that a compound of formula wherein R2, R6 and X have the same significance as given above in formula (I), is reacted in the presence of a phase transfer catalyst and a base with a compound of fType: GrantFiled: December 20, 2002Date of Patent: June 8, 2004Assignee: Syngenta Crop Protection, Inc.Inventors: Gottfried Seifert, Thomas Rapold, Verena Gisin
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Patent number: 6703425Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof which is useful for the treatment of conditions associated with glutamate hypofunction, such as psychiatric and neurological disordersType: GrantFiled: November 15, 2002Date of Patent: March 9, 2004Assignee: Eli Lilly and CompanyInventors: James Allen Knobelsdorf, Timothy Alan Shepherd, Eric George Tromiczak, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Patent number: 6677341Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral heteroaryl aminoalcohols.Type: GrantFiled: December 12, 2001Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6596863Abstract: Process for producing a nitroetheneamine derivative or its stereoisomer, its tautomer or a salt thereof comprising reacting a compound of the formula with a compound of the formula R6—CH2NO2 to obtain a compound of the formula and reacting the resulting compound with a compound of the formulaType: GrantFiled: April 29, 2002Date of Patent: July 22, 2003Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Fuminori Kato, Keizo Miyata, Hirohiko Kimura, Kazuhiro Yamamoto, Hiroyuki Ikegami, Hiromi Takeo
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Patent number: 6552086Abstract: The present invention provides certain sulfonamide derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.Type: GrantFiled: January 23, 2001Date of Patent: April 22, 2003Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, Paul Leslie Ornstein, Edward C. R. Smith, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Publication number: 20030055271Abstract: Alcohols are catalytically oxidized to aldehydes, in particular to benzaldehyde and diformylfuran, which are useful as intermediates for a multiplicity of purposes. The invention also relates to the polymerization of the dialdehyde and to the decarbonylation of the dialdehyde to furan.Type: ApplicationFiled: August 14, 2002Publication date: March 20, 2003Inventors: Vladimir Grushin, Walter Partenheimer, Leo E. Manzer
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Patent number: 6528651Abstract: The present invention relates to a process for the preparation of compounds of the formula (I) by reacting compounds of the formula (II) in which Het, R1, R2 and R4 are as defined in the description, with anhydrous hydrogen chloride or compounds which generate hydrogen chloride.Type: GrantFiled: June 14, 2002Date of Patent: March 4, 2003Assignee: Bayer AktiengesellschaftInventors: Kai van Laak, Wolfram Sirges, Detlef Wollweber
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Patent number: 6451792Abstract: A medical composition containing, as an active constituent, a nitroetheneamine derivative represented by the formula (I): wherein the substituents are as defined in the disclosure, its stereoisomers, its tautomers or a salt thereof.Type: GrantFiled: March 20, 2001Date of Patent: September 17, 2002Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Fuminori Kato, Keizo Miyata, Hirohiko Kimura, Kazuhiro Yamamoto, Hiroyuki Ikegami, Hiromi Takeo
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Patent number: 6444840Abstract: The invention provides novel prostaglandin analogs. In particular, the present invention relates to compounds having a structure according to formula (I) wherein R1, R2, R3, R4, R5, R6, W, X, Z, a, b, p and q are defined below. This invention also includes optical isomers, diastereomers and enantiomers of formula (I), and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using these compounds or the compositions containing them.Type: GrantFiled: September 28, 2000Date of Patent: September 3, 2002Assignee: The Procter & Gamble Co.Inventors: Mitchell Anthony deLong, Jack Snyder Amburgey, Jr., John August Wos, Biswanath De, David Lindsey Soper
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Patent number: 6410780Abstract: The invention provides novel prostaglandin analogs. In particular, the present invention relates to compounds having a structure according to formula (I) wherein R1, R2, R3, R4, R5, R6, W, X, Z, a, b, p and q are defined below. This invention also includes optical isomers, diastereomers and enantiomers of formula (I), and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using these compounds or the compositions containing them.Type: GrantFiled: September 28, 2000Date of Patent: June 25, 2002Assignee: The Procter & Gamble Co.Inventors: Mitchell Anthony deLong, Jack Snyder Amburgey, Jr., John August Wos, Biswanath De, David Lindsey Soper
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Patent number: 6380429Abstract: Disclosed is a process for the oxidation of sulfonamides to sulfonyl imines using chromium (IV) dioxide as the oxidant.Type: GrantFiled: September 15, 2000Date of Patent: April 30, 2002Assignee: E. I. du Pont Nemours and CompanyInventor: Eric Maurice Smith
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Patent number: 6359156Abstract: The invention relates to compounds having usefulness in the control of Take-All disease in plants, particularly cereals, a method for the control of Take-All disease, and fungicidal compositions for carrying out the method. Compounds of the invention are oximes or hydrazones of arylgloxamides or heteroarylglyoxamides or cycloalkenylglyoxamides.Type: GrantFiled: August 21, 2001Date of Patent: March 19, 2002Assignee: Monsanto Technology LLCInventor: Dennis P. Phillion
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Patent number: 6358981Abstract: The present invention relates to the potentiation of glutamate receptor function using certain sulphonamide derivatives. It also relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.Type: GrantFiled: January 23, 2001Date of Patent: March 19, 2002Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, David Michael Bender, Andrew Hendley Fray, Winton Dennis Jones, Paul Leslie Ornstein, Richard Lee Simon, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Patent number: 6342633Abstract: Compounds of the formula I in which Y is hydrogen, C1-C4alkyl, C1-C4alkoxy, OH, CN, NO2, Si(CH3)3, CF3 or halogen, Z is a group a) R1 is hydrogen, C1-C4alkyl, C2-C4alkenyl, C2-C4alkynyl, C3-C6cycloalkyl, phenyl which is unsubstituted or at most trisubstituted by halogen, C1-C4alkyl, C1-C4alkoxy, C1-C4alkylthio, or benzyl which is unsubstituted or at most trisubstituted in the aromatic ring in the same manner, or is cyclopropylmethyl, C1-C4haloalkyl, C2-C5alkoxyalkyl, cyanomethyl, CO—R6, OH, NH2, C1-C4alkylamine or C1-C4alkoxycarbonyl-C1-C2alkyl; X is oxygen, sulfur or NR5; R2 is hydrogen, C1-C4alkyl, C2-C4alkenyl, C2-C4alkynyl, C3-C6cycloalkyl, C(O)R6, OH or C1-C4alkoxy, NH2 or C1-C4alkylamine; R5 is hydrogen, C1-C4alkyl, C2-C4alkenyl or C2-C4alkynyl; R6 is hydrogen, C114 C4alkyl, C1-C4haloalkyl, C1-C4alkoxy, C3-C6cycloalkyl, C1-C4alkoxycarbonyl or phenyl which is unsubstituted or at most trisubstituted; and in which R3 and R4 independently of one another are hyType: GrantFiled: September 27, 2000Date of Patent: January 29, 2002Assignee: Bayer AktiengesellschaftInventor: René Zurflüh
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Patent number: 6255340Abstract: A pesticidal composition comprising prallethrin and a neonicotinoid compound given in the following formula (1), (2) or (3), as an active ingredient wherein, A represents a 6-chloro-3-pyridyl, 2-chloro-5-thiazolyl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, 5-methyltetrahydrofuran-3-yl, 3-pyridyl, 6-bromo-3-pyridyl, 3-cyanophenyl, 2-methyl-5-thiazolyl, 2-phenyl-5-thiazolyl or 2-bromo-5-thiazolyl group; R1 represents a hydrogen atom, methyl, ethyl, formyl or acetyl group; R2 represents a methyl, amino, methylamino, N,N-dimethylamino, ethylamino, N,N-diethylamino, N-methyl-N-ethylamino, 1-pyrrolidinyl, (6-chloro-3-pyridyl) methylamino or N-methyl-N-(6-chloro-3-pyridyl)methylamino group; R3 represents a methyl, ethyl, propyl, propenyl or propynyl group; X represents a nitrogen atom or CH group; Y represents a cyano, nitro or trifluoroacetyl group; Z represents a NH group or sulfur atom; D represents an oxygen atom or —N(CH3)— group; m represents 0 or 1; and n represents 2 or 3, hasType: GrantFiled: April 7, 1999Date of Patent: July 3, 2001Assignee: Sumitomo Chemical Company, LimitedInventor: Izumi Fujimoto
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Patent number: 6211240Abstract: Compounds of the formula I in which Y is hydrogen, C1-C4alkyl, C1-C4alkoxy, OH, CN, NO2, Si(CH3)3, CF3 or halogen, Z is a group a) R1 is hydrogen, C1-C4alkyl, C2-C4alkenyl, C2-C4-alkynyl, C3-C6cycloalkyl, phenyl which is unsubstituted or at most trisubstituted by halogen, C1-C4alkyl, C1-C4alkoxy, C1-C4alkylthio, or benzyl which is unsubstituted or at most trisubstituted in the aromatic ring in the same manner; or is cyclopropylmethyl, C1-C4haloalkyl, C2-C5alkoxyalkyl, cyanomethyl, CO—R6, OH, NH2, C1-C4alkylamine or C1-C4alkoxycarbonyl-C1-C2alkyl; X is oxygen, sulfur or NR5; R2 is hydrogen, C1-C4alkyl, C2-C4alkenyl, C2-C4alkynyl, C3-C6cycloalkyl, C(O)R6, OH or C1-C4alkoxy, NH2 or C1-C4alkylamine; R5 is hydrogen, C1-C4alkyl, C2-C4alkenyl or C2-C4alkynyl; R6 is hydrogen, C114 C4alkyl, C1-C4haloalkyl, C1-C4alkoxy, C3-C6cycloalkyl, C1-C4alkoxycarbonyl or phenyl which is unsubstituted or at most trisubstituted; and in which R3 and R4 independently of one another are hType: GrantFiled: October 29, 1996Date of Patent: April 3, 2001Assignee: Novartis CorporationInventor: René Zurflüh
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Patent number: 6200353Abstract: Couplers for hair coloring compositions for oxidative dyeing of hair are compounds of the formula at least one coupler comprising a compound of the formula: wherein R is selected from the group consisting of C1 to C2 alkyl and hydroxyethyl, R1 is selected from the group consisting of hydrogen, chlorine, bromine, C1 to C3 alkyl, C1 to C3 alkoxy, C1 to C3 hydroxyalkyl and C1 to C3 hydroxyalkoxy, and X is O, S or NH.Type: GrantFiled: February 1, 2000Date of Patent: March 13, 2001Assignee: Bristol Myers Squibb CompanyInventors: Mu-Ill Lim, Linas R. Stasaitis, Yuh-Guo Pan
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Patent number: 6187944Abstract: Acrylonitrile compounds having pesticidal activity of formula (I) and salts thereof. wherein Q is Y is ═C(R4)— or ═N—, R1 is alkyl, haloalkyl, etc., each of R2 and R3 is halogen, alkyl which may be substituted, alkenyl which may be substituted, etc., R4 is hydrogen, halogen, alkyl or haloalkyl, 1 is from 1 to 4, m is from 0 to 5, n is from 0 to 3, q is from 0 to 4, when 1 is 2 or more, a plurality of R2 may be the same or different, when each of m, n and q is 2 or more, a plurality of R3 may be the same or different.Type: GrantFiled: August 16, 1999Date of Patent: February 13, 2001Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Toru Koyanagi, Yuji Nakamura, Masayuki Morita, Koji Sugimoto, Tsuyoshi Ikeda, Munekazu Ogawa
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Patent number: 6166003Abstract: A compound comprising a heterocyclic moiety, such as a thiophene, covalently attached to an alkylene isothiocyanate moiety. The compound is effective to prevent the occurrence or progression of cancer or a precancerous condition, and can be used for therapeutic or prophylactic purposes. The compound can be provided and administered in the form of a pharmaceutical composition, a cosmetic, a food additive, supplement, or the like. Methods for synthesis and use of the chemopreventive compound of the invention are also provided.Type: GrantFiled: February 17, 1999Date of Patent: December 26, 2000Assignee: LKT Laboratories, Inc.Inventor: Luke K. T. Lam
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Patent number: 6143790Abstract: There is disclosed a novel amino glycol derivatives of L-N.sup.6 -(1-iminoethyl)lysine, pharmaceutical compositions containing these novel compounds, and to their use in therapy, in particular their use as nitric oxide synthase inhibitors.Type: GrantFiled: September 6, 1996Date of Patent: November 7, 2000Assignee: G.D. Searle & Co.Inventors: E. Ann Hallinan, Foe S. Tjoeng, Kam F. Fok, Timothy J. Hagen, Mihaly V. Toth, Sofya Tsymbalov, Barnett S. Pitzele
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Patent number: 6124466Abstract: A novel nitroisourea derivative and a process for producing the same, which is an important intermediate for the production of a nitroguanidine derivative having an insecticidal activity, and a process for producing a nitroguanidine derivative having an insecticidal activity using the nitroisourea derivative. The process for producing a nitroguanidine derivative represented by formula (1), effective as an insecticide is shown by reaction scheme (2): ##STR1## wherein R.sub.1 represents an alkyl group having from 1 to 4 carbon atoms or a benzyl group; R.sub.2 represents an alkyl group having from 1 to 4 carbon atoms; R.sub.3, R.sub.4, R.sub.5 and R.sub.6 each independently represents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms; and Q represents a 5-membered or 6-membered heterocyclic ring having at least one of the following: a nitrogen atom, an oxygen atom or a sulfur atom, one of the hydrogen atoms being substitutable with a halogen atom.Type: GrantFiled: July 19, 1999Date of Patent: September 26, 2000Assignee: Mitsui Chemicals, Inc.Inventors: Hirozumi Matsuno, Kiyoshi Arai, Takeshi Oura, Kenji Kodaka
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Patent number: 6124356Abstract: A fungicidal compound of formula (I): or a stereoisomer thereof, wherein A is CH or N, B is OCH.sub.3 or NHCH.sub.3, E is --NR.sup.1 --C(CH.sub.3).dbd.N-- or --N.dbd.C(CH.sub.3)--NR.sup.1 --, R.sup.1 is H, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl or optionally substitute benzyl, R.sup.2 is H, C.sub.1-4 alkyl, halo(C.sub.1-4)alkyl, C.sub.3-6 cycloalkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl, and R.sup.3 is optionally substituted aryl or optionally substituted heterocyclyl.Type: GrantFiled: January 6, 1999Date of Patent: September 26, 2000Assignee: Zeneca LimitedInventors: George Tseriotis, Ian Henry Aspinall, Paul Anthony Worthington
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Patent number: 6100253Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the present description, or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.Type: GrantFiled: August 17, 1999Date of Patent: August 8, 2000Assignee: Novo Nordisk A/SInventors: Knud Erik Andersen, Tine Krogh J.o slashed.rgensen, Rolf Hohlweg, Erik Fischer, Uffe Bang Olsen, Zdenek Polivka, Karel Sindelar, Vladimir Valenta