Three-membered Ring In Substituent Q Patents (Class 564/190)
  • Publication number: 20140357722
    Abstract: Provided herein are compounds and pharmaceutical compositions for use in the treatment of neuropathic pain and the neuropathic pain syndromes.
    Type: Application
    Filed: July 10, 2014
    Publication date: December 4, 2014
    Inventors: Birgit Hasse, Guido Koopmans
  • Publication number: 20140343108
    Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and specifically relates to novel amidated derivatives of oleanolic acid according to formula (I) or a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments.
    Type: Application
    Filed: November 30, 2012
    Publication date: November 20, 2014
    Inventors: Frank Rong, Rongzhen Xu, Fuwen Xie, Hongxi Lai
  • Patent number: 8835472
    Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: August 17, 2011
    Date of Patent: September 16, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Gerald Juergen Roth, Martin Fleck, Niklas Heine, Joerg Kley, Thorsten Lehmann-Lintz, Heike Neubauer, Bernd Nosse
  • Patent number: 8779003
    Abstract: Disclosed herein is a method for prolonging analgesic effect of a membrane permeable local anesthetic in a subject in need thereof. The method uses cinnamaldehyde as an adjuvant which, when administered prior to or simultaneously with the administration of a local anesthetic, prolongs the analgesic effect of the local anesthetic. Also disclosed herein is a method for providing analgesic effect in a subject in need thereof. The method uses cinnamaldehyde as an analgesic compound which, when administered alone to the subject in an analgesically effective amount, provides the analgesic effect.
    Type: Grant
    Filed: December 29, 2011
    Date of Patent: July 15, 2014
    Assignee: Mackay Memorial Hospital
    Inventor: Yu-Chun Hung
  • Publication number: 20140171315
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Publication number: 20140142337
    Abstract: The present invention relates to 1-amino-2-vinylcyclopropane carboxylic acid amide or a salt thereof. By obtaining optically active 1-amino-2-vinylcyclopropane carboxylic acid amide or a salt thereof by hydrolyzing optically active 1-amino-2-vinylcyclopropane carbonitrile or a salt thereof according to the production method of the present invention, 1-amino-2-vinylcyclopropane carboxylic acid amide or a salt thereof, which is useful as a pharmaceutical/agrochemical intermediate, can be easily obtained. The present invention is capable of providing a substrate to be subjected to optical resolution, which enables the production of optically active 1-amino-2-vinylcyclopropane carboxylic acid, which is widely used as a raw material for pharmaceutical and agrochemical products and is especially important as an intermediate for therapeutic agents for hepatitis C, inexpensively with high purity and high yield.
    Type: Application
    Filed: June 18, 2012
    Publication date: May 22, 2014
    Applicant: MITSUBISHI GAS CHEMICAL COMPANY, INC.
    Inventor: Masahiro Matsumoto
  • Publication number: 20140127709
    Abstract: A method of determining the presence or absence in a sample of a biomarker, the method comprising: (a) linking an antigen to colloidal gold to provide a gold-antigen species; (b) contacting the gold-antigen species with the sample; (c) adding a diagnosis agent to the sample; and (d) observing the colour of the sample.
    Type: Application
    Filed: May 4, 2012
    Publication date: May 8, 2014
    Applicant: Bangor University
    Inventors: Christopher David Gwenin, Mark Stephen Baird, Vanessa Valerie Gwenin, Mark Pitts
  • Publication number: 20140121217
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein A, Y, L, R1, W1 and W2 are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: January 2, 2014
    Publication date: May 1, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Lijun Sun, Jun Jiang, Yu Xie
  • Patent number: 8604241
    Abstract: The present invention relates to a method for synthesizing a pharmaceutically acceptable acid addition salt of (1S, 2R)-milnacipran comprising the following successive steps: (a) reaction of phenylacetonitrile and of (R)-epichlorhydrin in the presence of a base containing an alkaline metal, followed by a basic treatment, and then by an acid treatment in order to obtain a lactone; (b) reaction of said lactone with MNEt2, wherein M represents an alkaline metal, or with NHEt2 in the presence of a Lewis acid-amine complex, in order to obtain an amide-alcohol; (c) reaction of said amide-alcohol with thionyl chloride in order to obtain a chlorinated amide; (d) reaction of said chlorinated amide with a phthalimide salt in order to obtain a phthalimide derivative; (e) hydrolysis of the phthalimide group of said phthalimide derivative in order to obtain (1S, 2R)-milnacipran, and (f) salification of (1S, 2R)-milnacipran in a suitable solvent system in the presence of a pharmaceutically acceptable acid.
    Type: Grant
    Filed: January 29, 2010
    Date of Patent: December 10, 2013
    Assignee: Pierre Fabre Medicament
    Inventors: Marc Nicolas, Paul Hellier, Catherine Diard, Laurent Subra
  • Patent number: 8518979
    Abstract: Novel Alpha-halo- and Alpha-alkyl-cyclopropylcarboxy compounds, and uses of these and related compounds in the treatment of a variety of neurological diseases and disorders, and particularly epilepsy, are provided.
    Type: Grant
    Filed: February 19, 2008
    Date of Patent: August 27, 2013
    Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.
    Inventors: Meir Bialer, Boris Yagen, Neta Pessah
  • Publication number: 20130184279
    Abstract: Compounds of formula Ia and Ib wherein A, B, C, R1 and R14 are described herein.
    Type: Application
    Filed: December 18, 2012
    Publication date: July 18, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • Patent number: 8481598
    Abstract: The present invention relates to stable dosage forms of levomilnacipran and pharmaceutically acceptable salts thereof. Processes for the preparation of these dosage forms and methods of using these dosage forms are also described.
    Type: Grant
    Filed: January 14, 2011
    Date of Patent: July 9, 2013
    Inventors: Rahul Surana, Murali Divi, Anil Chhettry
  • Publication number: 20130123505
    Abstract: A carboxamide can be produced in a high yield by a method for producing a carboxamide, for example, represented by formula (4): (wherein R1 and R3 are as defined below), the method comprising a step of allowing a carboxylic acid ester represented by formula (1): (wherein R1 represents an optionally substituented C1-C20 hydrocarbon group or an optionally substituented C3-C20 heterocyclic group, and R2 represents an optionally substituented C1-C20 hydrocarbon group), an amine represented by formula (2): R3—NH2 ??(2) (wherein R3 represents a hydrogen atom or an optionally substituented C1-C20 hydrocarbon group), and a formamide compound represented by formula (3): (wherein R3 is as defined above) to react in the presence of a metal alkoxide.
    Type: Application
    Filed: July 13, 2011
    Publication date: May 16, 2013
    Inventors: Junichi Tomokawa, Takahiro Kimura, Norihiko Hirata
  • Patent number: 8426643
    Abstract: The present invention provides synthetic routes for preparing various isomers of cyclohexane-based coolants, such as menthyl esters and menthanecarboxamide derivatives, in particular those substituted at the amide nitrogen, for example with an aromatic ring or aryl moiety. Such structures have high cooling potency and long lasting sensory effect, which make them useful in a wide variety of consumer products. One synthetic route involves a copper catalyzed coupling of a primary menthanecarboxamide with an aryl halide, such reaction working best in the presence of potassium phosphate and water. Using this synthetic route, specific isomers can be prepared including the menthanecarboxamide isomer having the same configuration as l-menthol and new isomers such as a neoisomer having opposite stereochemistry at the carboxamide (C-1) position. The neoisomer unexpectedly has potent and long lasting cooling effect.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: April 23, 2013
    Assignee: The Procter & Gamble Company
    Inventors: Kenneth Edward Yelm, Gregory Mark Bunke, John Christian Haught
  • Patent number: 8314270
    Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.
    Type: Grant
    Filed: September 9, 2010
    Date of Patent: November 20, 2012
    Assignee: Abbott Laboratories
    Inventors: James T. Link, Qi Shuai, Martin Winn, Hong Yong
  • Publication number: 20120214858
    Abstract: Imidamide (amidine) analogs that can inhibit the activity of sphingosine kinase 1 and sphingosine kinase 2 (SphK1 & SphK2) are provided. The compounds can prevent angiogenesis in tumors.
    Type: Application
    Filed: August 16, 2010
    Publication date: August 23, 2012
    Applicant: University of Virginia Patent Foundation
    Inventors: Kevin R. Lynch, Timothy L. Macdonald, Thomas P. Mathews, Andrew Kennedy, Yugesh Kharel
  • Patent number: 8222454
    Abstract: The present invention discloses a process for preparing optically pure milnacipran and their pharmaceutically acceptable salts, which adopts racemic milnacipran as starting material, tartaric acid derivatives and their compositions as resolving agents to resolve.
    Type: Grant
    Filed: November 28, 2007
    Date of Patent: July 17, 2012
    Assignee: Zhejiang Haisen Pharmaceutical Co., Ltd.
    Inventors: Lin Ai, Xiao Liu
  • Patent number: 8026396
    Abstract: This invention relates to processes for the production of optically active 2-(disubstituted aryl)cyclopropylamine compounds and optically active 2-(disubstituted aryl)cyclopropane carboxamide compounds which are useful intermediates for the preparation of pharmaceutical agents, and in particular the compound [1S-(1?,2?,3?(1S*,2R*),5?)]-3-[7-[2-(3,4-difluorophenyl)-cyclopropyl]amino]-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)-cyclopentane-1,2-diol.
    Type: Grant
    Filed: August 11, 2010
    Date of Patent: September 27, 2011
    Assignee: AstraZeneca AB
    Inventors: Masaru Mitsuda, Tadashi Moroshima, Kentaro Tsukuya, Kazuhiko Watabe, Masahiko Yamada
  • Patent number: 7947852
    Abstract: Compounds of formula (I): wherein: R1 represents alkyl, alkenyl, haloalkyl, polyhaloalkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl, X represents a group N—OR2 wherein R2 represents a hydrogen atom or an alkyl group. Medicinal products containing the same which are useful in treating disorders of the melatoninergic system.
    Type: Grant
    Filed: July 1, 2008
    Date of Patent: May 24, 2011
    Assignee: Les Laboratoires Servier
    Inventors: Said Yous, Mohamed Ettaoussi, Ahmed Sabaouni, Pascal Berthelot, Michael Spedding, Philippe Delagrange, Daniel-Henri Caignard, Mark Millan
  • Patent number: 7919133
    Abstract: The present invention relates to the use of a compound of formula (I) or a mixture of compounds of formula (I) wherein: R1, R2, and R3 are independently H or an alkyl group having 1 to 3 C-atom, wherein at least one of R1, R2, and R3 is not H; R4 is H, an alkyl group having 1 to 6 C-atom, or an alkenyl group having 2 to 6 C-atom; R5, R6, R7, and R8 are independently H or methyl; and R9 is H, an alkyl group having 5 to 12 C-atoms, or an alkenyl group having 5 to 12 C-atoms; as a flavoring substance or mixture of flavoring substances.
    Type: Grant
    Filed: May 8, 2008
    Date of Patent: April 5, 2011
    Assignee: SYMRISE GmbH & Co. KG
    Inventors: Jan Looft, Tobias Vössing, Jakob Ley, Michael Backes, Maria Blings
  • Publication number: 20110034461
    Abstract: The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R9, Ar, Q1, Q2 and Q3 are each as defined below. The compounds of the formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of the formula I and to the use thereof as a medicament.
    Type: Application
    Filed: August 5, 2010
    Publication date: February 10, 2011
    Applicant: sanofi-aventis
    Inventors: Uwe HEINELT, Volkmar WEHNER, Matthias HERRMANN, Karl SCHOENAFINGER, Henning STEINHAGEN
  • Publication number: 20100152254
    Abstract: Novel Alpha-halo- and Alpha-alkyl-cyclopropylcarboxy compounds, and uses of these and related compounds in the treatment of a variety of neurological diseases and disorders, and particularly epilepsy, are provided.
    Type: Application
    Filed: February 19, 2008
    Publication date: June 17, 2010
    Applicant: Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.
    Inventors: Meir Bialer, Boris Yagen, Neta Pessah
  • Patent number: 7728171
    Abstract: A process for the preparation of acid halides of formula I which are useful as intermediates in the preparation of i.a. pharmaceutically active compounds.
    Type: Grant
    Filed: August 25, 2008
    Date of Patent: June 1, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ursula Hoffmann, Goesta Rimmler
  • Publication number: 20100029612
    Abstract: The present invention provides a combinatorial approach to a library of novel compounds having four diversity points. The compounds provide for the mapping of urotensin II and somatostatin 5 receptors by differential binding of said receptors. The present invention further relates to a method of treating diseases for which modulation of the urotensin II receptor produces a physiologically beneficial response in said disease, such as those associated with CNS function and cardiovascular diseases. The present invention further relates to pharmaceutical compositions comprising these agents for the treatment of these diseases adapted to modulate the urotensin II receptor.
    Type: Application
    Filed: February 18, 2004
    Publication date: February 4, 2010
    Inventor: Roger Olsson
  • Publication number: 20100010220
    Abstract: The present invention relates to a novel process for preparing amidrazones of the formula (I) wherein R, R1, R2, A, B, W, Y and n have the meanings as indicated in the description. Further, the invention relates to novel compounds used as intermediates in this process and to processes for their preparation.
    Type: Application
    Filed: July 25, 2007
    Publication date: January 14, 2010
    Applicant: BASF SE
    Inventors: Thomas Zierke, Christopher Koradin
  • Patent number: 7632972
    Abstract: Compounds and related methods for synthesis, and the use of compounds and combination therapies for the treatment of cancer and modulation of apoptosis in cells are disclosed. The generation of synthetic combinatorial libraries and the evaluation of library member compounds regarding induction of apoptosis selectively in cancer cells are disclosed. Compounds, methods of making the compounds, and therapeutic methods with application against breast cancer cells, melanoma cancer cells, colon cancer cells, and other cancer cells are described.
    Type: Grant
    Filed: October 27, 2004
    Date of Patent: December 15, 2009
    Assignee: The Board of Trustees of the University of Illionis
    Inventors: Paul J. Hergenrother, Vitaliy Nesterenko, Karson Putt, Brittany Joy Allen, Robin Shane Dothager, Benjamin James Leslie
  • Patent number: 7612237
    Abstract: The present invention is directed to a process for preparing ?-amino-?-hydroxycarboxamides. The process works with epoxycarboxamides of the formula 2 which are reacted with ammonia or other amines.
    Type: Grant
    Filed: June 29, 2007
    Date of Patent: November 3, 2009
    Assignee: Degussa GmbH
    Inventor: Günter Knaup
  • Patent number: 7601870
    Abstract: The present invention relates to aniline derivatives of the general formula I or salts thereof, described therein, and their use.
    Type: Grant
    Filed: December 20, 2005
    Date of Patent: October 13, 2009
    Assignee: H. Lundbeck A/S
    Inventors: Christian Wenzel Tornøe, Mario Rottländer, Daniel Rodriguez Greve, Nikolay Khanzhin, Andreas Ritzén, William Patrick Watson
  • Patent number: 7524885
    Abstract: The invention provides novel compounds of the Formula (I) that stimulate rates of glucose oxidation in myocardial cells: wherein W, Cyc, p, Y, X, Z, R, R1, R2, R3, R4, I, m and n are as defined for Formula (I) herein. The invention also relates to pharmaceutical compositions comprising compounds capable of stimulation of glucose oxidation, methods for increasing glucose oxidation rates in myocardial cells, and methods of treatment of myocardial ischemia.
    Type: Grant
    Filed: February 23, 2005
    Date of Patent: April 28, 2009
    Assignee: The Governors of the University of Alberta
    Inventors: Gary D. Lopaschuk, John C Vederas, Jason R. Dyck
  • Patent number: 7511175
    Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.
    Type: Grant
    Filed: January 5, 2006
    Date of Patent: March 31, 2009
    Assignee: Abbott Laboratories
    Inventors: Jyoti R. Patel, Qi Shuai, James T. Link, Jeffrey J. Rohde, Jurgen Dinges, Bryan K. Sorensen, Martin Winn, Hong Yong, Peer B. Jacobson, Michael E. Brune
  • Patent number: 7459585
    Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: March 24, 2005
    Date of Patent: December 2, 2008
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yukio Iino, Kohichi Fujita, Takashi Tsuji, Ariko Kodaira, Kenji Takehana, Tsuyoshi Kobayashi, Takashi Yamamoto
  • Publication number: 20080292763
    Abstract: The present invention relates to the use of a compound of formula (I) or a mixture of compounds of formula (I) wherein: R1, R2, and R3 are independently H or an alkyl group having 1 to 3 C-atom, wherein at least one of R1, R2, and R3 is not H; R4 is H, an alkyl group having 1 to 6 C-atom, or an alkenyl group having 2 to 6 C-atom; R5, R6, R7, and R8 are independently H or methyl; and R9 is H, an alkyl group having 5 to 12 C-atoms, or an alkenyl group having 5 to 12 C-atoms; as a flavoring substance or mixture of flavoring substances.
    Type: Application
    Filed: May 8, 2008
    Publication date: November 27, 2008
    Applicant: SYMRISE GmbH & Co. KG
    Inventors: Jan Looft, Tobias Vossing, Jakob Ley, Michael Backes, Maria Blings
  • Patent number: 7435849
    Abstract: A process for the preparation of acid halides of formula I which are useful as intermediates in the preparation of i.a. pharmaceutically active compounds.
    Type: Grant
    Filed: October 17, 2006
    Date of Patent: October 14, 2008
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ursula Hoffmann, Goesta Rimmler
  • Patent number: 7038085
    Abstract: The present invention relates generally to the enantiomers of para-hydroxy-milnacipran or congeners thereof. Biological assays revealed that racemic para-hydroxy-milnacipran is approximately equipotent in inhibiting serotonin and norepinephrine uptake (IC50=28.6 nM for norepinephrine, IC50=21.7 nM for serotonin). Interestingly, (+)-para-hydroxy-milnacipran is a more potent inhibitor of norepinephrine uptake than serotonin uptake (IC50=10.3 nM for norepinephrine, IC50=22 nM for serotonin). In contrast, (?)-para-hydroxy-milnacipran is a more potent inhibitor of serotonin uptake compared to norepinephrin uptake (IC50=88.5 nM for norepinephrine, IC50=40.3 nM for serotonin). The invention also relates to salts and prodrug forms of the aforementioned compounds. In certain embodiments, the compounds of the present invention and a pharmaceutically acceptable excipient are combined to prepare a formulation for administration to a patient.
    Type: Grant
    Filed: October 22, 2003
    Date of Patent: May 2, 2006
    Assignee: Collegium Pharmaceutical, Inc.
    Inventors: Roman V. Rariy, Michael Heffernan, Stephen L. Buchwald, Timothy M. Swager
  • Patent number: 7015349
    Abstract: Compositions including a conjugate of ?-difluoromethylornithine can be applied topically to reduce hair growth.
    Type: Grant
    Filed: March 26, 2003
    Date of Patent: March 21, 2006
    Assignee: The Gillette Company
    Inventors: Anwar Jardien, Roman Rariy, Gurpreet S. Ahluwalia, Douglas Shander
  • Patent number: 6992220
    Abstract: In one embodiment, the present application relates to a process of making a compound of formula I: and to certain intermediate compounds that are made within the process of making the compound of formula I.
    Type: Grant
    Filed: June 15, 2004
    Date of Patent: January 31, 2006
    Assignee: Schering Corporation
    Inventors: Minzhang Chen, Michael D. Green, Fucheng Zhang
  • Patent number: 6960687
    Abstract: New derivatives of N-Hydroxyalkyl-tetramethylcyclopropane carboxamide, pharmaceutical compositions thereof, methods for their preparation, and use thereof for the treatment of epilepsy, neurological, affective and psychotic disorders and for the treatment of pain and migraine.
    Type: Grant
    Filed: December 29, 2002
    Date of Patent: November 1, 2005
    Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem
    Inventors: Meir Bialer, Nina Isoherranen, Boris Yagen
  • Patent number: 6703379
    Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: March 12, 2001
    Date of Patent: March 9, 2004
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yukio Iino, Kohichi Fujita, Takashi Tsuji, Ariko Kodaira, Kenji Takehana, Tsuyoshi Kobayashi, Takashi Yamamoto
  • Patent number: 6683212
    Abstract: Compounds of Formula (I) are disclosed which are useful as fungicides wherein R1 is hydrogen; halogen; C1-C2 alkoxy; C1-C2 haloalkoxy, cyano; or C1-C2 alkyl optionally substituted with halogen, C1-C2 alkoxy or cyano; R2 is hydrogen; halogen; or C1-C4 alkyl optionally substituted with halogen, C1-C2 alkoxy or cyano; R3 is hydrogen; halogen; C1-C4 alkoxy; C1-C4 haloalkoxy; or C1-C4 alkyl optionally substituted with halogen, C1-C2 alkoxy or cyano; or R2 and R3 can be taken together as —CH2CH2—; R4 is C1-C2 alkyl; R5 is R6, CH(R8)OR6, CH(R8)CH(R7)R6 or C(R8)═C(R7)R6; and R6, R7 and R8 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (I) and a method for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound of Formula (I).
    Type: Grant
    Filed: February 20, 2001
    Date of Patent: January 27, 2004
    Inventors: Gregory S. Basarab, Lee Dalton Jennings, Dennis R. Rayner
  • Publication number: 20040002521
    Abstract: The present invention provides an NF-kappa B activation inhibitor, an inflammatory cytokine production inhibitor, a matrix metalloprotease production inhibitor, an inflammatory cell adhesion factor expression inhibitor, and an anti-inflammatory agent, an antirheumatic agent, an immuno-suppressive agent, an antiallergic agent, an antiviral agent, or a therapeutic agent for arteriosclerosis, which comprise, as the active ingredient, a cyclopropanecarboxylic acid amide compound or a pharmaceutically acceptable salt thereof effective for the treatment of inflammatory diseases.
    Type: Application
    Filed: April 30, 2003
    Publication date: January 1, 2004
    Applicant: AJINOMOTO CO. INC
    Inventors: Yukio Iino, Takashi Yamamoto, Tsuyoshi Kobayashi
  • Publication number: 20030191182
    Abstract: The invention provides novel compounds of the Formula (I) that stimulate rates of glucose oxidation in myocardial cells.
    Type: Application
    Filed: April 9, 2003
    Publication date: October 9, 2003
    Inventors: Gary David Lopaschuk, John Christopher Vederas, Jason R Dyck
  • Patent number: 6596898
    Abstract: A process for preparing compounds represented by the following general formula (I) wherein X represents chlorine atom, bromine atom, or iodine atom, and R includes alkoxy group and amino group which comprises the step of allowing a compound represented by the formula: CH2═CXF react with a compound represented by the formula: N2CHCOR in the presence of a catalyst containing a metal atom such as a transition metal of group 8 together with chiral carboxylic-type or amide-type ligands to preferentially obtain a stereoisomer of the compound of the general formula (I) wherein the stereochemical configuration at the 1-position is S-configuration
    Type: Grant
    Filed: February 27, 1998
    Date of Patent: July 22, 2003
    Assignees: Daiichi Pharmaceutical Co., Ltd., Sumitomo Chemical Co., Ltd.
    Inventors: Tsutomu Ebata, Toshifumi Akiba, Takanobu Ikeya, Ryuhei Wakita, Mikio Sasaki
  • Patent number: 6576792
    Abstract: The invention relates to a 2-halo-1-cycloalkenecarboxamides represented by Formula I: wherein n is 1 or 2; R is hydrogen or an alkyl group; and X is a halogen.
    Type: Grant
    Filed: May 4, 2001
    Date of Patent: June 10, 2003
    Assignee: Eastman Kodak Company
    Inventor: Chang-Kyu Kim
  • Patent number: 6552217
    Abstract: Disclosed is a 4-step process for the preparation of alkyl esters of 1-methylcyclopropanecarboxylic acid which comprises the steps of (1) converting &ggr;-butyrolactone to &agr;-methyl-&ggr;-butyrolactone; (2) converting the &agr;-methyl-&ggr;-butyrolactone from step (1) to an alkyl 4-halo-2-methylbutyrate; (3) producing a xylene solution of the alkyl 4-halo-2-methylbutyrate; and (4) contacting the xylene solution of an alkyl 4-halo-2-methylbutyrate from step (3) with an alkali metal alkoxide under conditions of temperature and pressure which causes vaporization of (i) an alkanol as it is formed and (ii) an alkyl 1-methylcyclopropanecarboxylate as it is formed from the alkyl 4-halo-2-methylbutyrate. Also disclosed are processes whereby the alkyl 1-methylcyclopropanecarboxylate, prepared as described above, is converted to 1-methylcyclopropylamine.
    Type: Grant
    Filed: July 2, 2001
    Date of Patent: April 22, 2003
    Assignee: Eastman Chemical Company
    Inventors: John Clark Hubbs, David Carl Attride, Neil Warren Boaz, James Charles Ciula, John Thorton Maddox, Thomas Nabih, William Dell Nottingham, David Chris Spencer
  • Publication number: 20020161053
    Abstract: The present invention discloses biscyclopropanecarboxamide compounds and pharmaceutically acceptable salts thereof; and also NF-kappa B activation inhibitors, Inflammatory cytokine production inhibitors, matrix metalloprotease production inhibitors, inflammatory cell adhesion molecules incidence inhibitors, antiinflammatory agents, antirheumatic agents, immunosuppressive agents, cancerous metastasis inhibitors or antiviral agents each containing such a compound as the active ingredient.
    Type: Application
    Filed: March 1, 2002
    Publication date: October 31, 2002
    Applicant: AJINOMOTO CO. INC.
    Inventors: Yukio Iino, Kohichi Fujita, Takashi Yamamoto, Kenji Takehana, Tsuyoshi Kobayashi
  • Patent number: 6441044
    Abstract: The present invention relates to cycloalkylcarboxamides of formula I where: A is optionally substituted C3-C6-cycloalkyl; Alk is straight-chain or branched C1-C6-alkylene; R1 is optionally substituted C1-C6-alkyl or C2-C6-alkenyl; R2, R3 is hydrogen, or is optionally halogenated C1-C6-alkyl or C2-C6-alkenyl; W is an optionally substituted fused bicyclic ring system having in each case six ring atoms, where one or two carbon ring atoms may be replaced by nitrogen atoms; and their agriculturally useful salts. Furthermore, the invention relates to fungicidal compositions comprising a compound of formula I as crop protection agent.
    Type: Grant
    Filed: February 26, 2001
    Date of Patent: August 27, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Ingo Rose, Frank Wetterich, Karl Eicken, Joachim Rheinheimer, Gisela Lorenz, Eberhard Ammermann, Thomas Grote, Siegfried Strathmann
  • Patent number: 6426365
    Abstract: The present invention provides a CETP activity inhibitor comprising as an active ingredient a compound represented by the formula (I): wherein R represents a straight chain or branched alkyl group; a straight chain or branched alkenyl group; a lower haloalkyl group; a substituted or unsubstituted cycloalkyl group; a substituted or unsubstituted cycloalkenyl group; a substituted or unsubstituted cycloalkylalkyl group; a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group, X1, X2, X3, and X4 may be the same or different and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower haloalkyl group; a lower alkoxy group; a cyano group; a nitro group; an acyl group; or an aryl group, Y represents —CO— or —SO2—, and Z represents a hydrogen atom or a mercapto-protecting group, or a prodrug compound, a pharmaceutically acceptable salt, or hydrate or solvate thereof.
    Type: Grant
    Filed: December 23, 1999
    Date of Patent: July 30, 2002
    Assignee: Japan Tobacco Inc.
    Inventors: Hisashi Shinkai, Kimiya Maeda, Hiroshi Okamoto
  • Patent number: 6423748
    Abstract: Amido polybiguanides and their use as antimicrobial agents in pharmaceutical compositions are disclosed. A method of synthesis of amido polybiguanides is also disclosed. The amido polybiguanides are useful in the preservation of pharmaceutical compositions, particulary opthalmic and otic pharmaceutical compositions and compositions for treating contact lenses. The compounds are especially useful for disinfecting contact lenses.
    Type: Grant
    Filed: September 19, 2000
    Date of Patent: July 23, 2002
    Assignee: Alcon Manufacturing, Ltd.
    Inventors: Joonsup Park, Nathaniel D. McQueen
  • Patent number: 6362183
    Abstract: An aromatic sulfonyl alpha-hydroxy hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
    Type: Grant
    Filed: June 4, 1999
    Date of Patent: March 26, 2002
    Assignee: G. D. Searle & Company
    Inventors: John N. Freskos, Terri L. Boehm, Brent V. Mischke, Robert M. Heintz, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard
  • Publication number: 20020019422
    Abstract: The present invention relates to novel cycloalkylalkanecarboxamides of the formula I 1
    Type: Application
    Filed: May 31, 2001
    Publication date: February 14, 2002
    Inventors: Frank Wetterich, Karl Eicken, Gisela Lorenz, Eberhard Ammermann, Siegfried Strathmann, Ingo Rose