Morpholine Ring Bonded Directly To The Nitrogen Patents (Class 544/164)
  • Publication number: 20150079035
    Abstract: The present invention provides, inter alia, a compound having the structure: (Formula (I). Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for treating or ameliorating the effects of an excitotoxic disorder in a subject, methods of modulating ferroptosis in a subject, methods of reducing reactive oxygen species (ROS) in a cell, and methods for treating or ameliorating the effects of a neurodegenerative disease.
    Type: Application
    Filed: April 2, 2013
    Publication date: March 19, 2015
    Inventors: Brent R. Stockwell, Scott J. Dixon, Rachid Skouta
  • Publication number: 20140329675
    Abstract: The present specification discloses honeybee repellents exhibiting repellent properties similar to 2-heptanone, compositions comprising such repellents, uses to repel a honeybee from a mammal, location, plant, structure treated of such repellents, and methods of treating a mammal, location, plant, structure by applying such repellents.
    Type: Application
    Filed: May 3, 2014
    Publication date: November 6, 2014
    Applicant: INSCENT, INC.
    Inventors: Daniel F. Woods, Spiros Dimitratos, Robin W. Justice
  • Publication number: 20140256702
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: March 4, 2014
    Publication date: September 11, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Erik Fenster, Melissa Fleury, Adam D. Hughes
  • Patent number: 8785208
    Abstract: The present invention provides fluorogenic compounds for the detection of target metal ions wherein the compounds exhibit a Stokes shift greater than 50 nm and the detectable signal is modulated by photoinduced electron transfer (PET). The present compounds consist of three functional elements, the ion sensing moiety (chelating moiety), the reporter moiety (fluorophore or fluorescent protein) and spacer or linker between the sensing and reporter moieties of the present compound that allows for PET upon binding of a metal ion and excitation by an appropriate wavelength.
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: July 22, 2014
    Assignee: Life Technologies Corporation
    Inventors: Kyle Gee, Vladimir Martin
  • Publication number: 20130196984
    Abstract: The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Application
    Filed: March 13, 2013
    Publication date: August 1, 2013
    Applicants: Siena Biotech S.p.A., Hoffmann-La Roche Inc.
    Inventors: Hoffmann-La Roche Inc., Siena Biotech S.p.A.
  • Publication number: 20120282629
    Abstract: The present invention relates to compounds suitable for modulating huntingtin protein processing and useful for treating or preventing huntingtin-related disorders. The invention provides pharmaceutical compositions comprising said compounds and methods of syntheses thereof.
    Type: Application
    Filed: August 19, 2010
    Publication date: November 8, 2012
    Applicant: MAX-DELBRUCK-CENTRUM FUR MOLEKULARE MEDIZIN
    Inventors: Erich Wanker, Thomas Wiglenda, Julius Tachu Babila, Annett Boddrich, Michael Schmidt, Sandra Neuendorf, Franziska Schiele
  • Patent number: 8138182
    Abstract: The present invention relates to a diketohydrazine derivative of formula (I) and a pharmaceutically acceptable salt thereof (the symbols in the formula have the same meaning as described in the specification). The compound of formula (I) has an inhibitory activity against cysteine protease, and it is useful for the treatment of inflammatory diseases, immune diseases, ischemic diseases, respiratory diseases, circulatory diseases, blood diseases, neuronal diseases, hepatic or biliary diseases, osseous or articular diseases, metabolic diseases, etc. And the compound has inhibitory activity against elastase and it is also useful for the treatment of COPD (chronic obstacle pulmonary diseases).
    Type: Grant
    Filed: September 24, 2009
    Date of Patent: March 20, 2012
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Akira Hatayama, Hiroshi Tsuruta, Yasuo Ochi, Haruo Imawaka, Kazuyuki Ohmoto
  • Patent number: 8088763
    Abstract: Novel cyclohexyl-1,4-diamine compounds corresponding to formula I, processes for the production thereof, pharmaceutical compositions containing these compounds, methods of producing pharmaceutical compositions including these compounds and related methods of treating or inhibiting certain diseases or conditions.
    Type: Grant
    Filed: November 9, 2006
    Date of Patent: January 3, 2012
    Assignee: Gruenenthal GmbH
    Inventors: Corinna Sundermann, Bernd Sundermann
  • Publication number: 20110306560
    Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.
    Type: Application
    Filed: August 19, 2011
    Publication date: December 15, 2011
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Julian Adams, Yu-Tung Ma, Ross Stein, Matthew Baevsky, Louis Grenier, Louis Plamondon
  • Patent number: 8053435
    Abstract: The present invention discloses novel naphthalenyloxypropenyl derivatives useful for inhibiting the enzyme activity of histone deacetylase, leading effective suppression of cancer cell proliferation.
    Type: Grant
    Filed: November 1, 2007
    Date of Patent: November 8, 2011
    Assignees: Korea Research Institute of Chemical Technology, Crystalgenomics, Inc.
    Inventors: Cheol Hae Lee, Hee Jung Jung, Jae Hak Kim, Won Jang Jeong, Joong Myung Cho, Seong Gu Ro, Young Lan Hyun, Cheol Soon Lee, Dongkyu Shin
  • Patent number: 7879999
    Abstract: The invention relates to a method for the synthesis of exocyclic derivatives of cycloalkyl-hydrazines and exocyclic derivatives of heterocycloalkyl-hydrazines The invention is characterised in that the method comprises a step consisting in demixing a solution containing said synthesised derivative, by reacting a heterocyclic amine with monochloramine, in an organic phase and an aqueous phase with the addition of anhydrous sodium hydroxide. According to the invention, the starting amine which has not reacted is collected and reused directly without any additional treatment. The inventive method can also be used to obtain the corresponding exocyclic heterocycloalkyl-hydrazine or cycloalkyl-hydrazinederivative derivative at a low cost compared to that of other known methods.
    Type: Grant
    Filed: December 17, 2004
    Date of Patent: February 1, 2011
    Assignees: Isochem, Centre National de la Recherche Scientifique (CNRS), Universite Claude Bernard Lyon, 1
    Inventors: Henri Delalu, Cécile Colas-Duriche, Jacques Berthet, Philippe Leurent
  • Publication number: 20100240654
    Abstract: A compound represented by the following general formula (1) or a salt thereof or a hydrate of the foregoing is safe while exhibiting suitable physicochemical stability, and is useful as therapeutic or prophylactic agents for diseases associated with thrombus formation. wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc., R2 represents optionally substituted phenyl, etc., R3 represents optionally substituted C6-10 aryl, etc., Z1, Z2 and Z3 each independently represent hydrogen, etc., Z4 represents hydrogen, etc. and X represents a single bond or —CO—, etc.
    Type: Application
    Filed: June 1, 2010
    Publication date: September 23, 2010
    Inventors: Richard CLARK, Shinsuke HIROTA, Hiroshi AZUMA, Kazunobu KIRA, Nobuhisa WATANABE, Tadashi NAGAKURA, Tatsuo HORIZOE
  • Publication number: 20090062271
    Abstract: This application relates to a compound of formula I (or a pharmaceutically acceptable salt of the compound) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor.
    Type: Application
    Filed: November 15, 2005
    Publication date: March 5, 2009
    Applicant: Eli Lilly And Company
    Inventors: Jeffry Bernard Franciskovich, David Kent Herron, Valentine Joseph Klimkowski, Angela Lynn Marquart, John Joseph Masters, David Mendel, Andrew Michael Ratz, Gerald Floyd Smith, Michael Robert Wiley, Ying Kwong Yee
  • Publication number: 20080317806
    Abstract: A compound of Formula (A), wherein R1 is C1-C5 alkyl, C3-C6 branched alkyl, C4-C7 cycloalkyl, C8-C12 fused or bridged polycycloalkyl, or heterocyclic ring, where any of the preceding alkyl, cycloalkyl or heterocyclic ring groups may be singly or multiply substituted with X; R2 is H or R1; and X is halo, carbonyl carboxylic acid, carboxylic ester, carboxamide, substituted carboxamide, hydroxy, alkoxy, thioalkyl, sulphoxide, sulphone, sulphonamide, substituted sulphonamide, phenoxy, substituted phenoxy, phenyl, substituted phenyl, amino, substituted amino (including quaternary ammonium salts), N-oxide, imino, 5-7 membered heterocycle, or substituted heterocycle.
    Type: Application
    Filed: April 11, 2006
    Publication date: December 25, 2008
    Applicant: Murdoch University
    Inventors: Wayne Morris Best, Colette Gloria Sims, Richard Christopher Andrew Thompson, Simon Andrew Reid, Anthony Armson, James Alexander Reynoldson
  • Publication number: 20080194551
    Abstract: The invention provides compounds of formula (I), wherein the substituents are as defined in the specification, to processes for their preparation and their use as pharmaceuticals.
    Type: Application
    Filed: April 24, 2006
    Publication date: August 14, 2008
    Inventors: Ralf Glatthar, Thomas J. Troxler
  • Publication number: 20080132507
    Abstract: A compound represented by the following general formula (1) or a salt thereof or a hydrate of the foregoing is safe while exhibiting suitable physicochemical stability, and is useful as therapeutic or prophylactic agents for diseases associated with thrombus formation. wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc., R2 represents optionally substituted phenyl, etc., R3 represents optionally substituted C6-10 aryl, etc., Z1, Z2 and Z3 each independently represent hydrogen, etc., Z4 represents hydrogen, etc. and X represents a single bond or —CO—, etc.
    Type: Application
    Filed: October 13, 2005
    Publication date: June 5, 2008
    Applicant: Eisai R&D Management Co., Ltd.
    Inventors: Richard Clark, Shinsuke Hirota, Hiroshi Azuma, Kazunobu Kira, Nobuhisa Watanabe, Tadashi Nagakura, Tatsuo Horizoe
  • Patent number: 7183277
    Abstract: Novel compounds of the formula I in which D, W, X, Y, T and R1 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours.
    Type: Grant
    Filed: March 31, 2003
    Date of Patent: February 27, 2007
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Werner Mederski, Johannes Gleitz, Bertram Cezanne, Christos Tsaklakidis, Christopher Barnes
  • Patent number: 7034110
    Abstract: A method for obtaining compounds having selected properties for a particular application by forming base modules having at least two structural diversity elements from the reaction of a first compound having at least one structural diversity element and a first reactive group, with a second compound having at least one structural diversity element and a second reactive group, wherein the first and second groups combine by an addition reaction; producing a first array of molecules by varying at least one of the structural diversity elements of the compounds when producing the base modules; and screening the array to determine a first suitable compound for the particular application. The base modules are preferably formed form oxazolone- and aminimide-derived compounds.
    Type: Grant
    Filed: January 23, 2004
    Date of Patent: April 25, 2006
    Assignee: ArQule, Inc.
    Inventor: Joseph C. Hogan, Jr.
  • Patent number: 6900244
    Abstract: The present invention is directed to selective LXR modulators, small molecule compounds corresponding to Formula I and is further directed to a process of treating a condition in a mammal that is modulated by LXR using a therapeutically effective dose of a compound of Formula I.
    Type: Grant
    Filed: May 23, 2003
    Date of Patent: May 31, 2005
    Assignee: Pharmacia Corporation
    Inventors: Jennifer Ann Van Camp, James W. Malecha, Julie M. Miyashiro, Gary A. DeCrescenzo, Joe T. Collins, Monica J. Kalman
  • Patent number: 6849733
    Abstract: There are disclosed novel neuropeptide Y ligands having the general formula I Wherein the symbols W, A, D, R1, R2, R3, R4 are further defined in the description. Compounds of formula I are agonists and antagonists of neuropeptide Y, and are therefore useful as regulators.
    Type: Grant
    Filed: August 22, 1997
    Date of Patent: February 1, 2005
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Yufeng Hong, Vlad Edward Gregor, Anthony Lai Ling, Eileen Valenzuela Tompkins
  • Patent number: 6638930
    Abstract: Substituted heterocycles of the general structural formula: are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
    Type: Grant
    Filed: April 17, 2001
    Date of Patent: October 28, 2003
    Assignee: Merck & Co. Inc.
    Inventors: Conrad P. Dorn, Paul E. Finke, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian John Williams
  • Patent number: 6596863
    Abstract: 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 formula
    Type: Grant
    Filed: April 29, 2002
    Date of Patent: July 22, 2003
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Fuminori Kato, Keizo Miyata, Hirohiko Kimura, Kazuhiro Yamamoto, Hiroyuki Ikegami, Hiromi Takeo
  • Publication number: 20030114435
    Abstract: An agent comprising the benzoic acid of formula (I) 1
    Type: Application
    Filed: August 16, 2002
    Publication date: June 19, 2003
    Inventors: Kousuke Tani, Kaoru Kobayashi, Takayuki Maruyama
  • Patent number: 6482827
    Abstract: A compound, which is an amine derivative of formula (I) wherein W is —CNHOH or —COOH: R1 and R2 are each hydrogen or an organic residue, R3 is an organic group, Q is a secondary or tertiary acyclic or cyclic amido group, and the pharmaceutically acceptable salts, solvates and hydrates thereof, are inhibitors of matrix metalloproteinases (MMPs) and of the release of tumor necrosis factor-alpha (TNF) from cells. They are therefore useful in the prevention, control and treatment of diseases in which MMPs or TNF are involved, especially tumoral and inflammatory diseases. Processes for their preparation and pharmaceutical compositions containing them are also described.
    Type: Grant
    Filed: March 10, 1999
    Date of Patent: November 19, 2002
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Marco Alpegiani, Pierluigi Bissolino, Francesca Abrate, Ettore Perrone, Riccardo Corigli, Daniela Jabes
  • Publication number: 20020169155
    Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation.
    Type: Application
    Filed: November 21, 2001
    Publication date: November 14, 2002
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima, Hiroki Sone, Osamu Kotera, Geraldine C.B. Harriman, Kenneth G. Carson
  • Patent number: 6479491
    Abstract: The present invention relates to compounds of formula (I), any of it enantiomers, or any mixture thereof, or a pharmaceutically acceptable acid addition salt thereof, wherein R1, R2, R3, R4, R11, R12, R13, R14 and R15 each independently are hydrogen, alkyl, alkoxy, halogen, trifluoromethyl, nitro, cyano, amino, acyl, alkylamino, dialkylamino, aminocarbonyl, or acylamino; R5 is hydrogen, alkyl, alkoxyalkyl, or phenylalkyl; X is —CH2—Z—, Z—CH2—, NH—CO—, —CO—NH—, or —CH═CH—; wherein Z is O, S, CH2, or NH; Y is O, —CH2—W—, —W—CH2—; wherein W is O, or S; and n is 0, 1 or 2. The compounds are useful in the treatment of psychotic disorders.
    Type: Grant
    Filed: November 13, 2000
    Date of Patent: November 12, 2002
    Assignee: Neurosearch A/S
    Inventors: Oskar Axelsson, Dan Peters, Jorgen Scheel-Kruger, Elsebet Ostergaard Nielsen
  • Patent number: 6465457
    Abstract: Fungicidal compounds of formula (I): wherein W is CH3O.
    Type: Grant
    Filed: August 18, 1994
    Date of Patent: October 15, 2002
    Assignee: Zeneca Limited
    Inventors: Ian Richard Matthews, Christopher Richard Ayles Godfrey, John Martin Clough
  • Patent number: 6451792
    Abstract: 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: Grant
    Filed: March 20, 2001
    Date of Patent: September 17, 2002
    Assignee: Ishihara Sangyo Kaisha Ltd.
    Inventors: Fuminori Kato, Keizo Miyata, Hirohiko Kimura, Kazuhiro Yamamoto, Hiroyuki Ikegami, Hiromi Takeo
  • Patent number: 6288123
    Abstract: The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: September 11, 2001
    Assignee: Cambridge NeuroSciences, Inc.
    Inventors: Stanley M. Goldin, James B. Fischer, Andrew Gannett Knapp, N. Laxma Reddy, David Berlove, Graham J. Durant, Subbarao Katragadda, Lain-Yen Hu, Sharad Magar, Wenhong Fan, Elizabeth Yost, Jun Qing Guo
  • Patent number: 6232309
    Abstract: Insecticidal heterocyclic compounds of the formula: wherein A represents a five-membered or six-membered heteroaryl group containing one to three hetero atoms selected from the group consisting of S, O and N, said heteroaryl group being unsubstituted or substituted by a halogen atom or C1-4 alkyl group, Z represents a three-membered straight chain, each member being selected from the group consisting of CH2—, O, S and N—R2 with at least one of said three members being O, S or N—R2; E represents CH2, O, S or N—R2, wherein R2 represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkoxy group or the group wherein R3 represents a hydrogen atom or halogen atom, X represents CH or N, Y represents a nitro group or cyano group, and R1 represents a hydrogen atom or methyl group.
    Type: Grant
    Filed: May 22, 2000
    Date of Patent: May 15, 2001
    Assignee: Nihon Bayer Agrochem K.K.
    Inventors: Kozo Shiokawa, Shinichi Tsuboi, Koichi Moriya, Katsuhiko Shibuya
  • Patent number: 6221824
    Abstract: The storage stability of bleach-activating acetonitrile derivatives in solid detergent compositions was to be improved. This was essentially achieved by the use of compounded compounds corresponding to formula R1R2R3NxCH2CN X−, in which R1, R2 and R3 independently of one another represent an alkyl, alkenyl or aryl group containing 1 to 18 carbon atoms, in addition to which the groups R2 and R3 may even be part of a heterocycle including the N atom and optionally other hetero atoms, and X is a charge-equalizing anion. “Compounds” of this type are produced by drying in vacuo, for which purpose a suspension of the acetonitrile derivative and a solid carrier material is introduced into a mixer and the resulting mixture is dried with superheated vapor. Dishwashing detergents, more particularly machine dishwashing detergents, contain about 1% by weight to 10% by weight of this bleach boosting compound.
    Type: Grant
    Filed: February 25, 2000
    Date of Patent: April 24, 2001
    Assignee: Henkel Kommanditgesellschaft auf Aktien
    Inventors: Andreas Lietzmann, Artiga Gonzalez, Stefan Hammelstein, Christian Nitsch, Horst-Dieter Speckmann
  • Patent number: 6174924
    Abstract: The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: January 16, 2001
    Assignee: Cambridge NeuroScience, Inc.
    Inventors: Stanley M. Goldin, James B. Fischer, Andrew Gannett Knapp, N. Laxma Reddy, David Berlove, Graham J. Durant, Subbarao Katragadda, Lain-Yen Hu, Sharad Magar, Wenhong Fan, Elizabeth Yost, Jun Qing Guo
  • Patent number: 6156741
    Abstract: The present invention provides therapeutically useful substituted guanidines of the following Formula: ##STR1## and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: December 5, 2000
    Assignee: Cambridge NeuroScience, Inc.
    Inventors: Graham J. Durant, Sharad Magar, Lain-Yen Hu
  • Patent number: 6153604
    Abstract: The present invention provides therapeutically useful substituted guanidines of the following Formula: ##STR1## and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: November 28, 2000
    Assignee: Cambridge NeuroScience, Inc.
    Inventors: Graham J. Durant, Sharad Magar, Lain-Yen Hu
  • Patent number: 6147063
    Abstract: The present invention provides therapeutically useful substituted guanidines of the following Formula: ##STR1## and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: November 14, 2000
    Assignee: Cambridge NeuroScience, Inc.
    Inventors: Graham J. Durant, Sharad Magar, Lain-Yen Hu
  • Patent number: 6143791
    Abstract: The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: November 7, 2000
    Assignee: Cambridge NeuroScience, Inc.
    Inventors: Stanley M. Goldin, James B. Fischer, Andrew Gannett Knapp, N. Laxma Reddy, David Berlove, Graham J. Durant, Subbarao Katragadda, Lain-Hu Hu, Sharad Magar, Wenhong Fan, Elizabeth Yost, Jun Qing Guo
  • Patent number: 5977360
    Abstract: The present invention relates to a process for producing alicyclic hydrazine derivatives, tetrahydropyridazine and hexahydropyridazine which are useful as intermediate starting materials such as medicines and agricultural chemicals. Especially, the present invention provides;a process for producing an alicyclic hydrazine derivative or its hydrohalogenic acid salt, which comprises reacting a hydrazine hydrohalogenic acid salt with a diol compound or an alicyclic ether compound in the presence of an excessive inorganic acid existing in a free form or in the form of an acid addition salt;a process for producing tetrahydropyridazine from 1-aminopyrrolidine, which comprises oxidizing 1-aminopyrrolidine with an oxidizing agent to form tetrahydropyridazine; anda process for producing hexahydropyridazine, which comprises oxidizing 1-aminopyrrolidine with an oxidizing agent, synthesizing tetrahydropyridazine, and thereafter, hydrogenating the tetrahydropyridazine in the presence of a base.
    Type: Grant
    Filed: December 24, 1997
    Date of Patent: November 2, 1999
    Assignee: Japan Hydrazine Co., Ltd.
    Inventors: Youichi Hasegawa, Shunji Hyoda, Hiroyuki Fujita, Hirotoshi Sawada, Yasuo Oki
  • Patent number: 5932733
    Abstract: The present invention discloses peptide aldehydes having a lactam group as part of the peptide backbone and having an original mimic group such as an amidinopiperidine or amidinophengyl tail. These compounds are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: August 3, 1999
    Assignee: Corvas International, Inc.
    Inventors: Joseph E. Semple, Odile E. Levy, Ruth F. Nutt, William C. Ripka
  • Patent number: 5914351
    Abstract: Compounds of the formula ##STR1## wherein Q is a hydrazone derivative;R.sup.1 is hydrogen, halogen, alkyl or alkoxy;R.sup.2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; andR.sup.6 is a substituted carboxamide, carbothioamide, phosphonosoamide, or phosphonothioamide,useful as anti-HIV agents.
    Type: Grant
    Filed: December 12, 1997
    Date of Patent: June 22, 1999
    Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.
    Inventors: Walter Gerhard Brouwer, Ewa Maria Osika
  • Patent number: 5869484
    Abstract: Phenylcarbamate derivatives suitable to the use as anticholinesterase substances having the general formula (I) ##STR1## wherein the meaning of R.sub.1 -R.sub.7 and X substituentes together with n will be defined in the text.
    Type: Grant
    Filed: January 17, 1997
    Date of Patent: February 9, 1999
    Assignee: Mediolanum Farmaceutici S.P.A.
    Inventors: Patrizia Terni, Lucia Mairani, Giacomina Mandelli, Pier Giuseppe Pagella, Donata Marchesini, Stefano Maiorana, Mario Brufani
  • Patent number: 5852009
    Abstract: The present invention relates to compositions and methods for inhibiting protein aging. Accordingly, a composition is disclosed which comprises an agent or compound capable of inhibiting the formation of advanced glycosylation end products of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. Suitable agents may contain an active nitrogen-containing group, such as a hydrazine group. Particular agents comprise aminoguanidine, .alpha.-hydrazinohistidine and mixtures thereof. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.
    Type: Grant
    Filed: January 16, 1997
    Date of Patent: December 22, 1998
    Assignee: The Rockefeller University
    Inventors: Anthony Cerami, Peter C. Ulrich, Michael A. Brownlee
  • Patent number: 5814656
    Abstract: A method for the treatment of mammalian tissue injured or at risk of injury during sepsis or shock including the administration to a mammal a diazeniumdiolate which releases a therapeutically effective amount of nitric oxide sufficient to protect the tissue from sepsis- or shock-induced injury.
    Type: Grant
    Filed: October 2, 1997
    Date of Patent: September 29, 1998
    Assignee: The United States Of America, as represented by the Department Of Health And Human Services
    Inventors: Joseph E. Saavedra, Larry K. Keefer
  • Patent number: 5756733
    Abstract: The invention relates to novel 1.alpha.-hydroxy vitamin D derivatives and their 20-epi analogues, comprising compounds of general formula (I) ##STR1## where R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen atom or an aliphatic, cycloaliphatic, araliphatic or aryl group or together with the nitrogen atom to which they are attached form a heterocyclic group; R.sup.3 represents a methyl group having .alpha.- or .beta.-configuration; X represents a valence bond or a C.sub.1-2 alkylene group; Y represents --O--, --S--, --CH.sub.2 -- or --NR-- where R is a hydrogen atom or an organic group; Z represents a valence bond or a C.sub.1-3 alkylene group; and A.dbd. represents a cyclohexylidene moiety characteristic of the A-ring of a 1.alpha.-hydroxylated vitamin D or analogue thereof, with the proviso that when --X--Y--Z-- together represent an alkylene group containing up to 4 carbon atoms A.dbd. does not carry an exocyclic methylene group at the 10-position.
    Type: Grant
    Filed: January 5, 1996
    Date of Patent: May 26, 1998
    Assignee: Research Institute for Medicine and Chemistry
    Inventors: Robert Henry Hesse, Sundara Katugam Srinivasasetty Setty, Malathi Ramgopal
  • Patent number: 5756426
    Abstract: Described herein are compounds of the formula I ##STR1## and the isomers thereof, in which either a) X is an N atom andY is OR.sub.11 or N(R.sub.12)R.sub.13, orb) X is CH andY is OR.sub.11,and in which furthermore:R.sub.11 is C.sub.1 -C.sub.4 alkyl;R.sub.12 and R.sub.13, independently, are hydrogen or C.sub.1 -C.sub.4 alkyl;A is an O atom or the group NR.sub.4 ; and whereinR.sub.1, R.sub.2 and R.sub.3 are as defined herein, are pesticidal active ingredients. They can be used for pest control, in particular as microbicides, insecticides and acaricides in agriculture, horticulture and in the hygiene sector.
    Type: Grant
    Filed: September 11, 1995
    Date of Patent: May 26, 1998
    Assignee: Novartis Corporation
    Inventors: Hugo Ziegler, Stephan Trah, Saleem Farooq, Rene Zurfluh
  • Patent number: 5753652
    Abstract: The invention relates to compounds of formula ##STR1## and salts, pharmaceutical compositions, intermediates and processes of preparation thereof.
    Type: Grant
    Filed: April 4, 1995
    Date of Patent: May 19, 1998
    Assignee: Novartis Corporation
    Inventors: Alexander Fassler, Guido Bold, Marc Lang, Shripad Bhagwat, Peter Schneider
  • Patent number: 5705639
    Abstract: This invention includes compounds of Formula II and IV and a process for preparing Formula I compounds by first preparing the compounds of Formula IV and then further reacting to form the compounds of Formula II and further reacting to prepare the compounds of Formula I wherein Q, Z, R.sup.2 are as defined within.
    Type: Grant
    Filed: September 21, 1995
    Date of Patent: January 6, 1998
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Rafael Shapiro
  • Patent number: 5637622
    Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: June 10, 1997
    Assignee: State of Oregon, acting by and through the Oregon State Board of Higher Education, acting for and on behalf of the Oregon Health Sciences University and the University of Oregon
    Inventors: Eckard Weber, John F. W. Keana
  • Patent number: 5612332
    Abstract: The present invention relates to compounds, compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises a di- or tri-aminoguanidine capable of inhibiting the formation of advanced glycosylation endproducts of target proteins. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 18, 1997
    Assignees: Alteon Inc., The Rockefeller University
    Inventors: Dilip R. Wagle, Peter C. Ulrich, Anthony Cerami
  • Patent number: 5519018
    Abstract: Substituted phenols of the formula I ##STR1## processes for their preparation and compositions containing substituted phenols of the formulae I and II ##STR2## for the treatment of disorders caused by cell proliferation, such as psoriasis, tumor disorders and immunological disorders, are described.
    Type: Grant
    Filed: May 1, 1995
    Date of Patent: May 21, 1996
    Assignee: Behringwerke Aktiengesellschaft
    Inventors: Rudolf Matusch, Manfred Hunz, Jorg Czech, Hans-Harald Sedlacek
  • Patent number: 5510344
    Abstract: Compounds of formula I ##STR1## wherein X is oxygen or sulphur, W is CH or N, m is 0 or 1, and either a) n is 1 and Q is a non-aromatic heterocyclic ring of 3 to 10 ring atoms, containing one to three hetero atoms selected from oxygen, sulphur and nitrogen, which may be substituted and may be fused to another ring, with the proviso a) that if Q is thiazol-2-in-2-yl, it is substituted but not by methylene, and b) Q is not a six membered ring containing only two nitrogen atoms, or b) n is 0 or 1 and Q is ##STR2## where R.sup.1 is alkyl, alkoxy or alkylthio, and R.sup.2 is heteroaryl, non aromatic heterocyclyl, optionally substituted cycloalkyl or optionally substituted alkyl containing at least 5 carbon atoms, phenyl substituted by one or more groups selected from halogen, optionally substituted alkyl, alkoxy, haloalkoxy, aryloxy, alkylthio and alkoxycarbonyl, and when R.sup.1 is alkyl or alkoxy, or, when W is nitrogen, R.sup.2 can also be unsubstituted phenyl, have pesticidal especially fungicidal activity.
    Type: Grant
    Filed: May 4, 1994
    Date of Patent: April 23, 1996
    Assignee: Schering Agrochemicals Limited
    Inventors: Geoffrey R. Cliff, Ian C. Richards