Patents Examined by Deborah Lambkin
  • Patent number: 5747518
    Abstract: The substituted thiophene derivative of the invention which is represented by the general formula (1) has a broad disease spectrum for a pathogenic fungus of various crops, exhibits an excellent controlling effect on disease such as gray mold, powdery mildew and rust in particular, and is also effective for a resistant fungus of conventional fungicides which has become a serious problem, and consequently is useful for an agricultural and horticultural fungicide.
    Type: Grant
    Filed: April 3, 1996
    Date of Patent: May 5, 1998
    Assignee: Mitsui Toatsu Chemicals, Inc.
    Inventors: Yukihiro Yoshikawa, Kanji Tomiya, Hiroyuki Katsuta, Hideo Kawashima, Osamu Takahashi, Shunichi Inami, Yuji Yanase, Junro Kishi, Hitoshi Shimotori, Naofumi Tomura
  • Patent number: 5747542
    Abstract: Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
    Type: Grant
    Filed: June 21, 1996
    Date of Patent: May 5, 1998
    Assignee: Allergan
    Inventors: Vidyasagar Vuligonda, Alan T. Johnson, Richard L. Beard, Min Teng, Tae K. Song, Harold N. Wong, Roshantha A. Chandraratna
  • Patent number: 5747540
    Abstract: Compounds such as ##STR1## or pharmaceutically acceptable salts thereof, are HIV protease inhibitors. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: October 21, 1996
    Date of Patent: May 5, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Craig A. Coburn, Randall W. Hungate, Richard C. A. Isaacs, Joseph P. Vacca, Mary Beth Young
  • Patent number: 5744621
    Abstract: Cis-epoxide compounds of formula (I-1) and pharmaceutically acceptable salts, hydrates and solvates thereof: ##STR1## wherein: R.sup.1 is a cycloalkyl, or aryl-substituted lower alkyl group;A is a functionalized acyl group of the formula ##STR2## wherein R.sup.2 is a C.sub.1-4 alkyl, or amide-substituted C.sub.1-2 alkyl group;R.sup.3 is a C.sub.1-4 alkoxy, aryloxyalkyl or arylalkoxy, or a nitrogen-containing aromatic radical, or a lower alkoxy group substituted with a nitrogen-containing aromatic radical, or a radical having the formula of ##STR3## wherein R.sup.4 is a hydrogen or a methyl group and R.sup.5 is an alkyl group substituted with a nitrogen-containing aromatic radical; and m is 0 or 1; and B is a functionalized amino group of the formula ##STR4## wherein R.sup.8 and R.sup.9 are independently a C.sub.1-4 alkyl group optionally substituted with an aromatic radical, or an aromatic group.
    Type: Grant
    Filed: June 20, 1996
    Date of Patent: April 28, 1998
    Assignee: Lucky Limited.
    Inventors: Sung Chun Kim, Nakyen Choy, Chang Sun Lee, Young Chan Son, Ho Il Choi, Jong Sung Koh, Heungsik Yoon, Chi Hyo Park, Sang Soo Kim
  • Patent number: 5744452
    Abstract: The new class of synthetic immunomodulatory molecules having a .gamma.-L-glutamyl- moiety at the amino terminus are provided as illustrated by Formula 1. ##STR1## In Formula 1, the Greek symbols designate the noted carbon atoms, R is hydrogen, acyl or alkyl, and X is an aromatic or heterocyclic amino acid or its derivative. Included as members of the new class (in addition to Bestim, .gamma.-L-glutamyl-L-tryptophan) are those compounds where R=hydrogen and X=L-tryptophan, such as .gamma.-L-glutamyl-N.sub.in -formyl-L-tryptophan, N-methyl-.gamma.-L-glutamyl-L-tryptophan, N-acetyl-.gamma.-L-glutamyl-L-tryptophan, and .gamma.-L-glutamyl-.beta.-thienyl-D-alanylamide. A preferred embodiment, termed "BESTIM," has the chemical structure of .gamma.-L-glutamyl-L-tryptophan.
    Type: Grant
    Filed: April 18, 1996
    Date of Patent: April 28, 1998
    Assignee: Edward T. Wei
    Inventors: Alexander A. Kolobov, Andrey S. Simbirtsev, Sergey V. Kulikov, Alexey N. Prusakov, Natalia M. Kalinina, Natalia V. Pigareva, Alexander U. Kotov, Vladimir M. Shpen, Oleg A. Kaurov, Sergey A. Ketlinsky
  • Patent number: 5744617
    Abstract: A process for the preparation of substituted phenols, in particular, the condensation of phenols having one or more alkyl substituents with a butadiene derivative comprising at least six carbon atoms, in particular myrcene and/or .beta.-springene is disclosed. The cyclization, in the form of chromans, of the products obtained during this condensation and their hydrogenation in order to prepare vitamin E is also disclosed.
    Type: Grant
    Filed: May 10, 1996
    Date of Patent: April 28, 1998
    Assignee: Rhone-Poulenc Nutrition Animale
    Inventors: Jean-Erick Ancel, Hugues Bienayme, Pierre Meilland
  • Patent number: 5741811
    Abstract: Novel polythiophene compounds useful as anti-tumor agents are described. Preferred compounds of the formula: ##STR1## wherein n is 0-2 and R.sub.2 and R.sub.3 are optionally substituted 2-thienyl or 3-thienyl have been found to exhibit selective cytotoxic activity against transformed human cells. Pharmaceutical compositions containing the described polythiophene compounds are expected to exhibit good chemotherapeutic activity against slow growing tumors based on tumor cell line assays. A method for treating patients having tumors utilizing the disclosed polythiophene compounds is also described.
    Type: Grant
    Filed: September 12, 1996
    Date of Patent: April 21, 1998
    Assignees: Purdue Research Foundation, Industrial Technology Research Institute
    Inventors: Ching Te Chang, Ching-Jer Chang, Chen-Tao Lee, Fen-Lan Lin, Jih-Dar Tsai, Curtis L. Ashendel, Thomas C. K. Chan, Robert L. Geahlen, David J. Waters
  • Patent number: 5741810
    Abstract: The present invention provides to cyclopentane heptanoic acid, 2 heteroaryl alkyl or alkenyl derivatives which may be substituted in the 1-position with hydroxyl, alkyloxy, amino and amido groups, e.g. 1-OH cyclopentane heptanoic acid, 2 heteroarylalkenyl derivatives. In particular, these derivatives are 7-?5-hydroxy-2-(heteroatom-substituted hydroxyhydrocarbyl)-3-hydroxycyclopentyl!heptanoic or heptenoic acids and amine, amide, ether, ester and alchohol derivatives of said acids wherein one or more of said hydroxy groups are replaced with an ether group. These compounds are potent ocular hypotensive and are particularly suited for the management of glaucoma.
    Type: Grant
    Filed: February 29, 1996
    Date of Patent: April 21, 1998
    Assignee: Allergan
    Inventor: Robert M. Burk
  • Patent number: 5741818
    Abstract: A compound of general formula I below useful as an anticonvulsant for disorders of the central nervous system: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3 and R.sup.4 may be the same or different and each represents a hydrogen or halogen atom, or a C.sub.1-9 alkyl, C.sub.3-9 cycloalkyl, cyano, C.sub.1-9 alkoxy or C.sub.6-10 aryloxy group; R.sup.5 represents a hydrogen atom or a C.sub.1-9 alkyl, C.sub.3-9 cycloalkyl or C.sub.6-10 aryl group; and X is oxygen or sulfur; or a pharmaceutically-acceptable salt thereof. The compound may be adimistered orally for treating convulsions in humans or animals.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: April 21, 1998
    Assignee: University of Saskatchewan
    Inventor: Jonathan Richard Dimmock
  • Patent number: 5739353
    Abstract: This invention relates to substituted N-arylindoles, a process for producing them and their use as herbicides. In particular, this invention relates to substituted N-arylindoles of the formula ##STR1## wherein R, R.sup.3, X, Z, n and k are defined herein.
    Type: Grant
    Filed: November 1, 1996
    Date of Patent: April 14, 1998
    Assignee: Zeneca Limited
    Inventors: Ferenc M. Pallos, Christopher J. Mathews
  • Patent number: 5736566
    Abstract: Heteroaromatic compounds of the formulae IA and IB ##STR1## where the dashed line is a double bond between the carbon atom and a Z atom, and the index and the substituents have the following meanings:R.sup.1 alkyl, alkoxy, alkylaminoR.sup.2 alkyl;A a direct bond; alkylene, alkenylene, alkynylene; O, S, S-oxides, N and alkylene derivatives or oxime radicals thereofB hydrogen, halogen, alkyl, alkenyl, alkynyl; cycloalkyl, cycloalkenyl, cycloalkynyl, heterocyclyl, aryl, hetarylU CH.sub.2, CHCl, CHR.sup.2 or NOR.sup.2 ;X hydrogen, cyano, nitro, halogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, hetaryl; oxi- and thio derivatives thereof, carbonyl derivatives thereof, carbonyloxy derivatives thereof, amino derivatives thereof, oxime derivatives thereof, amino which may bear one or two of the abovementioned groups;m 1 or 2,Y oxygen or sulfur;Z.sup.1 -Z.sup.2, Z.sub.3 -Z.sub.
    Type: Grant
    Filed: July 7, 1997
    Date of Patent: April 7, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Mueller, Hubert Sauter, Horst Wingert, Hartmann Koenig, Franz Roehl, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 5733850
    Abstract: Substituted 2-phenylpyridines I ##STR1## where the substituents have the meaning given in the specification and their use.
    Type: Grant
    Filed: July 3, 1997
    Date of Patent: March 31, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Peter Schafer, Gerhard Hamprecht, Elisabeth Heistracher, Ralf Klintz, Hartmann Konig, Albrecht Harreus, Norbert Gotz, Helmut Walter, Karl-Otto Westphalen, Ulf Misslitz
  • Patent number: 5734065
    Abstract: The present invention provides a thiophene derivative and the polymer thereof as expressed in the following formulas, which will respond to light and electricity and which are best suited for use as photorecording materials and light-electricity conversion elements. ##STR1## where n and m are independent integral numbers greater than 0; R.sub.1 is a hydrogen atom, a halogen atom or a trialkylsilyl group; the R.sub.2 s together with the ethylenic linkage form a ring and said R.sub.2 s taken together are an optionally substituted alkylene group or --COOCO-- or the R.sub.2 s independently represent cyano; and R.sub.3, R.sub.4 and R.sub.5 are hydrogen or alkyl.
    Type: Grant
    Filed: August 25, 1995
    Date of Patent: March 31, 1998
    Assignee: Research Development Corporation of Japan
    Inventor: Tetsuyuki Saika
  • Patent number: 5733936
    Abstract: 6-dimethylaminomethyl-1-phenyl-cyclohexane compounds, methods of preparing them and the use of these compounds in drugs are described.
    Type: Grant
    Filed: July 10, 1996
    Date of Patent: March 31, 1998
    Assignee: Gruenenthal GmbH
    Inventors: Helmut Heinrich Buschmann, Wolfgang Werner Alfred Strassburger, Norma Selve, Elmar Josef Friderichs
  • Patent number: 5731350
    Abstract: Benzenedicarboxylic acid diguanides of the formula I ##STR1## in which R(1) to R(5) have the meanings given in the claims, are useful antiarrhythmic pharmaceuticals having a cardioprotective component, even for the prevention of ischemically induced damage, in particular in the induction of ischemically induced cardiac arrhythmias. As a result of inhibition of the cellular Na.sup.+ /H.sup.+ exchange mechanism, they are used for the treatment of acute or chronic damage caused by ischemia. Moreover, they are distinguished by potent inhibitory action on the proliferation of cells. They are suitable for preventing the genesis of high blood pressure.
    Type: Grant
    Filed: November 7, 1996
    Date of Patent: March 24, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Werner Kleemann, Joachim Brendel, Jan-Robert Schwark, Andreas Weichert, Hans Jochen Lang, Udo Albus, Wolfgang Scholz
  • Patent number: 5731328
    Abstract: A method of inhibiting plasminogen activator inhibitor 1 comprising administering to a human in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneimino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.
    Type: Grant
    Filed: September 4, 1996
    Date of Patent: March 24, 1998
    Assignee: Eli Lilly and Company
    Inventors: David Thompson Berg, Brian William Grinnell, Mark Alan Richardson
  • Patent number: 5728699
    Abstract: The present invention presents a benzylsulfide derivative of the formula (I) or its salt: ##STR1## wherein R.sup.1 is a C.sub.1-6 alkyl group, a C.sub.1-6 haloalkyl group, a C.sub.2-4 alkenyl group, a cyano group, etc., and each of R.sup.2 and R.sup.3 is a hydrogen atom, a halogen atom, a cyano group, a C.sub.1-4 alkyl group, a C.sub.1-3 haloalkyl group, etc., R.sup.4 is a hydrogen atom, a halogen atom, a C.sub.1-4 alkyl group, etc., A is a hydrazinoaralkyl group or hydrazonoaralkyl group, and n is 0, 1 or 2; a process for its production; and a pesticide containing such a benzylsulfide derivative as an active ingredient. The benzylsulfide derivative of the present invention is capable of controlling various pests without adversely affecting crop plants.
    Type: Grant
    Filed: December 19, 1996
    Date of Patent: March 17, 1998
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Keiji Toriyabe, Hideharu Sasaki, Naoshi Masuyama, Akihide Nagai, Hiroyuki Yano, Mieko Kawashima, Yutaka Kurihara, Tomonori Shimazu
  • Patent number: 5728866
    Abstract: A method for preparing 3-oxo-2-pentyl-1-cyclopentaneacetic acid or methyl 3-oxo-2-pentyl-1-cyclopentaneacetate, essentially in the form of the (+)-(1R)-cis isomer thereof. The method includes the steps of(a) catalytically hydrogenating a compound of the formula (I), ##STR1## wherein M is a hydrogen atom, an alkali metal or alkaline earth metal atom, or a group NR.sub.4, where R is a hydrogen or a lower alkyl radical, in a suitable solvent and in the presence of a catalyst consisting of an Ru(II) complex comprising chiral ligands that contain a 2,2'-bis(diphenylphosphino)-1,1'-dinaphthyl (BINAP) radical or a 1,2-bis(2,5-dialkylphospholano)benzyl (DuPHOS) radical, wherein the alkyl is a C.sub.2 or C.sub.3 radical, to give a compound of formula (II), ##STR2## wherein M has the meaning given above, essentially in the form of the (+)-(1R)-cis isomer thereof;(b) if required, acidifying, in a per se known manner, the compound of formula (II), wherein M is an alkali metal or alkaline earth metal atom, or a group N.
    Type: Grant
    Filed: February 7, 1996
    Date of Patent: March 17, 1998
    Assignee: Firmenich SA
    Inventors: Valentin Rautenstrauch, Jean-Jacques Riedhauser
  • Patent number: 5728737
    Abstract: The present invention relates to novel N-alkoxy-arnidine derivatives of the formula (I), to a process for their preparation and to their use as pesticides. In addition, the invention also relates to novel intermediates and to a process for their preparation.
    Type: Grant
    Filed: January 23, 1997
    Date of Patent: March 17, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Heinemann, Bernd-Wieland Kruger, Ralf Tiemann, Stefan Dutzmann, Klaus Stenzel
  • Patent number: 5726124
    Abstract: A class of 2-arylpyrimidines which is useful in the control of weeds of the general formula: ##STR1## wherein R.sup.2 is an optionally substituted aromatic ring; R.sup.3 is a saturated or unsaturated alkyl group; R.sup.5 is selected from acyl, alkoxyalkyl, alkoxyimino, dialkoxyalkyl, formyl, hydroxyalkyl, alkoxyalkoxy, cyanoalkyl and hydroxyimino; R.sup.6 is selected from hydrogen, halo, alkyl, haloalkyl, aryl, and alkoxy; and X is oxygen or sulfur.
    Type: Grant
    Filed: October 28, 1994
    Date of Patent: March 10, 1998
    Assignee: Rohm and Haas Company
    Inventors: Colin Michael Tice, Vincent Angelo Musco, Renee Caroline Roemmele, Harlow Lester Warner