Patents Examined by Jane T. Fan
  • Patent number: 6576762
    Abstract: The present invention is a heteroaromatic substituted amide showing antagonist activity to neurokinin 1 (NK-1, substance P) receptors.
    Type: Grant
    Filed: July 9, 2001
    Date of Patent: June 10, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Torsten Hoffmann, Patrick Schnider, Heinz Stadler
  • Patent number: 5552558
    Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.
    Type: Grant
    Filed: March 27, 1995
    Date of Patent: September 3, 1996
    Assignee: Abbott Laboratories
    Inventors: Dale J. Kempf, Daniel W. Norbeck
  • Patent number: 5432285
    Abstract: A novel chromogenic substrate to peroxidase enzymes is provided which is comprised of a mixture of an adduct formed from a hydrozone and a dienophile, and an aromatic nucleophile. The mixture undergos an oxidative coupling in the presence of peroxidase enzymes and peroxides forming a purple indamine dye. The mixture is also stable and unaffected by oxygen of the air or by hydrogen peroxide.
    Type: Grant
    Filed: May 28, 1993
    Date of Patent: July 11, 1995
    Inventors: Spyros Theodoropulos, Natalie S. Rudolph, James E. Woiszwillo
  • Patent number: 5432286
    Abstract: Substituted thieno[3,2-b]thiophenes, processes for their preparation and their useCompounds of the formula I ##STR1## in which R is a C.sub.1 - to C.sub.22 -alkyl radical,A.sup.1 and A.sup.2 are hydrogen or methyl orA.sup.1 is hydrogen and A.sup.2 is the nitro group, andB is the cyano group, the nitro group or an electron-attracting organic group having a double bond which is in conjugation with the thieno[3,2-b]thiophene ring system,have a high dipole moment and a high polarizability and are suitable for purposes of nonlinear optics. If R in the formula I is a C.sub.12 - to C.sub.22 -alkyl radical, monomolecular layers can be applied to a substrate by the Langmuir-Blodgett method. The resulting layer elements are suitable, inter alia, as waveguides.
    Type: Grant
    Filed: October 7, 1993
    Date of Patent: July 11, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ivan Cabrera, Uwe Falk, Werner Hickel, Donald Lupo, Ude Scheunemann, Peter Boldt, Martin Blenkle
  • Patent number: 5430042
    Abstract: The novel compounds of the formula I ##STR1## and physiologically acceptable salts thereof, wherein R.sup.1 and R.sup.2, which are different is each H alkyl containing 1-4 carbon atoms or --C(O)--R.sup.5 ;whereinR.sup.5 is alkyl containing 1-4 carbon atoms or alkoxy containing 1-4 carbon atoms and one of R.sup.1, or R.sup.2 is always selected from the group --C(O)--R.sup.5 ;R.sup.3 and R.sup.4 are the same or different and selected from ##STR2## and --CH.sub.2 CH.sub.2 OCH.sub.3 or R.sup.3 and R.sup.4 together with the adjacent oxygen atoms atached to the pyridine ring and the carbon atoms in the pyridine ring form a ring, wherein the part constituted by R.sup.3 and R.sup.4 is --CH.sub.2 CH.sub.2 CH.sub.2 --, or --CH.sub.2 --CH.sub.2 -- or --CH.sub.2 --; as well as intermediates, pharmaceutical compositions containing such compounds as active ingredient and the use of the compounds in medicine.
    Type: Grant
    Filed: June 20, 1991
    Date of Patent: July 4, 1995
    Assignee: Aktiebolaget Astra
    Inventors: Per L. Lindberg, Gunnel E. Sunden
  • Patent number: 5424315
    Abstract: Benzothiophene analogs useful to treat herpes viral infections, particularly cytomegalovirus, are provided. These antiviral agents have the structural formula (I) ##STR1## wherein R and R.sup.1 are as defined herein, and may be in free base or acid addition salt form. Pharmaceutical compositions are provided containing the antiviral agents, as are methods of treating herpes-infected individuals.
    Type: Grant
    Filed: August 2, 1993
    Date of Patent: June 13, 1995
    Assignee: SRI International
    Inventor: Elmer J. Reist
  • Patent number: 5409940
    Abstract: The invention relates to a group of new 3,4-dehydropiperidine derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl group having 1-3 carbon atoms;Y is a group of the general formula 2 ##STR2## wherein R.sub.2 is a group of the formula --(CH.sub.2).sub.n --C(.dbd.X)--NR.sub.3 R.sub.4, --(CH.sub.2).sub.n --SO.sub.2 --NR.sub.3 R.sub.4, --(CH.sub.2).sub.n --NR.sub.5 --C(.dbd.X)--R.sub.6 or --(CH.sub.2).sub.n --NR.sub.5 --SO.sub.2 --R.sub.6, wherein R.sub.3, R.sub.4 and R.sub.5 independent of each other represent hydrogen or alkyl (1-3C), R.sub.6 is alkyl (1-3C), X represents O or S; n is 0-4, andR is hydrogen or alkyl (1-3C).These compounds have interesting serotonin-1-like (partial) agonistic activity and can be used for the treatment of migraine.
    Type: Grant
    Filed: October 19, 1993
    Date of Patent: April 25, 1995
    Assignee: Duphar International Research B.V.
    Inventors: Antonius Hulkenberg, Karin J. van Charldorp, Rolf van Hes, Ineke van Wijngaarden
  • Patent number: 5410058
    Abstract: The compounds of the present invention relates to tetrahydropyridine derivatives and have high affinity and specificity to .sigma. receptors, whereby these are thought to be effective for some psychoses.
    Type: Grant
    Filed: February 28, 1994
    Date of Patent: April 25, 1995
    Assignee: Shionogi & Co., Ltd.
    Inventors: Hiromu Matsumura, Toshisada Yano, Hiroshi Hashizume, Akira Matsushita, Masami Eigyo
  • Patent number: 5405966
    Abstract: Conjugates of trichothecenes and agents that bind to a defined population of cells are disclosed. Preferred are conjugates of trichothecene molecules with polyclonal or monoclonal antibodies or fragments thereof that recognize antigens that are present only on tumor cells or are augmented in their expression on tumor cells as compared to normal tissues. Trichothecene molecules are coupled to the agent through non-covalent and covalent linkages, such as peptide bonds, disulfide bonds, thioester bonds, or thioether bonds. A method for inhibiting the growth and metabolism of antigen-positive cells is also disclosed. Derivatized trichothecene compounds prepared for conjugation to targeting agents are also disclosed.
    Type: Grant
    Filed: June 7, 1993
    Date of Patent: April 11, 1995
    Inventors: Louis J. Theodore, John M. Reno, Sudhakar Kasina, James A. Sanderson, Paul G. Abrams
  • Patent number: 5405827
    Abstract: 5-Heterocyclic 2-(2-imidazolin-2-yl)pyridine compounds which are effective for the control of undesirable plant species are described. Also described are a method for the herbicidal use of said compounds and a method for their preparation.
    Type: Grant
    Filed: October 21, 1993
    Date of Patent: April 11, 1995
    Assignee: American Cyanamid Company
    Inventor: John M. Finn
  • Patent number: 5403849
    Abstract: 4-Heterocyclophenyl-substituted dihydropyridines ##STR1## are prepared either by reacting suitable aldehydes with amino esters and .beta.-keto esters, or preparing the heterocyclic substituents of the 4-phenyl by cyclization of corresponding amidines or hydrazides, or esterifying dihydropyridinecarboxylic acids, which are already substituted by heterocyclic radicals, with corresponding alcohols. The 4-heterocyclophenyl-substituted dihydropyridines can be employed in medicaments, in particular for treatment of diseases of the central nervous system.
    Type: Grant
    Filed: October 22, 1993
    Date of Patent: April 4, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rudolf Schohe-Loop, Wolfgang Hartwig, Bodo Junge, Heinrich Meier, Zhan Gao, Bernard Schmidt, Maarten de Jonge, Teunis Schuurman
  • Patent number: 5399697
    Abstract: The compounds of the formula: ##STR1## in which X, Y and Z are, independently, hydrogen, halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino, dialkylamino, alkyl, alkoxy or phenylalkyloxy; R.sub.1 is thienyl, imidazolyl, thiazolyl, pyridinyl, quinolinyl, pyrimidinyl, pyrazinyl, benzamidazolyl, phenylalkylpiperidinyl or morpholino or athaae analogous hetercyclic groups with from one to three substituents selected from halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino of 1 to 6 carbon atoms, dialkylamino in which each alkyl group has 1 to 6 carbon atoms, alkyl of 1 to 6 carbon atoms, or alkoxy of 1 to 6 carbon atoms; R.sub.2 is hydrogen, alkyl, cycloalkyl, phenyl, benzyl or substituted phenyl or benzyl in which said substituent is alkyl, alkoxy, halogen, cyano, trifluoromethyl amino, nitro, alkylamino or dialkylamino; and a pharmaceutically acceptable salt thereof; are ACAT inhibitors, some of which possess antioxidant properties.
    Type: Grant
    Filed: November 15, 1993
    Date of Patent: March 21, 1995
    Assignee: American Home Products Corporation
    Inventors: William F. Fobare, Donald P. Strike
  • Patent number: 5399566
    Abstract: The invention provides compounds represented by the following formula (I) ##STR1## or a pharmaceutically acceptable salts thereof wherein A represents ##STR2## B represents a carboxy or tetrazolyl group; and X represents --O--, --NH-- or --S(O).sub.t --.The compounds possess angiotensin II antagonism, and may be used as an antihypertensive agent, a therapeutic agent to congestive heart failure, an antianxiety agent and a cognitive enhancing agent.
    Type: Grant
    Filed: September 10, 1991
    Date of Patent: March 21, 1995
    Assignee: Meiji Seika Kabushiki Kaisha
    Inventors: Kiyoaki Katano, Hiroko Ogino, Eiki Shitara, Hiromi Watanabe, Jun Nagura, Naomi Osada, Yasuyuki Ichimaru, Fukio Konno, Tomoya Machinami, Takashi Tsuruoka
  • Patent number: 5399700
    Abstract: The present invention relates to a method for preparing enteric-coated oral drugs containing acid-unstable compound, in particular an enteric-coated oral drug prepared in the form of acid-stable dosage units as inclusion complex formed by reacting benzimidazole derivative, acid-unstable compound, with cyclodextrin in alkaline solution.
    Type: Grant
    Filed: December 29, 1992
    Date of Patent: March 21, 1995
    Assignee: Sunkyong Industries Co., Ltd.
    Inventors: Dong S. Min, Kee A. Um, Yong S. Kim, Pyong W. Park
  • Patent number: 5397793
    Abstract: A class of novel heterocyclicacetonitriles which is useful in the control of fungi, especially bitunicate asci and unitunicate asd, has been discovered. These compounds are of the general formula: ##STR1## wherein Ar.sub.1 and Ar.sub.2 are substituted or unsubstituted aryl groups; Het is a six-membered nitrogen-containing heterocyclic ring; n is the integer 2 or 3; and the agronomically acceptable enantiomorphs, add addition salts and metal complexes thereof.
    Type: Grant
    Filed: November 15, 1993
    Date of Patent: March 14, 1995
    Assignee: Rohm and Haas Company
    Inventors: Steven H. Shaber, Edward M. Szapacs, Charles H. Reynolds
  • Patent number: 5395817
    Abstract: Substituted N-arylindoles, a process for producing them and their use as herbicides. In particular, substituted N-arylindoles of the formula ##STR1## are disclosed in which: R is hydrogen; halogen; nitro; cyano; alkyl; alkoxy; alkenyloxy; alkynyloxy; alkoxyalkyl; carbonylalkoxy; alkyloxyalkoxy; cyanoalkoxy; benzyloxy; alkoxycarbonylalkoxy; alkylcarbonylalkoxy; haloalkyl; hydroxyalkyl; formyl; azido; carboxy or a salt thereof; amino; substituted amino; carboxyamido; substituted carboxyamido; sulfonamido wherein the N is substituted with hydrogen and/or alkyl; or YR.sup.4 wherein Y is O or S(O).sub.m and R.sup.4 is hydrogen, alkyl, haloalkyl, cyanoalkyl, alkoxycarbonylalkyl, hydroxycarbonylalkyl or aminocarbonylalkyl; R.sup.1 is hydrogen, alkyl, halogen, cyano, haloalkyl, alkoxy, or carboxy or a salt thereof; X is hydrogen, halogen, cyano, nitro, alkylthio, alkylsulfinyl, alkylsulfonyl, haloalkyl or alkoxy; R.sup.3 is hydrogen, haloalkyl, haloalkoxy, cyano, halogen, or SO.sub.y R.sup.5 wherein R.sup.
    Type: Grant
    Filed: December 9, 1992
    Date of Patent: March 7, 1995
    Assignee: Imperial Chemical Industries PLC
    Inventors: Ference M. Pallos, Christoper J. Mathews
  • Patent number: 5391540
    Abstract: Disclosed herein are herbicidal pyridine compounds substituted at the 2- or 6-position with an OR.sub.2 moiety where R.sub.2 is hydrogen, lower alkyl, halomethyl, lower cyanoalkyl, alkenyl or alkynyl, as well as herbicidal compositions and herbicidal use of these compounds.
    Type: Grant
    Filed: April 12, 1993
    Date of Patent: February 21, 1995
    Assignee: Rohm and Haas Company
    Inventors: Donald E. Korte, Len F. Lee
  • Patent number: 5391562
    Abstract: Insecticidal guanidine derivatives of the formula ##STR1## wherein Z represents an optionally substituted five- or six-membered ring containing at least one ring hetero atom selected from the group consisting of oxygen, sulfur and nitrogen,R.sup.1 represents hydrogen atoms or a C.sub.1-4 alkyl group,R.sup.2 and R.sup.3 each independently represents hydrogen, C.sub.1-4 alkyl, C.sub.1-4 haloalkyl or optionally substituted phenyl,R.sup.4 and R.sup.5 each independently represents hydrogen, C.sub.1-4 alkyl, C.sub.3-4 alkenyl, C.sub.3-4 alkynyl, optionally substituted benzyl or a group of the formula Z--C(R.sup.1)H--,n represents the integer 2 or 3, andY represents nitro or cyano.
    Type: Grant
    Filed: August 30, 1993
    Date of Patent: February 21, 1995
    Assignee: Nihon Bayer Agrochem K.K.
    Inventors: Shin-ichi Tsuboi, Koichi Moriya, Yumi Hattori, Shinzaburo Sone, Katsuhiko Shibuya
  • Patent number: 5391752
    Abstract: Anti-ulcer agents having a methylsulfinyl bridge between a substituted pyridine moiety and a substituted benzimidazole moiety are prepared by oxidizing the corresponding compounds, having a methylthio bridge, with magnesium monoperoxyphthalate in a suitable solvent. The reaction may be run in an aromatic hydrocarbon solvent, wherein the product may crystallize out of the reaction solution and may be directly isolated by filtration.
    Type: Grant
    Filed: February 22, 1993
    Date of Patent: February 21, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Robert S. Hoerrner, Joel J. Friedman, Joseph S. Amato, Thomas M. Liu, Ichiro Shinkai, Leonard M. Weinstock
  • Patent number: 5391751
    Abstract: The present invention relates to 2,2-dimethylchromene derivatives of the formula: ##STR1## in which Z represents a halogen atom or a cyano, nitro, acetyl, phosphono or dialkoxyphosohoryl group, the alkoxy group containing 1 to 3 carbon atoms, and the pharmaceutically acceptable salts of the phosphono group.These compounds show an antihypertensive and antiarrythmic activity.The present invention also relates to a process for the preparation of said compounds and to the pharmaceutical compositions in which the are present.
    Type: Grant
    Filed: August 19, 1991
    Date of Patent: February 21, 1995
    Inventors: Georges Garcia, Alain Di Malta, Patrick Gautier