C=o Bonded Directly To The Hetero Ring (x Is Chalcogen) Patents (Class 514/448)
  • Patent number: 5580893
    Abstract: Nitroxyalkylamide compounds having the formula: R.sup.1 --(A).sub.n --CONH--B'--ONO.sub.2 wherein R.sup.1 is an optionally substituted furyl, furyloxy, thienyl, thienyloxy, isoxazolyl, phenoxy, phenylthio or 1,4-dibenzodioxanyl, A is a C.sub.1 -C.sub.4 alkylene group; B' is a C.sub.1 -C.sub.4 alkylene group; and n is 0 or 1. The compounds of the present invention have a desirable vasodilator action for collateral vessels and an anti-anginal action, and are useful as therapeutic agents for treating angina pectoris.
    Type: Grant
    Filed: July 25, 1994
    Date of Patent: December 3, 1996
    Assignee: Sankyo Company, Limited
    Inventors: Sadao Ishihara, Fujio Saito, Mitsuru Kataoka, Hiroyuki Koike, Shigeki Miyake, Hiroshi Mizuno
  • Patent number: 5576337
    Abstract: A method of inhibiting the physiological disorder anxiety associated with an excess of neuropeptide Y or its symptoms 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, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.
    Type: Grant
    Filed: August 21, 1995
    Date of Patent: November 19, 1996
    Assignee: Eli Lilly and Company
    Inventors: Robert F. Bruns, Jr., Donald R. Gehlert, J. Jeffry Howbert, William H. W. Lunn
  • Patent number: 5567714
    Abstract: A method of inhibiting obesity, a physiological disorder associated with an excess of neuropeptide Y, or its symptoms 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, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.
    Type: Grant
    Filed: August 21, 1995
    Date of Patent: October 22, 1996
    Assignee: Eli Lilly and Company
    Inventors: Robert F. Bruns, Jr., Donald R. Gehlert, J. Jeffry Howbert, William H. W. Lunn
  • Patent number: 5567715
    Abstract: A method of inhibiting a physiological disorder associated with an excess of neuropeptide Y or its symptoms 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, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.
    Type: Grant
    Filed: August 21, 1995
    Date of Patent: October 22, 1996
    Assignee: Eli Lilly and Company
    Inventors: Robert F. Bruns, Jr., Donald R. Gehlert, J. Jeffry Howbert, William H. W. Lunn
  • Patent number: 5534527
    Abstract: The current invention provides methods and pharmaceutical formulations that are useful for inhibiting the loss of bone. These methods and formulations can be used without the associated adverse effects of estrogen therapy, and thus serve as an effective and acceptable treatment for osteoporosis.
    Type: Grant
    Filed: April 14, 1995
    Date of Patent: July 9, 1996
    Assignee: Eli Lilly and Company
    Inventors: Larry J. Black, George J. Cullinan
  • Patent number: 5534541
    Abstract: Halogen thiophene carboxylic acid derivatives of the General Formula ##STR1## in which Hal signifies chlorine or bromine, n the number 2 or 3, * signifies either an enantiomer or a racemate in the case of different R.sup.2 and R.sup.3 groups,R.sup.1 stands for hydrogen or an alkyl group,R.sup.2 stands for hydrogen, an alkyl group which can optionally be substituted by hydroxy-, carboxy-, alkoxy- or alkoxycarbonyl, mercapto- or alkylmercapto- or benzylmercapto, for an aryl group or aralkyl group, wherein the ring system can optionally be substituted with fluorine, chlorine or bromine atoms, for a cycloalkyl group or a cycloalkyl-methyl group,R.sup.3 stands for hydrogen, an alkyl group, an alkenyl or alkynyl group or, optionally, R.sup.1 and R.sup.3 or R.sup.2 and R.sup.3 together can form an alkylene bridge in which one CH.sup.2 unit can optionally be substituted by NR.sup.1, O or S,Y signifies OH, OR.sup.4 or NR.sup.5 R.sup.6,in whichR.sup.
    Type: Grant
    Filed: January 23, 1995
    Date of Patent: July 9, 1996
    Assignee: Degussa Aktiengesellschaft
    Inventors: Karlheinz Drauz, Jurgen Martens
  • Patent number: 5527829
    Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
    Type: Grant
    Filed: May 23, 1994
    Date of Patent: June 18, 1996
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventor: Vincent J. Kalish
  • Patent number: 5506224
    Abstract: N-acyl-derivatives of hydroxyamines suitable for the therapeutic treatment of pathologies characterized by degranulation of mast cells caused by a neurogenic and/or immunogenic hyperstimulation.
    Type: Grant
    Filed: November 8, 1993
    Date of Patent: April 9, 1996
    Assignee: Lifegroup S.P.A.
    Inventors: Francesco della Valle, Silvana Lorenzi, Jacobus C. J. J. Samson, Federica della Valle
  • Patent number: 5504094
    Abstract: A method of inhibiting a physiological disorder associated with an excess of neuropeptide Y or its symptoms 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, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.
    Type: Grant
    Filed: August 21, 1995
    Date of Patent: April 2, 1996
    Assignee: Eli Lilly and Company
    Inventors: Robert F. Bruns, Jr., Donald R. Gehlert, J. Jeffry Howbert, William H. W. Lunn
  • Patent number: 5492927
    Abstract: This invention encompasses methods for the treatment or prevention of a physiological disorder associated with an excess of tachykinins, said disorder being an allergy which method comprises administering to a mammal in need of said treatment an effective amount of a compound of Formula I ##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, hexamthylenemino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.
    Type: Grant
    Filed: December 21, 1993
    Date of Patent: February 20, 1996
    Assignee: Eli Lilly and Company
    Inventors: Bruce D. Gitter, William H. W. Lunn
  • Patent number: 5486621
    Abstract: This invention relates to 4,5-dimethyl-N-2-propenyl-2-(trimethylsilyl)-3-thiophenecarboxamide, a method for the control of Take-All disease (Gaeumannomyces species) in plants by the use of this compound, and to fungicidal compostions for carrying out the method.
    Type: Grant
    Filed: December 15, 1994
    Date of Patent: January 23, 1996
    Assignee: Monsanto Company
    Inventors: Dennis Phillion, Sai C. Wong, Barry Shortt
  • Patent number: 5478847
    Abstract: A method of inhibiting bone loss or resorption, or lowering serum cholesterol, comprising administering to a human in need thereof a compound having the formula ##STR1## or a pharmaceutically acceptable salt or solvate thereof, in a low dosage amount. Also encompased by the invention is a a pharmaceutical formulation in unit dosage form comprising, per unit dosage, a low dosage amount.
    Type: Grant
    Filed: March 2, 1994
    Date of Patent: December 26, 1995
    Assignee: Eli Lilly and Company
    Inventor: Michael W. Draper
  • Patent number: 5474999
    Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof, which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the amides and pharmaceutical compositions containing them.
    Type: Grant
    Filed: October 26, 1994
    Date of Patent: December 12, 1995
    Assignee: Imperial Chemical Industries PLC
    Inventors: Keith Russell, Cyrus J. Ohnmacht, Keith H. Gibson
  • Patent number: 5475022
    Abstract: Compounds of Formula 1 ##STR1## wherein m is 1-4; R.sub.1 --R.sub.4 independently are hydrogen, lower alkyl of 1 to 6 carbons, Cl, Br, or I; R.sub.5 is hydrogen, lower alkyl of 1 to 6 carbons, Cl, Br, I, lower alkoxy or lower thioalkoxy of 1-6 carbons; R.sub.6 is hydrogen, lower alkyl, Cl, Br, I, OR.sub.11, SR.sub.11, OCOR.sub.11, SCOR.sub.11, NH2, NHR.sub.11, N(R.sub.11).sub.2, NHCOR.sub.11 OR NR.sub.11 --COR.sub.11 ; R.sub.20 is independently hydrogen or lower alkyl; Y is an aromatic group such as phenyl or naphthyl, or a heteroaryl group selected from a group consisting of pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl and oxazolyl; A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.
    Type: Grant
    Filed: October 18, 1993
    Date of Patent: December 12, 1995
    Assignee: Allergan, Inc.
    Inventor: Roshantha A. Chandraratna
  • Patent number: 5466690
    Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## where R is hydrogen or lower alkyl; A is pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl or pyrazinyl; n is 0-5; and B is H, --COOH or an ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative thereof, or --CHO or an acetal derivative thereof, or --COR.sub.1 or a ketal derivative thereof where R.sub.1 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 18, 1994
    Date of Patent: November 14, 1995
    Assignee: Allergan, Inc.
    Inventor: Roshantha A. S. Chandraratna
  • Patent number: 5459157
    Abstract: A pharmaceutical aqueous solution for ophthalmic use comprising a nonsteroidal anti-inflammatory drug, having a carboxylic group, a decongestant drug and a mixture of a polysorbate and a poloxamer.
    Type: Grant
    Filed: March 21, 1994
    Date of Patent: October 17, 1995
    Assignee: Zambon Group S.p.A.
    Inventors: Federico Stroppolo, Daniele Bonadeo, Luigi Virgano', Annibale Gazzaniga
  • Patent number: 5457237
    Abstract: Certain dihydroxyindanone compounds, and their pharmaceutically-acceptable salts, are inhibitors of tyrosine kinase enzymes, and so are useful for the control of tyrosine kinase dependent diseases (e.g., cancer, atherosclerosis).
    Type: Grant
    Filed: November 23, 1993
    Date of Patent: October 10, 1995
    Assignee: Pfizer Inc.
    Inventor: Robert L. Dow
  • Patent number: 5455265
    Abstract: Process of treatment of mammals, including humans to treat diseases or conditions of the type which are normally treated with retinoid-like compounds is disclosed, with pharmaceutical compositions containing an active compound which is a selective agonist of the RXR retinoid receptor sites in preference to the RAR retinoid receptor sites. A compound is defined to be a selective agonist of the RXR receptor site if the compound is at least approximately ten times more effective as an agonist in the RXR receptor sites than in the RAR receptor sites.
    Type: Grant
    Filed: February 11, 1993
    Date of Patent: October 3, 1995
    Assignee: Allergan, Inc.
    Inventor: Roshantha A. S. Chandraratna
  • Patent number: 5455273
    Abstract: The invention relates to N,N-disubstituted arylcycloalkylamines of general formula ##STR1## wherein n, m, A, X and R.sup.1 to R.sup.7 are defined as in claim 1, the isomers, isomer mixtures and salts thereof, which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis.
    Type: Grant
    Filed: November 19, 1993
    Date of Patent: October 3, 1995
    Assignee: Karl Thomae GmbH
    Inventors: Roland Maier, Peter Muller, Eberhard Woitun, Rudolf Hurnaus, Michael Mark, Bernhard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
  • Patent number: 5447941
    Abstract: A method of inhibiting pulmonary hypertensive disease 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, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.
    Type: Grant
    Filed: December 21, 1993
    Date of Patent: September 5, 1995
    Assignee: Eli Lilly and Company
    Inventor: Steven H. Zuckerman
  • Patent number: 5446067
    Abstract: Oxime ethers of the formula ##STR1## wherein m, G, R, R.sup.1, X, Y, and Z are as defined herein and fungicides containing these compounds.
    Type: Grant
    Filed: July 12, 1994
    Date of Patent: August 29, 1995
    Assignee: BASF Aktiengesellschaft
    Inventors: Remy Benoit, Hubert Sauter, Reinhard Kirstgen, Gisela Lorenz, Eberhard Ammermann
  • Patent number: 5444085
    Abstract: The present invention discloses compounds which substantially inhibit HIV or the activation of HIV in HIV-infected individuals. The compounds, their derivatives, and pharmacologic salts may be formulated into a pharmacologic agent to treat HIV infections. These pharmacologic agents may be used to treat immunosuppression, and other diseases of the immune system. The present invention also provides methods for preparing the compounds and formulating the compounds into pharmacologic agents.
    Type: Grant
    Filed: December 19, 1994
    Date of Patent: August 22, 1995
    Assignee: Warner-Lambert Company
    Inventors: David T. Connor, Stephen J. Gracheck, Leonard Post
  • Patent number: 5439925
    Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function. Use is in human and veterinary medicine and in cosmetics.
    Type: Grant
    Filed: December 16, 1993
    Date of Patent: August 8, 1995
    Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)
    Inventors: Jean-Michel Bernardon, Willliam R. Pilgrim
  • Patent number: 5434180
    Abstract: The present invention relates to new polycyclic aromatic derivatives, to processes for their preparation and to their use in therapeutic and cosmetic formulations.
    Type: Grant
    Filed: March 27, 1992
    Date of Patent: July 18, 1995
    Assignee: Centre International de Recherches Dermatologiques Galderma (CIRD Galderma)
    Inventors: Braham Shroot, Jacques Eustache, Oliver Watts, Jean-Michel Bernardon, Philippe Nedoncelle
  • Patent number: 5434151
    Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: August 24, 1992
    Date of Patent: July 18, 1995
    Assignee: CytoMed, Inc.
    Inventors: Xiong Cai, Sajjat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
  • Patent number: 5424323
    Abstract: A biocidal, aqueous composition for killing bacteria, spores, fungi, and viruses on nonabsorbent surfaces comprises at least one quaternary ammonium compound, at least one aliphatic dialdehyde having from two to six carbon atoms, and at least one aliphatic hydroxyl compound having form one to eight carbon atoms.This sterilant is stable for weeks, is especially useful between pH 4 to 9, and may additionally comprise a chelating agent.
    Type: Grant
    Filed: March 23, 1994
    Date of Patent: June 13, 1995
    Assignee: Cetylite Industries, Inc.
    Inventors: Stanley L. Wachman, Sidney Karlan
  • Patent number: 5413997
    Abstract: A triphenylmethane derivative represented by the following general formula: ##STR1## exhibits bone absorption inhibiting effects and is useful as a medicament for treating osteoporosis.
    Type: Grant
    Filed: January 21, 1993
    Date of Patent: May 9, 1995
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Iwao Kinoshita, Daisuke Machii, Yasuo Onoda, Haruki Takai, Nobuo Kosaka, Katsuichi Shuto, Katsushige Gomi, Makoto Morimoto, Akio Ishii
  • Patent number: 5401510
    Abstract: Methods for preventing and treating corneal haze resulting from exposure of the eye to laser irradiation are disclosed. The methods include administration of compositions of wound healing modulators to the eye. Compositions for use in preventing and treating the corneal haze are also disclosed.
    Type: Grant
    Filed: July 25, 1994
    Date of Patent: March 28, 1995
    Assignee: Alcon Laboratories, Inc.
    Inventors: Stella M. Robertson, Herman M. Kunkle, Jr.
  • Patent number: 5399586
    Abstract: Retinoid-like compounds which act as agonists of the RXR retinoid receptor sites induce apoptosis of tumor cells in cell cultures, and are used as drugs to treat tumors in mammals including humans. Compounds which are specific agonists of RXR receptors and also compounds which are agonists of both RAR and RXR agonist (pan-agonists) induce apoptosis, although the RXR agonist compounds are preferred as drugs to avoid undesirable side effects associated with RAR agonist activity. The RXR agonists compounds are administered to mammals afflicted with tumors in pharmaceutical compositions adapted for systemic topical or for intralesional administration. The range of concentration of the active ingredient RXR agonist compound in the pharmaceutical compositions is approximately between 0.001 and 5 percent by weight, and such that the composition delivers approximately 0.1 mg to 100 mg of the active ingredient per kg body weight of the patient, per day of treatment.
    Type: Grant
    Filed: March 11, 1993
    Date of Patent: March 21, 1995
    Assignee: Allergan, Inc.
    Inventors: Peter A. J. Davies, Roshantha A. Chandraratna
  • Patent number: 5393763
    Abstract: The current invention provides methods and pharmaceutical formulations that are useful for inhibiting the loss of bone. These methods and formulations can be used without the associated adverse effects of estrogen therapy, and thus serve as an effective and acceptable treatment for osteoporosis.
    Type: Grant
    Filed: January 12, 1994
    Date of Patent: February 28, 1995
    Assignee: Eli Lilly and Company
    Inventors: Larry J. Black, George J. Cullinan
  • Patent number: 5369124
    Abstract: Novel substituted thiophenecarboxamides of the formula (I), ##STR1## in which R represents hydrogen or alkyl,A represents doubly linked alkanediyl,Ar represents optionally substituted aryl andn represents a number 0 or 1,with the exception of the compounds 4,5-dibromo-thiophene-2-carboxylic acid N-(4-bromophenyl)-amide, 4,5-dibromo-thiophene-2-carboxylic acid N-(2,3-dichlorophenyl)-amide and 4,5-dibromo-thiophene-2-carboxylic acid N-[2-(3,4-dimethoxyphenyl)-ethyl]-amide, and their use for combating pests.The novel compounds are described by the formula (I) and they can be prepared by analogous processes, e.g. by reacting suitable thiophenecarbonyl halides with suitable amines.
    Type: Grant
    Filed: September 24, 1993
    Date of Patent: November 29, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans-Ludwig Elbe, Ralf Tiemann, Gerd Hanssler
  • Patent number: 5362747
    Abstract: 2-Nitroaryl or 2-cyanoaryl compounds of the formula ##STR1## pharmaceutical compositions thereof, intermediates useful in the preparation of these compounds, and methods for treating disorders of vascular smooth muscles or diseases of the cartilage, macrophages, neurons, platelets, bronchial smooth muscles, optic muscles and gastrointestinal smooth muscles, in addition to sickle cell anemia, diabetes, synovitis, chondroarthritis and osteoarthritis by employing these compounds.
    Type: Grant
    Filed: November 3, 1993
    Date of Patent: November 8, 1994
    Assignee: Abbott Laboratories
    Inventors: Marlon Cowart, James F. Kerwin
  • Patent number: 5360611
    Abstract: Methods for treating the cornea following UV laser irradiation and resulting photoablation of corneal tissue are disclosed. The methods include administration of compositions of a non-steroidal antiinflammatory to the eye. Compositions for use in treating the cornea are also disclosed.
    Type: Grant
    Filed: August 4, 1993
    Date of Patent: November 1, 1994
    Assignee: Alcon Laboratories, Inc.
    Inventors: Stella M. Robertson, Herman M. Kunkle, Jr.
  • Patent number: 5358938
    Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl terahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiphenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: July 13, 1992
    Date of Patent: October 25, 1994
    Assignee: CytoMed, Inc.
    Inventors: Xiong Cai, Saijat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
  • Patent number: 5344838
    Abstract: A biocidal, aqueous composition for killing bacteria, spores, fungi, and viruses on nonabsorbent surfaces comprises at least one quaternary ammonium compound, at least one aliphatic dialdehyde having from two to six carbon atoms, and at least one aliphatic hydroxyl compound having form one to eight carbon atoms.This sterilant is stable for weeks, is especially useful between pH 4 to 9, and may additionally comprise a chelating agent.
    Type: Grant
    Filed: December 8, 1993
    Date of Patent: September 6, 1994
    Assignee: Cetylite Industries, Inc.
    Inventors: Stanley L. Wachman, Sidney Karlan
  • Patent number: 5334602
    Abstract: New aryloxy-alkylamine derivatives of the general formula I ##STR1## in which A signifies a benzene or thiophene ring, R and R.sub.1, independently of one another, each hydrogen, alkyl, halogen, CF.sub.3 or alkoxy, R.sub.2 alkyl, cycloalkyl, alkenyl, alkynyl, alkaryl or saturated or unsaturated aliphatic or aromatic acyl, R.sub.3 and R.sub.4 in each case hydrogen, alkyl, alkenyl, alkynyl or cycloalkyl with, in each case, up to 8 C-atoms, whereby R.sub.3 and R.sub.4 can be the same or different but are not simultaneously hydrogen or R.sub.3 and R.sub.4, together with the nitrogen atom connecting them, form a 5- to 7-membered saturated ring or a saturated heterocyclic ring which can possibly contain an oxygen or nitrogen atom as a further heteroatom in the ring, whereby an additional nitrogen atom can be substituted by an alkyl radical with up to 3 C-atoms, and their acid-addition salts possess interesting pharmaceutical properties and are especially suitable as anti-arrhythmics.
    Type: Grant
    Filed: September 3, 1991
    Date of Patent: August 2, 1994
    Assignee: Laevosan-Gesellschaft GmbH
    Inventors: Bernhard Lotz, Gerhard Greier
  • Patent number: 5330981
    Abstract: This application describes 3-arylalkyl esters of 4,5-dihydro-9,10-dioxo-2-anthracenecarboxylic acid and a process for making them. Also described is a method of using the compounds in the treatment of arthritis.
    Type: Grant
    Filed: December 30, 1992
    Date of Patent: July 19, 1994
    Assignee: Istituto Gentili S.p.A.
    Inventors: Sergio Rosini, Maurizio Mian
  • Patent number: 5331011
    Abstract: Disclosed is an N-benzyl-N-phenoxyethylamine selected from the group consisting of the N-benzyl-N-phenoxyethylamine represented by the following formula (I): ##STR1## and an agriculturally acceptable acid addition salt represented by the following formula (II): ##STR2## wherein m represents a number of 1 or 2 with a proviso that when m is 1 and a chlorine atom in the ring A is present at para(4)-position of the ring A, two chlorine atoms in the ring B are present at 2,3-, 2,5-, 2,6-, 3,4- or 3,5-positions of the ring B, and HX represents an acid.
    Type: Grant
    Filed: April 7, 1993
    Date of Patent: July 19, 1994
    Assignee: Mitsubishi Gas Chemical Co., Inc.
    Inventors: Mitsunori Oda, Kazutoshi Kikkawa, Akinori Tanaka, Satoko Imaruoka, Shigeo Yoshinaka
  • Patent number: 5292767
    Abstract: A compound of the formula [I] and pharmaceutically acceptable salts thereof; and a synthetic intermediate represented by the formula [II] and pharmaceutically acceptable salts thereof, ##STR1## wherein R 1 is hydrogen or lower alkyl;R 2 is hydrogen or a protective group of thiol;R 3 is hydroxy, a remainder of ester group or a remainder of amido group;A is straight or branched lower alkylene, andthe sulfur atom in the side chain may be directly join with --CO-- to conform a thiolactone ring.The compounds of this invention have excellent thymulin-like activities and are expected to be useful for treatment of various immune disorders such as immunodeficiency and autoimmune diseases.
    Type: Grant
    Filed: February 18, 1993
    Date of Patent: March 8, 1994
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Shiro Mita, Yoichi Kawashima, Nobuharu Kato, Hiroshi Suhara, Koji Yoneda, Masataka Morishita
  • Patent number: 5286750
    Abstract: Unsaturated phenylacetic acid derivatives of the general formula ##STR1## where U is .dbd.O, .dbd.CH--OCH.sub.3, .dbd.N--OCH.sub.3, .dbd.N--NH--CH.sub.3, .dbd.CH.sub.2, .dbd.CH--CH.sub.3, .dbd.CH--CH.sub.2 --CH.sub.3 or .dbd.CH--S--CH.sub.3 andZ.sup.1 and Z.sup.2 are hydrogen, halogen, trifluoromethyl, cyanide, NO.sub.2 or unsubstituted or substituted alkyl, alkenyl, aryl, alkynyl, alkoxy, aryloxy, arylalkoxy, acyloxy, hetaryl, --CO.sub.2 R.sup.1, --CONR.sup.2 R.sup.3, COR.sup.4 or NR.sup.5 R.sup.6, and Z.sup.1 and Z.sup.2 may also form a ring,A is meta or para and is (CH.sub.2).sub.n, CH.dbd.CH, O--(CH.sub.2).sub.n, O--(CH.sub.2).sub.n --CO, CH.sub.2 --O--CO--(CH.sub.2).sub.n, CO--O--(CH.sub.2).sub.n, O--CO--(CH.sub.2).sub.n, O--(CH.sub.2).sub.n --CO--O, O--(CH.sub.2).sub.n+2 --O, CH.sub.2 O--(CH.sub.2).sub.n, CH.sub.2 --S--(CH.sub.2).sub.n CH.sub.2 --NR.sup.7 --(CH.sub.2).sub.n, CH(CN)--O--CO--(CH.sub.2).sub.n, CH.dbd.N--(CH.sub.2).sub.n or CH.dbd.N--O--(CH.sub.2).sub.n.
    Type: Grant
    Filed: March 15, 1993
    Date of Patent: February 15, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Mueller, Hubert Sauter, Eberhard Ammermann, Gisela Lorenz, Franz Roehl
  • Patent number: 5271939
    Abstract: Methods for preventing and treating corneal haze resulting from exposure of the eye to laser irradiation are disclosed. The methods include administration of compositions of wound healing modulators to the eye. Compositions for use in preventing and treating the corneal haze are also disclosed.
    Type: Grant
    Filed: April 10, 1992
    Date of Patent: December 21, 1993
    Assignee: Alcon Laboratories, Inc.
    Inventors: Stella M. Robertson, Herman M. Kunkle, Jr.
  • Patent number: 5270301
    Abstract: The present invention relates to certain fluoro-amide derivatives, as described herein, which are human leukocyte elastase (HLE) inhibitors making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated, including treatment of tissue degenerative diseases such as pulmonary emphysema. The invention also includes intermediates useful in the synthesis of these fluoro-amide derivatives, processes for preparing them, pharmaceutical compositions containing such peptide derivatives and methods for their use.
    Type: Grant
    Filed: May 7, 1990
    Date of Patent: December 14, 1993
    Assignee: ICI Americas Inc.
    Inventor: Donald J. Wolanin
  • Patent number: 5246962
    Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## where R is hydrogen or lower alkyl; A is pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl or pyrazinyl; n is 0-5; and B is H, --COOH or an ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative thereof, or --CHO or an acetal derivative thereof, or --COR.sub.1 or a ketal derivative thereof where R.sub.1 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 21, 1992
    Date of Patent: September 21, 1993
    Assignee: Allergan, Inc.
    Inventor: Roshantha A. S. Chandraratna
  • Patent number: 5192753
    Abstract: This invention pertains to the novel use of anti-rheumatoid arthritic drugs in the treatment of dementia. A method of treating dementia in human beings which comprises administering to the human being a therapeutic amount of a non-steroidal anti-inflammatory drug (NSAID) which has the ability to inhibit prostaglandin synthesis in the human being.
    Type: Grant
    Filed: April 23, 1991
    Date of Patent: March 9, 1993
    Inventors: Patrick L. McGeer, Joseph Rogers, John Sibley, Edith McGeer
  • Patent number: 5183818
    Abstract: The present invention provides compounds having the structureY-Het-[Q.sub.1 ]-X-[Q.sub.2 ]-Zwhich inhibit the catalytic action of lipoxygenase enzymes, particularly 5-lipoxygenase, and thereby reduce the biosynthesis of leukotrienes B.sub.4, C.sub.4, D.sub.4, and E.sub.4.In the generic formula given above, X is oxygen or sulfur and Het is a heteroaryl group selected from the group consisting of furyl, thienyl, 2-, 3-, and 4-pyridyl, 2- and 3-benzo[b]furyl, 2- and 3-benzo[b]thienyl and thienothienyl.Y is one or two substituents independently selected from hydrogen, hydroxy, halogen, cyano, alkyl, haloalkyl, alkoxy, alkylthio, alkoxyaryl), alkylthioaryl, arylalkoxy, arylalkylthio, aryloxy, arylthio, alkylamido, cycloalkyl, alkanoyl, alkoxycarbonyl, amino, alkylamino, dialkylamino, and the following groups wherein R, at each occurrence, is independently selected from hydrogen and alkyl of from one to six carbon atoms: --CRROR, --NRC(O)R, --NRC(O)OR, and --C(O)NRR.The group Q.sub.
    Type: Grant
    Filed: August 27, 1991
    Date of Patent: February 2, 1993
    Assignee: Abbott Laboratories
    Inventors: Dee W. Brooks, Andrew O. Stewart, Jonathan G. Martin
  • Patent number: 5175183
    Abstract: Certain N-aryl, N-heteroaryl-, N-arylalkyl-, N-heteroarylalkyl-, N-arylcyclopropyl- and N-heteroaryl-cyclopropyl-N'-hydroxyurea compounds are inhibitors of lipoxygenase enzyme activity and are thus useful agents in treating disease states such as asthma, arthritis, allergy, psoriasis, inflammatory bowel disease, gout, adult respiratory distress syndrome, endotoxin shock, and other inflammatory conditions in which the products of the arachidonic acid cascade are implicated.
    Type: Grant
    Filed: July 10, 1991
    Date of Patent: December 29, 1992
    Assignee: Abbott Laboratories
    Inventors: Dee W. Brooks, James B. Summers, Karen E. Rodriques
  • Patent number: 5175185
    Abstract: Retinoid like activity is exhibited by compounds of the formula ##STR1## R.sub.1 -R.sub.3 independently are hydrogen, lower alkyl, cycloalkyl or lower alkenyl, A and A.sub.1 independently are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, SR.sub.4 or OR.sub.4 where R.sub.4 is lower alkyl, cycloalkyl or lower alkenyl; Y is selected from a group consisting of thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl or oxazolyl; E is lower alkenyl, lower alkynyl, lower cycloalkyl, lower branched chain alkyl, or is characterized by the formula (CH.sub.2).sub.n where n is 0-5, and Z is H, OH, OR.sub.5, OCOR.sub.5, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH, CH.sub.2 OR.sub.6, CH.sub.2 OCOR.sub.6, or --CHO, CH(OR.sub.7).sub.2, CHOR.sub.8 O, or COR.sub.9, CR.sub.9 (OR.sub.7).sub.2, CR.sub.9 OR.sub.8 O where R.sub.5 is lower alkyl, phenyl or lower alkylphenyl, R.sub.6 is lower alkyl, phenyl or lower alkylphenyl, R.sub.7 is lower alkyl, R.sub.
    Type: Grant
    Filed: March 14, 1991
    Date of Patent: December 29, 1992
    Assignee: Allergan, Inc.
    Inventor: Roshantha A. S. Chandraratna
  • Patent number: 5149705
    Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## where R is hydrogen or lower alkyl; A is pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl or pyrazinyl; n is 0-5; and B is H, --COOH or an ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative thereof, or --CHO or an acetal derivative thereof, or --COR.sub.1 or a ketal derivative thereof where R.sub.1 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 13, 1987
    Date of Patent: September 22, 1992
    Assignee: Allergan, Inc.
    Inventor: Roshantha A. S. Chandraratna
  • Patent number: 5124356
    Abstract: The dermal use of non-irritating retinoids such as the esters and amides of 13-cis and 13-trans-retinoic acid for effecting the reduction and reversal of photoaging and skin cancer is disclosed.
    Type: Grant
    Filed: November 6, 1990
    Date of Patent: June 23, 1992
    Assignee: Molecular Design International, Inc.
    Inventors: William P. Purcell, Harlie A. Parish, Jr.
  • Patent number: RE34075
    Abstract: The dermal use of non-irritating retinoids such as the esters and amides of 13-cis and 13-trans-retinoic acid for effecting the reduction and reversal of photoaging and skin cancer is disclosed.
    Type: Grant
    Filed: July 18, 1991
    Date of Patent: September 22, 1992
    Assignee: Molecular Design International, Inc.
    Inventors: William P. Purcell, Harlie A. Parish