Patents Examined by Mary C. Cebulak
  • Patent number: 5480857
    Abstract: 4-heteroaroylisoxazole derivatives of formula I: ##STR1## wherein: Ar represents an optionally substituted group Het, wherein Het represents a first heterocyclic ring containing from one to four heteroatoms in the ring selected from oxygen, nitrogen and sulphur, which is optionally fused with a benzene, or carbocyclic or second heterocyclic ring (which is optionally saturated or partially saturated) to form a bicyclic system, wherein the first heterocyclic ring of the group Het is attached to the carbonyl group in the 4-position of the isoxazole ring;R represents hydrogen or --CO.sub.2 R.sup.3 ;R.sup.1 represents alkyl or haloalkyl or a cycloalkyl group optionally substituted by one or more groups R.sup.4 ;R.sup.3 and R.sup.4 independently represent alkyl or haloalkyl;agriculturally acceptable salts thereof and their use in weed control is described.
    Type: Grant
    Filed: September 17, 1993
    Date of Patent: January 2, 1996
    Assignee: Rhone-Poulenc Agriculture Limited
    Inventors: Susan M. Cramp, Philip H. G. Smith
  • Patent number: 5478959
    Abstract: A method for preparing 1,4-(Z,Z)-disubstituted-1,4-disulfurated-1,3-butadienes is disclosed. The butadienes can be further elaborated to provide 3,6-unsymmetrically-substituted-1,2-dithiins. Also disclosed are butadienes prepared by the method of the invention. These butadienes are useful as intermediates in the synthesis of antibiotic 1,2-dithiins.
    Type: Grant
    Filed: October 5, 1994
    Date of Patent: December 26, 1995
    Assignee: The Research Foundation of State University of New York
    Inventors: Eric Block, Chuangxing Guo
  • Patent number: 5470846
    Abstract: A method of treating neurological and mental disorders which are associated with and/or related pathogenetically to deficient serotonin neurotransmission and impaired pineal melatonin functions in humans is described which comprises administering to a human in need thereof an effective amount of a composition which increases serotonin transmission to the patient to be treated followed by the application to the brain of the patient of a sufficient amount of an AC pulsed magnetic field of proper intensity and frequency to treat the disorder.
    Type: Grant
    Filed: January 14, 1994
    Date of Patent: November 28, 1995
    Inventor: Reuven Sandyk
  • Patent number: 5464863
    Abstract: An N-heteroaryl-N'-phenylurea derivative represented by the general formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are as defined in the description of the specification which is useful as a prophylactic and therapeutic agent for hypercholesterolemia, atherosclerosis and diseases caused by them.
    Type: Grant
    Filed: September 24, 1994
    Date of Patent: November 7, 1995
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Masashi Nagamine, Kenji Yamamoto, Yoshimitsu Matsui, Kenji Horiuchi, Masanori Yoshida
  • Patent number: 5463081
    Abstract: The invention relates to novel intermediates for the preparation of a certain group of novel phenylsulfonylurea herbicides, which herbicides are particularly advantageous for use in crop protection. The novel intermediate compounds are of the formula II ##STR1## and of the formula VI, ##STR2## as defined in the specification and claims. The intermediate compounds may be used to prepare herbicidal and plant growth regulating compounds of the formula I or salts thereof: ##STR3## as defined in the specification. The herbicides so obtained are particularly suitable for selectively controlling weeds.
    Type: Grant
    Filed: September 21, 1993
    Date of Patent: October 31, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Oswald Ort, Klaus Bauer, Hermann Bieringer
  • Patent number: 5456901
    Abstract: Liposomes suitable as ultrasound contrast agents which contain media of various types including gases, gaseous precursors activated by pH, temperature or pressure, as well as other solid or liquid contrast enhancing agents, are described. Methods of using the same as ultrasound contrast agents are also disclosed. The present invention also comprises novel methods for synthesizing liposomes having encapsulated therein gases.
    Type: Grant
    Filed: February 28, 1995
    Date of Patent: October 10, 1995
    Inventor: Evan C. Unger
  • Patent number: 5455264
    Abstract: RS-thioctic acid with a novel morphology which is obtained by a recrystallization process.
    Type: Grant
    Filed: October 12, 1993
    Date of Patent: October 3, 1995
    Assignee: ASTA Medica Aktiengesellschaft
    Inventors: Thomas Beisswenger, Horst Bethge, Joachim Goede, Frank Hubner, Klaus Huthmacher, Herbert Klenk, Roland Moller
  • Patent number: 5453540
    Abstract: Fluorochemical compositions comprising fluorinated compounds, wherein the fluorinated compound comprises fluorochemical oligomeric portion, an organic moiety, and a group that can impart soft hand, stain release, water repellency, or a durable property when the compound is applied to a fibrous substrate, wherein the fluorochemical oligomeric portion is bonded to the organic moiety through an isocyanate-derived linking group. Also disclosed are fluorochemical compositions in the form of fluorochemical liquid dispersions and methods for preparing substrates treated with such compositions. Substrates so treated exhibit particularly durable and abrasion-resistant oil and water repellent properties. Intermediates in the preparation of the fluorochemical compositions are also disclosed. Some of the intermediates are useful as emulsifiers in fluorochemical liquid dispersions.
    Type: Grant
    Filed: November 29, 1993
    Date of Patent: September 26, 1995
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Rudolf J. Dams, Johan E. De Witte
  • Patent number: 5451566
    Abstract: Herbicidal 1-aryl pyrrolopyridine compounds of the formula: ##STR1## wherein at least one of Y, Z or J is N or N--O and the remainder of Y, Z or J is C--R.
    Type: Grant
    Filed: November 17, 1993
    Date of Patent: September 19, 1995
    Assignee: Zeneca Limited
    Inventor: Christopher J. Mathews
  • Patent number: 5445813
    Abstract: Disclosed are injectable suspensions of gas filled microbubbles in an aqueous carrier liquid usable as contrast agents in ultrasonic echography. The suspensions comprise amphipathic compounds of which at least one may be a laminarized phospholipid as a stabiliser of the microbubbles against collapse with time and pressure. The concentration of phospholipids in the carrier liquid is below 0.01% wt but is at least equal to or above that at which phospholipid molecules are present solely at the gas microbubble-liquid interface. Also disclosed is a method of preparation of the stable suspensions of air or gas filled microbubbles.
    Type: Grant
    Filed: October 12, 1993
    Date of Patent: August 29, 1995
    Assignee: Bracco International B.V.
    Inventors: Michel Schneider, Jean Brochot, Jerome Puginier, Feng Yan
  • Patent number: 5444084
    Abstract: Substituted heterocyclic derivatives represented by the formula (I) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, Q.sup.1, Q.sup.2, Q.sup.3, Q.sup.4, X and Y are as defined, including, specifically, the compound (E)-3-[3-[3-(2-methoxymethyl-8,8-dimethyl-4-nonen-6-ynyl)phenoxymethyl]phe nyl]thiophene, exhibit squalene epoxidase inhibiting activity and are useful in the treatment or prophylaxis of hypercholesterolemia, hyperlipidemia and arteriosclerosis.
    Type: Grant
    Filed: February 11, 1994
    Date of Patent: August 22, 1995
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Yoshimi Tsuchiya, Takashi Nomoto, Morihiro Mitsuya, Katsumasa Nonoshita, Masahiro Hayashi, Toshihiko Satoh, Yoshio Sawasaki, Toshio Kamei
  • Patent number: 5444086
    Abstract: This invention relates to benzyl and naphthalenylmethyl thiophenones and cyclopentenones, some of which are novel, which have oral antihyperglycemic activity in diabetic mice, a genetic animal model of non-insulin dependent diabetes mellitus. These compounds are represented by the formula ##STR1## wherein: R.sup.2 and R.sup.3 are independently selected from hydrogen, C.sub.1-6 alkyl, halogen, C.sub.1-6 alkoxy, thio-C.sub.1-6 alkyl, or trifluoromethyl or R.sup.2 together with R.sup.3 forms a benzo ring fused to the phenyl ring and optionally substituted with one or two substituents independently selected from C.sub.1-6 alkyl, halogen, C.sub.1-6 alkoxy, thio-C.sub.1-6 alkyl, or trifiuoromethyl;R.sup.1 is selected from hydrogen, C.sub.1-6 alkyl, halogen, C.sub.1-6 alkoxy, thio-C.sub.1-6 alkyl, or trifluoromethyl;andR.sup.4 is selected from the group consisting of: ##STR2## wherein R.sup.5 is H or C.sub.1-6 alkyl or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 31, 1994
    Date of Patent: August 22, 1995
    Assignee: American Home Products Corporation
    Inventor: Michael S. Malamas
  • Patent number: 5440050
    Abstract: A process for the production of ambergris-type labdane spiroketals of general formulae I and II ##STR1## where R represents oxygen or sulphur, useful in the perfumery industry, the said process being characterized by the intramolecular cyclisation of the epoxyketone or its thio analog of general formula III ##STR2## where R.sub.1 represents COCH.sub.3 and R.sub.2 oxygen or sulphur.
    Type: Grant
    Filed: October 18, 1994
    Date of Patent: August 8, 1995
    Assignee: Givaudan-Roure Corporation
    Inventors: Maria do Ceu Goncalves da Costa, Maria J. V. de Oliveira Baptista Marcelo Curto, Maria R. de Loureiro da Silva Tavares da Rosa, William B. Motherwell
  • Patent number: 5428048
    Abstract: This invention relates to compounds which inhibit lipoxygenase in the metabolism of arachidonic acid and thus inhibits formation of leukotrienes which are implicated in inflammatory processes and bronchoconstriction and inhibits the oxidation of LDL which is implicated in formation of atherosclerotic plaque.The compounds useful in this invention are represented by the formula: ##STR1## wherein: R.sup.2 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl; Y of O or S; R.sup.5 is hydrogen or methyl R.sup.6 is --NH.sub.2, --CH.sub.3 or --OCH.sub.3 ;and R.sup.1 is ##STR2## wherein R.sup.7, R.sup.8 and R.sup.10 are independently halogen, trifluoromethyl, alkyl, alkoxy, methanesulfonyl or trifiuoromethanesulfonyl; R.sup.9 is hydrogen or methyl; and Z is O or S,or a pharmaceutically acceptable salt thereof.Compounds of the above formula where R.sup.1 is not ##STR3## when R.sup.3 is H and R.sup.6 is --NH.sub.2 are novel.
    Type: Grant
    Filed: November 8, 1993
    Date of Patent: June 27, 1995
    Assignee: American Home Products Corporation
    Inventors: Michael S. Malamas, Iwan Gunawan
  • Patent number: 5426115
    Abstract: A method of treatment for improving encephalic function which comprises administering, to a subject in need of such treatment, a 15-keto-prostaglandin compound in an amount effective for improvement of encephalic function.
    Type: Grant
    Filed: October 29, 1993
    Date of Patent: June 20, 1995
    Assignee: Kabushikikaisha Ueno Seiyaku Oyo Kenkyujo
    Inventors: Ryuji Ueno, Hiroyoshi Osama, Tomio Oda
  • Patent number: 5424325
    Abstract: Aminoketone derivatives according to the present invention strongly inhibit thiol protease such as calpain, papain, cathepsin B, cathepsin H, cathepsin L or the like and have excellent properties concerning absorbance on oral administration, tissue distribution and cell membrane permeability. The aminoketone derivatives cart thus be used as therapeutic agents for treating muscular dystrophy, cataract, cardiac infarction, stroke, Alzheimer's disease, amyotrophy, osteoporosis and hypercalcemia and so on. It may also be used as therapeutic agents for preventing metastasis of cancer. In addition, the present derivatives are also applicable as intermediates for the preparation of ketone derivatives, which have inhibitory activity against thiol protease.
    Type: Grant
    Filed: December 22, 1993
    Date of Patent: June 13, 1995
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Ryoichi Ando, Naoko Ando, Hirokazu Masuda, Toshiro Sasaki, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
  • Patent number: 5422359
    Abstract: Alpha-aminoketone derivatives of the present invention strongly inhibit thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L and calpain or the like and have excellent properties in absorbance on oral administration, tissue distribution and cell membrane permeability. The alpha-aminoketone derivatives can thus be used as therapeutic agents for treating muscular dystrophy, amyotrophy, cardiac infarction, stroke, Alzheimer's disease, disturbance of consciousness or dyskinesia caused upon brain trauma, multiple sclerosis, peripheral nervous neuropathy, cataract, inflammation, allergosis, fulminant hepatitis, osteoporosis, hypercalcemia, breast carcinoma, prostatic carcinoma or prostatomegaly. They may also be used as therapeutic agents for suppressing growth of cancer cells, preventing metastasis of cancer or suppressing aggregation of plaques.
    Type: Grant
    Filed: December 22, 1993
    Date of Patent: June 6, 1995
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Ryoichi Ando, Toshiro Sakaki, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao
  • Patent number: 5420151
    Abstract: 3-amino-5-carbamoylchromans and 8-fluoro-3-amino-5-carbamoylchromans, as well as enantiomers and salts thereof, are disclosed. Pharmaceutical compositions containing the compounds as active ingredients are also disclosed. The compounds are useful in the treatment of 5-hydroxytryptamine-mediated disorders of the central nervous system.
    Type: Grant
    Filed: October 28, 1993
    Date of Patent: May 30, 1995
    Assignee: Aktiebolaget Astra
    Inventors: Eva M. Hammarberg, Lars G. Johansson, Svante B. Ross, Seth-Olov Thorberg
  • Patent number: 5411970
    Abstract: A method of inhibiting lentivirus is disclosed which comprises mammalian host susceptible to said lentivirus with a virally inhibitory effective amount of an O-acylated derivative of 1,5-dideoxy-1,5-imino-D-glucitol and their N-alkyl, N-acyl and N-aroyl derivatives in which from one to four of the free hydroxyl groups are O-acylated with carboxylic alkanoyl radicals selected from the group consisting of .omega.,.omega.,.omega.-trifluoroalkanoyl having from three to eight carbon atoms, carboxylic cycloalkanoyl groups having from four to eight carbon atoms and carboxylic acyclic alkanoyl groups having from two to ten carbon atoms, wherein the N-aroyl groups contain from 7 to 14 carbon atoms, the N-acyl groups contain from 4 to 8 carbon atoms and the N-alkyl groups contain from 1 to 14 carbon atoms.
    Type: Grant
    Filed: December 21, 1993
    Date of Patent: May 2, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Partis, Francis J. Koszyk, Richard A. Mueller
  • Patent number: 5391753
    Abstract: Compounds of the formula ##STR1## where R.sub.1, R.sub.2, R.sub.3 and R.sub.4 independently are hydrogen, lower alkyl of 1-6 carbons, halogen or lower alkoxy of 1-6 carbons; R.sub.5 and R.sub.5 ' independently are hydrogen or lower alkyl of 1-6 carbons; Y is oxygen or sulfur; Z is n-alkyl having 1-10 carbons, cyclo or branch-chained alkyl of 3-10 carbons, and straight chain alkenyl having 2-10 carbons, or cyclo or branched chained alkenyl of 3-10 carbons; X is thienyl, pyridyl, 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.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, or CR.sub.
    Type: Grant
    Filed: September 27, 1993
    Date of Patent: February 21, 1995
    Assignee: Allergan, Inc.
    Inventor: Roshantha A. S. Chandraratna