Patents Examined by E. C. Ward
  • Patent number: 5145965
    Abstract: Novel 2,6-methanopyrrolo-3-benzazocines, intermediates, processes for the preparation thereof, and methods for alleviating pain utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: March 11, 1991
    Date of Patent: September 8, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Richard C. Allen, David G. Wettlaufer
  • Patent number: 5143920
    Abstract: Substituted 4-aminoquinazoline derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkoxy C.sub.1-6 alkyl,C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkyl C.sub.1-6 alkyl, phenyl C.sub.1-6 alkyl, the phenyl group being optionally substituted;R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, amino, C.sub.1-6 alkylthio, halogen, cyano, hydroxy, C.sub.1-6 alkanoyl or trifuromethyl;m is 1 to 3;R.sup.3 is hydrogen, C.sub.1-6 alkyl, phenyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-6 alkanoyl, amino, C.sub.1-6 alkylamino, ci-C.sub.1-6 alkylamino, halogen, trifluoromethyl or cyano;n is 1 or 2; andR.sup.4 is hydrogen; or a salt thereof are useful as inhibitors of gastric acid secretion.
    Type: Grant
    Filed: February 23, 1989
    Date of Patent: September 1, 1992
    Assignee: SmithKline Beckman Intercredit B.V.
    Inventors: Robert J. Ife, Thomas H. Brown, Colin A. Leach
  • Patent number: 5142046
    Abstract: An optically action pyridobenzoxazine derivative, a process for preparing the same and a novel intermediate useful for preparing the optically active pyridobenzoxazine derivative are disclosed. The optically active pyridobenzoxazine derivative possesses increased antimicrobial activity and reduced toxicity. The intermediate is useful for preparing such optically active pyridobenzoxazine derivatives such as Ofloxacin and anolog compounds.
    Type: Grant
    Filed: August 28, 1991
    Date of Patent: August 25, 1992
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Isao Hayakawa, Shohgo Atarashi, Masazumi Imamura, Shuichi Yokohama, Nobuyuki Higashihashi, Katsuichi Sakano, Masayuki Ohshima
  • Patent number: 5142052
    Abstract: Aryl- and heterocyclic-methanamines are prepared by reacting a hydroxy-aryl carbinol or a heterocyclic carbinol with a primary or a secondary amine in the presence of a cationic effect reagent.
    Type: Grant
    Filed: October 21, 1988
    Date of Patent: August 25, 1992
    Assignee: Laboratoires Syntex
    Inventors: Serge Beranger, Bruno Francois
  • Patent number: 5141945
    Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl or lower alkenyl, R.sup.2 is hydrogen, lower alkyl, or halogen, R.sup.3 is imidazolyl or pyridyl, each of which may have suitable substituents, and R.sup.4 is hydrogen, lower alkyl, lower alkenyl or hydroxy (lower) alkyl and R.sup.5 is hydrogen, hydroxy, or alkanoyloxy, or R.sup.4 and R.sup.5 are linked together to form an additional bond or novel pyridoindole derivatives which are useful as potent in selective antagonists of 5-HT receptors.
    Type: Grant
    Filed: September 20, 1989
    Date of Patent: August 25, 1992
    Assignee: Fujisawa Pharmaceutical Company, Ltd.
    Inventors: Masayuki Kato, Kiyotaka Ito, Hisashi Takasugi
  • Patent number: 5141936
    Abstract: Pyrimido-(6,1-a)-isoquinolin-4-one derivatives of the formula ##STR1## in which the substituents R.sup.1 -R.sup.6 have the meanings mentioned, are suitable for the prevention of hair loss and for strengthening hair growth.
    Type: Grant
    Filed: May 17, 1989
    Date of Patent: August 25, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Richard H. Rupp, Bansi Lal
  • Patent number: 5136059
    Abstract: Propoxybenzene derivatives represented by the following formula ##STR1## wherein Ra represents a nitro group, an amino group which may have a protecting group or an --NHCH.dbd.C(COO--C.sub.1-6 -Alkyl).sub.2 group, Rb represents a hydrogen atom, a protecting group for the hydroxyl group or a substituted sulfonyl group and Xa and Xb, which may be the same or different, each represents a halogen atom, and processes for preparation thereof are disclosed. These derivatives are useful in preparing antibacterial agents.
    Type: Grant
    Filed: December 27, 1988
    Date of Patent: August 4, 1992
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Toshihiro Fujiwara, Tutomu Ebata
  • Patent number: 5135737
    Abstract: Disclosed are amplifier molecules: various organic compounds having branched structures terminating with amine groups to which pharmacologically active groups can be chemically attached. A number of MRI contrast-enhancing agents were synthesized, each comprising plural active groups, such as stable nitroxides and complexes of trivalent metal cations. Such syntheses were successfully performed using a number of amplifiers having different branched structures, demonstrating the general utility of the pertinent chemistry in the synthesis of amplifiers having any of a wide variety of pharmacologically active groups. Amplifiers were also synthesized having linkers terminating with chemically reactive groups such as isothiocyanates, which render the amplifier bifunctional: attachable to polymers, biomacromolecules, or other biocompatible entity possessing multiple reactive sites such as terminal amines.
    Type: Grant
    Filed: September 5, 1989
    Date of Patent: August 4, 1992
    Assignee: The State of Oregon Acting by and through the State Board of Higher Education on behalf of the University of Oregon
    Inventor: John F. W. Keana
  • Patent number: 5135913
    Abstract: Methods and compositions for (a) improving and/or maintaining the health of skin, and (b) increasing subcutaneous fat in warm-blooded animals are disclosed. The methods utilize an effective amount of a composition comprising GHL-Cu or a derivative of GHL-Cu.
    Type: Grant
    Filed: June 16, 1988
    Date of Patent: August 4, 1992
    Assignee: ProCyte Corporation
    Inventor: Loren R. Pickart
  • Patent number: 5134135
    Abstract: 2'-Alkylsulfonylsteroido[2,3-d]oxazoles, for example 2'-methylsulfonyl-5.alpha.-pregn-2-en-20-yno[2,3-d]oxazol-17.beta.-ol, which are useful as antiandrogenic agents, and proceses for preparation, method of use and compositions thereof are disclosed.
    Type: Grant
    Filed: June 21, 1990
    Date of Patent: July 28, 1992
    Assignee: Sterling Drug Inc.
    Inventors: John P. Mallamo, Joseph R. Wetzel
  • Patent number: 5132299
    Abstract: New 11.beta. phenyl-4,9,15-estratrienes of formula I ##STR1## are described, where X implies an oxygen atom or a hydroxyimino grouping N.about.OH,R.sup.1 stands for a hydrogen atom or a methyl group,R.sup.2 implies a hydrogen atom, an alkyl radical or an acyl radical with in each case 1 to 10 carbon atoms,R.sup.3 stands for a hydrogen atom, a cyanomethyl group, --(CH.sub.2).sub.n CH.sub.2 Z where n implies the numbers 0, 1, 2, 3, 4 or 5, Z=--H or --OR.sup.5 with R.sup.5 having the significance of a hydrogen atom or an alkyl or acyl group with in each case 1 to 10 carbon atoms, or for --(CH.sub.2).sub.m --C.tbd.C--Y where m=0-2 and Y implies a hydrogen, chlorine, fluorine, iodine or bromine atom, an alkyl, hydroxyalkyl, alkoxyalkyl or acyloxyalkyl group with in each case 1 to 10 carbon atoms,R.sup.4 represents a straight-chain or branched-chain, saturated or unsaturated hydrocarbon radical with up to 8 carbon atoms which contains the grouping ##STR2## with X having the above significance.
    Type: Grant
    Filed: January 16, 1990
    Date of Patent: July 21, 1992
    Assignee: Schering Aktiengesellschaft
    Inventors: Eckhard Ottow, Helmut Hofmeister, Stefan Scholz, Guenter Neef, Walter Elger, Sybille Beier, Krzysztof Chwalisz
  • Patent number: 5132101
    Abstract: Dihydro- and tetrahydro-acetylene-cumulene porphycene compounds having the structure shown below ##STR1## are useful as photogynamic therapy agents.
    Type: Grant
    Filed: September 6, 1990
    Date of Patent: July 21, 1992
    Assignee: Cytopharm, Inc.
    Inventors: Emanuel Vogel, Alexander D. Cross, Norbert Jux, Eduardo Rodriguez-Val, Stefan Boehm, Wolfgang Hennig
  • Patent number: 5132423
    Abstract: Reactions between a solid polar and a non-polar compound, especially nucleophilic aromatic substitution reactions between an alkali metal salt of a hydroxyaromatic compound or thio analog thereof and an activated halo- or nitro-substituted aromatic compound, are conducted in a non-polar organic solvent such as toluene or xylene, in the presence of a hexaalkylguanidinium or .alpha.,.omega.-bis(pentaalkylguanidinium)alkane salt, or a corresponding heterocyclic salt, as a phase transfer catalyst. The method is particularly useful for the preparation of bisimides from bisphenol A or 4,4'-biphenol salts and 4-nitro- or 4-halophthalimides.
    Type: Grant
    Filed: March 13, 1991
    Date of Patent: July 21, 1992
    Assignee: General Electric Company
    Inventors: Daniel J. Brunelle, Deborah A. Haitko, James P. Barren, Sunita Singh
  • Patent number: 5128465
    Abstract: A cephem derivative represented by the following formula: ##STR1## wherein R.sub.1 means a fluorine-substituted lower alkyl and A.sub.1 denotes a cyclic or acyclic ammonio group, or a non-toxic salt thereof, is prepared by reacting a compound represented by the following formula: ##STR2## wherein A.sub.1 has the same meaning as defined above, with another compound represented by the following formula: ##STR3## wherein R.sub.1 has the same meaning as defined above, and if necessary, removing the protecting groups.
    Type: Grant
    Filed: January 22, 1990
    Date of Patent: July 7, 1992
    Assignee: Eisai Co., Ltd.
    Inventors: Takashi Kamiya, Toshihiko Naito, Yuuki Komatu, Yasunobu Kai, Takaharu Nakamura, Manabu Sasho, Shigeto Negi, Isao Sugiyama, Kanemasa Katsu, Hiroshi Yamauchi
  • Patent number: 5128070
    Abstract: Process for the acid-catalyzed hydrolysis of fatty acid glycerides, wherein the process is carried out continuously with the glyceride and the water being moved countercurrent to each other, and apparatus therefor.
    Type: Grant
    Filed: August 1, 1989
    Date of Patent: July 7, 1992
    Assignee: Henkel Kommanditgesellschaft auf Aktien
    Inventors: Reinhold Sedelies, Wilhelm Johannisbauer, Guenter Wozny, Lutz Jeromin, Gerhard Dieckelm, Manfred Lindemann, Gerd Matrong
  • Patent number: 5126354
    Abstract: Inhibiting leucotriene synthesis in patients with novel disubstituted (quinolin-3-yl-methoxy)phenylacetic acid derivatives of the formula ##STR1## in which A, B, D, E, G, K and M each independently is H, OH, halogen, CF.sub.3, OCF.sub.3, COOH, alkyl, alkoxycarbonyl or aryl,R.sup.1 is alkyl or cycloalkyl,R.sup.2 and R.sup.3 each independently is H, alkyl or aryl, andX is O or S,and salts thereof.
    Type: Grant
    Filed: August 1, 1990
    Date of Patent: June 30, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Mohrs, Siegfried Raddatz, Romanis Fruchtmann, Christian Kohlsdorfer, Reiner Muller-Peddinghaus, Pia Theisen-Popp
  • Patent number: 5120716
    Abstract: A percutaneous absorption promoting agent comprising (A) at least one anionic surfactant and one or two or more of surfactants having a nitrogen atom in the molecule other than anionic surfactants, (B) one or two or more of anionic surfactants and one or two or more of nonionic surfactants not having a nitrogen atom in the molecule, (C) one or two or more of surfactants selected from the group consisting of amphoteric surfactant and semi-polar surfactants and at least one nonionic surfactant having a nitrogen atom in the molecule, (D) one or two or more of surfactants selected from the group consisting of nonionic surfactants, amphoteric surfactants, semi-polar surfactants and cationic surfactants having a nitrogen atom in the molecule, and one or two or more of nonionic surfactants not having a nitrogen atom in the molecule, or (E) an amine oxide as the active ingredient, and a dermatological preparation containing these percutaneous absorption promoting agent and drug components.
    Type: Grant
    Filed: October 5, 1988
    Date of Patent: June 9, 1992
    Assignee: Shiseido Company Ltd.
    Inventors: Kiyoshi Miyazawa, Tadahiro Chiba, Yuhei Iwata, Uhei Tamura, Isao Murotani, Shuya Tamaki
  • Patent number: 5120717
    Abstract: Pharmaceutical compositions containing at least one of benanomicins A and B and their salts are now provided, which are useful to inhibit the infection of human T-cells with HIV, namely a virus causative of acquired human immunodeficiency syndrome (AIDS). Thus, benanomicins A and B as well as their salts are useful as antiviral agent against HIV.
    Type: Grant
    Filed: August 16, 1989
    Date of Patent: June 9, 1992
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Tomio Takeuchi, Shinichi Kondo, Hiroo Hoshino
  • Patent number: 5120763
    Abstract: A composition of matter which consists of (a) from about 13.0 to about 27.5% by weight of at least one compound selected from the group consisting of linolenic acid and derivatives thereof, calculated as the free acid, said derivatives of linolenic acid being both physiologically hydrolyzable and pharmacologically acceptable, and (b) about 87.0 to about 72.5% by weight of at least one compound selected from the group consisting of linoleic acid and derivatives thereof, calculated as the free acid, said derivatives of linoleic acid being both physiologically hydrolyzable and pharmacologically acceptable, is utilized e.g. as a pharmaceutical formulation or nutritional composition, in absence of an oily carrier or diluent which comprises at least one member of the group consisting of C.sub.
    Type: Grant
    Filed: July 6, 1989
    Date of Patent: June 9, 1992
    Assignee: Bar Ilan University
    Inventor: Shlomo Yehuda
  • Patent number: 5118681
    Abstract: S-beta-dicarbonyl substituted beta-thioacrylamide compounds have been discovered to be useful as biocides and fungicides. Compositions comprising the compound and isothiazolin-3-ones and/or carries, methods of preparation of the compounds and methods of using the compounds and compositions are also disclosed.
    Type: Grant
    Filed: July 28, 1989
    Date of Patent: June 2, 1992
    Assignee: Rohm and Haas Company
    Inventors: David R. Amick, Katherine E. Flynn, Cherylann Schieber