Patents Examined by E. C. Ward
  • Patent number: 5232915
    Abstract: 9.alpha.-Hydroxy-19,11.beta.-bridged steroids of general formula I ##STR1## are described. The more detailed meaning of A, B, R.sup.1, R.sup.2, G, Z, R.sup.4 --Y and R.sup.4' --Y' follows from the description. The steroids of general formula I have antigestagen and/or antiglucocorticoidal action and can be used for the production of pharmaceutical agents.
    Type: Grant
    Filed: January 14, 1992
    Date of Patent: August 3, 1993
    Assignee: Schering Aktiengesellschaft
    Inventors: Eckhard Ottow, Gunter Neef, Rudolf Wiechert, Walter Elger, Sybille Beier, Karl-Heinrich Fritzemeier
  • Patent number: 5232916
    Abstract: Compounds having the formula: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.
    Type: Grant
    Filed: October 28, 1991
    Date of Patent: August 3, 1993
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Robert Zamboni, Petpiboon Prasit, Robert N. Young
  • Patent number: 5229508
    Abstract: A process for the preparation of a copper phthalocyanine pigment, which comprises dry grinding crude copper phthalocyanine, treating the dry ground crude copper phthalocyanine with an aqueous solution of a mineral acid under such conditions of acid concentration and temperature as not to transform the .beta. form contained in the ground crude copper phthalocyanine into the .alpha. one to thereby carry out the pigmentation and removing the mineral acid from the resulting mixture.
    Type: Grant
    Filed: December 13, 1991
    Date of Patent: July 20, 1993
    Assignee: Toyo Ink Manufacturing Co., Inc.
    Inventors: Toshimitsu Ikegaya, Yusaku Ide, Tsuneo Kawamura, Michichika Hikosaka
  • Patent number: 5227474
    Abstract: The present invention provides bifunctional chelating agents comprising a unique substrate reactive moiety incorporated into a carboxymethyl arm of a polyaminopolycarboxylate chelating framework capable of forming stable complexes with metal ions.
    Type: Grant
    Filed: May 28, 1991
    Date of Patent: July 13, 1993
    Assignee: Abbott Laboratories
    Inventors: David K. Johnson, Steven J. Kline
  • Patent number: 5227375
    Abstract: Novel aromatase inhibitors are disclosed for use in therapeutic preparations for treatment of estrogen-dependent diseases. The compounds are specified 7.alpha.-substituted androstanedione and androstenedione derivatives which show a strong inhibitory activity towards aromatase. The invention includes synthesis and pharmaceutical compositions of said compounds.
    Type: Grant
    Filed: February 8, 1990
    Date of Patent: July 13, 1993
    Assignee: Endorecherche, Inc.
    Inventors: Fernand Labrie, Yves Merand
  • Patent number: 5225551
    Abstract: An imaging member comprised of a supporting substrate, a photogenerating layer comprised of a titanyl phthalocyanine of the type selected from the group consisting of Type IV, Type X, Type Z-1, and Type Z-2, prepared by the process which comprises dissolving a titanyl phthalocyanine in a solution of trifluoroacetic acid and methylene chloride; adding the resultant solution to a solvent or solvent mixture that will enable precipitation; and separating the product titanyl phthalocyanine from the solution followed by an optional washing, and a charge transport layer.
    Type: Grant
    Filed: October 5, 1992
    Date of Patent: July 6, 1993
    Assignee: Xerox Corporation
    Inventors: James M. Duff, James D. Mayo, Cheng-Kuo Hsiao, Ah-Mee Hor, Terry L. Bluhm, Gordon K. Hamer, Peter M. Kazmaier
  • Patent number: 5225402
    Abstract: Novel carbostyril derivatives of the formula: ##STR1## wherein R.sup.1 is H, NO.sub.2, alkoxy, alkoxycarbonyl, alkyl, halogen, optionally substituted amino, OH, CN, COOH, alkanoyloxy, hydrazinocarbonyl; q is 1 to 3, and R is a group of the formula ##STR2## [wherein R.sup.2 is H, alkoxycarbonyl, optionally substituted phenoxycarbonyl, phenylalkenyl-CO-, optionally substituted phenylalkanoyl, alkanoyl, alkenyl-CO-, optionally substituted phenyl--SO.sub.2 --, --CONR.sup.8 R.sup.9, optionally substituted heterocyclic group--CO--, naphthyl--CO--, thienylalkanoyl, tricyclo[3.3.1.1]alkanoyl, ##STR3## (R.sup.13 is OH, optionally substituted alkoxy, --NR.sup.32 R.sup.33, --O--A--(E).sub.l --NR.sup.4 R.sup.5, --(B).sub.l 'NR.sup.6 R.sup.7, etc.), n is 1 or 2, m is 0 or 1 to 3, R.sup.3 is alkyl, R.sup.10 is --(CO).sub.l --NR.sup.11 R.sup.
    Type: Grant
    Filed: September 18, 1991
    Date of Patent: July 6, 1993
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Hidenori Ogawa, Hisashi Miyamoto, Kazumi Kondo, Hiroshi Yamashita, Kenji Nakaya, Michiaki Tominaga, Yoichi Yabuuchi
  • Patent number: 5223494
    Abstract: Disclosed is a pharmaceutical composition for oral administration to control heme oxygenase comprising mettaloprotoporhyrins and mettalomesoporphyrins.
    Type: Grant
    Filed: September 21, 1990
    Date of Patent: June 29, 1993
    Assignee: The Rockefeller University
    Inventors: Attallah Kappas, Daniel W. Rosenberg, George S. Drummond
  • Patent number: 5223492
    Abstract: This invention relates to the field of chemistry and more precisely to the field of medicinal Chemistry.It has specifically as subject matter the compounds of general formula I ##STR1## wherein R is a hydrogen, a lower alkyl radical a methoxymethyl, a tetrahydropyranyl or the acyl residue of an organic carboxylic.
    Type: Grant
    Filed: August 26, 1991
    Date of Patent: June 29, 1993
    Inventors: Nejib M. Nasraoui, Alain Piasco
  • Patent number: 5219862
    Abstract: Compounds of formula I ##STR1## in which R.sup.2 means optionally substituted C.sub.1-7 alkyl, C.sub.2-7 alkenyl, CH.sub.2 --O--C.sub.1-4 alkyl or CH.sub.2 --S--C.sub.1-4 alkylR.sup.6 means C.sub.2-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-5 -cycloalkyl-C.sub.1-2 alkyl andR.sup.8 means CH.sub.2 --X, ##STR2## in which X stands for CN, OCH.sub.3, SCH.sub.3 or CONH.sub.2 and R.sup.1 stands for hydrogen, halogen, methyl or methoxy, and R.sup.3 and R.sup.4 each mean C.sub.1-4 alkyl or (CH.sub.2).sub.n --N(CH.sub.3).sub.2, in which n=1-4, and their acid addition salts, the process for their production, their use as pharmaceutical agents as well as intermediate compounds are described.
    Type: Grant
    Filed: December 21, 1990
    Date of Patent: June 15, 1993
    Assignee: Schering Aktiengesellschaft
    Inventors: Gerhard Sauer, Thomas Brumby, Helmut Wachtel, Jonathan Turner, Peter A. Loschmann
  • Patent number: 5218109
    Abstract: Steroid compounds of the following general formulas (I), (II) and (III) are provided: ##STR1## In the above formulas, R.sup.1 and R.sup.2 each is a hydrogen atom or a hydroxyl-protecting group, R is a group of the formula --CH.sub.2 --X (in which X is a substituent such as a hydroxyl group), a carboxyl group or a protected carboxyl group, A.sup.1 is an aryl group, a lower alkyl group or an aralkyl group, and Z.sup.1, Z.sup.2, Z.sup.3 and Z.sup.4 each is a hydrogen atom, a hydroxyl group or a protected hydroxyl group.The above steroid compounds are useful as intermediates for the synthesis of vitamin D.sub.3 derivatives having a hydroxyl group at the 1.alpha.-position.
    Type: Grant
    Filed: March 5, 1990
    Date of Patent: June 8, 1993
    Assignee: Kuraray Co., Ltd.
    Inventors: Jiro Tsuji, Takashi Takahashi, Masao Tsuji, Naoshi Nakagawa, Tetsuo Takigawa
  • Patent number: 5217977
    Abstract: The invention concerns a heterocyclic cycloalkane of the formula I ##STR1## wherein Q is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms;A is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene;X is oxy, thio, sulphinyl, sulphonyl or imino;Ar is phenylene which may optionally bear one or two substituents or Ar is an optionally substituted 6-membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl; and R.sup.2 and R.sup.3 together form a (3-6C)alkylene group which, together with the carbon atom to which R.sup.2 and R.sup.3 are attached, defines a ring having 4 to 7 ring atoms, and which ring may bear one or two substituents;or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.
    Type: Grant
    Filed: November 15, 1991
    Date of Patent: June 8, 1993
    Assignees: Imperial Chemical Industries PLC, ICI Pharma
    Inventors: Graham C. Crawley, Jean-Marc M. M. Girodeau
  • Patent number: 5214036
    Abstract: Green porphyrins (Gp), compounds important in photodynamic therapy, have been associated with lipocomplexes to reduce the required amount of photosensitizer through higher effective absorption and increased specificity. BPDs, especially in conjunction with the HDL fraction of plasma lipoproteins, has been shown to be particularly effective in this context. Pharmaceutical compositions in which these combinations are the active ingredients for use in diagnosis and treatment of tumors are also disclosed.
    Type: Grant
    Filed: March 8, 1990
    Date of Patent: May 25, 1993
    Assignee: University of British Columbia
    Inventors: Beth A. Allison, Anna M. Richter, P. Haydn Pritchard, Julia G. Levy
  • Patent number: 5214171
    Abstract: Process for fractionating phosphatide mixtures into two or more fractions which are enriched in one or more of phosphatidyl choline (PC), phosphatidyl ethanolamine (PE), phosphatidyl inositol (PI) and phosphatidic acid (PA) by carrying out extraction steps using alcoholic solvent in which the solubilities of PC, PE and PA are controlled by suitably adjusting the acidity of the solvent, the pH being adjusted to above 8 for solubilizing PC and PE and to below 5 for solubilizing PA. PI is substantially insoluble in the solvent used in the process and thus is mainly recovered in the extraction residue. Further parameters influencing the solubility of the components of the phosphatide mixtures to be fractionated are water content of the alcoholic solvent, temperature and choice of bases and acids for adjusting the pH. For further separating fractions rich in PC and PE di- or trivalent metal salt solutions are used.
    Type: Grant
    Filed: November 19, 1991
    Date of Patent: May 25, 1993
    Assignee: N.V. Vandemoortele International
    Inventors: Albert J. Dijkstra, Jan De Kock
  • Patent number: 5212158
    Abstract: The L-proline derivatives of the invention correspond to the Formula I: ##STR1## in which R.sub.1 corresponds to the Formula II: ##STR2## in which R is a carbonyl group, an acyl group --Y--CO-- or an oxy-acyl group --O--Y--CO--, Y being an alkyl or an alkenyl chain, Z being one or more hydrogen atoms, or one or more substituents chosen from among halogen atoms, CF.sub.3, alkyl or alkoxy groups and an alkylenedioxy group in the case of two neighbouring substituents,R.sub.2 is --NH.sub.2, --OH, or a derivative of these groups,A.sub.1 and A.sub.2 are amino acid residues andB.sub.1 and B.sub.2 represents a hydrogen atom or a methyl group, and the pharmacologically acceptable salts of these derivatives.These derivatives are useful particularly as the active principles of medicines possessing, in particular, a nootropic action.
    Type: Grant
    Filed: November 3, 1988
    Date of Patent: May 18, 1993
    Assignee: Inorgan SA Recherche & Developpement Pharmaceutiques, CAS
    Inventor: Pierre-Yves Fiez Vandai
  • Patent number: 5212179
    Abstract: The invention concerns the preparation of compounds of formula ##STR1## and acid addition and quaternary ammonium salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula ##STR2## in which Q is O, S, --CR.sup.7 .dbd.CR.sup.8 --, --N.dbd.CR.sup.8 -- and --N.dbd.N--; R.sup.4, R.sup.5 and R.sup.6 ; and R.sup.7 and R.sup.8 when present, each represent hydrogen or a substituent selected from lower alkyl, lower alkenyl, lower alkoxy, NO.sub.2, NH.sub.2, haloloweralkyl, hydroxyloweralkyl, aminoloweralkyl, substituted amino, halogen, loweralkoxycarbonyl, cyano, CONH.sub.2 and hydroxy; and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.
    Type: Grant
    Filed: October 25, 1990
    Date of Patent: May 18, 1993
    Assignee: John Wyeth and Brother Limited
    Inventors: John L. Archibald, Terence J. Ward
  • Patent number: 5210301
    Abstract: Novel squarium compounds which have a flat photosensitivity in the wide range from visible ray region to the near infrared ray region as a charge generator and which can be prepared by reacting squaric acid and an aniline derivative, and electrophotographic photoreceptors containing the squarium compounds are disclosed.
    Type: Grant
    Filed: August 17, 1988
    Date of Patent: May 11, 1993
    Assignee: Fuji Xerox Co., Ltd.
    Inventors: Satoshi Saeki, Seki Kin, Kaoru Torikoshi, Hiroyuki Tanaka, Lyong S. Pu
  • Patent number: 5206231
    Abstract: Novel 2,5-benzodiazocines of formulas II and IV, pharmaceutical compositions containing them, processes for preparing them and methods of treating cardiac arrhythmias in mammals utilizing them.
    Type: Grant
    Filed: September 10, 1991
    Date of Patent: April 27, 1993
    Assignee: Sterling Drug Inc.
    Inventor: Robert E. Johnson
  • Patent number: 5206233
    Abstract: Substituted thiazepines are described as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as antipsychotic and antidepressant agents as well as for treating cerebral ischemia or cerebral infarction.
    Type: Grant
    Filed: August 27, 1991
    Date of Patent: April 27, 1993
    Assignee: Warner-Lambert Company
    Inventors: William J. Smith, III, Lawrence D. Wise, David J. Wustrow
  • Patent number: 5202319
    Abstract: There are disclosed various compounds of the formula below, ##STR1## where n is 1 or 2;m is 1 or 2;each X is independently hydrogen or loweralkoxy;Y is hydrogen, halogen or trifluoromethyl;R.sub.1 is hydrogen, loweralkyl, arylloweralkyl, heteroarylloweralkyl, pyridinyl, loweralkylcarbonyl, arylloweralkylcarbonyl, heteroarylloweralkylcarbonyl, trifluoromethylcarbonyl or arylcarbonyl; andR.sub.2 is hydrogen, loweralkyl, loweralkoxycarbonyl, aminoloweralkylcarbonyl, loweralkylaminoloweralkylcarbonyl or diloweralkylaminoloweralkylcarbonyl;which are useful as modulators of neurotransmitter function such as serotonergic and adrenergic, and as such are useful as antidepressants and for the treatment of personality disorders such as obsessive compulsive disorders.
    Type: Grant
    Filed: September 23, 1991
    Date of Patent: April 13, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Joseph T. Klein