Patents Examined by Joseph A. Lipovsky
  • Patent number: 4927815
    Abstract: This invention provides novel side chain homologs of 1.alpha.,25-dihydroxyvitamin D.sub.3 which exhibit enhanced and highly selective activity in inducing differentiation of malignant cells. It also provides a general method of synthesis applicable to the preparation of a variety of vitamin D side chain analogs, and a method of treatment of neoplastic diseases which takes advantage of the selective differentiation activity of the new vitamin D homologs.
    Type: Grant
    Filed: April 29, 1988
    Date of Patent: May 22, 1990
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Heinrich K. Schnoes, Kato L. Perlman, Andrzej Kutner
  • Patent number: 4925834
    Abstract: A 3-methylene-4-androsten-17-one of formula I ##STR1## wherein R.sub.a represents a hydrogen atom or a saturated or unsaturated straight-chain or branched-chain, optionally substituted alkyl radical with 1-6 carbon atoms, in which R.sub.a is in the alpha- or beta-position, andR.sub.b represents a hydrogen atom, a hydroxyl or an --S(O).sub.n R.sub.c group, in which R.sub.c is a hydrogen atom or an alkyl or acyl group with 1-4 carbon atoms, n=0, 1 or 2, andX represents CH.sub.2, CHF, CHCl or CHBr, in which if R.sub.a is hydrogen and R.sub.b is hydroxyl or R.sub.a and R.sub.b each are hydrogen, X is not CH.sub.2.The new compounds of formula I are suitable for fertility control and for treatment of diseases which are promoted by estrogens.
    Type: Grant
    Filed: April 29, 1988
    Date of Patent: May 15, 1990
    Assignee: Schering Aktiengesellschaft
    Inventors: Rolf Bohlmann, Henry Laurent, David Henderson, Yukishige Nishino
  • Patent number: 4923854
    Abstract: A method and composition are described for the solubilization of hydrophobic materials using a lysophospholipid. The method includes drying a composition comprising a hydrophobic material-solubilizing effective amount of phospholipid from organic solvent and hydrating the resulting film with an aqueous medium at either a pH of between about 8.5 and about 14.0, or at pH 7.0 followed by reduction of the temperature to less then 0.degree. C.
    Type: Grant
    Filed: January 22, 1986
    Date of Patent: May 8, 1990
    Assignee: The Liposome Company, Inc.
    Inventors: Colin P. S. Tilcock, Pieter R. Cullis, Michael J. Hope, Andrew S. Janoff
  • Patent number: 4923897
    Abstract: The addition of nonionic surfactants to aqueous pyrethroid insecticidal formulations increases the pyrethroid stability when the formulation is stored in a polyvinylchloride (PVC) container. The pyrethroids can be synthetic or naturally occurring pyrethroids. The nonionic surfactants are alkylphenol ethoxylates, ethoxylated primary alcohols, polyoxyethylene thioethers or mixtures thereof and have HLB values of between about 10 and about 14.
    Type: Grant
    Filed: May 4, 1989
    Date of Patent: May 8, 1990
    Assignee: S. C. Johnson & Son, Inc.
    Inventor: Stanley J. Flashinski
  • Patent number: 4921844
    Abstract: Novel fungicidal compositions comprising a 25-azasterol composition and a .beta.-ketothiolase inhibitor compound are disclosed.
    Type: Grant
    Filed: April 18, 1988
    Date of Patent: May 1, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Janet C. Onishi, Arthur A. Patchett
  • Patent number: 4921846
    Abstract: Steroids with a 17-spiro substituent of 3,4 or 6 ring members of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of carbocyclic aryl, heterocyclic aryl and aralkyl, R.sub.2 is a hydrocarbon of 1 to 18 carbon atoms in the .alpha.-or .beta.-position, the wavy line of the spiro ether indicates the oxygen is .alpha.-or .beta.-, X is selected from the group consisting of --CH.dbd.CH--CH.sub.2 --CH.sub.2 -- and --(CH.sub.2).sub.n --, n is 1, 2 or 4, the A and B rings have a structure selected from the group consisting of ##STR2## R' and R" are individually hydrogen or alkyl of 1 to 4 carbon atoms, R.sub.e is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, substituted alkyl of 1 to 6 carbon atoms and acyl and their non-toxic, pharmaceutically acceptable acid addition salts having a remarkable antiprogestomimetic activity.
    Type: Grant
    Filed: September 16, 1988
    Date of Patent: May 1, 1990
    Assignee: Roussel Uclaf
    Inventors: Lucien Nedelec, Andre Claussner, Daniel Philibert, Martine Moguilewsky
  • Patent number: 4921843
    Abstract: A method of contraception is disclosed which comprises a two-stage protocol. In the first stage, an estrogenic compound in a first composition is administered daily as the sole contraceptively active substance to a human female from about Day 2 to about Day 7 of her menstrual cycle, where Day 1 is the first day of menses. The second stage of the protocol occurs immediately thereafter during which at least one follow-up composition containing a progestin is administered daily to the same human female. The follow-up composition can contain a progestin as the sole contraceptively active ingredient, or can contain a combination of an estrogenic compound with a progestin in different weight ratios. A drug delivery system containing daily dosage units is also described.
    Type: Grant
    Filed: October 20, 1988
    Date of Patent: May 1, 1990
    Inventor: Samuel A. Pasquale
  • Patent number: 4921848
    Abstract: Compounds of formula I ##STR1## wherein: R.sub.1 is hydrogen or hydroxy, and the methyl and hydroxy groups at 6- and 7-positions respectively can be either in .alpha. or .beta. configuration, are useful in human therapy. Compounds I are prepared by methylation of the corresponding appropriately protected 7-keto-derivatives.
    Type: Grant
    Filed: October 19, 1988
    Date of Patent: May 1, 1990
    Assignee: Gipharmex S.P.A.
    Inventors: Giuliano Frigerio, Roberto Pellicciari, Aldo Roda
  • Patent number: 4921845
    Abstract: The invention relates to new 11-arylsteroid compounds, having a strong antiprogestin and a weak or nonexistent antiglucocorticoid activity, to processes for preparing said compounds and also to pharmaceutical preparations which contain these derivatives as active constituent, characterized in that said steroids have the following formula: ##STR1## in which R.sub.1 is an aryl group with a ##STR2## group as substituent, X and Y each being separately H or a (1-4 C) hydrocarbyl group or together a (2-C) hydrocarbyl group which forms a 3- to 7-membered ring together with the nitrogen atom;R.sub.2 is hydrogen, hydroxyl, an acyloxy or an alkoxy group or a saturated or unsaturated hydrocarbyl group containing 1-8 carbon atoms, which hydrocarbyl group is provided with at least one hydroxyl, oxo, azido, cyano and/or halogen group;R.sub.3 is a hydroxyl, an acyloxy or an alkoxy group or an acyl group optionally substituted by a hydroxyl, alkoxy, acyloxy or halogen group; or R.sub.2 and R.sub.
    Type: Grant
    Filed: December 8, 1988
    Date of Patent: May 1, 1990
    Assignee: Akzo N.V.
    Inventors: Hendrick Paul de Jongh, Nicolaas P. van Vliet
  • Patent number: 4921638
    Abstract: The invention is the compound 17.beta.-cyano-9.alpha., 17.alpha.-dihydroxyandrost-4-en-3-one (I) which is particularly useful as an intermediate in the production of the 17.alpha.-halo silyl ethers (II).
    Type: Grant
    Filed: October 3, 1988
    Date of Patent: May 1, 1990
    Assignee: The Upjohn Company
    Inventors: Douglas A. Livingston, Bruce A. Pearlman, Scott Denmark, Joel E. Huber
  • Patent number: 4921849
    Abstract: Disclosed herein is an injection containing 3-benzoyloxy-1,3,5(10)-estratriene-17-[4-{p-bis(2-chloroethyl)amino)phenyl }butanoyloxy]acetate, which has been known as an orally administrable anti-tumor substance, as an active ingredient and an ester of iodinated poppy oil fatty acid as a solvent.
    Type: Grant
    Filed: July 18, 1988
    Date of Patent: May 1, 1990
    Assignee: Kureha Kagaku Kogyo Kabushiki Kaisha
    Inventors: Kiro Asano, Satoshi Mitsuhashi, Kenji Bannai, Hisayuki Wada, Humio Tamura
  • Patent number: 4920113
    Abstract: Novel fungicidal compositions comprising a 25-azasterol compound and a HMG-CoA synthase inhibitor compound are disclosed.
    Type: Grant
    Filed: April 18, 1988
    Date of Patent: April 24, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Janet C. Onishi, Arthur A. Patchett
  • Patent number: 4920111
    Abstract: Novel fungicidal composition comprising a 25-azasterol compound and a HMG-CoA reductase inhibitor compound are disclosed.
    Type: Grant
    Filed: April 18, 1988
    Date of Patent: April 24, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Janet C. Onishi, Arthur A. Patchett
  • Patent number: 4920109
    Abstract: Method of potentiating antifungal agents with 25-azasterol compound to produce superior antifungal compositions and use of the compositions to control mycotic infections is disclosed.
    Type: Grant
    Filed: April 18, 1988
    Date of Patent: April 24, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Janet C. Onishi, Arthur A. Patchett
  • Patent number: 4920114
    Abstract: 19-Fluoro- and cyano- substituted 21-hydroxyprogesterone derivatives and related compounds which are active as 19-hydroxylase inhibitors and useful as antihypertensive agents are described herein. The compounds are prepared using appropriate synthetic pathways which will vary according to the nature of the specific 19-substituted progesterone or related compound desired.
    Type: Grant
    Filed: June 28, 1988
    Date of Patent: April 24, 1990
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Gene W. Holbert, J. O'Neal Johnston
  • Patent number: 4920112
    Abstract: Novel fungicidal compositions comprising a 25-azasterol compound and a squalene epoxidase inhibitor compound are disclosed.
    Type: Grant
    Filed: April 18, 1988
    Date of Patent: April 24, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Janet C. Onishi, Arthur A. Patchett
  • Patent number: 4920123
    Abstract: A method for controlling and/or reducing a patient's serum cholesterol and/or triglyceride level is disclosed.
    Type: Grant
    Filed: October 21, 1988
    Date of Patent: April 24, 1990
    Inventor: Karl H. Beyer, Jr.
  • Patent number: 4920216
    Abstract: This invention concerns a method of substituting a chlorine atom for a predetermined hydrogen atom located within an organic compound which comprises contacting the organic compound containing the predetermined hydrogen atom with an esterifying agent comprising a pyridine ring or a substituted or fused ring derivative of a pyridine ring so as to produce an ester and treating the ester with a chlorinating agent so as to substitute the chlorine atom for the predetermined hydrogen atom. The ester comprises the pyridine ring or the substituted or fused ring derivative of the pyridine ring so positioned within the ester with respect to the predetermined hydrogen atom that a chlorine atom attached to the nitrogen atom of the pyridine ring or substituted or fused ring derivative of the pyridine ring reacts with the predetermined hydrogen atom.
    Type: Grant
    Filed: May 28, 1987
    Date of Patent: April 24, 1990
    Assignee: The Trustees of Columbia in the City of New York
    Inventors: Ronald Breslow, Michael Brandl, Alan D. Adams, Jurgen Hunger
  • Patent number: 4918229
    Abstract: A novel process for producing hindered and unhindered primary amines represented by the formula RNH.sub.2 and R*NH.sub.2 in high yields from novel intermediates RBMe.sub.2 or R*BMBe.sub.2 wherein R is an organo group, R* is a chiral organo group attached to boron, B is boron and Me is methyl.
    Type: Grant
    Filed: July 29, 1988
    Date of Patent: April 17, 1990
    Assignee: Aldrich Chemical Company, Inc.
    Inventor: Herbert C. Brown
  • Patent number: 4917827
    Abstract: 9(11)-dehydroandrostanes and 9(11)-dehydropregnanes are prepared by dehydrating the corresponding 9-alpha-hydroxy steroid in the presence of a Lewis acid. The corresponding 8(9)-dehydro-isomer was not detectable. The resulting products are valuable intermediates in steroid synthesis especially in the preparation of corticosteroids.
    Type: Grant
    Filed: June 10, 1988
    Date of Patent: April 17, 1990
    Assignee: Gist-Brocades N.V.
    Inventors: Jacobus N. M. Batist, Nicolaas C. M. E. Barendse, Arthur F. Marx