Patents Examined by Kimberly J. Prior
  • Patent number: 5665716
    Abstract: New 24-homo vitamin D derivatives of formula I ##STR1## are described, in which R.sup.1 means a hydrogen atom, a hydroxy, an alkanoyloxy group with 1 to 8 carbon atoms or an aralkanoyloxy group with up to 8 carbon atoms,R.sup.2 and R.sup.3, independently of one another, mean a linear or branched alkyl group with 1 to 4 carbon atoms, a trifluoromethyl group or together mean a saturated carbocyclic ring with 3 to 9 carbon atoms formed with carbon atom 25,R.sup.4 and R.sup.5, independently of one another, mean a hydrogen atom, an alkanoyl group with 1 to 8 carbon atoms or an aralkanoyl group with up to 8 carbon atoms, andA and B each mean a hydrogen or together a second bond, andn stands for 1, 2, 3,4 or 5.
    Type: Grant
    Filed: October 2, 1990
    Date of Patent: September 9, 1997
    Assignee: Schering Aktiengesellschaft
    Inventors: Gerald Kirsch, Gunter Neef, Katicia Schwarz, Matthias Brautigam, Ruth Thieroff-Ekerdt, Petra Rach
  • Patent number: 5663386
    Abstract: The invention discloses the use of anthraquinones of the formula ##STR1## where R.sup.3 is unsubstituted or substituted C.sub.1 -C.sub.18 -alkyl or unsubstituted or substituted phenyl for marking mineral oils. Also disclosed are the marked mineral oils and a method of detecting the anthraquinones in mineral oils.
    Type: Grant
    Filed: September 18, 1995
    Date of Patent: September 2, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Friedrich-Wilhelm Raulfs, Christos Vamvakaris
  • Patent number: 5663157
    Abstract: 22-En-24-a-oxa derivatives in the vitamin D series of general formula I ##STR1## in which R.sup.1, R.sup.2 and R.sup.4, independently of one another, each mean a hydrogen atom, an alkanoyl group with 1 to 9 carbon atoms or an aroyl group,R.sup.3 mean a hydrogen atom each or a linear or branched alkyl group each with 1 to 4 carbon atoms, a trifluoromethyl group each or a saturated or unsaturated carbocyclic or heterocyclic 3-, 4-, 5- or 6-membered ring formed together with the tertiary carbon atom, andX means an alkylene radical --(CH.sub.2).sub.n --with n=1, 2 or 3, process for their production and their pharmaceutical use for treating hyperproliferative diseases are disclosed.
    Type: Grant
    Filed: March 16, 1995
    Date of Patent: September 2, 1997
    Assignee: Schering Aktiengesellschaft
    Inventors: Andreas Steinmeyer, Gerald Kirsch, Gunter Neef, Katica Schwarz, Ruth Thieroff-Ekerdt, Herbert Wiesinger, Martin Haberey
  • Patent number: 5661141
    Abstract: The present invention provides compounds and methods of inducing a variety of therapeutic responses in a subject in need of such treatment. The method includes administering a compound of Formula (I) ##STR1## wherein R.sub.1 -R.sub.7 are as defined in the specification; and wherein said compound of Formula (I) is ethylenically unsaturated at a set of locations selected from the group consisting of (a) between C.sub.4 and C.sub.5 ; (b) both between C.sub.3 and C.sub.4 and between C.sub.5 and C.sub.6 ; (c) between C.sub.5 and C.sub.6 ; (d) both between C.sub.4 and C.sub.5 and between C.sub.6 and C.sub.7 ; (e) both between C.sub.3 and C.sub.4 between C.sub.5 and C.sub.6 and between C.sub.7 and C.sub.8 ; (f) both between C.sub.4 and C.sub.5 and between C.sub.7 and C.sub.8 ; and (g) both between C.sub.5 and C.sub.6 and between C.sub.7 and C.sub.8.The compounds of Formula (I) are administered in an amount effective to induce the desired therapeutic response.
    Type: Grant
    Filed: March 27, 1995
    Date of Patent: August 26, 1997
    Inventor: Vladimir Petrow
  • Patent number: 5656657
    Abstract: 3-amino-5-carbonylchromans, 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: May 30, 1995
    Date of Patent: August 12, 1997
    Assignee: Astra Aktiebolag
    Inventors: Eva Maria Hammarberg, Lars George Johansson, Lars-Gunnar Larsson, Rolf Noreen, Lucy Anna Renyi, Svante Bertil Ross, Daniel Dungan Sohn, Bjorn Eric Svensson, Seth-Olov Thorberg
  • Patent number: 5650526
    Abstract: The invention is drawn to a process for the preparation of oxoetiocholenic acid of the formula I ##STR1## by reacting a compound of the formula II ##STR2## with a halonitrile in the presence of a base followed by formation of a 3-ketone group. The intermediate formed is reacted with an acid of the formula HX in an anhydrous medium followed by dehydrohalogenation of the resulting compound in the presence of a base. The intermediate produced then undergoes alkaline hydrolysis followed by a conventional acid treatment to obtain the compound of formula I.
    Type: Grant
    Filed: August 28, 1995
    Date of Patent: July 22, 1997
    Assignee: Roussel Uclaf
    Inventors: Patrick Roussel, Michel Vivat
  • Patent number: 5648507
    Abstract: Provided are stable hydrate crystals of 14.alpha.-hydroxy-4-androstene-3,6,17-trione having a biological activity of human placenta-originating estrodiene synthesis enzyme inhibitory action. These hydrate crystals include two kinds of 14.alpha.-hydroxy-4-androstene-3,6,17-trione hydrate crystals having a diffraction pattern having characteristic peaks at diffraction angles in crystalline powder X-ray diffraction. Processes for producing these hydrate crystals are also provided.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: July 15, 1997
    Assignees: Nippon Kayaku Kabushiki Kaisha, Snow Brank Milk Products Co., Ltd.
    Inventors: Kazuo Ohtsuki, Akikazu Mitsunobu, Yoshihiro Imaizumi, Nobuyoshi Honda, Satoshi Inoue
  • Patent number: 5641765
    Abstract: Invented are 17.alpha. and 17.beta.-substituted acyl-3-carboxy-3,5-diene analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods for using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are intermediates and processes used in preparing these compounds.
    Type: Grant
    Filed: May 17, 1995
    Date of Patent: June 24, 1997
    Assignee: SmithKline Beecham Corporation
    Inventors: Dennis Alan Holt, Mark Alan Levy
  • Patent number: 5641767
    Abstract: The invention relates to linker-modified bile acid derivatives of the formula I: ##STR1## wherein the radicals X.sup.1, X.sup.2, X.sup.3 and Y and n are as defined in the claims, and to a process for their preparation. The compounds according to the invention are therapeutically active and are thus suitable as drugs, especially as hypolipldemics. The invention further relates to the use of the bile acid derivatives according to the invention as drugs.
    Type: Grant
    Filed: September 12, 1995
    Date of Patent: June 24, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gunther Wess, Alfons Ehnsen, Werner Kramer, Klaus Bock
  • Patent number: 5641877
    Abstract: Invented are 17.alpha. and 17.beta.-substituted acyl-3-carboxy-3,5-diene analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods for using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are intermediates and processes used in preparing these compounds.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: June 24, 1997
    Assignee: SmithKline Beecham Corporation
    Inventors: Dennis Alan Holt, Mark Alan Levy
  • Patent number: 5639744
    Abstract: An amide of formula ##STR1## and its pharmacologically acceptable organic or inorganic salt shows a metabolic stability, both enteric and hepatic, greater than that of the corresponding bile acids conjugated with glycine or taurine physiologically present in the enterohepatic circulation. The pharmacological activity of the compounds of formula I or their pharmacologically acceptable organic or inorganic salt makes the use effective for the therapy of biliary calculosis from cholesterol and in every pathology caused by cholestasis like chronic hepatitis from cholestasis, primitive biliary cirrhosis and juvenile hepatopathy associated with cystic fibrosis.
    Type: Grant
    Filed: April 4, 1995
    Date of Patent: June 17, 1997
    Assignee: Alfa Wassermann S.p.A.
    Inventors: Egidio Marchi, Maria Rita Milani, Silvano Piani, Aldo Roda, Gianfranco Cainelli
  • Patent number: 5637742
    Abstract: The invention relates to a new vitamin D compound, substituted in the 18-position with an alkyl group, a hydroxy group, an alkoxy group, an alkenyl group, an alkynyl group, a fluorinated alkyl group or a fluorinated alkenyl group.The invention also relates to a method of preparing said vitamin D compound and to a lactone and a hydrindane intermediate.
    Type: Grant
    Filed: November 1, 1994
    Date of Patent: June 10, 1997
    Assignee: Duphar International Research B.V.
    Inventors: Maria J. Valles, Jose L. Mascarenas, Antonio Mourino, Sebastianus J. Halkes, Jan Zorgdrager
  • Patent number: 5633393
    Abstract: Conjugates of the formula ##STR1## are prepared by reacting an estradiol derivative with a compound of the formula: ##STR2## in the presence of thionyl chloride or a metal hydride at -30.degree. to 150.degree. C. for 3 minutes to 48 hours and then recovering and purifying the product.
    Type: Grant
    Filed: August 5, 1996
    Date of Patent: May 27, 1997
    Assignee: Kureha Kagaku Kogyo Kabushiki Kaisha
    Inventors: Koichi Niimura, Takako Kawabe, Tsutomu Wada, Tsuyoshi Saitoh, Kenji Bannai
  • Patent number: 5629302
    Abstract: New biotenside esters and phosphatides formed with Vitamin-D and Vitamin-E compounds possessing a pronounced antitumor activity, processes for their production as well as for the preparation of concentrates and pharmaceutical compositions containing these new esters and phosphatides, and their use for treating tumors are described.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: May 13, 1997
    Assignee: Marigen S.A.
    Inventors: Carl Eugster, Conrad Hans Eugster, Walter Haldemann, Giorgio Rivara
  • Patent number: 5621124
    Abstract: The invention relates to a process for the alkylation of estrone derivatives, which is characterized in that a suspension of the estrone derivatives in dimethylformamide is produced and carbonic acid diester and guanidine and/or alkyl guanidines are dissolved in it and in the largely oxygen-free mixture, the reaction is performed at 100.degree.-200.degree. C. under the reaction pressure being established.
    Type: Grant
    Filed: May 26, 1995
    Date of Patent: April 15, 1997
    Assignee: Schering Aktiengesellschaft
    Inventors: Carsten Seilz, Dieter Hubl
  • Patent number: 5620966
    Abstract: The invention relates to a 11,21-bisphenyl-19-norpregnane derivative of formula I ##STR1## wherein R.sub.1 is selected from H, halogen, (1-6C)alkoxy, and NR.sub.5 R.sub.6, R.sub.5 and R.sub.6 being independently hydrogen or (1-6C)alkyl or R.sub.5 and R.sub.6 together are (3-6C)alkylene; R.sub.2 is hydrogen; or R.sub.1 and R.sub.2 together are a (1-3C)alkylenedioxy group, optionally substituted by one or more halogen atoms; R.sub.3 is methyl or ethyl; R.sub.4 is selected from C(O)-NR.sub.5 R.sub.6, SO.sub.n -(1-6C)alkyl optionally substituted by one or more halogen atoms, SO.sub.n -(3-6C)cycloalkyl, n being 1 or 2, SO.sub.2 -NR.sub.5 R.sub.6, 2-oxypyrrolidinyl, and NR.sub.5 R.sub.6 ; R.sub.7 is H or (1-6C)alkyl; R.sub.8 is H or carboxy-1-oxo(1-6C)alkyl; and X is selected from (H,OH), O, and NOH; 11 or a pharmaceutically acceptable salt thereof.The compounds of the invention have anti-glucocorticoid activity and can be used in treating or preventing glucocorticoid-dependent diseases.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: April 15, 1997
    Assignee: Akzo Nobel N.V.
    Inventors: Ronald Gebhard, Hendrikus A. A. van der Voort
  • Patent number: 5618806
    Abstract: Invented are 17.alpha. and 17.beta.-substituted acyl-3-carboxy aromatic A ring analogues of steroidal synthetic compounds. Representative of such compounds include the following ##STR1## wherein Z is .alpha. or .beta. ##STR2## in which A is absent or present as a linear or branched, saturated or unsaturated hydrocarbon chain containing from 1-6 carbon atoms and R isa) a linear or branched, saturated or unsaturated hydrocarbon chain containing 1-12 carbon atoms substituted with one or more substituents selected from the group consisting of: --OC.sub.6 -C.sub.12 aryl, --OC.sub.1 -C.sub.4 alkyl, halogen, carboxy and --S(O).sub.n .sup.R.sup.7, where n is 0-2 and R.sup.7 is hydrogen or C.sub.1-4 alkyl;b) C.sub.3 -C.sub.8 nonaromatic, unsaturated or saturated, cycloalkyl, optionally substituted with one or more substituents selected from the group consisting of:--OC.sub.6 -C.sub.12 aryl, --(CH.sub.2).sub.m OH, --OC.sub.1 -C.sub.4 alkyl, C.sub.6 -C.sub.12 aryl, C.sub.1 -C.sub.
    Type: Grant
    Filed: October 28, 1994
    Date of Patent: April 8, 1997
    Assignee: SmithKline Beecham Corporation
    Inventors: Dennis A. Holt, Mark A. Levy
  • Patent number: 5616573
    Abstract: Glucocorticoids of general formula IR--Val--O--GC (II),are described,in whichO-GC is the radical of a 21-hydroxycorticoid that has an antiinflammatory action,Val represents a valine radical in the 21-position of the corticoid andR means a hydrogen atom or a hydrocarbon radical with up to 32 carbon atoms that is optionally substituted by hydroxy groups, amino groups, oxo groups and/or halogen atoms and/or interrupted by oxygen atoms, SO.sub.2 groups and/or NH groups and their salts.
    Type: Grant
    Filed: October 6, 1995
    Date of Patent: April 1, 1997
    Assignee: Schering Aktiengesellschaft
    Inventors: Hans J. Zentel, Michael Topert, Henry Laurent, Thomas Brumby, Peter Esperling
  • Patent number: 5616734
    Abstract: The invention relates to the use of compounds of the formula IR.sup.1.sub.a Re.sub.b O.sub.c (I),where a is from 1 to 6, b is from 1 to 4 and c is from 1 to 14 and the sum of a, b and c is in accordance with the valence of from 5 to 7 of the rhenium, with the proviso that c is not greater than 3.multidot.b, and where R.sup.1 is identical or different and is an aliphatic hydrocarbon radical having from 1 to 10 carbon atoms, an aromatic hydrocarbon radical having from 6 to 10 carbon atoms or an arylalkyl radical having from 7 to 9 carbon atoms, with the radicals R.sup.1 being able, if desired, to be identically or differently substituted independently of one another and, in the case of .sigma.-bonded radicals, at least one hydrogen atom still being bonded to the carbon atom in the .alpha. position, as catalysts for the oxidation of electron-rich aromatic compounds and their derivatives and to a process for the oxidation of electron-rich aromatic compounds which comprises oxidizing electron-rich C.sub.6 -C.sub.
    Type: Grant
    Filed: January 25, 1995
    Date of Patent: April 1, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wolfgang A. Herrmann, Joao D. G. Correia, Richard Fischer, Waldemar Adam, Jianhua Lin, Chantu R. Saha-Moller, Masao Shimizu
  • Patent number: 5616744
    Abstract: A 19-nor intermediate compound of the formula ##STR1## where R is the sidechain of a vitamin D derivative and where X.sub.1 and X.sub.2 are hydrogen or a hydroxy protecting group. The compounds are used in the preparation of 19-nor-vitamin D end products.
    Type: Grant
    Filed: May 23, 1995
    Date of Patent: April 1, 1997
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Heinrich K. Schnoes, Fariba Aria