Patents Examined by Elbert L. Roberts
  • Patent number: 4634694
    Abstract: The invention relates to novel steroids having the formula: ##STR1## wherein X=CH.sub.2 --S--R.sub.3 or S--S--R.sub.4 ;R.sub.1 =O or H (.beta.R.sub.5);R.sub.2 =O or H (.beta.R.sub.6);R.sub.3 =H, acyl (1-18C) or alkyl (1-4C);R.sub.4 =H, acyl (1-18C) or hydrocarbyl (1-18C), the acyl or hydrocarbyl group being optionally substituted;R.sub.5 =OH, O acyl (1-18C) or an ether group;R.sub.6 =OH, O acyl (1-18C) or an ether group;and the dotted lines represent a carbon-carbon bond in 4,5- or 5,6 position; to processes for their preparation and to pharmaceutical compositions containing these steroids as active constituents.The novel compounds possess particularly aromatase-inhibiting properties.
    Type: Grant
    Filed: January 2, 1985
    Date of Patent: January 6, 1987
    Assignee: Akzo N.V.
    Inventors: Hubert J. J. Loozen, Pieter J. N. van Luit
  • Patent number: 4634696
    Abstract: Novel 19-nor-steroids of the formula ##STR1## wherein R.sub.1 is an organic group of 1 to 18 carbon atoms optionally containing at least one heteroatom with the atom immediately adjacent the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is the remainder of a pentagonal or hexagonal ring optionally substituted and optionally containing one unsaturated--bond, the A and B rings are selected from the group consisting of ##STR2## R' and R" are individually selected from the group consisting of hydrogen, --CN and alkyl of 1 to 4 carbon atoms with at least one being other than hydrogen, R.sub.x is selected from the group consisting of hydrogen and OR.sub.e, R.sub.e is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and acyl, R.sub.a may be in the E or Z positions as indicated by the wavy line and is selected from the group consisting of ##STR3## and acyloxy, R.sub.a ' and R.sub.
    Type: Grant
    Filed: July 30, 1985
    Date of Patent: January 6, 1987
    Assignee: Roussel Uclaf
    Inventors: Jean-Georges Teutsch, Vesperto Torelli, Roger Deraedt, Daniel Philibert
  • Patent number: 4634693
    Abstract: Tin steroids and methods of using the same. The tin steroid compounds are prepared by the reaction of various organotin compounds with various steroids. Said compounds inhibit the growth of malignant tumors. They are also useful as insecticides, larvicides, bactericides and fungicides.
    Type: Grant
    Filed: August 12, 1985
    Date of Patent: January 6, 1987
    Inventors: Nathan F. Cardarelli, Sebastian V. Kanakkanatt
  • Patent number: 4632784
    Abstract: The invention is directed to a process and intermediates for the preparation of 1.alpha., 23,25-trihydroxycholecalciferol-26-oic acid 23,26-lactone.
    Type: Grant
    Filed: July 30, 1984
    Date of Patent: December 30, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Enrico G. Baggiolini, Milan R. Uskokovic, Peter M. Wovkulich
  • Patent number: 4632820
    Abstract: Novel radioactive .DELTA..sup.4,9,11 -estratrienes marked with iodine 125 or 131 having the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and acyl of an organic carboxylic acid of 2 to 12 carbon atoms, R.sub.1 is the reminder of an amino acid of the formula R.sub.1 NH.sub.2 or a derivative thereof being marked with iodine 125 or 131 and the wavy lines indicate the --OR is in the .alpha.- or .beta.-position and the oximido group is in the syn or anti position, a process and intermediates for their preparation, antigens prepared therefrom and use thereof to prepare antibodies.
    Type: Grant
    Filed: December 12, 1983
    Date of Patent: December 30, 1986
    Assignee: Roussel Uclaf
    Inventors: Alain Jouquey, Gaetan Touyer, Jean Salmon, Michel Mouren
  • Patent number: 4632828
    Abstract: A water-swellable, water-insoluble polymer is loaded with methylhydroxyprogesterone acetate (MAP) by:(a) preparing and grinding a mixture of a said polymer and MAP; or(b)(i) preparing a mixture of a said polymer which is stable under the heating to which the mixture is subjected in step (ii) and MAP and (ii) heating the mixture up to the melting temperature of MAP; or(c) swelling a said polymer with a MAP solution capable thereof and drying the resulting swollen polymer/MAP system.The MAP loaded polymer is useful as a pharmaceutical composition.
    Type: Grant
    Filed: February 6, 1985
    Date of Patent: December 30, 1986
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventor: Fabio Carli
  • Patent number: 4628052
    Abstract: The present invention is concerned with compositions and methods of treating rheumatoid arthritis, osteoarthritis, and arthritis associated with psoriasis and with lupus and other auto-immune diseases, and also for treating non-specific joint pain associated with stress or incidental to another ailment, using dehydroepiandrosterone and/or other anesthetic steroids dissolved in an oily vehicle, and preferably administered topically or orally.
    Type: Grant
    Filed: May 28, 1985
    Date of Patent: December 9, 1986
    Inventor: Raymond F. Peat
  • Patent number: 4628050
    Abstract: Disclosed herein is a pharmaceutical composition in dosage unit form, which comprises a dosage effective for treating nephritic disease of a compound of 24,25-dihydroxycholecalciferol as an active ingredient and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: November 20, 1985
    Date of Patent: December 9, 1986
    Assignee: Kureha Kagaku Kogyo Kabushiki Kaisha
    Inventors: Yuji Maeda, Hideyuki Yamato, Takayoshi Fujii, Yasuhiko Kobayashi, Kenichi Saito, Tadaaki Kato, Chikao Yoshikumi
  • Patent number: 4628051
    Abstract: A method of contraception in which an estrogen and a progestogen are administered daily in a three phase sequence for 21 days is disclosed. In the first phase a combination of an estrogen and a progestogen in a low but contraceptively effective daily dosage corresponding in estrogenic activity to 0.02-0.05 mg of 17.alpha.-ethinylestradiol and in progestogenic activity to 0.065-0.75 mg of norethindrone is administered for 5-8 days; followed by the administering of the same dosage of estrogen and a progestogen corresponding in progestogenic activity to 0.25-1.0 mg of norethindrone for 7-11 days; followed by the administering of the same dosage of estrogen and a progestogen corresponding in progestogenic activity to 0.35-2.0 mg of norethindrone for 3-7 days; followed by 6-8 days without administering either an estrogen or a progestogen.
    Type: Grant
    Filed: June 11, 1985
    Date of Patent: December 9, 1986
    Assignee: Ortho Pharmaceutical Corporation
    Inventor: Samuel A. Pasquale
  • Patent number: 4626531
    Abstract: A pharmaceutical composition containing a prostaglandin and an antigestagen is suitable for induction of labor and for abortion.
    Type: Grant
    Filed: October 12, 1984
    Date of Patent: December 2, 1986
    Assignee: Schering Aktiengesellschaft
    Inventors: Walter Elger, Sybille Beier
  • Patent number: 4622181
    Abstract: A process of preparing radical anions which comprises reacting sodium and a polycyclic aromatic compound in a reaction solvent to prepare radical anions and supplying androstane-1,4-diene-3,17-dione-17-acetal into the obtained reaction mixture to reduce the same into an estrone acetal, characterized in that a solvent comprising polyethers having three or more ether bonds and maintained at a concentration higher than a predetermined value is used as the reaction solvent and the reaction is carried out at a temperature of from the melting point of sodium to 105.degree. C. The process according to this invention can produce an estrone acetal at a high yield and with economical advantages in the industrial scale and the estrone acetal thus obtained is useful as an estrone precursor which is important as a female hormone.
    Type: Grant
    Filed: September 21, 1984
    Date of Patent: November 11, 1986
    Assignee: Mitsubishi Chemical Industries Ltd.
    Inventors: Kazumasa Kinugasa, Eiichiro Tanaka, Yoshihiro Tanaka, Yoshiharu Morita
  • Patent number: 4622317
    Abstract: Disorders of the skin resulting from over androgenicity, such as acne vulgaris, may be treated by applying, to affected areas of the skin, a composition containing a therapeutically effective amount of pregnenolone.
    Type: Grant
    Filed: October 7, 1985
    Date of Patent: November 11, 1986
    Assignee: University of Miami
    Inventors: Sung L. Hsia, Walter Voigt, Marty Sawaya, Kathryn Zeoli
  • Patent number: 4621079
    Abstract: A multistage combination preparation is useful for oral contraception and comprises a surprisingly low amount of gestodene as the gestagen and comprises ethinylestradiol as the estrogen.
    Type: Grant
    Filed: December 21, 1984
    Date of Patent: November 4, 1986
    Assignee: Schering Aktiengesellschaft
    Inventors: Ursula Lachnit-Fixson, Renate Unger
  • Patent number: 4619920
    Abstract: The invention provides a new derivative of vitamin D.sub.3, 26,26,26,27,27-pentafluoro-1.alpha.-hydroxy-27-methoxy-cholecalciferol and a process for preparing the same.The compound is characterized by some vitamin D-like activity except that it exhibits negligible activity in mobilizing bone. This characteristic indicates that the compound would find ready application in the treatment of disease or physiological states which evince loss of bone mass and application in other situations where metabolic calcium imbalances are found.
    Type: Grant
    Filed: September 16, 1985
    Date of Patent: October 28, 1986
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Nobuo Ikekawa, Yoshiro Kobayashi, Yoko Tanaka
  • Patent number: 4619922
    Abstract: 6.alpha.,16.alpha.-Dimethyl corticoids of general Formula I ##STR1## wherein the bond is a single bond or a double bond,X is a hydrogen atom, a fluorine atom, a chlorine atom, or a bromine atom,R.sub.1 is a formyl group, an alkanoyl group or alkoxyalkyl group of 2-8 carbon atoms, or a benzoyl group, andY is a hydrogen atom, a chlorine atom, a hydroxy group, a formyl group, an alkanoyloxy group of 2-8 carbon atoms, or a benzoyloxy group,are pharmacologically effective compounds.
    Type: Grant
    Filed: January 2, 1985
    Date of Patent: October 28, 1986
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Annen, Henry Laurent, Helmut Hofmeister, Michael Topert
  • Patent number: 4618605
    Abstract: Disclosed is a process for the production of .beta.-elemonic acid from an alcoholic solution of gum elemi by recovering a crude mixture of elemi acids containing .beta.-elemonic acid, .DELTA..sup.7 .alpha.-elemonic acid and .DELTA..sup.8 .alpha.-elemolic acid by the use of a basic ion exchanger, isomerizing the .DELTA..sup.7 .alpha.-elemolic acid to .DELTA..sup.8 .alpha.-elemolic acid in a chlorinated hydrocarbon by use of a mineral acid, oxidizing the .DELTA..sup.8 .alpha.-elemolic acid to yield additional .beta.-elemonic acid and separating and purifying the total resulting .beta.-elemonic acid from the acid mixture. Also disclosed are pharmaceutical preparations for the treatment of inflammatory conditions containing .beta.-elemonic acid as the active ingredient.
    Type: Grant
    Filed: October 15, 1984
    Date of Patent: October 21, 1986
    Inventors: Gunter Stapel, Karl-Heinz Gober, Sigurd Leyck, Helmut Wetzig, Christian Birkner, Kurt Kesselring, Bruno Christ, Klaus Steiner, Friedhelm Schroder
  • Patent number: 4618456
    Abstract: The process of the present invention transforms 16.alpha.- or 16.beta.-methyl-17-keto steroids (I) to the corresponding 17.alpha.-ethynyl-17.beta.-hydroxy-16.alpha.- or 16.beta.-methyl steroids (II) without epimerization and loss of stereochemistry of the 16.alpha.- or 16.beta.-methyl group.
    Type: Grant
    Filed: April 26, 1984
    Date of Patent: October 21, 1986
    Assignee: The Upjohn Company
    Inventor: Joseph M. Timko
  • Patent number: 4617297
    Abstract: The present invention relates to the method of treating disease states characterized by higher than normal levels of endogenously produced 1.alpha.,25 dihydroxy-cholecalciferol or conditions where there is an increased sensitivity to 1.alpha., 25 dihydroxy-cholecalciferol by administering to an organism suffering from such a disease state a pharmaceutically effective amount of the R or S epimer of 1.alpha.,25,26 trihydroxy-cholecalciferol.
    Type: Grant
    Filed: April 3, 1984
    Date of Patent: October 14, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alfred Boris, John J. Partridge, Milan R. Uskokovic
  • Patent number: 4617299
    Abstract: A novel pharmacologic therapy for treatment of idiopathic primary open angle glaucoma, drug-induced glaucoma and elevated intraocular pressure is disclosed. The pharmacologic therapy consists of a novel composition comprised of a selected anabolic androgenic compound and a physiologically tolerable carrier. In accordance with a method aspect of this invention, the pharmacologic substance is administered to the eye of a warm blooded animal in such a manner as to maintain physiologic or normal intraocular pressure, or to return elevated intraocular pressure to normal levels. The method aspect of this invention may also be employed to prevent drug induced elevated intraocular pressure.
    Type: Grant
    Filed: October 22, 1984
    Date of Patent: October 14, 1986
    Inventor: Paul A. Knepper
  • Patent number: 4616006
    Abstract: A method of contraception in which an estrogen and a progestogen are administered daily in a three phase sequence for 21 days is disclosed. In the first phase a combination of an estrogen and a progestogen in a low but contraceptively effective daily dosage corresponding in estrogenic activity to 0.02-0.05 mg of 17.alpha.-ethinylestradiol and in progestogenic activity to 0.065-0.75 mg of norethindrone is administered for 5-8 days; followed by the administering of the same dosage of estrogen and a progestogen corresponding in progestogenic activity to 0.25-1.0 mg of norethindrone for 7-11 days; followed by the administering of the same dosage of estrogen and a progestogen corresponding in progestogenic activity to 0.35-2.0 mg of norethindrone for 3-7 days; followed by 6-8 days without administering either an estrogen or a progestogen.
    Type: Grant
    Filed: June 13, 1985
    Date of Patent: October 7, 1986
    Assignee: Ortho Pharmaceutical Corporation
    Inventor: Samuel A. Pasquale