Patents Examined by Elbert L. Roberts
  • 7.alpha.-Acylthio-1.alpha.,2.alpha.-methylene- 3-oxo-17.alpha.-pregn-4-ene-21,17-carbolactones, their production and pharmaceutical preparations containing them
    Patent number: 4511565
    Abstract: 7.alpha.-acylthio-1.alpha.,2.alpha.-methylene-3-oxo-17.alpha.-pregn-4-ene-2 1,17-carbolactones of Formula I ##STR1## wherein ##STR2## and R is a lower saturated acyl radical of 2 to 4 carbon atoms,have a stronger antialdosterone effect and lower side effects than spironoloctone.
    Type: Grant
    Filed: October 28, 1983
    Date of Patent: April 16, 1985
    Assignee: Schering Aktiengesellschaft
    Inventors: Henry Laurent, Klaus Nickisch, Dieter Bittler, Rudolf Wiechert, Wolfgang Losert
  • Prednisolone derivatives
    Patent number: 4511511
    Abstract: Novel prednisolone derivatives modified at C-17,C-20 and/or C-21 positions. Many of the compounds are anti-inflammatory agents which do not significantly suppress the pituitary-adrenal axis.
    Type: Grant
    Filed: December 15, 1982
    Date of Patent: April 16, 1985
    Assignee: Crozer-Chester Medical Center
    Inventor: Marvin L. Lewbart
  • Methods of controlling the concentration of calcium in the serum of warm-blooded animals and pharmaceutical compositions to be used therefor
    Patent number: 4511564
    Abstract: The present invention relates to a method of controlling the concentration of calcium in the serum of warm-blooded animals characterized by the administration of a pharmaceutically effective amount of 25-hydroxyvitamin D.sub.3 -26,23-lactones expressed by the following formula (I) ##STR1## wherein R indicates a hydrogen atom or a hydroxyl group and X indicates --O-- or --O--O--, to warm-blooded animals, and a pharmaceutical composition to be used for controlling the concentration of calcium in the serum of warm-blooded animals which comprises 25-hydroxyvitamin D.sub.3 -26,23-lactones expressed by the above-mentioned formula (I) and a pharmaceutically acceptable carrier.25-hydroxyvitamin D.sub.3 -26,23-lactones are desirably used especially for the treatment or prevention of the diseases resulting from the high calcium levels in the serum.
    Type: Grant
    Filed: December 29, 1982
    Date of Patent: April 16, 1985
    Assignee: Teijin Limited
    Inventors: Seiichi Ishizuka, Junji Kubo
  • Synthesis of 1.alpha.,25-dihydroxyergocalciferol
    Patent number: 4508651
    Abstract: The invention is directed to a process and intermediates for the preparation of 1.alpha.,25-dihydroxyergocalciferol as well as substantially pure and crystalline 1.alpha.,25-dihydroxyergocolciferol. The end-product 1.alpha.,25-dihydroxyergocalciferol is useful in the treatment of disease states which are characterized by insufficient amounts of 1.alpha.,25-dihydroxycholecalciferol.
    Type: Grant
    Filed: March 21, 1983
    Date of Patent: April 2, 1985
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Enrico G. Baggiolini, Andrew D. Batcho, Alfred Boris, Milan R. Uskokovic
  • Manufacture of androstandione
    Patent number: 4507242
    Abstract: 5-.beta.-androstandione is produced in high yield by contacting androstendione with a palladium catalyst and thereafter recovering the 5-.beta.-androstandione thus produced.
    Type: Grant
    Filed: April 10, 1984
    Date of Patent: March 26, 1985
    Assignee: Progenics, Inc.
    Inventor: George Krsek
  • Treatment of diabetes and other symptoms of hypercorticoidism using a synergistic combination of etiocholanolones and estrogen
    Patent number: 4507289
    Abstract: Diabetes obesity syndromes and associated hypercorticoidism are treated with a synergistic combination of .alpha.- and/or .beta.-etiocholanolone and an estrogen.
    Type: Grant
    Filed: December 28, 1983
    Date of Patent: March 26, 1985
    Assignees: Progenics, Inc., The Jackson Laboratory
    Inventors: Douglas L. Coleman, Norman Applezweig
  • Esters of 17 .alpha.-ethynyl 19-nor-testosterone and 17 .alpha.-ethynyl-18-homo-19-nor-testosterone and pharmaceutical compositions containing the same
    Patent number: 4507290
    Abstract: Esters of 17 .alpha.-ethynyl 19-nor-testosterone and 17 .alpha.-ethynyl-18-homo-19-nor-testosterone and the 3-oximes thereof having long-active contraceptive activity.
    Type: Grant
    Filed: April 7, 1981
    Date of Patent: March 26, 1985
    Assignee: World Health Organization
    Inventors: Sydney Archer, Giuseppe Benagiano, Pierre Crabbe, Egon Diczfalusy, Carl Djerassi, Josef Fried
  • Process for the preparation of 3-(.DELTA..sup.4 -3-ketosteroid-17.alpha.-yl)propionic acid lactones
    Patent number: 4507238
    Abstract: A simple process for preparing 3-(.DELTA..sup.4 -3-keto-steroid-17.alpha.-yl)propionic acid lactones of the androstane series represented by the general partial formula ##STR1## wherein ABCD represents an optionally substituted cyclopentanophenanthrene steroid molecule skeleton, from corresponding 17.alpha.-(3-hydroxypropynyl)-17.beta.-hydroxy steroids, comprises reducing the latter to the 17.alpha.-(3-hydroxypropenyl)17.beta.-hydroxy steroid, effecting ring closure to the lactol, and subsequently oxidizing with chromic acid to the lactone.
    Type: Grant
    Filed: February 22, 1984
    Date of Patent: March 26, 1985
    Assignee: Schering Aktiengesellschaft
    Inventor: Klaus Junghans
  • Hydroxyvitamin D.sub.2 isomers
    Patent number: 4505906
    Abstract: The invention provides, as novel vitamin D derivatives, isomers of 25-hydroxyvitamin D.sub.2 and 1.alpha.,25-dihydroxyvitamin D.sub.2 characterized by a double bond at the 23,24-position.The compounds are characterized by vitamin D-like activity as assessed by competitive binding assays and would therefore, find application as substitutes for vitamin D or various of its metabolites in their various known applications and in the treatment of vitamin D-responsive bone diseases.
    Type: Grant
    Filed: January 30, 1984
    Date of Patent: March 19, 1985
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Heinrich K. Schnoes, Rafal R. Sicinski, Yoko Tanaka
  • 23,23-Difluoro-1.alpha.,25-dihydroxy-vitamin D.sub.3
    Patent number: 4502991
    Abstract: The invention provides a new derivative of vitamin D, 23,23-difluoro-1,25-dihydroxycholecalciferol.The compound is characterized by vitamin D-like activity as evidenced by its ability to increase intestinal calcium transport. It is further characterized by its resistance to hydroxylation at C-23, which is recognized as an essential metabolic step to the inactivation of vitamin D, and therefore should provide vitamin D-like activity of greater time duration.
    Type: Grant
    Filed: August 18, 1983
    Date of Patent: March 5, 1985
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Yoko Tanaka, Nobuo Ikekawa, Yoshiro Kobayashi
  • Aldosterone-antagonistic steroids
    Patent number: 4502989
    Abstract: Novel spironolactone derivatives characterized by the C.sub.11 -C.sub.12 double bond which have a potent aldosterone-antagonistic activity without causing potassium loss, used alone in diagnosis and improvement of condition of primary aldosteronism, or together with other drugs in treatment of essential or renal hypertension as well as cardiac or renal edema; prepared from 3,17-bis(ethylene-dioxy)-5,11-androstadiene.
    Type: Grant
    Filed: January 5, 1984
    Date of Patent: March 5, 1985
    Assignee: Shionogi & Co., Ltd.
    Inventors: Susumu Kamata, Takeaki Matsui, Nobuhiro Haga
  • Spironalactone process
    Patent number: 4501695
    Abstract: The present invention relates to processes for the conversion of a 3-protected steroidal 17-ketone to a 17-spiro-.gamma.-lactone having the appropriate 17-stereochemistry for spironolactone. Novel intermediates (II, II', II", II'", II.sup.a, II.sup.b, II.sup.c, II.sup.d, II.sub.x, II'.sub.x and II".sub.x) are also disclosed.
    Type: Grant
    Filed: May 16, 1983
    Date of Patent: February 26, 1985
    Assignee: The Upjohn Company
    Inventor: Verlan H. Van Rheenen
  • 20-Isocyano-.DELTA..sup.17(20) -steroids
    Patent number: 4501701
    Abstract: Novel 20-isocyano-.DELTA..sup.17(20) -steroids of the formula ##STR1## wherein R.sup.1 is selected from the group consisting of (1) hydrogen, (2) alkyl of 1 to 4 carbon atoms optionally substituted with a member of the group consisting of halogen, an oxygen function and a nitrogen function and (3) alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.2 is alkyl of 1 to 4 carbon atoms, Alk.sub.1, is alkyl of 1 to 8 carbon atoms and the A,B,C, and D rings may contain one or more double bonds and may be optionally substituted with at least one member of the group consisting of --OH, .dbd.0, halogens, alkyl and alkoxy of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms and a process for their preparation and their use to prepare 17.alpha.-ol-20-keto steroids.
    Type: Grant
    Filed: July 7, 1981
    Date of Patent: February 26, 1985
    Assignee: Roussel Uclaf
    Inventors: Derek H. R. Barton, William B. Motherwell, Sammir Z. Zard
  • Antimicrobial composition for a semipermeable membrane
    Patent number: 4500517
    Abstract: An antimicrobial composition useful to prevent microorganism growth on semipermeable membranes comprises an aqueous medium having a pH of less than 4.5 and sulfurous acid or a source of sulfurous acid.
    Type: Grant
    Filed: December 7, 1981
    Date of Patent: February 19, 1985
    Assignee: H. B. Fuller Co.
    Inventor: V. Gerold Luss
  • Suppression of premature labor by use of aromatase inhibitors
    Patent number: 4500523
    Abstract: This invention relates to the use of aromatase inhibitors to suppress premature labor in mammals by administering an aromatase inhibitor preferably 4-hydroxy-4-androstene-3,17-dione or 4-acetoxy-4-androstene-3,17-dione to a pregnant mammal.
    Type: Grant
    Filed: April 9, 1984
    Date of Patent: February 19, 1985
    Assignee: Cornell Research Foundation, Inc.
    Inventor: Nathanielsz
  • 7.alph a.-Acylthio-15,16-methylene-3-oxo-17.alpha.-pregna-1,4-diene-21,17-carbol actones, their preparation and use as medicinal agents
    Patent number: 4500522
    Abstract: 7.alpha.-acylthio-15,16-methylene-3-oxo-17.alpha.-pregna-1,4-diene-21,17-ca rbolactones of the formula ##STR1## wherein the 15,16-methylene group can be in the .alpha.- or .beta.-configuration, andR is a lower alkyl residue,have altialdosterone activity.They are prepared from corresponding .DELTA..sup.4 -unsaturated compounds by chemical or microbiological 1,2-dehydrogenation.
    Type: Grant
    Filed: July 22, 1983
    Date of Patent: February 19, 1985
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Nickisch, Dieter Bittler, Henry Laurent, Rudolf Wiechert, Wolfgang Losert
  • Cyanohydrin process
    Patent number: 4500461
    Abstract: Using cyanohydrin intermediates, 17-keto steroids are transformed to corticoids and 17.alpha.-acyl progesterones.
    Type: Grant
    Filed: February 3, 1984
    Date of Patent: February 19, 1985
    Assignee: The Upjohn Company
    Inventor: Verlan H. VanRheenen
  • 23,23-Difluoro-25-hydroxy-vitamin D.sub.3 and process for preparing same
    Patent number: 4500460
    Abstract: The invention provides a new derivative of vitamin D, 23,23-difluoro-25-hydroxycholecalciferol, a method for preparing said compound and various new intermediates utilized in such process.The compound is characterized by vitamin D-like activity as evidenced by its ability to increase intestinal calcium transport and serum calcium. It is further characterized by its resistance to hydroxylation at C-23, which is recognized as an essential metabolic step to the inactivation of vitamin D, and therefore should provide vitamin D-like activity of greater time duration.
    Type: Grant
    Filed: August 18, 1983
    Date of Patent: February 19, 1985
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Yoko Tanaka, Nobuo Ikekawa, Yoshiro Kobayashi
  • Mixed anhydrides and processes thereof
    Patent number: 4499020
    Abstract: Mixed anhydrides products are described. These mixed anhydrides are produced by reaction of a carboxylic acid-containing steroid with a material having the formula: ##STR1## wherein: X is a halogenZ is an oxygen or sulfurR is a hydrocarbonin an inert organic solvent containing a Lewis base. These mixed anhydrides may in turn be reacted with, for example, an alcohol ammonia or amine to produce the corresponding ester or amide steroid.
    Type: Grant
    Filed: February 22, 1983
    Date of Patent: February 12, 1985
    Assignee: Montefiore Hospital and Medical Center, Inc.
    Inventor: Iraj Lalezari
  • 17.beta.(Substituted thio)-16-ketoandrostene-17.alpha...-carboxylic acid derivatives
    Patent number: 4499021
    Abstract: Topical antiinflammatory activity is exhibited by steroids having the formula ##STR1## and the 1,2-dehydro derivative thereof whereinR.sub.1 is alkyl, cycloalkyl, aryl, alkanoyloxyalkyl or arylcarbonyloxyalkyl;R.sub.2 is alkoxy, aryloxy, arylalkoxy, alkylthio, arylthio, or dialkylamino;R.sub.3 is carbonyl, .beta.-hydroxymethylene or .beta.-acetyloxymethylene;R.sub.4 is hydrogen or halogen;R.sub.5 is hydrogen, methyl, hydroxy, alkanoyl, alkanoyloxy, or halogen; andn is 0, 1 or 2.
    Type: Grant
    Filed: April 12, 1984
    Date of Patent: February 12, 1985
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Ravi K. Varma