Patents Examined by Joseph A. Lipovsky
  • Patent number: 4719110
    Abstract: The present invention provides for boron-containing wood preserving solutions and a method for their preparation. The wood preserving solutions of the invention are noncrystallizable at ambient temperatures and are prepared from a dispersion of a particulated sodium tetraborate, phosphoric acid and water by heating the dispersion at elevated temperatures and for a period of time sufficient to provide a clear solution. The particulated sodium tetraborate and phosphoric are present in the dispersion in a specific molar ratio of 5:3, said ratio being critical to achieving the noncrystallizable characteristic of the wood preserving solutions of the invention.
    Type: Grant
    Filed: August 26, 1985
    Date of Patent: January 12, 1988
    Assignee: Kerr-McGee Chemical Corporation
    Inventors: Keshav P. Patel, William C. Laughlin, Roger A. Baldwin
  • Patent number: 4719054
    Abstract: A process and novel starting materials for the production of 17.alpha.-ethynyl-17.beta.-hydroxy-18-methyl-4,15-estradien-3-one of Formula I ##STR1## are disclosed. Novel 17-ketone starting materials have the Formula II ##STR2## wherein R is an alkyl residue of 1-3 carbon atoms and ##STR3## is the grouping ##STR4## wherein R' is an acyl group of up to 10 carbon atoms.
    Type: Grant
    Filed: May 9, 1986
    Date of Patent: January 12, 1988
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Hofmeister, Henry Laurent, Hans-Peter Lorenz, Rudolf Wiechert
  • Patent number: 4717721
    Abstract: This invention relates to a method for enhancing cell differentiation in malignant cells by exposing the cells to a 1.alpha.-hydroxylated vitamin D derivative characterized by a 17-side chain greater in length than the cholesterol or ergosterol side chains.The method finds application in the treatment of neoplastic diseases including leukemoid diseases and, specifically, leukemia.
    Type: Grant
    Filed: May 30, 1985
    Date of Patent: January 5, 1988
    Assignee: Howard W. Bremer
    Inventors: Hector F. DeLuca, Heinrich K. Schnoes, Nobuo Ikekawa, Voula Ostrem
  • Patent number: 4711881
    Abstract: 1.alpha.,25-Dihydroxy-26,27-dimethylcholecalciferol represented by formula: ##STR1## This compound is prepared by irradiating 26,27-dimethylcholesta-5,7-diene-1.alpha.,3.beta.,25-triol with ultraviolet light, and is useful for the prevention or treatment of calcium pathobolism or osteoporosis.
    Type: Grant
    Filed: August 7, 1985
    Date of Patent: December 8, 1987
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventor: Nobuo Ikekawa
  • Patent number: 4710495
    Abstract: Novel soft steroid anti-inflammatory agents, said agents being esters or thioesters of 17.alpha.-alkoxy-11.beta.-hydroxyandrost-4-en-3-one-17.beta.-carboxylic acids, pharmaceutical compositions containing said agents, novel chemical intermediates useful in the preparation of said agents and methods of administering same to mammals in the treatment of inflammation. Preferred compounds are the haloalkyl esters of 17.alpha.-alkoxy-11.beta.-hydroxyandrost-4-en-3-one-17.beta.-carboxylic acids.
    Type: Grant
    Filed: April 8, 1985
    Date of Patent: December 1, 1987
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventor: Nicholas S. Bodor
  • Patent number: 4708823
    Abstract: Known pregnane derivatives are prepared by esterificiation of known androstane derivatives to give new ester of Formula III ##STR1## wherein in each case symbolizes a single bond or a double bond,n is 1 or 2,R.sub.1 is hydrogen or methyl,R.sub.2 is hydrogen or formyl, andR.sub.3 is chlorine, hydroxy or an alkanoyloxy group of up to 6 carbon atoms,and reaction of the latter with Ag(I) and formic acid.
    Type: Grant
    Filed: September 17, 1985
    Date of Patent: November 24, 1987
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Hofmeister, Klaus Annen, Henry Laurent, Rudolf Wiechert
  • Patent number: 4704455
    Abstract: C.sub.16 -unsaturated corticoids are readily transformed to the corresponding 16.alpha.-methyl-17.alpha.-hydroxy corticoids by use of a .DELTA..sup.17 (.sup.20)-20-silyl ether.
    Type: Grant
    Filed: April 18, 1985
    Date of Patent: November 3, 1987
    Assignee: The Upjohn Company
    Inventors: Verlan H. VanRheenen, Joel E. Huber
  • Patent number: 4701451
    Abstract: Compounds of Formula I ##STR1## wherein the bond is a single bond or a double bond,X is hydrogen, fluorine, chlorine, or bromine,R.sub.1 is formyl, alkanoyl or alkoxyalkyl each of which contains 2-8 carbon atoms, or benzoyl, andY is chlorine, hydroxy, formyl, alkanoyloxy of 2-8 carbon atoms, or benzoyloxy,have valuable anti-inflammatory properties.
    Type: Grant
    Filed: October 29, 1985
    Date of Patent: October 20, 1987
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Annen, Henry Laurent, Helmut Hofmeister, Rudolf Wiechert, Michael Toepert, Hans Wendt
  • Patent number: 4701450
    Abstract: The invention relates to a group of .DELTA..sup.4 - and .DELTA..sup.5(10) -oestrene derivatives having an alkyl(1-4 C) substituent in position 6 or 7, an oxy substituent in position 17.beta. and optionally an oxo- or oxy-substituent in position 3 and a hydrocarbyl(1-4 C) group in position 17.alpha., for use as immunomodulator. The compounds are in particular suitable for therapeutic use in the treatment of auto-immune diseases.
    Type: Grant
    Filed: March 18, 1985
    Date of Patent: October 20, 1987
    Assignee: Akzo N.V.
    Inventors: Jan Kelder, Hermanus A. M. Verheul
  • Patent number: 4701454
    Abstract: The invention relates to a method of combatting fungal diseases with the aid of(a) an oomycetes controlling fungicide of formula I ##STR1## wherein R.sub.1, R.sub.2, independently, are H or CH.sub.3R.sub.3 is H, Cl, Br,X is CH(CH.sub.3)COOCH.sub.3, 2-oxo-tetrahydrofuran-3-yl, 2-oxo-tetrahydrothien-3-yl or 2-oxo-1,3-oxazolidin-3-yl andY is Ch.sub.2 OCH.sub.3, 2-furyl, benzyl, CH.sub.2 Cl, cyclopropyl or 3-isoxazolyl,in association with(b) Anilazine of formula II ##STR2## in admixture or separately in a fungicidally effective aggregate amount, and optionally other fungicides, and to fungicidal compositions comprising such fungicides.
    Type: Grant
    Filed: February 19, 1986
    Date of Patent: October 20, 1987
    Assignee: Sandoz Ltd.
    Inventors: Helmut Kaspers, Jiri Duben, Ulrich Gisi
  • Patent number: 4701449
    Abstract: Novel 10-substituted steroids of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl and substituted alkyl of 1 to 8 carbon atoms, alkenyl, substituted alkenyl, alkynyl and substituted alkynyl of 2 to 8 carbon atoms, aryl and substituted aryl, aralkyl and substituted aralkyl, protected hydroxy, optionally esterified carboxy, --NH.sub.2, protected amino, mono and di-alkyl amino of 1 to 4 alkyl carbon atoms, halogen and trialkylsilyl, R.sub.2 is methyl or ethyl, R.sub.6 and R.sub.7 together with the carbon atoms to which they are attached form cyclopropyl or R.sub.6 is hydrogen and R.sub.7 is R.sub.1, R.sub.1 is selected from the group consisting of hydrogen, alkyl and substituted alkyl of 1 to 6 carbon atoms, acetylthio and alkenyl, substituted alkenyl, alkynyl and substituted alkynyl of 2 to 6 carbon atoms, X is optionally acylated or etherified hydroxyl and Y is selected from the group consisting of hydrogen, R.sub.4, --CH.sub.2 --CH.sub.2 COOM and --CH.sub.2 --CH.sub.
    Type: Grant
    Filed: August 23, 1985
    Date of Patent: October 20, 1987
    Assignee: Roussel Uclaf
    Inventors: Vesperto Torelli, Lucien Nedelec, Martine Moguilewski, Anne-Marie Moura
  • Patent number: 4695625
    Abstract: A process for the preparation of 16,17 acetals of pregnane derivatives by trans-ketalization of 16,17-acetonides is described.In the instance of the preparation of 16.alpha.,17.alpha.-butylidenedioxy-11.beta.,21-dihydroxypregna-1,4-diene- 3,20-dione, a compound having useful therapeutic properties, known also as budesonide, it is possible to obtain the more active epimer with high selectivity and remarkable economic advantages in comparison with the known methods.New 16,17 acetals of pregnane derivatives, which can be prepared by the method of the invention, are also described.
    Type: Grant
    Filed: May 30, 1985
    Date of Patent: September 22, 1987
    Assignee: Sicor Societa Italiana Corticosteroidi S.p.A.
    Inventor: Peter Macdonald
  • Patent number: 4694012
    Abstract: This invention concerns a method of treatment using 1,4-dihydropyridine derivatives having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is aryl or heteroaryl;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl or 2-methoxyethyl;Y is --(CH.sub.2).sub.n --, --CH.sub.2 CH(CH.sub.3)-- or --CH.sub.2 C(CH.sub.3).sub.2 --;X is a 5 or 6 membered nitrogen containing aromatic heterocyclic ring which may optionally be substituted by one or more C.sub.1 -C.sub.4 alkyl, phenyl, benzyl, CN, --N(R.sup.3).sub.2, (CH.sub.2).sub.m CO.sub.2 H, (CH.sub.2).sub.m CO.sub.2 (C.sub.1 -C.sub.4 alkyl) or (CH.sub.2).sub.m CON(R.sup.3).sub.2 groups wherein each R.sup.3 is independently H or C.sub.1 -C.sub.4 alkyl and m is 0 or 1;and n is 1 to 3 when X is linked by a ring carbon atom or 2 or 3 when X is linked by a ring nitrogen atom.
    Type: Grant
    Filed: July 30, 1985
    Date of Patent: September 15, 1987
    Assignee: John Wyeth & Brother Limited
    Inventors: John L. Archibald, Terence J. Ward, Albert Opalko
  • Patent number: 4693889
    Abstract: This invention relates to bird repellent. In particular, this invention relates to new compositions for protecting surfaces from birds and to repelling birds from various areas. It is also directed to a method of preventing birds from remaining in selected areas.
    Type: Grant
    Filed: December 9, 1985
    Date of Patent: September 15, 1987
    Assignee: Velsicol Chemical Corporation
    Inventors: Michael T. Chirchirillo, Terrance Cannan
  • Patent number: 4689328
    Abstract: A process for controlling hyperlipidemia in mammals is disclosed. In this process a mammal suffering from hyperlipidemia is treated with a hyperlipidemia controlling effective amount of a compound having the structural formula ##STR1## wherein R.sup.1 is mercapto, amino, hydroxy or C.sub.1 -C.sub.4 alkylthio; R.sup.2 is amino, hydroxy or mercapto; and R.sup.3 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.7 -C.sub.9 alkoxyphenyl or C.sub.7 -C.sub.9 aralkyl.In another aspect of the present invention a pharmaceutical composition comprising the above compound in combination with a pharmaceutically acceptable carrier therefor is provided.
    Type: Grant
    Filed: December 31, 1985
    Date of Patent: August 25, 1987
    Assignee: Research Corporation
    Inventors: Iris H. Hall, George H. Cocolas
  • Patent number: 4689180
    Abstract: The invention provides a novel vitamin D derivative, 1.alpha.,25-dihydroxy-22Z-dehydrovitamin D.sub.2.The compound is characterized by unexpectedly high ability to raise serum calcium levels. The compound could therefore, find ready application as a substitute for vitamin D or its metabolites in the treatment of metabolic bone diseases or in other of their known applications.
    Type: Grant
    Filed: November 4, 1985
    Date of Patent: August 25, 1987
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Heinrich K. Schnoes, Rafal R. Sicinski, Yoko Tanaka
  • Patent number: 4689326
    Abstract: A process for controlling hyperlipidemia in mammals is disclosed. In this process a hyperlipidemia controlling effective amount of a compound having structural formula: ##STR1## where R.sup.1 is hydrogen, oxo, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl; R.sup.2 is hydrogen or oxo; and R.sup.3 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkanoyl, C.sub.2 -C.sub.6 carboxyalkyl, phenyl, benzyl or phenyl substituted with C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkanoyl, C.sub.1 -C.sub.6 alkoxy or halo is applied to mammals. A pharmaceutical composition comprising the above class of compounds having the meanings given herein and a pharmaceutical carrier therefor is also taught.
    Type: Grant
    Filed: October 17, 1985
    Date of Patent: August 25, 1987
    Assignee: Research Corporation
    Inventors: Iris H. Hall, Steven D. Wyrick, James M. Chapman, Jr.
  • Patent number: 4684636
    Abstract: 1'-Sulfonylsteroido[3,2-c]pyrazoles, for example, (5.alpha.,17.alpha.)-1'-(methylsulfonyl)-1'H-pregn-20-yno[3,2-c]pyrazol-17 -ol, which are useful as antiandrogenic agents, and processes for preparation, method of use and compositions thereof are disclosed.
    Type: Grant
    Filed: April 8, 1986
    Date of Patent: August 4, 1987
    Assignee: Sterling Drug Inc.
    Inventors: Robert G. Christiansen, Malcolm R. Bell, John L. Herrmann, Jr., Chester J. Opalka, Jr.
  • Patent number: 4681876
    Abstract: A valuable alternative antifungal antibiotic, for treatment especially of candidiasis, particularly vaginal candidiasis, is proposed. The antibiotic is a bile acid or simple derivative (salt or conjugate) thereof. Cholic, deoxycholic, chenodeoxycholic and lithocholic acid are preferred bile acids. The antibiotic is formulated for topical application. It can be used in association with an anti-inflammatory steroid for the treatment of fungal infections of the skin. It is also proposed to inhibit fungal growth in a variety of pharmaceutical compositions (containing some other active ingredient) by including in the composition, or coating a tablet, pill or capsule with, the bile acid component.
    Type: Grant
    Filed: July 15, 1985
    Date of Patent: July 21, 1987
    Assignee: National Research Development Corporation
    Inventors: Brian A. Marples, Reginald J. Stretton
  • Patent number: 4681875
    Abstract: Estriol esters of Formula I ##STR1## wherein R, in each case, means the residue of a monocarboxylic acid of 2-10 carbon atoms.The novel estriol esters surpass estriol in strength and duration of estrogen effect.
    Type: Grant
    Filed: May 16, 1985
    Date of Patent: July 21, 1987
    Assignee: Schering Aktiengesellschaft
    Inventors: Henry Laurent, Dieter Bittler, Sybille Beier, Walter Elger