Patents Examined by Elbert L. Roberts
  • Patent number: 4444689
    Abstract: 17.alpha.-Acyloxy-5.beta.-pregnanes (I) and 17.alpha.-acyloxy-5.alpha.-pregnanes (IV) have an excellent activity split providing high topical anti-inflammatory activity with very low systemic side effects.
    Type: Grant
    Filed: September 3, 1981
    Date of Patent: April 24, 1984
    Assignee: The Upjohn Company
    Inventors: Donald E. Ayer, Carl A. Schlagel
  • Patent number: 4443440
    Abstract: Novel solution stable ester prodrugs of corticosteroids of the formula ##STR1##
    Type: Grant
    Filed: August 30, 1982
    Date of Patent: April 17, 1984
    Assignee: The Upjohn Company
    Inventors: Bradley D. Anderson, Robert A. Conradi
  • Patent number: 4443377
    Abstract: 17.alpha.-Hydroxy-6,16-dimethylenepregn-4-ene-3,20-dione simultaneously isomerized and acylated to 17.alpha.-hydroxy-6-methyl-16-methylenepregna-4,6-diene-3,20-dione 17-acetate.
    Type: Grant
    Filed: September 20, 1982
    Date of Patent: April 17, 1984
    Assignee: The Upjohn Company
    Inventor: Verlan H. Van Rheenen
  • Patent number: 4442119
    Abstract: Estrogenic cyclopropyl analogs, when administered to a female subject, function as anti-fertility agents to prevent pregnancy in the subject. Further, the estrogenic cyclopropyl analogs may be used as estrogenic agents to produce an estrogenic response in a female subject. The estrogenic cyclopropyl analogs useful as estrogenic agents have the general structure: ##STR1## wherein: X is a halogen or hydrogen atom:R.sub.1 is a hydrogen atom, an alkyl group containing from 1 to about 3 carbon atoms, a monocyclic group, a hydroxy substituted monocyclic group, or an alkoxy substituted monocyclic group in which the alkyl substitutent contains from 1 to about 3 carbon atoms;R.sub.2 is a hydrogen atom, an acetate group, a hydroxyl group, an alkoxy group in which the alkyl substituent contains from 1 to about 3 carbon atoms, a beta-dialkylaminoethoxy group in which the alkyl substituent contains from 1 to about 3 carbon atoms, a beta-monoaminoheterocycloethoxy group, or pharmaceutically acceptable salts thereof;R.sub.
    Type: Grant
    Filed: July 26, 1982
    Date of Patent: April 10, 1984
    Assignee: The Board of Regents for the University of Oklahoma
    Inventors: Robert A. Magarian, Joseph T. Pento
  • Patent number: 4442037
    Abstract: Complexes of albumin combined with organic dibasic acid half esters, such as those of succinic acid and phthalic acid, of 7-hydroxycholesterol are soluble in water and have excellent immunosuppressive and anti-inflammatory action.
    Type: Grant
    Filed: September 28, 1982
    Date of Patent: April 10, 1984
    Inventors: Yoshio Arakawa, Atsuyuki Takanabe, Yahiro Uemura, Satoshi Funakoshi, Tadakazu Suyama
  • Patent number: 4442093
    Abstract: Pharmaceutical composition in dosage unit form, comprising a therapeutically effective amount of 24,25-dihydroxycholecalciferol and a pharmaceutically acceptable carrier. The compound of 24,25-dihydroxycholecalciferol has anti-hypercalcemic activity, anti-ulcer activity, activity of preventing reduction of immunity, activity of controlling magnesium-metabolism, anti-hyperphosphatemic activity, activity of controlling blood sugar level and anti-tumor activity.
    Type: Grant
    Filed: May 4, 1982
    Date of Patent: April 10, 1984
    Assignee: Kureha Kagaku Kogyo Kabushiki Kaisha
    Inventors: Yuji Maeda, Takayoshi Fujii, Yasuhiko Kobayashi, Kenichi Saito, Tadaaki Kato, Chikao Yoshikumi
  • Patent number: 4442035
    Abstract: Acyclic amines are used to transform 9.alpha.-substituted-11.beta.-hydroxy 21-acyloxy steroids to the corresponding 9.beta.,11.beta.-epoxy 21-acyloxy steroids without removal of the C.sub.17 or C.sub.21 ester. The acyclic amines are cheaper and easier to prepare than previously disclosed dehydrohalogenating agents which do not produce cleavage of the C.sub.21 ester.
    Type: Grant
    Filed: October 25, 1982
    Date of Patent: April 10, 1984
    Assignee: The Upjohn Company
    Inventor: Clifford E. Sacks
  • Patent number: 4440689
    Abstract: There is disclosed novel intermediates, i.e. acyloxysteroids, which are useful for the preparation of corticoids such as hydrocortisone and prednisolone, and a process for producing the same.
    Type: Grant
    Filed: July 8, 1982
    Date of Patent: April 3, 1984
    Assignee: Mitsubishi Chemical Industries, Limited
    Inventors: Issei Nitta, Shinichiro Fujimori, Toshio Haruyama, Shinya Inoue
  • Patent number: 4440684
    Abstract: A process for preparing 6-methyl-.DELTA..sup.4,6 -3-keto steroids of the formula ##STR1## comprises reacting a corresponding .DELTA..sup.4 -3-keto steroid with methoxymethyl acetate (CH.sub.3 --O--CH.sub.2 --OAc) in an inert solvent at temperatures above room temperature in the presence of an alkali metal acetate.
    Type: Grant
    Filed: February 4, 1983
    Date of Patent: April 3, 1984
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Annen, Henry Laurent, Helmut Hofmeister, Rudolf Wiechert
  • Patent number: 4440688
    Abstract: Novel compounds which are 7-acylderivatives of ursodeoxycholic acid are described of formula ##STR1## in which R-CO is the residue from a linear, saturated or unsaturated, carboxylic acid of 2-18 carbon atoms or the residue from a cycloalkanecarboxylic acid of 3-7 carbon atoms in the cycloalkane ring. The novel compounds are useful in the therapy of biliary calculosis, biliary diskinesia and hypertriglyceridemia.
    Type: Grant
    Filed: June 28, 1982
    Date of Patent: April 3, 1984
    Inventors: Carlo Scolastico, Cesare Sirtori, David Kritchevsky
  • Patent number: 4440764
    Abstract: Water-soluble esters of steroid-oxazole derivatives of formula I ##STR1## wherein R is O or a H, (.beta.-OH) group, R.sub.1 is hydrogen, lower alkyl or phenyl, X is hydrogen, fluorine or chlorine, A stands for a direct carbon-carbon bond or a hydrocarbon chain containing from 1 to 4 carbon atoms, and M is hydrogen or a pharmaceutically acceptable cation are described as well as pharmaceutical compositions containing them particularly suitable for parenteral administration.
    Type: Grant
    Filed: April 27, 1981
    Date of Patent: April 3, 1984
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Giangiacomo Nathansohn, Giorgio Winters
  • Patent number: 4440690
    Abstract: Disclosed is an improved process for the synthesis of 6-bromo-17,21-dihydroxy-3,11,20-trioxo-1,4,-pregnadienes 17,21-diesters. In particular, this invention relates to the conversion of 17,21-dihydroxy-3,11,20-trioxo-1,4-pregnadienes 17,21-diesters to 6-borom-17,21-dihyroxy-3,11,20-trioxo-1,4-pregnadienes-17-21-diesters via bromination under ionic conditions, e.g. bromine in acetic acid.
    Type: Grant
    Filed: December 27, 1982
    Date of Patent: April 3, 1984
    Assignee: Schering Corporation
    Inventors: Elliot L. Shapiro, Lawrence E. Finkenor
  • Patent number: 4439432
    Abstract: This invention relates to the composition of a biologically compatible high concentration solution of progesterone, which is stable and non-toxic, and which can be used transdermally, orally, and in suppository and pessary form for the correction of progesterone deficiency states and other diseases.
    Type: Grant
    Filed: March 22, 1982
    Date of Patent: March 27, 1984
    Inventor: Raymond F. Peat
  • Patent number: 4439366
    Abstract: Novel compounds are described, which are 7-acyl-chenodeoxycholic acid of formula (I) ##STR1## in which R-CO is the residue from a linear, saturated or unsaturated carboxylic acid of 3-18 carbon atoms or the residue from a cycloalkanecarboxylic acid of 3-7 carbon atoms in the cycloalkane ring. The compounds are prepared by selective hydrolysis of the 3,7-diacyl derivatives of chenodeoxycholic acid. The compounds are valuable against biliary calculosis, diskinesia and hypertriglyceridemia.
    Type: Grant
    Filed: June 28, 1982
    Date of Patent: March 27, 1984
    Inventors: Carlo Scolastico, Cesare Sirtori, David Kritchevsky
  • Patent number: 4438033
    Abstract: New steroidal chiral phosphines of formula ##STR1## wherein R represents a phosphorated group selected between ##STR2## methods for their preparation; catalytic systems comprising metal complexes and the above steroidal chiral phosphines; asymmetrical catalytic processes like hydrogenation, hydroformylation and hydrocarbalkoxylation of prochiral compounds which employ said catalytic systems.
    Type: Grant
    Filed: November 18, 1982
    Date of Patent: March 20, 1984
    Assignee: Consiglio Nazionale Delle Ricerche
    Inventors: Carlo Botteghi, Serafino G. Gladiali, Mauro Marchetti, Giovanni A. Faedda
  • Patent number: 4438115
    Abstract: An agent for treating diseases in circulatory organs which comprises a piperazine compound of the formula ##STR1## wherein R.sub.1, R.sub.2 and A are as defined hereunder, or a salt thereof and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: June 10, 1981
    Date of Patent: March 20, 1984
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Hiroyuki Nagano, Mitiro Takagi, Noboru Kubodera, Isao Matsunaga, Tamotsu Yamazaki, Hiroyuki Nabata, Kazushige Sakai, Shun-ichi Hata
  • Patent number: 4436738
    Abstract: Loss of potency of estradiol cream compositions found to be due to unexpected oxidation of estradiol. Improved cream composition comprises 1% or less 17.beta.-estradiol in the presence of stabilizing members selected from phenolic-type antioxidants, metal chelating agents, and suspending agents.
    Type: Grant
    Filed: March 15, 1982
    Date of Patent: March 13, 1984
    Assignee: Mead Johnson & Company
    Inventors: Robert J. Bequette, Linda G. Hobbs, Joseph A. Scott
  • Patent number: 4435327
    Abstract: A process for the preparation of 3.beta.,7.beta.,15.alpha.-trihydroxy-5-androsten-17-one and the 3,15-dipivalate thereof comprises epimerizing 3.beta.,7.alpha.,15.alpha.-trihydroxy-5-androsten-17-one in the presence of a ketone with or without a solvent, with dilute mineral acid and subsequent treatment with an organic base, and optionally subsequently esterifying the 3.beta.- and 15.alpha.-positions of the resultant 3.beta.,7.beta.,15.alpha.-triol with a reactive derivative of pivalic acid.
    Type: Grant
    Filed: September 21, 1982
    Date of Patent: March 6, 1984
    Assignee: Schering, Aktiengesellschaft
    Inventors: Karl Petzoldt, Henry Laurent, Rudolf Wiechert
  • Patent number: 4435326
    Abstract: Androstenes having the formula ##STR1## wherein R.sub.1 hydrogen and R.sub.2 is alkyl, cycloalkyl, aryl, arylalkyl, alkylthioalkyl, alkoxyalkyl, alkanoyloxyalkyl, aroyloxyalkyl, alkoxycarobnylalkyl, carboxyalkyl, or arylalkyl, or R.sub.1 is alkanoyl or aroyl and R.sub.2 is alkyl;R.sub.3 is hydrogen, hydroxy, alkoxy, aryloxy, oxo, methylene, alkylthio, arylthio, alkanoyl, alkanoyloxy, or halogen;R.sub.4 is carbonyl, .beta.-hydroxymethylene or .beta.-acetyloxymethylene;R.sub.5 is hydrogen or halogen; and R.sub.6 is hydrogen, methyl, hydroxy, alkanoyl or halogen are useful intermediates for the preparation of steroids having antiinflammatory activity.
    Type: Grant
    Filed: September 9, 1982
    Date of Patent: March 6, 1984
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Ravi K. Varma
  • Patent number: 4435325
    Abstract: The monohydrate of 1.alpha.,25-dihydroxy-cholecalciferol having a remarkable vitamin activity and a process for its preparation.
    Type: Grant
    Filed: May 5, 1980
    Date of Patent: March 6, 1984
    Assignee: Roussel Uclaf
    Inventors: Jean Jolly, Primo Rizzi, Jean Taillardat