Patents Examined by Elbert L. Roberts
  • Patent number: 4529546
    Abstract: Crude vitamin D.sub.3 is purified by reaction with a dienophile followed by short-path distillation.
    Type: Grant
    Filed: May 23, 1984
    Date of Patent: July 16, 1985
    Assignee: BASF Aktiengesellschaft
    Inventor: Martin Fischer
  • Patent number: 4528138
    Abstract: Antiinflammatory activity is exhibited by steroids having the formula ##STR1## and the 1,2-dehydro derivative thereof, wherein R.sub.1 is alkyl, mono-, di- or trifluoroalkyl, ##STR2## aryl or alkylthioalkyl, wherein R.sub.6 is alkyl or aryl and m is 1, 2, 3 or 4;R.sub.2 is ##STR3## wherein R.sub.7, R.sub.8 and R.sub.9 are each independently hydrogen or alkyl of 1 to 4 carbon atoms;R.sub.3 is carbonyl or .beta.-hydroxymethylene;R.sub.4 is hydrogen or halogen;R.sub.5 is hydrogen, methyl or fluorine; andn is 0, 1 or 2;with the proviso that if R.sub.1 is alkylthioalkyl, n is 0.
    Type: Grant
    Filed: June 20, 1984
    Date of Patent: July 9, 1985
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Ravi K. Varma, Donald S. Karanewsky
  • Patent number: 4528137
    Abstract: A fluorine-containing 3-oxygenated-.DELTA..sup.3,5 -steroid is prepared in a good yield by fluorinating a steroid with a compound of the formula:RCOOFwherein R is a hydrocarbon group.
    Type: Grant
    Filed: January 10, 1984
    Date of Patent: July 9, 1985
    Assignee: Daikin Kogyo Co., Ltd.
    Inventors: Takao Takahara, Kazuhiro Shimokawa
  • Patent number: 4528197
    Abstract: Method and composition for enhancing protein anabolism in an hypercatabolic mammal. The method comprises parenterally administering to the mammal nutritionally sufficient sources for amino acids, carbohydrates and lipids, the lipids comprising a controlled triglyceride source which, on hydrolysis, yields both long chain fatty acids and medium chain fatty acids, preferably about 20 to 80% long chain fatty acids and about 80 to 20% medium chain fatty acids. In one embodiment, the composition has the additional benefit of being capable of providing more than 60% of the total caloric requirements of the mammal via the lipid source without immunological impairment of the reticuloendothelial system of the mammal.
    Type: Grant
    Filed: January 26, 1983
    Date of Patent: July 9, 1985
    Assignee: KabiVitrum AB
    Inventor: George L. Blackburn
  • Patent number: 4526720
    Abstract: The process of the present invention uses an amine to prepare monolithium acetylide which is sufficiently stable at up to 0.degree. and yet is sufficiently reactive to react with 16-substituted-17-keto steroids producing the useful 17.alpha.-ethynyl-17.beta.-hydroxy-16-substituted steroids.
    Type: Grant
    Filed: January 5, 1984
    Date of Patent: July 2, 1985
    Assignee: The Upjohn Company
    Inventors: Verlan H. Van Rheenen, Dae Y. Cha
  • Patent number: 4525303
    Abstract: A novel process for preparing a steroid of the following formula (to be referred to as compound .circle.13 ) is provided. ##STR1## This compound is known to have marked anti-inflammatory and anti-rheumatoid arthritic activity with very much reduced side effects on humans, such as weight loss, sodium retention, potassium loss and adrenal and pituitary inhibition which are observed in many steroids. The process is characterized in that starting from hydrocortisone, it can produce the desired compound .circle.13 at low cost and that it goes through the following two novel compounds (I) and (II) as intermediates. ##STR2## In the above formulae, >W--X represents >C.dbd.O or >CH--OH, >Y--Z-- represents >C.dbd.CH-- or ##STR3## Q represents a hydrogen or bromine atom, and OR.sup.1 and OR.sup.2 are identical or different and each represents an acyloxy group or a sulfuric or phosphoric acid ester residue.
    Type: Grant
    Filed: June 17, 1983
    Date of Patent: June 25, 1985
    Assignee: Dainippon Ink and Chemicals Inc.
    Inventors: Hidetsugu Takagaki, Shigenori Nakanishi, Yasuyuki Tanaka, Michihiro Watanabe, Yoriko Yonehara
  • Patent number: 4522831
    Abstract: Ovarian follicular development and related hormonal secretions are totally suppressed for periods of several months or longer by a single intramuscular injection of anordrin administered during menstruation given preferably on the first day of menstrual bleeding. The amount of anordrin administered is in the range of 2 to 10 mg per kg of body weight, and is effective to produce the suppression without administration of additional anordrin by any route. Suppression of progesterone and estradiol secretions is of therapeutic value in the treatment of endometrosis, breast cancer, and other conditions aggravated by ovarian hormones.
    Type: Grant
    Filed: May 2, 1983
    Date of Patent: June 11, 1985
    Assignee: Northwestern University
    Inventor: Robert T. Chatterton, Jr.
  • Patent number: 4522758
    Abstract: 2-Fluoro-17.beta.-estradiol is synthesized by mercurating a 17.beta.-estradiol diacylate or dietherate at C-2, replacing the mercury group with fluorine and then cleaving the acyl or ether protecting groups.
    Type: Grant
    Filed: December 22, 1983
    Date of Patent: June 11, 1985
    Assignee: Eli Lilly and Company
    Inventors: John S. Ward, C. David Jones
  • Patent number: 4521410
    Abstract: A compound which is biologically active in maintaining calcium and phosphorous metabolism in animals, selected from the group consisting of formula (IA) and (IB): ##STR1## wherein the bond between carbons C-22 and C-23 is single or double; Y is hydrogen, F, --CH.sub.3 or --CH.sub.2 CH.sub.3 ; Z is F, H or X; Y' is H, --CH.sub.3 or --CH.sub.2 CH.sub.3 ; Z' is F or H; Q.sup.a is CF.sub.3 or CH.sub.2 X; Q.sup.b is CF.sub.3 or CH.sub.3 ; X is selected from the group consisting of hydrogen and --OR.sup.1, wherein R.sup.1 is hydrogen or an orthoester glycoside radical of the formula (II) ##STR2## where A represents a glucofuranosyl or glucopyranosyl ring; R.sup.2 is hydrogen, lower alkyl, aralkyl, or aryl; and R.sup.3 is hydrogen or a straight or branched chain glycosidic residue containing 1-100 glycosidic units per residue; with the proviso that at least one of the R.sup.1 is an orthoester glycoside moiety of formula (II).
    Type: Grant
    Filed: May 3, 1984
    Date of Patent: June 4, 1985
    Assignee: The General Hospital Corporation
    Inventors: Michael F. Holick, Sally A. Holick
  • Patent number: 4519949
    Abstract: New .DELTA.1,4,9(11)-pregnatrien-3-one-2o-carboxlic acid compounds are described, corresponding to general formula I below: ##STR1## in which X represents halogen, particularly chlorine or bromine or NH.sub.2. There is also described the process for producing compounds corresponding to general formula I by dehydrating the corresponding saturated starting compounds hydroxylated in the 11-position to form the 9(11)-ene-bond, after which the product obtained is, if desired, subjected to chemical transformation into the end products corresponding to general formula I. In particular, it is possible to carry out formation of the 20-acid halides and dehydration in the 9(11)-position in a single process step.
    Type: Grant
    Filed: September 24, 1982
    Date of Patent: May 28, 1985
    Assignee: Henkel Kommanditgesellschaft auf Aktien
    Inventor: Wolfgang Preuss
  • Patent number: 4518595
    Abstract: Diabetes is treated by orally administering a dehydroepiandrosterone (DHEA) compound selected from the group consisting of DHEA, DHEA sulfate and soluble DHEA compounds. The DHEA compound is preferably administered in finely dispersed form, powdered or solution, mixed with the food diet of the diabetic in a dosage range of up to 0.4% by weight of the food diet. The pharmacological activity and utility of DHEA as a potent anti-diabetic agent and anti-hyperglycemic agent over a variable range of genetic background is documented.
    Type: Grant
    Filed: July 19, 1983
    Date of Patent: May 21, 1985
    Assignee: The Jackson Laboratory
    Inventors: Douglas L. Coleman, Norman Applezweig, Edward H. Leiter
  • Patent number: 4517125
    Abstract: There are disclosed 6,19-epidioxyvitamin D.sub.3 derivatives which are represented by the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each a hydrogen atom or a hydroxyl group; when R.sub.1 is a hydrogen atom, R.sub.2 represents a hydroxyl group and R.sub.3 is a hydrogen atom or a hydroxyl group; when both R.sub.1 and R.sub.2 represent a hydroxyl group, R.sub.3 is a hydrogen atom or a hydroxyl group; and when R.sub.1 is a hydroxyl group and R.sub.2 is a hydrogen atom, R.sub.3 represents a hydroxyl group. The compounds are highly capable of inducing differentiation of human myeloid leukemia cells with minimum effects on calcium metabolism and are useful as an agent to treat leukemia.
    Type: Grant
    Filed: February 3, 1983
    Date of Patent: May 14, 1985
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Hiroaki Takayama, Sachiko Yamada, Keiko Nakayama, Tatsuo Suda
  • Patent number: 4515786
    Abstract: R.sup.3 is a C.sub.1-6 alkyl group or a C.sub.3-7 cycloalkyl group; andR.sup.4 is a group --OR.sup.5 or --OCOR.sup.6 whereR.sup.5 is an optionally substituted alkyl or alkenyl group which may contain up to 6 carbon atoms, an optionally substituted C.sub.3-7 cycloalkyl group, a phenyl group or a carbon-attached 5-7 membered heterocyclic ring in which the hetero-atom is selected from nitrogen, oxygen and sulphur, andR.sup.6 is a hydrogen atom or a group R.sup.5 as defined above;provided that when the compounds contain a 5.beta.-hydrogen atom, R.sup.2 is a hydrogen atom and salts thereof, which compounds have activity as antidysthythmic agents.
    Type: Grant
    Filed: June 30, 1983
    Date of Patent: May 7, 1985
    Assignee: Glaxo Group Limited
    Inventors: Gordon H. Phillipps, David C. Humber, George B. Ewan, Barry A. Coomber
  • Patent number: 4515810
    Abstract: A pharmaceutical composition of matter useful as a topical medicament which comprises an E-type prostaglandin compound or other water unstable active ingredient in a quick-breaking foam formulation to be dispensed from a pressurized container through a metered valve.
    Type: Grant
    Filed: October 6, 1983
    Date of Patent: May 7, 1985
    Assignee: American Cyanamid Company
    Inventors: San-Laung Chow, Bernard Sims
  • Patent number: 4515787
    Abstract: Novel 9.alpha.,11.beta.-dichloro-16.alpha.-methyl-.DELTA..sup.1,4 -pregnadiene 3,20-diones of the formula ##STR1## wherein R is selected from the group consisting of trimethylsilylphenyl, cyclododecyloxy, dicyclopentylmethoxy and cyclohexylmethoxy having a suprising "in loco" anti-inflammatory activity limited to place of inflammation without systemic effects and a process for their preparation.
    Type: Grant
    Filed: September 15, 1983
    Date of Patent: May 7, 1985
    Assignee: Roussel Uclaf
    Inventors: Jean G. Teutsch, Roger Deraedt, Josette Benzoni
  • Patent number: 4515778
    Abstract: The present invention provides a preparation for conditioning and grooming the hair. The active ingredients are vegetable lecithins, as well as cytochromes, phosphatidyl inositols, phosphatides and phosphatidic acids. Apart from the vegetable lecithins the other active ingredients are obtained by aqueous or ethereal extraction from fresh animal hearts, more particularly bovine hearts.
    Type: Grant
    Filed: April 27, 1983
    Date of Patent: May 7, 1985
    Inventor: Wolfgang Kastell
  • Patent number: 4514393
    Abstract: Derivatives of biliary acids having formula I ##STR1## wherein St has the meaning of the 17-etiocholanyl residue, having two or more hydroxyl groups both in the .alpha. and .beta. conformation, some of which being optionally replaced by keto groups, and their pharmaceutically acceptable salts with alkaline or alkali-earth metals, or with organic bases.
    Type: Grant
    Filed: July 22, 1983
    Date of Patent: April 30, 1985
    Assignee: Lehner AG
    Inventors: Virginio Castagnola, Giuliano E. Frigerio, Roberto Pellicciari
  • Patent number: 4512986
    Abstract: Novel steroids having the formula ##STR1## wherein R.sup.1 is selected from the group consisting of methyl, ethyl, and propyl;R.sup.2 is selected from the group consisting of H and methyl;R.sup.3 is selected from the group consisting of OXO and H(OR.sup.5); ##STR2## wherein R.sub.4 is selected from the group consisting of H.sub.2, H(methyl), H(Cl), H(F), and .dbd.CH.sub.2 ; or ##STR3## wherein R is selected from the group consisting of H, methyl, Cl, and F. Q-S is selected from the group consisting of --CH.dbd.CH-- and --CH.sub.2 CH--.Also disclosed is a method for making and therapeutically using the steroids and for making the intermediates.
    Type: Grant
    Filed: July 26, 1983
    Date of Patent: April 23, 1985
    Assignee: Research Triangle Institute
    Inventors: Jerry R. Reel, Clarence E. Cook
  • Patent number: 4512925
    Abstract: This invention provides novel 1,23-dihydroxyvitamin D compounds, a process for preparing such compounds of novel intermediates in such process.As indicated by its binding affinity for the 1.alpha.,25-dihydroxyvitamin D.sub.3 receptor protein, the compounds of this invention would function as effective substitutes for vitamin D and certain vitamin D metabolites for the regulation of calcium and phosphorous metabolism and for treatment of bone-related diseases.
    Type: Grant
    Filed: September 14, 1983
    Date of Patent: April 23, 1985
    Assignee: Wisconsin Alumini Research Foundation
    Inventors: Hector F. DeLuca, Heinrich K. Schnoes, Seok-Ho Lee
  • Patent number: 4512987
    Abstract: The invention concerns new pharmaceutical preparations for topical administration, such as creams, ointments, foams, pastes or gels, which contain the anti-inflammatorily active glucocorticoid 2-chloro-6.alpha.,9.alpha.-difluoro-16.alpha.-methyl-11.beta.,17.alpha.,21 -trihydroxy-pregna-1,4-diene-3,20-dione (2-chloroflumethasone, halometasone) and the antimicrobial agent 2,4,4'-trichloro-2'-hydroxy-diphenyl ether (triclosan). The new dermatics may contain, besides these two components, pharmaceutical carriers as usually present in formulations for topical administration. The new dermatics are especially suitable for the treatment of inflected forms of acute eczematous dermatoses of different origin, for the initial treatment of strongly inflamed dermatomycoses or strongly inflamed forms of pyodermias.
    Type: Grant
    Filed: October 13, 1982
    Date of Patent: April 23, 1985
    Assignee: Ciba-Geigy Corporation
    Inventor: Ctibor Schindlery