Patents by Inventor Helmut Vorbruggen

Helmut Vorbruggen has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 4105792
    Abstract: Prostan-1-ol esters and intermediates for their preparation are described; the former compounds exhibit improved organ specificity and a longer duration of activity at lower dosages than the corresponding non-esterified prostaglandins and are useful, inter alia, in triggering abortion, inducing labor and regulating the menstrual cycle.
    Type: Grant
    Filed: May 25, 1976
    Date of Patent: August 8, 1978
    Assignee: Schering Aktiengesellschaft
    Inventors: Werner Skuballa, Bernd Raduchel, Helmut Vorbruggen, Walter Elger, Olaf Loge, Eckehard Schillinger
  • Patent number: 4090021
    Abstract: N.sup.6 -substituted adenosines of the formula ##STR1## wherein R.sub.1 and R.sub.2 each are a hydrogen atom or an alkyl, aralkyl, aryl or heterocyclic ring, or R.sub.1 is a hydrogen atom and R.sub.2 is hydroxy, amino, alkyl terminally substituted, or R.sub.1 and R.sub.2 collectively with the nitrogen atom are a heterocyclic ring; R.sub.3 is a hydrogen atom, amino or silylated amino; and Z is a phosphoric acid esterified sugar radical; possess antiproliferative activity and have beneficial effects upon the cardiovascular system; are produced by reacting a 6-trialkylsilyloxy purine of the formula ##STR2## wherein each alkyl are alike; R.sub.3 ' is a hydrogen atom or trialkyl silylamine; and Z' is a sugar radical blocked with a phosphoric acid ester group, with ammonia or a primary or secondary amine, or with a corresonding salt of the amine, employing the amine salt or a Lewis acid as reaction catalyst.
    Type: Grant
    Filed: August 27, 1975
    Date of Patent: May 16, 1978
    Assignee: Schering Aktiengesellschaft
    Inventor: Helmut Vorbruggen
  • Patent number: 4088775
    Abstract: Prostanoic acid derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom, alkyl of 1-10 carbon atoms, aryl or --CH.sub.2 --U--V wherein U is a direct bond, carbonyl, or carbonyloxy and V is phenyl or substituted phenyl, e.g. substituted by at least one of phenyl, alkoxy of 1-2 carbon atoms or a halogen atom; one of R.sub.2 and R.sub.3 is hydroxy and the other is a hydrogen atom or R.sub.2 and R.sub.3 collectively are an oxygen atom; A is --CH.sub.2 --CH.sub.2 -- or trans--CH.dbd.CH; B is --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH; D and E collectively are a direct bond, or D is alkylene or 1-5 carbon atoms and E is an oxygen or sulfur atom; R.sub.4 is alkyl of 1-10 carbon atoms, alkyl of 1-5 carbon atoms substituted by unsubstituted or substituted aryl, unsubstituted or substituted aryl, or benzodioxol-2-yl-; X--Y is ##STR2## when one of R.sub.2 and R.sub.3 is a hydroxy group and the other is a hydrogen atom or X--Y is ##STR3## or --CH.dbd.CH-- when R.sub.2 and R.sub.
    Type: Grant
    Filed: July 11, 1975
    Date of Patent: May 9, 1978
    Assignee: Schering Aktiengesellschaft
    Inventors: Werner Skuballa, Bernd Raduchel, Helmut Vorbruggen, Walter Elger, Wolfgang Losert, Olaf Loge
  • Patent number: 4082911
    Abstract: The use of trialkylsilyl ester catalysts in place of Lewis acid or Friedel-Crafts catalysts in nucleoside synthesis gives increased yields and a simplified working-up process for recovering the nucleoside product.
    Type: Grant
    Filed: February 23, 1976
    Date of Patent: April 4, 1978
    Assignee: Schering Aktiengesellschaft
    Inventor: Helmut Vorbruggen
  • Patent number: 4004020
    Abstract: Prostaglandins of the formula ##STR1## wherein R.sub.1 is hydroxymethyl, carboxy, aryloxycarbonyl, alkoxycarbonyl of 1-8 carbon atoms in the alkoxy group, or the group -COO-CH.sub.2 -U-V wherein U is a direct C-C bond, carbonyl or carbonyloxy and V is phenyl substituted by phenyl, alkoxy of 1-2 carbon atoms or halogen; R.sub.2 is hydroxy and R.sub.3 is a hydrogen atom or R.sub.2 and R.sub.3 collectively are an oxygen atom; A is -CH.sub.2 -CH.sub.2 or trans-CH=CH; B is -CH.sub.2 -CH.sub.2 or CH=CH; one of R.sub.4 and R.sub.5 is hydroxy and the other is a hydrogen atom; R.sub.6 and R.sub.7 each are alkyl of 1-10 carbon atoms or collectively are alkylene of up to 7 carbon atoms and with 2-3 carbon atoms in the chain, phenylene or naphthylene; R.sub.8 is a hydrogen atom or alkyl of 1-5 carbon atoms; ##STR2## when R.sub.2 is hydroxy and R.sub.3 is a hydrogen atom or is ##STR3## or -CH=CH- when R.sub.2 and R.sub.3 collectively are an oxygen atom; or, when R.sub.
    Type: Grant
    Filed: December 19, 1974
    Date of Patent: January 18, 1977
    Assignee: Schering Aktiengesellschaft
    Inventors: Werner Skuballa, Bernd Raduchel, Helmut Vorbruggen, Walter Elger, Wolfgang Losert, Olaf Loge
  • Patent number: 3984454
    Abstract: Prostanoic acid esters of the formulaPG -- CH.sub.2 -- X -- Ywherein PG is the prostanoyloxy radical of a prostaglandin, X is a carbon-carbon single bond, carbonyl or carbonyloxy, and Y is substituted phenyl are easily crystallized compounds at least as active as the unesterified prostanoic acid and useful for the purification of the parent prostaglandin are prepared by reacting, in the presence of an agent which splits off hydrogen halide, the unesterified prostaglandin with a halide of the formula Hal--CH.sub.2 --X--Y, wherein Hal is a halogen atom and X and Y have the values given above.
    Type: Grant
    Filed: May 2, 1974
    Date of Patent: October 5, 1976
    Assignee: Schering Aktiengesellschaft
    Inventors: Werner Skuballa, Bernd Raduchel, Helmut Vorbruggen, Walter Elger, Olaf Loge, Wolfgang Losert
  • Patent number: 3983104
    Abstract: Novel N.sup.6 -substituted adenosines and a novel process for the preparation of N.sup.6 -substituted adenosines from 6-trialkylsiloxypurine derivatives. The derivatives are reacted in the presence of a tertiary base or a Lewis acid with ammonia or an amine of the formula HNR.sub.1 R.sub.2, wherein R.sub.1 and R.sub.2 are the same or different represent hydrogen, alkyl of 1-6 carbon atoms, aralkyl or 7 to 10 carbon atoms unsubstituted or substituted with hydroxy or alkoxy with 1-4 carbon atoms, aryl unsubstituted or substituted with hydroxy or alkoxy with 1 to 4 carbon atoms, a heterocyclic ring of 4 to 7 members, containing a total of 1-3 hetero atoms which can be nitrogen, oxygen or sulfur; or when R.sub.1 is hydrogen R.sub.
    Type: Grant
    Filed: October 6, 1972
    Date of Patent: September 28, 1976
    Assignee: Schering Aktiengesellschaft
    Inventor: Helmut Vorbruggen
  • Patent number: 3970692
    Abstract: Prostaglandin F.sub.2.sub..alpha. and analogs thereof of the formula ##SPC1##Wherein one of R.sub.1 and R.sub.2 is hydroxy and the other is H or CH.sub.3, R.sub.3 is the remainder of the lower side chain and X is the remainder of the upper side chain thereof are produced in two steps from a 3-acyloxy mono ester of a lactone of the formula ##SPC2##Wherein R.sub.1, R.sub.2 and R.sub.3 have the values given below, by reacting the lactone with excess diisobutylaluminum hydride and reacting the thus-produced ketol, in the presence of strong anhydrous base, with a Wittig reagent of the formula Ph.sub.3 P=CH--X--COOH wherein Ph is a phenyl group and X has the values given above.
    Type: Grant
    Filed: May 23, 1974
    Date of Patent: July 20, 1976
    Assignee: Schering Aktiengesellschaft
    Inventors: Bernd Raduchel, Werner Skuballa, Helmut Vorbruggen
  • Patent number: 3962218
    Abstract: Prostaglandins of the formula ##SPC1##Wherein R.sub.1 is HOCH.sub.2, --COOH, a salt thereof or an ester thereof; R.sub.2 is OH; and R.sub.3 is H or R.sub.2 and R.sub.3 collectively are = O. A is --CH.sub. 2 --CH.sub.2 -- or --(trans)--CH=CH--, B is --CH.sub. 2 CH.sub.2 --or --(cis)--CH=CH-- and R.sub.4 --O--O--R.sub.5 is a ketal group, are superior in physiological activity to the corresponding 15-.alpha.-hydroxy-prostaglandins.
    Type: Grant
    Filed: May 23, 1974
    Date of Patent: June 8, 1976
    Assignee: Schering Aktiengesellschaft
    Inventors: Bernd Raduchel, Werner Skuballa, Helmut Vorbruggen, Walter Elger, Wolfgang Losert, Olaf Loge