Patents by Inventor Robert Nickolson

Robert Nickolson 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: 5190973
    Abstract: The invention concerns 20-alkyl-7-oxoprostacyclin derivatives of general Formula I ##STR1## wherein R.sub.1 is the residue OR.sub.3 where R.sub.3 means hydrogen or alkyl of 1-10 carbon atoms optionally substituted by halogen, phenyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -dialkylamino; cycloalkyl, aryl or a heterocyclic residue, or the residue NHR.sub.4 where R.sub.4 means hydrogen or an alkanoyl or alkanesulfonyl residue of respectively 1-10 carbon atoms,n is 1 or 2,A is a CH.sub.2 --CH.sub.2 --, cis--CH.dbd.CH-- or trans--CH.dbd.CH--group,W is a ##STR2## or a ##STR3## wherein the OH-group can respectively be esterified with a benzoyl or alkanoic acid residue of 1-4 carbon atoms, or etherified with a tetrahydropyranol, tetrahydrofuranyl, alkoxyalkyl or trialkylsilyl residue, wherein the free or esterified OH-group can be in the .alpha.- or .beta.-position,R.sub.2 is a straight-chain or branched-chain alkyl group of 1-6 carbon atoms,R.sub.
    Type: Grant
    Filed: October 19, 1990
    Date of Patent: March 2, 1993
    Assignee: Schering Aktiengesellschaft
    Inventors: Robert Nickolson, Helmut Vorbrueggen, Claus S. Stuerzebecher, Martin Haberey
  • Patent number: 4721729
    Abstract: Carbacyclins of Formula I ##STR1## wherein R.sub.1 is an alkyl, cycloalkyl, aryl, aralkyl, or heterocyclic group,Y is a keto group or a hydroxymethylene group,X is a --CH.sub.2 -- group or an oxygen atom,A is a --CH.sub.2 --CH.sub.2 --, a trans--CH.dbd.CH-- or a --C.tbd.C-- group,W is a hydroxymethylene group or a ##STR2## D is the group ##STR3## a straight-chain or branched, saturated alkylene group or unsaturated alkylene group of up to 5 carbon atoms which can optionally be substituted by 1-2 fluorine atoms,n is 1, 2 or 3,E is a direct bond, a --C.tbd.C-- group or a --CR.sub.4 .dbd.CR.sub.5 -- group wherein R.sub.4 is hydrogen or an alkyl group and R.sub.5 is hydrogen, halogen or an alkyl group,R.sub.2 is an alkyl, cycloalkyl, aryl, or heterocyclic group, andR.sub.3 is a hydroxy group,are valuable, e.g., as cytoprotective agents.
    Type: Grant
    Filed: February 8, 1985
    Date of Patent: January 26, 1988
    Assignee: Schering Aktiengesellschaft
    Inventors: Werner Skuballa, Bernd Raduechel, Helmut Vorbrueggen, Robert Nickolson, Martin Haberey, Olaf Loge, Claus-Steffen Stuerzebecher
  • Patent number: 4532236
    Abstract: Prostacyclin derivatives of general Formula I ##STR1## wherein R.sub.1 is the residue OR.sub.3 wherein R.sub.3 means hydrogen or alkyl of 1-10 carbon atoms substituted, if desired, by halogen, aryl, C.sub.1 -C.sub.4 -alkoxy, or C.sub.1 -C.sub.4 -dialkylamino; cycloalkyl, aryl, or a heterocyclic residue; or is the residue NHR.sub.4 wherein R.sub.4 means hydrogen, an alkanoyl residue, or an alkanesulfonyl residue of respectively 1-10 carbon atoms,A is a --CH.sub.2 --CH.sub.2 -- or trans--CH.dbd.CH--group,W is a ##STR2## wherein the OH-group can be respectively esterified with a benzoyl or alkanoic acid residue of 1-4 carbon atoms, or can be etherified with a tetrahydropyranyl, tetrahydrofuranyl, C.sub.1 -C.sub.4 -alkoxyalkyl, or tri(C.sub.1 -C.sub.4 -alkyl)-silyl residue, wherein the free or esterified OH-group can be in the .alpha.- or .beta.-position,D and E jointly mean a direct bond orD is a straight-chain or branched alkylene group of 1-5 carbon atoms,E is an oxygen atom or a direct bond,R.sub.
    Type: Grant
    Filed: July 27, 1983
    Date of Patent: July 30, 1985
    Assignee: Schering Aktiengesellschaft
    Inventors: Robert Nickolson, Helmut Vorbrueggen, Jorge Casals-Stenzel, Martin Haberey
  • Patent number: 4472310
    Abstract: The disclosure concerns 5.beta.-hydroxy-.DELTA..sup.6 -steroids of the general formula ##STR1## wherein R.sup.1 is hydrogen, acyl, lower alkyl, or the tetrahydropyranyl residue andR.sup.2, R.sup.3 individually are respectively hydrogen or jointly are methylene andX stands for oxygen, the groupings ##STR2## (wherein R.sup.4 means hydrogen or acyl) and ##STR3## (wherein R.sup.5 means hydrogen or lower alkyl) and a process for the preparation thereof by reacting corresponding 7.alpha.-chloro-5.beta.,6.beta.-epoxy steroids in an inert solvent with metallic zinc in a lower aliphatic carboxylic acid or dilute mineral acid at temperatures of between room temperature and 100.degree. C., preferably at 40.degree.-70.degree. C.The compounds producible by this method are intermediates for the preparation of 3-keto-.DELTA..sup.4 -6.beta.,7.beta.-methylene steroids constituting pharmacologically valuable compounds, for example aldosterone antagonists.
    Type: Grant
    Filed: March 11, 1982
    Date of Patent: September 18, 1984
    Assignee: Schering Aktiengesellschaft
    Inventors: Dieter Bittler, Henry Laurent, Klaus Nickisch, Robert Nickolson, Rudolf Wiechert
  • Patent number: 4348327
    Abstract: 17.alpha.-hyroxy- and 17a.alpha.-hydroxy-D-homoetiocarboxylic acids of the formula ##STR1## wherein n is 1 or 2,A is ##STR2## and R.sub.1 is H or CH.sub.3are prepared by hydrating the corresponding 17-nitriles with a mixture of a lower carboxylic acid and its anhydride in the presence of perchloric acid. The resultant 17.beta.-N-acylcarboxamide is then treated with an alkali metal hydroxide in a polyhydric alcohol at an elevated temperature. The product acids are intermediates, e.g., for the production of steroids having antiinflammatory activity.
    Type: Grant
    Filed: June 23, 1981
    Date of Patent: September 7, 1982
    Assignee: Schering Aktiengesellschaft
    Inventors: Robert Nickolson, Ulrich Kerb, Rudolf Wiechert, Leo Alig, Andor Furst, Marcel Muller
  • Patent number: 4089852
    Abstract: .DELTA..sup.16 -21-HYDROXY-20-KETO STEROIDS OF THE PREGNANE SERIES HAVING AN OTHERWISE UNSUBSTITUTED D-ring and a 13-methyl or -ethyl group, and 21-ethers and -esters thereof, are produced by reaction of a corresponding D-ring saturated 17-keto steroid with a lithium compound of the formula ##STR1## thereby converting the 17-keto group to a 17.beta.-hydroxy-20.alpha.-enol ether in which the 17.alpha.-side chain has the formula ##STR2## wherein R.sub.3 and R.sub.4 have the values given above, and, in any desired sequence, splitting off R.sub.3 and/or R.sub.4 enol ether by hydrolysis; eliminating 17.beta.-hydroxy group, preferably after acylation, with formation of a .DELTA..sup.16 -double bond; and, if desired, splitting off any blocking group.
    Type: Grant
    Filed: May 4, 1976
    Date of Patent: May 16, 1978
    Assignee: Schering Aktiengesellschaft
    Inventor: Robert Nickolson
  • Patent number: 4029692
    Abstract: The present disclosure relates to steroid carboxylic acids and derivatives thereof. More particularly, the disclosure is concerned with D-homosteroid carboxylic acids and their derivatives, a process for the preparation thereof and pharmaceutical compositions containing same. The instant compounds are active endocrinal agents, especially as antiinflammatory agents.
    Type: Grant
    Filed: March 29, 1976
    Date of Patent: June 14, 1977
    Inventors: Leo Alig, Robert Nickolson, Rudolf Wiechert, Andor Furst, Klaus Kieslich, Marcel Muller, Ulrich Kerb