Patents by Inventor Klaus Nickisch

Klaus Nickisch 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: 4859659
    Abstract: Dermatics are claimed which are characterized in that they contain as the active compound one or two 17.beta.-methyl-18-nor steroids of general Formula I ##STR1## wherein is a single bond or a double bond,R.sub.1 is a hydrogen atom or a methyl group, andR.sub.2 is an alkyl group of maximally 6 carbon atoms, optionally substituted by an alkanoyloxy group containing 2-6 carbon atoms.
    Type: Grant
    Filed: December 17, 1986
    Date of Patent: August 22, 1989
    Assignee: Schering Aktiengesellschaft
    Inventors: Dieter Bittler, Henry Laurent, Klaus Nickisch, Petra Rach
  • Patent number: 4851526
    Abstract: Novel 1-(4-substituted phenyl)-1H-imidazoles and their use as antiarrhythmic, anti-hypertensive and anti-ischemic agents is described. Pharmaceutical formulations containing such compounds are also discussed.
    Type: Grant
    Filed: September 4, 1987
    Date of Patent: July 25, 1989
    Assignee: Schering A.G.
    Inventors: Stanley S. Greenberg, Randall E. Lis, William C. Lumma, Jr., Klaus Nickisch, Ronald A. Wohl
  • Patent number: 4804662
    Abstract: Novel substituted 4-[1H-imidazol-1-yl]benzamides and their use in the treatment of cardiac arrthythmias especially as Class III or combination Class I/III antiarrhythmic agents is described. Pharmaceutical formulations containing such compounds are also disclosed.
    Type: Grant
    Filed: May 5, 1987
    Date of Patent: February 14, 1989
    Assignee: Schering A.G.
    Inventors: Klaus Nickisch, Randall E. Lis, William C. Lumma, Jr., Thomas K. Morgan, Jr., Ronald A. Wohl
  • Patent number: 4789668
    Abstract: The disclosure relates to novel 1.alpha.,7.alpha.-dithio-substituted spirolactones of general Formula I ##STR1## wherein R.sup.1 is C.sub.1-3 -alkyl and C.sub.1-3 -acyl andR.sup.2 is hydrogen, C.sub.1-3 -alkyl and C.sub.1-3 -acyl,to their preparation, and to their use as medicinal agents.The compounds of this invention exhibit anti-aldosterone activity and show the profile of effectiveness of a pro-drug.
    Type: Grant
    Filed: October 17, 1986
    Date of Patent: December 6, 1988
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Nickisch, Henry Laurent, Dieter Bittler, Rudolf Wiechert, Wolfgang Losert
  • Patent number: 4614616
    Abstract: A process for preparing a 3.beta.,7.beta.-dihydroxy-.DELTA..sup.5 -steroid of the formula ##STR1## wherein Q is ##STR2## and R.sub.1 is hydrogen, trimethylacetyl, tert-butyldimethylsilyl, dimethyl-2-(3-methylbutyl)silyl or tribenzylsilyl, comprises fermenting a 3.beta.-hydroxy-.DELTA..sup.5 -steroid of the formula ##STR3## wherein Q is as defined above, andR.sub.2 is hydrogen or alkanoyl of 2-6 carbon atoms, with a culture of Botryodiplodia malorum to obtain the corresponding 3.beta.,7.beta.-dihydroxy-.DELTA..sup.5 -steroid; and, optionally, reacting the resultant product with trimethylacetic anhydride, tert-butyldimethylsilyl chloride, dimethyl-2-(3-methylbutyl)silyl chloride, or tribenzylsilyl chloride.
    Type: Grant
    Filed: September 26, 1983
    Date of Patent: September 30, 1986
    Assignee: Schering Aktiengesellschaft
    Inventors: Karl Petzoldt, Rudolf Wiechert, Henry Laurent, Klaus Nickisch, Dieter Bittler
  • Patent number: 4587235
    Abstract: Androstane derivatives of Formula I ##STR1## wherein is a single bond or a double bond,R.sub.1 is methyl or ethyl,R.sub.2 is hydrogen or alkyl of 1-8 carbon atoms,--X-- is --(CH.sub.2).sub.n --, --CH.dbd.CH(CH.sub.2).sub.m --, or --C.tbd.C--(CH.sub.2).sub.m -- wherein n is 2 to 6 and m is 1 to 4,--A--B-- is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --CCl.dbd.CH--, ##STR2## --U--V< is --CH.sub.2 --CH<, --CH.dbd.C<, --C(OH).dbd.C<, or --CCl.dbd.C<, and--W--Y-- is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --C(CH.sub.3).sub.2 --, or ##STR3## with the proviso that the compound is not 17.alpha.-(3-acetoxypropyl)-17.beta.-hydroxy-4,6-androstadien-3-one, are pharmacologically efficacious compounds, e.g., are sebum suppressive.
    Type: Grant
    Filed: June 27, 1984
    Date of Patent: May 6, 1986
    Assignee: Schering Aktiengesellschaft
    Inventors: Dieter Bittler, Henry Laurent, Klaus Nickisch, Rudolf Wiechert
  • Patent number: 4559331
    Abstract: Novel 7.alpha.-substituted 3-oxo-17.alpha.-pregn-4-ene-21,17-carbolactones of the formula ##STR1## wherein ##STR2## is a CC single or CC double bond or the group ##STR3## R.sup.7 is the group SR', R' being a hydrogen atom or a straight-chain or branched alkyl residue of 1-6 carbon atoms optionally substituted by a hydroxy or acyloxy group, the group COOR" or the group COR" wherein R" is an alkyl group of 1-4 carbon atoms and ##STR4## is a CC single bond or the group ##STR5## have antialdosterone activity with reduced endocrinological side effects.
    Type: Grant
    Filed: August 17, 1984
    Date of Patent: December 17, 1985
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Nickisch, Henry Laurent, Peter Esperling, Dieter Bittler, Rudolf Wiechert, Wolfgang Losert
  • Patent number: 4542024
    Abstract: New 15,16-methylene-17.alpha.-pregna-4,6-diene-21-carboxylic acid salts of formula I ##STR1## wherein R.sup.1 and R.sup.2 each alone is hydrogen or together they form an additional CC bond or a methylene group,M is an alkali metal,and the methylene group in the 15,16 position is in the .alpha. or .beta. position, in addition to having a strong antialdosterone effect, have reduced antiandrogenic and progestogenic side effects.
    Type: Grant
    Filed: July 13, 1984
    Date of Patent: September 17, 1985
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Nickisch, Dieter Bittler, Henry Laurent, Rudolf Wiechert, Wolfgang Losert
  • Patent number: 4542128
    Abstract: 17.alpha.-Pregn-4-ene-3-oxo-21-carboxylic acid esters of Formula I ##STR1## wherein C.sub.1 C.sub.2 is a CC single or C.dbd.C double bond,--A--B--is ##STR2## --C--D--is ##STR3## and R is an alkyl or alkenyl residue of up to 6 carbon atoms,in addition to antialdosterone activity, exhibit greatly reduced antiandrogenic and progestational side effects.
    Type: Grant
    Filed: July 22, 1983
    Date of Patent: September 17, 1985
    Assignee: Schering Aktiengesellschaft
    Inventors: Dieter Bittler, Henry Laurent, Klaus Nickisch, Rudolf Weichert, Jorge Casals-Stenzel
  • Patent number: 4511565
    Abstract: 7.alpha.-acylthio-1.alpha.,2.alpha.-methylene-3-oxo-17.alpha.-pregn-4-ene-2 1,17-carbolactones of Formula I ##STR1## wherein ##STR2## and R is a lower saturated acyl radical of 2 to 4 carbon atoms,have a stronger antialdosterone effect and lower side effects than spironoloctone.
    Type: Grant
    Filed: October 28, 1983
    Date of Patent: April 16, 1985
    Assignee: Schering Aktiengesellschaft
    Inventors: Henry Laurent, Klaus Nickisch, Dieter Bittler, Rudolf Wiechert, Wolfgang Losert
  • Patent number: 4500522
    Abstract: 7.alpha.-acylthio-15,16-methylene-3-oxo-17.alpha.-pregna-1,4-diene-21,17-ca rbolactones of the formula ##STR1## wherein the 15,16-methylene group can be in the .alpha.- or .beta.-configuration, andR is a lower alkyl residue,have altialdosterone activity.They are prepared from corresponding .DELTA..sup.4 -unsaturated compounds by chemical or microbiological 1,2-dehydrogenation.
    Type: Grant
    Filed: July 22, 1983
    Date of Patent: February 19, 1985
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Nickisch, Dieter Bittler, Henry Laurent, Rudolf Wiechert, Wolfgang Losert
  • 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: 4457925
    Abstract: Androstane derivatives of Formula I ##STR1## wherein ---- is a single bond or a double bond,R.sub.1 is methyl or ethyl,R.sup.2 is hydrogen or alkyl of 1-8 carbon atoms,--X-- is --(CH.sub.2).sub.n --, --CH.dbd.CH(CH.sub.2).sub.m --, or --C.tbd.C--(CH.sub.2).sub.m --wherein n is 2 to 6 and m is 1 to 4,--A--B-- is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --CCl.dbd.CH--, ##STR2## --U--V< is --CH.sub.2 --CH<, --CH.dbd.C<, --C(OH).dbd.C<, or --CCl.dbd.C<, and--W--Y-- is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --C(CH.sub.3).sub.2 --, or ##STR3## with the proviso that the compound is not 17.alpha.-(3-acetoxypropyl)-17.beta.-hydroxy-4,6-androstadien-3-one, are pharmacologically efficacious compounds, e.g., are sebum suppressive.
    Type: Grant
    Filed: July 29, 1982
    Date of Patent: July 3, 1984
    Assignee: Schering, Aktiengesellschaft
    Inventors: Dieter Bittler, Henry Laurent, Klaus Nickisch, Rudolf Wiechert
  • Patent number: 4450107
    Abstract: 7.alpha.-Alkoxycarbonyl-15.beta.,16.beta.-methylene-4-androstene compounds of Formula I ##STR1## wherein R.sup.1 is hydrogen or methyl,R.sup.2 is alkyl of 1-4 carbon atoms,X is ##STR2## and Y is carbonyl, andthe bond between the C-1 and C-2 carbon atoms is a single or double bond, orwhen the bond between the C-1 and C-2 carbon atoms is a single bond,X can also be ##STR3## when Y is ##STR4## possess valuable pharmacological properties, e.g., as aldosterone antagonists, i.e. they reverse the effect of deoxycorticosterone on the excretion of sodium and potassium.
    Type: Grant
    Filed: March 23, 1982
    Date of Patent: May 22, 1984
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Nickisch, Henry Laurent, Rudolf Wiechert, Jorge Casals-Stenzel
  • Patent number: 4416985
    Abstract: A process for preparing a 3.beta.,7.beta.-dihydroxy-.DELTA..sup.5 steroid of the formula ##STR1## wherein Q is ##STR2## and R.sub.1 is hydrogen, trimethylacetyl, tert-butyldimethylsilyl, dimethyl-2-(3-methylbutyl)silyl or tribenzylsilyl,comprises fermenting a 3.beta.-hydroxy-.DELTA..sup.5 -steroid of the formula ##STR3## wherein Q is as defined above, andR.sub.2 is hydrogen or alkanoyl of 2-6 carbon atoms,with a culture of Botryodiplodia malorum to obtain the corresponding 3.beta.,7.beta.-dihydroxy-.DELTA..sup.5 -steroid; and, optionally, reacting the resultant product with trimethylacetic anhydride, tert-butyldimethylsilyl chloride, dimethyl-2-(3-methylbutyl)silyl chloride, or tribenzylsilyl chloride.
    Type: Grant
    Filed: November 3, 1981
    Date of Patent: November 22, 1983
    Assignee: Schering, Aktiengesellschaft
    Inventors: Karl Petzoldt, Rudolf Wiechert, Henry Laurent, Klaus Nickisch, Dieter Bittler