Patents by Inventor Michael H. Town

Michael H. Town 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: 5157042
    Abstract: Carbacyclin derivatives of Formula I ##STR1## wherein R.sub.1 is OR.sub.2, wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, ##STR2## or a heterocyclic residue; or R.sub.1 is NHR.sub.3 wherein R.sub.3 is an acid residue (acyl) or R.sub.2 ;A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH--, or --C.tbd.C--;W is a free or functionally modified hydroxymethylene group or a free or functionally modified ##STR3## wherein the OH-group can be in the .alpha.- or .beta.-position; D is ##STR4## a straight-chain, saturated aliphatic group of 1-10 carbon atoms; or a branched, saturated or straight-chain or branched, unsaturated aliphatic group of 2-10 carbon atoms; all of which are substituted by fluorine atoms;n is 1, 2, or 3;E is a direct bond, --C.tbd.C--, or --CR.sub.6 .dbd.CR.sub.7 --, wherein R.sub.6 is hydrogen or alkyl of 1-5 carbon atoms and R.sub.7 is hydrogen, halogen or alkyl of 1-5 carbon atoms;R.sub.4 is an aliphatic group, cycloalkyl, optionally substituted aryl, or a heterocyclic group; andR.sub.
    Type: Grant
    Filed: June 10, 1991
    Date of Patent: October 20, 1992
    Assignee: Schering Aktiengesellschaft
    Inventors: Werner Skuballa, Bernd Raduechel, Helmut Vorbrueggen, Jorge Casals-Stenzel, Gerda Mannesmann, Michael H. Town
  • Patent number: 5124343
    Abstract: The invention relates to carbacyclins of general Formula I ##STR1## wherein R.sub.1 is the residue CH.sub.2 OH or ##STR2## with R.sub.2 meaning a hydrogen atom, an alkyl, cycloalkyl, aryl residue, a ##STR3## or heterocyclic residue, or R.sub.1 is the residue ##STR4## with R.sub.3 meaning an alkanoyl or alkanesulfonyl residue of respectively 1-10 carbon atoms or the residue R.sub.2, orR.sub.1 is the residue ##STR5## wherein m is the number 1 or 2, X is an oxygen atom or a CH.sub.2 -group,A is a trans--CH.dbd.CH- or --.tbd.C--group,W is a free or functionally modified hydroxymethylene group wherein the OH-group can be in the .alpha.- or .beta.- position,n is the number 1, 2, or 3,D is a straight-chain alkylene group of 1-5 carbon atoms,E is a --C.tbd.C---bond or a --CR.sub.6 =CR.sub.7 --group wherein R.sub.6 and R.sub.7 are different from each other and mean a hydrogen atom or an alkyl group of 1-5 carbon atoms or a hydrogen atom or a halogen atom, preferably chlorine,R.sub.
    Type: Grant
    Filed: January 6, 1988
    Date of Patent: June 23, 1992
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Vorbrueggen, Hernd Raduechel, Werner Skuballa, Norbert Schwarz, Jorge Casals-Stenzel, Gerda Mannesmann, Michael H. Town
  • Patent number: 5013758
    Abstract: (5E)-13,14,18,18,19,19-hexadehydro-3-oxa-6a-carbaprostaglandin I.sub.2 derivatives of Formula I ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 are hydrogen or alkyl of 1-5 carbon atoms, andR.sub.5 is an alkyl group of 1-5 carbon atoms, as well as the physiologically compatible salts thereof;have pharmacologically valuable activity.
    Type: Grant
    Filed: November 13, 1989
    Date of Patent: May 7, 1991
    Assignee: Schering Aktiengesellschaft
    Inventors: Werner Skuballa, Bernd Raduechel, Helmut Vorbrueggen, Claus-Steffen Stuerzebecher, Martin Haberey, Ekkehard Schillinger, Michael H. Town
  • Patent number: 4954524
    Abstract: Carbacyclin derivatives of Formula I ##STR1## wherein R.sub.1 is hydrogen or OR.sub.2, wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, ##STR2## or a heterocyclic residue; or R.sub.1 is NHR.sub.3 wherein R.sub.3 is an acid residue (acyl) or R.sub.2,n is 2, 3, 4, or 5,X is hydrogen or fluorine,A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH--, or --C.tbd.C--,W is a free or functionally modified hydroxymethylene group or a free or functionally modified ##STR3## wherein the OH-group can be in the .alpha.- or .beta.-position, D is ##STR4## a straight-chain, saturated aliphatic group of 1-10 carbon atoms, a branched, saturated or a straight-chain or branched, unsaturated aliphatic group of 2-10 carbon atoms, all of which can optionally be substituted by fluorine atoms,m is 1, 2, or 3,E is a direct bond, --C.tbd.C--, or --CR.sub.6 .dbd.CR.sub.7 -- wherein R.sub.6 and R.sub.7 are different from each other and are hydrogen or alkyl or 1-5 carbon atoms, or are hydrogen or halogen,R.sub.
    Type: Grant
    Filed: April 6, 1989
    Date of Patent: September 4, 1990
    Assignee: Schering Aktiengesellschaft
    Inventors: Werner Skuballa, Bernd Raduechel, Helmut Vorbrueggen, Jorge Casals-Stenzel, Gerda Mannesmann, Ekkehard Schillinger, Michael H. Town
  • Patent number: 4708963
    Abstract: Carbacyclin derivatives of Formula I ##STR1## wherein R.sub.1 is OR.sub.2, wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, a heterocyclic residue, or NHR.sub.3, wherein R.sub.3 is an acid residue or hydrogen;X is oxygen;A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH--, or --C.tbd.C--;W is free or functionally modified hydroxymethylene or free or functionally modified ##STR2## wherein the OH-group can be in the .alpha.- or .beta.-position; D is a straight-chain or branched, saturated or unsaturated aliphatic group of 1-10 carbon atoms, which can optionally be substituted by fluorine atoms, 1,2-methylene, 1,1-trimethylene;E is --C.tbd.C-- or --CR.sub.6 .dbd.CH.sub.7 -- wherein R.sub.6 and R.sub.7 are hydrogen or alkyl of 1-5 carbon atoms;R.sub.4 is an aliphatic group, cycloalkyl, optionally substituted aryl, or a heterocyclic group;R.sub.5 is free or functionally modified hydroxy and,when R.sub.
    Type: Grant
    Filed: May 28, 1985
    Date of Patent: November 24, 1987
    Assignee: Schering Aktiengesellschaft
    Inventors: Werner Skuballa, Bernd Raduchel, Norbert Schwarz, Helmut Vorbruggen, Jorge Casals-Stenzel, Ekkehard Schillinger, Michael H. Town
  • Patent number: 4567195
    Abstract: Azaprostacyclins of Formula I ##STR1## wherein R.sub.1 is hydrogen, alkyl, cycloalkyl, aryl, a heterocyclic residue, or a phenacyl residue optionally substituted on the phenyl ring by bromine, phenyl, alkoxy, or dialkoxy,W is a free or functionally modified carbonyl group or a ##STR2## wherein R.sub.8 is hydrogen or alkyl of 1-5 carbon atoms and R.sub.9 is hydrogen or a readily cleavable ether or acyl residue and wherein the OR.sub.9 -group can be in the .alpha.- or .beta.-position,R.sub.2 is a free or functionally modified hydroxy group,R.sub.3 and R.sub.4 each independently is hydrogen, alkyl of 1-5 carbon atoms, or fluorine,D is alkylene of 1-2 carbon atoms which can be substituted by alkyl groups of 1-5 carbon atoms,R.sub.5 is hydrogen or alkyl of 1-2 carbon atoms or, when D is alkylene of 1 or 2 carbon atoms, R.sub.5, together with R.sub.6, represents a bond,R.sub.6 and R.sub.7 each independently is hydrogen or alkyl of 1-2 carbon atoms, whereinR.sub.6 (R.sub.7) is halogen when R.sub.7 (R.sub.
    Type: Grant
    Filed: March 21, 1984
    Date of Patent: January 28, 1986
    Assignee: Schering, Aktiengesellschaft
    Inventors: Norbert Schwarz, Werner Skuballa, Helmut Vorbrueggen, Jorge Casals-Stenzel, Ekkehard Schillinger, Michael H. Town
  • Patent number: 4552875
    Abstract: Carbacyclinamides of Formula I ##STR1## wherein R.sub.1 is NHR.sub.4, wherein R.sub.4 is H, --(CH.sub.2).sub.n --R.sub.8 or straight-chained or branched aliphatic groups of 1-10 carbon atoms, cycloalkyl of 3-10 carbon atoms, aryl, or lower mono- or polyhydroxyalkyl of 2-8 carbon atoms, or R.sub.1 is NR.sub.4 R.sub.5 wherein R.sub.4 and R.sub.5 each are straight-chained or branched, lower, mono- or polyhydroxyalkyl of 2-8 carbon atoms, or R.sub.4 and R.sub.5 together with the adjoining N-atom form a 5- or 6-membered heterocycle which can optionally contain additional hetero atoms and can be substituted; or R.sub.1 is NR.sub.4 R.sub.5 wherein R.sub.4 is an aliphatic group of 1-10 carbon atoms, cycloalkyl of 3-10 carbon atoms, and R.sub.5 is straight-chained or branched aliphatic group of 1-10 carbon atoms, cycloalkyl of 3-10 carbon atoms, aryl, or lower, mono- or polyhydroxyalkyl of 2-8 carbon atoms;n is 1-4;R.sub.8 is --CONH.sub.2 or --N(C.sub.1 -C.sub.4 -alkyl).sub.2 ;R.sub.
    Type: Grant
    Filed: July 1, 1983
    Date of Patent: November 12, 1985
    Assignee: Schering Aktiengesellschaft
    Inventors: Werner Skuballa, Bernd Raduechel, Helmut Vorbrueggen, Gerda Mannesmann, Bob Nieuweboer, Michael H. Town
  • Patent number: 4446147
    Abstract: Azaprostacyclins of Formula I ##STR1## wherein R.sub.1 is hydrogen, alkyl, cycloalkyl, aryl, a heterocyclic residue, or a phenacyl residue optionally substituted on the phenyl ring by bromine, phenyl, alkoxy, or dialkoxy,W is a free or functionally modified carbonyl group or a ##STR2## wherein R.sub.8 is hydrogen or alkyl of 1-5 carbon atoms and R.sub.9 is hydrogen or a readily cleavable ether or acyl residue and wherein the OR.sub.9 -group can be in the .alpha.- or .beta.-position,R.sub.2 is a free or functionally modified hydroxy group.
    Type: Grant
    Filed: February 22, 1982
    Date of Patent: May 1, 1984
    Assignee: Schering Aktiengesellschaft
    Inventors: Norbert Schwarz, Werner Skuballa, Helmut Vorbrueggen, Jorge Casals-Stenzel, Ekkehard Schillinger, Michael H. Town
  • Patent number: 4423067
    Abstract: Carbacyclin derivatives of Formula I ##STR1## wherein R.sub.1 is OR.sub.2, wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, a heterocyclic residue, or NHR.sub.3, wherein R.sub.3 is an acid residue or hydrogen;X is oxygen;A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH--, or --C.tbd.C--;W is free or functionally modified hydroxymethylene or free or functionally modified ##STR2## wherein the OH-group can be in the .alpha.- or .beta.-position; D is a straight-chain or branched, saturated or unsaturated aliphatic group of 1-10 carbon atoms, which can optionally be substituted by fluorine atoms, 1,2-methylene, 1,1-trimethylene;E is --C.tbd.C-- or --CR.sub.6 .dbd.CR.sub.7 -- wherein R.sub.6 and R.sub.7 are hydrogen or alkyl of 1-5 carbon atoms;R.sub.4 is an aliphatic group, cycloalkyl, optionally substituted aryl, or a heterocyclic group;R.sub.5 is free or functionally modified hydroxy and,when R.sub.
    Type: Grant
    Filed: December 21, 1981
    Date of Patent: December 27, 1983
    Assignee: Schering Aktiengesellschaft
    Inventors: Werner Skuballa, Bernd Raduchel, Norbert Schwarz, Helmut Vorbruggen, Jorge Casals-Stenzel, Ekkehard Schillinger, Michael H. Town
  • Patent number: 4364950
    Abstract: 5-cyano-prostacyclins of the formula ##STR1## wherein R.sub.1 is OR.sub.2 or NHR.sub.3 ; R.sub.2 and R.sub.3 each independently is (a) H, (b) C.sub.1-10 -alkyl, (c) C.sub.1-10 -alkyl substituted by halo, C.sub.1-4 -alkoxy or phenyl, 1-naphthyl or 2-naphthyl, each optionally substituted as defined below, (d) C.sub.4-10 -cycloalkyl, (e) C.sub.4-10 -cycloalkyl substituted by C.sub.1-4 -alkyl, (f) phenyl, 1-naphthyl or 2-naphthyl, (g) phenyl, 1-naphthyl or 2-naphthyl substituted by 1-3 halogen atoms, phenyl, 1-3 alkyl groups of 1-4 C atoms each, or a chloromethyl-, fluoromethyl-, trifluoromethyl-, carboxyl-, hydroxy- or alkoxy-group of 1-4 C atoms, or (h) an aromatic, 5- or 6-membered heterocyclic ring containing one hetero atom which is O, N or S, the remaining atoms being carbon; R.sub.3 also possibly being an acyl group of a C.sub.
    Type: Grant
    Filed: November 2, 1981
    Date of Patent: December 21, 1982
    Assignee: Schering Aktiengesellschaft
    Inventors: Werner Skuballa, Helmut Vorbruggen, Bernd Raduchel, Jorge Casals-Stenzel, Ekkehard Schillinger, Michael H. Town