Patents by Inventor Karl Schonafinger

Karl Schonafinger 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: 5166166
    Abstract: The present invention relates to pharmacologically active substituted 3-dicyclohexylaminosydnone imines of the general formula I ##STR1## and their pharmacologically acceptable acid addition salts, in which R.sup.1 denotes hydrogen or the radical --COR.sup.2 and R.sup.2 denotes (C.sub.1 to C.sub.4)-alkyl, (C.sub.1 to C.sub.4)alkoxy-(C.sub.1 to C.sub.4)alkyl, (C.sub.1 to C.sub.4) alkoxy, (C.sub.1 to C.sub.4)alkoxy-(C.sub.1 to C.sub.4 )alkoxy, (C.sub.5 to C.sub.7)cycloalkyl, phenyl, a phenyl radical which is mono-, di- or trisubstituted by 1 to 3 halogen atoms and/or 1 to 3 alkyl radicals having 1 to 4 C atoms and/or 1 to 3 alkoxy radicals having 1 to 4 C atoms, a nicotinoyl radical or an allylmercaptoacetyl radical, and to a process for the preparation of the compounds according to the invention and their use.
    Type: Grant
    Filed: July 16, 1991
    Date of Patent: November 24, 1992
    Assignee: Cassella Aktiengesellschaft
    Inventors: Karl Schonafinger, Rudi Beyerle, Helmut Bohn, Melitta Just
  • Patent number: 5155109
    Abstract: The invention relates to pharmacologically active substituted 3-aminosydnone imines of the general formula I ##STR1## in which R.sup.1 denotes (C.sub.1 -C.sub.4)-alkyl, di-(C.sub.1 -C.sub.4)-alkylamino or (C.sub.6 -C.sub.12)-aryl, which can optionally be substituted by (C.sub.1 -C.sub.4)-alkyl;R.sup.2 denotes hydrogen or COR.sup.3 and R.sup.3 denotes (C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxy, (C.sub.1 -C.sub.4)-alkoxy-(C.sub.1 -C.sub.4)-alkyl, acetoxy-(C.sub.1 -C.sub.4)-alkyl, (C.sub.6 -C.sub.12)-aryl, which can be substituted by (C.sub.1 -C.sub.4)-alkyl or (C.sub.1 -C.sub.4)-alkoxy, pyridyl, pyridyl(C.sub.1 -C.sub.4)alkyl or (C.sub.3 -C.sub.8)-cycloalkyland their pharmacologically acceptable acid addition salts.
    Type: Grant
    Filed: July 16, 1991
    Date of Patent: October 13, 1992
    Assignee: Cassella Aktiengesellschaft
    Inventors: Karl Schonafinger, Helmut Bohn, Melitta Just
  • Patent number: 5120732
    Abstract: Substituted 3-aminosydnone imines of the formula I ##STR1## and their pharmacologically acceptable acid addition salts, in which A denotes, for example, --CH.sub.2 --,R.sup.1 denotes hydrogen or the radical --COR.sup.5,R.sup.2, R.sup.3 denote alkyl having 1 to 4 C atoms,R.sup.5 denotes, for example, an aliphatic radical having 1 to 4 C atoms,and methods for preparing such compounds by cyclization of a compound of the formula II ##STR2## and if desired subsequent acylation. The invention also includes formulations containing effective amounts of such compounds, and methods for administering same to patients for the control and prophylaxis of cardiovascular disorders.
    Type: Grant
    Filed: August 29, 1990
    Date of Patent: June 9, 1992
    Assignee: Cassella Aktiengesellschaft
    Inventors: Karl Schonafinger, Rudi Beyerle, Helmut Bohn, Melitta Just
  • Patent number: 5091398
    Abstract: The 1,2,3,4-oxatriazolium-5-olates of the formula I ##STR1## in which R.sup.1 denotes, for example, (C.sub.2 to C.sub.4)alkyl,R.sup.2 and R.sup.3 denotes (C.sub.1 to C.sub.4)alkyl have useful pharmacological properties.
    Type: Grant
    Filed: April 6, 1990
    Date of Patent: February 25, 1992
    Assignee: Cassella Aktiengellschaft
    Inventors: Karl Schonafinger, Helmut Bohn, Rudi Beyerle, Melitta Just
  • Patent number: 5015659
    Abstract: The present invention relates to thienylacetic acid derivatives of the general formula I ##STR1## in which X denotes --O-- or --NH--;R.sup.1 denotes hydrogen, the group --CH.sub.2 --CO--R.sup.3 or the group --CO--CH.sub.2 --NH.sub.2 ;R.sup.2 denotes hydrogen, (C.sub.1 -C.sub.4)-alkyl or the radical R.sup.1 andR.sup.3 denotes (C.sub.1 -C.sub.4)-alkoxy, hydroxyl or amino, it not being possible for both R.sup.1 and R.sup.2 to represent hydrogen when X denotes O,as well as the pharmaceutically tolerated salts thereof, process for the preparation thereof, the use thereof, and pharmaceuticals containing these and the preparation thereof.
    Type: Grant
    Filed: March 14, 1990
    Date of Patent: May 14, 1991
    Assignee: Cassella Aktiengesellschaft
    Inventors: Karl Schonafinger, Rudi Beyerle, Ursula Schindler, Bernd Jablonka, Jeffery Troke
  • Patent number: 5006540
    Abstract: Substituted 3-aminosydnonimines of the formula I ##STR1## and their pharmacologically acceptable acid addition salts, wherein R.sup.1 denotes, for example, alkyl having 1 to 8 C atoms, R.sup.2 denotes hydrogen or the radical --COR.sup.3 and R.sup.3 denotes, for example, an aliphatic radical having 1 to 4 C atoms, are prepared, for example, by cyclization of a compound of the formula II ##STR2## and if appropriate subsequent acylation and have useful pharmacological properties.
    Type: Grant
    Filed: October 17, 1989
    Date of Patent: April 9, 1991
    Assignee: Cassella Aktiengesellschaft
    Inventors: Karl Schonafinger, Rudi Beyerle, Melitta Just, Helmut Bohn, Jorg Ostrowski
  • Patent number: 4987134
    Abstract: The present invention relates to thienylpiperazines of the general formula I ##STR1## in which R.sup.1 denotes hydrogen or double-bonded oxygen and R.sup.2 denotes hydrogen or double-bonded oxygen, with R.sup.1 and R.sup.2 not both having the same meaning, as well as the pharmaceutically tolerated salts thereof, process for the preparation thereof, the use thereof, and pharmaceuticals containing these and the preparation thereof.
    Type: Grant
    Filed: March 16, 1990
    Date of Patent: January 22, 1991
    Assignee: Cassella Aktiengesellschaft
    Inventors: Karl Schonafinger, Rudi Beyerle, Ursula Schindler, Bernd Jablonka, Jeffery Troke
  • Patent number: 4942168
    Abstract: There are disclosed novel compounds of the formula ##STR1## where X is hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, nitro or trifluoromethyl; R.sub.1 is hydrogen or loweralkyl; R.sub.2 is hydrogen, loweralkyl, arylloweralkyl or --(CH.sub.2).sub.m R.sub.7 wherein m is 1, 2 or 3 and R.sub.7 is cyano or amino; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R.sub.5 and R.sub.6 are independently hydrogen or loweralkyl, or R.sub.5 +R.sub.6 taken together with the carbon atom to which they are attached constitute a cyclobutane, cyclopentane, cyclohexane, cycloheptane, pyrrolidine, piperidine, morpholine or thiomorpholine ring, or R.sub.5 is hydrogen and R.sub.6 is aryl or --CH.sub.2 OR.sub.8 wherein R.sub.8 is hydrogen, loweralkyl or loweralkylcarbonyl, which are useful for enhancing memory.
    Type: Grant
    Filed: March 7, 1988
    Date of Patent: July 17, 1990
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Karl Schonafinger, Helen H. Ong
  • Patent number: 4937241
    Abstract: Pharmacologically useful N-substituted-N-nitrosoaminoacetonitriles of the general formula I ##STR1## wherein A denotes the radical --CH.sub.2 --, --O--, --S(O.sub.n)--, --N(R.sup.2)-- or a direct bond,R.sup.1 and R.sup.
    Type: Grant
    Filed: December 27, 1988
    Date of Patent: June 26, 1990
    Assignee: Cassella Aktiengesellschaft
    Inventors: Karl Schonafinger, Rudi Beyerle, Helmut Bohn
  • Patent number: 4937244
    Abstract: Substituted 3-aminosydnonimines of the formula I ##STR1## and their pharmacologically acceptable acid addition salts wherein A denotes, for example, --CH.sub.2 --,R.sup.1 denotes hydrogen or the radical --COR.sup.7,R.sup.2, R.sup.3, R.sup.4 and R.sup.5 denote alkyl with 1 to 4 C atoms andR.sup.7 denotes, for example, an aliphatic radical and 1 to 4 C atoms, are prepared by cyclization of a compound of the formula II ##STR2## and if appropriate subsequent acylation and have useful pharmacological properties. The invention includes pharmaceutical preparations containing the present compounds, and the use thereof for treating patients having cardiovascular ailments.
    Type: Grant
    Filed: August 3, 1988
    Date of Patent: June 26, 1990
    Assignee: Cassella Aktiengesellschaft
    Inventors: Karl Schonafinger, Rudi Beyerle
  • Patent number: 4898866
    Abstract: 3-(Thien-2-yl)-piperazin-2-ones, substituted in the 3-position, of the general formula ##STR1## wherein R dentoes, for example, phenyl or (C.sub.1 -C.sub.6)-alkyl and R.sup.1 denotes 2-thienyl and pharmacologically tolerable acid addition salts thereof, which possess valuable nootropic properties. The invention also includes methods for making such compounds, formulations containing such compounds and methods for treating a host in need thereof.
    Type: Grant
    Filed: May 9, 1989
    Date of Patent: February 6, 1990
    Assignee: Cassella Aktiengesellschaft
    Inventors: Karl Schonafinger, Rudi Beyerle, Ursula Schindler
  • Patent number: 4880818
    Abstract: There are disclosed compounds of the formula ##STR1## where X,Y are each independently hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, trifluoromethyl or nitro; R.sub.1 is hydrogen or loweralkyl; R.sub.2 ' is hydrogen or loweralkyl and R.sub.4 is hydrogen, loweralkyl or aryl, which are useful as hypotensive agents and as intermediates.
    Type: Grant
    Filed: July 12, 1988
    Date of Patent: November 14, 1989
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Karl Schonafinger, Helen Hu Ong
  • Patent number: 4845091
    Abstract: Optically active substituted 3-aminosydnonimines of the general formula I ##STR1## and their pharmacologically acceptable acid addition salts, wherein R.sup.1 denotes, for example, the radical R.sup.3 (R.sup.4)N-,R.sup.2 denotes the radical 1-methoxyethyl (--CH(CH.sub.3)OCH.sub.3), acetoxy-phenyl-methyl (--CH(C.sub.6 H.sub.5)O--COCH.sub.3), 1-(ethoxycarbonyl)-ethoxy (--O--CH.sub.3)CO.sub.2 C.sub.2 H.sub.5),R.sup.3 denotes alkyl(C.sub.1 -C.sub.4) andR.sup.4 denotes for example alkyl(C.sub.1 -C.sub.4),possess valuable pharmaceutical properties.
    Type: Grant
    Filed: July 14, 1986
    Date of Patent: July 4, 1989
    Assignee: Cassella Aktiengesellschaft
    Inventors: Karl Schonafinger, Rudi Beyerle, Helmut Bohn, Melitta Just, Piero Martorana, Rolf-Eberhard Nitz
  • Patent number: 4771052
    Abstract: There are disclosed compounds of the formula ##STR1## where X and Y are independently hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, trifluoromethyl or nitro; R.sub.1 is hydrogen or loweralkyl; R.sub.2 is hydrogen, loweralkyl, loweralkylcarbonyl or arylcarbonyl; and R.sub.3 is hydrogen, loweralkyl, arylloweralkyl, ##STR2## loweralkylcarbonyl or arylcarbonyl, n being an interger of 1 to 6 inclusive and Z being hydrogen, loweralkyl, loweralkoxy, hydroxy or halogen; which are useful as hypotensive agents.
    Type: Grant
    Filed: February 5, 1987
    Date of Patent: September 13, 1988
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Karl Schonafinger, Helen H. Ong
  • Patent number: 4760147
    Abstract: Optically active substituted 1,4-dihydropyridines of the formula I having calcium antogonistic properties: ##STR1## wherein R denotes alkyl with 1 to 5 C atoms, alkoxy-alkyl with 1 to 4 C atoms, in the alkoxy part and 2 to 4 C atoms in the alkyl part, dialkylaminioalkyl with a total of 3 to 6 C atoms each of the alkyl groups as substituents on the amino group having 1 to 3 C atoms, or --CH(CH.sub.3)CO.sub.2 R.sup.5 in the optically active (R)-forms,R.sup.1 denotes phenyl which is monosubstituted by cyano, nitro or chlorine or is disubstituted by chlorine, R.sup.2 denotes oxadiazolyl, or an oxadiaxolyl which is substituted by methyl, ethyl, i-propyl, tert.-butyl, benzyl, methylthio, i-propylthio, aminocarbonylthio or methoxymethyl,R.sup.5 denotes alkyl with 1 to 4 C atoms, and acid-addition salts thereof, and acid addition salts thereof.
    Type: Grant
    Filed: December 12, 1986
    Date of Patent: July 26, 1988
    Assignee: Cassella Aktiengesellschaft
    Inventors: Karl Schonafinger, Helmut Bohn, Piero Martorana, Rolf-Eberhard Nitz
  • Patent number: 4743601
    Abstract: There are disclosed novel compounds of the formula ##STR1## where X is hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, nitro or trifluoromethyl; R.sub.1 is hydrogen or loweralkyl; R.sub.2 is hydrogen, loweralkyl, arylloweralkyl or --(CH.sub.2).sub.m R.sub.7 wherein m is 1, 2 or 3 and R.sub.7 is cyano or amino; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R.sub.5 and R.sub.6 are independently hydrogen or loweralkyl, or R.sub.5 +R.sub.6 taken together with the carbon atom to which they are attached constitute a cyclobutane, cyclopentane, cyclohexane, cycloheptane, pyrrolidine, piperidine, morpholine or thiomorpholine ring, or R.sub.5 is hydrogen and R.sub.6 is aryl or --CH.sub.2 OR.sub.8 wherein R.sub.8 is hydrogen, loweralkyl or loweralkylcarbonyl, which are useful for enhancing memory.
    Type: Grant
    Filed: July 13, 1987
    Date of Patent: May 10, 1988
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Karl Schonafinger, Helen H. Ong
  • Patent number: 4681891
    Abstract: 1,4-dihydropyridines of the formula I ##STR1## wherein R.sup.1 denotes optionally substituted phenyl, pyridyl or thienyl, R.sup.2 denotes optionally substituted oxadiazolyl, thiadiazolyl or thiazolyl and R.sup.3 denotes hydrogen or --COOH, their preparation by a modified Hantzsch synthesis and their use as a calcium-agonist in pharmacy.
    Type: Grant
    Filed: November 12, 1985
    Date of Patent: July 21, 1987
    Assignee: Cassella Aktiengesellschaft
    Inventors: Karl Schonafinger, Helmut Bohn, Piero Martorana, Rolf-Eberhard Nitz
  • Patent number: 4610984
    Abstract: This invention relates to certain 4-acyl-piperazine-1-acetamides. These compounds are useful as memory and learning enhancers and for the treatment and prevention of cerebral insufficiency.
    Type: Grant
    Filed: April 18, 1984
    Date of Patent: September 9, 1986
    Assignee: Cassella Aktiengesellschaft
    Inventors: Karl Schonafinger, Rudi Beyerle, Ursula Schindler, Piero Martorana, Rolf-Eberhard Nitz
  • Patent number: 4558058
    Abstract: 1,4-dihydropyridines of the formula I ##STR1## in which R denotes, for example, --CO.sub.2 R.sup.3 or cyano, R.sup.1 denotes, for example, an optionally substituted phenyl, pyridyl or thienyl, R.sup.2 denotes the radical of a 5-membered, optionally substituted, ring having at least one double bond and at least 2 heteroatoms or heteroatom groups from the series comprising O, N, NH and S, and R.sup.3 denotes, for example, alkyl or alkoxyalkyl, and their acid addition salts, have valuable pharmacological properties.
    Type: Grant
    Filed: December 9, 1983
    Date of Patent: December 10, 1985
    Assignee: Cassella Aktiengesellschaft
    Inventors: Karl Schonafinger, Helmut Bohn, Melitta Just, Piero Martorana
  • Patent number: 4551454
    Abstract: Pharmacologically-active 3-aminosydnonimines (which are optionally substituted in the N.sup.6 -position) and their physiologically-acceptable acid-addition salts are compounded into standard dosage-form medicament compositions and are useful for prophylaxis for and treatment of cardiovascular-system disorders, such as high blood pressure and angina pectoris. The 3-aminosydnonimines are 3-[4-(lower alkoxy)carbonylpiperazin-1-yl]sydnonimines and 3-[N-(lower alkyl)-N-(tetrahydro-3-thienyl S,S-dioxide)]-sydnonimines.
    Type: Grant
    Filed: May 6, 1983
    Date of Patent: November 5, 1985
    Assignee: Cassella Aktiengesellschaft
    Inventors: Karl Schonafinger, Rudi Beyerle, Helmut Bohn, Melitta Just, Piero A. Martorana, Rolf-Eberhard Nitz