Patents by Inventor Rolf-Eberhard Nitz

Rolf-Eberhard Nitz 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: 4888333
    Abstract: Substituted allylmercaptoacetylsydnonimines of the general formula I ##STR1## and their pharmacologically acceptable acid addition salts, in which R.sub.1 represents a secondary amino group of the formula ##STR2## and X denotes ##STR3## R.sub.2 denotes one of the radicals R.sub.3 OOC--, R.sub.4 SO.sub.2 -- or alkyl having1-4 C atoms,n denotes one of the values 1, 1 or 2,and R.sub.3 denotes alkyl having 1-4 C atoms,and R.sub.4 represents R.sub.3 or (R.sub.3).sub.2 N--, have valuable pharmacological properties.
    Type: Grant
    Filed: August 10, 1988
    Date of Patent: December 19, 1989
    Assignee: Cassella Aktiengessellschaft
    Inventors: Helmut Bohn, Melitta Just, Rolf-Eberhard Nitz
  • 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: 4837225
    Abstract: 2,5-Dimethylpyrrole derivatives of the formula I ##STR1## in which R denotes alkyl which is substituted by --NH.sub.2, acylamino of the formula--NH--CX--R.sup.1or by an optionally substituted heterocycle having 1 hetero member; or denotes an optionally substituted heterocycle having 1 member, and X and R.sup.1 have the meanings givenand their pharmacologically acceptable acid addition salts, their preparation by reaction of amines of the formula IIR--NH.sub.2 (II)with acetonylacetone or by acylating N-aminoalkyl-2,5-dimethylpyrroles, and their use as pharmaceutical active compounds.
    Type: Grant
    Filed: July 17, 1986
    Date of Patent: June 6, 1989
    Assignee: Cassell Aktiengesellschaft
    Inventors: Gerhard Zoller, Rudi Beyerle, Ursula Schindler, Rolf-Eberhard Nitz, Piero Martorana
  • Patent number: 4816454
    Abstract: Substituted 4,5-dihydro-3(2H)-pyridazinones of the formula I ##STR1## wherein R, for example, denotes a radical of the formula ##STR2## R.sup.1 and R.sup.2, for example, denote hydrogen or methyl, R.sup.3, for example, denotes 2-methoxy-ethoxy, 3-pyridyl-methoxy, amino-carbonyl-methoxy, hydroxy-carbonyl-methoxy, methyl-thio, (2-methoxy-ethyl)-amino-carbonyl-methoxy, 3-pyridyl-methyl or 5-methyl-1,3,4-oxadiazol-2-yl and R.sup.4, for example, denotes hydrogen, have useful pharmacological properties and can therefore be used for the preparation of pharmacological products.
    Type: Grant
    Filed: September 12, 1985
    Date of Patent: March 28, 1989
    Assignee: Cassella Aktiengesellschaft
    Inventors: Gerhard Zoller, Rudi Beyerle, Melitta Just, Helmut Bohn, Piero Martorana, Rolf-Eberhard Nitz
  • Patent number: 4785010
    Abstract: 2-(Aminoalkyl)-pyrrole derivatives of the formula ##STR1## wherein R denotes hydrogen, alkyl or phenyl, R.sup.1 denotes, for example, hydrogen, alkyl, alkoxy-carbonyl, aryl, substituted aryl or heteroaryl, R.sup.2 and R.sup.3 denote, for example, hydrogen, alkyl, alkanoyl, arylcarbonyl, heteroarylcarbonyl or arylenedicarbonyl and n denotes 1, 2 or 3, and their acid addition salts, are used as pharmacological active compounds for combating cerebral aging processes.
    Type: Grant
    Filed: November 12, 1985
    Date of Patent: November 15, 1988
    Assignee: Cassella Aktiengesellschaft
    Inventors: Gerhard Zoller, Rudi Beyerle, Ursula Schindler, Rolf-Eberhard Nitz, Piero A. Martorana
  • 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: 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: 4666902
    Abstract: Tetrahydropyridazinones of the formula I ##STR1## wherein R denotes an optionally substituted carbocyclic or heterocyclic radical, R.sup.1 denotes hydrogen; alkyl; aralkyl, which is optionally substituted in the aryl part; or acyl, and R.sup.2 denotes hydrogen; alkyl, which can optionally be substituted; or optionally substituted phenyl; and their acid addition compounds, if these can be prepared.The tetrahydropyridazinone derivatives of the formula I according to the invention and their physiologically acceptable salts exhibit useful pharmacological actions.
    Type: Grant
    Filed: June 8, 1984
    Date of Patent: May 19, 1987
    Assignee: Cassella Aktiengesellschaft
    Inventors: Gerhard Zoller, Rudi Beyerle, Melitta Just, Piero Martorana, Helmut Bohn, 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: 4598079
    Abstract: Aryl-substituted piperazinones and their physiologically-acceptable acid-addition salts have a useful nootropic action. They are administered enterally or parenterally in conventional dosage forms.
    Type: Grant
    Filed: May 15, 1984
    Date of Patent: July 1, 1986
    Assignee: Cassella Aktiengesellschaft
    Inventors: Rudi Beyerle, Heinz Bender, Ursula Schindler, Rolf-Eberhard Nitz, Piero A. 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
  • Patent number: 4532239
    Abstract: Basically-substituted pyridazines of the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3, independently of one another, denote hydrogen, halogen, hydroxyl, nitro, trifluoromethyl, alkyl, alkoxyalkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, phenyl, alkoxy, hydroxyalkoxy, alkoxy-alkoxy, alkenyloxy, alkynyloxy, cycloalkoxy, phenalkoxy, alkanoyl, alkanoylamino and --NH--CO--R.sup.9, R.sup.9 representing morpholino, piperidino or 1-pyrrolididinyl, or an optionally substituted ureido radical, R.sup.4 denotes hydrogen or lower alkyl and W denotes hydrogen, chlorine or bromine; and the acid-addition salts thereof are useful alone or in pharmaceutical preparations for treating cardiac complaints, circulatory complaints and high blood pressure. Several methods for preparing the basically-substituted pyridazines are also provided.
    Type: Grant
    Filed: December 20, 1983
    Date of Patent: July 30, 1985
    Assignee: Cassella Aktiengesellschaft
    Inventors: Thomas Raabe, Helmut Bohn, Piero A. Martorana, Rolf-Eberhard Nitz
  • Patent number: 4452797
    Abstract: Physiologically-acceptable 3-aminosydnonimines of the formula ##STR1## and their pharmacologically-acceptable acid-addition salts, when formulated into medicament dosage forms, are useful for reducing systemic blood pressure, pulmonary artery pressure and left ventricular end diastolic pressure when orally administered to patients in need of such pressure reduction. These compounds are prepared by cyclizing a compound which, in its free-base state, is of the formula ##STR2## to a corresponding product which, in its free-base state, is of the formula ##STR3## and, when R.sup.2 is other than -H, acylating that product.
    Type: Grant
    Filed: February 10, 1981
    Date of Patent: June 5, 1984
    Assignee: Cassella Aktiengesellschaft
    Inventors: Karl Schonafinger, Rudi Beyerle, Rolf-Eberhard Nitz, Piero A. Martorana, Volker Fiedler
  • Patent number: 4436743
    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: February 19, 1982
    Date of Patent: March 13, 1984
    Assignee: Cassella Aktiengesellschaft
    Inventors: Karl Schonafinger, Rudi Beyerle, Helmut Bohn, Melitta Just, Piero A. Martorana, Rolf-Eberhard Nitz
  • Patent number: 4416893
    Abstract: Pharmaceutical compositions comprising as pharmacologically active component a 1,2,5-oxadiazole-2-oxide of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 have the following meaning:______________________________________ R.sup.1 R.sup.2 ______________________________________ 1. CO--NH.sub.2 CH.sub.3 2. COOC.sub.2 H.sub.5 CH.sub.3 3. CO--NHNH.sub.2 CH.sub.3 4. COOH CH.sub.3 5. --NH--COOC.sub.2 H.sub.5 CH.sub.3 6. --NH--COOC.sub.3 H.sub.7 (n) CH.sub.3 7. --NH--COOC.sub.3 H.sub.7 (i) CH.sub.3 8. --NH--COOC.sub.4 H.sub.9 (n) CH.sub.3 9. --NH--COOCH.sub.2 --phenyl CH.sub.3 10. CO--NH.sub.2 CO--NH.sub.2 11. CN CN 12. COOH COOCH.sub.3 13. COOCH.sub.3 COOCH.sub.3 14. COOC.sub.2 H.sub.5 COOC.sub.2 H.sub.5 15. CH.sub.3 CO--NH.sub.2 16. CH.sub.3 COOC.sub.2 H.sub.5 17. CH.sub.3 CO--NHNH.sub.2 18. CH.sub.3 COOH 19. CN CO--NH.sub.2 20. CO--NH--phenyl CO--NH--phenyl 21. CH.sub.3 NH--COOC.sub.2 H.sub.5 22. CH.sub.3 NH--COOC.sub.3 H.sub.7 (n) 23. CH.sub.3 NH--COOC.sub.3 H.sub.7 (i) 24. CH.sub.3 NH--COOC.sub.4 H.
    Type: Grant
    Filed: March 24, 1981
    Date of Patent: November 22, 1983
    Assignee: Cassella Aktiengesellschaft
    Inventors: Karl Schonafinger, Rudi Beyerle, Anton Mogilev, Helmut Bohn, Piero Martorana, Rolf-Eberhard Nitz
  • Patent number: 4356178
    Abstract: Pharmacologically-valuable 3,4-(bis-substituted)-1,2,5-oxdiazole 2-oxides of formula I ##STR1## [wherein R denotes --NHR.sup.1, --NR.sup.2 R.sup.3, --NHR.sup.4 OR.sup.2, --NHR.sup.5 COR.sup.6 or ##STR2## R.sup.1 denotes alkyl having from 1 to 6 C atoms or cycloalkyl having 4 to 7 ring C atoms, R.sup.2 and R.sup.3 denote alkyl having from 1 to 4 C atoms, R.sup.4 denotes an alkylene radical of the formula --C.sub.n H.sub.2n --(wherein n denotes 2, 3 or 4), R.sup.5 denotes an alkylene radical of the formula --C.sub.m H.sub.2m -- (wherein m denotes 1, 2 or 3), R.sup.6 denotes --OR.sup.2, --NHR.sup.1, --NR.sup.2 R.sup.3 or --NH.sub.2, X denotes --(CH.sub.2).sub.p --, --(CH.sub.2).sub.2 --O--(CH.sub.2).sub.2 -- or ##STR3## and p is 4, 5 of 6] and their pharmacologically-acceptable acid-addition compounds are prepared by elimination of hydrogen chloride from a hydroxamoyl chloride of the formulaR--CO--C(Cl).dbd.NOH (II)and dimerization.
    Type: Grant
    Filed: December 18, 1981
    Date of Patent: October 26, 1982
    Assignee: Cassella Aktiengesellschaft
    Inventors: Karl Schonafinger, Rudi Beyerle, Anton Mogilev, Helmut Bohn, Melitta Just, Piero A. Martorana, Rolf-Eberhard Nitz
  • Patent number: 4335123
    Abstract: A 1-acyl-8-[2,3-epoxypropoxy]- and/or 1-acyl-8-[3-halo-2-hydroxypropoxy]-1,2,3,4-tetrahydroquinoline are reacted with primary and secondary amines to obtain corresponding physiologically-active 1-acyl-8-[3-amino-2-hydroxypropoxy]-1,2,3,4-tetrahydroquinolines and pharmacologically-acceptable acid-addition salts thereof. These compounds are useful as such or in conventional medicament compositions for treating those afflicted with heart ailments and/or hypertension.
    Type: Grant
    Filed: August 15, 1980
    Date of Patent: June 15, 1982
    Assignee: Cassella Aktiengesellschaft
    Inventors: Otto Grawinger, Thomas Raabe, Rudi Beyerle, Josef Scholtholt, Rolf-Eberhard Nitz
  • Patent number: 4332801
    Abstract: Physiologically-acceptable 3-aminosyndnonimines of the formula ##STR1## and their pharmacologically-acceptable acid-addition salts, when formulated into medicament dosage forms, are useful for reducing systemic blood pressure, pulmonary artery pressure and left ventricular end diastolic pressure when orally administered to patients in need of such pressure reduction. These compounds are prepared by cyclizing a compound which, in its free-base state, is of the formula ##STR2## to a corresponding product which, in its free-base state, is of the formula ##STR3## and, when R.sup.2 is other than --H, acylating that product.
    Type: Grant
    Filed: February 10, 1981
    Date of Patent: June 1, 1982
    Assignee: Cassella Aktiengesellschaft
    Inventors: Karl Schonafinger, Rudi Beyerle, Rolf-Eberhard Nitz, Piero A. Martorana, Volker Fiedler
  • Patent number: 4305939
    Abstract: Physiologically-acceptable 3-aminosydnonimines of the formula ##STR1## and their pharmacologically-acceptable acid-addition salts, when formulated into medicament dosage forms, are useful for reducing systemic blood pressure, pulmonary artery pressure and left ventricular end diastolic pressure when orally administered to patients in need of such pressure reduction. These compounds are prepared by cyclizing a compound which, in its free-base state, is of the formula ##STR2## to a corresponding product which, in its free-base state, is of the formula ##STR3## and, when R.sup.2 is other than --H, acylating that product.
    Type: Grant
    Filed: July 8, 1980
    Date of Patent: December 15, 1981
    Assignee: Cassella AG
    Inventors: Karl Schonafinger, Rudi Beyerle, Rolf-Eberhard Nitz, Piero A. Martorana, Volker Fiedler
  • Patent number: 4088764
    Abstract: The present invention relates to new pharmacologically valuable derivatives of 1-phenoxy-3-amino-propan-2-ol having the formula ##STR1## Wherein A denotes -CH.sub.2 -alkoxy, -O-alkoxyalkyl, -O-hydroxyalkyl, or ##STR2## R.sub.1 denotes hydrogen or methyl, Het denotes the radical of a pyrrole, pyrazole, imidazole, furane, thiophene, thiazole, pyridine, pyridazine, pyrimidine or pyrazine, which can additionally be substituted by one or more methyl groups, said radical is linked through a C atom, and R.sub.2 and R.sub.3 denote hydrogen, alkyl, alkenyl or cycloalkyl or conjointly with the N atom to which they are linked, and optionally with a further oxygen or sulfur hetero-atom, denote a saturated, 5-membered or 6-membered, monocyclic, heterocyclic structure, and alkyl radicals contain 1 to 4 carbon atoms, alkoxy radicals contain 1 to 4 carbon atoms, alkenyl radicals contain 3 or 4 carbon atoms and cycloalkyl radicals contain 5 to 7 carbon atoms; and aldehyde condensation products and acid addition salts thereof.
    Type: Grant
    Filed: December 10, 1974
    Date of Patent: May 9, 1978
    Assignee: Cassella Farbwerke Mainkur Aktiengesellschaft
    Inventors: Thomas Raabe, Otto Grawinger, Josef Scholtholt, Rolf-Eberhard Nitz, Eckhard Schraven