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).
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Patent number: 4888333Abstract: 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: GrantFiled: August 10, 1988Date of Patent: December 19, 1989Assignee: Cassella AktiengessellschaftInventors: Helmut Bohn, Melitta Just, Rolf-Eberhard Nitz
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Patent number: 4845091Abstract: 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: GrantFiled: July 14, 1986Date of Patent: July 4, 1989Assignee: Cassella AktiengesellschaftInventors: Karl Schonafinger, Rudi Beyerle, Helmut Bohn, Melitta Just, Piero Martorana, Rolf-Eberhard Nitz
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Patent number: 4837225Abstract: 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: GrantFiled: July 17, 1986Date of Patent: June 6, 1989Assignee: Cassell AktiengesellschaftInventors: Gerhard Zoller, Rudi Beyerle, Ursula Schindler, Rolf-Eberhard Nitz, Piero Martorana
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Patent number: 4816454Abstract: 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: GrantFiled: September 12, 1985Date of Patent: March 28, 1989Assignee: Cassella AktiengesellschaftInventors: Gerhard Zoller, Rudi Beyerle, Melitta Just, Helmut Bohn, Piero Martorana, Rolf-Eberhard Nitz
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Patent number: 4785010Abstract: 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: GrantFiled: November 12, 1985Date of Patent: November 15, 1988Assignee: Cassella AktiengesellschaftInventors: Gerhard Zoller, Rudi Beyerle, Ursula Schindler, Rolf-Eberhard Nitz, Piero A. Martorana
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Patent number: 4760147Abstract: 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: GrantFiled: December 12, 1986Date of Patent: July 26, 1988Assignee: Cassella AktiengesellschaftInventors: Karl Schonafinger, Helmut Bohn, Piero Martorana, Rolf-Eberhard Nitz
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Patent number: 4681891Abstract: 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: GrantFiled: November 12, 1985Date of Patent: July 21, 1987Assignee: Cassella AktiengesellschaftInventors: Karl Schonafinger, Helmut Bohn, Piero Martorana, Rolf-Eberhard Nitz
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Patent number: 4666902Abstract: 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: GrantFiled: June 8, 1984Date of Patent: May 19, 1987Assignee: Cassella AktiengesellschaftInventors: Gerhard Zoller, Rudi Beyerle, Melitta Just, Piero Martorana, Helmut Bohn, Rolf-Eberhard Nitz
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Patent number: 4610984Abstract: 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: GrantFiled: April 18, 1984Date of Patent: September 9, 1986Assignee: Cassella AktiengesellschaftInventors: Karl Schonafinger, Rudi Beyerle, Ursula Schindler, Piero Martorana, Rolf-Eberhard Nitz
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Patent number: 4598079Abstract: 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: GrantFiled: May 15, 1984Date of Patent: July 1, 1986Assignee: Cassella AktiengesellschaftInventors: Rudi Beyerle, Heinz Bender, Ursula Schindler, Rolf-Eberhard Nitz, Piero A. Martorana
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Patent number: 4551454Abstract: 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: GrantFiled: May 6, 1983Date of Patent: November 5, 1985Assignee: Cassella AktiengesellschaftInventors: Karl Schonafinger, Rudi Beyerle, Helmut Bohn, Melitta Just, Piero A. Martorana, Rolf-Eberhard Nitz
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Patent number: 4532239Abstract: 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: GrantFiled: December 20, 1983Date of Patent: July 30, 1985Assignee: Cassella AktiengesellschaftInventors: Thomas Raabe, Helmut Bohn, Piero A. Martorana, Rolf-Eberhard Nitz
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Patent number: 4452797Abstract: 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: GrantFiled: February 10, 1981Date of Patent: June 5, 1984Assignee: Cassella AktiengesellschaftInventors: Karl Schonafinger, Rudi Beyerle, Rolf-Eberhard Nitz, Piero A. Martorana, Volker Fiedler
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Patent number: 4436743Abstract: 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: GrantFiled: February 19, 1982Date of Patent: March 13, 1984Assignee: Cassella AktiengesellschaftInventors: Karl Schonafinger, Rudi Beyerle, Helmut Bohn, Melitta Just, Piero A. Martorana, Rolf-Eberhard Nitz
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Patent number: 4416893Abstract: 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: GrantFiled: March 24, 1981Date of Patent: November 22, 1983Assignee: Cassella AktiengesellschaftInventors: Karl Schonafinger, Rudi Beyerle, Anton Mogilev, Helmut Bohn, Piero Martorana, Rolf-Eberhard Nitz
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Patent number: 4356178Abstract: 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: GrantFiled: December 18, 1981Date of Patent: October 26, 1982Assignee: Cassella AktiengesellschaftInventors: Karl Schonafinger, Rudi Beyerle, Anton Mogilev, Helmut Bohn, Melitta Just, Piero A. Martorana, Rolf-Eberhard Nitz
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Patent number: 4335123Abstract: 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: GrantFiled: August 15, 1980Date of Patent: June 15, 1982Assignee: Cassella AktiengesellschaftInventors: Otto Grawinger, Thomas Raabe, Rudi Beyerle, Josef Scholtholt, Rolf-Eberhard Nitz
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Patent number: 4332801Abstract: 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: GrantFiled: February 10, 1981Date of Patent: June 1, 1982Assignee: Cassella AktiengesellschaftInventors: Karl Schonafinger, Rudi Beyerle, Rolf-Eberhard Nitz, Piero A. Martorana, Volker Fiedler
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Patent number: 4305939Abstract: 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: GrantFiled: July 8, 1980Date of Patent: December 15, 1981Assignee: Cassella AGInventors: Karl Schonafinger, Rudi Beyerle, Rolf-Eberhard Nitz, Piero A. Martorana, Volker Fiedler
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Patent number: 4088764Abstract: 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: GrantFiled: December 10, 1974Date of Patent: May 9, 1978Assignee: Cassella Farbwerke Mainkur AktiengesellschaftInventors: Thomas Raabe, Otto Grawinger, Josef Scholtholt, Rolf-Eberhard Nitz, Eckhard Schraven