Patents by Inventor Oswald Lockhoff
Oswald Lockhoff 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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Publication number: 20050037423Abstract: The invention concerns isotopically coded marker (ICAT) for mass spectrometric analysis of proteins, and the preparation and use of said markers.Type: ApplicationFiled: October 30, 2002Publication date: February 17, 2005Applicant: Bayer Healthcare AGInventors: Hans-Georg Lerchen, Oswald Lockhoff, Dorian Immler, Hans-Ulrich Siegmund
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Publication number: 20020183256Abstract: The present invention relates to cytostatics which have a tumor-specific action as a result of linkage to &agr;v&bgr;3 integrin antagonists via preferred linking units which can be selevtively cleaved by enzymes such as metallo matrixproteases (MMPs), i.e. by enzymes which can especially be found in tumor tissue. The preferred linking units guarantee the serum stability of the conjugate of cytostatic and &agr;v&bgr;3 integrin antagonist and, at the same time, the desired intracellular action within tumor cells as a result of its specific enzymatic or hydrolytic cleavability with release of the cytostatic.Type: ApplicationFiled: December 21, 2001Publication date: December 5, 2002Inventors: Hans-Georg Lerchen, Jorg Baumgarten, Oswald Lockhoff, Markus Albers, Andreas Schoop
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Publication number: 20020173452Abstract: The present invention relates to cytostatics which have a tumor-specific action as a result of linkage to specific carbohydrate moeities via preferred linking units which can be selevtively cleaved by enzymes such as metallo matrixproteases (MMPs), elastase or cathepsines, i.e. by enzymes which can especially be found in tumor tissue. The preferred linking units guarantee sufficient serum stability of the conjugate of cytostatic and carbohydrate moeity and, at the same time, the desired intracellular action within tumor cells as a result of its specific enzymatic or hydrolytic cleavability with release of the cytostatic.Type: ApplicationFiled: December 21, 2001Publication date: November 21, 2002Inventors: Hans-Georg Lerchen, Joerg Baumgarten, Oswald Lockhoff
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Patent number: 6034055Abstract: The present invention relates to (2-aminoacylamino-2-deoxy-glycosyl)-amides, which are substituted on the nitrogen atom of the amino acid, of the general formula (I) ##STR1## in which the substituents have the meaning given in the description, to processes for their preparation and to their use in medicaments.Type: GrantFiled: February 22, 1999Date of Patent: March 7, 2000Assignee: Bayer AktiengesellschaftInventors: Oswald Lockhoff, Burkhard Mielke, Helmut Brunner, Klaus Schaller
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Patent number: 5998448Abstract: The invention relates to new combinations of dihydropyridines of the general formula (I) ##STR1## in which R.sup.1 to R.sup.5 have the meaning indicated in the description, for the prevention and treatment of vascular disorders, in particular of cardiovascular and cerebrovascular disorders, containing dihydropyridines having calcium antagonist activity, acetylsalicylic acid nitroesters and vitamins, and, if appropriate, also further auxiliaries or active compounds.Type: GrantFiled: October 24, 1997Date of Patent: December 7, 1999Assignee: Bayer AktiengeselechaftInventors: Eva Lesur, Dieter Neuser, Oswald Lockhoff, Elisabeth Perzborn, Johannes Peter Stasch, Peter Kurka
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Patent number: 5905071Abstract: The present invention relates to (2-aminoacylamino-2-deoxy-glycosyl)-amides, which are substituted on the nitrogen atom of the amino acid, of the general formula (I) ##STR1## in which the substituents have the meaning given in the description, to processes for their preparation and to their use in medicaments.Type: GrantFiled: June 25, 1996Date of Patent: May 18, 1999Assignee: Bayer AktiengesellschaftInventors: Oswald Lockhoff, Burkhard Mielke, Helmut Brunner, Klaus Schaller
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Patent number: 5859053Abstract: The invention relates to new derivatives of acetylsalicylic acid (called ASA in the following), which contain an NO.sub.3 structure. They are therapeutically active either as the intact active compound molecule or after cleavage (NO release). The invention also relates to processes for their preparation and their use as medicaments, in particular for the alleviation of pain, inhibition of platelet aggregation, lowering of fever and for the prevention of cardiovascular disorders and oncoses.Type: GrantFiled: October 24, 1997Date of Patent: January 12, 1999Assignee: Bayer AktiengesellschaftInventors: Eva Lesur, Dieter Neuser, Oswald Lockhoff, Elisabeth Perzborn, Peter Kurka, Johannes Peter Stasch
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Patent number: 5070190Abstract: The invention relates to new N-glycosylamides of the general formula I ##STR1## in which R.sup.1 denotes a saturated alkyl radical or a singly, doubly or triply unsaturated alkenyl radical having up to 50 carbon atoms,R.sup.2 denotes a saturated alkyl radical or a singly, doubly or triply unsaturated alkenyl radical having up to 50 carbon atoms,A represents --CO-- or represents a group ##STR2## in which R.sup.3 represents hydrogen, C.sub.1 -C.sub.7 alkyl, hydroxymethyl, 1-hydroxyethyl, mercaptomethyl, 2-methylthioethyl, 3-aminopropyl, 2-ureidopropyl, 3-guanidylpropyl, 4-aminobutyl, carboxymethyl, carbamoylmethyl, 2-carboxyethyl, 2-carbamoylethyl, benzyl, 4-hydroxybenzyl, 3-indolylmethyl or 4-imidazolylmethyl, andn represents 0 to 10,and which are substituted in the sugar residue with an amino acid residue, as well as process for their preparation and their use as medicaments.Type: GrantFiled: April 12, 1989Date of Patent: December 3, 1991Assignee: Bayer AktiengesellschaftInventors: Oswald Lockhoff, John Goossens, Helmut Brunner, Michael Sperzel, Klaus G. Stunkel
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Patent number: 4891425Abstract: A N-glycosylamide derivative of the formula (I) ##STR1## in which R.sup.1 denotes hydrogen or a saturated or mono- or polyunsaturated alkyl radical with one to 50 carbon atoms,R.sup.2 denotes hydrogen or a saturated or mono- or polyunsaturated alkyl radical with one to 50 carbon atoms,R.sup.3 denotes hydrogen or an acyl radical with up to 20 carbon atoms,R.sup.4 denotes hydrogen or an alkyl radical with up to 4 carbon atoms andR.sup.5 and R.sup.6 independently of one another denote hydrogen or an acyl radical with up to 10 carbon atoms or a saturated or an unsaturated alkyl radical or an aralkyl radical with up to 10 carbon atoms, orR.sup.5 l and R.sup.6 together denote a grouping ##STR2## wherein R.sup.7 and R.sup.8 independently of one another denote hydrogen or lower alkyl with up to 5 carbon atoms or an unsubstituted or substituted aryl radical with up to 10 C atoms in the aromatic part. The N-glycosylamide derivatives exhibiting a broad defense-increasing action in the body.Type: GrantFiled: January 28, 1987Date of Patent: January 2, 1990Assignee: Bayer AktiengesellschaftInventors: Oswald Lockhoff, Yutaka Hayauchi, Peter Stadler, Helmut Brunner
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Patent number: 4855283Abstract: Compounds of the formula ##STR1## in which R.sup.1 denotes hydrogen or a saturated or singly or multiply unsaturated alkyl radical having up to 50 carbon atoms,X represents --CH.sub.2 --, --O-- or --NH--,R.sup.2 denotes hydrogen or a saturated or singly or multiply unsaturated alkyl radical having up to 50 carbon atoms,R.sup.3, R.sup.4 and R.sup.5, independently of one another, denotes hydrogen or acyl--CO--R.sup.6, R.sup.6 being an alkyl radical having up to 10 carbon atoms,R.sup.7 denotes hydrogen, C.sub.1 -C.sub.7 -alkyl-, hydroxymethyl, 1-hydroxyethyl, mercaptomethyl, 2-(methylthio)-ethyl, 3-aminopropyl, 3-ureidopropyl, 3-guanidyl-propyl, 4-aminobutyl, carboxymethyl, carbamylmethyl, 2-carboxyethyl, 2-carbamoylethyl, benzyl, 4-hydroxybenzyl, 3-indolylmethyl or 4-imidazolylmethyl, andR.sup.8 represents hydrogen or methyl, andR.sup.9 represents hydrogen, acetyl, benzoyl, trichloroacetyl, trifluoroacetyl, methoxycarbonyl, t-butyloxycarbonyl or benzyloxycarbonyl andR.sup.7 and R.sup.8 together can denote --CH.Type: GrantFiled: June 16, 1986Date of Patent: August 8, 1989Assignee: Bayer AktiengesellschaftInventors: Oswald Lockhoff, Yutaka Hayauchi, Peter Stadler, Klaus G. Stunkel, Gert Streissle, Arnold Paessens, Volker Klimetzek, Hans-Joachim Zeiler, Karl G. Metzger, Hein-Peter Kroll, Helmut Brunner, Klaus Schaller
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Patent number: 4737488Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, an optionally substituted aromatic hydrocarbon radical, an aralkyl radical or an optionally substituted aliphatic hydrocarbon radical having up to 45 C atoms,R.sup.2 is an optionally substituted aromatic hydrocarbon radical, an aralkyl radical or an optionally substituted aliphatic hydrocarbon radical having 5-50 C atoms,X is O, S, NH or NR, R being an alkyl radical having up to 20 C atoms, andZ is a glycosyl radical bonded via the anomeric carbon atom,or pharmaceutically acceptable salts thereof stimulate the immune system.Type: GrantFiled: November 29, 1984Date of Patent: April 12, 1988Assignee: Bayer AktiengesellschaftInventors: Oswald Lockhoff, Bernd-Wieland Kruger, Peter Stadler, Karl G. Metzger, Hans-Georg Opitz, Klaus Schaller, Klaus G. Stunkel, Hans-Joachim Zeiler
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Patent number: 4716152Abstract: Compounds of the formula ##STR1## in which X is hydrogen or the radical CH.sub.2 OR.sup.5,R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each independently is hydrogen or the radical ##STR2## Y is oxygen, sulphur, NH or CH.sub.2, and R.sup.1 and R.sup.6 each independently is an optionally substituted hydrocarbon radical having up to 50 carbon atoms, with the proviso that at least one of the radicals R.sup.1 and/or R.sup.6 contains between 9 to 50 carbon atoms,some of which are known, stimulate the immune system's response and antibody production.Type: GrantFiled: November 28, 1984Date of Patent: December 29, 1987Assignee: Bayer AktiengesellschaftInventors: Bernd-Wieland Kruger, Oswald Lockhoff, Karl G. Metzger, Hans-Georg Opitz, Klaus Schaller, Klaus G. Stunkel, Hans-Joachim Zeiler
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Patent number: 4710491Abstract: A method of combating rheumatic diseases which comprises administering to a patient afflicted therewith an amount effective to combat such disease of a compound of the formula ##STR1## in which Z is a glycosyl radical bonded via the anomeric carbon atom,R.sub.1 is hydrogen or an optionally substituted hydrocarbon radical with up to 30 C atoms, which hydrocarbon radical is optionally interrupted by O, N or S, andR.sub.2 is hydrogen or an alkyl or aralkyl radical with up to 30 C atoms, which is optionally interrupted by O, N or S or substituted by an oxygen-containing group or halogen,with the proviso that COR.sub.1 is not an acyl group with 1-5 C atoms if R.sub.2 is alkyl with 10-20 C atoms.Type: GrantFiled: December 14, 1984Date of Patent: December 1, 1987Assignee: Troponwerke GmbH & Co., KGInventors: Oswald Lockhoff, Peter Stadler, Hans-Georg Opitz, Harald Horstmann, Bodo Junge, Bernhard Pelster
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Substituted O-sulphonyl-glycosylamides, processes for their preparation and their use as medicaments
Patent number: 4699899Abstract: Novel compounds of the formula ##STR1## in which X is hydrogen or --CH.sub.2 --OR.sup.5,Z represents OR.sup.4, NH.sub.2 or ##STR2## R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each independently is hydrogen or ##STR3## at least one of R.sup.2, R.sup.3, R.sup.4 and R.sup.5 being ##STR4## Y and W each independently is oxygen, sulphur, NH or CH.sub.2, and R.sup.1, R.sup.6, R.sup.7 and R.sup.8 each independently is an optionally substituted hydrocarbon radical with up to 50 C atoms,stimulate the immune system.Type: GrantFiled: February 21, 1986Date of Patent: October 13, 1987Assignee: Bayer AktiengesellschaftInventors: Bernd-Wieland Kruger, Yutaka Hayauchi, Oswald Lockhoff, Peter Stadler, Karl G. Metzger, Klaus G. Stunkel, Hans-Joachim Zeiler -
Patent number: 4686208Abstract: Compounds of the formula ##STR1## in which R.sup.1 represents an optionally substituted, straight-chain or branched, saturated, monounsaturated or polyunsaturated alkyl radical, an optionally substituted, saturated or one- or polyunsaturated cycloalkyl radical or an optionally substituted aryl radical or aralkyl radical,X represents CH.sub.2, O, S, NH or N-alkyl with up to 20 C atoms,R.sup.2 has the meaning of R.sup.1, and can represent hydrogen if X denotes CH.sub.2, the radicals R.sup.3 independently of one another represent hydrogen, an acyl radical or alkyl radical with in each case up to 20 C atoms, a silyl radical and/or a phosphoric acid or phosphoric acid ester radical andR.sup.4 denotes hydrogen, methyl or --CH.sub.2 --OR.sup.3, with the proviso that one of the radicals R.sup.3 always represents a phosphoric acid or phosphoric acid ester radical, which stimulate a patient's immune system and are thereby effective in combating viral disease and bacterial infection.Type: GrantFiled: November 21, 1984Date of Patent: August 11, 1987Assignee: Bayer AktiengesellschaftInventors: Oswald Lockhoff, Bernd-Wieland Kruger, Peter Stadler, Arnold Paessens, Gert Streissle, Peter Taylor, Hans-Joachim Zeiler, Karl-Georg Metzger
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Patent number: 4683222Abstract: The invention relates to N-glycosylated carboxamide derivatives of Formula I which are useful for influencing the body's inherent defenses, e.g. for increasing immune system antibodies. Also included in the invention are compositions containing said N-glycosylated carboxamide derivative of Formula I as active ingredients and methods for the use of said compounds and compositions.Type: GrantFiled: April 19, 1985Date of Patent: July 28, 1987Assignee: Bayer AktiengesellschaftInventors: Peter Stadler, Oswald Lockhoff, Hans-Georg Opitz, Klaus Schaller
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Patent number: 4680287Abstract: Growth of animals is promoted by inclusion in their feed of compounds of the formula ##STR1## in which Z is a glycosyl radical bonded via the anomeric carbon atom,R.sub.1 is hydrogen or an optionally substituted hydrocarbon radical having up to 30 Carbon atoms optionally interrupted by O, N or S, andR.sub.2 is hydrogen or an alkyl or aralkyl radical having up to 30 Carbon atoms optionally interrupted by O or substituted by groups containing oxygen or by halogen, with the proviso that COR.sub.1 is not an acyl group having 1-5 Carbon atoms when R.sub.2 is an alkyl group having 10-20 Carbon atoms.Type: GrantFiled: October 26, 1984Date of Patent: July 14, 1987Assignee: Bayer AktiengesellschaftInventors: Oswald Lockhoff, Peter Stadler, Martin Scheer, Friedrich Berschauer, Anno de Jong
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Patent number: 4631272Abstract: Compounds of the formula ##STR1## in which R.sup.1 represents hydrogen or an optionally substituted, straight-chain or branched alkyl or mono- or poly-unsaturated alkenyl radical with in each case up to 30 C atoms,X represents CH.sub.2, O, S or NR,whereinR denotes hydrogen or an alkyl group with up to 20 C atoms, andR.sup.2 represents hydrogen or an optionally substituted, straight-chain or branched, saturated or mono- or poly-unsaturated hydrocarbon radical with up to 30 C atoms,or pharmaceutically acceptable salts thereof, stimulate the immune system and help fight infection.Type: GrantFiled: February 8, 1985Date of Patent: December 23, 1986Assignee: Bayer AktiengesellschaftInventors: Oswald Lockhoff, Bernd-Wieland Kruger, Peter Stadler, Karl G. Metzger, Hein-Peter Kroll, Klaus Schaller, Hans-Joachim Zeiler
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Patent number: 4574122Abstract: Compounds of the formula ##STR1## in which X is hydrogen or the radical --CH.sub.2 OR.sup.5,three of R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each independently is hydrogen or ##STR2## and the fourth is ##STR3## Z each independently is oxygen, sulphur, NH or CH.sub.2, and R.sup.1, R.sup.6 and R.sup.7 each independently is an optionally substituted hydrocarbon radical having up to 50 carbon atoms,stimulate the immune system's response and antibody production.Type: GrantFiled: November 28, 1984Date of Patent: March 4, 1986Assignee: Bayer AktiengesellschaftInventors: Bernd-Wieland Kruger, Oswald Lockhoff, Peter Stadler, Karl G. Metzger, Hans-Georg Opitz, Klaus G. Stunkel, Hans-Joachim Zeiler
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Patent number: 4438260Abstract: The invention relates to sisomicin derivatives of formula (I) and methods for their preparation. Also included in the invention are compositions containing said sisomicin derivatives and the use of said derivatives and compositions for the treatment of bacterial infections.Type: GrantFiled: December 24, 1981Date of Patent: March 20, 1984Assignee: Bayer AktiengesellschaftInventors: Uwe Petersen, Peter Stadler, Oswald Lockhoff, Hans-Joachim Zeiler, Karl G. Metzger