Patents by Inventor Harald Zilch
Harald Zilch 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: 7176011Abstract: A membranous enzyme not yet described in the state-of-the-art can be extracted from cellular membrane fractions of blood leukocytes or monocytes/macrophages. Also disclosed is the use of substrates of this enzyme to prepare medicaments that contain these substrates as pharmaceutical active substance. These medicaments are useful to direct pharmacologically active substances to target cells and to enrich target cells with said substances. Also disclosed are in-vitro research systems containing this enzyme used to detect other substrates of this enzyme.Type: GrantFiled: August 5, 2002Date of Patent: February 13, 2007Assignee: Heidelberg Pharma AGInventors: Dieter Herrmann, Hans-George Opitz, Harald Zilch
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Publication number: 20030082167Abstract: A membranous enzyme not yet described in the state-of-the-art can be extracted from cellular membrane fractions of blood leukocytes or monocytes/macrophages. Also disclosed is the use of substrates of this enzyme to prepare medicaments that contain these substrates as pharmaceutical active substance. These medicaments are useful to direct pharmacologically active substances to target cells and to enrich target cells with said substances. Also disclosed are in-vitro research systems containing this enzyme used to detect other substrates of this enzyme.Type: ApplicationFiled: August 5, 2002Publication date: May 1, 2003Applicant: Heidelberg Pharma Holding GmbHInventors: Dieter Herrmann, Hans-George Opitz, Harald Zilch
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Publication number: 20020106363Abstract: A membranous enzyme not yet described in the state-of-the-art can be extracted from cellular membrane fractions of blood leukocytes or monocytes/macrophages. Also disclosed is the use of substrates of this enzyme to prepare medicaments that contain these substrates as pharmaceutical active substance. These medicaments are useful to direct pharmacologically active substances to target cells and to enrich target cells with said substances. Also disclosed are in-vitro research systems containing this enzyme used to detect other substrates of this enzyme.Type: ApplicationFiled: December 27, 1999Publication date: August 8, 2002Inventors: DIETER HERRMANN, HANS-GEORGE OPTIZ, HARALD ZILCH
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Patent number: 6372725Abstract: The present invention concerns new phospholipid derivatives of nucleosides of the general formula (I) in which R1 represents a straight-chained or branched, saturated or unsaturated aliphatic residue with 9-14 carbon atoms which can optionally be substituted once or several times; R2 can represent a straight-chained or branched, saturated or unsaturated aliphatic residue with 8-12 carbon atoms which can optionally be substituted once or several times; m is 2 or 3; A can represent a methylene group or an oxygen; Nuc can be a nucleoside or a residue derived from a nucleoside derivative; and tautomers thereof and their physiologically tolerated salts of inorganic and organic acids and bases as well as pharmaceutical preparations containing these compounds.Type: GrantFiled: December 4, 1998Date of Patent: April 16, 2002Inventors: Harald Zilch, Dieter Herrmann
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Patent number: 6177469Abstract: The present invention concerns new immunosuppressive and antiviral pharmaceutical agents using lipid alcohols of the general formulae I and II in which R1 represents a straight-chained or branched, saturated or unsaturated alkyl chain with 1-30 carbon atoms which can optionally be substituted once or several times by halogen, C1-C6 alkoxy, C1-C6 alkylmercapto, C1-C6 alkoxycarbonyl, carboxy, C1-C6 alkylsulfinyl or C1-C6 alkylsulfonyl groups, R2 represents hydrogen, a straight-chained or branched, saturated or unsaturated alkyl chain with 1-20 carbon atoms which can optionally be substituted once or several times by halogen, C1-C6 alkoxy, C1-C6 alkylmercapto, C1-C6 alkoxycarbonyl or C1-C6 alkylsulfonyl groups, X represents a valency dash, oxicarbonyl, carbonyloxy, amidocarbonyl, carbonylamido, oxygen, sulphur, a sulfinyl or sulfonyl group Y represents a valency dash, oxicarbonyl, carbonyloxy, amidocarbonyl, carbonylamido, oxygen, sulphur, a sulfinyl or sulfonyl group n represents an integType: GrantFiled: June 22, 1998Date of Patent: January 23, 2001Inventors: Harald Zilch, Dieter Herrmann, Hans-Georg Opitz
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Patent number: 6136797Abstract: The present invention concerns new lipid derivatives of phosphonocarboxylic acids of the general formula I, ##STR1## in which the meaning of the symbols is elucidated in the description, tautomers thereof and their physiologically tolerated esters and salts of inorganic or organic bases as well as processes for the production thereof and pharmaceutical agents containing these compounds.Type: GrantFiled: August 27, 1998Date of Patent: October 24, 2000Inventors: Harald Zilch, Dieter Herrmann, Hans-George Opitz, Gerd Zimmermann
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Patent number: 6080734Abstract: The present invention is directed to new phospholipid derivatives of acyclovir and ganciclovir that link a lipid moiety, which represents a substituted C3 backbone, to acyclovir or ganciclovir via phosphate or thiophosphate. The compounds are particularly suitable for the therapy of viral infections.Type: GrantFiled: December 11, 1998Date of Patent: June 27, 2000Assignee: Roche Diagnostic GmbHInventors: Harald Zilch, Dieter Herrmann
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Patent number: 6025343Abstract: The present invention is directed to new nucleoside monophosphate derivatives of lipid ester residues of general formula (I) ##STR1## wherein R.sup.1 represents an optionally substituted alkyl chain having 1-20 carbon atoms;R.sup.2 represents hydrogen, an optionally substituted alkyl chain having 1-20 carbon atoms;R.sup.3, R.sup.4 and R.sup.5 represent hydrogen, hydroxy, azido, amino, cyano, or halogen;X represents a valence dash, oxygen, sulfur, a sulfinyl or sulfonyl group;Y represents a valence dash, an oxygen or sulfur atom;B represents a purine and/or pyrimidine base;with the proviso that at least one of the residues R.sup.3 or R.sup.5 is hydrogen;to their tautomers and their physiologically acceptable salts of inorganic and organic acids and/or bases, as well as to processes for their preparation, and to drugs containing said compounds.Type: GrantFiled: November 27, 1996Date of Patent: February 15, 2000Assignee: Roche Diagnostics GmbHInventors: Dieter Herrmann, Hans-Georg Opitz, Harald Zilch, Alfred Mertens
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Covalent lipid-phosphono-carboxylic acid conjugates and application thereof as antiviral medicaments
Patent number: 5955452Abstract: The present invention concerns new lipid derivatives of phosphonocarboxylic acids of the general formula I, ##STR1## in which the meaning of the symbols is elucidated in the description, tautomers thereof and their physiologically tolerated salts of inorganic and organic bases as well as processes for the production thereof and pharmaceutical agents containing these compounds.Type: GrantFiled: August 26, 1998Date of Patent: September 21, 1999Assignee: Roche Diagnostics GmbHInventors: Harald Zilch, Dieter Herrmann, Hans-George Opitz, Gerd Zimmermann, Edgar Voss -
Patent number: 5756711Abstract: Compounds of the formula I ##STR1## in which R.sub.1 and R.sub.2 represent a possibly substituted C.sub.8 -C.sub.15 -alkyl chain, n the number 0, 1 or 2 and A the residue of a nucleoside, processes for their preparation, as well as antiviral medicaments which contain these compounds.Type: GrantFiled: June 10, 1996Date of Patent: May 26, 1998Assignee: Boehringer Mannheim GmbHInventors: Harald Zilch, Herbert Leinert, Alfred Mertens, Dieter Herrmann
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Patent number: 5734042Abstract: The present invention concerns a process for the production of asymmetrical phosphoric acid diesters.The process is characterized in that a phosphoric acid ester is condensed with a compound containing hydroxy groups in the presence of an arylsulfonic acid chloride and an organic base, the residue of evaporation is stirred out with an organic solvent after the hydrolysis, the arylsulfonic acid pyridine salt which forms is nearly completely crystallized and recycled, the lipid derivative that is formed is precipitated as a sparingly soluble salt by addition of a solution containing alkaline-earth ions and isolated, the sparingly soluble salt is isolated as the free acid in an organic solvent by suspension in a water-immiscible organic solvent and a dilute aqueous mineral acid, the crude product is purified if desired, by means of preparative chromatography on a RP phase and subsequently the free acid is converted if desired into any desired salt.Type: GrantFiled: July 29, 1996Date of Patent: March 31, 1998Assignee: Boehringer Mannheim GmbHInventors: Einhard Kiegel, Harald Zilch
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Patent number: 5563257Abstract: Liponucleotides containing an ether linkage in the 2-position and a thioether, sulfoxide, or sulfone linkage in the 3-position. The nucleoside component of said liponucleotide is AZT or 3'-deoxy-3'-fluorothymidine. These compounds exhibit antiviral activity.Type: GrantFiled: May 9, 1995Date of Patent: October 8, 1996Assignee: Boehringer Mannheim GmbHInventors: Harald Zilch, Herbert Leinert, Alfred Mertens, Dieter Herrmann
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Patent number: 5543561Abstract: Compounds of the formula I ##STR1## in which R.sup.1 signifies hydrogen, a straight-chained, branched, saturated or unsaturated alkyl radical with 1-9 carbon atoms possibly substituted by phenyl or a phenyl ring which is possibly substituted by C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 -alkoxy or halogen, R.sup.2 signifies hydrogen or C.sub.1 -C.sub.3 -alkyl, whereby the two radicals can be the same or different, R represents hydrogen or a straight-chained or branched alkyl radical with 1-4 carbon atoms, X signifies an alkylene chain with 1-6 carbon atoms which can be substituted one or more times by C.sub.1 -C.sub.Type: GrantFiled: March 28, 1995Date of Patent: August 6, 1996Assignee: Boehringer Mannheim GmbHInventors: Harald Zilch, Frieder Bauss
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Patent number: 5512564Abstract: The present invention concerns thiazolo- 2,3-a!pyrrole and oxazolo- 1,2-a!pyrrole derivatives of formula I ##STR1## in which HET represents a heterocyclic ring with 3-7 ring atoms which can be substituted by one, two or three residues R.sup.1 which can be the same or different,Y represents an oxygen or sulphur atom, or a SO or SO.sub.2 group,X can be an oxygen or sulphur atom,R denotes an aliphatic residue with 1-9 C-atoms which can be substituted by phenyl or denotes a phenyl ring or a carbocyclic ring with 7-15 C atoms or a heterocyclic ring system each having 5 or 6 ring atoms,in which the aforementioned phenyl rings, carbocyclic rings or heterocyclic ring system can be substituted once or several times, if desired, and R1-R5 denote hydrogen or an aliphatic residue, as well as their tautomers, enantiomers, diastereomers and physiologically tolerated salts.Type: GrantFiled: March 4, 1994Date of Patent: April 30, 1996Assignee: Boehringer Mannheim GmbHInventors: Harald Zilch, Herbert Leinert, Alfred Mertens
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Patent number: 5446139Abstract: The invention concerns nucleoside derivatives of the formula I ##STR1## in which Ba signifies an indolyl (A), benzimidazolyl (B), pyrrolopyridinyl (C), imidazopyridinyl (D), triazolopyrimidinyl (E), imidazotriazinyl (F) or imidazopyrimidinyl (G) group substituted by R.sup.1, R.sup.2 and R.sup.3, in which R.sup.1, R.sup.2 and R.sup.3, which can be the same or different, signify hydrogen, halogen, a C.sub.1 -C.sub.7 -alkyl, C.sub.2 -C.sub.7 -alkenyl, hydroxy, mercapto, C.sub.1 -C.sub.7 -alkylthio, C.sub.1 -C.sub.7 -alkoxy, C.sub.2 -C.sub.7 -alkenyloxy, ar-C.sub.1 -C.sub.5 -alkyl, ar-C.sub.2 -C.sub.5 -alkenyl, ar-C.sub.1 -C.sub.5 -alkoxy, ar-C.sub.2 -C.sub.5 -alkenyloxy, aryloxy, nitro, amino-C.sub.1 -C.sub.7 -alkyl, C.sub.1 -C.sub.7 -alkylamino-C.sub.1 -C.sub.7 -alkyl, di-C.sub.1 -C.sub.7 -alkylamino-C.sub.1 -C.sub.7 -alkyl, amino, a substituted amino group --NMR.sup.4 or --N(R.sup.4).sub.2 or an imino group --N.dbd.CH--R.sup.4, and R.sup.4 has the meaning given in the description, R.sup.5, R.sup.6, R.sup.Type: GrantFiled: February 21, 1992Date of Patent: August 29, 1995Assignee: Boehringer Mannheim GmbHInventors: Frank Seela, Werner Bourgeouis, Rainer Gumbiowski, Angelika Roling, Helmut Rosemeyer, Alfred Mertens, Harald Zilch, Bernhard Konig, Edith Koch
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Patent number: 5414088Abstract: The invention concerns compounds of formula I ##STR1## where R.sup.1 is hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.3 -C.sub.7 -cycloalkyl, R.sup.2 is C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, cyano, carboxy [carbonyl substituted by hydroxyl], C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, amino, C.sub.1 -C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino or hydrazino or R.sup.1 and R.sup.2 together are C.sub.2 -C.sub.6 -alkylidene or C.sub.3 -C.sub.6 -cycloalkylidene or R.sup.1 and R.sup.2, together with the carbon atoms to which they are attached, form a C.sub.3 -C.sub.7 -spirocycle, n is 0 or 1, R.sup.3 is hydrogen, C.sub.1 -C.sub.8 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, C.sub.3 -C.sub.7 -cycloalkyl, benzyl, carboxy-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkyloxycarbonyl-C.sub.1 -C.sub.6 -alkyl or di-C.sub.1 -C.sub.6 -alkyloxophosphinyl-C.sub.1 -C.sub.6 -alkyl and R.sup.4 -R.sup. 6 are as in the specification.Type: GrantFiled: April 14, 1992Date of Patent: May 9, 1995Assignee: Boehringer Mannheim GmbHInventors: Wolfgang Von Der Saal, Harald Zilch, Erwin Bohm
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Patent number: 5397794Abstract: The present invention concerns the use of compounds of the general formula I ##STR1## for the preparation of medicaments for the treatment of viral or retroviral infections, whereby R signifies a hydrogen atom or a straight-chained or branched, saturated or unsaturated alkyl radical with 1-7 carbon atoms, which can possibly be substituted by phenyl, or a phenyl ring which can possibly be substituted one or more times by C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, hydroxyl, trifluoromethyl, methylsulphonyl or halogen, such as fluorine, chlorine or bromine, n stands for the numbers 0, 1 or 2, as well as of their pharmacologically compatible salts or tautomers.Type: GrantFiled: July 20, 1993Date of Patent: March 14, 1995Assignee: Boehringer Mannheim GmbHInventors: Harald Zilch, Alfred Mertens, Herbert Leinert, Ulrike Leser, Bernhard Konig, Hans Seidel
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Patent number: 5373019Abstract: The present invention provides compounds and pharmaceutical compositions containing indolones of the general formula: ##STR1## These indolones where n.dbd.o and the pharmaceutical compositions containing these compounds are used for the treatment of diseases in which erythrocyte and thrombocyte aggregation play an important part, especially for the inhibition of aggregation of these cells.Type: GrantFiled: January 11, 1991Date of Patent: December 13, 1994Assignee: Boehringer Mannheim GmbHInventors: Harald Zilch, Alfred Mertens, Wolfgang Von Der Saal, Erwin Boehm, Klaus Strein
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Patent number: 5366969Abstract: Compounds of the formula I ##STR1## in which R can be hydrogen or C.sub.1 -C.sub.4 -alkyl, R.sup.1 hydrogen, C.sub.1 -C.sub.6 -alkyl, aryl, aryl-C.sub.1 -C.sub.4 -alkyl, amino-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkylamino-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.6 -dialkylamino-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkylthio-C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.7 -alkenyl, R.sup.2 R.sup.1 or C.sub.2 -C.sub.7 -alkenyl, C.sub.1 -C.sub.6 -alkylmercapto, C.sub.1 -C.sub.6 -alkoxy, phenoxy-C.sub.1 -C.sub.4 -alkyl,amino, C.sub.1 -C.sub.4 -alkylamino, di-C.sub.1 -C.sub.4 -alkylamino, morpholino, thiomorpholino, pyrrolidino, piperidino, hexamethyleneimino, pyrasolino, imidazolino, n 0, 1 or 2 and R.sup.1 and R.sup.Type: GrantFiled: March 6, 1992Date of Patent: November 22, 1994Assignee: Boehringer Mannheim GmbHInventors: Elmar Bosies, Harald Zilch
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Patent number: 5158942Abstract: The present invention is concerned with the use of compounds of the general formula: ##STR1## and of the pharmacologically acceptable salts thereof, as well as of the optical isomers thereof for the preparation of pharmaceutical compositions with antiviral action.The present invention also provides new phospholipid derivatives.Type: GrantFiled: August 23, 1990Date of Patent: October 27, 1992Assignee: Boehringer Mannheim GmbHInventors: Dieter Herrmann, Elmar Bosies, Harald Zilch, Edith Koch