Patents by Inventor Henrich H. Paradies
Henrich H. Paradies 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: 5604206Abstract: New complexes of S(+)-ibuprofen and amino sugars are described. These complexes are particularly suitable for the treatment of inflammations and pains.Type: GrantFiled: February 18, 1994Date of Patent: February 18, 1997Assignee: Medice Chem.-Pharm. Fabrik Putter GmbH & Co. KGInventor: Henrich H. Paradies
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Patent number: 5380927Abstract: A chemical process is disclosed for the preparation of a pharmaceutically active compound in stereospecific form selected from the group of compounds having the formula: ##STR1## and their physiologically compatible salts and esters, wherein R is a lower alkyl and Ar a monocyclic, polycyclic or orthocondensed polycyclic aromatic group having up to 12 carbon atoms in the aromatic ring, and which may be substituted or unsubstituted in the aromatic ring, comprising the steps:a) reacting a carbonyl substrate of the formula: ##STR2## where R and Ar have the meanings given above, with a stereospecific reagent in the presence of a reducing agent and an organic solvent to form the enatiomeric carbinol andb) reacting the enantiomeric carbinol obtained to form the end product.Type: GrantFiled: May 16, 1990Date of Patent: January 10, 1995Assignee: Medice Chem.-Pharm. Fabrik Putter GmbH & Co. KGInventors: Henrich H. Paradies, Samir B. Hanna, Bernd Schneider
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Patent number: 5266723Abstract: A chemical process is disclosed for the preparation of a pharmaceutically active compound in an enantiomeric form either (R) or (S) of the structure ##STR1## and a suitable pharmaceutical salt, e.g. alkali or earth metal, D-glucamine or D-ribamine, where R.sub.1 represents an optionally substituted aryl group same as phenyl or naphthyl group, optionally including a heterocyclic ring system, which is optionally substituted, or represents a hetero-aromatic ring system optionally containing in addition to carbon atoms one or more atoms selected from the group consisting of nitrogen and oxygen; the enantiomeric R or S-compounds of (I) are obtained from a suitable ketone (II) by reduction with an LiAlH.sub.4.sup.Type: GrantFiled: February 27, 1990Date of Patent: November 30, 1993Assignee: Medice, Ltd., Chem.-Pharm. Fabrik Putter GmbH & Co. KGInventors: Samir B. Hanna, Bernd Schneider, Henrich H. Paradies
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Patent number: 5254728Abstract: Complexes containing S(+)-ibuprofen, method for the production of these complexes and pharmaceutical preparations containing these complexes are described.Type: GrantFiled: November 15, 1991Date of Patent: October 19, 1993Assignee: Medice Chem.-pharm. Fabrik Putter GmbH & Co. KGInventor: Henrich H. Paradies
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Patent number: 5248815Abstract: The present invention relates to a stereospecific chemical synthesis of optically pure enantiomers of 2-aryl-alkanoic acids, especially those of the biologically active (S)-aryl-propionic acids, in good chemical yields, useful for preparing large quantities thereof, and having a high optical purity.Type: GrantFiled: December 27, 1991Date of Patent: September 28, 1993Inventor: Henrich H. Paradies
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Patent number: 5143917Abstract: The synthesis and application of N(1)-n-alkyl-pyrimidinium-salts are described. These surfactants have a very small critical micelle concentration ()CMC) in the order of 10.sup.-5 -10.sup.-7 Mol/Liter. These N(1)-n-alkyl-pyrimidinium components have pharmacological activities and can act as antimetabolites.Type: GrantFiled: May 24, 1990Date of Patent: September 1, 1992Assignee: Medice Chem.-Pharm. Fabrik Putter GmbH & Co. KGInventor: Henrich H. Paradies
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Patent number: 5118808Abstract: The synthesis and application of N(1)-n-alkyl-pyrimidinium-salts are described. These surfactants have a very small critical micelle concentration (CMC) in the order of 10.sup.-5 -10.sup.-7 Mol/Liter. These N(1)-n-alkyl-pyrimidinium components have pharmacological activities and can act as antimetabolites.Type: GrantFiled: May 24, 1990Date of Patent: June 2, 1992Assignee: Medice Chem.-Pharm. Fabrik Putter GmbH & Co. KGInventor: Henrich H. Paradies
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Patent number: 5112844Abstract: The synthesis of quaternary five membered N-n-alkyl-heterocycles, especially of 4-hydroxy-N(1)-n-alkyl-imidazolium, 2,5-substituted N(3)-n-alkyl-thiazolium and substituted N(2) pyrazolium salts are described. The N-surfactants obtained have a very small critical micelle concentration (CMC) of 10.sup.-5 -10.sup.-7 Mol/Liter, and are capable of forming micelles of different sizes and forms depending on the nature of the anions. The N-detergents can be used as pharmaceuticals.Type: GrantFiled: April 3, 1991Date of Patent: May 12, 1992Assignee: Medice chem.-pharm. Fabrik Putter GmbH & Co. KGInventor: Henrich H. Paradies
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Patent number: 5110929Abstract: The synthesis of 4-, 4-(1,1)-and 3,5-substituted N-alkyl-pyridinium salts as well as of 2-carboxamide substituted N(1,4)diazinium compounds are described. The N-surfactants obtained have a small critical micelle concentration (CMC) of 10.sup.-5 -10.sup.-7 Mol/Liter. These surfactants produce micells of different size and form depending on the nature of the anions. 4-(1,1)-substituted and 3,5-substituted N-alkyl-pyridinium components are capable of forming vesicles in equeous solutions of different forms and sizes. The N-surfactants synthesized can be used as pharmaceuticals.Type: GrantFiled: June 14, 1990Date of Patent: May 5, 1992Assignee: Medice Cham.-Pharm. Fabrik Putter GmbH & Co. KGInventor: Henrich H. Paradies
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Patent number: 5057518Abstract: The synthesis and application of N(1)-n-alkyl-pyrimidinium-salts are described. These surfactants have a very small critical micelle concentration (CMC) in the order of 10.sup.-5 -10.sup.-7 Mol/Liter. These N(1)-n-alkyl-pyrimidinium components have pharmacological activities and can act as antimetabolites.Type: GrantFiled: May 24, 1990Date of Patent: October 15, 1991Assignee: Medice Hem.-Pharm. Fabrik Putter GmbH & Co. KGInventor: Henrich H. Paradies
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Patent number: 5051435Abstract: The synthesis of quaternary five membered N-n-alkyl-hetero-cycles, especially of 4-hydroxy-N(1)-n-alkyl-imidazolium, 2,5-substituted N(3)-n-alkyl-thiazolium and substituted N(2) pyrazolium salts are described. The N-surfactants obtained have a very small critical micelle concentration (CMC) of 10.sup.-5 -10.sup.-7 Mol/Liter, and are capable of forming micelles of different sizes and forms depending on the nature of the anions. The N-detergents can be used as pharmaceuticals.Type: GrantFiled: June 4, 1990Date of Patent: September 24, 1991Assignee: Medice Chem.-Pharm. Fabrik Putter GmbH & Co. KGInventor: Henrich H. Paradies
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Patent number: 5045530Abstract: A pharmaceutical preparation is disclosed which is made up of a micelle or a vesicle each consisting of a cationic tenside with a monovalent ion and a hydrophobic cyclic or linear peptide, dispersed in a solvent whose pH value lies between pH 7-pH 8, the critical micellization concentration (cmc) lying in the range of 1.0.10.sup.-7 to 7.0.10.sup.-5 mol/liter. The preparations disclosed have in particular the advantage that by the increasing of the hydrophobicity of the alkyl or aryl chain or the radical at the N.sup.+ tenside both the membrane permeability is increased and furthermore the pharmaceutical active substance, in particular linear and cyclic tyrocidines (A-J), can be transferred actively into the cytosol. They thus act on the transciption level. In addition, linear and cyclic tyrocidines in particular have antiviral effects.Type: GrantFiled: April 27, 1989Date of Patent: September 3, 1991Assignee: Medici Chem.-Pharm. Fabrik Putter GmbHInventor: Henrich H. Paradies
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Patent number: 4999435Abstract: The synthesis of 7-n-alkyl-imidazolium [4,5-d]-pyrimidines, 6-substituted-3n-alkyl-benzimidazolium- and 3n-alkyl-5,6-substituted-benzthiazolium salts are described. These N.sup.+ -surfactants having a substituted heterocycle as a head group have distinguished small critical micelle concentrations (CMC) in the range of 10.sup.-5 -10.sup.-7 Mol/Liter. The size and shape of these micelles in watery solutions are determined by the nature of the anion. The N-surfactants can be used as pharmaceuticals as well as reporter groups in fluorescence studies including immunological assays.Type: GrantFiled: July 24, 1989Date of Patent: March 12, 1991Assignee: Medice Chem.-Pharm. Fabrik Putter GmbH & Co. KGInventor: Henrich H. Paradies
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Patent number: 4965357Abstract: The synthesis and application of N(1)-n-alkyl-pyrimidinium-salts are described. These surfactants have a very small critical micelle concentration (CMC) in the order of 10.sup.-5 -10.sup.-7 Mol/Liter. These N(1)-n-alkyl-pyrimidinium components have pharmacological activities and can act as antimetabolites.Type: GrantFiled: August 6, 1987Date of Patent: October 23, 1990Assignee: Medice Chem.-Pharm. Fabrik Putter GmbH & Co. KGInventor: Henrich H. Paradies
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Patent number: 4894454Abstract: The synthesis of 4-, 4-(1,1)- and 3,5- substituted N-alkyl-pyridinium salts as well as of 2-carboxamide substituted N(1,4)diazinium compounds are described. The N-surfactants obtained have a small critical micelle concentration (CMC) of 10.sup.-5 -10.sup.-7 Mol/Liter. These surfactants produce micells of different size and form depending on the nature of the anions. 4-(1,1)-substituted and 3,5-substituted N-alkyl-pyridinium components are capable of forming vesicles in equeous solutions of different forms and sizes. The N-surfactants synthesized can be used as pharmaceuticals.Type: GrantFiled: August 6, 1987Date of Patent: January 16, 1990Assignee: Medice Chem.-Pharm. Fabrik, Putter GmbH & Co., KGInventor: Henrich H. Paradies
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Patent number: 4877883Abstract: The synthesis of quaternary five membered N-n-alkyl-heterocycles, especially of 4-hydroxy-N(1)-n-alkyl-imidazolium, 2,5-substituted N(3)-n-alkyl-thiazolium and substituted N(2) pyrazolium salts are described. The N-surfactants obtained have a very small critical micelle concentration (CMC) of 10.sup.-5 -10.sup.-7 Mol/Liter, and are capable of forming micelles of different sizes and forms depending on the nature of the anions. The N-detergents can be used as pharmaceuticals.Type: GrantFiled: August 6, 1987Date of Patent: October 31, 1989Assignee: Medice chem.-pharm. Fabrik Putter GmbH & Co. KGInventor: Henrich H. Paradies
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Patent number: 4874850Abstract: A pharmaceutical preparation is disclosed which is made up of a micelle or a vesicle each consisting of a cationic tenside with a monovalent ion and a hydrophobic cyclic or linear peptide, dispersed in a solvent whose pH value lies between pH 7-pH 8, the critical micellization concentration (cmc) lying in the range of 1.0 . 10.sup.-7 to 7.0 . 10.sup.-5 mol/liter. The preparation disclosed have in particular the advantage that by the increasing of the hydrophobicity of the alkyl or aryl chain or the radical at the N.sup.+ tenside both the membrane permeability is increased and furthermore the pharmaceutical active substance, in particular linear and cyclic tyrocidines (A-E), can be transferred actively into the cytosol. They thus act on the transcription level. In addition, linear and cyclic tyrocidines in particular have antiviral effects.Type: GrantFiled: August 6, 1987Date of Patent: October 17, 1989Assignee: Medice Chem.-Pharm. Fabrik Putter GmbH & Co.Inventor: Henrich H. Paradies
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Patent number: 4870174Abstract: The synthesis of 7-n-alkyl-imidazolium[4,5-d]-pyrimidines, 6-substituted-3n-alkyl-benzimidazolium- and 3n-alkyl-5,6-substituted-benzthiazolium salts are described. There N.sup.+ -surfactants having a substituted heterocycle as a head group have distinguished small critical micelle concentrations (CMC) in the range of 10.sup.-5 -10.sup.-7 Mol/Liter. The size and shape of these micelles in watery solutions are determined by the nature of the anion. The N-surfactants can be used as pharmaceuticals as well as reporter groups in fluorescence studies including immunological assays.Type: GrantFiled: August 6, 1987Date of Patent: September 26, 1989Assignee: Medice chem.-pharm. FabrikInventor: Henrich H. Paradies