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).

  • Patent number: 5604206
    Abstract: New complexes of S(+)-ibuprofen and amino sugars are described. These complexes are particularly suitable for the treatment of inflammations and pains.
    Type: Grant
    Filed: February 18, 1994
    Date of Patent: February 18, 1997
    Assignee: Medice Chem.-Pharm. Fabrik Putter GmbH & Co. KG
    Inventor: Henrich H. Paradies
  • Patent number: 5380927
    Abstract: 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: Grant
    Filed: May 16, 1990
    Date of Patent: January 10, 1995
    Assignee: Medice Chem.-Pharm. Fabrik Putter GmbH & Co. KG
    Inventors: Henrich H. Paradies, Samir B. Hanna, Bernd Schneider
  • Patent number: 5266723
    Abstract: 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: Grant
    Filed: February 27, 1990
    Date of Patent: November 30, 1993
    Assignee: Medice, Ltd., Chem.-Pharm. Fabrik Putter GmbH & Co. KG
    Inventors: Samir B. Hanna, Bernd Schneider, Henrich H. Paradies
  • Patent number: 5254728
    Abstract: Complexes containing S(+)-ibuprofen, method for the production of these complexes and pharmaceutical preparations containing these complexes are described.
    Type: Grant
    Filed: November 15, 1991
    Date of Patent: October 19, 1993
    Assignee: Medice Chem.-pharm. Fabrik Putter GmbH & Co. KG
    Inventor: Henrich H. Paradies
  • Patent number: 5248815
    Abstract: 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: Grant
    Filed: December 27, 1991
    Date of Patent: September 28, 1993
    Inventor: Henrich H. Paradies
  • Patent number: 5143917
    Abstract: 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: Grant
    Filed: May 24, 1990
    Date of Patent: September 1, 1992
    Assignee: Medice Chem.-Pharm. Fabrik Putter GmbH & Co. KG
    Inventor: Henrich H. Paradies
  • Patent number: 5118808
    Abstract: 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: Grant
    Filed: May 24, 1990
    Date of Patent: June 2, 1992
    Assignee: Medice Chem.-Pharm. Fabrik Putter GmbH & Co. KG
    Inventor: Henrich H. Paradies
  • Patent number: 5112844
    Abstract: 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: Grant
    Filed: April 3, 1991
    Date of Patent: May 12, 1992
    Assignee: Medice chem.-pharm. Fabrik Putter GmbH & Co. KG
    Inventor: Henrich H. Paradies
  • Patent number: 5110929
    Abstract: 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: Grant
    Filed: June 14, 1990
    Date of Patent: May 5, 1992
    Assignee: Medice Cham.-Pharm. Fabrik Putter GmbH & Co. KG
    Inventor: Henrich H. Paradies
  • Patent number: 5057518
    Abstract: 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: Grant
    Filed: May 24, 1990
    Date of Patent: October 15, 1991
    Assignee: Medice Hem.-Pharm. Fabrik Putter GmbH & Co. KG
    Inventor: Henrich H. Paradies
  • Patent number: 5051435
    Abstract: 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: Grant
    Filed: June 4, 1990
    Date of Patent: September 24, 1991
    Assignee: Medice Chem.-Pharm. Fabrik Putter GmbH & Co. KG
    Inventor: Henrich H. Paradies
  • Patent number: 5045530
    Abstract: 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: Grant
    Filed: April 27, 1989
    Date of Patent: September 3, 1991
    Assignee: Medici Chem.-Pharm. Fabrik Putter GmbH
    Inventor: Henrich H. Paradies
  • Patent number: 4999435
    Abstract: 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: Grant
    Filed: July 24, 1989
    Date of Patent: March 12, 1991
    Assignee: Medice Chem.-Pharm. Fabrik Putter GmbH & Co. KG
    Inventor: Henrich H. Paradies
  • Patent number: 4965357
    Abstract: 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: Grant
    Filed: August 6, 1987
    Date of Patent: October 23, 1990
    Assignee: Medice Chem.-Pharm. Fabrik Putter GmbH & Co. KG
    Inventor: Henrich H. Paradies
  • Patent number: 4894454
    Abstract: 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: Grant
    Filed: August 6, 1987
    Date of Patent: January 16, 1990
    Assignee: Medice Chem.-Pharm. Fabrik, Putter GmbH & Co., KG
    Inventor: Henrich H. Paradies
  • Patent number: 4877883
    Abstract: 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: Grant
    Filed: August 6, 1987
    Date of Patent: October 31, 1989
    Assignee: Medice chem.-pharm. Fabrik Putter GmbH & Co. KG
    Inventor: Henrich H. Paradies
  • Patent number: 4874850
    Abstract: 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: Grant
    Filed: August 6, 1987
    Date of Patent: October 17, 1989
    Assignee: Medice Chem.-Pharm. Fabrik Putter GmbH & Co.
    Inventor: Henrich H. Paradies
  • Patent number: 4870174
    Abstract: 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: Grant
    Filed: August 6, 1987
    Date of Patent: September 26, 1989
    Assignee: Medice chem.-pharm. Fabrik
    Inventor: Henrich H. Paradies