Patents by Inventor Michael Entzeroth

Michael Entzeroth 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: 10414728
    Abstract: The present invention provides a method of treating one or more sodium channel related diseases or disorders in an individual, including related symptoms. The method comprises administering to the individual a tetrahydropyridine derivative in an amount effective to treat sodium channel related diseases or disorders in individuals. These compounds are generally categorized as Ritalin related compounds. The present invention also provides compounds for use in the treatment of and also for use in the manufacture of a medicament for the treatment of sodium channel related diseases or disorders in an individual. A method is further provided for the preparation and isolation of the derivatives of the compound of the present invention.
    Type: Grant
    Filed: November 19, 2015
    Date of Patent: September 17, 2019
    Assignee: CENNERV PHARMA (S) PTE LTD
    Inventors: Anil Kumar Ratty, Michael Entzeroth
  • Publication number: 20180141907
    Abstract: The present invention provides a method of treating one or more sodium channel related diseases or disorders in an individual, including related symptoms. The method comprises administering to the individual a tetrahydropyridine derivative in an amount effective to treat sodium channel related diseases or disorders in individuals. These compounds are generally categorised as Ritalin related compounds. The present invention also provides compounds for use in the treatment of and also for use in the manufacture of a medicament for the treatment of sodium channel related diseases or disorders in an individual. A method is further provided for the preparation and isolation of the derivatives of the compound of the present invention.
    Type: Application
    Filed: January 18, 2018
    Publication date: May 24, 2018
    Inventors: Anil Kumar Ratty, Michael Entzeroth
  • Publication number: 20170355676
    Abstract: The present invention provides a method of treating one or more sodium channel related diseases or disorders in an individual, including related symptoms. The method comprises administering to the individual a tetrahydropyridine derivative in an amount effective to treat sodium channel related diseases or disorders in individuals. These compounds are generally categorised as Ritalin related compounds. The present invention also provides compounds for use in the treatment of and also for use in the manufacture of a medicament for the treatment of sodium channel related diseases or disorders in an individual. A method is further provided for the preparation and isolation of the derivatives of the compound of the present invention.
    Type: Application
    Filed: November 19, 2015
    Publication date: December 14, 2017
    Inventors: Anil Kumar Ratty, Michael Entzeroth
  • Publication number: 20090163480
    Abstract: The present invention relates to modified amino acids of general formula wherein A, Z, X, n, m, R, R2, R3, R4 and R11 are defined as in claims 1 to 5, their tautomers, their diastereomers, their enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them as well as their use for the production and purification of antibodies and as labelled compounds in RIA- and ELISA assays and as diagnostic or analytical aids in neurotransmitter research.
    Type: Application
    Filed: December 17, 2008
    Publication date: June 25, 2009
    Applicant: Dr. Karl Thomae GmbH
    Inventors: Klaus RUDOLF, Wolfgang EBERLEIN, Wolfhard ENGEL, Helmut PIEPER, Henri DOODS, Gerhard HALLERMAYER, Michael ENTZEROTH, Wolfgang WIENEN
  • Patent number: 7498325
    Abstract: The present invention relates to modified amino acids of general formula wherein A, Z, X, n, m, R, R2, R3, R4 and R11 are defined as in claims 1 to 5, their tautomers, their diastereomers, their enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them as well as their use for the production and purification of antibodies and as labelled compounds in RIA- and ELISA assays and as diagnostic or analytical aids in neurotransmitter research.
    Type: Grant
    Filed: April 29, 2004
    Date of Patent: March 3, 2009
    Assignee: Karl Thomas GmbH
    Inventors: Klaus Rudolf, Wolfgang Eberlein, Wolfhard Engel, Helmut Pieper, Henri Doods, Gerhard Hallermayer, Michael Entzeroth, Wolfgang Wienen
  • Publication number: 20040214819
    Abstract: The present invention relates to modified amino acids of general formula 1
    Type: Application
    Filed: April 29, 2004
    Publication date: October 28, 2004
    Applicant: Dr. Karl Thomae GmbH
    Inventors: Klaus Rudolf, Wolfgang Eberlein, Wolfhard Engel, Helmut Pieper, Henri Doods, Gerhard Hallermayer, Michael Entzeroth, Wolfgang Wienen
  • Publication number: 20030069231
    Abstract: The present invention relates to modified amino acids of general formula 1
    Type: Application
    Filed: April 10, 2002
    Publication date: April 10, 2003
    Inventors: Klaus Rudolf, Wolfgang Eberlein, Wolfhard Engel, Helmut Pieper, Henri Doods, Gerhard Hallermayer, Michael Entzeroth, Wolfgang Wienen
  • Patent number: 6344449
    Abstract: The present invention relates to modified amino acids of general formula wherein A, Z, X, n, m, R, R2, R3, R4 and R11 are defined as in claims 1 to 5, their tautomers, their diastereomers, their enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them as well as their use for the production and purification of antibodies and as labelled compounds in RIA- and ELISA assays and as diagnostic or analytical aids in neurotransmitter research.
    Type: Grant
    Filed: October 12, 1999
    Date of Patent: February 5, 2002
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Klaus Rudolf, Wolfgang Eberlein, Wolfhard Engel, Helmut Pieper, Henri Doods, Gerhard Hallermayer, Michael Entzeroth, Wolfgang Wienen
  • Publication number: 20010036946
    Abstract: The present invention relates to modified amino acids of general formula 1
    Type: Application
    Filed: February 21, 2001
    Publication date: November 1, 2001
    Inventors: Klaus Rudolf, Wolfgang Eberlein, Wolfhard Engel, Helmut Pieper, Henri Doods, Gerhard Hallermayer, Michael Entzeroth, Wolfgang Wienen
  • Patent number: 6114390
    Abstract: NPY-antagonistic compounds of the formula ##STR1## Exemplary are: (A) (R)-N-[[4-(Aminocarbonylaminomethyl)phenyl]methyl]-N.sup.2 -bis(4-hydroxyphenyl)acetyl]-argininamide-trifluoracetate;(B) (R)-N-[[4-(Aminocarbonylaminomethyl)phenyl]methyl]-N.sup.2 -[bis(4-chlorphenyl)acetyl]-argininamide-trifluoracetate;(C) (R)-N-[[4-Aminocarbonylaminomethyl)phenyl]methyl]-N.sup.2 -(diphenylacetyl)-argininamide-trifluoracetate;(D) (R)-N.sup.2 -(Diphenylacetyl)-N-[[4-(ethoxycarbonylmethylamino-carbonylaminomethyl)phe nyl]methyl]-argininamide-trifluoroacetate;(E) (R,S)-N.sup.5 -(Aminoiminomethyl)-N.sup.2 -(diphenylacetyl)-N-[(4-hy-droxyphenyl)methyl]-N.sup.5 -methyl-ornithinamide-hydrochloride;(F) (R)-N-[[4-(Aminocarbonylmethyl)phenyl]methyl]-N.sup.2 -(diphenyl-acetyl)-argininamide-diacetate;(G) (R)-N.sup.2 -(Diphenylacetyl)-N-[[4-(ethylaminocarbonylamino-methyl)-phenyl]methyl]-ar gininamide-bis-(trifluoroacetate); and,(H) (R)-N.sup.
    Type: Grant
    Filed: October 14, 1997
    Date of Patent: September 5, 2000
    Assignee: Karl Thomae GmbH
    Inventors: Wolfhard Engel, Wolfgang Eberlein, Klaus Rudolf, Henri Doods, Heike-Andrea Wieland, Klaus-Dieter Willim, Michael Entzeroth, Wolfgang Wienen
  • Patent number: 5864043
    Abstract: The invention relates to benzimidazoles of the formula ##STR1## in which R.sub.1 to R.sub.4 are as defined in claim 1,1 and 3 isomer mixtures thereof and addition salts thereof which have valuable properties.In particular, the novel compounds are angiotensin II antagonists.
    Type: Grant
    Filed: September 23, 1997
    Date of Patent: January 26, 1999
    Assignee: Karl Thomae GmbH
    Inventors: Berthold Narr, Andres Bomhard, Norbert Hauel, Jacques Van Meel, Wolfgang Wienen, Michael Entzeroth
  • Patent number: 5807875
    Abstract: Amino acid derivatives, suitable for the treatment of obesity. The following compound is exemplary of the class: (R,S)-N.sup.2 -(diphenylacetyl)-N-?(4-hydroxyphenyl)methyl!-N.sup.5 -(1H-imidazol-2-yl)-ornithinamide.
    Type: Grant
    Filed: December 11, 1996
    Date of Patent: September 15, 1998
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Klaus Rudolf, Wolfgang Eberlein, Wolfhard Engel, Gerhard Mihm, Henri Doods, Heike Andrea Wieland, Klaus-Dieter Willim, Jurgen Krause, Horst Dollinger, Franz Esser, Gerd Schnorrenberg, Michael Entzeroth, Wolfgang Wienen
  • Patent number: 5684029
    Abstract: The invention relates to benzimidazoles of general formula ##STR1## wherein R.sub.1 to R.sub.4 are as defined herein, the 1-, 3-isomer mixtures thereof and the addition salts thereof. The new compounds are useful, in particular, as angiotensin antagonists.
    Type: Grant
    Filed: February 20, 1996
    Date of Patent: November 4, 1997
    Assignee: Karl Thomae GmbH
    Inventors: Berthold Narr, Norbert Hauel, Jacques Van Meel, Wolfgang Wienen, Michael Entzeroth, Uwe Ries
  • Patent number: 5641772
    Abstract: New condensed diazepinones of general formula I ##STR1## wherein B represents one of the divalent groups ##STR2## and X, l, m, n and R.sup.1 to R.sup.7 are as defined herein, as well as the salts thereof with inorganic or organic acids and processes for preparing them.These compounds are useful for improving or normalising arteriosclerotically induced disorders of cerebral blood flow, for treating diseases of the central nervous system, particularly Alzheimer's disease and Parkinson's disease, and as vagal pacemakers for treating bradycardia and bradyarrhythmia, and also for improving memory performance.
    Type: Grant
    Filed: April 13, 1995
    Date of Patent: June 24, 1997
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Wolfgang Eberlein, Gerhard Mihm, Wolfhard Engel, Klaus Rudolf, Henri Doods, Harald Ziegler, Michael Entzeroth
  • Patent number: 5616620
    Abstract: Amino acid derivatives, suitable for the treatment of obesity. The following compound is exemplary of the class: (R)-N2-(diphenylacetyl)-N-[(4-hydroxyphenyl) methyl]-argininamide-acetate.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: April 1, 1997
    Assignee: Karl Thomae GmbH
    Inventors: Klaus Rudolf, Wolfgang Eberlein, Wolfhard Engel, Gerhard Mihm, Henri Doods, Heike A. Wieland, Klaus-Dieter Willim, Jurgen Krause, Horst Dollinger, Franz Esser, Gerd Schnorrenberg, Michael Entzeroth, Wolfgang Wienen
  • Patent number: 5614519
    Abstract: Angiotensin-II antagonists of the formula ##STR1## wherein R.sub.1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R.sub.2 is, inter alia, optionally substituted benzimidazol-2-yl, 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-yl, butanesultam-1-yl, imidazol-4-yl, and tetrahydobenzimidazol-2-yl; R.sub.3 is, inter alia, lower alkyl; and, R.sub.4 is an acidic group, such as carboxyl or tetrazolyl. An exemplary compound is: 4'-[(2-n-propyl-4-methyl-6-(1-(2-N-morpholinoethyl)-imidazol-4-yl)-benzimi dazol-1-yl)-methyl]-biphenyl-2-carboxylic acid.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: March 25, 1997
    Assignee: Karl Thomae GmbH
    Inventors: Norbert Hauel, Berthold Narr, deceased, Uwe Ries, Jacobus C. Antonius van Meel, Wolfgang Wienen, Michael Entzeroth
  • Patent number: 5610155
    Abstract: New condensed diazepinones of general formula I ##STR1## wherein B represents one of the divalent groups ##STR2## and X, l, m, n and R.sup.1 to R.sup.7 are as defined herein, as well as the salts thereof with inorganic or organic acids and processes for preparing them.These compounds are useful for improving or normalising arteriosclerotically induced disorders of cerebral blood flow, for treating diseases of the central nervous system, particularly Alzheimer's disease and Parkinson's disease, and as vagal pacemakers for treating bradycardia and bradyarrhythmia, and also for improving memory performance.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: March 11, 1997
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Wolfgang Eberlein, Gerhard Mihm, Wolfhard Engel, Klaus Rudolf, Henri Doods, Harald Ziegler, Michael Entzeroth
  • Patent number: 5602127
    Abstract: Angiotensin-II antagonists of the formula ##STR1## wherein R.sub.1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R.sub.2 is, inter alia, optionally substituted benzimidazol-2-yl, 5,6,7,8-tetrahydro-imidazo [1,2-a]pyridin-2-yl, butanesultam-1-yl, imidazol-4-yl, and tetrahydobenzimidazol-2-yl; R.sub.3 is, inter alia, lower alkyl; and, R.sub.4 is an acidic group, such as carboxyl or tetrazolyl. An exemplary compound is: 4'-[(2-n-propyl-4-methyl-6-(butanesultam-1-yl)benzimidazol-1-yl)-methyl]-b iphenyl-2-carboxylic acid.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: February 11, 1997
    Assignee: Karl Thomae GmbH
    Inventors: Norbert Hauel, Berthold Narr, deceased, Uwe Ries, Jacobus C. A. van Meel, Wolfgang Wienen, Michael Entzeroth
  • Patent number: 5594003
    Abstract: Angiotensin-II antagonists of the formula ##STR1## wherein R.sub.1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R.sub.2 is, inter alia, optionally substituted benzimidazol-2-yl, 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-yl, butanesultam-1-yl, imidazol-4-yl, and tetrahydobenzimidazol-2-yl; R.sub.3 is, inter alia, lower alkyl; and, R.sub.4 is an acidic group, such as carboxyl or tetrazolyl. An compound is:4'-[(2-Ethyl-4-methyl-6-(5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-yl)-ben zimidazol-1-yl)-methyl]-biphenyl-2-carboxylic acid.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: January 14, 1997
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Norbert Hauel, Berthold Narr, deceased, Uwe Ries, Jacobus C. A. van Meel, Wolfgang Wienen, Michael Entzeroth
  • Patent number: 5591762
    Abstract: Disclosed herein are angiotensin-II antagonists of the formula ##STR1## wherein R.sub.1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R.sub.2 is, inter alia, optionally substituted benzimidazol-2-yl, 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-yl, butanesultam-1-yl, imidazol-4-yl, and tetrahydobenzimidazol-2-yl; R.sub.3 is, inter alia, lower alkyl; and, R.sub.4 is an acidic group, such as carboxyl or tetrazolyl.An exemplary compound is:(a) 4'-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazole-2-yl)-benzimidazol-1-yl] methyl]-biphenyl-2-carboxylic acid.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: January 7, 1997
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Norbert Hauel, Berthold Narr, deceased, Uwe Ries, Jacobus C. A. van Meel, Wolfgang Wienen, Michael Entzeroth