Patents by Inventor Heinz-Hermann Bokel

Heinz-Hermann Bokel 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: 9308205
    Abstract: The present invention relates to 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride solvates and crystalline modifications thereof. The present invention further relates to processes of manufacturing these crystalline modifications as well as their use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, e.g. pathophysiological conditions such as cancer.
    Type: Grant
    Filed: January 29, 2015
    Date of Patent: April 12, 2016
    Assignee: MERCK PATENT GMBH
    Inventors: Axel Becker, Clemens Kuehn, Christoph Saal, Oliver Schadt, Dieter Dorsch, Heinz-Hermann Bokel, Frank Stieber, Cristina Donini
  • Patent number: 9289427
    Abstract: The present invention relates to 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride solvates and crystalline modifications thereof. The present invention further relates to processes of manufacturing these crystalline modifications as well as their use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, e.g. pathophysiological conditions such as cancer.
    Type: Grant
    Filed: January 17, 2014
    Date of Patent: March 22, 2016
    Assignee: MERCK PATENT GMBH
    Inventors: Axel Becker, Clemens Kuehn, Christoph Saal, Oliver Schadt, Dieter Dorsch, Heinz-Hermann Bokel, Frank Stieber, Cristina Donini
  • Publication number: 20150148351
    Abstract: The present invention relates to 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride solvates and crystalline modifications thereof. The present invention further relates to processes of manufacturing these crystalline modifications as well as their use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, e.g. pathophysiological conditions such as cancer.
    Type: Application
    Filed: January 29, 2015
    Publication date: May 28, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Axel BECKER, Clemens KUEHN, Christoph SAAL, Oliver SCHADT, Dieter DORSCH, Heinz-Hermann BOKEL, Frank STIEBER, Cristina DONINI
  • Publication number: 20140200221
    Abstract: The present invention relates to 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride solvates and crystalline modifications thereof. The present invention further relates to processes of manufacturing these crystalline modifications as well as their use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, e.g. pathophysiological conditions such as cancer.
    Type: Application
    Filed: January 17, 2014
    Publication date: July 17, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Axel BECKER, Clemens KUEHN, Christoph SAAL, Oliver SCHADT, Dieter DORSCH, Heinz-Hermann BOKEL, Frank STIEBER, Cristina DONINI
  • Patent number: 8710058
    Abstract: Compounds of the present invention concern 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride solvates and crystalline modifications thereof. The compound, 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile, has the following structural formula: The hydrochloride solvates and crystalline modifications thereof according to the invention are useful for treatment of physiological and/or pathophysiological conditions, such as cancer, that are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, especially Met-kinase. The present invention further relates to processes of manufacturing these crystalline modifications.
    Type: Grant
    Filed: December 4, 2009
    Date of Patent: April 29, 2014
    Assignee: MERCK PATENT GmbH
    Inventors: Axel Becker, Clemens Kuehn, Christoph Saal, Oliver Schadt, Dieter Dorsch, Heinz Hermann Bokel, Frank Stieber, Cristina Donini
  • Publication number: 20110269767
    Abstract: The present invention relates to 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride solvates and crystalline modifications thereof. The present invention further relates to processes of manufacturing these crystalline modifications as well as their use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, e.g. pathophysiological conditions such as cancer.
    Type: Application
    Filed: December 4, 2009
    Publication date: November 3, 2011
    Applicant: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Axel Becker, Clemens Kuehn, Christoph Saal, Oliver Schadt, Dieter Dorsch, Heinz Hermann Bokel, Frank Stieber, Cristina Donini
  • Patent number: 7528256
    Abstract: The invention relates to a process for the preparation of nicotinaldehydes by reduction of the corresponding nicotinic acid morpholinamides.
    Type: Grant
    Filed: March 27, 2004
    Date of Patent: May 5, 2009
    Assignee: Merck Patent GmbH
    Inventors: Heinz-Hermann Bokel, Mike Brandner, Ludwig Gantzert, Ralf Knierieme
  • Publication number: 20060199965
    Abstract: The invention relates to a process for the preparation of nicotinaldehydes by reduction of the corresponding nicotinic acid morpholinamides.
    Type: Application
    Filed: March 27, 2004
    Publication date: September 7, 2006
    Inventors: Heinz-Hermann Bokel, Mike Brandner, Ludwig Gantzert, Ralf Knierieme
  • Patent number: 7045629
    Abstract: The present invention relates to a process for the preparation of 2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]chroman, the enantiomers and its salts, characterised in that 5-(4-fluorophenyl)pyridine-3-carbaldehyde is reacted directly with aminomethylchroman or its salts under reducing conditions to give 2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]chroman, and the latter is, if desired, converted into one of its physiologically acceptable salts by treatment with an acid.
    Type: Grant
    Filed: April 8, 2002
    Date of Patent: May 16, 2006
    Assignee: Merck Patent GmbH
    Inventors: Heinz-Hermann Bokel, Steffen Neuenfeld, Ludwig Gantzert, Ralf Knierieme, Elke Simon, Ralf Devant, Udo Helm, Helmut Reubold
  • Publication number: 20040235920
    Abstract: Substituted aminomethyl chromans, one of their optical isomers or pharmaceutically acceptable salts, used for the manufacture of a medicament for the treatment of adverse effects of anti-Parkinsonian drugs in extrapyramidal movement disorders and/or for the manufacture of a medicament for the treatment of extrapyramidal symptoms (EPS) induced by neuroleptics. A preferred compound is (−)-(R)-2-{4-[[3,4-dihydro-2H-benzopyran-2-yl)-methyl!amino!butyl}-1,2-benzoisothiazol-3-(2H)-on-1,1-dioxide or a physiologically acceptable salt thereof.
    Type: Application
    Filed: March 11, 2004
    Publication date: November 25, 2004
    Inventors: Gerd Bartoszyk, Henning Bottcher, Christoph Seyfried, Hermann Russ, Heinz-Hermann Bokel, Uschi Schmid-Grobmann
  • Patent number: 6812353
    Abstract: Chromanone derivatives of the formula I in which R1 to R4 are each, independently of one another, H, A, CN, Hal, OR5, COOR5, CF3, OCF3, NO2, Ar, OAr, N(R5)2 or CON(R5)2, R5 is H or A, A is alkyl having 1 to 6 carbon atoms, Ar is phenyl which is unsubstituted or substituted by A, OR5, CN, Hal, CF3, OCF3, NO2 or N(R5)2, Hal is F, Cl, Br or I, and their salts, are suitable as intermediates in the synthesis of medicaments.
    Type: Grant
    Filed: July 29, 2003
    Date of Patent: November 2, 2004
    Assignee: Merck Patent Gesellschaft mit beschränkter Haftung
    Inventors: Heinz-Hermann Bokel, Christoph Muermann, Uschi Schmid-Grossmann
  • Publication number: 20040138266
    Abstract: The present invention relates to a process for the preparation of 2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]chroman, the enantiomers and its salts, characterised in that 5-(4-fluorophenyl)pyridine-3-carbaldehyde is reacted directly with aminomethylchroman or its salts under reducing conditions to give 2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]chroman, and the latter is, if desired, converted into one of its physiologically acceptable salts by treatment with an acid.
    Type: Application
    Filed: October 27, 2003
    Publication date: July 15, 2004
    Inventors: Heinz-Hermann Bokel, Steffen Neuenfeld, Ludwig Gantzert, Ralf Knierieme, Elke Simon, Ralf Devant, Udo Helm, Helmut Reubold
  • Publication number: 20040092579
    Abstract: Chromanone derivatives of the formula I 1
    Type: Application
    Filed: July 29, 2003
    Publication date: May 13, 2004
    Inventors: Heinz-Hermann Bokel, Christoph Muermann, Uschi Schmid
  • Patent number: 5518588
    Abstract: The present invention relates to a method for preparing 3-aminopyridines from 3-nitropyridines, in which the nitropyridines are reduced electrochemically in acidic solution.
    Type: Grant
    Filed: September 30, 1994
    Date of Patent: May 21, 1996
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Ulrich Fechtel, Karlheinz Wembacher, Heinz-Hermann Bokel
  • Patent number: 5321137
    Abstract: The invention relates to a novel process for the preparation of imidazopyridines of formula I: ##STR1## in which R is an alkyl having 1-6 C atoms, characterized in that 3,4-diamino-2-chloropyridine (II) is reacted with an acid anhydride of the formula RCO--O--COR 40 (III), in which R is as defined and R' is R or can be another aliphatic or aromatic radical, to give a 4-amino-2-chloro-3-R-CO-aminopyridine (IV), this is converted with 4'-bromomethyl-2-cyanobiphenyl (V), in the presence of an alkali metal alcoholate in an inert solvent, to a 4-amino-2-chloro-3-R-CO-[N-(2'-cyano-biphenyl-4-ylmethyl)-amino]pyridine (VI) and this is treated with a strong acid, a 2-R-4-chloro-3-(2'-cyano-biphenyl-4-ylmethyl)-3H-imidazo[4,5-c]pyridine (VII) being formed as an intermediate.
    Type: Grant
    Filed: August 4, 1993
    Date of Patent: June 14, 1994
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Werner Mederski, Heinz-Hermann Bokel
  • Patent number: 4762933
    Abstract: New 1-oxa-2-oxo-3-R-3-aza- 5-Z-cyclopentane derivatives, whereinR is alkyl or hydroxyalkyl having in each case 1-6 C atoms, cycloalkyl having 3-8 C atoms, unsubstituted aryl or aralkyl or aryl or aralkyl each of which has a total of 6-15 C atoms and, in the aryl radical, is monosubstituted to trisubstituted by alkyl, alkoxy, OH and/or Cl or monosubstituted by methylenedioxy,Z is --(CHOH).sub.n --H andn is 2, 3, 4 or 5,can be used as intermediate products for the preparation of active compounds for medicaments, such as toloxatone.
    Type: Grant
    Filed: July 17, 1986
    Date of Patent: August 9, 1988
    Inventor: Heinz-Hermann Bokel