Patents by Inventor Karl-August Ackermann

Karl-August Ackermann 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: 7745434
    Abstract: Compounds of the formula (I), in which R6, R7, R8, R9, Het1, X and X? have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be employed, inter alia, for the treatment of tumours.
    Type: Grant
    Filed: October 20, 2005
    Date of Patent: June 29, 2010
    Assignee: Merck Patent GmbH
    Inventors: Guenter Hoelzemann, Karl-August Ackermann, Helene Crassier, Alfred Jonczyk, Wilfried Rautenberg, Gema Tarrason, Elisabet Rosell-Vives, Jaume Adan, Claudia Cases
  • Patent number: 7547695
    Abstract: The invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X and X? have the designations cited in patent claim 1. Said compounds are inhibitors of tyrosine kinases, especially TIE-2, and Raf kinases, and can, inter alia, be used for the treatment of tumors.
    Type: Grant
    Filed: October 14, 2004
    Date of Patent: June 16, 2009
    Assignee: Merck Patent GmbH
    Inventors: Guenter Hoelzemann, Helene Crassier, Karl-August Ackermann, Wolfgang Staehle, Alfred Jonczyk, Wilfried Rautenberg, Francesc Mitjans, Elisabet Rosell-Vives, Jaume Adan, Marta Soler Riera
  • Publication number: 20080146560
    Abstract: Compounds of the formula (I), in which R6, R7, R8, R9, Het1, X and X? have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be employed, inter alia, for the treatment of tumours
    Type: Application
    Filed: October 20, 2005
    Publication date: June 19, 2008
    Inventors: Guenter Hoelzemann, Karl-August Ackermann, Helene Grassier, Alfred Jonczyk, Wilfried Rautenberg, Gema Tarrason, Elisabet Rosell-Vives, Jaume Adan, Claudia Cases
  • Publication number: 20070099910
    Abstract: The invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X and X? have the designations cited in patent claim 1. Said compounds are inhibitors of tyrosine kinases, especially TIE-2, and Raf kinases, and can, inter alia, be used for the treatment of tumours.
    Type: Application
    Filed: October 14, 2004
    Publication date: May 3, 2007
    Applicant: Merck Patent GmbH
    Inventors: Guenter Hoelzemann, Helene Crassier, Karl-August Ackermann, Wolfgang Staehle, Alfred Jonczyk, Wilfried Rautenberg, Francesc Mitjans, Elisabet Rosell-Vives, Jaume Adan, Marta Soler Riera
  • Publication number: 20070021456
    Abstract: Novel compounds of formula (I) are disclosed, where R1, R1?, L, Y, m and p have the meanings given in claim 1, which are inhibitors of tyrosine kinases, in particular, TIE-2 and Raf kinases and can be used for the treatment of tumors.
    Type: Application
    Filed: July 19, 2004
    Publication date: January 25, 2007
    Applicant: MERCK PATENT GMBH
    Inventors: Francesc Mitjans, Elisabet Rosel-Vives, Jaume Adan, Marta Soler, Guenter Hoelzemann, Helene Crassier, Karl-August Ackermann, Wolfgang Staehle, Alfred Jonczyk, Wilfried Rautenberg
  • Publication number: 20060264419
    Abstract: The compounds of the formula (I) and salts and solvates thereof, in which X, R1, R2, R3, R4 and R5 have the meanings indicated in Claim (1), are suitable as ligands of 5 HT receptors.
    Type: Application
    Filed: March 8, 2004
    Publication date: November 23, 2006
    Inventors: Kai Schiemann, Karl-August Ackermann, Michael Arlt, Dirk Finsinger, Christoph Van Amsterdam, Gerd Bartoszyk, Christoph Seyfried, Oliver Schadt
  • Publication number: 20060241301
    Abstract: The invention relates to novel urea derivatives which inhibit tyrosinkinases, especially TIE-2, and Raf kinases and which are used in the treatment of tumors.
    Type: Application
    Filed: July 2, 2004
    Publication date: October 26, 2006
    Inventors: Gunter Hoelzemann, Karl-August Ackermann, Wolfgang Staehle, Alfred Jonczyk, Wilfried Rautenberg, Helerie Crassier, Francesc Mitjans, Elisabet Rosell-Vives, Jaume Adan, Marta Soler Riera
  • Patent number: 6756370
    Abstract: The invention relates to compounds of formula (I), wherein R1, R2 and A have the meanings given in claim 1, are potent 5-HT2A antagonists and are suitable for treating psychoses, schizophrenia, depression, neurological disorders, impaired memory, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, eating disorders such as bulimia and anorexia nervosa, Pre-Menstrual Syndrome and/or for positively influencing obsessive-compulsive disorders, (OCD).
    Type: Grant
    Filed: February 21, 2002
    Date of Patent: June 29, 2004
    Assignee: Merck Patent GmbH
    Inventors: Helmut Prücher, Henning Böttcher, Karl-August Ackermann, Rudolf Gottschlich, Christoph van Amsterdam, Christoph Seyfried, Jürgen Harting, Gerd Bartoszyk, Hartmut Greiner
  • Patent number: 6613778
    Abstract: Compounds of the formula I in which R1 denotes CONR4R5, R2 denotes H or A, R4 and R5, independently of one another, each denote H or A1, R3 denotes Hal, Hal denotes F, Cl, Br or I, A denotes alkyl having 1-4 carbon atoms, A1 denotes alkyl having 1-10 carbon atoms, X denotes alkylene having 1-4 carbon atoms, in which an ethylene group may also be replaced by a double or triple bond, and their physiologically acceptable salts and/or solvates, as phosphodiesterase VII inhibitors, and their use for the preparation of a medicament.
    Type: Grant
    Filed: May 3, 2002
    Date of Patent: September 2, 2003
    Assignee: Merck Patent Gesellschaft mit beschränkter Haftung
    Inventors: Hanse-Michael Eggenweiler, Karl-August Ackermann, Rochust Jonas, Michael Wolf, Michael Gassen, Thomas Welge
  • Publication number: 20030130287
    Abstract: Compounds of the formula I 1
    Type: Application
    Filed: November 5, 2002
    Publication date: July 10, 2003
    Inventors: Karl-August Ackermann, Henning Boettcher, Helmut Pruecher, Christoph V. Amsterdam, Christoph Seyfried, Hartmug Greiner, Gerd Bartoszyk, Juergen Harting
  • Patent number: 6344566
    Abstract: The invention relates to a novel process for the alternative preparation of N-methyl-N-[(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)ethyl]-2,2-diphenylacetamide or N-methyl-N-[(1R)-1-phenyl-2-((3R)-3-hydroxypyrrolidin-1-yl)ethyl]-2,2-diphenylacetamide, and the novel compounds N-methyl-N-[(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)ethane] and N-methyl-N[(1R)-1-phenyl-2-((3R)-3-hydroxypyrrolidin-1-yl) ethane], which are prepared as intermediates.
    Type: Grant
    Filed: January 26, 2001
    Date of Patent: February 5, 2002
    Assignee: Merck Patent GmbH
    Inventors: Andreas Bathe, Bernd Helfert, Karl-August Ackermann, Rudolf Gottschlich, Ingeborg Stein, Jens Budak
  • Patent number: 6028080
    Abstract: The invention relates to quinoline-2-(1H)-one derivatives of the general formula I ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 are in each case independently of one another H, Hal, A or OA; R.sup.4 is H, --(CH.sub.2).sub.m --NR.sup.6 R.sup.7 ; R.sup.5 is H, --(CH.sub.2).sub.n --NR.sup.6 R.sup.7 ; R.sup.6 is H, A or, together with R.sup.7, --(CH.sub.2).sub.4 -- or --(CH.sub.2).sub.5 --; R.sup.7 is H, A or --(CH.sub.2).sub.m -- with a bond to the same ring or adjacent ring B or D or, together with R.sup.6, --(CH.sub.2).sub.4 -- or --(CH.sub.2).sub.5 --; X is --CHR.sup.5 --, --NR.sup.5 --, --O--, --S--; A is alkyl having 1-6 C atoms; Hal is F, Cl, Br or I; m is 1-3 and n is 0-3, where at least one of the two radicals R.sup.4 or R.sup.5 has the meaning --(CH.sub.2).sub.m --NR.sup.6 R.sup.7 or --(CH.sub.2).sub.n --NR.sup.6 R.sup.7, their enantiomers, stereoisomers, salts and solvates. Such compounds are useful for the treatment of neurodegenerative diseases.
    Type: Grant
    Filed: July 17, 1998
    Date of Patent: February 22, 2000
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Karl-August Ackermann, Rudlof Gottschlich, Gunter Holzemann, Joachim Leibrock, Wilfried Rautenberg, Christoph Seyfried
  • Patent number: 5532266
    Abstract: Novel arylacetamides of the formula I ##STR1## in which Q is R.sup.4 --CH(CH.sub.2 Z)--NA--, ##STR2## R.sup.1 is Ar, cycloalkyl with 3-7 C atoms or C.sub.4 -C.sub.8 -cycloalkyl-C.sub.1 -C.sub.7 -alkyl,R.sup.2 is Ar,R.sup.3 is H, OH, OA or A,R.sup.4 is A or phenyl which can optionally be substituted once or twice by F, Cl, Br, I, OH, OA, CF.sub.3, NO.sub.2, NH.sub.2, NHA, NHCOA, NHSO.sub.2 A or NA.sub.2,R.sup.5 and R.sup.6 are each, independently of one another, H, F, Cl, Br, I, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA, NHCONH.sub.2, NO.sub.2 or taken together are methylenedioxy,A is alkyl with 1-7 C atoms, and physiologically acceptable salts thereof.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: July 2, 1996
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Rudolf Gottschlich, Karl-August Ackermann, Helmut Prucher, Christoph Seyfried, Hartmut Greiner, Gerd Bartoszyk, Frank Mauler, Manfred Stohrer, Andrew Barber
  • Patent number: 5472961
    Abstract: Novel acetamides of the formula I ##STR1## in which Q, R, X and Y have the meanings defined herein, have analgesic and neuroprotective properties and bind with high affinity to kappa receptors.
    Type: Grant
    Filed: March 2, 1995
    Date of Patent: December 5, 1995
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Rudolf Gottschlich, Karl-August Ackermann, Christoph Seyfried, Andrew Barber, Gerd Bartoszyk, Hartmut Greiner
  • Patent number: 5232978
    Abstract: Novel 1-(2-arylethyl)-pyrrolidines of the formula ##STR1## in which, Ar is a phenyl group which is unsubstituted or monosubstituted by OH, --O--CO--NH.sub.2, --O--CO--NHA, --O--CO--NA.sub.2, NH.sub.2, --NH--CHO, --NH--CO--A, --NH--CO--NH.sub.2, --NH--CO--NHA or NH--SO.sub.2 --A,R.sup.1 is A,R.sup.2 is a phenyl, naphthyl, thienyl, benzothienyl or pyridyl group which is unsubstituted or mono- or disubstituted by A, Hal, CF.sub.3, OH, OA, --O--CO--NH.sub.2, --O--CO--NHA, --O--CO--NA.sub.2, NO.sub.2, NH.sub.2, --NH--CHO, --NH--CO--A, --NH--CO--NH.sub.2, --NH--CO--NHA, --NH--SO.sub.2 A, --CO--A, --CONH.sub.2, --CONHA, --CONA.sub.2, --CH.sub.2 --CONH.sub.2 and/or --O--CH.sub.2 --CONH.sub.2,R.sup.3 is OH or CH.sub.2 OH,A is alkyl with 1-4 C atoms andHal is F, Cl, Br or I,or a pharmaceutically acceptable salt thereof for use as an analgesic in humans and veterinary medicine.
    Type: Grant
    Filed: November 1, 1991
    Date of Patent: August 3, 1993
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Rudolf Gottschlich, Karl-August Ackermann, Helmut Prucher, Andrew Barbar, Anton Haase, Hartmut Greiner, Gerd Bartoszyk