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).
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Patent number: 7745434Abstract: 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: GrantFiled: October 20, 2005Date of Patent: June 29, 2010Assignee: Merck Patent GmbHInventors: Guenter Hoelzemann, Karl-August Ackermann, Helene Crassier, Alfred Jonczyk, Wilfried Rautenberg, Gema Tarrason, Elisabet Rosell-Vives, Jaume Adan, Claudia Cases
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Patent number: 7547695Abstract: 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: GrantFiled: October 14, 2004Date of Patent: June 16, 2009Assignee: Merck Patent GmbHInventors: Guenter Hoelzemann, Helene Crassier, Karl-August Ackermann, Wolfgang Staehle, Alfred Jonczyk, Wilfried Rautenberg, Francesc Mitjans, Elisabet Rosell-Vives, Jaume Adan, Marta Soler Riera
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Publication number: 20080146560Abstract: 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 tumoursType: ApplicationFiled: October 20, 2005Publication date: June 19, 2008Inventors: Guenter Hoelzemann, Karl-August Ackermann, Helene Grassier, Alfred Jonczyk, Wilfried Rautenberg, Gema Tarrason, Elisabet Rosell-Vives, Jaume Adan, Claudia Cases
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Publication number: 20070099910Abstract: 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: ApplicationFiled: October 14, 2004Publication date: May 3, 2007Applicant: Merck Patent GmbHInventors: Guenter Hoelzemann, Helene Crassier, Karl-August Ackermann, Wolfgang Staehle, Alfred Jonczyk, Wilfried Rautenberg, Francesc Mitjans, Elisabet Rosell-Vives, Jaume Adan, Marta Soler Riera
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Publication number: 20070021456Abstract: 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: ApplicationFiled: July 19, 2004Publication date: January 25, 2007Applicant: MERCK PATENT GMBHInventors: Francesc Mitjans, Elisabet Rosel-Vives, Jaume Adan, Marta Soler, Guenter Hoelzemann, Helene Crassier, Karl-August Ackermann, Wolfgang Staehle, Alfred Jonczyk, Wilfried Rautenberg
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Publication number: 20060264419Abstract: 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: ApplicationFiled: March 8, 2004Publication date: November 23, 2006Inventors: Kai Schiemann, Karl-August Ackermann, Michael Arlt, Dirk Finsinger, Christoph Van Amsterdam, Gerd Bartoszyk, Christoph Seyfried, Oliver Schadt
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Publication number: 20060241301Abstract: 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: ApplicationFiled: July 2, 2004Publication date: October 26, 2006Inventors: Gunter Hoelzemann, Karl-August Ackermann, Wolfgang Staehle, Alfred Jonczyk, Wilfried Rautenberg, Helerie Crassier, Francesc Mitjans, Elisabet Rosell-Vives, Jaume Adan, Marta Soler Riera
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Patent number: 6756370Abstract: 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: GrantFiled: February 21, 2002Date of Patent: June 29, 2004Assignee: Merck Patent GmbHInventors: Helmut Prücher, Henning Böttcher, Karl-August Ackermann, Rudolf Gottschlich, Christoph van Amsterdam, Christoph Seyfried, Jürgen Harting, Gerd Bartoszyk, Hartmut Greiner
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Patent number: 6613778Abstract: 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: GrantFiled: May 3, 2002Date of Patent: September 2, 2003Assignee: Merck Patent Gesellschaft mit beschränkter HaftungInventors: Hanse-Michael Eggenweiler, Karl-August Ackermann, Rochust Jonas, Michael Wolf, Michael Gassen, Thomas Welge
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Publication number: 20030130287Abstract: Compounds of the formula I 1Type: ApplicationFiled: November 5, 2002Publication date: July 10, 2003Inventors: Karl-August Ackermann, Henning Boettcher, Helmut Pruecher, Christoph V. Amsterdam, Christoph Seyfried, Hartmug Greiner, Gerd Bartoszyk, Juergen Harting
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Patent number: 6344566Abstract: 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: GrantFiled: January 26, 2001Date of Patent: February 5, 2002Assignee: Merck Patent GmbHInventors: Andreas Bathe, Bernd Helfert, Karl-August Ackermann, Rudolf Gottschlich, Ingeborg Stein, Jens Budak
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Patent number: 6028080Abstract: 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: GrantFiled: July 17, 1998Date of Patent: February 22, 2000Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Karl-August Ackermann, Rudlof Gottschlich, Gunter Holzemann, Joachim Leibrock, Wilfried Rautenberg, Christoph Seyfried
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Patent number: 5532266Abstract: 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: GrantFiled: May 30, 1995Date of Patent: July 2, 1996Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Rudolf Gottschlich, Karl-August Ackermann, Helmut Prucher, Christoph Seyfried, Hartmut Greiner, Gerd Bartoszyk, Frank Mauler, Manfred Stohrer, Andrew Barber
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Patent number: 5472961Abstract: 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: GrantFiled: March 2, 1995Date of Patent: December 5, 1995Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Rudolf Gottschlich, Karl-August Ackermann, Christoph Seyfried, Andrew Barber, Gerd Bartoszyk, Hartmut Greiner
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Patent number: 5232978Abstract: 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: GrantFiled: November 1, 1991Date of Patent: August 3, 1993Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Rudolf Gottschlich, Karl-August Ackermann, Helmut Prucher, Andrew Barbar, Anton Haase, Hartmut Greiner, Gerd Bartoszyk