Patents by Inventor Werner Tueckmantel
Werner Tueckmantel 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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Publication number: 20230140635Abstract: A compound of Formula I, which possesses 5-HT2A and/or 5-HT2C selective receptor activity, but lacks at lease some of the undesirable characteristics of 5-HT2B-agonist related activities, is disclosed. Methods of preparing said compounds are also described. The compound of Formula I may be useful in the treatment of depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headache, PTSD, seizure disorders and other CNS disorders.Type: ApplicationFiled: March 12, 2021Publication date: May 4, 2023Inventors: Alan Kozikowski, Gideon Shapiro, Werner Tueckmantel, John McCorvy
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Patent number: 8653278Abstract: One aspect of the invention relates to isoform-selective HDAC inhibitors. Also provided are methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy. The invention also provides methods for treating cancer, methods for treating neurological diseases and methods for treating malaria. Additionally, the invention provides pharmaceutical compositions comprising an HDAC inhibitor of the invention; and kits comprising an HDAC inhibitor of the invention.Type: GrantFiled: August 2, 2007Date of Patent: February 18, 2014Assignees: Georgetown University, The Board of Trustees of the University of IllinoisInventors: Alan P. Kozikowski, Mira Jung, Anatoly Dritschilo, Arsen Gaysin, Pavel A. Petukhov, Werner Tueckmantel, Hongbin Yuan, Yufeng Chen
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Publication number: 20130184313Abstract: The invention relates to pyridinyl nicotinic acetylcholine receptor ligands, compositions comprising an effective amount of a pyridinyl nicotinic acetylcholine receptor ligand and methods to treat or prevent a condition, such as depression and nicotine dependence, comprising administering to an animal in need thereof an effective amount of a pyridinyl nicotinic acetylcholine receptor ligand.Type: ApplicationFiled: March 7, 2013Publication date: July 18, 2013Applicants: The Board of Trustees of the University of Illinois, PsychoGenics, Inc.Inventors: Jayaraman Chandrasekhar, Alan P. Kozikowski, Jianhua Liu, Werner Tueckmantel, Joel R. Walker, Po-wai Yuen
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Patent number: 8445684Abstract: The invention relates to pyridinyl nicotinic acetylcholine receptor ligands, compositions comprising an effective amount of a pyridinyl nicotinic acetylcholine receptor ligand and methods to treat or prevent a condition, such as depression and nicotine dependence, comprising administering to an animal in need thereof an effective amount of a pyridinyl nicotinic acetylcholine receptor ligand.Type: GrantFiled: October 13, 2009Date of Patent: May 21, 2013Assignees: PsycoGenics Inc., The Board of Trustee of the University of ILInventors: Jayaraman Chandrasekhar, Alan P. Kozikowski, Jianhua Liu, Werner Tueckmantel, Joel R. Walker, Po-wai Yuen
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Publication number: 20100196502Abstract: One aspect of the invention relates to isoform-selective HDAC inhibitors. Also provided are methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy. The invention also provides methods for treating cancer, methods for treating neurological diseases and methods for treating malaria. Additionally, the invention provides pharmaceutical compositions comprising an HDAC inhibitor of the invention; and kits comprising a an HDAC inhibitor of the invention.Type: ApplicationFiled: August 2, 2007Publication date: August 5, 2010Applicant: Georgetown UniversityInventors: Alan P. Kozikowski, Mira Jung, Anatoly Dritschilo, Arsen Gaysin, Pavel A. Petukhov, Werner Tueckmantel, Hongbin Yuan
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Publication number: 20100152450Abstract: The invention relates to pyridinyl nicotinic acetylcholine receptor ligands, compositions comprising an effective amount of a pyridinyl nicotinic acetylcholine receptor ligand and methods to treat or prevent a condition, such as depression and nicotine dependence, comprising administering to an animal in need thereof an effective amount of a pyridinyl nicotinic acetylcholine receptor ligand.Type: ApplicationFiled: October 13, 2009Publication date: June 17, 2010Applicants: PSYCHOGENICS, INC., The Board of Trustees of the University of IllinoisInventors: Jayaraman Chandrasekhar, Alan P. Kozikowski, Jianhua Liu, Werner Tueckmantel, Joel R. Walker, Po-wai Yuen
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Publication number: 20100048606Abstract: The present invention relates to substituted cytisine compounds that are useful in treating diseases impacted by a nicotinic ACh receptor. One aspect of the invention relates to 10-substituted cytisine compounds. In certain instances, the cytisine is substituted in the 10-position by an alkyl, aryl or aralkyl group. The present invention also relates to a pharmaceutical composition comprises the substituted cytisine compound or the 10-substituted cytisine compound. The invention also relates to a method of modulation a nicotinic ACh receptor in a mammal, comprising the step of administering to a mammal in need thereof a therapeutically effective amount of a substituted cytisine. In certain instances, the substituted cytisine is a 10-substituted cytisine. Another aspect of the present invention relates a method of treating a disease impacted by a nicotinic ACh receptor, comprising the step of administering to a mammal in need thereof a therapeutically effective amount of a substituted cytisine.Type: ApplicationFiled: March 29, 2007Publication date: February 25, 2010Applicant: Georgetown University Office of Technology CommercializationInventors: Alan P. Kozikowski, Werner Tueckmantel, Sheela Chellappan, Kenneth J. Kellar, Yingxian Xiao
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Patent number: 7507831Abstract: Various processes are disclosed for preparing protected epicatechin oligomers having (4?,8)-interflavan linkages. In one process, a tetra-O-protected epicatechin monomer or oligomer is coupled with a protected, C-4 activated epicatechin monomer in the presence of an acidic clay such as a mortmorillonite clay. In another process, a 5,7,3?,4?-benzyl protected or a 3 -acetyl-, 5,7,3?,4?-benzyl protected epicatechin or catechin monomer or oligomer is reacted with 3 -O-acetyl-4-[(2-benzothiazolyl)thio]-5,7,3?,4?-tetra-O-benzylepicatechin in the presence of silver tetrafluoroborate. In another process, two 5,7,3?,4?-benzyl protected epicatechin monomers activated with 2-(benzothiazolyl)thio groups at the C-4 positions are cross-coupled in the presence of silver tetrofluoroborate. A process is also disclosed for reacting an unprotected epicatechin or catechin monomer with 4-(benzylthio) epicatechin or catechin.Type: GrantFiled: January 11, 2006Date of Patent: March 24, 2009Inventors: Alan P. Kozikowski, Werner Tückmantel, Leo J. Romanczyk, Jr.
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Patent number: 7268240Abstract: A process is disclosed for the production of polyphenol oligomers having n polyphenol monomeric units, n being an integer from 2-18. The process includes coupling of a protected polyphenol, having protected phenolic hydroxyl groups, with a C-4 functionalized polyphenol monomer. The protected polyphenol may be a protected polyphenol monomer or a protected polyphenol oligomer having 2-17 monomeric units. Advantageously, polyphenol monomeric units forming the polyphenol oligomers may be the same or different flavanoid compounds.Type: GrantFiled: May 28, 2004Date of Patent: September 11, 2007Inventors: Leo J. Romanczyk, Jr., Alan P. Kozikowski, Werner Tueckmantel, Marc E. Lippman
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Patent number: 7244855Abstract: Various processes are disclosed for preparing procyanidin oligomers having (4,8)-interflavan linkages. In an improved process, a tetra-O-protected-epicatechin or -catechin monomer or oligomer is coupled with a protected, C-4 alkoxy-activated-epicatechin or -catechin monomer in the presence of an acidic clay instead of a Lewis acid. In a second process, a 5,7,3?,4?-tetra-O-protected or preferably penta-O-protected-epicatechin or -catechin monomer or oligomer is reacted with a tetra-O-protected or preferably penta-O-protected-epicatechin or -catechin monomer having a thio activating group at the C-4 position; the coupling is carried out in the presence of silver tetrafluoroborate. In third process, two molecules of a penta-O-protected-epicatechin or -catechin monomer activated with a 2-(benzothiazolyl)thio group at the C-4 position are self-condensed in the presence of silver tetrafluoroborate.Type: GrantFiled: October 2, 2003Date of Patent: July 17, 2007Inventors: Alan P. Kozikowski, Werner Tückmantel, Leo J. Romanczyk, Jr., Xingquan Ma
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Patent number: 7126014Abstract: Oligomeric procyanidins containing 4?-linked epicatechin units are rare in nature and have hitherto not been accessible through stereoselective synthesis. Provided herein is the preparation of the prototypical dimer, epicatechin-4?,8-epicatechin, by reaction of the protected 4-ketones with aryllithium reagents derived by halogen/metal exchange from the aryl bromides. Removal of the 4-hydroxyl group from the resulting tertiary benzylic alcohols is effected by tri-n-butyltin hydride and trifluoroacetic acid in a completely stereoselective manner, resulting in hydride delivery exclusively from the ? face.Type: GrantFiled: February 20, 2004Date of Patent: October 24, 2006Inventors: Alan P. Kozikowski, Leo J. Romanczyk, Jr., Werner Tückmantel
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Patent number: 7067679Abstract: Various processes are disclosed for preparing protected epicatechin oligomers having (4?,8)-interflavan linkages. In one process, a tetra-O-protected epicatechin monomer or oligomer is coupled with a protected, C-4 activated epicatechin monomer in the presence of an acidic clay such as a mortmorillonite clay. In another process, a 5,7,3?,4?-benzyl protected or a 3-acetyl-, 5,7,3?,4?-benzyl protected epicatechin or catechin monomer or oligomer is reacted with 3-O-acetyl-4-[(2-benzothiazolyl)thio]-5,7,3?,4?-tetra-O-benzylepicatechin in the presence of silver tetrafluoroborate. In another process, two 5,7,3?,4?-benzyl protected epicatechin monomers activated with 2-(benzothiazolyl)thio groups at the C-4 positions are cross-coupled in the presence of silver tetrofluoroborate. A process is also disclosed for reacting an unprotected epicatechin or catechin monomer with 4-(benzylthio)epicatechin or catechin.Type: GrantFiled: September 9, 2003Date of Patent: June 27, 2006Inventors: Alan P. Kozikowski, Werner Tückmantel, Leo J. Romanczyk, Jr.
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Patent number: 6849746Abstract: A process is disclosed for the production of polyphenol oligomers having n polyphenol monomeric units, n being an integer from 2-18. The process includes coupling of a protected polyphenol, having protected phenolic hydroxyl groups, with a C-4 functionalized polyphenol monomer. The protected polyphenol may be a protected polyphenol monomer or a protected polyphenol oligomer having 2-17 monomeric units. Advantageously, polyphenol monomeric units forming the polyphenol oligomers may be the same or different flavanoid compounds.Type: GrantFiled: January 31, 2003Date of Patent: February 1, 2005Assignee: Mars, Inc.Inventors: Leo J. Romanczyk, Jr., Alan P. Kozikowski, Werner Tueckmantel, Marc E. Lippman
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Patent number: 6825211Abstract: The present invention provides bicyclic metabotropic glutamate receptor ligands, as well as compositions comprising such ligands, and methods for their use.Type: GrantFiled: August 20, 2003Date of Patent: November 30, 2004Assignee: Georgetown UniversityInventors: Alan P. Kozikowski, Darryl Hugh Steensma, Werner Tueckmantel, Gian Luca Araldi
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Publication number: 20040236123Abstract: A process is disclosed for the production of polyphenol oligomers having n polyphenol monomeric units, n being an integer from 2-18. The process includes coupling of a protected polyphenol, having protected phenolic hydroxyl groups, with a C-4 functionalized polyphenol monomer. The protected polyphenol may be a protected polyphenol monomer or a protected polyphenol oligomer having 2-17 monomeric units. Advantageously, polyphenol monomeric units forming the polyphenol oligomers may be the same or different flavanoid compounds.Type: ApplicationFiled: May 28, 2004Publication date: November 25, 2004Applicant: M&M/Mars Inc.Inventors: Leo J. Romanczyk, Alan P. Kozikowski, Werner Tueckmantel, Marc E. Lippman
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Patent number: 6720432Abstract: Oligomeric procyanidins containing 4&agr;-linked epicatechin units are rare in nature and have hitherto not been accessible through stereoselective synthesis. Provided herein is the preparation of the prototypical dimer, epicatechin-4&agr;,8-epicatechin, by reaction of the protected 4-ketones with aryllithium reagents derived by halogen/metal exchange from the aryl bromides. Removal of the 4-hydroxyl group from the resulting tertiary benzylic alcohols is effected by tri-n-butyltin hydride and trifluoroacetic acid in a completely stereoselective manner, resulting in hydride delivery exclusively from the &bgr; face.Type: GrantFiled: August 8, 2002Date of Patent: April 13, 2004Assignee: Mars IncorporatedInventors: Alan P. Kozikowski, Leo J. Romanczyk Jr., Werner Tückmantel
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Publication number: 20030176620Abstract: A process is disclosed for the production of polyphenol oligomers having n polyphenol monomeric units, n being an integer from 2-18. The process includes coupling of a protected polyphenol, having protected phenolic hydroxyl groups, with a C-4 functionalized polyphenol monomer. The protected polyphenol may be a protected polyphenol monomer or a protected polyphenol oligomer having 2-17 monomeric units. Advantageously, polyphenol monomeric units forming the polyphenol oligomers may be the same or different flavanoid compounds.Type: ApplicationFiled: January 31, 2003Publication date: September 18, 2003Applicant: Mars IncorporatedInventors: Leo J. Romanczyk, Alan P. Kozikowski, Werner Tueckmantel, Marc E. Lippman
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Patent number: 6610743Abstract: The present invention provides bicyclic metabotropic glutamate receptor ligands, as well as compositions comprising such ligands, and and methods for their use.Type: GrantFiled: March 6, 2002Date of Patent: August 26, 2003Assignee: Georgetown UniversityInventors: Alan P. Kozikowski, Darryl Hugh Steensma, Werner Tueckmantel, Gian Luca Araldi
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Patent number: 6528664Abstract: A process is disclosed for the production of polyphenol oligomers having n polyphenol monomeric units, n being an integer from 2-18. The process includes coupling of a protected polyphenol, having protected phenolic hydroxyl groups, with a C-4 functionalized polyphenol monomer. The protected polyphenol may be a protected polyphenol monomer or a protected polyphenol oligomer having 2-17 monomeric units. Advantageously, polyphenol monomeric units forming the polyphenol oligomers may be the same or different flavanoid compounds.Type: GrantFiled: December 14, 2001Date of Patent: March 4, 2003Assignee: Mars, IncorporatedInventors: Leo J. Romanczyk, Jr., Alan P. Kozikowski, Werner Tueckmantel, Marc E. Lippman
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Publication number: 20020165200Abstract: The present invention provides bicyclic metabotropic glutamate receptor ligands, as well as compositions comprising such ligands, and and methods for their use.Type: ApplicationFiled: March 6, 2002Publication date: November 7, 2002Inventors: Alan P. Kozikowski, Darryl Hugh Steensma, Werner Tueckmantel, Gian Luca Araldi