Patents by Inventor Theodros Asberom
Theodros Asberom 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: 9181236Abstract: In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein each of the variables shown in the formula are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including Alzheimer's disease, are also disclosed.Type: GrantFiled: August 21, 2012Date of Patent: November 10, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Wen-Lian Wu, Duane A. Burnett, Andrew W. Stamford, Jared N. Cumming, Theodros Asberom, Chad Bennett, Thavalakulamgara K. Sasiskumar, Jack D. Scott
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Publication number: 20140200213Abstract: In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein each of the variables shown in the formula are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including Alzheimer's disease, are also disclosed.Type: ApplicationFiled: August 21, 2012Publication date: July 17, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Wen-Lian Wu, Duane A. Burnett, Andrew W. Stamford, Jared N. Cumming, Theodros Asberom, Chad Bennett, Thavalakulamgara K. Sasiskumar, Jack D. Scott
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Patent number: 8759337Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (Chemical formula should be inserted here as it appears on abstract in paper form). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).Type: GrantFiled: December 18, 2009Date of Patent: June 24, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Theodros Asberom, Xianhai Huang, Zhaoning Zhu, John W. Clader, Dmitri A. Pissarnitski, Hubert B. Josien, Hongmei Li
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Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors
Patent number: 8618123Abstract: Disclosed are novel gamma secretase inhibitors of the formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, wherein L1, n, X, Ar, Y, Z, Q, and Q1 are as defined herein. Also disclosed are methods for inhibiting gamma secretase, methods for treating Alzheimer's disease, methods of treating one or more neurodegenerative diseases, and methods of inhibiting the deposition of amyloid protein (e.g., amyloid beta protein) in, on or around neurological tissue (e.g., the brain) using the compounds of formula 1.0.Type: GrantFiled: July 15, 2008Date of Patent: December 31, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Thavalakulamgara K. Sasikumar, Duane A. Burnett, Theodros Asberom, Wen-Lian Wu, Hongmei Li, Ruo Xu, Hubert B. Josien -
Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors
Patent number: 8569521Abstract: This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.Type: GrantFiled: October 6, 2011Date of Patent: October 29, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Theodros Asberom, Thomas A. Bara, Chad E. Bennett, Duane A. Burnett, Mary Anne Caplen, John W. Clader, David J. Cole, Martin S. Domalski, Hubert B. Josien, Chad E. Knutson, Hongmei Li, Mark D. McBriar, Dmitri A. Pissarnitski, Li Qiang, Murali Rajagopalan, Thavalakulamgara K. Sasikumar, Jing Su, Haiqun Tang, Wen-Lian Wu, Ruo Xu, Zhiqiang Zhao -
Patent number: 8487099Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).Type: GrantFiled: November 3, 2008Date of Patent: July 16, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: William J. Greenlee, Zhaoning Zhu, Theodros Asberom, Xianhai Huang, Hubert B. Josien
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Patent number: 8357682Abstract: The present invention provides a novel class of heterocyclic compounds of Formula (I) as modulators of gamma secretase, wherein the definitions of the variables of Formula (I) are defined herein, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: GrantFiled: May 5, 2008Date of Patent: January 22, 2013Inventors: Zhaoning Zhu, William J. Greenlee, Zhong-Yue Sun, Gioconda Gallo, Theodros Asberom, Xianhai Huang, Xiaohong Zhu, Mark D. McBriar, Dmitri A. Pissarnitski, Zhiqiang Zhao, Ruo Xu, Hongmei Li, Anandan Palani, Johannes H. Voigt, Robert D. Mazzola, Jr., John Clader, Hubert Josien, Jun Qin
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BENZENESULFONYL-CHROMANE, THIOCHROMANE, TETRAHYDRONAPHTHALENE AND RELATED GAMMA SECRETASE INHIBITORS
Publication number: 20120264736Abstract: This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.Type: ApplicationFiled: October 6, 2011Publication date: October 18, 2012Applicant: Schering CorporationInventors: Theodros Asberom, Thomas A. Bara, Chad E. Bennett, Duane A. Burnett, Mary Ann Caplen, John W. Clader, David J. Cole, Martin S. Domalski, Hubert B. Josien, Chad E. Knutson, Hongmei Li, Mark D. McBriar, Dmitri A. Pissarnitski, Li Qiang, Murali Rajagopalan, Thavalakulamgara K. Sasikumar, Jing Su, Haiqun Tang, Wen-Lian Wu, Ruo Xu, Zhiqiang Zhao -
Publication number: 20120135980Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (Chemical formula should be inserted here as it appears on abstract in paper form). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).Type: ApplicationFiled: December 18, 2009Publication date: May 31, 2012Inventors: Theodros Asberom, Zhaoning Zhu, John W. Clader, Zhong-Yue Sun, Mihirbaran Mandal, Gioconda Gallo, Xiaoxiang Liu
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Publication number: 20120107328Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).Type: ApplicationFiled: November 3, 2008Publication date: May 3, 2012Inventors: William J. Greenlee, Zhaoning Zhu, Theodros Asberom, Xianhai Huang, Hubert B. Josien
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Publication number: 20110294784Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (Chemical formula should be inserted here as it appears on abstract in paper form). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).Type: ApplicationFiled: December 18, 2009Publication date: December 1, 2011Inventors: Theodros Asberom, Xianhai Huang, Zhaoning Zhu, John Clader, Dmitri Pissarnitski, Hubert Josien, Hongmei Li
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Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors
Patent number: 8067621Abstract: This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substitutents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.Type: GrantFiled: January 18, 2007Date of Patent: November 29, 2011Assignee: Schering CorporationInventors: Theodros Asberom, Thomas A. Bara, Chad E. Bennett, Duane A. Burnett, Mary Ann Caplen, John W. Clader, David J. Cole, Martin S. Domalski, Hubert B. Josien, Chad E. Knutson, Hongmei Li, Mark D. McBriar, Dmitri A. Pissarnitski, Li Qiang, Murali Rajagopalan, Thavalakulamgara K. Sasikumar, Jing Su, Haiqun Tang, Wen-Lian Wu, Ruo Xu, Zhiqiang Zhao -
Publication number: 20110257156Abstract: In its many embodiments, the present invention provides novel heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: ApplicationFiled: November 5, 2009Publication date: October 20, 2011Inventors: Zhaoning Zhu, William J. Greenlee, David James Cole, Dmitri A. Pissarnitski, Gioconda V. Gallo, Hongmei Li, Hubert B. Josien, Jun Qin, Chad E. Knutson, Mihirbaran Mandal, Monica L. Vicarel, Murali Rajagopalan, Pawan Kumar Dhondi, Ruo Xu, Zhong-Yue Sun, Thomas A. Bara, Xianhai Huang, Xiaohong Zhu, Zhiqiang Zhao, John W. Clader, Anandan Palani, Theodros Asberom, Troy McCracken, Chad E. Bennett
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BENZENESULFONYL-CHROMANE, THIOCHROMANE, TETRAHYDRONAPHTHALENE AND RELATED GAMMA SECRETASE INHIBITORS
Publication number: 20110110948Abstract: Disclosed are novel gamma secretase inhibitors of the formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, wherein L1, n, X, Ar, Y, Z, Q, and Q1 are as defined herein. Also disclosed are methods for inhibiting gamma secretase, methods for treating Alzheimer's disease, methods of treating one or more neurodegenerative diseases, and methods of inhibiting the deposition of amyloid protein (e.g., amyloid beta protein) in, on or around neurological tissue (e.g., the brain) using the compounds of formula 1.0.Type: ApplicationFiled: July 15, 2008Publication date: May 12, 2011Applicant: SCHERING CORPORATIONInventors: Thavalakulamgara K. Sasikumar, Duane A. Burnett, Theodros Asberom, Wen-Lian Wu, Hongmei Li, Ruo Xu, Hubert B. Josien -
Publication number: 20100247514Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: ApplicationFiled: May 5, 2008Publication date: September 30, 2010Inventors: Zhaoning Zhu, William J. Greenlee, Zhong-Yue Sun, Gioconda Gallo, Theodros Asberom, Xianhai Huang, Xiaohong Zhu, Mark D. McBriar, Dmitri A. Pissarnitski, Zhiqiang Zhao, Ruo Xu, Hongmei Li, Anandan Palani, Johannes H. Voigt, Robert D. Mazzola, JR., John Clader, Hubert Josien, Jun Qin
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Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors
Publication number: 20070197581Abstract: This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substitutents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.Type: ApplicationFiled: January 18, 2007Publication date: August 23, 2007Inventors: Theodros Asberom, Thomas Bara, Chad Bennett, Duane Burnett, Mary Ann Caplen, John Clader, David Cole, Martin Domalski, Hubert Josien, Chad Knutson, Hongmei Li, Mark McBriar, Dmitri Pissarnitski, Li Qiang, Murali Rajagopalan, Thavalakulamgara Sasikumar, Jing Su, Haiqun Tang, Wen-Lian Wu, Ruo Xu, Zhiqiang Zhao -
Patent number: 7256186Abstract: This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —XC(O)Y, alkylene-XC(O)Y, cycloalkylene-X—C(O)—Y, —CH—X—C(O)—NR3—Y or —CH—X—C(O)—Y, wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.Type: GrantFiled: September 15, 2004Date of Patent: August 14, 2007Assignee: Schering CorporationInventors: Dimitri A. Pissarntiski, Hubert B. Josien, Elizabeth M. Smith, John W. Clader, Theodros Asberom, Tao Guo, Douglas W. Hobbs
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Patent number: 7208602Abstract: This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —X(CO)Y, or alkylene-X(CO)Y wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.Type: GrantFiled: February 5, 2003Date of Patent: April 24, 2007Assignees: Schering Corporation, Pharacopeia Drug Discovery, Inc.Inventors: Dmitri A. Pissarnitski, Hubert B. Josien, Elizabeth M. Smith, John W. Clader, Theodros Asberom, Tao Guo, Douglas W. Hobbs
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Patent number: 7122675Abstract: Novel aryl and heteroaryl sulfonamides are disclosed. The sulfonamides, which are gamma secretase inhibitors, are represented by the formula: wherein Ar1 and Ar2 independently represent aryl or heteroaryl and Y represents a bond or a —(C(R3)2)1-3 group. Also disclosed is a method of inhibiting gamma secretase, and a method of treating Alzheimer's disease using the compounds of formula I.Type: GrantFiled: August 1, 2002Date of Patent: October 17, 2006Assignee: Schering CorporationInventors: Hubert B. Josien, John W. Clader, Theodros Asberom, Dmitri A. Pissarnitski
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Publication number: 20060100427Abstract: This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —X(CO)Y, or alkylene-X(CO)Y wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.Type: ApplicationFiled: October 3, 2005Publication date: May 11, 2006Inventors: Dmitri Pissarnitski, Hubert Josien, Elizabeth Smith, John Clader, Theodros Asberom, Tao Guo, Douglas Hobbs