Patents by Inventor Oleg Epstein
Oleg Epstein 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: 9777019Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A3, A4, A5, A6, L, R2, R7, X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.Type: GrantFiled: February 11, 2016Date of Patent: October 3, 2017Assignee: Amgen Inc.Inventors: Ryan White, Yuan Cheng, Ana Elena Minatti, Bryant Yang, Xiao Mei Zheng, Patricia Lopez, Jason B. Human, Oleg Epstein, Ted Judd, Kelvin Sham, Qiufen Xue
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Patent number: 9725469Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, L, R2, R7, X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.Type: GrantFiled: November 12, 2013Date of Patent: August 8, 2017Assignee: Amgen, Inc.Inventors: Ryan White, Oleg Epstein, Jason B. Human, Xiao Mei Zheng, Yuan Cheng, Kelvin Sham, Qingyian Liu, Ning Chen
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Patent number: 9556135Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-II.Type: GrantFiled: October 10, 2013Date of Patent: January 31, 2017Assignee: Amgen, Inc.Inventors: Richard T. Lewis, Jennifer R. Allen, Yuan Cheng, Deborah Choquette, Oleg Epstein, Angel Guzman-Perez, Paul E. Harrington, Zihao Hua, Randall W. Hungate, Jason Brooks Human, Ted Judd, Qingyian Liu, Patricia Lopez, Ana Elena Minatti, Philip Olivieri, Karina Romero, Shannon Rumfelt, Robert M. Rzasa, Laurie Schenkel, John Stellwagen, Ryan White, Qiufen Xue, Xiao Mei Zheng, Wenge Zhong
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Patent number: 9365522Abstract: The present invention relates to a novel compound having a function of inhibiting ROR? activity. The present invention also relates to pharmaceutical composition comprising the compound, a use of the compound in treating or preventing autoimmune diseases, inflammatory diseases, metabolic diseases, or cancer diseases.Type: GrantFiled: February 27, 2015Date of Patent: June 14, 2016Assignees: AMGEN INC., TEIJIN PHARMA LIMITEDInventors: Hilary Plake Beck, Shon Keith Booker, Howard Bregman, Victor J. Cee, Nagasree Chakka, Timothy D. Cushing, Oleg Epstein, Brian M. Fox, Stephanie Geuns-Meyer, Xiaolin Hao, Kenta Hibiya, Jun Hirata, Zihao Hua, Jason Human, Shinji Kakuda, Patricia Lopez, Ryota Nakajima, Kazuhisa Okada, Steven H. Olson, Hiroyuki Oono, Lewis D. Pennington, Kosuke Sasaki, Keiko Shimada, Youngsook Shin, Ryan D. White, Ryan P. Wurz, Shuyan Yi, Xiao Mei Zheng
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Publication number: 20160159818Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A3, A4, A5, A6, L, R2, R7, X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.Type: ApplicationFiled: February 11, 2016Publication date: June 9, 2016Applicant: AMGEN INC.Inventors: Ryan WHITE, Yuan CHENG, Ana Elena MINATTI, Bryant YANG, Xiao Mei ZHENG, Patricia LOPEZ, Jason B. HUMAN, Oleg EPSTEIN, Ted JUDD, Kelvin SHAM, Qiufen XUE
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Patent number: 9309263Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A5, A6, A8, R1, R2, R3, R7, X, Y, n and o of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, compounds of Formula III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III, and sub-Formulas thereof.Type: GrantFiled: January 28, 2014Date of Patent: April 12, 2016Assignee: Amgen Inc.Inventors: Ryan White, Jennifer R. Allen, Oleg Epstein, Fang-Tsao Hong, Zihao Hua, Jason Brooks Human, Patricia Lopez, Philip R. Olivieri, Karina Romero, Laurie Schenkel, John Stellwagen, Nuria A. Tamayo, Xiao Mei Zheng
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Patent number: 9296759Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, L, R2, R7, X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.Type: GrantFiled: September 21, 2012Date of Patent: March 29, 2016Assignee: Amgen Inc.Inventors: Ryan White, Yuan Cheng, Ana Elena Minatti, Bryant Yang, Xiao Mei Zheng, Patricia Lopez, Jason B. Human, Oleg Epstein, Ted Judd, Kelvin Sham, Qiufen Xue
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Publication number: 20150307521Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, L, R2, R7, X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.Type: ApplicationFiled: November 12, 2013Publication date: October 29, 2015Inventors: Ryan WHITE, Oleg EPSTEIN, Jason B. HUMAN, Xiao Mei ZHENG, Yuan CHENG, Kelvin SHAM, Qingyian Liu, Ning CHEN
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Publication number: 20150266824Abstract: The present invention relates to a novel compound having a function of inhibiting ROR? activity. The present invention also relates to pharmaceutical composition comprising the compound, a use of the compound in treating or preventing autoimmune diseases, inflammatory diseases, metabolic diseases, or cancer diseases.Type: ApplicationFiled: February 27, 2015Publication date: September 24, 2015Inventors: Hilary Plake Beck, Shon Keith Booker, Howard Bregman, Victor J. Cee, Nagasree Chakka, Timothy D. Cushing, Oleg Epstein, Brian M. Fox, Stephanie Geuns-Meyer, Xiaolin Hao, Kenta Hibiya, Jun Kirata, Zihao Hua, Jason Human, Shinji Kakuda, Patricia Lopez, Ryota Nakajima, Kazuhisa Okada, Steven H. Olson, Hiroyuki Oono, Lewis D. Pennington, Kosuke Sasaki, Keiko Shimada, Youngsook Shin, Ryan D. White, Ryan P. Wurz, Shuyan Yi, Xiao Mei Zheng
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Publication number: 20150259308Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-II.Type: ApplicationFiled: October 10, 2013Publication date: September 17, 2015Applicant: AMGEN INC.Inventors: Richard T. Lewis, Jennifer R. Allen, Yuan Cheng, Deborah Choquette, Oleg Epstein, Angel Guzman-Perez, Paul E. Harrington, Zihao Hua, Randall W. Hungate, Jason Brooks Human, Ted Judd, Qingyian Liu, Patricia Lopez, Ana Elena Minatti, Philip Olivieri, Karina Romero, Shannon Rumfelt, Robert M. Rzasa, Laurie Schenkel, John Stellwagen, Ryan White, Qiufen Xue, Xiao Mei Zheng, Wenge Zhong
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Patent number: 8962859Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A1, A3, A5, A6, A8, R2, R7, X, Y and Z of Formula I are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to plaque formation and deposition, resulting from the activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits and impairments, schizophrenia and other central nervous system conditions and disorders. The invention further provides compounds of Formulas II and III, and of sub-formulas of Formulas I, II and III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III.Type: GrantFiled: February 13, 2012Date of Patent: February 24, 2015Assignee: Amgen Inc.Inventors: Oleg Epstein, Ryan White, Vinod F. Patel, Jason Brooks Human
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Patent number: 8957083Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A1, A3, A4, A5, A6, A8, L, R2, R7, R9, W and Y of Formula I are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to plaque formation and deposition, resulting from the activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, sub-Formula embodiments of Formulas I, II and III, intermediates and processes and methods useful for the preparation of compounds of Formulae I-III.Type: GrantFiled: November 18, 2011Date of Patent: February 17, 2015Assignee: Amgen Inc.Inventors: Ana Elena Minatti, Oleg Epstein, Ryan White, Matthew Weiss, Wenge Zhong, Jonathan D. Low
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Patent number: 8883782Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and other related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, R2, R7, X and Y of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.Type: GrantFiled: March 14, 2011Date of Patent: November 11, 2014Assignee: Amgen Inc.Inventors: Yuan Cheng, Ryan White, Albert Amegadzie, James Brown, Alan C. Cheng, Erin F. Dimauro, Thomas Dineen, Oleg Epstein, Vijay Keshav Gore, Jason Brooks Human, Ted Judd, Charles Kreiman, Qingyian Liu, Patricia Lopez, Vu Van Ma, Isaac Marx, Ana Minatti, Hanh Nho Nguyen, Nick A. Paras, Vinod F. Patel, Wenyuan Qian, Matthew Weiss, Qiufen Xue, Xiao Mei Zheng, Wenge Zhong
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Publication number: 20140296226Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, L, R2, R7, X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.Type: ApplicationFiled: September 21, 2012Publication date: October 2, 2014Inventors: Ryan White, Yuan Cheng, Ana Elena Minatti, Bryant Yang, Xiao Mei Zheng, Patricia Lopez, Jason B. Human, Oleg Epstein, Ted Judd, Kelvin Sham, Qiufen Xue
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Publication number: 20140213581Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A5, A6, A8, R1, R2, R3, R7, X, Y, n and o of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, compounds of Formula III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III, and sub-Formulas thereof.Type: ApplicationFiled: January 28, 2014Publication date: July 31, 2014Inventors: Ryan WHITE, Jennifer R. ALLEN, Oleg EPSTEIN, Fang-Tsao HONG, Zihao HUA, Jason Brooks HUMAN, Patricia LOPEZ, Philip R. OLIVIERI, Karina ROMERO, Laurie SCHENKEL, John STELLWAGEN, Nuria A. TAMAYO, Xiao Mei ZHENG
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Publication number: 20140107109Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-II.Type: ApplicationFiled: December 18, 2013Publication date: April 17, 2014Inventors: Richard T. LEWIS, Jennifer R. ALLEN, Yuan CHENG, Deborah CHOQUETTE, Oleg EPSTEIN, Angel GUZMAN-PEREZ, Paul E. HARRINGTON, Zihao HUA, Randall W. HUNGATE, Jason Brooks HUMAN, Ted JUDD, Qingyian LIU, Patricia LOPEZ, Ana Elena MINATTI, Philip OLIVIERI, Karina ROMERO, Shannon RUMFELT, Robert M. RZASA, Laurie SCHENKEL, John STELLWAGEN, Ryan WHITE, Qiufen XUE, Xiao ZHENG, Wenge ZHONG
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Publication number: 20140045828Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, R2, R7, X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.Type: ApplicationFiled: June 27, 2013Publication date: February 13, 2014Inventors: Jian CHEN, Wenge ZHONG, Bryant YANG, Wenyuan QIAN, Patricia LOPEZ, Ryan WHITE, Matthew WEISS, Tedd JUDD, Timothy POWERS, Yuan CHENG, Thomas DINEEN, Oleg EPSTEIN, Jason HUMAN, Jonathan D. LOW, Isaac E. MARX, Ana Elena MINATTI, Michele POTASHMAN, Nick A. PARAS, Qingyian LIU
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Publication number: 20140038954Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I, wherein variables A1, A3, A4, A5, A6, A8, R2, R7, X, Y and Z of Formula I are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to plaque formation and deposition, resulting from the activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits and impairments, schizophrenia and other central nervous system conditions and disorders. The invention further provides compounds of Formulas II and III, and of sub-formulas of Formulas I, II and III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III.Type: ApplicationFiled: February 13, 2012Publication date: February 6, 2014Applicant: AMGEN INC.Inventors: Oleg Epstein, Ryan White, Vinod F. Patel, Jason Human
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Publication number: 20130338177Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula (I), wherein variables A1, A3, A4, A5, A6, A8, L, R2, R7, R9, W and Y of Formula (I) are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to plaque formation and deposition, resulting from the activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas (II) and (III), sub-Formula embodiments of Formulas (I), (II) and (III), intermediates and processes and methods useful for the preparation of compounds of Formulae (I-III).Type: ApplicationFiled: November 18, 2011Publication date: December 19, 2013Applicant: AMGEN INC.Inventors: Ana Elena Minatti, Oleg Epstein, Ryan White, Matthew Weiss, Wenge Zhong, Jonathan D. Low
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Patent number: 8426447Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, T1, T2, W, X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.Type: GrantFiled: September 11, 2009Date of Patent: April 23, 2013Assignee: Amgen Inc.Inventors: Ryan White, Albert Amegadzie, Marian C. Bryan, Jian Jeffrey Chen, Alan C. Cheng, Thomas Dineen, Oleg Epstein, Vijay Keshav Gore, Zihao Hua, Jason Brooks Human, Hongbing Huang, Charles Kreiman, Daniel La, Qingyian Liu, Vu Van Ma, Isaac Marx, Vinod F Patel, Wenyuan Qian, Matthew Weiss, Chester Chenguang Yuan