Patent number: 9309263
Abstract: 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:
Grant
Filed:
January 28, 2014
Date of Patent:
April 12, 2016
Assignee:
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
Publication number: 20150259308
Abstract: 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:
Application
Filed:
October 10, 2013
Publication date:
September 17, 2015
Applicant:
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
Publication number: 20150249223
Abstract: A compound including a Ligand L of Formula I: as well as, a first device and a formulation containing the same, are disclosed. In the compound including the Ligand L of Formula I: X is selected from the group consisting of S, Se, SiRR? and GeRR?; R1, R2, R, and R? are each independently selected from the group consisting of hydrogen, deuterium, halide, alkyl, cycloalkyl, heteroalkyl, arylalkyl, alkoxy, aryloxy, amino, silyl, alkenyl, cycloalkenyl, heteroalkenyl, alkynyl, aryl, heteroaryl, acyl, carbonyl, carboxylic acids, ester, nitrile, isonitrile, sulfanyl, sulfinyl, sulfonyl, phosphino, and combinations thereof; any adjacent substitutions or substituents of R1, R2, R, and R? are optionally linked together to form a ring; the Ligand L is coordinated to a metal M having an atomic number of 40 or greater, and the Ligand L is optionally linked with other ligands to comprise a tridentate, tetradentate, pentadentate or hexadentate ligand.
Type:
Application
Filed:
February 28, 2014
Publication date:
September 3, 2015
Applicant:
Universal Display Corporation
Inventors:
Geza SZIGETHY, Jason BROOKS
Publication number: 20150249222
Abstract: A compound including a ligand L according to Formula I: as well as, a first device and a formulation containing the same, are disclosed. In the compound including the Ligand L of Formula I: R1 and R2 are independently selected from group consisting of hydrogen, deuterium, halide, alkyl, cycloalkyl, heteroalkyl, arylalkyl, alkoxy, aryloxy, amino, silyl, alkenyl, cycloalkenyl, heteroalkenyl, alkynyl, aryl, heteroaryl, acyl, carbonyl, carboxylic acids, ester, nitrile, isonitrile, sulfanyl, sulfinyl, sulfonyl, phosphino, cyano, and combinations thereof; two adjacent substituents of R1 or R2 are optionally joined to form a fused ring; ligand L is coordinated to transition metal M having an atomic number greater than 40; R1 represent mono, di, tri, or tetra-substitution, or no substitution; R2 represent mono, di, or tri-substitution, or no substitution; and at least one substituent of R1 or R2 is cyano.
Type:
Application
Filed:
February 28, 2014
Publication date:
September 3, 2015
Applicant:
Universal Display Corporation
Inventors:
Geza SZIGETHY, Christopher B. MURRAY, Jason BROOKS
Publication number: 20150236279
Abstract: A compound having a structure of Formula M(LA)x(LB)y(LC)z, where ligand LA is ligand LB is and ligand LC is is disclosed. In Formula M(LA)x(LB)y(LC)z, M is a metal having an atomic number greater than 40; x is 1, 2, or 3; y and z are 0, 1, or 2; x+y+z is the oxidation state of metal M; Z1-Z6 are each C or N; ZD is N or a carbene carbon; rings C and D are independently a 5 or 6-membered carbocyclic or heterocyclic ring; R4 is substituted, while each of R1, R2, R3, RC, RD, R11, R12, and R13 are selected from hydrogen and a variety of moieties; and any adjacent substituents of R1, R2, R3, R4, RC, RD, R11, R12, and R13 are optionally joined to form a ring. Formulations and devices, such as an OLEDs, that include the compound of formula M(LA)x(LB)y(LC)z are also described.
Type:
Application
Filed:
February 6, 2015
Publication date:
August 20, 2015
Applicants:
Universal Display Corporation, University of Southern California
Inventors:
Geza SZIGETHY, Jason Brooks, Mark E. Thompson, Patrick Saris, Peter I. Djurovich