Patents by Inventor Robert M. Rzasa
Robert M. Rzasa 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: 20200048265Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphoType: ApplicationFiled: October 17, 2019Publication date: February 13, 2020Applicant: Amgen Inc.Inventors: Yi CHEN, Timothy D. CUSHING, Jason A. DUQUETTE, Felix GONZALEZ LOPEZ DE TURISO, Xiaolin HAO, Xiao HE, Brian S. LUCAS, Lawrence R. MCGEE, Andreas REICHELT, Robert M. RZASA, Jennifer L. SEGANISH, Youngsook SHIN, Dawei ZHANG
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Publication number: 20180105532Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphoType: ApplicationFiled: December 13, 2017Publication date: April 19, 2018Applicant: Amgen Inc.Inventors: Yi CHEN, Timothy D. CUSHING, Jason A. DUQUETTE, Felix GONZALEZ LOPEZ DE TURISO, Xiaolin HAO, Xiao HE, Brian S. LUCAS, Lawrence R. MCGEE, Andreas REICHELT, Robert M. RZASA, Jennifer L. SEGANISH, Youngsook SHIN, Dawei ZHANG
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Patent number: 9873701Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphoType: GrantFiled: October 22, 2014Date of Patent: January 23, 2018Assignee: AMGEN INC.Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian S. Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer L. Seganish, Youngsook Shin, Dawei Zhang
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Publication number: 20170267673Abstract: 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, and each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and 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 Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.Type: ApplicationFiled: November 17, 2016Publication date: September 21, 2017Applicant: AMGEN INC.Inventors: Jennifer R. ALLEN, Albert AMEGADZIE, Matthew P. BOURBEAU, James A. BROWN, Jian J. CHEN, Yuan CHENG, Michael J. FROHN, Angel GUZMAN-PEREZ, Paul E. HARRINGTON, Longbin LIU, Qingyian LIU, Jonathan D. LOW, Vu Van MA, James R. MANNING, Ana Elena MINATTI, Thomas T. NGUYEN, Nobuko NISHIMURA, Mark H. NORMAN, Liping H. PETTUS, Alexander J. PICKRELL, Wenyuan QIAN, Shannon RUMFELT, Robert M. RZASA, Aaron C. SIEGMUND, Markian M. STEC, Ryan D. WHITE, Qiufen XUE
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Patent number: 9718803Abstract: Unsaturated nitrogen heterocyclic compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, Huntington's Disease, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: GrantFiled: December 17, 2015Date of Patent: August 1, 2017Assignee: Amgen Inc.Inventors: Jennifer R. Allen, Jian J. Chen, Michael J. Frohn, Essa Hu Harrington, Qingyian Liu, Alexander J. Pickrell, Shannon Rumfelt, Robert M. Rzasa, Wenge Zhong
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Patent number: 9611261Abstract: 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, each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and 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 Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.Type: GrantFiled: November 4, 2015Date of Patent: April 4, 2017Assignee: Amgen Inc.Inventors: Ana Elena Minatti, Jonathan D. Low, Jennifer R. Allen, Albert Amegadzie, James Brown, Michael J. Frohn, Angel Guzman-Perez, Paul E. Harrington, Patricia Lopez, Vu Van Ma, Nobuko Nishimura, Wenyuan Qian, Shannon Rumfelt, Robert M. Rzasa, Kelvin Sham, Adrian L. Smith, Ryan White, Qiufen Xue
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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: 9550762Abstract: 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, and each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and 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 Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.Type: GrantFiled: August 5, 2015Date of Patent: January 24, 2017Assignee: Amgen, Inc.Inventors: Jennifer R. Allen, Albert Amegadzie, Matthew P. Bourbeau, James A. Brown, Jian J. Chen, Yuan Cheng, Michael J. Frohn, Angel Guzman-Perez, Paul E. Harrington, Longbin Liu, Qingyian Liu, Jonathan D. Low, Vu Van Ma, James Manning, Ana Elena Minatti, Thomas T. Nguyen, Nobuko Nishimura, Mark H. Norman, Liping H. Pettus, Alexander J. Pickrell, Wenyuan Qian, Shannon Rumfelt, Robert M. Rzasa, Aaron C. Siegmund, Markian M. Stec, Ryan D. White, Qiufen Xue
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Patent number: 9493459Abstract: Azetidine and piperidine compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds and intermediates thereof. Provided herein also are methods of treating cognitive disorders or diseases treatable by inhibition of PDE10, such as Huntington's Disease, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: GrantFiled: March 1, 2016Date of Patent: November 15, 2016Assignee: AMGEN INC.Inventors: Jennifer R. Allen, Jian J. Chen, Michael J. Frohn, Matthew R. Kaller, Qingyian Liu, Thomas T. Nguyen, Alexander J. Pickrell, Wenyuan Qian, Robert M. Rzasa, Wenge Zhong
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Publication number: 20160280695Abstract: 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, each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and 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 Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.Type: ApplicationFiled: November 4, 2015Publication date: September 29, 2016Applicant: AMGEN INC.Inventors: Ana Elena MINATTI, Jonathan D. LOW, Jennifer R. ALLEN, Albert AMEGADZIE, James BROWN, Michael J. FROHN, Angel GUZMAN-PEREZ, Paul E. HARRINGTON, Patricia LOPEZ, Vu Van MA, Nobuko NISHIMURA, Wenyuan QIAN, Shannon RUMFELT, Robert M. RZASA, Kelvin SHAM, Adrian L. SMITH, Ryan WHITE, Qiufen XUE
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Patent number: 9376450Abstract: Heteroaryloxyheterocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.Type: GrantFiled: May 10, 2013Date of Patent: June 28, 2016Assignee: AMGEN INC.Inventors: Jennifer R. Allen, Daniel B. Horne, Essa Hu Harrington, Matthew R. Kaller, Holger Monenschein, Thomas T. Nguyen, Andreas Reichelt, Robert M. Rzasa
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Publication number: 20160176874Abstract: Azetidine and piperidine compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds and intermediates thereof. Provided herein also are methods of treating cognitive disorders or diseases treatable by inhibition of PDE10, such as Huntington's Disease, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: March 1, 2016Publication date: June 23, 2016Inventors: Jennifer R. ALLEN, Jian J. CHEN, Michael J. FROHN, Matthew R. KALLER, Qingyian LIU, Thomas T. NGUYEN, Alexander J. PICKRELL, Wenyuan QIAN, Robert M. RZASA, Wenge ZHONG
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Publication number: 20160102075Abstract: Unsaturated nitrogen heterocyclic compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, Huntington's Disease, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: December 17, 2015Publication date: April 14, 2016Applicant: AMGEN INC.Inventors: Jennifer R. ALLEN, Jian J. CHEN, Michael J. FROHN, Essa Hu HARRINGTON, Qingyian LIU, Alexander J. PICKRELL, Shannon RUMFELT, Robert M. RZASA, Wenge ZHONG
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Patent number: 9303028Abstract: Azetidine and piperidine compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds and intermediates thereof. Provided herein also are methods of treating cognitive disorders or diseases treatable by inhibition of PDE10, such as Huntington's Disease, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: GrantFiled: January 31, 2014Date of Patent: April 5, 2016Assignee: AMGEN INC.Inventors: Jennifer R. Allen, Jian J. Chen, Michael J. Frohn, Matthew R. Kaller, Qingyian Liu, Thomas T. Nguyen, Alexander J. Pickrell, Wenyuan Qian, Robert M. Rzasa, Wenge Zhong
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Patent number: 9296734Abstract: 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, each of R1 and R2, R3 and R7 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 Formulas II and III, and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III.Type: GrantFiled: February 27, 2014Date of Patent: March 29, 2016Assignee: Amgen Inc.Inventors: Ana Elena Minatti, Jonathan D. Low, Jennifer R. Allen, Jian Chen, Ning Chen, Yuan Cheng, Ted Judd, Qingyian Liu, Patricia Lopez, Wenyuan Qian, Shannon Rumfelt, Robert M. Rzasa, Nuria A. Tamayo, Qiufen Xue, Bryant Yang, Wenge Zhong
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Publication number: 20160046618Abstract: 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, and each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and 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 Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.Type: ApplicationFiled: August 5, 2015Publication date: February 18, 2016Applicant: AMGEN INC.Inventors: Jennifer R. ALLEN, Albert AMEGADZIE, Matthew P. BOURBEAU, James A. BROWN, Jian J. CHEN, Yuan CHENG, Michael J. FROHN, Angel GUZMAN-PEREZ, Paul E. HARRINGTON, Longbin LIU, Qingyian LIU, Jonathan D. LOW, Vu Van MA, James MANNING, Ana Elena MINATTI, Thomas T. NGUYEN, Nobuko NISHIMURA, Mark H. NORMAN, Liping H. PETTUS, Alexander J. PICKRELL, Wenyuan QIAN, Shannon RUMFELT, Robert M. RZASA, Aaron C. SIEGMUND, Markian M. STEC, Ryan D. WHITE, Qiufen XUE
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Patent number: 9174992Abstract: Heterobicyclic compounds of Formula (I): or a pharmaceutically-acceptable salt, tautomer, or stereoisomer thereof, as defined in the specification, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, Huntington's Disease, and the like.Type: GrantFiled: February 28, 2013Date of Patent: November 3, 2015Assignee: Amgen Inc.Inventors: Jennifer R. Allen, Albert Amegadzie, Kristin L. Andrews, James Brown, Jian J. Chen, Ning Chen, Essa Hu Harrington, Qingyian Liu, Thomas T. Nguyen, Alexander J. Pickrell, Wenyuan Qian, Shannon Rumfelt, Robert M. Rzasa, Chester Chenguang Yuan, Wenge Zhong
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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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Publication number: 20150252011Abstract: 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, each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and 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 Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.Type: ApplicationFiled: April 21, 2015Publication date: September 10, 2015Inventors: Ana Elena Minatti, Jonathan D. LOW, Jennifer R. ALLEN, Albert AMEGADZIE, James BROWN, Michael J. FROHN, Angel GUZMAN-PEREZ, Paul E. HARRINGTON, Patricia LOPEZ, Vu Van MA, Nobuko NISHIMURA, Wenyuan QIAN, Shannon RUMFELT, Robert M. RZASA, Kelvin SHAM, Adrian L. SMITH, Ryan WHITE, Qiufen XUE
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Patent number: 9090593Abstract: The invention relates to bicyclic compounds of formula (1?), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.Type: GrantFiled: December 7, 2011Date of Patent: July 28, 2015Assignee: AMGEN INC.Inventors: Hui-Ling Wang, Kaustav Biswas, Victor J. Cee, Frank Chavez, Jr., Bradley J. Herberich, Claire L. M. Jackson, Brian A. Lanman, Matthew Lee, Thomas Nixey, Liping H. Pettus, Anthony B. Reed, Robert M. Rzasa, Shannon Rumfelt, Andrew Tasker, Bin Wu, Ryan Wurz