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).

  • Publication number: 20200048265
    Abstract: 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 Lympho
    Type: Application
    Filed: October 17, 2019
    Publication date: February 13, 2020
    Applicant: 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
  • Publication number: 20180105532
    Abstract: 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 Lympho
    Type: Application
    Filed: December 13, 2017
    Publication date: April 19, 2018
    Applicant: 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
  • Patent number: 9873701
    Abstract: 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 Lympho
    Type: Grant
    Filed: October 22, 2014
    Date of Patent: January 23, 2018
    Assignee: 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
  • Publication number: 20170267673
    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, 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: Application
    Filed: November 17, 2016
    Publication date: September 21, 2017
    Applicant: 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
  • Patent number: 9718803
    Abstract: 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: Grant
    Filed: December 17, 2015
    Date of Patent: August 1, 2017
    Assignee: 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
  • Patent number: 9611261
    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, 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: Grant
    Filed: November 4, 2015
    Date of Patent: April 4, 2017
    Assignee: 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
  • Patent number: 9556135
    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: Grant
    Filed: October 10, 2013
    Date of Patent: January 31, 2017
    Assignee: 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
  • Patent number: 9550762
    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, 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: Grant
    Filed: August 5, 2015
    Date of Patent: January 24, 2017
    Assignee: 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
  • Patent number: 9493459
    Abstract: 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: Grant
    Filed: March 1, 2016
    Date of Patent: November 15, 2016
    Assignee: 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
  • Publication number: 20160280695
    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, 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: Application
    Filed: November 4, 2015
    Publication date: September 29, 2016
    Applicant: 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
  • Patent number: 9376450
    Abstract: 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: Grant
    Filed: May 10, 2013
    Date of Patent: June 28, 2016
    Assignee: 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
  • Publication number: 20160176874
    Abstract: 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: Application
    Filed: March 1, 2016
    Publication date: June 23, 2016
    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
  • Publication number: 20160102075
    Abstract: 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: Application
    Filed: December 17, 2015
    Publication date: April 14, 2016
    Applicant: 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
  • Patent number: 9303028
    Abstract: 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: Grant
    Filed: January 31, 2014
    Date of Patent: April 5, 2016
    Assignee: 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
  • Patent number: 9296734
    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, 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: Grant
    Filed: February 27, 2014
    Date of Patent: March 29, 2016
    Assignee: 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
  • Publication number: 20160046618
    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, 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: Application
    Filed: August 5, 2015
    Publication date: February 18, 2016
    Applicant: 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
  • Patent number: 9174992
    Abstract: 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: Grant
    Filed: February 28, 2013
    Date of Patent: November 3, 2015
    Assignee: 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
  • 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: 20150252011
    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, 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: Application
    Filed: April 21, 2015
    Publication date: September 10, 2015
    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
  • Patent number: 9090593
    Abstract: 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: Grant
    Filed: December 7, 2011
    Date of Patent: July 28, 2015
    Assignee: 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