Patents by Inventor Timothy Machajewski

Timothy Machajewski 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).

  • Patent number: 8865732
    Abstract: New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
    Type: Grant
    Filed: February 14, 2012
    Date of Patent: October 21, 2014
    Assignee: Novartis AG
    Inventors: Zilin Huang, Jeff Jin, Timothy Machajewski, William R. Antonios-McCrea, Maureen McKenna, Daniel Poon, Paul A. Renhowe, Martin Sendzik, Cynthia Shafer, Aaron Smith, Yongjin Xu, Qiong Zhang, Zheng Chen
  • Publication number: 20140303182
    Abstract: A lacate salt of a compound of Formula I or a tautomer of the compound, wherein Formula I has the following structure and R1-R9 and R12-R14 are as defined herein
    Type: Application
    Filed: March 17, 2014
    Publication date: October 9, 2014
    Applicant: NOVARTIS AG
    Inventors: Shaopei Cai, Joyce Chou, Eric Harwood, Timothy Machajewski, David Ryckman, Xiao Shang, Shuguang Zhu, Augustus Okhamate, Marc S. Tesconi
  • Publication number: 20130338171
    Abstract: A lacate salt of a compound of Formula I or a tautomer of the compound, wherein Formula I has the following structure and R1-R9 and R12-R14 are as defined herein
    Type: Application
    Filed: August 1, 2013
    Publication date: December 19, 2013
    Applicant: Novartis AG
    Inventors: Shaopei Cai, Joyce Chou, Eric Harwood, Timothy Machajewski, David Ryckman, Xiao Shang, Shuguang Zhu, Augustus Okhamafe, Marc S. Tesconi
  • Publication number: 20130210818
    Abstract: New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
    Type: Application
    Filed: February 14, 2012
    Publication date: August 15, 2013
    Inventors: Zilin Huang, Jeff Jin, Timothy Machajewski, William R. Antonios-McCrea, Maureen McKenna, Daniel Poon, Paul A. Renhowe, Martin Sendzik, Cynthia Shafer, Aaron Smith, Yongjin Xu, Qiong Zhang, Zheng Chen
  • Publication number: 20130018058
    Abstract: A lacate salt of a compound of Formula I or a tautomer of the compound, wherein Formula I has the following structure and R1-R9 and R12-R14 are as defined herein
    Type: Application
    Filed: December 2, 2011
    Publication date: January 17, 2013
    Inventors: Shaopei Cai, Joyce Chou, Eric Harwood, Timothy Machajewski, David Ryckman, Xiao Shang, Shuguang Zhu, Augustus O. Okhamafe, Marc S. Tesconi
  • Publication number: 20120277434
    Abstract: A method of synthesizing a substituted or unsubstituted 4-amino-3-benzimidazolyl quinolinone compound includes reacting a first compound having the formula I with a second compound having the formula II in a suitable solvent in the presence of a sodium or potassium salt of a base.
    Type: Application
    Filed: July 2, 2012
    Publication date: November 1, 2012
    Inventors: Shaopei Cai, Joyce Chou, Eric Harwood, Timothy MacHajewski, David Ryckman, Xiao Shang, Shuguang Zhu, Augustus O. Okhamafe, Marc S. Tesconi
  • Patent number: 8129394
    Abstract: Novel imidazole compounds of the general formula are disclosed, wherein R1 and R2 comprise heteroaryl groups. These compounds and compositions containing them are useful in methods to treat Raf kinase-mediated disorders such as cancer.
    Type: Grant
    Filed: March 19, 2009
    Date of Patent: March 6, 2012
    Assignee: Novartis AG
    Inventors: Zilin Hunag, Jeff Jin, Timothy Machajewski, William R. Antonios-McCrea, Maureen McKenna, Daniel Poon, Paul A. Renhowe, Martin Sendzik, Cynthia Shafer, Aaron Smith, Yongjin Xu, Qiong Zhang, Zheng Chen
  • Patent number: 7838527
    Abstract: Methods of treating cancer using 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one are provided. In particular, the methods are effective for the treatment of solid tumors or leukemias, including prostate, colorectal, breast, multiple myeloma, pancreatic, small cell carcinoma, acute myelogenous leukemia, chronic myelogenous leukemia, or myelo-proliferative disease. Further provided are methods of measuring the amount of 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one and determining a metabolic profile therefore.
    Type: Grant
    Filed: November 12, 2003
    Date of Patent: November 23, 2010
    Assignee: Novartis Vaccines and Diagnostics, Inc.
    Inventors: Alison Hannah, Eric Harwood, Peter Haroldsen, Carla Heise, Timothy Machajewski, Emil Samara, Xiao Shang, Jayesh Vora, Shuguang Zhu
  • Publication number: 20100003246
    Abstract: New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
    Type: Application
    Filed: March 19, 2009
    Publication date: January 7, 2010
    Inventors: Zilin Hunag, Jeff Jin, Timothy Machajewski, William R. Antonios-McCrea, Maureen McKenna, Daniel Poon, Paul A. Renhowe, Martin Sendzik, Cynthia Shafer, Aaron Smith, Yongjin Xu, Qiong Zhang, Zheng Chen
  • Publication number: 20090181979
    Abstract: A lacate salt of a compound of Formula I or a tautomer of the compound, wherein Formula I has the following structure and R1-R9 and R12-R14 are as defined herein
    Type: Application
    Filed: March 4, 2009
    Publication date: July 16, 2009
    Inventors: Shaopei Cai, Joyce Chou, Eric Harwood, Timothy Machajewski, David Ryckman, Xiao Shang, Shuguang Zhu, Augustus O. Okhamafe, Marc S. Tesconi
  • Patent number: 7368459
    Abstract: Organic compounds having the structural formula I are provided where the variables have the values described herein and R1 and R2 join together to form a 6 membered substituted or unsubstituted ring including at least one O, N, or S atom, and Z is an O, S, NH or NR group. Pharmaceutical formulations include the organic compound or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: October 11, 2006
    Date of Patent: May 6, 2008
    Assignee: Chiron Corporation
    Inventors: Paul A. Renhowe, Timothy Machajewski, Cynthia Shafer, Mary Ellen Wernette Hammond, Sabina Pecchi
  • Publication number: 20080070906
    Abstract: Organic compounds having the formulas I and II are provided where the variables have the values described herein. Pharmaceutical formulations include the organic compounds or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier and may be prepared by mixing the organic compounds or pharmaceutically acceptable salts of the organic compounds with a carrier and water. A method of treating a patient includes administering a pharmaceutical formulation according to the invention to a patient in need thereof.
    Type: Application
    Filed: October 2, 2007
    Publication date: March 20, 2008
    Inventors: Paul Renhowe, Sabina Pecchi, Timothy Machajewski, Cynthia Shafer, Clarke Taylor, William McCrea, Christopher McBride, Elisa Jazan
  • Publication number: 20070123546
    Abstract: Disclosed are 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, their stereoisomers, tautomers, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent. Disclosed also are methods of using the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of cellular proliferative, viral, autoimmune, cardiovascular, and central nervous system diseases.
    Type: Application
    Filed: September 28, 2006
    Publication date: May 31, 2007
    Inventors: Timothy Machajewski, Cynthia Shafer, Christopher McBride, William Antonios-McCrea, Brandon Doughan, Barry Levine, Yi Xia, Maureen McKeena, X. Wang, Kris Mendenhall, Yasheen Zhou, Baoquing Gong, Dan Gu, John Dolan, John Tulinsky, Kristin Brinner, Zhenhai Gao
  • Publication number: 20070032528
    Abstract: Organic compounds having the structural formula I are provided where the variables have the values described herein and R1 and R2 join together to form a 6 membered substituted or unsubstituted ring including at least one O, N, or S atom, and Z is an O, S, NH or NR group. Pharmaceutical formulations include the organic compound or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: October 11, 2006
    Publication date: February 8, 2007
    Inventors: Paul Renhowe, Timothy Machajewski, Cynthia Shafer, Mary Ellen Hammond, Sabina Pecchi
  • Publication number: 20070027150
    Abstract: 2-Amino-quinazolin-5-one compounds, stereoisomers, tautomers, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the 2-amino-quinazolin-5-one compounds, either alone or in combination with at least one additional therapeutic agent. Methods of using the 2-amino-quinazolin-5-one compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of cell proliferative diseases.
    Type: Application
    Filed: April 14, 2006
    Publication date: February 1, 2007
    Inventors: Cornelia Bellamacina, Abran Costales, Brandon Doughan, Susan Fong, Zhenhai Gao, Thomas Hendrickson, Barry Levine, Xiaodong Lin, Timothy Machajewski, Christopher McBride, William Antonios-McCrea, Maureen McKenna, Kris Mendenhall, Alice Rico, Cynthia Shafer, X. Wang, Yi Xia, Yasheen Zhou
  • Patent number: 7138409
    Abstract: Organic compounds having the structural formula I are provided where the variables have the values described herein and R1 and R2 join together to form a 6 membered substituted or unsubstituted ring including at least one O, N, or S atom, and Z is an O, S, NH or NR group. Pharmaceutical formulations include the organic compound or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: April 14, 2004
    Date of Patent: November 21, 2006
    Assignee: Chiron Corporation
    Inventors: Paul A. Renhowe, Timothy Machajewski, Cynthia Shafer, Mary Ellen Wernette Hammond, Sabina Pecchi
  • Publication number: 20060063219
    Abstract: An in vitro protein kinase assay technology that (1) exhibits a high assay signal to background ratio (S/B) and range (S-B); (2) is homogenous; (3) is non-radioactive; and (4) does not require a phospho-specific antibody involves complexing a trivalent metal ion (e.g. Ga3+, Fe3+, Al3+, In3+, Ru3+, Sc3+, Y3+) to the surface of amplified luminescent proximity assay acceptor or donor beads, e.g., via a suitable linker such as nitrilotriacetic acid (NTA; also referred to as carboxymethyl-lysine), iminodiacetic acid (IDA), or an appropriately substituted N-containing heterocycle, for example a triazoheterocycle, for example a triazocyclononaneononane, such as 1-propylamino-4-acetato-1,4,7-triazacyclononane. A protein (or constituent part) or other kinase substrate is bound to the surface of the other of an amplified luminescent proximity assay acceptor or donor bead and, if phosphorylated, brought into proximity with the trivalent metal ion-complexed acceptor bead to generate a luminescent signal.
    Type: Application
    Filed: September 19, 2005
    Publication date: March 23, 2006
    Inventors: Richard Kuo, Timothy Dawes, Timothy Machajewski
  • Publication number: 20050261307
    Abstract: Methods of inhibiting fibroblast growth factor receptor 3 and treating various conditions mediated by fibroblast growth factor receptor 3 are provided that include administering to a subject a compound of Structure I, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I have the following structure where and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting fibroblast growth factor receptor 3 and for use in treating conditions mediated by fibroblast growth factor receptor 3 such as multiple myeloma.
    Type: Application
    Filed: November 5, 2004
    Publication date: November 24, 2005
    Inventors: Shaopei Cai, Joyce Chou, Eric Harwood, Carla Heise, Timothy Machajewski, David Ryckman, Xiao Shang, Marion Wiesmann, Shuguang Zhu
  • Publication number: 20050209247
    Abstract: A lacate salt of a compound of Formula I or a tautomer of the compound, wherein Formula I has the following structure and R1-R9 and R12-R14 are as defined herein
    Type: Application
    Filed: November 5, 2004
    Publication date: September 22, 2005
    Inventors: Shaopei Cai, Joyce Chou, Eric Harwood, Timothy Machajewski, David Ryckman, Xiao Shang, Shuguang Zhu, Augustus Okhamafe, Marc Tesconi
  • Publication number: 20050209456
    Abstract: A method for synthesizing a 4-amino substituted quinolinone includes reacting a substituted or unsubstituted 2-benzimidazolyl-2-acetate with a substituted or unsubstituted 2-aminobenzonitrile in the presence of a base or an acid. A 4-amino substituted quinolinone compound is formed by the reaction, and the 4-amino substituted quinolinone compound comprises a benzimidazole group.
    Type: Application
    Filed: March 29, 2005
    Publication date: September 22, 2005
    Inventors: Paul Renhowe, Cynthia Shafer, Timothy Machajewski, Sabina Pecchi, Christopher McBride