Patents by Inventor Michael B. Tollefson

Michael B. Tollefson 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: 8518956
    Abstract: The present invention comprises 1-(1-(2-ethoxyethyl)-3-ethyl-7-(4-methylpyridin-2-ylamino)-1H-pyrazolo[4,3-d]pyrimidin-5-yl)piperidine-4-carboxylic acid and its salts. The invention further comprises pharmaceutical compositions, methods of treatment, and synthetic methods relating to 1-(1-(2-ethoxyethyl)-3-ethyl-7-(4-methylpyridin-2-ylamino)-1H-pyrazolo[4,3-d]pyrimidin-5-yl)piperidine-4-carboxylic acid and its salts.
    Type: Grant
    Filed: November 17, 2010
    Date of Patent: August 27, 2013
    Assignee: Pharmacia & Upjohn Company LLC
    Inventor: Michael B. Tollefson
  • Publication number: 20110059993
    Abstract: The present invention comprises 1-(1-(2-ethoxyethyl)-3-ethyl-7-(4-methylpyridin-2-ylamino)-1H-pyrazolo[4,3-d]pyrimidin-5-yl)piperidine-4-carboxylic acid and its salts. The invention further comprises pharmaceutical compositions, methods of treatment, and synthetic methods relating to 1-(1-(2-ethoxyethyl)-3-ethyl-7-(4-methylpyridin-2-ylamino)-1H-pyrazolo[4,3-d]pyrimidin-5-yl)piperidine-4-carboxylic acid and its salts.
    Type: Application
    Filed: November 17, 2010
    Publication date: March 10, 2011
    Inventor: Michael B. Tollefson
  • Patent number: 7902195
    Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: wherein R2, R6A, R6B and R8 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, synthetic methods, and intermediates are also disclosed.
    Type: Grant
    Filed: April 20, 2007
    Date of Patent: March 8, 2011
    Assignee: Pharmacia & Upjohn Company LLC
    Inventors: Robert O Hughes, Andrew Simon Bell, David Graham Brown, Dafydd Owen, Michael John Palmer, Christopher Phillips, David L. Brown, Yvette M. Fobian, John N. Freskos, Steven E. Heasley, E. Jon Jacobsen, Todd Maddux, Brent Mischke, John M. Molyneaux, Joseph B. Moon, D. Joseph Rogier, Jr., Michael B. Tollefson, John K. Walker
  • Patent number: 7700658
    Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.
    Type: Grant
    Filed: January 29, 2008
    Date of Patent: April 20, 2010
    Assignee: Pfizer Inc.
    Inventors: James A. Sikorsky, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Publication number: 20090227634
    Abstract: The invention relates to compounds of formula (I) processes for their preparation, their use as 5-lipoxygenase inhibitors and pharmaceutical compositions containing the same.
    Type: Application
    Filed: November 24, 2008
    Publication date: September 10, 2009
    Inventors: Edgardo Alvira, Matthew J. Graneto, Margaret Lanahan Grapperhaus, Kaliappan Iyanar, Todd M. Maddux, Matthew W. Mahoney, Mark A. Massa, Kirby R. Sample, Michelle A. Schmidt, Ronald E. Seidel, Jon G. Selbo, Michael B. Tollefson, Richard A. Vonder Embse, Grace M. Wagner, Scott S. Woodard
  • Publication number: 20090156685
    Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.
    Type: Application
    Filed: January 29, 2008
    Publication date: June 18, 2009
    Inventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Publication number: 20090156618
    Abstract: The present invention comprises 1-(1-(2-ethoxyethyl)-3-ethyl-7-(4-methylpyridin-2-ylamino)-1H-pyrazolo[4,3-d]pyrimidin-5-yl)piperidine-4-carboxylic acid and its salts. The invention further comprises pharmaceutical compositions, methods of treatment, and synthetic methods relating to 1-(1-(2-ethoxyethyl)-3-ethyl-7-(4-methylpyridin-2-ylamino)-1H-pyrazolo[4,3-d]pyrimidin-5-yl)piperidine-4-carboxylic acid and its salts.
    Type: Application
    Filed: November 9, 2006
    Publication date: June 18, 2009
    Inventor: Michael B. Tollefson
  • Patent number: 7253211
    Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.
    Type: Grant
    Filed: March 9, 2006
    Date of Patent: August 7, 2007
    Assignee: Pfizer Inc.
    Inventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 7186743
    Abstract: The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.
    Type: Grant
    Filed: April 25, 2005
    Date of Patent: March 6, 2007
    Assignee: Pharmacia Corporation
    Inventors: Arija A. Bergmanis, Michael Clare, Joyce Z. Crich, Lifeng Geng, Timothy J. Hagen, Gunnar J. Hanson, Stephen C. Houdek, He Huang, Donna M. Iula, Francis J. Koszyk, Shuyuan Liao, Scott B. Mohler, Maria Nguyen, Richard A. Partis, Michael A. Stealey, Michael B. Tollefson, Richard M. Weier, Xiangdong Xu, Dominique Bonafoux, Theresa R. Fletcher, Bruce C Hamper, Patrick J. Lennon, Subo Liao, Suzanne Metz, David S. Oburn, Thomas J. Owen, Angela M. Scates, Michael L. Vazquez, Serge G. Wolfson
  • Patent number: 7122536
    Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.
    Type: Grant
    Filed: August 27, 2004
    Date of Patent: October 17, 2006
    Assignee: Pfizer Inc.
    Inventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 7119098
    Abstract: The present invention relates to a class of compounds represented by formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of Formula (I), and methods of selectively antagonizing the ???3 and/or the ???5 integrin without significantly antagonizing the IIb/IIIa integrin.
    Type: Grant
    Filed: June 15, 2001
    Date of Patent: October 10, 2006
    Assignee: Pharmacia Corporation
    Inventors: Srinivasan Raj Nagarajan, Ish Kumar Khanna, Michael B. Tollefson, Scott B. Mohler, Barbara B. Chen, Mark Russell, Balekudru Devadas, Thomas D. Penning, Lori A. Schretzman, Dale P. Spangler, Mark L. Boys, Nizal S. Chandrakumar, Hwang-Fun Lu
  • Patent number: 6956052
    Abstract: The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.
    Type: Grant
    Filed: September 19, 2002
    Date of Patent: October 18, 2005
    Assignee: Pharmacia Corporation
    Inventors: Arija A. Bergmanis, Michael Clare, Joyce Z. Crich, Lifeng Geng, Timothy J. Hagen, Gunnar J. Hanson, Stephen C. Houdek, He Huang, Donna M. Iula, Francis J. Koszyk, Shuyuan Liao, Scott B. Mohler, Maria Nguyen, Richard A. Partis, Michael A. Stealey, Michael B. Tollefson, Richard M. Weier, Xiangdong Xu, Dominique Bonafoux, Theresa R. Fletcher, Bruce C. Hamper, Patrick J. Lennon, Subo Liao, Suzanne Metz, David S. Oburn, Thomas J. Owen, Angela M. Scates, Michael L. Vazquez, Serge G. Wolfson
  • Patent number: 6933304
    Abstract: The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively antagonizing the ?V?3 and/or the ?V?5 integrin without significantly antagonizing the IIb/IIIa or ?V?6 integrin.
    Type: Grant
    Filed: June 15, 2001
    Date of Patent: August 23, 2005
    Assignee: Pharmacia Corporation
    Inventors: Srinivasan Raj Nagarajan, Ish Kumar Khanna, Michael B. Tollefson, Scott B. Mohler, Barbara Chen, Mark Russell, Balekudru Devadas, Thomas D. Penning, Lori A. Schretzman, Dale P. Spangler, Mark Laurence Boys, Nizal Samuel Chandrakumar, Hung-Fun Lu
  • Patent number: 6828446
    Abstract: The present invention is directed to selective LXR modulators, small molecule compounds corresponding to Formula I and is further directed to a process of treating a condition in a mammal that is modulated by LXR using a therapeutically effective dose of a compound of Formula I.
    Type: Grant
    Filed: December 23, 2002
    Date of Patent: December 7, 2004
    Assignee: Pharmacia Corporation
    Inventors: Nizal S. Chandrakumar, Christopher R. Dalton, James W. Malecha, Michael B. Tollefson, Jennifer Ann Van Camp, Phillip B. Cox
  • Publication number: 20040235818
    Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.
    Type: Application
    Filed: December 29, 2003
    Publication date: November 25, 2004
    Inventors: Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Gary A. DeCrescenzo, Yvette M. Fobian, John N. Freskos, Daniel P. Getman, Susan L. Hockerman, Carol P. Howard, Stephen A. Kolodziej, Madeleine H. Li, Joseph J. McDonald, Deborah A. Mischke, Joseph G. Rico, Nathan W. Stehle, Michael B. Tollefson, William F. Vernier, Clara I. Villamil
  • Publication number: 20040209914
    Abstract: This invention is directed to aromatic sulfone hydroxamates (also known as aromatic sulfone hydroxamic acids) and salts thereof that, inter alia, tend to inhibit matrix metalloproteinase (also known as matrix metalloprotease or MMP) activity and/or aggrecanase activity. This invention also is directed to a treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP activity and/or aggrecanase activity.
    Type: Application
    Filed: December 8, 2003
    Publication date: October 21, 2004
    Inventors: Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Gary A. DeCrescenzo, Yvette M. Fobian, John N. Freskos, Daniel P. Getman, Susan L. Hockerman, Carol P. Howard, Darren J. Kassab, Stephen A. Kolodziej, Madeleine H. Li, Joseph J. McDonald, Deborah A. Mischke, Joseph G. Rico, Nathan W. Stehle, Michael B. Tollefson, William F. Vernier, Clara I. Villamil
  • Patent number: 6803388
    Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral N,N-bis-phenyl aminoalcohols. A preferred specific (R)-Chiral N,N-bis phenyl aminoclcohol is the compound.
    Type: Grant
    Filed: December 12, 2001
    Date of Patent: October 12, 2004
    Assignee: Pfizer, Inc.
    Inventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6765023
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted reverse aminoalcohols.
    Type: Grant
    Filed: May 23, 2002
    Date of Patent: July 20, 2004
    Assignee: Pfizer, Inc.
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6750228
    Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.
    Type: Grant
    Filed: May 12, 2000
    Date of Patent: June 15, 2004
    Assignee: Pharmacia Corporation
    Inventors: Thomas E Barta, Daniel P Becker, Louis J Bedell, Terri L Boehm, Jeffrey N Carroll, Gary A DeCrescenzo, Yvette M Fobian, John N Freskos, Daniel P Getman, Joseph J McDonald, Madeleine H Li, Susan L Hockerman, Susan C Howard, Steve A Kolodziej, Deborah A Mischke, Joseph G Rico, Nathan W Stehle, Michael B Tollefson, William F Vernier, Clara I Villamil
  • Patent number: 6750233
    Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.
    Type: Grant
    Filed: September 17, 2001
    Date of Patent: June 15, 2004
    Assignee: Pharmacia Corporation
    Inventors: Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Gary A. DeCrescenzo, Yvette M. Fobian, John N. Freskos, Daniel P. Getman, Joseph J. McDonald, Susan L. Hockerman, Susan C. Howard, Steve A. Kolodziej, Hui Li, Deborah A. Mischke, Joseph G. Rico, Nathan W. Stehle, Michael B. Tollefson, William F. Vernier, Clara I. Villamil