Patents by Inventor Charles G. Caldwell

Charles G. Caldwell 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).

  • Inhibition of HIF-2? heterodimerization with HIF1? (ARNT)
    Patent number: 9757379
    Abstract: Provided is a method of inhibiting heterodimerization of HIF-2? to HIF1? (ARNT) comprising binding certain small molecules to the HIF-2? PAS-B domain cavity but not to HIF1? and inhibiting HIF-2? heterodimerization to HIF1? (ARNT) but not inhibiting HIF1? heterodimerization to HIF1? (ARNT). Those certain small molecules are also referenced synonymously as HIF2-HDI and HIF2? heterodimerization inhibitors and also simply as certain small molecules.
    Type: Grant
    Filed: November 14, 2013
    Date of Patent: September 12, 2017
    Assignee: The Board of Regents of the University of Texas System
    Inventors: Richard K. Bruick, Charles G. Caldwell, Doug E. Frantz, Kevin H. Gardner, John B. MacMillan, Thomas H. Scheuermann, Uttam K. Tambar
  • INHIBITION OF HIF-2ALPHA HETERODIMERIZATION WITH HIF1BETA (ARNT)
    Publication number: 20160250216
    Abstract: Provided is a method of inhibiting heterodimerization of HIF-2? to HIF1? (ARNT) comprising binding certain small molecules to the HIF-2? PAS-B domain cavity but not to HIF1? and inhibiting HIF-2? heterodimerization to HIF1? (ARNT) but not inhibiting HIF1? heterodimerization to HIF1? (ARNT). Those certain small molecules are also referenced synonymously as HIF2-HDI and HIF2? heterodimerization inhibitors and also simply as certain small molecules.
    Type: Application
    Filed: November 14, 2013
    Publication date: September 1, 2016
    Applicant: tHE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM
    Inventors: Richard K. BRUICK, Charles G. CALDWELL, Doug E. FRANTZ, Kevin H. GARDNER, John B. MACMILLAN, Thomas H. SCHEUERMANN, Uttam K. TAMBAR
  • Bicyclic pyrimidines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
    Patent number: 7956061
    Abstract: The present invention is directed to novel substituted bicyclic pyrimidines which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: January 18, 2006
    Date of Patent: June 7, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Wallace T. Ashton, Charles G. Caldwell, Hong Dong, Ying-Duo Gao, Giovanna Scapin, Ann E. Weber
  • Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
    Patent number: 7910596
    Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: February 9, 2007
    Date of Patent: March 22, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tesfaye Biftu, Charles G Caldwell, Ann E. Weber, Ping P Chen, Xiaoxia Qian, Danqing Feng, Jason M. Cox
  • Aminotetrahydropyrans as Dipeptidyl Peptidase-IV Inhibitors for the Treatment or Prevention of Diabetes
    Publication number: 20100234403
    Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Application
    Filed: February 9, 2007
    Publication date: September 16, 2010
    Inventors: Tesfaye Biftu, Charles G. Caldwell, Ann E. Weber, Ping Chen, Xiaoxia Qian, Danqing Feng, Jason M. Cox
  • Bicyclic Pyrimidines as Dipeptidyl Peptidase-IV Inhibitors for the Treatment or Prevention of Diabetes
    Publication number: 20090105210
    Abstract: The present invention is directed to novel substituted bicyclic pyrimidines which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Application
    Filed: January 18, 2006
    Publication date: April 23, 2009
    Inventors: Wallace T. Ashton, Charles G. Caldwell, Hong Dong, Ying-Duo Gao, Giovanna Scapin, Ann E. Weber
  • 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
    Patent number: 7388019
    Abstract: The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: January 27, 2004
    Date of Patent: June 17, 2008
    Assignee: Merck & Co., Inc.
    Inventors: Wallace T. Ashton, Charles G. Caldwell, Joseph L. Duffy, Robert J. Mathvink, Liping Wang, Ann E. Weber
  • 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
    Patent number: 7265128
    Abstract: The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: January 13, 2004
    Date of Patent: September 4, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Wallace T. Ashton, Charles G. Caldwell, Robert J. Mathvink, Hyun O. Ok, Leah Bitalac Reigle, Ann E. Weber
  • Pyrrolidine modulators of CCR5 chemokine receptor activity
    Patent number: 7125887
    Abstract: Pyrrolidine compounds of Formula (I), (wherein R1, R2, R3, R4, R5, R6a, R6b, R7 and R8 are defined herein) are described. The compounds are modulators of CCR5 chemokine receptor activity. The compounds are useful, for example, in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: October 9, 2001
    Date of Patent: October 24, 2006
    Assignee: Merck & Co., Inc.
    Inventors: Jeffrey J. Hale, Charles G. Caldwell, Dooseop Kim, Dong-Ming Shen, Sander G. Mills, Kevin T. Chapman, Liya Chen, Malcolm MacCoss, Amy Gentry, Christopher L. Lynch, Yuan Cheng, legal representative, Christopher A. Willoughby, deceased
  • Dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
    Patent number: 7026316
    Abstract: The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: March 22, 2002
    Date of Patent: April 11, 2006
    Assignee: Merck & Co., Inc.
    Inventors: Wallace T. Ashton, Charles G. Caldwell, Hyun O. Ok, Emma R. Parmee, Ann E. Weber
  • Dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
    Publication number: 20040106656
    Abstract: The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Application
    Filed: September 24, 2003
    Publication date: June 3, 2004
    Inventors: Wallace T Ashton, Charles G Caldwell, Hyun O Ok, Emma R Parmee, Ann E Weber
  • Pyrrolidine modulators of ccr5 chemokine receptor activity
    Publication number: 20040087552
    Abstract: Pyrrolidine compounds of Formula (I), (wherein R1, R2, R3, R4, R5, R6a, R6b, R7 and R8 are defined herein) are described. The compounds are modulators of CCR5 chemokine receptor activity. The compounds are useful, for example, in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Application
    Filed: July 17, 2003
    Publication date: May 6, 2004
    Inventors: Jeffrey J Hale, Charles G. Caldwell, Dooseop Kim, Dong-Ming Shen, Sander G. Mills, Kevin T. Chapman, Liya Chen, Malcolm MacCoss, Amy Gentry, Christopher L. Lynch, Christopher A. Willoughby, Yuan Cheng
  • Pyrrolidine modulators of chemokine receptor activity
    Patent number: 6498161
    Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6 and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.
    Type: Grant
    Filed: April 4, 2000
    Date of Patent: December 24, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Charles G. Caldwell, Kevin T. Chapman, Jeffrey Hale, Dooseop Kim, Christopher Lynch, Malcolm MacCoss, Sander G. Mills, Christopher Willoughby, Scott Berk, Ronald M. Kim
  • Cyclic amine modulators of chemokine receptor activity
    Patent number: 6476054
    Abstract: The present invention is directed to cyclic amines of the formula I: (wherein R1, R2, R3, m and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.
    Type: Grant
    Filed: October 17, 2000
    Date of Patent: November 5, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Charles G. Caldwell, Paul E. Finke, Malcolm Maccoss, Sander G. Mills, Bryan Oates, Dooseop Kim, Shankaran Kothandaraman, Liping Wang
  • Pyrrolidine modulators of CCR5 chemokine receptor activity
    Publication number: 20020094989
    Abstract: Pyrrolidine compounds of Formula I: 1
    Type: Application
    Filed: October 10, 2001
    Publication date: July 18, 2002
    Inventors: Jeffrey J. Hale, Christopher L. Lynch, Charles G. Caldwell, Christopher A. Willoughby, Dooseop Kim, Dong-Ming Shen, Sander G. Mills, Kevin T. Chapman, Liya Chen, Amy Gentry, Malcolm MacCoss, Zenon D. Konteatis
  • Pyrrolidine modulators of chemokine receptor activity
    Patent number: 6399619
    Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6 and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.
    Type: Grant
    Filed: April 4, 2000
    Date of Patent: June 4, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Scott Berk, Charles G. Caldwell, Kevin T. Chapman, Jeffrey Hale, Christopher Lynch, Malcolm MacCoss, Sander G. Mills, Christopher Willoughby
  • Hexahydro-5-imino-1,4-1,4-thiazepine derivatives as inhibitors of nitric oxide synthases
    Patent number: 6372733
    Abstract: Disclosed herein are compounds of Formula I and pharmaceutically acceptable salts thereof which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders, including neurodegenerative disorders, disorders of gastrointestinal motility and inflammation.
    Type: Grant
    Filed: January 4, 2000
    Date of Patent: April 16, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Charles G. Caldwell, Malcolm Maccoss, William K. Hagmann, Shrenik K. Shah, Kothandaraman Shankaran, Karla L. Furman
  • Cyclic amine modulators of chemokine receptor activity
    Patent number: 6140349
    Abstract: The present invention is directed to cyclic amines of the formula I: ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, m and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.
    Type: Grant
    Filed: February 1, 1999
    Date of Patent: October 31, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Charles G. Caldwell, Malcolm Maccoss, Paul E. Finke, Sander G. Mills, Bryan Oates, Shankaran Kothandaraman, Dooseop Kim, Liping Wang
  • Cyclic amine modulations of chemokine receptor activity
    Patent number: 6136827
    Abstract: The present invention is directed to cyclic amines of the formula I: ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, m and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.
    Type: Grant
    Filed: July 21, 1998
    Date of Patent: October 24, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Charles G. Caldwell, Paul E. Finke, Malcolm Maccoss, Laura C. Meurer, Sander G. Mills, Bryan Oates
  • Hexahydro-5-imino-1,4-heteroazepine derivatives as inhibitors of nitric oxide synthases
    Patent number: 6043358
    Abstract: Disclosed herein are compounds of Formula I and pharmaceutically acceptable salts thereof which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders, including neurodegenerative disorders, disorders of gastrointestinal motility and inflammation.
    Type: Grant
    Filed: September 25, 1996
    Date of Patent: March 28, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Charles G. Caldwell, William K. Hagmann, Malcolm Maccoss, Shrenik K. Shah, Kothandaraman Shankaran, Karla L. Furman