Patents Represented by Attorney, Agent or Law Firm Philippe L. Durette
  • Patent number: 7326708
    Abstract: The dihydrogenphosphate salt of 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine is a potent inhibitor of dipeptidyl peptidase-IV and is useful for the prevention and/or treatment of non-insulin dependent diabetes mellitus, also referred to as type 2 diabetes. The invention also relates to a crystalline monohydrate of the dihydrogenphosphate salt as well as a process for its preparation, pharmaceutical compositions containing this novel form and methods of use for the treatment of diabetes, obesity, and high blood pressure.
    Type: Grant
    Filed: June 23, 2004
    Date of Patent: February 5, 2008
    Assignee: Merck & Co., Inc.
    Inventors: Stephen Howard Cypes, Alex Minhua Chen, Russell R. Ferlita, Karl Hansen, Ivan Lee, Vicky K. Vydra, Robert M. Wenslow, Jr.
  • Patent number: 7309714
    Abstract: The present invention is directed to phenylalanine 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: November 26, 2003
    Date of Patent: December 18, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Joseph L. Duffy, Robert J. Mathvink, Ann E. Weber, Jinyou Xu
  • Patent number: 7307164
    Abstract: The present invention is directed to compounds 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.
    Type: Grant
    Filed: March 21, 2003
    Date of Patent: December 11, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Linda L. Brockunier, Joseph L. Duffy, Dooseop Kim, Emma R. Parmee, Ann E. Weber
  • 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
  • Patent number: 7259160
    Abstract: The present invention is directed to hexahydrodiazepinone compounds 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: July 27, 2004
    Date of Patent: August 21, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Gui-Bai Liang, Tesfaye Biftu, Danqing Dennis Feng, Ann E. Weber
  • Patent number: 7253172
    Abstract: Compounds having Formula I, including pharmaceutically acceptable salts and prodrugs thereof: (I) are inhibitors of the dipeptidyl peptidase-IV enzyme (DP-IV), and are useful in the treatment of DP-IV mediated diseases and conditions, such as non-insulin dependent diabetes mellitus
    Type: Grant
    Filed: June 19, 2002
    Date of Patent: August 7, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Linda Brockunier, Emma Parmee, Ann E. Weber
  • Patent number: 7238683
    Abstract: The present invention is directed to fused phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-RV 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: October 29, 2004
    Date of Patent: July 3, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Wallace T. Ashton, Hong Dong, Jinyou Xu
  • Patent number: 7208498
    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: July 11, 2003
    Date of Patent: April 24, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Robert J. Mathvink, Scott D. Edmondson, Ann E. Weber
  • Patent number: 7202224
    Abstract: The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.
    Type: Grant
    Filed: July 31, 2006
    Date of Patent: April 10, 2007
    Assignees: Merck & Co., Inc., ISIS Pharmaceuticals, Inc.
    Inventors: Anne B. Eldrup, Marija Prhavc, Phillip Dan Cook, Steven S. Carroll, David B. Olsen
  • Patent number: 7157490
    Abstract: The present invention is directed to phenylalanine 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: November 3, 2003
    Date of Patent: January 2, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Vincent J. Colandrea, Scott D. Edmondson, Robert J. Mathvink, Anthony Mastracchio, Ann E. Weber, Jinyou Xu
  • Patent number: 7125873
    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: July 5, 2002
    Date of Patent: October 24, 2006
    Assignee: Merck & Co., Inc.
    Inventors: Scott D Edmondson, Michael H. Fisher, Dooseop Kim, Malcolm Maccoss, Emma R. Parmee, Ann E Weber, Jinyou Xu
  • Patent number: 7125855
    Abstract: The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.
    Type: Grant
    Filed: October 17, 2003
    Date of Patent: October 24, 2006
    Assignee: Merck & Co., Inc.
    Inventors: Balkrishen Bhat, Neelima Bhat, Anne B. Eldrup, Thazha P. Prakash, Marija Prhavc, Quanlai Song, Phillip Dan Cook, Steven S. Carroll, Malcolm Maccoss, David B. Olsen
  • Patent number: 7105499
    Abstract: The present invention provides nucleoside derivatives which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside derivatives alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside derivatives of the present invention.
    Type: Grant
    Filed: January 18, 2002
    Date of Patent: September 12, 2006
    Assignees: Merck & Co., Inc., Isis Pharmaceuticals, Inc.
    Inventors: Steven S. Carroll, David B. Olsen, Malcolm MacCoss, Balkrishen Bhat, Phillip Dan Cook, Anne B. Eldrup, Thazha P. Prakash
  • Patent number: 7101871
    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: October 14, 2003
    Date of Patent: September 5, 2006
    Assignee: Merck & Co., Inc.
    Inventors: Tesfaye Biftu, Gui-Bai Liang, Xiaoxia Qian, Ann E. Weber, Danqing Dennis Feng
  • Patent number: 7098239
    Abstract: Compounds having Formula I, including pharmaceutically acceptable salts and prodrugs thereof: (Formula I) are inhibitors of the dipep tidyl peptidase-IV enzyme (DP-IV), and are useful in the treatment of DP-IV mediated diseases and conditions, such as non-insulin dependent diabetes mellitus.
    Type: Grant
    Filed: June 19, 2002
    Date of Patent: August 29, 2006
    Assignee: Merck & Co., Inc
    Inventors: Scott D. Edmondson, Emma Parmee, Ann E. Weber, Jinyou Xu
  • Patent number: 7034167
    Abstract: A novel process is provided for the preparation of ribofuranose sugar derivatives which are useful in the synthesis of branched-chain ribonucleoside inhibitors of HCV polymerase for the treatment of HCV infection. Also provided are useful intermediates obtained from the instant process.
    Type: Grant
    Filed: December 5, 2003
    Date of Patent: April 25, 2006
    Assignee: Merck & Co., Inc.
    Inventors: Kimberly A. Savary, Zhiguo J. Song, J. Michael Williams, Feng Xu
  • 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
  • Patent number: 6870067
    Abstract: The present invention is concerned with a process for the preparation of trifluorophenylacetic acids using a Grignard reagent and an allylating agent, such as allyl bromide.
    Type: Grant
    Filed: October 7, 2003
    Date of Patent: March 22, 2005
    Assignee: Merck & Co., Inc.
    Inventors: Norihiro Ikemoto, Spencer D. Dreher
  • Patent number: 6777395
    Abstract: The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.
    Type: Grant
    Filed: January 18, 2002
    Date of Patent: August 17, 2004
    Assignees: Merck & Co., Inc., Isis Pharmaceuticals, Inc.
    Inventors: Balkrishen Bhat, Neelima Bhat, Anne B. Eldrup, Thazha P. Prakash, Marija Prhavc, Quanlai Song, Phillip Dan Cook, Steven S. Carroll, Malcolm Maccoss, David B. Olsen
  • Patent number: 6730690
    Abstract: Compounds having Formula I, including pharmaceutically acceptable salts, hydrates and solvates thereof: are selective inhibitors of the 11&bgr;-HSD1 enzyme. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dylsipidemia, hyperlipidemia, hypertension, Syndrome X, and other symptoms associated with NIDDM.
    Type: Grant
    Filed: June 9, 2003
    Date of Patent: May 4, 2004
    Assignee: Merck & Co., Inc.
    Inventors: Steven H. Olson, James M. Balkovec, Yuping Zhu