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.
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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.
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
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