Abstract: The present invention relates to pyridine substituted ethanol compounds and derivatives thereof having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
Type:
Grant
Filed:
January 29, 2007
Date of Patent:
December 20, 2011
Assignee:
Merck Sharp & Dohme
Inventors:
B. Wesley Trotter, Kausik K. Nanda, Nathan R. Kett
Abstract: The present invention relates to pyridin-3-yl pyridin-3-amine compounds and derivatives thereof having the structure formula (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
Type:
Grant
Filed:
January 29, 2007
Date of Patent:
November 29, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Mark T. Bilodeau, Jacob M. Hoffman, M. Brad Nolt
Abstract: A compound having the structure wherein R is an angiotensin receptor antagonist active group, Y is selected from the group consisting of and —C(R1H)OC(O)X((CR12R13)—(CHR10)m—(CH2)n—Zp—(CH2)q—(CHR11)r—(CR16R17))—R5;??2) Z is —O— or —(CR14R15)—; m, n, p, q, and r are independently selected from the group consisting of 0 and 1; X is —O— or —(CR18R19)—; R1 is selected from the group consisting of hydrogen, C1-4 alkyl, aryl and C1-4 alkylaryl; R5 is —O—N?N(O)—R3R4; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.
Type:
Grant
Filed:
April 25, 2011
Date of Patent:
November 8, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Amjad Ali, Michael Man-Chu Lo, Christopher Franklin, Brent Whitehead
Abstract: The present invention relates to dipyridin-3-ylmethoxy compounds and derivatives thereof having the structure I useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
Type:
Grant
Filed:
January 29, 2007
Date of Patent:
October 4, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
B. Wesley Trotter, Richard C. A. Isaacs, Zhicai Wu, Jacob M. Hoffman, Mark T. Bilodeau, Ahren Iver Green
Abstract: Triazole derivatives of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.
Type:
Grant
Filed:
May 26, 2004
Date of Patent:
September 27, 2011
Assignee:
Merck Sharp and Dohme Corp.
Inventors:
Sherman T. Waddell, Gina M. Santorelli, Milana M. Maletic, Aaron H. Leeman, Xin Gu, Donald W. Graham, James M. Balkovec, Susan D. Aster
Abstract: A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein X1 to X4 independently represent a carbon atom or the like; the ring A represents a 5- to 6-membered heteroaryl having 1 to 4 heteroatoms independently selected from the group consisting of a nitrogen atom, a sulfur atom and an oxygen atom; X5 represents an oxygen atom or the like; X represents a carbon atom or the like; Het represents a 5- or 6-membered aliphatic heterocycle; R1 represents an aryl or the like; R2 represents a formyl group or the like; and R3 represents a —C1-6 alkyl or the like. The compound or salt has a glucokinase activation effect and is useful as a therapeutic agent for diabetes.
Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
Type:
Grant
Filed:
March 19, 2007
Date of Patent:
August 2, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Ronald M. Kim, Emma R. Parmee, Qiang Tan, Ashley Rouse Lins, Jiang Chang, Cangming Yang
Abstract: The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus.
Type:
Grant
Filed:
March 19, 2009
Date of Patent:
August 2, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Emma Parmee, Subharekha Raghavan, Teresa Beeson, Dong-Ming Shen
Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
Type:
Grant
Filed:
May 11, 2007
Date of Patent:
May 3, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Ronald M. Kim, Emma R. Parmee, Qiang Tan, Cangming Yang, Ashley Rouse Lins
Abstract: Triazole derivatives of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.
Type:
Grant
Filed:
January 9, 2007
Date of Patent:
April 26, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Nancy J. Kevin, Xin Gu, Sherman T. Waddell
Abstract: Novel crystalline salts of 3-[1-(4-chlorophenyl)-trans-3-fluorocyclobutyl]-4,5-dicyclopropyl-r-4H-1,2,4-triazole are potent inhibitors of 11?-hydroxysteroid dehydrogenase Type 1 and are useful for the treatment of conditions associated with Metabolic Syndrome as well as cognitive impairment. The invention also relates to pharmaceutical compositions containing these novel salts, processes to prepare these salts and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes, hyperglycemia, obesity, dyslipidemia, hypertension, and cognitive impairment.
Type:
Grant
Filed:
January 21, 2005
Date of Patent:
January 25, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Yuri Bereznitski, Mark A. Huffman, Joseph E. Lynch, Matthew Zhao
Abstract: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
Type:
Grant
Filed:
September 17, 2004
Date of Patent:
November 2, 2010
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Christopher J. Dinsmore, Jeffrey M. Bergman
Abstract: The present invention relates to compounds having the structure formula (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
Type:
Grant
Filed:
September 22, 2004
Date of Patent:
August 24, 2010
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Richard Isaacs, Christopher J. Dinsmore, Charles J. McIntyre, Linda S. Payne, David A. Claremon
Abstract: The present invention relates to compounds of structural formula I: I useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
Type:
Grant
Filed:
September 22, 2004
Date of Patent:
July 27, 2010
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Richard Isaacs, Christopher J. Dinsmore, B. Wesley Trotter, Nigel Liverton, Douglas C. Beshore, Nathan R. Kett, Charles J. McIntyre, Kausik K. Nanda, David A. Claremon
Abstract: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
Type:
Grant
Filed:
September 17, 2004
Date of Patent:
June 22, 2010
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Christopher J. Dinsmore, Jeffrey M. Bergman, Charles J. McIntyre, Richard Isaacs, David A. Claremon
Abstract: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
Type:
Grant
Filed:
September 17, 2004
Date of Patent:
May 25, 2010
Assignee:
Merck Sharp & Dohme
Inventors:
B. Wesley Trotter, Christopher Claiborne, Gerald S. Ponticello, Charles J. McIntyre, Nigel Liverton, David A. Claremon
Abstract: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
Type:
Grant
Filed:
September 17, 2004
Date of Patent:
May 4, 2010
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Christopher J. Dinsmore, Jeffrey M. Bergman, Charles J. McIntyre, David A. Claremon
Abstract: There are provided non-human primate and rat GPR103 genes and proteins and a compound evaluation method employing the genes or proteins. There are also provided highly useful novel ligands for functional analysis of the GPR103 genes and proteins and for the compound evaluation. The nucleic acids or proteins having the sequences listed as SEQ ID NOS: 1 to 4 provide non-human primate or rat GPR103 genes and proteins and information based on the genes and proteins. The genes and proteins can be used for evaluation of compounds. The nucleic acids or proteins having the sequence listed as SEQ ID NO: 5 or 6 provide a GPR103 ligand.
Abstract: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
Type:
Grant
Filed:
September 17, 2004
Date of Patent:
April 6, 2010
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
B. Wesley Trotter, Kausik K. Nanda, Nathan R. Kett, Christopher J. Dinsmore, Gerald S. Ponticello, David A. Claremon
Abstract: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
Type:
Grant
Filed:
September 17, 2004
Date of Patent:
April 6, 2010
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Christopher J. Dinsmore, Jeffrey M. Bergman