Abstract: The present invention relates to substituted benzimidazoles, 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:
May 5, 2004
Date of Patent:
July 21, 2009
Assignee:
Merck & Co., Inc.
Inventors:
Emma R. Parmee, Ronald M. Kim, Rui Liang, Jiang Chang, Elizabeth Ashley Rouse, Kevin T. Chapman
Abstract: In the examination of obesity or leanness, the examination is based on the expression level of the MCP-1 gene or the MCP-1 protein in a tissue or cell analyte, or on the polymorphism in the gene. In the evaluation of compounds, including screening for therapeutic agents for obesity or leanness, the properties of the MCP-1 gene or the MCP-1 protein are utilized to carry out the evaluation.
Abstract: Compounds represented by formula (I): as well as their pharmaceutically acceptable salts are disclosed. The compounds are useful as glucokinase activating agents for the treatment of diabetes and related conditions. Compositions and methods of treatment are also included.
Abstract: Certain novel piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
Abstract: Certain novel piperazine urea derivatives are agonists of the human melanocortin-4 receptor (MC-4R) and, in particular, are receptor-subtype selective agonists of MC-4R. They are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity and diabetes.
Type:
Grant
Filed:
September 5, 2003
Date of Patent:
August 19, 2008
Assignee:
Merck & Co., Inc.
Inventors:
Raman Kumar Bakshi, Ravi P. Nargund, Brenda L. Palucki, Min K. Park, Zhixiong Ye
Abstract: Indoles having aryloxyalkanoic acid substituents or arylalkanoic acid substituents are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
Type:
Grant
Filed:
August 28, 2003
Date of Patent:
July 1, 2008
Assignee:
Merck & Co., Inc.
Inventors:
John J. Acton, III, Peter T. Meinke, Harold B. Wood, Regina M. Black
Abstract: Indoles having aryloxyalkanoic acid substituents or arylalkanoic acid substituents are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
Type:
Grant
Filed:
March 6, 2007
Date of Patent:
March 18, 2008
Assignee:
Merck & Co., Inc.
Inventors:
John J. Acton, III, Sheryl D. Debenham, Kun Liu, Peter T. Meinke, Harold B. Wood, Regina M. Black
Abstract: Certain novel N-acylated spiropiperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
Type:
Grant
Filed:
March 31, 2004
Date of Patent:
February 12, 2008
Assignee:
Merck & Co., Inc.
Inventors:
Liangqin Guo, Shuwen He, Tianying Jian, Yingjie Lai, Jian Liu, Ravi P. Nargund, Iyassu K. Sebhat, Feroze Ujjainwalla, Zhixiong Ye, Jonathan R. Young
Abstract: A class of N-cyclohexylaminocarbonyl benzenesulfonamide derivatives are agonists or partial agonists or antagonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
Type:
Grant
Filed:
January 13, 2004
Date of Patent:
January 15, 2008
Assignee:
Merck & Co., Inc.
Inventors:
Soumya P. Sahoo, Hiroo Koyama, Daniel J. Miller
Abstract: Fluoro substituted cycloalkanoindole derivatives are antagonists of prostaglandins, and as such are useful for the treatment of prostaglandin mediated diseases.
Type:
Grant
Filed:
January 22, 2003
Date of Patent:
January 8, 2008
Assignee:
Merck Frosst Canada & Co.
Inventors:
Carl Berthelette, Nicolas Lachance, Lianhai Li, Claudio Sturino, Zhaoyin Wang
Abstract: The present invention relates to cyclic guanidines, 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:
December 15, 2004
Date of Patent:
November 27, 2007
Assignee:
Merck & Co., Inc.
Inventors:
Emma R. Parmee, Ronald M. Kim, Elizabeth A. Rouse, Darby R. Schmidt, Christopher Joseph Sinz, Jiang Chang
Abstract: The present invention addresses substituted thiophene derivatives, as well as compositions containing such compounds and methods of treatment. The compounds in the present invention are glucagon antagonists. The compounds block the action of glucagon at its receptor and thereby decrease the levels of plasma glucose providing a treatment of diabetes.
Type:
Grant
Filed:
September 8, 2003
Date of Patent:
September 25, 2007
Assignee:
Merck & Co., Inc.
Inventors:
Joseph Duffy, Elizabeth Louise Campbell, Rui Liang, Zenon Konteatis
Abstract: This invention relates to a novel compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 is āS(O)p-A, āSā(O)q-B or āO-D, wherein p and q, which are the same or different, each represent an integer from 0 to 2, A is a straight chain C1-C10 alkyl group which may be substituted by R10, and B and D each independently represent R12 which may be substituted by R10; R2 is a hydrogen atom, a halogen atom, or a straight chain or branched C1-C6 alkyl group which may be substituted by R10; X1 and X2 each independently represent N or CH, but cannot both be N; the formula (II): shows a monocyclic or bicyclic heteroaryl group which has a nitrogen atom adjacent to the carbon atom bonded to the amide group, and the heteroaryl group may be substituted by R10; R10 is R11, or a hydrocarbon group which may be substituted by R11; R11 is, for example, a hydrogen atom or amino; and R12 is, for example, phenyl, thiazolyl, pyridyl or methylene dioxyphenyl.
Abstract: The present invention addresses substituted cyanothiophene derivatives of the formula I: as well as compositions containing such compounds and methods of treatment. The compounds in the present invention are glucagon antagonists. The compounds block the action of glucagon at its receptor and thereby decrease the levels of plasma glucose providing a treatment of diabetes.
Type:
Grant
Filed:
November 4, 2003
Date of Patent:
March 27, 2007
Assignee:
Merck & Co., Inc
Inventors:
Joseph L. Duffy, Elizabeth Louise Campbell, Brian A. Kirk, Rui Liang, James R. Tata, Kevin T. Chapman, Zenon Konteatis
Abstract: Compounds having Formula I, including pharmaceutically acceptable salts, hydrates and solvates thereof: are selective inhibitors of the 11?-HSD1 enzyme. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dylsipidernia, hyperlipidemia, hypertension, Syndrome X, and other symptoms associated with NIDDM.
Type:
Grant
Filed:
October 30, 2003
Date of Patent:
February 20, 2007
Assignee:
Merck & Co., Inc.
Inventors:
Steven H. Olson, James M. Balkovec, Yuping Zhu
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:
December 18, 2003
Date of Patent:
February 1, 2005
Assignee:
Merck & Co., Inc.
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: This invention is directed to a method of retarding or preventing the transformation of a colonic adenoma to a colonic adenocarcinoma comprising the administration to a patient with FAP or a patient with one or more of said adenomas a non-toxic therapeutically effective amount of NSAID, said amount effective to inhibit the PGHS-2 in said adenoma. The preferred method comprises the administration of a specific PGHS-2 inhibiting agent as defined herein.
Abstract: This invention encompasses the novel compounds of formula A, which are useful in the treatment of prostaglandin mediated diseases,
or a pharmaceutically acceptable salt, hydrate or ester thereof. The invention also encompasses certain pharmaceutical compositions and methods for treatment of prostaglandin mediated diseases comprising the use of compounds of formula A.
Type:
Grant
Filed:
September 14, 2000
Date of Patent:
April 9, 2002
Assignee:
Merck Frosst Canada & Co.
Inventors:
Patrick Lacombe, Marc Labelle, Rejean Ruel