Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, m, n, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.
Type:
Grant
Filed:
May 7, 2007
Date of Patent:
December 8, 2009
Assignee:
Merck & Co., Inc.
Inventors:
Michael R. Wood, Steven N. Gallicchio, Harold G. Selnick, C. Blair Zartman, Ian M. Bell, Craig A. Stump
Abstract: The present invention relates to fluorinated dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
Abstract: A class of compounds having Formula I and pharmaceutically acceptable salts thereof are useful as therapeutic compounds, particularly in the treatment of hyperlipidemia, hypercholesterolemia, dyslipidemia, and other lipid disorders, and in delaying the onset of or reducing the risk of developing conditions and sequelae that are associated with these diseases, such as atherosclerosis.
Type:
Grant
Filed:
September 12, 2005
Date of Patent:
December 8, 2009
Assignee:
Merck & Co., Inc.
Inventors:
James F. Dropinski, Guo Q. Shi, Yong Zhang
Abstract: The instant invention provides compounds of formula: (I) which are 5-lipoxygenase activating protein inhibitors: formula (I). Compounds of formula (I) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cyto-protective agents.
Inventors:
Lin Chu, Mark T. Goulet, Feroze Ujjainwalla, Linda Chang, Richard Frenette, Yves Girard, Michel Therien, Dwight Macdonald, John H. Hutchinson
Abstract: The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
Type:
Grant
Filed:
March 10, 2006
Date of Patent:
December 1, 2009
Assignee:
Merck & Co. Inc.
Inventors:
Paul J. Coleman, Christopher D. Cox, George D. Hartman
Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uterus of a female patient. These compounds are therefore useful in the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, cancer cachexia, muscular dystrophies, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.
Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uterus of a female patient.
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:
July 19, 2005
Date of Patent:
December 1, 2009
Assignee:
Merck & Co., Inc.
Inventors:
Linda Brockunier, Jian Guo, Rui Liang, Emma R. Parmee, Subharekha Raghavan, George Scott Tria, Yusheng Xiong
Abstract: The present invention encompasses compounds of Formula I: or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.
Type:
Grant
Filed:
September 26, 2007
Date of Patent:
December 1, 2009
Assignee:
Merck & Co., Inc.
Inventors:
Amjad Ali, James M. Balkovec, Donald W. Graham, Christopher F. Thompson, Nazia Quraishi
Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, m, n, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.
Type:
Grant
Filed:
June 19, 2008
Date of Patent:
December 1, 2009
Assignee:
Merck & Co., Inc.
Inventors:
Michael R. Wood, Steven N. Gallicchio, Harold G. Selnick, C. Blair Zartman, Ian M. Bell, Craig A. Stump
Abstract: The present invention is directed to novel fused triazole derivatives 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.
Abstract: Indoles of Formula I having —X-aryl-(CH2)x-oxazolidinedione and —X-heteroaryl-(CH2)x-oxazolidinedione substituents on the N atom of the indole ring, where x is 0 or 1, and —X— is a bond or —CH2—, and their thiazolidinedione analogs, are PPAR gamma agonists or partial agonists and are useful in the treatment and control of type II diabetes, including hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
Type:
Grant
Filed:
June 28, 2005
Date of Patent:
December 1, 2009
Assignee:
Merck & Co., Inc.
Inventors:
Kun Liu, Peter T. Meinke, Harold B. Wood
Abstract: The present invention relates to 2-phenylpyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
Type:
Grant
Filed:
December 15, 2004
Date of Patent:
December 1, 2009
Assignee:
Merck & Co. Inc
Inventors:
Kenneth L. Arrington, Mark E. Fraley, George D. Hartman
Abstract: The present invention provides rhesus monkey dickkopf-1 (rhDkk-1) and nucleotide sequences encoding it. Also provided herein are recombinant vectors, and recombinant hosts comprising rhDkk-1-encoding nucleotide sequences. Isolated rhDkk-1 can be used to screen and identify novel osteoanabolic compounds that stimulate bone formation for the treatment of osteoporosis or other disorders characterized by insufficient bone mass.
Type:
Grant
Filed:
November 12, 2004
Date of Patent:
November 24, 2009
Assignee:
Merck & Co., Inc.
Inventors:
Shun-ichi Harada, Viera Kasparcova, Helmut Glantschnig
Abstract: The present invention relates to tetrahydropyridine compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
Abstract: This invention provides cholesterol absorption inhibitors of Formula I: and the pharmaceutically acceptable salts and esters thereof. The compounds are useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating and preventing atherosclerosis and atherosclerotic disease events.
Type:
Grant
Filed:
June 15, 2005
Date of Patent:
November 24, 2009
Assignee:
Merck & Co., Inc.
Inventors:
Mark T. Goulet, Feroze Ujjainwalla, Anthony Ogawa, Derek Von Langen
Abstract: Compounds of structural formula (I) are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uterus of a female patient.
Type:
Grant
Filed:
October 28, 2003
Date of Patent:
November 24, 2009
Assignee:
Merck & Co., Inc.
Inventors:
Yuntae Kim, Barbara Hanney, Mark E. Duggan, Keith L. Spencer
Abstract: The present invention relates to tetrahydropyridine compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
Type:
Grant
Filed:
December 16, 2003
Date of Patent:
November 24, 2009
Assignee:
Merck & Co., Inc.
Inventors:
Mark E. Fraley, Robert M. Garbaccio, Christy M. Olson, Edward S. Tasber
Abstract: Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein Z, R1, R2, R3, R4, R5, R6, R7, R8 and R9 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
Type:
Grant
Filed:
March 4, 2005
Date of Patent:
November 17, 2009
Assignee:
Merck & Co., Inc.
Inventors:
Matthew M. Morrissette, Peter D. Williams, John S. Wai, Thorsten E. Fisher, Terry A. Lyle