Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and 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:
Application
Filed:
November 10, 2011
Publication date:
May 17, 2012
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginnetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Heather E. Stevenson, Cheng Wang, C. Blair Zartman
Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and 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:
Application
Filed:
November 10, 2011
Publication date:
May 17, 2012
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginnetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Cheng Wang, C. Blair Zartman
Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and 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.
Abstract: The present invention is directed to radiolabeled CGRP receptor antagonists which are useful for the quantitative imaging of CGRP receptors in mammals.
Type:
Application
Filed:
July 20, 2010
Publication date:
May 17, 2012
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Ian M. Bell, Eric Hostetler, Harold G. Selnick, Craig A. Stump
Abstract: 2,5-Diaryl-1,2,4-triazole derivatives of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase Type 1 enzyme (11?-HSD-1). The compounds are useful for the treatment of diabetes, hyperglycemia, obesity, insulin resistance, atherosclerosis, dyslipidemia, hyperlipidemia, hypertension, and Metabolic Syndrome. Also disclosed are novel compounds of structural formula II which are inhibitors of 11?-HSD-1.
Type:
Grant
Filed:
April 14, 2010
Date of Patent:
May 15, 2012
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Susan D. Aster, James M. Balkovec, Donald W. Graham, Xin Gu, Nancy J. Kevin, Gool F. Patel, Mitree Ponpipom
Abstract: The present invention is directed to benzyl-substituted quinolone compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of diseases in which the M1 receptor is involved.
Type:
Grant
Filed:
June 27, 2007
Date of Patent:
May 15, 2012
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Craig Lindsley, William D. Shipe, Feng Yang, Jaime Lynn Bunda
Abstract: Fluoro substituted cycloalkanoindole derivatives are antagonists of prostaglandins, and as such are useful for the treatment of prostaglandin mediated diseases.
Type:
Application
Filed:
January 19, 2012
Publication date:
May 10, 2012
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Carl Berthelette, Nicolas Lachance, Lianhai Li, Claudio Sturino, Zhaoyin Wang
Abstract: The present invention is directed to certain Inidazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.
Type:
Application
Filed:
February 22, 2010
Publication date:
May 10, 2012
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Ping Liu, Robert J. DeVita, Linus S. Lin, Marc D. Chioda, Terence G Hamill, Wenping Li
Abstract: The present invention relates to natural products that possess fatty acid synthesis inhibitor activity and can be used to treat and prevent diseases such as obesity, cancer, diabetes, fungal infections, Mycobacterium tuberculosis infections, malarial infections and other apicomplexan protozoal diseases.
Type:
Grant
Filed:
September 18, 2007
Date of Patent:
May 8, 2012
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Sheo B. Singh, Michael R. Tota, Jun Wang
Abstract: Compounds of formula I: (wherein variables A1, A2, B, m, n, J, R4, G1, G2, G3 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:
April 11, 2008
Date of Patent:
May 8, 2012
Assignee:
Merck, Sharp & Dohme Corp.
Inventors:
Ian M. Bell, Harold G. Selnick, Craig A. Stump
Abstract: The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
Type:
Grant
Filed:
March 11, 2009
Date of Patent:
May 8, 2012
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Scott D. Kuduk, Ronald K. Chang, Christina Ng Di Marco
Abstract: The present invention relates to substituted 4-hydroxypyrimidine-5-carboxamides useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
Type:
Application
Filed:
June 21, 2010
Publication date:
May 3, 2012
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Matthew J. Clements, John S. Debenham, Jeffrey J. Hale, Christina Madsen-Duggan
Abstract: The present invention features PD-1 binding proteins, a subset of which inhibits binding of PD-L1 to the PD-1 receptor. These binding proteins can be employed to modulate the immune system through the manipulation of the PD-1 signaling pathway, enhancing host immunity to treat infections and cancer.
Type:
Grant
Filed:
March 3, 2009
Date of Patent:
May 1, 2012
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Adam C. Finnefrock, Tong-Ming Fu, Daniel C. Freed, Danilo R. Casimiro, Fengsheng Li, Aimin Tang
Abstract: A process for the preparation of a compound of formula (I), or a salt, hydrate or solvate thereof; wherein R1 and R2 are each independently hydrogen, or C1-6 alkyl groups or R1 and R2 are linked and, together with the cyclopentane carbon atoms to which they are attached, form a cyclopropyl ring.
Type:
Grant
Filed:
April 20, 2006
Date of Patent:
May 1, 2012
Assignee:
Merck Sharpe & Dohme Ltd.
Inventors:
Michael Stewart Ashwood, Matthew Bio, Edward Cleator, David Hands, Faye Julia Sheen, Robert Darrin Wilson
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:
January 27, 2010
Date of Patent:
May 1, 2012
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Scott D. Edmondson, Dooseop Kim, Malcolm Maccoss, Emma R. Parmee, Ann E. Weber, Jinyou Xu
Abstract: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
Type:
Grant
Filed:
March 3, 2010
Date of Patent:
May 1, 2012
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Philip E. Sanderson, Mark E. Layton, Kevin J. Rodzinak
Abstract: The present invention relates to a novel class of compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo.
Type:
Grant
Filed:
February 23, 2007
Date of Patent:
May 1, 2012
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Jonathan B. Grimm, Jed L. Hubbs, Thomas Miller, Karin M. Otte, Phieng Siliphaivanh, Matthew G. Stanton, Kevin Wilson, David Witter, Hua Zhou
Abstract: A compound of the formula (I): wherein R1, R2, R3, R4, Ar, A, n and m are defined herein, is disclosed as a GlyT1 inhibitor; pharmaceutical compositions containing the compound of the formula (I) are also disclosed as are their use in medicine, for example in the treatment of schizophrenia.
Type:
Grant
Filed:
June 13, 2006
Date of Patent:
April 24, 2012
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Wesley Peter Blackaby, Ian Thomas Huscroft, Linda Elizabeth Keown, Richard Thomas Lewis, Piotr Antoni Raubo, Leslie Joseph Street, Christopher George Thomson, Joanne Thomson
Abstract: Compounds of formula I: wherein variables A1, A2, B, m, n, J, R4, G1, G2, G3 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.
Abstract: The present invention relates to substituted 1,3,8-triazaspiro[4.5]decame-2,4-diones useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
Type:
Application
Filed:
June 7, 2010
Publication date:
April 19, 2012
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Joan M. Pierce, Jeffrey J. Hale, Shouwu Miao, Petr Vachal