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Assignee: Merck Sharp & Dohme Corp.


Location: Rahway, NJ
No. of patents: 248

1              
NumberTitleIssue Date
8185367Systems and methods for reconstructing gene networks in segregating populations
The reconstruction of genetic networks in mammalian systems is one of the primary goals in biological research, especially as such reconstructions relate to elucidating not only common, polygenic human disease, but living systems more generally. The present inventio...
05/22/2012
8183275Substituted imidazoles as bombesin receptor subtype-3 modulators
Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders ...
05/22/2012
8183245Pyrazine substituted pyrrolopyridines as inhibitors of JAK and PDK1
The present invention relates to pyrazine substituted pyrrolopyridines having formula (I) useful as inhibitors of JAK kinases (JAK1, JAK2, JAK3 and/or TYK2) and/or PDK1 and for the treatment of myeloproliferative disorders ...
05/22/2012
8178667Benzyl-substituted quinolone M1 receptor positive allosteric modulators
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 recept...
05/15/2012
8178546Diaryltriazoles as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1
2,5-Diaryl-1,2,4-triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase Type 1 enzyme (11β-HSD-1). The compounds are useful for the treatment of diabetes, hyperglycemia, obesity, insulin resistance, atheroscle...
05/15/2012
8173672Quinolizidinone M1 receptor positive allosteric modulators
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 disord...
05/08/2012
8173629Method of treatment using fatty acid synthesis inhibitors
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 ...
05/08/2012
8168757PD-1 binding proteins
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 immuni...
05/01/2012
8168658Inhibitors of histone deacetylase
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...
05/01/2012
8168652Inhibitors of AKT activity
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 compo...
05/01/2012
8168637Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment of diabetes
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 diabet...
05/01/2012
8163956Inhibitors of GLYT1 transporters
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 ...
04/24/2012
8158825Modified malonate derivatives
The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing termin...
04/17/2012
8153778RNA interference mediated inhibition of vascular cell adhesion molecule (VCAM) gene expression using short interfering nucleic acid (siNA)
This invention relates to compounds, compositions, and methods useful for modulating vascular cell adhesion molecule gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for...
04/10/2012
8153626Substituted diazepine sulfonamides as bombesin receptor subtype-3 modulators
Certain novel substituted diazepine sulfonamides are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases an...
04/10/2012
8148535Potassium channel inhibitors
The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like. ...
04/03/2012
8148349Nucleoside cyclic phosphoramidates for the treatment of RNA-dependent RNA viral infection
The present invention provides nucleoside cyclic phosphoramidates of formula (I), pharmaceutical compositions comprising the compounds of formula (I) and methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treat...
04/03/2012
8143289Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzym...
03/27/2012
8142794Hepatitis C virus vaccine
The present invention features Ad6 vectors and a nucleic acid encoding a Met-NS3-NS4A-NS4B-NS5A-NS5B polypeptide containing an inactive NS5B RNA-dependent RNA polymerase region. The nucleic acid is particularly useful as a component of an adenovector or DNA plasmid ...
03/27/2012
8138219Tryptamine sulfonamides as 5-HTantagonists
Novel compounds of the structural formula (I) are antagonists of the 5-HT6 receptor and are useful in the treatment, prevention and suppression of diseases mediated by the 5-HT6 receptor. The compounds of the present invention are useful in the...
03/20/2012
8138197Spirochromanon derivatives
The invention relates to a compound of a general formula (I): wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of benzene, pyrazole, isoxazole, pyridine, indole, 1H-indazole, 1H-furo[2,3-c]pyrazole, 1H-thieno[2,3-c]pyrazol...
03/20/2012
8138164HCV NS3 protease inhibitors
The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections. ...
03/20/2012
8133885Non steroidal glucocorticoid receptor modulators
The present invention relates to compounds having general Formula (I) or a pharmaceutically acceptable salt thereof. The present invention also relates to pharmaceutical compositions comprising said compounds and the use of these derivatives to modulate glucocortico...
03/13/2012
8129413Crystalline forms of MC4R agonist and process for synthesis
The present invention relates to a process for producing N-{(1S)-1-[2-(1-{[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl]carbonyl}piperidin-4-yl)-5-chlorophenyl]ethyl}acetamide, and novel crystalline salts, hydrates, solvates, and polymorphic forms ther...
03/06/2012
8128930Anti-ADDL antibodies and uses thereof
The present invention relates to antibodies that differentially recognize multi-dimensional conformations of Aβ-derived diffusible ligands, also known as ADDLs. The antibodies of the invention can distinguish between Alzheimer's Disease and control human brain extr...
03/06/2012
8124633Hydroxymethyl ether hydroisoindoline tachykinin receptor antagonists
The present invention is directed to certain hydroxymethyl ether hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical ...
02/28/2012
8124628Diaryl substituted alkanes
The instant invention provides compounds of Formula II which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula II are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and...
02/28/2012
8124108Polypeptides for inducing a protective immune response against
The present invention features polypeptides comprising an amino acid sequence structurally related to SEQ ID NO: 1 and uses of such polypeptides. SEQ ID NO: 1 is a truncated derivative of a full-length S. epidermidis polypeptide. The full-length naturally occ...
02/28/2012
8119806Cicletanine derivatives
A compound having the structure wherein X is selected from the group consisting of: a bond, —NHCH2(CH2)nCH2OC(O)—, —CH2NHC(O)CH2
02/21/2012
8119685Disubstituted aniline compounds
The present invention relates to a novel class of disubstituted aniline 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 cel...
02/21/2012
81196812-[1-phenyl-5-hydroxy or methoxy-4alpha-methyl-hexahydrocyclopenta [ƒ]indazole-5-YL]ethyl phenyl derivatives as glucocorticoid receptor ligands
The present invention is directed to 2-[1-phenyl-5-hydroxy or methoxy-4alpha-methyl-hexahydrocyclopenta[f]indazol-5-yl]ethyl phenyl derivatives of formula I (I) as glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases ...
02/21/2012
8119652Aryl-fused spirocyclic compounds
The present invention relates to a novel class of aryl-fused spirocyclic 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 ce...
02/21/2012
8106070Substituted imidazoles as bombesin receptor subtype-3 modulators
Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders ...
01/31/2012
8106034Angiotensin II receptor antagonists
A compound having the structure wherein R is an angiotensin receptor blocking group Y is —(CR1R20)1-7R5, or —C(O)(CR1R
01/31/2012
8105777Methods for diagnosis and/or prognosis of colon cancer
The present invention relates to genetic markers whose expression is correlated with colon cancer. In one aspect, the invention provides sets of markers whose expression can be used for classifying colon cancer patients into different prognostic categories. In anoth...
01/31/2012
8105593Anti-ADDL monoclonal antibody and use thereof
The present invention relates to antibodies that differentially recognize multi-dimensional conformations of Aβ-derived diffusible ligands, also known as ADDLs. The antibodies of the invention can distinguish between Alzheimer's Disease and control human brain extr...
01/31/2012
8101603Tyrosine kinase inhibitors
The present invention relates to 5H-benzo[4,5]cyclohepta[1,2-b]pyridine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention...
01/24/2012
8093389Substituted spirochromanone derivatives
The invention relates to a compound of a general formula (I): wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of indole, 1H-indazole, 2H-indazole, 1H-thieno[2,3-c]pyra...
01/10/2012
8093295Formulations of suberoylanilide hydroxamic acid and methods for producing the same
The present invention provides a pharmaceutical composition or crystalline composition with a specific dissolution profile, which comprises suberoylanilide hydroxamic acid or a pharmaceutically acceptable salt or hydrate thereof as an active ingredient. The present ...
01/10/2012
8080654Macrocyclic quinoxaline compounds as HCV NS3 protease inhibitors
The present invention relates to macrocyclic a compound of formula (I) and its use as inhibitors of the hepatitis C virus (HCV) NS3 protease, and in treating or preventing HCV infections. ...
12/20/2011
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