Assignee: Merck Sharp & Dohme Corp.

Location: Rahway, NJ
No. of patents: 394

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Number	Title	Issue Date
8445680	Tetrahydrothieno pyridines The present invention relates to tetrahydrothienopyridine compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions. ...	05/21/2013
8445538	Glucagon receptor antagonist compounds 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. ...	05/21/2013
8445499	Bipiperidinyl compounds, compositions, containing such compounds and methods of treatment Bipiperidinyl compounds of the formula: are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are usefu...	05/21/2013
8445480	CETP inhibitors derived from benzoxazole arylamides Compounds having the structure of Formula I1 including pharmaceutically acceptable salts of the compounds, are potent CETP (cholesterol ester transfer protein) inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or prev...	05/21/2013
8440702	1,3-oxazolidin -2-one derivatives useful as CETP inhibitors Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. The compounds have 3...	05/14/2013
8440672	Diphenyl substituted alkanes The instant invention provides compounds of Formula I which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula (I) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents. ...	05/14/2013
8440443	MEK1 polypeptides The present invention provides, inter alia, crystals of the MEK1 polypeptide which are particularly useful for structure based drug design as well as methods of use thereof. ...	05/14/2013
8436185	Pharmaceutically acceptable salts of 2-{4-[(3)-piperidin-3-yl]phenyl}-2-indazole-7-carboxamide The present invention relates to pharmaceutically acceptable salts of an amide substituted indazole which are inhibitors of the enzyme poly(ADP-ribose)polymerase (PARP), previously known as poly(ADP-ribose)synthase and poly(ADP-ribosyl) transferase. The compounds of...	05/07/2013
8436015	Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use Glucagon receptor antagonist compounds of formula I are disclosed: The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included. ...	05/07/2013
8435994	Substituted [1,2,4]triazolo[4,3-alpha]quinoxalines as adenosine A2a receptor antagonists The present invention relates to certain fused tricyclic heteroaryl rings compounds of the Formula (I) (also referred to herein as the “Fused Tricyclic Compounds”), wherein M, Q, U, W, X, Y, Z, R1, R2, and R3, and rings C and D a...	05/07/2013
RE44205	Adenosine Areceptor antagonists Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alky...	05/07/2013
8431569	Inhibitors of janus kinases The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK...	04/30/2013
8426581	RNA interference mediated inhibition of the FCεR1α gene The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of FCεR1α gene expression and/or activity, and/or modulate a FCεR1α gene expression pa...	04/23/2013
8426573	Nucleic acids encoding TNFγ Nucleic acids encoding mammalian, e.g., primate or rodent, genes, purified proteins and fragments thereof. Antibodies, both polyclonal and monoclonal, are also provided. Methods of using the compositions for both diagnostic and therapeutic utilities are provided.	04/23/2013
8426438	Heterocyclic-fused pyrazolo[4,3-]pyridin-3-one M1 receptor positive allosteric modulators The present invention is directed to heterocyclic fused pyrazole[4,3-c]pyridine-3-one 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 Alzhei...	04/23/2013
8426413	Diaryl 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...	04/23/2013
8420695	Inhibitors of janus kinases The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2). The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 a...	04/16/2013
8420122	Process for the precipitation and isolation of 6,6-dimethyl-3-aza-bicyclo [3.1.0] hexane-amide compounds by controlled precipitation and pharmaceutical formulations containing same The present invention provides a method of continuous precipitation and isolation of an amorphous solid particulate form of 3-[2-(3-tert-Butyl-ureido)-3,3-dimethyl-butyryl]-6,6-dimethyl-3-aza-bicyclo[3.1.0]hexane-2-carboxylic acid (2-carbamoyl-1-cyclobutylmethyl-2-o...	04/16/2013
8420093	Anti-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...	04/16/2013
8415460	Methods of making antibodies specific for cysteine-rich soluble protein C23 Nucleic acids encoding a new family of small cysteine rich soluble proteins, from a mammal, reagents related thereto, including specific antibodies, and purified proteins are described. Methods of using said reagents and related diagnostic kits are also provided.	04/09/2013
8415353	Amino-quinoxaline and amino-quinoline compounds for use as adenosine Areceptor antagonists Compounds of the Formula (I), where W represents CH or N; and Q represents —CN, —C(═NOH)NH2, —CONHR1 or various herein described heterocyclic radicals; as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof ...	04/09/2013
8415346	Inhibitors of Janus kinases The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2). The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 a...	04/09/2013
8415297	Aminotetrahydropyrans 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...	04/09/2013
8414921	Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with metformin Disclosed are pharmaceutical compositions comprising fixed-dose combinations of a dipeptidyl peptidase-4 inhibitor and metformin, methods of preparing such pharmaceutical compositions, and methods of treating Type 2 diabetes with such pharmaceutical compositions.	04/09/2013
8410142	Bipyridine carboxamide orexin receptor antagonists The present invention is directed to bipyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The inv...	04/02/2013
8410122	Bicyclic heterocycle derivatives and methods of use thereof The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascul...	04/02/2013
8410111	Hexahydro-1H-4,7-methanoisoindole-1,3-dione compounds The present invention is directed to therapeutic agents which are atypical antipsychotics and which are useful in the treatment of neurological and psychiatric disorders associated with dopamine D2 and serotonin 5-HT2A neurotransmission dysfunction. ...	04/02/2013
8404856	Non-nucleoside reverse transcriptase inhibitors Heteroaromatic compounds of Formula (I) are HIV reverse transcriptase inhibitors, wherein ring A is: (ii-a), (ii-b), (ii-c), (ii-d), or (ii-e); and wherein n, L, M, U, X, Y, Z, RE, RF, R1, R2A, R2B, R2C	03/26/2013
8404845	2,3-substituted azaindole derivatives for treating viral infections The present invention relates to 2,3-Substituted Azaindole Derivatives, compositions comprising at least one 2,3-Substituted Azaindole Derivatives, and methods of using the 2,3-Substituted Azaindole Derivatives for treating or preventing a viral infection or a virus...	03/26/2013
8404813	Engineered anti-IL-23P19 antibodies Engineered antibodies to human IL-23p19 are provided, as well as uses thereof, e.g. in treatment of inflammatory, autoimmune, and proliferative disorders. ...	03/26/2013
8399507	Antidiabetic tricyclic compounds Tricyclic compounds containing a cyclopropanecarboxylic acid fused to a bicyclic ring, including pharmaceutically acceptable salts, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2...	03/19/2013
8399494	2,5-disubstituted phenyl carboxamide orexin receptor antagonists The present invention is directed to 2,5-disubstituted phenyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are in...	03/19/2013
8399485	Acyl bipiperidinyl compounds useful as GPR 119 agonists Bipiperidyl compounds of the formula: (I) are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled re...	03/19/2013
8399480	Hydroxymethyl pyrrolidines as beta 3 adrenergic receptor agonists The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of β3-adrenoceptor. ...	03/19/2013
8399248	Methods of using MIR34 as a biomarker for TP53 functional status In one aspect, the invention generally relates to use of miR-34 as a biomarker to estimate TP53 function in a cell. In another aspect, the invention generally relates to multiple uses of miR-34 and siRNAs functionally and structurally related to miR-34 for the treat...	03/19/2013
8394969	Cyclic benzimidazole derivatives useful as anti-diabetic agents Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatme...	03/12/2013
8394960	Thiazole carboxamide derivatives and their use to treat cancer The present invention relates to novel Heterocyclic Ether or Thioether Derivatives, compositions comprising the Heterocyclic Ether or Thioether Derivatives, and methods for using the Heterocyclic Ether or Thioether Derivatives for treating or preventing a proliferat...	03/12/2013
8394819	Indole derivatives as CRTH2 receptor antagonists Compound of formula I are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-mediated diseases such as asthma. ...	03/12/2013
8392127	Methods and gene expression signature for assessing growth factor signaling pathway regulation status Methods, biomarkers, and expression signatures are disclosed for assessing the regulation status of growth factor pathway signaling in a cell sample or subject. More specifically, several aspects of the invention provide a set of genes which can be used as biomarker...	03/05/2013
8389720	Quinolone neuropeptide S receptor antagonists The present invention is directed to quinolone compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. T...	03/05/2013

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Assignee: Merck Sharp & Dohme Corp.