Assignee: Merck & co., Inc.

Location: Rahway, NJ
No. of patents: 154

Number	Title	Issue Date
7893081	Tyrosine kinase inhibitors This invention relates to salt forms of the compound N-[(2R)-1,4-dioxan-2-ylmethyl]-N-methyl-N′-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]sulfamide, an inhibitor of tyrosine kinases, in particular the receptor tyrosine kinase M...	02/22/2011
7820680	HIV integrase inhibitors Bicyclic uracils and related compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the compounds are of Formula I: wherein a, b, Y, R1, R2, R3 and R...	10/26/2010
7811563	Anti-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...	10/12/2010
7807829	Process for {3-[2()-[(1)-1-[3,5-bis(trifluoromethyl) phenyl]ethoxy]-3()-(4-fluorophenyl)morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonic acid The present invention is concerned with a process for the preparation of the compound {3-[2(R)-[(1R)-1-[3,5-bis(tri-fluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)-morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonic acid, and pharmaceutically ...	10/05/2010
7786287	Hepatitis C virus assay systems The present invention features assays employing a beta-lactamase reporter system, an HCV replicon enhanced cell, and/or a chimeric HCV replicon containing a 3′ UTR based on the HCV-1a 3′ UTR. These features can be employed alone or together, and are preferably c...	08/31/2010
7780963	Anti-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...	08/24/2010
7767399	Purification process for plasmid DNA Methods of isolating clinical-grade plasmid DNA from manufacturing processes, including large-scale fermentation regimes, are disclosed which encompass alternatives to two core unit operations common to plasmid DNA purification processes. The novel upstream and down...	08/03/2010
7763634	Inhibitors of janus kinases The instant invention provides for tetracyclic 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 ...	07/27/2010
7756644	System and method for automated selection of T-cell epitopes Methodology for the automated selection and/or optimization of T-cell epitopes is disclosed. The invention provides a data processing system which utilizes sequence-based statistical pattern recognition to compute an epitope selection matrix based on the information...	07/13/2010
7754213	High affinity antibody antagonists of interleukin-13 receptor alpha 1 High affinity antibody antagonists of human interleukin-13 receptor alpha 1 are disclosed. The antibody molecules are effective in the inhibition of IL-13Rα1-mediated activities and, accordingly, present desirable antagonists for the use in the treatment of conditi...	07/13/2010
7745639	Mitotic kinesin inhibitors 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 com...	06/29/2010
7744887	Human antibodies interacting with HIV gp41 Human scFvs are disclosed which interact with a conformational epitope along the pre-hairpin, N-helix coiled coil structure within the heptad repeat 1 (HR1) region of gp41 of HIV. These antibodies, as well as IgG conversions, are shown to neutralize diverse HIV isol...	06/29/2010
7732472	Mitotic kinesin inhibitors The present invention relates to dihydroisoxazoles that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise th...	06/08/2010
7731962	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...	06/08/2010
7723365	Mitotic kinesin inhibitors The present invention relates to oxadiazoles that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these co...	05/25/2010
7714021	Pyrrolidin-3-yl compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease The present invention is directed to pyrrolidin-3-yl derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is...	05/11/2010
7704988	Anti-hypercholesterolemic compounds 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 cholest...	04/27/2010
7700591	Benzoxazinyl-amidocyclopentyl-heterocyclic modulators of chemokine receptors Cyclopentyl compounds linked to a benzoxazinyl group through an amido moiety utilizing the ring nitrogen of the benzoxazine, and further substituted with a heterocyclic moiety, such compounds represented by formula I: which...	04/20/2010
7700103	Optimized expression of HPV 52 L1 in yeast Synthetic DNA molecules encoding the HPV 52 L1 protein are provided. Specifically, the present invention provides polynucleotides encoding HPV 52 L1 protein, wherein said polynucleotides are codon-optimized for high level expression in a yeast cell. In alternative e...	04/20/2010
7700099	Non-immunostimulatory antibody and compositions containing the same The present invention relates to a non-immunostimulatory antibody which lacks antibody-dependent cell-mediated cytotoxicity, Fc gamma receptor binding and complement-mediated cytotoxicity. In some embodiments, the antibody contains a modified immunoglobulin G2 (IgG2...	04/20/2010
7687541	Prodrugs of diaryl-2-(5H)-furanone cyclooxygenase-2 inhibitors The invention encompasses the novel compounds of Formula (I) and Formula (II), which are prodrugs that convert in vivo to diaryl-2-(5H)-furanones useful in the treatment of cyclooxygenase-2 mediated diseases. These prodrugs are far more soluble in aqueous media than...	03/30/2010
7667053	Bicyclic amides Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are...	02/23/2010
7666862	Mitotic Kinesin Inhibitors The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention is also related to compositions which c...	02/23/2010
7659294	2-(aryl)azacyclylmethyl carboxylates, sulfonates, phosphonates, phosphinates and heterocycles as S1P receptor agonists The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts thereof. The compounds are S1P1/Edg1 receptor agonists and thus have immunosuppressive, anti-inflammatory...	02/09/2010
7652049	CETP inhibitors Compounds having the structures 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: ...	01/26/2010
7649009	Pyrazole amide derivatives, compositions containing such compounds and methods of use Pyrazole amides are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included. ...	01/19/2010
7638530	Inhibitors of Akt activity The present invention is directed to compounds which contain a five-membered heterocyclic ring fused to a substituted pyridine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic composit...	12/29/2009
7632833	Mitotic kinesin inhibitors The present invention relates to tricyclic pyrazoles according to Formula (I) that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to com...	12/15/2009
7632832	CGRP receptor antagonists Compounds of Formula I: (where variables R1, R2, R3, R7, G, J, Q, T, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster...	12/15/2009
7632821	Ribonucleoside cyclic acetal derivatives for the treatment of RNA-dependent RNA viral infection The present invention provides ribonucleoside 2′,3′-cyclic acetals of structural formula I which are precursors or prodrugs of inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors of inhibitors of RNA-dependent RNA viral replication a...	12/15/2009
7629470	Formation of tetra-substituted enamides and stereoselective reduction thereof The present invention is directed to a practical process for the preparation of an enamide (II) by palladium catalyzed coupling of a primary amide (IV) with a compound of structural formula (III), as shown below: As well as to crystalline forms of a compound produce...	12/08/2009
7629467	Diphenyl substituted cycloalkanes, compositions containing such compounds and methods of use 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.	12/08/2009
7629372	Compounds for the treatment of dyslipidemia and other lipid disorders 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 r...	12/08/2009
7629367	-(2-benzyl)-2-phenylbutanamides as androgen receptor modulators Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorat...	12/08/2009
7629338	Substituted monocyclic CGRP receptor antagonists Compounds of formula I: (wherein variables A1, A2, A3, A4, m, n, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, R	12/08/2009
7625938	Substituted pyrazoles, compositions containing such compounds and methods of use 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.	12/01/2009
7625937	1H-benzo[F]indazol-5-YL derivatives as selective glucocorticoid receptor modulators 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 infl...	12/01/2009
7625933	Indoles having anti-diabetic activity 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 thia...	12/01/2009
7625920	Fluorinated 4-azasteroid derivatives as androgen receptor modulators 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 uteru...	12/01/2009
7625919	4-azasteroid derivatives as androgen receptor modulators 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 uteru...	12/01/2009

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Assignee: Merck & co., Inc.