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Assignee: Merck & Co., Inc.


Location: Rahway, NJ
No. of patents: 4515

1                      
NumberTitleIssue Date
8133670Method for making populations of defined nucleic acid molecules
The present invention provides methods of making a population of nucleic acid molecules, wherein each nucleic acid molecule comprises a predetermined nucleic acid sequence, each of said methods comprising the steps of: (a) synthesizing, on a substrate, a population ...
03/13/2012
7569589Potassium channel inhibitors
The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like. ...
08/04/2009
7563815Benzamidazoles, compositions containing such compounds and methods of use
The present invention relates to substituted benzimidazoles, 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 mellitu...
07/21/2009
7560546Tyrosine kinase inhibitors
The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises a...
07/14/2009
7557124Tetrahydropyranyl cyclopentyl tetrahydropyridopyridine modulators of chemokine receptor activity
Compounds of Formula I: (wherein n, R1, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, Y and Z are as defi...
07/07/2009
7553841Amino cyclobutylamide modulators of chemokine receptor activity
The present invention is directed to compounds of the formulas I and II: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R
06/30/2009
7550481Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of Alzheimer's disease
The present invention is directed to phenylamide and pyridylamide derivative compounds of 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. ...
06/23/2009
7550477Inhibitors of checkpoint kinases
The instant invention provides for compounds which comprise fused pyrazoles that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patie...
06/23/2009
RE40794Crystalline forms of carbapenem antibiotics and methods of preparation
A process for preparing a crystalline, carbapenem monosodium salt of formula IIa: characterized by the steps a) adding about 10 to 30% of an organic solvent to an aqueous solution of the carbapenem, b) cooling the resulting solut...
06/23/2009
7544695Spirocyclic compounds
The present invention relates to a novel class of substituted 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 c...
06/09/2009
7544677Inhibitors of Akt activity
The present invention is directed to compounds which contain substituted 5-deazapteridine moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of th...
06/09/2009
7538112HIV integrase inhibitors
Hydroxy-substituted pyrazinopyrrolopyridazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I) wherein R1, R2, R3, R4, R5
05/26/2009
7534918Histone deacetylase inhibitors
This invention relates to hydroxamic acid derivatives having a sulfonamide linkage, that are inhibitors of histone deacetylase (HDAC), and are useful in the prevention and/or treatment of cellular proliferative diseases, for example cancer, autoimmune, allergic and ...
05/19/2009
7534767C-purine nucleoside analogs as inhibitors of RNA-dependent RNA viral polymerase
The present invention provides C-purine nucleoside analogs and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependen...
05/19/2009
7462633Cyclopropyl group substituted oxazolidinone antibiotics and derivatives thereof
This invention relates to new oxazolidinones having a cyclopropyl moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and enterococci, Bacteroides spp., Clostridia spp. species, ...
12/09/2008
7462619Pyridazine, pyrimidine and pyrazine ethyne compounds
In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted or unsubstituted six membered heterocyclic ring that includes at least two nitrogen atoms. The ring additionally inc...
12/09/2008
7456204Cyclohexylglycine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
The present invention is directed to novel cyclohexylglycine derivatives 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 i...
11/25/2008
7456009Adenovirus formulations
The invention relates to viral formulations and related pharmaceutical products for use in gene therapy and/or vaccine applications. Especially preferred viral formulations disclosed herein are liquid adenovirus formulations, which show improved stability when store...
11/25/2008
7452903CGRP receptor antagonists
The present invention is directed to compounds of Formula I: and Formula II: (where variables R1, R2, R3, R4, A, B, G, J, Q, T, U, V, W...
11/18/2008
74528934-cycloakylaminopyrazolo pyrimidine NMDA/NR2B antagonists
Compounds represented by Formula (I) or pharmaceutically acceptable salts thereof, are effective as NMDA/NR2B antagonists useful for treating neurological conditions such as, for example, pain, Parkinson's disease, Alzheimer's disease, epilepsy, depression, anxiety,...
11/18/2008
744611017-Heterocyclic-4-azasteroid derivatives 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...
11/04/2008
7442808Antidiabetic bicyclic compounds
Tricyclic compounds containing a cyclopropyl carboxylic acid or carboxylic acid derivative (e.g. amide) fused to a bicyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful a...
10/28/2008
7435735Hydroxy pyridopyrrolopyrazine dione compounds useful as HIV integrase inhibitors
Hydroxy-substituted pyridopyrrolopyrazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I): (I) wherein a, b, A, B, R1, R2, R3, R4...
10/14/2008
7432414Transgenic mouse having an amyloid precursor protein with a modified beta secretase cleavage site
The present invention provides transgenic animals having an amyloid precursor protein wherein the amino acids flanking the &bgr; secretase cleavage site are NF and EV. The invention also provides tissues and cell lines derived from such animals. The invention furthe...
10/07/2008
7432284Estrogen receptor modulators
The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a v...
10/07/2008
7427380Automated system and method for simultaneously performing a plurality of signal-based assays
An automated detection system includes a robotic fluid handling system for performing a plurality of assays; a detection system for imaging the assays as they are performed; and a computer control, data acquisition, and data analysis system for controlling the opera...
09/23/2008
7423067Diphenyl cyclopentyl amides as cannabinoid-1 receptor inverse agonists
Novel compounds of 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 use...
09/09/2008
7419990Piperidine derivatives as melanocortin-4 receptor agonists
Certain novel piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disor...
09/02/2008
7414055Inhibitors of Akt activity
The present invention is directed to compounds which contain a substituted pyridine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this inven...
08/19/2008
7414110Human calcium channel compositions and methods
Isolated DNA encoding each of human calcium channel α1-, α2-, β- and γ-subunits, including subunits that arise as splice variants of primary transcripts, is provided. Cells and vectors containing the DNA and methods for identifying compound...
08/19/2008
7414057Piperazine urea derivatives as melanocortin-4 receptor agonists
Certain novel piperazine urea derivatives are agonists of the human melanocortin-4 receptor (MC-4R) and, in particular, are receptor-subtype selective agonists of MC-4R. They are useful for the treatment, control, or prevention of diseases and disorders responsive t...
08/19/2008
74109612,6-disubstituted piperiddines as modulators
The present invention is further directed to compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R16, R17, R
08/12/2008
7410976Spirochromanone derivatives
The invention relates to a compound of a formula (I): or a pharmaceutically acceptable salt or ester thereof, useful as a therapeutic agent for various ACC-related disorders. ...
08/12/2008
7411088Stereoselective synthesis of a 4,4-disubstituted cyclohexanepropanoic acid
There is provided stereoselective route to a compound of formula I: wherein R represents H or an alkali metal, Ar1 represents 4-chlorophenyl and Ar2 represents 2,5-difluorophenyl. ...
08/12/2008
7411073Selective non-steroidal glucocorticoid receptor modulators
The present invention encompasses compounds of Formula (I) or pharmaceutically acceptable salts or hydrates thereof, which are useful as novel non-steroidal selective glucocorticoid receptor modulators for treating a variety of autoimmune and inflammatory diseases o...
08/12/2008
7410977Fluorinated 4-azasteroids 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...
08/12/2008
7407772Screening and selection methods for statin drug combinations
A method for screening statins in their open acid form to determine the susceptibility of each tested statin to metabolic glucuronidation is provided. Also provided is a method for determining if a non-statin pharmaceutical drug co-administered with a statin that is...
08/05/2008
7405221Substituted pyrimidines
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...
07/29/2008
7402577Androstane 17-beta-carboxamides as androgen receptor modulators
Compounds of structural formula as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of activating the function of the androgen recepto...
07/22/2008
73997638-hydroxy-1-oxo-tetrahydropyrrolopyrazine compounds useful as HIV integrase inhibitors
8-Hydroxy-1-oxo-tetrahydropyrrolopyrazine compounds are inhibitors of HIV integrase and inhibitors of HIV replication. More particularly, the compounds are of Formula (I): wherein R1, R2, R3, R4, R5 and R6 ...
07/15/2008
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