1
Kevin Rodzinak
Jeannie M Arruda, Brian T Campbell, Nicholas D P Cosford, Jacob M Hoffman, Essa H Hu, Mark E Layton, Yiwei Li, Jun Liang, Kevin J Rodzinak, Tony Siu, Brian A Stearns, Lida R Tehrani, Mark T Bilodeau, Peter J Manley: Inhibitors of Akt activity. Merck Sharp & Dohme, Matthew A Leff, David A Muthard, March 22, 2011: US07910561 (1 worldwide citation)

The present invention is directed to compounds which contain substituted naphthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer ...


2
Jean Michel Vernier, Nicholas D P Cosford, Ian A McDonald: Substituted pyridine compounds useful as modulators of acetylcholine receptors. Merck & Co, David Rubin, David L Rose, October 14, 2003: US06632823 (39 worldwide citation)

In accordance with the present invention, a novel class of substituted pyridine compounds (optionally containing ether, ester, amide, ketone or thioether substitutions) that promote the release of ligands involved in neurotransmission have been discovered. In a particular aspect compounds of the pre ...


3
Mark T Bilodeau, Peter C Chua, Nicholas D P Cosford, Jacob M Hoffman, Johnny Yasuo Nagasawa: Inhibitors of Akt activity. Merck Sharp & Dohme, Matthew A Leff, David A Muthard, February 2, 2010: US07655649 (9 worldwide citation)

The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and method ...


4
Nicholas D P Cosford, Ian A McDonald, Stephen D Hess, Mark A Varney: Methods of modulating processes mediated by excitatory amino acid receptors. Merck & Co, David Rubin, David Rose, October 18, 2005: US06956049 (6 worldwide citation)

In accordance with the present invention, there are provided methods of modulating the activity of excitatory amino acid receptors using a specifically defined class of heterocyclic compounds. In one embodiment, there are provided methods of modulating metabotropic glutamate receptors. The present i ...


5
Mark T Bilodeau, Nicholas D P Cosford, John C Hartnett, Yiwei Li, Jun Liang, Peter J Manley, Lou Anne Neilson, Tony Siu, Zhicai Wu: Inhibitors of Akt activity. Merck & Co, Matthew A Leff, David A Muthard, June 9, 2009: US07544677 (5 worldwide citation)

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 this invention and methods for treat ...


6
Mark T Bilodeau, Chixu Chen, Nicholas D P Cosford, Brian W Eastman, John C Hartnett, Essa H Hu, Peter J Manley, Lou Anne Neilson, Lida R Tehrani, Zhicai Wu: Inhibitors of Akt activity. Merck Sharp & Dohme, Matthew A Leff, David A Muthard, July 6, 2010: US07750151 (4 worldwide citation)

The present invention is directed to compounds which contain substituted napthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer c ...


7
Nicholas D P Cosford, Mark E Layton, Jun Liang, Craig W Lindsley, Philip E Sanderson, Zhijian Zhao: Inhibitors of Akt activity. Merck & Co, Matthew A Leff, David A Muthard, September 15, 2009: US07589068 (4 worldwide citation)

The instant invention provides for 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 ...


8
Nicholas D P Cosford, Chixu Chen, Thomas S Reger, Jeffrey R Roppe, Nicholas D Smith: Heteroaryl substituted tetrazole modulators of metabotrophic glutamate receptor-5. Merck & Co, David Rubin, William Krovatin, August 7, 2007: US07253190 (4 worldwide citation)

Tetrazole compounds substituted directly, or by a bridge, with a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, and panic, ...


9
Mark T Bilodeau, Peter C Chua, Nicholas D P Cosford, Jacob M Hoffman, Johnny Yasuo Nagasawa: Inhibitors of Akt activity. Merck Sharp & Dohme, Matthew A Leff, David A Muthard, August 23, 2011: US08003643 (3 worldwide citation)

The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and method ...


10
Ze ev A Ronai, Anindita Bhoumik, Nicholas D P Cosford, Russell Dahl: Compositions and methods for inhibiting growth and metastasis of melanoma. Burnham Institute for Medical Research, DLA Piper, August 17, 2010: US07776894 (3 worldwide citation)

There are provided methods of inhibiting growth and metastasis of melanoma, methods of sensitizing melanoma cells to apoptosis, and methods of treating a subject having melanoma using acetyl isogambogic acid, celastrol, or a derivative thereof. There are further provided derivatives of celastrol and ...



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