Patents by Inventor Nicholas D. P. Cosford
Nicholas D. P. Cosford has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Publication number: 20120071503Abstract: The disclosure provides compounds and compositions, and methods of using these compounds and compositions, as positive allosteric modulators of the metabotropic glutamate subtype 2 (mGlu2) receptor, and for treating CNS disorders associated with the mGlu2 receptor including schizophrenia, anxiety, addiction, e.g. cocaine addiction, nicotine addiction, and the like.Type: ApplicationFiled: March 18, 2011Publication date: March 22, 2012Applicant: Sanford-Burnham Medical Research InstituteInventors: Nicholas D. P. Cosford, Dhanya Raveendra Panickar, Shyama Sidique
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Publication number: 20110257233Abstract: The disclosure provides new compounds and compositions thereof, and methods for treating or ameliorating a disorder relating to CDG-Ia. In particular, the disclosure provides benzoisothiazolone inhibitors of PMI, which have been synthesized and their ability to drive glycosylation has been demonstrated. The disclosure provides two synthetic routes for these compounds, including a new copper-catalyzed N-arylation reaction amenable to parallel derivitization. The disclosed compounds represent potent inhibitors of PMI, and their dose-dependent efficacy in cell-based models of glycosylation have been demonstrated. In addition, the disclosed compounds are selective over PMM and therefore, are useful in treating or ameliorating a disorder relating to CDG-Ia.Type: ApplicationFiled: March 18, 2011Publication date: October 20, 2011Applicant: Sanford-Burnham Medical Research InstituteInventors: Nicholas D. P. Cosford, Hudson H. Freeze, Russell Dahl, Yalda Bravo, Vandana Sharma, Mie Ichikawa
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Patent number: 8003643Abstract: 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 methods for treating cancer comprising administration of the compounds of the invention.Type: GrantFiled: November 18, 2009Date of Patent: August 23, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Mark T. Bilodeau, Peter C. Chua, Nicholas D. P. Cosford, Jacob M. Hoffman, Johnny Yasuo Nagasawa
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Publication number: 20110166216Abstract: 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 compositions comprising acetyl isogambogic acid, celastrol, or a derivative thereof.Type: ApplicationFiled: February 4, 2011Publication date: July 7, 2011Inventors: Ze'ev A. Ronai, Anindita Bhoumik, Nicholas D. P. Cosford, Russell Dahl
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Patent number: 7910561Abstract: 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 comprising administration of the compounds of the invention. These substituted naphthyridines have unexpected advantageous properties when compared to other naphthyridines reported in PCT publication WO2003/086394, such unexpected advantageous properties may include increased cellular potency/solubility, greater selectivity, enhanced pharmacokinetic properties, lack of off target activity and so on.Type: GrantFiled: December 9, 2005Date of Patent: March 22, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: 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
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Patent number: 7888355Abstract: 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 compositions comprising acetyl isogambogic acid, celastrol, or a derivative thereof.Type: GrantFiled: August 11, 2010Date of Patent: February 15, 2011Assignee: Burnham Institute for Medical ResearchInventors: Ze′ev A. Ronai, Anindita Bhoumik, Nicholas D. P. Cosford, Russell Dahl
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Publication number: 20100305129Abstract: 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 compositions comprising acetyl isogambogic acid, celastrol, or a derivative thereof.Type: ApplicationFiled: August 11, 2010Publication date: December 2, 2010Applicant: Burnham Institute for Medical ResearchInventors: Zéev A. Ronai, Anindita Bhoumik, Nicholas D.P. Cosford, Russell Dahl
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Patent number: 7776894Abstract: 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 compositions comprising acetyl isogambogic acid, celastrol, or a derivative thereof.Type: GrantFiled: August 15, 2008Date of Patent: August 17, 2010Assignee: Burnham Institute for Medical ResearchInventors: Ze'ev A. Ronai, Anindita Bhoumik, Nicholas D. P. Cosford, Russell Dahl
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Patent number: 7750151Abstract: 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 comprising administration of the compounds of the invention.Type: GrantFiled: April 5, 2005Date of Patent: July 6, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: 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
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Publication number: 20100075970Abstract: 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 methods for treating cancer comprising administration of the compounds of the invention.Type: ApplicationFiled: November 18, 2009Publication date: March 25, 2010Inventors: Mark T. Bilodeau, Peter C. Chua, Nicholas D.P. Cosford, Jacob M. Hoffman, Johnny Yasou Nagasawa
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Patent number: 7655649Abstract: 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 methods for treating cancer comprising administration of the compounds of the invention.Type: GrantFiled: April 5, 2005Date of Patent: February 2, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Mark T. Bilodeau, Peter C. Chua, Nicholas D. P. Cosford, Jacob M. Hoffman, Johnny Yasuo Nagasawa
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Patent number: 7592337Abstract: Tetrazole compounds substituted directly, or by a bridge, with i) a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl and ii) another heteroaryl or aryl ring, with at least one of the rings being further substituted with another ring, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, panic, and bipolar disorder, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal, obesity and other diseases.Type: GrantFiled: March 7, 2003Date of Patent: September 22, 2009Assignee: Merck & Co., Inc.Inventors: Chixu Chen, Nicholas D. P. Cosford, Brian W. Eastman, Dehua Huang, Steve F. Poon, Thomas S. Reger, Jeffrey R. Roppe, Nicholas D. Smith
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Patent number: 7589068Abstract: 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 the compound to a patient in need of treatment of cancer.Type: GrantFiled: February 10, 2006Date of Patent: September 15, 2009Assignee: Merck & Co., Inc.Inventors: Nicholas D. P. Cosford, Mark E. Layton, Jun Liang, Craig W. Lindsley, Philip E. Sanderson, Zhijian Zhao
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Patent number: 7569592Abstract: Pyrazole 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, bipolar disorder and panic, as well as in the treatment of pain, circadian rhythm disorders, and other diseases.Type: GrantFiled: December 13, 2002Date of Patent: August 4, 2009Assignee: Merck & Co., Inc.Inventors: Nicholas D. P. Cosford, Chixu Chen, Brian W. Eastman, Dehua Huang, Benito Munoz, Petpiboon Prasit, Nicholas D. Smith
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Patent number: 7544677Abstract: 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 treating cancer comprising administration of the compounds of the invention.Type: GrantFiled: August 19, 2005Date of Patent: June 9, 2009Assignee: Merck & Co., Inc.Inventors: Mark T. Bilodeau, Nicholas D. P. Cosford, John C. Hartnett, Yiwei Li, Jun Liang, Peter J. Manley, Lou Anne Neilson, Tony Siu, Zhicai Wu
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Publication number: 20090131384Abstract: The invention provides novel compounds, methods for treating or preventing a condition related to ER-stress, e.g. hypercholesterolemia, atherosclerosis and related conditions, and pharmaceutical compositions related thereto.Type: ApplicationFiled: March 22, 2007Publication date: May 21, 2009Applicant: SYNDEXA PHARMACEUTICALS CORPORATIONInventors: Teoman Uysal, Nicholas D.P. Cosford
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Publication number: 20090054438Abstract: 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 compositions comprising acetyl isogambogic acid, celastrol, or a derivative thereof.Type: ApplicationFiled: August 15, 2008Publication date: February 26, 2009Applicant: Burnham Institute for Medical ResearchInventors: Ze'ev A. Ronai, Anindita Bhoumik, Nicholas D.P. Cosford, Russell Dahl
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Publication number: 20080287457Abstract: 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 comprising administration of the compounds of the invention. These substituted naphthyridines have unexpected advantageous properties when compared to other naphthyridines reported in PCT publication WO2003/086394, such unexpected advantageous properties may include increased cellular potency/solubility, greater selectivity, enhanced pharmacokinetic properties, lack of off target activity and so on.Type: ApplicationFiled: December 9, 2005Publication date: November 20, 2008Inventors: 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
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Publication number: 20080280889Abstract: 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 methods for treating cancer comprising administration (if the compounds of the invention.Type: ApplicationFiled: April 5, 2005Publication date: November 13, 2008Inventors: Mark T. Bilodeau, Peter C. Chua, Nicholas D.P. Cosford, Jacob M. Hoffman, Johnny Yasuo Nagasawa
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Publication number: 20080280899Abstract: 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 comprising administration of the compounds of the invention.Type: ApplicationFiled: April 5, 2005Publication date: November 13, 2008Inventors: 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