1
Kevin Rodzinak
Vadim Y Dudkin, Mark E Fraley, Kenneth L Arrington, Mark E Layton, Alexander J Reif, Kevin J Rodzinak, Joseph E Pero: Positive allosteric modulators of MGLUR2. Merck Sharp & Dohme, Keith D MacMillan, John C Todaro, March 31, 2015: US08993779 (1 worldwide citation)

The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involve ...


2
Jose Luis Castro Pineiro, Timothy Harrison, Peter Alan Hunt, Alan John Nadin: Gamma-secretase inhibitors. Merck Sharp & Dohme, John C Todaro, Melvin Winokur, June 29, 2004: US06756511 (30 worldwide citation)

Gamma-secretase inhibitors, useful in the treatment or prevention of Alzheimer's disease, are disclosed. The preferred compounds have, as the central portion of the molecule, the structure (a) and are di-astereoisomers of known protease inhibitors.


3
Craig A Coburn, Shawn J Stachel, Joseph P Vacca: Phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimers disease. Merck & Co, John C Todaro, Melvin Winokur, September 19, 2006: US07109217 (28 worldwide citation)

Disclosed are compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease and pharmaceutical compositions comprising these compounds and the use o ...


4
Craig A Coburn, Shawn J Stachel, Joseph P Vacca, Harold G Selnick: N-alkyl phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimers disease. Merck Co, William Krovatin, John C Todaro, November 6, 2007: US07291620 (25 worldwide citation)

The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and which are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions ...


5
Shubh D Sharma: Structurally determined metallo-constructs and applications. RhoMed Incorporated, Stephen A Slusher, John C Todaro, Deborah A Peacock, February 22, 2000: US06027711 (21 worldwide citation)

A metallo-construct, which may be a peptide, is provided for use as a biological, therapeutic, diagnostic imaging, or radiotherapeutic agent, and for use in library or combinatorial chemistry methods. The construct has a conformationally constrained global secondary structure obtained upon complexin ...


6
Philippe G Nantermet, Hemaka Anthony Rajapakse, Harold G Selnick: Phenylcarboxylate beta-secretase inhibitors for the treatment of alzheimers disease. Merck & Co, William Krovatin, John C Todaro, March 25, 2008: US07348448 (16 worldwide citation)

The present invention is directed to 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 also directed to pharmaceutical compositions comprising thes ...


7
Alan John Nadin, Graeme Irvine Stevenson: Gamma-secretase inhibitors. Merck Sharp & Dohme, John C Todaro, Melvin Winokur, January 10, 2006: US06984626 (16 worldwide citation)

A class of compounds is disclosed which are diasteroisomers of a known class of protease inhibitors. The compound inhibit gamma-secretase, and find use in the treatment of and/or prevention of Alzheimer's disease.


8
Jose Luis Castro Pineiro, Ian Churcher, Alexander Richard Guiblin, Timothy Harrison, Sonia Kerrard, Andrew Madin, Alan John Nadin, Andrew Pate Owens, Timothy Jason Sparey, Martin Richard Teall, Susannah Williams: Benzodiazepine derivatives as APP modulators. Merck Sharp & Dohme, John C Todaro, Melvin Winokur, September 12, 2006: US07105509 (15 worldwide citation)

A novel class of 1,4- and 1,5-benzodiazepines of formula (I) is disclosed. The compounds modulate the processing of amyloid precursor protein by γ-secretase, and hence find use in the treatment or prevention of conditions associated with the deposition of β-amyloid, such as Alzheimer's disease


9
Craig A Coburn, Shawn J Stachel, Joseph P Vacca: Macrocyclic β-secretase inhibitors for the treatment of Alzheimers disease. Merck & Co, William Krovatin, John C Todaro, May 13, 2008: US07371853 (15 worldwide citation)

The present invention is directed to compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention of diseases in which the beta-secretase enzyme in involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical ...


10
Theresa M Williams, Christopher S Burgey, Thomas J Tucker, Craig A Stump, Ian M Bell: Carboxamide spirolactam CGRP receptor antagonists. Merck & Co, John C Todaro, William Krovatin, June 24, 2008: US07390798 (15 worldwide citation)

The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c 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 a ...



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