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
Kevin Rodzinak
Jeannie M Arruda, Brian T Campbell, Nicholas DP 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 And Co, November 20, 2008: US20080287457-A1

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 ...


3
Theresa M Williams, Terrence M Ciccarone, Walfred S Saari, John S Wai, William J Greenlee, Suresh K Balani, Mark E Goldman, Anthony D Theoharides deceased, Jacob M Hoffman Jr, William C Lumma Jr, Joel R Huff, Clarence S Rooney, Philip E Sanderson: Inhibitors of HIV reverse transcriptase. Merck & Co, Carol S Quagliato, Roy D Meredith, Charles M Caruso, June 18, 1996: US05527819 (38 worldwide citation)

Novel indole compounds inhibit HIV reverse transcriptase, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, ...


4
Jacob M Hoffman Jr, Walfred S Saari, Clarence S Rooney, John S Wai: Inhibitors of HIV reverse transcriptase. Merck & Co, Roy D Meredith, Jack L Tribble, May 3, 1994: US05308854 (34 worldwide citation)

Novel aminopyridones inhibit HIV reverse transcriptase, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, an ...


5
William A Bolhofer, Edward J Cragoe Jr, Jacob M Hoffman Jr: Cyclic imidazole cyanoguanidines. Merck & Co, David L Rose, Harry E Westlake, September 2, 1980: US04220654 (26 worldwide citation)

There are disclosed novel compounds described as imidazole cyanoguanidines in which the imidazole moiety is connected to the cyanoguanidine moiety through a cyclic group which may optionally contain one or two alkylene linkages. The cyclic groups may be phenyl, cyclohexyl, thienyl and the like. Proc ...


6
William A Bolhofer, Edward J Cragoe Jr, Jacob M Hoffman Jr: Pyridinyl ureas and pharmaceutical use. Merck & Co, David L Rose, Harry E Westlake, May 20, 1980: US04203988 (25 worldwide citation)

Compounds of the formula ##STR1## have been found to inhibit gastric secretion in mammalian species.


7
Jacob M Hoffman, Raymond S L Chang: .alpha..sub.1a adrenergic receptor antagonists. Merck & Co, Kenneth R Walton, Melvin Winokur, August 1, 2000: US06096763 (21 worldwide citation)

This invention relates to novel compounds, their synthesis and use as selective .alpha..sub.1a adrenergic receptor antagonists. One application of the compounds is in the treatment of benign prostatic hyperplasia. The compounds are selective in their ability to relax smooth muscle tissue enriched in ...


8
William A Bolhofer, Edward J Cragoe Jr, Jacob M Hoffman Jr: Substituted naphthyridinones. Merck & Co, David L Rose, Harry E Westlake, January 9, 1979: US04133885 (21 worldwide citation)

Organic chemical compounds based upon the naphthyridine molecule are disclosed which have potent gastric secretion inhibitory properties. The naphthyridinone is substituted with a substituted amino alkyl group at the 1-position, and variously substituted at the remaining positions. The compounds hav ...


9
Mark W Embrey, John S Wai, Debra S Perlow, Jacob M Hoffman: Inhibitors of prenyl-protein transferase. Merck & Co, Dianne Pecoraro, Mark R Daniel, January 9, 2001: US06172076 (17 worldwide citation)

The present invention is directed to conformationally constrained compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiti ...


10
Jacob M Hoffman, Mark G Bock, Robert M DiPardo, Linda S Payne, Michael A Patane: Arylhydantoin derivatives and uses thereof. Merck & Co, Baerbel R Brown, Kenneth R Walton, Catherine D Fitch, August 20, 2002: US06436962 (16 worldwide citation)

Arylhydantoin derivatives and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds a ...