Search Results - "Guernon, Jason M"

3-Bromocyclohexane-1,2-dione as a useful reagent for Hantzsch synthesis of thiazoles and the synthesis of related heterocycles by Guernon, Jason M., Wu, Yong-Jin

“…We describe the use of 3-bromocyclohexane-1,2-dione, an air stable, versatile reagent for the Hantzsch thiazole synthesis and the synthesis of other closely…”
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The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu4 PAM development candidate by Panarese, Joseph D., Engers, Darren W., Wu, Yong-Jin, Guernon, Jason M., Chun, Aspen, Gregro, Alison R., Bender, Aaron M., Capstick, Rory A., Wieting, Joshua M., Bronson, Joanne J., Macor, John E., Westphal, Ryan, Soars, Matthew, Engers, Julie E., Felts, Andrew S., Rodriguez, Alice L., Emmitte, Kyle A., Jones, Carrie K., Blobaum, Anna L., Jeffrey Conn, P., Niswender, Colleen M., Hopkins, Corey R., Lindsley, Craig W.

“…[Display omitted] •First description of the SAR that led to the discovery of VU2957 (Valiglurax).•Valiglurax is only the second mGlu4 PAM clinical candidate…”
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Macrocyclic prolinyl acyl guanidines as inhibitors of β-secretase (BACE) by Boy, Kenneth M., Guernon, Jason M., Wu, Yong-Jin, Zhang, Yunhui, Shi, Joe, Zhai, Weixu, Zhu, Shirong, Gerritz, Samuel W., Toyn, Jeremy H., Meredith, Jere E., Barten, Donna M., Burton, Catherine R., Albright, Charles F., Good, Andrew C., Grace, James E., Lentz, Kimberley A., Olson, Richard E., Macor, John E., Thompson, Lorin A.

“…[Display omitted] The synthesis, evaluation, and structure–activity relationships of a class of acyl guanidines which inhibit the BACE-1 enzyme are presented…”
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Identification and Preclinical Evaluation of the Bicyclic Pyrimidine γ‑Secretase Modulator BMS-932481 by Boy, Kenneth M, Guernon, Jason M, Zuev, Dmitry S, Xu, Li, Zhang, Yunhui, Shi, Jianliang, Marcin, Lawrence R, Higgins, Mendi A, Wu, Yong-Jin, Krishnananthan, Subramaniam, Li, Jianqing, Trehan, Ashok, Smith, Daniel, Toyn, Jeremy H, Meredith, Jere E, Burton, Catherine R, Kimura, S. Roy, Zvyaga, Tatyana, Zhuo, Xiaoliang, Lentz, Kimberley A, Grace, James E, Denton, Rex, Morrison, John S, Mathur, Arvind, Albright, Charles F, Ahlijanian, Michael K, Olson, Richard E, Thompson, Lorin A, Macor, John E

“…A triazine hit identified from a screen of the BMS compound collection was optimized for potency, in vivo activity, and off-target profile to produce the…”
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Synthesis of the Spirocyclic Cyclohexadienone Ring System of the Schiarisanrins by Coleman, Robert S, Guernon, Jason M, Roland, Jason T

“…Studies on the synthesis of the spirocyclic cyclohexadienone ring system 2 of the schiarisanrin family of natural products 1 are described and were based on…”
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Monosubstituted γ-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors of β-secretase (BACE) by Boy, Kenneth M., Guernon, Jason M., Shi, Jianliang, Toyn, Jeremy H., Meredith, Jere E., Barten, Donna M., Burton, Catherine R., Albright, Charles F., Marcinkeviciene, Jovita, Good, Andrew C., Tebben, Andrew J., Muckelbauer, Jodi K., Camac, Daniel M., Lentz, Kimberley A., Bronson, Joanne J., Olson, Richard E., Macor, John E., Thompson, Lorin A.

“…The synthesis, evaluation, and structure–activity relationships of a class of γ-lactam 1,3-diaminopropan-2-ol transition-state isostere inhibitors of BACE are…”
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Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors by Thompson, Lorin A., Shi, Jianliang, Decicco, Carl P., Tebben, Andrew J., Olson, Richard E., Boy, Kenneth M., Guernon, Jason M., Good, Andrew C., Liauw, Ann, Zheng, Changsheng, Copeland, Robert A., Combs, Andrew P., Trainor, George L., Camac, Daniel M., Muckelbauer, Jodi K., Lentz, Kimberley A., Grace, James E., Burton, Catherine R., Toyn, Jeremy H., Barten, Donna M., Marcinkeviciene, Jovita, Meredith, Jere E., Albright, Charles F., Macor, John E.

“…The synthesis, evaluation, and structure–activity relationships of a set of related constrained diaminopropane inhibitors of BACE-1 are described. The full in…”
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3-Thio-quinolinone maxi-K openers for the treatment of erectile dysfunction by BOY, Kenneth M, GUERNON, Jason M, STARRETT, John E, SIT, Sing-Yuen, XIE, Kai, HEWAWASAM, Piyasena, BOISSARD, Christopher G, DWORETZKY, Steven I, NATALE, Joanne, GRIBKOFF, Valentin K, LODGE, Nicholas

“…A series of Maxi-K openers for the treatment of erectile dysfunction based on the 3-thio-quinolinone core is described. Significant levels of channel opening…”
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The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu 4 PAM development candidate by Panarese, Joseph D, Engers, Darren W, Wu, Yong-Jin, Guernon, Jason M, Chun, Aspen, Gregro, Alison R, Bender, Aaron M, Capstick, Rory A, Wieting, Joshua M, Bronson, Joanne J, Macor, John E, Westphal, Ryan, Soars, Matthew, Engers, Julie E, Felts, Andrew S, Rodriguez, Alice L, Emmitte, Kyle A, Jones, Carrie K, Blobaum, Anna L, Conn, P Jeffrey, Niswender, Colleen M, Hopkins, Corey R, Lindsley, Craig W

“…This letter describes the first account of the chemical optimization (SAR and DMPK profiling) of a new series of mGlu positive allosteric modulators (PAMs),…”
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Synthesis of 2-aminoethyl-5-carbethoxythiazoles utilizing a Michael-like addition strategy by Boy, Kenneth M., Guernon, Jason M.

“…Ethyl 4-(trifluoromethyl)-2-vinylthiazole-5-carboxylate was utilized as a precursor to ethyl 4-(trifluoromethyl)-2-(aminoethyl)thiazole-5-carboxylate analogs…”
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Monosubstituted I super(3)-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors of I super(2)-secretase (BACE) by Boy, Kenneth M, Guernon, Jason M, Shi, Jianliang, Toyn, Jeremy H, Meredith, Jere E, Barten, Donna M, Burton, Catherine R, Albright, Charles F, Marcinkeviciene, Jovita, Good, Andrew C, Tebben, Andrew J, Muckelbauer, Jodi K, Camac, Daniel M, Lentz, Kimberley A, Bronson, Joanne J, Olson, Richard E, Macor, John E, Thompson, Lorin A

“…The synthesis, evaluation, and structure-activity relationships of a class of I super(3)-lactam 1,3-diaminopropan-2-ol transition-state isostere inhibitors of…”
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