Search Results - "Wells, Gregory J"

Strategies to Mitigate the Bioactivation of 2-Anilino-7-Aryl-Pyrrolo[2,1-f][1,2,4]triazines: Identification of Orally Bioavailable, Efficacious ALK Inhibitors by Mesaros, Eugen F, Thieu, Tho V, Wells, Gregory J, Zificsak, Craig A, Wagner, Jason C, Breslin, Henry J, Tripathy, Rabindranath, Diebold, James L, McHugh, Robert J, Wohler, Ashley T, Quail, Matthew R, Wan, Weihua, Lu, Lihui, Huang, Zeqi, Albom, Mark S, Angeles, Thelma S, Wells-Knecht, Kevin J, Aimone, Lisa D, Cheng, Mangeng, Ator, Mark A, Ott, Gregory R, Dorsey, Bruce D

“…Chemical strategies to mitigate cytochrome P450-mediated bioactivation of novel 2,7-disubstituted pyrrolo­[2,1-f]­[1,2,4]­triazine ALK inhibitors are described…”
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Allosteric modulators of G protein-coupled receptors by Wells, Gregory J

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Nonpeptide angiotensin II receptor antagonists: the discovery of a series of N-(biphenylylmethyl)imidazoles as potent, orally active antihypertensives by Carini, David J, Duncia, John V, Aldrich, Paul E, Chiu, Andrew T, Johnson, Alexander L, Pierce, Michael E, Price, William A, Santella, Joseph B, Wells, Gregory J

“…A new series of nonpeptide angiotensin II (AII) receptor antagonists has been prepared. These N-(biphenylyl-methyl)imidazoles, e.g…”
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1,2-Benzothiazine 1,1-Dioxide P2−P3 Peptide Mimetic Aldehyde Calpain I Inhibitors by Wells, Gregory J, Tao, Ming, Josef, Kurt A, Bihovsky, Ron

“…A series of peptide mimetic aldehyde inhibitors of calpain I was prepared in which the P2 and P3 amino acids were replaced by substituted…”
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2,7-Disubstituted-pyrrolo[2,1-f][1,2,4]triazines: New Variant of an Old Template and Application to the Discovery of Anaplastic Lymphoma Kinase (ALK) Inhibitors with in Vivo Antitumor Activity by Ott, Gregory R, Wells, Gregory J, Thieu, Tho V, Quail, Matthew R, Lisko, Joseph G, Mesaros, Eugen F, Gingrich, Diane E, Ghose, Arup K, Wan, Weihua, Lu, Lihui, Cheng, Mangeng, Albom, Mark S, Angeles, Thelma S, Huang, Zeqi, Aimone, Lisa D, Ator, Mark A, Ruggeri, Bruce A, Dorsey, Bruce D

“…A novel 2,7-disubstituted-pyrrolo[2,1-f][1,2,4]triazine scaffold has been designed as a new kinase inhibitor platform mimicking the bioactive conformation of…”
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The discovery of potent nonpeptide angiotensin II receptor antagonists: a new class of potent antihypertensives by Duncia, John V, Chiu, Andrew T, Carini, David J, Gregory, George B, Johnson, Alexander L, Price, William A, Wells, Gregory J, Wong, Pancras C, Calabrese, Joseph C, Timmermans, Pieter B. M. W. M

“…A new class of potent antihypertensives has been discovered that exert their effect through blockade of the angiotensin II (AII) receptor. Most AII antagonists…”
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2,7-Pyrrolo[2,1- f][1,2,4]triazines as JAK2 inhibitors: Modification of target structure to minimize reactive metabolite formation by Weinberg, Linda R., Albom, Mark S., Angeles, Thelma S., Breslin, Henry J., Gingrich, Diane E., Huang, Zeqi, Lisko, Joseph G., Mason, Jennifer L., Milkiewicz, Karen L., Thieu, Tho V., Underiner, Ted L., Wells, Gregory J., Wells-Knecht, Kevin J., Dorsey, Bruce D.

“…The JAK2/STAT pathway has important roles in hematopoiesis. With the discovery of the JAK2 V617F mutation and its presence in many patients with…”
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2,7-Disubstituted-Pyrrolotriazine Kinase Inhibitors with an Unusually High Degree of Reactive Metabolite Formation by Wells-Knecht, Kevin J, Ott, Gregory R, Cheng, Mangeng, Wells, Gregory J, Breslin, Henry J, Gingrich, Diane E, Weinberg, Linda, Mesaros, Eugen F, Huang, Zeqi, Yazdanian, Mehran, Ator, Mark A, Aimone, Lisa D, Zeigler, Kelli, Dorsey, Bruce D

“…There are numerous published studies establishing a link between reactive metabolite formation and toxicity of various drugs. Although the correlation between…”
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1,2-Benzothiazine 1,1-dioxide α-ketoamide analogues as potent calpain I inhibitors by BIHOVSKY, Ron, MING TAO, MALLAMO, John P, WELLS, Gregory J

“…A series of potent 1,2-benzothiazine 1,1-dioxide alpha-ketoamide inhibitors of calpain I is described…”
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Synthesis and structure–activity relationships of novel poly(ADP-ribose) polymerase-1 inhibitors by Tao, Ming, Park, Chung Ho, Bihovsky, Ron, Wells, Gregory J., Husten, Jean, Ator, Mark A., Hudkins, Robert L.

“…Pyrrolocarbazole 1 was identified as a potent PARP-1 inhibitor (IC 50 = 36 nM) from our internal database. The synthesis and SAR optimization around this…”
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Synthesis and structure–activity relationships of novel pyrrolocarbazole lactam analogs as potent and cell-permeable inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1) by Wells, Gregory J., Bihovsky, Ron, Hudkins, Robert L., Ator, Mark A., Husten, Jean

“…A series of novel pyrrolocarbazole lactams was identified as potent PARP-1 inhibitors in vitro and in a PC12 cellular NAD + depletion assay. The SAR trends of…”
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Practical synthesis and regioselective alkylation of methyl 4(5)-(pentafluoroethyl)-2-propylimidazole-5(4)-carboxylate to give DuP 532, a potent angiotensin II antagonist by Pierce, Michael E, Carini, David J, Huhn, George F, Wells, Gregory J, Arnett, John F

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Novel Peptidyl Phosphorus Derivatives as Inhibitors of Human Calpain I by Tao, Ming, Bihovsky, Ron, Wells, Gregory J, Mallamo, John P

“…Dipeptidyl phosphorus compounds were synthesized as potential bioisosteric mimics of peptide α-ketoesters and α-ketoacids. α-Ketophosphonate…”
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Silicon in organic synthesis. 26. Expedient synthesis of dicyclopropylideneethane via functionalized 1-(trimethylsilyl)cyclopropanes by Paquette, Leo A, Wells, Gregory J, Wickham, Geoffrey

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Angiotensin II Receptor Antagonists From Discovery to Antihypertensive Drugs by Timmermans, Pieter B.M.W.M, Carini, David J, Chiu, Andrew T, Duncia, John V, Price, William A, Wells, Gregory J, Wong, Pancras C, Wexler, Ruth R, Johnson, Alexander L

“…Some simple JV-benzylimidazoles, originally described by Takeda Chemical Industries (Osaka, Japan), were characterized to be very weak but selective nonpeptide…”
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1,2-Benzothiazine 1,1-Dioxide P 2 −P 3 Peptide Mimetic Aldehyde Calpain I Inhibitors by Wells, Gregory J., Tao, Ming, Josef, Kurt A., Bihovsky, Ron

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Silicon in organic synthesis. 27. A method for the generation of electronegatively substituted cyclopropyl anions under preparatively useful conditions. Aldol condensation with carbonyl partners by Paquette, Leo A, Blankenship, Craig, Wells, Gregory J

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Silicon in organic synthesis. 25. Thermolysis and desiliconation-alkylation of [1-(trimethylsilyl)cyclopropyl]ethylenes as a route to spirocyclic sesquiterpenes by Paquette, Leo A, Yan, Tu Hsin, Wells, Gregory J

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Silicon in organic synthesis. 24. Preparation and selected reactions of functionalized 1-(trimethylsilyl)-substituted cyclopropanes by Wells, Gregory J, Yan, Tu Hsin, Paquette, Leo A

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Electronic control of stereoselectivity. 9. The stereochemical course of electrophilic additions to aryl-substituted benzobicyclo[2.2.2]octadienes by Paquette, Leo A, Bellamy, Francois, Wells, Gregory J, Boehm, Michael C, Gleiter, Rolf

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