Search Results - "ANDISIK, Donald"

Efficient synthesis of a 7-azabicyclo[2.2.1]heptane based GlyT1 uptake inhibitor by Xiong, Hui, Frietze, William, Andisik, Donald W., Ernst, Glen E., Palmer, William E., Hinkley, Lindsay, Varnes, Jeffrey G., Albert, Jeffrey S., Veale, Chris A.

“…Generation and subsequent electrophilic reaction of a Boc-protected azabicyclo[2.2.1]heptane anion led to efficient preparation of the potent GlyT1 uptake…”
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4-Piperidin-4-ylidenemethyl-benzamides as δ-opioid receptor agonists for CNS indications: Identifying clinical candidates by Dantzman, Cathy L., King, Megan M., Ernst, Glen E., Wang, Xia, McCauley, John P., Andisik, Donald W., Brush, Kelly, Bui, Khanh H., Frietze, William, Hoesch, Valerie, Liu, Jay, Palmer, William E., Spear, Nathan, Hudzik, Thomas J., Wesolowski, Steven S.

“…A series of 4-piperidin-4-ylidenemethyl-benzamide δ-opioid receptor agonists is described with an emphasis on balancing the potency, subtype selectivity and in…”
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Multiparameter exploration of piperazine derivatives as δ-opioid receptor agonists for CNS indications by McCauley, John P., Dantzman, Cathy L., King, Megan M., Ernst, Glen E., Wang, Xia, Brush, Kelly, Palmer, William E., Frietze, William, Andisik, Donald W., Hoesch, Valerie, Doring, Kenneth, Hulsizer, James, Bui, Khanh H., Liu, Jay, Hudzik, Thomas J., Wesolowski, Steven S.

“…A novel series of piperazine derivatives exhibits sub-nanomolar binding and enhanced subtype selectivity as δ-opioid agonists. The synthesis and SAR are…”
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Design, Synthesis, and SAR of Tachykinin Antagonists:  Modulation of Balance in NK1/NK2 Receptor Antagonist Activity by Albert, Jeffrey S, Aharony, David, Andisik, Donald, Barthlow, Herbert, Bernstein, Peter R, Bialecki, Russell A, Dedinas, Robert, Dembofsky, Bruce T, Hill, Daniel, Kirkland, Karin, Koether, Gerard M, Kosmider, Benedict J, Ohnmacht, Cyrus, Palmer, William, Potts, William, Rumsey, William, Shen, Lihong, Shenvi, Ashok, Sherwood, Scott, Warwick, Paul J, Russell, Keith

“…Through optimization of compounds based on the dual NK1/NK2 antagonist ZD6021, it was found that alteration of two key regions could modulate the balance of…”
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Naphtho[2,1-b][1,5] and [1,2-f][1,4]oxazocines as selective NK1 antagonists by OHNMACHT, Cyrus J, ALBERT, Jeffrey S, BERNSTEIN, Peter R, RUMSEY, William L, MASEK, Brian B, DEMBOFSKY, Bruce T, KOETHER, Gerard M, ANDISIK, Donald W, AHARONY, David

“…Previously we reported on the synthesis and properties of a series of highly potent piperidinyl 2-subsituted-3-cyano-1-naphthamide NK1 antagonists that…”
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Design, synthesis, and kinetic evaluation of a unique class of elastase inhibitors, the peptidyl .alpha.-ketobenzoxazoles, and the x-ray crystal structure of the covalent complex between porcine pancreatic elastase and Ac-Ala-Pro-Val-2-benzoxazole by Edwards, Philip D, Meyer, Edgar F, Vijayalakshmi, J, Tuthill, Paul A, Andisik, Donald A, Gomes, Bruce, Strimpler, Anne

“…Peptidyl alpha -ketobenzoxazoles are potent, competitive, reversible inhibitors of the serine proteinases HLE and PPE. These inhibitors were designed to…”
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Discovery of novel, orally active dual NK1/NK2 antagonists by BERNSTEIN, Peter R, AHARONY, David, KOSMIDER, Benedict J, KIRKLAND, Karin, OHNMACHT, Cyrus J, POTTS, William, RUMSEY, William L, LIHONG SHEN, SHENVI, Ashok, SHERWOOD, Scott, STOLLMAN, David, RUSSELL, Keith, ALBERT, Jeffrey S, ANDISIK, Donald, BARTHLOW, Herbert G, BIALECKI, Russell, DAVENPORT, Timothy, DEDINAS, Robert F, DEMBOFSKY, Bruce T, KOETHER, Gerard

“…Exploration of the SAR around selective NK2 antagonists, SR48968 and ZD7944, led to the discovery that naphth-1-amide analogues provide potent dual NK1 and NK2…”
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Peptidyl .alpha.-ketoheterocyclic inhibitors of human neutrophil elastase. 2. Effect of varying the heterocyclic ring on in vitro potency by Edwards, Philip D, Wolanin, Donald J, Andisik, Donald W, Davis, Matthew W

“…A series of peptidyl alpha-ketoheterocycles were synthesized and evaluated for their in vitro inhibition of human neutrophil elastase (HNE). Several…”
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Discovery and Biological Activity of Orally Active Peptidyl Trifluoromethyl Ketone Inhibitors of Human Neutrophil Elastase by Edwards, Philip D, Andisik, Donald W, Bryant, Craig A, Ewing, Barbara, Gomes, Bruce, Lewis, Joseph J, Rakiewicz, Donna, Steelman, Gary, Strimpler, Ann, Trainor, Diane A, Tuthill, Paul A, Mauger, Russell C, Veale, Chris A, Wildonger, Richard A, Williams, Joseph C, Wolanin, Donald J, Zottola, Mark

“…Previously we had shown that tripeptidyl trifluoromethyl ketones (TFMKs) possessing an N-terminal diarylacylsulfonamide, such as ICI 200,880 and ICI 200,355,…”
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Nonpeptidic Inhibitors of Human Neutrophil Elastase. 7. Design, Synthesis, and in Vitro Activity of a Series of Pyridopyrimidine Trifluoromethyl Ketones by Edwards, Philip D, Andisik, Donald W, Strimpler, Anne M, Gomes, Bruce, Tuthill, Paul A

“…Using molecular modeling and the information derived from X-ray crystal structures of human neutrophil elastase (HNE) and porcine pancreatic elastase (PPE)…”
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Design of Orally Active, Non-Peptidic Inhibitors of Human Leukocyte Elastase by Brown, Frederick J, Andisik, Donald W, Bernstein, Peter R, Bryant, Craig B, Ceccarelli, Chris, Damewood, James R. Jr, Edwards, Philip D, Earley, Roger A, Feeney, Scott

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Application of Fragment-Based Lead Generation to the Discovery of Novel, Cyclic Amidine β-Secretase Inhibitors with Nanomolar Potency, Cellular Activity, and High Ligand Efficiency by Edwards, Philip D, Albert, Jeffrey S, Sylvester, Mark, Aharony, David, Andisik, Donald, Callaghan, Owen, Campbell, James B, Carr, Robin A, Chessari, Gianni, Congreve, Miles, Frederickson, Martyn, Folmer, Rutger H. A, Geschwindner, Stefan, Koether, Gerard, Kolmodin, Karin, Krumrine, Jennifer, Mauger, Russell C, Murray, Christopher W, Olsson, Lise-Lotte, Patel, Sahil, Spear, Nate, Tian, Gaochao

“…Fragment-based lead generation has led to the discovery of a novel series of cyclic amidine-based inhibitors of β-secretase (BACE-1). Initial fragment hits…”
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Synthetic methods. 19. Lewis acid catalyzed conversion of alkenes and alcohols to azides by Hassner, Alfred, Fibiger, Richard, Andisik, Donald

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Naphtho[2,1- b][1,5] and [1,2- f][1,4]oxazocines as selective NK 1 antagonists by Ohnmacht, Cyrus J., Albert, Jeffrey S., Bernstein, Peter R., Rumsey, William L., Masek, Brian B., Dembofsky, Bruce T., Koether, Gerard M., Andisik, Donald W., Aharony, David

“…A series of stepwise structural modifications of the NK 1-selective ZD4974 enabled further refinement of a previously reported NK 1 pharmacophore model…”
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Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity by Albert, Jeffrey S, Aharony, David, Andisik, Donald, Barthlow, Herbert, Bernstein, Peter R, Bialecki, Russell A, Dedinas, Robert, Dembofsky, Bruce T, Hill, Daniel, Kirkland, Karin, Koether, Gerard M, Kosmider, Benedict J, Ohnmacht, Cyrus, Palmer, William, Potts, William, Rumsey, William, Shen, Lihong, Shenvi, Ashok, Sherwood, Scott, Warwick, Paul J, Russell, Keith

“…Through optimization of compounds based on the dual NK(1)/NK(2) antagonist ZD6021, it was found that alteration of two key regions could modulate the balance…”
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Design, Synthesis, and SAR of Tachykinin Antagonists:  Modulation of Balance in NK 1 /NK 2 Receptor Antagonist Activity by Albert, Jeffrey S., Aharony, David, Andisik, Donald, Barthlow, Herbert, Bernstein, Peter R., Bialecki, Russell A., Dedinas, Robert, Dembofsky, Bruce T., Hill, Daniel, Kirkland, Karin, Koether, Gerard M., Kosmider, Benedict J., Ohnmacht, Cyrus, Palmer, William, Potts, William, Rumsey, William, Shen, Lihong, Shenvi, Ashok, Sherwood, Scott, Warwick, Paul J., Russell, Keith

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Discovery of novel, orally active dual NK 1/NK 2 antagonists by Bernstein, Peter R., Aharony, David, Albert, Jeffrey S., Andisik, Donald, Barthlow, Herbert G., Bialecki, Russell, Davenport, Timothy, Dedinas, Robert F., Dembofsky, Bruce T., Koether, Gerard, Kosmider, Benedict J., Kirkland, Karin, Ohnmacht, Cyrus J., Potts, William, Rumsey, William L., Shen, Lihong, Shenvi, Ashok, Sherwood, Scott, Stollman, David, Russell, Keith

“…Exploration of the SAR around selective NK 2 antagonists, SR48968 and ZD7944, led to the discovery that naphth-1-amide analogues provide potent dual NK 1 and…”
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Intramolecular azide-olefin cycloadditions. A novel synthesis of 2,5-dihydrooxazoles by HASSNER, A, AMARASEKARA, A. S, ANDISIK, D

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Lewis acid catalyzed conversion of alkenes and alcohols to azides by HASSNER, A, FIBIGER, R, ANDISIK, D

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Cycloadditions. 34. Intramolecular azide-olefin cycloadditions. A novel synthesis of 2,5-dihydrooxazoles by Hassner, Alfred, Amarasekara, Ananda S, Andisik, Donald

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