Search Results - "KOETHER, Gerard M"

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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Synthesis and SAR of sulfoxide substituted carboxyquinolines as NK3 receptor antagonists by Xiong, Hui, Kang, James, Woods, James M., McCauley, John P., Koether, Gerard M., Albert, Jeffrey S., Hinkley, Lindsay, Li, Yan, Gadient, Reto A., Simpson, Thomas R.

“…Synthesis and SAR of a series of C3-alkylsulfoxide substituted quinolines as potent NK3 receptor antagonists are reported. These compounds have excellent NK3…”
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4-Aryl piperazine and piperidine amides as novel mGluR5 positive allosteric modulators by Xiong, Hui, Brugel, Todd A., Balestra, Michael, Brown, Dean G., Brush, Kelly A., Hightower, Caprice, Hinkley, Lindsay, Hoesch, Valerie, Kang, James, Koether, Gerard M., McCauley, John P., McLaren, Francis M., Panko, Laura M., Simpson, Thomas R., Smith, Reed W., Woods, James M., Brockel, Becky, Chhajlani, Vijay, Gadient, Reto A., Spear, Nathan, Sygowski, Linda A., Zhang, Minli, Arora, Jalaj, Breysse, Nathalie, Wilson, Julie M., Isaac, Methvin, Slassi, Abdelmalik, King, Megan M.

“…Positive allosteric modulation of metabotropic glutamate receptor 5 (mGluR5) is regarded as a potential novel treatment for schizophrenic patients. Herein we…”
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SAR development of a series of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as kappa opioid receptor antagonists. Part 2 by Brugel, Todd A., Smith, Reed W., Balestra, Michael, Becker, Christopher, Daniels, Thalia, Koether, Gerard M., Throner, Scott R., Panko, Laura M., Brown, Dean G., Liu, Ruifeng, Gordon, John, Peters, Matthew F.

“…Additional SAR for an extended set of structural modification to key moieties of a novel series of selective kappa opioid receptor antagonists based on a…”
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Discovery of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as selective antagonists of the kappa opioid receptor. Part 1 by Brugel, Todd A., Smith, Reed W., Balestra, Michael, Becker, Christopher, Daniels, Thalia, Hoerter, Tiffany N., Koether, Gerard M., Throner, Scott R., Panko, Laura M., Folmer, James J., Cacciola, Joseph, Hunter, Angela M., Liu, Ruifeng, Edwards, Philip D., Brown, Dean G., Gordon, John, Ledonne, Norman C., Pietras, Mark, Schroeder, Patricia, Sygowski, Linda A., Hirata, Lee T., Zacco, Anna, Peters, Matthew F.

“…Discovery and SAR studies of a novel series of potent and selective kappa opioid receptor antagonists containing an 8-azabicylo[3.2.1]octane core is described…”
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Design and optimization of cyclized NK1 antagonists with controlled atropisomeric properties by Albert, Jeffrey S, Ohnmacht, Cyrus, Bernstein, Peter R, Rumsey, William L, Aharony, David, Masek, Brian B, Dembofsky, Bruce T, Koether, Gerard M, Potts, William, Evenden, John L

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Design and optimization of cyclized NK 1 antagonists with controlled atropisomeric properties by Albert, Jeffrey S, Ohnmacht, Cyrus, Bernstein, Peter R, Rumsey, William L, Aharony, David, Masek, Brian B, Dembofsky, Bruce T, Koether, Gerard M, Potts, William, Evenden, John L

“…We have previously described a series of antagonists that showed high potency and selectivity for the NK 1 receptor. However, these compounds also had the…”
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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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