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34 results on '"Perkins, James J."'

1. Invention of MK-7845, a SARS-CoV-2 3CL Protease Inhibitor Employing a Novel Difluorinated Glutamine Mimic

Author

Shurtleff, Valerie W., primary, Layton, Mark E., additional, Parish, Craig A., additional, Perkins, James J., additional, Schreier, John D., additional, Wang, Yunyi, additional, Adam, Gregory C., additional, Alvarez, Nadine, additional, Bahmanjah, Soheila, additional, Bahnck-Teets, Carolyn M., additional, Boyce, Christopher W., additional, Burlein, Christine, additional, Cabalu, Tamara D., additional, Campbell, Brian T., additional, Carroll, Steven S., additional, Chang, Wonsuk, additional, de Lera Ruiz, Manuel, additional, Dolgov, Enriko, additional, Fay, John F., additional, Fox, Nicholas G., additional, Goh, Shih Lin, additional, Hartingh, Timothy J., additional, Hurzy, Danielle M., additional, Kelly, Michael J., additional, Klein, Daniel J., additional, Klingler, Franca-Maria, additional, Krishnamurthy, Harini, additional, Kudalkar, Shalley, additional, Mayhood, Todd W., additional, McKenna, Philip M., additional, Murray, Edward M., additional, Nahas, Debbie, additional, Nawrat, Christopher C., additional, Park, Steven, additional, Qian, Dongming, additional, Roecker, Anthony J., additional, Sharma, Vijeta, additional, Shipe, William D., additional, Su, Jing, additional, Taggart, Robert V., additional, Truong, Quang, additional, Wu, Yin, additional, Zhou, Xiaoyan, additional, Zhuang, Ningning, additional, Perlin, David S., additional, Olsen, David B., additional, Howe, John A., additional, and McCauley, John A., additional

Published
2024
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2. Identification of an anabolic selective androgen receptor modulator that actively induces death of androgen-independent prostate cancer cells

Author

Schmidt, Azriel, Meissner, Robert S., Gentile, Michael A., Chisamore, Michael J., Opas, Evan E., Scafonas, Angela, Cusick, Tara E., Gambone, Carlo, Pennypacker, Brenda, Hodor, Paul, Perkins, James J., Bai, Chang, Ferraro, Damien, Bettoun, David J., Wilkinson, Hilary A., Alves, Stephen E., Flores, Osvaldo, and Ray, William J.

Published
2014
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4. Discovery of [11C]MK-8056: A Selective PET Imaging Agent for the Study of mGluR2 Negative Allosteric Modulators.

Author

Perkins, James J., McQuade, Paul, Bungard, Christopher J., Diamond, Tracy L., Gantert, Liza T., Gotter, Anthony L., Hanney, Barbara, Hills, Ivory D., Hurzy, Danielle M., Joshi, Aniket, Kern, Jonathan T., Schlegel, Kelly-Ann S., Manikowski, Jesse J., Meng, Zhaoyang, O'Brien, Julie A., Roecker, Anthony J., Smith, Sean M., Uslaner, Jason M., Hostetler, Eric, and Meissner, Robert S.

Published
2023
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6. Discovery of the Selective Androgen Receptor Modulator MK-0773 Using a Rational Development Strategy Based on Differential Transcriptional Requirements for Androgenic Anabolism Versus Reproductive Physiology

Author

Schmidt, Azriel, Kimmel, Donald B., Bai, Chang, Scafonas, Angela, Rutledge, SuJane, Vogel, Robert L., McElwee-Witmer, Sheila, Chen, Fang, Nantermet, Pascale V., Kasparcova, Viera, Leu, Chih-tai, Zhang, Hai-Zhuan, Duggan, Mark E., Gentile, Michael A., Hodor, Paul, Pennypacker, Brenda, Masarachia, Patricia, Opas, Evan E., Adamski, Sharon A., Cusick, Tara E., Wang, Jiabing, Mitchell, Helen J., Kim, Yuntae, Prueksaritanont, Thomayant, Perkins, James J., Meissner, Robert S., Hartman, George D., Freedman, Leonard P., Harada, Shun-ichi, and Ray, William J.

Published
2010
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10. Photoredox Catalysis for Silyl‐Mediated C–H Alkylation of Heterocycles with Non‐Activated Alkyl Bromides.

Author

Perkins, James J., Schubert, Jeffrey W., Streckfuss, Eric C., Balsells, Jaume, and ElMarrouni, Abdellatif

Subjects
*ALKYL bromides, *CATALYSIS, *ALKYLATION, *HETEROCYCLIC compounds, *HETEROARENES
Abstract

The development of a Minisci reaction of electron‐deficient heteroarenes with non‐activated alkyl bromides under visible‐light photoredox catalysis is disclosed. Optimization of the reaction led to identification of mild, general, and practical reaction conditions compatible with sensitive functional groups. The scope of this transformation allowed late‐stage functionalization of pharmaceutical products containing electron‐deficient heteroarenes in a parallel fashion. [ABSTRACT FROM AUTHOR]

Published
2020
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17. Non-peptide α v β 3 antagonists: Identification of potent, chain-shortened RGD mimetics that incorporate a central pyrrolidinone constraint

Author

Perkins, James J, primary, Duong, L.T, additional, Fernandez-Metzler, Carmen, additional, Hartman, George D, additional, Kimmel, Donald B, additional, Leu, Chih-Tai, additional, Lynch, Joseph J, additional, Prueksaritanont, Thomayant, additional, Rodan, Gideon A, additional, Rodan, Sevgi B, additional, Duggan, Mark E, additional, and Meissner, Robert S, additional

Published
2003
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18. Nonpeptide αvβ3 Antagonists. 8. In Vitro and in Vivo Evaluation of a Potent αvβ3 Antagonist for the Prevention and Treatment of Osteoporosis

Author

Hutchinson, John H., primary, Halczenko, Wasyl, additional, Brashear, Karen M., additional, Breslin, Michael J., additional, Coleman, Paul J., additional, Duong, Le T., additional, Fernandez-Metzler, Carmen, additional, Gentile, Michael A., additional, Fisher, John E., additional, Hartman, George D., additional, Huff, Joel R., additional, Kimmel, Donald B., additional, Leu, Chih-Tai, additional, Meissner, Robert S., additional, Merkle, Kara, additional, Nagy, Rose, additional, Pennypacker, Brenda, additional, Perkins, James J., additional, Prueksaritanont, Thomayant, additional, Rodan, Gideon A., additional, Varga, Sandor L., additional, Wesolowski, Greg A., additional, Zartman, Amy E., additional, Rodan, Sevgi B., additional, and Duggan, Mark E., additional

Published
2003
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19. Non-Peptide αvβ3 Antagonists. Part 4: Potent and Orally Bioavailable Chain-Shortened RGD Mimetics

Author

Coleman, Paul J., primary, Askew, Ben C., additional, Hutchinson, John H., additional, Whitman, David B., additional, Perkins, James J., additional, Hartman, George D., additional, Rodan, Gideon A., additional, Leu, Chih-Tai, additional, Prueksaritanont, Thomayant, additional, Fernandez-Metzler, Carmen, additional, Merkle, Kara M., additional, Lynch, Robert, additional, Lynch, Joseph J., additional, Rodan, Sevgi B., additional, and Duggan, Mark E., additional

Published
2002
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20. Nonpeptide αvβ3 antagonists. Part 2: constrained glycyl amides derived from the RGD tripeptide

Author

Meissner, Robert S., primary, Perkins, James J., additional, Duong, Le T., additional, Hartman, George D., additional, Hoffman, William F., additional, Huff, Joel R., additional, Ihle, Nathan C., additional, Leu, Chih-Tai, additional, Nagy, Rose M., additional, Naylor-Olsen, Adel, additional, Rodan, Gideon A., additional, Rodan, Sevgi B., additional, Whitman, David B., additional, Wesolowski, Gregg A., additional, and Duggan, Mark E., additional

Published
2002
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21. Nonpeptide αvβ3 Antagonists. 1. Transformation of a Potent, Integrin-Selective αIIbβ3 Antagonist into a Potent αvβ3 Antagonist

Author

Duggan, Mark E., primary, Duong, Le T., additional, Fisher, John E., additional, Hamill, Terence G., additional, Hoffman, William F., additional, Huff, Joel R., additional, Ihle, Nathan C., additional, Leu, Chih-Tai, additional, Nagy, Rose M., additional, Perkins, James J., additional, Rodan, Sevgi B., additional, Wesolowski, Gregg, additional, Whitman, David B., additional, Zartman, Amy E., additional, Rodan, Gideon A., additional, and Hartman, George D., additional

Published
2000
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25. Non-peptide αvβ3 antagonists: Identification of potent, chain-shortened RGD mimetics that incorporate a central pyrrolidinone constraint

Author

Perkins, James J., Duong, L.T., Fernandez-Metzler, Carmen, Hartman, George D., Kimmel, Donald B., Leu, Chih-Tai, Lynch, Joseph J., Prueksaritanont, Thomayant, Rodan, Gideon A., Rodan, Sevgi B., Duggan, Mark E., and Meissner, Robert S.

Subjects
*INTEGRINS, *OSTEOPOROSIS, *BONE resorption, *PEPTIDES
Abstract

Antagonists of the integrin receptor αvβ3 are expected to have utility in the treatment of osteoporosis through inhibition of bone resorption. A series of potent, chain-shortened, pyrrolidinone-containing αvβ3 receptor antagonists is described. Two sets of diasteromeric pairs of high-affinity antagonists demonstrated marked differences in log P values, which translated into differing dog pharmacokinetic properties. One member of this set was demonstrated to be effective in reducing bone resorption in rats. [Copyright &y& Elsevier]

Published
2003
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31. Non-Peptide αvβ3 Antagonists. Part 4: Potent and Orally Bioavailable Chain-Shortened RGD Mimetics

Author

Coleman, Paul J., Askew, Ben C., Hutchinson, John H., Whitman, David B., Perkins, James J., Hartman, George D., Rodan, Gideon A., Leu, Chih-Tai, Prueksaritanont, Thomayant, Fernandez-Metzler, Carmen, Merkle, Kara M., Lynch, Robert, Lynch, Joseph J., Rodan, Sevgi B., and Duggan, Mark E.

Subjects
*PEPTIDES, *AMIDES, *PHARMACOKINETICS
Abstract

Potent non-peptidic αvβ3 antagonists have been prepared where deletion of an amide bond from an earlier series of linear RGD-mimetics provides a novel series of chain-shortened αvβ3 antagonists with significantly improved oral pharmacokinetics. These chain-shortened αvβ3 antagonists represent structurally novel integrin inhibitors. [Copyright &y& Elsevier]

Published
2002
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32. Discovery of [ 11 C]MK-8056: A Selective PET Imaging Agent for the Study of mGluR 2 Negative Allosteric Modulators.

Author

Perkins JJ, McQuade P, Bungard CJ, Diamond TL, Gantert LT, Gotter AL, Hanney B, Hills ID, Hurzy DM, Joshi A, Kern JT, Schlegel KS, Manikowski JJ, Meng Z, O'Brien JA, Roecker AJ, Smith SM, Uslaner JM, Hostetler E, and Meissner RS

Abstract

Modification of potent, selective metabotropic glutamate receptor 2 negative allosteric modulator (mGluR 2 NAM) led to a series of analogues with excellent binding affinity, lipophilicity, and suitable physicochemical properties for a PET tracer with convenient chemical handles for incorporation of a 11 C or 18 F radiolabel. [ 11 C]MK-8056 was synthesized and evaluated in vivo and demonstrated appropriate affinity, selectivity, and physicochemical properties to be used as a positron emission tomography tracer for mGluR 2 ., Competing Interests: The authors declare no competing financial interest., (© 2023 American Chemical Society.)

Published
2023
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33. Development of a sp 2 -sp 3 Stille Cross-Coupling for Rapid Synthesis of HIV NNRTI Doravirine Analogues.

Author

ElMarrouni A, Campbell M, Perkins JJ, and Converso A

Abstract

The development of a C(sp 2 )-C(sp 3 ) cross-coupling reaction for rapid, parallel synthesis of analogues of two HIV NNRTI clinical candidates is described. This method allowed easy access to the C-ring space using a practical alkylation with commercially available tributyl(iodomethyl)stannane followed by a palladium-catalyzed coupling with a variety of aryl halides (I, Br) in the presence of copper chloride. Optimization and scope of this method are reported.

Published
2017
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34. Nonpeptide alphavbeta3 antagonists. 8. In vitro and in vivo evaluation of a potent alphavbeta3 antagonist for the prevention and treatment of osteoporosis.

Author

Hutchinson JH, Halczenko W, Brashear KM, Breslin MJ, Coleman PJ, Duong LT, Fernandez-Metzler C, Gentile MA, Fisher JE, Hartman GD, Huff JR, Kimmel DB, Leu CT, Meissner RS, Merkle K, Nagy R, Pennypacker B, Perkins JJ, Prueksaritanont T, Rodan GA, Varga SL, Wesolowski GA, Zartman AE, Rodan SB, and Duggan ME

Subjects
Animals, Bone Density drug effects, Bone Resorption drug therapy, Bone Resorption etiology, Bone Resorption metabolism, Dogs, Female, Humans, Macaca mulatta, Male, Naphthyridines chemistry, Naphthyridines pharmacology, Ovariectomy, Oxidation-Reduction, Propionates chemistry, Propionates pharmacology, Rats, Rats, Sprague-Dawley, Stereoisomerism, Structure-Activity Relationship, Integrin alphaVbeta3 antagonists & inhibitors, Naphthyridines chemical synthesis, Osteoporosis drug therapy, Osteoporosis prevention & control, Propionates chemical synthesis
Abstract

3(S)-(6-methoxypyridin-3-yl)-3-[2-oxo-3-[3-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)propyl]imidazolidin-1-yl]propionic acid 6 was identified as a potent and selective antagonist of the alpha(v)beta(3) receptor. This compound has an excellent in vitro profile (IC(50) = 0.08 nM), a significant unbound fraction in human plasma (12%), and good pharmacokinetics in rat, dog, and rhesus monkey. On the basis of the efficacy shown in three in vivo models of bone turnover, the compound was selected for clinical development. To support the ongoing metabolism and safety studies, a novel strategy was employed in which a series of oxidized derivatives of 6 were prepared by exposure of 6 (or the methyl ester) to chemical oxidizing agents. These products proved useful in the identification of active metabolites generated by either in vitro or in vivo metabolism.

Published
2003
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