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Review

Neurokinin receptor antagonists

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Pages 571-582 | Published online: 25 Feb 2005

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Hongxing Yan, Jeffrey K. Kerns, Qi Jin, Chongjie Zhu, Mary S. Barnette, James F. Callahan, DouglasW. P. Hay, Larry J. Jolivette, Mark A. Luttmann, Henry M. Sarau, Keith W. Ward, Katherine L. Widdowson & Zehong Wan. (2005) A Highly Convergent Synthesis of 2‐Phenyl Quinoline as Dual Antagonists for NK2 and NK3 Receptors. Synthetic Communications 35:24, pages 3105-3112.
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Duncan F Rogers. (2001) Tachykinin receptor antagonists for asthma and COPD. Expert Opinion on Therapeutic Patents 11:7, pages 1097-1121.
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Peter Norman. (2001) Therapeutic approaches to respiratory diseases excluding asthma:Trends from the patent literature 1997 - 2000. Expert Opinion on Therapeutic Patents 11:2, pages 307-322.
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Giuseppe AM Giardina, Mario Grugni & Luca F Raveglia. (2000) Recent advances in neurokinin-3 receptor antagonists. Expert Opinion on Therapeutic Patents 10:6, pages 939-960.
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RW Clarke. (2000) Synaptic mechanisms in nociception: emerging targets for centrally-acting analgesics. Emerging Therapeutic Targets 4:2, pages 173-189.
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Vincent Leroy, Peter Mauser, Zhongli Gao & Norton P Peet. (2000) Neurokinin receptor antagonists. Expert Opinion on Investigational Drugs 9:4, pages 735-746.
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Fabio M. Sabbatini, Romano Di Fabio, Cristiana Griffante, Giorgio Pentassuglia, Laura Zonzini, Sergio Melotto, Giuseppe Alvaro, Anna M. Capelli, Lara Pippo, Elisabetta Perdona’, Yves St. Denis, Silvano Costa & Mauro Corsi. (2010) Synthesis and pharmacological characterization of constrained analogues of Vestipitant as in vitro potent and orally active NK1 receptor antagonists. Bioorganic & Medicinal Chemistry Letters 20:2, pages 623-627.
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Sunil Paliwal, Gregory A. Reichard, Sapna Shah, Michelle Laci Wrobleski, Cheng Wang, Carmine Stengone, Hon-Chung Tsui, Dong Xiao, Ruth A. Duffy, Jean E. Lachowicz, Amin A. Nomeir, Geoffrey B. Varty & Neng-Yang Shih. (2008) Discovery of a novel, potent and orally active series of γ-lactams as selective NK1 antagonists. Bioorganic & Medicinal Chemistry Letters 18:14, pages 4168-4171.
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Narciso M. Garrido, Mercedes García, David Díez, M. Rosa Sánchez, F. Sanz & Julio G. Urones. (2008) Diastereoselective Synthesis of δ-Aminoacids through Domino Ireland−Claisen Rearrangement and Michael Addition. Organic Letters 10:9, pages 1687-1690.
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Michel Guillaume, Jef Cuypers & Jul Dingenen. (2007) Process Development of the Synthetic Route to R116301. Organic Process Research & Development 11:6, pages 1079-1086.
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Peter Lin, Lehua Chang, Robert J. DeVita, Jonathan R. Young, Ronsar Eid, Xinchun Tong, Song Zheng, Richard G. Ball, Nancy N. Tsou, Gary G. Chicchi, Marc M. Kurtz, Kwei-Lan C. Tsao, Alan Wheeldon, Emma J. Carlson, WaiSi Eng, H. Donald Burns, Richard J. Hargreaves & Sander G. Mills. (2007) The discovery of potent, selective, and orally bioavailable hNK1 antagonists derived from pyrrolidine. Bioorganic & Medicinal Chemistry Letters 17:18, pages 5191-5198.
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Jeffrey T. Kuethe, Jean-Francois Marcoux, Audrey Wong, Jimmy Wu, Michael C. Hillier, Peter G. Dormer, Ian W. Davies & David L. Hughes. (2006) Stereoselective Preparation of a Cyclopentane-Based NK1 Receptor Antagonist Bearing an Unsymmetrically Substituted Sec−Sec Ether. The Journal of Organic Chemistry 71:19, pages 7378-7390.
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Michelle Laci Wrobleski, Gregory A. Reichard, Sunil Paliwal, Sapna Shah, Hon-Chung Tsui, Ruth A. Duffy, Jean E. Lachowicz, Cynthia A. Morgan, Geoffrey B. Varty & Neng-Yang Shih. (2006) Cyclobutane derivatives as potent NK1 selective antagonists. Bioorganic & Medicinal Chemistry Letters 16:14, pages 3859-3863.
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Ho-Jane Shue, Xiao Chen, John H. Schwerdt, Sunil Paliwal, David J. Blythin, Ling Lin, Danlin Gu, Cheng Wang, Gregory A. Reichard, Hongwu Wang, John J. Piwinski, Ruth A. Duffy, Jean E. Lachowicz, Vicki L. Coffin, Amin A. Nomeir, Cynthia A. Morgan, Geoffrey B. Varty & Neng-Yang Shih. (2006) Cyclic urea derivatives as potent NK1 selective antagonists. Part II: Effects of fluoro and benzylic methyl substitutions. Bioorganic & Medicinal Chemistry Letters 16:4, pages 1065-1069.
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Ho-Jane Shue, Xiao Chen, Neng-Yang Shih, David J. Blythin, Sunil Paliwal, Ling Lin, Danlin Gu, John H. Schwerdt, Sapna Shah, Gregory A. Reichard, John J. Piwinski, Ruth A. Duffy, Jean E. Lachowicz, Vicki L. Coffin, Fei Liu, Amin A. Nomeir, Cynthia A. Morgan & Geoffrey B. Varty. (2005) Cyclic urea derivatives as potent NK1 selective antagonists. Bioorganic & Medicinal Chemistry Letters 15:17, pages 3896-3899.
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Michel JournetDongwei CaiDavid L. HughesJason J. KowalRobert D. LarsenPaul J. Reider. (2005) Synthesis of a Substance P Antagonist:  An Efficient Synthesis of 5-Substituted-4- N,N -dimethylamino-1,2,3-triazoles . Organic Process Research & Development 9:4, pages 490-498.
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Zhongxi Zack Zhao, Xue-Zhi Qin, Allen Wu & Yang Yuan. (2004) Novel rearrangements of an N-oxide degradate formed from oxidation of a morpholine acetal substance P antagonist. Journal of Pharmaceutical Sciences 93:8, pages 1957-1961.
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A.Roderick MacKenzie, Allan P. Marchington, Donald S. Middleton, Sandra D. Newman, Christopher N. Selway & Nicholas K. Terrett. (2003) 4-Amino-2-(aryl)-butylbenzamides and Their conformationally constrained analogues. Potent antagonists of the human neurokinin-2 (NK2) receptor. Bioorganic & Medicinal Chemistry Letters 13:13, pages 2211-2215.
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Frederik J.R Rombouts, Jeroen Van den Bossche, Suzanne M Toppet, Frans Compernolle & Georges J Hoornaert. (2003) Synthesis and conformational analysis of Substance P antagonist analogues based on a 1,7-naphthyridine scaffold. Tetrahedron 59:26, pages 4721-4731.
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Konrad H Bleicher, Yves Wüthrich, Geo Adam, Torsten Hoffmann & Andrew J Sleight. (2002) Parallel solution- and solid-phase synthesis of spiropyrrolo-Pyrroles as novel neurokinin receptor ligands. Bioorganic & Medicinal Chemistry Letters 12:21, pages 3073-3076.
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Konrad H. Bleicher, Yves Wüthrich, Maxime De Boni, Sabine Kolczewski, Torsten Hoffmann & Andrew J. Sleight. (2002) Parallel solution- and solid-Phase synthesis of spirohydantoin derivatives as neurokinin-1 receptor ligands. Bioorganic & Medicinal Chemistry Letters 12:18, pages 2519-2522.
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Laura C Cooper, Emma J Carlson, Jose L Castro, Gary G Chicchi, Kevin Dinnell, Jerry Di Salvo, Jason M Elliott, Gregory J Hollingworth, Marc M Kurtz, Mark P Ridgill, Wayne Rycroft, Kwei-Lan Tsao & Christopher J Swain. (2002) 4,4-Disubstituted cyclohexylamine NK1 receptor antagonists II. Bioorganic & Medicinal Chemistry Letters 12:13, pages 1759-1762.
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Jason M Elliott, Jose L Castro, Gary G Chicchi, Laura C Cooper, Kevin Dinnell, Gregory J Hollingworth, Mark P Ridgill, Wayne Rycroft, Marc M Kurtz, Duncan E Shaw, Christopher J Swain, Kwei-Lan Tsao & Lihu Yang. (2002) 4,4-Disubstituted cyclohexylamine NK1 receptor antagonists I. Bioorganic & Medicinal Chemistry Letters 12:13, pages 1755-1758.
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Nicholas J.S Harmat, Danilo Giannotti, Rossano Nannicini, Enzo Perrotta, Marco Criscuoli, Riccardo Patacchini, Anna-Rita Renzetti, Sandro Giuliani, Maria Altamura & Carlo A Maggi. (2002) Insertion of 2-Carboxysuccinate and Tricarballylic Acid Fragments into Cyclic-Pseudopeptides: New Antagonists for the Human Tachykinin NK-2 Receptor. Bioorganic & Medicinal Chemistry Letters 12:4, pages 693-696.
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Duncan Shaw, Gary G Chicchi, Jason M Elliott, Marc Kurtz, Denise Morrison, Mark P Ridgill, Nicola Szeto, Alan P Watt, Angela R Williams & Christopher J Swain. (2001) 2-Aryl indole NK1 antagonists: optimisation of the amide substituent. Bioorganic & Medicinal Chemistry Letters 11:23, pages 3031-3034.
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Timothy Harrison, Andrew P. Owens, Brian J. Williams, Christopher J. Swain, Angela Williams, Emma J. Carlson, Wayne Rycroft, F. David Tattersall, Margaret A. Cascieri, Gary G. Chicchi, Sharon Sadowski, Nadia M. J. Rupniak & Richard J. Hargreaves. (2001) An Orally Active, Water-Soluble Neurokinin-1 Receptor Antagonist Suitable for Both Intravenous and Oral Clinical Administration. Journal of Medicinal Chemistry 44:24, pages 4296-4299.
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Valerie A. Ashwood, Mark J. Field, David C. Horwell, Christine Julien-Larose, Russell A. Lewthwaite, Scott McCleary, Martyn C. Pritchard, Jenny Raphy & Lakhbir Singh. (2001) Utilization of an Intramolecular Hydrogen Bond To Increase the CNS Penetration of an NK 1 Receptor Antagonist . Journal of Medicinal Chemistry 44:14, pages 2276-2285.
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Frank E. BlaneyLuca F. RavegliaMarco ArticoStefano CavagneraCatherine DartoisCarlo FarinaMario GrugniStefania GagliardiMark A. LuttmannMarisa MartinelliGuy M. M. G. NadlerCarlo PariniPaola PetrilloHenry M. SarauMark A. ScheidelerDouglas W. P. HayGiuseppe A. M. Giardina. (2001) Stepwise Modulation of Neurokinin-3 and Neurokinin-2 Receptor Affinity and Selectivity in Quinoline Tachykinin Receptor Antagonists. Journal of Medicinal Chemistry 44:11, pages 1675-1689.
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Kevin Dinnell, Gary G Chicchi, Madhumeeta J Dhar, Jason M Elliott, Gregory J Hollingworth, Marc M Kurtz, Mark P Ridgill, Wayne Rycroft, Kwei-Lan Tsao, Angela R Williams & Christopher J Swain. (2001) 2-Aryl indole NK1 receptor antagonists: optimisation of the 2-Aryl ring and the indole nitrogen substituent. Bioorganic & Medicinal Chemistry Letters 11:9, pages 1237-1240.
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Laura C. Cooper, Gary G. Chicchi, Kevin Dinnell, Jason M. Elliott, Gregory J. Hollingworth, Marc M. Kurtz, Karen L. Locker, Denise Morrison, Duncan E. Shaw, Kwei-Lan Tsao, Alan P. Watt, Angela R. Williams & Christopher J. Swain. (2001) 2-Aryl Indole NK1 receptor antagonists: optimisation of indole substitution. Bioorganic & Medicinal Chemistry Letters 11:9, pages 1233-1236.
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