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TRPV1 antagonists: a survey of the patent literature

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Pages 977-996 | Published online: 21 Jun 2006

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Yoonji Lee, Sunhye Hong, Minghua Cui, Pankaz K Sharma, Jeewoo Lee & Sun Choi. (2015) Transient receptor potential vanilloid type 1 antagonists: a patent review (2011 – 2014). Expert Opinion on Therapeutic Patents 25:3, pages 291-318.
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Eric A Voight & Michael E Kort. (2010) Transient receptor potential vanilloid-1 antagonists: a survey of recent patent literature. Expert Opinion on Therapeutic Patents 20:9, pages 1107-1122.
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Wayne E Childers, Adam M Gilbert, Jeffrey D Kennedy & Garth T Whiteside. (2008) Advances in the development of novel analgesics. Expert Opinion on Therapeutic Patents 18:9, pages 1027-1067.
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Articles from other publishers (17)

Luis Apaza Ticona, Ángel Rumbero Sánchez, Cristina Thiebaut Estrada & Olga M. Palomino. (2020) Identification of TRPV1 Ion Channels Agonists of Tropaeolum tuberosum in Human Skin Keratinocytes. Planta Medica 87:05, pages 383-394.
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Andras Garami, Yury P. Shimansky, Zoltan Rumbus, Robson C.L. Vizin, Nelli Farkas, Judit Hegyi, Zsolt Szakacs, Margit Solymar, Alexandra Csenkey, Dan A. Chiche, Ram Kapil, Donald J. Kyle, Wade D. Van Horn, Peter Hegyi & Andrej A. Romanovsky. (2020) Hyperthermia induced by transient receptor potential vanilloid-1 (TRPV1) antagonists in human clinical trials: Insights from mathematical modeling and meta-analysis. Pharmacology & Therapeutics 208, pages 107474.
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Larry V. Pearce, Jihyae Ann, Peter M. Blumberg & Jeewoo Lee. (2019) Combination of a Rapidly Penetrating Agonist and a Slowly Penetrating Antagonist Affords Agonist Action of Limited Duration at the Cellular Level. Biomolecules & Therapeutics 27:5, pages 435-441.
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Hiromasa Oka, Koichi Yonezawa, Akio Kamikawa, Kazuhiro Ikegai, Norio Asai, Shohei Shirakami, Satoshi Miyamoto, Toshihiro Watanabe, Tetsuo Kiso, Yukihiro Takemoto, Seiji Tamura & Takahiro Kuramochi. (2018) Design, synthesis, and biological evaluation of novel biphenyl-4-carboxamide derivatives as orally available TRPV1 antagonists. Bioorganic & Medicinal Chemistry 26:12, pages 3716-3726.
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Chen Liao, Yan Liu, Chunxia Liu, Jiaqi Zhou, Huilan Li, Nasi Wang, Jieming Li, Taiyu Liu, Hesham Ghaleb, Wenlong Huang & Hai Qian. (2018) Phenylquinoline transient receptor potential vanilloid 1 antagonists for the treatment of pain: Discovery of 1-(2-phenylquinoline-4-carbonyl)-N-(4-(trifluoromethyl)phenyl)pyrrolidine-3-carboxamide. Bioorganic & Medicinal Chemistry 26:4, pages 845-854.
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Rajendra Kristam, Shashidhar N. Rao, Anne Sudha D’Cruz, Vijayalakshmi Mahadevan & Vellarkad N. Viswanadhan. (2017) TRPV1 antagonism by piperazinyl-aryl compounds: A Topomer-CoMFA study and its use in virtual screening for identification of novel antagonists. Journal of Molecular Graphics and Modelling 72, pages 112-128.
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Lin Yan, Jingjie Wang, Miaobo Pan, Qianqian Qiu, Wenlong Huang & Hai Qian. (2015) Synthesis of Analogues of BCTC Incorporating a Pyrrolidinyl Linker and Biological Evaluation as Transient Receptor Potential Vanilloid 1 Antagonists . Chemical Biology & Drug Design 87:2, pages 306-311.
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Ruben Vardanyan & Victor Hruby. 2016. Synthesis of Best-Seller Drugs. Synthesis of Best-Seller Drugs 15 64 .
Eric A. Voight, Arthur R. Gomtsyan, Jerome F. Daanen, Richard J. Perner, Robert G. Schmidt, Erol K. Bayburt, Stanley DiDomenico, Heath A. McDonald, Pamela S. Puttfarcken, Jun Chen, Torben R. Neelands, Bruce R. Bianchi, Ping Han, Regina M. Reilly, Pamela H. Franklin, Jason A. Segreti, Richard A. Nelson, Zhi Su, Andrew J. King, James S. Polakowski, Scott J. Baker, Donna M. Gauvin, LaGeisha R. Lewis, Joseph P. Mikusa, Shailen K. Joshi, Connie R. Faltynek, Philip R. Kym & Michael E. Kort. (2014) Discovery of ( R )-1-(7-Chloro-2,2-bis(fluoromethyl)chroman-4-yl)-3-(3-methylisoquinolin-5-yl)urea (A-1165442): A Temperature-Neutral Transient Receptor Potential Vanilloid-1 (TRPV1) Antagonist with Analgesic Efficacy . Journal of Medicinal Chemistry 57:17, pages 7412-7424.
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Laykea Tafesse, Toshiyuki Kanemasa, Noriyuki Kurose, Jianming Yu, Toshiyuki Asaki, Gang Wu, Yuka Iwamoto, Yoshitaka Yamaguchi, Chiyou Ni, John Engel, Naoki Tsuno, Aniket Patel, Xiaoming Zhou, Takuya Shintani, Kevin Brown, Tsuyoshi Hasegawa, Manjunath Shet, Yasuyoshi Iso, Akira Kato & Donald J. Kyle. (2014) Structure–Activity Relationship Studies and Discovery of a Potent Transient Receptor Potential Vanilloid (TRPV1) Antagonist 4-[3-Chloro-5-[(1 S )-1,2-dihydroxyethyl]-2-pyridyl]- N -[5-(trifluoromethyl)-2-pyridyl]-3,6-dihydro-2 H -pyridine-1-carboxamide (V116517) as a Clinical Candidate for Pain Management . Journal of Medicinal Chemistry 57:15, pages 6781-6794.
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Natalie A. Hawryluk, Jeffrey E. Merit, Alec D. Lebsack, Bryan J. Branstetter, Michael D. Hack, Nadia Swanson, Hong Ao, Michael P. Maher, Anindya Bhattacharya, Qi Wang, Jamie M. Freedman, Brian P. Scott, Alan D. Wickenden, Sandra R. Chaplan & J. Guy Breitenbucher. (2010) Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrimido-[4,5-d]azepines as novel TRPV1 antagonists. Bioorganic & Medicinal Chemistry Letters 20:23, pages 7137-7141.
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Tugba Taskin & Fatma Sevin. (2009) QSAR Approach to Correlate TRPV1 Antagonist Activity for a Series of Heteroaromatic Urea. QSAR & Combinatorial Science 28:10, pages 1098-1111.
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Scott D. Kuduk, Ronald K. Chang, Jenny M.-C. Wai, Christina N. Di Marco, Victoria Cofre, Robert M. DiPardo, Sean P. Cook, Matthew J. Cato, Aneta Jovanovska, Mark O. Urban, Michael Leitl, Robert H. Spencer, Stefanie A. Kane, George D. Hartman & Mark T. Bilodeau. (2009) Amidine derived inhibitors of acid-sensing ion channel-3 (ASIC3). Bioorganic & Medicinal Chemistry Letters 19:15, pages 4059-4063.
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Philip R. Kym, Michael E. Kort & Charles W. Hutchins. (2009) Analgesic potential of TRPV1 antagonists. Biochemical Pharmacology 78:3, pages 211-216.
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Dong Xiao, Anandan Palani, Robert Aslanian, Brian A. McKittrick, Andrew T. McPhail, Craig C. Correll, P. Tara Phelps, John C. Anthes & Diane Rindgen. (2009) Spiro-piperidine azetidinones as potent TRPV1 antagonists. Bioorganic & Medicinal Chemistry Letters 19:3, pages 783-787.
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Anindya Bhattacharya, Brian P. Scott, Nadia Nasser, Hong Ao, Michael P. Maher, Adrienne E. Dubin, Devin M. Swanson, Nigel P. Shankley, Alan D. Wickenden & Sandra R. Chaplan. (2007) Pharmacology and Antitussive Efficacy of 4-(3-Trifluoromethyl-pyridin-2-yl)-piperazine-1-carboxylic Acid (5-Trifluoromethyl-pyridin-2-yl)-amide (JNJ17203212), a Transient Receptor Potential Vanilloid 1 Antagonist in Guinea Pigs. Journal of Pharmacology and Experimental Therapeutics 323:2, pages 665-674.
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Michele C. Jetter, Mark A. Youngman, James J. McNally, Mark E. McDonnell, Sui-Po Zhang, Adrienne E. Dubin, Nadia Nasser, Ellen E. Codd, Christopher M. Flores & Scott L. Dax. (2007) Heteroaryl β-tetralin ureas as novel antagonists of human TRPV1. Bioorganic & Medicinal Chemistry Letters 17:22, pages 6160-6163.
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