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Transient receptor potential vanilloid-1 antagonists: a survey of recent patent literature

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Pages 1107-1122 | Published online: 30 Jun 2010

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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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János Szolcsányi & Erika Pintér. (2013) Transient receptor potential vanilloid 1 as a therapeutic target in analgesia. Expert Opinion on Therapeutic Targets 17:6, pages 641-657.
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Antonio Ferrer-Montiel, Asia Fernández-Carvajal, Rosa Planells-Cases, Gregorio Fernández-Ballester, José Manuel González-Ros, Àngel Messeguer & Rosario González-Muñiz. (2012) Advances in modulating thermosensory TRP channels. Expert Opinion on Therapeutic Patents 22:9, pages 999-1017.
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Jin Mi Kang, Sun Ok Kwon, Jihyae Ann, Sunho Lee, Changhoon Kim, Nayeon Do, Jin Ju Jeong, Peter M. Blumberg, Heejin Ha, Thi Ngoc Lan Vu, Sanghee Yoon, Sun Choi, Robert Frank-Foltyn, Bernhard Lesch, Gregor Bahrenberg, Hannelore Stockhausen, Thomas Christoph & Jeewoo Lee. (2021) 2-(Halogenated Phenyl) acetamides and propanamides as potent TRPV1 antagonists. Bioorganic & Medicinal Chemistry Letters 48, pages 128266.
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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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Mircea Iftinca, Manon Defaye & Christophe Altier. (2020) TRPV1-Targeted Drugs in Development for Human Pain Conditions. Drugs 81:1, pages 7-27.
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Jin Mi Kang, Sun Ok Kwon, Jihyae Ann, Peter M. Blumberg, Heejin Ha, Young Dong Yoo, Robert Frank-Foltyn, Bernhard Lesch, Gregor Bahrenberg, Hannelore Stockhausen, Thomas Christoph & Jeewoo Lee. (2020) Discovery of 1-(1H-indazol-4-yl)-3-((1-phenyl-1H-pyrazol-5-yl)methyl) ureas as potent and thermoneutral TRPV1 antagonists. Bioorganic & Medicinal Chemistry Letters 30:23, pages 127548.
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Yiding Chen, Jingxi Mu, Min Zhu, Arjudeb Mukherjee & Hu Zhang. (2020) Transient Receptor Potential Channels and Inflammatory Bowel Disease. Frontiers in Immunology 11.
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Songyeon Ahn, Yong Soo Kim, Myeong Seup Kim, Jihyae Ann, Heejin Ha, Young Dong Yoo, Young Ho Kim, Peter M. Blumberg, Robert Frank-Foltyn, Gregor Bahrenberg, Hannelore Stockhausen, Thomas Christoph & Jeewoo Lee. (2020) Discovery of indane propanamides as potent and selective TRPV1 antagonists. Bioorganic & Medicinal Chemistry Letters 30:3, pages 126838.
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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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Changhoon Kim, Jihyae Ann, Sunho Lee, Wei Sun, Peter M. Blumberg, Robert Frank-Foltyn, Gregor Bahrenberg, Hannelore Stockhausen, Thomas Christoph & Jeewoo Lee. (2018) Discovery of 2-(3,5-difluoro-4-methylsulfonaminophenyl)propanamides as potent TRPV1 antagonists. Bioorganic & Medicinal Chemistry Letters 28:14, pages 2539-2542.
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Changhoon Kim, Jihyae Ann, Sunho Lee, Eunhye Kim, Sun Choi, Peter M. Blumberg, Robert Frank-Foltyn, Gregor Bahrenberg, Hannelore Stockhausen, Thomas Christoph & Jeewoo Lee. (2018) 4-Aminophenyl acetamides and propanamides as potent transient receptor potential vanilloid 1 (TRPV1) ligands. Bioorganic & Medicinal Chemistry 26:15, pages 4509-4517.
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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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Seol Rin Park, Juhyun Kim, Sun Young Lee, Young-Ho Park & Hee-Doo Kim. (2018) 2-Methylacrylamide as a bioisoster of thiourea group for 1,3-dibenzylthioureido TRPV1 receptor antagonists. Bioorganic & Medicinal Chemistry Letters 28:11, pages 2080-2083.
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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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Larry V. Pearce, Jihyae Ann, Aeran Jung, Shivaji A. Thorat, Brienna K. A. Herold, Amelework D. Habtemichael, Peter M. Blumberg & Jeewoo Lee. (2017) Novel Radiolabeled Vanilloid with Enhanced Specificity for Human Transient Receptor Potential Vanilloid 1 (TRPV1). Journal of Medicinal Chemistry 60:19, pages 8246-8252.
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Katsushi Kumata, Joji Yui, Yiding Zhang, Yusuke Kurihara, Masanao Ogawa, Wakana Mori, Masayuki Fujinaga & Ming-Rong Zhang. (2017) [ 11 C]BCTC: Radiosynthesis and in vivo binding to transient receptor potential vanilloid subfamily member 1 (TRPV1) receptor in the mouse trigeminal nerve. Bioorganic & Medicinal Chemistry Letters 27:19, pages 4521-4524.
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Yelena Mostinski, Gilad Noy, Rakesh Kumar, Dmitry Tsvelikhovsky & Avi Priel. (2017) Tricyclic Spirolactones as Modular TRPV1 Synthetic Agonists. ACS Chemical Neuroscience 8:8, pages 1688-1696.
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