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Novel CRTH2 antagonists: a review of patents from 2006 to 2009

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Pages 1505-1530 | Published online: 15 Oct 2010

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Christina Lamers, Daniel Flesch, Manfred Schubert-Zsilavecz & Daniel Merk. (2013) Novel prostaglandin receptor modulators: a patent review (2002 – 2012) – part I: non-EP receptor modulators. Expert Opinion on Therapeutic Patents 23:1, pages 47-77.
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Peter Norman. (2011) A novel DP2 receptor antagonist (AM-461): a patent evaluation of WO2011085033. Expert Opinion on Therapeutic Patents 21:12, pages 1931-1936.
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Veit J. Erpenbeck, Eva Vets, Lien Gheyle, Wande Osuntokun, Michael Larbig, Srikanth Neelakantham, David Sandham, Gerald Dubois, Walid Elbast, Paul Goldsmith & Markus Weiss. (2016) Pharmacokinetics, Safety, and Tolerability of Fevipiprant (QAW039), a Novel CRTh2 Receptor Antagonist: Results From 2 Randomized, Phase 1, Placebo‐Controlled Studies in Healthy Volunteers. Clinical Pharmacology in Drug Development 5:4, pages 306-313.
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Sathya Babu, Santhosh Kumar Nagarajan, Sung Haeng Lee & Thirumurthy Madhavan. (2016) Structural characterization of human CRTh2: a combined homology modeling, molecular docking and 3D-QSAR-based in silico approach. Medicinal Chemistry Research 25:4, pages 653-671.
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Sathya Babu. (2015) Pharmacophore-Based Comparative Molecular Similarity Indices Analysis of CRTh2 Antagonists. Journal of the Chosun Natural Science 8:4, pages 273-284.
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Sathya Babu, Seema A. Kulkarni, Honglae Sohn & Thirumurthy Madhavan. (2015) Identification of leads through in silico approaches utilizing benzylthio-1H-benzo[d]imidazol-1-yl acetic acid derivatives: A potent CRTh2 antagonist. Journal of Molecular Structure 1102, pages 25-41.
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Sathya Babu & Thirumurthy Madhavan. (2015) Pharmacophore Based Comparative Molecular Field Analysis of CRTh2 Antagonists. Journal of the Chosun Natural Science 8:2, pages 89-98.
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Daniel S. Strasser, Hervé Farine, Martin Holdener, Jochen Zisowsky, René Roscher, Julie Hoerner, Martine Gehin, Patricia N. Sidharta, Jasper Dingemanse & Peter M.A. Groenen. (2015) Development of a decision-making biomarker for CRTH2 antagonism in clinical studies. European Journal of Molecular & Clinical Medicine 2:4-5, pages 118.
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Sathya Babu, Honglae Sohn & Thirumurthy Madhavan. (2015) Computational Analysis of CRTh2 receptor antagonist: A Ligand-based CoMFA and CoMSIA approach. Computational Biology and Chemistry 56, pages 109-121.
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Sathya Babu & Thirumurthy Madhavan. (2015) Ligand Based HQSAR Analysis of CRTh2 Antagonists. Journal of the Chosun Natural Science 8:1, pages 1-12.
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Patricia N. Sidharta, Zuzana Diamant & Jasper Dingemanse. (2014) Single- and multiple-dose tolerability and pharmacokinetics of the CRTH2 antagonist setipiprant in healthy male subjects. Fundamental & Clinical Pharmacology 28:6, pages 690-699.
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Juan Antonio Alonso, Miriam Andrés, Mónica Bravo, Maria Antonia Buil, Marta Calbet, Jordi Castro, Paul R. Eastwood, Peter Eichhorn, Cristina Esteve, Elena Gómez, Jacob González, Marta Mir, Silvia Petit, Richard S. Roberts, Bernat Vidal, Laura Vidal, Pere Vilaseca & Miriam Zanuy. (2014) Structure–activity relationships (SAR) and structure–kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists I. Bioorganic & Medicinal Chemistry Letters 24:21, pages 5118-5122.
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Juan Antonio Alonso, Miriam Andrés, Mónica Bravo, Marta Calbet, Paul R. Eastwood, Peter Eichhorn, Cristina Esteve, Manel Ferrer, Elena Gómez, Jacob González, Marta Mir, Imma Moreno, Silvia Petit, Richard S. Roberts, Sara Sevilla, Bernat Vidal, Laura Vidal, Pere Vilaseca & Miriam Zanuy. (2014) Structure–activity relationships (SAR) and structure–kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists II: Lead optimization. Bioorganic & Medicinal Chemistry Letters 24:21, pages 5123-5126.
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Juan Antonio Alonso, Miriam Andrés, Mónica Bravo, Maria Antonia Buil, Marta Calbet, Jordi Castro, Paul R. Eastwood, Cristina Esteve, Manel Ferrer, Pilar Forns, Elena Gómez, Jacob González, Estrella Lozoya, Marta Mir, Imma Moreno, Silvia Petit, Richard S. Roberts, Sara Sevilla, Bernat Vidal, Laura Vidal & Pere Vilaseca. (2014) Structure–activity relationships (SAR) and structure–kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists III: The role of a hydrogen-bond acceptor in long receptor residence times. Bioorganic & Medicinal Chemistry Letters 24:21, pages 5127-5133.
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Miriam Andrés, Maria Antonia Buil, Marta Calbet, Oscar Casado, Jordi Castro, Paul R. Eastwood, Peter Eichhorn, Manel Ferrer, Pilar Forns, Imma Moreno, Silvia Petit & Richard S. Roberts. (2014) Structure–activity relationships (SAR) and structure–kinetic relationships (SKR) of pyrrolopiperidinone acetic acids as CRTh2 antagonists. Bioorganic & Medicinal Chemistry Letters 24:21, pages 5111-5117.
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Haixia Liu, Mingrui Zheng, Jianou Qiao, Yajie Dang, Pengyu Zhang & Xianqiao Jin. (2014) Role of prostaglandin D 2 /CRTH2 pathway on asthma exacerbation induced by Aspergillus fumigatus . Immunology 142:1, pages 78-88.
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Dong Xiao, Xiaohong Zhu, Younong Yu, Ning Shao, Jie Wu, Kevin D. McCormick, Pawan Dhondi, Jun Qin, Robert Mazzola, Haiqun Tang, Ashwin Rao, Phieng Siliphaivanh, Hongchen Qiu, Xiaoxin Yang, Maria Rivelli, Charles G. Garlisi, Steve Eckel, Gitali Mukhopadhyay, Craig Correll, Diane Rindgen, Robert Aslanian & Anandan Palani. (2014) Quality by design (QbD) of amide isosteres: 5,5-Disubstituted isoxazolines as potent CRTh2 antagonists with favorable pharmacokinetic and drug-like properties. Bioorganic & Medicinal Chemistry Letters 24:6, pages 1615-1620.
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Miriam Andrés, Mónica Bravo, Maria Antonia Buil, Marta Calbet, Marcos Castillo, Jordi Castro, Peter Eichhorn, Manel Ferrer, Martin D. Lehner, Imma Moreno, Richard S. Roberts & Sara Sevilla. (2014) 2-(1H-Pyrazol-1-yl)acetic acids as chemoattractant receptor-homologous molecule expressed on Th2 lymphocytes (CRTh2) antagonists. European Journal of Medicinal Chemistry 71, pages 168-184.
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Noel Snell, Martyn Foster & Jørgen Vestbo. (2013) Efficacy and safety of AZD1981, a CRTH2 receptor antagonist, in patients with moderate to severe COPD. Respiratory Medicine 107:11, pages 1722-1730.
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Miriam Andrés, Mónica Bravo, Maria Antonia Buil, Marta Calbet, Jordi Castro, Teresa Domènech, Peter Eichhorn, Manel Ferrer, Elena Gómez, Martin D. Lehner, Imma Moreno, Richard S. Roberts & Sara Sevilla. (2013) 2-(1H-Pyrazol-4-yl)acetic acids as CRTh2 antagonists. Bioorganic & Medicinal Chemistry Letters 23:11, pages 3349-3353.
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JA Schmidt, FM Bell, E Akam, C Marshall, IA Dainty, A Heinemann, IG Dougall, RV Bonnert & CA Sargent. (2013) Biochemical and pharmacological characterization of AZD1981, an orally available selective DP 2 antagonist in clinical development for asthma . British Journal of Pharmacology 168:7, pages 1626-1638.
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Miriam Sedej, Ralf Schröder, Kathrin Bell, Wolfgang Platzer, Anela Vukoja, Evi Kostenis, Akos Heinemann & Maria Waldhoer. (2012) D-type prostanoid receptor enhances the signaling of chemoattractant receptor–homologous molecule expressed on TH2 cells. Journal of Allergy and Clinical Immunology 129:2, pages 492-500.e9.
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