A novel DP2 receptor antagonist (AM-461): A patent evaluation of WO2011085033

Expert Opinion on Therapeutic Patents

Volumn 21, Issue 12, 2011, Pages 1931-1936

  Norman, Peter ^a  

^a NORMAN CONSULTING   (United Kingdom)

Author keywords

AM 211; AM 461; asthma; COPD; DP2 receptor; inflammation; PGD 2

Indexed keywords

2 [3 [2 (TERT BUTYLSULFANYLMETHYL) 4 (2,2 DIMETHYLPROPANOYLAMINO)PHENOXY] 4 METHOXY PHENYL]ACETIC ACID SODIUM SALT; AM 156; AM 206; AM 211; AM 432; AM 461; AZD 1981; DOPAMINE 2 RECEPTOR BLOCKING AGENT; DRUG METABOLITE; PROSTAGLANDIN D2; UNCLASSIFIED DRUG; AM-461; ANTIASTHMATIC AGENT; ANTIINFLAMMATORY AGENT; IMMUNOGLOBULIN RECEPTOR; METHYLUREA; PHENYLACETIC ACID DERIVATIVE; PROSTAGLANDIN D2 RECEPTOR; PROSTAGLANDIN RECEPTOR;

ALLERGIC RHINITIS; AREA UNDER THE CURVE; ARTICLE; ASTHMA; CELL STRAIN HEK293; CHO CELL; CHRONIC OBSTRUCTIVE LUNG DISEASE; CRYSTAL STRUCTURE; DRUG ABSORPTION; DRUG EFFICACY; DRUG HALF LIFE; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TOLERABILITY; HUMAN; IC 50; NONHUMAN; PATENT; ANIMAL; CHEMICAL STRUCTURE; CHEMISTRY; DRUG ANTAGONISM; DRUG DESIGN; METABOLISM; REVIEW; STRUCTURE ACTIVITY RELATION;

ANIMALS; ANTI-ASTHMATIC AGENTS; ANTI-INFLAMMATORY AGENTS; ASTHMA; DRUG DESIGN; HUMANS; METHYLUREA COMPOUNDS; MOLECULAR STRUCTURE; PATENTS AS TOPIC; PHENYLACETATES; RECEPTORS, IMMUNOLOGIC; RECEPTORS, PROSTAGLANDIN; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 81855168393     PISSN: 13543776     EISSN: 17447674     Source Type: Journal    
DOI: 10.1517/13543776.2011.636738     Document Type: Article

References (20)

1. Wenzel SE, Westcott JY, Smith HR Larsen GL. Spectrum of prostanoid release after bronchoalveolar allergen challenge in atopic asthmatics and in control groups. An alteration in the ratio of bronchoconstrictive to bronchoprotective mediators. Am Rev Respir Dis 1989;139(12):450-7
2. Coleman RA, Smith WL, Narumiya S. International union of pharmacology classification of prostanoid receptors: properties, distribution, and structure of the receptors and their subtypes. Pharmacol Rev 1994;46(2):205-29
3. Hirai H, Tanaka K, Yoshie O, et al. Prostaglandin D2 selectively induces chemotaxis in T helper type 2 cells, eosinophils, and basophils via seven-transmembrane receptor CRTH2. J Exp Med 2001;193(2):255-61
4. Sawyer N, Cauchon E, Chateauneuf A, et al. Molecular pharmacology of the human prostaglandin D2 receptor, CRTH2. Br J Pharmacol 2002;137(8):1163-72
5. Ulven T, Kostenis E. Novel CRTH2 antagonists: a review of patents from 2006 to 2009. Expert Opin Ther Path 2010;20(11):1505-30
6. Norman P. DP2 receptor antagonists in development. Expert Opin Investig Drugs 2010;19(8):947-61
7. Parnes J, Banfield C, Chow V, et al. Multiple-dose study of AMG853 in healthy adults: Safety and pharmacokinetics [Abstract 1165].
8. Barnes N, Pavord I, Chuchalin A, et al. A randomized, double-blind, placebo-controlled study of the CRTH2 antagonist OC000459 in moderate persistent asthma. Clin Exp Allergy. 15 July 2011; [Epub ahead of print]
9. Amira Pharmaceuticals press release 30 June 2009 Amira Pharmaceuticals Announces Initial Positive Phase 1 Clinical Data for AM211, A Novel Product Candidate for the Treatment of respiratory Disease Results
10. Amira Pharmaceuticals press release 3 December 2009 Amira Pharmaceuticals Announces Initial Positive Phase I Clinical Data for AM461, A Back-Up to Amira's Lead DP2 Antagonist, AM211
11. Amira Pharmaceuticals, Inc. Antagonists ofPGD2 receptors. WO2009061676; 2009
12. Amira Pharmaceuticals, Inc. Antagonists of Prostaglandin D2 receptors. WO2009108720; 2009
13. Amira Pharmaceuticals, Inc. Antagonists of Prostaglandin D2 receptors. WO2010003127; 2010
14. Amira Pharmaceuticals, Inc. Heterocyclic Antagonists of Prostaglandin D2 receptors. WO2010057118; 2010
15. Stearns BA, Baccei C, Bain G, et al. Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis. Bioorg Med Chem Lett 2009;19(16):4647-51
16. Stebbins K, Broadhead AR, Baccei CS, et al. Pharmacological blockade of the DP2 receptor inhibits cigarette smoke-induced inflammation, mucus cell metaplasia and epithelial hyperplasia in the mouse lung. J Pharmacol Exp Ther 2010;332(3):764-75
17. Stebbins KJ, Broadhead AR, Correa LD, et al. Therapeutic efficacy of AM156, a novel prostanoid DP2 receptor antagonist, in murine models of allergic rhinitis and house dust mite-induced pulmonary inflammation. Eur J Pharmacol 2010;638(1-3):142-9
18. Scott JM, Baccei C, Bain G, et al. Discovery and optimization of a biphenylacetic acid series of prostaglandin D2 receptor DP2 antagonists with efficacy in a murine model of allergic rhinitis. Bioorg Med Chem Lett 2011;21(21):6608-12 ThechemicalapproachtoAM-211.
19. Bain G, Lorrain DS, Stebbins KJ, et al. Pharmacology of AM211, a potent and selective prostaglandin D2 receptor type 2 antagonist that is active in animal models of allergic inflammation. J Pharmacol Exp Ther 2011;338(1):290-301
20. Luker T, Bonnert R, Brough S, et al. Substituted indole-1-acetic acids as potent and selective CRTh2 antagonists-discovery of AZD1981. Bioorg Med Chem Lett 2011;21(21):6288-92