Novel 5,6-dihydropyrazolo-[3,4-E][1,4]diazepin-4 (1H)-one derivatives for the treatment of asthma and chronic obstructive pulmonary disease: AstraZeneca: WO2007040435

Expert Opinion on Therapeutic Patents

Volumn 17, Issue 9, 2007, Pages 1183-1189

  Dyke, Hazel J ^a  

^a Argenta Discovery Ltd   (United Kingdom)

Author keywords

Asthma; Chronic obstructive pulmonary disease; COPD; Phosphodiesterase 4; Respiratory disease

Indexed keywords

5,6 DIHYDROPYRAZOLO[4,3 E][1,4]DIAZEPIN 4(1H) ONE DERIVATIVE; ANTIINFLAMMATORY AGENT; APREMILAST; CILOMILAST; CYCLIC AMP; IPL 455903; MK 0952; N (3,5 DICHLORO 4 PYRIDYL) [1 (4 FLUOROBENZYL) 5 HYDROXY 3 INDOLYL]GLYOXYLIC ACID AMIDE; OGLEMILAST; PHOSPHODIESTERASE IV; PHOSPHODIESTERASE IV INHIBITOR; ROFLUMILAST; ROLIPRAM; TETOMILAST; UK 500 001; UNCLASSIFIED DRUG;

ANTIINFLAMMATORY ACTIVITY; ARTICLE; ASTHMA; BINDING AFFINITY; BINDING SITE; CHRONIC OBSTRUCTIVE LUNG DISEASE; CLINICAL TRIAL; DRUG APPROVAL; DRUG EFFICACY; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG STRUCTURE; HUMAN; NAUSEA AND VOMITING; PATENT; STRUCTURE ANALYSIS;

EID: 35348981799     PISSN: 13543776     EISSN: None     Source Type: Journal    
DOI: 10.1517/13543776.17.9.1183     Document Type: Article

References (37)

1. NICHOLSON CD, CHALLISS RAJ, SHAHID M: Differential modulation of tissue function and therapeutic potential of selective inhibitors of cyclic nucleotide phosphodiesterase isoenzymes. Trends Pharmacol. (1991) 12:19-27.
2. NICHOLSON CD, SHAHID M: Inhibitors of cyclic nucleotide phosphodiesterase isoenzymes - their potential utility in the therapy of asthma. Pulm. Pharmacol. (1994) 7:1-17.
3. SHEPHERD MC: Phosphodiesterase 4 regulation of cyclic AMP in pulmonary remodelling: potential roles for isoform selective inhibitors. Pulm. Pharmacol. Ther. (2006) 19:24-31.
4. BEAVO JA: Cyclic nucleotide phosphodiesterases: functional implications of multiple isoforms. Physiol. Rev. (1995) 75:725-748.
5. CONTI M, NEMOZ G, SETTE CE, VICINI E: Recent progress in understanding the hormonal regulation of phosphodiesterases. Endocr. Rev. (1995) 16:370-389.
6. MANANIELLO VC, MURATA T, TAIRA M, BELFRAGE P, DEGERMAN E: Diversity in cyclic nucleotide isoenzyme families. Arch. Biochem. Biophys. (1995) 322:1-13.
7. FRANCIS SH, TURKO IV. CORBIN JD: Cyclic nucleotide phosphodiesterases: relating structure and function. Prog. Nucleic Acid. Res. (2000) 65:1-52.
8. CONTI M, JIN SLC: The molecular biology of cyclic nucleotide phosphodiesterases. Prog. Nucleic Acid. Res. (2000) 63:1-38.
9. SODERLING SH, BEAVO JA: Regulation of cAMP and cGMP signalling: new phosphodiesterases and new functions. Curr. Opin. Cell Biol. (2000) 12:174-179.
10. TORPHY TJ: Phosphodiesterase isozymes. Molecular targets for novel antiasthma agents. Am. J. Repir. Crit. Care Med. (1998) 157:351-370.
11. SOUNESS JE, ALDOUS D, SARGENT C: Immunosuppressive and anti-inflammatory effects of cyclic AMP phosphodiesterase (PDE) type 4 inhibitors. Immunopharmacology (2000) 47:127-162.
12. DYKE HJ, MONTANA JG: The therapeutic potential of PDE4 inhibitors. Expert Opin. Investig. Drugs (1999) 8(9):1301-1325.
13. DYKE HJ, MONTANA JG: Update on the therapeutic potential of PDE4 inhibitors. Expert Opin. Investig. Drugs (2002) 11(1):1-13.
14. SPINA D, LANDELLS LJ, PAGE CP: The role of phosphodiesterase enzymes in allergy and asthma. Adv. Pharmcol. (1998) 44:33-89.
15. SPINA D: The potential of PDE4 inhibitors in asthma or COPD, Curr. Opin. Investig. Drugs (2000) 1:204-213.
16. BARNETTE MS, UNDERWOOD DC: New phosphodiesterase inhibitors as therapeutics for the treatment of chronic lung disease Curr. Opin. Pulm. Med. (2000) 6:164-169.
17. WOLDA SL: PDE4 inhibitors and chronic obstructive pulmonary disease. Emerging Drugs (2000) 5:309-319.
18. HOUSLEY MD, SULLIVAN M, BOLGER GB: The multienzyme PDE4 cyclic adenosine monophosphate-specific phosphodiesterase family: intracellular signalling, regulation, and selective inhibition by compounds exerting anti-inflammatory and antidepressant actions. Adv. Pharmacol. (1998) 44:225-342.
19. HOUSLEY MD, ADAMS CR: PDE4 cAMP phosphodiesterases: modular enzymes that orchestrate signalling cross-talk, desensitisation and compartmentalization. Biochem. J. (2003) 370:1-18.
20. KROEGEL C, FOERSTER M: Phosphodiesterase-4 inhibitors as a novel approach for the treatment of respiratory disease: cilomilast. Expert Opin. Investig. Drugs (2007) 16(1):109-124.
21. HANSEN G, JIN S, UMETSU DT, CONTI M: Absence of muscarinic cholinergic airway responses in mice deficient in the cyclic nucleotide phosphodiesterase PDE4D. Proc. Natl. Acad. Sci. USA (2000) 98:6751-6756.
22. JIN CL, CONTI M: Induction of the cyclic nucleotide phosphodieterase PDE4B is essential for LPS activated TNF-α response. Proc. Natl. Acad. Sci. USA (2002) 99:7628-7633.
23. MEHATS C, JIN SL, WAHLSTROM J, LAW E, UMETSU DT, CONTI M: PDE4D plays a critical role in the control of airway smooth muscle contraction. FASEB J. (2003) 17:1831-1841.
24. PIAZ VD, GIOVANNONI MP: Phosphodiesterase 4 inhibitors, structurally unrelated to rolipram, as promising agents for the treatment of asthma and other pathologies. Eur. J. Med. Chem. (2000) 35:463-480.
25. NORMAN P: PDE4 inhibitors: sustained patenting activity as leading drugs near the market. Expert Opin. Ther. Patents (2000) 10(9):1415-1427.
26. NORMAN P: PDE4 inhibitors 2001. Patent and literature activity 2000 - September 2001. Expert Opin. Ther. Patents (2002) 12(1):93-111.
27. ODINGO JO: Inhibitors of PDE4: a review of recent patent literature. Expert Opin. Ther. Patents (2005) 15(7):773-787.
28. PANDORA C: Roflumilast: as selective phosphodiesterase 4 inhibitor. Drugs Today (2005) 41:667-675.
29. MCINTYRE JA, CASTANER J, CASTANER RM: Tetomilast: treatment of inflammatory bowel disease treatment of antioxidant PDE4 inhibitor. Drugs Fut. (2004) 29:1003-1006.
30. GUTHE H-J, GUSEJ-H, KHOBZAOUI M, RENUKAPPA-GUTKE T, BURNET M: AWD-12-281 (inhaled). Curr. Opin. Investig. Drugs (2005) 6:1149-1158.
31. SOUNESS JE, RAO S: A proposal for pharmacologically distinct conformers of PDE4. Cell Signal. (1997) 9:227-236.
32. LALIBERTE F, HAN Y, GOVINDARAJAN A et al.: Conformational difference between PDE4 apoenzyme and holoenzyme. Biochemistry (2000) 39:6449-6458.
33. LIU S, LALIBERTE F, BOBECHKO B et al.: Dissecting the cofactor-dependent and independent bindings of PDE4 inhibitors. Biochemistry (2001) 40:10179-10186.
34. XU RX, HASSELL AM, VANDERWALL D et al.: Atomic structure of PDE4: insights into phosphodiesterase mechanism and specificity. Science (2000) 288:1822-1825.
35. 3H]rolipram binding. Biochem. Pharmacol. (1996) 51:949-956.
36. ROCQUE WJ, TIAN G, WISEMAN JS et al.: Human recombinant phosphodiesterase aB2B binds (R)-rolipram at a single site with two affinities. Biochemistry (1997) 36:14250-14261.
37. BURNOUF C, PRUNIAUX MP: Recent advances in PDE4 inhibitors as immunoregulators and anti-inflammatory drugs. Curr. Pharm. Design (2002) 8:1255-1296.