439660-78-3Relevant articles and documents
Design, synthesis and evaluation of dual pharmacology β2- adrenoceptor agonists and PDE4 inhibitors
Huang, Ling,Shan, Wenjun,Zhou, Qi,Xie, Jiaxing,Lai, Kefang,Li, Xingshu
supporting information, p. 249 - 253 (2014/01/17)
A novel series of formoterol-phthalazinone hybrids were synthesised and evaluated as dual pharmacology β2-adrenoceptor agonists and PDE4 inhibitors. Most of the hybrids displayed high β2-adrenoceptor agonist and moderate PDE4 inhibitory activities. The most potent compound, (R,R)-11c, exhibited agonist (EC50 = 1.05 nM, pEC50 = 9.0) and potent PDE4B2 inhibitory activities (IC50 = 0.092 μM).
Phthalazinones
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, (2008/06/13)
PCT No. PCT/EP98/00124 Sec. 371 Date Jul. 14, 1999 Sec. 102(e) Date Jul. 14, 1999 PCT Filed Jan. 12, 1998 PCT Pub. No. WO98/31674 PCT Pub. Date Jul. 23, 1998Compounds of formula I wherein R1, R2, R3, R4 and R5 have the means set forth in the description are selective cyclic nucleotide phosphodiesterase (PDE) inhibitors (specifically of type 4), which are effective bronchial therapeutics.