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. 2024 Jul 24;25(15):8052. doi: 10.3390/ijms25158052

Table 3.

Structures, IUPAC names, therapeutic indications, IC50 values on different PDE4 isoforms, and related references of the catechol PDE4Is under clinical investigation.

Compound Structure Condition or Disease IC50 Literature Data
Rolipram
(±) 4-(3-(cyclopentyloxy)-4-methoxyphenyl)pyrrolidin-2-one		 graphic file with name ijms-25-08052-i005.jpg Multiple sclerosis,
depression,
Huntington’s disease,
major depressive disorder		 PDE4D = 0.24 µM [72]
Tanimilast (CHF6001)
(S)-3,5-dichloro-4-(2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)-2-((3-(cyclopropylmethoxy)-4-(methylsulfonamido)benzoyl)oxy)ethyl)pyridine 1-oxide		 graphic file with name ijms-25-08052-i006.jpg COPD,
asthma		 PDE4 = 26 pM [74,75]
Cilomilast
(SB-207499)
4-cyano-4-(3-(cyclopentyloxy)-4-methoxyphenyl)cyclohexane-1-carboxylic acid		 graphic file with name ijms-25-08052-i007.jpg COPD PDE4 = 120 nM [75,76,77]
Difamilast
(OPA-15406/MM36)
N-((2-(4-(difluoromethoxy)-3-isopropoxyphenyl)oxazol-4-yl)methyl)-2-ethoxybenzamide		 graphic file with name ijms-25-08052-i008.jpg Chronic thromboembolic pulmonary hypertension,
joint disease,
atopic dermatitis		 PDE4A = 0.0832 µM
PDE4B = 0.0112 µM
PDE4C = 0.2493 µM
PDE4D = 0.0738 µM		 [78,79,80,81]
LEO 29102
2-(6-(2-(3,5-dichloropyridin-4-yl)acetyl)-2,3-dimethoxyphenoxy)-N-propylacetamide		 graphic file with name ijms-25-08052-i009.jpg Atopic dermatitis, psoriasis PDE4 = 5 nM [82,83]
HT-0712
(3S,5S)-5-(3-(cyclopentyloxy)-4-methoxyphenyl)-3-(3-methylbenzyl)piperidin-2-one		 graphic file with name ijms-25-08052-i010.jpg Age-associated memory impairment PDE4D = 150 nM [84,85]