57724-78-4Relevant articles and documents
PHOSPHODIESTERASE 4 INHIBITORS
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Page/Page column 99; 100, (2008/06/13)
Selective PDE4 inhibition is achieved by novel compounds, e.g., 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds of the present invention are of formula (I) wherein R1, R2, and R3 are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and use for treating cognition impairment memory impairment, psychosis, schizophrenia, depression, allergic or inflammatory disease, chronic obstructive pulmonary disease, neurodegeneration, stroke, Alzheimer’s disease, multiple sclerosis.
PHOSPHODIESTERASE 4 INHIBITORS
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Page 103, (2010/02/09)
Selective PDE4 inhibition is achieved by 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds exhibit improved PDR4, inhibition as compared to compounds like rolipram and show selectivity with regard to inhibition of other classes of PDEs. The compounds of the present invention are of formula (I); wherein R1, R2, and R3 are as defined herein.
Phosphodiesterase 4 inhibitors
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, (2008/06/13)
Selective PDE4 inhibition is achieved by 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds like rolipram and show selectivity with regard to inhibition of other classes of PDEs. The compounds of the present invention are of formula I: wherein R1, R2, and R3 are as defined herein.
Inhibition of cyclic adenosine-3',5'-monophosphate phosphodiesterase from vascular smooth muscle by rolipram analogues
Marivet,Bourguignon,Lugnier,Mann,Stoclet,Wermuth
, p. 1450 - 1457 (2007/10/02)
Rolipram [(R,S)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]-2-pyrrolidone] has been shown to inhibit selectively the cAMP phopshodiesterase (PDE) of vascular smooth muscle. In order to further explore the structural requirements for selective PDE inhibition, we synthesized a series of rolipram derivatives differently substituted either at the pyrrolidinone or at the aromatic ring. Among these compounds, rolipram was the most active compound. Semirigid analogues were prepared and used for an evaluation of the active conformation of rolipram. Structural comparison with two other potent and chemically different smooth muscle cAMP-PDE inhibitors, trequinsin and Ro 20-1724, allows us to propose a first topological model of the smooth muscle cAMP-PDE pharmacophore.
4-(Polyalkoxy phenyl)-2-pyrrolidones
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, (2008/06/13)
4-(Polyalkoxyphenyl)-2-pyrrolidones of the formula STR1 wherein R1 and R2 each are hydrocarbon of up to 18 carbon atoms at least one being other than methyl, a heterocyclic ring, or alkyl of 1-5 carbon atoms substituted by halogen, OH, COOH, alkoxy, alkoxycarbonyl or an amino group; R' is H, alkyl, aryl or acyl; and X is O or S; possess neuropsychotropic activity. The compounds wherein X is O can be produced by saponifying and decarboxylating a corresponding 2-pyrrolidone-3-carboxylic acid alkyl ester or cyclizing a corresponding 3-phenyl-4-amino-butyric acid or alkyl ester thereof. The pyrrolidones can be converted to the corresponding thiopyrrolidones by reaction with phosphorous pentasulfide in the presence of base.
