Back to results
US 2003/0199693 A1Published application
Theophylline and 3-isobutyl-1-methylxanthine based N-7 substituted derivatives displaying inhibitory activies on PDE-5 phosphodiesterase
OwnerIng-Jun Cheninventor
Life of this patent
Estimating the term…
Abstract
Compounds of the theophylline and 3-isobutyl-1-methylxanthine (IBMX) based on N-7 substituted derivatives, X being florine, chlorine, bromine or iodine, are provided. These compounds possess pharmacologically inhibitory activities on PDE-5 Phosphodiesterase, relaxation of corpus carvernosal smooth muscle and increase of intracarvernosal pressure (ΔICP). A process is also provided for the synthesis of some novel theophyline derivatives.
Claims6
A compound containing the theophylline moiety of formula I,
- 53
- wherein
- R1 is —(CH2)2CH3;R2 is a member selected from the group
- 54
- wherein R4 is a member selected from the group of H, —(CH2)n CH3, X,—NH2 and —NO2 and X designates F, Cl, Br or I
- wherein R5 is a member selected from the group of H,
- 55
- wherein
- R3 is a member selected from the group of halogen, hydroxyl group, a saturated straight chain of 1-3 carbon atoms and when one of R3 is hydrogen, n is 0, 1, 2 or 3.
6 more elements
A compound containing the theophylline moiety of formula II
- 56
- wherein
- R1 is —(CH2)n;
- CH3;
- R2 is a member selected from the group of
- 57
- wherein
- R4 is a member selected from the group of H, —(CH2)n CH3, X, —NH2 and —NO2;
- X designates F, Cl, Br or I.
- R3 is a member selected from the group of H,
- 58
- R3 is a member selected from the group of halogen, hydroxyl group (OH), a saturated straight chain of 1-3 carbon atoms and when one of R3 is hydrogen;
- n is 0, 1, 2 or 3.
10 more elements
Dependencies are inferred from the claim text.