Cyclic GMP-specific phosphodiesterase inhibitors

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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Details

C544S342000

Reexamination Certificate

active

06825197

ABSTRACT:

FIELD AND BACKGROUND OF THE INVENTION
This invention relates to a series of compounds, to methods of preparing the compounds, to pharmaceutical compositions containing the compounds, and to their use as therapeutic agents. In particular, the invention relates to compounds that are potent and selective inhibitors of cyclic guanosine 3′,5′-monophosphate specific phosphodiesterase (cGMP-specific PDE), in particular PDE5, and have utility in a variety of therapeutic areas wherein such inhibition is considered beneficial, including the treatment of cardiovascular disorders and erectile dysfunction.


REFERENCES:
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patent: WO 96/32003 (1996-10-01), None
patent: WO 97/03985 (1997-02-01), None
patent: WO 97/43287 (1997-11-01), None
patent: WO 00/15639 (2000-03-01), None
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Fritz et al, “Stimulation of the Nitric Oxide-Guanosine 3′,5′-Cyclic Monophoshate Pathway by Sildenafil: Effect on Rectal Muscle Tone, Distensibility, and Perception in Health and in Irrittable Bowel Syndrome” Am. J. Gastroenterology, vol. 98(10), pp. 2253-2260. (2003).*
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Perry and Higgs, “Chemotherapeutic potential of phosphodiesterase inhibitors” Current Opinion in Chemical Biology, vol. 2, pp. 472-481 (1998).*
Willette et al, “Identification, Characterization, and Functional Role of Phosphodiesterase Type IV in Cerebral Vessels: Effects Selective Phosphodiesterase Inhibitors” J. Cerebral Blood Flow and Metabolism, vol. 17, pp. 210-219 (1997).*
Sybertz and Czarnieki, “Inhibitors of PDE1 and PDE5 cGMP phosphodiesterases: patents and therapeutic potential” Expert Opinion on Therapeutic Patents, vol. 7(6), pp. 631-639 (1997).
Madrigal et al, “Stereochemical issues related to the synthesis of 7,10,16,16a-tetrahydro-11H-quinazolino-[2′,3′,:3,4]pyrazino[1,2-b]-&bgr;-carboline-5,8-diones” Tetrahedron: Asymmetry, vol. 9(17), pp. 3115-3123 (1998). cas online abstract.
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