Indole derivatives as cGMP-PDE inhibitors

Details Indole derivatives as cGMP-PDE inhibitors Indole derivatives as cGMP-PDE inhibitors

1997-12-10

2000-05-30

McKane, Joseph

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514365, 514514, 5462774, 548491, 548493, 548159, 548454, 548465, A01N 4340, C07D40106, C07D20904, C07D20908

Patent

active

060691565

DESCRIPTION:

BRIEF SUMMARY
This application is a 371 of PCT/JP96/00892, filed Apr. 2, 1996.


BACKGROUND OF THE INVENTION



Field of the Invention

The present invention relates to novel compounds having pharmacological activity, to a process for their production and to a pharmaceutical c position containing the same.
More particularly, it relates to novel indole compounds, which have pharmaceutical activity such as inhibiting activity of cyclic guanosine 3',5'-monophosphate phosphodiesterase (hereinafter described as cGMP-PDE), to a process for their production, to a pharmaceutical composition containing the same and to a use thereof.


SUMMARY OF THE INVENTION

Accordingly, one object of this invention is to provide the novel indole compounds, which have an inhibiting activity of cGMP-PDE.
Another object of this invention is to provide a process for production of the indole compounds.
A further object of this invention is to provide a pharmaceutical composition containing, as active ingredients, the indole compounds.
Still further object of this invention is to provide a use of the indole compounds for treating or preventing various diseases.
Further, this invention also relates to a new use of inhibitors of cyclic nucleotide phosphodiesterases. (hereinafter described as cyclic nucleotide-PDEs)


DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

In more detail, this invention relates to a new use of cyclic nucleotide-PDEs inhibitors for preventing or treating glomerular diseases, tubulo-interstitial diseases or renal failure, or diabetic complications.
Accordingly, this invention provides a new use of cyclic nucleotide-PDE inhibitors for preventing or treating glomerular diseases, tubulo-interstitial diseases or renal failure, or diabetic complications.
Further, this invention provides an agent and a pharmaceutical composition for preventing or treating glomerular diseases, tubulo-interstitial diseases or renal failure, or diabetic complications, which comprises cyclic nucleotide-PDE inhibitors.
Still further, this invention provides a method for preventing or treating glomerular diseases, tubulo-interstitial diseases or renal failure, or diabetic complications, which comprises administering cyclic nucleotide-PDE inhibitors.
The new indole compounds of this invention can be represented by the following general formula: ##STR2## wherein R.sup.1 is hydrogen, halogen, nitro, carboxy, protected carboxy, acyl, cyano, hydroxyimino(lower)alkyl, lower alkenyl optionally substituted with oxo, or lower alkyl optionally substituted with protected carboxy, carboxy or hydroxy; optionally substituted with protected carboxy, carboxy, lower alkoxy or hydroxy; substituted with one or more substituent(s) selected from the group consisting of from the group consisting of halogen, aryl, lower alkoxy, lower alkylenedioxy, cyano, nitro, carboxy, protected carboxy, acyl, and amino optionally substituted with acyl or protected carboxy, and group, amino optionally substituted with acyl or protected carboxy, or lower alkyl optionally substituted with protected carboxy, carboxy or acyl; attached, represent a 4- to 7-membered carbocyclic ring optionally substituted with oxo,
The compounds of formula (I) may contain one or more asymmetric centers and thus they can exist as enantiomers or diastereoisomers. Furthermore certain compounds of formula (I) which contain alkenyl groups may exist as cis- or trans-isomers. In each instance, the invention includes both mixtures and separate individual isomers.
The compounds of formula (I) may also exist in tautomeric forms and the invention includes both mixtures and separate individual tautomers.
The compound of the formula (I) and its salt can be in the form of a solvate, which is included within the scope of the present invention. The solvate preferably include a hydrate and an ethanolate.
Also included in the scope of invention are radiolabelled derivatives of compounds of formula (I) which are suitable for biological studies.
A preferred group of compounds of formula (I) is that wherein substituted with lower alk

REFERENCES:
patent: 4898863 (1990-02-01), Brown et al.
patent: 5234942 (1993-08-01), Bernstein et al.
patent: 5767139 (1998-06-01), Maw et al.

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