Use of pyridazino[4,5-b]indole-1-acetamide...

Details Use of pyridazino[4,5-b]indole-1-acetamide... Use of pyridazino[4,5-b]indole-1-acetamide...

2001-07-25

2002-05-28

Henley, III, Raymond (Department: 1614)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

active

06395729

ABSTRACT:

Use of pyridazino[4,5-b]indole-1-acetamide derivatives for the preparation of medicaments for diseases linked to the dysfunctioning of peripheral-type benzodiazepine receptors.
In the context of the search for compounds which can promote the regeneration of the axons of the peripheral nerve cells after lesion, there has been identified, among the compounds of international patent application PCT/FR98/01667, a subclass of compounds of general formula (I)
in which
X represents a halogen atom,
Y represents one or more atoms or groups chosen from hydrogen, halogens and hydroxyl, methyl, methoxy and nitro groups,
R
1
represents a (C
1
-C
4
)alkyl group,
R
2
and R
3
each represent, independently of each other, a hydrogen atom or a (C
1
-C
4
)alkyl group, or alternatively R
2
and R
3
form, with the nitrogen atom carrying them, a pyrrolidinyl, piperidinyl or morpholinyl group.
These compounds possess a high affinity for the peripheral-type benzodiazepine receptors (p sites, or PBR), and some induce, in particular, a reduction in neuronal loss in the facial nucleus after cutting of the facial nerve. They also have cardio- and renoprotective effects.
A particularly advantageous compound for use according to the invention is, for example, 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide.


REFERENCES:
patent: 31 21 137 (1982-12-01), None
patent: 2 290 292 (1995-12-01), None
patent: 98/15552 (1998-04-01), None
patent: 99/06406 (1999-02-01), None
Derwent Abstract (1999)-153682.
Derwent Abstract (1998)-240772.
Derwent Abstract (1982)-09422J.

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