Bis-(quinolyl)-diamines

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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Details

C546S153000, C546S156000, C546S159000, C546S160000, C546S162000, C546S163000, C514S313000

Reexamination Certificate

active

06174897

ABSTRACT:

The present invention relates to novel bis-(quinolyl)-diamines, to processes for their preparation and to their use in drugs, especially as agents acting on the brain.
It is already known that N,N-bis-(7-chloroquinolin-4-yl)-alkanediamines are used as antimalarial drugs [cf. WO 95/35 287; J. Med. Chem. 35 (11), 1992, 2129-34; J. Med. Chem. 14 (4), 1971, 283-286; Chem. Pharm. Bull. 23 (8), 1975, 1869-73; PCT WO 93/07126].
Also, bis-quinaldines are know as drugs for topical infections and leukaemia, as monofunctional AT-selective DNA-intercalating agents and as antibacterial, anti-tubercular and antitumoral drugs [cf. J. Med. Chem. 20 (11), 1977, 1528-31; Agricultural and Biological Chemistry Vol. 35, 1971, 1, 119-21; FEBS Lett. 228 (2), 1988, 235-40; GB 12 46 733; U.S. Pat. Nos. 3,362,875; 3,974,279; Mutat. Res. 232 (2), 1990, 337-43; U.S. Pat. No. 3,026,322].
The publication J. Med. Chem. 1996, 39, 359-370, describes the synthesis and structure-activity relationship of dequalinium derivatives which are capable of inhibiting dequalinium-sensitive afterhyperpolarization.


REFERENCES:
patent: 3026322 (1962-03-01), Schock
patent: 3362875 (1968-01-01), Strauss et al.
patent: 3974279 (1976-08-01), Geiszler
patent: 1 246 733 (1971-09-01), None
patent: WO 93/07126 (1993-04-01), None
patent: WO 95/35287 (1995-12-01), None
J.Med.Chem. 35(11), 1992, 2129-34.
J.Med.Chem. 14(4), 1971, 283-286.
Chem.Pharm.Bull. (1975), 23(8), 1869-73.
J.Med.Chem. 20(11), 1977, 1528-31.
Agr.Biol.Chem. (1971), 35(1), 119-21.
FEBS Lett. (1988), 228(2)235-40.
Mut.Res. (1990), 232(2), 337-43.
J.Med.Chem. 1996, 39, 359-370.
J.Org.Chem. 1994, 59, 5886-5890.
Sinha, et al., J. Med. Chem., 1977, 20(11), p. 1528.
McFadgen et al, Chemical Abstracts vol. 113, entry 52145 (1990).
McFadgen et al, Biochimica et Biophysic Acta, 1048 (1990) pp. 50-58.
Singh, Chem. Pharm Bull 23(8) pp. 1869-1873 (1975).
Deshpande et al, Agr. Biol. Chem., vol. 35, No. 1, pp. 118-121 (1971).

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