3-heteroaliphatyl- and 3-hetero(aryl)aliphatyl-2(1H)-quinolone d

Details 3-heteroaliphatyl- and 3-hetero(aryl)aliphatyl-2(1H)-quinolone d 3-heteroaliphatyl- and 3-hetero(aryl)aliphatyl-2(1H)-quinolone d

1995-06-01

1997-05-27

Ivy, C. Warren

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

A61K 3147, C07D215227, C07D21520, C07D21536

Patent

active

056333790

ABSTRACT:
3-Heteroaliphatyl- and 3-hetero(aryl)aliphatyl-2(1H)quinolone derivatives of formula I ##STR1## wherein the radicals R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently of the others hydrogen, an aliphatic hydrocarbon radical, free or etherified hydroxy, mercapto or etherified and/or oxidised mercapto, unsubstituted or aliphaticaliy substituted amino, nitro, free or esterified or amidated carboxy, cyano, free or amidated sulfamoyl, halogen or trifluoromethyl, X is oxy or optionally oxidised thio, A is a divalent aliphatic radical and R.sub.5 is an optionally partially hydrogenated aryl or heteroaryl radical that is unsubstituted or substituted by aliphatic or araliphatic hydrocarbon radicals, by free or etherified hydroxy, by mercapto or etherified and/or oxidised mercapto, by unsubstituted or aliphatically substituted amino, by aliphatic acyl, by free or esterified or amidated carboxy, by cyano, by free or amidated sulfamoyl, by halogen and/or by trifluoromethyl; free or etherified hydroxymethyl; cyano; or free or esterified or amidated carboxy, and tautomers and/or salts thereof, have antagonistic properties with respect to excitatory amino acids and can be used for the treatment of pathological conditions that are responsive to glycine-antagonistic blocking of NMDA-sensitive receptors.

REFERENCES:
Leeson, Paul "Glycine-Site N-Methyl-D-Aspartate Receptor Antagonists" Drug Design for Neuroscience: 339-361 (1993).
McQuaid et al., "3-Phenyl-4-Hydroxyquinolin-2(1H)-ones": Patent and Selective Antagonists at the.
Carling, Robert et al. "3-Nitro-3,4-Dihydro-2(1H)-Quinolones Excitatory Amino Acid Antagonists Acting".
"At Glycine-Site NMDA and (RS)-.alpha.-Amino-3-Hydroxy-5-Methyl-4-Isoxazolepropionic Acid receptors" J. Med. Chem. 36: 3397-3408 (1993).
Rowley, Michael et al "3-Acyl-4-Hydroxyquinolin-2(1H)-ones". Systemically Active Anticonvolsants Acting by Antagonism at the Glycine Site of the N-Methyl-D-Aspartate Receptor Complex J. Med. Chem. 36: 3386-3396 (1993).
Leeson, Paul D. et al. "Amino Acid Bioisosteres: Design of 2-Quinolone Derivatives as Glycine-Site N-Methyl-D-Aspartate Receptor Antagonists" Bioorganic & Medicinal Chemistry Letters, 3(2): 299-304 (1993).

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