US 6,642,256 B2 · Piperidine derivatives as subtype selective N-Methyl-D-Aspartate antagonists

Abstract

Described are piperidines of Formula I and pharmaceutically acceptable salts thereof. The compounds of Formula I are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, stroke, cerebral ischemia, central nervous system disorders, depression, trauma, hypoglycemia, neurodegenerative disorders, anxiety, migraine headache, convulsions, Parkinson's disease, aminoglycoside antibiotics-induced hearing loss, psychosis, glaucoma, CMV retinitis, opioid tolerance or withdrawal, pain, especially chronic pain, neuropathic pain, or surgical pain, or urinary incontinence.

Claims8

Dependent claims

A compound of formula (IV)

and pharmaceutically acceptable salts thereof wherein:
X2 is selected from O, S, NH and CH2;
Z is O or S;
R1 is independently selected from alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkoxy, substituted alkoxy, alkylaminoalkyl, hydroxyalkyl, (aminocarbonyl)-alkyl, (alkylthio)-alkyl, carboxyalkyl, haloalkyl and halogen;
g is an integer from 0 to 3;
R2 is H or OH;
R3 is H or OH;
V is (CH2)n or (CH2)m—C═O, wherein n is an integer from 1 to 4 and m is an integer from 0 to 4;
B is a ring selected from
wherein X is selected from O, S and N—R, wherein R is hydrogen or alkyl;
X1 is alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkoxy, substituted alkoxy, aralkyl, substituted aralkyl, halogen, haloalkyl, cyano, nitro, amino, aminoalkyl, alkylaminoalkyl, hydroxyalkyl, , carboxyalkyl, (aminocarbonyl)-alkyl, (alkylthio)-alkyl or C(O)-alkyl;
and
d is an integer from 0 to 2.

10 more elements

Dependencies are inferred from the claim text.

Piperidine derivatives as subtype selective N-Methyl-D-Aspartate antagonists

Life of this patent

Piperidine derivatives as subtype selective N-Methyl-D-Aspartate antagonists

Life of this patent

Abstract

Claims8