N-(2-phenyl-4-amino-butyl)-1-naphthamides as neurokinin-1 receptor antagonists
AssigneeAstraZeneca AB
InventorPeter Robert Bernstein
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Abstract
A compound having the general formula (I): R1R2N—CH2CH2—CHAr1—CH2—NR3—CO—R4 wherein: R1 is hydrogen, C1-6 alkyl, C2-6 alkenyl, aryl, C1-6 alkanoyl C1-6 alkoxycarbonyl or arylcarbonyl; any of such groups being optionally substituted; R2 is hydrogen or C1-6 alkyl; or R1 or R2 are joined to form an optionally substituted morpholino ring; Ar1 is phenyl mono- or di-substituted by halo; R3 is hydrogen or C1-6 alkyl; R4 is optionally substituted naphth-1-yl; or pharmaceutically acceptable salts thereof. These compounds antagonize the pharmacological actions of the endogenous neuropeptide tachykinins, particularly the neurokinin 1 (NK1) receptor.
Claims11
A compound of the formula (I):
- R1R2N—CH2CH2—CHAr1—CH2—NR3—CO—R4 (I)
- wherein:
- R1 is hydrogen, C1-6alkyl, C2-6alkenyl, aryl, C1-6alkanoyl, C1-6alkoxycarbonyl or arylcarbonyl;
- any of such groups being optionally substituted;
- R2 is hydrogen or C1-6alkyl;
- Ar1 is phenyl mono- or di-substituted by halo;
- R3 is hydrogen or C1-6alkyl;
- R4 is optionally substituted naphth-1-yl;
- or
- pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.