Pyrrolidinyl and pyrrolinyl ethylamine compounds as kappa agonists
AssigneePfizer Inc.
InventorsFumitaka Ito, Hiroshi Kondo
Life of this patent
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Abstract
A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, or hydroxy; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, or pyridyl, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, or C1-C4 alkyl; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.
Claims4
A compound of the following formula:
- and the salts thereof, wherein
- A is hydrogen, halo, hydroxy, C1-C6 alkyl, halo C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkoxy, oxo, OY wherein Y is a hydroxy protecting group, or absent;
- the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent;
- Ar1 is phenyl optionally substituted by one or more substituents selected from halo, hydroxy, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkoxy-C1-C4 alkoxy, CF3, carboxy-C1-C4 alkoxy and C1-C4 alkoxy-carbonyl-C1-C4 alkoxy;
- Ar2 is pyrimidyl, optionally substituted by one or more substituents selected from halo, hydroxy, amino, nitro, carboxy, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkylamino, di C1-C4 alkylamino, halo C1-C4 alkyl, C1-C4 alkythio and sulfonyl methyl;
- R1 is hydrogen, hydroxy, C1-C4 alkyl, C1-C4 alkoxy or OY wherein Y is a hydroxy protecting group;
- and
- R2 and R3 are independently selected from hydrogen, hydroxy, C1-C7 alkyl optionally substituted by one or more hydroxy or halo, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C7 alkoxy, phenyl optionally substituted by halo, phenyl C1-C7 alkyl, halo substituted phenyl C1-C7 alkyl, and (CH2)nX-R4 wherein n is one or two;
- X is O, NH or S and R4 is C1-C3 alkyl, or
- R2 and R3, together with the nitrogen atom to which they are attached, form a pyrrolidine, piperidine or morpholine ring, optionally substituted by C1-C3 alkyl or halo.
Dependencies are inferred from the claim text.