主权项 |
1. A compound of the formula (I) or a pharmaceutically acceptable salt, solvate, or hydrate thereof, wherein
R1 is selected from the group consisting of:a cyano,a (2-4C)alkynyl,a (1-4C)alkyl,a (3-6C)cycloalkyl,a (4-6C)cycloalkenyl,a group selected from a (6-8C)bicycloalkyl group and a (8-10C)bicyclic group,wherein each group is optionally substituted with a (1-4C)alkyl,a group selected from a phenyl group, a biphenyl group, and a naphthyl group,
wherein each group is optionally substituted with at least one substituent independently selected from the group consisting of a halogen, a (1-4C)alkyl optionally substituted with at least one fluoro atom, a (2-4C)alkynyl, a (1-4C)alkoxy optionally substituted with at least one fluoro atom, an amino, a di(1-4C)alkylamino, a —SO2(1-4C)alkyl, a —CO-(1-4C)alkyl, a —CO—O-(1-4C)alkyl, a —NH—CO-(1-4C)alkyl, and a (3-6C)cycloalkyl,a phenyl group substituted with a substituent selected from the group consisting of a phenoxy, a benzyl, a benzyloxy, a phenylethyl, and a monocyclic heterocycle, wherein each substituent is optionally substituted with a (1-4C)alkyl,a monocyclic heterocycle optionally substituted with a substituent selected from the group consisting of a halogen, a (1-4C)alkyl, and a phenyl optionally substituted with a (1-4C)alkyl, and a bicyclic heterocycle optionally substituted with a (1-4C)alkyl; A is selected from the group consisting of —CO—O—, —O—CO—, —NH—CO—, —CO—NH, —C═C—, —CCH3—O—, and the linking group —Y—(CH2)n—X—, wherein
Y is attached to R1 and selected from the group consisting of a bond, —O—, —S—, —SO—, —SO2, —CH2—O—, —CO—, —O—CO—, —CO—O—, —CO—NH—, —NH—CO—, —C═C—, and —C≡C—;n is an integer selected from 1 to 10; andX is attached to the phenylene/pyridyl group and selected from the group consisting of a bond, —O—, —S—, —SO—, —SO2, —NH, —CO—, —C═C—, and —C≡C—; ring structure B optionally contains one nitrogen atom; R2 is selected from the group consisting of a H, a (1-4C)alkyl optionally substituted with at least one fluoro atom, a (1-4C)alkoxy optionally substituted with at least one fluoro atom, and a halogen; and R3 is selected from the group consisting of
a (1-4C)alkylene-R5 wherein the alkylene group may be substituted with a substituent selected from a (CH2)2 to form a cyclopropyl moiety, and one or two halogen atoms, a (3-6C)cycloalkylene-R5, and a —CO—CH2—R5; R4 is selected from the group consisting of H and a (1-4C)alkyl; R5 is selected from the group consisting of —OH, —OPO3H2, —OPO3H2, —COOH, —COO(1-4C)alkyl, and a tetrazol-5-yl, R6 is at least one substituent, and each R6 substituent is independently selected from the group consisting of H, a (1-4C)alkyl, and an oxo; and W is —O—; with the proviso that the compound of formula (I) is not 2-(4-ethylphenyl)-4-morpholinoethanol, 2-(4-ethylphenyl)-4-morpholinoethanol hydrochloride, 4-[4-(2-hydroxyethyl)-2-morpholinyl]benzeneacetonitrile, 4-[4-(2-hydroxyethyl)-2-morpholinyl]benzeneacetonitrile hydrochloride, or 3-methyl-2-[4-(phenylmethoxy)phenyl]-4-morpholinoethanol hydrochloride. |