초록 ▼

OMEGA-(Hydroxy, ether and ester) alkyl-2-Amino-Cycloalkenyl and -cycloalkyl amide compounds of the formula: [Figure] (I) where the wavy line bonds, m, n, p, A, R, R1, R2, X, Y and Z are as defined in the specification, e.g., 3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-3-(3-acetyloxypropyl)cyclohexen

OMEGA-(Hydroxy, ether and ester) alkyl-2-Amino-Cycloalkenyl and -cycloalkyl amide compounds of the formula: [Figure] (I) where the wavy line bonds, m, n, p, A, R, R1, R2, X, Y and Z are as defined in the specification, e.g., 3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-3-(3-acetyloxypropyl)cyclohexenyl]benzamide, and pharmacologically acceptable salts thereof, are useful as analgesic drug compounds having low physical dependence liability, compared to morphine and methadone. Pharmaceutical compositions and methods for using these compounds and compositions as analgesics are disclosed. Processes for preparing this class of compounds are also disclosed.

대표청구항 ▼

A compound of the formula [Figure] (I) where p is a whole number integer, 0, 1, 2, 3 or 4 and n is a whole number integer 0, 1, 2, 3 or 4, so that the resulting cycloaliphatic ring containing them has 5, 6 or 7 carbon atoms; m is 3 or 4; A is －(CH2)q where q is a whole number integer 0 to 4 or －CH(

A compound of the formula [Figure] (I) where p is a whole number integer, 0, 1, 2, 3 or 4 and n is a whole number integer 0, 1, 2, 3 or 4, so that the resulting cycloaliphatic ring containing them has 5, 6 or 7 carbon atoms; m is 3 or 4; A is －(CH2)q where q is a whole number integer 0 to 4 or －CH(CH3)－; X and Y are independently selected from the group consisting of hydrogen, a halogen having an atomic number of from 9 to 35, trifluoromethyl, nitro, methoxy, hydroxy, azido, C1 to C3-alkyl, phenyl, methanesulfonyl, cyano, －NH2, C1 to C3-alkoxycarbonyl, C1 to C3-alkanoyloxy and C1 to C3-carboxyacylamino; R is hydrogen or C1 to C3-alkyl; R1 and R2, taken together with the nitrogen to which they are bonded complete a ring selected from the group consisting of pyrrolidinyl, pyrrolyl, 3-pyrrolinyl, 3-azabicyclo[3.1.0]-hexan-3-yl and 3-azabicyclo[3.2.0]heptan-3-yl; Z is selected from the group consisting of hydrogen, C1 to C3-alkyl, and C1 to C3-alkanoyl, and perforated lines in the cycloaliphatic ring denote the option of a saturated cycloaliphatic ring, and mixed or separated cycloalkenyl rings at one of the two indicated positions of that cycloaliphatic ring; or a pharmaceutically acceptable salt thereof. A method for alleviating pain in a warm-blooded animal which comprises administering to an animal suffering pain an analgesically effective amount of a compound of claim 1 in a pharmaceutical dosage unit form.