Derivatives of 4,5,6,7-tetrahydroimidazo-[4,5-c]pyridinyl-6-carboxylic acid

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United States of America Patent

PATENT NO 5262537
SERIAL NO

08033522

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Abstract

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This invention pertains to a method for treating a condition of nausea and vomiting in a mammal which comprises administering a therapeutically effective amount of a 4,5,6,7-tetrahydroimidazo[4,5-c]pyridinyl-6-carboxylic acid derivative represented by the formula: ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen or lower-alkyl; R.sub.3 is selected from the group consisting of hydrogen, lower-alkyl, nitro, amino, cyano, and alkylmercapto; R.sub.4 and R.sub.5 are selected from the group consisting of hydrogen, lower-alkyl, aryl, and aryl lower-alkyl, or R.sub.4 and R.sub.5 together with the carbon atom to which they are attached form a 5- or 6-member saturated hydrocarbon ring; R.sub.6 is selected from the group consisting of hydrogen, lower-alkyl, aryl lower-alkyl, formyl, lower-alkyl carbonyl, and aryl carbonyl; R.sub.7 is selected from the group consisting of phenyl, thienyl, indolyl, indazolyl, benzo[b]furanyl, benzo[b]thiophenyl, and R.sub.8 R.sub.9 --N--; R.sub.8 is selected from the group consisting of 8-[1,2,3,4,-tetrahydroquinolinyl], pyridinyl, 3-quinolinyl, 2-naphthalinyl, 2-thiazolyl, 2-benzothiazolyl, 4-[2,1,3]benzothiadiazolyl, 2-(4,5,6,7-tetrahydrobenzo)thiazolyl, 7-(2,2-dimethyl-2,3-dihydrobenzo)furanyl, and phenyl; R.sub.9 is hydrogen or lower-alkyl; R.sub.8 R.sub.9 --N-- is selected from the group consisting of 1-indolinyl, 1-(3,3-dimethylindolinyl), and 1-(1,2,3,4-tetrahydroquinolinyl); wherein the groups represented by R.sub.7 other than R.sub.8 R.sub.9 N-- may be unsubstituted or substituted with one or more substituents selected from the group consisting of lower-alkyl, lower-alkoxy, di-lower-alkylamino, and aryloxy, and the groups represented by R.sub.8 and the radical R.sub.8 R.sub.9 N-- may have one or more substituents selected from the group consisting of hydroxy, halogen, lower-alkyl, lower-alkoxy, amino, mono- or di-lower-alkylamino, lower-alkyl carbonyl, lower-alkoxy carbonyl, and aryloxy; wherein each aryloxy group may be unsubstituted or substituted with substituents independently selected from the group consisting of lower-alkyl, lower-alkoxy, halogen, and trifluoromethyl with the proviso that, when R.sub.8 is phenyl, said phenyl group contains at least one substituent.

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Patent Owner(s)

Patent OwnerAddress
OHMEDA PHARMACEUTICAL PRODUCTS DIVISION INC110 ALLEN ROAD LIBERTY CORNER NJ 07938

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Evans, Suzanne M Springfield, NJ 1 7
Feng, Danging D Branchburg Township, Somerset County, NJ 1 7
Gall, Martin Morris Township, Morris County, NJ 59 691
Huang, Bao-Shan Edison, NJ 19 514
Latham, Tamara B North Plainfield, NJ 1 7
Nair, Raghunathan V Basking Ridge, NJ 3 9
Paradkar, Vidyadhar M Basking Ridge, NJ 9 97

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