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US 4,064,132 AGranted
Aroyl-substituted phenylacetamide derivatives
AssigneeJanssen Pharmaceutica NV
InventorsPaul Adriaan Jan Janssen, Georges Henri Paul Van Daele, Jozef Martin Boey
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Abstract
Compounds of the class of aroyl-substituted phenylacetic acids and corresponding esters, amides and hydroxamic acids, useful as anti-inflammatory agents and certain novel precursors therefor.
Claims2
An aroyl substituted .alpha.-R.sub.2 -.alpha.-R.sub.3 -phenylacetic acid derivative having the formula:
- ##STR32## wherein:
- ArCO is an aroyl substituent the Ar function of which is a member selected from the group consisting of 2-thienyl, 5-loweralkyl-2-thienyl, 5-halo-2-thienyl, 2-naphthyl and 3-pyridyl, said ArCO being in the meta- or para-position relative to the acetic acid function;
- either of R and R.sub.1 is hydrogen, the other being a member selected from the group consisting of hydrogen, halo and loweralkyl, provided that, when said R is halo or loweralkyl, then said ArCO is in the aforementioned paraposition, and when said R.sub.1 is halo or loweralkyl, then said ArCO is in the aforementioned meta-position, and further provided that when said R or R.sub.1 is halo, then said Ar is a member selected from the group consisting of 2-thienyl, 5-loweralkyl-2-thienyl and 5-halo-2-thienyl;
- either of R.sub.2 and R.sub.3 is a member selected from the group consisting of hydrogen, allyl and loweralkyl, the other being a member selected from the group consisting of hydrogen and loweralkyl, provided that, when either of said R.sub.2 and R.sub.3 is allyl, the other is hydrogen, and when either of said R.sub.2 and R.sub.3 is loweralkyl, the other is a member selected from the group consisting of hydrogen and loweralkyl;
- R.sub.2 and R.sub.3 taken together, is an alkylene bridge attached to the .alpha.-carbon of the acetic acid function:
- ##STR33## wherein n is an integer from 2 to 5;
- and Y is a member selected from the group consisting of amino, anilino, halo-substituted anilino, loweralkylanilino, loweralkyloxyanilino, piperidino, hydroxyethylamino, and hydroxyamino.
4 more elements
An aroyl substituted .alpha.-R.sub.2 -.alpha.-R.sub.3 -phenylacetic acid derivative having the formula:
- ##STR34## wherein ArCO is an aroyl substituent the Ar function of which is a member selected from the group consisting of 2-thienyl, 5-methyl-2-thienyl, 5-chloro-2-thienyl, 2-naphthyl and 3-pyridyl, said ArCO being in the meta- or para-position relative to the acetic acid function;
- either of R and R.sub.1 is hydrogen, the other being a member selected from the group consisting of hydrogen, chloro and methyl, provided that when said R is chloro or methyl, then said ArCO is in the forementioned para-position, and when said R.sub.1 is chloro or methyl, then said Ar-CO is in the aforementioned meta-position, and further provided that, when said R or R.sub.1 is chloro, then said Ar is a member selected from the group consisting of 2-thienyl, 5-methyl-2-thienyl and 5-chloro-2-thienyl;
- either of R.sub.2 and R.sub.3 is a member selected from the group consisting of hydrogen, allyl and loweralkyl, the other being a member selected from the group consisting of hydrogen and loweralkyl, provided that, when either of said R.sub.2 and R.sub.3 is allyl, the other is hydrogen, and when either of said R.sub.2 and R.sub.3 is loweralkyl, the other is a member selected from the group consisting of hydrogen and loweralkyl;
- R.sub.2 and R.sub.3, taken together, is an alkylene bridge attached to the .alpha.-carbon of the acetic acid function:
- ##STR35## wherein n is an integer from 2 to 5;
- and Y is a member selected from the group consisting of amino, anilino, halosubstituted anilino, preferably chloro-anilino, loweralkyl-anilino, such as methylanilino;
- loweralkyloxyanilino, preferably methoxyanilino;
- piperidino, hydroxyethylamino, and hydroxylamino.
5 more elements
Dependencies are inferred from the claim text.