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Generated: August 17, 2017

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Title: Aroyl-substituted phenylacetic acid derivatives
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.
Inventor(s): Janssen; Paul Adriaan Jan (Vosselaar (Turnhout), BE), Van Daele; Georges Henri Paul (Turnhout, BE), Boey; Jozef Martin (Wilrijk (Antwerp), BE)
Assignee: Janssen Pharmaceutica N.V. (Beerse, BE)
Application Number:05/620,906
Patent Claims: 1. 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 para-position, 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; Y is a member selected from the group consisting of hydroxy, alkoxy having from 1 to 8 carbon atoms and diloweralkylamino-loweralkyloxy; and

wherein loweralkyl as above employed is a radical having from 1 to 5 carbon atoms.

2. 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 aforementioned 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 functon: ##STR35## wherein n is an integer from 2 to 5; Y is a member selected from the group consisting of hydroxy, alkoxy having from 1 to 8 carbon atoms and diloweralkylamino-loweralkyloxy; and

wherein loweralkyl as above employed is a radical having from 1 to 5 carbon atoms.

3. An aroyl substituted .alpha.-R.sub.2 -.alpha.-R.sub.3 -phenylacetic acid derivative having the formula: ##STR36## 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 and 5-halo-2-thienyl, 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 para-position, and when said R.sub.1 is halo or loweralkyl, then said ArCO is in the aforementioned meta-position;

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 together is also an alkylene bridge with the .alpha.-carbon of the acetic acid function: ##STR37## wherein n is an integer from 2 to 5; Y is a member selected from the group consisting of hydroxy, alkoxy having from 1 to 8 carbon atoms and diloweralkyl-aminoloweralkyloxy; and

wherein loweralkyl as above employed is a radical having from 1 to 5 carbon atoms.

4. An aroyl substituted .alpha.-R.sub.2 -.alpha.-R.sub.3 -phenylacetic acid derivative having the formula: ##STR38## 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 and 5-chloro-2-thienyl, said Ar-CO 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 aforementioned para-position, and when said R.sub.1 is chloro or methyl, then said Ar--CO is in the aforementioned meta-position;

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 together is also an alkylene bridge with the .alpha.-carbon of the acetic acid function: ##STR39## wherein n is an integer from 2 to 5; Y is a member selected from the group consisting of hydroxy, alkoxy having from 1 to 8 carbon atoms and diloweralkylamino-loweralkyloxy; and

wherein loweralkyl as above employed is a radical having from 1 to 5 carbon atoms.

5. p-(2-Thenoyl)hydratropic acid.

6. Ethyl p-(2-thenoyl)hydratropate.

7. Octyl p-(2-thenoyl)hydratropate.

8. 3-Chloro-4-(2-thenoyl)hydratropic acid.

9. p-(3-Pyridylcarbonyl)hydratropic acid.

10. p-(5-Methyl-2-thenoyl)hydratropic acid.

11. p-(2-Naphthoyl)hydratropic acid.

12. m-(2-Thenoyl)hydratropic acid.

13. p-(2-Thenoyl)-.alpha.-ethyl-phenylacetic acid.

14. p-(2-Thenoyl)-.alpha.-allyl-phenylacetic acid.

15. (+)-p-(2-Thenoyl)hydratropic acid.

16. (-)-p-(2-Thenoyl)hydratropic acid.

17. 3-(Dimethylamino)propyl p-(2-thenoyl)hydratropate oxalate.

18. 2-(Diethylamino)ethyl p-(2-thenoyl)hydratropate hydrochloride.

19. 3-Methyl-4-(2-thenoyl)hydratropic acid.

20. .alpha.-Methyl-p-(2-thenoyl)hydratropic acid.

21. 2-(Dimethylamino)-ethyl-p-(2-thenoyl)hydratropate oxalate.

22. p-(5-Chloro-2-thenoyl)hydratropic acid.

23. p-(2-Thenoyl)hydratropohydroxamic acid.

24. 2-[3-(2-Thenoyl)-o-tolyl]acetic acid.
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