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Claims for Patent: 4,215,215

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Claims for Patent: 4,215,215

Title: 9-Phenyl-nonate traene compounds
Abstract:Novel 9-phenyl 5,6-dimethyl-nona-2,4,6,8-tetraenoic acid, tetraenal or tetraenol derivatives useful as anti-tumor agents.
Inventor(s): Bollag; Werner (Basel, CH), Ruegg; Rudolf (Bottmingen, CH), Ryser; Gottlieb (Basel, CH)
Assignee: Hoffmann-La Roche Inc. (Nutley, NJ)
Application Number:06/055,437
Patent Claims: 1. A compound of the formula: ##STR17## wherein R.sub.1 and R.sub.2 are lower alkyl; R.sub.3 is hydrogen, lower alkyl, lower alkoxy, lower alkenyloxy, nitro, amino, lower alkylamino, lower alkanoylamino or N-heterocyclyl; R.sub.4 is lower alkoxy; R.sub.5 is hydrogen, lower alkyl, lower alkenyl, lower alkoxy, lower alkenyloxy, nitro, amino, lower alkanoylamino, lower alkylamino or N-heterocyclyl; and R.sub.6 is alkanoyloxymethylene, alkenyloxycarbonyl, alkynyloxycarbonyl, carbamoyl, mono(lower alkyl)-carbamoyl, di(lower alkyl)-carbamoyl, N-heterocyclylcarbonyl, or alkoxycarbonyl where its alkoxy moiety is unsubstituted or substituted with alkylamino, morpholino, piperdyl, pyridyl, alkyl substituted piperidyl or alkyl substituted pyridyl,

or pharmaceutically acceptable salts thereof.

2. A compound of the formula: ##STR18## wherein R.sub.1 and R.sub.2 are lower alkyl; R.sub.3 is hydrogen or lower alkyl; R.sub.4 is lower alkoxy; R.sub.5 is hydrogen, lower alkyl or lower alkoxy; and R.sub.6 is alkoxycarbonyl or carbamoyl,

or pharmaceutically acceptable salts thereof.

3. The compound of claim 1 wherein R.sub.6 is alkoxycarbonyl.

4. The compound of claim 3 wherein said compound is 9-(4-methoxy-2,3,6-trimethyl-phenyl)-3,7-dimethyl-nona-2,4,6,8-tetraen-1-o ic acid methyl ester.

5. The compound of claim 3 wherein said compound is 9-(4-methoxy-2,3,6-trimethyl-phenyl)-3,7-dimethyl-nona-2,4,6,8-tetraen-1-o ic acid ethyl ester.

6. The compound of claim 3 wherein said compound is 9-(4-methoxy-2,3,6-trimethyl-phenyl)-3,7-dimethyl-nona-2-trans,4-cis,6-tra ns,8-trans-tetraen-1-oic acid ethyl ester.

7. The compound of claim 3 wherein said compound is 9-(4-methoxy-2,3,6-trimethyl-phenyl)-3,7-dimethyl-nona-2,4,6,8-tetraen-1-o ic isopropyl ester.

8. The compound of claim 3 wherein said compound is 9-(4-methoxy-2,3,6-trimethyl-phenyl)-3,7-dimethyl-nona-2,4,6,8-tetraen-1-o ic acid butyl ester.

9. The compound of claim 3 wherein the alkoxy group of the alkoxycarbonyl moiety is substituted with alkylamino, morpholino, piperidyl, pyridyl, alkyl substituted piperidyl or alkyl substituted pyridyl.

10. The compound of claim 9 wherein said compound is 9-(4-methoxy-2,3,6-trimethyl-phenyl)-3,7-dimethyl-nona-2,4,6,8-tetraen-1-o ic acid diethyl aminoethyl ester.

11. The compound of claim 9 wherein said compound is 9-(4-methoxy-2,3,6-trimethyl-phenyl)-3,7-dimethyl-nona-2,4,6,8-tetraen-1-o ic acid (3-pyridyl)methyl ester.

12. The compound of claim 1 wherein R.sub.6 is alkynyloxycarbonyl.

13. The compound of claim 12 wherein said compound is 9-(4-methoxy-2,3,6-trimethyl-phenyl)-3,7-dimethyl-nona-2,4,6,8-tetraen-1-o ic acid allyl ester.

14. The compound of claim 1 wherein R.sub.6 is alkynyloxycarbonyl.

15. The compound of claim 14 wherein said compound is 9-(4-methoxy-2,3,6-trimethyl-phenyl)-3,7-dimethyl-nona-2,4,6,8-tetraen-1-o ic acid propargyl ester.

16. The compound of claim 1 wherein R.sub.6 is alkanoyloxymethylene.

17. The compound of claim 16 wherein said compound is 1-acetoxy-9-(4-methoxy-2,3,6-trimethyl-phenyl)-3,7-dimethyl-nona-2,4,6,8-t etraene.

18. The compound of claim 1 wherein R.sub.6 is carbamoyl.

19. The compound of claim 18 wherein said compound is 9-(4-methoxy-2,3,6-trimethyl-phenyl)-3,7-dimethyl-nona-2,4,6,8-tetraen-1-o ic acid amide.

20. The compound of claim 1 wherein R.sub.6 is mono or dilower alkylcarbamoyl.

21. The compound of claim 20 wherein said compound is 9-(4-methoxy-2,3,6-trimethyl-phenyl)-3,7-dimethyl-nona-2,4,6,8-tetraen-1-o ic acid ethyl amide.

22. The compound of claim 21 wherein said compound is 9-(4-methoxy-2,3,5,6-tetramethyl-phenyl)-3,7-dimethyl-nona-2,4,6,8-tetraen -1-oic acid ethyl amide.

23. The compound of claim 20 wherein said compound is 9-(4-methoxy-2,3,6-trimethyl-phenyl)-3,7-dimethyl-nona-2,4,6,8-tetraen-1-o ic acid diethylamide.

24. The compound of claim 1 wherein R.sub.6 is N-heterocyclylcarbonyl.

25. The compound of claim 24 wherein said compound is 9-(4-methoxy-2,3,6-trimethyl-phenyl)-3,7-dimethyl-nona-2,4,6,8-tetraen-1-o ic acid morpholide.

26. The compound of claim 1 wherein R.sub.5 is lower alkenyl.

27. The compound of claim 1 wherein at least one of R.sub.3 and R.sub.5 is nitro and R.sub.6 is alkoxycarbonyl.

28. The compound of claim 27 wherein said compound is 9-(4-methoxy-3-nitro-2,6-dimethyl-phenyl)-3,7-dimethyl-nona-2,4,6,8-tetrae n-1-oic acid ethyl ester.

29. The compound of claim 1 wherein at least one of R.sub.3 and R.sub.5 is lower alkylamino and R.sub.6 is alkoxycarbonyl.

30. The compound of claim 1 wherein at least one R.sub.3 or R.sub.5 is lower alkenyloxy.
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