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1. WO1997028143 - DIHYDROBENZOFURAN AND RELATED COMPOUNDS USEFUL AS ANTI-INFLAMMATORY AGENTS

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[ EN ]

A compound having the structure



wherein
(a) n is from 1 to about 3;
(b) X is selected from the group consisting of O, S, SO, or SO2,
(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 3 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from 3 to about 7 atoms,
(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen,


(f) Ri , R2 and R3 are independently hydrogen, straight, branched or cyclic alkyl having from 1 to about 10 carbon atoms, aryl, heterocyclyl, heteroaryl, hydroxy, or alkoxy; or R-j , R2 and R3 may be bonded to form one or more rings, each ring having from 3 to about 7 atoms wherein one to three atoms may be heteroatoms.

2 The compound of Claim 1 wherein X is oxygen or sulphur, and R-| and R2 are hydrogen or methyl.

3 The compound of Claim 1 wherein each Y is independently selected from the group consisting of hydrogen, methyl and ethyl; and Z is selected from the group consisting of C4-C6 branched alkanyl having 2 branches, unsubstituted C3-C5 cycloalkanyl.

4 The compound of Claim 3 wherein X is oxygen, both Y are methyl, and Z is t-butyl

5 The compound of Claim 4 wherein R3 is C- .CQ straight or single-branched alkyl or straight alkyl with a terminal cyclic alkyl, saturated or unsaturated with one double bond between non-terminal carbon atoms, or C3-C6 cycloalkanyl 6 The compound of Claim 5 wherein X is oxygen, and R-| and R2 are hydrogen.

7 The compound of Claim 6 wherein n is one.

8. The compound of Claim 7 wherein R3 is selected from the group consisting of methyl, ethyl, n-propyl, i-propyl, n-butyl, 1-methylpropyl, 2-methylpropyl, 1-methylbutyl, ethoxy, benzyl, phenethyl, cyclobutyl, cyclopentyl and cyclohexyl.

9. The compound of Claim 8 wherein W is oxygen.

10. The compound of Claim 9 wherein R3 is selected from the group consisting of methyl, ethyl, n-propyl, n-butyl and ethoxy.

11 The compound of Claim 10 wherein R3 is methyl, ethyl or propyl.

12. A composition compπsing a compound of Claim 1 and a pharmaceutically- acceptable carrier.

13 A method of treating inflammation or pain comprising administation, to a human or lower animal in need of such treatment, of a safe and effective amount of a compound of Claim 1.

14 A method of treating arthritis comprising daily peroral administration, to a human in need of such treatment, of from about 1 mg/kg to about 20 mg/kg of a compound of Claim 1.

15. A composition comprising a compound of Claim 11 and a pharmaceutically- acceptable carrier.

16. A method of treating inflammation or pain comprising administation, to a human or lower animal in need of such treatment, of a safe and effective amount of a compound of Claim 11.

17. A method of treating arthritis comprising daily peroral administration, to a human in need of such treatment, of from about 1 mg/kg to about 20 mg/kg of a compound of Claim 11.