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Generated: July 26, 2017

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Title: 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indoles as estrogenic agents
Abstract:The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds having the general structures below: ##STR1## which are useful in the treatment or inhibition of osteoarthritis.
Inventor(s): Miller; Chris P. (Strafford, PA), Collini; Michael D. (Clifton Heights, PA), Tran; Bach D. (Baltimore, MD), Santilli; Arthur A. (Havertown, PA)
Assignee: Wyeth (Madison, NJ)
Filing Date:Oct 24, 2003
Application Number:10/692,777
Claims:1. A method of treating or inhibiting osteoarthritis in a mammal in need thereof, which comprises administering to said mammal an effective amount of a compound of formula I or II, having the structures ##STR181##

wherein: R.sub.1 is selected from H, OH or the C.sub.1 -C.sub.12 esters (straight chain or branched) or C.sub.1 -C.sub.12 (straight chain or branched or cyclic) alkyl ethers thereof, or halogens; or C.sub.1 -C.sub.4 halogenated ethers including triflouromethyl ether and trichloromethyl ether; R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are independently selected from H, OH or the C.sub.1 -C.sub.12 esters (straight chain or branched) or C.sub.1 -C.sub.12 alkyl ethers (straight chain or branched or cyclic) thereof, halogens, or C.sub.1 -C.sub.4 halogenated ethers including triflouromethyl ether and trichloromethyl ether, cyano, C.sub.1 -C.sub.6 alkyl (straight chain or branched), or trifluoromethyl, with the proviso that, when R.sub.1 is H, R.sub.2 is not OH; X is selected from H, C.sub.1 -C.sub.6 alkyl, cyano, nitro, trifluoromethyl, halogen; n is 2 or 3; Y is selected from: a) the moiety: ##STR182## wherein R.sub.7 and R.sub.8 are independently selected from the group of H, C.sub.1 -C.sub.6 alkyl, or phenyl optionally substituted by CN, C.sub.1 -C.sub.6 alkyl (straight chain or branched), C.sub.1 -C.sub.6 alkoxy (straight chain or branched), halogen, --OH, --CF.sub.3, or --OCF.sub.3 ; b) a five-membered saturated, unsaturated or partially unsaturated heterocycle containing up to two heteroatoms selected from the group consisting of --O--, --NH--, --N(C.sub.1 C.sub.4 alkyl)--, --N.dbd., and --S(O).sub.m --, wherein m is an integer of from 0-2, optionally substituted with 1-3 substituents independently selected from the group consisting of hydrogen, hydroxyl, halo, C.sub.1 -C.sub.4 alkyl, trihalomethyl, C.sub.1 -C.sub.4 alkoxy, trihalomethoxy, C.sub.1 -C.sub.4 acyloxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkylsulfonyl, hydroxy (C.sub.1 -C.sub.4)alkyl, --CO.sub.2 H--, --CN--, --CONHR.sub.1 --, --NH.sub.2 --, C.sub.1 -C.sub.4 alkylamino, di(C.sub.1 -C.sub.4)alkylamino, --NHSO.sub.2 R.sub.1 --, --NHCOR.sub.1 --, --NO.sub.2, and phenyl optionally substituted with 1-3 (C.sub.1 -C.sub.4)alkyl; c) a six-membered saturated, unsaturated or partially unsaturated heterocycle containing up to two heteroatoms selected from the group consisting of --O--, --NH--, --N(C.sub.1 C.sub.4 alkyl)--, --N.dbd., and --S(O).sub.m --, wherein m is an integer of from 0-2, optionally substituted with 1-3 substituents independently selected from the group consisting of hydrogen, hydroxyl, halo, C.sub.1 -C.sub.4 alkyl, trihalomethyl, C.sub.1 -C.sub.4 alkoxy, trihalomethoxy, C.sub.1 -C.sub.4 acyloxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkylsulfonyl, hydroxy (C.sub.1 -C.sub.4)alkyl, --CO.sub.2 H--, --CN--, --CONHR.sub.1 --, --NH.sub.2 --, C.sub.1 -C.sub.4 alkylamino, di(C.sub.1 -C.sub.4)alkylamino, --NHSO.sub.2 R.sub.1 --, --NHCOR.sub.1 --, --NO.sub.2, and phenyl optionally substituted with 1-3 (C.sub.1 -C.sub.4)alkyl; d) a seven-membered saturated, unsaturated or partially unsaturated heterocycle containing up to two heteroatoms selected from the group consisting of --O--, --NH--, --N(C.sub.1 C.sub.4 alkyl)--, --N.dbd., and --S(O).sub.m --, wherein m is an integer of from 0-2, optionally substituted with 1-3 substituents independently selected from the group consisting of hydrogen, hydroxyl, halo, C.sub.1 -C.sub.4 alkyl, trihalomethyl, C.sub.1 -C.sub.4 alkoxy, trihalomethoxy, C.sub.1 -C.sub.4 acyloxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkylsulfonyl, hydroxy (C.sub.1 -C.sub.4)alkyl, --CO.sub.2 H--, --CN--, --CONHR.sub.1 --, --NH.sub.2 --, C.sub.1 -C.sub.4 alkylamino, di(C.sub.1 -C.sub.4)alkylamino, --NHSO.sub.2 R.sub.1 --, --NHCOR.sub.1 --, --NO.sub.2, and phenyl optionally substituted with 1-3 (C.sub.1 -C.sub.4)alkyl; or e) a bicyclic heterocycle containing from 6-12 carbon atoms either bridged or fused and containing up to two heteroatoms selected from the group consisting of --O--, --NH--, --N(C.sub.1 C.sub.4 alkyl)--, and --S(O).sub.m --, wherein m is an integer of from 0-2, optionally substituted with 1-3 substituents independently selected from the group consisting of hydrogen, hydroxyl, halo, C.sub.1 -C.sub.4 alkyl, trihalomethyl, C.sub.1 -C.sub.4 alkoxy, trihalomethoxy, C.sub.1 -C.sub.4 acyloxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkylsulfonyl, hydroxy (C.sub.1 -C.sub.4)alkyl, --CO.sub.2 H--, --CN--, --CONHR.sub.1 --, --NH.sub.2 --, C.sub.1 -C.sub.4 alkylamino, di(C.sub.1 -C.sub.4)alkylamino, --NHSO.sub.2 R.sub.1 --, --NHCOR.sub.1 --, --NO.sub.2, and phenyl optionally substituted with 1-3 (C.sub.1 -C.sub.4)alkyl;

or a pharmaceutically acceptable salt thereof.

2. The method according to claim 1 wherein: R.sub.1 is selected from H, OH or the C.sub.1 -C.sub.4 esters or alkyl ethers thereof, halogen; R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are independently selected from H, OH or the C.sub.1 -C.sub.4 esters or alkyl ethers thereof, halogen, cyano, C.sub.1 -C.sub.6 alkyl, or trifluoromethyl, with the proviso that, when R.sub.1 is H, R.sub.2 is not OH; X is selected from H, C.sub.1 -C.sub.6 alkyl, cyano, nitro, triflouromethyl, halogen; Y is the moiety ##STR183## R.sub.7 and R.sub.8 are selected independently from H, C.sub.1 -C.sub.6 alkyl, or combined by --(CH.sub.2).sub.p --, wherein p is an integer of from 2 to 6, so as to form a ring, the ring being optionally substituted by up to three substituents selected from the group of hydrogen, hydroxyl, halo, C.sub.1 -C.sub.4 alkyl, trihalomethyl, C.sub.1 -C.sub.4 alkoxy, trihalomethoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkylsulfonyl, hydroxy (C.sub.1 -C.sub.4)alkyl, --CO.sub.2 H, --CN, --CONH(C.sub.1 -C.sub.4), --NH.sub.2, C.sub.1 -C.sub.4 alkylamino, di(C.sub.1 -C.sub.4)alkylamino, --NHSO.sub.2 (C.sub.1 -C.sub.4), --NHCO(C.sub.1 -C.sub.4), and --NO.sub.2 ;

or a pharmaceutically acceptable salt thereof.

3. The method according to claim 1 wherein: R.sub.1 is OH; R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are independently selected from H, OH or the C.sub.1 -C.sub.4 esters or alkyl ethers thereof, halogen, cyano, C.sub.1 -C.sub.6 alkyl, or trifluoromethyl, with the proviso that, when R.sub.1 is H, R.sub.2 is not OH; X is selected from the group of Cl, NO.sub.2, CN, CF.sub.3, or CH.sub.3 ; ##STR184## R.sub.7 and R.sub.8 are concatenated together as --(CH.sub.2).sub.r, wherein r is an integer of from 4 to 6, to form a ring optionally substituted by up to three subsituents selected from the group of hydrogen, hydroxyl, halo, C.sub.1 -C.sub.4 alkyl, trihalomethyl, C.sub.1 -C.sub.4 alkoxy, trihalomethoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkylsulfonyl, hydroxy (C.sub.1 -C.sub.4)alkyl, --CO2H, --CN, --CONH(C.sub.1 -C.sub.4), --NH.sub.2, C.sub.1 -C.sub.4 alkylamino, di(C.sub.1 -C.sub.4)alkylamino, --NHSO.sub.2 (C.sub.1 -C.sub.4), --NHCO(C.sub.1 -C.sub.4), and --NO.sub.2 ;

or a pharmaceutically acceptable salt thereof.

4. The method according to claim 1, wherein the compound is 1-[4-(2-azepan-1-yl-ethoxy)-benzyl]-2-(4-hydroxy-phenyl)-3-methyl-1H-indol -5-ol or a pharmaceutically acceptable salt thereof.

5. The method according to claim 1, wherein the compound is 2-(4-hydroxy-phenyl)-3-methyl-1-[4-(2-piperidin-1-yl-ethoxy)-benzyl]-1H-in dol-5-ol or a pharmaceutically acceptable salt thereof.
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