4-substituted indole and indoline compounds

1. A compound of the formula (I):

wherein:

represents a single bond or a double bond;

n is 0, 1, 2 or 3;

m is 0, 1 or 2;

each R 0 is independently selected from:

(a) hydrogen,

(b) halogen,

(c) C 1-6 -alkyl,

(d) C 3-7 -cycloalkyl,

(e) hydroxy-C 1-4 -alkyl,

(f) —COOR 6 ,

(g) —CONR 5 R 5 ,

(i) —CN,

(j) aryl, and

(k) heteroaryl,

wherein any heteroaryl or aryl residue is optionally independently substituted in one or more positions with a substituent selected from:

(a) halogen,

(b) C 1-4 -alkyl,

(c) C 1-4 -alkylthio,

(d) C 1-4 -alkoxy,

(e) —CF 3 ,

(f) —CN, and

(g) hydroxymethyl;

R 1 is a group selected from:

(a) C 1-6 -alkyl,

(b) C 3-7 -cycloalkyl,

(c) C 3-6 -alkenyl,

(d) aryl,

(e) aryl-C 2-6 -alkenyl,

(f) aryl-C 1-6 -alkyl,

(g) heteroaryl,

(h) heteroaryl-C 2-6 -alkenyl, and

(i) heteroaryl-C 1-6 -alkyl,

wherein any heteroaryl or aryl residue, alone or as part of another group, is optionally independently substituted in one or more positions with a substituent selected from:

(a) halogen,

(b) C 1-6 -alkyl,

(c) fluoro-C 1-6 -alkyl,

(d) C 3-7 -cycloalkyl,

(e) C 2-6 -alkenyl,

(f) fluoro-C 2-6 -alkenyl,

(g) ethynyl,

(h) hydroxy-C 1-4 -alkyl,

(i) hydroxy,

(j) C 1-6 -alkoxy,

(k) fluoro-C 1-6 -alkoxy,

(l) —SCF 3 ,

(m) —SCF 2 H,

(n) —SO 2 NR 5 R 5 ,

(o) —S(O) e R 8 , wherein e is 0, 1, 2 or 3,

(p) —CN,

(q) —NR 5 R 5 ,

(r) —NHSO 2 R 8 ,

(s) —NR 6 COR 8 ,

(t) —NO 2 ,

(u) —CONR 5 R 5 ,

(v) —C(═O)R 8 ,

(w) —COOH,

(x) C 1-6 -alkoxycarbonyl,

(y) C 3-7 -cycloalkoxy

(z) phenyl, optionally substituted with one or more of halogen, C 1-4 -alkyl, C 1-4 -alkylthio, C 1-4 -alkoxy, cyano, or trifluoromethyl,

(aa) phenoxy, optionally substituted with one or more of halogen, C 1-4 -alkyl, C 1-4 -alkylthio, C 1-4 -alkoxy, cyano, or trifluoromethyl,

(ab) benzyloxy, optionally substituted with one or more of halogen, C 1-4 -alkyl, C 1-4 -alkylthio, C 1-4 -alkoxy, cyano, or trifluoromethyl,

(ac) benzoyl, optionally substituted with one or more of halogen, C 1-4 -alkyl, C 1-4 -alkylthio, C 1-4 -alkoxy, cyano, or trifluoromethyl; and

(ad) heteroaryl, optionally substituted with trifluoromethyl and methyl;

each R 2 is independently selected from:

(a) hydrogen,

(b) halogen,

(c) C 1-6 -alkyl,

(d) fluoro-C 1-6 -alkyl,

(e) C 3-7 -cycloalkyl,

(f) C 2-6 -alkenyl,

(g) fluoro-C 2-6 -alkenyl,

(h) ethynyl,

(i) hydroxy-C 1-4 -alkyl,

(j) hydroxy,

(k) C 1-6 -alkoxy,

(l) fluoro-C 1-6 -alkoxy,

(m) C 3-7 -cycloalkoxy,

(n) fluoro-C 3-7 -cycloalkoxy,

(o) —SCF 3 ,

(p) —SCF 2 H,

(q) —SO 2 NR 5 R 5 ,

(r) —S(O) e R 8 , wherein e is 0, 1, 2 or 3,

(s) —CN,

(t) —NR 5 R 5 ,

(u) —NHSO 2 R 8 ,

(v) —NR 6 COR 8 ,

(w) —NO 2 ,

(x) —CONR 5 R 5 ,

(y) —OCONR 5 R 5 ,

(z) —C(═O)R 8 ,

(aa) —COOH,

(ab) C 1-6 -alkoxycarbonyl, and

(ac) —OR 11 ;

R 3 is a group selected from:

wherein:

X is selected from O and —NR 6 ;

z is 2; and

(i) both of the R 4 substituents are hydrogen; or

(ii) one of the two R 4 substituents is hydrogen, and the other of the two R 4 substituents is C 1-4 alkyl, fluoro-C 1-4 -alkyl, hydroxy-C 1-4 -alkyl, or cyano; or

(iii) both of the R 4 substituents are CH 3 ;

each R 5 is independently selected from:

(a) hydrogen,

(b) C 1-6 -alkyl,

(c) fluoro-C 1-6 -alkyl,

(d) heteroaryl-C 1-2 -alkyl, and

(e) C 3-7 -cycloalkyl, or

two R 5 groups together with the nitrogen to which they are attached form a heterocyclic ring;

each R 6 is independently selected from:

(a) hydrogen,

(b) C 1-4 -alkyl, and

(b) fluoro-C 2-4 -alkyl, and

(c) hydroxy-C 1-3 -alkyl;

R 7 is selected from:

(a) hydrogen,

(b) C 1-4 -alkyl,

(b) fluoro-C 2-4 -alkyl,

(c) 2-cyanoethyl,

(d) hydroxy-C 2-4 -alkyl,

(e) C 3-4 -alkenyl,

(f) C 3-4 -alkynyl,

(g) C 3-7 -cycloalkyl,

(h) C 3-4 -cycloalkyl-C 1-4 -alkyl, and

(i) C 1-4 -alkoxy-C 2-4 -alkyl;

each R 8 is independently selected from:

(a) C 1-6 -alkyl,

(a) fluoro-C 1-6 -alkyl,

(b) C 3-7 -cycloalkyl,

(c) aryl, and

(d) heteroaryl,

wherein any heteroaryl or aryl residue is optionally independently substituted in one or more positions with a substituent selected from:

(a) halogen,

(b) C 1-4 -alkyl,

(c) C 1-4 -alkylthio,

(d) C 1-4 -alkoxy,

(e) —CF 3 ,

(f) —OCF 3 ,

(g) —CN, and

(h) hydroxymethyl;

R 9 is selected from:

(a) hydrogen,

(b) fluorine, provided that the said fluorine is not attached to a carbon atom adjacent to a ring nitrogen atom,

(c) C 1-4 -alkyl,

(d) —NR 6 R 6 , provided that the said —NR 6 R 6 group is not attached to a carbon atom adjacent to a ring nitrogen atom,

(e) hydroxy, provided that the said hydroxy group is not attached to a carbon atom adjacent to a ring nitrogen atom, and

(f) hydroxy-C 1-4 -alkyl;

each R 10 is independently selected from:

(a) hydrogen,

(b) hydroxy-C 2-4 -alkyl,

(c) C 1-3 -alkoxy-C 2-4 -alkyl,

(d) cyclopropyl,

(e) cyclobutyl,

(f) benzyl, and

(g) C 1-4 -alkyl, provided that when both R 10 represent ethyl, then

represents a double bond;

R 11 is selected from:

(a) —CH 2 CN and

(b) benzyl; and

each R 12 is independently selected from:

(a) hydrogen,

(b) C 1-4 -alkyl,

(c) fluoro-C 1-4 -alkyl,

(d) hydroxy-C 1-3 -alkyl, and

(e) C 1-6 -alkoxycarbonyl;

or a pharmaceutically acceptable salt thereof,

with the proviso that the compound of formula (I) is not {[1-(phenylsulfonyl)-1H-indol-4-yl]methyl}amine, N-methyl-1-(phenylsulfonyl)-1H-indole-4-methanamine or N,N-dimethyl-1-[1-(phenylsulfonyl)-1H-indol-4-yl]methanamine.

2. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein:

represents a single bond or a double bond;

n is 1;

m is 1;

R 0 is a group selected from:

(a) hydrogen,

(b) C 1-6 -alkyl,

(c) C 3-7 -cycloalkyl,

(d) hydroxy-C 1-4 -alkyl,

(e) —COOR 6 ,

(f) —CONR 5 R 5,

(h) —CN,

(i) aryl, and

(j) heteroaryl,

wherein when R 0 is or includes a heteroaryl or aryl residue, each heteroaryl or aryl residue can be optionally substituted in one or more positions with a substituent independently selected from:

(a) halogen,

(b) C 1-4 -alkyl,

(c) C 1-4 -alkylthio,

(d) C 1-4 -alkoxy,

(e) —CF 3 ,

(f) —CN, and

(g) hydroxymethyl; and

R 3 is a group selected from:

3. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein X is —NR 6 .

4. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein

represents a double bond;

R 0 is a group selected from:

(a) hydrogen,

(b) C 1-6 -alkyl,

(c) C 3-7 -cycloalkyl,

(d) hydroxy-C 1-4 -alkyl,

(f) —CN,

(g) aryl, and

(h) heteroaryl,

wherein any heteroaryl or aryl residue is optionally independently substituted in one or more positions with a substituent selected from:

(a) halogen,

(b) C 1-4 -alkyl,

(c) C 1-4 -alkylthio,

(d) C 1-4 -alkoxy,

(e) —CF 3 ,

(f) —CN, and

(g) hydroxymethyl;

R 1 is a group selected from:

(a) aryl, and

(b) heteroaryl,

wherein any heteroaryl or aryl residue is optionally independently substituted in one or more positions with a substituent selected from:

(a) halogen,

(b) C 1-6 -alkyl,

(c) fluoro-C 1-6 -alkyl,

(d) C 3-7 -cycloalkyl,

(e) C 2-6 -alkenyl,

(f) fluoro-C 2-6 -alkenyl,

(g) ethynyl,

(h) hydroxy-C 1-4 -alkyl,

(i) hydroxy,

(j) C 1-6 -alkoxy,

(k) fluoro-C 1-6 -alkoxy,

(l) —SCF 3 ,

(m) —SCF 2 H,

(n) —SO 2 NR 5 R 5 ,

(o) —S(O) e R 8 , wherein e is 0, 1, or 2,

(p) —CN,

(q) —NR 5 R 5 ,

(r) —NHSO 2 R 8 ,

(s) —NR 6 COR 8 ,

(t) —NO 2 ,

(u) —CONR 5 R 5 , and

(v) —C(═O)R 8 ;

R 2 is a group selected from:

(a) hydrogen,

(b) halogen,

(c) C 1-6 -alkyl,

(d) C 3-7 -cycloalkyl,

(e) hydroxy-C 1-4 -alkyl,

(f) hydroxy,

(g) C 1-6 -alkoxy,

(h) —SCF 3 ,

(i) —SCF 2 H,

(j) —SO 2 NR 5 R 5 ,

(k) —S(O) e R 8 , wherein e is 0, 1, 2 or 3,

(l) —CN,

(m) —NR 5 R 5 ,

(n) —NHSO 2 R 8

(o) —NR 6 COR 8 ,

(p) —CONR 5 R 5 ,

(q) —OCONR 5 R 5 ,

(r) —C(═O)R 8 , and

(s) —OR 11 ;

R 3 is a group selected from:

R 4 is a group selected from:

(a) hydrogen,

(b) C 1-4 -alkyl, and

(c) hydroxy-C 1-4 -alkyl;

each R 5 is independently selected from:

(a) hydrogen, and

(b) C 1-3 -alkyl,

or two R 5 groups together with the nitrogen to which they are attached form a heterocyclic ring;

each R 6 is independently selected from:

(a) hydrogen,

(b) methyl, and

(c) ethyl;

R 7 is selected from:

(a) hydrogen,

(b) C 1-4 -alkyl,

(c) 2-cyanoethyl,

(d) 2-hydroxyethyl,

(e) C 3-4 -alkenyl,

(f) C 3-7 -cycloalkyl,

(h) C 3-4 -cycloalkyl-C 1-4 -alkyl, and

(i) C 1-4 -alkoxy-C 2-4 -alkyl;

each R 8 is independently selected from:

(a) C 1-3 -alkyl,

(b) C 3-7 -cycloalkyl,

(c) aryl, and

(d) heteroaryl,

wherein any heteroaryl or aryl residue is optionally independently substituted in one or more positions with a substituent selected from:

(a) fluorine,

(b) chlorine,

(c) bromine,

(d) C 1-4 -alkyl,

(e) C 1-4 -alkylthio,

(f) C 1-4 -alkoxy,

(g) —CF 3 ,

(h) —CN, and

(i) hydroxymethyl;

R 9 is selected from:

(a) hydrogen,

(b) C 1-4 -alkyl,

(c) —NR 6 R 6 , provided that the said —NR 6 R 6 group is not attached to a carbon atom adjacent to a ring nitrogen atom,

(d) hydroxy, provided that the said hydroxy group is not attached to a carbon atom adjacent to a ring nitrogen atom, and

(e) hydroxymethyl;

each R 10 is independently selected from:

(a) hydrogen,

(b) hydroxy-C 2-4 -alkyl,

(c) C 1-3 -alkoxy-C 2-4 -alkyl,

(d) C 1-4 -alkyl,

(e) cyclopropyl, and

(f) cyclobutyl;

R 11 is selected from

(a) —CH 2 CN, and

(b) benzyl; and

each R 12 is independently selected from:

(a) hydrogen,

(b) C 1-2 -alkyl, and

(c) hydroxy-C 1-2 -alkyl.

5. A compound according to claim 4 , or a pharmaceutically acceptable salt thereof, wherein:

R 0 is a group selected from:

(a) hydrogen,

(b) methyl, and

(c) hydroxymethyl;

R 1 is a group selected from:

(a) aryl, and

(b) heteroaryl;

wherein any heteroaryl or aryl residue is optionally independently substituted in one or more positions with a substituent selected from:

(a) halogen,

(b) methyl,

(c) trifluoromethyl,

(d) methoxy,

(e) t-butyl, and

(f) —CN;

R 2 is a group selected from:

(a) hydrogen,

(b) fluorine,

(c) chlorine,

(d) bromine,

(e) hydroxy,

(f) methoxy,

(g) ethoxy,

(h) iso-propoxy,

(i) —OCON(Me) 2 , and

(j) —OR 11 ;

R 4 is hydrogen;

R 7 is selected from:

(a) hydrogen,

(b) methyl,

(c) n-propyl,

(d) i-propyl, and

(e) 2-methoxyethyl;

R 9 is selected from:

(a) hydrogen,

(b) methyl,

(c) —NH 2 , provided that the said —NH 2 group is not attached to a carbon atom adjacent to a ring nitrogen atom,

(d) hydroxy, provided that the said hydroxy group is not attached to a carbon atom adjacent to a ring nitrogen atom, and

(e) hydroxymethyl;

each R 10 is independently selected from:

(a) hydrogen,

(b) methyl,

(c) ethyl,

(d) i-propyl,

(e) 2-hydroxyethyl,

(f) 2-methoxyethyl,

(g) cyclopropyl, and

(h) cyclobutyl;

R 11 is selected from

(a) —CH 2 CN,

(b) benzyl; and

each R 12 is independently selected from:

(a) hydrogen,

(b) methyl, and

(c) hydroxymethyl.

6. A compound according to claim 5 , or a pharmaceutically acceptable salt thereof, wherein:

R 1 is a group selected from:

(a) phenyl,

(b) pyridyl, and

(c) 2-thienyl,

wherein any heteroaryl or aryl residue is optionally independently substituted in one or more positions with a substituent selected from:

(a) chlorine,

(b) fluorine,

(c) methyl,

(d) trifluoromethyl,

(e) methoxy, and

(f) —CN;

R 2 is a group selected from:

(a) hydrogen,

(b) fluorine,

(c) hydroxy,

(d) methoxy,

(e) ethoxy,

(f) iso-propoxy,

(g) —OCON(Me) 2 , and

(h) —OR 11 ; and

R 11 is selected from

(a) —CH 2 CN,

(b) benzyl.

7. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein:

R 3 is a group selected from:

R 4 is hydrogen or methyl;

R 9 is hydrogen; and

R 10 is each independently selected from:

(a) hydrogen, and

(b) methyl.

8. A compounds according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein:

R 3 is

R 4 is H or methyl; and

each R 10 is independently selected from:

(a) hydrogen, and

(b) methyl.

9. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof, of formula (Ib):

wherein

R 0 is a group selected from:

(a) hydrogen,

(b) methyl, and

(c) hydroxymethyl;

R 1 is a group selected from:

(a) phenyl,

(b) 2-naphthyl,

(c) 2-thienyl, and

(d) 6-chloroimidazo[2,1-b][1,3]thiazol-5-yl;

wherein any heteroaryl or aryl residue is optionally independently substituted in one, two or three positions with a substituent selected from:

(a) chlorine,

(b) fluorine,

(c) bromine,

(d) methyl,

(e) trifluoromethyl,

(f) methoxy, and

(g) —CN;

R 2 is a group selected from:

(a) hydrogen,

(b) fluorine,

(c) hydroxy,

(d) methoxy,

(e) ethoxy,

(f) iso-propoxy,

(g) —OCON(Me) 2 , and

(h) —OR 11 ; and

R 11 is selected from

(a) —CH 2 CN, and

(b) benzyl.

10. A compound according to claim 1 , wherein or a pharmaceutically acceptable salt thereof, wherein:

represents a single bond;

R 1 is a group selected from:

(a) phenyl,

(b) pyridyl, and

(c) 2-thienyl,

wherein any heteroaryl or aryl residue is optionally independently substituted in one or more positions with a substituent selected from:

(a) chlorine,

(b) fluorine,

(c) methyl,

(d) trifluoromethyl,

(e) methoxy, and

(f) —CN;

R 2 is a group selected from:

(a) hydrogen,

(b) fluorine,

(c) hydroxy,

(d) methoxy,

(e) ethoxy,

(f) iso-propoxy,

(g) —OCON(Me) 2 , and

(h) —OR 11 ; and

R 11 is selected from:

(a) —CH 2 CN and

(b) benzyl.

11. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof, which is a compound selected from:

1-(Phenylsulfonyl)-4-(piperazin-1-ylmethyl)-1H-indole,

4-(1,4-Diazepan-1-ylmethyl)-1-(phenylsulfonyl)-1H-indole,

1-{[1-(Phenylsulfonyl)-1H-indol-4-yl]methyl}pyrrolidin-3-amine,

1-{[1-(Phenylsulfonyl)-1H-indol-4-yl]methyl}pyrrolidin-3-amine,

1-[(4-Methylphenyl)sulfonyl]-4-(piperazin-1-ylmethyl)-1H-indole,

1-[(4-Methylphenyl)sulfonyl]-4-[(3-methylpiperazin-1-yl)methyl]-1H-indole,

4-(1,4-Diazepan-1-ylmethyl)-1-[(4-methylphenyl)sulfonyl]-1H-indole,

4-[(4-Methyl-1,4-diazepan-1-yl)methyl]-1-[(4-methylphenyl)sulfonyl]-1H-indole,

1-[(4-Methylphenyl)sulfonyl]-4-[(4-methylpiperazin-1-yl)methyl]-1H-indole,

4-[(4-Isopropylpiperazin-1-yl)methyl]-1-[(4-methylphenyl)sulfonyl]-1H-indole,

1-[(4-Methylphenyl)sulfonyl]-4-[(4-propylpiperazin-1-yl)methyl]-1H-indole,

1-[(4-Methylphenyl)sulfonyl]-4-(pyrrolidin-1-ylmethyl)-1H-indole,

1-[(2-Methoxy-5-methylphenyl)sulfonyl]-4-(piperazin-1-ylmethyl)-1H-indole,

1-[(2-Methoxy-5-methylphenyl)sulfonyl]-4-[(3-methylpiperazin-1-yl)methyl]-1H-indole,

N-({1-[(2-Methoxy-5-methylphenyl)sulfonyl]-1H-indol-4-yl}methyl)piperidin-4-amine,

1-Isopropyl-N-({1-[(2-methoxy-5-methylphenyl)sulfonyl]-1H-indol-4-yl }methyl)piperidin-4-amine,

1-[(2-Methoxy-5-methylphenyl)sulfonyl]-4-[(2-methylpyrrolidin-1-yl)methyl]-1 H-indole,

1-[(2-Methoxy-5-methylphenyl)sulfonyl]-4-[(3-methylpiperazin-1-yl)methyl]indoline,

1-[(2-Methoxy-5-methylphenyl)sulfonyl]-4-[(4-methylpiperazin-1-yl)methyl]indoline,

1-[(2-Methoxy-5-methylphenyl)sulfonyl]-4-(pyrrolidin-1-ylmethyl)indoline,

({1-[(2-Methoxy-5-methylphenyl)sulfonyl]-2,3-dihydro-1H-indol-4-yl}methyl)dimethylamine,

1-[(4-Fluorophenyl)sulfonyl]-4-[(3-methylpiperazin-1-yl)methyl]-1H-indole,

4-(1,4-Diazepan-1-ylmethyl)-1-[(4-fluorophenyl)sulfonyl]-1H-indole,

1-[(4-Fluorophenyl)sulfonyl]-4-(pyrrolidin-1-ylmethyl)-1H-indole,

({1-[(4-Fluorophenyl)sulfonyl]-1H-indol-4-yl}methyl)dimethylamine,

1-[(4-Fluorophenyl)sulfonyl]-4-(piperazin-1-ylmethyl)-1H-indole,

1-[(2-Methylphenyl)sulfonyl]-4-(piperazin-1-ylmethyl)-1H-indole,

1-[(2-Methylphenyl)sulfonyl]-4-[(4-methylpiperazin-1-yl)methyl]-1H-indole,

1-({1-[(2-Methylphenyl)sulfonyl]-1H-indol-4-yl}methyl)pyrrolidin-3-ol,

1-[(2-Methylphenyl)sulfonyl]-4-(pyrrolidin-1-ylmethyl)-1H-indole,

2-[Methyl({1-[(2-methylphenyl)sulfonyl]-1H-indol-4-yl}methyl)amino]ethanol,

N,N-Dimethyl-1-{1-[(2-methylphenyl)sulfonyl]-1H-indol-4-yl}methanamine,

4-(piperazin-1-ylmethyl)-1-{[3-(trifluoromethyl)phenyl]sulfonyl}-1H-indole,

{(2R)-1-[(1-{[3-(Trifluoromethyl)phenyl]sulfonyl}-1H-indol-4-yl)methyl]pyrrolidin-2-yl}methanol,

4-(Pyrrolidin-1-ylmethyl)-1-{[3-(trifluoromethyl)phenyl]sulfonyl}-1H-indole,

2-{Methyl[(1-{[3-(trifluoromethyl)phenyl]sulfonyl}-1H-indol-4-yl)methyl]amino}ethanol,

N,N-Dimethyl-1-(1-{[3-(trifluoromethyl)phenyl]sulfonyl}-1H-indol-4-yl)methanamine,

4-(piperazin-1-ylmethyl)-1-(2-thienylsulfonyl)-1H-indole,

N-Ethyl-N-{[1-(2-thienylsulfonyl)-1H-indol-4-yl]methyl}ethanamine,

4-(Pyrrolidin-1-ylmethyl)-1-(2-thienylsulfonyl)-1H-indole,

4-[(4-Propylpiperazin-1-yl)methyl]-1-(2-thienylsulfonyl)-1H-indole,

N,N-Dimethyl-1-[1-(2-thienylsulfonyl)-1H-indol-4-yl]methanamine,

4-(piperazin-1-ylmethyl)-1-(pyridin-3-ylsulfonyl)-1H-indole,

N,N-Dimethyl-1-[1-(pyridin-3-ylsulfonyl)-1H-indol-4-yl]methanamine,

1-(Pyridin-3-ylsulfonyl)-4-(pyrrolidin-1-ylmethyl)-1H-indole,

1-(Phenylsulfonyl)-4-(pyrrolidin-1-ylmethyl)-1H-indole,

N,N-Dimethyl-1-[1-(phenylsulfonyl)-1H-indol-4-yl]methanamine,

3-Methyl-1-(phenylsulfonyl)-4-(piperazin-1-ylmethyl)-1H-indole,

3-Methyl-4-[(4-methylpiperazin-1-yl)methyl]-1-(phenylsulfonyl)-1H-indole,

3-Methyl-1-(phenylsulfonyl)-4-(pyrrolidin-1-ylmethyl)-1H-indole,

N,N-Dimethyl-1-[3-methyl-1-(phenylsulfonyl)-1H-indol-4-yl]methanamine,

6-Methoxy-1-(phenylsulfonyl)-4-(piperazin-1-ylmethyl)-1H-indole,

{[6-Methoxy-1-(phenylsulfonyl)-1H-indol-4-yl]methyl}dimethylamine,

6-Methoxy-4-{[(3R)-3-methylpiperazin-1-yl]methyl}-1-(phenylsulfonyl)-1H-indole,

6-Methoxy-4-{[(3S)-3-methylpiperazin-1-yl]methyl}-1-(phenylsulfonyl)-1H-indole,

6-Methoxy-4-[(4-methylpiperazin-1-yl)methyl]-1-(phenylsulfonyl)-1H-indole,

4-(1,4-Diazepan-1-ylmethyl)-6-methoxy-1-(phenylsulfonyl)-1H-indole,

6-Methoxy-1-(phenylsulfonyl)-4-(pyrrolidin-1-ylmethyl)-1H-indole,

2-[{[6-Methoxy-1-(phenylsulfonyl)-1H-indol-4-yl]methyl}(methyl)amino]ethanol,

6-Fluoro-1-(phenylsulfonyl)-4-(piperazin-1-ylmethyl)-1H-indole,

4-(1,4-Diazepan-1-ylmethyl)-6-fluoro-1-(phenylsulfonyl)-1H-indole,

6-Fluoro-4-{[(3S)-3-methylpiperazin-1-yl]methyl}-1-(phenylsulfonyl)-1H-indole,

6-Fluoro-4-{[(3R)-3-methylpiperazin-1-yl]methyl}-1-(phenylsulfonyl)-1H-indole,

6-Fluoro-1-(phenylsulfonyl)-4-(pyrrolidin-1-ylmethyl)-1H-indole,

2-[{[6-Fluoro-1-(phenylsulfonyl)-1H-indol-4-yl]methyl}(methyl)amino]ethanol,

{[6-Fluoro-1-(phenylsulfonyl)-1H-indol-4-yl]methyl}dimethylamine,

6-Fluoro-4-[(4-methylpiperazin-1-yl)methyl]-1-(phenylsulfonyl)-1H-indole,

1-(Phenylsulfonyl)-4-(pyrrolidin-1-ylmethyl)-1H-indol-6-yl dimethylcarbamate,

4-(1,4-Diazepan-1-ylmethyl)-1-(phenylsulfonyl)-1H-indol-6-ol,

1-[(4-Fluorophenyl)sulfonyl]-6-methoxy-4-(piperazin-1-ylmethyl)-1H-indole,

6-Methoxy-4-(piperazin-1-ylmethyl)-1-{[3-(trifluoromethyl)phenyl]sulfonyl}-1H-indole,

1-[(2-Chlorophenyl)sulfonyl]-6-methoxy-4-(piperazin-1-ylmethyl)-1H-indole,

1-[(3-Chloro-2-methylphenyl)sulfonyl]-6-methoxy-4-(piperazin-1-ylmethyl)-1H-indole,

1-[(2,5-Dimethoxyphenyl)sulfonyl]-6-methoxy-4-(piperazin-1-ylmethyl)-1H-indole,

2-{[6-Methoxy-4-(piperazin-1-ylmethyl)-1H-indol-1-yl]sulfonyl}benzonitrile,

({1-[(4-Fluorophenyl)sulfonyl]-1H-indol-4-yl}methyl)amine,

N-({1-[(4-Fluorophenyl)sulfonyl]-1H-indol-4-yl}methyl)ethanamine,

7-Methoxy-1-(phenylsulfonyl)-4-(piperazin-1-ylmethyl)-1H-indole,

2-Methyl-1-(phenylsulfonyl)-4-(piperazin-1-ylmethyl)-1H-indole,

Methyl 4-{[1-(phenylsulfonyl)-1H-indol-4-yl]methyl}piperazine-2-carboxylate,

(4-{[1-(Phenylsulfonyl)-1H-indol-4-yl]methyl}piperazin-2-yl)methanol,

(2-Methoxyethyl) {[1-(phenylsulfonyl)-1H-indol-4-yl]methyl}amine,

N-{[1-(Phenylsulfonyl)-1H-indol-4-yl]methyl}propan-2-amine,

4-{[4-(2-Methoxyethyl)piperazin-1-yl]methyl}-1-(phenylsulfonyl)-1H-indole,

((2R)-1-{[1-(Phenylsulfonyl)-1H-indol-4-yl]methyl}pyrrolidin-2-yl)methanol,

4-(Azetidin-1-ylmethyl)-1-(phenylsulfonyl)-1H-indole,

Ethyl 5-methoxy-1-(phenylsulfonyl)-4-(piperazin-1-ylmethyl)-1H-indole-2-carboxylate,

5-Methoxy-N-methyl-1-(phenylsulfonyl)-4-(piperazin-1-ylmethyl)-1H-indole-2-carboxamide,

N-Ethyl-5-methoxy-1-(phenylsulfonyl)-4-(piperazin-1-ylmethyl)-1H-indole-2-carboxamide,

5-Ethoxy-1-(phenylsulfonyl)-4-(piperazin-1-ylmethyl)-N-(2-thienylmethyl)-1H -indole-2-carboxamide,

4-(Azetidin-1-ylmethyl)-6-methoxy-1-(phenylsulfonyl)-1H-indole, 1-(Phenylsulfonyl)-4-(piperazin-1-ylmethyl)-1H-indol-5-ol,

1-(Phenylsulfonyl)-4-piperazin-2-yl-1H-indole,

4-(1,4-Dimethylpiperazin-2-yl)-1-(phenylsulfonyl)-1H-indole,

[7-Methoxy-1-(phenylsulfonyl)-1H-indol-4-yl](piperazin-1-yl)acetonitrile,

4-(Azetidin-1-ylmethyl)-7-methoxy-1-(phenylsulfonyl)-1H-indole,

{[1-(Phenylsulfonyl)-4-(piperazin-1-ylmethyl)-1H-indol-5-yl]oxy}acetonitrile,

5-Isopropoxy-1-(phenylsulfonyl)-4-(piperazin-1-ylmethyl)-1H-indole,

5-(Benzyloxy)-1-(phenylsulfonyl)-4-(piperazin-1-ylmethyl)-1H-indole,

4-{[(2-Hydroxyethyl)(methyl)amino]methyl}-1-(phenylsulfonyl)-1H-indol-5-ol,

4-[(3-Hydroxypyrrolidin-1-yl)methyl]-1-(phenylsulfonyl)-1H-indol-5-ol,

[1-(Phenylsulfonyl)-4-(piperazin-1-ylmethyl)-6-(trifluoromethyl)-1H-indol-2-yl]methanol,

5-Methoxy-1-(phenylsulfonyl)-4-(piperazin-1-ylmethyl)-1H-indole,

5-Ethoxy-1-(phenylsulfonyl)-4-(piperazin-1-ylmethyl)-1H-indole,

1-Phenyl-N-{[1-(phenylsulfonyl)-1H-indol-4-yl]methyl}methanamine,

N-{[5-Methoxy-1-(phenylsulfonyl)-1H-indol-4-yl]methyl}cyclopropanamine,

{[5-Methoxy-1-(phenylsulfonyl)-1H-indol-4-yl]methyl}dimethylamine,

N-{[5-Methoxy-1-(phenylsulfonyl)-1H-indol-4-yl]methyl}cyclobutanamine,

N-{[5-Methoxy-1-(phenylsulfonyl)-1H-indol-4-yl]methyl}-N-methylcyclobutanamine,

1-{[1-(Phenylsulfonyl)-1H-indol-4-yl]methyl}azetidin-3-ol,

4-(Azetidin-1-ylmethyl)-5-methoxy-1-(phenylsulfonyl)-1H-indole,

4-{[4-(Azetidin-1-ylmethyl)-1H-indol-1-yl]sulfonyl}benzonitrile,

2-((2S)-1-{[1-(Phenylsulfonyl)-1H-indol-4-yl]methyl}azetidin-2-yl)propan-2-ol,

4-(Azetidin-1-ylmethyl)-2-methyl-1-(phenylsulfonyl)-1H-indole,

4-(Azetidin-1-ylmethyl)-1-[(2-chlorophenyl)sulfonyl]-1H-indole,

4-(Azetidin-1-ylmethyl)-1-[(5-chloro-2-thienyl)sulfonyl]-1H-indole,

4-(Azetidin-1-ylmethyl)-1-(2-naphthylsulfonyl)-1H-indole,

4-(Azetidin-1-ylmethyl)-1-[(2-methoxy-5-methylphenyl)sulfonyl]-1H-indole,

4-(Azetidin-1-ylmethyl)-1-[(6-chloroimidazo[2,1-b][1,3]thiazol-5-yl)sulfonyl]-1H-indole,

4-(Azetidin-1-ylmethyl)-1-[(4-tert-butylphenyl)sulfonyl]-1H-indole,

4-(Azetidin-1-ylmethyl)-1-[(2,6-difluorophenyl)sulfonyl]-1H-indole,

4-(Azetidin-1-ylmethyl)-1-{[2-(trifluoromethyl)phenyl]sulfonyl}-1H-indole,

3-{[4-(Azetidin-1-ylmethyl)-1H-indol-1-yl]sulfonyl}benzonitrile,

4-(Azetidin-1-ylmethyl)-1-{[4-bromo-2-(trifluoromethyl)phenyl]sulfonyl}-1H-indole,

4-(Azetidin-1-ylmethyl)-1-(2-thienylsulfonyl)-1H-indole,

4-(Azetidin-1-ylmethyl)-1-[(2,5-difluorophenyl)sulfonyl]-1H-indole,

[(5-Methoxy-1-{[3-(trifluoromethyl)phenyl]sulfonyl}-1H-indol-4-yl)methyl]dimethylamine,

4-(Azetidin-1-ylmethyl)-7-(benzyloxy)-1-(methylsulfonyl)-1H-indole,

({1-[(6-Chloroimidazo[2,1-b][1,3]thiazol-5-yl)sulfonyl]-5-methoxy-1H-indol-4-yl}methyl)dimethylamine,

4-[(Dimethylamino)methyl]-1-(phenylsulfonyl)-1H-indol-5-ol,

{[5-Ethoxy-1-(phenylsulfonyl)-1H-indol-4-yl]methyl}dimethylamine,

({5-Ethoxy-1-[(2-methoxy-5-methylphenyl)sulfonyl]-1H-indol-4-yl}methyl)dimethylamine,

{[5-Ethoxy-1-(1-naphthylsulfonyl)-1H-indol-4-yl]methyl}dimethylamine,

{[5-Ethoxy-1-(2-naphthylsulfonyl)-1H-indol-4-yl]methyl}dimethylamine,

({1-[(2-Chlorophenyl)sulfonyl]-5-ethoxy-1H-indol-4-yl}methyl)dimethylamine,

({1-[(3-Chloro-2-methylphenyl)sulfonyl]-5-ethoxy-1H-indol-4-yl}methyl)dimethylamine,

({5-Methoxy-1-[(2-methoxy-5-methylphenyl)sulfonyl]-1H-indol-4-yl}methyl)dimethylamine,

({1-[(2,3-Dichlorophenyl)sulfonyl]-5-methoxy-1H-indol-4-yl}methyl)dimethylamine,

{[5-Ethoxy-1-(quinolin-8-ylsulfonyl)-1H-indol-4-yl]methyl}dimethylamine,

{[5-Ethoxy-1-({5-[1-methyl-3-(trifluoromethyl)-1H-pyrazol-5-yl]-2-thienyl}sulfonyl)-1H-indol-4-yl]methyl}dimethylamine,

({1-[(2,5-Dichlorophenyl)sulfonyl]-5-ethoxy-1H-indol-4-yl}methyl)dimethylamine,

({5-Ethoxy-1-[(2,4,6-trichlorophenyl)sulfonyl]-1H-indol-4-yl}methyl)dimethylamine,

1-[5-Methoxy-1-(phenylsulfonyl)-1H-indol-4-yl]-N-methylmethanamine,

({1-[(2-Methoxy-5-methylphenyl)sulfonyl]-1H-indol-4-yl}methyl)methylamine,

4-[(Dimethylamino)methyl]-6-fluoro-1-(phenylsulfonyl)-1H-indol-5-ol,

1-[6-Fluoro-5-methoxy-1-(phenylsulfonyl)-1H-indol-4-yl]-N,N -dimethylmethanamine,

6-Fluoro-1-(phenylsulfonyl)-4-(pyrrolidin-1-ylmethyl)-1H-indol-5-ol,

6-Fluoro-5-methoxy-1-(phenylsulfonyl)-4-(pyrrolidin-1-ylmethyl)-1H-indole,

4-(Azetidin-1-ylmethyl)-6-fluoro-1-(phenylsulfonyl)-1H-indol-5-ol,

4-(Azetidin-1-ylmethyl)-6-fluoro-5-methoxy-1-(phenylsulfonyl)-1H-indole,

4-{([Ethyl(methyl)amino]methyl}-6-fluoro-1-(phenylsulfonyl)-1H-indol-5-ol,

N-{[6-Fluoro-5-methoxy-1-(phenylsulfonyl)-1H-indol-4-yl]methyl}-N-methylethanamine,

6-Fluoro-4-[(methylamino)methyl]-1-(phenylsulfonyl)-1H-indol-5-ol,

{[6-Fluoro-5-methoxy-1-(phenylsulfonyl)-1H-indol-4-yl]methyl}methylamine,

1-{5-Methoxy-1-[(4-methoxyphenyl)sulfonyl]-1H-indol-4-yl}-N,N-dimethylmethanamine,

1-{1-[(3-Chlorophenyl)sulfonyl]-5-methoxy-1H-indol-4-yl}-N,N-dimethylmethanamine,

1-{1-[(2,5-Difluorophenyl)sulfonyl]-5-methoxy-1H-indol-4-yl}-N,N-dimethylmethanamine,

1-(1-{[4-Fluoro-3-(trifluoromethyl)phenyl]sulfonyl}-5-methoxy-1H-indol-4-yl) -N,N-dimethylmethanamine,

1-[5-Methoxy-1-(quinolin-8-ylsulfonyl)-1H-indol-4-yl]-N,N-dimethylmethanamine,

1-{1-[(2-Chlorophenyl)sulfonyl]-5-methoxy-1H-indol-4-yl}-N,N-dimethylmethanamine,

1-{1-[(2-Chloro-6-methylphenyl)sulfonyl]-5-methoxy-1H-indol-4-yl}-N,N-dimethylmethanamine,

1-{1-[(3-Chloro-4-fluorophenyl)sulfonyl]-5-methoxy-1H-indol-4-yl}-N,N-dimethylmethanamine,

1-{5-Methoxy-1-[(2-methylphenyl)sulfonyl]-1H-indol-4-yl}-N,N-dimethylmethanamine,

2-({4-[(Dimethylamino)methyl]-5-methoxy-1H-indol-1-yl}sulfonyl)benzonitrile,

1-{1-[(2,6-Difluorophenyl)sulfonyl]-5-methoxy-1H-indol-4-yl}-N,N-dimethylmethanamine,

1-{1-[(1,2-Dimethyl-1H-imidazol-4-yl)sulfonyl]-5-methoxy-1H-indol-4-yl}-N,N-dimethylmethanamine,

1-{5-Methoxy-1-[(5-methyl-1-benzothien-2-yl)sulfonyl]-1H-indol-4-yl}-N,N-dimethylmethanamine,

1-{5-Methoxy-1-[(2-methoxy-4-methylphenyl)sulfonyl]-1H-indol-4-yl}-N,N-dimethylmethanamine,

1-{1-[(2,4-Dichlorophenyl)sulfonyl]-5-methoxy-1H-indol-4-yl}-N,N-dimethylmethanamine,

1-{1-[(5-Bromo-2-methoxyphenyl)sulfonyl]-5-methoxy-1H-indol-4-yl}-N,N-dimethylmethanamine,

1-[1-(2,1,3-Benzothiadiazol-4-ylsulfonyl)-5-methoxy-1H-indol-4-yl]-N,N-dimethylmethanamine,

1-[1-(3,4-Dihydro-2H-1,5-benzodioxepin-7-ylsulfonyl)-5-methoxy-1H-indol-4-yl]-N,N-dimethylmethanamine,

1-{1-[(2,5-Dimethoxyphenyl)sulfonyl]-5-methoxy-1H-indol-4-yl}-N,N-dimethylmethanamine,

1-(5-Methoxy-1-{[2-(trifluoromethyl)phenyl]sulfonyl}-1H-indol-4-yl)-N,N-dimethylmethanamine,

1-(5-Methoxy-1-{[4-(trifluoromethoxy)phenyl]sulfonyl}-1H-indol-4-yl)-N,N-dimethylmethanamine,

3-({4-[(Dimethylamino)methyl]-5-methoxy-1H-indol-1-yl}sulfonyl)benzonitrile,

1-[5-Methoxy-1-(pyridin-3-ylsulfonyl)-1H-indol-4-yl]-N,N-dimethylmethanamine,

Methyl {1-[1-(phenylsulfonyl)-1H-indol-4-yl]ethyl}amine,

{1-[1-(Phenylsulfonyl)-1H-indol-4-yl]ethyl}amine,

Dimethyl {1-[1-(phenylsulfonyl)-1H-indol-4-yl]ethyl}amine,

4-(Azetidin-1-ylmethyl)-2,3-dichloro-5-methoxy-1-(phenylsulfonyl)-1H-indole,

4-[(dimethylamino)methyl]-6-methoxy-1-(phenylsulfonyl)-1H-indol-5-ol,

1-[5,6-dimethoxy-1-(phenylsulfonyl)-1H-indol-4-yl]-N,N-dimethylmethanamine,

{[3-chloro-5-methoxy-1-(phenylsulfonyl)-1H-indol-4-yl]methyl}dimethylamine,

{[3-Chloro-5-methoxy-1-(phenylsulfonyl)-1H-indol-4-yl]methyl}methylamine,

{[5-Methoxy-1-(phenylsulfonyl)-1H-indol-4-yl]methyl}amine,

6-Fluoro-4-[1-(methylamino)ethyl]-1-(phenylsulfonyl)-1H-indol-5-ol,

4-[1-(Dimethylamino)ethyl]-6-fluoro-1-(phenylsulfonyl)-1H-indol-5-ol,

{1-[6-Fluoro-5-methoxy-1-(phenylsulfonyl)-1H-indol-4-yl]ethyl}methylamine, and

{1-[6-Fluoro-5-methoxy-1-(phenylsulfonyl)-1H-indol-4-yl]ethyl}dimethylamine,

or a pharmaceutically acceptable salt thereof.

12. A pharmaceutical composition comprising a compound according to claim 1 or a pharmaceutically acceptable salt thereof, in combination with a pharmaceutically acceptable diluent or carrier.

13. A method for reducing body weight or reducing body weight gain, the method comprising administering to a subject in need thereof an effective amount of a compound according to claim 1 or a pharmaceutically acceptable salt thereof.

14. A method for inhibititing 5-HT 6 receptor activity, comprising administering to a subject in need of such treatment an effective amount of a compound according to claim 1 or a pharmaceutically acceptable salt thereof.

15. A cosmetic composition comprising a compound according to claim 1 or a pharmaceutically acceptable salt thereof as an active ingredient, in combination with a cosmetically acceptable diluent or carrier.

16. A method for preparing a compound according to claim 1 , comprising:

a) reacting 4-methyl-1-R 1 -substituted sulfonyl-1H-indole with N-bromosuccinimide;

b) reacting the product from step a) under conditions sufficients to introduce a group selected from

wherein the groups R 1 , R 7 , R 9 , R 10 , and R 12 and X are as defined for formula (I), or a salt or a protected derivative thereof; and optionally thereafter forming a pharmaceutically acceptable salt of the compound of formula (I).

17. A method for preparing the compound of claim 1 , wherein

represents a double bond, comprising:

aa) reacting a 4-bromoindole derivative of formula (III),

wherein m, n, R 0 , R 1 and R 2 are as defined in claim 1 ,

with a sulfonyl chloride of the formula R 1 SO 2 Cl wherein R 1 is as defined in claim 1 , to give a compound of formula (IV):

wherein m, n, R 0 , R 1 and R 2 are as defined in claim 1 ;

bb) reacting the compound of formula (IV) with tributyl(vinyl)stannane in the presence of a palladium complex as a catalyst, to give a compound of formula (V):

wherein m, n, R 0 , R 1 and R 2 are as defined in claim 1 ;

cc) reacting the compound of formula (V) with osmium tetroxide (OsO 4 ) and sodium periodate, to produce the aldehyde derivative of formula (VI):

wherein m, n, R 0 , R 1 and R 2 are as defined in claim 1 ; and

dd) reacting the compound of formula (VI) with an appropriate amine selected from:

wherein X is NR 6 , and R 6 , R 7 , R 9 , R 10 , and R 12 are as defined in claim 1 , or a salt or a protected derivative thereof,

in the presence of a suitable reducing agent,

to produce a compound of formula (I) as defined in claim 1 wherein

represents a double bond; and optionally thereafter forming a pharmaceutically acceptable salt of the compound of formula (I).

18. A method for preparing the compound of claim 1 , wherein

represents a single bond, comprising:

aaa) reacting a compound of formula (IV):

wherein m, n, R 0 , R 1 and R 2 are as defined in claim 1 ;

with a reducing agent to give a compound of formula (VII):

wherein m, n, R 0 , R 1 and R 2 are as defined in claim 1 ;

bbb) reacting a compound of formula (VII) with tributyl(vinyl)stannane in the presence of a palladium complex as a catalyst, to give a compound of formula (XII):

wherein m, n, R 0 , R 1 and R 2 are as defined in claim 1 ;

ccc) reacting the compound of formula (V) with osmium tetroxide (OsO 4 ) and sodium periodate, to produce the aldehyde derivative of formula (XIII):

wherein m, n, R 0 , R 1 and R 2 are as defined in claim 1 ; and

ddd) reacting the compound of formula (XIII) with an appropriate amine selected from:

wherein X is NR 6 , and R 6 , R 7 , R 10 , and R 12 are as defined in claim 1 , or a salt or a protected derivative thereof,

in the presence of a suitable reducing agent,

to produce a compound of formula (I) as defined in claim 1 wherein

represents a single bond; and optionally thereafter forming a pharmaceutically acceptable salt of the compound of formula (I).

19. A compound according to claim 2 , or a pharmaceutically acceptable salt thereof, wherein:

R 0 is a group selected from:

(b) C 1-6 -alkyl,

(c) C 3-7 -cycloalkyl,

(d) hydroxy-C 1-4 -alkyl,

(e) —COOR 6 ,

(f) —CONR 5 R 5 ,

(h) —CN,

(i) aryl, and

(j) heteroaryl,

wherein when R 0 is or includes a heteroaryl or aryl residue, each heteroaryl or aryl residue can be optionally substituted in one or more positions with a substituent independently selected from:

(a) halogen,

(b) C 1-4 -alkyl,

(c) C 1-4 -alkylthio,

(d) C 1-4 -alkoxy,

(e) —CF 3 ,

(f) —CN, and

(g) hydroxymethyl.

20. A compound according to claim 2 , or a pharmaceutically acceptable salt thereof, wherein

each R 2 is independently selected from:

(b) halogen,

(c) C 1-6 -alkyl,

(d) fluoro-C 1-6 -alkyl,

(e) C 3-7 -cycloalkyl,

(f) C 2-6 -alkenyl,

(g) fluoro-C 2-6 -alkenyl,

(h) ethynyl,

(i) hydroxy-C 1-4 -alkyl,

(j) hydroxy,

(k) C 1-6 -alkoxy,

(l) fluoro-C 1-6 -alkoxy,

(m) C 3-7 -cycloalkoxy,

(n) fluoro-C 3-7 -cycloalkoxy,

(o) —SCF 3 ,

(p) —SCF 2 H,

(q) —SO 2 NR 5 R 5 ,

(r) —S(O) e R 8 , wherein e is 0, 1, 2 or 3,

(s) —CN,

(t) —NR 5 R 5 ,

(u) —NHSO 2 R 8 ,

(v) —NR 6 COR 8 ,

(w) —NO 2,

(x) —CONR 5 R 5 ,

(y) —OCONR 5 R 5 ,

(z) —C(═O)R 8 ,

(aa) —COOH,

(ab) C 1-6 -alkoxycarbonyl, and

(ac) —OR 11 .

21. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 0 is halogen.

22. A compound according to claim 21 , or a pharmaceutically acceptable salt thereof, wherein m is 1 or 2.

23. A compound according to claim 2 , or a pharmaceutically acceptable salt thereof, wherein R 2 is hydroxy.

24. A compound according to claim 2 , or a pharmaceutically acceptable salt thereof, wherein R 2 is C 1-6 -alkoxy.

25. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein each R 10 is ethyl.

26. A method according to claim 17 wherein the palladium catalyst in step bb) is bis(triphenylphosphine)palladium(II) diacetate and the reducing agent in step dd) is NaBH 4 , NaBH 3 CN or sodium triacetoxyborohydride.

27. A method according to claim 18 wherein the reducing agent in step aaa) is NaBH 3 CN in trifluoroacetic acid (TFA), the palladium complex in step bbb) is bis(triphenylphosphine)palladium(II) diacetate, and the reducing agent in step ddd) is NaBH 4 , NaBH 3 CN or sodium triacetoxyborohydride.