Benzothiazole derivatives

1. A compound of formula (I),

racemic-diastereomeric mixtures thereof, optical isomers thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, and isotopes, wherein,

Q is H

Y is O or S;

W is H, Cl, Br, I, NO 2 , CN, SCN, OCF 3 , —X q —(C(R 10 ) 2 ) a —Y 1 q —(C(R 10 ) 2 ) a —Z 1 q , or an optionally substituted group selected from the group consisting of alkyl, alkenyl and alkynyl;

Y 1 and X are each independently selected from the group consisting of phenyl, NR 10 , O, S, SO, SO 2 , CF 2 , CFR, C═O, (C═O)NR 10 , SONR 10 , SO 2 NR 10 , NR 10 (C═O), NR 10 SO,

NR 10 SO 2 , NR 10 SO 2 NR 10 , NR 10 (C═O)NR 10 ,

q for each occurrence is independently 0 or 1;

a for each occurrence is independently 0 or an integer from 1 to 5;

R 10 for each occurrence is independently selected from the group consisting of H, optionally substituted aryl, and an optionally substituted alkyl group optionally substituted with one or more of the following: a C 1-6 alkyl group optionally substituted by one or more hydroxy, halo or optionally substituted amino; a C 1-6 alkoxy group optionally substituted by one or more hydroxy, halo or optionally substituted amino; hydroxy; halo; or optionally substituted amino;

Z 1 is H, optionally substituted alkyl or optionally substituted aryl

X 1 is hydrogen, alkyl or hydroxyalkyl;

R 1 and R 2 are each independently hydrogen, halogen, hydroxy, nitro, cyano, COOH, COOX 3 , SX 3 , SO 2 X 3 , SOX 3 , C(O)X 3 , NHC(O)X 3 , C(O)NHX 3 , NHSO 2 X 3 or selected from an optionally substituted group consisting of alkyl, alkenyl, alkynyl, alkoxy, amino, —NHX 3 , —NX 3 X 3 , alkylamino, arylamino, alkylthio, alkylsulfonato, aryl, aryloxy, arylalkyl, arylalkenyl, arylalkynyl, arylalkyloxy, cycloalkyl, —(CH 2 ) m —(CHX 2 )CN, —(CH 2 ) m —(CHX 2 )COOH, —(CH 2 ) m —(CHX 2 )COOX 3 , —(CH 2 ) m —(CHX 2 )SO 2 X 3 , —(CH 2 ) m —(CHX 2 )C(O)X 3 , —(CH 2 ) m —(CHX 2 )C(O)NHX 3 and

—(CH 2 ) m —(CHX 2 )NHSO 2 X 3 provided that the alkylamino and arylamino are attached to the phenyl ring via the nitrogen of the amino group;

where m is 0 to 4;

X for each occurrence is independently H or an optionally substituted moiety selected from the group consisting of alkyl, alkenyl, alkynyl, carbonyl, S(O) p alkyl, S(O) p aryl, S(O) p heterocyclyl, amino, alkoxy, alkylthio, arylthio, perhaloalkyl, aryl, aryloxy, arylalkyl, and arylalkyloxy;

p is 0, 1 or 2;

X 3 for each occurrence is independently H or an optionally substituted moiety selected from the group consisting of mono- or di-alkylamino, alkyl, alkenyl, alkynyl, aryl; and arylalkyl;

R 3 is hydrogen, or an optionally substituted moiety selected from the group consisting of carbonyl, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, arylalkyl, amino, alkylamino, arylamino, alkoxy; and acyl;

where each of the optionally substituted moieties described hereinabove is optionally substituted by one or more substituents each independently selected from the group consisting of oxo, amino, nitro, mono- or bi-(C 1 –C 6 )alkylamino, hydroxy, nitrile, chloro, fluoro, bromo, iodo, CF 3 , (C 1 –C 6 )alkyl, —C(O)(C 1 –C 6 )alkyl, —COOH, —COO(C 1 –C 6 )alkyl, —S—(C 1 –C 6 )alkyl, —S-aryl, (C 1 –C 6 )alkoxy, —SO 2 NH 2 , phenyl, phenyl(C 1 –C 6 )alkyl, —O—(C 1 –C 6 )alkyl-OH, —O—(C 1 –C 6 )alkyl-O—(C 1 —C 6 )alkyl, —O—(C 2 –C 6 )alkyl-N—((C 1 –C 6 )alkyl) n , —N—(C 1 –C 6 )alkyl-OH, —N—(C 1 –C 6 )alkyl-O—(C 1 –C 6 )alkyl, —C(O)NH 2 , —C(O)N((C 1 –C 6 )alkyl) n , , —S(O) n (C 1 –C 6 )alkyl; and —S(O) n aryl—where the alkyl groups mentioned herein optionally have one or more unsaturated bonds in the alkyl portion;

n is 0, 1 or 2;

provided that

1) when Q is H; Y is O; R 1 and R 2 are each hydrogen, halogen, alkyl, alkoxy, alkylthio, carboxyalkyl or optionally substituted phenyl; and X 1 is hydrogen or alkyl; then R 3 is not alkyl, alkenyl, alkoxy, cycloalkyl or optionally substituted phenyl;

2) when Q is H; Y is O; R 1 and R 2 are each hydrogen, halogen, alkyl, alkoxy, alkylthio, carboxyalkyl or optionally substituted phenyl; then X 1 and R 3 are not taken together to form

3) when W is Cl, Br or I; Q is hydrogen; Y is O; X 1 is H; then R 3 is not

or phenyl optionally substituted by 1 to 3 substituents independently selected from the group consisting of amino, mono- or bi-(C 1 –C 6 )alkylamino, hydroxy, chloro, fluoro, bromo, iodo, (C 1 –C 6 )alkyl, (C 1 –C 6 )alkoxy and —SO 2 NH 2 ;

4) when W is Cl, Br or I; Q is H; R 1 is 7-Cl; R 2 is H; and X 1 is alkyl; then R 3 is not alkyl, alkoxy or cycloalkyl;

5) when W is Cl, Br or I; Q is H; R 1 is 7-Cl; R 2 is H; and X 1 is H; then R 3 is not alkyl or cycloalkylamino;

6) when W is Cl, Br, I or NO 2 ; Q is H; Y is O; X 1 is H; R 1 is OH; R 2 is NO 2 , amino, alkyl, alkoxy, hydroxy lower alkyl or dialkylamino; then R 3 is not H or alkyl;

7) when W is Cl, Br or I; Q is H; Y is O; R 1 is CF 3 , CH 2 F, NO 2 , alkyl or alkoxy; R 2 is H; X 1 is H; then R 3 is not naphthyl or phenyl optionally substituted with halo, CF 3 , alkyl or alkoxy;

8) when W is Cl, Br or I; Q is H; R 1 is alkyl; R 2 is H; X 1 is H or alkyl; then R 3 is not alkyl or alkoxy;

9) when W is Cl; Q is H; Y is S; R 1 and R 2 are each H; X 1 is H; then R 3 is not ethyl;

10) when W is Cl; Q is H; Y is O; R 1 and R 2 are each H; X 1 is H; then R 3 is not n-butyl;

11) when W is H, then R 1 and R 2 are not H at the same time.

12) the compound is not

2. A compound according to claim 1 , racemic-diastereomeric mixtures thereof, optical isomers thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, and isotopes, wherein

the alkyl, alkenyl and alkynyl moieties, and the alkyl portion of a moiety is an optionally substituted straight or branched chain having one to eight carbon atoms;

the aryl moiety and the aryl portion of a moiety is an optionally substituted phenyl,

or naphthyl.

3. A compound according to claim 2 , racemic-diastereomeric mixtures thereof, optical isomers thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, and isotopes, wherein

R 3 is an optionally substituted moiety selected from the group consisting of (C 1 –C 8 )alkyl, phenyl, phenyl(C 1 –C 8 )alkyl, cycloalkyl and cycloalkyl(C 1 –C 8 )alkyl.

4. A compound of formula (IA),

racemic-diastereomeric mixtures thereof, optical isomers thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, and isotopes, wherein

W is NO 2 or CN;

Y is O or S;

R 1 is in the 7-position and is hydrogen, methyl, ethyl, allyl, phenyl, benzyl, —CH 2 —C(O)—CH 3 , —CH 2 —CO 2 -t-Bu, —CH 2 —SO 2 -aryl, -alkyl-CN, or -alkyl(CN)(CH 2 -aryl);

X 1 is hydrogen, alkyl or hydroxyalkyl;

R 3 is selected from the group consisting of ethyl, n-butyl, t-butyl, n-propyl, allyl, hydroxyalkyl, aminoalkyl, -alkyl-NH-alkyl-OH, -alkyl-O-alkyl-OH,di-hydroxyalkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, hydroxycycloalkyl, alkylesteralkyl, 2,4-dimethoxyphenyl, 3,5-trifluoromethylphenyl, 3-chlorophenyl, 4-chlorophenyl 2,6-dichlorophenyl, 2-methylphenyl, 3-methylphenyl, (substituted phenyl)alkyl, phenylalkyl, heterocyclylalkyl, N-alkylaminoalkyl and N,N-dialkylaminoalkyl.

5. A compound according to claim 4 , racemic-diastereomeric mixtures thereof, optical isomers thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, and isotopes, wherein R 1 is hydrogen and X 1 is hydrogen.

6. A compound according to claim 4 , racemic-diastereomeric mixtures thereof, optical isomers thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, and isotopes, wherein

W is NO 2 ;

Q is hydrogen;

R 1 is in the 7-position and is hydrogen, methyl, ethyl or phenyl;

R 2 are each hydrogen;

X 1 is hydrogen; and

R 3 is selected from the group consisting of ethyl, n-Bu, t-Bu, n-Pr, allyl, cyclopropyl, cyclobutyl, 2,4-dimethoxyphenyl, 3,5-bis-trifluoromethylphenyl, 3-chlorophenyl, 4-chlorophenyl, 2,6-dichlorophenyl, 2-methylphenyl and 3-methylphenyl.

7. A compound according to claim 3 , racemic-diastereomeric mixtures thereof, optical isomers thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, and isotopes, wherein

Q is H;

W is NO 2 ;

Y is S;

R 1 is in the 7-position and is hydrogen, —CH 2 —SO 2 -phenyl, —CH 2 —CN, —CH(CH 3 )(CN), or —CH(CN)(CH 2 -phenyl);

R 2 is hydrogen;

X 1 is hydrogen, methyl or —(CH 2 ) 2 —OH;

R 3 is selected from the group consisting of ethyl, benzyl, EtOH, n-PrOH, n-BuOH, n-pentanol, n-hexanol, —(CH 2 ) 2 —NH—(CH 2 ) 2 —OH, —(CH 2 ) 2 —O—(CH 2 ) 2 —OH, —CH(CH 2 CH 3 )(CH 2 OH), —CH(CH 2 OH)(CH 2 -i-Pr), 2,3-di-hydroxy-propyl, 2-hydroxypropyl, —CH(CH 3 )(CH 2 OH), —C(CH 3 ) 2 (CH 2 OH), —CH 2 (CH 3 )(CH 2 OCH 3 ), 1,3-dihydroxyisopropyl, —CH(CH 2 OH)(CH 2 CH 2 SCH 3 ), cyclopropyl, cyclopropylmethyl, 4-hydroxycyclohexyl, 3-chlorophenyl, 4-chlorophenyl, 2-methylphenyl, 3-methylphenyl, 4-aminobenzyl, (4-aminophenyl)ethyl, —(CH 2 ) 3 —N(Et) 2 , and —(CH 2 ) 2 —N(Me).

8. A compound according to claim 3 , racemic-diastereomeric mixtures thereof, optical isomers thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, and isotopes, wherein

Y is O;

R 1 is in the 7-position and is hydrogen, —CH 2 —SO 2 -phenyl, —CH 2 —CN, —CH(CH 3 )(CN), or —CH(CN)(CH 2 -phenyl);

R 2 is hydrogen;

X 1 is hydrogen, methyl or —(CH 2 ) 2 —OH;

R 3 is selected from the group consisting of benzyl, EtOH, n-PrOH, t-BuOH, n-hexanol, aminoethyl, aminopropyl, —(CH 2 ) 2 —NH—(CH 2 ) 2 —OH, —(CH 2 ) 2 —O—(CH 2 ) 2 —OH, —CH(CH 2 CH 3 )(CH 2 OH),

—CH(CH 2 OH)(CH 2 -i-Pr), 2,3-di-hydroxy-propyl, 2-hydroxypropyl, —CH(CH 3 )(CH 2 OH), 1,3-dihydroxyisopropyl, —CH(CH 2 OH)(CH 2 CH 2 SCH 3 ), cyclobutyl, 4-hydroxycyclohexyl, —CH(COOEt)(CH 2 ) 2 —SCH 3 , —(CH 2 ) 2 —COOEt, —(CH 2 ) 5 —COOEt, (2-aminophenyl)methyl, 4-aminobenzyl, (4-aminophenyl)ethyl, —C(CH 3 ) 2 (phenyl), —CH 2 (2,4-difluorophenyl), —CH(i-Pr)(COOEt), —CH(i-Pr) (CH 2 OH), 3-(N-methylamino)propyl, —(CH 2 ) 3 —N(Et) 2 , —(CH 2 ) 4 —N(Et) 2 , —CH(Me)(CH 2 ) 4 —CH 3 , —CH(Me)(CH 2 ) 3 —N(Et) 2 , and —(CH 2 ) 2 —(4—(SO 2 NH 2 )phenyl).

9. A compound according to claim 3 , racemic-diastereomeric mixtures thereof, optical isomers thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, and isotopes, wherein

W is NO 2 ;

Q is hydrogen;

R 1 is in the 7-position and is —CH 2 —CO 2 -t-Bu, allyl or benzyl;

R are each hydrogen;

X 1 is hydrogen; and

R 3 is ethyl.

10. A compound according to claim 3 , racemic-diastereomeric mixtures thereof, optical isomers thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, and isotopes, wherein

W is NO 2 ;

R 1 is in the 7-position and is hydrogen, —CH(CH 3 )(CN) or —CH(CN)(CH 2 -phenyl); and

R 2 is hydrogen.

11. A compound according to claim 2 , racemic-diastereomeric mixtures thereof, optical isomers thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, and isotopes, wherein

W is NO 2 ;

Q is H;

R 1 and R 2 are each hydrogen.

12. A compound according to claim 3 , racemic-diastereomeric mixtures thereof, optical isomers thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, and isotopes, wherein

W is NO 2 ;

R 1 is hydrogen or is in the 7-position and is —CH 2 —CN, —CH 2 —CONH 2 and —CH 2 —COO-t-Bu;

R 2 is hydrogen;

X 1 is hydrogen or —CH 2 —O—CH 3 ;

R 3 is methyl, ethyl, n-BuOH, —CH 2 CF 3 , —(CH 2 ) 7 —N(Me) 2 , 2-phenyl—phenyl, n-BuOH, —CH 2 CF 3 , —(CH 2 ) 4 —N(Me) 2 , —(CH 2 ) 2 —N(Me) 2 , —(CH 2 ) 3 —NHMe, benzyl or —CH 2 —O—CH 3 .

13. A compound according to claim 1 , racemic-diastereomeric mixtures thereof, optical isomers thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, and isotopes, wherein

W is Cl or Br;

Q is H;

R 3 is an optionally substituted moiety selected from the group consisting of alkyl, alkenyl, phenyl, phenylalkyl, or aminoalkyl.

14. A compound according to claim 13 , racemic-diastereomeric mixtures thereof, optical isomers thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, and isotopes, wherein

R 3 is alkyl, haloalkyl, esteralkyl, N,N-dialkylaminoalkyl, alkenyl, phenyl, phenylalkyl, halophenyl, alkoxyphenyl, aryloxyphenyl or aminoalkyl.

15. A compound according to claim 14 , racemic-diastereomeric mixtures thereof, optical isomers thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, and isotopes, wherein

W is Cl;

R 3 is ethyl, propyl, butyl, t-butyl, 2,4,6-trichlorophenyl, 2,4-dimethoxyphenyl, allyl, 2-bromoethyl, 2-phenoxyphenyl, benzyl, —(CH 2 ) 2 —COOEt, —(CH 2 ) 3 —N(Et) 2 , —(CH 2 ) 4 —N(Et) 2 , or —(CH 2 ) 2 —N(Me) 2 .

16. A compound according to claim 15 , racemic-diastereomeric mixtures thereof, optical isomers thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, and isotopes, wherein R 3 is allyl, 2-bromoethyl, 2-phenoxyphenyl, benzyl, —(CH 2 ) 2 —COOEt, —(CH 2 ) 3 —N(Et) 2 , —(CH 2 ) 4 —N(Et) 2 , or —(CH 2 ) 2 —N(Me) 2 .

17. A compound of the formula

racemic-diastereomeric mixtures thereof, optical isomers thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, and isotopes, wherein

R 3 is ethyl, propyl, t-butyl, 2,4,6-trichlorophenyl or 2,4-dimethoxyphenyl.

18. A compound according to claim 14 , racemic-diastereomeric mixtures thereof, optical isomers thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, and isotopes, wherein

R 1 is hydroxy, nitro, or an optionally substituted moiety selected from the group consisting of alkyl, alkoxy, arylalkyloxy and sulfonato;

R is halo or nitro; and

R 3 is alkyl or phenylalkyl.

19. A compound according to claim 18 , racemic-diastereomeric mixtures thereof, optical isomers thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, and isotopes, wherein

R 1 is hydroxy, nitro, methyl, methoxy, isopropoxy, benzyloxy, 4-fluorobenzyloxy, —O—C(CH 3 ) 2 (C(O)NH 2 ), —O—(CH 2 ) 2 —O—(CH 2 ) 2 —OMe or —O—SO 2 —CF 3 ;

R 2 is Cl or nitro; and

R 3 is ethyl or benzyl.

20. A compound according to claim 19 , racemic-diastereomeric mixtures thereof, optical isomers thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, and isotopes, wherein X 1 is H.

21. A compound according to claim 20 , racemic-diastereomeric mixtures thereof, optical isomers thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, and isotopes, wherein W is Cl; R 1 is in the 7-position; and R 2 is in the 4- or 5-position.

22. A compound of the formula

racemic-diastereomeric mixtures thereof, optical isomers thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, and isotopes, wherein R 1 is methyl, methoxy or isopropoxy.

23. A pharmaceutical composition comprising a compound according to claim 1 and a pharmaceutically acceptable diluent or carrier.

24. A pharmaceutical composition, which composition comprises a pharmaceutically acceptable carrier or diluent and an effective amount of a compound of formula (I) of claim 1 as defined hereinabove, racemic-diastereomeric mixtures thereof, optical isomers thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, and isotopes.

25. A compound according to claim 1 , wherein W is —(CH 2 ) 2 —NH—C(O)—NH—(C(R 10 ) 2 ) a —Z 1 q ; R 1 and R 2 are each H; Q is H; Y is O; X 1 is H; and R 3 is an optionally substituted alkyl.

26. A compound according to claim 25 wherein W is:

—(CH 2 ) 2 —NH—C(O)—NH—Et, —CH 2 —NH—C(O)—NH-ethyl, —CH 2 —NH 2 , —NH-phenyl, —C(O)—NH 2 , —CH 2 —NH—S(O) 2 —Ph, —C(O)—NH-phenyl, —CH 2 —NH—S(O) 2 —CF 3 , —CH 2 —CN, —(CH 2 ) 2 —NH—C(O)—NH-(phenyl), or —(CH 2 ) 2 —NH—C(O)—NH-(p-toluyl).

27. A compound according to claim 26 , wherein R 3 is ethyl.

28. A compound according to claim 1 , wherein W is CN; R 1 and R 2 are each H; Q is H; Y is O; and X 1 is H.

29. A compound according to claim 1 , wherein W is H; and R 1 is —S—X 3 , —S(O)X 3 or —S(O) 2 X 3 .

30. A compound according to claim 1 , wherein W is Br, Cl or p-fluorophenoxy, R 1 and R 2 are each H; Q is H; Y is O; X 1 is H; and R 3 is alkyl-chloro,

-alkyl-COOEt, -alkyl-COOH, -alkyl-(N—(N,N-diethylaminoethyl)-N-(methyl)amino), -alkylamino, or -alkyl-(N,N-diethylaminoethylamino).

31. A compound according to claim 30 , wherein the alkyl group is methylene, ethylene or propylene.

32. A compound according to claim 1 , wherein R 2 is H; Q is H; Y is O; X 1 is H and R 3 is ethyl.

33. A compound according to claim 32 , wherein W is H or Br; and R 1 is in the 7-position of the benzothiazolyl ring and is —C≡CH, —C≡C—CH 2 —N(CH 3 ) 2 , —O—CH(CH 3 ) 2 , phenyl or —CH═CH 2 .

34. A compound according to claim 32 , wherein R 1 is —CH═CH 2 and W is —CH═CH 2 .

35. A compound according to claim 32 , wherein R 1 is H and W is benzyl or p-fluorophenoxy.

36. A compound according to claim 32 , wherein W is F; R 1 is in the 7-position of the benzothiazolyl ring and is H or Cl; and R is in the 5-position of the benzothiazolyl ring and is H or Cl.

37. A compound according to claim 32 , wherein R 1 is H and W is —CH≡CH, —C≡C—Ph, —C≡C—CH 2 —N(CH 3 ) 2 , —C≡C-(4-fluorophenyl), —C≡C-(p-toluyl), —(CH 2 ) 2 —Ph, —(CH 2 ) 2 -(4-fluorophenyl), —CH═CH-phenyl, —CH═CH—CH 2 —N(CH 3 ) 2 , —CH═CH-(4-fluorophenyl) or —CH═CH-(p-toluyl).

38. A compound according to claim 1 , wherein W is p-fluorophenoxy or —(CH 2 ) 3 —NHMe; and R 3 is —CH 2 —C(Me) 2 —CH 2 —N(CH 3 ) 2 .

39. A compound according to claim 1 , wherein R 1 is in the 7-position of the benzothiazolyl ring and is H or CN; R 2 is H; Y is O; Q and X 1 are each H; W is C 1 , NO 2 , —CH 2 —OH, —CH 2 —O—C(O)—NH-Et, —S-phenyl, —O-phenyl, —S—CH 3 , —C(O)-phenyl, —S(O)-phenyl, —S-p-nitrophenyl, —S-p-methylphenyl, —S-p-chlorophenyl, —S-p-methoxyphenyl, —S-m-CF 3 -phenyl, —S-o-chlorophenyl, —C(O)—CH 3 , —S(O) 2 -p-(carboxymethylamino)-phenyl, —NH—C(O)—NH-Et, —NH—C(O)—NH—CH 2 -phenyl, —S-p-chlorophenyl, —S-p-bromophenyl, —S-m-CF 3 -phenyl, or —S-p-fluorophenyl;

R 3 is ethyl.

40. A compound of the formula

wherein W is H, —OCF 3 , —O-Et, F, CH 3 , —OCH 3 , —SO 2 —Me, NH 2 , —NH—C(O)—Me, —NH—CH 2 -phenyl, —NH—S(O) 2 —Me, —NH—S(O) 2 —CH 2 -phenyl, —NH—C(O)—O—CH 2 —CCl 3 , —NH—C(O)—O—CH 2 —Ph, —NH—C(O)—O—Me or NO 2 ;

R 1 is H, F or —CH 2 —S(O) 2 -phenyl; and

R 2 is H, 4-Cl, 4-methyl, 5-methyl, 5-Cl, 5-F or 5-OCH 3 provided that the compound is not