7-BENZYL-4-(2-METHYLBENZYL)-2,4,6,7,8,9-HEXAHYDROIMIDAZO [1,2-A]PYRIDO[3,4-E]PYRIMIDIN-5(1H)-ONE, ANALOGS THEREOF, AND SALTS THEREOF AND METHODS FOR THEIR USE IN THERAPY

1 . A compound having formula (10)

or a pharmaceutically acceptable salt thereof; wherein R 1 and R 2 are independently selected from the group consisting of H, C 1-4 alkyl, C 1-4 alkylphenyl, C 1-4 alkylphenylketone, C 1-4 benzyl-piperazine, C 1-4 alkylthienyl, C 1-4 alkylpyridinyl, C 1-4 alkylisoxazolidinyl, C 1-4 alkylmorpholinyl, C 1-4 alkylthiazolyl, and C 1-4 alkylpyrazinyl wherein C 1-4 alkyl, C 1-4 alkylphenyl, C 1-4 alkylphenylketone, C 1-4 benzyl-piperazine, C 1-4 alkylthienyl, C 1-4 alkylpyridinyl, C 1-4 alkylisoxazolidinyl, C 1-4 alkylmorpholinyl, C 1-4 alkylthiazolyl, and C 1-4 alkylpyrazinyl are optionally substituted with C 1-4 alkyl, C 1-4 alkoxyl, hydroxyl, perhalogenated C 1-4 alkyl, or halogen, and wherein when R 1 represents CH 2 Ph, R 2 does not represent CH 2 -((2-CH 3 )-Ph).

2 . The compound of claim 1 , wherein R 1 and/or R 2 is a benzyl optionally substituted with one or more of the following substituents on the benzyl ring: X, —CH 3 , —NO 2 , —OCH 3 , —CN, —CXH 2 , —CX 2 H, C 2 -C 4 alkyl, —CX 3 , —CH 2 (CX 3 ), —CH(CX 3 ) 2 , —C(CX 3 ) 3 , —C p X 2p+1 , —OCX 3 , —OC p H 2p+1 , —OC p X 2p+1 , OR m , SR m , NR m R n , NR m C(O)R n , SOR m , SO 2 R m , C(O)R m , and C(O)OR m ;

where R m and R n are independently selected from hydrogen or a C 1 -C 4 alkyl;

where p is an integer from 2 to 20; and

X represents a halogen.

3 . The compound of claim 1 , wherein R 1 is a hydrogen or an unsubstituted benzyl.

4 .- 7 . (canceled)

8 . The compound of claim 1 , wherein the compound is represented by formula (40)

or a pharmaceutically acceptable salt thereof; wherein

wherein R a1 , R a2 , R a3 , R a4 , and R a5 are each independently selected from the group consisting of hydrogen, X, —CH 3 , —NO 2 , —OCH 3 , —CN, —CXH 2 , —CX 2 H, C 2 -C 4 alkyl, —CX 3 , —CH 2 (CX 3 ), —CH(CX 3 ) 2 , —C(CX 3 ) 3 , —C p X 2p+1 , —OCX 3 , —OC p H 2p+1 , —OC p X 2p+1 , OR m , SR m , NR m R n , NR m C(O)R n , SOR m , SO 2 R m , C(O)R m , and C(O)OR m ;

where R m and R n are independently selected from hydrogen or a C 1 -C 4 alkyl;

p is an integer from 2 to 20; and

X represents a halogen.

9 . (canceled)

10 . The compound of claim 8 , wherein the compound is represented by formula (45)

or a pharmaceutically acceptable salt thereof.

11 . (canceled)

12 . (canceled)

13 . The compound of claim 1 having formula (50)

or a pharmaceutically acceptable salt thereof; wherein

R b is selected from the group consisting of X, —CH 3 , —NO 2 , —OCH 3 , —CN, —CXH 2 , —CX 2 H, C 2 -C 4 alkyl, —CX 3 , —CH 2 (CX 3 ), —CH(CX 3 ) 2 , —C(CX 3 ) 3 , —C p X 2p+1 , —OCX 3 , —OC p H 2p+1 , —OC p X 2p+1 , OR m , SR m , NR m R n , NR m C(O)R n , SOR m , SO 2 R m , C(O)R m , and C(O)OR m ;

R a1 , R a2 , R a4 , and R a5 are each independently selected from the group consisting of hydrogen, X, —CH 3 , —NO 2 , —OCH 3 , —CN, —CXH 2 , —CX 2 H, C 2 -C 4 alkyl, —CX 3 , —CH 2 (CX 3 ), —CH(CX 3 ) 2 , —C(CX 3 ) 3 , —C p X 2p+1 , —OCX 3 , —OC p H 2p+1 , —OC p X 2p+1 , OR m , SR m , NR m R n , NR m C(O)R n , SOR m , SO 2 R m , C(O)R m , and C(O)OR m ;

where R m and R n are independently selected from hydrogen or a C 1 -C 4 alkyl;

p is an integer from 2 to 20;

and X represents a halogen.

14 . (canceled)

15 . The compound of claim 13 , wherein the compound is represented by formula (55)

or a pharmaceutically acceptable salt thereof.

16 .- 18 . (canceled)

19 . The compound of claim 13 , wherein R b is a CH 3 or a OCH 3 substituent.

20 . (canceled)

21 . A composition comprising a salt of a compound of claim 1 .

22 . (canceled)

23 . The composition according to claim 21 , wherein the salt is a di-salt.

24 . The composition according to claim 23 , wherein the di-salt is a hydrochloride di-salt.

25 . (canceled)

26 . A pharmaceutical composition comprising a compound according to claim 1 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

27 . A method of treatment, comprising administering to a subject in need of such treatment a pharmaceutically acceptable amount of a compound according to claim 1 or a pharmaceutically acceptable salt thereof.

28 .- 119 . (canceled)

120 . A method of identifying whether a subject having cancer is likely to be responsive to administration of compound (1), comprising:

(i) obtaining a biological sample from the subject;

(ii) measuring expression, post-translational modifications, or activity levels of or mutations in at least one dopamine receptor in the sample;

(iii) comparing the levels measured and/or the mutations found in the sample to those for a pre-determined standard; and

(iv) determining whether the subject is likely to be responsive to administration of compound (1), based on the levels measured and/or mutations found in the sample to those for the pre-determined standard.

121 . The method of claim 120 , wherein the dopamine receptor is selected from DRD2, DRD2S, DRD2L, and DRD3.

122 . The method of claim 120 , wherein the dopamine receptor is from the D2-like family of dopamine receptors.

123 . The method of claim 120 , further comprising the step of administering an effective amount of compound (1) to the subject.

124 .- 138 . (canceled)

139 . A method of assessing the effectiveness of or monitoring a subject having cancer and undergoing administration of compound (1), comprising:

(i) obtaining a biological sample from the subject;

(ii) measuring prolactin levels;

(iii) determining whether the subject is likely to be responsive to administration of compound (1), based on the levels measured relative to those for a pre-determined standard.

140 . (canceled)

141 . (canceled)

142 . The compound of claim 10 , wherein R a1 , R a4 , R a5 , are each hydrogen; and R a2 and R a3 are each selected from fluorine or chlorine.

143 . The compound of claim 10 , wherein R a1 , R a2 , R a4 , R a5 , are each hydrogen; and wherein R a3 is OCH 3 .