IP Library › Patent Application 15061961

Patent Application

App. No. 15/061,961

COMPOSITIONS AND METHODS FOR THE TREATMENT OF METABOLIC DISORDERS

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Patent No.: US None
App. No.: 15/061,961

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Abstract

The present invention relates to treatment and/or prevention of one or more metabolic disorders utilizing fatostatin A and/or a derivative and/or analog thereof. In other aspects, the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B-C tripartite structure, wherein A, B, and C are identical or non-identical structures and are described in detail herein. In specific aspects, the metabolic disorder includes obesity or diabetes, for example.

Claims (489)

1 . A compound comprising the general formula:

wherein R1 is hydrogen, methyl, ethyl, or propyl;

R2, R3, and R4 are the same or different and are selected from the group consisting of:

a) hydroxy;

b) substituted or unsubstituted C1-10 alkyl;

c) substituted or unsubstituted C2-10 alkenyl;

d) substituted or unsubstituted C2-10 alkynyl;

e) substituted or unsubstituted C3-6 cycloalkyl;

f) substituted or unsubstituted aryl;

g) substituted or unsubstituted heteroaryl;

wherein said substitutions in b), c), d), e), f), and/or g) are optionally further substituted with 1-5 groups selected from the group consisting of:

1) hydroxy;

2) —(C═O)R a ;

3) —(C═O)OR a ;

4) —(C═O)H;

5) —(C═O)OH;

6) —O(CH 2 )nCOOR a , wherein n=1-10;

7) halo;

8) cyano;

9) carboxy;

10) amino;

11) mono-substituted amino;

12) di-substituted amino;

13) amido;

14) mono-substituted amido;

15) di-substituted amido; and

16) any combination thereof,

wherein in 2), 3), or 6) R a is a C1-10 alkyl, C2-10 alkenl, C2-10 alkynyl, C3-6 cycloalkyl, aryl, or heteroaryl;

h) —(C═O)R a ;

i) —(C═O)OR a ;

j) —(C═O)H;

k) —(C═O)OH;

l) —O(CH 2 )nCOOR a , wherein n=1-10,

wherein in h), i), or l), R a is a C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-6 cycloalkyl, aryl or heteroaryl;

m) halo;

n) cyano;

o) carboxy;

p) amino;

q) mono-substituted amino;

r) di-substituted amino,

s) amido;

t) mono-substituted amido; and

u) di-substituted amido;

wherein one or more of said mono-substituted amino, di-substituted amino, mono-substituted amido, and di-substituted amido have a substitution selected from the group consisting of C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-6 cycloalkyl, aryl, heteroaryl, sulfoxide, sulfone, sulfonate, alkyl sulfonate, sulfonic acid, and any combination thereof,

wherein in u) said alkyl, alkenyl, alkynyl, cycloalkyl, aryl or heteroaryl are optionally further substituted with 1-5 groups selected from the group consisting of:

i) hydroxy;

ii) —(C═O)R a ;

iii) —(C═O)OR a ;

iv) —(C═O)H;

v) —(C═O)OH;

vi) —O(CH 2 )nCOOR a , wherein n=1-10,

wherein in ii), iii), or vi) R a is a C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-6 cycloalkyl, aryl or heteroaryl;

vii) halo;

viii) cyano;

ix) carboxy;

x) amino;

xi) mono-substituted amino;

xii) di-substituted amino;

xiii) amido;

xiv) mono-substituted amido;

xv) di-substituted amido; and

xvi) any combination thereof;

R5 is a substituted alkyl, aryl heteroaryl or —SO 2 R wherein R is a substituted alkyl, aryl or heteroaryl; and,

Y1 is nitrogen, Y2 and Y3 are the same or different and are sulfur or methylene.

2 . A compound comprising the general formula:

wherein R1 is substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or heteroaryl;

R2, R3, and R4 are the same or different and are selected from the group consisting of:

a) hydroxy;

b) substituted or unsubstituted C1-10 alkyl;

c) substituted or unsubstituted C2-10 alkenyl;

d) substituted or unsubstituted C2-10 alkynyl;

e) substituted or unsubstituted C3-6 cycloalkyl;

f) substituted or unsubstituted aryl;

g) substituted or unsubstituted heteroaryl;

wherein said substitutions in b), c), d), e), f), and/or g) are optionally further substituted with 1-5 groups selected from the group consisting of:

1) hydroxy;

2) —(C═O)R a ;

3) —(C═O)OR a ;

4) —(C═O)H;

5) —(C═O)OH;

6) —O(CH 2 )nCOOR a , wherein n=1-10;

7) halo;

8) cyano;

9) carboxy;

10) amino;

11) mono-substituted amino;

12) di-substituted amino;

13) amido;

14) mono-substituted amido;

15) di-substituted amido; and

16) any combination thereof,

wherein in 2), 3), or 6) R a is a C1-10 alkyl, C2-10 alkenyl, 2-10 alkynyl, C3-6 cycloalkyl, aryl, or heteroaryl;

h) —(C═O)R a ;

i) —(C═O)OR a ;

j) —(C═O)H;

k) —(C═O)OH;

l) —O(CH 2 )nCOOR a , wherein n=1-10,

wherein in h), i), or l), R a is a C110 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-6 cycloalkyl, aryl or heteroaryl;

m) halo;

n) cyano;

o) carboxy;

p) amino;

q) mono-substituted amino;

r) di-substituted amino,

s) amido;

t) mono-substituted amido; and

u) di-substituted amido;

wherein in u) said alkyl, alkenyl, alkynyl, cycloalkyl, aryl or heteroaryl are optionally further substituted with 1-5 groups selected from the group

consisting of:

i) hydroxy;

ii) —(C═O)R a ;

iii) —(C═O)OR a ;

iv) —(C═O)H;

v) —(C═O)OH;

vi) —O(CH 2 )nCOOR a , wherein n=1-10,

wherein in ii), iii), or vi) R a is a C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-6 cycloalkyl, aryl or heteroaryl;

vii) halo;

viii) cyano;

ix) carboxy;

x) amino;

xi) mono-substituted amino;

xii) di-substituted amino;

xiii) amido;

xiv) mono-substituted amido;

xv) di-substituted amido; and

xvi) any combination thereof;

R5 is a substituted alkyl, aryl, heteroaryl or —SO 2 R wherein R is a substituted alkyl, aryl or heteroaryl;

X is —CH 2 —, oxygen, sulfur, substituted amino, —(C═O)—, or —(C═O)NH—; and,

Y1 is nitrogen, Y2 and Y3 are the same or different and are sulfur or methylene.

3 . A compound comprising the general formula:

wherein R1 is hydrogen, methyl, ethyl, or propyl;

R2, R3, and R4 are the same or different and are selected from the group consisting of:

a) hydroxy;

b) substituted or unsubstituted C1-10 alkyl;

c) substituted or unsubstituted C2-10 alkenyl;

d) substituted or unsubstituted C2-10 alkynyl;

e) substituted or unsubstituted C3-6 cycloalkyl;

f) substituted or unsubstituted aryl;

g) substituted or unsubstituted heteroaryl;

wherein said substitutions in b), c), d), e), f), and/or g) are optionally further substituted with 1-5 groups selected from the group consisting of:

1) hydroxy;

2) —(C═O)R a ;

3) —(C═O)OR a ;

4) —(C═O)H;

5) —(C═O)OH;

6) —O(CH 2 )nCOOR a , wherein n=1-10;

7) halo;

8) cyano;

9) carboxy;

10) amino;

11) mono-substituted amino;

12) di-substituted amino;

13) amido;

14) mono-substituted amido;

15) di-substituted amido; and

16) any combination thereof,

wherein in 2), 3), or 6) R a is a C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-6 cycloalkyl, aryl, or heteroaryl;

h) —(C═O)R a ;

i) —(C═O)OR a ;

j) —(C═O)H;

k) —(C═O)OH;

l) —O(CH 2 )nCOOR a , wherein n=1-10,

wherein in h), i), or l), R a is a C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-6 cycloalkyl, aryl or heteroaryl;

m) halo;

n) cyano;

o) carboxy;

p) amino;

q) mono-substituted amino;

r) di-substituted amino,

s) amido;

t) mono-substituted amido; and

u) di-substituted amido;

wherein in u) said alkyl, alkenyl, alkynyl, cycloalkyl, aryl or heteroaryl are optionally further substituted with 1-5 groups selected from the group consisting of:

i) hydroxy;

ii) —(C═O)R a ;

iii) —(C═O)OR a ;

iv) —(C═O)H;

v) —(C═O)OH;

vi) —O(CH 2 )nCOOR a , wherein n=1-10,

wherein in ii), iii), or vi) R a is a C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-6 cycloalkyl, aryl or heteroaryl;

vii) halo;

viii) cyano;

ix) carboxy;

x) amino;

xi) mono-substituted amino;

xii) di-substituted amino;

xiii) amido;

xiv) mono-substituted amido;

xv) di-substituted amido; and

xvi) any combination thereof;

Y1 is nitrogen, Y2 and Y3 are the same or different and are sulfur or methylene.

4 . A compound comprising the general formula:

wherein X is CH 2 ;

R1 is substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or heteroaryl;

R2, R3, and R4 are the same or different and are selected from the group consisting of:

a) hydroxy;

b) substituted or unsubstituted C1-10 alkyl;

c) substituted or unsubstituted C2-10 alkenyl;

d) substituted or unsubstituted C2-10 alkynyl;

e) substituted or unsubstituted C3-6 cycloalkyl;

f) substituted or unsubstituted aryl;

g) substituted or unsubstituted heteroaryl;

wherein said substitutions in b), c), d), e), f), and/or g) are optionally further substituted with 1-5 groups selected from the group consisting of:

1) hydroxy;

2) —(C═O)R a ;

3) —(C═O)OR a ;

4) —(C═O)H;

5) —(C═O)OH;

6) —O(CH 2 )nCOOR a , wherein n=1-10;

7) halo;

8) cyano;

9) carboxy;

10) amino;

11) mono-substituted amino;

12) di-substituted amino;

13) amido;

14) mono-substituted amido;

15) di-substituted amido; and

16) any combination thereof, wherein in 2), 3), or 6) R a is a C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-6 cycloalkyl, aryl, or heteroaryl;

h) —(C═O)R a ;

i) —(C═O)OR a ;

j) —(C═O)H;

k) —(C═O)OH;

1) —O(CH 2 )nCOOR a , wherein n=1-10,

wherein in h), i), or l), R a is a C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-6 cycloalkyl, aryl or heteroaryl;

m) halo;

n) cyano;

o) carboxy;

p) amino;

q) mono-substituted amino;

r) di-substituted amino,

s) amido;

t) mono-substituted amido; and

u) di-substituted amido;

wherein in u) said alkyl, alkenyl, alkynyl, cycloalkyl, aryl or heteroaryl are optionally substituted with 1-5 groups selected from the group consisting of:

i) hydroxy;

ii) —(C═O)R a ;

iii) —(C═O)OR a ;

iv) —(C═O)H;

v) —(C═O)OH;

vi) —O(CH 2 )nCOOR a , wherein n=1-10,

wherein in ii), iii), or vi) R a is a C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-6 cycloalkyl, aryl or heteroaryl;

vii) halo;

viii) cyano;

ix) carboxy;

x) amino;

xi) mono-substituted amino;

xii) di-substituted amino;

xiii) amido;

xiv) mono-substituted amido;

xv) di-substituted amido; and

xvi) any combination thereof; and,

wherein Y1 is nitrogen, Y2 is sulfur and Y3 is —CH—; or Y1 is nitrogen, Y2 is —CH—, and Y3 is sulfur; or Y1 is —CH═CH—, Y2 is —CH— and Y3 is —CH—.

5 . The compound of claim 1 wherein the R 2 di-substituted amino is substituted with —S(O) 2 —C1-10 alkyl where the C1-10 alkyl is substituted with 1-5 halo.

6 . The compound of claim 1 wherein the R 3 monosubstituted amido has a —S(O) 2 —C-10 alkyl substitution on the amino.

7 . The compound of claim 1 wherein the R 3 di-substituted amido is substituted with —S(O) 2 —C1-10 alkyl.

8 . The compound of claim 7 wherein the R 3 di-substituted amido is substituted with —S(O) 2 —C1-10 alkyl where the C1-10 alkyl is substituted with 1-5 halo.

9 . The compound of claim 1 wherein R 5 is —S(O) 2 R.

10 . The compound of claim 2 wherein the R 2 di-substituted amino is substituted with —S(O) 2 —C1-10 alkyl where the C1-10 alkyl is substituted with 1-5 halo.

11 . The compound of claim 10 where the R 2 monosubstituted amido has a —S(O) 2 —C1-10 alkyl substitution on the amino where the C1-10 alkyl is substituted with 1-5 halo.

12 . The compound of claim 3 wherein the R 2 di-substituted amido is substituted with —S(O) 2 —C1-10 alkyl.

13 . The compound of claim 12 wherein the R 2 di-substituted amido is substituted with —S(O) 2 —C1-10 alkyl where the C1-10 alkyl is substituted with 1-5 halo.

14 . The compound of claim 13 wherein the R 3 di-substituted amido is substituted with —S(O) 2 —C1-10 alkyl.

15 . The compound of claim 14 wherein the R 3 di-substituted amido is substituted with —S(O) 2 —C1-10 alkyl where the C1-10 alkyl is substituted with 1-5 halo.

16 . The compound of claim 15 wherein R 4 is —S(O) 2 R.

17 . The compound of claim 16 wherein where R 3 has one substitution which is —S(O) 2 —C1-10 alkyl.

18 . The compound of claim 17 wherein R 4 is halo.

19 . The compound of claim 4 wherein the R 2 di-substituted amido is substituted with —S(O) 2 —C1-10 alkyl.

20 . The compound of claim 19 wherein the R 2 di-substituted amido is substituted with —S(O) 2 —C1-10 alkyl where the C1-10 alkyl is substituted with 1-5 halo.

21 . The compound of claim 20 wherein the R 3 di-substituted amido is substituted with —S(O) 2 —C1-10 alkyl.

22 . The compound of claim 21 wherein the R 3 di-substituted amido is substituted with —S(O) 2 —C1-10 alkyl where the C1-10 alkyl is substituted with 1-5 halo.

23 . The compound of claim 22 where R 4 —S(O) 2 R.

24 . The compound of claim 4 wherein where R 3 has one substitution which is —S(O) 2 —C1-10 alkyl.

25 . The compound of claim 24 wherein R 4 is halo.

26 . A method of blocking cancer cell growth by selectively inhibiting SREBP activation comprising administering a compound according to claim 1 .

27 . A method of treating cancer comprising administering a compound according to claim 1 .

28 . A method of treating prostate cancer comprising administering a compound according to claim 1 .

29 . A method of treating breast cancer comprising administering a compound according to claim 1 .

30 . A method of treating cancer comprising administering a compound according to claim 4 .

29 . The compound of claim 19 wherein R 1 is methyl, ethyl, or propyl.

30 . The compound of claim 19 wherein R 1 is methyl.

31 . The compound of claim 19 wherein R 1 is ethyl.

32 . The compound of claim 19 wherein R 1 is propyl.

33 . The compound of claim 19 wherein R 2 is hydrogen.

34 . The compound of claim 19 wherein R 2 is cyano.

35 . The compound of claim 19 wherein R 2 is hydroxy.

36 . The compound of claim 19 wherein R 2 is substituted or unsubstituted C1-10 alkyl.

37 . The compound of claim 36 where R 2 is unsubstituted C1-10 alkyl.

38 . The compound of claim 37 where R 2 is substituted C1-C10 alkyl.

39 . The compound of claim 38 . where the R 2 substituted C1-10 alkyl is substituted with 1-5 halo.

40 . The compound of claim 38 . where the R 2 substituted C1-10 alkyl is substituted with 1-5 hydroxy.

41 . The compound of claim 19 wherein R 2 is substituted or unsubstituted C3-6 cycloalkyl.

42 . The compound of claim 19 wherein R 2 is substituted C3-6 cycloalkyl.

43 . The compound of claim 19 wherein R 2 is unsubstituted C3-6 cycloalkyl.

44 . The compound of claim 19 wherein R 2 is —C(O)OH.

45 . The compound of claim 19 wherein R 2 is —C(O)OR a .

46 . The compound of claim 43 wherein R a in the R 2 —C(O)OR a is C1-10 alkyl.

47 . The compound of claim 19 wherein R 2 is amino.

48 . The compound of claim 19 wherein R 2 is mono-substituted amino.

49 . The compound of claim 48 where the R 2 mono-substituted amino is an amino which has a C1-10 alkyl substitution.

50 . The compound of claim 48 where the R 2 mono-substituted amino is an amino which has a C2-10 alkenyl substitution.

51 . The compound of claim 48 where the R 2 mono-substituted amino is an amino which has a C3-6 cycloalkyl substitution.

52 . The compound of claim 48 where the R 2 mono-substituted amino is an amino which has a —S(O) 2 —C1-10 alkyl substitution.

53 . The compound of claim 52 where the R 2 mono-substituted amino is an amino which has a —S(O) 2 —C1-10 alkyl substitution where the C1-10 alkyl is substituted with 1-5 halo.

54 . The compound of claim 19 wherein R 2 is di-substituted amino.

55 . The compound of claim 54 where the R 2 di-substituted amino is an amino which has C1-10 alkyl substitution.

56 . The compound of claim 54 wherein the R 2 di-substituted amino is substituted with C2-10 alkenyl.

57 . The compound of claim 54 wherein the R 2 di-substituted amino is substituted with C3-6 cycloalkyl.

58 . The compound of claim 54 wherein the R 2 di-substituted amino is substituted with —S(O) 2 —C1-10 alkyl.

59 . The compound of claim 58 wherein the R 2 di-substituted amino is substituted with —S(O) 2 —C1-10 alkyl where the C1-10 alkyl is substituted with 1-5 halo.

60 . The compound of claim 19 wherein R 2 is amido.

61 . The compound of claim 19 wherein R 2 is mono-substituted amido.

62 . The compound of claim 61 where the R2 mono-substituted amido has a C1-10 alkyl substitution on the amino

63 . The compound of claim 61 where the R2 mono-substituted amido has a C2-10 alkenyl substitution on the amino.

64 . The compound of claim 61 where the R2 mono-substituted amido has a C3-6 cycloalkyl substitution on the amino.

65 . The compound of claim 61 where the R2 mono-substituted amido has a —S(O) 2 —C1-10 alkyl substitution on the amino.

66 . The compound of claim 65 where the R2 mono-substituted amido has a —S(O) 2 —C1-10 alkyl substitution on the amino where the C1-10 alkyl is substituted with 1-5 halo.

67 . The compound of claim 19 wherein R 2 is di-substituted amido.

68 . The compound of claim 67 wherein the R 2 di-substituted amido is substituted with C1-10 alkyl.

69 . The compound of claim 67 wherein the R 2 di-substituted amido is substituted with C2-10 alkenyl.

70 . The compound of claim 67 wherein the R 2 di-substituted amido is substituted with C3-6 cycloalkyl.

71 . The compound of claim 67 wherein the R 2 di-substituted amido is substituted with —S(O) 2 —C1-10 alkyl.

72 . The compound of claim 65 wherein the R 2 di-substituted amido is substituted with —S(O) 2 —C1-10 alkyl where the C1-10 alkyl is substituted with 1-5 halo.

73 . The compound of claim 19 where R 3 is hydrogen.

74 . The compound of claim 19 where R 3 is halo.

75 . The compound of claim 19 where R 3 is cyano.

76 . The compound of claim 19 where R 3 is hydroxy.

77 . The compound of claim 19 where R 3 is substituted or unsubstituted C1-10 alkyl.

78 . The compound of claim 19 where R 3 is unsubstituted C1-10 alkyl.

79 . The compound of claim 19 where R 3 is substituted C1-10 alkyl.

80 . The compound of claim 79 where the R 3 substituted C1-10 alkyl is substituted with 1-5 halo.

81 . The compound of claim 79 . where the R 3 substituted C1-10 alkyl is substituted with 1-5 hydroxy.

82 . The compound of claim 19 where R 3 is substituted or unsubstituted C1-10 alkenyl.

83 . The compound of claim 19 where R 3 is substituted or unsubstituted C1-10 alkynyl.

84 . The compound of claim 19 where R 3 is substituted or unsubstituted C3-6 cycloalkyl.

85 . The compound of claim 19 where R 3 is —C(O)OH.

86 . The compound of claim 19 where R 3 is —C(O)OR a .

87 . The compound of claim 19 where R 3 is amido.

88 . The compound of claim 19 where R 3 is mono-substituted amido.

89 . The compound of claim 88 where the R 3 mono-substituted amido has a C1-10 alkyl substitution on the amino.

90 . The compound of claim 88 wherein the R 3 mono-substituted amido has a C2-10 alkenyl substitution on the amino.

91 . The compound of claim 88 wherein the R 3 mono-substituted amido has a C3-6 cycloalkyl substitution on the amino.

92 . The compound of claim 88 wherein the R 3 mono-substituted amido has a —S(O) 2 —C1-10 alkyl substitution on the amino.

93 . The compound of claim 92 wherein the R 3 mono-substituted amido has a —S(O) 2 —C1-10 alkyl substitution on the amino where the C1-10 alkyl is substituted with 1-5 halo.

94 . The compound of claim 19 where R 3 is di-substituted amido.

95 . The compound of claim 94 where the R 3 di-substituted amido is substituted with C1-10 alkyl.

96 . The compound of claim 94 wherein the R 3 di-substituted amido is substituted with C2-10 alkenyl.

97 . The compound of claim 94 wherein the R 3 di-substituted amido is substituted with C3-6 cycloalkyl.

98 . The compound of claim 94 wherein the R 3 di-substituted amido is substituted with —S(O) 2 —C1-10 alkyl.

99 . The compound of claim 98 wherein the R 3 di-substituted amido is substituted with —S(O) 2 —C1-10 alkyl where the C1-10 alkyl is substituted with 1-5 halo.

100 . The compound of claim 19 wherein R 4 is H.

101 . The compound of claim 19 wherein R 4 is —C(O)OR a .

102 . The compound of claim 101 wherein the R a in the R 4 —C(O)OR a is C1-10 alkyl.

103 . The compound of claim 19 wherein R 4 is substituted or unsubstituted C1-10 alkyl.

104 . The compound of claim 19 wherein R 4 is unsubstituted C1-10 alkyl.

105 . The compound of claim 19 wherein R 4 is substituted C1-10 alkyl.

106 . The compound of claim 105 wherein the R 4 substituted C1-10 alkyl is substituted with 1-5 hydroxy.

107 . The compound of claim 105 wherein the R 4 substituted C1-10 alkyl is substituted with 1-5 amino.

108 . The compound of claim 105 wherein the R 4 substituted C1-10 alkyl is substituted with 1-5 mono-substituted amino.

109 . The compound of claim 105 wherein the R 4 substituted C1-10 alkyl is substituted with 1-5 di-substituted amino.

110 . The compound of claim 19 wherein R 5 is —S(O) 2 R.

111 . The compound of claim 110 wherein R is substituted alkyl.

112 . The compound of claim 111 where the alkyl is substituted with 1-5 groups selected from the group consisting of hydroxy, —(C═O)R a ; —(C═O)OR a , —(C═O)H, —(C═O)OH, O(CH 2 ) n COOR a , aryl, heteroaryl, fluoro, chloro, bromo, iodo, cyano, carboxy, amino, mono-substituted amino and di-substituted amino, mono-substituted amido and di-substituted amido and any combination thereof; and wherein n=1-10 and wherein R a is a C 1-10 alkyl, C 2-10 alkenyl, C 2-10 alkynyl, or C 3-6 cycloalkyl.

113 . The compound of claim 111 where the alkyl is substituted with 1-5 fluoro.

114 . The compound of claim 110 wherein R is substituted aryl.

115 . The compound of claim 110 wherein R is substituted heteroaryl.

116 . The compound of claim 19 where R 4 is H and R 5 is —S(O) 2 R.

117 . The compound of claim 116 where wherein R is substituted alkyl.

118 . The compound of claim 117 where the alkyl is substituted with 1-5 groups selected from the group consisting of hydroxy, —(C═O)R a ; —(C═O)OR a , —(C═O)H, —(C═O)OH, O(CH 2 ) n COOR a , aryl, heteroaryl, fluoro, chloro, bromo, iodo, cyano, carboxy, amino, mono-substituted amino and di-substituted amino, mono-substituted amido and di-substituted amido and any combination thereof; and wherein n=1-10 and wherein R a is a C 1-10 alkyl, C 2-10 alkenyl, C 2-10 alkynyl, or C 3-6 cycloalkyl.

119 . The compound of claim 118 where the alkyl is substituted with 1-5 fluoro.

120 . A method of blocking cancer cell growth by selectively inhibiting SREBP activation comprising administering a compound according to any one of the above claims.

121 . A method of treating cancer comprising administering a compound according to any one of the above claims.

121 . A method of treating prostate cancer comprising administering a compound according to any one of the above claims.

122 . A method of treating breast cancer comprising administering a compound according to any one of the above claims.

123 . The compound of claim 20 wherein R 1 is alkyl.

124 . The compound of claim 20 wherein R 1 is cycloalkyl.

125 . The compound of claim 20 wherein R 2 is hydrogen.

126 . The compound of claim 20 wherein R 2 is cyano.

127 . The compound of claim 20 wherein R 2 is hydroxy.

128 . The compound of claim 20 wherein R 2 is substituted or unsubstituted C1-10 alkyl.

129 . The compound of claim 20 where R 2 is unsubstituted C1-10 alkyl.

130 . The compound of claim 20 where R 2 is substituted C1-C10 alkyl.

131 . The compound of claim 130 where the R 2 substituted C1-10 alkyl is substituted with 1-5 halo.

132 . The compound of claim 130 where the R 2 substituted C1-10 alkyl is substituted with 1-5 hydroxy.

133 . The compound of claim 20 wherein R 2 is substituted or unsubstituted C3-6 cycloalkyl.

134 . The compound of claim 20 wherein R 2 is substituted C3-6 cycloalkyl.

135 . The compound of claim 20 wherein R 2 is unsubstituted C3-6 cycloalkyl.

136 . The compound of claim 20 wherein R 2 is —C(O)OH.

137 . The compound of claim 20 wherein R 2 is —C(O)OR a .

138 . The compound of claim 137 wherein R a in the R 2 —C(O)OR a is C1-10 alkyl.

139 . The compound of claim 20 wherein R 2 is amino.

140 . The compound of claim 20 wherein R 2 is mono-substituted amino.

141 . The compound of claim 140 where the R 2 mono-substituted amino is an amino which has a C1-10 alkyl substitution.

142 . The compound of claim 140 where the R 2 mono-substituted amino is an amino which has a C2-10 alkenyl substitution.

143 . The compound of claim 140 where the R 2 mono-substituted amino is an amino which has a C3-6 cycloalkyl substitution.

144 . The compound of claim 140 where the R 2 mono-substituted amino is an amino which has a —S(O) 2 —C1-10 alkyl substitution.

145 . The compound of claim 144 where the R 2 mono-substituted amino is an amino which has a —S(O) 2 —C1-10 alkyl substitution where the C1-10 alkyl is substituted with 1-5 halo.

146 . The compound of claim 20 wherein R 2 is di-substituted amino.

147 . The compound of claim 146 wherein the R 2 di-substituted amino is substituted with C1-10 alkyl.

148 . The compound of claim 146 wherein the R 2 di-substituted amino is substituted with C2-10 alkenyl.

149 . The compound of claim 146 wherein the R 2 di-substituted amino is substituted with C3-6 cycloalkyl.

150 . The compound of claim 146 wherein the R 2 di-substituted amino is substituted with —S(O) 2 —C1-10 alkyl.

151 . The compound of claim 150 wherein the R 2 di-substituted amino is substituted with —S(O) 2 —C1-10 alkyl where the C1-10 alkyl is substituted with 1-5 halo.

152 . The compound of claim 20 wherein R 2 is amido.

153 . The compound of claim 20 wherein R 2 is mono-substituted amido.

154 . The compound of claim 153 where the R2 mono-substituted amido has a C1-10 alkyl substitution on the amino.

155 . The compound of claim 153 where the R2 mono-substituted amido has a C2-10 alkenyl substitution on the amino.

156 . The compound of claim 153 where the R2 mono-substituted amido has a C3-6 cycloalkyl substitution on the amino.

157 . The compound of claim 153 where the R2 mono-substituted amido has a —S(O) 2 —C1-10 alkyl substitution on the amino.

158 . The compound of claim 157 where the R2 mono-substituted amido has a —S(O) 2 —C1-10 alkyl substitution on the amino where the C1-10 alkyl is substituted with 1-5 halo.

159 . The compound of claim 20 wherein R 2 is di-substituted amido.

160 . The compound of claim 159 wherein the R 2 di-substituted amido is substituted with C1-10 alkyl.

161 . The compound of claim 159 wherein the R 2 di-substituted amido is substituted with C2-10 alkenyl.

162 . The compound of claim 159 wherein the R 2 di-substituted amido is substituted with C3-6 cycloalkyl.

163 . The compound of claim 159 wherein the R 2 di-substituted amido is substituted with —S(O) 2 —C1-10 alkyl.

164 . The compound of claim 163 wherein the R 2 di-substituted amido is substituted with —S(O) 2 —C1-10 alkyl where the C1-10 alkyl is substituted with 1-5 halo.

165 . The compound of claim 20 wherein X is CH 2 .

166 . The compound of claim 20 wherein X is —O—.

167 . The compound of claim 20 wherein X is —C(O)NH—

168 . The compound of claim 20 where R 3 is hydrogen.

169 . The compound of claim 20 where R 3 is halo.

170 . The compound of claim 20 where R 3 is cyano.

171 . The compound of claim 20 where R 3 is hydroxy.

172 . The compound of claim 20 where R 3 is substituted or unsubstituted C1-10 alkyl.

173 . The compound of claim 20 where R 3 is unsubstituted C1-10 alkyl.

174 . The compound of claim 20 where R 3 is substituted C1-10 alkyl.

175 . The compound of claim 174 where the R 3 substituted C1-10 alkyl is substituted with 1-5 halo.

176 . The compound of claim 174 . where the R 3 substituted C1-10 alkyl is substituted with 1-5 hydroxy.

177 . The compound of claim 20 where R 3 is substituted or unsubstituted C1-10 alkenyl.

178 . The compound of claim 20 where R 3 is substituted or unsubstituted C1-10 alkynyl.

179 . The compound of claim 20 where R 3 is substituted or unsubstituted C3-6 cycloalkyl.

180 . The compound of claim 20 where R 3 is —C(O)OH.

181 . The compound of claim 20 where R 3 is —C(O)OR a .

182 . The compound of claim 20 where R 3 is amido.

183 . The compound of claim 20 where R 3 is mono-substituted amido.

184 . The compound of claim 183 where the R 3 mono-substituted amido has a C1-10 alkyl substitution on the amino.

185 . The compound of claim 183 wherein the R 3 mono-substituted amido has a C2-10 alkenyl substitution on the amino.

186 . The compound of claim 183 wherein the R 3 mono-substituted amido has a C3-6 cycloalkyl substitution on the amino.

187 . The compound of claim 183 wherein the R 3 mono-substituted amido has a —S(O) 2 —C1-10 alkyl substitution on the amino.

188 . The compound of claim 92 wherein the R 3 mono-substituted amido has a —S(O) 2 —C1-10 alkyl substitution on the amino where the C1-10 alkyl is substituted with 1-5 halo.

189 . The compound of claim 20 where R 3 is di-substituted amido.

190 . The compound of claim 189 where the R 3 di-substituted amido is substituted with C1-10 alkyl.

191 . The compound of claim 189 wherein the R 3 di-substituted amido is substituted with C2-10 alkenyl.

192 . The compound of claim 189 wherein the R 3 di-substituted amido is substituted with C3-6 cycloalkyl.

193 . The compound of claim 189 wherein the R 3 di-substituted amido is substituted with —S(O) 2 —C1-10 alkyl.

194 . The compound of claim 193 wherein the R 3 di-substituted amido is substituted with —S(O) 2 —C1-10 alkyl where the C1-10 alkyl is substituted with 1-5 halo.

195 . The compound of claim 20 wherein R 4 is H.

196 . The compound of claim 20 wherein R 4 is —C(O)OR a .

197 . The compound of claim 196 wherein the R a in the R 4 —C(O)OR a is C1-10 alkyl.

198 . The compound of claim 20 wherein R 4 is substituted or unsubstituted C1-10 alkyl.

199 . The compound of claim 20 wherein R 4 is unsubstituted C1-10 alkyl.

200 . The compound of claim 20 wherein R 4 is substituted C1-10 alkyl.

201 . The compound of claim 200 wherein the R 4 substituted C1-10 alkyl is substituted with 1-5 hydroxy.

202 . The compound of claim 200 wherein the R 4 substituted C1-10 alkyl is substituted with 1-5 amino.

203 . The compound of claim 200 wherein the R 4 substituted C1-10 alkyl is substituted with 1-5 mono-substituted amino.

204 . The compound of claim 200 wherein the R 4 substituted C1-10 alkyl is substituted with 1-5 di-substituted amino.

205 . The compound of claim 20 wherein R 5 is —S(O) 2 R.

206 . The compound of claim 205 wherein R is substituted alkyl.

207 . The compound of claim 206 where the alkyl is substituted with 1-5 groups selected from the group consisting of hydroxy, —(C═O)R a ; —(C═O)OR a , —(C═O)H, —(C═O)OH, O(CH 2 ) n COOR a , aryl, heteroaryl, fluoro, chloro, bromo, iodo, cyano, carboxy, amino, mono-substituted amino and di-substituted amino, mono-substituted amido and di-substituted amido and any combination thereof; and wherein n=1-10 and wherein R a is a C 1-10 alkyl, C 2-10 alkenyl, C 2-10 alkynyl, or C 3-6 cycloalkyl.

208 . The compound of claim 206 where the alkyl is substituted with 1-5 fluoro.

209 . The compound of claim 205 wherein R is substituted aryl.

210 . The compound of claim 205 wherein R is substituted heteroaryl.

211 . The compound of claim 20 where R 4 is H and R 5 is —S(O) 2 R.

212 . The compound of claim 211 where wherein R is substituted alkyl.

213 . The compound of claim 212 where the alkyl is substituted with 1-5 groups selected from the group consisting of hydroxy, —(C═O)R a ; —(C═O)OR a , —(C═O)H, —(C═O)OH, O(CH 2 ) n COOR a , aryl, heteroaryl, fluoro, chloro, bromo, iodo, cyano, carboxy, amino, mono-substituted amino and di-substituted amino, mono-substituted amido and di-substituted amido and any combination thereof; and wherein n=1-10 and wherein R a is a C 1-10 alkyl, C 2-10 alkenyl, C 2-10 alkynyl, or C 3-6 cycloalkyl.

214 . The compound of claim 212 where the alkyl is substituted with 1-5 fluoro.

214 a. A method of blocking cancer cell growth by selectively inhibiting SREBP activation comprising administering a compound according to any one of claims 123 - 214 .

214 b. A method of treating cancer comprising administering a compound according to any one of claims 123 - 214 .

214 c. A method of treating prostate cancer comprising administering a compound according to any one of claims 123 - 214 .

214 d. A method of treating breast cancer comprising administering a compound according to any one of claims 123 - 214 .

215 . The compound of claim 21 where R 1 is methyl, ethyl, or propyl.

216 . The compound of claim 21 where R 1 is methyl.

217 . The compound of claim 21 where R 1 is ethyl.

218 . The compound of claim 21 where R 1 is propyl.

219 . The compound of claim 21 where Y 1 is nitrogen, Y 2 is sulfur and Y 3 is —CH—.

220 . The compound of claim 21 where Y 1 is nitrogen, Y 2 is —CH— and Y 3 is sulfur.

221 . The compound of claim 21 where R 3 is mono-substituted amino.

222 . The compound of claim 221 wherein the R 3 mono-substituted amino is an amino which has a —S(O) 2 —C1-10 alkyl substitution.

223 . The compound of claim 222 wherein the C1-10 alkyl in —S(O) 2 —C1-10 alkyl is further substituted with 1-5 halo.

224 . The compound of claim 21 wherein where R 3 is di-substituted amino.

225 . The compound of claim 224 wherein the di-substituted amino has one substitution which is —S(O) 2 —C1-10 alkyl.

226 . The compound of claim 21 wherein R 4 is halo.

227 . A method of blocking cancer cell growth by selectively inhibiting SREBP activation comprising administering a compound according to any one of claims 215 - 226 .

228 . A method of treating cancer comprising administering a compound according to any one of claims 215 - 226 .

229 . A method of treating prostate cancer comprising administering a compound according to any one of claims 215 - 226 .

230 . A method of treating breast cancer comprising administering a compound according to any one of claims 215 - 226 .