Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases

1. A compound having Formula (IIIa):

or a therapeutically acceptable salt thereof, wherein

A 1 is C(A 2 );

A 2 is H;

B 1 is OR 1 , or NHR 1 , wherein R 1 is alkyl substituted with R 10 ;

D 1 is H;

E l is H;

Y 1 is NO 2 ;

G 1 is alkyl substituted with OP(O)(OH)(OH);

R 10 C 3 -C 10 -cycloalkyl, each having one or two CH 2 moieties unreplaced or replaced with independently selected O;

wherein the moiety represented by R 10 is unsubstituted or substituted with one or two or three or four or five substituents independently selected from the group consisting of R 50 , OR 50 , F, Cl, Br, and I; and

R 50 is alkyl.

2. The compound or therapeutically acceptable salt of claim 1 , wherein the compound is selected from the group consisting of:

(5- {5-(4- {[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-[({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)carbamoyl]phenoxy}-7H-pyrrolo[2,3-b]pyridin-7-yl)methyl dihydrogen phosphate;

{5-[5-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-{[(4-{[(trans-4-methoxycyclohexyl)methyl]amino }-3-nitrophenyl)sulfonyl]carbamoyl}phenoxy]-7H-pyrrolo[2,3-b]pyridin-7-yl }methyl dihydrogen phosphate; and

(5-{5-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-[({4- [(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)carbamoyl]phenoxy}-7H-pyrrolo[2,3-b]pyridin-7-yl)methyl dihydrogen phosphate.

3. A pharmaceutical composition comprising the compound or therapeutically acceptable salt of claim 1 and an excipient.

4. A pharmaceutical composition comprising the compound or therapeutically acceptable salt of claim 2 and an excipient.

5. A method for inhibiting anti-apoptotic Bc1-2 protein function in a cell comprising contacting a cell comprising anti-apoptotic Bc1-2 protein with the compound or therapeutically acceptable salt of any one of claims 1 and 2 .