11-Beta HSD1 Inhibitors

Abstract

This invention relates to inhibiting 11βHSD1.

1 - 93 . (canceled) 
   
   
       94 . A method for treating a disease or condition mediated by excess or uncontrolled amounts of cortisol and/or other corticosteroids, the method comprising administering to a subject in need thereof an effective amount of a compound of formula I: 
     
       
         
         
             
             
         
       
     
     wherein:
 R 1  is: 
 i) C 6 -C 18  aryl or heteroaryl including 5-20 atoms, each of which is optionally substituted with from 1-10 R a ; or 
 (ii) C 7 -C 20  aralkyl; heteroaralkyl including 6-20 atoms; arylheterocyclyl including 8-20 atoms; arylcycloalkenyl including 8-20 atoms; or arylheterocycloalkenyl including 8-20 atoms; each of which is optionally substituted with from 1-10 R b ; 
 R 2  is C 6 -C 18  aryl or heteroaryl including 5-20 atoms, each of which is optionally substituted with from 1-10 R c ; 
 X is S(O) n  or S(O) n NR 6 , wherein n is 1 or 2 and R 6  is hydrogen, C 1 -C 12  alkyl, or C 3-16  cycloalkyl; 
 each of V and Y is, independently, CR 7  or N, wherein R 7  is hydrogen or C 1 -C 12  alkyl, provided that Y and V cannot both be CR 7 ; 
 one, two, three, or four of W 1 , Z 1 , W 2 , and Z 2  are each, independently: 
 (i) C 1 -C 12  alkyl; or 
 (ii) oxo; or 
 (iii) C 6 -C 18  aryl or heteroaryl including 5-20 atoms, each of which is optionally substituted with from 1-10 R a ; or 
 (iv) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; and the others are hydrogen; 
 R a  at each occurrence is, independently: 
 (i) halo; NR d R e ; nitro; azido; hydroxy; C 1 -C 12  alkoxy or C 1 -C 12  thioalkoxy, each of which is optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy, heteroaryloxy including 5-20 atoms, or thioaryloxy including 5-20 atoms, each of which is optionally substituted with 1-5 R a′ ; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3-6  cycloalkyloxy, C 3 -C 16  cycloalkenyloxy, heterocyclyloxy including 3-16 atoms, heterocycloalkenyloxy including 3-16 atoms, C 7 -C 20  aralkoxy, or heteroaralkoxy including 6-20 atoms, each of which is optionally substituted with 1-5 R b ; mercapto; cyano; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; or 2 R a  together form C 1 -C 3  alkylenedioxy; 
 (ii) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (iii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; or 
 (iv) C 2 -C 20  alkenyl or C 2 -C 20  alkynyl; or 
 (v) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a ; 
 R a′  at each occurrence is, independently, C 1 -C 12  alkyl, C 1 -C 12  haloalkyl, C 2 -C 12  alkenyl; C 1 -C 12  alkynyl; C 3 -C 16  cycloalkyl; C 3 -C 16  cycloalkenyl, heterocyclyl including 3-16 atoms, heterocycloalkenyl including 3-16 atoms; C 7 -C 20  aralkyl; C 6 -C 16  aryl; heteroaryl including 5-16 atoms; halo; NR d R e ; nitro; azido, hydroxy; C 1 -C 12  alkoxy; C 1 -C 12  thioalkoxy; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy; heteroaryloxy including 5-20 atoms; thioaryloxy including 5-20 atoms; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy; C 3 -C 16  cycloalkenyloxy; heterocyclyloxy including 3-16 atoms; heterocycloalkenyloxy including 3-16 atoms; C 7 -C 20  aralkoxy; heteroaralkoxy including 6-20 atoms; mercapto; cyano; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; or 2 R a′  together form C 1 -C 3  alkylenedioxy; or 2 R a′  together form C 1 -C 3  alkylenedioxy; 
 R b  at each occurrence is, independently: 
 (i) halo; NR d R e ; nitro; azido; hydroxy; oxo, thioxo, ═NR k , C 1 -C 12  alkoxy or C 1 -C 12  thioalkoxy, each of which is optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy, heteroaryloxy including 5-20 atoms, or thioaryloxy including 5-20 atoms, each of which is optionally substituted with 1-5 R a ; C 2 -C 12  alkenyloxy; C 1 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy, C 3 -C 16  cycloalkenyloxy, heterocyclyloxy including 3-16 atoms, heterocycloalkenyloxy including 3-16 atoms, C 7 -C 20  aralkoxy, or heteroaralkoxy including 6-20 atoms, each of which is optionally substituted with 1-5 R b′ ; mercapto; cyano; —C(O)R g , —C(O)OR g , —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; or 2 R b  together form C 1 -C 3  alkylenedioxy, or 
 (ii) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (iii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b′ ; or 
 (iv) C 2 -C 20  alkenyl or C 2 -C 20  alkynyl; or 
 (v) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a ; 
 R b′  at each occurrence is, independently, C 1 -C 12  alkyl or C 1 -C 12  haloalkyl, each of which is optionally substituted with 1-5 R j ; C 2 -C 12  alkenyl; C 2 -C 12  alkynyl; C 3 -C 16  cycloalkyl; C 1 -C 16  cycloalkenyl, heterocyclyl including 3-16 atoms, heterocycloalkenyl including 3-16 atoms; C 7 -C 20  aralkyl; C 6 -C 16  aryl; heteroaryl including 5-16 atoms; halo; NR d R e ; nitro; azido, hydroxy; oxo, thioxo, ═NR k , C 1 -C 12  alkoxy; C 1 -C 12  thioalkoxy; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy; heteroaryloxy including 5-20 atoms; thioaryloxy including 5-20 atoms; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy; C 3 -C 16  cycloalkenyloxy; heterocyclyloxy including 3-16 atoms; heterocycloalkenyloxy including 3-16 atoms; C 7 -C 20  aralkoxy; heteroaralkoxy including 6-20 atoms; mercapto; cyano; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; or —OC(O)NR d R e ; or 2 R b′  together form C 1 -C 3  alkylenedioxy; 
 R c  at each occurrence is, independently: 
 (i) halo; nitro; hydroxy; C 1 -C 12  alkoxy optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; cyano; SO 2 R m ; or 2 R c  together form C 1 -C 3  alkylenedioxy; or 
 (ii) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (iii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; or 
 (iv) C 2 -C 20  alkenyl or C 2 -C 20  alkynyl; or 
 (v) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a ; 
 each of R d , R e , R g , R h , and R k , at each occurrence is, independently: 
 (i) hydrogen; or 
 (ii) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (iii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; or 
 (iv) C 2 -C 20  alkenyl or C 2 -C 20  alkynyl; or 
 (v) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a ; 
 R f  is NR d R e ; nitro; azido; hydroxy; oxo, thioxo, ═NR k , C 1 -C 12  alkoxy or C 1 -C 12  thioalkoxy, each of which is optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy, heteroaryloxy including 5-20 atoms, or thioaryloxy including 5-20 atoms, each of which is optionally substituted with 1-5 R a′ ; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy, C 3 -C 16  cycloalkenyloxy, heterocyclyloxy including 3-16 atoms, heterocycloalkenyloxy including 3-16 atoms, C 7 -C 20  aralkoxy, or heteroaralkoxy including 6-20 atoms, each of which is optionally substituted with 1-5 R b ; mercapto; cyano; —C(O)R g , —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; 
 R i  is R g ; OR g ; or NR d R e ; 
 R j  is NR d R e ; nitro; azido; hydroxy; oxo; thioxo; ═NR k ; C 1 -C 12  alkoxy or C 1 -C 12  thioalkoxy, each of which is optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy, heteroaryloxy including 5-20 atoms, or thioaryloxy including 5-20 atoms, each of which is optionally substituted with 1-5 R a′ ; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy, heterocyclyloxy including 3-16 atoms, heterocycloalkenyloxy including 3-16 atoms, C 7 -C 20  aralkoxy, or heteroaralkoxy including 6-20 atoms, each of which is optionally substituted with 1-5 R b ; mercapto; cyano; C 1 -C 3  alkylenedioxy; —C(O)R g , —C(O)OR g , —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; 
 R m  is 
 (i) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (ii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; or 
 (iii) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a ; and 
 provided: 
 (a) when V and Y are both N, and R 2  is substituted pyridyl or pyrimidinyl, then R c  cannot be C 1 -C 12  alkoxy optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; or SO 2 R m ; and 
 (b) when V and Y are both N, X is SO 2 , one of Z 1  and W 2  is CH 3 , and R 2  is phenyl substituted with from 1-5 R c , then 1 R c  must be halo; C 1 -C 12  haloalkoxy; cyano; or C 1 -C 12  haloalkyl, optionally substituted with from 1-5 R j ; or a pharmaceutically acceptable salt and/or N-oxide thereof. 
 
   
   
       95 - 102 . (canceled) 
   
   
       103 . A method for treating a disease or condition selected from type 2 diabetes, Syndrome X, obesity, dyslipidemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, low HDL, high LDL, atherosclerosis, and a cognitive disorder, the method comprising administering to a subject in need thereof an effective amount of a compound of formula I: 
     
       
         
         
             
             
         
       
     
     wherein:
 R 1  is: 
 (i) C 6 -C 18  aryl or heteroaryl including 5-20 atoms, each of which is optionally substituted with from 1-10 R a ; or 
 (ii) C 7 -C 20  aralkyl; heteroaralkyl including 6-20 atoms; arylheterocyclyl including 8-20 atoms; arylcycloalkenyl including 8-20 atoms; or arylheterocycloalkenyl including 8-20 atoms; each of which is optionally substituted with from 1-10 R b ; 
 R 2  is C 6 -C 18  aryl or heteroaryl including 5-20 atoms, each of which is optionally substituted with from 1-10 R c ; 
 X is S(O) n  or S(O) n NR 6 , wherein n is 1 or 2, and R 6  is hydrogen, C 1 -C 12  alkyl, or C 3 -C 16  cycloalkyl; 
 each of V and Y is, independently, CR 7  or N, wherein R 7  is hydrogen or C 1 -C 12  alkyl, provided that Y and V cannot both be CR 7 ; 
 one, two, three, or four of W 1 , Z 1 , W 2 , and Z 2  are each, independently: 
 (i) C 1 -C 12  alkyl; or 
 (ii) oxo; or 
 (iii) C 6 -C 18  aryl or heteroaryl including 5-20 atoms, each of which is optionally substituted with from 1-10 R a ; or 
 (iv) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; and the others are hydrogen; 
 R a  at each occurrence is, independently: 
 (i) halo; NR d R e ; nitro; azido; hydroxy; C 1 -C 12  alkoxy or C 1 -C 12  thioalkoxy, each of which is optionally substituted with 1-5 R f , C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy, heteroaryloxy including 5-20 atoms, or thioaryloxy including 5-20 atoms, each of which is optionally substituted with 1-5 R a′ ; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy, C 3 -C 16  cycloalkenyloxy, heterocyclyloxy including 3-16 atoms, heterocycloalkenyloxy including 3-16 atoms, C 7 -C 20  aralkoxy, or heteroaralkoxy including 6-20 atoms, each of which is optionally substituted with 1-5 R b ; mercapto; cyano; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; or 2 R a  together form C 1 -C 3  alkylenedioxy; 
 (ii) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (iii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; or 
 (iv) C 2 -C 20  alkenyl or C 2 -C 20  alkynyl; or 
 (v) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a′ ; 
 R a′  at each occurrence is, independently, C 1 -C 12  alkyl, C 1 -C 12  haloalkyl, C 2 -C 12  alkenyl; C 2 -C 12  alkynyl; C 3 -C 16  cycloalkyl; C 3 -C 16  cycloalkenyl, heterocyclyl including 3-16 atoms, heterocycloalkenyl including 3-16 atoms; C 7 -C 20  aralkyl; C 6 -C 16  aryl; heteroaryl including 5-16 atoms; halo; NR d R e ; nitro; azido, hydroxy; C 1 -C 12  alkoxy; C 1 -C 12  thioalkoxy; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy; heteroaryloxy including 5-20 atoms; thioaryloxy including 5-20 atoms; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy; C 3 -C 16  cycloalkenyloxy; heterocyclyloxy including 3-16 atoms; heterocycloalkenyloxy including 3-16 atoms; C 7 -C 20  aralkoxy; heteroaralkoxy including 6-20 atoms; mercapto; cyano; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; or 2 R a′  together form C 1 -C 3  alkylenedioxy; or 2 R a′  together form C 1 -C 3  alkylenedioxy; 
 R b  at each occurrence is, independently: 
 (i) halo; NR d R e ; nitro; azido; hydroxy; oxo, thioxo, ═NR k , C 1 -C 12  alkoxy or C 1 -C 12  thioalkoxy, each of which is optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy, heteroaryloxy including 5-20 atoms, or thioaryloxy including 5-20 atoms, each of which is optionally substituted with 1-5 R a ; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy, C 3 -C 16  cycloalkenyloxy, heterocyclyloxy including 3-16 atoms, heterocycloalkenyloxy including 3-16 atoms, C 7 -C 20  aralkoxy, or heteroaralkoxy including 6-20 atoms, each of which is optionally substituted with 1-5 R b′ ; mercapto; cyano; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; or 2 R b  together form C 1 -C 3  alkylenedioxy; or 
 (ii) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (iii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b′ ; or 
 (iv) C 2 -C 20  alkenyl or C 2 -C 20  alkynyl; or 
 (v) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a ; 
 R b′  at each occurrence is, independently, C 1 -C 12  alkyl or C 1 -C 12  haloalkyl, each of which is optionally substituted with 1-5 R j ; C 2 -C 12  alkenyl; C 2 -C 12  alkynyl; C 3 -C 16  cycloalkyl; C 3 -C 16  cycloalkenyl, heterocyclyl including 3-16 atoms, heterocycloalkenyl including 3-16 atoms; C 7 -C 20  aralkyl; C 6 -C 16  aryl; heteroaryl including 5-16 atoms; halo; NR d R e ; nitro; azido, hydroxy; ox, thioxo, ═NR k , C 1 -C 12  alkoxy; C 1 -C 12  thioalkoxy; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy; heteroaryloxy including 5-20 atoms; thioaryloxy including 5-20 atoms; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy; C 3 -C 16  cycloalkenyloxy; heterocyclyloxy including 3-16 atoms; heterocycloalkenyloxy including 3-16 atoms; C 7 -C 20  aralkoxy; heteroaralkoxy including 6-20 atoms; mercapto; cyano; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; or —OC(O)NR d R e ; or 2 R b′  together form C 1 -C 3  alkylenedioxy; 
 R c  at each occurrence is, independently: 
 (i) halo; nitro; hydroxy; C 1 -C 12  alkoxy optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; cyano; SO 2 R m ; or 2 R c  together form C 1 -C 3  alkylenedioxy; or 
 (ii) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (iii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; or 
 (iv) C 2 -C 20  alkenyl or C 2 -C 20  alkynyl; or 
 (v) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a ; 
 each of R d , R e , R g , R h , and R k , at each occurrence is, independently: 
 (i) hydrogen; or 
 (ii) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (iii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; or 
 (iv) C 2 -C 20  alkenyl or C 2 -C 20  alkynyl; or 
 (v) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a ; 
 R f  is NR d R e ; nitro; azido; hydroxy; oxo, thioxo, ═NR k , C 1 -C 12  alkoxy or C 1 -C 12  thioalkoxy, each of which is optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy, heteroaryloxy including 5-20 atoms, or thioaryloxy including 5-20 atoms, each of which is optionally substituted with 1-5 R a′ ; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy, C 3 -C 16  cycloalkenyloxy, heterocyclyloxy including 3-16 atoms, heterocycloalkenyloxy including 3-16 atoms, C 7 -C 20  aralkoxy, or heteroaralkoxy including 6-20 atoms, each of which is optionally substituted with 1-5 R b ; mercapto; cyano; —C(O)R g , —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; 
 R i  is R g ; OR g ; or NR d R e ; 
 R j  is NR d R e ; nitro; azido; hydroxy; oxo; thioxo; ═NR k ; C 1 -C 12  alkoxy or C 1 -C 12  thioalkoxy, each of which is optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy, heteroaryloxy including 5-20 atoms, or thioaryloxy including 5-20 atoms, each of which is optionally substituted with 1-5 R a′ ; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy, C 3 -C 16  cycloalkenyloxy, heterocyclyloxy including 3-16 atoms, heterocycloalkenyloxy including 3-16 atoms, C 7 -C 20  aralkoxy, or heteroaralkoxy including 6-20 atoms, each of which is optionally substituted with 1-5 R b ; mercapto; cyano; C 1 -C 3  alkylenedioxy; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; 
 R m  is 
 (i) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (ii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; or 
 (iii) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a ; and 
 provided: 
 (a) when V and Y are both N, and R 2  is substituted pyridyl or pyrimidinyl, then R c  cannot be C 1 -C 12  alkoxy optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; or SO 2 R m ; and 
 (b) when V and Y are both N, X is SO 2 , one of Z 1  and W 2  is CH 3 , and R 2  is phenyl substituted with from 1-5 R c , then 1 R c  must be halo; C 1 -C 12  haloalkoxy; cyano; or C 1 -C 12  haloalkyl, optionally substituted with from 1-5 R j ; or a pharmaceutically acceptable salt and/or N-oxide thereof. 
 
   
   
       104 . The method of  claim 103 , wherein the disease or condition is type 2 diabetes. 
   
   
       105 . The method of  claim 103 , wherein the disease or condition is Syndrome X. 
   
   
       106 . The method of  claim 103 , wherein the disease or condition is obesity. 
   
   
       107 . The method of  claim 103 , wherein the disease or condition is selected from dyslipidemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, low HDL and high LDL. 
   
   
       108 . The method of  claim 103 , wherein the disease or condition is atherosclerosis. 
   
   
       109 . The method of  claim 103 , wherein the disease or condition is a cognitive disorder. 
   
   
       110 . The method of  claim 109 , wherein the cognitive disorder is Alzheimer's disease. 
   
   
       111 . A method for promoting wound healing, the method comprising administering to a subject in need thereof an effective amount of a compound of formula I: 
     
       
         
         
             
             
         
       
     
     wherein:
 R 1  is: 
 (i) C 6 -C 18  aryl or heteroaryl including 5-20 atoms, each of which is optionally substituted with from 1-10 R a ; or 
 (ii) C 7 -C 20  aralkyl; heteroaralkyl including 6-20 atoms; arylheterocyclyl including 8-20 atoms; arylcycloalkenyl including 8-20 atoms; or arylheterocycloalkenyl including 8-20 atoms; each of which is optionally substituted with from 1-10 R b ; 
 R 2  is C 6 -C 18  aryl or heteroaryl including 5-20 atoms, each of which is optionally substituted with from 1-10 R c ; 
 X is S(O) n  or S(O) n NR 6 , wherein n is 1 or 2, and R 6  is hydrogen, C 1 -C 12  alkyl, or C 3 -C 16  cycloalkyl; 
 each of V and Y is, independently, CR 7  or N, wherein R 7  is hydrogen or C 1 -C 12  alkyl, provided that Y and V cannot both be CR 7 ; 
 one, two, three, or four of W 1 , Z 1 , W 2 , and Z 2  are each, independently: 
 (i) C 1 -C 12  alkyl; or 
 (ii) oxo; or 
 (iii) C 6 -C 18  aryl or heteroaryl including 5-20 atoms, each of which is optionally substituted with from 1-10 R a ; or 
 (iv) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; and the others are hydrogen; 
 R a  at each occurrence is, independently: 
 (i) halo; NR d R e ; nitro; azido; hydroxy; C 1 -C 12  alkoxy or C 1 -C 12  thioalkoxy, each of which is optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy, heteroaryloxy including 5-20 atoms, or thioaryloxy including 5-20 atoms, each of which is optionally substituted with 1-5 R a′ ; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy, C 3 -C 16  cycloalkenyloxy, heterocyclyloxy including 3-16 atoms, heterocycloalkenyloxy including 3-16 atoms, C 7 -C 20  aralkoxy, or heteroaralkoxy including 6-20 atoms, each of which is optionally substituted with 1-5 R b ; mercapto; cyano; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; or 2 R a  together form C 1 -C 3  alkylenedioxy; 
 (ii) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (iii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; or 
 (iv) C 2 -C 20  alkenyl or C 2 -C 20  alkynyl; or 
 (v) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a′ ; 
 R a′  at each occurrence is, independently, C 1 -C 12  alkyl, C 1 -C 12  haloalkyl, C 2 -C 12  alkenyl; C 2 -C 12  alkynyl; C 3 -C 16  cycloalkyl; C 3 -C 16  cycloalkenyl, heterocyclyl including 3-16 atoms, heterocycloalkenyl including 3-16 atoms; C 7 -C 20  aralkyl; C 6 -C 16  aryl; heteroaryl including 5-16 atoms; halo; NR d R e ; nitro; azido, hydroxy; C 1 -C 12  alkoxy; C 1 -C 12  thioalkoxy; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy; heteroaryloxy including 5-20 atoms; thioaryloxy including 5-20 atoms; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy; C 3 -C 16  cycloalkenyloxy; heterocyclyloxy including 3-16 atoms; heterocycloalkenyloxy including 3-16 atoms; C 7 -C 20  aralkoxy; heteroaralkoxy including 6-20 atoms; mercapto; cyano; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; or 2 R a′  together form C 1 -C 3  alkylenedioxy; or 2 R a′  together form C 1 -C 3  alkylenedioxy; 
 R b  at each occurrence is, independently: 
 (i) halo; NR d R e ; nitro; azido; hydroxy; oxo, thioxo, ═NR k , C 1 -C 12  alkoxy or C 1 -C 12  thioalkoxy, each of which is optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy, heteroaryloxy including 5-20 atoms, or thioaryloxy including 5-20 atoms, each of which is optionally substituted with 1-5 R a ; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy, C 3 -C 16  cycloalkenyloxy, heterocyclyloxy including 3-16 atoms, heterocycloalkenyloxy including 3-16 atoms, C 7 -C 20  aralkoxy, or heteroaralkoxy including 6-20 atoms, each of which is optionally substituted with 1-5 R b′ ; mercapto; cyano; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; or 2 R b  together form C 1 -C 3  alkylenedioxy; or 
 (ii) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (iii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b′ ; or 
 (iv) C 2 -C 20  alkenyl or C 2 -C 20  alkynyl; or 
 (v) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a ; 
 R b′  at each occurrence is, independently, C 1 -C 12  alkyl or C 1 -C 12  haloalkyl, each of which is optionally substituted with 1-5 R j ; C 2 -C 12  alkenyl; C 2 -C 12  alkynyl; C 3 -C 16  cycloalkyl; C 3 -C 16  cycloalkenyl, heterocyclyl including 3-16 atoms, heterocycloalkenyl including 3-16 atoms; C 7 -C 20  aralkyl; C 6 -C 16  aryl; heteroaryl including 5-16 atoms; halo; NR d R e ; nitro; azido, hydroxy; oxo, thioxo, ═NR k , C 1 -C 12  alkoxy; C 1 -C 12  thioalkoxy; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy; heteroaryloxy including 5-20 atoms; thioaryloxy including 5-20 atoms; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy; C 3 -C 16  cycloalkenyloxy; heterocyclyloxy including 3-16 atoms; heterocycloalkenyloxy including 3-16 atoms; C 7 -C 20  aralkoxy; heteroaralkoxy including 6-20 atoms; mercapto; cyano; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; or —OC(O)NR d R e ; or 2 R b′  together form C 1 -C 3  alkylenedioxy; 
 R c  at each occurrence is, independently: 
 (i) halo; nitro; hydroxy; C 1 -C 12  alkoxy optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; cyano; SO 2 R m ; or 2 R c  together form C 1 -C 3  alkylenedioxy; or 
 (ii) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (iii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; or 
 (iv) C 2 -C 20  alkenyl or C 2 -C 20  alkynyl; or 
 (v) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a ; 
 each of R d , R e , R g , R h , and R k , at each occurrence is, independently: 
 (i) hydrogen; or 
 (ii) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (iii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; or 
 (iv) C 2 -C 20  alkenyl or C 2 -C 20  alkynyl; or 
 (v) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a ; 
 R f  is NR d R e ; nitro; azido; hydroxy; oxo, thioxo, ═NR k , C 1 -C 12  alkoxy or C 1 -C 12  thioalkoxy, each of which is optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy, heteroaryloxy including 5-20 atoms, or thioaryloxy including 5-20 atoms, each of which is optionally substituted with 1-5 R a′ ; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy, C 3 -C 16  cycloalkenyloxy, heterocyclyloxy including 3-16 atoms, heterocycloalkenyloxy including 3-16 atoms, C 7 -C 20  aralkoxy, or heteroaralkoxy including 6-20 atoms, each of which is optionally substituted with 1-5 R b ; mercapto; cyano; —C(O)R g , —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; 
 R i  is R g ; OR g ; or NR d R e ; 
 R j  is NR d R e ; nitro; azido; hydroxy; oxo; thioxo; ═NR k ; C 1 -C 12  alkoxy or C 1 -C 12  thioalkoxy, each of which is optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy, heteroaryloxy including 5-20 atoms, or thioaryloxy including 5-20 atoms, each of which is optionally substituted with 1-5 R a′ ; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy, C 3 -C 16  cycloalkenyloxy, heterocyclyloxy including 3-16 atoms, heterocycloalkenyloxy including 3-16 atoms, C 7 -C 20  aralkoxy, or heteroaralkoxy including 6-20 atoms, each of which is optionally substituted with 1-5 R b ; mercapto; cyano; C 1 -C 3  alkylenedioxy; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; 
 R m  is 
 (i) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (ii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; or 
 (iii) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a ; and 
 provided: 
 (a) when V and Y are both N, and R 2  is substituted pyridyl or pyrimidinyl, then R c  cannot be C 1 -C 12  alkoxy optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; or SO 2 R m ; and 
 (b) when V and Y are both N, X is SO 2 , one of Z 1  and W 2  is CH 3 , and R 2  is phenyl substituted with from 1-5 R c , then 1 R c  must be halo; C 1 -C 12  haloalkoxy; cyano; or C 1 -C 12  haloalkyl, optionally substituted with from 1-5 R j ; or a pharmaceutically acceptable salt and/or N-oxide thereof. 
 
   
   
       112 . A method for treating a disease or condition mediated by excess or uncontrolled amounts of cortisol and/or other corticosteroids, the method comprising administering to a subject in need thereof an effective amount of a compound of formula (I): 
     
       
         
         
             
             
         
       
     
     wherein:
 R 1  is: 
 (i) C 6 -C 18  aryl or heteroaryl including 5-20 atoms, each of which is optionally substituted with from 1-10 R a ; or 
 (ii) C 7 -C 20  aralkyl or heteroaralkyl including 6-20 atoms; each of which is optionally substituted with from 1-10 R b ; 
 R 2  is: 
 (i) C 6 -C 18  aryl substituted with from 1-10 R c ; or heteroaryl including 5-20 atoms, optionally substituted with from 1-10 R c ; or 
 (iii) OR 1 ; SR 1 ; or NR 3 R 4 , wherein R 3  and R 4  are each, independently, hydrogen or R 1 ; 
 X is S(O) n  or S(O) n NR 6 , wherein n is 1 or 2, and R 6  is hydrogen, C 1 -C 12  alkyl, or C 3 -C 16  cycloalkyl; 
 each of V and Y is, independently, CR 7  or N, wherein R 7  is hydrogen or C 1 -C 12  alkyl, provided that Y and V cannot both be CR 7 ; 
 each of W 1 , Z 1 , W 2 , and Z 2  is hydrogen; 
 R a  at each occurrence is, independently: 
 (i) halo; NR d R e ; nitro; azido; hydroxy; C 1 -C 12  alkoxy or C 1 -C 12  thioalkoxy, each of which is optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy, heteroaryloxy including 5-20 atoms, or thioaryloxy including 5-20 atoms, each of which is optionally substituted with 1-5 R a′ ; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy, C 3 -C 16  cycloalkenyloxy, heterocyclyloxy including 3-16 atoms, heterocycloalkenyloxy including 3-16 atoms, C 7 -C 20  aralkoxy, or heteroaralkoxy including 6-20 atoms, each of which is optionally substituted with 1-5 R b ; mercapto; cyano; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; or 2 R a  together form C 1 -C 3  alkylenedioxy; 
 (ii) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (iii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; or 
 (iv) C 2 -C 20  alkenyl or C 2 -C 20  alkynyl; or 
 (v) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a′ ; 
 R a′  at each occurrence is, independently, C 1 -C 12  alkyl, C 1 -C 12  haloalkyl, C 2 -C 12  alkenyl; C 2 -C 12  alkynyl; C 3 -C 16  cycloalkyl; C 3 -C 16  cycloalkenyl, heterocyclyl including 3-16 atoms, heterocycloalkenyl including 3-16 atoms; C 7 -C 20  aralkyl; C 6 -C 16  aryl; heteroaryl including 5-16 atoms; halo; NR d R e ; nitro; azido, hydroxy; C 1 -C 12  alkoxy; C 1 -C 12  thioalkoxy; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy; heteroaryloxy including 5-20 atoms; thioaryloxy including 5-20 atoms; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy; C 3 -C 16  cycloalkenyloxy; heterocyclyloxy including 3-16 atoms; heterocycloalkenyloxy including 3-16 atoms; C 7 -C 20  aralkoxy; heteroaralkoxy including 6-20 atoms; mercapto; cyano; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; or 2 R a′  together form C 1 -C 3  alkylenedioxy; or 2 R a′  together form C 1 -C 3  alkylenedioxy; 
 R b  at each occurrence is, independently: 
 (i) halo; NR d R e ; nitro; azido; hydroxy; oxo, thioxo, ═NR k , C 1 -C 12  alkoxy or C 1 -C 12  thioalkoxy, each of which is optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy, heteroaryloxy including 5-20 atoms, or thioaryloxy including 5-20 atoms, each of which is optionally substituted with 1-5 R a ; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy, C 3 -C 16  cycloalkenyloxy, heterocyclyloxy including 3-16 atoms, heterocycloalkenyloxy including 3-16 atoms, C 7 -C 20  aralkoxy, or heteroaralkoxy including 6-20 atoms, each of which is optionally substituted with 1-5 R b′ ; mercapto; cyano; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; or 2 R b  together form C 1 -C 3  alkylenedioxy; or 
 (ii) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (iii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b′ ; or 
 (iv) C 2 -C 20  alkenyl or C 2 -C 20  alkynyl; or 
 (v) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a ; 
 R b′  at each occurrence is, independently, C 1 -C 12  alkyl or C 1 -C 12  haloalkyl, each of which is optionally substituted with 1-5 R j ; C 2 -C 12  alkenyl; C 2 -C 12  alkynyl; C 3 -C 16  cycloalkyl; C 3 -C 16  cycloalkenyl, heterocyclyl including 3-16 atoms, heterocycloalkenyl including 3-16 atoms; C 7 -C 20  aralkyl; C 6 -C 16  aryl; heteroaryl including 5-16 atoms; halo; NR d R e ; nitro; azido, hydroxy; oxo, thioxo, ═NR k , C 1 -C 12  alkoxy; C 1 -C 12  thioalkoxy; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy; heteroaryloxy including 5-20 atoms; thioaryloxy including 5-20 atoms; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy; C 3 -C 16  cycloalkenyloxy; heterocyclyloxy including 3-16 atoms; heterocycloalkenyloxy including 3-16 atoms; C 7 -C 20  aralkoxy; heteroaralkoxy including 6-20 atoms; mercapto; cyano; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; or —OC(O)NR d R e ; or 2 R b′  together form C 1 -C 3  alkylenedioxy; 
 R c  at each occurrence is, independently: 
 (i) halo; nitro; hydroxy; C 1 -C 12  alkoxy optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; cyano; SO 2 R m ; or 2 R c  together form C 1 -C 3  alkylenedioxy; or 
 (ii) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (iii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; or 
 (iv) C 2 -C 20  alkenyl or C 2 -C 20  alkynyl; or 
 (v) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a ; 
 each of R d , R e , R f , R g , R h , and R k , at each occurrence is, independently: 
 (i) hydrogen; or 
 (ii) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (iii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; or 
 (iv) C 2 -C 20  alkenyl or C 2 -C 20  alkynyl; or 
 (v) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a ; 
 R f  is NR d R e ; nitro; azido; hydroxy; oxo, thioxo, ═NR k , C 1 -C 12  alkoxy or C 1 -C 12  thioalkoxy, each of which is optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy, heteroaryloxy including 5-20 atoms, or thioaryloxy including 5-20 atoms, each of which is optionally substituted with 1-5 R a′ ; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy, C 3 -C 16  cycloalkenyloxy, heterocyclyloxy including 3-16 atoms, heterocycloalkenyloxy including 3-16 atoms, C 7 -C 20  aralkoxy, or heteroaralkoxy including 6-20 atoms, each of which is optionally substituted with 1-5 R b ; mercapto; cyano; —C(O)R g , —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; 
 R i  is R g ; OR g ; or NR d R e ; 
 R j  is NR d R e ; nitro; azido; hydroxy; oxo, thioxo, ═NR k , C 1 -C 12  alkoxy or C 1 -C 12  thioalkoxy, each of which is optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy, heteroaryloxy including 5-20 atoms, or thioaryloxy including 5-20 atoms, each of which is optionally substituted with 1-5 R a′ ; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy, C 3 -C 16  cycloalkenyloxy, heterocyclyloxy including 3-16 atoms, heterocycloalkenyloxy including 3-16 atoms, C 7 -C 20  aralkoxy, or heteroaralkoxy including 6-20 atoms, each of which is optionally substituted with 1-5 R b ; mercapto; cyano; C 1 -C 3  alkylenedioxy; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; 
 R m  is 
 (i) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (ii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; or 
 (iii) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a ; and 
 provided: 
 (a) when V and Y are both N, and R 2  is substituted pyridyl or pyrimidinyl, then R c  cannot be C 1 -C 12  alkoxy optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; or SO 2 R m ; and 
 (b) when V and Y are both N and X is SO 2 , then R 1  cannot be 4-chlorophenyl; and 
 (c) when V and Y are both N and X is SO 2 , then R 1  cannot be 1-chlorophenyl when R 2  is: phenyl monosubstituted with hydroxyl, C 1 -C 6  alkoxy, chloro, or nitro; unsubstituted pyridyl; pyridyl monosubstituted with hydroxyl, chloro, or nitro; unsubstituted thiazolyl; thiazolyl monosubstituted with nitro or hydroxymethyl; unsubstituted indolyl; or unsubstituted indazolyl; and 
 (d) when V and Y are both N and X is SO 2 , then R 1  cannot be naphthyl when R 2  is: unsubstituted pyridyl; unsubstituted pyrimidinyl; phenyl monosubstituted with hydroxyl or C 1 -C 6  alkoxy; unsubstituted thiazolyl; or 5-chloro-2-methylphenyl; and 
 (e) when Y is N and V is CH and X is SO 2 , then R 1  cannot be 1-chlorophenyl when R 2  is: phenyl monosubstituted with C 1 -C 6  alkoxy or C 1 -C 6  alkyl; or substituted benzo[d]isoxazole; and 
 (f) when Y is N and V is CH and X is SO 2 , then R 1  cannot be naphthyl when R 2  is phenyl monosubstituted with hydroxymethyl;
 or a pharmaceutically acceptable salt and/or N-oxide thereof. 
 
 
   
   
       113 . A method for treating a disease or condition mediated by excess or uncontrolled amounts of cortisol and/or other corticosteroids, the method comprising administering to a subject in need thereof an effective amount of a compound of formula (I): 
     
       
         
         
             
             
         
       
     
     wherein:
 R 1  is C 7 -C 20  aralkyl, C 3 -C 16  cycloalkyl, or (C 1 -C 12  alkyl)-(C 3 -C 16  cycloalkyl), each of which is optionally substituted with from 1-10 R b ; 
 R 2  is: 
 (i) C 6 -C 18  aryl or heteroaryl including 5-20 atoms, each of which is optionally substituted with from 1-10 R c ; or 
 (ii) OR 1 ; SR 1 ; or NR 3 R 4 , wherein R 3  and R 4  are each, independently, hydrogen or R 1 ; 
 X is CO; 
 each of V and Y is, independently, CR 7  or N, wherein R 7  is hydrogen or C 1 -C 12  alkyl, provided that Y and V cannot both be CR 7 ; 
 each of W 1 , Z 1 , W 2 , and Z 2  is, independently: 
 (i) hydrogen; or 
 (ii) oxo; or 
 (iii) C 1 -C 12  alkyl; or 
 (iv) C 6 -C 18  aryl or heteroaryl including 5-20 atoms, each of which is optionally substituted with from 1-10 R a ; or 
 (v) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; 
 R a  at each occurrence is, independently: 
 (i) halo; NR d R e ; nitro; azido; hydroxy; C 1 -C 12  alkoxy or C 1 -C 12  thioalkoxy, each of which is optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy, heteroaryloxy including 5-20 atoms, or thioaryloxy including 5-20 atoms, each of which is optionally substituted with 1-5 R a′ ; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy, C 3 -C 16  cycloalkenyloxy, heterocyclyloxy including 3-16 atoms, heterocycloalkenyloxy including 3-16 atoms, C 7 -C 20  aralkoxy, or heteroaralkoxy including 6-20 atoms, each of which is optionally substituted with 1-5 R b ; mercapto; cyano; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; or 2 R a  together form C 1 -C 3  alkylenedioxy; 
 (ii) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (iii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; or 
 (iv) C 2 -C 20  alkenyl or C 2 -C 20  alkynyl; or 
 (v) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a′ ; 
 R a′  at each occurrence is, independently, C 1 -C 12  alkyl, C 1 -C 12  haloalkyl, C 2 -C 12  alkenyl; C 2 -C 12  alkynyl; C 3 -C 16  cycloalkyl; C 3 -C 16  cycloalkenyl, heterocyclyl including 3-16 atoms, heterocycloalkenyl including 3-16 atoms; C 7 -C 20  aralkyl; C 6 -C 16  aryl; heteroaryl including 5-16 atoms; halo; NR d R e ; nitro; azido, hydroxy; C 1 -C 12  alkoxy; C 1 -C 12  thioalkoxy; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy; heteroaryloxy including 5-20 atoms; thioaryloxy including 5-20 atoms; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy; C 3 -C 16  cycloalkenyloxy; heterocyclyloxy including 3-16 atoms; heterocycloalkenyloxy including 3-16 atoms; C 7 -C 20  aralkoxy; heteroaralkoxy including 6-20 atoms; mercapto; cyano; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; or 2 R a′  together form C 1 -C 3  alkylenedioxy; or 2 R a′  together form C 1 -C 3  alkylenedioxy; 
 R b  at each occurrence is, independently: 
 (i) halo; NR d R e ; nitro; azido; hydroxy; oxo, thioxo, ═NR k , C 1 -C 12  alkoxy or C 1 -C 12  thioalkoxy, each of which is optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy, heteroaryloxy including 5-20 atoms, or thioaryloxy including 5-20 atoms, each of which is optionally substituted with 1-5 R a ; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy, C 3 -C 16  cycloalkenyloxy, heterocyclyloxy including 3-16 atoms, heterocycloalkenyloxy including 3-16 atoms, C 7 -C 20  aralkoxy, or heteroaralkoxy including 6-20 atoms, each of which is optionally substituted with 1-5 R b ; mercapto; cyano; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; or 2 R b  together form C 1 -C 3  alkylenedioxy; or 
 (ii) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (iii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b′ ; or 
 (iv) C 2 -C 20  alkenyl or C 2 -C 20  alkynyl; or 
 (v) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a ; 
 R b′  at each occurrence is, independently, C 1 -C 12  alkyl or C 1 -C 12  haloalkyl, each of which is optionally substituted with 1-5 R j ; C 2 -C 12  alkenyl; C 2 -C 12  alkynyl; C 3 -C 16  cycloalkyl; C 3 -C 16  cycloalkenyl, heterocyclyl including 3-16 atoms, heterocycloalkenyl including 3-16 atoms; C 7 -C 20  aralkyl; C 6 -C 16  aryl; heteroaryl including 5-16 atoms; halo; NR d R e ; nitro; azido, hydroxy; oxo, thioxo, ═NR k , C 1 -C 12  alkoxy; C 1 -C 12  thioalkoxy; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy; heteroaryloxy including 5-20 atoms; thioaryloxy including 5-20 atoms; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy; C 3 -C 16  cycloalkenyloxy; heterocyclyloxy including 3-16 atoms; heterocycloalkenyloxy including 3-16 atoms; C 7 -C 20  aralkoxy; heteroaralkoxy including 6-20 atoms; mercapto; cyano; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; or —OC(O)NR d R e ; or 2 R b′  together form C 1 -C 3  alkylenedioxy; 
 R c  at each occurrence is, independently: 
 (i) halo; nitro; hydroxy; C 1 -C 12  alkoxy optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; cyano; SO 2 R m ; or 2 R c  together form C 1 -C 3  alkylenedioxy; or 
 (ii) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (iii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; or 
 (iv) C 2 -C 20  alkenyl or C 2 -C 20  alkynyl; or 
 (v) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a ; 
 each of R d , R e , R g , R h , and R k , at each occurrence is, independently: 
 (i) hydrogen; or 
 (ii) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (iii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; or 
 (iv) C 2 -C 20  alkenyl or C 2 -C 20  alkynyl; or 
 (v) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a ; 
 R f  is NR d R e ; nitro; azido; hydroxy; oxo, thioxo, ═NR k , C 1 -C 12  alkoxy or C 1 -C 12  thioalkoxy, each of which is optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy, heteroaryloxy including 5-20 atoms, or thioaryloxy including 5-20 atoms, each of which is optionally substituted with 1-5 R a′ ; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy, C 3 -C 16  cycloalkenyloxy, heterocyclyloxy including 3-16 atoms, heterocycloalkenyloxy including 3-16 atoms, C 7 -C 20  aralkoxy, or heteroaralkoxy including 6-20 atoms, each of which is optionally substituted with 1-5 R b ; mercapto; cyano; —C(O)R g , —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; 
 R i  is R g ; OR g ; or NR d R e ; 
 R j  is NR d R e ; nitro; azido; hydroxy; oxo, thioxo, ═NR k , C 1 -C 12  alkoxy or C 1 -C 12  thioalkoxy, each of which is optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy, heteroaryloxy including 5-20 atoms, or thioaryloxy including 5-20 atoms, each of which is optionally substituted with 1-5 R a′ ; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy, C 3 -C 16  cycloalkenyloxy, heterocyclyloxy including 3-16 atoms, heterocycloalkenyloxy including 3-16 atoms, C 7 -C 20  aralkoxy, or heteroaralkoxy including 6-20 atoms, each of which is optionally substituted with 1-5 R b ; mercapto; cyano; C 1 -C 3  alkylenedioxy; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; and 
 R m  is 
 (i) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (ii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; or 
 (iii) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a ;
 or a pharmaceutically acceptable salt and/or N-oxide thereof. 
 
 
   
   
       114 . A method for treating a disease or condition mediated by excess or uncontrolled amounts of cortisol and/or other corticosteroids, the method comprising administering to a subject in need thereof an effective amount of a compound of formula (I): 
     
       
         
         
             
             
         
       
     
     wherein:
 R 1  is C 6 -C 18  aryl or heteroaryl including 5-20 atoms, each of which is optionally substituted with from 1-10 R a ; 
 R 2  is C 6 -C 16  cycloalkyl; C 6 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; 
 X is S(O) n  or S(O) n NR 6 , wherein n is 1 or 2, and R 6  is hydrogen, C 1 -C 12  alkyl, or C 3 -C 16  cycloalkyl; 
 each of V and Y is, independently, CR 7  or N, wherein R 7  is hydrogen or C 1 -C 12  alkyl, provided that Y and V cannot both be CR 7 ; 
 each of W 1 , Z 1 , W 2 , and Z 2  is, independently: 
 (i) hydrogen; or 
 (ii) oxo; or 
 (iii) C 1 -C 12  alkyl; or 
 (iv) C 6 -C 18  aryl or heteroaryl including 5-20 atoms, each of which is optionally substituted with from 1-10 R a ; or 
 (v) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; 
 R a  at each occurrence is, independently: 
 (i) halo; NR d R e ; nitro; azido; hydroxy; C 1 -C 12  alkoxy or C 1 -C 12  thioalkoxy, each of which is optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy, heteroaryloxy including 5-20 atoms, or thioaryloxy including 5-20 atoms, each of which is optionally substituted with 1-5 R a′ ; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy, C 3 -C 16  cycloalkenyloxy, heterocyclyloxy including 3-16 atoms, heterocycloalkenyloxy including 3-16 atoms, C 7 -C 20  aralkoxy, or heteroaralkoxy including 6-20 atoms, each of which is optionally substituted with 1-5 R b ; mercapto; cyano; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; or 2 R a  together form C 1 -C 3  alkylenedioxy; 
 (ii) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (iii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; or 
 (iv) C 2 -C 20  alkenyl or C 2 -C 20  alkynyl; or 
 (v) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a′ ; 
 R a′  at each occurrence is, independently, C 1 -C 12  alkyl, C 1 -C 12  haloalkyl, C 2 -C 12  alkenyl; C 2 -C 12  alkynyl; C 3 -C 16  cycloalkyl; C 3 -C 16  cycloalkenyl, heterocyclyl including 3-16 atoms, heterocycloalkenyl including 3-16 atoms; C 7 -C 20  aralkyl; C 6 -C 16  aryl; heteroaryl including 5-16 atoms; halo; NR d R e ; nitro; azido, hydroxy; C 1 -C 12  alkoxy; C 1 -C 12  thioalkoxy; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy; heteroaryloxy including 5-20 atoms; thioaryloxy including 5-20 atoms; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy; C 3 -C 16  cycloalkenyloxy; heterocyclyloxy including 3-16 atoms; heterocycloalkenyloxy including 3-16 atoms; C 7 -C 20  aralkoxy; heteroaralkoxy including 6-20 atoms; mercapto; cyano; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; or 2 R a′  together form C 1 -C 3  alkylenedioxy; or 2 R a′  together form C 1 -C 3  alkylenedioxy; 
 R b  at each occurrence is, independently: 
 (i) halo; NR d R e ; nitro; azido; hydroxy; oxo, thioxo, ═NR k , C 1 -C 12  alkoxy or C 1 -C 12  thioalkoxy, each of which is optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy, heteroaryloxy including 5-20 atoms, or thioaryloxy including 5-20 atoms, each of which is optionally substituted with 1-5 R a ; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy, C 3 -C 16  cycloalkenyloxy, heterocyclyloxy including 3-16 atoms, heterocycloalkenyloxy including 3-16 atoms, C 7 -C 20  aralkoxy, or heteroaralkoxy including 6-20 atoms, each of which is optionally substituted with 1-5 R b′ ; mercapto; cyano; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; or 2 R b  together form C 1 -C 3  alkylenedioxy; or 
 (ii) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (iii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b′ ; or 
 (iv) C 2 -C 20  alkenyl or C 2 -C 20  alkynyl; or 
 (v) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a ; 
 R b′  at each occurrence is, independently, C 1 -C 12  alkyl or C 1 -C 12  haloalkyl, each of which is optionally substituted with 1-5 R j ; C 2 -C 12  alkenyl; C 2 -C 12  alkynyl; C 3 -C 16  cycloalkyl; C 3 -C 16  cycloalkenyl, heterocyclyl including 3-16 atoms, heterocycloalkenyl including 3-16 atoms; C 7 -C 20  aralkyl; C 6 -C 16  aryl; heteroaryl including 5-16 atoms; halo; NR d R e ; nitro; azido, hydroxy; oxo, thioxo, ═NR k , C 1 -C 12  alkoxy; C 1 -C 12  thioalkoxy; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy; heteroaryloxy including 5-20 atoms; thioaryloxy including 5-20 atoms; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy; C 3 -C 16  cycloalkenyloxy; heterocyclyloxy including 3-16 atoms; heterocycloalkenyloxy including 3-16 atoms; C 7 -C 20  aralkoxy; heteroaralkoxy including 6-20 atoms; mercapto; cyano; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; or —OC(O)NR d R e ; or 2 R b′  together form C 1 -C 3  alkylenedioxy; 
 each of R d , R e , R g , R h , and R k , at each occurrence is, independently: 
 (i) hydrogen; or 
 (ii) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (iii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; or 
 (iv) C 2 -C 20  alkenyl or C 2 -C 20  alkynyl; or 
 (v) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a ; 
 R f  is NR d R e ; nitro; azido; hydroxy; oxo, thioxo, ═NR k , C 1 -C 12  alkoxy or C 1 -C 12  thioalkoxy, each of which is optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy, heteroaryloxy including 5-20 atoms, or thioaryloxy including 5-20 atoms, each of which is optionally substituted with 1-5 R a′ ; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy, C 3 -C 16  cycloalkenyloxy, heterocyclyloxy including 3-16 atoms, heterocycloalkenyloxy including 3-16 atoms, C 7 -C 20  aralkoxy, or heteroaralkoxy including 6-20 atoms, each of which is optionally substituted with 1-5 R b ; mercapto; cyano; —C(O)R g , —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; 
 R i  is R g ; OR g ; or NR d R e ; 
 R j  is NR d R e ; nitro; azido; hydroxy; oxo, thioxo, ═NR k , C 1 -C 12  alkoxy or C 1 -C 12  thioalkoxy, each of which is optionally substituted with 1-5 R f ; C 1 -C 12  haloalkoxy; C 6 -C 16  aryloxy, C 6 -C 16  thioaryloxy, heteroaryloxy including 5-20 atoms, or thioaryloxy including 5-20 atoms, each of which is optionally substituted with 1-5 R a ; C 2 -C 12  alkenyloxy; C 2 -C 12  alkynyloxy; C 3 -C 16  cycloalkyloxy, C 3 -C 16  cycloalkenyloxy, heterocyclyloxy including 3-16 atoms, heterocycloalkenyloxy including 3-16 atoms, C 7 -C 20  aralkoxy, or heteroaralkoxy including 6-20 atoms, each of which is optionally substituted with 1-5 R b ; mercapto; cyano; C 1 -C 3  alkylenedioxy; —C(O)R g , —C(O)OR g ; —OC(O)R g ; —C(O)SR g ; —SC(O)R g ; —C(S)SR g ; —SC(S)R g ; —C(O)NR d R e ; —NR h C(O)R i ; —OC(O)NR d R e ; and 
 R m  is 
 (i) C 1 -C 12  alkyl or C 1 -C 12  haloalkyl; each of which is optionally substituted with from 1-5 R j ; or 
 (ii) C 7 -C 20  aralkyl; C 3 -C 16  cycloalkyl; heteroaralkyl including 6-20 atoms; C 3 -C 16  cycloalkenyl; heterocyclyl including 3-16 atoms; or heterocycloalkenyl including 3-16 atoms; each of which is optionally substituted with from 1-10 R b ; or 
 (iii) C 6 -C 16  aryl or heteroaryl including 5-16 atoms, each of which is optionally substituted with from 1-10 R a ; and 
 provided: 
 (a) when V and Y are both N and X is SO 2 , then R 1  cannot be 1-chlorophenyl when R 2  is unsubstituted adamantyl or substituted or unsubstituted cyclohexyl; and 
 (b) when Y is N, V is CH, and X is SO 2 , then R 1  cannot be 1-chlorophenyl when R 2  is unsubstituted piperidyl, piperidyl substituted with oxo, unsubstituted morpholinyl, or unsubstituted pyrrolidinyl; or a pharmaceutically acceptable salt thereof.